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51. 发明申请

US20170073345A1 COMPOSITIONS AND METHODS FOR THE TREATMENT OF DIABETES AND PRE-DIABETES 审中-公开
标题翻译：用于治疗糖尿病和预防糖尿病的组合物和方法
公开(公告)号：US20170073345A1
公开(公告)日：2017-03-16
申请号：US14938131
申请日：2015-11-11
申请人： Mohan Murali Alapati
发明人： Mohan Murali Alapati
IPC分类号： C07D487/04 , C07D471/04 , C07C233/49 , C07D401/04 , C07C235/28
CPC分类号： C07D487/04 , C07B2200/05 , C07C219/08 , C07C229/22 , C07C229/24 , C07C233/38 , C07C233/49 , C07C235/28 , C07C279/14 , C07C309/08 , C07C309/12 , C07C309/14 , C07C313/14 , C07C323/41 , C07C323/43 , C07C327/30 , C07D401/04 , C07D471/04
摘要： The invention relates to the compounds and compositions of Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprises a salt of dipeptidyl peptidase-4 inhibitor and the methods for treating or preventing metabolic syndrome, prediabetes and diabetes may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compounds and compositions may be used to treatment of diabetes mellitus, obesity, lipid disorders, hypertriglyceridemia, hyperglycemia, hyperinsulinemia and insulin resistance.
摘要翻译：本发明涉及式I，式II，式III，式IV，式V，式VI或其药学上可接受的多晶型物，溶剂合物，对映异构体，立体异构体和水合物的化合物和组合物。药物组合物包含二肽基肽酶-4抑制剂的盐和治疗或预防代谢综合征的方法，糖尿病前期和糖尿病可以配制用于口服，口腔，直肠，局部，透皮，经粘膜，静脉内，肠胃外给药，糖浆或注射。这些化合物和组合物可用于治疗糖尿病，肥胖，脂质障碍，高甘油三酯血症，高血糖症，高胰岛素血症和胰岛素抵抗。

52. 发明授权

US09422308B2 Derivatives of docosahexaenoylethanolamide and uses thereof 有权
标题翻译：二十二碳六烯酰乙醇酰胺的衍生物及其用途
公开(公告)号：US09422308B2
公开(公告)日：2016-08-23
申请号：US14387410
申请日：2013-03-15
申请人： The United States of America, as represented by the Secretary, Department of Health and Human Services
发明人： Hee-Yong Kim , Juan Jose Marugan , Erika E. Englund , Samarjit Patnaik
IPC分类号： C07D495/04 , C07D213/40 , C07D319/20 , C07D205/04 , C07C235/28 , C07D309/04 , C07D333/20 , C07D235/14 , C07C233/09 , C07C233/13 , C07C233/20 , C07C233/23 , C07C233/31 , C07C233/38 , C07C233/49 , C07C255/29 , C07D295/13 , C07D295/135 , C07D295/185 , C07D307/52
CPC分类号： C07D495/04 , C07C233/09 , C07C233/13 , C07C233/20 , C07C233/23 , C07C233/31 , C07C233/38 , C07C233/49 , C07C235/28 , C07C255/29 , C07C2601/04 , C07C2601/14 , C07D205/04 , C07D213/40 , C07D235/14 , C07D295/13 , C07D295/135 , C07D295/185 , C07D307/52 , C07D309/04 , C07D319/20 , C07D333/20
摘要： The invention provides derivatives of DEA which have increased potency and hydrolysis resistance as compared to DEA, and compositions thereof, as well as methods of using these derivatives to promote neurogenesis, neurite growth and/or length, and/or promote synaptogenesis.
摘要翻译：本发明提供了与DEA相比具有增强的耐药性和耐水解性的DEA衍生物及其组合物，以及使用这些衍生物促进神经发生，神经突生长和/或长度和/或促进突触发生的方法。

