Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof

Compounds of Formula (IA), (IB), (IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Azaindazole compounds as CCR1 receptor antagonists

Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (IA) wherein R1, R2, R3, R4 and R5 are as defined herein for Formula (IA), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid Mimetics, Methods of Making Them, Pharmaceutical Compositions and Uses Thereof

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, X, R7, and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

A compound of Formula (IA) or Formula (IB) wherein R¹, R², R³, R⁴, R⁵, R⁶, R⁷, and R⁸ are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Heterocyclic compounds useful as inhibitors of tyrosine kinases

Disclosed are novel compounds of formula (I): wherein Ar 1 , X, Y, P, Q and Het are defined herein, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating diseases resulting from inappropriate cell proliferation, which include autoimmune diseases, chronic inflammatory diseases, allergic diseases, transplant rejection and cancer, as well as conditions resulting from cerebral ischemia, such as stroke. Also disclosed are pharmaceutical compositions comprising these compounds, processes for preparing these compounds and novel intermediate compounds useful in these processes.

Indazole and pyrazolopyridine compounds as CCR1 receptor antagonists

Disclosed are CCR1 receptor antagonists of the formula (I) wherein Ar1, Ar2, R1, X and G are disclosed herein. Also disclosed are compositions, methods of making and using compounds of the formula (I).

Glucocorticoid Mimetics, Methods of Making Them, Pharmaceutical Compositions and Uses Thereof

Compounds of Formula (I) wherein R1, R2, X, and Y are as defined herein, or a tautomer, optical isomer, prodrug, co-crystal, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and thereof

Compounds of Formula (IA) wherein R1, R2, R3, R4 and R5 are as defined herein for Formula (IA), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Azaindazole compounds as CCR1 receptor antagonists

Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are intermediates thereof, and methods of making and methods of using same.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Diastereoselective synthesis of (±)-epianastrephin, (±)-anastrephin and analogs thereof

A process for the synthesis of trans-fused γ-lactones having Formula (IV) from substituted cyclic ketones having Formula (I). A diastereoselective synthesis of (±)-epianastrephin (1) (wherein: R1is ethenyl, R2and R3is methyl, and n is 1), (±)-anastrephin (2) (wherein: R2is ethenyl, R1and R3is methyl and n is 1), and analogs thereof (wherein: R1is H, C1-5alkyl, C2-6alkenyl or C2-6alkynyl, R2is H, C1-5alkyl, C2-6alkenyl or C2-6alkynyl, R1and R2together with the carbon atom they are attached form a C3-6cycloalkyl ring, R3is C1-5alkyl and n is 0-2): ...

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Heterocyclic Compounds As CCR1 Receptor Antagonists

Disclosed are CCR1 receptor antagonists of the formula (I) wherein Ar1, Ar2, R1-R3, X and L are disclosed herein. Also disclosed are compositions, methods of making and using compounds of the formula (I).

1-phenylpydrrolidin-2-ones and -thiones and 1-(4-pyridyl)pydrrolidin-2-ones and -thiones which are useful in the treatment of inflammatory disease

Novel compounds of the formula I:which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are:3-(4-bromobenzyl)-1-(3,5-dichlorophenyl)-1,3-dihydroindol-2-one;3-(4-bromobenzyl)-1-(3,5-dichlorophenyl)-3-methyl-1,3-dihydro-indol-2-one;3-benzyl-1-(3,5-dichlorophenyl)-3-methyl-1,3-dihydroindol-2-one;3-(4-bromobenzyl)-1-(3,5-dichlorophenyl)-4-hydroxy-3-methyl-1,3-dihydroindol-2-one; and,3-(4-bromobenzyl)-1-(3,5-dichlorophenyl)-5-fluoro-1,3-dihydroindol-2-one.

Pyrazolopiperidine compounds as CCR1 receptor antagonists

Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (IA) and Formula (IB) wherein R1, R2, R3, R4, R5, and R6 are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid Mimetics, Methods of Making Them, Pharmaceutical Compositions and Uses Thereof

Compounds of Formula (IA) wherein R1, R2, R3, A, B, C, D, E, G, X, Y, and Z are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

A compound of Formula (IA) or Formula (IB) wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (IA) and Formula (IB) wherein R¹, R², R³, R⁴, R⁵, and R⁶ are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Heterocyclic compounds useful as inhibitors of tyrosine kinases

