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Cyclopenta [d] hydroxylated pyrimidines as AKT protein kinase inhibitors
专利权人:
Array Biopharma, Inc.;Genentech, Inc.
发明人:
Mitchell, Ian,Blake, James,Xu, Rui,Kallan, Nicholas,Xiao, Dengming,Spencer, Keith,Bencsik, Josef,Liang, Jun,Safina, Brian,Zhang, Birong,Chabot, Christine,Do, Steven,Wallace, Eli,Banka, Anna,Schlachter
申请号:
ES11166123
公开号:
ES2554228T3
申请日:
2007.07.05
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
Compound of formula I: ** Formula ** and tautomers, separate enantiomers, separated diastereoisomers, solvates and salts thereof, wherein: R1 is H, Me, Et, vinyl, CF3, CHF2 or CH2F; R2 is H; R5 is H, Me, Et or CF3; A is selected from formulas 2 and 4 ** Formula ** G is phenyl optionally substituted with 1 to 4 R9 groups or a 5-6 membered heteroaryl optionally substituted with a halogen; R6 and R7 are independently H, OCH3, (C3-C6 cycloalkyl) - (CH2), (C3-C6 cycloalkyl) - (CH2CH2), V- (CH2) 0-1 in which V is a 5-6 heteroaryl members, W- (CH2) 1-2 wherein W is phenyl optionally substituted with F, Cl, Br, I, OMe, CF3 or Me, C3-C6 cycloalkyl optionally substituted with C1-C3 alkyl or O (C1- alkyl C3), hydroxy- (C3-C6 cycloalkyl), fluoro- (C3-C6 cycloalkyl), CH (CH3) CH (OH) phenyl, 4-6 membered heterocycle optionally substituted with F, OH, C1-C3 alkyl, cyclopropylmethyl or C (>; = O) (C1-C3 alkyl), or C1-C6 alkyl optionally substituted with one or more groups independently selected from OH, oxo, O (C1-C6 alkyl), CN, F, NH2, NH (alkyl C1-C6), N (C1-C6 alkyl) 2, cyclopropyl, phenyl, imidazolyl, piperidinyl, pyrrolidinyl, morpholinyl, tetrahydrofuranoyl, oxetanyl or tetrahydropyranyl, or R6 and R7 together with the nitrogen to which they are attached form a heterocyclic ring of 4 -7 members optionally substituted with one or more selected groups independently between OH, halogen, oxo, CF3, CH2CF3, CH2CH2OH, O (C1-C3 alkyl), C (>; = O) CH3, NH2, NHMe, N (Me) 2, S (O) 2CH3, cyclopropylmethyl and C1 alkyl -C3; Rc and Rd are H or Me, or Rc and Rd together with the atom to which they are attached form a cyclopropyl ring; R8 is H, Me, F or OH, or R8 and R6 together with the atoms to which they are attached form a 5-6 membered heterocyclic ring having one or two ring nitrogen atoms; each R9 is independently halogen, C1-C6 alkyl, C3-C6 cycloalkyl, O (C1-C6 alkyl), CF3, OCF3, S (C1-C6 alkyl), CN, OCH2-phenyl, CH2O-phenyl, NH2, NH ( C1-C6 alkyl), N (C1-C6 alkyl) 2, piperidine,
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