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    5/5-OR 5/6-MEMBERED CONDENSED RING CYCLOALKYLAMINE DERIVATIVE
    1.
    发明申请
    5/5-OR 5/6-MEMBERED CONDENSED RING CYCLOALKYLAMINE DERIVATIVE 审中-公开
    5/5或5/6会议凝结环状环丙基胺衍生物

    公开(公告)号：US20110124674A1

    公开(公告)日：2011-05-26

    申请号：US13054804

    申请日：2009-07-14

    申请人： Hiroyuki Kishino ,  Nagaaki Sato ,  Takao Suzuki

    发明人： Hiroyuki Kishino ,  Nagaaki Sato ,  Takao Suzuki

    IPC分类号： A61K31/454 ,  C07D401/06 ,  C07D417/14 ,  C07D471/04 ,  A61K31/4545 ,  C07D405/06 ,  A61K31/4525 ,  C07D495/04 ,  A61P3/10

    CPC分类号： C07D401/06 ,  A61K31/4525 ,  A61K31/454 ,  A61K31/4545 ,  C07D401/14 ,  C07D405/06 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04

    摘要： Disclosed are a compound of a formula (I) and its pharmaceutically-acceptable salt: wherein Q is CH or N; R1a, R1b, R1c and R1d are independently a C1-6 alkyl, a halo-C1-6 alkyl, etc.; R2 is a hydrogen atom, etc.; R3 is independently a hydrogen atom, a C1-6 alkyl, etc., or two R3's, taken together, form a bridge such as methylene, etc.; R4a and R4b are independently a hydrogen atom, a C1-6 alkyl, etc.; Z is a bicyclic aromatic hetero ring, etc.; Ar is a benzene ring, etc.; m1 and m2 are independently 0, 1 or 2; n is an integer of from 1 to 4. The compound and its salt act as a melanin concentrating hormone receptor antagonist, and are useful as a preventive or remedy for central system disorders, cardiovascular disorders, metabolic disorders, etc.

    摘要翻译： 公开了式（I）化合物及其药学上可接受的盐：其中Q是CH或N; R1a，R1b，R1c和R1d独立地为C1-6烷基，卤代-C1-6烷基等; R2是氢原子等; R 3独立地为氢原子，C 1-6烷基等，或两个R 3一起形成桥，例如亚甲基等; R4a和R4b独立地为氢原子，C1-6烷基等; Z是双环芳香杂环等; Ar是苯环等; m1和m2分别为0,1或2; n为1〜4的整数。化合物及其盐作为黑色素浓缩激素受体拮抗剂，可用作中枢系统疾病，心血管疾病，代谢紊乱等的预防或治疗。

    3 ARYL OR HETEROARYL-SUBSTITUTED INDOLE DERIVATIVE
    2.
    发明申请
    3 ARYL OR HETEROARYL-SUBSTITUTED INDOLE DERIVATIVE 审中-公开
    3 ARYL或HETEROARYL取代的INDOLE DERIVATIVE

    公开(公告)号：US20120028990A1

    公开(公告)日：2012-02-02

    申请号：US13260746

    申请日：2010-04-14

    申请人： Takashi Fujimura ,  Hiroyuki Kishino ,  Takashi Mizutani ,  Shunji Sakuraba ,  Takahide Sasaki ,  Nagaaki Sato

    发明人： Takashi Fujimura ,  Hiroyuki Kishino ,  Takashi Mizutani ,  Shunji Sakuraba ,  Takahide Sasaki ,  Nagaaki Sato

    IPC分类号： A61K31/404 ,  A61K31/4439 ,  A61K31/4725 ,  A61P3/04 ,  C07D403/12 ,  A61K31/496 ,  C07D417/14 ,  C07D409/14 ,  C07D405/14 ,  A61K31/454

    CPC分类号： C07D405/04 ,  C07D209/18 ,  C07D405/14 ,  C07D409/04 ,  C07D417/04

    摘要： A 3-aryl or heteroaryl-substituted indole derivative which is effective as a preventive or remedy for various diseases is provided. [Means for Resolution] A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof is provided. In the formula, R1 represents a hydrogen atom, C1-6 alkyl et al; R2 represents a hydrogen atom, C1-6 alkyl et al; Z represents aryl or heteroaryl (with the proviso that imidazolyl is excluded); and W represents a group represented by the formula (w-1) or (w-2). In the formula, R3 represents C1-6 alkyl et al; Yl and Y2 both represent a hydrogen atom or Y1 and Y2 together form —CH2-CH2-; Q represents CH or N; Ar represents phenyl, furyl et al; R4 and R5 each independently represent a hydrogen atom or C1-6 alkyl or R4 and R5 together with the nitrogen atom form pyrrolidine et al.