Disclosed are novel compounds of formula (I):wherein Ar1, X, Y, P, Q and Het are defined herein, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating diseases resulting from inappropriate cell proliferation, which include autoimmune diseases, chronic inflammatory diseases, allergic diseases, transplant rejection and cancer, as well as conditions resulting from cerebral ischemia, such as stroke. Also disclosed are pharmaceutical compositions comprising these compounds, processes for preparing these compounds and novel intermediate compounds useful in these processes.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (IA) and Formula (IB) wherein R1, R2, R3, R4, R5, and R6are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof

Compounds of Formula (IA) and Formula (IB) where in R1 stands for the following group (the dashed line indicates the point of attachment) and R2, R3, R4, R5, R6, Y, Z, X1 and X2 are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid Mimetics, Methods of Making Them, Pharmaceutical Compositions, and Uses Thereof

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, X, R7, and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Indazole compounds as CCR1 receptor antagonists

Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and X are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof, pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

A compound of Formula (IA) or Formula (IB) wherein R¹, R², R³, R⁴, R⁵, R⁶, R⁷ and R⁸ are as defined herein, or a tautomer prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid Mimetics, Methods of Making Them, Pharmaceutical Compositions and Uses Thereof

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (IA) and Formula (IB) wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof

Compounds of Formula (IA) and Formula (IB) where in R1 stands for the following group (the dashed line indicates the point of attachment) and R2, R3, R4, R5, R6, Y, Z, X1 and X2 are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (IA) and Formula (IB) wherein R¹, R², R³, R⁴, R⁵, and R⁶ are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Indazole Compounds As CCR1 Receptor Antagonists

Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and X are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof, pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6 and X are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and thereof

Compounds of Formula (IA) wherein R1, R2, R3, R4 and R5 are as defined herein for Formula (IA), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Cyclohexanol ethers as mediterranean fruit fly attractants

Disclosed are novel cyclohexanol ethers of Formula (I) useful as Mediterranean fruit fly, Ceratitas capitata , attractants: wherein R 1 is C 1-5 alkyl optionally substituted with 0-3 halogens, and R 2 is C 1-3 alkyl. Also disclosed are methods of preparation, methods of formulation, and methods of use.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof

Compounds of Formula (IA), (IB), (IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof

Compounds of Formula (I) wherein R1, R2, X, and Y are as defined herein, or a tautomer, optical isomer, prodrug, co-crystal, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (IA) wherein R1, R2, R3, R4 and R5 are as defined herein for Formula (IA), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Diastereoselective Synthesis of (±)-Epianastrephin, (±)-Anastrephin and Analogs Thereof

A process for the synthesis of trans-fused γ-lactones having Formula (IV) from substituted cyclic ketones having Formula (I). A diastereoselective synthesis of (±)-epianastrephin (1) (wherein: R 1 is ethenyl, R 2 and R 3 is methyl, and n is 1), (±)-anastrephin (2) (wherein: R 2 is ethenyl, R 1 and R 3 is methyl and n is 1), and analogs thereof (wherein: R 1 is H, C 1-5 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, R 2 is H, C 1-5 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, R 1 and R 2 together with the carbon atom they are attached form a C 3-6 cycloalkyl ring, R 3 is C 1-5 alkyl and n is 0-2):

Small molecules useful in the treatment of inflammatory disease

Novel compounds of the formula Iwhich are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are:2-(3,5-Dichlorophenyl)-7-(R*)-phenyl-7a-(R*)-tetrahydropyrrolo[1,2-c]imidazole-1,3-dione;2-(3,5-Dichlorophenyl)-7a-(R*)-methyl-7-(R*)-phenyl-tetrahydropyrrolo[1,2-c]imidazole-1,3-dione; and, 7-(R*)-(4-Bromophenyl)-2-(3,5-dichlorophenyl)-7a-(R*)-tetrahydropyrrolo[1,2-c]imidazole-1,3-dione.

