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    Nitrogen-containing heterocyclic compound and use of same
    3.
    发明授权
    Nitrogen-containing heterocyclic compound and use of same 有权
    含氮杂环化合物及其用途

    公开(公告)号：US08592454B2

    公开(公告)日：2013-11-26

    申请号：US13119743

    申请日：2009-09-18

    申请人： Junya Shirai ,  Hideyuki Sugiyama ,  Taku Kamei ,  Hironobu Maezaki

    发明人： Junya Shirai ,  Hideyuki Sugiyama ,  Taku Kamei ,  Hironobu Maezaki

    IPC分类号： A61K31/445 ,  A61K31/40 ,  A61K31/535 ,  A61K31/00 ,  C07D211/58 ,  C07D295/03

    CPC分类号： C07D401/04 ,  C07D207/14 ,  C07D211/58 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/08 ,  C07D413/14 ,  C07D417/08

    摘要： The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like. The compound has a superior tachykinin receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of various diseases such as lower urinary tract diseases, digestive tract diseases, central neurological disease and the like.

    摘要翻译： 本发明涉及由下式表示的化合物：其中环A是含氮杂环; 环B是任选具有取代基的芳香环; 环D是任选具有取代基的芳香环; L是由式R2表示的基团，R3，R4a和R4b各自独立地为氢原子，任选卤代的C 1-6烷基或任选卤代的C 3-6环烷基，或者R 2和R 3经由亚烷基 链或亚链烯基，或者R4a和R4b任选地通过亚烷基链或亚烯基链键合; R1是氢原子或取代基; m和n各自独立地为0〜5的整数; m + n为2〜5的整数。 并且是单键或双键，或其盐; 等等。 该化合物具有优异的速激肽受体拮抗作用，可用作预防或治疗诸如下尿路疾病，消化道疾病，中枢神经疾病等各种疾病的药剂。

    Fused heterocyclic compounds
    4.
    发明申请
    Fused heterocyclic compounds 失效
    稠合杂环化合物

    公开(公告)号：US20060135530A1

    公开(公告)日：2006-06-22

    申请号：US10523531

    申请日：2003-08-07

    申请人： Satoru Oi ,  Hironobu Maezaki ,  Koji Ikedou

    发明人： Satoru Oi ,  Hironobu Maezaki ,  Koji Ikedou

    IPC分类号： A61K31/496 ,  C07D215/38 ,  A61K31/47 ,  C07D403/02

    CPC分类号： C07D401/04 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/20 ,  C07D215/48 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12

    摘要： A compound represented by the formula wherein ring A is an optionally substituted 5- to 10-membered aromatic ring; R1 and R2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X and Y are the same or different and each is a bound, —O—, —S—, —SO—, —SO?2#191- or —NR3— (R3 is a hydrogen atom or an optionally substituted hydrocarbon group); and L is a divalent hydrocarbon group, or a salt thereof shows a superior peptidase-inhibitory activity and is useful as a prophylactic or therapeutic agent of diabetes and the like.

    摘要翻译： 由下式表示的化合物其中环A是任选取代的5至10元芳环; R 1和R 2相同或不同，各自为任选取代的烃基或任选取代的杂环基; X和Y相同或不同，并且各自为结合的-O - ， - S - ， - SO - ， - SO 2＃191-或-NR 3 - 3是氢原子或任选取代的烃基）; L是二价烃基，或其盐表现出优异的肽酶抑制活性，可用作糖尿病等的预防或治疗剂。

    Fused heterocyclic compounds as peptidase inhibitors
    6.
    发明授权
    Fused heterocyclic compounds as peptidase inhibitors 失效
    稠合杂环化合物作为肽酶抑制剂

    公开(公告)号：US07547710B2

    公开(公告)日：2009-06-16

    申请号：US10523531

    申请日：2003-08-07

    申请人： Satoru Oi ,  Hironobu Maezaki ,  Koji Ikedou

    发明人： Satoru Oi ,  Hironobu Maezaki ,  Koji Ikedou

    IPC分类号： A61K31/47 ,  C07D215/12

    CPC分类号： C07D401/04 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/20 ,  C07D215/48 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12

    摘要： A compound represented by the formula wherein ring A is an optionally substituted 5- to 10-membered aromatic ring; R1 and R2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X and Y are the same or different and each is a bound, —O—, —S—, —SO—, —SO?2#191- or —NR3— (R3 is a hydrogen atom or an optionally substituted hydrocarbon group); and L is a divalent hydrocarbon group, or a salt thereof shows a superior peptidase-inhibitory activity and is useful as a prophylactic or therapeutic agent of diabetes and the like.

