| 主权项 |
1. A compound of formula (I)Wherein
R1 is hydrogen, halogen, or C1-6alkyl; R2 is hydrogen, halogen, or C1-6alkyl; R3 is hydrogen, halogen, or C1-6alkyl; R4 is hydrogen, or C1-6alkyl; R5 is hydrogen, or halogen; R6 is hydrogen, halogen, hydroxy, C1-6alkoxy, carboxy, morpholinyl, or 4-C0-6alkylpiperazin-1-yl; R7 is hydrogen, halogen, C1-6alkyl, C1-6alkoxy, C1-6alkylaminocarbonyl, diC1-6alkylaminocarbonyl, C1-6alkylsulfonyl, phenoxy, or hydroxy(CH2)2-6—O—; R8 is hydrogen, halogen, or C1-6alkoxy; R9 is hydrogen, C1-6alkyl, or ═O; R10 is hydrogen, or ═O, provided that R9 and R10 are not ═O simultaneously; A is nitrogen, or —C—R11, wherein R11 is hydrogen, halogen, C1-6alkyl, cycloalkyl, C1-6alkoxy, trifluoromethyl, trifluoromethoxy, pyridinyloxy, C1-6alkoxy(CH2)1-6—O—, difluoromethoxy, cyano, nitro, amino, vinyl, acetylenyl, aminocarbonyl, hydroxy(CH2)2-6—O—, C1-6alkylsulfinyl, C1-6alkylsulfonyl, hydroxy(CH2)1-6, deuteratedC1-6alkyl, carboxyl, C1-6alkoxycarbonyl, hydroxy, difluoromethyl, —CH(hydroxy) C1-6alkyl, or C1-6alkylsulfanyl; X is —CH2—, —O—, —NH—, —CF2—, —C(C1-6alkyl)(OH)—, —S—, —C(═O)—, —C(═NOC0-6alkyl)-, —S(═O)—, —S(O2)— or —S(═O)(NH)—; Y is —CH—, or nitrogen; Q is hydrogen; halogen; C1-6alkyl, unsubstituted or once or twice substituted by amino or hydroxy, provided that di-substitution is not on the same carbon; amino(CH2)2-6aminosulfonyl; 2-amino-4,5-dihydro-1,3-oxazol-4-yl(CH2)1-6; carboxy(CH2)1-6; phenylsulfonyl; piperidin-4-yl-carbonyl; 1H-pyrazol-3-yl; pyrrolidin-3-yloxy; piperidin-4-yloxy; amino(CH2)2-6—O—; or NR12R13, wherein one of R12 and R13 is hydrogen, C1-6alkyl, or hydroxy(CH2)2-6, and the other one is {1-[amino(CH2)0-6]-3,3-difluorocyclobutyl}(CH2)1-6; guanidino(CH2)2-6; (S—C1-6alkylsulfonimidoyl)(CH2)2-6; 2-oxa-6-aza-spiro[3.4]oct-8-yl; {3-[amino(CH2)0-6]tetrahydrofuran-3-yl}(CH2)1-6; 3-aminomethyl-1,1-dioxidothietan-3-ylmethyl; 3-amino-1,1-dioxidothietan-3-ylmethyl; 3-(aminomethyl)thietan-3-ylmethyl;(1,1-dioxidothiomorpholin-4-yl)ethyl; C0-6alkyl(oxetanyl)N(CH2)2-6; 4,5-dihydro-1H-imidazol-2-yl; amino(CH2)2-6—O—(CH2)2-6; amino(CH2)2-10; amino(CH2)1-6difluoromethyl(CH2)1-6; amino(CH2)1-6difluoromethyldifluoromethyl(CH2)1-6; amino(CH2)1-6fluoromethyl(CH2)1-6; amino(CH2)1-6oxetanyl(CH2)0-6; amino(CH2)0-6oxetanyl(CH2)1-6; amino(CH2)2-6sulfanyl(CH2)2-6; amino(CH2)2-6sulfonyl(CH2)2-6; amino(CH2)0-6carbonyl(CH2)0-6; aminocycloalkyl(CH2)0-6; 2-aminodihydrooxazol-4-yl(CH2)1-6; 2-aminodihydrooxazol-5-yl(CH2)1-6; (2-amino-5-methyl-4,5-dihydro-1,3-oxazol-5-yl)methyl; aminophenyl; 