Chelatbildende Gruppen enthaltende Somastotatin-Analoge und deren radiomarkierteZusammensetzungen

Chelatbildende Gruppen enthaltende Somatostatin Analoge und deren radiomarkierten Zusammensetzungen

SYNTHESIS OF PEPTIDE ALCOHOLS

A process for the production of a peptide alcohol which at the C-terminal end of the peptide chain bears two alcohol groups or one alcohol group and one thiol group, by acidic hydrolysis of an acetal of the peptide alcohol and a resin containing formylphenyl residues. Thus a peptide alcohol (where Y is a peptide residue, X is 0 or S, R is H or methyl) may be prepared by hydrolysis of acetalised resin (where P is an insoluble resin and Z is a band or linking group). The acetalised resin may be prepared by reacting a polymer of formula with a compound of formula (e.g. the N-trifluoromethyl carbonyl-Threoninol acetal of P-formylphenoxyacetic acid).

SOMATOSTATIN SIMILAR CONNECTIONS

3,5-DI (ARYL - OR HETERO ARYL) ISOXAZOLE AND 1.2, 4-OXADIAZOLE AS S1P1-REZEPTORAGONISTEN, the IMMUNE SYSTEM SUPPRESSING AND RESOLVENTS

2-AMINO-PROPANOL of DERIVATIVES

Treatment of autoimmune diseases

Diazacycloalkanedione derivatives

PARATHYROID HORMONE ANALOGS HAVING PARATHYROID HORMONE-LIKE ACTIVITY

... of the invention PTH compounds having PTH-like activity and comprising at least one modification, said modification being either 1. at least one radical selected from a L- or D-.alpha.-amino acid, C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to the terminal amino group of the PTH compound, and/or at least one radical selected from C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to one or more side chain amino groups of the PTH compound, or 2. at least one .alpha.-amino acid unit in the positions 1 to 38 of a naturally occurring PTH sequence being replaced by a natural or unnatural amino acid unit optionally in protected form, whereby the .alpha.-amino acid units present in positions 1 and 2 at the amino terminus of the PTH sequence may be replaced by a pseudo-peptide, or a combination of such modifications ...

PEPTIDES

Abstract of the Invention Somatostatin peptides bearing a chelating group selected from a bifunctional N4-chelating group particularly suitable for Tc, Rh, Cu, Co or Re-labelling, and a bifunctional polyamino-polycarboxylic acid chelating group are complexed with a .alpha.-, .beta.-, .gamma.- or positron-emitting nuclide or a nuclide with Auger-e--cascades and are useful as radiopharmaceuticals.

PEPTIDES

Compounds of formula I (see formula I) wherein M is a cation equivalent and A is Phe or Tyr, in free form or in salt form are useful as radiopharmaceuticals when complexed with an .alpha.- or .beta.-emitting radionuclide or a nuclide with Auger-e- -cascades.

PEPTIDVERBINDUNGEN WITH PHARMAKOLOGI EFFECT.

Peptide derivatives selected from (i) a calcitonin peptide and an LHRH antagonist peptide modified by at least one sugar residue and/or at least one short polyhydroxy compound or derivative, and (ii) a calcitonin peptide modified by at least one formyl and/or at least C3-5alkyl attached to an amino group other than an N-terminal amino group, and (iii) a calcitonin peptide modified by a combination of said substituents, with the provisos that i) when the calcitonin peptide comprises at least one sugar residue a), this sugar residue is attached by a coupling other than a direct N-glycosidic bond to an omega -amino group of an omega -amino substituted side chain in the 24 position, and ii) when the LHRH antagonist comprises at least one sugar residue a), this sugar residue is an Amadori sugar residue attached by a coupling other than a direct N-glycosidic bond to an omega -amino group of an omega -amino substituted side chain in the 8 position in free form or in salt or complex form, have pharmacological activity.

SOMATOSTATINDERIVATE WITH PHARMACODYNAMIC CHARACTERISTICS AND YOUR PRODUCTION.

Somatostatin peptides bearing at least one chelating group for a detectable element, said chelating group being linked to an amino group of said peptide, and said amino group having no significant binding affinity for somatostatin receptors, in free or salt form, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of somatostatin receptor positive tumors or for therapy.

3,5-DI(ARYL OR HETEROARYL)ISOXAZOLES AND 1,2,4-OXADIAZOLES AS S1P1 RECEPTOR AGONISTS, IMMUNOSUPPRESSSIVE AND ANTI-INFLAMMATORY AGENTS

2-AMINO-PROPANOL DERIVATE

Peptides

Compounds of formula I wherein A is a radical of formula (???1) or (???1> wherein R is C1-11 alkylene or C2-11 alkenylene Z is -OH, NR4R5, -NR4R5R6, -NHOH, or guanidino or ureido, R1 is C1-5 alkylene R2 is hydrogen, -CO-NH2, or a sugar residue R3 is hydrogen or a sugar residue, R4 is hydrogen, C1-3 alkyl or a sugar residue R5 is hydrogen or C1-3 alkyl, and R6 is C1-3 alkyl and >N-CH(Z1)-CO-, A', Y1, Y2, B, C, D, E and F have the meanings recited in Claim 1 in free form, salt form or complex form, have pharmacological activity, in particular GH-, gastric and pancreatic secretion inhibiting activity.

SOMATOSTATINPEPTID

TREATMENT OF AUTOCIMMUNE DISEASES

PARATHYROID HORMONE ANALOGS HAVING PARATHYROID HORMONE-LIKE ACTIVITY

PTH compounds having PTH-like activity and comprising at least one modification, said modification being either 1. at least one radical selected from a L- or D-a-amino acid, C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to the terminal amino group of the PTH compound, and/or at least one radical selected from C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to one or more side chain amino groups of the PTH compound, or 2. at least one .alpha.-amino acid unit in the positions 1 to 38 of a naturally occurring PTH sequence being replaced by a natural or unnatural amino acid unit optionally in protected form, whereby the .alpha.-amino acid units present in positions 1 and 2 at the amino terminus of the PTH sequence may be replaced by a pseudo-peptide, or a combination of such modifications, in free form ...

POLYPEPTIDES

... 100-7774 POLYPEPTIDES of the Invention Cyclic or linear somatostatin peptides bearing a specific chelating group on the terminal amino group, in free or salt form, are complexed with a .beta.-, .gamma.- or positron-emitting element and are useful as radiopharmaceuticals.

INDOLYLMALEIMIDE DERIVATIVES AS PROTEIN KINASE C INHIBITORS

Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer. © KIPO & WIPO 2007 ...

TREATMENT OF AUTOIMMUNE DISEASES

Methods of treating various autoimmune diseases, such as multiple sclerosis, peripheral neuritis, optica! neuritis, amylotrophic lateral sclerosis, and uveitis utilizing specific amino alcohol derivatives are provided herein. © KIPO & WIPO 2008 ...

