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11. 发明授权

US07060832B2 Nitrogen-containing fused heterocyclic carboxylic acids having an absolute configuration of “R” 失效
标题翻译：具有绝对构型“R”的含氮稠合杂环羧酸
公开(公告)号：US07060832B2
公开(公告)日：2006-06-13
申请号：US10118920
申请日：2002-04-10
申请人： Takayuki Kawaguchi , Sumihiro Nomura , Kenji Tsujihara
发明人： Takayuki Kawaguchi , Sumihiro Nomura , Kenji Tsujihara
IPC分类号： C07D215/58
CPC分类号： C07D491/14 , C07B2200/07 , C07D209/42 , C07D217/26
摘要： Nitrogen-containing fused heterocyclic carboxylic acid having an absolute configuration of “R” of the formula [XIX]: wherein Y is substituted or unsubstituted arylsulfonyl group or an alkylsulfonyl group, and n is 0 or 1, or a salt thereof.
摘要翻译：具有式[XIX]的绝对构型“R”的含氮稠合杂环羧酸：其中Y为取代或未取代的芳基磺酰基或烷基磺酰基，n为0或1，或其盐。

12. 发明授权

US06716983B2 S type 2-substituted hydroxy-2-indolidinylbutyric ester compounds and process for preparation thereof 失效
标题翻译： S型2-取代羟基-2-吲哚哩啶基丁酸酯化合物及其制备方法
公开(公告)号：US06716983B2
公开(公告)日：2004-04-06
申请号：US10337476
申请日：2003-01-08
申请人： Takayuki Kawaguchi , Sumihiro Nomura , Kenji Tsujihara
发明人： Takayuki Kawaguchi , Sumihiro Nomura , Kenji Tsujihara
IPC分类号： C07D49120
CPC分类号： C07D491/14 , C07B2200/07 , C07D209/42 , C07D217/26
摘要： A process for preparing S type 2-substituted hydroxy-2-indolidinylbutyric ester compound [II]: wherein Ro is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of “R” (in which the nitrogen atom is protected), R1 and R2 are lower alkyl groups, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound [I]: wherein the symbols are as defined above.
摘要翻译：制备S型2-取代羟基-2-吲哚哩啶基丁酸酯化合物[II]的方法：其中R 0是具有绝对构型“R”（其中氮原子被保护的）的含氮稠合杂环羧酸的残基），R1和R2是低级烷基，E是酯残基，其可用作制备具有抗肿瘤活性的喜树碱衍生物的中间体，其包括2-乙基化2-取代的羟基-2-吲哚哩啶基乙酸酯化合物[I]：其中符号如上所述。

13. 发明授权

US6114529A S type 2-substituted hydroxy-2-indolidinylbutyric ester compounds and process for preparation thereof 失效
公开(公告)号：US6114529A
公开(公告)日：2000-09-05
申请号：US421335
申请日：1999-10-18
申请人： Takayuki Kawaguchi , Sumihiro Nomura , Kenji Tsujihara
发明人： Takayuki Kawaguchi , Sumihiro Nomura , Kenji Tsujihara
IPC分类号： C07D487/04 , A61K31/436 , A61K31/4375 , C07D209/42 , C07D217/26 , C07D471/10 , C07D471/12 , C07D471/20 , C07D471/22 , C07D491/14 , C07D491/147 , C07D491/20 , C07D491/22
CPC分类号： C07D491/14 , C07D209/42 , C07D217/26 , C07B2200/07
摘要： A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound [II]: ##STR1## wherein R.sup.0 is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of "R"(in which the nitrogen atom is protected), R.sup.1 and R.sup.2 are lower alkyl group, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound [I]: ##STR2## wherein the symbols are as defined above.

14. 发明授权

US5932732A S type 2-substituted hydroxy-2-indolidinylbutyric ester compounds and process for preparation thereof 失效
标题翻译： S型2-取代羟基-2-吲哚哩啶基丁酸酯化合物及其制备方法
公开(公告)号：US5932732A
公开(公告)日：1999-08-03
申请号：US958979
申请日：1997-10-28
申请人： Takayuki Kawaguchi , Sumihiro Nomura , Kenji Tsujihara
发明人： Takayuki Kawaguchi , Sumihiro Nomura , Kenji Tsujihara
IPC分类号： C07D487/04 , A61K31/436 , A61K31/4375 , C07D209/42 , C07D217/26 , C07D471/10 , C07D471/12 , C07D471/20 , C07D471/22 , C07D491/14 , C07D491/147 , C07D491/20 , C07D491/22
CPC分类号： C07D491/14 , C07D209/42 , C07D217/26 , C07B2200/07
摘要： A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound �II!: ##STR1## wherein R.sup.o is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of "R"(in which the nitrogen atom is protected), R.sup.1 and R.sup.2 are lower alkyl group, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound �I!: ##STR2## wherein the symbols are as defined above.
摘要翻译：制备S型2-取代羟基-2-吲哚哩啶基 - 丁酸酯化合物[II]的方法：其中Ro是具有绝对构型“R”（其中保护氮原子）的含氮稠合杂环羧酸的残基， R 1和R 2为低级烷基，E为酯残基，其可用作制备具有抗肿瘤活性的喜树碱衍生物的中间体，其包括2-乙基化2-取代的羟基-2-吲哚哩啶基乙酸酯化合物[I]：其中符号如上所述。

