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1. 发明申请

US20180339968A1 QUATERNARY HETEROATOM CONTAINING COMPOUNDS 审中-公开
公开(公告)号：US20180339968A1
公开(公告)日：2018-11-29
申请号：US16049434
申请日：2018-07-30
申请人： California Institute of Technology
发明人： Brian M. Stoltz , Scott C. Virgil , David E. White , Taiga Yurino , Yiyang Liu , Douglas C. Behenna , Douglas Duquette , Christian Eidamshaus
IPC分类号： C07D211/78 , C07D223/10 , C07D309/04 , C07D207/16 , C07D211/60 , C07D211/90 , C07D207/277 , C07D207/273 , C07D207/267 , C07D309/30 , C07D211/96 , C07D211/94 , C07D211/88 , C07D211/76 , C07D211/38 , C07D211/34 , C07D211/22 , C07D211/18 , C07D211/16 , C07D207/46 , C07D207/27 , C07D207/263 , C07D207/26 , C07D207/10 , C07D207/08 , C07D265/30 , C07D207/06 , C07D241/52 , C07D241/08 , C07D241/04 , C07D223/04 , C07D265/32
CPC分类号： C07D211/78 , C07D207/06 , C07D207/08 , C07D207/10 , C07D207/16 , C07D207/26 , C07D207/263 , C07D207/267 , C07D207/27 , C07D207/273 , C07D207/277 , C07D207/46 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/34 , C07D211/38 , C07D211/60 , C07D211/76 , C07D211/88 , C07D211/90 , C07D211/94 , C07D211/96 , C07D223/04 , C07D223/10 , C07D241/04 , C07D241/08 , C07D241/52 , C07D265/30 , C07D265/32 , C07D309/04 , C07D309/30
摘要： The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): comprising treating a compound of Formula (I): with a transition metal catalyst and under alkylation conditions as valence and stability permit.

2. 发明申请

US20180222859A1 Process for the Selective Production of N-Methyl-2-Pyrrolidone (NMP) 审中-公开
公开(公告)号：US20180222859A1
公开(公告)日：2018-08-09
申请号：US15749426
申请日：2016-05-17
申请人： COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
发明人： Indrajit Kumar GHOSH , Suman Lata JAIN , Praveen Kumar KHATRI , Siddharth Sankar RAY , Madhukar Onkarnath GARG
IPC分类号： C07D207/267 , B01J29/06 , B01J29/076 , B01J29/90 , B01J35/10
CPC分类号： C07D207/267 , B01J29/061 , B01J29/076 , B01J29/90 , B01J35/1019 , Y02P20/584
摘要： This invention relates to an improved process for the selective production of N-methyl pyrrolidone (NMP) from gamma-butyrolactone and monomethyl amine preferably in aqueous form in the presence of a catalyst under comparatively milder conditions than the processes well known in the prior art of literature. The process is economically viable as it provides higher yield and selectivity for NMP which reduces the cost of separation of NMP from GBL. The catalyst shows good recyclability without significant loss in catalytic activity and no frequent regeneration is required.

4. 发明申请

US20180072682A1 COMPOSITIONS FOR THE TREATMENT OF FIBROSIS AND FIBROSIS-RELATED CONDITIONS 审中-公开
公开(公告)号：US20180072682A1
公开(公告)日：2018-03-15
申请号：US15557762
申请日：2016-03-18
申请人： VECTUS BIOSYSTEMS LIMITED
发明人： KAREN ANNETTE DUGGAN
IPC分类号： C07D233/78 , C07C215/54 , C07D207/26 , C07D207/38 , C07D233/96 , C07D261/14 , C07D263/38 , C07C239/20 , C07D263/44 , C07D209/48 , C07C59/54 , C07C39/12
CPC分类号： C07D233/78 , C07C39/12 , C07C39/15 , C07C47/575 , C07C59/52 , C07C59/54 , C07C215/48 , C07C215/54 , C07C239/20 , C07D207/26 , C07D207/267 , C07D207/36 , C07D207/38 , C07D207/408 , C07D207/448 , C07D209/48 , C07D233/96 , C07D261/14 , C07D263/38 , C07D263/44
摘要： The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of fibrosis and fibrosis-related conditions.

5. 发明授权

US09822116B2 Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds 有权
公开(公告)号：US09822116B2
公开(公告)日：2017-11-21
申请号：US15012422
申请日：2016-02-01
申请人： OPKO Health, Inc.
发明人： George G. Wu , Gerald Werne , Xiaoyong Fu , Robert K. Orr , Frank Xing Chen , Jian Cui , Victoria M. Sprague , Fucheng Zhang , Ji Xie , Liansheng Zeng , Louis Peter Castellanos , Yuyin Chen , Marc Poirier , Ingrid Mergelsberg
IPC分类号： C07D207/267 , C07C217/46 , C07D207/28 , C07D471/10 , C07D207/26 , C07D498/04 , C07C217/48
CPC分类号： C07D471/10 , C07C217/46 , C07C217/48 , C07D207/26 , C07D207/267 , C07D207/28 , C07D498/04
摘要： This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.