3,5-DI(ARYL - ODER HETEROARYL) ISOXAZOLE UND 1,2,4-OXADIAZOLE ALS S1P1-REZEPTORAGONISTEN, DAS IMMUNSYSTEM UNTERDRÜCKENDE UND ENTZÜNDUNGSHEMMENDE MITTEL

MODIFIED SOMATOSTATIN

Somatostatin peptides containing at least one residue of formula (a), (b) or (c> <IMAGE> wherein one of Y1 and Y2 is hydrogen and the other is hydroxy or both are hydrogen, each of f and g independently is 0 or 1, one of X1 and X2 is hydrogen and the other is hydrogen or an amino protecting group, and X3 is C2-4 alkylene, the free bond in each residue (a), (b) or (c) being located at the N-terminal group of the peptide, and the physiologically-acceptable others and physiologically-hydrolysable and - acceptable esters thereof when the peptide contains at least one residue of formula (a) or (b), in free form, salt form or complex form have pharmacological activity, in particular GH-, gastric and pancreatic secretion inhibiting activity.

SUBSTITUTED DIAZEPAN

MARKED POLYPEPTIDDERIVATE.

INDOLYLMALEIMIDDERIVATIVE AS PROTEIN KINASE C INHIBITORS

AMINOPROPANOLDERIVATE

BIPIPERIDIN DERIVATIVES AND YOUR USE AS INHIBITORS THAT CHEMOKINREZEPTOREN

Somatostatin peptides linked to chelating groups via spaces

Improvements in or relating to organic compounds

PEPTIDE DERIVATIVES

Somatostatin peptides bearing at least one chelating group for a detectable element, said chelating group being linked to an amino group of said peptide, and said amino group having no significant binding affinity for somatostatin receptors, in free or salt form, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of somatostatin receptor positive tumors or for therapy.

SOMATOSTATIN PEPTIDES

Somatostatin analogues comprising the amino acid sequence of the formula (I): -(D/L)Trp-Lys-X1-X2, wherein X1 is a substituted Thr, Ser, Tyr, Glu or Cys residue and X2 is an .alpha.-amino acid having an aromatic residue on the C.alpha. side chain, or an amino acid unit selected from Dab, Dpr, Dpm, His (Bzl)HyPro, thienyl-Ala, cyclohexyl-Ala and t.-butyl-Ala, the residue Lys of said sequence corresponding to the residue Lys9 of the native somatostatin-14, in free form, in salt form or complexed with a detectable element have interesting pharmacological properties.

2-AMINO-PROPANOL DERIVATE

CALCITONIN PEPTIDE DERIVATIVES

PIPERIDINDERIVATE AS CCR5-INHIBITOREN

CHELATBILDENDE GROUPS ABSTENTIONS SOMASTOTATIN SIMILAR ONES AND THEIR RADIO MARKING COMPOSITIONS

SOMATOSTATINPEPTIDE

SYNTHESIS OF PEPTIDES CONTAINING SACCHARIDES

SYNTHESIS OF PEPTIDES CONTAINING SACCHARIDES

Indolylmaleimide derivatives as protein kinase C inhibitors

PHENYL-OXETANYL-DERIVATIVES

Novel organic compounds are described and claimed which may in particular be useful in the treatment of diseases being triggered by the (human) autoimmune system.

PEPTIDE DERIVATIVES

The present invention provides a sugar derivative of a biologically active peptide, which derivative has a prolonged duration of action when compared to the non-sugar modified peptide, and contains at least on one of the amino acid units a sugar residue which is attached to an amino group thereof by a coupling other than a direct N-glycosidic bond, and additionally, when it is a condensation product of a carboxyl group containing sugar and a peptide with less than 8 amino acid units, by a coupling other than a direct amide bond.

PEPTIDE DERIVATIVES

Somatostatin peptides

2-AMINO-PROPANOL DERIVATIVES

Compounds of formula (I), wherein m, R, R1 and R3 to R6 are as defined in the specification, m, is 1, 2 or 3 and X is O or a direct bond, and the corresponding unphosporylated compounds have interesting properties, e.g. immunosuppressive properties. © KIPO & WIPO 2007 ...

SOMATOSTATIN ANALOGUES

The invention provides cyclo[{4-(NH-CH- NH-CO-O-)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which has interesting pharmaceutical properties.224 © KIPO & WIPO 2007 ...

Treatment of autoimmune diseases

Somatostatin peptides

Somatostain analogues comprising the amino acid sequence of the formula (I): -(D/L)Trp-Lys-X1-X2, wherein X1 is a substituted Thr, Ser, Tyr, Glu or Cys residue and X2 is an alpha-amino acid having an aromatic residue on the Calpha side chain, or an amino acid unit selected from Dab, Dpr, Dpm, His (Bzl)HyPro, thienyl-Ala, cyclohexyl-Ala and t.-butyl-Ala, the residue Lys of said sequence corresponding to the residue Lys9 of the native somatostatin-14, in free form, in salt form or complexed with a detectable element have interesting pharmacological properties.

BEHANDLUNG VON AUTOIMMUNKRANKHEITEN

PEPTIDE DERIVATIVES

MODIFIED SOMATOSTATIN.

Somatostatin peptides containing at least one residue of formula (a), (b) or (c> wherein one of Y1 and Y2 is hydrogen and the other is hydroxy or both are hydrogen, each of f and g independently is 0 or 1, one of X1 and X2 is hydrogen and the other is hydrogen or an amino protecting group, and X3 is C2-4 alkylene, the free bond in each residue (a), (b) or (c) being located at the N-terminal group of the peptide, and the physiologically-acceptable ethers and physiologically-hydrolysable and -acceptable esters thereof when the peptide contains at least one residue of formula (a) or (b). In free form, salt form or complex form have pharmacological activity, in particular GH-, gastric and pancreatic secretion inhibiting activity.

Peptide derivatives

Peptide derivatives selected from (i) a calcitonin peptide and a LHRH antagonist peptide modified by at least one sugar residue and/or at least one short polyhydroxy compound or derivative, and (ii) a calcitonin peptide modified by at least one formyl and/or at least C3-5 alkyl attached to an amino group other than a N-terminal amino group, and (iii) a calcitonin peptide modified by a combination of said substituents, with the provisos that i) when the calcitonin peptide comprises at least one sugar residue a), this sugar residue is attached by a coupling other than a direct N-glycosidic bond to an omega -amino group of an omega -amino substituted side chain in the 24 position, and ii) when the LHRH antagonist comprises at least one sugar residue a), this sugar residue is an Amadori sugar residue attached by a coupling other than a direct N-glycosidic bond to an omega -amino group of an omega -amino substituted side chain in the 8 position in free form or in salt or complex form have pharmacological activity.

Peptides

IMPROVEMENTS IN OR RELATING TO ORGANIC COMPOUNDS

Variants of parathyroid hormone and its fragments

POLYPEPTIDE DERIVATIVES

A biologically active peptide selected from growth factors, peptide hormones, interferons and cytokines and analogues and derivatives thereof, and bearing at least one chelating group linked to an amino group of said peptide, the chelating group being capable of complexing a detectable element and such amino group having no significant binding affinity to target receptors, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of target tissues or for therapy.

