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1.
公开(公告)号:US08969376B2
公开(公告)日:2015-03-03
申请号:US13579095
申请日:2011-02-25
申请人: Eiji Kawanishi , Mitsuya Hongu , Yoshihito Tanaka
发明人: Eiji Kawanishi , Mitsuya Hongu , Yoshihito Tanaka
IPC分类号: A61K31/415 , C07D293/00 , C07D487/00 , C07D487/04
CPC分类号: C07D487/04
摘要: The present invention relates to a compound represented by formula [I]: wherein: R1 is hydrogen, halogen, lower alkyl or cyano; Ring A is an optionally substituted heterocyclic group; Ring B is an optionally substituted 3 to 6-membered monocyclic group; and Y is optionally substituted amino, optionally substituted cyclic amino, optionally substituted aliphatic 3 to 6-membered monocyclyloxy, optionally substituted lower alkyl or optionally substituted lower alkyl-O—, or a pharmaceutically acceptable salt thereof, and to their use as PDE10 inhibitor.
摘要翻译: 本发明涉及由式[I]表示的化合物:其中:R 1是氢,卤素,低级烷基或氰基; 环A是任选取代的杂环基; 环B是任选取代的3至6元单环基团; 并且Y是任选取代的氨基,任选取代的环状氨基,任选取代的脂族3至6元单环氧基,任选取代的低级烷基或任选取代的低级烷基-O-或其药学上可接受的盐,以及它们作为PDE10抑制剂的用途。
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2.
公开(公告)号:US20120309754A1
公开(公告)日:2012-12-06
申请号:US13579095
申请日:2011-02-25
申请人: Eiji Kawanishi , Mitsuya Hongu , Yoshihito Tanaka
发明人: Eiji Kawanishi , Mitsuya Hongu , Yoshihito Tanaka
IPC分类号: A61K31/519 , C07D487/04 , A61P25/00 , A61P25/22 , A61P25/30 , A61K31/5377 , A61P25/18
CPC分类号: C07D487/04
摘要: The present invention relates to a compound represented by formula [I]: wherein: R1 is hydrogen, halogen, lower alkyl or cyano; Ring A is an optionally substituted heterocyclic group; Ring B is an optionally substituted 3 to 6-membered monocyclic group; and Y is optionally substituted amino, optionally substituted cyclic amino, optionally substituted aliphatic 3 to 6-membered monocyclyloxy, optionally substituted lower alkyl or optionally substituted lower alkyl-O—, or a pharmaceutically acceptable salt thereof, and to their use as PDE10 inhibitor.
摘要翻译: 本发明涉及由式[I]表示的化合物:其中:R 1是氢,卤素,低级烷基或氰基; 环A是任选取代的杂环基; 环B是任选取代的3至6元单环基团; 并且Y是任选取代的氨基,任选取代的环状氨基,任选取代的脂族3至6元单环氧基,任选取代的低级烷基或任选取代的低级烷基-O-或其药学上可接受的盐,以及它们作为PDE10抑制剂的用途。
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3.
公开(公告)号:US09024009B2
公开(公告)日:2015-05-05
申请号:US12207252
申请日:2008-09-09
申请人: Ahmed F. Abdel-Magid , Maureen Chislom , Steven Mehrman , Lorraine Scott , Kenneth M. Wells , Fan Zhang-Plasket , Sumihiro Nomura , Mitsuya Hongu , Yuichi Koga
发明人: Ahmed F. Abdel-Magid , Maureen Chislom , Steven Mehrman , Lorraine Scott , Kenneth M. Wells , Fan Zhang-Plasket , Sumihiro Nomura , Mitsuya Hongu , Yuichi Koga
IPC分类号: C07H7/04 , C07H7/06 , C07D409/10 , C07D409/14 , C07D417/14 , A61K31/7042 , A61K31/7056 , A61K31/706 , A61P3/10 , C07D309/12 , C07D309/10
CPC分类号: C07D409/10 , C07D309/10 , C07D309/12 , C07D409/14 , C07D417/14
摘要: The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.
摘要翻译: 本发明涉及一种制备具有抑制活性的化合物的新方法,所述化合物对存在于肠或肾中的钠依赖性葡萄糖转运蛋白(SGLT)具有抑制活性。
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公开(公告)号:US20080027014A1
公开(公告)日:2008-01-31
申请号:US11878761
申请日:2007-07-26
申请人: Sumihiro Nomura , Mitsuya Hongu
发明人: Sumihiro Nomura , Mitsuya Hongu
IPC分类号: A61K31/7056 , A61K31/381 , A61P3/00 , C07D409/10 , C07H19/044
CPC分类号: C07D335/02 , C07D309/10
摘要: Novel compounds of formula (A) or a pharmaceutically acceptable salt thereof: wherein symbols are as defined in claims, which are useful as SGLT inhibitors and for treatment of diabetes and related diseases.
