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41. 发明授权

US09351484B2 N-alkyl lactam ethers, and compositions and uses thereof 有权
标题翻译： N-烷基内酰胺醚及其组合物和用途
公开(公告)号：US09351484B2
公开(公告)日：2016-05-31
申请号：US14057075
申请日：2013-10-18
申请人： Osama M. Musa , Kolazi S. Narayanan
发明人： Osama M. Musa , Kolazi S. Narayanan
IPC分类号： C07D401/12 , A01N25/02 , C07D403/12 , B01F17/00 , C07D223/10 , C07D207/27 , C07D211/76 , C11D7/26 , C11D7/32 , C09D7/00 , C09D7/12 , C09D9/00 , A61K9/00 , A61K47/18 , A61K9/70 , A61K8/49 , A61K47/22 , A61Q19/00 , C08K5/3415 , C09D11/36 , C09K3/18 , C11D3/43 , A61Q17/00
CPC分类号： A61K47/22 , A01N25/02 , A01N43/653 , A01N43/78 , A01N53/00 , A61K8/4913 , A61K8/58 , A61K9/0014 , A61K9/7084 , A61K31/405 , A61K31/4174 , A61K31/65 , A61K31/7048 , A61K47/18 , A61Q5/02 , A61Q17/005 , A61Q19/00 , B01D53/1468 , B01D53/1487 , B01D53/1493 , B01F17/0042 , C07D207/27 , C07D211/76 , C07D223/10 , C07D401/12 , C07D403/12 , C08F2/06 , C08K5/3415 , C08L71/02 , C08L2201/56 , C09D7/20 , C09D7/63 , C09D9/005 , C09D11/033 , C09D11/36 , C09D17/002 , C09K3/00 , C09K3/18 , C09K8/524 , C09K15/30 , C09K2208/22 , C10M133/44 , C10M2215/224 , C11D3/32 , C11D3/43 , C11D7/263 , C11D7/3281 , G01N21/88 , H01M10/056 , A01N37/18 , A01N37/50 , A01N43/40 , A01N43/54 , A01N43/90 , A01N47/46 , A01N65/00
摘要： Described is a class of symmetrical and asymmetrical N-alkyl lactam ethers. One preferred ether is bis-N-ethyl pyrrolidone ether. Preferred compositions and uses of the ethers are in performance chemicals, personal care, and pharmaceutical fields, where they function a variety of roles, including as a solvent, solubilizer, freezing point depressor, diluent, extracting agent, cleaning agent, degreaser, absorbent and/or dispersion agent.
摘要翻译：描述了一类对称和不对称的N-烷基内酰胺醚。一种优选的醚是双-N-乙基吡咯烷酮醚。醚的优选组合物和用途是在性能化学品，个人护理和制药领域中，其中它们起多种作用，包括作为溶剂，增溶剂，凝固点抑制剂，稀释剂，提取剂，清洁剂，脱脂剂，吸收剂和 /或分散剂。

42. 发明授权

US09334236B2 Lactam-based compounds with a urethane or urea functional group, and uses thereof 有权
标题翻译：具有氨基甲酸酯或脲官能团的基于内酰胺的化合物及其用途
公开(公告)号：US09334236B2
公开(公告)日：2016-05-10
申请号：US13390852
申请日：2010-08-18
申请人： Osama M. Musa
发明人： Osama M. Musa
IPC分类号： C08F126/10 , C07D223/10 , C08F226/10 , C07D207/12 , C07D207/27 , C08G18/28 , C08G18/81
CPC分类号： C07D207/27 , C07D223/10 , C08G18/2855 , C08G18/8108
摘要： Compounds comprising a lactam moiety, and a urethane or urea functional group are presented. By a preferred synthesis route, they are prepared using at least one polymerizable compound comprising an isocyanate moiety and reacting it with at least one hydroxyalkyl lactam compound or one aminoalkyl lactam compound. In preferred embodiments the lactam moiety is a pyrrolidone or caprolactam ring, and the polymerizable compound is a functionalized aryl isocyanate. The compounds and homopolymers and non-homopolymers thereof find useful application in a wide variety of arts, including: adhesive, agricultural, biocides, cleaning, coating, electronics, encapsulation, membrane, microelectronics, oilfield, performance chemical, personal care, sealant, and sensor applications.
摘要翻译：提供了包含内酰胺部分和氨基甲酸酯或脲官能团的化合物。通过优选的合成途径，它们使用至少一种包含异氰酸酯部分的可聚合化合物制备，并使其与至少一种羟烷基内酰胺化合物或一种氨基烷基内酰胺化合物反应。在优选的实施方案中，内酰胺部分是吡咯烷酮或己内酰胺环，并且可聚合化合物是官能化的芳基异氰酸酯。化合物及其均聚物和非均聚物可用于广泛的领域，包括：粘合剂，农业，杀生物剂，清洁，涂料，电子，封装，膜，微电子学，油田，性能化学品，个人护理，密封剂和传感器应用。