53. 发明授权

US09266853B2 Orally available viridiofungin derivative possessing anti-HCV activity 有权
标题翻译：具有抗HCV活性的口服有效的维生素E衍生物
公开(公告)号：US09266853B2
公开(公告)日：2016-02-23
申请号：US14421577
申请日：2013-08-16
申请人： Chugai Seiyaku Kabushiki Kaisha
发明人： Yasunori Kohchi , Kimitaka Nakama , Susumu Komiyama , Fumio Watanabe
IPC分类号： C07D293/00 , C07D317/00 , C07D317/36 , C07D293/06 , C07D317/34 , C07D317/40 , C07C235/28 , A61K31/192 , A61K31/357 , C07C235/74
CPC分类号： C07D317/36 , A61K31/192 , A61K31/357 , C07C235/28 , C07C235/74 , C07C2601/16 , C07D293/06 , C07D317/34 , C07D317/40
摘要： An object of the present invention is to provide a compound that is useful as an orally available anti-HCV agent. The present invention relates to a compound represented by formula (1) or a pharmaceutically acceptable salt thereof. This compound has an anti-HCV activity and is useful as a medicine.
摘要翻译：本发明的目的是提供可用作口服抗HCV药剂的化合物。本发明涉及由式（1）表示的化合物或其药学上可接受的盐。该化合物具有抗HCV活性，可用作药物。

54. 发明授权

US09029593B2 Method for manufacturing spilanthol and intermediate manufacturing product therefor 有权
标题翻译：制备微量金属的方法及其中间制造产品
公开(公告)号：US09029593B2
公开(公告)日：2015-05-12
申请号：US13383547
申请日：2010-07-14
申请人： Shigeru Tanaka , Kenya Ishida , Kenji Yagi , Hideo Ujihara
发明人： Shigeru Tanaka , Kenya Ishida , Kenji Yagi , Hideo Ujihara
IPC分类号： C07C231/12 , C07C235/28 , A61K31/16 , A61K8/42 , A61Q13/00 , C07C233/09 , A23L2/56 , A23L1/226 , C11B9/00
CPC分类号： A61K31/16 , A23L2/56 , A23L27/202 , A61K8/42 , A61Q13/00 , C07C231/12 , C07C233/09 , C07C235/28 , C11B9/0007
摘要： Provided is an amide ester that is useful as an intermediate manufacturing product for an aroma compound such as spilanthol or the like. Also provided is a spilanthol manufacturing method using said amide ester. High-purity spilanthol can be manufactured by reacting an amide ester represented by general formula (1) with a basic compound. (In the formula, R1 represents a C1-6 alkyl group or a phenyl group that may be substituted with a C1-4 alkyl group, a C1-4 alkoxy group, or a halogen atom; R2 represents a C1-8 hydrocarbon group; and the wavy lines represent cis configurations, trans configurations, or a mixture of the two configurations.)
摘要翻译：提供一种酰胺酯，其可用作芳香化合物如稀释剂等的中间制造产品。还提供了使用所述酰胺酯的稀释剂制造方法。可以通过使通式（1）表示的酰胺与碱性化合物反应来制备高纯度的稀释剂。（式中，R 1表示可被C 1-4烷基，C 1-4烷氧基或卤素原子取代的C 1-6烷基或苯基; R 2表示碳原子数1〜8的烃基; 并且波浪线表示顺式构型，反式构型或两种构型的混合物）

