公开(公告)号：US20220378921A1

公开(公告)日：2022-12-01

申请号：US17857531

申请日：2022-07-05

申请人： ALNYLAM PHARMACEUTICALS, INC.

发明人： Jayaprakash K. Nair ,  Alexander V. Kel'in ,  Pachamuthu Kandasamy ,  Kallanthottathil G. Rajeev ,  Muthiah Manoharan

IPC分类号： A61K47/54 ,  C07H1/00 ,  A61K31/7088 ,  C07C231/14 ,  C07D207/12 ,  C07H15/26 ,  C12N15/113

摘要： This disclosure relates to an improved process for the preparation of carbohydrate conjugates. The disclosure also relates to carbohydrate conjugated iRNA agents comprising these carbohydrate conjugates, which have improved purity and are advantageous for the in vivo delivery of the iRNA agents.

公开(公告)号：US20210387942A1

公开(公告)日：2021-12-16

申请号：US17323349

申请日：2021-05-18

申请人： DUPONT SAFETY & CONSTRUCTION, INC.

发明人： James A. Schultz ,  SOURAV KUMAR SENGUPTA ,  VENKATESWARA RAO SURISETTY

IPC分类号： C07C231/14 ,  B01J21/16 ,  B01J29/70 ,  B01J39/20 ,  B01J8/02 ,  B01J19/14

摘要： A method of making N-(2,4-dinitrophenyl)-4-nitrobenzamide from a mixture of 2,4-dinitroaniline, 4-nitrobenzoyl chloride, and solid acid catalyst in an organic solvent, wherein the solid acid catalyst is not soluble in the organic solvent, the solid acid catalyst being an acidic clay, an ion exchange resin, a beta zeolite, a sulfonated tetrafluoroethylene-based fluoropolymer-copolymer, or some mixture of these.

公开(公告)号：US20210338623A1

公开(公告)日：2021-11-04

申请号：US17245861

申请日：2021-04-30

申请人： MBI Distributing

发明人： Ned L. Jensen

IPC分类号： A61K31/22 ,  A61K31/4045 ,  A61K47/24 ,  A61K47/10 ,  A61K47/14 ,  A61K9/127 ,  C07C231/14 ,  A61P15/00 ,  A61P25/22 ,  A61P25/28 ,  A61P25/20 ,  A61P25/06

摘要： The present invention is directed to compositions comprising N-Acetyl Methyl GABA, methods of preparing N-Acetyl Methyl GABA and compositions including N-Acetyl Methyl GABA, and methods of using N-Acetyl Methyl GABA for instance to improve sleep and control anxiety.

公开(公告)号：US20210188775A1

公开(公告)日：2021-06-24

申请号：US17249457

申请日：2021-03-02

申请人： Genentech, Inc.

发明人： Christian CUNNINGHAM ,  Paul Powell BEROZA ,  James John CRAWFORD ,  Wendy Lee ,  Olivier RENE ,  Jason Robert ZBIEG ,  Jiangpeng LIAO ,  Tao WANG ,  Chen YU

IPC分类号： C07D213/76 ,  C07C311/08 ,  C07C303/40 ,  C07C235/46 ,  C07C231/14 ,  C07D213/82 ,  C07D209/08 ,  C07D237/24

摘要： The invention is concerned with the compounds of formula (I) and formula (II): and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of using the compounds of formula (I) and formula (II) as well as pharmaceutical compositions containing such compounds. The compounds are useful in treating diseases and conditions mediated by TEAD, such as cancer.

公开(公告)号：US10766854B2

公开(公告)日：2020-09-08

申请号：US16756577

申请日：2018-10-19

申请人： SABIC GLOBAL TECHNOLOGIES B.V.

发明人： Shirish Shrikant Abhyankar ,  Abbas-Alli Ghudubhai Shaikh ,  Sivalingam Gunasekaran ,  Jaiprakash Brijlal Sainani

IPC分类号： C07C231/14

摘要： The present invention relates to a process for synthesis of a compound according to Formula (A): wherein R1 is a substituted or unsubstituted aryl having 6 to 20 carbon atoms; preferably substituted or unsubstituted phenyl; R2 is a straight or branched alkyl having 1 to 12 carbon atoms; and R3 is a straight or branched alkyl having 1 to 12 carbon atoms; starting from a di-keto compound according to Formula (B) wherein R3 is as shown above, which compound is converted into a ketoenamine compound according to Formula (C) wherein R2 and R3 are as shown above, which ketoenamine compound is then reduced to an amino alcohol according to Formula (D), wherein R2 and R3 are as shown above, that is subsequently converted into a compound according to Formula (A): characterized in that the ketoenamine is reduced into an amino alcohol using a nickel aluminium alloy in an aqueous solution of an inorganic base.

