Novel Compounds

The present invention relates to the new compounds of general formula I 19. A compound of the formula I according to claim 1 , wherein{'sup': '3', 'claim-text': [{'sup': 3.1', '3.2', '3.3, '(a) a 6 or 10-membered aryl group substituted by the groups R, Rand R,'}, {'sup': 3.1', '3.2', '3.3, '(b) a 5- or 6-membered heteroaryl group substituted by the groups R, Rand Rwhich is attached via a carbon atom, or'}, {'sup': '3.2', '(c) a 5- or 6-membered heteroaryl group substituted by a group Rwhich is attached via a carbon atom and is additionally fused to a phenyl ring,'}], 'Rdenotes'}{'sup': '3.1', 'claim-text': (a) H,', {'sub': 2', '1-4', '1-4', '2, '(b) halogen, —NH, C-alkyl-NH—, (C-alkyl)N—, —CN, —OH'}, {'sub': 1-4', '1-3', '1-3, 'sup': '3.1.1', '(c) C-alkyl, R—C-alkylene, C-alkyl-O, cyclopropyl,'}, {'sub': 1-3', '1-3, '(d) a C-alkyl or C-alkyl-O— group wherein each methylene group is substituted by up to two fluorine atoms and each methyl group is substituted by up to three fluorine atoms,'}], 'Rdenotes'}{'sup': '3.1.1', 'claim-text': (a) H,', {'sub': '3-6', '(b) C-cycloalkyl,'}, {'sub': 1-4', '2', '1-4', '1-3, '(c) (C-alkyl)N—, C-alkyl-NH—, C-alkyl-O—,'}], 'Rdenotes'}{'sup': '3.2', 'claim-text': (a) H,', {'sub': 2', '1-4', '1-4', '2', '1-3', '1-3, '(b) NH, C-alkyl-NH—, (C-alkyl)N—, C-alkyl-C(O)—NH—, HO, C-alkyl-O—,'}, {'sub': '1-3', '(c) C-alkyl or'}, {'sub': 1-3', '1-3, '(d) a C-alkyl- or C-alkyl-O— group wherein each methylene group is substituted by up to two fluorine atoms and each methyl group is substituted by up to three fluorine atoms,'}], 'Rdenotes'}{'sup': '3.3', 'claim-text': (a) H,', '(b) F, Cl, Br,', {'sub': 1-3', '1-3, '(c) C-alkyl, C-alkyl-O— or'}, {'sub': 1-3', '1-3, '(d) a C-alkyl- or C-alkyl-O— group wherein each methylene group is substituted by up to two fluorine atoms and each methyl group is substituted by up to three fluorine atoms, or'}], 'Rdenotes'}{'sup': 3.2', '3.3, 'claim-text': the previously mentioned heterocycles may contain a carbonyl, ...

NOUVEL COMPOUNDS

The present invention relates to new CGRP-antagonists of general formulae Ia and Ib 5. A compound of the formula Ia or Ib according to claim 1 , wherein{'sup': '3', 'claim-text': (a) H,', {'sub': '1-6', '(b) C-alkyl,'}, {'sub': '3-6', 'sup': '3.2', '(c) a C-cycloalkyl group substituted by one or two groups R, or'}, {'sub': '1-3', '(d) a C-alkyl group wherein each methylene group is substituted by up to two fluorine atoms and each methyl group is substituted by up to three fluorine atoms,'}], 'Rdenotes'}{'sup': '3.2', 'claim-text': (a) H,', {'sub': 1-3', '1-3, '(b) halogen, C-alkyl, —OH, —O—C-alkyl, or'}, {'sub': 1-3', '1-3, '(c) a C-alkyl or —O—C-alkyl group wherein each methylene group is substituted by up to two fluorine atoms and each methyl group is substituted by up to three fluorine atoms,'}], 'Rindependently of one another denote'}{'sup': '4', 'claim-text': (a) H,', {'sub': '1-6', 'sup': '4.1', '(b) C-alkylene-R,'}, {'sub': '3-6', 'sup': '4.2', '(c) a C-cycloalkyl group substituted by one or two groups R,'}, {'sub': '5-7', 'sup': '4.2', '(d) a C-cycloalkenyl group substituted by one or two groups R,'}, {'sup': '4.2', '(e) an aryl group substituted by one or two groups R,'}, {'sub': '5-7', 'sup': '4.2', '(f) a C-cycloalkyl group which may be fused to an aryl, thiazolyl or thienyl group, while the resultant bicyclic group is additionally substituted by one or two groups R, or'}, {'sup': '4.2', '(g) a heteroaryl group substituted by one or two groups R,'}], 'Rdenotes'}{'sup': '4.1', 'claim-text': (a) H,', {'sup': 4.1.1', '4.1.2, '(b) a phenyl group substituted by the groups Rand R, or'}, {'sup': 4.1.1', '4.1.2, '(c) a heteroaryl group substituted by the groups Rand R,'}], 'Rdenotes'}{'sup': '4.1.1', 'claim-text': (a) H,', {'sub': 1-3', '1-3', '1-3', '1-3, 'sup': 4.1.1.1', '4.1.1.2', '4.1.1.1', '4.1.1.1', '4.1.1.2', '4.1.1.3, '(b) halogen, C-alkyl, —OH, —CN, —O—C-alkyl, —NRR, —S—C-alkyl, —NR—C(O)—C-alkyl, —C(O)—NRR, C(O)—O—R, or'}, {'sub': 1-3', '1-3, '(c) a C- ...

