Substituted heterocyclic diarylamine analogues

Arylalkylamino-substituted quinazoline analogues

Imidazopyrimidines and imidazopyridines for the treatment of neurological disorders

Imidazopyrimidinyl and imidazopyridinyl derivatives

Capsaicin receptor ligands

Imidazopyrimidines and imidazopyridines for the treatment of neurological disorders

Pyrrolo (3,4-d) pyrimidines as corticotropin releasing factor (crf) antagonists

Arylamino fused pyridines and pyrimidines

Substituted biaryl quinolin-4-ylamine analogues

Substituted biphenyl-4-carboxylic acid arylamide analogues as capsaicin receptor modulators

Substituted pyridin-2-ylamine analogues

Aryloxy- and arylthio-fused pyridines and pyrimidines and derivatives

Aryl substituted purine analogues

Capsaicin receptor ligands

Heteroaryl amide analogues

Melanin concentrating hormone receptor ligands

SUBSTITUTED PYRIMIDINE COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF

The present disclosure relates to pyrimidine compounds of formula (I), their stereoisomers, tautomers, pharmaceutically acceptable salts, polymorphs, solvates, and hydrates thereof. The present disclosure also relates to process of preparation of these pyrimidine compounds, and to pharmaceutical compositions containing them. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders mediated by epidermal growth factor receptor (EGFR) family kinases.

Spiro(isobenzofuran-1,4'-piperidin)-3-ones and 3h-spiroisobenzofuran-1,4'-piperidines

2-SUBSTITUTED QUINAZOLIN-4-YLAMINE ANALOGUES AS CAPSAICIN RECEPTOR MODULATORS

Substituted quinolin-4-ylamine analogues

2-phenoxy pyrimidinone analogues

Biaryl piperazinyl-pyridine analogues

5-membered heterocyclic amides and related compounds

5-membered heterocyclic amides and related compounds

The invention provides 5-Membered heterocyclic amides and related compounds of the following formula, wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

SUBSTITUTED BIPHENYL-4-CARBOXYLIC ACID ARYLAMIDE ANALOGUES

4 - heterobicyclyamino - substituted quinazolines and analogues therof as capsaicin - antagonists

1h-imidazo(4,5-d)pyridazin-7-ones, 3h-imidazo(4,5-c)pyridin-4-ones and corresponding thiones as corticotropin releasing factor (crf) receptor ligands

4-amino (AZA) quinoline derivatives as capsaicin receptor agonists

CARBOXYLIC ACID, PHOSPHATE OR PHOSPHONATE SUBSTITUTED QUINAZOLIN-4-YLAMINE ANALOGUES AS CAPSAICIN RECEPTOR MODULATORS

Piperazinyl-pyridine analogues

Aryloxy- and arylthio-fused pyridines and pyrimidines and derivatives

Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone (crh) antagonists, useful for treating cns and stress-related disorders

Capsaicin receptor ligands

Piperazinyl-pyridine analogues

Heteroaryl amide analogues

Compounds, pharmaceutical compositions, and methods of use are disclosed for heteroaryl amide analogues of formula Ia and/or Ib. In certain embodiments, the heteroaryl amide analogues are agonists and/or ligands of dopamine receptors and may be useful, inter alia, for the treatment of a condition responsive to P2X7 receptor modulation, for example, pain, inflammation, a neurological or neurodegenerative disorder, a cardiovascular disorder, an ocular disorder or an immune system disorder.

