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71. 发明申请

US20160130227A1 PRODRUGS OF ANTI-PLATELET AGENTS 审中-公开
标题翻译：抗药剂原料
公开(公告)号：US20160130227A1
公开(公告)日：2016-05-12
申请号：US14859377
申请日：2015-09-21
申请人： Cellix Bio Private Limited
发明人： Mahesh Kandula
IPC分类号： C07D211/54 , C07D513/04
CPC分类号： C07D211/54 , C07D211/72 , C07D495/04 , C07D513/04
摘要： The invention relates to the compounds of formula II, formula Ia, formula IIa or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula II, formula Ia, formula IIa and methods for treating or preventing atherothrombosis may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment or management of ischemia, stroke, cerebral thrombosis, arterial thrombosis, thrombotic cerebrovascular, cardiovascular diseases and blood clots.
摘要翻译：本发明涉及式II，式Ia，式IIa化合物或其药学上可接受的盐，以及其多晶型物，溶剂合物，对映体，立体异构体和水合物。包含有效量的式II，式Ia，式IIa的化合物和用于治疗或预防动脉粥样硬化血栓形成的方法的药物组合物可以配制用于口服，口腔，直肠，局部，透皮，经粘膜，静脉内，肠胃外给药，糖浆或注射。这样的组合物可用于治疗或治疗缺血，中风，脑血栓形成，动脉血栓形成，血栓性脑血管，心血管疾病和血块。

72. 发明授权

US09221855B2 Thionation process and a thionating agent 有权
标题翻译：硫化过程和硫化剂
公开(公告)号：US09221855B2
公开(公告)日：2015-12-29
申请号：US13807104
申请日：2012-02-03
申请人： Birgitta Pettersson , Vedran Hasimbegovic , Per H Svensson , Jan Bergman
发明人： Birgitta Pettersson , Vedran Hasimbegovic , Per H Svensson , Jan Bergman
IPC分类号： C07C325/02 , C07C327/48 , C07F9/58 , C07B45/06 , C07B45/04 , C07D207/24 , C07D209/30 , C07D211/72 , C07D211/84 , C07D213/63 , C07D239/93 , C07D213/83 , C07D309/36 , C07D215/36 , C07D311/84 , C07D219/04 , C07D219/08 , C07D223/06 , C07D341/00 , C07D239/58 , C07D241/08 , C07D241/44 , C07D243/22 , C07D245/04 , C07D471/04 , C07D473/36 , C07D487/04 , C07D207/416 , C07D209/08 , C07D209/34 , C07D209/42 , C07D209/88 , C07D213/70 , C07D211/88 , C07D239/70 , C07D243/14 , C07B45/00
CPC分类号： C07F9/58 , C07B45/00 , C07B45/04 , C07C325/02 , C07C327/48 , C07D207/24 , C07D207/416 , C07D209/08 , C07D209/30 , C07D209/34 , C07D209/42 , C07D209/88 , C07D211/72 , C07D211/84 , C07D211/88 , C07D213/63 , C07D213/70 , C07D213/83 , C07D215/36 , C07D219/04 , C07D219/08 , C07D223/06 , C07D239/58 , C07D239/70 , C07D239/93 , C07D241/08 , C07D241/44 , C07D243/14 , C07D243/22 , C07D245/04 , C07D309/36 , C07D311/84 , C07D341/00 , C07D471/04 , C07D473/36 , C07D487/04
摘要： A process for transforming a group >C═O (I) in a compound into a group >C═S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline P2S5.2 C5H5N as a thionating agent. A thionating agent which is crystalline P2S5.2 C5H5N.
摘要翻译：在通过使用结晶P2S5的反应中将化合物中的基团> C = O（I）转化为基团> C = S（II）或互变异构形式的基团（II）的方法，得到硫化反应产物 .2 C5H5N作为硫化剂。结晶P2S5.2 C5H5N的硫化剂。

