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    NITROGEN-CONTAINING HETEROCYCLIC COMPOUND
    1.
    发明申请
    NITROGEN-CONTAINING HETEROCYCLIC COMPOUND 审中-公开
    含氮杂环化合物

    公开(公告)号：US20090281097A1

    公开(公告)日：2009-11-12

    申请号：US12296874

    申请日：2007-04-13

    申请人： Kohji Fukatsu ,  Makoto Kamata ,  Tohru Yamashita ,  Satoshi Endo

    发明人： Kohji Fukatsu ,  Makoto Kamata ,  Tohru Yamashita ,  Satoshi Endo

    IPC分类号： A61K31/5377 ,  C07D413/14 ,  A61K31/4535 ,  C07D409/06 ,  C07D409/14 ,  A61K31/4545 ,  A61P3/10

    CPC分类号： C07D401/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

    摘要： The object of the present invention is to provide a compound having an ACC inhibitory action, which is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and has superior properties such as efficacy, duration of activity, specificity, low toxicity and the like.The present invention provides a compound represented by the following formula wherein ring M is a 5- or 6-membered aromatic ring; W is C or N; K is an optionally substituted methylene group or an optionally substituted imino group; R is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted hydroxy group or an optionally substituted heterocyclic group; T and U are independently a hydrogen atom or a substituent or, T and U form, together with ring M, an optionally substituted bicyclic ring; D and G are independently a carbonyl group or a sulfonyl group; ring P is an optionally substituted piperidine or an optionally substituted piperazine; B is CH or N; ring Q is an optionally substituted monocyclic ring; A is C, CH or N; and J is an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted amino group, provided that when the W moiety of ring M is ═N— or —N═, then U should be absent, or a salt thereof.

    摘要翻译： 本发明的目的是提供具有ACC抑制作用的化合物，其可用于预防或治疗肥胖，糖尿病，高血压，高脂血症，心力衰竭，糖尿病并发症，代谢综合征，肌肉减少症等，并且具有 优异的性质如功效，活性持续时间，特异性，低毒性等。 本发明提供由下式表示的化合物，其中环M为5或6元芳环; W是C或N; K是任选取代的亚甲基或任选取代的亚氨基; R是氢原子，任选取代的烃基，任选取代的羟基或任选取代的杂环基; T和U独立地是氢原子或取代基，或者T和U与环M一起形成任选取代的双环; D和G独立地为羰基或磺酰基; 环P是任选取代的哌啶或任选取代的哌嗪; B是CH或N; 环Q是任选取代的单环; A是C，CH或N; 并且J是任选取代的烃基，任选取代的杂环基或任选取代的氨基，条件是当环M的W部分为-N-或-N-时，则U不应为其或其盐。

    SPIRO-RING COMPOUND
    3.
    发明申请
    SPIRO-RING COMPOUND 审中-公开
    螺环化合物

    公开(公告)号：US20100093777A1

    公开(公告)日：2010-04-15

    申请号：US12449084

    申请日：2008-01-24

    申请人： Kohji Fukatsu ,  Makoto Kamata ,  Tohru Yamashita

    发明人： Kohji Fukatsu ,  Makoto Kamata ,  Tohru Yamashita

    IPC分类号： A61K31/4545 ,  C07D471/10 ,  C07D498/10 ,  C07D513/10 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P35/00

    CPC分类号： C07D519/00 ,  C07D495/04 ,  C07D498/10 ,  C07F7/1804

    摘要： The present invention aims to provide a compound having an acetyl-CoA carboxylase (ACC) inhibitory action, which is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy.The present invention provides a compound represented by the formula (I): wherein R1 is a hydrogen atom or a substituent; ring P is an optionally substituted 6-membered nitrogen-containing aromatic heterocycle; ring Q is an optionally further substituted 5- to 7-membered nitrogen-containing non-aromatic heterocycle; and ring R is an optionally fused 5- to 7-membered non-aromatic ring, which is further optionally substituted, or a salt thereof.

    摘要翻译： 本发明旨在提供一种具有乙酰-CoA羧化酶（ACC）抑制作用的化合物，其可用于预防或治疗肥胖，糖尿病，高血压，高脂血症，心力衰竭，糖尿病并发症，代谢综合征，肌肉减少症，癌症和 并具有优越的疗效。 本发明提供由式（I）表示的化合物：其中R1是氢原子或取代基; 环P是任选取代的6元含氮芳族杂环; 环Q是任选进一步取代的5-至7-元含氮非芳族杂环; 并且环R是任选稠合的5至7元非芳族环，其进一步任选被取代，或其盐。

    Amine derivative
    10.
    发明申请
    Amine derivative 失效
    胺衍生物

    公开(公告)号：US20060128690A1

    公开(公告)日：2006-06-15

    申请号：US10545120

    申请日：2004-02-12

    申请人： Yuji Ishihara ,  Makoto Kamata ,  Shiro Takekawa

    发明人： Yuji Ishihara ,  Makoto Kamata ,  Shiro Takekawa

    IPC分类号： A61K31/55 ,  A61K31/401 ,  A61K31/445

    CPC分类号： C07D211/16 ,  A61K31/55 ,  C07C233/73 ,  C07C235/42 ,  C07D207/09 ,  C07D207/12 ,  C07D211/14 ,  C07D213/82 ,  C07D233/24 ,  C07D295/135

    摘要： The present invention provides a compound represented by the formula wherein Ar1 is a cyclic group optionally having substituent(s); R is a hydrogen atom, an optionally halogenated C1-6 alkyl, a phenyl optionally having substituent(s) or a pyridyl optionally having substituent(s); Ra1, Ra2, Ra3 and Ra4 are the same or different and each is a hydrogen atom, an optionally halogenated C1-6 alkyl or the like; Ar is a monocyclic aromatic ring optionally having substituent(s); Y is an optionally halogenated alkylene group; and R1 and R2 are (1) the same or different and each is a hydrogen atom or a C1-6 alkyl, (2) R1 and R2 form a nitrogen-containing heterocycle optionally having substituent(s) together with the adjacent nitrogen atom, or (3) R1 and Y form a nitrogen-containing heterocycle optionally having substituent(s) together with the adjacent nitrogen atom, and R2 is a hydrogen atom or a C1-6 alkyl; provided that when the nitrogen-containing heterocycle formed by R1 and R2 together with the adjacent nitrogen atom is a piperazine, or when R is a C1-4 alkyl, Ar1 is a cyclic group having substituent(s), or a salt thereof, having a melanin-concentrating hormone antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like.

    摘要翻译： 本发明提供由下式表示的化合物：其中Ar 1是任选具有取代基的环状基团; R是氢原子，任选卤代的C 1-6烷基，任选具有取代基的苯基或任选具有取代基的吡啶基; Ra 1，R 2，R 3，R 3和R 4相同或不同，各自为氢原子 ，任选卤代的C 1-6烷基等; Ar是任选具有取代基的单环芳环; Y是任选卤代的亚烷基; 且R 1和R 2均为（1）相同或不同，并且各自为氢原子或C 1-6烷基，（ 2）R 1和R 2 2形成任选具有取代基的氮杂环与相邻的氮原子，或（3）R 1， Y和Y形成任选具有取代基的氮杂环与相邻的氮原子一起形成，R 2是氢原子或C 1-6 烷基; 条件是当由R 1和R 2与相邻氮原子一起形成的含氮杂环是哌嗪时，或当R是C 1〜 4个烷基，Ar 1是具有取代基的环状基团或其盐，其具有黑色素浓缩激素拮抗作用并且可用作预防或治疗的药剂 肥胖等。