- HETEROARYL INHIBITORS OF PAD4
-
The present invention provides compounds useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.
- -
-
Paragraph 00167-00168
(2017/09/15)
-
- NOVEL CRYSTALLINE POLYMORPHS OF PYRIDINE DERIVATIVE AND METHOD FOR PRODUCING THE SAME
-
Disclosed are crystals of 2-(5-chloropyridin-3-yl)-1-(2,5-dichlorobenzyl)-4-methyl-1H-imidazole-5-carboxylic acid useful as therapeutic or prophylactic agents for gout, hyperuricemia, and the like, and a method for producing the crystals.
- -
-
Paragraph 0060-0061
(2017/06/20)
-
- PYRAZINE DERIVATIVE
-
Provided is a novel pyrazine derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof, or a solvate thereof which is useful for treating or preventing diseases in which URAT1 is involved, including gout, hyperurice
- -
-
Paragraph 0083; 0084
(2017/04/04)
-
- PYRIDINE DERIVATIVE
-
Provided is a pyridine derivative represented by formula (I), a prodrug thereof, a pharmaceutically acceptable salt of the pyridine derivative or the prodrug, or a solvate of the pyridine derivative, the prodrug or the pharmaceutically acceptable salt, wh
- -
-
Paragraph 0126; 0127; 0128
(2015/10/28)
-
- IMIDAZOLE DERIVATIVE
-
PROBLEM TO BE SOLVED: To provide a novel pyrazine derivative that is useful as a therapeutic agent or preventive agent for diseases associated with URAT1, such as gout, hyperuricemia, hypertension, kidney diseases such as interstitial nephritis, diabetes,
- -
-
Paragraph 0140; 0141; 0142
(2016/10/08)
-
- Discovery of 6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3- ylmethylamines, a novel class of corticotropin-releasing factor receptor type 1 (CRF1R) antagonists
-
A novel series of [6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a] imidazol-3-ylmethyl]-dialkylamines was discovered as potent CRF1R antagonists. The optimization of binding affinity in the series by the parallel reaction approach is discus
- Zuev, Dmitry,Vrudhula, Vivekananda M.,Michne, Jodi A.,Dasgupta, Bireshwar,Pin, Sokhom S.,Huang, Xiaohua Stella,Wu, Dedong,Gao, Qi,Zhang, Jie,Taber, Matthew T.,MacOr, John E.,Dubowchik, Gene M.
-
scheme or table
p. 3669 - 3674
(2010/09/04)
-
- (2-Aryl-5-methylimidazol-4-ylcarbonyl)guanidines and (2-aryl-5-methyloxazol-4-ylcarbonyl)guanidines as NHE-1 inhibitors
-
A series of (2-aryl-5-methylimidazol-4-ylcarbonyl)guanidines and (2-aryl-5-methyloxazol-4-ylcarbonyl)guanidines were synthesized and evaluated as NHE-1 inhibitors. The structure-activity relationships well matched those of furan derivatives, which were previously investigated. The (2,5-disubstituted)phenyl compounds showed better activities than the other analogues in both imidazole and oxazole compounds. Especially, 2-(2,5-dichlorophenyl)imidazole 52, and 2-(2-methoxy-5-chlorophenyl)imidazole 54 compounds exhibited potent cardioprotective efficacy both in vitro and in vivo as well as high NHE-1 inhibitory activities.
- Lee, Sunkyung,Yi, Kyu Yang,Youn, Sung Jun,Lee, Byung Ho,Yoo, Sung-eun
-
scheme or table
p. 1329 - 1331
(2009/10/02)
-
- ORGANIC COMPOUNDS
-
The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
- -
-
Page/Page column 19
(2009/07/03)
-
- 4-METHYLIMIDAZOL-5-YLCARBONYLGUANIDINE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD, AND PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF THE ISCHEMIC HEART DISEASES CONTAINING THE SAME AS AN ACTIVE INGREDIENT
-
Disclosed are novel 4-methylimidazol-5- ylcarbonylguanidine derivatives, pharmaceutically acceptable salts thereof, preparation methods thereof, and pharmaceutical composition for the prevention and treatment of ischemic heart diseases, comprising the same as an active ingredient. Having potent inhibitory activity against NHE-I and excellent protective effects on the heart against ischemia/reperfusion, the novel 4-methylimidazol-5- ylcarbonylguanidine derivatives can be used for the prophylaxis and treatment of ischemic cardiac diseases such as myocardiac infarction, arrhythmia, and angina pectoris and can serve as a cardioprotective agent applicable for coronary reperfusion therapy with coronary artery bypass, percutaneous transluminal coronary angioplasty, and/or thrombolytics for myocardiac infarction.
- -
-
Page/Page column 27
(2008/12/07)
-