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1. 发明授权

US10053414B2 Treprostinil derivatives and compositions and uses thereof 有权
公开(公告)号：US10053414B2
公开(公告)日：2018-08-21
申请号：US15617243
申请日：2017-06-08
申请人： CORSAIR PHARMA, INC.
发明人： Xiaoming Zhang , Meenakshi S. Venkatraman , Cyrus K. Becker
IPC分类号： C07C69/734 , C07C69/732 , A61K31/216 , C07C69/26 , C07C69/675 , C07C69/708 , C07C69/712 , C07C69/96 , C07D303/48 , A61K9/00 , A61K9/70 , A61K45/06 , C07C69/013
CPC分类号： C07C69/734 , A61K9/0014 , A61K9/7023 , A61K31/216 , A61K45/06 , C07C69/013 , C07C69/26 , C07C69/675 , C07C69/708 , C07C69/712 , C07C69/732 , C07C69/96 , C07C2601/04 , C07C2601/14 , C07C2603/14 , C07D303/48
摘要： The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.

2. 发明授权

US09701616B2 Treprostinil derivatives and compositions and uses thereof 有权
公开(公告)号：US09701616B2
公开(公告)日：2017-07-11
申请号：US15178637
申请日：2016-06-10
申请人： CORSAIR PHARMA, INC.
发明人： Xiaoming Zhang , Meenakshi S. Venkatraman , Cyrus K. Becker
IPC分类号： C07C69/732 , A61K31/216 , C07C69/013 , C07C69/26 , C07C69/675 , C07C69/708 , C07C69/712 , C07C69/96 , C07D303/48 , A61K9/00 , A61K9/70 , A61K45/06
CPC分类号： C07C69/734 , A61K9/0014 , A61K9/7023 , A61K31/216 , A61K45/06 , C07C69/013 , C07C69/26 , C07C69/675 , C07C69/708 , C07C69/712 , C07C69/732 , C07C69/96 , C07C2601/04 , C07C2601/14 , C07C2603/14 , C07D303/48
摘要： The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.

3. 发明授权

US09630957B2 2,3-butanediamide epoxide compound and preparation method and use thereof 有权
公开(公告)号：US09630957B2
公开(公告)日：2017-04-25
申请号：US14893391
申请日：2014-05-28
申请人： Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
发明人： Song Li , Junhai Xiao , Xian Zhang , Wu Zhong , Zhibing Zheng , Lili Wang , Yunde Xie , Xingzhou Li , Xinbo Zhou , Xiaokui Wang
IPC分类号： C07D417/12 , C07D303/48 , C07D417/14
CPC分类号： C07D417/12 , C07D303/48 , C07D417/14
摘要： Provided are a compound of formula I which can be used as a drug against small RNA virus infections, and optical isomers, pharmaceutically acceptable salts, solvates or hydrates thereof. Also provided are the preparation method of the compound, the method for using the compound for treating bacterial infections and the use of the compound in the preparation of a drug for preventing and/or treating viral diseases caused by small RNA viruses.

4. 发明授权

US09403843B2 Cysteine protease inhibitors and uses thereof 有权
标题翻译：半胱氨酸蛋白酶抑制剂及其用途
公开(公告)号：US09403843B2
公开(公告)日：2016-08-02
申请号：US14376361
申请日：2013-02-01
申请人： The Trustees of Columbia University in the City of New York
发明人： Gregory R. J. Thatcher , Isaac Thomas Schiefer , Ottavio Arancio , Mauro Fa
IPC分类号： C07D403/12 , C07D409/12 , C07D417/12 , C07D417/14 , C07D303/48 , C07D495/04 , C07D405/12
CPC分类号： C07D417/12 , C07D303/48 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/14 , C07D495/04
摘要： The invention provides for novel cysteine protease inhibitors and compositions comprising novel cysteine protease derivatives. The invention further provides for methods for treatment of neurodegenerative diseases comprising administration novel cysteine protease inhibitors or compositions comprising novel cysteine protease inhibitors. In some embodiments, the cysteine protease inhibitors are calpain inhibitors.
摘要翻译：本发明提供了新型半胱氨酸蛋白酶抑制剂和包含新型半胱氨酸蛋白酶衍生物的组合物。本发明进一步提供治疗神经变性疾病的方法，包括给予新型半胱氨酸蛋白酶抑制剂或包含新型半胱氨酸蛋白酶抑制剂的组合物。在一些实施方案中，半胱氨酸蛋白酶抑制剂是钙蛋白酶抑制剂。

