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121. 发明授权

US09056849B2 Amine derivative compounds for treating ophthalmic diseases and disorders 有权
标题翻译：用于治疗眼科疾病和病症的胺衍生物化合物
公开(公告)号：US09056849B2
公开(公告)日：2015-06-16
申请号：US14226665
申请日：2014-03-26
申请人： Acucela Inc.
发明人： Ian L. Scott , Vladimir A. Kuksa , Mark W. Orme , Feng Hong , Thomas L. Little , Ryo Kubota
IPC分类号： C07C213/00 , C07D335/02 , C07C211/27 , C07C215/28 , C07C215/30 , C07C215/42 , C07C217/16 , C07C217/48 , C07C217/54 , C07C217/72 , C07C219/22 , C07C225/16 , C07C225/18 , C07C233/18 , C07C235/34 , C07C235/54 , C07C237/20 , C07C237/38 , C07C237/40 , C07C257/14 , C07C279/08 , C07C317/28 , C07C323/25 , C07C323/29 , C07D213/30 , C07D309/06 , C07D333/16 , C07D333/20 , C07C215/20 , C07C217/74 , C07D213/38
CPC分类号： A61K31/382 , A61K31/138 , A61K31/165 , A61K31/351 , C07C211/27 , C07C213/00 , C07C215/20 , C07C215/28 , C07C215/30 , C07C215/42 , C07C217/16 , C07C217/48 , C07C217/54 , C07C217/72 , C07C217/74 , C07C219/22 , C07C225/16 , C07C225/18 , C07C233/18 , C07C235/34 , C07C235/54 , C07C237/20 , C07C237/38 , C07C237/40 , C07C257/14 , C07C279/08 , C07C317/28 , C07C323/25 , C07C323/29 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D213/30 , C07D213/38 , C07D309/06 , C07D333/16 , C07D333/20 , C07D335/02
摘要： Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
摘要翻译：提供的是胺衍生物化合物，其药物组合物，以及使用所述化合物和组合物治疗眼科疾病和失调症的方法，例如年龄相关性黄斑变性和Stargardt氏病。

122. 发明授权

US08981153B2 Alkoxy compounds for disease treatment 有权
公开(公告)号：US08981153B2
公开(公告)日：2015-03-17
申请号：US13111679
申请日：2011-05-19
申请人： Ian L. Scott , Vladimir A. Kuksa , Mark W. Orme , Thomas Little , Anna Gall , Feng Hong
发明人： Ian L. Scott , Vladimir A. Kuksa , Mark W. Orme , Thomas Little , Anna Gall , Feng Hong
IPC分类号： C07C211/00 , C07C215/20 , C07C217/20 , C07C217/60 , C07C217/62 , C07C217/64 , C07C217/72 , C07C225/16 , C07C229/38 , C07C233/18 , C07C235/08 , C07C251/86 , C07C279/08 , C07C317/28 , C07C323/25 , C07D277/24 , C07C309/06
CPC分类号： A61K31/137 , A61K31/165 , A61K31/222 , C07C215/20 , C07C217/20 , C07C217/60 , C07C217/62 , C07C217/64 , C07C217/72 , C07C217/84 , C07C225/16 , C07C229/38 , C07C233/18 , C07C235/08 , C07C251/86 , C07C279/08 , C07C309/06 , C07C317/28 , C07C323/25 , C07C323/33 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07D277/24 , C07D309/06
摘要： The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

123. 发明授权

US08604085B2 Bupropion hydrobromide polymorphs 有权
标题翻译：安非他酮氢溴酸盐多晶型物
公开(公告)号：US08604085B2
公开(公告)日：2013-12-10
申请号：US13653503
申请日：2012-10-17
申请人： Stefano Turchetta , Maurizio Zenoni
发明人： Stefano Turchetta , Maurizio Zenoni
IPC分类号： A61K31/137 , C07C225/16
CPC分类号： C07C225/10 , A61K9/2886 , A61K31/137 , A61K45/06 , C07C225/16
摘要： Polymorphous and amorphous forms of bupropion hydrobromide are described.
摘要翻译：描述了安非他酮氢溴酸盐的多晶型和无定形形式。

