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1. 发明授权

US10633329B2 Method for preparing lisinopril intermediate 有权
公开(公告)号：US10633329B2
公开(公告)日：2020-04-28
申请号：US16461589
申请日：2017-11-17
申请人： ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD. , ZHEJIANG HUAHAI TIANCHENG PHARMACEUTICALS CO., LTD. , ZHEJIANG HUAHAI LICHENG PHARMACEUTICALS CO., LTD.
发明人： Songqing Wang , Peng Dong , Yang Zheng , Quanjun Li
IPC分类号： C07C227/08 , C07C303/00 , C07C303/28 , C07C229/36
CPC分类号： C07C227/08 , C07C303/28 , C07C229/36
摘要： A method for preparing a lisinopril intermediate is provided. The method includes: treating (R)-hydroxy-4-phenylbutyrate with sulfonyl chloride in an organic solvent in the presence of a base to obtain a solution of sulfonate; reacting the obtained solution with a salt of trifluoroacetyl lysine; and obtaining a N2-[1-(S)-alkoxycarbonyl-3-phenylpropyl]-N6-trifluoroacetyl-L-lysine by separating after the reaction is completed. The method provided has a shorter synthesis route, is easy to operate, has a low cost, and is suitable for industrial production.

2. 发明申请

US20160122294A1 METHODS FOR CO-PRODUCTION OF ALKYLBENZENE AND AN OLEOCHEMICAL FROM NATURAL OILS 审中-公开
标题翻译：从天然油中共同生产烷基苯酚和化学成分的方法
公开(公告)号：US20160122294A1
公开(公告)日：2016-05-05
申请号：US14527592
申请日：2014-10-29
申请人： UOP LLC
发明人： Daniel L. Ellig , Andrea G. Bozzano
IPC分类号： C07C303/00 , C07C5/327 , C07C2/66 , C07C1/20
CPC分类号： C07C1/20 , C07C1/2078 , C07C1/213 , C07C1/22 , C07C2/66 , C07C5/327 , C07C67/08 , C07C303/00 , C07C303/26 , C07C2527/1206 , C07C2527/126 , C10G3/42 , C10G3/50 , C10G29/205 , C10G57/005 , C10G2300/1011 , C10G2400/30 , C11C1/005 , C11C1/04 , C11C3/00 , C11C3/003 , Y02P30/20 , C07C11/02 , C07C309/67 , C07C69/52 , C07C15/107 , C07C9/14
摘要： Embodiments of methods for co-production of linear alkylbenzene and oleochemicals from a natural oil are provided. An exemplary method includes fat splitting the natural oil to form a stream comprising free fatty chains. The method includes fractionating the stream of free fatty chains to separate a first portion of free fatty chains and a second portion of free fatty chains. Further, the method includes processing the first portion of free fatty chains to provide the alkylbenzene product and processing the second portion of free fatty chains to form the oleochemical products.
摘要翻译：提供了从天然油共生产线性烷基苯和油化合物的方法的实施方案。一种示例性的方法包括将天然油分解成形成包含游离脂肪链的物流。该方法包括分离游离脂肪链流以分离游离脂肪链的第一部分和游离脂肪链的第二部分。此外，该方法包括加工游离脂肪链的第一部分以提供烷基苯产物并加工第二部分游离脂肪链以形成油化学产物。

