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1. 发明授权

US08513202B2 Crystalline form of 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate 有权
标题翻译： 1-（β-D-吡喃葡萄糖基）-4-甲基-3- [5-（4-氟苯基）-2-噻吩甲基]苯半水合物的结晶形式
公开(公告)号：US08513202B2
公开(公告)日：2013-08-20
申请号：US13103557
申请日：2011-05-09
申请人： Sumihiro Nomura , Eiji Kawanishi
发明人： Sumihiro Nomura , Eiji Kawanishi
IPC分类号： A61K31/7034 , C07H7/04
CPC分类号： A61K31/7034 , C07H7/04
摘要： A novel crystal form of 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate, and having favorable characteristics, is characterized by its x-ray powder diffraction pattern and/or by its infra-red spectrum.
摘要翻译： 1-（β-D-吡喃葡萄糖基）-4-甲基-3- [5-（4-氟苯基）-2-噻吩甲基]苯半水合物的新晶体形式，具有良好的特性，其特征在于其X-射线粉末衍射图案和/或其红外光谱。

2. 发明申请

US20110105424A1 GLUCOPYRANOSIDE COMPOUND 有权
标题翻译：葡萄糖苷化合物
公开(公告)号：US20110105424A1
公开(公告)日：2011-05-05
申请号：US13005757
申请日：2011-01-13
申请人： Sumihiro NOMURA , Eiji Kawanishi , Kiichiro Ueta
发明人： Sumihiro NOMURA , Eiji Kawanishi , Kiichiro Ueta
IPC分类号： A61K31/70 , C07H19/00 , A61P3/10 , A61P17/02 , A61P7/00 , A61P9/00 , A61P3/04
CPC分类号： C07H19/048 , A61K45/06 , C07D405/04 , C07D409/04 , C07D409/10 , C07H19/06
摘要： A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); or a pharmaceutically acceptable salt thereof, or a prodrug thereof.
摘要翻译：下式的化合物：其中环A和环B是：（1）环A是任选取代的不饱和单环杂环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环，或任选取代的苯环，（2）环A是任选取代的苯环，环B是任选取代的不饱和单环杂环或任选取代的不饱和稠环杂双环，或（3）环A是任选取代的不饱和稠合杂双环环和环B独立地是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的苯环; X是碳原子或氮原子; Y为 - （CH 2）n - （n为1或2）; 或其药学上可接受的盐，或其前药。

3. 发明授权

US08969376B2 Pyrazolopyrimidine compounds and their use as PDE10 inhibitors 有权
标题翻译：吡唑并嘧啶化合物及其作为PDE10抑制剂的用途
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。

4. 发明申请

US20120058941A1 GLUCOPYRANOSIDE COMPOUND 有权
标题翻译：葡萄糖苷化合物
公开(公告)号：US20120058941A1
公开(公告)日：2012-03-08
申请号：US13174814
申请日：2011-07-01
申请人： Sumihiro NOMURA , Eiji Kawanishi , Kiichiro Ueta
发明人： Sumihiro NOMURA , Eiji Kawanishi , Kiichiro Ueta
IPC分类号： A61K31/7034 , A61K38/28 , A61K38/26 , A61P3/10 , A61P27/02 , A61P25/02 , A61P13/12 , A61P17/02 , A61P5/48 , A61P7/00 , A61P3/06 , A61P3/04 , A61P3/00 , A61P9/10 , A61P9/12 , A61P7/02 , A61K31/7056
CPC分类号： C07H19/048 , A61K45/06 , C07D405/04 , C07D409/04 , C07D409/10 , C07H19/06
摘要： A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); or a pharmaceutically acceptable salt thereof, or a prodrug thereof.
摘要翻译：下式的化合物：其中环A和环B是：（1）环A是任选取代的不饱和单环杂环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环，或任选取代的苯环，（2）环A是任选取代的苯环，环B是任选取代的不饱和单环杂环或任选取代的不饱和稠环杂双环，或（3）环A是任选取代的不饱和稠合杂双环环和环B独立地是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的苯环; X是碳原子或氮原子; Y为 - （CH 2）n - （n为1或2）; 或其药学上可接受的盐，或其前药。

