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1. 发明申请

US20090156572A1 Nitrogen-containing heterocyclic compound and use thereof 有权
标题翻译：含氮杂环化合物及其用途
公开(公告)号：US20090156572A1
公开(公告)日：2009-06-18
申请号：US12314015
申请日：2008-12-02
申请人： Yoshinori Ikeura , Junya Shirai , Hideyuki Sugiyama , Yuji Nishikimi , Taku Kamei , Nobuki Sakauchi
发明人： Yoshinori Ikeura , Junya Shirai , Hideyuki Sugiyama , Yuji Nishikimi , Taku Kamei , Nobuki Sakauchi
IPC分类号： A61K31/397 , C07D413/12 , A61K31/5377 , C07D401/12 , A61K31/4545 , C07D417/14 , A61K31/541 , C07D401/14 , A61K31/497 , C07D487/04 , A61K31/4985
CPC分类号： C07D211/58 , C07D401/12 , C07D401/14 , C07D407/12 , C07D409/12 , C07D417/14
摘要： The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B is an aromatic ring optionally having substituent(s), ring C is a cyclic group optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group, a heterocyclic group optionally having substituent(s) or an amino group optionally having substituent(s), R2 is an optionally halogenated C1-6 alkyl group, m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, and is a single bond or a double bond, or a salt thereof and the like. Since 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, gastrointestinal diseases, central nervous system diseases and the like.
摘要翻译：本发明涉及一种由下式表示的化合物：其中环A为任选具有取代基的含氮杂环，环B为任选具有取代基的芳环，环C为任选具有取代基的环状基团 R 1为氢原子，任选具有取代基的烃基，酰基，任选具有取代基的杂环基或任选具有取代基的氨基，R2为任选卤代的C1 -6烷基，m和n各自为0至5的整数，m + n为2至5的整数，并且是单键或双键，或其盐等。由于该化合物具有优异的速激肽受体拮抗作用，并且可用作预防或治疗诸如下尿路疾病，胃肠道疾病，中枢神经系统疾病等各种疾病的药剂。

2. 发明申请

US20070254877A1 Indole Derivative and Use for Treatment of Cancer 审中-公开
标题翻译：吲哚衍生物和用于治疗癌症的用途
公开(公告)号：US20070254877A1
公开(公告)日：2007-11-01
申请号：US11628386
申请日：2005-06-01
申请人： Yuji Nishikimi , Hideto Fukushi , Hiroshi Miki
发明人： Yuji Nishikimi , Hideto Fukushi , Hiroshi Miki
IPC分类号： A61K31/4162 , A61K31/454 , A61K31/5377 , A61P43/00 , C07D403/14 , C07D413/14 , C07D487/04
CPC分类号： C07D401/14 , C07D403/04 , C07D487/04
摘要： The present invention relates to a compound represented by the formula wherein A is a benzene ring optionally having substituents, R1, R2a and R3 are each a hydrogen atom, a hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, R1 and R2a may form a ring via X, when R1 and R2a form a ring via X, R1 and R2a are each a bond or a divalent C1-5 acyclic hydrocarbon group optionally having substituents, and X is a bond, an oxygen atom, an optionally oxidized sulfur atom or an imino group optionally having a substituent, provided that R1, R2a and X are not bonds at the same time, or a salt thereof, and an agent for inhibiting kinase (phosphorylation enzyme), which contains this compound or a prodrug thereof. The compound of the present invention has an inhibitory activity against kinase such as a vascular endothelial growth factor receptor (VEGFR) and the like, and is useful as an agent for the prophylaxis or treatment of cancer and the like.
摘要翻译：本发明涉及由下式表示的化合物：其中A是任选具有取代基的苯环，R 1，R 2，R 2和R 3，各自为氢原子，任选具有取代基的烃基或任选具有取代基的杂环基，R 1和R 2可以通过X形成环，当R 0 > 1和R 2a通过X形成环，R 1和R 2 2各自为一个键或二价C < 任选具有取代基的无环烃基，X为键，氧原子，任选氧化的硫原子或任选具有取代基的亚氨基，条件是R 1〜 > R 2a，X不同时键合，或其盐，以及含有该化合物或其前药的抑制激酶（磷酸化酶）的试剂。本发明的化合物对激素例如血管内皮生长因子受体（VEGFR）等具有抑制活性，可用作预防或治疗癌症等的药剂。

