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1. 发明申请

US20200271553A1 COMPOSITION FOR BIOTISSUE CLEARING AND BIOTISSUE CLEARING METHOD USING SAME 审中-公开
公开(公告)号：US20200271553A1
公开(公告)日：2020-08-27
申请号：US16462973
申请日：2017-11-20
申请人： BINAREE CO., LTD.
发明人： Sun Hyun Park
IPC分类号： G01N1/30 , C07F1/04 , C07C235/12 , G01N33/483
摘要： The present invention relates to a composition for clearing a biotissue and a method for clearing a biotissue using thereof.

2. 发明授权

US10131625B2 Method for preparing 3-carbamoymethyl-5-methylhexanoic acid in recycling way 有权
公开(公告)号：US10131625B2
公开(公告)日：2018-11-20
申请号：US15521021
申请日：2015-10-13
申请人： Zhejiang Huahai Pharmaceutical Co., Ltd.
发明人： Shudong Wang , Xuehai You , Wenling Zhang
IPC分类号： C07C235/12 , C07C233/05 , C07C231/24 , C07C211/27 , C01D1/04
摘要： The present invention provides a method for recycling 3-carbamoylmethyl-5-methylhexanoic acid from 3-carba carbamoylmethyl moymethyl-5-methylhexanoic acid chiral resolving mother liquor. The method comprises the following steps: (a) distilling 3-carbamoylmethyl-5-methylhexanoic acid chiral resolving mother liquor, adding aromatic hydrocarbon, heating to dissolve, keeping the temperature and stirring; (b) after completing the reaction in step (a), cooling the reaction solution to 30-60° C., then adding alkali liquor dropwise, keeping the temperature and reacting; and (c) after completing the reaction in step (b), cooling the reactant to 20-30° C., layering, adjusting the pH of the separated water layer to 1 to 2, performing extraction by using an organic solvent, distilling an organic phase under a reduced pressure, and crystallizing at 0±5° C. to obtain 3-carbamoylmethyl-5-methylhexanoic acid. The method provided in the present invention is convenient to operate, and the recycled product is high in purity (≥99.8%) and yield.

3. 发明授权

US10053417B2 Neprilysin inhibitors 有权
公开(公告)号：US10053417B2
公开(公告)日：2018-08-21
申请号：US15806722
申请日：2017-11-08
申请人： THERAVANCE BIOPHARMA R&D IP, LLC
发明人： Erik Fenster , Melissa Fleury , Adam D. Hughes
IPC分类号： A61K31/40 , A61K31/42 , A61K31/44 , A61K31/197 , A61K31/397 , A61K31/5375 , C07D205/04 , C07D207/09 , C07D207/14 , C07D213/56 , C07C235/34 , C07D261/04 , C07D295/32 , C07C243/38 , A61K31/341 , A61K31/4409 , C07D213/86 , C07D213/87 , C07C235/80 , A61K31/4406 , A61K31/192 , C07D213/65 , A61K45/06 , A61K31/495 , A61K31/4015 , C07D307/68 , C07D213/61 , C07D211/62 , C07D211/60 , C07D211/48 , C07D211/46 , C07D211/42 , C07D211/38 , C07D211/22 , C07C243/32 , C07C243/24 , C07D493/10 , C07D207/16 , C07D207/12 , C07D207/08 , C07D265/30 , C07C235/78 , C07C235/74 , C07C235/20 , C07C235/12 , C07C233/56 , C07D261/02 , C07D239/36 , C07D405/06 , C07D401/04 , C07D233/06 , C07D309/08 , C07C259/04 , C07D213/75 , C07D491/107
CPC分类号： C07C243/38 , A61K31/192 , A61K31/197 , A61K31/341 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/42 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/495 , A61K31/5375 , A61K45/06 , C07C233/56 , C07C235/12 , C07C235/20 , C07C235/34 , C07C235/74 , C07C235/78 , C07C235/80 , C07C243/24 , C07C243/32 , C07C259/04 , C07C2601/08 , C07C2601/16 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/22 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/60 , C07D211/62 , C07D213/56 , C07D213/61 , C07D213/65 , C07D213/75 , C07D213/86 , C07D213/87 , C07D233/06 , C07D239/36 , C07D261/02 , C07D261/04 , C07D265/30 , C07D295/32 , C07D307/68 , C07D309/08 , C07D401/04 , C07D405/06 , C07D491/107 , C07D493/10
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