CGRP ANTAGONISTS

The present invention relates to new CGRP-antagonists of general formula I 7. A compound of the formula I according to claim 1 , wherein Rdenotes a hydrogen atom claim 1 ,or a tautomer or salt thereof.16. A compound of the formula I according to claim 1 , whereinU—V—X denotes{'sup': 11', '10', '10', '10', '11', '9', '9', '11', '9', '11', '9', '10', '9', '11', '9', '10', '11, '—N═N—(C—R)═, —N═(C—R)—N═, —N═(C—R)—(C—H)═, —(N-oxide)=(C—R)—(C—R)═, —(CR)═N—N═, —(CR)═N—(CR)═, —(C—R)═N(oxide)-(C—R)═, —(CR)═(C—R)—N═, —(CR)═(C—R)—(N-oxide)=, or —(CR)═(C—R)—(CR)═,'}{'sup': '9', 'claim-text': (a) H,', {'sub': 1-6', '1-3, 'sup': '9.1', '(b) a C-alkyl- or C-alkyl-O— group which may each be substituted by a group R,'}, {'sup': 9.2', '9.3', '9.2', '9.3, 'sub': '1-3', '(c) RRN, RRN—C-alkylene-,'}, {'sub': 1-3', '1-3', '3-6', '3-6', '1-4', '1-3', '1-3, '(d) halogen, —CN, —OH, _-COOH, C-alkyl-O—C-alkylene-, C-cycloalkyl, C-cycloalkyl-C-alkylene-, C-alkyl-C(O)—O—C-alkylene,'}, {'sub': 1-3', '1-3, '(e) a C-alkyl or C-alkyl-O— group wherein each methylene group is substituted by up to two fluorine atoms and each methyl group is substituted by up to three fluorine atoms,'}], 'Rdenotes'}{'sup': '9.1', 'sub': '3', 'Rdenotes H, OH or —O—CH,'}{'sup': '9.2', 'sub': '1-3', 'Rdenotes H or C-alkyl,'}{'sup': '9.3', 'sub': '1-3', 'Rdenotes H or C-alkyl, or'}{'sup': 9.2', '9.3, 'Rand Rtogether with the nitrogen atom to which they are attached denote a 3- to 6-membered heterocyclic group,'}{'sup': '10', 'claim-text': (a) H,', {'sub': 1-6', '1-3, 'sup': '10.1', '(b) a C-alkyl or C-alkyl-CO— group which may each be substituted by a group R'}, {'sup': 10.1', '10.2', '10.1', '10.2, 'sub': '1-3', '(c) —NRR, NRR—C-alkylene-,'}, {'sub': 1-3', '1-3', '3-6', '3-6', '1-4', '1-3', '1-3, '(d) halogen, —CN, —OH, C-alkyl-O—C-alkylene, C-cycloalkyl, C-cycloalkyl-C-alkylene, C-alkyl-C(O)—O—C-alkylene,'}, {'sub': '0-3', '(e) aryl-C-alkylene-O—,'}, {'sub': 1-3', '1-3, '(f) a C-alkyl or C-alkyl-O— group wherein each ...

NOVEL COMPOUNDS

This invention relates to compounds of formula I 4. The compound according to claim 3 , wherein{'sup': 3', '4', '3', '4, 'sub': 2', '3, 'Rand Rindependently represent hydrogen, methyl, ethyl, propyl or —CH—O—CHwhich latter four groups are optionally substituted with one or more fluorine atoms with the proviso that Rand Rboth are not hydrogen;'}or{'sup': 3', '4, 'Rand Rif both are attached to the same carbon atom, they may together with the carbon atom to which they are attached form a ring selected from cyclopropyl, cyclobutyl and cyclopentyl which latter three groups are optionally substituted with one or more fluorine atoms.'}5. The compound according to claim 4 , wherein{'sup': 3', '4, 'Rand Rrepresent methyl.'}13. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable adjuvant claim 1 , diluent and/or carrier.14. A method of treating schizophrenia claim 1 , schizoaffective disorder and substance induced psychotic disorder; cognitive disorders and dementias including age-associated learning and memory impairments or losses claim 1 , post stroke dementia claim 1 , deficits in concentration claim 1 , mild cognitive impairment claim 1 , the cognitive dysfunction in Alzheimers disease or the cognitive dysfunction of schizophrenia comprising administering to a patient a therapeutically effective amount of a compound according to . This invention relates to piperazines and their use as positive allosteric modulators of mGluR5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment.Glutamate is the primary excitatory amino acid in the mammalian central nervous system. Neurotransmission ...

NOVEL COMPOUNDS

The present invention relates to new CGRP-antagonists of general formulae Ia and Ib 9. A compound of the formula Ia or Ib according to claim 1 , wherein{'sup': '5', 'sub': '1-3', 'Rdenotes H or C-alkyl, or a tautomer or salt thereof.'}12. A physiologically acceptable salt of a compound according to any one of to .13. A pharmaceutical composition comprising a compound according to any one of to or a physiologically acceptable salt thereof and an carrier or diluent.14. A method for treating migraine claim 1 , cluster or tension headache which comprises administering to a host in need of such treatment a therapeutically effective amount of a compound according to any one of to or a physiologically acceptable salt thereof. The present invention relates to new CGRP-antagonists of general formulae Ia and Ibwherein R, R, R, Rand Rare defined as mentioned below, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.In the above general formulae Ia and Ib in a first embodimentandA second embodiment of the present invention comprises the compounds of the above general formulae Ia and Ib, wherein R, Rand Rare defined as hereinbefore in the first embodiment andandA third embodiment of the present invention comprises the compounds of the above general formulae Ia and Ib, wherein R, Rand Rare defined as hereinbefore in the first embodiment andandA fourth embodiment of the present invention comprises the compounds of the above general formulae Ia and Ib, wherein R, Rand Rare defined as hereinbefore in the first embodiment andandthe tautomers, the diastereomers, the enantiomers, the hydrates, the mixtures thereof and the salts thereof as well as the hydrates of the salts, ...

6,7,8,9-Tetrahydro-5H-1,4,7,10a-tetraaza-cyclohept[f]indene derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them

The present invention relates to compounds defined by formula I wherein the groups X, Y, W and R 1 to R 4 are defined as in claim 1 , possessing valuable pharmacological activity. Particularly the compounds are agonists of the 5-HT2C receptor, and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this receptor, such as metabolic and CNS-related disorders.

NOVEL (CYANO-DIMETHYL-METHYL)-ISOXAZOLES AND -[1,3,4]THIADIAZOLES

This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

2-[Thiophen-2-yl)formamido]-N-(phenyl)-2-methylpropanamide derivatives and the use therof as medicament

The present invention relates to novel 2-[thiophen-2-yl)formamido]-N-(phenyl)-2-methylpropanamides of formula A and pharmaceutically acceptable salts thereof, wherein R 1 to R 3 are as defined herein. The invention also relates to processes for the preparation of these compound, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions in which inhibition of the indoleamine 2,3-dioxygenase 1 (IDO1) enzyme may be beneficial.