5-MEMBERED HETEROCYCLIC AMIDES AND RELATED COMPOUNDS

2-phenoxy pyrimidinone analogues

... 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

2-PHENOXY PYRIMIDINONE ANALOGUES

2-Phenoxy pyrimidinone analogues are provided, of the Formula: 7. A compound or salt or hydrate thereof according to claim 2 , wherein Rrepresents from 1 to 3 substituents independently chosen from halogen claim 2 , cyano claim 2 , C-Calkyl and C-Chaloalkyl.8. A compound or salt or hydrate thereof according to claim 7 , wherein one substituent represented by Ris a halogen or cyano at the para position.9. A compound or salt or hydrate thereof according to claim 7 , wherein Rrepresents exactly one substituent.10. A compound or salt or hydrate thereof according to claim 1 , wherein Rrepresents from 1 to 3 substituents independently chosen from halogen claim 1 , cyano claim 1 , C-Calkyl claim 1 , C-Chaloalkyl and C-Calkoxy.15. A compound or salt or hydrate thereof according to claim 1 , wherein the compound is:1-(4-bromophenyl)-9-methyl-2-(2,3,4-trifluorophenoxy)-1,9-dihydro-6H-purin-6-one;1-(4-chlorophenyl)-2-(2,3-difluorophenoxy)-9-methyl-1,9-dihydro-6H-purin-6-one;1-(4-chlorophenyl)-2-(2,4-difluorophenoxy)-9-methyl-1,9-dihydro-6H-purin-6-one;1-(4-chlorophenyl)-2-[2-fluoro-3-(trifluoromethyl)phenoxy]-9-methyl-1,9-dihydro-6H-purin-6-one;1-(4-chlorophenyl)-9-methyl-2-(2,3,4-trifluorophenoxy)-1,9-dihydro-6H-purin-6-one;1-(4-chlorophenyl)-9-methyl-2-(2,3,5-trifluorophenoxy)-1,9-dihydro-6H-purin-6-one;1-(4-chlorophenyl)-9-methyl-2-(2,3,6-trifluorophenoxy)-1,9-dihydro-6H-purin-6-one;1-(4-chlorophenyl)-9-methyl-2-(2,4,5-trifluorophenoxy)-1,9-dihydro-6H-purin-6-one;1-(4-chlorophenyl)-9-methyl-2-(2,4,6-trifluorophenoxy)-1,9-dihydro-6H-purin-6-one;1-(4-chlorophenyl)-9-methyl-2-(3,4,5-trifluorophenoxy)-1,9-dihydro-6H-purin-6-one;1-(4-fluorophenyl)-2-[2-fluoro-3-(trifluoromethyl)phenoxy]-9-methyl-1,9-dihydro-6H-purin-6-one;1-(4-fluorophenyl)-2-[3-fluoro-5-(trifluoromethyl)phenoxy]-9-methyl-1,9-dihydro-6H-purin-6-one;1-(4-fluorophenyl)-9-methyl-2-(2,3,4-trifluorophenoxy)-1,9-dihydro-6H-purin-6-one;1-(4-fluorophenyl)-9-methyl-2-(2,3,5-trifluorophenoxy)-1,9-dihydro-6H-purin-6-one;1 ...

COMPOUNDS USEFUL AS CCR9 MODULATORS

The present invention relates to compounds useful as CCR9 modulators, to compositions containing them, to methods of making them, and to methods of using them. In particular, the present invention relates to compounds capable of modulating the function of the CCR9 receptor by acting as partial agonists, antagonists or inverse agonists. Such compounds may be useful to treat, prevent or ameliorate a disease or condition associated with CCR9 activation, including inflammatory and immune disorder diseases or conditions such as inflammatory bowel diseases (IBD). 2. A compound of Formula (I) as claimed in claim 1 , or a salt or solvate thereof claim 1 , including a solvate of such a salt claim 1 , wherein Ris hydrogen.3. A compound of Formula (I) as claimed in or claim 1 , or a salt or solvate thereof claim 1 , including a solvate of such a salt claim 1 , wherein X is a direct bond.4. A compound of Formula (I) as claimed in or claim 1 , or a salt or solvate thereof claim 1 , including a solvate of such a salt claim 1 , wherein X is CH.5. A compound of Formula (I) as claimed in any of the preceding claims claim 1 , or a salt or solvate thereof claim 1 , including a solvate of such a salt claim 1 , wherein Ris selected from optionally substituted aryl claim 1 , optionally substituted heteroaryl claim 1 , and optionally substituted Cheterocycloalkyl.6. A compound of Formula (I) as claimed in claim 5 , or a salt or solvate thereof claim 5 , including a solvate of such a salt claim 5 , wherein Ris selected from optionally substituted phenyl claim 5 , optionally substituted pyridyl claim 5 , optionally substituted thiophenyl claim 5 , optionally substituted pyrazolyl claim 5 , optionally substituted pyrimidinyl claim 5 , optionally substituted imidazolyl claim 5 , and optionally substituted thiazolyl.7. A compound of Formula (I) as claimed in claim 6 , or a salt or solvate thereof claim 6 , including a solvate of such a salt claim 6 , wherein Ris selected from cyanophenyl claim ...