5. 发明申请

US20160102067A1 OXIRAN AMINES 审中-公开
公开(公告)号：US20160102067A1
公开(公告)日：2016-04-14
申请号：US14442229
申请日：2013-11-15
申请人： V-BIOTEK HOLDING APS
发明人： Jens Steen OLSEN
IPC分类号： C07D303/48
CPC分类号： C07D303/48 , C07C233/09
摘要： Disclosed herein are oxiran amines useful for the treatment of a variety of diseases. The oxiran amines are useful in the manufacture of pharmaceutical compositions. The pharmaceutical composition may be used for the treatment or prevention of a disease caused by a virus having a lipid membrane or the pharmaceutical composition may be used for diseases requiring cell proliferation or immune-regulation.
摘要翻译：本文公开了可用于治疗各种疾病的环氧乙烷胺。环氧乙烷胺可用于制备药物组合物。药物组合物可用于治疗或预防由具有脂质膜的病毒引起的疾病，或者该药物组合物可用于需要细胞增殖或免疫调节的疾病。

6. 发明授权

US09174955B2 Manufacture of an epoxyethyl carboxylate or glycidyl carboxylate 有权
标题翻译：环氧乙基羧酸酯或羧酸缩水甘油酯的制备
公开(公告)号：US09174955B2
公开(公告)日：2015-11-03
申请号：US13574693
申请日：2011-01-26
申请人： Prasad Muppa , Ron Postma , Caspar Schoolderman , Sandra Rens , Kostas Stoitsas
发明人： Prasad Muppa , Ron Postma , Caspar Schoolderman , Sandra Rens , Kostas Stoitsas
IPC分类号： C07D303/12 , C07D301/12 , C07D303/48
CPC分类号： C07D301/12 , C07D303/48
摘要： The invention relates to a process for the manufacture of an epoxyethyl carboxylate or glycidyl carboxylate, including reacting a vinyl carboxylate or an allyl carboxylate using an oxidant and a water-soluble manganese complex in an aqueous reaction medium, and the water-soluble manganese complex comprises an oxidation catalyst, characterized in that the water-soluble manganese complex is a mononuclear species of the general formula (I) [LMnX3]Y (I), or a binuclear species of the general formula (II): [LMn(μ-X)3MnL]Yn (II), wherein Mn is a manganese; L is a ligand and each L is independently a polydentate ligand, each X is independently a coordinating species and each μ-X is independently a bridging coordinating species, Y is a non-coordinating counter ion, and wherein the epoxidation is carried out at a pH in the range of from 1.0 to 7.0.
摘要翻译：本发明涉及一种制备环氧乙基羧酸酯或缩水甘油羧酸酯的方法，包括在水性反应介质中使用氧化剂和水溶性锰络合物使羧酸乙烯酯或烯丙基羧酸酯反应，并且水溶性锰络合物包括其特征在于所述水溶性锰络合物是通式（I）[LMnX 3] Y（I）的单核物种或通式（II）的双核物种：[LMn（μ-X ）3MnL] Yn（II），其中Mn是锰; L是配体，每个L独立地是多齿配体，每个X独立地是配位物质，每个μ-X独立地是桥联配位物质，Y是非配位抗衡离子，其中环氧化在 pH范围为1.0-7.0。

