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1. 发明申请

US20210130315A1 METHOD FOR THE SYNTHESIS OF CYCLIC DEPSIPEPTIDES 有权
公开(公告)号：US20210130315A1
公开(公告)日：2021-05-06
申请号：US16762068
申请日：2018-11-06
申请人： Bayer Animal Health GmbH , THE KITASATO INSTITUTE
发明人： Dirk HEIMBACH , Satoshi OMURA , Toshiaki SUNAZUKA , Tomoyasu HIROSE , Yoshihiko NOGUCHI , Johannes KÖBBERLING , Zhijie WU , Shuibiao FU , Wei WU , Jinfeng QIU , Liu HE , Xudong WEI
IPC分类号： C07D325/00 , A61K38/15
摘要： The present invention relates to a method for the synthesis of cyclic depsipeptides, in particular emodepside, from the open form.

2. 发明申请

US20200297724A1 COVALENT INHIBITORS OF CDK-7 审中-公开
公开(公告)号：US20200297724A1
公开(公告)日：2020-09-24
申请号：US16661054
申请日：2019-10-23
申请人： Newave Pharmaceutical Inc.
发明人： Yi Chen , Yan Lou
IPC分类号： A61K31/506 , C07D498/08 , C07D491/06 , A61K31/165 , C07D325/00
摘要： The disclosure includes compounds of Formula (I) wherein R0, R1, R2, R3, R4, R5, and L are defined herein. Also disclosed is a method for treating a neoplastic disease, autoimmune disease, and inflammatory disorder with these compounds.

3. 发明授权

US10195200B2 Covalent inhibitors of CDK-7 有权
公开(公告)号：US10195200B2
公开(公告)日：2019-02-05
申请号：US15706980
申请日：2017-09-18
申请人： Newave Pharmaceutical Inc.
发明人： Yi Chen , Yan Lou
IPC分类号： A61K31/506 , A61K31/165 , A61K31/397 , A61K31/4015 , A61K31/45 , A61K31/497 , C07D498/08 , C07D491/06 , C07D325/00
摘要： The disclosure includes compounds of Formula (I) wherein R0, R1, R2, R3, R4, R5, and L are defined herein. Also disclosed is a method for treating a neoplastic disease, autoimmune disease, and inflammatory disorder with these compounds.

4. 发明申请

US20160096791A1 DIRECT ANTI-MARKOVNIKOV ADDITION OF ACIDS TO ALKENES 审中-公开
标题翻译：直接的抗马尔可维尔添加酸对阿尔卑斯
公开(公告)号：US20160096791A1
公开(公告)日：2016-04-07
申请号：US14787179
申请日：2014-05-02
申请人： THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL
发明人： David A. Nicewicz , David S. Hamilton
IPC分类号： C07C41/05 , C07C67/00 , B01J35/00 , C08F4/00 , C07B37/02 , B01J31/02 , C07D325/00 , C08F2/00
CPC分类号： C07C41/05 , B01J31/0217 , B01J31/0239 , B01J31/0244 , B01J31/1815 , B01J31/2295 , B01J35/004 , B01J2231/324 , B01J2531/842 , C07B37/02 , C07C67/00 , C07D207/46 , C07D209/26 , C07D213/89 , C07D291/06 , C07D325/00 , C08F2/00 , C08F4/00
摘要： A method of making an anti-Markovnikov addition product, comprises reacting an acid with an alkene or alkyne in a dual catalyst reaction system to the exclusion of oxygen to produce said anti-Markovnikov addition product; the dual catalyst reaction system comprising a single electron oxidation catalyst in combination with a hydrogen atom donor catalyst. Dual catalyst composition useful for carrying out such methods are also described.
摘要翻译：制备抗马尔可夫尼科夫加成产物的方法包括使酸与双催化剂反应体系中的烯烃或炔反应排除氧以产生所述抗马尔科夫尼科夫加成产物; 双重催化剂反应体系包括与氢原子供体催化剂组合的单电子氧化催化剂。还描述了用于实施这些方法的双重催化剂组合物。