Benzene sulfonamides as ccr9 inhibitors

The present invention relates to compounds useful as CCR9 modulators, to compositions containing them, to methods of making them, and to methods of using them. In particular, the present invention relates to compounds capable of modulating the function of the CCR9 receptor by acting as partial agonists, antagonists or inverse agonists. Such compounds may be useful to treat, prevent or ameliorate a disease or condition associated with CCR9 activation, including inflammatory and immune disorder diseases or conditions such as inflammatory bowel diseases (IBD).

5-Membered Heterocyclic Amides And Related Compounds

5-Membered heterocyclic amides and related compounds are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies. 1122-. (canceled)126. A compound or salt or hydrate thereof according to claim 123 , wherein Y is C-Ccycloalkyl claim 123 , 6- to 10-membered aryl or 5- to 10-membered heteroaryl claim 123 , each of which is substituted with from 0 to 4 substituents independently chosen from halogen claim 123 , hydroxy claim 123 , cyano claim 123 , amino claim 123 , C-Calkyl claim 123 , C-Calkenyl claim 123 , C2-Calkynyl claim 123 , C-Chaloalkyl claim 123 , C-Chydroxyalkyl claim 123 , C-Calkoxy claim 123 , and mono- or di-(C-Calkyl)amino.127. A compound or salt or hydrate thereof according to claim 123 , wherein Y is phenyl or a 5- or 6-membered heteroaryl; each of which is optionally fused to a 5- to 7-membered carbocycle or a 5- to 7-membered heterocycle; and each of which phenyl claim 123 , heteroaryl claim 123 , carbocycle and heterocycle is substituted with from 0 to 4 substituents independently chosen from halogen claim 123 , hydroxy claim 123 , cyano claim 123 , amino claim 123 , C-Calkyl claim 123 , C-Calkenyl claim 123 , C-Calkynyl claim 123 , C-Chaloalkyl claim 123 , C-Chydroxyalkyl claim 123 , C-Calkoxy claim 123 , and mono- or di-(C-Calkyl)amino.129. The compound of selected from the group consisting of1-(4-amino-5-methylpyrimidin-2-yl)-N-[2-(4-chlorophenyl)-4-methylpentyl]-3-methyl-1H-pyrazole-4-carboxamide;1-(4-amino-5-fluoropyrimidin-2-yl)-N-[2-(4-chlorophenyl)-4-methylpentyl]-3-methyl-1H-pyrazole-4- ...