5. 发明申请

US20080146515A1 Crystalline form of 1-(beta-D-glucopyransoyl)-4-methyl-3-[5-(4-fluorophenyl)-2- thienylmethyl]benzene hemihydrate 有权
标题翻译： 1-（β-D-吡喃葡萄糖基）-4-甲基-3- [5-（4-氟苯基）-2-噻吩甲基]苯半水合物的结晶形式
公开(公告)号：US20080146515A1
公开(公告)日：2008-06-19
申请号：US11987670
申请日：2007-12-03
申请人： Sumihiro Nomura , Eiji Kawanishi
发明人： Sumihiro Nomura , Eiji Kawanishi
IPC分类号： A61K31/7042 , C07H7/06 , A61P3/12 , A61P3/06 , A61P3/00
CPC分类号： A61K31/7034 , C07H7/04
摘要： A novel crystal form of 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate, and having favorable characteristics, is characterized by its x-ray powder diffraction pattern and/or by its infra-red spectrum.
摘要翻译： 1-（β-D-吡喃葡萄糖基）-4-甲基-3- [5-（4-氟苯基）-2-噻吩甲基]苯半水合物的新晶体形式，具有良好的特性，其特征在于其X-射线粉末衍射图案和/或其红外光谱。

6. 发明授权

US06652599B1 Treatment agent for elastic polyurethane fibers and elastic polyurethane fibers treated therewith 失效
标题翻译：弹性聚氨酯纤维和经过处理的弹性聚氨酯纤维的处理剂
公开(公告)号：US06652599B1
公开(公告)日：2003-11-25
申请号：US09639619
申请日：2000-08-15
申请人： Yoshinobu Inuzuka , Yasushi Miyamoto , Eiji Kawanishi , Noboru Watanabe
发明人： Yoshinobu Inuzuka , Yasushi Miyamoto , Eiji Kawanishi , Noboru Watanabe
IPC分类号： D06M1100
CPC分类号： D06M15/6436 , D06M7/00 , D06M13/188 , D06M13/192 , D06M15/6433 , D06M2101/38 , D06M2200/40 , Y10S8/01 , Y10T428/2913
摘要： A treatment agent for elastic polyurethane fibers comprising a dispersion in which a higher fatty acid magnesium salt is colloidally dispersed in a silicone mixture consisting of a silicone oil with a viscosity of 5×10−6−50×10−6 m2/S at 25° C. as a dispersion medium and a dispersant mainly comprising a modified silicone at a ratio by weight of the dispersion medium/the dispersant=100/0.5-100/4.5, wherein the amount of the higher fatty acid magnesium salt is 1 to 10 parts by weight per 100 parts by weight of the silicone oil.
摘要翻译：一种用于弹性聚氨酯纤维的处理剂，其包含将高分子量脂肪酸镁盐胶体地分散在由硅油组成的硅氧烷混合物中的分散体，所述硅氧烷混合物的粘度为5×10 -6 -50×10 -6 m 2 / S为分散介质，分散剂主要含有改性硅酮，分散介质/分散剂的重量比= 100 / 0.5-100 / 4.5，其中高级脂肪酸镁盐为相对于100重量份硅油为1〜10重量份。