摘要翻译: 式(A)的新型化合物或其药学上可接受的盐:其中符号如权利要求中所定义,其可用作SGLT抑制剂和用于治疗糖尿病和相关疾病。
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公开(公告)号:US5767094A
公开(公告)日:1998-06-16
申请号:US745048
申请日:1996-11-07
申请人: Kenji Tsujihara , Kunio Saito , Mitsuya Hongu , Mamoru Matsumoto , Kozo Oka
发明人: Kenji Tsujihara , Kunio Saito , Mitsuya Hongu , Mamoru Matsumoto , Kozo Oka
IPC分类号: A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7048 , A61P3/08 , A61P3/10 , A61P43/00 , C07H15/203 , C07H15/26 , A01N43/04 , A01N43/16 , C07H15/00
CPC分类号: C07H15/203 , A61K31/70 , C07H15/26 , Y10S514/866
摘要: A propiophenone derivative the formula �I!: ##STR1## wherein R' is a lower alkanoyl group and R" is a hydrogen atom, or R' is a hydrogen atom and R" is a lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof. Said compounds have excellent hypoglycemic activity so that they are useful in the prophylaxis or treatment of diabetes.
摘要翻译: 式[I]的苯丙酮衍生物:其中R'为低级烷酰基,R“为氢原子,或R'为氢原子,R”为低级烷氧基羰基,或 其药学上可接受的盐。 所述化合物具有优异的降血糖活性,因此它们可用于预防或治疗糖尿病。
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公开(公告)号:US20100256165A1
公开(公告)日:2010-10-07
申请号:US12795323
申请日:2010-06-07
IPC分类号: A61K31/497 , C07D233/64 , A61K31/4178 , C07D401/14 , A61K31/4439 , C07D217/14 , A61K31/4725 , C07D403/04 , A61P13/00 , A61P9/10
CPC分类号: C07D277/20 , A61K31/00 , A61K31/4164 , A61K31/4178 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/506 , C07D233/54 , C07D233/68 , C07D263/30 , C07D263/32 , C07D263/34 , C07D333/04 , C07D333/28 , C07D333/52
摘要: A large conductance calcium-activated K channel opener comprising as an active ingredient a nitrogen-containing 5-membered heterocyclic compound represented by the following formula (I): wherein X represents N—R4, O or S, R1 and R2 each independently represent hydrogen, halogen, carboxyl, amino, lower alkyl, lower alkoxycarbonyl, lower alkenyl, cyclo-lower alkyl, carbamoyl, aryl, heterocyclic or heterocyclic-substituted carbonyl group, R3 represents aryl, heterocyclic or lower alkyl group, and R4 represents hydrogen or lower alkyl group, or a pharmaceutically acceptable salt thereof.
摘要翻译: 一种大电导钙活化的K通道开放剂,其包含作为活性成分的由下式(I)表示的含氮5元杂环化合物:其中X表示N-R 4,O或S,R 1和R 2各自独立地表示氢 ,卤素,羧基,氨基,低级烷基,低级烷氧基羰基,低级烯基,环低级烷基,氨基甲酰基,芳基,杂环或杂环取代的羰基,R3表示芳基,杂环或低级烷基,R4表示氢或低级烷基 基团或其药学上可接受的盐。
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公开(公告)号:US5830873A
公开(公告)日:1998-11-03
申请号:US429567
申请日:1995-04-27
IPC分类号: C07H15/203 , C07H15/26 , A61K31/70 , C07K15/00
CPC分类号: C07H15/203 , C07H15/26
摘要: A propiophenone derivative of the formula �I!: ##STR1## wherein X is O, S or methylene, OY is a protected or unprotected OH, Z is .beta.-D-glucopyranosyl or 4-O-(.alpha.-D-glucopyranosyl)-.beta.-D-glucopyranosyl or wherein one or more hydroxy groups of these groups may optionally be acylated, and the dotted line means the presence or absence of a double bond, or a pharmaceutically acceptable salt thereof. Said compounds have excellent hypoglycemic activity so that they are useful in the prophylaxis or treatment of diabetes.