Indazole and Pyrazolopyridine Compounds As CCR1 Receptor Antagonists

Diclosed are CCR1 receptor antagonists of the formula (I) 2. The compound according to claim 1 , and wherein{'sub': 'g', 'Cyclic G is carbocycle-optionally substituted by one to two R'}or a pharmaceutically acceptable salt thereof.3. The compound according to claim 2 , and whereinX is nitrogen;{'sub': 1', 'a, 'Aris carbocycle optionally substituted by one to three R;'}{'sub': 2', 'b, 'Aris carbocycle or heteroaryl, each optionally substituted by one to three R;'}{'sub': '1', 'Ris hydrogen;'}{'sub': a', '1-3', '1', '3', '1', '6, 'Ris Calkyl, C-alkoxy, di-C-alkylamino, methylsulfonyl, halogen, or cyano;'}{'sub': b', '2', 'n', '2', 'n', '2', '1-6', '3', '1', '6', '2', '6', '2', '6', '3-10', '1', '6', '1-6', '2', 'n', 'c', 'd', '3', 'm', '2', '0-1', '3', 'm', 'e', '3', 'e', 'm', '2', '0-1', 'f', 'e', '2', 'y', '2', 'n', 'c', 'd', 'b', '1-6', '1', '6', '1', '6', '1', '6', 'm, 'Ris hydroxyl, carboxyl, halogen, —(CH)—CN, —(CH)—COCalkyl, nitro, —SOH, C-alkyl, C-alkenyl, C-alkynyl, Ccycloalkyl, C-alkoxy, CalkylC(O)—, —(CH)—NRR, R—S(O)(CH)—, R—S(O)—NR—, R—NR—S(O)(CH)—, —NR—C(O)—R, —(CH)—C(O)—(CH)—NRR, heterocyclyl, aryl or heteroaryl, each Rwhere possible is optionally halogenated or substituted with 1 to 3 Calkyl, C-acyl, C-alkoxycarbonyl, C-alkyl-S(O)—, aryl or carboxyl;'}{'sub': 3', '1-6', '3-6', '2', '0-1', '1', '6', '1-6', '2', '2-3', '1-6', '1', '6', '3-6', '1', '6', 'e', 'f', '1', '6', '1', '6', '1', '6, 'Ris hydrogen, Calkyl, Ccycloalkyl, heterocyclyl(CH), mono-or di-C-alkylamino, mono-or di-alkylamino(CH)N(Calkyl)-, aryl or heteroaryl each optionally substituted with 1 to 2 C-alkyl, Ccycloalkyl, C-alkoxy, halogen, hydroxyl, oxo, carboxyl, —C(O)NRR, amino, mono-or di-C-alkylamino, C-alkoxycarbonyl or C-acylamino'}or a pharmaceutically acceptable salt thereof.4. The compound according to claim 3 , and wherein{'sub': 1', 'a, 'Aris phenyl is substituted by one to two R;'}{'sub': 2', 'b, 'Aris phenyl, thiadiazolyl, oxadiazolyl, pyrimidinyl, furanyl, thiazolyl or pyridyl, ...

Heterocyclic compounds useful as inhibitors of tyrosine kinases

Disclosed are novel compounds of formula (I): wherein Ar1, X, Y, P, Q and Het are defined herein, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating diseases resulting from inappropriate cell proliferation, which include autoimmune diseases, chronic inflammatory diseases, allergic diseases, transplant rejection and cancer, as well as conditions resulting from cerebral ischemia, such as stroke. Also disclosed are pharmaceutical compositions comprising these compounds, processes for preparing these compounds and novel intermediate compounds useful in these processes.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

A compound of Formula (IA) or Formula (IB) wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof

Compounds of Formula (IA) wherein R1, R2, R3, A, B, C, D, E, G, X, Y, and Z are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Indazole compounds as CCR1 receptor antagonists

Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Pyridinyl compounds useful as intermediates

Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are intermediates thereof, and methods of making and methods of using same.

Heterocyclic compounds as CCR1 receptor antagonists

Disclosed are CCR1 receptor antagonists of the formula (I) wherein Ar1, Ar2, R1-R3, X and L are disclosed herein. Also disclosed are compositions, methods of making and using compounds of the formula (I).

Heterocyclic compounds useful as inhibitors of tyrosine kinases

Disclosed are novel compounds of formula (I):wherein Ar1, X, Y, P, Q and Het are defined herein, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating diseases resulting from inappropriate cell proliferation, which include autoimmune diseases, chronic inflammatory diseases, allergic diseases, transplant rejection and cancer, as well as conditions resulting from cerebral ischemia, such as stroke. Also disclosed are pharmaceutical compositions comprising these compounds, processes for preparing these compounds and novel intermediate compounds useful in these processes.

Azaindazole compounds as CCR1 receptor antagonists

Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.

GLUCOCORTICOID MIMETICS, METHODS OF MAKING THEM, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6 and X are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

A compound of Formula (IA) or Formula (IB) wherein R1, R2, R3, R4, R5, R6, R7,and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (IA) and Formula (IB) wherein R1, R2, R3, R4, R5, and R6 are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Pyridinyl Compounds Useful As Intermediates

Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are intermediates thereof, and methods of making and methods of using same.