SUBSTITUTED IMIDAZOLES AS N-TYPE CALCIUM CHANNEL BLOCKERS

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: 2. The compound of wherein Ris{'sub': 1-4', '1-4, 'i) phenyl independently substituted with one to three substituents that are selected from the group consisting of chloro, fluoro, bromo, cyano, trifluoromethyl, Calkyl, difluoromethoxy, and Calkoxy; provided that when phenyl of group (i) is substituted with a single substituent, that substituent is at the 4-position;'}{'sub': 1-4', '1-4, 'ii) a heteroaryl that is pyridinyl; wherein said pyridinyl is optionally independently substituted with one or two substituents that are chloro, fluoro, bromo, cyano, trifluoromethyl, Calkyl, or Calkoxy;'}{'sub': 1-4', '1-4, 'iii) phenylmethyl, wherein the phenyl portion of phenylmethyl is optionally independently substituted with one or two substituents that are selected from the group consisting of chloro, fluoro, bromo, cyano, trifluoromethyl, Calkyl, and Calkoxy; provided that when phenylmethyl of group (iii) is substituted with a single substituent, that substituent is at the 4-position;'}{'sub': 1-4', '1-4, 'iv) phenylsulfonyl, wherein the phenyl portion of phenylsulfonyl is optionally independently substituted with one or two substituents that are selected from the group consisting of chloro, fluoro, bromo, cyano, trifluoromethyl, Calkyl, and Calkoxy; provided that when phenylsulfonyl of group (iv) is substituted with a single substituent, that substituent is at the 4-position;'}{'sub': '1-4', 'v) Calkylsulfonyl; or'}vi) trifluoromethylsulfonyl.3. The compound of wherein Ris{'sub': '1-2', 'i) phenyl independently substituted with one to three substituents that are selected from the group consisting of chloro, fluoro, bromo, cyano, trifluoromethyl, methyl, difluoromethoxy, and Calkoxy; provided that when phenyl of group (i) is substituted with a single substituent, that substituent is at ...

SUBSTITUTED IMIDAZOLES AS N-TYPE CALCIUM CHANNEL BLOCKERS

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: 2. The substituted imidazole of claim 1 , wherein the substituted imidazole is 4-[2-(2-Methoxyphenyl)-4-(2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethyltetrahydro-2H-pyran-4-yl)-1H-imidazol-1-yl]-benzonitrile claim 1 , and enantiomers claim 1 , diastereomers and pharmaceutically acceptable salts thereof.3. The substituted imidazole of claim 1 , wherein the substituted imidazole is 3-[1-(4-Chlorophenyl)-4-(2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethyltetrahydro-2H-pyran-4-yl)-1H-imidazol-2-yl]-2-methoxypyridine claim 1 , and enantiomers claim 1 , diastereomers and pharmaceutically acceptable salts thereof.4. The substituted imidazole of claim 1 , wherein the substituted imidazole is 1-(4-Chlorophenyl)-2-(2-methoxyphenyl)-4-(2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethyltetrahydro-2H-pyran-4-yl)-1H-imidazole claim 1 , and enantiomers claim 1 , diastereomers and pharmaceutically acceptable salts thereof.5. The substituted imidazole of claim 1 , wherein the substituted imidazole is 3-[1-(4-Chlorophenyl)-4-(2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethyltetrahydro-2H-pyran-4-yl)-1H-imidazol-2-yl]-2-ethoxypyridine claim 1 , and enantiomers claim 1 , diastereomers and pharmaceutically acceptable salts thereof.6. The substituted imidazole of claim 1 , wherein the substituted imidazole is 3-[5-Chloro-1-(4-fluorophenyl)-4-(2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethyltetrahydro-2H-pyran-4-yl)-1H-imidazol-2-yl]-2-methoxypyridine claim 1 , and enantiomers claim 1 , diastereomers and pharmaceutically acceptable salts thereof.7. The substituted imidazole of claim 1 , wherein the substituted imidazole is 4-[1-(4-Chlorophenyl)-2-(2-methoxyphenyl)-1H-imidazol-4-yl]-2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethyltetrahydro-2H-pyran-4-ol claim 1 , and enantiomers claim 1 , diastereomers and ...