公开(公告)号：US20200207727A1

公开(公告)日：2020-07-02

申请号：US16634707

申请日：2018-08-23

申请人： 3M INNOVATIVE PROPERTIES COMPANY

发明人： Sean M. Smith

IPC分类号： C07D265/32 ,  C07C231/14 ,  C07D207/24

摘要： Described herein is an hydrofluorocarboximidate of formula (I) where: RH is a linear or branched alkyl group comprising 1 or 2 carbon atoms and (a) Rf1 and Rf2 are independent-selected from a linear or branched perfluorinated alkyl group comprising 1-8 carbon atoms and optionally comprising at least one catenated atom selected from oxygen, nitrogen, or combinations thereof; or (b) Rf1 and Rf2 are connected to form a ring structure comprising a total of 4-8 carbon atoms and in addition to the nitrogen atom from the carboximidate the ring structure may optionally comprises at least one catenated atom selected from oxygen, nitrogen, or combinations thereof. A method of making the hydrofluorocarboximidate with improved yield is described as well as various uses for the hydrofluorocarboximidate of Formula (I).

公开(公告)号：US20200095192A1

公开(公告)日：2020-03-26

申请号：US16618902

申请日：2018-05-30

申请人： PTT Global Chemical Public Company Limited

发明人： Papapida PORNSURIYASAK ,  Sophon KAEOTHIP

IPC分类号： C07C233/49 ,  C07C233/47 ,  C07C233/83 ,  C07C231/14

摘要： The present invention relates to a new diethanolamine derivative chelating agent having a high water solubility, a good chelating property, and biological degradation. The said new chelating agent can be prepared from reaction of diethanolamine and cyclic anhydride compound using lewis acid as the catalyst. The said process is uncomplicated, and does not use a severe condition, and also reduces the use of harmful chemicals.

公开(公告)号：US20200087248A1

公开(公告)日：2020-03-19

申请号：US16489474

申请日：2018-04-19

申请人： SICHUAN KELUN-BIOTECH BIOPHARMACEUTICAL CO., LTD.

发明人： Jiawang ZHU ,  Zhiquan SONG ,  Long YANG ,  Rui LI ,  Shuai ZHANG ,  Lin ZHOU ,  Mingliang ZHAO ,  Zujian TANG ,  Wei ZHONG ,  Hong ZENG ,  Hongmei SONG ,  Xin ZHOU ,  Yuting TANG ,  Xiao HU ,  Lichun WANG ,  Jingyi WANG

IPC分类号： C07C235/56 ,  C07C231/14 ,  C07D217/04 ,  C07D277/24 ,  C07D209/44 ,  C07D211/16 ,  C07D239/26 ,  C07D235/18 ,  C07D277/66 ,  C07C211/24 ,  C07D309/14 ,  C07D213/40 ,  C07D319/16

摘要： The present invention relates to a fluoroallylamine derivative and use thereof. In particular, the present invention relates to a compound as shown in Formula I, a prodrug, an isomer, an isotope-labeled compound, a solvate or a pharmaceutically acceptable salt thereof, which has VAP-1/SSAO inhibitory activity, and can be used for treating a disease associated with VAP-1/SSAO overactivity.

公开(公告)号：US10259776B2

公开(公告)日：2019-04-16

申请号：US16001146

申请日：2018-06-06

申请人： BAYER INTELLECTUAL PROPERTY GMBH

发明人： Michael Hahn ,  Thomas Lampe ,  Johannes-Peter Stasch ,  Karl-Heinz Schlemmer ,  Frank Wunder ,  Volkhart Min-Jian Li ,  Eva-Maria Becker-Pelster ,  Friederike Stoll ,  Andreas Knorr ,  Elisabeth Woltering

IPC分类号： C07C231/14 ,  A61K9/00 ,  A61K31/196 ,  A61K45/06 ,  C07C233/55 ,  C07C235/38

摘要： The present application relates to novel 3-phenylpropionic acid derivatives which carry a branched or cyclic alkyl substituent in the 3-position, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular diseases.

公开(公告)号：US20180370904A1

公开(公告)日：2018-12-27

申请号：US15779852

申请日：2016-02-29

申请人： HYBIO PHARMACEUTICAL CO., LTD.

发明人： Youjin CHEN ,  Pengcheng MI ,  Anjin TAO ,  Jiancheng YUAN

IPC分类号： C07C231/14 ,  C07C237/22 ,  B01J31/02

CPC分类号： C07C231/14 ,  B01J31/0247 ,  B01J2231/49 ,  C07B41/12 ,  C07B43/06 ,  C07B2200/07 ,  C07C231/02 ,  C07C231/12 ,  C07C235/08 ,  C07C237/22 ,  C07C269/06 ,  Y02P20/55 ,  C07C271/16 ,  C07C237/08 ,  C07C237/12

摘要： The present invention relates to a preparation method of a long-chain compound, which includes the following steps: (1) carrying out condensation reaction on H—R2 and R5N-Glu(OR4)—OR3, wherein, R3 is a carboxyl protecting group, R4 is a carboxyl activating group, and R5 is an amino protecting group; obtaining a compound of formula II; (2) removing carboxyl protecting group R3 and amino protecting group R5 of the compound shown in formula II to obtain a compound of formula III; (3) carrying out condensation reaction on the compound shown in formula III and to obtain a compound shown in formula I. The method reduces the time of deprotection, and all the reactions can be carried out in a solvent with low boiling point. The post-processing requires only simple washing and recrystallization to obtain the product with higher purity, so the method is suitable for large-scale production.