公开(公告)号：US20230331666A1

公开(公告)日：2023-10-19

申请号：US18026877

申请日：2021-12-21

申请人： KAO CORPORATION

发明人： Yoshinori MITSUDA ,  Keisuke CHIBA ,  Masato NOMURA

IPC分类号： C07C303/28 ,  C09K23/10 ,  C11D1/28

CPC分类号： C07C303/28 ,  C09K23/10 ,  C11D1/28

摘要： A method for producing a sulfonate composition including, reacting a diester of a predetermined unsaturated carboxylic acid [hereinafter referred to as component (A)] in the presence of one or more solvents selected from (B) (B1) an organic solvent [hereinafter referred to as component (B1)] and (B2) water [hereinafter referred to as component (B2)] with (C) a sulfonating agent to obtain a mixture containing (S) a predetermined sulfonate having a diester structure [hereinafter referred to as component (S)], and removing an insoluble component from the mixture, wherein in the mixture from which the removal of the insoluble component is made, the content of component (B1) to a total content of components (S), (B1) and (B2) is 0.05 or more and 0.65 or less, and the content of component (B2) to the total content of components (S), (B1) and (B2) is 0.03 or more and 0.26 or less.

公开(公告)号：US11649205B2

公开(公告)日：2023-05-16

申请号：US17055124

申请日：2019-06-20

申请人： ASAHI KASEI KABUSHIKI KAISHA

发明人： Nobuyuki Uematsu ,  Hideki Date ,  Yasuhiro Nagato ,  Akitake Nakamura ,  Kenichi Yakigaya

IPC分类号： C07C309/10 ,  C07C303/22 ,  C07C303/28 ,  C07C303/32 ,  C07C309/65 ,  C07C309/66 ,  C07C309/80

CPC分类号： C07C309/10 ,  C07C303/22 ,  C07C303/28 ,  C07C303/32 ,  C07C309/65 ,  C07C309/66 ,  C07C309/80

摘要： The present disclosure is directed to provide a vinylsulfonic anhydride which is useful as a synthetic intermediate for synthesis of a fluorinated monomer. It is also directed to efficiently produce the vinylsulfonic anhydride. It is further directed to efficiently produce a fluorinated monomer using the vinylsulfonic anhydride. A vinylsulfonic anhydride of the present disclosure is expressed by the general formula (1). Further, a process for producing a vinylsulfonic anhydride of the present disclosure includes making a vinylsulfonic acid compound represented by the general formula (2) come in contact and be mixed with an anhydridization agent. Further, a process for producing a vinylsulfonyl fluoride of the present disclosure includes a step (b) of making a vinylsulfonic anhydride represented by the general formula (1) come in contact and be mixed with a fluorinating agent to prepare a reaction mixture including a vinylsulfonyl fluoride represented by the general formula (3) and a vinylsulfonic acid compound represented by the general formula (2).

公开(公告)号：US10005712B2

公开(公告)日：2018-06-26

申请号：US15116176

申请日：2015-01-14

申请人： Bizen Chemical Co., Ltd.

发明人： Yoshio Shimizu ,  Naomichi Bamba ,  Mitsumasa Mankura

IPC分类号： C07C51/00 ,  C07C67/24 ,  C07C51/353

CPC分类号： C07C67/24 ,  C07C17/093 ,  C07C17/361 ,  C07C29/147 ,  C07C51/353 ,  C07C67/32 ,  C07C67/343 ,  C07C303/28 ,  C07C69/587 ,  C07C33/02 ,  C07C69/602 ,  C07C309/73 ,  C07C21/215

摘要： The present invention relates to a method for the chemical conversion of an unsaturated fatty acid, particularly a carbon chain extension reaction. According to the present invention, a method for extending the length of a carbon chain in an unsaturated fatty acid by two carbon atoms is provided, said method comprising a step of heating a malonic acid ester derivative of an unsaturated fatty acid to reflux in a lower fatty acid solution in the presence of an antioxidative agent. It is preferred that the unsaturated fatty acid is an unsaturated fatty acid having 16 to 24 carbon atoms. It is preferred that the unsaturated fatty acid is selected from the group consisting of linoleic acid, linolenic acid, arachidonic acid, stearidonic acid, icosatetraenoic acid, icosapentaenoic acid, tetracosahexaenoic acid and docosahexaenoic acid. According to the method of the present invention, a carbon chain extension reaction can be completed within a shorter time.