7. 发明授权

US06171516B2 Treatment agent for elastic polyurethane fibers, and elastic polyurethane fibers treated therewith 有权
标题翻译：弹性聚氨酯纤维的处理剂和用其处理的弹性聚氨酯纤维
公开(公告)号：US06171516B2
公开(公告)日：2001-01-09
申请号：US09180256
申请日：1998-11-06
申请人： Yoshinobu Inuzuka , Yasushi Miyamoto , Eiji Kawanishi , Noboru Watanabe
发明人： Yoshinobu Inuzuka , Yasushi Miyamoto , Eiji Kawanishi , Noboru Watanabe
IPC分类号： D06M13184
CPC分类号： D06M15/6436 , D06M7/00 , D06M13/188 , D06M13/192 , D06M15/6433 , D06M2101/38 , D06M2200/40 , Y10S8/01 , Y10T428/2913
摘要： A treatment agent for elastic polyurethane fibers comprising a dispersion in which a higher fatty acid magnesium salt is colloidally dispersed in a silicone mixture consisting of a silicone oil with a viscosity of 5×10−6−50×10−6 m2/S at 25° C. as a dispersion medium and a dispersant mainly comprising a modified silicone at a ratio by weight of the dispersion medium/the dispersant=100/0.5−100/4.5, wherein the amount of the higher fatty acid magnesium salt is 1 to 10 parts by weight per 100 parts by weight of the silicone oil.
摘要翻译：一种用于弹性聚氨酯纤维的处理剂，其包含将高分子量脂肪酸镁盐胶体分散在由25℃粘度为5×10-6-50×10-6m2 / S的硅油组成的硅氧烷混合物中的分散体，作为主要包含改性硅酮的分散介质和分散剂，分散介质/分散剂的重量比= 100 / 0.5-100 / 4.5，其中高级脂肪酸镁盐的量为1至10重量份 100重量份的硅油。

8. 发明申请

US20120258913A1 GLUCOPYRANOSIDE COMPOUND 有权
公开(公告)号：US20120258913A1
公开(公告)日：2012-10-11
申请号：US13494602
申请日：2012-06-12
申请人： Sumihiro NOMURA , Eiji KAWANISHI , Kiichiro UETA
发明人： Sumihiro NOMURA , Eiji KAWANISHI , Kiichiro UETA
IPC分类号： A61K31/7042 , A61P3/10 , A61K38/26 , A61K31/7056 , A61K38/28
CPC分类号： C07H19/056 , A61K31/7042 , A61K31/7056 , A61K38/24 , A61K38/28 , A61K45/06 , C07H7/04 , C07H7/06 , C07H19/04 , C07H19/044 , C07H19/048 , A61K2300/00
摘要： A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); or a pharmaceutically acceptable salt thereof, or a prodrug thereof.

9. 发明申请

US20110212905A1 CRYSTALLINE FORM OF 1-(BETA-D-GLUCOPYRANOSYL)-4-METHYL-3-[5-(4-FLUOROPHENYL)-2-THIENYLMETHYL]BENZENE HEMIHYDRATE 有权
标题翻译： 1-（β-D-吡喃葡糖基）-4-甲基-3- [5-（4-氟苯基）-2-甲苯基]苯甲酸乙酯的晶体形式
公开(公告)号：US20110212905A1
公开(公告)日：2011-09-01
申请号：US13103557
申请日：2011-05-09
申请人： Sumihiro Nomura , Eiji Kawanishi
发明人： Sumihiro Nomura , Eiji Kawanishi
IPC分类号： A61K31/7042 , C07H7/06 , A61P3/10 , A61P3/06 , A61P17/02 , A61P3/04 , A61P9/10 , A61P9/12
CPC分类号： A61K31/7034 , C07H7/04
摘要： A novel crystal form of 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate, and having favorable characteristics, is characterized by its x-ray powder diffraction pattern and/or by its infra-red spectrum.
摘要翻译：具有良好特性的1 - （＆bgr。-D-吡喃葡萄糖基）-4-甲基-3- [5-（4-氟苯基）-2-噻吩甲基]苯半水合物的新晶体形式的特征在于其X-射线粉末衍射图案和/或其红外光谱。