NOVEL (CYANO-DIMETHYL-METHYL)-ISOXAZOLES AND -[1,3,4]THIADIAZOLES

This invention relates to novel (Cyano-dimethyl-methyl)-isoxazolesand-[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions. 2. The compound according to for use as a medicament.3. A pharmaceutical composition comprising at least one compound according to io or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable adjuvant claim 1 , diluent and/or carrier.4. The compound according to or a pharmaceutically acceptable salt thereof for use in the treatment or prevention of pain.5. The compound for use according to claim 4 , characterized in that the pain is neuropathic pain.6. The compound for use according to or claim 4 , characterized in that the pain is selected from the group consisting of peripheral neuropathic pain claim 4 , pain associated with diabetic peripheral neuropathy claim 4 , pain associated with lumbosacral radiculopathy and pain associated with post herpetic neuralgia. This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles- and [1,3,4]thiadiazoles and their use as cannabinoid receptor 2 agonists (CB2 receptor agonists), pharmaceutical compositions containing the same, and methods of using the same as agents for the treatment of CB2 receptor mediated disorders or conditions.WO2008014199 and WO2008039645 discuss the CB2 receptor, and the therapeutic uses of the CB2 receptor agonist compounds disclosed therein. Further supporting evidence has more recently emerged in which the expression of CB2 in dorsal root ganglion neurons has been demonstrated in multiple species (Anand et al., 2008 Pain 138: 667-680). Neuronal expression of CB2 has been shown to be altered under pathological pain conditions suggesting a key role for CB2 neuronal signalling. A role for centrally located CB2 has been suggested by recent reports of an effect of CB2 on addictive behaviour (Xi ...

Novel (Cyano-Dimethyl-Methyl)-Isoxazoles and -[1,3,4]Thiadiazoles

This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions. 16-. (canceled)9. The method of claim 7 , wherein the pain is acute pain.10. The method of claim 8 , wherein the pain is acute pain.11. The method of claim 9 , wherein the acute pain is trigeminal neuralgia.12. The method of claim 10 , wherein the acute pain is trigeminal neuralgia.13. The method of claim 7 , wherein the pain is visceral pain.14. The method of claim 8 , wherein the pain is visceral pain.15. The method of claim 7 , wherein the pain is neuropathic pain.16. The method of claim 8 , wherein the pain is neuropathic pain.17. The method of claim 15 , wherein the neuropathic pain is post-herpetic neuralgia.18. The method of claim 16 , wherein the neuropathic pain is post-herpetic neuralgia.19. The method of claim 15 , wherein the neuropathic pain is due to multiple sclerosis.20. The method of claim 16 , wherein the neuropathic pain is due to multiple sclerosis.21. The method of claim 15 , wherein the neuropathic pain is due to chemotherapy caused nerve injury.22. The method of claim 16 , wherein the neuropathic pain is due to chemotherapy caused nerve injury.23. The method of claim 7 , wherein the compound is administered in the form of a tablet claim 7 , pill claim 7 , or capsule.24. The method of claim 8 , wherein the compound is administered in the form of a tablet claim 8 , pill claim 8 , or capsule.25. The method of claim 9 , wherein the compound is administered in the form of a tablet claim 9 , pill claim 9 , or capsule.26. The method of claim 15 , wherein the compound is administered in the form of a tablet claim 15 , pill claim 15 , or capsule. This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles- and -[1,3,4]thiadiazoles and their use as cannabinoid receptor 2 ...

NOVEL (CYANO-DIMETHYL-METHYL)-ISOXAZOLES AND -[1,3,4]THIADIAZOLES

This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions. 16-. (canceled) This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles- and -[1,3,4]thiadiazoles and their use as cannabinoid receptor 2 agonists (CB2 receptor agonists), pharmaceutical compositions containing the same, and methods of using the same as agents for the treatment of CB2 receptor mediated disorders or conditions.WO2008014199 and WO2008039645 discuss the CB2 receptor, and the therapeutic uses of the CB2 receptor agonist compounds disclosed therein. Further supporting evidence has more recently emerged in which the expression of CB2 in dorsal root ganglion neurons has been demonstrated in multiple species (Anand et al., 2008 Pain 138: 667-680). Neuronal expression of CB2 has been shown to be altered under pathological pain conditions suggesting a key role for CB2 neuronal signalling. A role for centrally located CB2 has been suggested by recent reports of an effect of CB2 on addictive behaviour (Xi et al., Nat. Neuroscience 2012, 14, 1160-1166; Morales & Bonci et al., Nature Med. 2012, 18, 504-505; Aracil-Fernandez et al., Neuropsychopharmacology 2012, 37, 1749-1763) and other conditions in which maladaptive impulsivity plays a role (Navarrete et al., Br. J. Pharmacol. 2012, 165, 260-273). A role of the hepatic CB2 in the pathogenesis of steatohepatitis and fibrotic liver diseases has also been suggested by several preclinical studies (Munoz-Luque et al., JPET 2008, 324, 475-483; Reichenbach et al., JPET 2012, 340, 629-637, WO2011009883). It is believed that the highly selective activation of the CB2 receptor with an agonist may offer avenues of harnessing the beneficial effects while avoiding the adverse effects seen with dual CB1/CB2 cannabinoid receptor agonists (see e.g ...

