发明名称 DIAZOLE LACTAMS
摘要 Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
申请公布号 US2014171420(A1) 申请公布日期 2014.06.19
申请号 US201314099541 申请日期 2013.12.06
申请人 ChemoCentryx, Inc. 发明人 Chen Xi;Fan Pingchen;Li Yandong;Powers Jay P.;Malathong Viengkham;Punna Sreenivas;Tanaka Hiroko;Zhang Penglie;Dragoli Dean
分类号 A61K31/55;A61K31/4196;A61K31/4155;A61K31/4178;C07D401/14;A61K45/06;C07D405/14;C07D471/04;A61K31/437;C07D487/04;A61K31/519;C07D403/14;A61K31/454 主分类号 A61K31/55
代理机构 代理人
主权项 1. A compound represented by the structure (I): wherein n is an integer of from 0 to 3; each A is independently selected from the group consisting of N and CH; X and Z are each independently selected from the group consisting (i) monocyclic or fused-bicyclic aryl and heteroaryl, wherein the heteroaryl group has from 1-4 heteroatoms as ring members selected from N, O and S;(ii) monocyclic four-, five-, six- or seven-membered ring selected from the group consisting of cycloalkane, and heterocycloalkane, wherein the heterocycloalkane rings have from 1-3 heteroatoms as ring members selected from N, O and S;wherein each of the rings in (i) and (ii) are optionally substituted with from 1 to 5 substituents selected from halogen, CN, C1-8 alkyl, C3-8 cycloalkyl, C2-8 alkenyl, C2-8 alkynyl, C1-8 haloalkyl, C1-8 hydroxyalkyl, —ORa, —CO2Ra, —SO2Ra, —NRaRb, —CONRaRb, aryl, 5- or 6-membered heteroaryl, and 3-, 4-, 5- or 6-membered heterocycloalkane wherein the heteroatoms present as ring vertices of the heteroaryl and heterocycloalkane rings are selected from N, O and S, and wherein the alkyl, cycloalkyl, aryl, heteroaryl and hetereocycloalkane portions of the substituents are optionally further substituted with 1-3 Ra; and optionally, two substituents on adjacent ring vertices are connected to form an additional 5- or 6-membered ring which is saturated, unsaturated or aromatic having ring vertices selected from C, O, N and S;R3 is a member selected from the group consisting of H, halogen, CN, C1-8 alkyl, C3-8 cycloalkyl, C2-8 alkenyl, C2-8 alkynyl, C1-8 haloalkyl, C1-8 hydroxyalkyl, —ORa, —CO2Ra, —NRaRb, —CONRaRb, aryl, 5- or 6-membered heteroaryl, and 3-, 4-, 5- or 6-membered heterocycloalkane wherein the heteroatoms present as ring vertices of the heteroaryl and heterocycloalkane rings are selected from N, O and S, and wherein the alkyl, cycloalkyl, aryl, heteroaryl and hetereocycloalkane portions of R3 are optionally further substituted with 1-3 Ra;R4 is a member selected from the group consisting of H, —ORa and C1-8 alkyl optionally substituted with —ORa;R9 is a member selected from the group consisting of H and C1-8 alkyl optionally substituted with —ORa;each Ra and Rb is independently selected from the group consisting of hydrogen, hydroxyl, halogen, cyano, C1-8 alkyl, C1-8 alkoxy, C1-8 haloalkyl, C3-6 cycloalkyl, C3-6 cycloalkylalkyl, amino, C1-8 alkylamino, di C1-8 alkylamino, carboxamide, carboxy C1-4 alkyl ester, carboxylic acid, and —SO2—C1-8 alkyl,or any salts, solvates, hydrates, N-oxides or rotamers thereof.
地址 Mountain View CA US