55. 发明授权

US08946224B2 Substituted [1,2,4]triazolo[4,3-A]pyrazines for medicaments and pharmaceutical compositions 有权
标题翻译：用于药物和药物组合物的取代的[1,2,4]三唑并[4,3-A]吡嗪
公开(公告)号：US08946224B2
公开(公告)日：2015-02-03
申请号：US13883713
申请日：2011-11-11
申请人： Mark Craighead , Ronald Palin , Neil Murray , Derek Lindsay
发明人： Mark Craighead , Ronald Palin , Neil Murray , Derek Lindsay
IPC分类号： A61K31/4985 , C07D487/04 , C07D498/06 , C07D413/12 , C07C63/64 , C07D213/60 , C07C217/58 , C07D403/06 , C07C69/12 , C07C235/16 , C07D257/04 , C07D313/04 , C07D407/06 , C07C43/205 , C07C215/46 , C07C255/25 , C07D205/08 , C07D281/06 , C07D417/06 , C07D413/04 , C07D401/04 , C07C63/66 , C07D499/88 , C07D401/12 , C07D519/00 , C07D209/18 , C07D307/00 , C07D501/00 , C07C233/22 , C07D473/00 , C07H19/052 , C07C251/40 , C07D403/12 , C07D513/06 , C07C251/54 , C07C257/14 , C07C251/48 , C07C57/00 , C07C233/36 , C07H19/173 , C07D411/10 , C07C229/18 , C07D295/02 , C07H19/06 , C07C235/28 , C07D233/54 , C07J5/00 , C07D471/04 , C07D241/04 , C07D235/16 , C07D277/40 , C07D417/12 , C07D309/32 , C07C237/20 , C07C251/58 , C07D401/14 , C07D491/04
CPC分类号： C07D487/04 , C07C43/205 , C07C57/00 , C07C63/64 , C07C63/66 , C07C69/12 , C07C215/46 , C07C217/58 , C07C229/18 , C07C233/22 , C07C233/36 , C07C235/16 , C07C235/28 , C07C237/20 , C07C251/40 , C07C251/48 , C07C251/54 , C07C251/58 , C07C255/25 , C07C257/14 , C07C2601/16 , C07C2602/10 , C07C2603/74 , C07D205/08 , C07D209/18 , C07D213/60 , C07D233/54 , C07D235/16 , C07D241/04 , C07D257/04 , C07D277/40 , C07D281/06 , C07D295/02 , C07D307/00 , C07D309/32 , C07D313/04 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D407/06 , C07D411/10 , C07D413/04 , C07D413/12 , C07D417/06 , C07D417/12 , C07D471/04 , C07D473/00 , C07D491/04 , C07D498/06 , C07D499/88 , C07D501/00 , C07D513/06 , C07D519/00 , C07H19/052 , C07H19/06 , C07H19/173 , C07J5/00 , C07J71/0031
摘要： The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. Exemplary derivatives have the formula
摘要翻译：本发明涉及已知的活性药物化合物的衍生物。由于活性化合物的氧化还原衍生物，这些衍生物与母体活性化合物不同。这意味着活性化合物中的一个或多个官能团已经在一个或多个反应中被转化为另一个基团，这可被认为代表氧化态的变化。我们通常将这些化合物称为氧化还原衍生物。本发明的衍生物可以仅通过单步转化与原始的母体活性药物化合物相关，或者可以通过包括氧化态的一个或多个变化的几个合成步骤相关。示例性衍生物具有式

56. 发明申请

US20150025257A1 DOCOSAHEXAENOYL ETHANOLAMIDES 有权
标题翻译： DOCOSAHEXAENOYL乙醇胺
公开(公告)号：US20150025257A1
公开(公告)日：2015-01-22
申请号：US14124761
申请日：2012-06-08
申请人： Charles N. Serhan , Rong Yang
发明人： Charles N. Serhan , Rong Yang
IPC分类号： C07D303/46 , C07C235/28
CPC分类号： C07C235/28 , A61K47/64 , C07D303/14 , C07D303/46 , C07K5/0215
摘要： The invention describes novel mono or dihydroxy docosahexaenoic acid (DHA) analogues, their preparation, isolation, identification, purification and uses thereof.
摘要翻译：本发明描述了新型单或二羟基二十二碳六烯酸（DHA）类似物，其制备，分离，鉴定，纯化和用途。