    摘要翻译： 提供作为各种疾病的预防或治疗有效的3-芳基或杂芳基取代的吲哚衍生物。 [解决方法]提供由式（I）表示的化合物或其药学上可接受的盐。 在该式中，R 1表示氢原子，C 1-6烷基等; R2表示氢原子，C1-6烷基等; Z表示芳基或杂芳基（条件是不包括咪唑基）; W表示由式（w-1）或（w-2）表示的基团。 在该式中，R 3表示C 1-6烷基等; Y 1和Y 2均表示氢原子或Y 1和Y 2一起形成-CH 2 -CH 2 - ; Q表示CH或N; Ar表示苯基，呋喃基等; R4和R5各自独立地表示氢原子或C1-6烷基或R4和R5以及氮原子形成吡咯烷等。

    ARYL INDOLE DERIVATIVES
    3.
    发明申请
    ARYL INDOLE DERIVATIVES 审中-公开
    ARYL INDOLE DORIVATIVES

    公开(公告)号：US20120022078A1

    公开(公告)日：2012-01-26

    申请号：US13258006

    申请日：2010-04-07

    申请人： Hiroyuki Kishino ,  Sayaka Mizutani ,  Shunji Sakuraba ,  Nagaaki Sato

    发明人： Hiroyuki Kishino ,  Sayaka Mizutani ,  Shunji Sakuraba ,  Nagaaki Sato

    IPC分类号： A61K31/496 ,  A61P3/04 ,  C07D403/10 ,  C07D417/14 ,  C07D401/14

    CPC分类号： C07D401/04 ,  A61K31/496 ,  C07D209/14 ,  C07D417/04

    摘要： A novel aryl indole derivative is provided that is effective as a preventive or remedy for various diseases. A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R1 is a hydrogen atom, halogen, C1-6alkyl, haloC1-6alkyl, C1-6alkyloxy, or haloC1-6alkyloxy; R2 represents C1-6alkyl or haloC1-6alkyl; R3 represents a hydrogen atom, C1-6alkyl, or haloC1-6alkyl; and Ar represents an aryl or heteroaryl, wherein the aryl or the heteroaryl may be substituted with 1 to 3 substituents such as halogen, C1-6alkyl, haloC1-6alkyl, and C1-6alkyloxy.

    摘要翻译： 提供了一种新的芳基吲哚衍生物，其作为各种疾病的预防或补救是有效的。 由式（I）表示的化合物或其药学上可接受的盐：（I）其中R 1是氢原子，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基或卤代C 1-6烷氧基; R 2表示C 1-6烷基或卤代C 1-6烷基; R 3表示氢原子，C 1-6烷基或卤代C 1-6烷基; 并且Ar表示芳基或杂芳基，其中芳基或杂芳基可以被1至3个取代基例如卤素，C 1-6烷基，卤代C 1-6烷基和C 1-6烷氧基取代。

    Imidazopyridine Derivatives
    5.
    发明申请
    Imidazopyridine Derivatives 失效
    咪唑并吡啶衍生物

    公开(公告)号：US20080200494A1

    公开(公告)日：2008-08-21

    申请号：US10567269

    申请日：2004-08-13

    申请人： Hiroyuki Kishino ,  Minoru Moriya ,  Toshihiro Sakamoto ,  Hidekazu Takahashi ,  Shunji Sakuraba ,  Takao Suzuki ,  Akio Kanatani

    发明人： Hiroyuki Kishino ,  Minoru Moriya ,  Toshihiro Sakamoto ,  Hidekazu Takahashi ,  Shunji Sakuraba ,  Takao Suzuki ,  Akio Kanatani

    IPC分类号： A61K31/437 ,  A61P3/10 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： The invention provides imidazopyridine derivatives represented by the general formula [I] [in which R1 and R2 may be the same or different and stand for C1-6 alkyl or the like, R3 and R4 stand for hydrogen atom, methyl group or the like, W stands for mono- or bi-cyclic 3- to 8-membered aromatic or aliphatic heterocycle or the like, and Ar stands for optionally substituted aromatic heterocycle or the like]. These compounds act as melanin-concentrating hormone receptor antagonist and are useful as medicines for central nervous system disorders, cardiovascular system disorders and metabolic disorders.

    摘要翻译： 本发明提供由通式[I]表示的咪唑并吡啶衍生物[其中R 1'和R 2'可以相同或不同，代表C 1〜 6个烷基等，R 3和R 4代表氢原子，甲基等，W代表单环或双环3 - 至8-元芳族或脂族杂环等，Ar表示任选取代的芳族杂环等〕。 这些化合物作为黑色素浓缩激素受体拮抗剂起作用，可用作中枢神经系统疾病，心血管系统疾病和代谢紊乱的药物。

    Spiro compounds
    6.
    发明授权
    Spiro compounds 失效
    螺环化合物

    公开(公告)号：US07205417B2

    公开(公告)日：2007-04-17

    申请号：US10485955

    申请日：2002-08-02

    申请人： Takehiro Fukami ,  Katsumasa Nonoshita ,  Takeshi Sagara ,  Hiroyuki Kishino

    发明人： Takehiro Fukami ,  Katsumasa Nonoshita ,  Takeshi Sagara ,  Hiroyuki Kishino