COMPOUNDS FOR REGULATING FAK AND/OR SRC PATHWAYS

The present application provides novel optionally substituted fused pyridine and pyrimidine bicyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating FAK and/or Src activity by administering a therapeutically effective amount of one or more of the compounds to a subject. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the FAK and/or Src pathway. Advantageously, these compounds perform as dual FAK and/or Src inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer. 10. The compound according to claim 1 , wherein Ris H claim 1 , CH claim 1 , or F.11. The compound according to claim 1 , wherein Rand Rare claim 1 , independently claim 1 , H or CH.12. The compound according to claim 1 , wherein Rand Rare joined to form a cyclopropyl.13. The compound according to claim 1 , wherein Ris optionally substituted heteroaryl.14. The compound according to claim 13 , wherein Ris optionally substituted imidazole claim 13 , pyridine claim 13 , thiophene claim 13 , quinoline claim 13 , naphthalene claim 13 , benzothiazole claim 13 , or benzothiodiazole.15. The compound according to claim 14 , wherein Ris optionally substituted imidazole.16. The compound according to claim 15 , wherein Ris imidazole substituted with 1 or 2 C-Calkyl.17. The compound according to claim 16 , wherein Ris imidazole substituted with 1 or 2 CHgroups.18. The compound according to claim 14 , wherein Ris optionally substituted pyridine.19. The compound according to claim 18 , wherein Ris pyridine substituted with 1 or more C-Calkoxy claim 18 , N(C-Calkyl)OSO(C-Calkyl) claim 18 , N(C-Calkyl)(SO(C-Calkyl) claim 18 , or N(C-Calkyl)SO(C-Ccycloalkyl).20. The compound according to claim 19 , wherein ...

COMPOUNDS USEFUL AS CCR9 MODULATORS

The present invention relates to compounds useful as CCR9 modulators, to compositions containing them, to methods of making them, and to methods of using them. In particular, the present invention relates to compounds capable of modulating the function of the CCR9 receptor by acting as partial agonists, antagonists or inverse agonists. Such compounds may be useful to treat, prevent or ameliorate a disease or condition associated with CCR9 activation, including inflammatory and immune disorder diseases or conditions such as inflammatory bowel diseases (IBD). 135-. (canceled)37. The method of claim 36 , wherein Ris hydrogen.38. The method of claim 36 , wherein X is a direct bond.39. The method of claim 36 , wherein X is CH.40. The method of claim 36 , wherein Ris selected from optionally substituted aryl and optionally substituted heteroaryl.41. The method of claim 40 , wherein Ris selected from optionally substituted phenyl claim 40 , optionally substituted pyridyl claim 40 , optionally substituted thiophenyl claim 40 , optionally substituted pyrazolyl claim 40 , optionally substituted pyrimidinyl claim 40 , optionally substituted imidazolyl claim 40 , and optionally substituted thiazolyl.42. The method of claim 40 , wherein Ris selected from cyanophenyl claim 40 , acetylphenyl claim 40 , methoxy-phenyl claim 40 , pyridine N-oxide claim 40 , methyl-pyridine N-oxide claim 40 , methoxy-pyridine N-oxide claim 40 , ethoxy-pyridine N-oxide claim 40 , pyridyl claim 40 , methoxy-pyridyl claim 40 , ethoxy-pyridyl claim 40 , methyl-pyridyl claim 40 , cyano-pyridyl claim 40 , thiophenyl claim 40 , carboxy-thiophenyl claim 40 , carboxymethyl-thiophenyl claim 40 , pyrazolyl claim 40 , methyl-pyrazolyl claim 40 , imidazolyl claim 40 , and methyl-imidazolyl.43. The method of claim 36 , wherein each Ris independently selected from halo claim 36 , cyano claim 36 , Calkyl claim 36 , Calkoxy claim 36 , Chaloalkyl claim 36 , and cyclopropyl.44. The method of claim 43 , wherein each Ris ...

Substituted imidazoles as n-type calcium channel blockers

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R 1 , R 2 , R 3 , and G are defined herein.

Arylamino fused pyridines

Corticotropin releasing factor (CRF) antagonists of formula I; and their use in treating anxiety, depression, and other psychiatric and neurological disorders.

5-membered heterocyclic amides and related compounds

5-Membered heterocyclic amides and related compounds are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Biaryl piperazinyl-pyridine analogues

Biaryl piperazinyl -pyri dine analogues are provided, of the Formula (I): wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands, for receptor localization studies.