POLYPEPTIDES

Cyclic or linear somatostatin peptides bearing a specific chelating group on the terminal amino group, in free or salt form, are complexed with a .beta.-, .gamma.- or positron-emitting element and are useful as radiopharmaceuticals.

SOMATOSTATIN ANALOGS CONTAINING CHELATING GROUPS AND THEIR RADIOLABELED COMPOSITIONS

Compounds of formula I (see formula I) wherein M is a cation equivalent and A is Phe or Tyr, in free form or in salt form are useful as radiopharmaceuticals when complexed with an .alpha.- or .beta.-emitting radionuclide or a nuclide with Auger-e- -cascades.

Peptide derivatives of LH-RH antagonists, their preparation and their use as medicinal products

The subject of the present invention is new derivatives of LH-RH antagonising peptides which are substituted by at least one carbohydrate residue and/or at least one short polyhydroxy compound, in free form or in the form of a salt or a complex. These compounds can be used as medicinal products.

BIPIPERIDINYL-DERIVATIVES AND THEIR USE AS CHEMOKINE RECEPTORS INHIBITORS

SUBSTITUIERTE DIAZEPAN

PEPTIDE DERIVATIVES

Parathyroid hormone variants

PTH compounds having PTH-like activity and comprising at least one modification, said modification being either 1. at least one radical selected from a L- or D-* small Greek alpha *-amino acid, C* subscript minus * oxycarbonyl and optionally substituted C* three eighths * yl, C* subscript minus * enyl, C* subscript minus * ynyl, aralkyl, aralkenyl or C* superscript dot; dot above * loalkyl-C* three eighths * yl and attached to the terminal amino group of the PTH compound, and/or at least one radical selected from C* subscript minus * oxycarbonyl and optionally substituted C* three eighths * yl, C* subscript minus * enyl, C* subscript minus * ynyl, aralkyl, aralkenyl or C* superscript dot; dot above * loalkyl-C* three eighths * yl and attached to one or more side chain amino groups of the PTH compound, ``` or 2. at least one * small Greek alpha *-amino acid unit in the positions 1 to 38 of a naturally occurring PTH sequence being replaced by a natural or unnatural amino acid unit optionally ...

Aminopropanol derivatives as sphingosine-1-phosphate receptor modulators

Somatostatin analogues

SOMATOSTATIN PEPTIDE WITH CHELATING GROUP(S)

Uso del 2-amino-2[4-(benciloxifeniltio)-2-cloro -fenil]propil-1,3-propanodiol en el tratamiento de la esclerosis lateral amiotrófica y uveítis. (divisional de la solicitud cl 2370-06)

SOMATOSTATIN ANALOGUES CONTAINING CHELATING GROUPS.

Somatostatin peptides bearing at least one chelating group for a detectable element, said chelating group being linked to an amino group of said peptide, and said amino group having no significant binding affinity for somatostatin receptors, in free or salt form, are complexed with a detectable element and as such are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of somatostatin receptor positive tumors or for therapy.

SOLID PHASE SYNTHESIS OF PEPTIDE ALCOHOLS

Oxadiazole derivatives with anti-inflammatory and immunosuppressive properties

Indolylmaleimide derivatives as protein kinase C inhibitors

Treatment of autoimmune diseases

POLYCYCLIC OXADIAZOLES OR I SOXAZOLES AND THEIR USE AS SlP RECEPTOR LIGANDS

Disclosed are polycyclic compounds of formula I which are useful as sphingosine-1-phosphate (S 1 P) receptor ligands, particularly as immunosuppressants. © KIPO & WIPO 2008 ...

Somatostatin analogues

The invention provides cyclo[{4-(NH2C2H4NHCOO)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which has interesting pharmaceutical properties.

PEPTIDE DERIVATIVE

NEW MATERIAL: Somatostatin peptide containing at least one residue shown by formula I (Y1, Y2 are H, OH; f,g are 0.1), formula II, or formula III (X1, X2 are H, amino protection group; X3 is 2-8C alkkylene) and its physiologically allowable free ether and ester, or acid adduct, or complex. USE: Remedy of terminal macrosis, true diabete, etc. PROCESS: For example, a compound given by formula IV (Z2 is CHO, CH2CH2OH, etc.) is aminated reductively by a compound shown by formula P-NH2 (P is a protected somatostantin perptide residue), and a somatostatin peptide derivative is obtained by removing the protective group as required. COPYRIGHT: (C)1989,JPO ...

Improvements in or relating to organic compounds

PEPTIDE DERIVATIVES

Somatostatin peptides

Somatostatin analogues

3,5-DI (ARYL OR HETEROARYL) ISOXAZOLES AND 1, 2, 4-OXADIAZOLES AS S1P1 RECEPTOR AGONISTS, IMMUNOSUPPRESSIVE AND ANTI -INFLAMMATORY AGENTS

The present invention relates to polycyclic compounds of formula (I), processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.

DIARYL OXADIAZOL DERIVATIVES

Disclosed are polycyclic compounds of the following formula (I) and their use as anti-inflammatory and immunosuppressive agents.

Peptide derivatives

SOMATOSTATIN PEPTIDES AND PROCESSES FOR THEIR PRODUCTION

Aminopropanol derivatives

POLYPEPTIDE DERIVATIVES

... of the invention A biologically active peptide selected from growth factors, peptide hormones, interferons and cytokines and analogues and derivatives thereof, and bearing at least one chelating group linked to an amino group of said peptide, the chelating group being capable of complexing a detectable element and such amino group having no significant binding affinity to target receptors, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of target tissues or for therapy.

AMINOPROPANOLDERIVATE

LHRH peptide derivatives.

A LHRH antagonist peptide modified by at least one sugar residue and/or at least one short polyhydroxy compound or derivative, with the proviso that when the LHRH antagonist comprises at least one sugar residue, this sugar residue is an Amadori sugar residue attached by a coupling other than a direct N-glycosidic bond to an omega -amino group of an omega -amino substituted side chain in the 8 position. The peptide may be in free form or in salt or complex form. A process for the preparation of these compounds is disclosed. The LHRH peptide derivatives have pharmological activity.

LHRH PEPTIDE DERIVATIVES

IMPROVEMENTS IN OR RELATING TO ORGANIC COMPOUNDS

IMPROVEMENTS IN OR RELATING TO ORGANIC COMPOUNDS

SOMATOSTATIN PEPTIDES

Somatostatin analogues comprising the amino acid sequence of the formula (I): -(D/L)Trp-Lys-X1-X2, wherein X1 is a substituted Thr, Ser, Tyr, Glu or Cys residue and X2 is an .alpha.-amino acid having an aromatic residue on the C.alpha. side chain, or an amino acid unit selected from Dab, Dpr, Dpm, His (Bzl)HyPro, thienyl-Ala, cyclohexyl-Ala and t.-butyl-Ala, the residue Lys of said sequence corresponding to the residue Lys9 of the native somatostatin-14, in free form, in salt form or complexed with a detectable element have interesting pharmacological properties.