Pyrazolopiperidine Compounds As CCR1 Receptor Antagonists

Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. 2. The compound according to and wherein{'sub': 1', 'a, 'Aris aryl substituted by one to three R;'}{'sub': 2', 'b, 'Aris aryl or heteroaryl, each optionally substituted by one to three R;'}{'sub': 2', '3', 'm, 'Y is (CRR);'}{'sub': '1', 'Ris hydrogen;'}{'sub': e', 'f', '1-6', '1-6, 'each R, Rare independently hydrogen, Calkyl or hydroxyCalkyl;'}{'sub': 2', '3', '1-6', '2-6', '1-6', '2-6, 'R, Rare each independently hydrogen, Calkyl or Calkenyl, wherein the Calkyl or Calkenyl is optionally partially or fully halogenated,'}{'sub': 2', '3', '3-7', '2', '3, 'or R, Rcan form a Ccycloalkyl ring provided that R, Rare attached to the same carbon atom,'}{'sub': 5', '1-6', '2', 'e', 'f', '1-6, 'Ris hydrogen, CalkylCO—, carboxyl, N(R)(R)—C(O)— or Calkyl optionally partially or fully halogenated;'}{'sub': 6', '1-6, 'Ris hydrogen, Calkyl;'}{'sub': '7', 'Ris hydrogen.'}3. The compound according to and wherein{'sub': 1', 'a, 'Aris phenyl substituted by one to three R;'}{'sub': '2', 'Aris phenyl or heteroaryl chosen from furanyl, pyranyl, benzoxazolyl, benzothiazolyl, benzimidazolyl, oxazolyl, isoxazolyl, thiazolyl, pyrazolyl, pyrrolyl, imidazolyl, thienyl, thiadiazolyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, quinolinyl, isoquinolinyl, quinazolinyl, indazolyl, indolyl, isoindolyl, benzofuranyl, benzopyranyl, pyrrolopyridinyl and benzodioxolyl;'}{'sub': 'b', 'each optionally substituted by one to three R.'}4. The compound according to and wherein{'sub': '2', 'Aris phenyl, benzyl, phenethyl or heteroaryl chosen from pyridinyl, pyrimidinyl, pyridazinyl and pyrazinyl;'}{'sub': 'b', 'each optionally substituted by one to three R.'}5. The compound according to and wherein{'sub': '2', 'Aris phenyl, benzyl, phenethyl or pyridinyl ...

Indazole compounds as ccr1 receptor antagonists

Indazole and pyrazolopyridine compounds as ccr1 receptor antagonists

Heterocyclic compounds as ccr1 receptor antagonists

Pyrazolopiperidine compounds as ccr1 receptor antagonists

1,1,1-trifluoro-4-phenyl-4-methyl-2-(1h-pyrrolo

Compounds of Formula (IA), IB), IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Indazole and pyrazolopyridine compounds as ccr1 receptor antagonists

Diclosed are CCRl receptor antagonists of the formula (I), wherein X is nitrogen or, C-R2; Ar1 is carbocycle, heteroaryl or heterocyclyl each optionally substituted by one to three Ra; Ar2 is carbocycle, heteroaryl or heterocyclyl, each optionally substituted by one to three Rb; Cyclic G is carbocycle, or heterocyclyl each optionally substituted by one to two R8; R1 is hydrogen, C1-6 alkyl or C 1-6 alkoxyC1-6 alkyl. Also disclosed are compositions, methods of making and using compounds of the formula (I).

Azaindazole compounds as CCR1 receptor antagonists

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (IA), and Formula (IB), wherein R1, R2, R3, A, B, C, D, E, G, X, Y, and Z are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

1,2,1-Trifluoro-4-phenyl-4-methyl-2-(1H-pyrrolo[2,3-C]pyridin-2-ylmethyl)pentan-2-ol derivatives and related compounds as glucocorticoid ligands for the treatment of inflammatory diseases and diabetes.

Disclosed are compounds of Formula IA, IB, IC and ID wherein R1 is an optionally substituted aryl or heteroaryl group, R5 is an optionally substituted heteroaryl group and wherein the rest of the substituents are disclosed within the specification. Also disclosed is the preparation of a compound of formula IA, IB, IC or ID and the use of compound of formula IA, IB, IC and ID in the manufacture of a medicament for modulating glucocorticoid receptor function.

AZAINDAZOL COMPOUNDS AS AN RECRUITOR OF THE RECEIVER OF CCR1

Se describen compuestos de la fórmula (I), útiles para tratar una diversidad de enfermedades y trastornos que están mediados o sostenidos por la actividad de CCR1 incluyendo enfermedades autoinmunes, tales como artritis reumatoide y esclerosis múltiple.(I)También se describen métodos para su preparación y métodos de uso de los mismos.

