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    Heterocyclic compound
    5.
    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

    申请人： Satoshi Yamamoto ,  Junya Shirai ,  Atsuko Ochida ,  Yoshiyuki Fukase ,  Yoshihide Tomata ,  Ayumu Sato ,  Shotaro Miura ,  Kazuko Yonemori ,  Ryokichi Koyama

    发明人： Satoshi Yamamoto ,  Junya Shirai ,  Atsuko Ochida ,  Yoshiyuki Fukase ,  Yoshihide Tomata ,  Ayumu Sato ,  Shotaro Miura ,  Kazuko Yonemori ,  Ryokichi Koyama

    IPC分类号： C07D277/30 ,  C07D277/56 ,  C07D211/90 ,  C07D417/12 ,  C07D471/04 ,  C07D401/12 ,  C07D277/24 ,  C07D401/04 ,  C07D417/04 ,  C07D417/14 ,  C07D491/107

    CPC分类号： C07D471/04 ,  C07D417/04 ,  C07D417/14 ,  C07D491/107

    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。

    Process for Production of Cyclopentenenitrile Derivatives
    6.
    发明申请
    Process for Production of Cyclopentenenitrile Derivatives 审中-公开
    环戊烯腈衍生物生产工艺

    公开(公告)号：US20070219389A1

    公开(公告)日：2007-09-20

    申请号：US10592298

    申请日：2005-03-07

    申请人： Masaaki Miyashita ,  Keiji Tanino ,  Yoshihide Tomata ,  Yasuhiro Shiina

    发明人： Masaaki Miyashita ,  Keiji Tanino ,  Yoshihide Tomata ,  Yasuhiro Shiina

    IPC分类号： C07C253/30

    CPC分类号： C07C253/30 ,  C07C255/47 ,  C07C2602/24 ,  C07C2602/26 ,  C12P13/002 ,  C12P41/00

    摘要： [Problems] To provide a process for the synthesis of cyclopentenenitrile derivatives through conjugate addition of a nitrile derivative to an α,β-unsaturated ketone whereby cyclopentenenitrile derivatives, particularly those capable of optical resolution, can be obtained in high yield without expensive reagents or compounds in a decreased number of steps. [Means for Solving Problems] A novel process for the production of cyclopentenenitrile derivatives in high yield, which comprises trapping a compound obtained by conjugate addition of a 4-alkoxy-3-butenenitrile which may have alkyl or allyl at the α-position (e.g., 4-methoxy-3-butenenitrile) to an α,β-unsaturated ketone as an enol ester with acetic anhydride, chlorocarbonic ester, or the like and treating the enol ester with a strong acid or the like to form a five-membered ring.

    摘要翻译： [问题]提供通过将腈衍生物偶联加成到α，β-不饱和酮中合成环戊烯腈衍生物的方法，由此可以高产率获得环戊烯腈衍生物，特别是能够进行光学拆分的衍生物，而不需要昂贵的试剂或化合物 减少步数。 [解决问题的手段]以高产率生产环戊烯腈衍生物的新方法，其包括捕获通过在α-位上共轭加成可以具有烷基或烯丙基的4-烷氧基-3-丁烯腈获得的化合物（例如 ，4-甲氧基-3-丁烯腈）与乙酸酐，氯代碳酸酯等作为烯醇酯的α，β-不饱和酮，用强酸等处理烯醇酯以形成五元环 。

    HETEROCYCLIC COMPOUND
    7.
    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

    申请人： Satoshi Yamamoto ,  Junya Shirai ,  Atsuko Ochida ,  Yoshiyuki Fukase ,  Yoshihide Tomata ,  Ayumu Sato ,  Shotaro Miura ,  Kazuko Yonemori ,  Ryokichi Koyama

    发明人： Satoshi Yamamoto ,  Junya Shirai ,  Atsuko Ochida ,  Yoshiyuki Fukase ,  Yoshihide Tomata ,  Ayumu Sato ,  Shotaro Miura ,  Kazuko Yonemori ,  Ryokichi Koyama

    IPC分类号： C07D491/107 ,  C07D417/04 ,  C07D471/04 ,  C07D417/14

    CPC分类号： C07D471/04 ,  C07D417/04 ,  C07D417/14 ,  C07D491/107

    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。