73. 发明申请

US20150353492A1 MIXED DISULFIDE CONJUGATES OF THIENOPYRIDINE COMPOUNDS AND USES THEREOF 有权
标题翻译：三烯吡啶化合物的混合的共聚物及其用途
公开(公告)号：US20150353492A1
公开(公告)日：2015-12-10
申请号：US14758736
申请日：2014-01-06
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN
发明人： Haoming Zhang , Paul Hollenberg
IPC分类号： C07D211/72 , C07D405/12 , C07K5/093 , A61K31/445 , A61K47/48 , A61K31/4545 , A61K31/4525 , A61K38/06 , A61K45/06 , C07D401/12 , A61K31/501
CPC分类号： C07D211/72 , A61K31/445 , A61K31/4525 , A61K31/4545 , A61K31/501 , A61K38/06 , A61K45/06 , A61K47/54 , A61K47/542 , A61K47/545 , A61K47/64 , A61P9/00 , C07D401/12 , C07D405/12 , C07K5/0819 , A61K2300/00
摘要： This invention is in the field of medicinal chemistry. In particular, the invention relates to mixed disulfide conjugates of thienopyridine compounds, and their use as therapeutics for the treatment, amelioration, and prevention of cardiovascular diseases.
摘要翻译：本发明在医药化学领域。特别地，本发明涉及噻吩并吡啶化合物的混合二硫键，以及它们作为治疗，改善和预防心血管疾病的治疗剂的用途。

74. 发明授权

US09115158B2 Thionating agent 有权
公开(公告)号：US09115158B2
公开(公告)日：2015-08-25
申请号：US13936423
申请日：2013-07-08
申请人： VIRONOVA THIONATION AB
发明人： Birgitta Pettersson , Vedran Hasimbegovic , Per H Svensson , Jan Bergman
IPC分类号： C07B45/00 , C07F9/58 , C07B45/04 , C07C325/02 , C07C327/48 , C07D207/24 , C07D209/30 , C07D211/72 , C07D211/84 , C07D213/63 , C07D239/93 , C07D213/83 , C07D309/36 , C07D215/36 , C07D311/84 , C07D219/04 , C07D219/08 , C07D223/06 , C07D341/00 , C07D239/58 , C07D241/08 , C07D241/44 , C07D243/22 , C07D245/04 , C07D471/04 , C07D473/36 , C07D487/04 , C07D207/416 , C07D209/08 , C07D209/34 , C07D209/42 , C07D209/88 , C07D213/70 , C07D211/88 , C07D239/70 , C07D243/14
CPC分类号： C07F9/58 , C07B45/00 , C07B45/04 , C07C325/02 , C07C327/48 , C07D207/24 , C07D207/416 , C07D209/08 , C07D209/30 , C07D209/34 , C07D209/42 , C07D209/88 , C07D211/72 , C07D211/84 , C07D211/88 , C07D213/63 , C07D213/70 , C07D213/83 , C07D215/36 , C07D219/04 , C07D219/08 , C07D223/06 , C07D239/58 , C07D239/70 , C07D239/93 , C07D241/08 , C07D241/44 , C07D243/14 , C07D243/22 , C07D245/04 , C07D309/36 , C07D311/84 , C07D341/00 , C07D471/04 , C07D473/36 , C07D487/04
摘要： A process for transforming a group >C═O (I) in a compound into a group >C═S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline P2S5.2C5H5N as a thionating agent. A thionating agent which is crystalline P2S5.2C5H5N.
摘要翻译：在通过使用结晶P2S5的反应中将化合物中的基团> C = O（I）转化为基团> C = S（II）或互变异构形式的基团（II）的方法，得到硫化反应产物 .2C5H5N作为硫化剂。结晶P2S5.2C5H5N的硫化剂。