GAS TURBINE DISMOUNTING METHOD AND CALIBRATION DEVICE

Disclosed is a dismounting method for gas turbines (11) for replacing and/or inspecting and/or repairing components located in a front bearing compartment (5) of the gas turbine (11), the gas turbine (11) comprising at least one fan module (1), a gas turbine casing, a low-pressure system and a high-pressure system, the low-pressure system comprising a low-pressure compressor (4), a low-pressure turbine (9), a connecting shaft (13), a flanged shaft (8) and an N1 shaft (10) which is connected to the low-pressure compressor (4) via the flanged shaft (8) and the connecting shaft (1); the connecting shaft (13) is mounted in the gas turbine casing via a first bearing unit (6), and the flanged shaft (8) is mounted in the gas turbine casing via a second bearing unit (7); the dismounting method comprises at least the following steps: a) dismounting the fan module (1), b) securing the N1 shaft (10) relative to the gas turbine casing in the axial direction using a securing device (14), and c) dismounting ...

TREATMENT OF AUTOIMMUNE DISEASES

Methods of treating various autoimmune diseases, such as multiple sclerosis, peripheral neuritis, optical neuritis, amylotrophic lateral sclerosis, and uveitis utilizing specific amino alcohol derivatives are provided herein.

PEPTIDE DERIVATIVE

NEW MATERIAL: Somatostatin peptide (salt) having a chelating group for a detectable element linked to its amino group represented by formula I [wherein A is 1-12C alkyl or a group represented by formula RCO (R is H, 1-11C alkyl or phenyl); A' is H or 1-12C alkyl; Y1 and Y2 are combined to form a direct bond or a group represented by formula II (Ra is methyl; Rb is H or methyl; and (m) is 1-4); B is (substd.) Phe; C is (substd.) Trp; D is Lys; and E is Thr; G is carboxylic acid, ester or amide]. USE: A remedy and a diagnostic imaging reagent of somatostatin receptor positive tumors. PROCESS: For example, two peptide fragments are successively linked by an amido linkage obtaining desired amino acid sequences to obtain somatostatin peptide and, thereafter, a chelating group is introduced into an N-amino group by a chelating agent and a mercapto group of a Cys group is oxidized to perform S-S crosslinking to obtain peptide represented by formula I. COPYRIGHT: (C)1990,JPO ...

SOMATOSTATINPEPTIDE

DETECTABLE SOMATOSTATIN ANALOGUES CONTAINING A CHELATING GROUP

POLYPEPTIDES

Aminopropanol derivatives

Indolylmaleimide derivatives

Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.

AMINOPROPANOL DERIVATIVES

Compounds of formula I: 1. (canceled)4. (canceled)6. A method according to claim 7 , wherein the HPLC of step (b) is using a chiral ion-exchange phase based on quinine carbamate or quinidine carbamate.8. (canceled)9. A method for preventing or treating acute or chronic transplant rejection or T-cell mediated inflammatory or autoimmune diseases in a subject in need of such treatment claim 2 , which method comprises administering to said subject an effective amount of a compound as defined in claim 2 , or a pharmaceutically acceptable salt thereof.11. A compound of formula II according to claim 3 , wherein said compound comprises the S enantiomer of phosphoric acid mono-[2-amino-2-hydroxymethyl-4-(4-octyl-phenyl)-butyl]ester.12. A compound of formula II according to claim 2 , wherein greater than 90% of the compound by weight is in the form of the R or S enantiomer.13. A compound of formula II according to claim 2 , wherein greater than 95% of the compound by weight is in the form of the R or S enantiomer.14. A compound of formula II according to claim 2 , wherein greater than 99% of the compound by weight is in the form of the R or S enantiomer. The present invention relates to organic compounds, a process for their production and pharmaceutical compositions containing them.More particularly the present invention provides a compound of formula I:wherein each of m and n, independently, is 1, 2 or 3; X is O or a direct bond;When in the compounds of formula I the carbon chain as Ris substituted, it is preferably substituted by halogen, nitro, amino, hydroxy or carboxy. When the carbon chain is interrupted by an optionally substituted phenylene, the carbon chain is preferably unsubstituted. When the phenylene moiety is substituted, it is preferably substituted by halogen, nitro, amino, methoxy, hydroxy or carboxy.In the compounds of the invention, the following significances are preferred individually or in any sub-combination:A particularly preferred compound is ...

Hydrothermal synthesis of zeolites or zeolite-like materials using modified mixed hydroxides

This invention relates to a process for producing aluminium silicates in the form of zeolite L, as well as the intermediate and end products of this process. The invention further relates to the use of these aluminium silicates for the conversion or adsorption of hydrocarbons.

IMPROVED METHOD FOR THE CATALYZED HYDROISOMERISATION OF HYDROCARBONS

The invention relates to an arrangement of several layers of catalysts arranged in series in a reactor for the hydroisomerisation of hydrocarbons, to a method for the hydroisomerisation of hydrocarbons and to the use of the arrangement for the hydroimerisation of hydrocarbons. 1. Catalyst arrangement in a reactor for hydroisomerisation of hydrocarbons , wherein at least two catalyst layers are arranged in the reactor , wherein the first catalyst layer is arranged upstream and the second catalyst layer is arranged downstream , and wherein the catalyst of the first catalyst layer is a supported precious metal catalyst for a hydrogenation of the reaction fluid and the catalyst of the second catalyst layer is a bifunctional supported precious metal catalyst , the support of which has acidic or basic properties , for the isomerisation of the reaction fluid after passing through the first catalyst layer.2. Catalyst arrangement according to claim 1 , wherein the support of the catalyst of the first catalyst layer comprises an aluminium oxide claim 1 , silicon oxide claim 1 , a metal foam claim 1 , ceramic or a thermally stable polymer.3. Catalyst arrangement according to claim 1 , wherein the catalyst of the second catalyst layer comprises claim 1 , as active component claim 1 , an amorphous aluminosilicate claim 1 , zeolite claim 1 , chlorinated aluminium oxide claim 1 , tungstenated zirconium oxide or sulfonated zirconium oxide.4. Catalyst arrangement according to claim 3 , wherein the catalyst of the second catalyst layer comprises claim 3 , as active component claim 3 , tungstenated zirconium oxide or sulfated zirconium oxide claim 3 , and has been promoted with a transition element or rare earth element.5. Catalyst arrangement according to claim 1 , wherein the downstream catalyst has an immobilized acid or ionic liquid on the support.6. Catalyst arrangement according to claim 1 , wherein the active component of the downstream catalyst has been embedded in a thermally ...