3. 发明授权

US08853448B2 Aromatic sulfonylimides, preparation thereof and use thereof as electrolyte 有权
标题翻译：芳族磺酰亚胺，其制备及其作为电解质的用途
公开(公告)号：US08853448B2
公开(公告)日：2014-10-07
申请号：US12309462
申请日：2007-07-17
申请人： Jean-Yves Sanchez , Bernard Langlois , Maurice Medebielle , Fabien Toulgoat , Fannie Alloin , Elie Paillard , Cristina Iojoiu
发明人： Jean-Yves Sanchez , Bernard Langlois , Maurice Medebielle , Fabien Toulgoat , Fannie Alloin , Elie Paillard , Cristina Iojoiu
IPC分类号： C07C303/00 , C07F7/08 , H01M10/0525 , C07C317/14 , H01M6/16 , H01M6/18 , C07C323/67 , H01G11/62 , H01G9/022 , H01M10/0565 , H01M10/0566 , H01M6/06
CPC分类号： C07C323/67 , C07C317/14 , C07F7/081 , H01G9/038 , H01G11/62 , H01M6/06 , H01M6/166 , H01M6/181 , H01M6/183 , H01M6/188 , H01M10/0525 , H01M10/0565 , H01M10/0566 , Y02E60/122 , Y02E60/13
摘要： The invention relates to a process for preparing aromatic sulfonylimides, to the sulfonylimides obtained, and to the use thereof as salt of an electrolyte. The sulfonylimides correspond to the formula [R—SO2—N—SO2R′]rM (I). R′ is an ArZL- group. R′ is a perfluoroalkyl group or an ArZL- group. Z is an S, SO or SO2 group. L is a —(CF2)n—CFRf— group. n is 0 or 1; Rf represents F or a C1 to C8 perfluoroalkyl group; Ar is an aromatic group. M represents H, an alkali metal cation, an alkaline earth metal cation, a trivalent or tetravalent metal cation, or an organic cation. The process consists in preparing a compound RSO2N(R′)SO2R′ from RSO2F, and in replacing the group R′ by nucleophilic substitution reaction so as to obtain the compound (I), R′ being a benzyl or trimethylsilyl group.
摘要翻译：本发明涉及制备芳族磺酰亚胺，所得磺酰亚胺及其作为电解质盐的用途的方法。磺酰亚胺对应于式[R-SO 2 -N-SO 2 R'] r M（I）。 R'是一个ArZL-组。 R'是全氟烷基或ArZL-基团。 Z是S，SO或SO2基团。 L是 - （CF2）n-CFRf-基团。 n为0或1; Rf表示F或C1〜C8全氟烷基; Ar是芳族基团。 M表示H，碱金属阳离子，碱土金属阳离子，三价或四价金属阳离子或有机阳离子。该方法包括从RSO2F制备化合物RSO2N（R'）SO2R'，并通过亲核取代反应代替基团R'，得到化合物（I），R'为苄基或三甲基甲硅烷基。

4. 发明授权

US08772541B2 Cannabinoid receptor 2 (CB2) inverse agonists and therapeutic potential for multiple myeloma and osteoporosis bone diseases 有权
标题翻译：大麻素受体2（CB2）反向激动剂和多发性骨髓瘤和骨质疏松症骨病的治疗潜力
公开(公告)号：US08772541B2
公开(公告)日：2014-07-08
申请号：US13715603
申请日：2012-12-14
申请人： University of Pittsburgh—Of the Commonwealth System of Higher Education
发明人： Xiang-qun Xie , Peng Yang , Rentian Feng
IPC分类号： A01N41/06 , A01N37/18 , A01N33/02 , A61K31/18 , A61K31/165 , A61K31/135 , C07C303/00 , C07C307/00 , C07C309/00 , C07C311/00 , C07C239/00 , C07C321/00
CPC分类号： C07C233/40 , C07C69/78 , C07C233/11 , C07C233/13 , C07C233/22 , C07C233/36 , C07C233/63 , C07C233/78 , C07C311/05 , C07C311/18 , C07C311/20 , C07C311/29 , C07C311/48 , C07C2601/14 , C07C2603/74 , C07D203/08 , C07D211/06 , C07D213/56 , C07D235/12 , C07D295/135
摘要： Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 are independently H, alkyl, or alkenyl; R3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; R4 and R5 are independently a bond, alkylenyl, or alkenylenyl; each R6 and R7 is independently selected from the group consisting of OH, F, Cl, Br, I, (C1-C6)alkyl, alkoxy, amino, COOH, CONH2, SO3H, PO3H2, CN, SH, NO2 and CF3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma.
摘要翻译：大麻素受体-2反向拮抗剂包括由式IV表示的化合物或其药学上可接受的盐：其中：R 1和R 2独立地为H，烷基或烯基; R3是烷基，烯基，芳基，芳烷基，芳烯基，杂环基，杂环基烷基，杂芳基，杂芳基烷基; R4和R5独立地是键，亚烷基或烯基; 每个R 6和R 7独立地选自OH，F，Cl，Br，I，（C 1 -C 6）烷基，烷氧基，氨基，COOH，CONH 2，SO 3 H，PO 3 H 2，CN，SH，NO 2和CF 3; 且p和q独立地为0,1,2,3,4或5.这些化合物可用于治疗骨质疏松症或多发性骨髓瘤。