NOVEL (CYANO-DIMETHYL-METHYL)-ISOXAZOLES AND -[1,3,4]THIADIAZOLES

This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions. 2. The compound according to for use as a medicament.3. A pharmaceutical composition comprising at least one compound according to or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable adjuvant claim 1 , diluent and/or carrier.4. The compound according to or a pharmaceutically acceptable salt thereof for use in the treatment or prevention of pain.5. The compound for use according to claim 4 , characterized in that the pain is neuropathic pain.6. The compound for use according to claim 4 , characterized in that the pain is selected from the group consisting of peripheral neuropathic pain claim 4 , pain associated with diabetic peripheral neuropathy claim 4 , pain associated with lumbosacral radiculopathy and pain associated with post herpetic neuralgia. This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles- and -[1,3,4]thiadiazoles and their use as cannabinoid receptor 2 agonists (CB2 receptor agonists), pharmaceutical compositions containing the same, and methods of using the same as agents for the treatment of CB2 receptor mediated disorders or conditions.WO2008014199 and WO2008039645 discuss the CB2 receptor, and the therapeutic uses of the CB2 receptor agonist compounds disclosed therein. Further supporting evidence has more recently emerged in which the expression of CB2 in dorsal root ganglion neurons has been demonstrated in multiple species (Anand et al., 2008 Pain 138: 667-680). Neuronal expression of CB2 has been shown to be altered under pathological pain conditions suggesting a key role for CB2 neuronal signalling. A role for centrally located CB2 has been suggested by recent reports of an effect of CB2 on addictive behaviour (Xi et ...

(Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles

Disclosed are (cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

(Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles

This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

(Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles

This invention relates to novel (Cyano-dimethyl-methyl)-isoxazolesand-[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

(Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles

This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

(Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles

This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

Selected cgrp antagonists, method for producing the same and the use thereof as drugs

The invention relates to the CGRP antagonists of general formula (I), wherein A, X and R1 to R3 are defined as in claim 1. The invention also relates to the tautomers, diastereomers, enantiomers, hydrates, mixtures and salts thereof and to the hydrates of said salts, especially their physiologically acceptable salts with inorganic or organic acids, to drugs comprising said compounds, to their use and to a method for producing the same.

Selected cgrp antagonists, methods for the production thereof and their use as medicaments

The invention relates to CGRP antagonists of general formula (I), in which R1, R2, R3 and R4 are described in Claim 1, to the tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures and salts thereof, to the hydrates of the salts, particularly their physiologically compatible salts with inorganic or organic acids or bases, to the compounds of general formula (I), in which one or more hydrogen atoms are exchanged for deuterium, to medicaments containing these compounds, the use thereof, and to methods for producing them.

(hetero)aryl compounds with mch antagonistic activity and medicaments comprising these compounds

The present invention relates to (hetero)aryl compounds of general formula (I) wherein the groups and radicals A, B, Q, W, X, Y, Z, R1, R2, R4a, R4b, R5a, R5b, have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to 10 the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

New amide compounds having MCH antagonist activity and medicaments containing these compounds

Die vorliegende Erfindung betrifft Amid-Verbindungen der allgemeinen Formel I, DOLLAR F1 in der die Gruppen und Reste A, B, b, W, X, Y, Z, R·1·, R·2· und R·3· die in Anspruch 1 angegebenen Bedeutungen aufweisen. Ferner betrifft die Erfindung Arzneimittel, enthaltend mindestens ein erfindungsgemäßes Amid. Auf Grund der MCH-Rezeptor antagonistischen Aktivität eignen sich die erfindungsgemäßen Arzneimittel zur Behandlung von metabolischen Störungen und/oder Essstörungen, insbesondere von Obesitas, Bulimie, Anorexie, Hyperphagia und Diabetes.

Sic bipolar semiconductor devices with few crystal defects

A bipolar device (30) has at least one p-type layer (34) of single crystal silicon carbide and at least one n-type layer (33) of single crystal silicon carbide, wherein those portions of those stacking faults (40) that grow under forward operation are segregated from at least one of the interfaces between the active region and the remainder of the device.

CGRP antagonists

CGRP antagonists of the formula of which the following are exemplary: (1) 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylic acid-{(R)-1-(3,4-diethyl-benzyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amide, (2) 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylic acid-{(R)-1-(3,4-diethyl-benzyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amide.

Piperazine derivatives and their use as positive allosteric modulators of mGluR5 receptors

This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. R 1 , R 2 , R 3 , R 4 , Q have meanings given in the description.

New (hetero)aryl compounds with MCH antagonistic activity and medicaments comprising these compounds

Novel compounds

The present invention relates to novel compounds of general formula (I), in which A, U, V, X, Y, R 1 , R 2 , and R 3 are defined as described below, and to tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures, salts and hydrates of salts thereof, in particular physiologically compatible salts thereof with organic or inorganic acids or bases. The invention also relates to medicaments containing said compounds, to the use thereof and to a method for the production thereof.

CGRP antagonists, method for production thereof, and their use as medicaments

Novel alkyne compounds having an mch-antagonistic effect and medicaments containing said compounds

The invention relates to alkyne compounds of general formula (I), in which groups and residues A, B, W, X, Y, Z, R1 and R2 have the meanings cited in Claim 1. The invention also relates to medicaments containing at least one inventive alkyne. The MCH receptor antagonistic effect renders the inventive medicaments suitable for treating metabolic disorders and/or eating disorders, in particular, obesity and diabetes.

Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions

CGRP Antagonists

The invention relates to a method for preventing and treating visceral pain and gastrointestinal disorders such as functional bowel disorders and inflammatory bowel diseases through the use of effective amounts of a compound acting as CGRP antagonist.

Treatment of gastrointestinal disorders with cgrp antagonists

The invention relates to a method for preventing and treating visceral pain and gastrointestinal disorders such as functional bowel disorders and inflammatory bowel diseases through the use of effective amounts of a compound acting as CGRP antagonist.

Selected CGRP antagonists, methods for their preparation and use thereof as drugs.

New pyridone derivatives with mch antagonistic activity and medicaments comprising these compounds

The present invention relates to compounds of general formula (I) wherein the groups and radicals B, k, L, U,V, W, X, Y, Z, R1, R2, have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH- receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

Selected cgrp antagonists, methods for the production thereof, and use thereof as medicaments

The invention relates to the CGRP antagonists of general formula (I), wherein A and R1 to R3 are defined as indicated in claim 1, the tautomers, diastereomers, enantiomers, hydrates, mixtures and salts thereof, the hydrates of the salts, especially the physiologically acceptable salts thereof with inorganic or organic acids, medicaments containing said compounds, the use thereof, and methods for the production thereof.