Somatostatin Analogues

The invention provides cyclo[{4-(NH—CH—NH—CO—O—)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which has interesting pharmaceutical properties. 2. The method according to wherein said somatostatin receptor expressing or accumulating tumor is a malignant bowel obstruction.3. The method according to wherein said somatostatin receptor expressing or accumulating tumor is a neuroendocrine tumor.5. The method according to wherein said gastrointestinal hormone secreting tumor is a carcinoid tumor. This application is a divisional of U.S. application Ser. No. 12/265,135 filed Nov. 5, 2008 which is a divisional of application Ser. No. 10/343,288 filed Aug. 26, 2003 now U.S. Pat. No. 7,473,761 which is a National Stage of International Application PCT/EP01/08824 filed on Jul. 30, 2001, which in its entirety is herein incorporated by reference.The present invention relates to somatostatin peptidomimetics, a process for their production and pharmaceutical preparations containing them.More particularly the present invention provides the compound of formulaalso called cyclo[{4-(NH—CH—NH—CO—O—)Pro}-Phg-DTrp-Lys-Tyr(4-Bzl)-Phe], referred herein to as Compound A, as well as diastereoisomers and mixtures thereof, in free form, in salt or complex form or in protected form. Phg means —HN—CH(CH)—CO— and Bzl means benzyl.Compound A in protected form corresponds to above molecule wherein at least one of the amino groups is protected and which by deprotection leads to Compound A, preferably physiologically removable. Suitable amino protecting groups are e.g. as disclosed in “Protective Groups in Organic Synthesis”, T. W. Greene, J. Wiley & Sons NY (1981), 219-287, the contents of which being incorporated herein by reference. Example of such an amino protecting group is acetyl.When Compound A exists in complex form, it may conveniently be a Compound A bearing a chelating group on the side chain amino group of Pro ...

Disassembly Method for a Gas Turbine

Disassembly method for gas turbines () for replacing and/or inspecting and/or repairing components arranged in a front bearing region () of the gas turbine (), 1. A method for disassembling a gas turbine for replacing and/or inspecting and/or repairing components arranged in a front bearing region of the gas turbine , comprising:providing a fixing device;providing a guide device; at least one fan module,', 'a gas turbine housing,', 'a low-pressure system, and', 'a high-pressure system,', a low-pressure compressor,', 'a low-pressure turbine,', 'a connecting shaft,', 'a stub shaft, and', 'an N1 shaft,', 'wherein the N1 shaft is connected to the low-pressure compressor via the stub shaft and the connecting shaft,', 'wherein the connecting shaft is supported in the gas turbine housing via a first bearing unit,, 'wherein the low-pressure system comprises, 'wherein the stub shaft is supported in the gas turbine housing via a second bearing unit; and, 'providing a gas turbine, wherein the gas turbine comprisesdismounting the fan module;fixing the N1 shaft in an axial direction relative to the gas turbine housing using the fixing device;dismounting the stub shaft using the guide device,wherein an orientation of the guide device relative to the gas turbine in at least one spatial direction is determined by a component of a portion of the gas turbine not yet dismounted,wherein dismounting the stub shaft comprises dismounting the stub shaft after fixing the N1 shaft in an axial direction relative to the gas turbine housing using the fixing device and after dismounting the fan module.2. The method according to claim 1 , dismounting an exhaust gas cone; and then', 'mounting the fixing device in the location of the exhaust gas cone; and then', 'connecting the N1 shaft to the fixing device., 'wherein fixing the N1 shaft in the axial direction relative to the gas turbine housing using the fixing device comprises3. The method according to claim 1 , further comprising:providing a ...

Peptide derivatives

Somatostatin polypeptides containing at least one radical of the formula (a), (b) or (c) <IMAGE> in which Y1 is hydrogen, Y2 is hydrogen or hydroxyl, f and g are, independently of one another, 0 or 1, X1 is hydrogen, X2 is hydrogen or an amino protective group, and X3 is C2-6-alkylene, where the free valency in the radical (a), (b) or (c) is linked to the N-terminal amino group of the peptide, and the physiologically acceptable ethers and physiologically hydrolysable and acceptable esters thereof when the peptide contains at least one radical of the formula (a) or (b), in free form or in the form of an acid addition salt or complex. Compounds of this type have valuable pharmaceutical properties, in particular inhibiting GH, gastric and pancreatic secretion.

Patent CH677795A5

Process for preparing a biologically active, post- translationally modified protein hormone which is composed of several subunits, a eucaryotic cell which is transfected with one or more expression vectors and is able to produce such a hormone, and expression vector which comprises heterologous DNA which encodes the subunits of the hormone, a set of expression vectors in which each vector comprises heterologous DNA which encodes a different one of the subunits of the hormone, and a process for producing a pharmacetuial preparation.

Modified somatostatin

Somatostatin peptides containing at least one residue of formula (a), (b) or (c> < IMAGE > wherein one of Y1 and Y2 is hydrogen and the other is hydroxy or both are hydrogen, each of f and g independently is 0 or 1, one of X1 and X2 is hydrogen and the other is hydrogen or an amino protecting group, and X3 is C2-4 alkylene, the free bond in each residue (a), (b) or (c) being located at the N-terminal group of the peptide, and the physiologically-acceptable others and physiologically-hydrolysable and - acceptable esters thereof when the peptide contains at least one residue of formula (a) or (b), in free form, salt form or complex form have pharmacological activity, in particular GH-, gastric and pancreatic secretion inhibiting activity.

NOVEL SOMATOSTATIN PEPTIDES, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS

Somatostatin peptide derivatives

SOMATOSTATINIC PEPTIDES, PROCEDURE FOR THEIR PRODUCTION, PHARMACEUTICAL PREPARATIONS THAT CONTAIN THEM AND USE THEM AS MEDICATIONS

Process for producing peptonic derivatives modified with sugar and pharmaceutical preparatives containing these compounds as active substance

NOVEL PEPTIDES OF SOMATOSTATIN, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS

L'invention concerne les peptides de la somatostatine comprenant au moins un reste de formule a, b ou c (CF DESSIN DANS BOPI) dans lesquelles l'un des symboles Y1 et Y2 signifie l'hydrogène et l'autre un groupe hydroxy ou bien les deux symboles Y1 et Y2 signifient l'hydrogène, f et g signifient indépendamment 0 ou 1, l'un des symboles X1 et X2 signifie l'hydrogène et l'autre signifie l'hydrogène ou un groupement protecteur du groupe amino et X3 signifie un groupe alkylène en C2 -C6 , la valence libre dans chaque reste a, b ou c étant située sur le groupe amino N-terminal du peptide. Ces composés peuvent être utilisés comme médicaments. The invention relates to somatostatin peptides comprising at least one residue of formula a, b or c (DRAWING CF IN BOPI) in which one of the symbols Y1 and Y2 signifies hydrogen and the other a hydroxy group or else the two symbols Y1 and Y2 mean hydrogen, f and g independently mean 0 or 1, one of the symbols X1 and X2 means hydrogen and the other means hydrogen or a protecting group of the amino group and X3 means a C2 -C6 alkylene group, the free valence in each a, b or c residue being located on the N-terminal amino group of the peptide. These compounds can be used as drugs.

