发明名称 COMPOUNDS AND THERAPEUTIC USES THEREOF
摘要 The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and other complications associated with these diseases and disorders.
申请公布号 US2015353538(A1) 申请公布日期 2015.12.10
申请号 US201514589939 申请日期 2015.01.05
申请人 Willardsen J. Adam;Lockman Jeffrey W.;Murphy Brett R.;Judd Weston R.;Kim In Chul;Kim Se-Ho;Zigar Daniel Feodore;Yager Kraig M.;Fleischer Tracey C.;Terry-Lorenzo Ryan T.;Boniface J. Jay;Parker Daniel P.;McAlexander Ian A.;Bursavich Matthew Gregory;Dastrup David D. 发明人 Willardsen J. Adam;Lockman Jeffrey W.;Murphy Brett R.;Judd Weston R.;Kim In Chul;Kim Se-Ho;Zigar Daniel Feodore;Yager Kraig M.;Fleischer Tracey C.;Terry-Lorenzo Ryan T.;Boniface J. Jay;Parker Daniel P.;McAlexander Ian A.;Bursavich Matthew Gregory;Dastrup David D.
分类号 C07D471/04;C07D213/61;C07D213/65;C07D401/12;C07D235/06;C07D213/71;C07D409/12;C07D213/75;C07D413/12;C07D213/64;C07D213/73;C07D333/22;C07D417/12;C07D213/68;C07D233/64;C07D307/48;C07D237/20;C07D213/53 主分类号 C07D471/04
代理机构 代理人
主权项 1. A compound having a structure according to Formula IIIband pharmaceutically acceptable salts and solvates thereof;wherein: Y is 3-pyridinyl or 4-pyridinyl, wherein any ring carbon is optionally independently substituted with halo, C1-5 alkyl, nitro, cyano, C1-5 alkoxy, C-amido, N-amido, C-carboxy, O-carboxy, sulfonamide, amino, hydroxyl, mercapto, alkylthio, sulfonyl, or sulfinyl; Y2 is —OCH2—, —SCH2—, —N(R)CH2—, —N(R)C(═O)—, —C(═O)N(R)—, —S(═O)2CH2—, —S(═O)CH2—, —CH2O—, —CH2CH2O—, —CH2S—, —CH2N(R)—, —CH2S(═O)2—, —CH2S(═O)—, —C(═O)O—, —OC(═O)—, —SO2N(R)—, —N(R)SO2—, ethylene, propylene, n-butylene, —O—C1-4 alkylene-N(R)C(═O)—, —O—C1-4 alkylene-C(═O)N(R)—, —N(R)C(═O)—C1-4 alkylene-O—, —C(═O)N(R)—C1-4 alkylene-O—, —C1-4 alkylene-S(═O)2—, —C1-4 alkylene-S(═O)—, —S(═O)2—C1-4 alkylene-, —S(═O)—C1-4 alkylene-, —C1-4 alkylene-SO2N(R)—, —C1-4 alkylene-N(R)SO2—, —SO2N(R)—C1-4 alkylene-, —N(R)SO2—C1-4 alkylene-, —C1-4 alkylene-O—C1-4 alkylene-, —O—C1-4 alkylene-, —C1-4 alkylene-O—, —S—C1-4 alkylene-, —C1-4 alkylene-S—, —C1-4 alkylene-S—C1-4 alkylene-, —N(R)—C1-4 alkylene-, —C1-4 alkylene-N(R)—, —C1-4 alkylene-N(R)—C1-4 alkylene-, —C1-4 alkylene-C(═O)—O—C1-4 alkylene-, —C1-4 alkylene-O—C(═O)—C1-4 alkylene-, —C1-4 alkylene-C(═O)—N(R)—C1-4 alkylene-, —C1-4 alkylene-N(R)—C(═O)—C1-4 alkylene-, —C(═O)—N(R)—C1-4 alkylene-SO2N(R)—, or —N(R)—C(═O)—C1-4 alkylene-SO2N(R)—; wherein for the purpose of Y2, R is H, C1-5 alkyl, C1-5 alkenyl, C1-5 alkynyl, or is methylene or ethylene that forms a 5- or 6-membered heterocycle with a carbon atom of Y3; Y3 is aryl or heteroaryl, wherein any ring carbon is optionally independently substituted with halo, C1-5 alkyl, nitro, cyano, trihalomethyl, C1-5 alkoxy, C-amido, N-amido, sulfonamide, amino, aminosulfonyl, hydroxyl, mercapto, alkylthio, sulfonyl, or sulfinyl, wherein C1-5 alkyl, C1-5 alkoxy, C-amido, N-amido, amino, and alkylthio are each optionally substituted with heterocyclo, cycloalkyl, or amino; Y4 is optionally present, and when present is aryl, heteroaryl, carbocycle, or heterocycle, wherein any ring atom is optionally independently substituted with halo, C1-5 alkyl, nitro, cyano, trihalomethyl, C1-5 alkoxy, C-amido, N-amido, sulfonamide, amino, aminosulfonyl, hydroxyl, mercapto, alkylthio, sulfonyl, sulfinyl, wherein