Cgrp antagonists, method for the production thereof, and their use as medicaments

The invention relates to CGRP antagonists of general formula (I) in which: R1, R2, R3, R4 and X are defined as in Claim 1, to their tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures and salts as well as the hydrates of the salts, in particular, their physiologically compatible salts with inorganic or organic acids and bases, and those compounds of general formula (I) in which one or more hydrogen atoms are replaced by deuterium. The invention also relates to medicaments containing these compounds, the use thereof, and to methods for producing them.

1-substituted 4-heterocyclylpiperidines for use as cgrp antagonists

The invention relates to the novel CGRP antagonists of general formula (I), wherein A, X, R1, R2 and R3 are defined as in the description, to the tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures and salts thereof and to the hydrates of the salts, especially their physiologically acceptable salts with inorganic or organic acids or bases. The invention further relates to drugs containing said compounds, to their use and to methods for producing the same.

Selected cgrp antagonists, methods for the production thereof and their use as medicaments

The invention relates to CGRP antagonists of general formula (I), in which R1, R2, R3 and R4 are described in Claim 1, to the tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures and salts thereof, to the hydrates of the salts, particularly their physiologically compatible salts with inorganic or organic acids or bases, to the compounds of general formula (I), in which one or more hydrogen atoms are exchanged for deuterium, to medicaments containing these compounds, the use thereof, and to methods for producing them.

Novel phenylethanolamine derivatives and the use of the same as beta-3-agonists

The invention relates to novel beta agonists of general formula (I) wherein the radicals R1 to R12 have the designations cited in the claims and in the description. The invention also relates to the isomers thereof, to methods for producing said compounds and to the use of the same as medicaments.

Selected cgrp antagonists, methods for the production thereof and their use as medicaments

The invention relates to the CGRP antagonists of general formula (I) in which R1, R2, R3 and R4 are defined as in claim 1, to their tautomers, isomers, diastereoisomers and enantiomers, hydrates, mixtures and their salts as well as the hydrates of the salts, particularly their physiologically compatible salts with inorganic or organic acids or bases, as well as to the compounds of general formula (I) in which one or more hydrogen atoms are exchanged for deuterium, to medicaments containing these compounds, the use thereof and to methods for the production thereof.

New pyridone derivatives with MCH antagonistic activity and medicaments comprising these compounds

The present invention relates to compounds of general formula (I) wherein the groups and radicals B, k, L, U,V, W, X, Y, Z, R

Selected cgrp antagonists, method for production and use thereof as medicament

2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl-piperidines used as cgrp antagonists

CGRP antagonisti opće formule I naznačeni time, da su oni odabrani iz skupine koju čine: (nastavak) CGRP antagonists of general formula I, selected from the group consisting of: (continued)

Cgrp antagonists

The present invention relates to novel CGRP antagonists of the general formula (I) in which U, V, X, Y, R 1 , R 2 , R 3 are defined as described below, the tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures and salts thereof, and the hydrates of the salts, particularly the physiologically compatible salts thereof having inorganic or organic acids or bases, pharmaceuticals comprising said compounds, the use thereof, and the method for the production thereof.

(hetero)aryl compounds with mch antagonistic activity and medicaments comprising these compounds

The present invention relates to (hetero)aryl compounds of general formula (I) wherein the groups and radicals A, B, Q, W, X, Y, Z, R1, R2, R4a, R4b, R5a, R5b, have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to 10 the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

N- (1-benzyl-2-oxo-2- (1-piperazinyl) ethyl) -1-piperidincarboxamid-derivatives and related compounds use as CGRP-antagonists for treating a headache

New beta-agonists, processes for preparing them and their use as pharmaceutical compositions

The invention relates to novel beta agonists of general formula (I) wherein the radicals R1 to R12 have the designations cited in the claims and in the description. The invention also relates to the isomers thereof, to methods f or producing said compounds and to the use of the same as medicaments.

Selected cgrp-antagonists, their preparation processes and their use as medicaments

CGRP-antagonists are disclosed having the general formula (I), in which A, X and R1-R3 have the definition given in claim 1, as well as their tautomers, diastereomers, enantiomers, hydrates, mixtures and salts, as well as their salt hydrates, in particular their physiologically compatible salts with inorganic or organic acids, medicaments containing these compounds, their use and their preparation processes.

2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl-piperidines used as cgrp antagonists

The invention relates to novel CGRP antagonists of general formula (I), in which B, R1 and R2 are defined as cited in claim 1, to their tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures and salts, in addition to the hydrates of their salts, in particular their physiologically compatible salts, with inorganic or organic acids or bases. The invention also relates to medicaments containing said compounds, to their use and to a method for their production.

CGRP antagonists, their preparation and use as a medicament

Selected Cgrp-Antagonists, Processes for Preparing Them and Their Use as Pharmaceutical Compositions

The invention relates to CGRP-antagonists of general formula (I), wherein R 1 , R 2 , R 3 , R 4 and R 5 are defined in claim 1 , to the tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures salts and salt hydrates thereof, in particular to 10 salts thereof, which are physiologically compatible with acids or inorganic or organic bases and to compounds of general formula (I), wherein one or several hydrogen atoms are substituted by deuterium. Drugs containing said compounds, the use thereof and a method for the production thereof are also disclosed.

Compounds

The invention relates to novel CGRP antagonists of general formula (I) in which U, V, X, Y, R 1 , R 2 , R 3 , and R 4 are defined as indicated in the description, the tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures, and salts thereof, and the hydrates of the salts, especially the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing said compounds, the use thereof, and methods for the production thereof.

Substituted imidazoles, their preparation and use

A novel class of substituted imidazole compounds (I), pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders, in which an interaction with the histamine H3 receptor is beneficial.

New pyridone derivatives with mch antagonistic activity and medicaments comprising these compounds

The present invention relates to compounds of general formula (I) wherein the groups and radicals B, k, L, U,V, W, X, Y, Z, R1, R2, have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH- receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

Treatment of gastrointestinal disorders with cgrp-antagonists.

La invención se refiere a un método para prevenir y tratar el dolor visceral y los trastornos gastrointestinales tales como trastornos funcionales del intestino y enfermedades inflamatorias del intestino mediante el uso de cantidades eficaces de un compuesto que actúa cómo antagonista de CGRP.

