Substituted heterocyclic compounds with CXCR3 antagonist activity

作者: Neng-Yang Shih , Stuart B. Rosenblum , Bandarpalle B. Shankar , Joseph A. Kozlowski , Seong Heon Kim

DOI:

关键词: StereochemistryAlkoxy groupImidazoleArylTriazoleRing (chemistry)MoietyTetrazoleChemistryAlkyl

摘要: A compound having the general structure shown in Formula 1: or a salt, solvate ester of pharmaceutically acceptable thereof, wherein: G is selected from group consisting H, hydroxyl, alkoxy, R2R1N -, R2R1X-C (R145) (R1S) - and heteroaryl heterocyclenyl ring containing 5-membered at least one -C = N- moiety as part said being dihydroimidazole, imidazole, dihydrooxazole, oxazole, dihydrooxadiazole, oxadiazole, triazole tetrazole, wherein can be both (i) unsubstituted, (ii) optionally independently substituted on more carbon atoms with substituents R910, nitrogen R8, R8 R9 identical different; L N CR4 OZ; R1 R2 are absent present, if present each alkyl, alkenyl, carbonyl, cycloalkyl, cycloalkenyl, alkylaryl, arylalkyl, aryl, amino, alkylamino, amidinyl , carboxamido, cyano, urea, -NoCH, NCN, (CH2) qOH, qOR31, qNH2, qNHR31, qN (R31) 2, ( CH2) qC (= O) NHR31, qSO2R31, qNHSO2R31, qSO2NHR31, S) (H) -N -S (O) 2 C -alkyl, 2N S (alkyl) 2aryl, NH2, -heteroaryl, heterocyclyl, heterocyclenyl; alternatively when X N, taken together form (NH2) 2; R3 -H, -Cl -CH3 R4 moieties same different, aralkyl, -CN, CF3, haloalkyl, halogen, hydroxyalkyl, CH- (R31), (R30) -OR30, -SO2 R31; R6 H O, heteroaryl, heterocyclyl qNSO2R31 QSO) 2NHR31; -NH2 CH2CH3 R10 CH3, -CH2 CH2 CH3 R11 residues R12 -H D phenyl pyridinyl, unsubstituted 1-5 R20 40; halogen amino. R21 alkynyl, alquiltiocarboxi, alkylheteroaryl, alkylthio, alkylsulfinyl, alkylsulfonyl, alkoxycarbonyl, aminoalkyl, amidinyl, aralkyl aralkenyl, aralkoxy, aralkoxycarbonyl, aralkylthio, aroyl, aryloxy, formyl, guanidinyl, heteroalkyl, heterocyclenyl, hydroxamate, nitro, trifluoromethoxy, (CH2 ) q-NH2, qNSO2R31, qS2NHR31, -alquinilC 2OR31, R30, NR30) NHR30, NOH) NOR31) OR 30, R31, -NHC OR31, NCN) SO2 (R30), R30) -OC -SR30, -SO2N -OSO2 OSi 3; Y c

参考文章(13)
Gopinadhan N. Anilkumar, Lisa Guise Zawacki, Joseph A. Kozlowski, Qingbei Zeng, Michael K.C. Wong, Seong Heon Kim, Wensheng Yu, De-Yi Yang, Neng-Yang Shih, Brian F. Mcguinness, Stuart B. Rosenblum, Douglas W. Hobbs, Heteroaryl substituted pyrazinyl-piperazine-piperidines with CXCR3 antagonist activity ,(2006)
Neng-Yang Shih, Stuart B. Rosenblum, Douglas W. Hobbs, Brian F. Mcguinness, Joseph A. Kozlowski, Heterocyclic substituted pyridine compounds with cxcr3 antagonist activity ,(2007)
Joseph A. Kozlowski, Qingbei Zeng, Neng-Yang Shih, Stuart B. Rosenblum, Douglas W. Hobbs, Brian F. Mcguinness, Heterocyclic compounds with cxcr3 antagonist activity ,(2007)
Brian Springthorpe, Matthew Perry, Christopher Luckhurst, Novel piperidine derivatives for use in the treatment of chemokine mediated disease states ,(2003)
Brian AstraZeneca R D Charnwood Springthorpe, Matthew AstraZeneca R D Charnwood Perry, Christopher AstraZeneca R D Charnwood Luckhurst, Piperidine derivatives for the treatment of chemokine or h1 mediated disease state ,(2004)
Youheng Shu, Brian F. Mcguinness, Yuefei Shao, Michael K. C. Wong, Stuart B. Rosenblum, Wensheng Yu, Douglas W. Hobbs, Joseph A. Kozlowski, Amine-linked pyridyl and phenyl substituted piperazine-piperidines with cxcr3 antagonist activity ,(2006)
Gopinadhan N. Anilkumar, Joseph A. Kozlowski, Qingbei Zeng, Stuart B. Rosenblum, Douglas W. Hobbs, Brian F. Mcguinness, Novel heterocyclic substituted pyridine or phenyl compounds with cxcr3 antagonist activity ,(2006)
Gopinadhan N. Anilkumar, Lisa Guise Zawacki, Guizhen Dong, Qingbei Zeng, Neng-Yang Shih, Yuefei Shao, Michael K.C. Wong, Stuart B. Rosenblum, John J. Baldwin, Wensheng Yu, Bandarpalle B. Shankar, Douglas W. Hobbs, Yueheng Jiang, Brian F. Mcguinness, Joseph A. Kozlowski, Seong Heon Kim, Pyrazinyl substituted piperazine-piperidines with cxcr3 antagonist activity ,(2006)
Gopinadhan N. Anilkumar, Qingbei Zeng, Brian F. McGuinness, Yuefei Shao, Michael K. C. Wong, Stuart B. Rosenblum, Douglas W. Hobbs, Joseph A. Kozlowski, Seong Heon Kim, Heterocyclic substituted piperazines with cxcr3 antagonist activity ,(2006)
Joseph A. Kozlowski, Brian F. Mcguiness, Neng-Yang Shih, Stuart B. Rosenblum, Douglas W. Hobbs, Heterocyclic substituted piperazine compounds with cxcr3 antagonist activity ,(2007)