| 主权项 |
1. A compound of formula (I) or a pharmaceutically acceptable salt thereof:wherein:
Y is CH or N; R1 is:
—OH,—OC1-6alkyl,—OC1-6alkyl-het1,—OC1-6alkyl-OH,—OC1-6alkyl-NRaRb,—O-het1,—OC1-6alkylCO2H,—OC1-6alkylC(═O)-het1,—O(CH2)1-6OC(═O)CH2NRaRb,—OC1-6alkyl-C1-6alkoxy,—OC1-6alkyl-C1-6alkoxy-C1-6alkoxy,—OC(O)C1-6alkyl,—OC(O)NRaRb,—OC1-6alkyl-S-het1,—OC1-6alkyl-phosphate,a phosphate group,—(CH2)1-6-het1,pyridinyl, orthiazolyl;wherein
said alkyl is optionally substituted with 1 or 2 fluoro substituents,said phosphate group is optionally substituted with 1, 2 or 3 C1-6alkyl;said het1 is:a) aryl selected from phenyl or napthyl optionally substituted with 1 or 2 substituents selected from —OH, C1-6alkyl, or halo;b) heteroaryl selected from 5- and 6-membered aromatic rings having 1, 2 or 3 heteroatoms independently selected from N, O and S, wherein said heteroaryl is attached through a ring atom selected from C or N and optionally substituted with 1 or 2 substituents independently selected from C1-6alkyl and —OH; orc) heterocycle selected from 4-7 membered monocyclic or 6-10 membered polycyclic bridged, linearly fused or spirocyclic saturated or unsaturated non-aromatic rings having 1, 2, 3 or 4 heteroatoms independently selected from N, O and S, wherein said heterocycle is attached through a ring atom selected from C or N and optionally substituted with 1 or 2 substituents independently selected from C1-6alkyl, oxo, —(CH2)mF, Boc, —(CH2)mCF3, —(CH2)mOCF3, —OH, —NRaRb, —C1-6alkoxy, —(CH2)mSO2CH3, aryl, —C1-6alkoxy-C1-6alkyl, —C1-6alkyl-C3-6alkoxy optionally substituted with CF3, cyano, C(═O)NH2, C3-6cycloalkyl, —C1-6alkyl-C3-6cycloalkyl, —COOC1-6alkyl, —C1-6alkyl-SO2C1-6alkyl, and benzimidazolyl wherein the benzimidazolyl is optionally substituted with F;Ra and Rb are independently selected from H; C1-6 alkyl; t-Boc; aryl; C3-6cycloalkyl optionally substituted with 1 or 2 fluoro; C1-6alkoxy-C1-6alkyl; tetrahydropyranyl; C1-6 alkyl-OH; C1-6alkyl-arylA; C1-6alkyl-C(OH)-arylA; C1-6alkyl-imidazolyl optionally substituted with methyl, C1-6alkyl-benzimidazolyl optionally substituted with methyl; C1-6alkyl-pyrazolyl; C1-6alkyl-dihydrotriazole optionally substituted with oxo; or C1-6alkyl-pyrrolidinyl optionally substituted with oxo;wherein
m is 0 or 1 to 4;said arylA is phenyl, naphthalenyl, tetrahydronapthalenyl, or 7-10 membered fused bicyclic ring structure wherein at least one of the rings is aromatic and is optionally substituted with 2-OH; said tetrahydropyranyl is optionally substituted with 1 oxo; R2 is C1-6alkyl, C2-6alkenyl, C3-C6cycloalkyl or NRcRd;
wherein
the C3-6cycloalkyl is optionally substituted with C1-6alkyl optionally substituted with —OH, morpholinyl, C1-6alkoxy, C1-6alkoxy-C1-6alkoxy, C1-6alkoxyphenyl, or C1-6alkenyl;Rc and Rd are independently H or C1-6alkyl, or may be taken together, with the N to which they are attached, to form a 4-7-membered monocyclic ring; R3 is C1-6alkyl, C2-6alkenyl, C3-C6cycloalkyl, CF2 or CF3; R4 is C1-8 alkyl, C3-8 cycloalkyl, C1-8 alkyl-C3-8 cycloalkyl, adamantyl, dihydroindenyl, or a 4-8 membered heterocycloalkyl having 1 or 2 heteroatoms selected from N, O, or S, wherein R4 is optionally substituted with one or two substituents independently selected from (C1-C6)alkyl, halo, and —O(C1-C6)alkyl; or R3 and R4 together form heptene; Z is C or N; R5 is H or C1-6alkyl; or R5 is absent when Z is N; W is a bond, O or NR; R is H or C1-6alkyl; X is absent or is halo, CF3, —OCHF2, —OCH2F, —OCD2F, —OCDF2, C1-C6alkyl, C1-6alkoxy, aryl, heteroaryl, or —O(CH2)1-6NRaRb; A is absent, O or N; B is (CH2)m; and n is 1-4. |