Cgrp-antagonists

Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds

Alkyne compounds having MCH-receptor antagonistic activity, which are useful for preparing pharmaceutical compositions for the treatment of metabolic disorders and/or eating disorders, particularly obesity and diabetes.

BENZODIAZEPINE-SUBSTITUTED PIPERDINES FOR USE IN THE TREATMENT OF CARDIOVASCULAR DISEASES

Substituted piperidines, drugs containing these compounds and processes for their preparation

New alkyne compounds having MCH antagonist activity and medicaments containing these compounds

Die vorliegende Erfindung betrifft einzelne Alkin-Verbindungen mit MCH-Rezeptor antagonistischer Aktivität, die sich zur Herstellung von Arzneimitteln zur Behandlung von metabolischen Störungen und/oder Essstörungen, insbesondere von Adipositas und Diabetes, eignen. The present invention relates to single alkyne compounds having MCH receptor antagonist activity which are useful in the preparation of medicaments for the treatment of metabolic disorders and / or eating disorders, particularly obesity and diabetes.

Novel (cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles

This invention relates to novel (Cyano-dimethyl-methyl)-isoxazolesand -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

Treatment of gastrointestinal disorders with cgrp-antagonists

The invention relates to a method for preventing and treating visceral pain and gastrointestinal disorders such as functional bowel disorders and inflammatory bowel diseases through the use of effective amounts of a compound acting as CGRP antagonist.

Use of selected cgrp antagonists in combination with other antimigraine medical substances for the treatment of migraine

The invention relates to a method for treating or preventing headaches, migraine, or cluster headache. Said method comprises jointly administering a therapeutically effective amount of a selected CGRP antagonist (A), a physiologically acceptable salt thereof or a hydrate of said salt, and a therapeutically effective amount of a second or third active antimigraine medical substance (B), particularly sumatriptan, zolmitriptan, or dihydroergotamine or a physiologically acceptable salt thereof. Also disclosed are the corresponding pharmaceutical compositions and the production thereof.

Beta-ketoamide compounds having an mch-antagonistic effect and medicaments containing said compounds

The invention relates to .beta.-ketoamide compounds of general formula (I) wherein the groups and radicals A, B, b, X, Y, Z, R1, R2, R3, R5a and R5b have the designations cited in patent claim 1. The invention also relates to medicaments containing at least one inventive amide. As a result of the MCH receptor antagonistic activity, the inventive medicaments are suitable for treating metabolic disorders and/or eating disorders, especially adipositas, bulimia, anorexia, hyperphagia and diabetes.

(Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles

This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

Method for producing semi-insulating resistivity in high purity silicon carbide crystals

3-(4-piperidine-1ylmethyl-phenyl)-propion acid-phenylamide-derivatives and related compounds used in the form of mch antagonists (melanine concentrating hormone) for treating eating disorders

The invention relates to amid compounds of general formula (I), wherein groups and residuals A, B, b, W, X, Y, Z, R1, R2 and R3 have significances given in a claim 1. In addition, said invention relates to drugs containing at least one type of inventive amid. Because of the antagonist activity of an MCH-receptor, the inventive drugs are suitable for treating metabolic disturbances and/or eating disorders, in particular adiposity, bulimia, anorexia, hyperphagia and diabetes.

Use of selected cgrp antagonists in combination with other antimigraine medical substances for the treatment of migraine

The invention relates to a method for treating or preventing headaches, migraine, or cluster headache. Said method comprises jointly administering a therapeutically effective amount of a selected CGRP antagonist (A), a physiologically acceptable salt thereof or a hydrate of said salt, and a therapeutically effective amount of a second or third active antimigraine medical substance (B), particularly sumatriptan, zolmitriptan, or dihydroergotamine or a physiologically acceptable salt thereof. Also disclosed are the corresponding pharmaceutical compositions and the production thereof.

Compounds

The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R 1 , R 2 , R 3 and R 4 are defined as mentioned in the description, the tautomers thereof, the isomers thereof, the diastereomers thereof, the enantiomers thereof, the hydrates thereof, the mixtures thereof and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, the use thereof and processes for the preparation thereof.

New pyridazine derivatives with mch antagonistic activity and medicaments comprising these compounds

The present invention relates to compounds of general formula I wherein the groups and radicals B, W, X, Y, Z, R1, R2, have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

Novel (cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles

6,7,8,9-tetrahydro-5h-1,4,7,10a-tetraaza-cyclohept[f]indene derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them

The present invention relates to compounds defined by formula (I), wherein the groups X, Y, W and R1 to R4 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are agonists of the 5-HT2C receptor, and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this receptor, such as metabolic and CNS-related disorders.

2-[thiophen-2-yl)formamido]-n-(phenyl)-2-methylpropanamide derivatives and the use thereof as medicament

The present invention relates to novel 2-[thiophen-2-yl)formamido]-N-(phenyl)-2- methylpropanamides of general formula (A), Formula (A), processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions in which inhibition of the indoleamine 2,3 -dioxygenase 1 (IDOl) enzyme may be beneficial.

Cgrp antagonists

The present invention relates to new CGRP antagonists of the general formula (I), where U, V, X, Y, R1, R2 and R3 are defined as described below, the tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures, and salts thereof, and the hydrates of said salts, particularly the physiologically compatible salts thereof having inorganic or organic acids or bases, pharmaceuticals comprising said compounds, the use thereof, and method for the production thereof.