6. 发明申请

US20170283380A1 Intermediate for Synthesizing Paroxetine, Method for Preparing the same, and Uses Thereof 审中-公开
公开(公告)号：US20170283380A1
公开(公告)日：2017-10-05
申请号：US15511244
申请日：2015-06-15
申请人： Zhejiang Jiuzhou Pharmaceutical Co., Ltd.
发明人： Xiaoming FENG , Yu ZHANG , Xiaohua LIU , Qian YAO , Lili LIN , Guoliang ZHU
IPC分类号： C07D211/88 , C07D231/12
CPC分类号： C07D211/88 , C07C201/12 , C07C205/53 , C07D207/267 , C07D231/12 , C07D231/16 , C07D405/06 , C07D409/06
摘要： A paroxetine intermediate, a method for preparing the same, and uses thereof are provided. Specifically, the method includes: reacting a compound of formula I below with a compound of formula II in the presence of air organic base under the catalysis of a complex formed from a chiral amine oxide L and a rare-earth metal compound Ln(OTf)3 to prepare a compound of formula III below: wherein R1 is alkyl, phenyl or benzyl; R2, R3, R4 are each independently C1-C6 alkyl or C6-C10 aryl; the chiral amine oxide L has the following structure: wherein n=1, 2; and R=Ph-, 2,6-Me2C6H3-, 2,6-Et2C6H3-, 2,6-iPr2C6H3-, Ph2CH—.

7. 发明申请

US20170247317A1 COMPOUNDS, MONOMERS, AND POLYMERS CONTAINING A CARBONATE LINKAGE 审中-公开
公开(公告)号：US20170247317A1
公开(公告)日：2017-08-31
申请号：US15592784
申请日：2017-05-11
申请人： ISP INVESTMENTS LLC
发明人： Ezat Khosravi , Osama M. Musa
IPC分类号： C07C69/96 , C08F226/10 , C08F226/06 , C08F218/08 , C07D207/27 , C08F126/06
CPC分类号： C07C69/96 , C07C69/54 , C07C303/02 , C07C303/36 , C07D205/08 , C07D205/12 , C07D207/26 , C07D207/263 , C07D207/267 , C07D207/27 , C07D207/28 , C07D227/12 , C07D245/00 , C07D245/02 , C07D245/04 , C07D245/06 , C08F20/36 , C08F26/06 , C08F26/10 , C08F120/36 , C08F126/06 , C08F218/08 , C08F220/00 , C08F226/06 , C08F226/10 , C08F2220/346
摘要： The invention provides compounds and monomers having a carbonate linkage. The monomers can be used to form homopolymers or can be coupled with other monomers to provide a wide variety of non-homopolymers. The invention further provides a wide variety of compositions comprising the compounds, monomers, and polymers. In the exemplary structures below, Q, A, R, and n are as described herein.

8. 发明授权

US09624158B2 Hydroxy aliphatic substituted phenyl aminoalkyl ether derivatives 有权
公开(公告)号：US09624158B2
公开(公告)日：2017-04-18
申请号：US14654661
申请日：2013-12-20
申请人： PROUS INSTITUTE FOR BIOMEDICAL RESEARCH, S.A.
发明人： Josep R. Prous , Neus Serradell , Ramon Flores , Noemi Garcia-Delgado , Marcel-li Carbo Banus
IPC分类号： A61K31/7028 , A61K31/138 , A61K31/192 , C07C217/04 , C07D207/267 , A61K31/4015 , C07D307/62 , A61K31/375 , C07C59/68 , A61K31/385 , A61K31/5375 , C07H15/22 , A61K31/7004 , A61K45/06 , C07D333/20 , C07D339/04 , C07H15/18 , C07D265/30 , C07D211/22 , C07C271/16 , C07C217/48 , C07C217/74 , C07C233/18 , C07D207/27 , C07D209/08
CPC分类号： A61K31/138 , A61K31/165 , A61K31/192 , A61K31/375 , A61K31/381 , A61K31/385 , A61K31/4015 , A61K31/4045 , A61K31/451 , A61K31/5375 , A61K31/7004 , A61K31/7034 , A61K45/06 , C07C59/68 , C07C217/04 , C07C217/48 , C07C217/74 , C07C233/18 , C07C271/16 , C07C2101/08 , C07C2101/14 , C07C2601/08 , C07C2601/14 , C07D207/267 , C07D207/27 , C07D209/08 , C07D211/22 , C07D265/30 , C07D307/62 , C07D333/20 , C07D339/04 , C07H15/18 , C07H15/22
摘要： New hydroxy aliphatic substituted phenyl aminoalkyi ether compounds of formula (I), compositions thereof and their use as a medicament in the treatment of nervous system diseases and/or the treatment of developmental, behavioral and/or mental disorders associated with cognitive deficits.