PEPTIDE DERIVATIVES

SOMATOSTATINIC PEPTIDES, PROCEDURE FOR THEIR PRODUCTION, PHARMACEUTICAL PREPARATIONS THAT CONTAIN THEM AND USE THEM AS MEDICATIONS

With sugar residues modified peptides.

Patent CH679045A5

Peptide derivatives.

SOMATOSTATIN PEPTIDES BEARING AT LEAST ONE CHELATING GROUP FOR A DETECTABLE ELEMENT, SAID CHELATING GROUP BEING LINKED TO AN AMINO GROUP OF SAID PEPTIDE, AND SAID AMINO GROUP HAVING NO SIGNIFICANT BINDING AFFINITY FOR SOMATOSTATIN RECEPTORS, IN FREE OR SALT FORM, ARE COMPLEXED WITH A DETECTABLE ELEMENT AND AS SUCH ARE USEFUL AS A PHARMACEUTICAL, E.G. A RADIOPHARMACEUTICAL FOR IN VIVO IMAGING OF SOMATOSTATIN RECEPTOR POSITIVE TUMORS OR FOR THERAPY.

Disassembly method for gas turbines and calibration device

PEPTIDE DERIVATIVES

NOVEL PEPTIDE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS

Cyclic somatostatin hexapeptides, pharmaceutical composition containing them and use thereof

Described are analogues of somatostatin, containing a sequence of somatostatin from the general formula (I), where X1 is a substituted residue Thr, Ser, Tyr, Glu or Cys and X2 is alpha-amino acid with aromatic residue on Calpha lateral chain, or the amino acid chosen from the group containing Dab, Dpr, Dpm, His, (Bzl)HyPro, thienyl-Ala, cyclohexyl-Ala and tert-butyl-Ala, in a free form, in a form of salt or in a complex with detectable element, where these have considerably interesting pharmacological properties.

Patent FR2609991B1

TREATMENT OF AUTOIMMUNE DISEASES

L'INVENTION PORTE SUR DES MÉTHODES DE TRAITEMENT DE DIVERSES MALADIES AUTO-IMMUNES, TELLES QUE LA SCLÉROSE EN PLAQUE, LA NÉVRITE PÉRIPHÉRIQUE, LA NÉVRITE OPTIQUE, LA SCLÉROSE AMYOTROPHIQUE LATÉRALE ET L'UVÉITE, CES MÉTHODES UTILISANT DES DÉRIVÉS AMINO-ALCOOL SPÉCIFIQUES. THE INVENTION INVOLVES METHODS OF TREATING VARIOUS AUTOIMMUNE DISEASES, SUCH AS PLATE SCLEROSIS, PERIPHERAL NEUROTNESS, OPTICAL NEVERTHRITIS, LATERAL AMYOTROPHIC SCLEROSIS, AND UREITY, THESE METHODS USING SPECIFIC AMINO ALCOHOL DERIVATIVES.

DIAZEPANES REPLACED.

Un sistema automatizado (10) para cargar una pluralidad de semillas (110) de radioisótopos de baja dosis en al menos una aguja de implante (130), para su uso en procedimientos de radioisótopos de baja dosis, incluyendo el mencionado sistema un cartucho reemplazable que tiene al menos una abertura (50) y teniendo un tambor (54) giratorio para precargar las mencionadas semillas de radioisótopos en cámaras (52) separadas alrededor de la periferia del mencionado tambor giratorio, incluyendo el mencionado cartucho además un par de motores por pasos (56, 58), en el que el primer motor por pasos (56) es para accionar el mencionado tambor giratorio, y el segundo motor por pasos (58) para accionar un conjunto de cabestrante (60) que es operable para accionar una barra de empuje (62) a lo largo de una línea de recorrido a través de una cámara indexada selectivamente de las mencionadas cámaras (52), y una estación de carga (12), que tiene una estructura de recepción del cartucho (16) para acoplarse con el mencionado cartucho, y un sistema de control de movimiento automatizado (32) para provocar selectivamente que las mencionadas semillas de radioisótopos sean eyectadas desde la mencionada cámara (52) indexada selectivamente del mencionado cartucho, cuando el mencionado cartucho sea montado en la mencionada estructura receptora de cartuchos, y siendo posicionada la mencionada aguja con respecto al menos a una abertura del mencionado cartucho. An automated system (10) for loading a plurality of seeds (110) of low dose radioisotopes into at least one implant needle (130), for use in low dose radioisotope procedures, said system including a replaceable cartridge that It has at least one opening (50) and having a rotating drum (54) for preloading said radioisotope seeds in chambers (52) separated around the periphery of said rotating drum, the said cartridge also including a pair of stepper motors ( 56, 58), in which the first stepper motor (56) is to drive said rotating drum, and ...

Aminopropanol derivatives as sphingosine-1-phosphate receptor modulators

Compounds of formula I, wherein X, a, b, R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.

POLYCYCLIC OXADIAZOLES OR I SOXAZOLES AND THEIR USE AS SlP RECEPTOR LIGANDS.

Se dan a conocer compuestos policiclicos de la Formula I: (ver formula I) los cuales son utiles como ligandos del receptor de esfingosina-1-fosfato (S1P), en particular como inmunosupresores.

Peptide derivatives

Somatostatin peptides bearing at least one chelating group for a detectable element, said chelating group being linked to an amino group of said peptide, and said amino group having no significant binding affinity for somatostatin receptors, in free or salt form, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of somatostatin receptor positive tumors or for therapy.

Peptides

PTH compounds having PTH-like activity and comprising at least one modification, said modification being either 1. at least one radical selected from a L- or D-α-amino acid, C 2-6 alcoxycarbonyl and optionally substituted C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, aralkyl, aralkenyl or C 3-6 cycloalkyl-C 1-4 alkyl and attached to the terminal amino group of the PTH compound, and/or at least one radical selected from C 2-6 alcoxycarbonyl and optionally substituted C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, aralkyl, aralkenyl or C 3-6 cycloalkyl-C 1-4 alkyl and attached to one or more side chain amino groups of the PTH compound, or 2. at least one α-amino acid unit in the positions 1 to 38 of a naturally occurring PTH sequence being replaced by a natural or unnatural amino acid unit optionally in protected form, whereby the α-amino acid units present in positions 1 and 2 at the amino terminus of the PTH sequence may be replaced by a pseudo-peptide, or a combination of such modifications, in free form or in salt form, have pharmacological activity, e.g. for preventing or treating all bone conditions which are associated with increased calcium depletion or resorption or in which calcium fixation in the bone is desirable.

Phenyl-oxetanyl-derivatives

Novel organic compounds are described and claimed which may in particular be useful in the treatment of diseases being triggered by the (human) autoimmune system.