New 4-heterocyclyl-1-acyl-piperidine derivatives, useful e.g. for treating headache, diabetes and cardiovascular disease, are antagonists of calcitonin-gene related peptide

4-heterocyclyl-1-acyl-piperidine derivatives (I), their tautomers, diastereomers, enantiomers, hydrates and/or (hydrated) salts are new. 4-heterocyclyl-1-acyl-piperidine derivatives of formula (I), their tautomers, diastereomers, enantiomers, hydrates and/or (hydrated) salts are new A and B each : N or CH; D : hydrogen or Me; E : hydrogen, fluoro, chloro, bromo, Me, Et or trifluoromethyl; X : CH2 or NH; R1>2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl or 5-oxo-3-phenyl-4,5-dihydro-1,2,4-triazol-1-yl; R2>4-Ra-piperidin-1-yl, 4-Rb-piperazin-1-yl or 4-Rc-perhydro-1,4-diazepin-1-yl; Ra : piperidin-1-yl, piperidin-4-yl (optionally N-substituted by Me, methoxycarbonylmethyl or methylsulfonyl), dimethylamino, piperazin-1-yl (optionally 4-methyl substituted), pyrrolidin-1-yl, perhydro-1,4-diazepin-1-yl (optionally 4-methyl substituted) or 4-fluorophenyl; Rb : piperidin-4-yl (optionally 4-methyl substituted), pyridin-4-yl or 4-fluorophenyl; Rc : piperidin-4-yl, optionally N-methyl substituted) . An independent claim is also included for 5 methods of preparing (I). [Image] ACTIVITY : Antimigraine; Analgesic; Antidiabetic; Cardiant; Antidiarrhea; Dermatological; Antiinflammatory; Antiarthritic; Antiallergic; Antiasthmatic; Antibacterial; Immunosuppressive; Gynecological; Cytostatic. No details of tests for these activities are given. MECHANISM OF ACTION : (I) are selective antagonists of calcitonin-gene related peptide, with IC50 below 104> nM.

Novel compounds

The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R 1 , R 2 , R 3 and R 4 are defined as in the description, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, their use and processes for preparing them.

CGRP antagonists

Selected cgrp antagonists, a method for the production thereof and use in the form of drugs

The invention relates to CGRP-antagonists of general formula (I), wherein R1, R2, R3, R4 and R5 are defined in claim 1, to the tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures salts and salt hydrates thereof, in particular to 10 salts thereof, which are physiologically compatible with acids or inorganic or organic bases and to compounds of general formula (I), wherein one or several hydrogen atoms are substituted by deuterium. Drugs containing said compounds, the use thereof and a method for the production thereof are also disclosed.

SELECTED CGRP ANTAGONISTS, PROCESS FOR THEIR PREPARATION AND THEIR USE AS DRUGS

6,7,8,9-tetrahydro-5H-1,4,7,10a-tetraaza-cyclohept[f]indene derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them

Neue alkin-verbindungen mit mch-antagonistischer wirkung und diese verbindungen enthaltende arzneimittel

Die vorliegende Erfindung betrifft Alkin-Verbindungen der allgemeinen Formel (I), in der die Gruppen und Reste A, B, W, X, Y, Z, R<1> und R<2> die in Anspruch 1 angegebenen Bedeutungen aufweisen. Ferner betrifft die Erfindung Arzneimittel enthaltend mindestens ein erfindungsgemäßes Alkin. Auf Grund der MCH-Rezeptor antagonistischen Aktivität eignen sich die erfindungsgemäßen Arzneimittel zur Behandlung von metabolischen Störungen und/oder Essstörungen, insbesondere von Adipositas und Diabetes.

(cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles

This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

New alkyne compounds with mch antagonistic activity and medicaments comprising these compounds

Compuestos alquinicos con accion antagonista sobre mch y composiciones que contienen estos compuestos

REFERIDA A UN COMPUESTO ALQUINICO DE FORMULA I, DONDE R1 ES ALQUENILO C3-C6, ALQUINILO C3-C6, ENTRE OTROS; R2 ES H, ALQUILO C1-C8, CICLOALQUILO C3-C7, ENTRE OTROS; X ES ALQUILENO C1-C4, ENTRE OTROS; W Y Z SON UN ENLACE SENCILLO O UN PUENTE ALQUILENO C1-C2, ENTRE OTROS; Y Y A SON FENILO, PIRIDINILO, PIRIMIDINILO, ENTRE OTROS; B ES ALQUILO C1-C6, ALQUENILO C1-C6, ALQUINILO C1-C6, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (3S,4R)-1-(2-{4-[5-(4-CLOROFENIL)-PIRIDIN-2-IL-ETINIL]-2-METIL-FENOXI}-ETIL)-4-TRIFLUOROMETIL-PIPERIDIN-3,4-DIOL, (S)-3-[(2-{4-[5-(4-CLOROFENIL)-PIRIDIN-2-IL-ETINIL]-2-METIL-FENOXI}-ETIL)-CICLOPROPILMETIL-AMINO]-PROPANO-1,2-DIOL, (R)-3-[(2-{4-[5-(4-CLOROFENIL)-PIRIDIN-2-IL-ETINIL]-2-METIL-FENOXI}-ETIL)-CICLOPROPILMETIL-AMINO]-PROPANO-1,2-DIOL, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION QUE CONTIENE DICHOS COMPUESTOS, LOS CUALES SON ANTAGONISTAS DEL RECEPTOR DE LA HORMONA CONCENTRADORA DE MELANINA (MCH) Y SON UTILES PARA EL TRATAMIENTO DE TRASTORNOS METABOLICOS Y/O TRASTORNOS ALIMENTARIOS, EN PARTICULAR DE LA ADIPOSIDAD Y DIABETES

Neue verbindungen

Gegenstand der vorliegenden Erfindung sind neue CGRP-Antagonisten der allgemeinen Formel (I) in der A, X, R1, R2 und R3 wie nachstehend erwähnt definiert sind, deren Tautomere, deren Isomere, deren Diastereomere, deren Enantiomere, deren Hydrate, deren Gemische und deren Salze sowie die Hydrate der Salze, insbesondere deren physiologisch verträgliche Salze mit anorganischen oder organischen Säuren oder Basen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung.