43. 发明授权

US09278908B2 Intermediates of neutral endopeptidase inhibitors and preparation method thereof 有权
公开(公告)号：US09278908B2
公开(公告)日：2016-03-08
申请号：US14739172
申请日：2015-06-15
申请人： David Hook , Jianguang Zhou , Yunzhong Li , Jie Ku
发明人： David Hook , Jianguang Zhou , Yunzhong Li , Jie Ku
IPC分类号： C07D207/267 , C07D207/27 , C07D207/38 , C07C231/10 , C07D207/26 , C07D207/263 , C07D207/277
CPC分类号： C07C231/10 , C07D207/26 , C07D207/263 , C07D207/267 , C07D207/27 , C07D207/277 , C07D207/38
摘要： The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a g-amino-d-biphenyl-a-methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.

45. 发明申请

US20150344413A1 COMPOUNDS FOR THE TREATMENT OF SEIZURES AND OTHER CENTRAL NERVOUS SYSTEM DISORDERS AND CONDITIONS 有权
标题翻译：治疗癫痫发作和其他中枢神经系统疾病和病症的化合物
公开(公告)号：US20150344413A1
公开(公告)日：2015-12-03
申请号：US14727979
申请日：2015-06-02
申请人： Ketogen Inc.
发明人： Joseph A. Araujo , John S. Andrews , Subhash C. Annedi , Guy A. Higgins , Norton W. Milgram , Paula J. Estey , Gary L.W.G. Robinson , Jaipal R. Nagireddy
IPC分类号： C07C233/47 , C07D207/27
CPC分类号： C07C233/47 , A61K31/4015 , C07C2601/14 , C07D207/27
摘要： The present application relates to novel compounds comprising a moiety that leads to the metabolic production of ketones bonded to a ketone-potentiated anti-epileptic drug, compositions comprising these compounds, and their use, for example for the treatment of epilepsy, and other CNS diseases, disorders or conditions. In particular, the present application includes compounds of Formula I, and compositions and uses thereof:
摘要翻译：本申请涉及包含导致与酮增强的抗癫痫药物结合的酮的代谢产生的部分的新型化合物，包含这些化合物的组合物及其用于治疗癫痫和其它CNS疾病，疾病或病症。特别地，本申请包括式I化合物及其组合物和用途：

46. 发明授权

US09169196B2 4-(p-quinonyl)-2-hydroxybutanamide derivatives for treatment of mitochondrial diseases 有权
标题翻译： 4-（对醌基）-2-羟基丁酰胺衍生物用于治疗线粒体疾病
公开(公告)号：US09169196B2
公开(公告)日：2015-10-27
申请号：US13924363
申请日：2013-06-21
申请人： Edison Pharmaceuticals, Inc.
发明人： Orion D. Jankowski , Kieron E. Wesson , Paul Mollard , William D. Shrader
IPC分类号： C07C235/78 , C07C317/28 , C07D295/13 , C07D295/192 , C07D207/27 , C07D211/46 , C07D213/40 , C07D233/61 , C07D265/30 , C07D311/66
CPC分类号： C07C235/80 , C07C235/78 , C07C317/28 , C07C2601/02 , C07C2601/16 , C07D207/26 , C07D207/27 , C07D211/46 , C07D213/40 , C07D213/50 , C07D233/61 , C07D265/30 , C07D295/116 , C07D295/13 , C07D295/185 , C07D295/192 , C07D311/66
摘要： Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.
摘要翻译：还公开了治疗或抑制线粒体疾病如弗里德里希共济失调（FRDA），Leber氏遗传性视神经病变（LHON），线粒体肌病，脑病，乳酸脱落和中风（MELAS），Kearns-Sayre综合征（KSS）的方法作为可用于本发明方法的化合物，例如4-（对 - 喹啉基）-2-羟基丁酰胺衍生物。还公开了可用于治疗其他疾病如肌萎缩性侧索硬化（ALS），亨廷顿氏病，帕金森病和普遍发育障碍如自闭症的方法和化合物。还公开了可用于评估受试者的代谢状态和治疗功效的能量生物标志物。还公开了调节，归一化或增强能量生物标志物的方法以及可用于这些方法的化合物。

47. 发明授权

US09096517B2 Oligomer-containing pyrrolidine compounds 有权
标题翻译：含低聚物的吡咯烷化合物
公开(公告)号：US09096517B2
公开(公告)日：2015-08-04
申请号：US14297149
申请日：2014-06-05
申请人： NEKTAR THERAPEUTICS
发明人： Jennifer Riggs-Sauthier
IPC分类号： C07D207/27 , A61K31/765 , A61K31/4015 , A61K47/48 , C07D207/267
CPC分类号： A61K31/4015 , A61K31/765 , A61K47/60 , C07D207/267 , C07D207/27
摘要： The invention relates to (among other things) oligomer-containing pyrrolidine compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.
摘要翻译：本发明涉及（尤其是）含低聚物的吡咯烷化合物。当通过任何多种施用途径给药时，本发明的化合物显示出相对于缺乏寡聚物的相应化合物的一个或多个优点。