C1-5 alkyl, C1-5 alkoxy, C-amido, N-amido, amino, and alkylthio are each optionally substituted with heterocyclo, cycloalkyl, or amino; o, p, and q are each independently 0, 1, or 2; any methylene group of the o, p, and q regions and Y2 is optionally independently substituted with C1-4 alkyl, halo, C1-4 haloalkyl, or C3 or C4 cycloalkyl; R6 is absent; wherein S, T, U, and V are carbon; with the proviso that when p is 0, Y2 is —C(═O)N(H)— or —OC(H)2C(═O)N(H)—, and Y3 is phenyl or pyridinyl, then either Y4 is present or any substituent on Y3 is not —C(═O)NH2; and with the proviso that the compound is NOT 1-(6-methoxy-3-pyridyl)-3-[[4-(3-pyridylmethoxy)phenyl]methyl]urea, ethyl 3-(pyridin-3-yl)-4-({4-[(3-{[(pyridin-3-ylmethyl)carbamoyl]amino}benzyl)oxy]phenyl}sulfonyl)butanoate; 4-({4-(3-[(3-{[(pyridin-3-ylmethyl)carbamoyl]amino}benzyl)oxy]phenyl}sulfonyl)-3-[4-(trifluoromethyl)phenyl]butanoic acid; 3-phenyl-4-({4-[(3-{[(pyridin-3-ylmethyl)carbamoyl]amino}benzyl)oxy]phenyl}sulfonyl)butanoic acid; 3-(4-chloro-3-fluorophenyl)-4-[(4-{[3-{[(pyridin-3-ylmethyl)carbamoyl]amino}-5-(trifluoromethyl)benzyl]oxy}phenyl)sulfonyl]butanoic acid; 3-phenyl-4-[(4-{[3-{[(pyridin-3-ylmethyl)carbamoyl]amino}-5-(trifluoromethyl)benzyl]oxy}phenyl) sulfonyl]butanoic acid; 3-(pyridin-3-yl)-4-({4-[(3-{[(pyridin-3-ylmethyl)carbamoyl]amino}benzyl)oxy]phenyl}sulfonyl)butanoic acid; 4-({4-[(4-fluoro-3-{[(pyridin-3-ylmethyl)carbamoyl]amino}benzyl)oxy]phenyl}sulfonyl)-3-(pyridin-3-yl)butanoic acid; Benzoic acid, 2-hydroxy-4-[[(3-pyridinylamino)carbonyl]amino]-, phenyl ester, Benzamide, N-(3-amino-4-pyridinyl)-4-[[[[(3-pyridinylmethyl)amino]carbonyl]amino]methyl]-, Benzamide, N-(2-amino-3-pyridinyl)-4-[[[[(3-pyridinylmethyl)amino]carbonyl]amino]methyl]-, Benzamide, N-(2-amino-5-fluorophenyl)-4-[[[[(3-pyridinylmethyl)amino]carbonyl]amino]methyl]-, Benzamide, N-(2-hydroxyphenyl)-4-[[[[(3-pyridinylmethyl)amino]carbonyl]amino]methyl]-, Benzamide, N-(2-amino-5-chlorophenyl)-4-[[[[(3-pyridinylmethyl)amino]carbonyl]amino]methyl]-, Benzamide, 2-chloro-5-nitro-N-[4-[[(4-pyridinylamino)carbonyl]amino]phenyl]-, Benzamide, N-[4-[[[3-(diethylamino)propyl]amino]carbonyl]phenyl]-4-[[(3-pyridinylamino)carbonyl]amino]-, Benzamide, N-(2-aminophenyl)-4-[[[(3-pyridinylamino)carbonyl]amino]methyl]-, Benzamide, N-(2-aminophenyl)-4-[2-[[[(3-pyridinylmethyl)amino]carbonyl]amino]ethyl]-, Benzamide, N-(2-aminophenyl)-4-[[[[(3-pyridinylmethyl)amino]carbonyl]amino]methyl]-, Benzoic acid, 2-hydroxy-4-[[(3-pyridinylamino)carbonyl]amino]-, phenyl ester, 1,3-Benzenedicarboxamide, N,N′-bis[3-(diethylamino)propyl]-5-[[4-[[(4-pyridinylamino)carbonyl]amino]benzoyl]amino]-, Urea, N-[4-(phenylmethoxy)phenyl]-N′-[2-(3-pyridinyl)ethyl]-, Urea, N-[4-(phenylmethoxy)phenyl]-N′-3-pyridinyl-, Urea, N-(6-methyl-3-pyridinyl)-N′-[2-[2-(phenylmethoxy)phenyl]ethyl]-, Urea, N-(6-methoxy-3-pyridinyl)-N′-[4-(phenylmethoxy)phenyl]-, N4-[[4-[[[(2,6-dichloro-4-pyridinyl)amino]carbonyl]amino]phenyl]methyl]-N6-[(3-methoxyphenyl)methyl]-4,6-pyrimidinedicarboxamide, Benzenesulfonamide, 4-fluoro-N-[4-[[(3-pyridinylamino)carbonyl]amino]phenyl]-, or Hexanamide, 2-[2,4-bis(1,1-dimethylpropyl)phenoxy]-N-[2-chloro-4-[[[(2-chloro-3-pyridinyl)amino]carbonyl]amino]-5-hydroxyphenyl]-.
地址 Draper UT US
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