    摘要翻译： 由下式表示的化合物其中环A是任选取代的5至10元芳环; R1和R2相同或不同，并且各自为任选取代的烃基或任选取代的杂环基; X和Y相同或不同，各自为结合的-O - ， - S - ， - SO - ， - SO 2＃191-或-NR 3 - （R 3为氢原子或任选取代的烃基） ; L是二价烃基，或其盐表现出优异的肽酶抑制活性，可用作糖尿病等的预防或治疗剂。

    Pyridine compounds as inhibitors of dipeptidyl peptidase IV
    7.
    发明申请
    Pyridine compounds as inhibitors of dipeptidyl peptidase IV 审中-公开
    吡啶化合物作为二肽基肽酶IV的抑制剂

    公开(公告)号：US20070037807A1

    公开(公告)日：2007-02-15

    申请号：US10577561

    申请日：2004-10-29

    申请人： Satoru Oi ,  Hironobu Maezaki ,  Nobuhiro Suzuki

    发明人： Satoru Oi ,  Hironobu Maezaki ,  Nobuhiro Suzuki

    IPC分类号： A61K31/5377 ,  A61K31/4439 ,  A61K31/44 ,  C07D413/02

    CPC分类号： C07D213/80 ,  C04B35/632 ,  C07D213/12 ,  C07D213/55 ,  C07D213/56 ,  C07D213/59 ,  C07D213/71 ,  C07D213/75 ,  C07D213/82 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/06 ,  C07D413/12 ,  C07F9/58

    摘要： A compound represented by the formula wherein R1 and R2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted hydroxy group; R3 is an optionally substituted aromatic group; R4 is an optionally substituted amino group; L is a divalent chain hydrocarbon group; Q is a bond or a divalent chain hydrocarbon group; and X is a hydrogen atom, a cyano group, a nitro group, an acyl group, a substituted hydroxy group, an optionally substituted thiol group, an optionally substituted amino group or an optionally substituted cyclic group; provided that when X is an ethoxycarbonyl group, then Q is a divalent chain hydrocarbon group. The compound has a peptidase inhibitory action, is useful as an agent for the prophylaxis or treatment of diabetes and the like, and is superior in efficacy, duration of action, specificity, lower toxicity and the like.

    摘要翻译： 由下式表示的化合物其中R 1和R 2各自相同或不同，并且各自为任选取代的烃基或任选取代的羟基; R 3是任选取代的芳族基团; R 4是任选取代的氨基; L是二价链烃基; Q是键或二价链烃基; X为氢原子，氰基，硝基，酰基，取代羟基，任选取代的硫醇基，任选取代的氨基或任意取代的环状基团; 条件是当X是乙氧基羰基时，则Q是二价链烃基。 该化合物具有肽酶抑制作用，可用作预防或治疗糖尿病等的药剂，其功效，作用时间，特异性，低毒性等优异。

    CONDENSED PYRIDINE DERIVATIVE AND USE THEREOF
    8.
    发明申请
    CONDENSED PYRIDINE DERIVATIVE AND USE THEREOF 审中-公开
    浓缩吡啶衍生物及其用途

    公开(公告)号：US20100266504A1

    公开(公告)日：2010-10-21

    申请号：US12742781

    申请日：2008-11-14

    申请人： Takahiro Matsumoto ,  Hiroyuki Nagamiya ,  Hironobu Maezaki ,  Tomokazu Kusumoto ,  Kyoko Yoshikawa ,  Hideki Furukawa ,  Izumi Kamo

    发明人： Takahiro Matsumoto ,  Hiroyuki Nagamiya ,  Hironobu Maezaki ,  Tomokazu Kusumoto ,  Kyoko Yoshikawa ,  Hideki Furukawa ,  Izumi Kamo

