12-12-2013 дата публикации
Номер: US20130331372A1
Автор:
Adamson Samantha E.,
Chen Yi-Heng,
Dong Guizhen,
Hunt Julianne,
Kallashi Florida,
LI HONG,
LU Zhijian,
Ondeyka Debra L.,
Qian Xiaoxia,
Sinclair Peter,
Smith Cameron,
Sun Wanying,
Sweis Ramzi,
Thompson Christopher F.,
Vachal Petr,
Zhao Kake
Принадлежит:
Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compound of Formula I, Ais a substituted phenyl group or indanyl group. Formula (I). 2. The compound of claim 1 , wherein{'sup': '1', 'sub': '1-3', 'Ris H or Calkyl;'}{'sup': 'a', 'sub': 3', '3', '3', '3, 'Each Ris independently CF, —OCF, CH, —OCH, halogen, —CN, or cyclopropyl which is optionally substituted with 1-3 halogens;'}{'sup': 'c1', 'sub': 3', '3', '3', '3, 'Each Ris independently CH, CF, —OCH, —OCFor halogen;'}{'sup': 'b', 'sub': 1-3', '1-3', '3-6', '1-3', '1-3', '3-6, 'Ris H, Calkyl, —OCalkyl, —OCcycloalkyl, or halogen, wherein Calkyl, —OCalkyl, and —OCcycloalkyl are optionally substituted with 1-3 halogens;'}{'sup': 'b1', 'sub': 3', '3, 'Each Ris independently halogen, CF, or CH; and'}X is:{'sub': 2-4', '5-6', '1-3', '3', '1-4', '1-4', '1-2, '(a) (i) Cl, (ii) —Calkyl, (iii) —Ccycloalkyl-Y or —Calkyl-Y wherein Y is —CN, —OH, or —OCH, or (iv) -phenyl which is substituted with 1-3 groups which are independently halogen, —CN, —OH, —Calkyl, —OCalkyl, or —C(═O)Calkyl, wherein alkyl and cycloalkyl in all occurrences are optionally substituted with 1-3 halogens;'}{'sup': 1', '1', '2', '3, 'sub': 2', '2', '1-4, '(b) D, wherein Dis —COH, —COCalkyl, or —C(═O)NRR;'}{'sub': '1-4', 'sup': '1', '(c) —Calkyl-D, wherein alkyl is optionally substituted with 1-3 F;'}{'sub': 3-6', '3', '3, 'sup': '1', '(d) —Ccycloalkyl-D, wherein cycloalkyl is optionally substituted with 1-2 groups which are independently —CH, CF, or halogen;'}{'sub': 3-6', '2', '3', '3, 'sup': '1', '(e) —Ccycloalkyl-CH-D, wherein cycloalkyl is optionally substituted with 1-2 groups which are independently —CH, CF, or halogen;'}{'sup': '1', 'sub': 3', '3', '3', '3, '(f) -phenyl-D, wherein phenyl is optionally substituted with 1-3 substituent groups which are ...
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