Heterocyclic compound
    8.
    发明授权
    Heterocyclic compound 有权
    杂环化合物

    公开(公告)号:US09156837B2

    公开(公告)日:2015-10-13

    申请号:US14235992

    申请日:2012-07-27

    摘要: A heterocyclic compound having an RORγt inhibitory activity, which is a compound of formula (I) or a salt thereof is provided. The compound has ring A, which is an optionally substituted cyclic group and is bound to a pyrazole ring though Q. Q is a bond, optionally substituted C1-10 alkylene, optionally substituted C2-10 alkenylene, or optionally substituted C2-10 alkynylene. R1 is a substituent. Ring B is a thiazole ring, an isothiazole ring or a dihydrothiazole ring, each of which is optionally further substituted by a substituent in addition to R2. R2 is an optionally substituted cyclyl-carbonyl-C1-6 alkyl group, an optionally substituted aminocarbonyl-C1-6 alkyl group, an optionally substituted cyclyl-C1-6 alkyl group, an optionally substituted cyclyl-C1-6 alkylamino-carbonyl group, an optionally substituted aminocarbonyl-C2-6 alkenyl group, an optionally substituted C1-6 alkylcarbonylamino-C1-6 alkyl group, an optionally substituted cyclyl-aminocarbonyl group, an optionally substituted cyclyl-carbonyl group or an optionally substituted non-aromatic heterocyclic group.

    摘要翻译: 提供具有RORγt抑制活性的杂环化合物,其为式(I)化合物或其盐。 该化合物具有环A,其为任选取代的环状基团,并且通过Q键合至吡唑环。Q为键,任选取代的C 1-10亚烷基,任选取代的C 2-10亚烯基或任选取代的C 2-10亚炔基。 R1是取代基。 环B是噻唑环,异噻唑环或二氢噻唑环,除了R2之外,它们各自任选进一步被取代基取代。 R 2是任选取代的环羰基-C 1-6烷基,任选取代的氨基羰基-C 1-6烷基,任选取代的环C 1-6烷基,任选取代的环C 1-6烷基氨基羰基, 任选取代的氨基羰基-C 2-6烯基,任选取代的C 1-6烷基羰基氨基-C 1-6烷基,任选取代的环 - 氨基羰基,任选取代的环羰基或任选取代的非芳族杂环基。

    Triazole derivative and use thereof
    9.
    发明授权
    Triazole derivative and use thereof 失效
    三唑衍生物及其用途

    公开(公告)号:US07803822B2

    公开(公告)日:2010-09-28

    申请号:US11887936

    申请日:2006-04-06

    IPC分类号: A61K31/41 C07D249/00

    摘要: The present invention relates to a thrombin receptor antagonist containing a compound represented by the formula (I) wherein R1a, R1b and R2 are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or an optionally substituted alkoxy, R3 is a group represented by the formula —NHCOR4, —NHSO2R5, —NHCON(R6a)(R6b), —NHCOOR7 or —CONHR8 wherein R4, R5, R6a, R6b, R7 and R8 are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group and the like), ring A is monocyclic aromatic ring optionally further having substituent(s), R1a and R1b are optionally bonded to each other to form an optionally substituted nitrogen-containing non-aromatic heterocycle, or a salt thereof or a prodrug thereof. The thrombin receptor antagonist of the present invention has a thrombin receptor (particularly PAR-1) antagonistic action and is useful for the prophylaxis or treatment of PAR-1 mediated pathological condition or disease.

    摘要翻译: 本发明涉及含有式(I)表示的化合物的凝血酶受体拮抗剂,其中R1a,R1b和R2各自为氢原子,任选取代的烃基,任选取代的杂环基或任选取代的烷氧基,R 3 是由式-NHCOR4,-NHSO2R5,-NHCON(R6a)(R6b),-NHCOOR7或-CONHR8表示的基团,其中R4,R5,R6a,R6b,R7和R8各自为氢原子,任选取代的烃基 ,任选取代的杂环基等),环A是任选进一步具有取代基的单环芳环,R 1a和R 1b任选地彼此键合以形成任选取代的含氮非芳族杂环或盐 或其前药。 本发明的凝血酶受体拮抗剂具有凝血酶受体(特别是PAR-1)拮抗作用,可用于预防或治疗PAR-1介导的病理状态或疾病。

    HETEROCYCLIC COMPOUND
    10.
    发明申请
    HETEROCYCLIC COMPOUND 有权
    杂环化合物

    公开(公告)号:US20140163001A1

    公开(公告)日:2014-06-12

    申请号:US14235992

    申请日:2012-07-27

    摘要: Provided is a heterocyclic compound having an RORγt inhibitory activity. A compound represented by the formula (I): wherein ring A is an optionally substituted cyclic group, Q is a bond, optionally substituted C1-10 alkylene, optionally substituted C2-10 alkenylene, or optionally substituted C2-10 alkynylene, R1 is a substituent, ring B is a thiazole ring, an isothiazole ring or a dihydrothiazole ring, each of which is optionally further substituted by a substituent in addition to R2, and R2 is an optionally substituted cyclyl-carbonyl-C1-6 alkyl group, an optionally substituted aminocarbonyl-C1-6 alkyl group, an optionally substituted cyclyl-C1-6 alkyl group, an optionally substituted cyclyl-C1-6 alkylamino-carbonyl group, an optionally substituted aminocarbonyl-C2-6 alkenyl group, an optionally substituted C1-6 alkylcarbonylamino-C1-6 alkyl group, an optionally substituted cyclyl-aminocarbonyl group, an optionally substituted cyclyl-carbonyl group or an optionally substituted non-aromatic heterocyclic group, or a salt thereof.

    摘要翻译: 提供具有RORγt抑制活性的杂环化合物。 由式(I)表示的化合物:其中环A是任选取代的环状基团,Q是键,任选取代的C 1-10亚烷基,任选取代的C 2-10亚烯基或任选取代的C 2-10亚炔基,R 1是 取代基,环B是噻唑环,异噻唑环或二氢噻唑环,其中R 2独立地任选被取代基任意地进一步被R 2取代,R 2是任选取代的环羰基-C 1-6烷基,任选地 取代的氨基羰基-C 1-6烷基,任选取代的环烷基-C 1-6烷基,任选取代的环基-C 1-6烷基氨基 - 羰基,任选取代的氨基羰基-C 2-6链烯基,任选取代的C 1-6 烷基羰基氨基-C 1-6烷基,任选取代的环 - 氨基羰基,任选取代的环羰基或任选取代的非芳族杂环基,或其盐。