7. 发明申请

US20140128255A1 Fungicidal Alkyl-Substituted 2-[2-chloro-4-(4-chloro-phenoxy)-phenyl]-1-[1,2,4]triazol-1-yl-ethanol Compounds 有权
标题翻译：杀真菌烷基取代的2- [2-氯-4-（4-氯 - 苯氧基） - 苯基] -1- [1,2,4]三唑-1-基 - 乙醇化合物
公开(公告)号：US20140128255A1
公开(公告)日：2014-05-08
申请号：US14232462
申请日：2012-07-11
申请人： Jochen Dietz , Richard Riggs , Nadege Boudet , Jan Klaas Lohmann , Ian Robert Craig , Egon Haden , Erica May Wilson Lauterwasser , Bernd Mueller , Wassilios Grammenos , Thomas Grote
发明人： Jochen Dietz , Richard Riggs , Nadege Boudet , Jan Klaas Lohmann , Ian Robert Craig , Egon Haden , Erica May Wilson Lauterwasser , Bernd Mueller , Wassilios Grammenos , Thomas Grote
IPC分类号： A01N43/653
CPC分类号： A01N43/653 , A01N43/02 , C07D249/08 , C07D303/18 , C07D303/48 , C07D405/06
摘要： The present invention relates to the use of alkyl-substituted 2-[2-chloro-4-(4-chloro-phenoxy)-phenyl]-1-[1,2,4]triazol-1-yl-ethanol compounds of formula I as defined in the description, and the N-oxides, and salts thereof for combating harmful fungi and seed coated with at least one such compound. The invention also relates to novel alkyl-substituted 2-[2-chloro-4-(4-chloro-phenoxy)-phenyl]-1-[1,2,4]triazol-1-yl-ethanol compounds, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound.
摘要翻译：本发明涉及使用烷基取代的2- [2-氯-4-（4-氯 - 苯氧基） - 苯基] -1- [1,2,4]三唑-1-基 - 乙醇式描述中所定义的I，以及用于防治有害真菌的N-氧化物及其盐和用至少一种这样的化合物包衣的种子。本发明还涉及新的烷基取代的2- [2-氯-4-（4-氯 - 苯氧基） - 苯基] -1- [1,2,4]三唑-1-基 - 乙醇化合物，方法和中间体用于制备这些化合物以及包含至少一种这样的化合物的组合物。

8. 发明申请

US20130184490A1 PROCESS TO PREPARE S-2-HYDROXY-3-METHOXY-3,3-DIPHENYL PROPIONIC ACID 审中-公开
标题翻译：制备S-2-羟基-3-甲氧基-3,3-二苯基丙酸的方法
公开(公告)号：US20130184490A1
公开(公告)日：2013-07-18
申请号：US13814038
申请日：2010-08-04
申请人： Amala Kompella , Kali Satya Bhujanga Rao Adibhatla , Veera Swamy Balina , Srinivasu Kasa , Venkaiah Chowdary Nannapaneni
发明人： Amala Kompella , Kali Satya Bhujanga Rao Adibhatla , Veera Swamy Balina , Srinivasu Kasa , Venkaiah Chowdary Nannapaneni
IPC分类号： C07C51/09
CPC分类号： C07C51/09 , C07B2200/07 , C07C51/02 , C07C51/412 , C07C67/31 , C07D303/48 , C07C59/66 , C07C69/734
摘要： Disclosed is a process for the preparation of S-2-Hydroxy-3-methoxy-3,3-diphenylpropionic acid (I) the key intermediate for the preparation of Ambrisentan [(+)-2(S)-(4,6-Dimethylpyrimidin-2-yloxy)-3-methoxy-3,3-diphenylpropionic acid]. Ambrisentan of the formula (IA) is approved under the trademark “Letairis ®” by the US Food and Drug Administration for the treatment of Pulmonary artery hypertension (PAH).
摘要翻译：公开了一种制备S-2-羟基-3-甲氧基-3,3-二苯基丙酸（I）的方法，该方法是制备安立生坦[（+） - 2（S） - （4,6-二 -2,3-二甲基嘧啶-2-基氧基）-3-甲氧基-3,3-二苯基丙酸]。式（IA）的安立生坦由美国食品和药物管理局以商标“Letairis®”批准用于治疗肺动脉高压（PAH）。