Indazole compounds as ccr1 receptor antagonists

Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Small molecules useful in the treatment of inflammatory disease

Novel compounds of the formula (I) which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are: 3-(4-bromobenzyl)-1-(3,5-dichlorophenyl)-1,3-dihydroindol-2-one; 3-(4-bromobenzyl)-1-(3,5-dichlorophenyl)-3-methyl-1,3-dihydro-indol-2-one; 3-benzyl-1-(3,5-dichlorophenyl)-3-methyl-1,3-dihydroindol-2-one; 3-(4-bromobenzyl)-1-(3,5-dichlorophenyl)-4-hydroxy-3-methyl-1,3-dihydroindol-2-one; and 3-(4-bromobenzyl)-1-(3,5-dichlorophenyl)-5-fluoro-1,3-dihydroindol-2-one.

Glucocorticoid mimetics, methods of their preparation, pharmaceutical compositions and uses thereof

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (IA) and Formula (IB) wherein R1, R2, R3, R4, R5 and R6 are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing su ch compounds, and methods of modulating the glucocorticoid receptor function an d methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Azaindazole compounds as ccr1 receptor antagonists

Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.

Indazole and pyrazolobidine compound as ccr1 receptor antagonists

L'INVENTION PORTE SUR DES ANTAGONISTES DU RÉCEPTEUR CCR1 REPRÉSENTÉ PAR LA FORMULE (I) (FORMULE (I)) DANS LAQUELLE X REPRÉSENTE L'AZOTE OU C-R2; AR1 REPRÉSENTE UN CARBOCYCLE, UN HÉTÉROARYLE OU UN HÉTÉROCYCLYLE CHACUN ÉVENTUELLEMENT SUBSTITUÉ PAR UN À TROIS RA ; AR2 REPRÉSENTE UN CARBOCYCLE, UN HÉTÉROARYLE OU UN HÉTÉROCYCLYLE CHACUN ÉVENTUELLEMENT SUBSTITUÉ PAR UN À TROIS RB; G CYCLIQUE REPRÉSENTE UN CARBOCYCLE OU UN HÉTÉROCYCLYLE CHACUN ÉVENTUELLEMENT SUBSTITUÉ PAR UN À DEUX R8; R1 REPRÉSENTE HYDROGÈNE, ALKYLE EN C1-6 OU (ALCOXY EN C1-6)(ALKYLE EN C1-6). L'INVENTION PORTE ÉGALEMENT SUR DES COMPOSITIONS, SUR DES PROCÉDÉS DE FABRICATION ET D'UTILISATION DE COMPOSÉS REPRÉSENTÉS PAR LA FORMULE (I). The invention relates to CCR1 RECEPTOR ANTAGONISTS REPRESENTED BY FORMULA (I) (FORMULA (I)) IN WHICH X REPRESENTS NITROGEN OR C-R2; AR1 REPRESENTS A CARBOCYCLE, A HETEROARYL OR A HETEROCYCLYL EACH SUFFICIENTLY SUBSTITUTED BY ONE TO THREE RA; AR2 REPRESENTS A CARBOCYCLE, A HETEROARYL OR A HETEROCYCLYL EACH WHICH CAN BE SUBSTITUTED BY ONE TO THREE BR; G CYCLIC REPRESENTS A CARBOCYCLE OR HETEROCYCLYL EACH THAT CAN BE SUBSTITUTED BY ONE TO TWO R8; R1 REPRESENTS HYDROGEN, C1-6 ALKYL OR (C1-6 ALCOXY) (C1-6 ALKYL). The invention also relates to compositions, processes for the manufacture and use of compounds represented by Formula (I).

Azaindazole Compounds As CCR1 Receptor Antagonists

Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.

Small molecules useful in the treatment of inflammatory disease

Novel compounds of formula (I) which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are: 2-(3,5-Dichlorophenyl)-7-(R*-phenyl-7a-(R*)-tetrahydropyrrolo[1,2-c]imidazole-1,3-dione; 2-(3,5-Dichlorophenyl)-7a-(R*-methyl-7-(R*)-phenyl-tetrahydropyrrolo[1,2-c]imidazole-1,3-dione; and, 7-(R*)-(4-Bromophenyl)-2-(3,5-dichlorophenyl)-7a-(R*)-tetrahydropyrrolo[1,2-c]imidazole-1,3-dione.