124. 发明申请

US20110270011A1 USE OF OPIOIDS OR OPIOID MIMETICS FOR THE TREATMENT OF RESISTANT CANCER PATIENTS 有权
标题翻译：用于治疗耐药性患者的OPIOIDS或OPIOIDMIMC的使用
公开(公告)号：US20110270011A1
公开(公告)日：2011-11-03
申请号：US13056918
申请日：2009-01-29
申请人： Erich Miltner , Claudia Friesen , Andreas Alt
发明人： Erich Miltner , Claudia Friesen , Andreas Alt
IPC分类号： A61N5/00 , C07D211/58 , C07D489/12 , C07D489/02 , C07D451/12 , A61P35/02 , A61K31/519 , A61K31/7068 , A61K31/7048 , A61K31/437 , A61K31/704 , A61P35/00 , C07C225/16 , A61K33/24
CPC分类号： A61K31/485 , A61K31/137 , A61K31/475 , A61K31/519 , A61K31/704 , A61K31/7068 , A61K33/24 , A61K41/00 , A61K45/06 , A61K2300/00
摘要： The use of opioids or opioid mimetics is suggested for the manufacture of a medicament for the treatment of resistant cancer patients.
摘要翻译：建议使用阿片样物质或阿片样物质来制备用于治疗耐药性癌症患者的药物。

125. 发明申请

US20110028423A1 AGENT THAT MODULATES PHYSIOLOGICAL CONDITION OF PESTS, INVOLVED IN INSECT CHOLINE ACETYLTRANSFERASE ACTIVITY 有权
标题翻译：调节生物物理条件的试剂，涉及胆固醇乙酰胆碱酯酶活性
公开(公告)号：US20110028423A1
公开(公告)日：2011-02-03
申请号：US12743866
申请日：2008-11-21
申请人： Junko Otsuki , Marc Van De Craen , Annelies Roobrouck , Guy Nys , Bert Demey
发明人： Junko Otsuki , Marc Van De Craen , Annelies Roobrouck , Guy Nys , Bert Demey
IPC分类号： A01N43/50 , C12Q1/48 , C07D513/04 , C07C239/08 , C07H19/173 , C07C225/16 , A01N43/78 , A01N33/24 , A01N33/12 , A01P7/04 , C12N9/10 , C07H21/00 , C12P19/34 , C12Q1/68 , C12N15/63 , C12N1/21 , C12N15/70 , G06F17/30
CPC分类号： C12N9/1029 , A01N35/10 , A01N37/12 , A01N43/90 , A01N61/00 , G01N33/68
摘要： The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect choline acetyltransferase; a method for assaying pesticidal activity of a test substance, which comprises measuring the activity of a choline acetyltransferase in a reaction system in which the choline acetyltransferase contacts with a test substance, and the like.
摘要翻译：本发明提供调节害虫生理状态的试剂，其中该试剂具有调节昆虫胆碱乙酰转移酶活性的能力; 用于测定被检物质的杀虫活性的方法，其包括测定胆碱乙酰转移酶与测试物质接触的反应体系中胆碱乙酰转移酶的活性等。