公开(公告)号：US20170246195A1

公开(公告)日：2017-08-31

申请号：US15294519

申请日：2016-10-14

申请人： Antipodean Pharmaceuticals Inc.

发明人： Kenneth Martin Taylor ,  Robin A.J. Smith

IPC分类号： A61K31/66 ,  C07C309/66 ,  C07C303/30 ,  C07F9/54 ,  A61K31/724 ,  C07C303/28

CPC分类号： A61K31/66 ,  A61K31/724 ,  C07C303/28 ,  C07C303/30 ,  C07C2601/16 ,  C07F9/5442 ,  C07C309/66

摘要： This invention relates to pharmaceutically acceptable amphiphilic antioxidant compounds, compositions and dosage forms comprising said compounds and methods and uses reliant on said compounds. The exemplified compounds are all mitoquinone derivatives, being methoxyphenyl alkyl triphenylphosphonium or methoxy dioxocyclohexadiene alkyl triphenylphosphonium derivatives. The compounds, compositions, dosage forms, uses and methods are useful in, for example, the treatment of diseases or conditions associated with oxidative stress.

公开(公告)号：US20170158652A1

公开(公告)日：2017-06-08

申请号：US15435964

申请日：2017-02-17

申请人： ADVERIO PHARMA GMBH

发明人： Peter FEY ,  Alfons GRUNENBERG ,  Donald BIERER

IPC分类号： C07D295/104

CPC分类号： C07D295/104 ,  C07B2200/13 ,  C07C303/28 ,  C07C309/04 ,  C07C317/04 ,  C07D265/30 ,  C07D295/067 ,  C07D471/04 ,  C07C309/65

摘要： The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.

公开(公告)号：US09388125B2

公开(公告)日：2016-07-12

申请号：US13697287

申请日：2011-05-11

申请人： Ajay Purohit ,  Pedro Benites ,  Edward H. Cheesman ,  Joel Lazewatsky ,  L. Veronica Lee ,  Richard R. Cesati ,  Richard J. Looby ,  Heike S. Radeke

发明人： Ajay Purohit ,  Pedro Benites ,  Edward H. Cheesman ,  Joel Lazewatsky ,  L. Veronica Lee ,  Richard R. Cesati ,  Richard J. Looby ,  Heike S. Radeke

IPC分类号： A61K51/00 ,  A61M36/14 ,  C07C277/08 ,  A61K51/04 ,  C07B59/00 ,  C07C53/06 ,  C07C217/58 ,  C07C255/54 ,  C07C279/10 ,  C07C279/24 ,  C07C309/65 ,  C07C309/66 ,  C07C309/73 ,  C07C53/10 ,  C07C53/18 ,  C07C63/08 ,  C07C213/02 ,  C07C303/28 ,  C07C303/30 ,  C07C309/04 ,  C07C309/30 ,  C07C277/00

CPC分类号： C07C303/30 ,  A61K51/00 ,  A61K51/04 ,  A61K51/0406 ,  C07B59/001 ,  C07B2200/05 ,  C07C53/06 ,  C07C53/10 ,  C07C53/18 ,  C07C63/08 ,  C07C213/02 ,  C07C217/58 ,  C07C255/54 ,  C07C277/00 ,  C07C277/08 ,  C07C279/10 ,  C07C279/24 ,  C07C303/28 ,  C07C309/04 ,  C07C309/30 ,  C07C309/65 ,  C07C309/66 ,  C07C309/73 ,  C07C279/08

摘要： The present invention generally relates to novel synthetic methods, systems, kits, salts, and precursors useful in medical imaging. In some embodiments, the present invention provides compositions comprising an imaging agent precursor, which may be formed using the synthetic methods described herein. An imaging agent may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 18F. In some cases, an imaging agent including salt forms (e.g., ascorbate salt) may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.

摘要翻译： 本发明一般涉及可用于医学成像的新型合成方法，系统，试剂盒，盐和前体。 在一些实施方案中，本发明提供了包含可以使用本文所述的合成方法形成的成像剂前体的组合物。 可以使用本文所述的方法将成像剂转化成成像剂。 在某些情况下，成像剂富集于18F。 在一些情况下，包括盐形式的成像剂（例如抗坏血酸盐）可用于对受试者感兴趣的区域进行成像，包括但不限于心脏，心血管系统，心脏血管，脑和其他器官 。

公开(公告)号：US20150210634A1

公开(公告)日：2015-07-30

申请号：US14511725

申请日：2014-10-10

申请人： Theracos, Inc.