4-aminotetrahydropyran-4-yl(CH2)1-6; azetidin-2-yl(CH2)1-6; azetidin-3-yl(CH2)0-6; azetidinylcarbonyl; C1-6alkoxy(CH2)2-6; C1-6alkoxy(CH2)2-6amino(CH2)2-6; C1-6alkyl; C1-6alkylamino(CH2)2-6; C1-6alkylaminocarbonyl(CH2)0-6; C1-6alkylaminooxetanyl(CH2)1-6; C1-6alkylcarbonyl; C1-6alkylcarbonylamino(CH2)2-6; C1-6alkylcarbonylamino(CH2)1-6oxetanyl(CH2)0-6; C1-6alkylsulfinyl(CH2)2-6; C1-6alkylsulfonyl; carboxy(CH2)1-6; cyano(CH2)1-6; diC1-6alkylamino(CH2)2-6;diC1-6alkylaminocarbonyl; difluoromethyl(CH2)1-6amino(CH2)2-6; hydrogen; hydroxy(CH2)2-10; hydroxy(CH2)2-6amino(CH2)2-6; hydroxy(CH2)1-6carbonyl; hydroxy(CH2)0-6oxetanyl(CH2)1-6; hydroxy(CH2)1-6oxetanyl(CH2)0-6; hydroxycycloalkyl; isoxazolyl; morpholin-2-yl(CH2)1-6; morpholin-4-yl(CH2)2-6; oxetanyl(CH2)0-6; N-oxetanylpyrrolidin-3-yl; oxo-pyrrolidinylcarbonyl; phenylaminocarbonyl; phenyl(CH2)0-6aminooxetanyl(CH2)1-6; phenylcarbonyl; piperazinyl(CH2)2-6; piperidin-1-yl(CH2)2-6; piperidin-2-yl(CH2)1-6; piperidin-3-yl(CH2)0-6; piperidin-4-yl(CH2)0-6; piperidinylcarbonyl; pyrazinylcarbonyl; pyrazol-3-yl; pyridazinylcarbonyl; pyridinyl(CH2)0-6carbonyl; pyridinylamino(CH2)2-6; pyrrolidin-3-yl, unsubstituted or 4-substituted by halogen; pyrrolidin-4-yl, unsubstituted or 3-substituted by hydroxy or C1-6alkoxy; pyrrolidin-2-yl(CH2)1-6; pyrrolidinylcarbonyl; tetrahydrofuran-3-yl; tetrahydropyran-4-yl; tetrazolyl(CH2)2-6; trifluoromethylcarbonylamino(CH2)1-6oxetanyl; trifluoromethylsulfonyl; wherein R14 is hydrogen, C1-6alkyl or hydroxy(CH2)1-6; R15 is hydroxy, C1-6alkyl, hydroxy(CH2)1-6 or amino; and R16 is C1-6alkyl, trifluoromethyl, hydroxy(CH2)1-6, amino(CH2)1-6, aminocarboxy or carboxy(CH2)1-6; wherein R17 is hydrogen, C1-6alkyl or hydroxy(CH2)1-6; R18 is hydroxy(CH2)1-6 or C1-6alkyl; R19 is hydroxy(CH2)1-6, amino(CH2)1-6, carboxy or aminocarboxy(CH2)0-6; or wherein R20 is hydrogen or C1-6alkyl; R21 is C1-6alkyl; R22 is C1-6alkoxy or amino; R12 and R13, with the nitrogen atom to which they are attached, may form a pyrrolidinyl, piperazinyl, piperidinyl, morpholinyl, azetidinyl, diazepanyl or oxopyrrolidinyl ring; which may be unsubstituted, once or twice substituted by a group selected from halogen, C1-6alkyl, C1-6alkoxy, gemdimethyl, amino, aminocarbonyl, hydroxy, oxetanylamino, C1-6alkylpiperazinyl, and amino(CH2)1-6; R12 and R13, with the nitrogen atom to which they are attached may form a bridge ring or a spiral ring selected from 2-oxa-6-aza-spiro[3.4]octan-6-yl, 2-oxa-5,7-diazaspiro[3.4]octan-6-one-5-yl, (4aS,7aR)-hexahydropyrrolo[3,4-b][1,4]oxazin-6(2H)-yl, 4,5,6,6a-tetrahydro-3aH-pyrrolo[3,4-d][1,3]oxazol-5-yl, 2-aza -bicyclo[2.1.1]hexan-2-yl, and 3-aza-bicyclo[3.1.0]hexan-3-yl; which may be unsubstituted or further substituted by amino; and pharmaceutically acceptable salt and stereoisomers thereof. |