MIMETICS OF GLUCOCORTICOIDS, PROCEDURES FOR THE PREPARATION, PHARMACEUTICAL COMPOSITIONS AND THEIR USE OF THEM.

Compuestos de fórmula (IA) y fórmula (IB) en las que R1, R2, R3, R4, R5, y R6, son como se definen en la presente memoria para la fórnula (IA) o la fórmula (IB), o uno de sus tautómeros, profármacos, solvatos o sales, composiciones farmacéuticas que contienen dichos compuestos y procedimientos para modular la función del receptor de glucocorticoides y procedimientos para tratar estados de enfermedad o trastornos mediados por la función del receptor de glucocorticoides o caracterizados por procesos inflamatorios, alérgicos o proliferativos en un paciente usando estos compuestos. Compounds of formula (IA) and formula (IB) in which R1, R2, R3, R4, R5, and R6, are as defined herein for the formula (IA) or formula (IB), or one of its tautomers, prodrugs, solvates or salts, pharmaceutical compositions containing said compounds and procedures for modulating the function of the glucocorticoid receptor and procedures for treating disease states or disorders mediated by the function of the glucocorticoid receptor or characterized by inflammatory, allergic processes or proliferative in a patient using these compounds.

GLUCOCORTICOID MIMETIC COMPOUNDS, METHODS OF PREPARATION AND PHARMACEUTICAL COMPOSITIONS

SE REFIERE A COMPUESTOS DE FORMULA (IB) DONDE R1 ES ARILO O HETEROARILO OPCIONALMENTE SUSTITUIDO CON ALQUILO C1-C5, ALQUENILO C2-C5, ALQUINILO C2-C5, ENTRE OTROS; R2 Y R3 SON CADA UNO ALQUILO C1-C5; R4 ES ALQUILO C1-C5, ALQUENILO C2-C5, ALQUINILO C2-C5 OPCIONALMENTE SUSTITUIDO CON ALQUILO C1-C3, HIDROXI, HALOGENO, AMINO, OXO; R5 ES HETEROARILO OPCIONALMENTE SUSTITUIDO CON ALCOXICARBONILO C1-C5, ALCANOILOXI C1-C5, AMINOCARBONILO, ENTRE OTROS; R6 ES H, ALQUILO C1-C8, ALQUENILO C2-C8, ENTRE OTROS, NO PUDIENDO SER TRIFLUOROMETILO, OPCIONALMENTE SUSTITUIDO CON ALQUILO C1-C5, ALQUENILO C2-C5, ALQUINILO C2-C5, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-CICLOPROPIL-4-(5-FLUORO-2-METOXIFENIL)-4-METIL-1-(1H-PIRROLO[3,2-c]PIRIDIN-2-IL)PENTAN-2-OL, METIL ESTER DEL ACIDO 4-(5-FLUORO-2-METOXIFENIL)-2-HIDROXI-4-METIL-2-(1H-PIRROLO[2,3-c]PIRIDIN-2-ILMETIL)PENTANOICO, 2-[2-DIFLUOROMETIL-2-HIDROXI-4-(5-METANSULFONIL-2,3-DIHIDROBENZOFURAN-7-IL)-4-METILPENTIL]-4-METIL-1H-INDOL-6-CARBONITRILO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON MODULADORES DEL RECEPTOR DE GLUCOCORTICOIDES SIENDO UTILES PARA EL TRATAMIENTO DE ENFERMEDADES PULMONARES, REUMATICAS, ALERGICAS, RENALES, HEPATICAS, CARDIOVASCULARES, NEUROLOGICAS, DIABETES TIPO I y II, OBESIDAD, ENFERMEDAD DE ALZHEIMER, ARTERIOESCLEROSIS, OSTEOARTRITIS, DOLOR GRAVE Y CRONICO REFERS TO FORMULA COMPOUNDS (IB) WHERE R1 IS ARYL OR HETEROARYL OPTIONALLY SUBSTITUTED WITH C1-C5 ALKYL, C2-C5 ALKENYL, C2-C5 ALKINYL, AMONG OTHERS; R2 AND R3 ARE EACH C1-C5 ALKYL; R4 IS C1-C5 ALKYL, C2-C5 ALKYL, C2-C5 ALKYL, OPTIONALLY SUBSTITUTED WITH C1-C3 ALKYL, HYDROXY, HALOGEN, AMINO, OXO; R5 IS HETEROARYL, OPTIONALLY SUBSTITUTED WITH C1-C5 ALCOXYCARBONYL, C1-C5 ALKANOYLOXY, AMINOCARBONYL, AMONG OTHERS; R6 IS H, C1-C8 ALKYL, C2-C8 ALKYL, AMONG OTHERS, IT CANNOT BE TRIFLUOROMETHYL, OPTIONALLY SUBSTITUTED WITH C1-C5 ALKYL, C2-C5 ALKENYL, C2-C5 ALKYL, AMONG OTHERS. PREFERRED COMPOUNDS ...