57. 发明授权

US08618314B2 Exo- and diastereo-selective synthesis of himbacine analogs 有权
标题翻译：烟草类似物的外切和非对映选择性合成
公开(公告)号：US08618314B2
公开(公告)日：2013-12-31
申请号：US13563136
申请日：2012-07-31
申请人： George G. Wu , Anantha Sudhakar , Tao Wang , Ji Xie , Frank X. Chen , Marc Poirier , Mingsheng Huang , Vijay Sabesan , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam , Jing Liao , Illia Zavialov , Hoa N. Nguyen , Ngiap Kie Lim
发明人： George G. Wu , Anantha Sudhakar , Tao Wang , Ji Xie , Frank X. Chen , Marc Poirier , Mingsheng Huang , Vijay Sabesan , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam , Jing Liao , Illia Zavialov , Hoa N. Nguyen , Ngiap Kie Lim
IPC分类号： C07D307/92
CPC分类号： C07D263/56 , C07C69/606 , C07C69/732 , C07C201/10 , C07C201/12 , C07C205/44 , C07C205/55 , C07C231/10 , C07C231/12 , C07C235/28 , C07C303/32 , C07C309/08 , C07C2601/16 , C07D277/64 , C07D307/92 , C07D333/56 , C07D405/06 , C07D413/06 , C07D417/06 , C07F7/1804 , C07F9/58 , Y02P20/55 , C07C233/28
摘要： This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:
摘要翻译：本申请公开了一种制备可用作凝血酶受体拮抗剂的烟肼类似物的新方法。该方法部分基于使用手性硝基中心的碱促进的动态差向异构化。本文教导的化学结构可以举例说明如下：

58. 发明申请

US20120328536A1 Taste Improving Substances 有权
标题翻译：味道改善物质
公开(公告)号：US20120328536A1
公开(公告)日：2012-12-27
申请号：US13605279
申请日：2012-09-06
申请人： Jan Visser , Harry Renes , Esther van Ommeren , Sander van Tondeur , Chris Winkel
发明人： Jan Visser , Harry Renes , Esther van Ommeren , Sander van Tondeur , Chris Winkel
IPC分类号： A23L1/22 , A61Q11/00 , A61K8/42
CPC分类号： C07C235/80 , A23L27/202 , C07C231/02 , C07C235/08 , C07C235/28
摘要： The present invention relates to taste improvement of foodstuffs, beverages, tobacco products and oral care products, using a substance according to formula (I), edible salts or edible esters thereof: It was found that substances represented by formula (I) are capable of modifying and complementing, the sensory impact of taste imparting substances. Thus, the present taste improving substances are advantageously applied in flavour compositions, foodstuffs, tobacco products and oral care products. Typical examples of taste improving substances according to the present invention include N-(2-hydroxyethyl) 3-hydroxypropionamide; N-(2-hydroxyethyl) 3-hydroxybutyramide; N-(2-hydroxyethyl) 4-hydroxybutyramide; N-(2-hydroxyethyl) N-5-hydroxypentanoylamide; N-(2-hydroxyethyl) 4-hydroxypentanoylamide; N-(2-hydroxyethyl) 3-hydroxypentanoylamide; N-(2-hydroxyethyl) 2-methyl-4-hydroxy-butyramide; N-(2-hydroxyethyl) 2-methyl-3-hydroxybutyramide; N-(2-hydroxyethyl) N-6-hydroxyhexanoylamide; N-(2-hydroxyethyl) 5-hydroxyhexanoylamide; N-(2-hydroxyethyl) 4-hydroxyhexanoylamide; N-(2-hydroxyethyl) 3-hydroxyhexanoylamide; N-(2-hydroxyethyl) 4-hydroxy-2-keto-3-methyl-pentanoylamide; N-(2-hydroxyethyl) 4-hydroxy-2-keto-3-methyl-hexanoylamide and mixtures thereof.
摘要翻译：本发明涉及使用根据式（I）的物质，食用盐或食用酯的食品，饮料，烟草制品和口腔护理产品的味道改进：发现由式（I）表示的物质能够修饰和补充，味觉赋予物质的感官影响。因此，本发明的味道改善物质有利地应用于风味组合物，食品，烟草制品和口腔护理产品中。根据本发明的味道改善物质的典型实例包括N-（2-羟乙基）3-羟基丙酰胺; N-（2-羟乙基）3-羟基丁酰胺; N-（2-羟乙基）-4-羟基丁酰胺; N-（2-羟乙基）N-5-羟基戊酰胺; N-（2-羟乙基）-4-羟基戊酰胺; N-（2-羟乙基）3-羟基戊酰胺; N-（2-羟乙基）2-甲基-4-羟基 - 丁酰胺; N-（2-羟乙基）2-甲基-3-羟基丁酰胺; N-（2-羟乙基）N-6-羟基己酰胺; N-（2-羟乙基）-5-羟基己酰胺; N-（2-羟乙基）-4-羟基己酰胺; N-（2-羟乙基）3-羟基己酰胺; N-（2-羟乙基）-4-羟基-2-酮-3-甲基 - 戊酰胺; N-（2-羟乙基）-4-羟基-2-酮-3-甲基 - 己酰胺及其混合物。