10. 发明申请

US20110166135A1 AROMATIC NITROGEN-CONTAINING 6-MEMBERED RING COMPOUNDS AND THEIR USE 审中-公开
标题翻译：含有硝酸的六元环化合物及其用途
公开(公告)号：US20110166135A1
公开(公告)日：2011-07-07
申请号：US13062841
申请日：2009-09-09
申请人： Hiroshi Morimoto , Toshiaki Sakamoto , Toshiyuki Himiyama , Eiji Kawanishi , Takehiko Matsumura
发明人： Hiroshi Morimoto , Toshiaki Sakamoto , Toshiyuki Himiyama , Eiji Kawanishi , Takehiko Matsumura
IPC分类号： A61K31/5377 , C07D401/14 , C07D487/04 , C07D413/14 , A61K31/517 , A61K31/506 , A61K31/497 , A61K31/519 , A61P25/18 , A61P25/24 , A61P25/22 , A61P25/16 , A61P25/28
CPC分类号： C07D401/14 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12
摘要： The present invention provides aromatic nitrogen-containing 6-membered ring compounds having excellent PDE10 inhibitory activity. The present invention relates to an aromatic nitrogen-containing 6-membered ring compound represented by the following formula [I0] or a pharmaceutically acceptable salt thereof, a method for preparing the same, and use of said compounds for PDE10 inhibitors, and a pharmaceutical composition comprising said compounds as an active ingredient: Formula [I0] wherein: X1, X2 and X3 each independently are N or CH, and at least two of X1, X2 and X3 are N; A is *—CH═CH—, *—C(Alk)=CH—, *—CH2—CH2— or *—O—CH2— (* is a bond with R1); Alk is a lower alkyl group; Ring B is an optionally substituted nitrogen-containing aliphatic heterocyclic group; R1 is an optionally substituted nitrogen-containing heterocyclic group, a nitrogen-containing heterocyclic moiety of which is a moiety selected from the group consisting of quinoxalinyl, quinolyl, isoquinolyl, quinazolinyl, pyrazinyl, pyrimidinyl and a moiety thereof fused with a 5 to 6-membered aliphatic ring thereto; Y0 is a group selected from the group consisting of the following (1) to (5): (1) an optionally substituted phenyl or an optionally substituted aromatic monocyclic 5 to 6-membered heterocyclic group; (2) an optionally substituted aminocarbonyl; (3) an optionally substituted amino lower alkyl; (4) —O—R2 wherein R2 is hydrogen, an optionally substituted lower alkyl, lower cycloalkyl, aliphatic monocyclic 5 to 6-membered heterocyclic group, or Formula [AA]; (5) mono- or di-substituted amino; provided that, when Y0 is mono- or di-substituted amino, the nitrogen-containing heterocyclic moiety of R1 is not quinoxalinyl or quinolyl.
摘要翻译：本发明提供具有优异的PDE10抑制活性的芳香族含氮6元环化合物。本发明涉及由下式[I0]表示的含芳族含氮的6元环化合物或其药学上可接受的盐，其制备方法以及所述化合物用于PDE10抑制剂的用途和药物组合物包括所述化合物作为活性成分：式[I0]其中：X1，X2和X3各自独立地为N或CH，X1，X2和X3中的至少两个为N; A是* -CH = CH-，* -C（Alk）= CH-，* -CH2-CH2-或* -O-CH2-（*是与R1的键）; Alk是低级烷基; 环B是任选取代的含氮脂族杂环基; R1是任选取代的含氮杂环基团，其含氮杂环部分是选自喹喔啉基，喹啉基，异喹啉基，喹唑啉基，吡嗪基，嘧啶基及其部分与5至6位稠合的部分，元环脂族环; Y0是选自下列（1）至（5）的基团：（1）任选取代的苯基或任选取代的芳族单环5至6元杂环基; （2）任选取代的氨基羰基; （3）任选取代的氨基低级烷基; （4）-O-R2，其中R2是氢，任选取代的低级烷基，低级环烷基，脂族单环5至6元杂环基或式[AA]; （5）单取代或二取代氨基; 条件是当Y 0是单取代或二取代的氨基时，R 1的含氮杂环部分不是喹喔啉基或喹啉基。

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