75. 发明授权

US09085606B2 Beta amino acid derivatives as integrin antagonists 有权
标题翻译： β氨基酸衍生物作为整合素拮抗剂
公开(公告)号：US09085606B2
公开(公告)日：2015-07-21
申请号：US13944599
申请日：2013-07-17
申请人： Saint Louis University
发明人： Peter Ruminski , David Griggs
IPC分类号： C07K5/06 , C07D403/12 , C07D309/06 , C07D309/08 , C07C279/18 , C07D233/50 , C07D401/12 , C07D239/16 , C07D405/12 , C07D211/72
CPC分类号： C07K5/06 , C07C279/18 , C07D211/72 , C07D233/50 , C07D239/16 , C07D309/06 , C07D309/08 , C07D401/12 , C07D403/12 , C07D405/12
摘要： Disclosed herein are novel pharmaceutical agents which are useful as integrin receptor antagonists that mediate the pathologic processes of angiogenesis and fibrosis and as such are useful in pharmaceutical compositions and in methods for treating conditions mediated by these integrins by inhibiting or antagonizing these integrins. The novel pharmaceutical agents include those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods and intermediates useful for making the pharmaceutical agents and methods of using the pharmaceutical agents are also provided.
摘要翻译：本文公开了可用作介导血管生成和纤维化的病理过程的整联蛋白受体拮抗剂的新型药剂，因此可用于药物组合物和通过抑制或拮抗这些整联蛋白来治疗由这些整联蛋白介导的病症的方法。新型药剂包括下式的化合物：其中变量在本文中定义。还提供了包含这种药剂的药物组合物，试剂盒和制品。还提供了可用于制备药剂的方法和中间体以及使用药剂的方法。

76. 发明授权

US09045444B2 Apoptosis promoters 有权
标题翻译：凋亡启动子
公开(公告)号：US09045444B2
公开(公告)日：2015-06-02
申请号：US14195666
申请日：2014-03-03
申请人： AbbVie Inc.
发明人： Hong Ding , Christopher L. Lynch , Xiaohong Song , Xilu Wang , Michael D. Wendt
IPC分类号： C07D451/02 , C07D205/04 , C07D207/04 , C07D211/20 , C07D213/38 , C07D215/12 , C07D231/12 , C07D233/06 , C07D239/38 , C07D241/04 , C07D249/18 , C07D401/10 , C07D295/155 , C07D207/06 , C07D207/08 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/20 , C07D207/24 , C07D207/50 , C07D211/14 , C07D211/26 , C07D211/34 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/58 , C07D211/62 , C07D211/70 , C07D211/72 , C07D213/36 , C07D213/42 , C07D213/70 , C07D213/74 , C07D213/81 , C07D213/82 , C07D231/56 , C07D233/61 , C07D233/64 , C07D235/08 , C07D239/06 , C07D257/04 , C07D261/20 , C07D263/12 , C07D263/22 , C07D263/58 , C07D265/30 , C07D267/10 , C07D273/01 , C07D277/36 , C07D277/74 , C07D295/185 , C07D295/30 , C07D307/14 , C07D307/22 , C07D307/81 , C07D309/14 , C07D309/20 , C07D317/66 , C07D333/20 , C07D333/34 , C07D335/02 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/10 , C07D413/04 , C07D471/08 , C07D487/04 , C07D487/08 , C07D491/04 , C07D491/08 , C07D498/08 , C07C311/51 , C07D207/09 , C07D209/02 , C07D233/24 , C07D239/20 , C07D277/04 , C07D491/048 , C07D209/52 , C07D233/22
CPC分类号： C07D295/155 , C07C311/51 , C07D205/04 , C07D207/06 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/20 , C07D207/24 , C07D207/50 , C07D209/02 , C07D209/52 , C07D211/14 , C07D211/20 , C07D211/26 , C07D211/34 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/58 , C07D211/62 , C07D211/70 , C07D211/72 , C07D213/36 , C07D213/38 , C07D213/42 , C07D213/70 , C07D213/74 , C07D213/81 , C07D213/82 , C07D215/12 , C07D231/12 , C07D231/56 , C07D233/06 , C07D233/22 , C07D233/24 , C07D233/61 , C07D233/64 , C07D235/08 , C07D239/06 , C07D239/20 , C07D239/38 , C07D241/04 , C07D249/18 , C07D257/04 , C07D261/20 , C07D263/12 , C07D263/22 , C07D263/58 , C07D265/30 , C07D267/10 , C07D273/01 , C07D277/04 , C07D277/36 , C07D277/74 , C07D295/185 , C07D295/30 , C07D307/14 , C07D307/22 , C07D307/81 , C07D309/14 , C07D309/20 , C07D317/66 , C07D333/20 , C07D333/34 , C07D335/02 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/10 , C07D413/04 , C07D451/02 , C07D471/08 , C07D487/04 , C07D487/08 , C07D491/04 , C07D491/048 , C07D491/08 , C07D498/08
摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
摘要翻译：公开了抑制抗凋亡蛋白家族成员的活性的化合物，含有化合物的组合物和该化合物用于制备用于治疗疾病的药物的用途，其中发生表达一种或多种抗凋亡蛋白家族成员。