9. 发明申请

US20130131359A1 PROCESSES AND INTERMEDIATES FOR PREPARING STERIC COMPOUNDS 审中-公开
标题翻译：制备化合物的方法和中间体
公开(公告)号：US20130131359A1
公开(公告)日：2013-05-23
申请号：US13740707
申请日：2013-01-14
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： GERALD J. TANOURY , Minzhang Chen , Young Chun Jung , Raymond E. Forslund
IPC分类号： C07C231/12 , C07C247/06 , C07C59/255 , C07J75/00 , C07J9/00 , C07D303/48 , C07C51/41
CPC分类号： C07C231/12 , C07B2200/05 , C07B2200/07 , C07C51/412 , C07C59/255 , C07C231/20 , C07C237/04 , C07C247/04 , C07C247/06 , C07C2601/02 , C07D209/52 , C07D301/14 , C07D303/48 , C07D401/14 , C07D403/12 , C07D403/14 , C07D498/10 , C07J9/005 , C07J75/00 , C07K5/0202 , C07K7/02
摘要： This invention relates to processes and intermediates for the preparation of an alpha-amino beta-hydroxy acid of Formula 1 wherein the variables R1, R′1 and R2 are defined herein and the compound of Formula 1 has an enantiomeric excess (ee) of 55% or greater.
摘要翻译：本发明涉及用于制备式1的α-氨基β-羟基酸的方法和中间体，其中变量R1，R'1和R2在本文中定义，式1的化合物具有55的对映体过量（ee）％以上。

10. 发明申请

US20130006001A1 MANUFACTURE OF AN EPOXYETHYL CARBOXYLATE OR GLYCIDYL CARBOXYLATE 有权
标题翻译：环氧乙烷羧酸酯或羧甲基纤维素的制备
公开(公告)号：US20130006001A1
公开(公告)日：2013-01-03
申请号：US13574693
申请日：2011-01-26
申请人： Prasad Muppa , Ron Postma , Caspar Schoolderman , Sandra Rens , Kostas Stoitsas
发明人： Prasad Muppa , Ron Postma , Caspar Schoolderman , Sandra Rens , Kostas Stoitsas
IPC分类号： C07D301/03 , C07D303/48 , C07D301/12
CPC分类号： C07D301/12 , C07D303/48
摘要： The invention relates to a process for the manufacture of an epoxyethyl carboxylate or glycidyl carboxylate, including reacting a vinyl carboxylate or an allyl carboxylate using an oxidant and a water-soluble manganese complex in an aqueous reaction medium, and the water-soluble manganese complex comprises an oxidation catalyst, characterized in that the water-soluble manganese complex is a mononuclear species of the general formula (I) [LMnX3]Y (I), or a binuclear species of the general formula (II): [LMn(μ−X)3MnL]Yn (II), wherein Mn is a manganese; L is a ligand and each L is independently a polydentate ligand, each X is independently a coordinating species and each μ−X is independently a bridging coordinating species, Y is a non-coordinating counter ion, and wherein the epoxidation is carried out at a pH in the range of from 1.0 to 7.0
摘要翻译：本发明涉及一种制备环氧乙基羧酸酯或缩水甘油羧酸酯的方法，包括在水性反应介质中使用氧化剂和水溶性锰络合物使羧酸乙烯酯或烯丙基羧酸酯反应，并且水溶性锰络合物包括其特征在于所述水溶性锰络合物是通式（I）[LMnX 3] Y（I）的单核物种或通式（II）的双核物种：[LMn（μ-X ）3MnL] Yn（II），其中Mn是锰; L是配体，每个L独立地是多齿配体，每个X独立地是配位物质，每个μ-X独立地是桥联配位物质，Y是非配位抗衡离子，其中环氧化在 pH范围为1.0-7.0

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