3. 发明授权

US08470816B2 Nitrogen-containing heterocyclic compound and use thereof 有权
标题翻译：含氮杂环化合物及其用途
公开(公告)号：US08470816B2
公开(公告)日：2013-06-25
申请号：US12314015
申请日：2008-12-02
申请人： Yoshinori Ikeura , Junya Shirai , Hideyuki Sugiyama , Yuji Nishikimi , Taku Kamei , Nobuki Sakauchi
发明人： Yoshinori Ikeura , Junya Shirai , Hideyuki Sugiyama , Yuji Nishikimi , Taku Kamei , Nobuki Sakauchi
IPC分类号： A61K31/5355 , A61K31/445 , A61K31/444 , A61K31/40 , C07D413/04 , C07D401/04 , C07D211/56 , C07D207/14
CPC分类号： C07D211/58 , C07D401/12 , C07D401/14 , C07D407/12 , C07D409/12 , C07D417/14
摘要： The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B is an aromatic ring optionally having substituent(s), ring C is a cyclic group optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group, a heterocyclic group optionally having substituent(s) or an amino group optionally having substituent(s), R2 is an optionally halogenated C1-6 alkyl group, m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, and is a single bond or a double bond, or a salt thereof and the like. Since 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, gastrointestinal diseases, central nervous system diseases and the like.
摘要翻译：本发明涉及一种由下式表示的化合物：其中环A为任选具有取代基的含氮杂环，环B为任选具有取代基的芳环，环C为任选具有取代基的环状基团 R 1为氢原子，任选具有取代基的烃基，酰基，任选具有取代基的杂环基或任选具有取代基的氨基，R2为任选卤代的C1 -6烷基，m和n分别为0〜5的整数，m + n为2〜5的整数，为单键或双键，或其盐等。由于该化合物具有优异的速激肽受体拮抗作用，并且可用作预防或治疗诸如下尿路疾病，胃肠道疾病，中枢神经系统疾病等各种疾病的药剂。

4. 发明申请

US20110112133A1 DIHYDRO PYRROLOQUINOLINE DERIVATIVES 审中-公开
标题翻译：二氢吡喃酚衍生物
公开(公告)号：US20110112133A1
公开(公告)日：2011-05-12
申请号：US12916721
申请日：2010-11-01
申请人： Kasei Miura , Yuji Nishikimi
发明人： Kasei Miura , Yuji Nishikimi
IPC分类号： A61K31/437 , C07D471/04 , A61P1/04 , A61P25/00
CPC分类号： C07D471/04
摘要： A compound represented by the formula (I) wherein A is a benzene ring optionally having substituent(s), R is a hydrogen atom, a hydrocarbon group optionally having substituent(s) or a heterocyclic group optionally having substituent(s), X1 and X2 are each a bond or a divalent C1-5 chain hydrocarbon group optionally having substituent(s), X3 is a methylene group having substituent(s), Y is a bond or the like, and Z is a hydrocarbon group optionally having substituent(s) or the like, or a salt thereof. The compound of the present invention or a salt thereof is useful as an NK receptor antagonist.
摘要翻译：由式（I）表示的化合物，其中A为任选具有取代基的苯环，R为氢原子，任选具有取代基的烃基或任选具有取代基的杂环基，X1和 X2各自为键或任选具有取代基的二价C 1-5链烃基，X 3为具有取代基的亚甲基，Y为键等，Z为任选具有取代基的烃基（ s）等，或其盐。本发明的化合物或其盐可用作NK受体拮抗剂。

5. 发明授权

US06423869B1 Polyol-amino acid compounds having anti-helicobacter pylori activity 失效
标题翻译：具有抗幽门螺杆菌活性的多元醇 - 氨基酸化合物
公开(公告)号：US06423869B1
公开(公告)日：2002-07-23
申请号：US09423118
申请日：1999-11-01
申请人： Ken-ichiro Miyagawa , Shigetoshi Tsubotani , Masafumi Nakao , Yoshitaka Nakano , Keiji Kamiyama , Motoo Izawa , Yohko Akiyama , Yuji Nishikimi
发明人： Ken-ichiro Miyagawa , Shigetoshi Tsubotani , Masafumi Nakao , Yoshitaka Nakano , Keiji Kamiyama , Motoo Izawa , Yohko Akiyama , Yuji Nishikimi
IPC分类号： C07C22900
CPC分类号： C12R1/07 , A61K38/00 , C07B2200/07 , C07C237/12 , C07C237/22 , C07C271/22 , C07D207/16
摘要： A compound of the formula (I): wherein R1 represents an amino group which may be substituted; R2 represents a carboxy group which may be esterified or amidated; R3, R4, R5 and R6 each represent a hydroxy group which may be protected; Q represents an aryl group which may be substituted; or a salt thereof is disclosed. The compound (I) possesses ant-Helicobacter pylori activity, and is useful in the prevention or treatment of various diseases associated with Helicobacter bacteria, such as duodenal ulcer, gastric ulcer, chronic gastritis and cancer of the stomach.
摘要翻译：式（I）的化合物：其中R 1表示可以被取代的氨基; R2表示可被酯化或酰胺化的羧基; R3，R4，R5和R6各自表示可被保护的羟基; Q表示可以被取代的芳基; 或其盐。化合物（I）具有抗幽门螺杆菌活性，可用于预防或治疗与幽门螺杆菌相关的各种疾病，例如十二指肠溃疡，胃溃疡，慢性胃炎和胃癌。

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