    IPC分类号： A61K49/00

    CPC分类号： A61K31/5377 ,  A61K31/4545 ,  A61K31/55 ,  C07D471/04 ,  G01N33/5088 ,  G01N33/6893 ,  G01N2800/34

    摘要： Provided are a condensed pyridine derivative having a serotonin 5-HT2C receptor activation action, a prophylactic or therapeutic agent for a lower urinary tract symptom, obesity and/or organ prolapse and the like containing the condensed pyridine derivative, a screening method for a substance that increases leak point pressure upon a rise in the intravesical pressure or a prophylactic or therapeutic drug for stress urinary incontinence, a prophylactic or therapeutic drug for cystoceles or enteroceles, containing a substance that activates serotonin 5-HT2C receptor, and a method of screening for a therapeutic drug for cystoceles or enteroceles, including increasing an intravesical pressure after bilateral transection of the hypogastric nerve and pudendal nerve of an animal, and measuring a closure response in the urethra, the rectum or the vagina observed at that time. A serotonin 5-HT2c receptor activator containing a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof.

    摘要翻译： 提供具有5-羟色胺5-HT 2C受体活化作用的缩合吡啶衍生物，含有缩合吡啶衍生物的下尿路症状，肥胖症和/或器官脱垂等的预防或治疗剂， 增加膀胱内压的上升时的泄漏点压力或压力性尿失禁的预防或治疗药物，包含激活5-羟色胺5-HT 2C受体的物质的用于膀胱或肠的预防或治疗药物的筛选方法 用于膀胱或肠道的治疗药物，包括在双侧横断动物的下腹神经和阴部神经之后增加膀胱内压力，并测量当时观察到的尿道，直肠或阴道中的闭合反应。 含有下式表示的化合物的5-羟色胺5-HT 2C受体活化剂：其中每个符号如说明书中所定义，或其盐。

    PYRIDYL ACETIC ACID COMPOUNDS
    9.
    发明申请
    PYRIDYL ACETIC ACID COMPOUNDS 审中-公开
    吡咯烷酮酸化合物

    公开(公告)号：US20090088419A1

    公开(公告)日：2009-04-02

    申请号：US11817088

    申请日：2006-02-24

    申请人： Hironobu Maezaki ,  Nobuhiro Suzuki

    发明人： Hironobu Maezaki ,  Nobuhiro Suzuki

    IPC分类号： C07D213/02 ,  A61K31/4439 ,  C07D401/02 ,  A61K31/445 ,  A61K31/496 ,  A61P3/10 ,  A61K31/4545 ,  A61K31/551 ,  A61K31/55

    CPC分类号： C07D213/75 ,  C07D213/55 ,  C07D213/56 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07D453/02 ,  C07D471/10

    摘要： The present invention provides a compound represented by the formula (I): wherein R1 is a C?1-6#191 alkyl group optionally substituted by a C?3-10#191 cycloalkyl group, R2 is a C?2-6#191 alkyl group, R3 is a hydrogen atom, a C?1-6#191 alkyl group or a halogen atom, and X is —OR6 or —NR4R5 wherein R4 and R6 are each independently a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R5 is an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted hydroxy group, or R4 and R5 optionally form, together with the adjacent nitrogen atom, an optionally substituted nitrogen-containing heterocycle, or a salt thereof. The compound of the present invention has a superior peptidase inhibitory action and is useful as an agent for the prophylaxis or treatment of diabetes and the like.

    摘要翻译： 本发明提供由式（I）表示的化合物：其中R 1是任选被C 3-10＃191环烷基取代的C 1-6〜11〜191烷基，R 2是C 2-6〜 191烷基，R3是氢原子，C1〜1-6个氨基烷基或卤素原子，X是-OR6或-NR4R5，其中R4和R6各自独立地是氢原子，任意取代的烃基或 任选取代的杂环基，R 5是任选取代的烃基，任选取代的杂环基或任选取代的羟基，或者R 4和R 5任选与相邻的氮原子一起形成任选取代的含氮杂环，或 的盐。 本发明的化合物具有优异的肽酶抑制作用，可用作预防或治疗糖尿病等的药剂。