5. 发明授权

US08759578B2 Method for manufacturing fluorine-containing imide compound 失效
标题翻译：含氟酰亚胺化合物的制造方法
公开(公告)号：US08759578B2
公开(公告)日：2014-06-24
申请号：US13699568
申请日：2011-05-25
申请人： Tsunetoshi Honda , Noriaki Matsumura
发明人： Tsunetoshi Honda , Noriaki Matsumura
IPC分类号： C07C303/00 , C07C307/00 , C07C309/00 , C07C311/00 , C07C303/38
CPC分类号： C07C303/38 , C07C311/48
摘要： With this method for manufacturing fluorine-containing imide compounds, a method for manufacturing a fluorine-containing imide compound ((Rf1SO2)(Rf2SO2)NH) is selected which includes reaction of a fluorine-containing sulfonic acid (Rf1SO3H) and a fluorine-containing sulfonamide (Rf2SO2NH) in the presence of thionyl chloride. Wherein, Rf1 and Rf2 are fluorine, or straight-chain or branched perfluoroalkyl groups with a carbon number of 1-4.
摘要翻译：利用这种制造含氟酰亚胺化合物的方法，选择含氟酰亚胺化合物（（Rf1SO2）（Rf2SO2）NH）的制造方法，其包括含氟磺酸（Rf 1 SO 3 H）与含氟酰亚胺化合物磺酰胺（Rf2SO2NH）在亚硫酰氯存在下反应。其中，Rf1和Rf2是氟，或碳数为1-4的直链或支链全氟烷基。

6. 发明授权

US08722005B1 Synthesis of hydrogen bis(fluorosulfonyl)imide 有权
标题翻译：双（氟磺酰基）酰亚胺的合成
公开(公告)号：US08722005B1
公开(公告)日：2014-05-13
申请号：US13951973
申请日：2013-07-26
申请人： Joseph Carl Poshusta , Jerry Lynn Martin , Rajendra P. Singh
发明人： Joseph Carl Poshusta , Jerry Lynn Martin , Rajendra P. Singh
IPC分类号： C01B21/086 , C07C303/00
CPC分类号： C01B21/0935 , H01G11/06 , H01G11/58
摘要： The invention provides a method for producing hydrogen bis(fluorosulfonyl)imide (HFSI) by reacting hydrogen bis(halosulfonyl)imide (HXSI) with hydrogen fluoride, where each X is independently a nonfluoro-halide, such as Cl, Br, or I.
摘要翻译：本发明提供了通过使双（卤代磺酰基）酰亚胺（HXSI）与氟化氢反应生成氢双（氟磺酰基）酰亚胺（HFSI）的方法，其中每个X独立地是非氟卤化物，例如Cl，Br或I.

7. 再颁专利

USRE44874E1 Phenethanolamine derivatives for treatment of respiratory diseases 有权
标题翻译：苯乙醇胺衍生物用于治疗呼吸系统疾病
公开(公告)号：USRE44874E1
公开(公告)日：2014-04-29
申请号：US13719797
申请日：2012-12-19
申请人： Glaxo Group Limited
发明人： Philip Charles Box , Diane Mary Coe , Brian Edgar Looker , Panayiotis Alexandrou Procopiou
IPC分类号： C07C273/00 , C07C303/00 , C07C233/00 , A61K31/00
摘要： The present invention relates to novel compounds of formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases
摘要翻译：本发明涉及式（I）的新化合物，其制备方法，含有它们的药物组合物及其在治疗中的用途，特别是其在预防和治疗呼吸系统疾病中的用途