Ausgewählte cgrp-antagonisten, verfahren zu deren herstellung sowie deren verwendung als arzneimittel

Benzodiazepin-substituierte piperdine zur verwendung in der behandlung von cardiovaskulären erkrankungen

Nuevos compuestos con estructura de alquino con accion antagonistas de mch y medicamentos que contienen estos compuestos

SE REFIERE A COMPUESTOS CON ESTRUCTURA ALQUINO DE FORMULA (I), EN DONDE R1 Y R2 SON INDEPENDIENTEMENTE H, ALQUILO(C1-C6), CICLOALQUILO(C3-C7), HIDROXI-ALQUILO(C2-C4), HIDROXICICLOALQUILO(C3-C7), ENTRE OTROS O JUNTOS CON EL N AL QUE ESTAN UNIDOS FORMAN UN HETEROCICLO SELECCIONADO DE PIRROLIDINA, PIPERIDINA, 8-AZA-BICICLO[3,2,1]OCTANO, PIPERAZINA, DONDE LA FUNCION IMINA LIBRE ESTA SUSTITUIDA CON R13 Y MORFOLINA; X ES UN PUENTE ALQUENILENO O ALQUINILENO(C3-C6) OPCIONALMENTE SUSTITUIDO POR F, Cl, OH, ALQUILO(C1-C3) Y CICLOPROPILO, O ES UN PUENTE ETOXI O ETILINIMINO, DONDE EL GRUPO IMINO ESTA OPCIONALMENTE SUSTITUIDO; W Y Z SON INDEPENDIENTEMENTE ENLACE SIMPLE O UN PUENTE ALQUILENO(C1-C2); Y, A SON INDEPENDIENTEMENTE UN CICLO BIVALENTE FENILO, PIRIDINILO, PIRIMIDILO, PIPERAZINILO, ENTRE OTROS, OPCIONALMENTE SUSTITUIDOS CON R20; B ES Y O A, SIENDO PREFERIDO FENILO O ALQUILO(C1-C6), CICLOALQUILO(C3-C7), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-((E)-3-{4-[5-(4-CLORO-FENIL)-PIRIDIN-2-ILETINIL]-FENIL}-ALILAMINO)-PROPAN-1,3-DIOL, (R)-5-(4-CLORO-FENIL)-2-{4-[2-(4-METIL-PIPERIDIN-1-IL)-PROPOXI-FENILETINIL}-PIRIDINA, (R)-1'-{4-[5-(4-CLORO-FENIL)-PIRIDIN-2-ILETINIL]-FENIL}-4-METIL-[1,3']-BIPIPERIDINILO, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE ELABORACION Y UNA COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS SON ANTAGONISTAS DE LOS RECEPTORES DE MCH (HORMONA CONCENTRADORA DE MELANINA) POR LO QUE SON APROPIADOS EN EL TRATAMIENTO DE TRANSTORNOS METABOLICOS Y/O ALIMENTICIOS

N- (1-benzyl-2-oxo-2- (1-piperazinyl) ethyl) -1- piperidincarboxamid-derivate und verwandte verbindungen als cgrp-antagonisten zur behandlung von kopfschmerzen

Nuevos compuestos alquínicos con acción antagonista sobre mch y medicamentos que contienen estos compuestos

La presente invención se refiere a compuestos alquínicos de la fórmula general en la que los grupos y restos A, B, W, X, Y, Z, R1 y R2 tienen los significados indicados en la reivindicación 1. Adicionalmente, la invención se refiere a medicamentos que contienen al menos un alquino según la invención. Debido a la actividad antagonista sobre el receptor de MCH, los medicamentos según la invención son apropiados para el tratamiento de trastornos metabólicos y/o trastornos alimentarios, en especial de la adiposidad y diabetes.

Neue verbindungen

Gegenstand der vorliegenden Erfindung sind neue CGRP-Antagonisten der allgemeinen Formel (I) in der R1, R2, R3, Ra, Rb, Rc, X, Y und Z wie nachstehend erwähnt definiert sind, deren individuelle Diastereomere, deren individuelle Enantiomere und deren Salze, insbesondere deren physiologisch verträgliche Salze mit anorganischen oder organischen Säuren oder Basen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung.

Selected CGRP antagonists, methods for the production thereof and their use as medicaments

Use of cgrp antagonists in treatment and prevention of hot flushes in prostate cancer patients

The invention relates to a method of treatment or prevention of hot flushes in men who underwent castration, e.g. due to androgen ablation treatment in prostate cancer therapy, comprising administration of an effective amount of a selected CGRP antagonist to the patient, and to the use of said active compounds for the manufacture of a pharmaceutical composition intended to be used in this method.

Use of cgrp antagonists in treatment and prevention of hot flushes in prostate cancer patients

The invention relates to a method of treatment or prevention of hot flushes in men who underwent castration, e.g. due to androgen ablation treatment in prostate cancer therapy, comprising administration of an effective amount of a selected CGRP antagonist to the patient, and to the use of said active compounds for the manufacture of a pharmaceutical composition intended to be used in this method.

Verfahren und anlage mit saathalter zur züchtung von siliziumkarbideinkristalle

New cgrp-antagonists, process for preparing them and their use as pharmaceutical compositions

Silicon carbide growth system and seeded sublimation method

Antagonistas de cgrp seleccionados, procedimiento para su preparación asi como su uso como medicamento

Objeto de la presente invención son los antagonistas de CGRP de l fórmula general en la que A,X, D, E, G, M, Q y R1 a R2 están definidos como en la reivindicación 1, sus tautómeros, sus diastereoisómeros, sus enantiómeros, sus hidratos, sus mezclas y sus sales, así como los hidratos de las sales, en particular sus sales fisiológicamente compatibles con ácidos o bases inogánicos u orgánicos, medicamentos que contienen estos compuestos, su uso y un procedimiento para su preparación.

Cgrp antagonisten

Gegenstand der vorliegenden Erfindung sind neue CGRP-Antagonisten der allgemeinen Formel (I): in der U, V, X, Y, R1, R2 und R3 wie nachstehend erwähnt definiert sind, deren Tautomere, deren Isomere, deren Diastereomere, deren Enantiomere, deren Hydrate, deren Gemische und deren Salze sowie die Hydrate der Salze, insbesondere deren physiologisch verträgliche Salze mit anorganischen oder organischen Säuren oder Basen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung.

Derivados de 2-[tiofen-2-il)formamido]-n-(fenil)-2-metilpropanamida y su uso como medicamento

Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula (A) en donde R¹ representa cloro, bromo; R² representa hidrógeno, flúor; R³ representa cloro, bromo. Reivindicación 8: Una sal de un compuesto de acuerdo con cualquiera de las reivindicaciones 1 a 7. Reivindicación 14: Una composición farmacéutica que comprende el compuesto de acuerdo con cualquiera de las reivindicaciones 1 a 8, caracterizado porque se mezcla con un adyuvante, diluyente y/o portador farmacéuticamente aceptable.