Glucocorticoid mimetics, pharmaceutical preparations and applications for the manufacture of drugs for the treatment of disease

Forbindelser med Formel (IA) og Formel (IB) hvor R, R, R, R, R5 og Rer som definert heri for Formel (IA) eller Formel (IB) eller en tautomer, prodrug, solvat eller salt derav; farmasøytiske preparater inneholdende slike forbindelser og metoder for å modulere glukocorticoidreseptorfunksjonen og metoder for behandling av sykdomstilstander eller forstyrrelser mediert av glukocorticoidreseptorfunksjonen ellerinflammatoriske, allergiske eller proliferative prosesser hos en pasient ved anvendelse av disse forbindelser.

THIOFENSULPHONAMIDES WHICH CAN BE USED AS CARBONIC ACID ANHYDRASE INHIBITORS

Tiofensulfonamider og farmasøytis- ke preparater som inneholder forbindel- sene, som kan anvendes ved regulering av intraokulart trykk. Fremgangsmåte -for regulering av intraokulart trykk ved administrering av preparatene.

Thiophene sulfonamides useful as carbonic anhydrase inhibitors

Thiophene sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, X, R7, and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Process for the preparation of therapeutically active thiophenesulfonamides

Alpha-trifluoromethyl alcohols or amines as glucocorticoid mimetics

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6 and X are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammtory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of preparing them, pharmaceutical compositions and applications thereof

Forbindelser med Formel (IA) og Formel (IB) hvor R, R, R, R, Rog Rer ran definert heri for Formel (IA) eller Formel (IB) eller en tautomer, prodrug, solvit eller salt derav; farmasøytiske preparater inneholdende slike forbindelser og metoder for å modulere glukocorticoidieseptorfunksjonen og metoder forfnwg av sykdomstilstander eller forstyrrelser mediert av glukocoiticoidicseptoifunksjonen ellerinflammatoriske, allergiske eller proliferative prosesser hos en pasient ved anvendelse av disse forbindelser.

1,1,1-Trifluoro-4-Phenyl-4-methyl-2-(1H-Pyrrolo

Small molecules useful in the treatment of inflammatory disease

Novel compounds of the formula (I) which are useful for treating or preventi ng inflammatory and immune cell-mediated diseases. Exemplary compounds are: 3-( 4- bromobenzyl)-1-(3,5-dichlorophenyl)-1,3-dihydroindol-2-one; 3-(4-bromobenzyl )- 1-(3,5-dichlorophenyl)-3-methyl-1,3-dihydro-indol-2-one; 3-benzyl-1-(3,5- dichlorophenyl)-3-methyl-1,3-dihydroindol-2-one; 3-(4-bromobenzyl)-1-(3,5- dichlorophenyl)-4-hydroxy-3-methyl-1,3-dihydroindol-2-one; and 3-(4- bromobenzyl)-1-(3,5-dichlorophenyl)-5-fluoro-1,3-dihydroindol-2-one.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, X, R7, and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

THIOPHENE SULFONAMIDES USED AS CARBOHYDRASE INHIBITORS

Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Pyrazolopiperidine compounds as ccr1 receptor antagonists

Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

A compound of Formula (IA) or Formula (IB) wherein R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

1,1,1-trifluoro-4-phenyl-4-methyl-2-(1H-pyrrolo [2,3-C]pyridin-2-ylmethyl)pentan-2-ol Derivatives and related compounds as glucocorticoid ligands for the treatment of inflammatory diseases and diabetes.

Compounds derived from pyrazolopyridine; Preparation process; Pharmaceutical composition and use in the treatment of diseases such as rheumatoid arthritis, psoriasis, multiple sclerosis, among others.