4. 发明申请

US20170369425A1 COMPOUND, SALT OF COMPOUND, EXTERNAL AGENT FOR SKIN, COSMETIC, AND FOOD ADDITIVE 审中-公开
公开(公告)号：US20170369425A1
公开(公告)日：2017-12-28
申请号：US15543261
申请日：2016-01-15
申请人： SHOWA DENKO K.K.
发明人： Toru TACHIBANA , Ryota NIIBAYASHI , Daisuke YAGYU
IPC分类号： C07C235/12 , A61K8/67 , A23L33/15 , A61Q19/00
CPC分类号： C07C235/12 , A23L33/15 , A23V2002/00 , A61K8/44 , A61K8/673 , A61K31/197 , A61K2800/10 , A61Q19/00
摘要： Provided is a compound represented by Formula (1) or a salt thereof (in the formula, R1 and R2 each independently represent a hydrogen atom or a linear or branched acyl group having 11 to 30 carbon atoms, a hydrocarbon group bonded to a carbonyl carbon of the acyl group is a saturated or unsaturated hydrocarbon group, and at least one of R1 and R2 represents the acyl group).

5. 发明申请

US20170327459A1 NEPRILYSIN INHIBITORS 审中-公开
公开(公告)号：US20170327459A1
公开(公告)日：2017-11-16
申请号：US15600998
申请日：2017-05-22
申请人： THERAVANCE BIOPHARMA R&D IP, LLC
发明人： Erik Fenster , Melissa Fleury , Adam D. Hughes
IPC分类号： C07C243/38 , C07D491/107 , A61K31/192 , C07D405/06 , C07D401/04 , C07D309/08 , C07D307/68 , C07D295/32 , C07D265/30 , C07D261/04 , C07D261/02 , C07D239/36 , C07D233/06 , C07D213/87 , C07D213/86 , C07D213/75 , C07D213/65 , C07D213/61 , C07D213/56 , C07D211/62 , C07D211/60 , C07D211/48 , C07D211/46 , C07D211/42 , C07D211/38 , C07D211/22 , C07D207/16 , C07D207/14 , C07D207/12 , C07D207/09 , C07D207/08 , C07D205/04 , C07C259/04 , C07C243/32 , C07C243/24 , C07C235/80 , C07C235/78 , C07C235/74 , C07C235/34 , C07C235/20 , C07C235/12 , C07C233/56 , A61K45/06 , A61K31/5375 , A61K31/495 , A61K31/4409 , A61K31/4406 , A61K31/44 , A61K31/42 , A61K31/4015 , A61K31/40 , A61K31/397 , A61K31/341 , A61K31/197 , C07D493/10 , C07C2601/16 , C07C2601/08
CPC分类号： C07C243/38 , A61K31/192 , A61K31/197 , A61K31/341 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/42 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/495 , A61K31/5375 , A61K45/06 , C07C233/56 , C07C235/12 , C07C235/20 , C07C235/34 , C07C235/74 , C07C235/78 , C07C235/80 , C07C243/24 , C07C243/32 , C07C259/04 , C07C2601/08 , C07C2601/16 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/22 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/60 , C07D211/62 , C07D213/56 , C07D213/61 , C07D213/65 , C07D213/75 , C07D213/86 , C07D213/87 , C07D233/06 , C07D239/36 , C07D261/02 , C07D261/04 , C07D265/30 , C07D295/32 , C07D307/68 , C07D309/08 , C07D401/04 , C07D405/06 , C07D491/107 , C07D493/10
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

6. 发明申请

US20170114006A1 SUBSTITUTED BIARYL ALKYL AMIDES 审中-公开
公开(公告)号：US20170114006A1
公开(公告)日：2017-04-27
申请号：US15381535
申请日：2016-12-16
申请人： BioTheryX, Inc.
发明人： Kyle W.H. Chan , Frank Mercurio , David I. Stirling
IPC分类号： C07C235/12 , C07C237/12 , C07D207/16 , C07C237/22 , C07C233/47 , C07D307/24
CPC分类号： C07C235/12 , C07B2200/07 , C07C229/34 , C07C233/47 , C07C233/63 , C07C235/20 , C07C235/78 , C07C237/12 , C07C237/22 , C07C271/22 , C07D207/16 , C07D307/24
摘要： Disclosed herein are substituted biaryl alkyl amide compounds, methods of synthesizing substituted biaryl alkyl amide compounds and methods of treating diseases and/or conditions with substituted biaryl alkyl amide compounds.