Substituted pyridin-2-ylamine analogues

Substituted pyridin-2-ylamine analogues are provided, of the formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Substituted heterocyclic diarylamine analogues

Substituted heterocyclic diarylamine analogues of Formula I are provided: wherein X, Y and Z are independently N or optionally substituted C, and other variables are as described in the specification. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Imidazopyrimidinyl and imidazopyri dinyl derivatives

Provided herein are compounds of the formula (I): as well as stereoisomers and pharmaceutically acceptable salts thereof. Such compounds are, because of their ability to antagonize CRF, useful in the treatment of a variety of disorders characterized by execssive CRF expression. These include, for example: affective disorder, anxiety, depression, headache, irritable bowel syndrome, post-traumatic stress disorder, supranuclear palsy, immune suppression, Alzheimer's disease, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, gastrointestinal diseases, anorexia nervosa or other feeding disorder, drug addiction, drug or alcohol withdrawal symptoms, inflammatory diseases, cardiovascular or heart-related diseases, fertility problems, human immunodeficiency virus infections, hemorrhagic stress, obesity, infertility, head and spinal cord traumas, epilepsy, stroke, ulcers, amyotrophic lateral sclerosis and hypoglycemia.

Compounds useful as ccr9 modulators

5-membered heterocyclic amides and related compounds

Disclosed is a compound of the formula I or a pharmaceutically acceptable salt or hydrate thereof, e.g. 1-(4-Amino-5-fluoropyrimidin-2-yl)-N-((1-(pyridin-3-yl)cyclohexyl)methyl)-3- (trifluoromethyl)-1H-pyrazole-4-carboxamide wherein Z represents pyrazole, thiazole, imidazole, oxazole or thiophene and the other substituents are defined in the specification for treating pain, osteoarthritis, rheumatoid arthritis, arthrosclerosis, glaucoma, irritable bowel syndrome, inflammatory bowel disease, cirrhosis, lupus, scleroderma, Alzheimer's disease, traumatic brain injury, asthma, chronic obstructive pulmonary disease, or interstitial fibrosis.

1h-imidazo 4,5-d]pyridazin-7-ones, 3h-imidazo 4,5-c]pyridin-4-ones and corresponding thiones as corticotropin releasing factor (crf) receptor ligands

Corticotropin releasing factor (CRF) antagonists of formula (I), and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.

Piperazinyl-pyridine analogues

Piperazinyl-pyridine analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals, and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Melanin concentrating hormone receptor ligands: substituted 1-benzyl-4-aryl piperazine analogues

Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).

2-phenoxy pyrimidinone analogues

2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Capsaicin receptor ligands

5-membered heterocyclic amides and related compounds

5-Membered heterocyclic amides and related compounds are provided, of the Formula: wherein variables are as described herein. Such compounds are liga nds that may be used to modulate specific receptor activity in vivo or in vi tro, and are particularly useful in the treatment of conditions associated w ith pathological receptor activation in humans, domesticated companion anima ls and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for usin g such ligands for receptor localization studies.

Melanin concentrating hormone receptor ligands

Disclosed are compounds of formula (I), and the pharmaceutically acceptable salts thereof wheren Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.

1h-imidazo[4,5-d]pyridazin-7-ones, 3h-imidazo[4,5-c]pyridin-4-ones and corresponding thiones as corticotropin releasing factor (crf) receptor ligands

Corticotropin releasing factor (CRF) antagonists of formula (I), and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.

Heteroaryl amide analogues

Compounds, pharmaceutical compositions, and methods of use are disclosed for heteroaryl amide analogues of formula Ia and/or Ib: . In certain embodiments, the heteroaryl amide analogues are agonists and/or ligands of dopamine receptors and may be useful, inter alia, for the treatment of a condition responsive to P2X7 receptor modulation, for example, pain, inflammation, a neurological or neurodegenerative disorder, a cardiovascular disorder, an ocular disorder or an immune system disorder.

2-phenoxy pyrimidinone analogues

2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity

Substituted imidazoles as N-type calcium channel blockers

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R

5-membered heterocyclic amides and related compounds

2-phenoxy pyrimidinone analogues

2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Substituted quinazolin-4-ylamine analogues as modulators of capsaicin

This invention relates generally to substituted quinazolin-4-ylamine analogues that are modulators of capsaicin receptors, and to the use of such compounds for treating conditions related to capsaicin receptor activation. The invention further relates to the use such compounds as probes for the detection and localization of capsaicin receptors.