77. 发明授权

US08796299B2 NK1 antagonists 有权
标题翻译： NK1拮抗剂
公开(公告)号：US08796299B2
公开(公告)日：2014-08-05
申请号：US13625799
申请日：2012-09-24
申请人： OPKO Health, Inc.
发明人： Sunil Paliwal , Gregory A. Reichard , Cheng Wang , Dong Xiao , Hon-Chung Tsui , Neng-Yang Shih , Juan D. Arredondo , Michelle Laci Wrobleski , Anandan Palani
IPC分类号： A61K31/44
CPC分类号： C07D498/10 , A61K31/166 , A61K31/40 , A61K31/4025 , A61K31/437 , A61K31/4375 , A61K31/438 , A61K31/451 , A61K31/454 , A61K31/4545 , A61K31/537 , A61K31/5377 , A61K31/573 , A61K45/06 , C07D207/14 , C07D207/50 , C07D211/28 , C07D211/32 , C07D211/42 , C07D211/56 , C07D211/60 , C07D211/72 , C07D211/76 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D413/10 , C07D413/12 , C07D471/10 , C07D487/10 , C07D491/10 , C07D513/10
摘要： A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
摘要翻译：具有式（I）的NK1拮抗剂，其中Ar1和Ar2是任选取代的苯基或杂芳基，X1是醚，硫代或亚氨基键，R4和R5不都是H或烷基，其余的变量如规范，用于治疗许多疾病，包括呕吐，抑郁，焦虑和咳嗽。药物组合物。还公开了治疗方法和与其它药剂的组合。

78. 发明授权

US08680100B2 Sulfonylhydrazide compounds for treating proliferative disorders 失效
标题翻译：用于治疗增殖性疾病的磺酰肼化合物
公开(公告)号：US08680100B2
公开(公告)日：2014-03-25
申请号：US13132106
申请日：2009-12-01
申请人： Jun Jiang , Teresa Kowalczyk-Przewloka , Stefan M. Schweizer , Zhi-Qiang Xia , Shoujun Chen , Christopher Borella , Lijun Sun
发明人： Jun Jiang , Teresa Kowalczyk-Przewloka , Stefan M. Schweizer , Zhi-Qiang Xia , Shoujun Chen , Christopher Borella , Lijun Sun
IPC分类号： A61K31/5375 , A61K31/4965 , A61K31/445 , A61K31/4409 , A61K31/426 , A61K31/421 , A61K31/402 , A61K31/381 , A61K31/357 , A61K31/341 , A61K31/27 , A61K31/16 , C07D295/215 , C07D241/28 , C07D211/98 , C07D213/78 , C07D277/56 , C07D263/34 , C07D207/12 , C07D333/68 , C07D317/46 , C07D307/68 , C07C333/12 , C07C327/18 , A61P35/00
CPC分类号： C07D295/195 , C07C327/56 , C07C333/12 , C07C335/40 , C07C337/02 , C07C337/06 , C07C2601/02 , C07C2601/04 , C07D211/72 , C07D213/86 , C07D213/87 , C07D241/24 , C07D277/56 , C07D295/155 , C07D307/68 , C07D317/68 , C07D333/38 , C07D333/68
摘要： The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.
摘要翻译：本发明涉及由结构式（I）表示的化合物或其药学上可接受的盐或过渡金属螯合物，其配位体或络合物或过渡金属螯合物，化合物去质子化形式的配位体或络合物。也包括这些化合物的药物组合物和使用方法。