摘要翻译: 式[I]的苯丙酮衍生物:其中X为O,S或亚甲基,OY为被保护或未被保护的OH,Z为β-D-吡喃葡萄糖基或4-O-(α-D- 吡喃葡萄糖基)-β-D-吡喃葡萄糖基或其中这些基团的一个或多个羟基可以任选地被酰化,并且虚线表示双键的存在或不存在或其药学上可接受的盐。 所述化合物具有优异的降血糖活性,因此它们可用于预防或治疗糖尿病。
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公开(公告)号:US07759373B2
公开(公告)日:2010-07-20
申请号:US10474850
申请日:2002-04-15
IPC分类号: A01N43/78 , A61K31/425 , C07D277/04 , C07D277/06
CPC分类号: C07D277/20 , A61K31/00 , A61K31/4164 , A61K31/4178 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/506 , C07D233/54 , C07D233/68 , C07D263/30 , C07D263/32 , C07D263/34 , C07D333/04 , C07D333/28 , C07D333/52
摘要: A large conductance calcium-activated K channel opener comprising as an active ingredient a nitrogen-containing 5-membered heterocyclic compound represented by the following formula (I): wherein X represents N—R4, O or S, R1 and R2 each independently represent hydrogen, halogen, carboxyl, amino, lower alkyl, lower alkoxycarbonyl, lower alkenyl, cyclo-lower alkyl, carbamoyl, aryl, heterocyclic or heterocyclic-substituted carbonyl group, R3 represents aryl, heterocyclic or lower alkyl group, and R4 represents hydrogen or lower alkyl group, or a pharmaceutically acceptable salt thereof.
摘要翻译: 一种大电导钙活化的K通道开放剂,其包含作为活性成分的由下式(I)表示的含氮5元杂环化合物:其中X表示N-R 4,O或S,R 1和R 2各自独立地表示氢 ,卤素,羧基,氨基,低级烷基,低级烷氧基羰基,低级烯基,环低级烷基,氨基甲酰基,芳基,杂环或杂环取代的羰基,R3表示芳基,杂环或低级烷基,R4表示氢或低级烷基 基团或其药学上可接受的盐。
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9.
公开(公告)号:US20090233874A1
公开(公告)日:2009-09-17
申请号:US12207252
申请日:2008-09-09
申请人: Ahmed F. Abdel-Magid , Maureen Chisholm , Steven Mehrman , Lorraine Scott , Kenneth M. Wells , Fan Zhang-Plasket , Sumihiro Nomura , Mitsuya Hongu , Yuichi Koga
发明人: Ahmed F. Abdel-Magid , Maureen Chisholm , Steven Mehrman , Lorraine Scott , Kenneth M. Wells , Fan Zhang-Plasket , Sumihiro Nomura , Mitsuya Hongu , Yuichi Koga
IPC分类号: A61K31/706 , C07H7/06 , A61P3/10
CPC分类号: C07D409/10 , C07D309/10 , C07D309/12 , C07D409/14 , C07D417/14
摘要: The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.
摘要翻译: 本发明涉及一种制备具有抑制活性的化合物的新方法,所述化合物对存在于肠或肾中的钠依赖性葡萄糖转运蛋白(SGLT)具有抑制活性。
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公开(公告)号:US6048842A
公开(公告)日:2000-04-11
申请号:US993523
申请日:1997-12-18
申请人: Kenji Tsujihara , Kunio Saito , Mitsuya Hongu , Mamoru Matsumoto , Akira Oku
发明人: Kenji Tsujihara , Kunio Saito , Mitsuya Hongu , Mamoru Matsumoto , Akira Oku
IPC分类号: C07D401/12 , A61K31/4178 , A61P31/04 , C07H15/203 , C07H15/26 , A61K31/70 , C07H15/00
CPC分类号: C07H15/203 , C07H15/26 , Y02P20/55
摘要: A propiophenone derivative of the formula (I): ##STR1## wherein OX is a hydroxy group which may optionally be protected, Y is a lower alkyl group, and Z is a .beta.-D-glucopyranosyl group wherein one or more hydroxy groups may optionally be protected, or a pharmaceutically acceptable salt thereof. Said compounds have excellent hypoglycemic activity so that they are useful in the prophylaxis or treatment of diabetes.
摘要翻译: 式(I)的苯丙酮衍生物:其中OX是任选被保护的羟基,Y是低级烷基,Z是β-D-吡喃葡萄糖基,其中一个或多个羟基可以被任选地被保护, 或其药学上可接受的盐。 所述化合物具有优异的降血糖活性,因此它们可用于预防或治疗糖尿病。
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