5. 发明申请

US20140343283A1 METHODS OF PREPARING ICOTINIB AND ICOTINIB HYDROCHLORIDE, AND INTERMEDIATES THEREOF 有权
标题翻译： ICOTINIB和ICOTINIB HYDROCHLORIDE的制备方法及其中间体
公开(公告)号：US20140343283A1
公开(公告)日：2014-11-20
申请号：US14355142
申请日：2012-12-28
申请人： BETTA PHARMACEUTICALS CO., LTD.
发明人： Shaojing Hu , Wei Long , Fei Wang , Zongquan Li
IPC分类号： C07D491/056 , C07D405/04 , C07D325/00
CPC分类号： C07D491/056 , C07D323/00 , C07D325/00 , C07D405/04
摘要： The present invention relates to the technical field of medicine, and specifically provides methods for preparing Icotinib, Icotinib hydrochloride, and intermediates thereof. These methods avoid the use of phosphorus oxychloride, thereby greatly reducing the emission of pollutants, which is of major benefits to the economy and environment.
摘要翻译：本发明涉及医药技术领域，具体提供了制备伊可比，盐酸伊必替灵及其中间体的方法。这些方法避免使用三氯氧化磷，从而大大减少污染物的排放，这对经济和环境有重要的影响。

6. 发明授权

US5739394A 3,3-dioxy-4,4,4-trifluorobutyric acid derivatives 失效
标题翻译： 3,3-二氧基-4,4,4-三氟丁酸衍生物
公开(公告)号：US5739394A
公开(公告)日：1998-04-14
申请号：US767581
申请日：1996-12-16
申请人： Norbert Lui
发明人： Norbert Lui
IPC分类号： C07C43/313 , C07C43/315 , C07C45/51 , C07C51/00 , C07C59/135 , C07C59/64 , C07C67/00 , C07C67/27 , C07C67/39 , C07C69/708 , C07C69/712 , C07D317/16 , C07D317/30 , C07D319/06 , C07D321/06 , C07D325/00 , C07C59/00
CPC分类号： C07D317/30 , C07C43/313 , C07C43/315 , C07C45/515 , C07C59/135 , C07C67/00 , C07C67/27 , C07C69/708 , C07D317/16
摘要： The invention relates to novel 3,3-dioxy-4,4,4-trifluorobutyric acid derivatives of the formula (I) ##STR1## in which R.sup.1 and R.sup.2 independently of one another represent C.sub.1 -C.sub.10 -alkyl, or represent cyclohexyl, or represent optionally substituted C.sub.6 -C.sub.10 -aryl or C.sub.7 -C.sub.14 -arylalkyl, or R.sup.1 and R.sup.2 together represent C.sub.2 -C.sub.4 -alkylene which is optionally mono- or disubstituted by methyl, or optionally substituted ortho-arylene, R.sup.3 represents hydrogen or C.sub.1 -C.sub.10 -alkyl, or represents cycloalkyl, or represents optionally substituted C.sub.6 -C.sub.10 -aryl or C.sub.7 -C.sub.14 -arylalkyl, and X represents hydrogen, fluorine, chlorine or bromine, excluding methyl 4,4,4-trifluoro-3,3-dimethoxybutyrate, 4,4,4-trifluoro-3,3-dimethoxybutyric acid, ethyl 4,4,4-trifluoro-3,3-diethoxybutyrate, ethyl 4,4,4-trifluoro-3,3-ethylenedioxybutyrate and 4,4,4-trifluoro-3,3-ethylenedioxybutyric acid, a process for their preparation and for the preparation of further 3,3-dioxy-4,4,4-trifluorobutyric acid derivatives, as well as novel intermediates and processes for their preparation.
摘要翻译：本发明涉及式（I）的新的3,3-二氧基-4,4,4-三氟丁酸衍生物彼此表示C1-C10-烷基或代表环己基，或代表任选取代的C 6 -C 10 - 芳基或 C 7 -C 14 - 芳基烷基或R 1和R 2一起表示任选被甲基或任选取代的邻 - 亚芳基单取代或二取代的C 2 -C 4 - 亚烷基，R 3表示氢或C 1 -C 10 - 烷基，或表示环烷基，或表示任选取代的C 6 -C 10 - 芳基或C 7 -C 14 - 芳烷基，X代表氢，氟，氯或溴，不包括4,4,4-三氟-3,3-二甲氧基丁酸甲酯，4,4,4-三氟-3 ，3-二甲氧基丁酸，4,4,4-三氟-3,3-二乙氧基丁酸乙酯，4,4,4-三氟-3,3-亚乙二氧基丁酸乙酯和4,4,4-三氟-3,3-亚乙二氧基丁酸，其制备方法和制备其它的3,3-二氧基-4,4,4-三氟丁酸衍生物，以及其制备新颖的中间体和方法。