15. 发明授权

US06277992B1 S type 2-substituted hydroxy-2-indolidinylbutyric ester compounds and process for preparation thereof 失效
标题翻译： S型2-取代羟基-2-吲哚哩啶基丁酸酯化合物及其制备方法
公开(公告)号：US06277992B1
公开(公告)日：2001-08-21
申请号：US09570172
申请日：2000-05-12
申请人： Takayuki Kawaguchi , Sumihiro Nomura , Kenji Tsujihara
发明人： Takayuki Kawaguchi , Sumihiro Nomura , Kenji Tsujihara
IPC分类号： C07D47112
CPC分类号： C07D491/14 , C07B2200/07 , C07D209/42 , C07D217/26
摘要： A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound [II]: wherein R0 is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of “R”(in which the nitrogen atom is protected), R1 and R2 are lower alkyl group, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound [I]: wherein the symbols are as defined above.
摘要翻译：一种制备S型2-取代羟基-2-吲哚哩啶基 - 丁酸酯化合物[II]的方法：其中R 0是具有绝对构型“R”（其中保护氮原子）的含氮稠合杂环羧酸的残基， R 1和R 2为低级烷基，E为酯残基，其可用作制备具有抗肿瘤活性的喜树碱衍生物的中间体，其包括2-乙基化2-取代的羟基-2-吲哚哩啶基乙酸酯化合物[I]：其中符号如上所述。

16. 发明授权

US09522931B2 Process for the preparation of compounds useful as inhibitors of SGLT-2 有权
标题翻译：制备可用作SGLT-2抑制剂的化合物的方法
公开(公告)号：US09522931B2
公开(公告)日：2016-12-20
申请号：US14118643
申请日：2012-05-18
申请人： Kenneth M. Wells , Ronald K. Russell , Xun Li , Shawn Branum , Derek A. Beauchamp , Sumihiro Nomura , Yosuke Matsumura
发明人： Kenneth M. Wells , Ronald K. Russell , Xun Li , Shawn Branum , Derek A. Beauchamp , Sumihiro Nomura , Yosuke Matsumura
IPC分类号： C07H19/044 , C07D407/04
CPC分类号： C07H19/044 , C07D407/04
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。

17. 发明申请

US20080027014A1 Novel SGLT inhibitors 审中-公开
标题翻译：新型SGLT抑制剂
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。

18. 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。

19. 发明授权

US07521430B2 N-glucoside compounds having an inhibitory activity against sodium-dependent glucose transporter 失效
标题翻译：对钠依赖性葡萄糖转运蛋白具有抑制活性的N-葡萄糖苷化合物
公开(公告)号：US07521430B2
公开(公告)日：2009-04-21
申请号：US10566585
申请日：2004-07-30
申请人： Sumihiro Nomura , Toshiaki Sakamoto , Kiichiro Ueta
发明人： Sumihiro Nomura , Toshiaki Sakamoto , Kiichiro Ueta
IPC分类号： A01N43/04 , A61K31/70 , C07H5/06 , C07H19/00
CPC分类号： C07H15/203 , C07H5/04 , C07H17/02
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, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, wherein —NR— group and —CH2— group are both on the same ring of the unsaturated fused heterobicyclic ring, and Ring B is an optionally substituted monocyclic unsaturated heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; and R is a hydrogen atom, a lower alkyl group, a lower alkanoyl group or a lower alkoxycarbonyl group, 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地取代的苯环，（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，任选取代的不饱和稠合杂双环或任选取代的苯环，或（3）环A是任选取代的不饱和稠合杂双环，其中-NR-基和-CH2-基都在不饱和稠合杂双环的相同环上，环B是任选取代的单环不饱和杂环，任选取代的不饱和稠合杂双环，或任选取代的苯环; 或其前体药物，R为氢原子，低级烷基，低级烷酰基或低级烷氧基羰基，或其药学上可接受的盐。

20. 发明申请

US20080027122A1 Indole derivatives 有权
标题翻译：吲哚衍生物
公开(公告)号：US20080027122A1
公开(公告)日：2008-01-31
申请号：US11878760
申请日：2007-07-26
申请人： Sumihiro Nomura , Shigeki Sakamaki
发明人： Sumihiro Nomura , Shigeki Sakamaki
IPC分类号： A61K31/40 , A61P3/00 , C07D209/04
CPC分类号： C07H19/04
摘要： Novel indole derivatives of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is fluorine, or chlorine, and R2 is hydrogen, or fluorine, which are SGLT inhibitors and are useful for treatment or prevention of diabetes and related conditions.
摘要翻译：式（I）的新型吲哚衍生物或其药学上可接受的盐：其中R 1是氟或氯，R 2是氢或氟，它们是SGLT 抑制剂，可用于治疗或预防糖尿病及相关病症。

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