公开(公告)号：US20240327384A1

公开(公告)日：2024-10-03

申请号：US18580564

申请日：2022-07-21

申请人： Amgen Inc.

发明人： Tian WU ,  Prashant AGARWAL ,  Andreas R. ROTHELI ,  Hyunsoo PARK ,  Michael J. FROHN

IPC分类号： C07D401/14 ,  A61K31/506 ,  C07C15/06 ,  C07C31/02 ,  C07C31/04 ,  C07C31/08 ,  C07C43/04 ,  C07C43/18 ,  C07C49/08 ,  C07C55/02 ,  C07C55/22 ,  C07C69/003 ,  C07C233/05 ,  C07C255/03 ,  C07C275/06 ,  C07C309/04 ,  C07C309/65 ,  C07C309/73 ,  C07D211/90 ,  C07D275/06 ,  C07D307/06 ,  C07D319/12 ,  C07D487/04

CPC分类号： C07D401/14 ,  A61K31/506 ,  C07C15/06 ,  C07C31/02 ,  C07C31/04 ,  C07C31/08 ,  C07C43/046 ,  C07C43/18 ,  C07C49/08 ,  C07C55/02 ,  C07C55/22 ,  C07C69/003 ,  C07C233/05 ,  C07C255/03 ,  C07C275/06 ,  C07C309/04 ,  C07C309/65 ,  C07C309/73 ,  C07D211/90 ,  C07D275/06 ,  C07D307/06 ,  C07D319/12 ,  C07D487/04 ,  C07B2200/13 ,  C07C2601/08

摘要： Disclosed herein is a salt, a crystalline anhydrous form, a hydrate, a solvate, or a co-crystal of a free base compound 2-(6-azaspiro[2.5]octan-6-yl)-N-[2-(4,4-difluoropiperidin-1-yl)-6-methylpyrimidin-4-yl]-4-[(2-hydroxyethanesulfonyl)amino]benzamide (Compound A); method of preparation, pharmaceutical compositions, and method of treating a disease mediated by a motor protein kinesin family member 18A (KIF18A) inhibition, wherein said disease is a neoplastic disease, including a cancer or a tumor.

公开(公告)号：US20240199541A9

公开(公告)日：2024-06-20

申请号：US16256522

申请日：2019-01-24

申请人： SUZHOU PENGXU PHARMATECH CO. LTD.

发明人： Peng WANG ,  Pixu LI ,  Qiang WEI ,  Yuanhua LIU

IPC分类号： C07D207/27 ,  A61K31/4015 ,  C07C53/19 ,  C07C53/50 ,  C07C67/307 ,  C07C69/63 ,  C07C71/00 ,  C07C209/08 ,  C07C231/14 ,  C07C233/05 ,  C07C237/06

CPC分类号： C07D207/27 ,  A61K31/4015 ,  C07C53/19 ,  C07C53/50 ,  C07C67/307 ,  C07C69/63 ,  C07C71/00 ,  C07C209/08 ,  C07C231/14 ,  C07C233/05 ,  C07C237/06

摘要： The present invention provides a scalable synthesis of enantiomerically pure brivaracetam, and related derivatives.

公开(公告)号：US20230242572A1

公开(公告)日：2023-08-03

申请号：US17801514

申请日：2020-08-19

申请人： JIANGXI NORMAL UNIVERSITY

发明人： Junfeng ZHAO ,  Zhengning WANG ,  Xuewei WANG

IPC分类号： C07K1/06 ,  C07C69/145 ,  C07C67/08 ,  C07C69/753 ,  C07C69/78 ,  C07D307/68 ,  C07D231/56 ,  C07D333/70 ,  C07C69/618 ,  C07C69/606 ,  C07C229/22 ,  C07C227/18 ,  C07D209/20 ,  C07C233/05 ,  C07C231/12 ,  C07D233/64 ,  C07D207/16 ,  C07C279/24 ,  C07C277/08 ,  C07C231/14 ,  C07C233/11 ,  C07C233/09 ,  C07D295/185 ,  C07K5/062 ,  C07K5/065 ,  C07K7/06 ,  C07K1/22

CPC分类号： C07K1/064 ,  C07C69/145 ,  C07C67/08 ,  C07C69/753 ,  C07C69/78 ,  C07D307/68 ,  C07D231/56 ,  C07D333/70 ,  C07C69/618 ,  C07C69/606 ,  C07C229/22 ,  C07C227/18 ,  C07D209/20 ,  C07C233/05 ,  C07C231/12 ,  C07D233/64 ,  C07D207/16 ,  C07C279/24 ,  C07C277/08 ,  C07C231/14 ,  C07C233/11 ,  C07C233/09 ,  C07D295/185 ,  C07K5/0606 ,  C07K5/06043 ,  C07K5/06052 ,  C07K5/06078 ,  C07K5/06069 ,  C07K7/06 ,  C07K1/22

摘要： There is provided an α-carbonyl alkenyl ester and a preparation method therefor, and the α-carbonyl alkenyl ester is further used to react with a primary or secondary amine to prepare an amide. The two reactions are combined to develop an amide bond and peptide bond formation method that directly use carboxylic acids and amines as starting materials and allenones as a condensing reagent. The α-carbonyl alkenyl ester corresponding to an α-amino acid serves as a peptide synthesis building block and is used in solid phase peptide synthesis. The method is carried out under mild reaction conditions, simple to operate, and has a high yield. Compared with existing amide bond condensation reagents, the allenones have the advantages of being simple to prepare, having good stability, a low molecular weight, not racemizing when activating α-chiral carboxylic acids, and is a novel amide bond and peptide bond condensing reagent.