7. 发明授权

US5710286A Processes and intermediates for the preparation of cyclic urea HIV protease inhibitors 失效
标题翻译：用于制备环状尿素蛋白酶抑制剂的方法和中间体
公开(公告)号：US5710286A
公开(公告)日：1998-01-20
申请号：US557254
申请日：1995-11-14
申请人： Lucius Thomas Rossano , Young Sek Lo
发明人： Lucius Thomas Rossano , Young Sek Lo
IPC分类号： C07D243/04 , C07D323/00 , C07D491/04 , C07D491/056 , C07D325/00
CPC分类号： C07D491/04 , C07D243/04 , C07D323/00
摘要： This invention relates to novel compounds and derivatives thereof containing a trioxepane protected diol in addition to a hydrazone, hydrazine, amine, or cyclic urea moiety; methods for the preparation of said compounds; and the use of said compounds in processes to prepare human immunodeficiency virus (HIV) protease inhibitors which effectively inhibit HIV. The novel compounds provided by this invention have the formulae: ##STR1## wherein the substituents are as defined herein.
摘要翻译：本发明涉及除了腙，肼，胺或环脲部分之外含有三氧杂环戊烷保护的二醇的新化合物及其衍生物; 所述化合物的制备方法; 以及所述化合物在制备有效抑制HIV的人类免疫缺陷病毒（HIV）蛋白酶抑制剂的方法中的用途。本发明提供的新化合物具有下式：其中取代基如本文所定义。其中取代基如本文所定义。

8. 发明授权

US5338865A Synthesis of halichondrin B and norhalichondrin B 失效
标题翻译：软组蛋白B和去氢软脂素B的合成
公开(公告)号：US5338865A
公开(公告)日：1994-08-16
申请号：US011104
申请日：1993-01-29
申请人： Yoshito Kishi , Francis G. Fang , Craig J. Forsyth , Paul M. Scola , Suk K. Yoon
发明人： Yoshito Kishi , Francis G. Fang , Craig J. Forsyth , Paul M. Scola , Suk K. Yoon
IPC分类号： C07D307/12 , A61K31/335 , A61K31/365 , A61K31/695 , A61P35/00 , C07D307/04 , C07D307/20 , C07D307/93 , C07D309/02 , C07D309/06 , C07D309/10 , C07D311/00 , C07D311/02 , C07D311/58 , C07D323/00 , C07D325/00 , C07D407/06 , C07D493/04 , C07D493/22 , C07F7/18 , C07D309/00
CPC分类号： C07D407/06 , C07D307/20 , C07D309/10 , C07D493/04 , C07D493/22
摘要： Novel chemical compounds that can be used to synthesize halichondrin B and norhalichondrin B, and related derivatives, are described. The synthesis of halichondrin B and norhalichondrin B from these compounds also is described.
摘要翻译：描述了可用于合成软骨素B和去氢软脂素B及相关衍生物的新型化合物。还描述了这些化合物的软组蛋白B和去氢软脂素B的合成。