DIAZEPANES, PROCESS FOR THE PREPARATION AND PHARMACEUTICAL COMPOSITION THAT CONTAINS THEM

La presente invención se relaciona con un compuesto de la fórmula l:<EMI FILE="00077443_1" ID="1" IMF=JPEG >en donde:n es1, 2, ó 3, R1 es H, alquilo de 1 a 4 átomos de carbono; arilo; o arilalquilo de 1 a 4 átomos de carbono;Y es alquileno de 1 a 4 átomos de carbono; -CO-C-alquileno de 1 a 4 átomos de carbono; -CO-C-alquenileno de 2 a 5 átomos de carbono; -CO-NH-; -CO-C-alquileno de 1 a 3 átomos de carbono-NH-; ó -CO-O-,R2 es un residuo aromático o heteroaromático, cada uno opcionalmente sustituido por CF3, halógeno, OH, alcoxilo de 1 a 4 átomos de carbono, amino, amino sustituido por mono- o di-alquilo de 1 a 4 átomos de carbono, fenilo, bencilo, o alquilo de 1 a 4 átomos de carbono opcionalmente sustituido por amino,R3 es la cadena lateral presente sobre el Ca de un a-aminoácido,R4 es bifenililo; o bencilo, hidroxibencilo, a - ó ß-naf-tilmetilo, 5,6,7,8-tetrahidro-ß-naftilmetilo, o indolilmetilo, cada uno opcionalmente sustituido sobre el anillo por CF3, halógeno, OH, alcoxilo de 1 a 4 átomos de carbono, amino, amino sustituido por mono- o di-alquilo de 1 a 4 átomos de carbono, fenilo, bencilo, o alquilo de 1 a 4 átomos de carbono opcionalmente sustituido por amino, yX es -CN; -NR5R6; u -O-R8, en donde R5 es H, alquilo de 1 a 6 átomos de carbono, arilo, o arilalquilo de 1 a 4 átomos de carbono, R6 es H ó alquilo de 1 a 6 átomos de carbono, y R8 es H, alquilo de 1 a 4 átomos de carbono, arilo, o arilalquilo de 1 a 4 átomos de carbono, en forma libre o en forma de sal. Igualmente, se refiere al proceso para la preparación de dicho compuesto y a composiciones farmacéuticas que lo contienen. The present invention relates to a compound of the formula l: <EMI FILE = "00077443_1" ID = "1" MFI = JPEG> wherein: n is 1, 2, or 3, R1 is H, alkyl of 1 to 4 atoms carbon; aryl; or arylalkyl of 1 to 4 carbon atoms, and is alkylene of 1 to 4 carbon atoms; -CO-C-alkylene of 1 to 4 carbon atoms; -CO-C-alkenylene of 2 to 5 carbon atoms; -CO ...

polypeptide derivatives

Indolylmaleimide derivatives

Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.

Process for producing peptide derivatives

2-amino-propanol derivatives

Compounds of formula I wherein m, R, R 1 and R 3 to R 6 are as defined in the specification, m, is 1, 2 or 3 and X is O or a direct bond, and the corresponding unphosporylated compounds have interesting properties, e.g. immunosuppressive properties.

SUBSTITUTED DIAZEPANES

Polypeptide

BIPIPERIDIN DERIVATIVES AND THEIR USE AS INHIBITORS OF CHEMOKIN RECEPTORS

Indolylmaleimidderivative als proteinkinase-c-inhibitoren

Indolylmaleimide derivatives as protein kinase c inhibitors

Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.

Peptides

Bipiperidinyl-derivatives and their use as chemokine receptors inhibitors

Piperidine derivatives of formula (I) as disclosed in the specification have interesting pharmaceutical properties e.g. as CCR5 inhibitors.

Oxadiazole derivatives with anti-inflammatory and immunosuppressive properties.

Se dan a conocer compuestos policíclicos de la siguiente fórmula I: (ver fórmula (I)) y su uso como agentes anti-inflamatorios e inmunosupresores.

Somatostatin analogues

The invention provides cyclo[{4-(NH2-C2H4-NH-CO-O-)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which has interesting pharmaceutical properties.

Aminopropanol derivatives as sphingosine-1-phosphate receptor modulators

Compounds of formula (I), wherein X, a, b, R1, R2, R3, R4and R5 are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.

2-aminopropanol derivatives

Forbindelser med formel I. hvori m, R, RI, og Rtil Rer som definert i beskrivelsen, m er 1, 2 eller 3 og X er O eller en direkte binding, og de korresponderende ufosforylerte forbindelser som har interessante egenskaper, for eksempel immunundertrykkende egenskaper.

Diazacycloalkanedione derivatives which are useful as lfa-1 antagonist

Compounds of formula (I) wherein R is carboxy, esterified carboxy or amidate d carboxy; R1 and R3 are independently lower alkyl, (hydroxy, lower alkoxy, amino, acylamino, mono- or di- lower alkylamino or mercapto)-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, cycloalkyl, aryl, biaryl, (cycloalkyl, aryl or biaryl)-lower alkyl, or (carboxy, esterified carboxy or amidated carboxy)-lower alkyl; R2 is hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, arylaminocarbonyl, or aryl-(oxy, thio or amino); n is 1 or 2; Y is lower-alkylene or lower alkenylene; and pharmaceutically acceptable salts thereof; which are useful as LFA-1 antagonists.

Substituted diazepans

The invention provides novel diazepanes having interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1, -ICAM-2 or -ICAM-3 interactions.

Somatostatin peptides

Somatostatin peptide derivative with a chelating group, for diagnostic use

Treatment of autoimmune diseases.

En la presente se proporcionan metodos para el tratamiento de diferentes enfermedades autoinmunes, tales como esclerosis multiple, neuritis periferica, neuritis optica, esclerosis lateral amiotrofica, y uveitis, utilizando derivados de amino-alcohol especificos.

Labeled Polypeptide Derivatives

A biologically active peptide selected from growth factors, peptide hormones, interferons and cytokines and analogues and derivatives thereof, and bearing at least one chelating group linked to an amino group of said peptide, the chelating group being capable of complexing a detectable element and such amino group having no significant binding affinity to target receptors, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of target tissues or for therapy.

Parathormone derivatives, process for their production and pharmaceutical compositions containing them

PTH compounds having PTH-like activity and comprising at least one modification, said modification being either 1) at least one radical selected from an L- or D-alpha-amino acid, C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to the terminal amino group of the PTH compound, and/or at least one radical selected from C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to one or more side chain amino groups of the PTH compound; or 2) at least one alpha-amino acid unit in the positions 1 to 38 of a naturally occurring PTH sequence being replaced by a natural or unnatural amino acid unit optionally in protected form, whereby the alpha-amino acid units present in positions 1 and 2 at the amino terminus of the PTH sequence may be replaced by a pseudo-peptide, or a combination of such modifications, in free form or in salt form, have pharmacological activity, e.g. for preventing or treating all bone conditions which are associated with increased calcium depletion or resorption or in which calcium fixation in the bone is desirable.

Substituted diazepanes

The invention provides novel diazepanes having interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1, -ICAM-2 or -ICAM-3 interactions.

2-amino-propanol derivatives

SOMATOSTATIN DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MEDICALLY

An indolylmaleimide compound, a method of its preparation, its use as a medication and a pharmaceutical composition containing this compound

Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.