7. 发明授权

US09546131B2 Substituted biaryl alkyl amides 有权
标题翻译：取代的联芳基烷基酰胺
公开(公告)号：US09546131B2
公开(公告)日：2017-01-17
申请号：US14447473
申请日：2014-07-30
申请人： BioTheryX, Inc.
发明人： Kyle W. H. Chan , Frank Mercurio , David I. Stirling
IPC分类号： C07C235/78 , C07C229/34 , C07D307/24 , C07D207/16 , C07C233/63 , C07C235/12 , C07C237/12 , C07C233/47 , C07C235/20 , C07C271/22
CPC分类号： C07C235/12 , C07B2200/07 , C07C229/34 , C07C233/47 , C07C233/63 , C07C235/20 , C07C235/78 , C07C237/12 , C07C237/22 , C07C271/22 , C07D207/16 , C07D307/24
摘要： Disclosed herein are substituted biaryl alkyl amide compounds, methods of synthesizing substituted biaryl alkyl amide compounds and methods of treating diseases and/or conditions with substituted biaryl alkyl amide compounds.
摘要翻译：本文公开了取代的联芳基烷基酰胺化合物，合成取代的联芳基烷基酰胺化合物的方法和用取代的联芳基烷基酰胺化合物治疗疾病和/或病症的方法。

8. 发明授权

US09422341B2 Method for producing cereulide and derivative thereof, intermediate for production of cereulide, and cereulide derivative 有权
标题翻译：方法及其衍生物，制备大肠杆菌的中间体和大脑溶液衍生物
公开(公告)号：US09422341B2
公开(公告)日：2016-08-23
申请号：US14377748
申请日：2013-02-07
申请人： Stella Pharma Corporation , Osaka Prefecture University Public Corporation
发明人： Mitsunori Kirihata , Kohki Uehara
IPC分类号： C07K11/02 , C07C229/08 , C07C235/12 , C07K14/32 , C07C229/24 , C07D273/00 , C07C237/12 , C07K11/00
CPC分类号： C07K11/02 , C07C229/08 , C07C229/24 , C07C235/12 , C07C237/12 , C07D273/00 , C07K11/00 , C07K14/32
摘要： The purpose of the present invention is to provide a novel method for producing cereulide and a derivative thereof; an intermediate for cereulide; and a novel cereulide derivative. A novel didepsipeptide, a novel tetradepsipeptide, a novel octadepsipeptide and a novel dodecadepsipeptide are prepared. A linear precursor of cereulide or a derivative thereof, which is composed of any one of the novel depsipeptides, is cyclized by forming an intramolecular amide bond.
摘要翻译：本发明的目的是提供一种制备大戟素及其衍生物的新方法; 大众中间物和一种新型的cereulide衍生物。制备了一种新型的七叶皂苷肽，一种新型的四肽类，一种新的十八肽和一种新的十二十一生物肽。通过形成分子内酰胺键将由任何一种新的缩肽组成的大脑或其衍生物的线性前体环化。

9. 发明授权

US09108942B1 Compositions and methods for the treatment of moderate to severe pain 有权
标题翻译：用于治疗中度至重度疼痛的组合物和方法
公开(公告)号：US09108942B1
公开(公告)日：2015-08-18
申请号：US14533135
申请日：2014-11-05
申请人： Mahesh Kandula
发明人： Mahesh Kandula
IPC分类号： C07C229/00 , A61K31/24 , C07D339/04 , C07C235/12
CPC分类号： C07D339/04 , C07C237/08 , C07C237/22
摘要： The invention relates to the compounds of formula I 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 I; and methods for treating or preventing moderate to severe pain, may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of muscle pain, spasticity, neuropathic pain, fibromyalgia, post-operative pain, muscle spasticity, headache, chronic pain, sub-chronic pain and local pain.
摘要翻译：本发明涉及式I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。药物组合物包含有效量的式I化合物; 以及用于治疗或预防中度至重度疼痛的方法可以配制用于口服，口腔，直肠，局部，透皮，经粘膜，静脉内，肠胃外给药，糖浆或注射。此类组合物可用于治疗肌肉疼痛，痉挛症，神经性疼痛，纤维肌痛，手术后疼痛，肌肉痉挛，头痛，慢性疼痛，亚慢性疼痛和局部疼痛。

10. 发明授权

US08946475B2 Processes for preparing a polymeric compound 有权
标题翻译：制备聚合物的方法
公开(公告)号：US08946475B2
公开(公告)日：2015-02-03
申请号：US13720298
申请日：2012-12-19
申请人： Cellceutix Corporation
发明人： Robert W. Kavash , Haizhong Tang , Carol Mulrooney , Dahui Liu
IPC分类号： C07C231/14 , C07C231/12 , C07C271/52 , C07C233/05 , C07C233/65 , C07C235/12 , C07C271/22
CPC分类号： C07C231/12 , C07C231/02 , C07C231/10 , C07C231/14 , C07C235/12 , C07C237/34 , C07C271/22 , C07C271/52 , C07C237/44
摘要： The present invention provides methods for preparing a polymeric compound of Formula I: or pharmaceutically acceptable salt thereof. The present invention also provides useful intermediates for preparing the compound of Formula I or pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供制备式I的高分子化合物或其药学上可接受的盐的方法。本发明还提供了制备式I化合物或其药学上可接受的盐的有用的中间体。

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