9. 发明授权

US4947005A Preparation of 1,1,2-trialkoxyethanes 失效
标题翻译： 1,1,2-三烷氧基乙醚的制备
公开(公告)号：US4947005A
公开(公告)日：1990-08-07
申请号：US398715
申请日：1989-08-25
申请人： Dieter Koeffer , Werner Bertleff
发明人： Dieter Koeffer , Werner Bertleff
IPC分类号： C07D325/00 , B01J31/20 , B01J31/26 , C07B61/00 , C07C41/48 , C07C43/315
CPC分类号： C07C41/48
摘要： 1,1,2-Trialkoxyethanes of the general formula I ##STR1## where R.sup.1 to R.sup.3 are each independently of the others C.sub.1 -C.sub.20 -alkyl or cycloalkyl, or R.sup.1 and R.sup.2 may be linked together to form a 5-, 6- or 7-membered ring, are prepared by reacting formaldehyde dialkyl acetals of the general formula II ##STR2## where R.sup.1 and R.sup.2 are each as defined above, or compounds which are capable of forming formaldehyde dialkyl acetals under the reaction conditions, with carbon monoxide, hydrogen and alkanols R.sup.3 OH under superatmospheric pressure at elevated temperature in the presence of a catalyst composed of a cobalt carbonyl compound and a promotor, wherein the promotor is an alkali metal, alkaline earth metal or ammonium salt of a protogenic compound having an acid constant K.sub.a of from 10.sup.-2 to 10.sup.-14, an alkali metal or alkaline earth metal hydroxide or an aminocarboxylic acid.
摘要翻译：其中R 1至R 3各自独立地为C 1 -C 20 - 烷基或环烷基的通式I（I）的1,1,2-三烷氧基乙基，或者R 1和R 2可以连接在一起形成5-， 6-或7-元环通过使通式II（II）的甲醛二烷基缩醛反应其中R1和R2各自如上所定义，或在反应条件下能够形成甲醛二烷基缩醛的化合物在由羰基钴化合物和促进剂组成的催化剂存在下，在高温下在超大气压下与一氧化碳，氢气和链烷醇R3OH反应，其中所述促进剂是原始化合物的碱金属，碱土金属或铵盐，其具有 10-2至10-14的酸常数K a，碱金属或碱土金属氢氧化物或氨基羧酸。

10. 发明授权

US4739081A New crown ether derivatives, process for the preparation thereof and ion-selective membrane electroes comprising the same 失效
标题翻译：新冠醚衍生物，其制备方法和包含其的离子选择性膜电极
公开(公告)号：US4739081A
公开(公告)日：1988-04-19
申请号：US667398
申请日：1984-11-01
申请人： Laszlo Toke , Bela gai , Istvan Bitter , Erno Pungor , Klara Szepesvary nee Toth , Erno Lindner , Maria Forro nee Horvath , Jeno Havas
发明人： Laszlo Toke , Bela gai , Istvan Bitter , Erno Pungor , Klara Szepesvary nee Toth , Erno Lindner , Maria Forro nee Horvath , Jeno Havas
IPC分类号： C08J5/22 , C07B61/00 , C07D323/00 , C07D405/00 , C07D405/14 , C07D407/00 , C07D407/04 , C07D407/12 , C07D407/14 , C08K5/15 , C08K5/159 , C08K5/20 , C08L27/06 , C08L83/04 , C09K3/00 , G01N27/333 , G01N27/40 , C07D325/00
CPC分类号： C07D405/14 , C07D323/00 , C07D407/14 , G01N27/3335
摘要： The invention relates to new crown ether derivatives of the general Formula I ##STR1## and a process for the preparation thereof wherein Z.sup.1 is a group of the general Formula ##STR2## R.sub.a and R.sub.b may be the same or different and R.sub.a represents an alkyl group having 1-4 carbon atoms and R.sub.b is an alkyl group having 1-20 carbon atoms.The new crown ethers are useful in the preparation of ion-selective electrodes having a long lifetime.

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