公开(公告)号：US20190233377A1

公开(公告)日：2019-08-01

申请号：US16379487

申请日：2019-04-09

申请人： ZENO ROYALTIES & MILESTONES, LLC

发明人： Kevin Duane Bunker ,  Chuangxing Guo ,  Mark Charles Grier ,  Chad Daniel Hopkins ,  Joseph Robert Pinchman ,  Deborah Helen Slee ,  Peter Qinhua Huang ,  Mehmet Kahraman

IPC分类号： C07D213/89 ,  A61K45/06 ,  C07C317/30 ,  A61K31/13 ,  C07C233/14 ,  C07C233/05 ,  A61K31/444 ,  A61K31/27 ,  A61K31/164 ,  A61K31/16 ,  A61K31/145 ,  C07C211/38 ,  C07C215/42 ,  C07C233/06 ,  C07C233/23 ,  C07C233/13 ,  C07C233/09

CPC分类号： C07D213/89 ,  A61K31/13 ,  A61K31/145 ,  A61K31/16 ,  A61K31/164 ,  A61K31/27 ,  A61K31/444 ,  A61K45/06 ,  C07C211/38 ,  C07C215/42 ,  C07C233/05 ,  C07C233/06 ,  C07C233/09 ,  C07C233/13 ,  C07C233/14 ,  C07C233/23 ,  C07C317/30 ,  C07C2601/02 ,  C07C2602/38 ,  C07C2603/62 ,  A61K2300/00

摘要： Disclosed herein are compounds of Formulae (I) and (II), methods of synthesizing compounds of Formulae (I) and (II), and methods of using compounds of Formulae (I) and (II) as an analgesic.

公开(公告)号：US20190210957A1

公开(公告)日：2019-07-11

申请号：US16311747

申请日：2017-01-20

申请人： Jiangxi Normal University

发明人： Junfeng ZHAO ,  Long HU ,  Silin XU ,  Zhenguang ZHAO

IPC分类号： C07C219/20 ,  C07C213/08 ,  C07C311/17 ,  C07C303/40 ,  C07C231/02 ,  C07C233/05

CPC分类号： C07C219/20 ,  C07C213/08 ,  C07C231/02 ,  C07C233/05 ,  C07C303/40 ,  C07C311/17 ,  C07D209/20 ,  C07D231/56 ,  C07D263/22 ,  C07D307/68 ,  C07D333/68 ,  C07K5/06

摘要： Disclosed are a mild and efficient preparation method for an α-acyloxyenamide compound and a use thereof in the synthesis of an amide and a polypeptide. The α-acyloxyenamide compound is obtained by an addition reaction of a ynamide and a carboxylic acid in dichloromethane under conditions where the temperature is 0° C. to 50° C.; the produced α-acyloxyenamide compound can react with an amine compound to produce an amide or a polypeptide; the two reactions can be carried out step by step, and can also be carried out in one pot. According to the invention, the reaction conditions are mild and no metal catalyst is required; when the carboxylic acid, which has chirality on an alpha site of carboxyl, forms an amide bond or a peptide bond, no racemization occurs; and the operation is simple and the application range is wide.

公开(公告)号：US09975994B2

公开(公告)日：2018-05-22

申请号：US15545546

申请日：2016-01-22

申请人： BASF SE

发明人： Simon Gramlich ,  Achim Stammer ,  Angela Ulzhöfer ,  Frank Niedermaier

IPC分类号： C08G63/02 ,  C08G65/46 ,  C07D207/267 ,  C07C233/05

CPC分类号： C08G65/46 ,  C07C233/05 ,  C07D207/267

摘要： A method for desalinating a salt-containing polymer (SP) comprising a polyaryl ether having a softening temperature TS and a salt (S), comprising the steps of a) providing the salt-containing polymer (SP) at a first temperature T1 above the softening temperature TS of the polyaryl ether, b) contacting the salt-containing polymer (SP) provided in step a) with an extractant (E) to obtain a desalinated polymer (DP) comprising the polyaryl ether, and a salt-containing extractant (SE) comprising the extractant (E) and the salt (S).

公开(公告)号：US20180104701A1

公开(公告)日：2018-04-19

申请号：US15562830

申请日：2016-03-01

申请人： Clariant International Ltd.