    IPC分类号： C07D307/94 ,  C07D407/12 ,  A61K31/4525

    CPC分类号： C07D401/12 ,  A61K31/4747 ,  C07D209/96 ,  C07D307/94 ,  C07D403/12 ,  C07D405/12 ,  C07D471/10 ,  C07D491/10

    摘要： Compounds of the formula (I): (wherein A is an optionally substituted straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally intervened by oxygen or nitrogen atom; Ar1 is aryl or heteroaryl, any of which is optionally substituted; n is 0 or 1; R0 is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A; T, U, V and W are independently nitrogen atom or optionally substituted methine, and at least two of T, U, V and W are said methine group; X is —N(SO2R1)—, —N(COR2)— or —CO—; Y is —C(R3)(R4)—, —O— or —N(R5)—; Z is methine or nitrogen atom) exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, etc., sexual and reproductive dysfunctions, and gastro-intestinal motility disorder.

    摘要翻译： 式（I）的化合物：

    Imidazopyridine Compound
    7.
    发明申请
    Imidazopyridine Compound 失效
    咪唑并吡啶化合物

    公开(公告)号：US20070249659A1

    公开(公告)日：2007-10-25

    申请号：US11579570

    申请日：2005-05-09

    申请人： Shunji Sakuraba ,  Minoru Moriya ,  Hidekazu Takahashi ,  Hiroyuki Kishino ,  Makoto Jitsuoka ,  Minoru Kameda ,  Akio Kanatani

    发明人： Shunji Sakuraba ,  Minoru Moriya ,  Hidekazu Takahashi ,  Hiroyuki Kishino ,  Makoto Jitsuoka ,  Minoru Kameda ,  Akio Kanatani

    IPC分类号： A61K31/44 ,  C07D471/02

    CPC分类号： A61K31/501 ,  A61K31/437 ,  A61K31/444 ,  A61K31/506 ,  C07D471/04

    摘要： The present invention provides an imidazopyridine compound represented by formula (I), wherein R1 and R2 each independently represent a C1-6 alkyl group et al; R3 and R4 each independently represent a hydrogen atom, a methyl et al; Ar1 is a divalent substituent representing a monocyclic or bicyclic, 3- to 8-membered aromatic or aliphatic heterocyclic group et al; Ar2 represents an aromatic carbocyclic group, or an aromatic heterocyclic group; W represents —(CH2)m et al, and m indicates an integer of from 0 to 10. This compound acts as a melanin concentrating hormone receptor antagonist, and is useful as treating agents for obesity.

    摘要翻译： 本发明提供由式（I）表示的咪唑并吡啶化合物，其中R 1和R 2各自独立地表示C 1-6烷基 集团等 R 3和R 4各自独立地表示氢原子，甲基等; Ar 1是表示单环或双环的3至8元芳族或脂族杂环基等的二价取代基; Ar 2表示芳族碳环基或芳族杂环基; W表示 - （CH 2）2，m表示0〜10的整数。该化合物作为黑色素浓缩激素受体拮抗剂起作用， 作为肥胖症的治疗剂。

    Bicyclic aromatic substituted pyridone derivative
    9.
    发明申请
    Bicyclic aromatic substituted pyridone derivative 审中-公开
    双环芳族取代吡啶酮衍生物

    公开(公告)号：US20090264426A1

    公开(公告)日：2009-10-22

    申请号：US11991334

    申请日：2006-09-05

    申请人： Shunji Sakuraba ,  Minoru Kameda ,  Hiroyuki Kishino ,  Yuji Haga ,  Norikazu Otake ,  Minoru Moriya

    发明人： Shunji Sakuraba ,  Minoru Kameda ,  Hiroyuki Kishino ,  Yuji Haga ,  Norikazu Otake ,  Minoru Moriya

    IPC分类号： A61K31/5377 ,  C07D401/10 ,  C07D413/14 ,  A61K31/47 ,  A61P9/10

    CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D405/04 ,  C07D471/04

    摘要： Disclosed is a compound represented by the formula (I): Wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like; X1, X2 and X3 independently represent a methine group or a nitrogen atom; Y1 and Y3 independently represent a single bond, —O— or the like; Y2 represents a lower alkylene group or the like; W1 to W4 independently represent a single bond, a methylene group or the like; L represents a single bond, a methylene group or the like; Z1 and Z2 independently represent a single bond, a C1-4 alkylene group or the like; Ar1 represents an aromatic carbocyclic ring or the like; and Ar2 represents a bicyclic aromatic carbocyclic ring or the like. The compound is useful as a pharmaceutical for a central disease, a cardiovascular disease or a metabolic disease.

    摘要翻译： 公开了由式（I）表示的化合物：其中R1和R2独立地表示氢原子，低级烷基等; X1，X2和X3独立地表示次甲基或氮原子; Y1和Y3独立地表示单键，-O-等; Y2表示低级亚烷基等; W1至W4独立地表示单键，亚甲基等; L表示单键，亚甲基等; Z 1和Z 2独立地表示单键，C 1-4亚烷基等; Ar 1表示芳香族碳环等， Ar 2表示双环芳香族碳环等。 该化合物可用作中枢性疾病，心血管疾病或代谢性疾病的药物。