59. 发明授权

US08163959B2 Method for the preparation of 4-fluoro-α-[2-methyl-1-oxopropyl]-γ-oxo-N-β-diphenylbenzenebutanamide and products therefrom 失效
标题翻译：制备4-氟-α-[2-甲基-1-氧代丙基]-γ-氧代-N- [b] - 二苯基苯丁酰胺及其产物的方法
公开(公告)号：US08163959B2
公开(公告)日：2012-04-24
申请号：US12944579
申请日：2010-11-11
申请人： Ganesh Gurpur Pai , K. Nanda Kishore , Narendra P. Chaudhari , N. Anjaneyulu , B. N. Ghogare
发明人： Ganesh Gurpur Pai , K. Nanda Kishore , Narendra P. Chaudhari , N. Anjaneyulu , B. N. Ghogare
IPC分类号： C07C233/05
CPC分类号： C07C231/12 , A61K31/167 , A61K31/40 , C07C231/02 , C07C235/28 , A61K2300/00 , C07C235/80
摘要： A method for the preparation of 4-fluoro-α-[2-methyl-1-oxopropyl]-γ-oxo-N-β-diphenylbenzenebutanamide also known as 2-[2-(4-fluorophenyl)-2-oxo-1-phenylethyl]-4-methyl-3-oxo-pentanoic acid phenylamide of the formula I containing about 0.1% or less of α-[2-methyl-1-oxopropyl]-γ-oxo-N-β-diphenylbenzene butanamide, about 0.05% or less of difluoro-α-[2-methyl-1-oxopropyl]-γ-oxo-N-β-diphenylbenzene butanamide and about 0.1% or less of 3-[2-(4-Fluorophenyl)-2-oxo-1-phenyl-ethoxy]-4-methyl-pent-2-enoic acid phenylamide.
摘要翻译：制备4-氟-α-[2-甲基-1-氧代丙基]-γ-氧代-N- [b]二苯基苯丁酰胺的方法，也称为2- [2-（4-氟苯基）-2-氧代 - 1-苯基乙基] -4-甲基-3-氧代 - 戊酸苯酰胺，其含有约0.1％或更少的α-[2-甲基-1-氧代丙基]-γ-氧代-N-苯基苯丁酰胺，约0.05％或更少的二氟-α-[2-甲基-1-氧代丙基]-γ-氧代-N- [b] - 二苯基苯丁酰胺和约0.1％或更少的3- [2-（4-氟苯基） - 2-氧代-1-苯基 - 乙氧基] -4-甲基 - 戊-2-烯酸苯基酰胺。

60. 发明授权

US07772276B2 Exo-selective synthesis of himbacine analogs 有权
标题翻译：非选择性合成替卡宾类似物
公开(公告)号：US07772276B2
公开(公告)日：2010-08-10
申请号：US11330521
申请日：2006-01-12
申请人： Tiruvettipuram K. Thiruvengadam , Anantha R. Sudhakar , Ngiap-Kie Lim , Daw-long Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
发明人： Tiruvettipuram K. Thiruvengadam , Anantha R. Sudhakar , Ngiap-Kie Lim , Daw-long Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
IPC分类号： A61K31/34
CPC分类号： C07D493/10 , C07C235/28 , C07D295/185 , C07D307/92 , C07D317/72 , C07D405/06
摘要： This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists. The chemistry disclosed herein is exemplified in the following synthesis sequence:
摘要翻译：本申请公开了一种用于合成烟肼类似物的新方法，以及由此制备的化合物。合成通过包括环状缩酮酰胺途径，手性氨基甲酸酯酰胺路线和手性氨基甲酸酯路线的替代途径进行。由此制备的化合物可用作凝血酶受体拮抗剂。本文公开的化学例如以下合成顺序：

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