Patent classifications
C07D231/54
Pyrazolyl substituted carbonic acid derivatives as modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto
Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH) and related disorders; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD). ##STR00001##
BTK inhibitor
- Xuehai Wang ,
- Chengde Wu ,
- Yong XU ,
- Chunli Shen ,
- Li'e Li ,
- Guoping Hu ,
- Yang Yue ,
- Jian Li ,
- Diliang Guo ,
- Nengyang Shi ,
- Lu Huang ,
- Shuhui Chen ,
- Ronghua Tu ,
- Zhongwen Yang ,
- Xuwen Zhang ,
- Qiang Xiao ,
- Hua Tian ,
- Yanping Yu ,
- Hailiang Chen ,
- Wenjie Sun ,
- Zhenyu He ,
- Jie Shen ,
- Jing Yang ,
- Jing Tang ,
- Wen Zhou ,
- Jing Yu ,
- Yi Zhang ,
- Quan Liu
Provided are a series of BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or prodrug thereof represented by formula (I), (II), (III) or (IV). ##STR00001##
BTK inhibitor
- Xuehai Wang ,
- Chengde Wu ,
- Yong XU ,
- Chunli Shen ,
- Li'e Li ,
- Guoping Hu ,
- Yang Yue ,
- Jian Li ,
- Diliang Guo ,
- Nengyang Shi ,
- Lu Huang ,
- Shuhui Chen ,
- Ronghua Tu ,
- Zhongwen Yang ,
- Xuwen Zhang ,
- Qiang Xiao ,
- Hua Tian ,
- Yanping Yu ,
- Hailiang Chen ,
- Wenjie Sun ,
- Zhenyu He ,
- Jie Shen ,
- Jing Yang ,
- Jing Tang ,
- Wen Zhou ,
- Jing Yu ,
- Yi Zhang ,
- Quan Liu
Provided are a series of BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or prodrug thereof represented by formula (I), (II), (III) or (IV). ##STR00001##
Tricyclic rho kinase inhibitors
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same. ##STR00001##
Tricyclic rho kinase inhibitors
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same. ##STR00001##
SPIROHEPTANE SALICYLAMIDES AND RELATED COMPOUNDS AS INHIBITORS OF ROCK
The present invention provides compounds of Formula (I):
##STR00001##
or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
SPIROHEPTANE SALICYLAMIDES AND RELATED COMPOUNDS AS INHIBITORS OF ROCK
The present invention provides compounds of Formula (I):
##STR00001##
or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE
Provided are IDO inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases such as chronic viral infection, chronic bacterial infections, cancer, sepsis or a neurological disorder.
##STR00001##
Spiroheptane salicylamides and related compounds as inhibitors of rock
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same. ##STR00001##
Benzene, Pyridine, and Pyridazine Derivatives
Disclosed are compounds and pharmaceutically acceptable salts of Formula I
##STR00001##
wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, n, Q.sub.1, Q.sub.2, Q.sub.3, Y, and X.sub.1-X.sub.4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.