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Hydroxylated and Methoxylated Cyclopenta [D] Pyrimidines as Act Protein Kinase Inhibitors
专利权人:
ЭРРЭЙ БИОФАРМА ИНК. (US);ДЖЕНЕНТЕК, ИНК. (US)
发明人:
МИТЧЕЛЛ Ян С. (US),БЛЭЙК Джеймс Ф. (US),КСУ Руи (US),КАЛЛАН Николас К. (US),КСИАО Денгминг (US),СПЕНСЕР Кит Ли (US),БЕНКСИК Йозеф Р. (US),ЛИАНГ Дзун (US),САФИНА Брайан (US),ЧЖАНГ Биронг (US),ЧАБОТ Кри
申请号:
RU2012155606/04
公开号:
RU2012155606A
申请日:
2012.12.20
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
1. A pharmaceutical composition comprising a compound selected from formula I: its tautomers, separated enantiomers, separated diastereomers, solvates, metabolites, and salts; and a second drug; an oral dosage form containing a composition selected from formula I, tautomers, resolved enantiomers, resolved diastereomers, solvates, metabolites, and salts thereof; where in formula I: R is H, Me, Et, vinyl, CF, CHF or CHF; R is H or Me; R represents H, Me, Et or CF; A represents the structure:; G represents phenyl optionally substituted with one to four R groups or a 5-6 membered heteroaryl optionally substituted with halogen; R and R independently represent H; OCH; (C-Cycloalkyl) - (CH); (C-Cycloalkyl) - (CHCH); V- (CH), where V is a 5-6 membered heteroaryl; W- (CH), where W is phenyl optionally substituted with F, Cl, Br, I, OMe, CF or Me; C-C-cycloalkyl optionally substituted with C-C1-6alkyl or O (C-C1-6alkyl); hydroxy- (C-C-cycloalkyl); fluoro- (C-C-cycloalkyl); CH (CH) CH (OH) phenyl; A 4-6 membered heterocycle optionally substituted with F, OH, C-C1-6 alkyl, cyclopropylmethyl or C (= O) (C1-6 alkyl); or CC-alkyl, optionally substituted by one or more groups independently selected from OH, oxo, O (CC-alkyl), CN, F, NH, NHCC-C-alkyl), N (CC-alkyl), cyclopropyl, phenyl, imidazolyl, piperidinyl, pyrrolidinyl, morpholinyl, tetrahydrofuranyl, oxetanyl or tetrahydropyranyl; or R and R together with the nitrogen atom to which they are attached form a 4-7 membered heterocyclic ring, optionally substituted with one or more groups independently selected from OH, halogen, oxo , CF, CHCF, CHCHOH, O (C-Calkyl), C (= O) CH, NH, NHMe, N (M1. Фармацевтическая композиция, содержащая соединение, выбранное из формулы I:его таутомеров, разделенных энантиомеров, разделенных диастереомеров, сольватов, метаболитов, и солей; и второе лекарственное средство; илипероральная лекарственная форма, содержащая композицию, выбранную из формулы I, таутомеров, разделенных энантиомеров, разделенных
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