Pyrrolo¬3,4-d|pyrimidines as corticotropin releasing factor (crf) antagonists

Corticotropin releasing factor (CRF) antagonists of Formula (I) or (II) and their use in treating anxiety, depression, and other psychiatric, neurologic al disorders as well as treatment of immunological, cardiovascular or heart- related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.

Substituted quinolin-4-ylamine analogues

Substituted quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

2-substituted quinazolin-4-ylamine analogues as capsaicin receptor modulators

Certain 2-substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone (crh) antagonists, useful for treating cns and stress-related disorders

Corticotropin releasing factor (CRF) antagonists of formula (I) and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.

Substituted imidazoles as N-type calcium channel blockers

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R

Imidazopyrimidines and imidazopyridines for the treatment of neurological disorders

Corticotropin releasing factor (CRF) antagonists of formula (I) and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heartrelated diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.

Substituted quinazolin-4-ylamine analogues as modulators of capsaicin

Predmetni pronalazak se generalno odnosi na supstituisane analoge hinazolin-4-ilamina koji su modulatori receptora kapsaicina, kao i na primenu takvih jedinjenja za lečenje stanja povezanih sa aktivacijom receptora kapsaicina. Pronalazak se dalje odnosi na primenu takvih jedinjenja kao proba za detekciju i lokalizaciju receptora kapsaicina.

Biaryl piperazinyl-pyridine analogues

Biaryl piperazinyl -pyri dine analogues are provided, of the Formula (I): wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands, for receptor localization studies.

Substituted pyrimidine compounds, compositions and medicinal applications thereof

The present disclosure relates to pyrimidine compounds of formula (I), their stereoisomers, tautomers, pharmaceutically acceptable salts, polymorphs, solvates, and hydrates thereof. The present disclosure also relates to process of preparation of these pyrimidine compounds, and to pharmaceutical compositions containing them. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders mediated by epidermal growth factor receptor (EGFR) family kinases.

4-amino (aza) quinoline derivatives as capsaicin receptor agonists

Capsaicin receptor agonists are provided. Such compounds are ligands that may be used to modulate VRl activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to capsaicin receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone (crh) antagonists, useful for treating cns and stress-related disorders

Corticotropin releasing factor (CRF) antagonists of formula (I) and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.

Aryl substituted purine analogues

Aryl-substituted purine analogues are provided, of the formula: (I) wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

5-membered heterocyclic amides and related compounds

Arylalkylamino-substituted quinazoline analogues

Arylalkylamino-substituted quinazoline analogues are provided, of the Formula wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Substituted quinazolin-4-ylamine analogues as modulators of capsaicin receptors

This invention relates generally to substituted quinazolin-4-ylamine analogues that are modulators of capsaicin receptors, and to the use of such compounds for treating conditions related to capsaicin receptor activation. The invention further relates to the use such compounds as probes for the detection and localization of capsaicin receptors.

2-phenoxy pyrimidinone analogues

2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Imidazopyrimidines and imidazopyridines for the treatment of neurological disorders

4-heterobicyclylamino-substituted quinazolines and analogues thereof as capsaicin-antagonists

Substituted bicyclic quinazolin-4-ylamine derivatives are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Benzene sulfonamides as CCR9 inhibitors

The present invention relates to compounds useful as CCR9 modulators, to compositions containing them, to methods of making them, and to methods of using them. In particular, the present invention relates to compounds capable of modulating the function of the CCR9 receptor by acting as partial agonists, antagonists or inverse agonists. Such compounds may be useful to treat, prevent or ameliorate a disease or condition associated with CCR9 activation, including inflammatory and immune disorder diseases or conditions such as inflammatory bowel diseases (IBD).

Arylamine-condensed pyridines and pyrimidines

Condensed naphthyridines as HIV reverse transcriptase inhibitors.

