发明名称 NITROGEN-CONTAINING BICYCLIC AROMATIC HETEROCYCLIC COMPOUND
摘要 [Problem] On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided.;[Means for Solution] It was found that a nitrogen-containing bicyclic heterocyclic compound has the excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has the cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.
申请公布号 US2015126488(A1) 申请公布日期 2015.05.07
申请号 US201314394373 申请日期 2013.04.17
申请人 ASTELLAS PHARMA INC. 发明人 Nakajima Yutaka;Imada Sunao;Takasuna Yuji;Aoyama Naohiro;Nigawara Takahiro;Shirakami Shohei;Shirai Fumiyuki;Sato Junji;Nakanishi Keita;Kubo Kaori
分类号 C07D487/04;C07D473/00 主分类号 C07D487/04
代理机构 代理人
主权项 1. A compound of formula (I) or a salt thereof: wherein X is CH or N; Y is CH, C-halogen, or N; W is —O— or —S(O)n—; L1 is a bond, -lower alkylene-, —O-lower alkylene-, —NH-lower alkylene-, or —C(O)-lower alkylene-; R1 is (i) lower alkyl which is optionally substituted with one or more substituents selected from the group consisting of a halogen, —OH, —O-lower alkyl, —NH2, —NH-(lower alkyl), —N(lower alkyl)2, —C(O)—NH2, —C(O)—NH-lower alkyl, —C(O)—N(lower alkyl)2, —C(O)—NH-nonaromatic heterocycle which is optionally substituted, —C(O)—N(lower alkyl))-nonaromatic heterocycle which is optionally substituted, a nonaromatic heterocycle which is optionally substituted, and —C(O)-nonaromatic heterocycle which is optionally substituted; (ii) nonaromatic heterocycle which is optionally substituted; or (iii) H; R2 is lower alkyl which is optionally substituted with a halogen, a halogen, or H; R3 is lower alkyl which is optionally substituted with a halogen, a halogen, or —CN; each R4 is independently lower alkyl which is optionally substituted with a halogen, —OH, —CN, or H; R5 is lower alkyl which is optionally substituted with a substituent selected from the group consisting of —OH, a halogen, —NH2, —NH-(lower alkyl), and —N(lower alkyl)2, —O-(lower alkyl which is optionally substituted with a halogen), C3-8 cycloalkyl which is optionally substituted, an aromatic heterocycle which is optionally substituted, or a nonaromatic heterocycle which is optionally substituted; and each n is independently an integer of from 0 to 2.
地址 Chuo-ku, Tokyo JP