126. 发明申请

US20090187028A1 Process for preparing Chiral Dipeptidyl Peptidase -IV Inhibitor Intermediates 有权
标题翻译：制备手性二肽基肽酶-IV抑制剂中间体的方法
公开(公告)号：US20090187028A1
公开(公告)日：2009-07-23
申请号：US12321533
申请日：2009-01-22
申请人： Feng Xu , Mary M. Kim , Yoshinori Kohmura , Tricia Sladicka , Jonathan D. Rosen , Michael J. Zacuto
发明人： Feng Xu , Mary M. Kim , Yoshinori Kohmura , Tricia Sladicka , Jonathan D. Rosen , Michael J. Zacuto
IPC分类号： C07D309/28 , C07D309/30 , C07C225/16 , C07C215/30 , C07D487/04 , C07D498/04
CPC分类号： C07C271/16 , C07C269/06 , C07C271/18 , C07C271/22 , C07D309/10 , C07D309/30 , C07D487/04 , C07D498/04 , Y02P20/55
摘要： A novel process is provided for the preparation of chiral trans-2,3-disubstituted 5-oxotetrahydropyrans of structural formula (I): wherein Ar is optionally substituted phenyl and P is a primary amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.
摘要翻译：提供了一种制备结构式（I）的手性反式-2,3-二取代的5-氧代四氢吡喃的新方法：其中Ar是任选取代的苯基，P是伯胺保护基。这些化合物可用于合成用于治疗2型糖尿病的二肽基肽酶-IV抑制剂。还提供了从该方法获得的有用的中间体。

127. 发明申请

US20080293808A1 Non-Steroidal Androgen Receptor Modulators, Preparation Process, Pharmaceutical Composition and Use Thereof 失效
标题翻译：非甾体雄激素受体调节剂，制备方法，药物组合物及其用途
公开(公告)号：US20080293808A1
公开(公告)日：2008-11-27
申请号：US11921088
申请日：2006-05-26
申请人： Mingwei Wang , Caihong Zhou , Xin Hui , Haoran Su , Jie Gao , Yong Deng , Dacheng Yang
发明人： Mingwei Wang , Caihong Zhou , Xin Hui , Haoran Su , Jie Gao , Yong Deng , Dacheng Yang
IPC分类号： A61K31/341 , C07C225/16 , A61K31/137 , C07C221/00 , A61P35/00 , C07D307/52
CPC分类号： C07D211/32 , C07C225/22 , C07C229/60 , C07D295/104 , C07D307/52
摘要： Non-steroidal androgen receptor modulating compounds of the general formula (I), their pharmaceutically acceptable salts, preparation process and pharmaceutically compositions containing the said compounds are disclosed. Such compounds of the general formula (I) or their pharmaceutically acceptable salts can be used for preparing non-steroidal medicines to treat and/or prevent conditions or diseases such as prostatic hyperplasia, prostate cancer, hirsutism, severe hormone-dependent alopecia or acne, etc. as a result of androgen receptor antagonistic activities.
摘要翻译：公开了通式（I）的非甾体雄激素受体调节化合物，其药学上可接受的盐，制备方法和含有所述化合物的药物组合物。通式（I）的化合物或其药学上可接受的盐可用于制备非甾体药物以治疗和/或预防诸如前列腺增生症，前列腺癌，多毛症，严重激素依赖性脱发或痤疮的病症或疾病，作为雄激素受体拮抗活性的结果。

128. 发明授权

US06911560B2 Process for preparing salmeterol 失效
标题翻译：制备沙美特罗的方法
公开(公告)号：US06911560B2
公开(公告)日：2005-06-28
申请号：US10297130
申请日：2001-06-13
申请人： Panayiotis Alexandrou Procopiou
发明人： Panayiotis Alexandrou Procopiou
IPC分类号： C07D319/08 , C07B61/00 , C07C213/00 , C07C213/08 , C07C215/34 , C07C217/10 , C07C225/16
CPC分类号： C07C213/08 , C07B2200/07 , C07C215/34 , C07C225/16 , Y02P20/55 , C07C217/10
摘要： Accordingly, the present invention provides a process for the preparation of a compound of formula (I) or a single enantiomer thereof, or a salt or a solvate thereof, wherein W is a chiral auxilary or hydrogen and P1 and P2 are each independently selected from hydrogen or a protecting group, which comprises: a) treatment of a compound of formula (II), or a salt or a solvate thereof, wherein W is a chiral auxilary and P3 and P4 are each independently selected from hydrogen or a protecting group, with a compound formula (III); b) treatment of the resulting product with a reducing agent; c) if required, deprotection to yield the compound of formula (I), or a salt or solvate thereof. In particular there is provided a process for producing a substantially pure single enantiomer of salmeterol
摘要翻译：因此，本发明提供了制备式（I）化合物或其单一对映异构体或其盐或溶剂合物的方法，其中W是手性辅助或氢和P 1 和P＆lt; 2＆gt;各自独立地选自氢或保护基，其包括：a）处理式（II）化合物或其盐或溶剂合物，其中W是手性辅助和P 3和P 4各自独立地选自氢或保护基与化合物式（III）; b）用还原剂处理所得产物; c）如果需要，脱保护得到式（I）化合物或其盐或溶剂合物。特别地，提供了生产沙美特罗基本上纯的单一对映异构体的方法