Spiro(isobenzofuran-1,4'-piperidin)-3-one und 3h- spiroisobenzofuran-1,4'-piperidine

Heterocyclyl-substituierte annellierte pyridine und pyrimidine als antagonisten des corticotropin freisetzenden hormons (crh), verwendbar für die behandlung von cns und stress

Substituted quinazolin-4-ylamine analogues as modulators of capsaicin.

Imidazo[1, 2-a] pyrazines for the treatment of irritable bowel syndrome

Provided herein are methods for treating a subject afflicted with irritable bowel syndrome comprising administering to the subject a therapeutically effective amount of a pharmaceutical composition that comprises a pharmaceutically acceptable carrier and a compound of the formula wherein: X is CHR 5 , NR 5 , O, S, S(O) n or a single bond, wherein n is equal to 0, 1 or 2; D is aryl or heteroaryl attached through an unsaturated carbon atom and wherein said aryl or heteroaryl is optionally substituted at any available position with from 1-5 of A 1 , A 2 , A 3 , A 4 and A 5 ; and R 2 is C 1-4 alkyl or C 3-8 cycloalkyl, each of which is optionally substituted with from 1-3 hydroxy, halogen or C 1-4 alkoxy, or wherein when X is a bond, R 2 is CN, CF 3 , or C 2 F 5 .

Kondenzált piridinek és pirimidinek aril-amino-származékai, eljárás előállításukra, valamint e vegyületeket tartalmazó gyógyászati készítmények, továbbá e vegyületek alkalmazása

A találmány szerinti kőndenzált piridinek és pirimidinek új aril-aminő-származékainak (I) és (II) általánős képletében aszűbsztitűensek főbb jelentései: R1 jelentése egymástól függetlenülhidrőgén- vagy halőgénatőm, CN vagy SH képletű csőpőrt, X, Y jelentéseN-atőm vagy -CR1 általánős képletű csőpőrt, Z jelentése O-atőm vgy NR3vagy S(O)n általánős képletű csőpőrt, G jelentése O- vagy S-atőm, Arjelentése adőtt esetben helyettesített karbő- vagy heterőciklűsőscsőpőrt, R4 hidrőgénatőm vagy adőtt esetben szűbsztitűált alkil-,allkil- vagy prőpargilcsőpőrt és R13 jelentése alkil-, halőgén-alkil-,alkőxi-alkil-, ciklőalkil-, ciklőalkil-alkil-, aril-, aralkil-,heterőaril-, heterőaril-alkil-csőpőrt. A találmány tárgyköréheztartőznak a fenti vegyületek előállítása, a hatóanyagként e vegyületettartalmazó gyógyászati készítmények tővábbá a vegyületek alkamazása. ŕ

Condensed naphthyridines as hiv reverse transcriptase inhibitors

用作hiv逆轉錄酶抑制劑的稠合1，5-二氮雜萘

Tricyklické sloučeniny použitelné jako inhibitory HIV reverzní transkriptasy

Substituted biaryl quinolin-4-ylamine analogues

Substituted biaryl quinolin-4-ylamine analogues of Formula I are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Substituted biaryl quinolin-4-ylamine analogues

Substituted biaryl quinolin-4-ylamine analogues of Formula I are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Substituted imidazoles as N-type calcium channel blockers

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R 1 , R 2 , R 3 , and G are defined herein.

Compounds useful as CCR9 modulators

The present invention relates to compounds useful as CCR9 modulators, to compositions containing them, to methods of making them, and to methods of using them. In particular, the present invention relates to compounds capable of modulating the function of the CCR9 receptor by acting as partial agonists, antagonists or inverse agonists. Such compounds may be useful to treat, prevent or ameliorate a disease or condition associated with CCR9 activation, including inflammatory and immune disorder diseases or conditions such as inflammatory bowel diseases (IBD).

Substituted imidazoles as N-type calcium channel blockers

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R 1 , R 2 , R 3 , and G are defined herein.