8. 发明授权

US08686179B2 Fluorinated aromatic bis(acyl)-containing compounds and polyesters prepared therefrom 有权
标题翻译：含氟芳香族双（酰基）的化合物和由其制备的聚酯
公开(公告)号：US08686179B2
公开(公告)日：2014-04-01
申请号：US13322217
申请日：2010-06-07
申请人： Yu Yang , Lei Wang , George G. I. Moore
发明人： Yu Yang , Lei Wang , George G. I. Moore
IPC分类号： C07C303/00
CPC分类号： C07C317/48 , C07C41/09 , C07C41/16 , C07C311/09 , C07C315/04 , C08G63/6856 , C08G63/6886 , C09D167/02 , C07C43/174
摘要： A fluorinated bis(acyl)-containing compound of Formula (I), where R1, Ar, L, R2, R3, Rf, n, p and q are as defined in the claims, and a fluorinated polyester formed from the fluorinated bis(acyl) compound are described. More particularly, the fluorinated bis(acyl) has an aromatic ring bonded to two acyl groups plus at least one third group that contains a perfluoroalkylsulfonamido group. The fluorinated polyesters formed from the fluorinated bis(acyl)-containing compound can be used to provide a low energy surface with a relatively low refractive index compared to many other polyesters. A method of preparing a monosubstituted-arylene compound of formula Rf1-L2-CH2—Ar2—CH2—W, where Ar2, Rf1, L2, R6 and W are as defined in the claims by reaction of a compound of formula Rf1-L2-H with a compound of formula W—CH2—Ar2—CH2—W.
摘要翻译：式（I）的含氟双（酰基）的化合物，其中R 1，Ar，L，R 2，R 3，R f，n，p和q如权利要求中所定义，和由氟化双酰基）化合物。更具体地，氟化双（酰基）具有键合到两个酰基加上含有全氟烷基磺酰氨基的至少三个基团的芳环。由含氟二（酰基）的化合物形成的氟化聚酯可以用于提供与许多其它聚酯相比折射率相对较低的低能量表面。制备式Rf1-L2-CH2-Ar2-CH2-W的单取代 - 亚芳基化合物的方法，其中Ar2，Rf1，L2，R6和W如权利要求中所定义，如式Rf1-L2- H与式W-CH 2 -Ar 2 -CH 2 -W的化合物反应。

9. 发明授权

US08642809B2 Methods of synthesis of certain hydroxamic acid compounds 有权
标题翻译：合成某些异羟肟酸化合物的方法
公开(公告)号：US08642809B2
公开(公告)日：2014-02-04
申请号：US12678594
申请日：2008-09-23
申请人： Helge A. Reisch , Peter Leeming , Prasad S. Raje
发明人： Helge A. Reisch , Peter Leeming , Prasad S. Raje
IPC分类号： C07C303/00
CPC分类号： C07C303/40 , C07C311/21
摘要： The present invention pertains to the general field of chemical synthesis, and more particularly to methods for the synthesis of certain hydroxamic acid compounds, and in particular, (E)-N-hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide, also known as PXD101 and Belinostat®, comprising, for example, the steps of: (SAF) sulfonamide formation; (PURC) optional purification; (AAA) alkenyl-acid addition, comprising: either (i): the steps of, in order: (ACAEA) alkenyl-carboxylic acid ester addition; (PURE) optional purification; and (CAD) carboxylic acid deprotection; or (ii): the step of: (ACAA) alkenyl-carboxylic acid addition; (PURF) optional purification; (HAF) hydroxamic acid formation; and (PURG) optional purification.
摘要翻译：本发明涉及化学合成的一般领域，更具体地涉及合成某些异羟肟酸化合物，特别是（E）-N-羟基-3-（3-苯基氨磺酰基 - 苯基） - 丙烯酰胺的方法，也称为PXD101和Belinostat，包括例如以下步骤：（SAF）磺酰胺的形成; （PURC）可选净化; （AAA）烯基酸添加，包括：（i）：以下步骤：按顺序：（ACAEA）烯基 - 羧酸酯添加; （PURE）可选净化; 和（CAD）羧酸脱保护; 或（ii）：步骤：（ACAA）烯基 - 羧酸添加; （PURF）可选净化; （HAF）异羟肟酸形成; 和（PURG）可选纯化。

10. 发明授权

US08642808B2 Bis-aryl sulfonamides 有权
标题翻译：双芳基磺酰胺
公开(公告)号：US08642808B2
公开(公告)日：2014-02-04
申请号：US13092615
申请日：2011-04-22
申请人： Solomon Ungashe , Zheng Wei , John J. Wright , Andrew Pennell , Brett Permack , Thomas Schall
发明人： Solomon Ungashe , Zheng Wei , John J. Wright , Andrew Pennell , Brett Permack , Thomas Schall
IPC分类号： C07C303/00 , A61K31/33 , A61K31/35 , A61K31/397
CPC分类号： C07D213/26 , A61K31/4245 , A61K31/433 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D213/50 , C07D213/70 , C07D213/74 , C07D213/84 , C07D213/89 , C07D241/12 , C07D413/12
摘要： Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists.
摘要翻译：提供了作为趋化因子受体的有效拮抗剂的化合物。化合物通常为芳基磺酰胺衍生物，可用于药物组合物，治疗趋化因子受体介导的疾病的方法，以及用于鉴定趋化因子拮抗剂的测定中的对照。

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