Compuestos derivados de pirazolopiridina; proceso de preparación; composición farmacéutica y uso en el tratamiento de enfermedades tales como artritis reumatoide, psoriasis, esclerosis múltiple, entre otras.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Spoj, naznačen time, da ima formulu (1) gdje: R1 je arilna ili heteroarilna skupina, svaka opcijski neovisno supstituirana s jednom, dvije ili tri supstituentske skupine odabrane od sljedećih: C1-C5 alkil, aminokarbonil, C1-C5 alkilaminokarbonil, C1-C5 dialkilaminokarbonil, aminosulfonil, C1-C5 alkilaminosulfonil, C1-C5 dialkilaminosulfonil, halogen, hidroksil, cijano i C1-C5 alkiltio, gdje je atom sumpora opcijski oksidiziran na sulfoksid ili sulfon; R2 je C1-C5 alkiltio gdje je atom sumpora opcijski oksidiziran na sulfoksid ili sulfon, opcijski neovisno supstituiran s jednom, dvije ili tri supstituentske skupine odabrane od sljedećih: halogen, hidroksi, okso, cijano, alkoksialkil i aminokarbonil; X je CH ili N; i Y je CH ili N, gdje X i Y nisu oba CH, ili njegov tautomer, optički izomer, ko-kristal, ili njegova sol. Patent sadrži još 28 patentnih zahtjeva. A compound of formula (1) wherein: R 1 is an aryl or heteroaryl group, each optionally independently substituted with one, two or three substituent groups selected from C1-C5 alkyl, aminocarbonyl, C1-C5 alkylaminocarbonyl, C1- C5 dialkylaminocarbonyl, aminosulfonyl, C1-C5 alkylaminosulfonyl, C1-C5 dialkylaminosulfonyl, halogen, hydroxyl, cyano and C1-C5 alkylthio, wherein the sulfur atom is optionally oxidized to a sulfoxide or sulfone; R 2 is C 1 -C 5 alkylthio wherein the sulfur atom is optionally oxidized to a sulfoxide or sulfone, optionally independently substituted with one, two or three substituent groups selected from halogen, hydroxy, oxo, cyano, alkoxyalkyl and aminocarbonyl; X is CH or N; and Y is CH or N, wherein X and Y are not both CH, or a tautomer thereof, an optical isomer, a co-crystal, or a salt thereof. The patent contains another 28 patent claims.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula I wherein R 1 , R 2 , X, and Y are as defined herein, or a tautomer, optical isomer, prodrug, co-crystal, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

2-propanol and 2-propylamine derivatives and their use as glucocorticoid ligands

Compounds of Formula (IA) and Formula (IB): wherein in R1 stands for the following group (the dashed line indicates the point of attachement) and R2, R3, R4, R5, R6, Y, Z, X1 and X2 are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Heterozyklische verbindungen als inhibitoren von tyrosin-kinasen

Glucocorticoidmimetika, verfahren zu deren herstellung, pharmazeutische zusammensetzungen und anwendungen davon

1-propanol and 1-propylamine derivatives and their use as glucocorticoid ligands

Kleine moleküle zur behandlung von endzündlichen erkrankungen

Als carbohydrase-inhibitoren verwendbare thiophen sulfonamide

Glucocorticoid-mimetika, verfahren zu deren herstellung, pharmazeutische zusammensetzungen und deren verwendung

Diastereoselective synthesis of (±)-epianastrephin, (±)-anastrephin and analogs thereof

A process for the synthesis of trans -fused γ -lactones having Formula (IV) from substituted cyclic ketones having Formula (I). A diastereoselective synthesis of (±)- epianastrephin (1) (wherein: R 1 i s ethenyl, R 2 and R 3 is methyl, and n is 1), (±)-anastrephin (2) (wherein: R 2 is ethenyl, R 1 and R 3 is methyl and n is 1), and analogs thereof (wherein :_R 1 is H, C 1-5 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, R 2 is H, C 1-5 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, R 1 and R 2 together with the carbon atom they are attached form a C 3-6 cycloalkyl ring, R 3 is C 1-5 alkyl and n is 0-2): Formula I, II, III, IV.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

A compound of Formula (IA) or Formula (IB) wherein R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Clucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

COMPOUNDS OF FORMULA (IA) AND FORMULA (IB) WHEREIN R1,R2,R3,R4,R5, AND R6 ARE AS DEFINED HEREIN FOR FORMULA (IA) OR FORMULA (IB), OR A TAUTOMER, PRODRUG, SOLVATE, OR SALT THEREOF; PHARMACEUTICAL COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF MODULATING THE GLOCOCORTICOID RECEPTOR FUNCTION AND METHODS OF TREATING DISEASE-STATES OR CONDITIONS MEDIATED BY THE GLUCOCORTICOID RECEPTOR FUNCTION OR CHARACTERIZED BY INFLAMMATORY, ALLERGIC, OR PROLIFERATIVE PROCESSES IN A PATIENT USING THESE COMPOUNDS.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.