发明名称 INDOLINE COMPOUNDS FOR TREATMENT AND/OR PREVENTION OF INFLAMMATION DISEASES
摘要 The invention is based on the discovery that 1-arylsulfonyl-5-(N-hydroxyacrylamide)indolines and 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles has great potential as a novel agent to be used in the treatment of inflammation-associated diseases, particularly, inflammatory arthritis and fibrosis.
申请公布号 US2015368195(A1) 申请公布日期 2015.12.24
申请号 US201414310587 申请日期 2014.06.20
申请人 Taipei Medical University 发明人 Liou Jing-Ping;Lin Chien-Huang;Pan Shiow-Lin;Yang Chia-Ron;Teng Che-Ming
分类号 C07D209/08 主分类号 C07D209/08
代理机构 代理人
主权项 1. A method for inhibiting cytokine release from a cell or a subject, comprising administering an effective amount of the compound having formula (I) or a pharmaceutically acceptable salt, prodrug or solvate thereof to the cell or the subject: wherein is a single bond or a double bond; R1 is SO2Ra, wherein Ra is aryl unsubstituted or substituted by 1 to 3 substituent selected from the group consisting of: —OC1-10alkyl, halogen, —NO2, —NH2, —OH, —C1-6alkyl, —C2-10alkenyl, —C2-10alkynyl, —C3-10cycloalkyl, —C1-10cycloalkenyl, 6 to 10 membered aryl or 6 to 10 membered heteroaryl; R2, R3, R5 and R6 are each independently H, —OC1-10alkyl, halogen, —NO2, —NH2, —OH, —C1-10alkyl, —C2-10alkenyl or —C2-10alkynyl; and R4 is H, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, aryl, 5 to 14 membered heteroaryl, C3-10cycloalkyl, C5-10cycloalkenyl, C3-14heterocycloC1-10alkyl, C5-14heterocyclo C2-10alkenyl, halo, cyano, nitro, ORb, SRb, S(O)Rb, CH═CH—C(O)NRcRd, NHC(O)—CH═CH—C(O)Rb, NHC(O)—CH═CH—C(O)NRcRd, SO2NRcRd, OC(O)Rb, C(O)NRcRd, NRcRd, NHC(O)Rb, NHC(O)NRcRd, or NHC(S)Rc, in which each of Rb, Rc, and Rd, independently, is H, hydroxy, C1-10alkoxy, C6-10aryloxy, C5-14heteroaryloxy, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, C6-10aryl, C5-14heteroaryl, C3-10cycloalkyl, C5-10cycloalkenyl, C3-14heterocycloC1-6alkyl, or C5-14heterocycloC2-10alkenyl.
地址 Taipei TW