发明人： Klaus-Ulrich PEDAIN ,  Jesús PITARCH LÓPEZ ,  Gunter LIPOWSKY ,  Jacques Collin BEZUIDENHOUT

IPC分类号： B03D1/008 ,  B03D1/01 ,  B03D1/02 ,  C07C53/126 ,  C07C233/05

CPC分类号： B03D1/008 ,  B03D1/01 ,  B03D1/021 ,  B03D2201/005 ,  B03D2201/02 ,  B03D2203/04 ,  B03D2203/06 ,  C07C53/126 ,  C07C233/05

摘要： This invention relates to a collector composition for the direct froth flotation of nonsulfide ores comprising a) 50-99 wt.-% of a mixture of fatty acids and b) 1-50 wt.-% of an N-acyl derivative of sarcosine of the formula (I) wherein R is a saturated or unsaturated hydrocarbon chain with 7 to 21 carbon atoms, wherein the mixture of comprises 10.0-35.0 wt.-% of fatty acid having a saturated C11 hydrocarbon group, 2.5-15.0 wt.-% of fatty acid having a saturated C13 hydrocarbon group, 10.0-25.0 wt.-% fatty acid having a monounsaturated C17 hydrocarbon group and 20.0-45.0 wt.-% fatty acid having a bisunsaturated C17 hydrocarbon group.

公开(公告)号：US20180009944A1

公开(公告)日：2018-01-11

申请号：US15545546

申请日：2016-01-22

申请人： BASF SE

发明人： SIMON GRAMLICH ,  Achim STAMMER ,  Angela ULZHÕFER

IPC分类号： C08G65/46 ,  C07D207/267 ,  C07C233/05

CPC分类号： C08G65/46 ,  C07C233/05 ,  C07D207/267

摘要： A method for desalinating a salt-containing polymer (SP) comprising a polyaryl ether having a softening temperature TS and a salt (S), comprising the steps of a) providing the salt-containing polymer (SP) at a first temperature T1 above the softening temperature TS of the polyaryl ether, b) contacting the salt-containing polymer (SP) provided in step a) with an extractant (E) to obtain a desalinated polymer (DP) comprising the polyaryl ether, and a salt-containing extractant (SE) comprising the extractant (E) and the salt (S).

公开(公告)号：US20170369422A1

公开(公告)日：2017-12-28

申请号：US15544095

申请日：2016-03-25

申请人： ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD

发明人： Musong Liu ,  Wenling Zhang ,  Peng Wang

IPC分类号： C07C231/02

CPC分类号： C07C231/02 ,  C07C231/24 ,  C07C233/05

摘要： The present invention provides a method for preparing a pregabalin intermediate 3-carbamoymethyl-5-methylhexanoic acid without solvent. The method comprises the following steps: a) cooling an ammonia water system to a certain temperature; b) adding 3-isobutylglutaric anhydride dropwise to the system, then keeping temperature, and reacting; c) after completing the reaction, adding an acid to the system to adjust pH; d) after adjusting pH, cooling, then keeping temperature, crystallizing, then suction filtering and drying; and e) adding a solvent to the dried substance, slurrying, and suction filtering and drying to obtain the final product. The method provided in the present invention for preparing 3-carbamoymethyl-5-methylhexanoic acid is high-yield, green, environmentally-friendly, simple and convenient, and of less pollution.

公开(公告)号：US09717242B2

公开(公告)日：2017-08-01

申请号：US15080971

申请日：2016-03-25

申请人： MEIJI SEIKA PHARMA CO., LTD.

发明人： Shinzo Kagabu ,  Masaaki Mitomi ,  Shigeki Kitsuda ,  Ryo Horikoshi ,  Masahiro Nomura ,  Yasumichi Onozaki

IPC分类号： C07D401/06 ,  A61K31/444 ,  A01N43/40 ,  C07D211/98 ,  A01N43/50 ,  A01N43/78 ,  A01N47/40 ,  C07C233/05 ,  C07C233/12 ,  C07C261/04 ,  C07C271/12 ,  C07C311/09 ,  C07F9/58 ,  A01N37/18 ,  A01N43/54 ,  A01N43/58 ,  A01N47/02 ,  A01N47/12 ,  A01N57/32 ,  C07D213/36 ,  C07D213/40 ,  C07D213/42 ,  C07D213/61 ,  C07D213/75 ,  C07D237/08 ,  C07D277/32 ,  C07D333/20 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

CPC分类号： A01N43/40 ,  A01N37/18 ,  A01N43/50 ,  A01N43/54 ,  A01N43/58 ,  A01N43/78 ,  A01N47/02 ,  A01N47/12 ,  A01N47/40 ,  A01N57/32 ,  C07C233/05 ,  C07C233/12 ,  C07C261/04 ,  C07C271/12 ,  C07C311/09 ,  C07D211/98 ,  C07D213/36 ,  C07D213/40 ,  C07D213/42 ,  C07D213/61 ,  C07D213/75 ,  C07D237/08 ,  C07D277/32 ,  C07D333/20 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  C07F9/58

摘要： A compound of formula (Ie′): wherein Ar′, R1, R4e and Y are as defined herein and a method of controlling pests using the compound.