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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。

    Tricyclic compounds, their production and use
    4.
    发明授权
    Tricyclic compounds, their production and use 有权
    三环化合物，其生产和使用

    公开(公告)号：US06218429B1

    公开(公告)日：2001-04-17

    申请号：US09309519

    申请日：1999-05-10

    申请人： Shigenori Ohkawa ,  Osamu Uchikawa ,  Kohji Fukatsu ,  Masaomi Miyamoto

    发明人： Shigenori Ohkawa ,  Osamu Uchikawa ,  Kohji Fukatsu ,  Masaomi Miyamoto

    IPC分类号： A01N34308

    CPC分类号： C07D263/52 ,  C07D265/34 ,  C07D307/93 ,  C07D311/94 ,  C07D317/70 ,  C07D319/14 ,  C07D491/04 ,  Y10S514/923

    摘要： A compound of the formula: wherein R1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R2 is H or an optionally substituted hydrocarbon group; R3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR4, NR4, O or S in which R4 is H or an optionally substituted hydrocarbon group; Y is C, CH or N; ring A is optionally substituted 5- to 7-membered ring; ring B is an optionally substituted benzene ring; and m is 1 to 4, or a salt thereof, a process for producing it, an intermediate for the production and a pharmaceutical composition comprising it are provided.

    摘要翻译： 下式的化合物：其中R 1是任选取代的烃，氨基或杂环基; R2是H或任选取代的烃基; R3是H或任选取代的烃或杂环基; X是CHR 4，NR 4，O或S，其中R 4是H或任选取代的烃基; Y为C，CH或N; 环A为任选取代的5-至7-元环; 环B是任选取代的苯环; 和m为1至4，或其盐，其制备方法，制备中间体和包含其的药物组合物。

    Tricyclic compounds, their production and use
    5.
    发明授权
    Tricyclic compounds, their production and use 失效
    三环化合物，其生产和使用

    公开(公告)号：US6034239A

    公开(公告)日：2000-03-07

    申请号：US812168

    申请日：1997-03-06

    申请人： Shigenori Ohkawa ,  Osamu Uchikawa ,  Kohji Fukatsu ,  Masaomi Miyamoto

    发明人： Shigenori Ohkawa ,  Osamu Uchikawa ,  Kohji Fukatsu ,  Masaomi Miyamoto

    IPC分类号： C07C233/00 ,  C07D307/92 ,  C07D413/00 ,  C07D493/00

    CPC分类号： C07D307/77 ,  C07D263/62 ,  C07D311/94 ,  C07D317/70 ,  C07D319/14 ,  C07D491/04

    摘要： A compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R.sup.2 is H or an optionally substituted hydrocarbon group; R.sup.3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR.sup.4, NR.sup.4, O or S in which R.sup.4 is H or an optionally substituted hydrocarbon group; Y is C, CH or N; ring A is optionally substituted 5- to 7-membered ring; ring B is an optionally substituted benzene ring; and m is 1 to 4, or a salt thereof, a process for producing it, an intermediate for the production and a pharmaceutical composition comprising it are provided.

    摘要翻译： 下式的化合物：其中R 1是任选取代的烃，氨基或杂环基; R2是H或任选取代的烃基; R3是H或任选取代的烃或杂环基; X是CHR 4，NR 4，O或S，其中R 4是H或任选取代的烃基; Y为C，CH或N; 环A为任选取代的5-至7-元环; 环B是任选取代的苯环; 和m为1至4，或其盐，其制备方法，制备中间体和包含其的药物组合物。

    SPIRO-RING COMPOUND
    6.
    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。

    Furan or thiophene derivative and medicinal use thereof
    7.
    发明授权
    Furan or thiophene derivative and medicinal use thereof 失效
    呋喃或噻吩衍生物及其医药用途

    公开(公告)号：US07553867B2

    公开(公告)日：2009-06-30

    申请号：US10526507

    申请日：2003-09-04

    申请人： Kazumasa Hamamura ,  Shigekazu Sasaki ,  Yuichiro Amano ,  Junichi Sakamoto ,  Kohji Fukatsu

    发明人： Kazumasa Hamamura ,  Shigekazu Sasaki ,  Yuichiro Amano ,  Junichi Sakamoto ,  Kohji Fukatsu

    IPC分类号： A61K31/341 ,  A61K31/381 ,  C07D307/40 ,  C07D333/14 ,  C07D333/18

    CPC分类号： C07D307/42 ,  C07D307/38 ,  C07D307/54 ,  C07D307/68 ,  C07D307/79 ,  C07D405/12 ,  C07D409/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12

    摘要： The present invention provides a compound represented by the formula (I): [wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, p is 0, 1 or 2, and when p is 2, each R may be the same or different, R1 is a hydrogen atom or an optionally substituted hydrocarbon group, R2 is an optionally substituted aromatic group, Ring A is an optionally substituted monocyclic aromatic ring or optionally substituted bicyclic aromatic fused ring, X1 is an oxygen atom or a sulfur atom, X2 is a bond, an oxygen atom or —S(O)n— (wherein n is 0, 1 or 2), Y is a bond, an oxygen atom, —S(O)m—, —C(═O)—N(R3)— or —N(R3)—C(═O)— (R3 is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, and m is 0, 1 or 2), M1, M2 and M3 may be the same or different and are each independently a bond or an optionally substituted divalent aliphatic hydrocarbon group, and M4 is an optionally substituted divalent aliphatic hydrocarbon group] or a salt thereof, which is useful as a prophylactic and/or therapeutic agent for lipid metabolism abnormality, arteriosclerotic disease and sequelae thereof, diabetes mellitus and the like.

    摘要翻译： 本发明提供由式（I）表示的化合物：[其中R是任选取代的烃基或任选取代的杂环基，p是0,1或2，当p是2时，每个R可以相同 或不同的，R 1是氢原子或任选取代的烃基，R 2是任选取代的芳族基团，环A是任选取代的单环芳族环或任选取代的双环芳族稠环，X 1是氧原子或硫原子， X 2是键，氧原子或-S（O）n - （其中n是0,1或2），Y是键，氧原子，-S（O）m - ， - C（-O） -N（R3） - 或-N（R3）-C（-O） - （R3是氢原子，任选取代的烃基或任选取代的杂环基，m是0,1或2），M1， M2和M3可以相同或不同，并且各自独立地为键或任选取代的二价脂族烃基，M4是任选取代的二价脂族氢 羰基]或其盐，其可用作脂质代谢异常的预防和/或治疗剂，动脉硬化疾病及其后遗症，糖尿病等。