129. 发明申请

US20050096361A1 Beta-amino ketones for the treatment of pain 审中-公开
标题翻译： β-氨基酮用于治疗疼痛
公开(公告)号：US20050096361A1
公开(公告)日：2005-05-05
申请号：US10917522
申请日：2004-08-13
申请人： Helmut Buschmann , Claudia Puetz , Dieter Enders , Stefan Oberboersch
发明人： Helmut Buschmann , Claudia Puetz , Dieter Enders , Stefan Oberboersch
IPC分类号： C07C225/16 , C07C271/18 , C07D307/52 , A61K31/44 , A61K31/325
CPC分类号： C07C225/16 , C07C271/18 , C07D307/52
摘要： Beta-amino ketone compounds corresponding to the formula (I) in which R1 through R4 have defined meanings, a method for producing such compounds, especially stereoselective production of such compounds, pharmaceutical compositions containing such beta-amino ketone compounds, and methods of using such compounds in the treatment of various conditions such as pain, anxiety, depression and/or epilepsy.
摘要翻译：对应于其中R 1至R 4具有定义含义的式（I）的β-氨基酮化合物，这种化合物的制备方法，特别是这些化合物的立体选择性生产，含有这种β-氨基酮化合物的药物组合物，以及使用该化合物的方法治疗各种病症如疼痛，焦虑，抑郁和/或癫痫的化合物。

130. 发明申请

US20040215038A1 Colorant precursor compositions 失效
标题翻译：着色剂前体组合物
公开(公告)号：US20040215038A1
公开(公告)日：2004-10-28
申请号：US10422755
申请日：2003-04-24
申请人： Xerox Corporation
发明人： Jeffery H. Banning , Donald R. Titterington , Clifford R. King
IPC分类号： C07C323/29 , C07C225/16
CPC分类号： C09B69/00
摘要： Disclosed are colorant precursor compounds of the formula 1 wherein R is an alkyl group, an aryl group, an arylalkyl group, or an alkylaryl group, and wherein R can be joined to the phenyl moiety to form a ring, each Rnull, independently of the others, is a halogen atom, an alkyl group, an alkoxy group, a nitrile group, a nitro group, an amide group, or a sulfonamide group, z is an integer of 0, 1, 2, 3, or 4, n is an integer representing the number of carbon atoms in each repeat alkylene oxide unit, and x is an integer representing the number of repeat alkylene oxide units, wherein said colorant precursor has no more than one nullOH, nullSH, or primary or secondary amino group per molecule.
摘要翻译：公开了下式的着色剂前体化合物其中R是烷基，芳基，芳基烷基或烷基芳基，其中R可以与苯基部分连接形成环，每个R'独立地为其余的是卤素原子，烷基，烷氧基，腈基，硝基，酰胺基或磺酰胺基，z是0,1,2,3或4的整数，n是表示每个重复烯化氧单元中的碳原子数的整数，x是代表重复烯化氧单元数的整数，其中所述着色剂前体不超过一个-OH，-SH或伯或仲氨基每分子。

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