发明人： Jacques Roberge ,  Carine Vaxelaire ,  Baohu Liu ,  Ge Xu ,  Jian Zhang ,  Xinxing Tang ,  Baihua Xu

IPC分类号： C07C309/75 ,  C07C41/09 ,  C07C37/50

CPC分类号： C07C309/73 ,  C07B2200/05 ,  C07B2200/13 ,  C07C37/055 ,  C07C37/50 ,  C07C41/09 ,  C07C41/16 ,  C07C41/24 ,  C07C41/26 ,  C07C41/40 ,  C07C303/28 ,  C07C309/75 ,  C07C2601/02 ,  C07C39/367 ,  C07C43/225 ,  C07C43/196

摘要： Methods for preparing intermediates of SGLT2 inhibitors are provided, including crystalline forms and methods of crystallizing intermediates.

摘要翻译： 提供了制备SGLT2抑制剂中间体的方法，包括结晶形式和中间体结晶方法。

公开(公告)号：US20140315926A1

公开(公告)日：2014-10-23

申请号：US14320875

申请日：2014-07-01

申请人： Bayer Intellectual Property GmbH

发明人： Peter FEY

IPC分类号： C07D471/04 ,  C07C309/04 ,  C07D265/30

CPC分类号： C07D295/104 ,  C07B2200/13 ,  C07C303/28 ,  C07C309/04 ,  C07C317/04 ,  C07D265/30 ,  C07D295/067 ,  C07D471/04 ,  C07C309/65

摘要： The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.

公开(公告)号：US08637713B2

公开(公告)日：2014-01-28

申请号：US13705884

申请日：2012-12-05

申请人： Novartis AG

发明人： Christian Mathes ,  Michael Foulkes ,  Martin Kesselgruber

IPC分类号： C07C37/00 ,  C07C213/02 ,  C07C269/00 ,  C07C309/65 ,  A61K31/095

CPC分类号： C07C269/04 ,  C07B2200/07 ,  C07C37/002 ,  C07C213/02 ,  C07C213/08 ,  C07C303/28 ,  C07C303/30 ,  C07C309/66 ,  C07C215/50 ,  C07C39/11

摘要： A catalytic process for the preparation of optically active compounds and their conversion thereafter to desired drug substances. In particular, the process relates to the preparation of (S)-3-(1-Dimethylamino-ethyl)-phenol using asymmetric catalytic reduction and transfer hydrogenation, thereby providing an improved route to forming drug substances such as rivastigimine and rivastigimine hydrogen tartrate.

摘要翻译： 用于制备光学活性化合物的催化方法及其转化为所需药物。 具体而言，该方法涉及使用不对称催化还原和转移氢化制备（S）-3-（1-二甲基氨基 - 乙基） - 苯酚，从而提供形成药物物质如拉伐斯他明和酒石酸氢铵的改进途径。

公开(公告)号：US20140012024A1

公开(公告)日：2014-01-09

申请号：US14006717

申请日：2012-03-16

申请人： Mohamed Amin Khan ,  Paul L. Wood

发明人： Mohamed Amin Khan ,  Paul L. Wood

IPC分类号： C07C51/09 ,  C07C303/28 ,  C07C67/317 ,  C07C69/606

CPC分类号： C07C51/09 ,  C07C29/103 ,  C07C67/30 ,  C07C67/303 ,  C07C67/317 ,  C07C69/606 ,  C07C303/28 ,  C07C309/73 ,  C07C69/608 ,  C07C69/587 ,  C07C57/03 ,  C07C33/04

摘要： A method for preparing docosahexaenoic acid (DHA). The method comprises coupling a compound represented by Formula I with a compound represented by Formula II followed by partial hydrogenation to obtain a compound represented by Formula III. The compound represented by Formula III acts as a DHA precursor and thus can be hydrolysed to obtain DHA. Novel starting materials represented by Formula I and Formula II, and synthetic routes for preparing the same are also provided.

摘要翻译： 二十二碳六烯酸（DHA）的制备方法。 该方法包括将由式I表示的化合物与由式II表示的化合物偶联，然后进行部分氢化，得到式III表示的化合物。 由式III表示的化合物用作DHA前体，因此可以水解以获得DHA。 还提供了由式I和式II表示的新型起始物质及其制备方法。