79. 发明申请

US20130303767A1 THIONATING AGENT 有权
标题翻译：代理代理
公开(公告)号：US20130303767A1
公开(公告)日：2013-11-14
申请号：US13936423
申请日：2013-07-08
申请人： VIRONOVA AB
发明人： Birgitta PETTERSSON , Vedran HASIMBEGOVIC , Per H SVENSSON , Jan BERGMAN
IPC分类号： C07F9/58
CPC分类号： C07F9/58 , C07B45/00 , C07B45/04 , C07C325/02 , C07C327/48 , C07D207/24 , C07D207/416 , C07D209/08 , C07D209/30 , C07D209/34 , C07D209/42 , C07D209/88 , C07D211/72 , C07D211/84 , C07D211/88 , C07D213/63 , C07D213/70 , C07D213/83 , C07D215/36 , C07D219/04 , C07D219/08 , C07D223/06 , C07D239/58 , C07D239/70 , C07D239/93 , C07D241/08 , C07D241/44 , C07D243/14 , C07D243/22 , C07D245/04 , C07D309/36 , C07D311/84 , C07D341/00 , C07D471/04 , C07D473/36 , C07D487/04
摘要： A process for transforming a group >C═O (I) in a compound into a group >C═S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline P2S5.2 C5H5N as a thionating agent. A thionating agent which is crystalline P2S5.2 C5H5N.
摘要翻译：在化合物中将C = O（I）的基团转化成组> C = S（II）的基团或通过使用结晶P2S5在产生硫酸化反应产物的反应中变成互变异构形式的基团（II）的方法 .2 C5H5N作为硫化剂。结晶P2S5.2 C5H5N的硫化剂。

80. 发明授权

US08173811B2 Apoptosis promoters 有权
标题翻译：凋亡启动子
公开(公告)号：US08173811B2
公开(公告)日：2012-05-08
申请号：US12800702
申请日：2010-05-19
申请人： Milan Bruncko , Hong Ding , Steven Elmore , Aaron Kunzer , Christopher L. Lynch , William McClellan , Cheol-Min Park , Andrew Petros , Xiaohong Song , Xilu Wang , Noah Tu , Michael Wendt
发明人： Milan Bruncko , Hong Ding , Steven Elmore , Aaron Kunzer , Christopher L. Lynch , William McClellan , Cheol-Min Park , Andrew Petros , Xiaohong Song , Xilu Wang , Noah Tu , Michael Wendt
IPC分类号： C07D235/02
CPC分类号： C07D295/155 , C07D207/24 , C07D211/20 , C07D211/26 , C07D211/48 , C07D211/70 , C07D211/72 , C07D213/38 , C07D213/70 , C07D213/74 , C07D213/81 , C07D215/12 , C07D257/04 , C07D277/36 , C07D295/185 , C07D295/30 , C07D307/22 , C07D309/20 , C07D333/20 , C07D333/34 , C07D401/12 , C07D403/12 , C07D487/04
摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
摘要翻译：公开了抑制抗凋亡蛋白家族成员的活性的化合物，含有化合物的组合物和该化合物用于制备用于治疗疾病的药物的用途，其中发生表达一种或多种抗凋亡蛋白家族成员。

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