48. 发明申请

US20150165400A1 CRYSTALLISATION PROCESS 审中-公开
标题翻译：水晶工艺
公开(公告)号：US20150165400A1
公开(公告)日：2015-06-18
申请号：US14400946
申请日：2013-05-15
申请人： University of Bradford
发明人： Chaitrali Kulkarni , Ravindra Dhumal , Adrian Kelly , Tim Gough , Anant Paradkar
IPC分类号： B01F7/08 , C07C311/58 , C07D223/26 , C07D207/27 , C07D493/18 , C07C303/42
CPC分类号： B01F7/081 , B01F2215/0032 , C07C303/42 , C07C311/58 , C07D207/27 , C07D223/26 , C07D223/28 , C07D493/08 , C07D493/18
摘要： The present invention relates to a method useful for forming products which are useful in a pharmaceutical context, and products formed by such a method. The invention relates particularly, but not exclusively, to methods of forming a metastable polymorph using screw extrusion, whereby temperature and shear induce transformational changes, and products obtained or obtainable via such methods.
摘要翻译：本发明涉及一种可用于形成可用于制药背景的产品的方法，以及通过这种方法形成的产品。本发明特别涉及但不排他地涉及使用螺杆挤出形成亚稳态多晶型物的方法，由此温度和剪切引起转化变化，以及通过这些方法获得或可获得的产物。

49. 发明授权

US08993785B2 Process for preparing 5-biphenyl-4-amino-2-methyl pentanoic acid 有权
公开(公告)号：US08993785B2
公开(公告)日：2015-03-31
申请号：US14224700
申请日：2014-03-25
申请人： David Hook , Thomas Ruch , Bernard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar Murlidhar Waykole
发明人： David Hook , Thomas Ruch , Bernard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar Murlidhar Waykole
IPC分类号： C07D207/38 , C07D207/267 , C07D207/44 , C07C269/04 , C07C227/16 , C07C227/22 , C07C227/32 , C07C229/34 , C07C231/02 , C07C233/47 , C07C271/22 , C07D207/24 , C07D207/26 , C07D207/27 , C07D207/273 , C07D207/277 , C07D207/40 , C07F7/10 , C07C219/18 , C07D207/12 , C07C227/20 , C07C231/12 , C07D207/404 , C07D403/06
CPC分类号： C07C231/02 , C07C219/18 , C07C227/16 , C07C227/20 , C07C227/22 , C07C227/32 , C07C229/34 , C07C231/12 , C07C231/14 , C07C233/47 , C07C269/04 , C07C271/22 , C07C2601/16 , C07D207/12 , C07D207/24 , C07D207/26 , C07D207/267 , C07D207/27 , C07D207/273 , C07D207/277 , C07D207/40 , C07D207/404 , C07D207/44 , C07D403/06 , C07F7/10 , Y02P20/55
摘要： The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.

50. 发明申请

US20140249320A1 Process for Preparing 5-biphenyl-4-amino-2-methyl Pentanoic Acid 有权
标题翻译： 5-联苯-4-氨基-2-甲基戊酸的制备方法
公开(公告)号：US20140249320A1
公开(公告)日：2014-09-04
申请号：US14224700
申请日：2014-03-25
申请人： David Hook , Thomas Ruch , Bernard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar Murlidhar Waykole
发明人： David Hook , Thomas Ruch , Bernard Riss , Bernhard Wietfeld , Gottfried Sedelmeier , Matthias Napp , Markus Bänziger , Steven Hawker , Lech Ciszewski , Liladhar Murlidhar Waykole
IPC分类号： C07F7/10 , C07D207/27 , C07C227/22 , C07D207/273 , C07C227/20 , C07D403/06 , C07C231/12 , C07D207/404 , C07D207/267 , C07C269/04
CPC分类号： C07C231/02 , C07C219/18 , C07C227/16 , C07C227/20 , C07C227/22 , C07C227/32 , C07C229/34 , C07C231/12 , C07C231/14 , C07C233/47 , C07C269/04 , C07C271/22 , C07C2601/16 , C07D207/12 , C07D207/24 , C07D207/26 , C07D207/267 , C07D207/27 , C07D207/273 , C07D207/277 , C07D207/40 , C07D207/404 , C07D207/44 , C07D403/06 , C07F7/10 , Y02P20/55
摘要： The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
摘要翻译：本发明涉及式（1）的吡咯烷-2-酮或其盐，其中R1是氢或氮保护基，其制备方法及其在制备NEP-抑制剂中的用途，特别是在制备N-（3-羧基-1-氧代丙基） - （4S） - （对苯基苯基甲基）-4-氨基 - （2R） - 甲基丁酸乙酯或其盐。

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