Somatostatin analogues

Solid phase synthesis of peptide alcohols

Treatment of autoimmune diseases

Peptides

Aminopropanol derivatives as sphingosine-1-phosphate receptor modulators

Compounds of formula (I), wherein X, a, b, R1, R2, R3, R4 and R5 are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.

NOVEL PEPTIDE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS

L'INVENTION CONCERNE UN DERIVE GLUCOSYLE D'UN PEPTIDE BIOLOGIQUEMENT ACTIF, LEQUEL DERIVE POSSEDE UNE DUREE D'ACTION PROLONGEE PAR RAPPORT AU PEPTIDE NON MODIFIE ET CONTIENT AU MOINS SUR UN DES RESTES D'AMINO-ACIDES, UN RESTE GLUCIDIQUE FIXE AU GROUPE AMINO DU RESTE D'AMINO-ACIDE PAR UNE LIAISON AUTRE QU'UNE LIAISON N-GLUCOSIDIQUE DIRECTE ET, LORSQUE LE DERIVE EST UN PRODUIT DE CONDENSATION D'UN GLUCIDE CONTENANT UN GROUPE CARBOXY AVEC UN PEPTIDE AYANT MOINS DE 8 RESTES D'AMINO-ACIDES, PAR UNE LIAISON AUTRE QU'UNE LIAISON AMIDE. CES DERIVES PEUVENT ETRE UTILISES EN THERAPEUTIQUE COMME MEDICAMENTS. THE INVENTION CONCERNS A GLUCOSYL DERIVATIVE OF A BIOLOGICALLY ACTIVE PEPTIDE, WHEREIN DERIVATIVE HAS A LONGER PERIOD OF ACTION IN RELATION TO THE UNMODIFIED PEPTIDE AND CONTAINS AT LEAST ON AN AMINO-ACID RESIN, A GLUCID RESIDUE FIXED AT THE AMINO GROUP THE AMINO ACID STAIN BY A BOND OTHER THAN A DIRECT N-GLUCOSIDIC BOND AND, WHEN THE DERIVATIVE IS A CARBOXY GROUP-CONTAINING CONDENSATION PRODUCT WITH A PEPTIDE HAVING LESS THAN 8 AMINO ACID RESINS BY ANY LINK OTHER THAN AN AMIDE BOND. THESE DERIVATIVES MAY BE USED IN THERAPEUTICS AS MEDICAMENTS.

Treatment of autoimmune diseases

Indolylmaleimide derivatives as protein kinase c inhibitors

Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.

peptides

Peptides, method of obtaining them and pharmaceutic agents containing such peptides

Analogs of pth.

SOMATOSTATIN ANALOGUE COMPOUNDS

System and process for the isomerisation of light naphtha

The invention relates to a light-naphtha isomerisation system, comprising a reactor for carrying out an isomerisation reaction and an auxiliary separator, upstream of the reactor in terms of flow, for separating treatment gas from a reactant fluid flowing in the reactor. The invention also relates to a process for the isomerisation of light naphtha.

Chelated peptides, complexes thereof, pharmaceutical compositions containing them and their use as radiopharmaceuticals

Compounds of formula I wherein M is a cation equivalent and A is Phe or Tyr, in free form or in salt form are useful as radiopharmaceuticals when complexed with a radionuclide.

Aminopropanol derivatives as sphingosine-1-phosphate receptor modulators

Compounds of formula (I), wherein X, a, b, R1, R2, R3, R4 and R5 are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.

Polypeptides and process for producing them

Phenyl-oxetanyl-derivatives.

Se describen y se reivindican compuestos orgánicos novedosos, los cuales pueden ser particularmente útiles en el tratamiento de las enfermedades desencadenadas por el sistema autoinmunitario (humano).

Peptide derivatives

Peptides

Somatostatin peptides bearing a chelating group selected from a bifunctional N 4 -chelating group particularly suitable for Tc, Rh, Cu, Co or Re-labelling, and a bifunctional polyamino-polycarboxylic acid chelating group are complexed with a α-, β-, γ- or positron-emitting nuclide or a nuclide with Auger-e - -cascades and are useful as radiopharmaceuticals.

Bipiperidinyl-derivatives and their use as chemokine receptors inhibitors

Piperidine derivatives of formula (I) as disclosed in the specification have interesting pharmaceutical properties e.g. as CCR5 inhibitors.

Hydrothermal synthesis of zeolites or zeolite-like materials using modified mixed hydroxides

This invention relates to a process for producing aluminum silicates in the form of zeolite L, as well as the intermediate and end products of this process. The invention further relates to the use of these aluminum silicates for the conversion or adsorption of hydrocarbons.

Somatostatin analogues, method for its preparation and pharmaceutical preparations containing said analogues, and their use

Cyclo [{4- (NH2-C2H4-NH-CO-O-) Pro}-Phg-DTrp-Lys-Tyr (4-benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which is somatostatin peptidomimetic. A pharmaceutical preparation effected in the prevention or treatment of disorders with an aetiology comprising or associated with excess GH-secretion and/or excess of IGF-1 and other metabolic disorders related to insulin or glucagon release and another disorders.

Treatment of autoimmune diseases

Methods of treating various autoimmune diseases, such as multiple sclerosis, peripheral neuritis, optical neuritis, amylotrophic lateral sclerosis, and uveitis utilizing specific amino alcohol derivatives are provided herein. Figure 1.

SOMATOSTATINE PEPTIDES

Un análogo de somatostatina que comprende la secuencia deaminoácidos de la fórmula (I). Trp-Lys-X1 -X2 (I)en donde X1 es un radical de la fórmula (a) o (b)en donde R1 es fenilo opcionalmente sustituido, R2 es -Z1 -CH2 -R1 , -CH2 -CO-O-CH2 -R1 ,en donde Z1 es O o S,yX2 es un alfa- aminoácido que tiene un residuo aromático sobre la cadena lateral Calfa o una unidad de aminoácido seleccionada de Dab, Dpr, Dpm, His (Bzl)HyPro, Tienil-Ala, Ciclohexil-Ala y terbutil-Ala,el residuo Lys de esa secuencia corresponde al residuo Lys de la somatostatina 14 original, en la forma libre o en la forma de sal o de complejo. A somatostatin analog comprising the amino acid sequence of formula (I). Trp-Lys-X1 -X2 (I) where X1 is a radical of formula (a) or (b) where R1 is optionally substituted phenyl, R2 is -Z1 -CH2 -R1, -CH2 -CO-O- CH2 -R1, where Z1 is O or S, and X2 is an alpha-amino acid having an aromatic residue on the Calfa side chain or an amino acid unit selected from Dab, Dpr, Dpm, His (Bzl) HyPro, Tienil-Ala , Cyclohexyl-Ala and terbutyl-Ala, the Lys residue of that sequence corresponds to the Lys residue of the original somatostatin 14, in the free form or in the salt or complex form.

peptides