9. 发明申请

US20170029353A1 METHODS FOR PREPARATION OF AMMONIUM SALTS OF C4 DIACIDS BY FERMENTATION AND INTEGRATED METHODS FOR MAKING C4 DERIVATIVES THEREOF 审中-公开
标题翻译：通过发酵和制备C4衍生物的一体化方法制备C4 DIACIDS的氨基磺酸盐的方法
公开(公告)号：US20170029353A1
公开(公告)日：2017-02-02
申请号：US15278649
申请日：2016-09-28
申请人： ARCHER DANIELS MIDLAND COMPANY
发明人： ChiCheng Ma , Todd Werpy
IPC分类号： C07C51/493 , C12P7/46
CPC分类号： C07C51/493 , C07C29/149 , C07C51/412 , C07C51/42 , C07D207/267 , C07D307/33 , C12P7/46 , C07C55/02 , C07C57/15 , C07C59/245 , C07C55/10
摘要： Disclosed herein are methods for forming ammonium salts of C4 diacids in a fermentation process with simultaneous removal of divalent metal carbonate salts. The pH of fermentation broths obtained during the production of fumaric, maleic, malic, and/or succinic acid by a microorganism is controlled by using alkaline oxygen containing calcium or magnesium compounds in the hydroxide, oxide, carbonate or bicarbonate forms—forming divalent metal salts of the diacids that are partially or wholly insoluble in the broth. The calcium or magnesium salts of the diacids are substituted with ammonium by introduction of ammonium salts at elevated temperature and pressure dissolving precipitated divalent metal cation salts of the diacids and forming soluble ammonium salts thereof. Carbonate in the form of CO2 or bicarbonate is simultaneously added to the fermentation media at the elevated temperature and pressure. The temperature and pressure are then reduced forming insoluble divalent metal carbonate salts that are separated from the solubilized ammonium diacid salts. The recovered metal carbonate salts can be recycled as pH control materials in subsequent fermentation reactions. Also disclosed is use of the solubilized ammonium diacid salts directly as a reagent for hydrogenation to form the derivatives N-methyl-2-pyrrolidone (NMP) gamma-butyrolactone (GBL) and 1,4-butane-diol (BDO) in single pot reactions.
摘要翻译：本文公开了在发酵过程中形成C4二酸铵盐的方法，同时除去二价金属碳酸盐。在微生物生产富马酸，马来酸，苹果酸和/或琥珀酸期间获得的发酵肉汤的pH值通过在氢氧化物，氧化物，碳酸盐或碳酸氢盐形式的二价金属盐中使用含有钙或镁的化合物来控制的部分或完全不溶于肉汤的二酸。二元酸的钙盐或镁盐通过在升高的温度下引入铵盐和溶解二酸的沉淀二价金属阳离子盐并形成其可溶性铵盐而被铵取代。 CO 2或碳酸氢盐形式的碳酸盐在升高的温度和压力下同时加入到发酵培养基中。然后降低温度和压力，形成不溶性二价金属碳酸盐，其与可溶性二铵酸盐分离。回收的金属碳酸盐可以在随后的发酵反应中作为pH控制材料再循环。还公开了将溶解的二铵二酸盐直接用作氢化的试剂以在单锅中形成N-甲基-2-吡咯烷酮（NMP）γ-丁内酯（GBL）和1,4-丁二醇（BDO）反应。

10. 发明申请

US20160347760A1 Bicyclic-Fused Heteroaryl or Aryl Compounds 审中-公开
标题翻译：双环稠合杂芳基或芳基化合物
公开(公告)号：US20160347760A1
公开(公告)日：2016-12-01
申请号：US15232892
申请日：2016-08-10
申请人： Pfizer Inc.
发明人： John David Trzupek , Katherine Lin Lee , Mark Edward Bunnage , Seungil Han , David Hepworth , Frank Eldridge Lovering , John Paul Mathias , Nikolaos Papaioannou , Betsy Susan Pierce , Joseph Walter Strohbach , Stephen Wayne Wright , Christoph Wolfgang Zapf , Lori Krim Gavrin , Arthur Lee , David Randolph Anderson , Kevin Joseph Curran , Christoph Martin Dehnhardt , Eddine Saiah , Joel Adam Goldberg , Xiaolun Wang , Horng-Chih Huang , Richard Vargas , Michael Dennis Lowe , Akshay Patny
IPC分类号： C07D491/056 , A61K31/4709 , C07D405/12 , C07D215/48 , A61K31/47 , A61K31/4725 , C07D417/12 , A61K31/541 , C07D413/12 , A61K31/5377 , C07D207/267 , A61K31/4015 , C07D207/08 , A61K31/40 , C07D407/14 , C07D487/04 , C07D403/12 , A61K31/517 , A61K45/06 , C07D401/12
CPC分类号： C07D491/056 , A61K31/40 , A61K31/4015 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , C07C69/94 , C07D207/08 , C07D207/26 , C07D207/267 , C07D207/273 , C07D209/52 , C07D215/48 , C07D217/02 , C07D217/22 , C07D217/24 , C07D239/86 , C07D239/88 , C07D263/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D407/14 , C07D413/12 , C07D417/12 , C07D487/04 , C07D498/04 , C07F7/1804
摘要： Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
摘要翻译：如说明书中所定义。还公开了相应的药物组合物，治疗方法，合成方法和中间体。

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