公开(公告)号：US20200299227A1

公开(公告)日：2020-09-24

申请号：US16088196

申请日：2017-03-28

申请人： PIRAMAL ENTERPRISES LIMITED

发明人： Milind GHARPURE ,  Ashutosh JAGTAP ,  Changdev RAUT ,  Nainesh KANSAGARA ,  Jaisankar KRISHNAPILLAI ,  Nirmal Kumar MANOHARAN ,  Navnath PATIL

IPC分类号： C07C229/36 ,  A61K9/16 ,  C07F15/04

摘要： The present invention provides an improved process for preparation of L-threo-(2S,3R)-3-(3,4-dihydroxyphenyl)serine (I) (Droxidopa) and its salts; comprising (a) reaction of the aldehyde compound (III) (as described herein) with Metal complex (II) (as described herein), and (h) hydrolysis of the compound (IV) obtained from step (a) in presence of acid. The present invention also relates to a novel intermediates metal chiral complex (IV) for the preparation of Droxidopa.

公开(公告)号：US10781192B2

公开(公告)日：2020-09-22

申请号：US16312688

申请日：2017-06-29

申请人： KEZAR LIFE SCIENCES

发明人： Henry Johnson ,  Sean Dalziel ,  Dustin McMinn

IPC分类号： C07D295/15 ,  C07D295/13 ,  C07D303/46 ,  C07D303/12 ,  C07C229/36 ,  C07D301/02 ,  C07D303/32

摘要： Disclosed herein are methods for preparing [(2S,3R)—N-[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide (compound “G”): and precursors thereof.

公开(公告)号：US20200206350A1

公开(公告)日：2020-07-02

申请号：US16644107

申请日：2018-08-31

申请人： Merck Sharp & Dohme Corp.

发明人： Lin Chu ,  Nathalie Y. Toussaint ,  Dong Xiao ,  Petr Vachal ,  Ramesh S. Kashi ,  Annette Bak

IPC分类号： A61K47/22 ,  C07K16/28 ,  A61K47/26 ,  C07D233/64 ,  C07C279/14 ,  C07C235/12 ,  C07C229/36 ,  A61K47/18

摘要： The present invention relates to pegylated amino acid compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3A, R3B and n are as defined herein. The present invention also relates to compositions which comprise a pegylated amino acid compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, in combination with a high concentration of an active biological ingredient (ABI). In embodiments of the invention, the ABI is an anti-PD-1 antibody or antigen binding fragment thereof that specifically binds human programmed death receptor 1 (PD-1). The invention further relates to methods for lowering the viscosity of an aqueous solution of a pharmaceutical composition comprising adding a compound of the invention to the solution. The invention also provides methods for treating a pathological disease or condition, such as cancer, by administering to a subject in need of such treatment a therapeutically effective amount of a pharmaceutical composition of the invention.

公开(公告)号：US10689624B2

公开(公告)日：2020-06-23

申请号：US15543488

申请日：2016-01-14

申请人： KYOTO UNIVERSITY

发明人： Hirohide Saito ,  Yi Kuang

IPC分类号： C12N5/00 ,  C12N5/16 ,  C12N5/10 ,  C07C229/36 ,  C07K14/00 ,  C08G69/10 ,  G01N33/50

摘要： [Problem to be Solved]To provide a compound for removing pluripotent cells from a cell population potentially containing the pluripotent cells.[Solution]A polyphenylalanine derivative is contacted with a cell population of interest.

公开(公告)号：US20200165192A1

公开(公告)日：2020-05-28

申请号：US16775564

申请日：2020-01-29

申请人： BEZWADA BIOMEDICAL, LLC

发明人： Rao S. Bezwada

IPC分类号： C07C235/12 ,  C07C235/10 ,  C08G18/66 ,  C08G18/48 ,  A61L26/00 ,  A61L24/04 ,  A61L17/10 ,  A61L15/26 ,  A61L31/10 ,  A61L31/06 ,  A61L27/18 ,  C08G18/38 ,  C08G18/78 ,  C08G18/77 ,  C07C229/36 ,  C07C229/42 ,  C07C265/14 ,  C07C237/36 ,  C07C265/12 ,  A61K47/34

摘要： The present invention relates to the discovery of new class of hydrolysable amino acid derivatives and absorbable polyester amides, polyamides, polyepoxides, polyureas and polyurethanes prepared therefrom. The resultant absorbable polymers are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention, bone wax formulations, medical device coatings, stents, stent coatings, highly porous foams, reticulated foams, wound care, cardiovascular applications, orthopedic devices, surface modifying agents and other implantable medical devices. In addition, these absorbable polymers should have a controlled degradation profile.

公开(公告)号：US20200031761A1

公开(公告)日：2020-01-30

申请号：US16365532

申请日：2019-03-26

申请人： ID4PHARMA, LLC

发明人： Xiang-Qun Xie ,  Garson David Roodman ,  Kyaw-Zeyar Myint ,  Noriyoshi Kurihara

IPC分类号： C07C229/36 ,  C07D309/40 ,  C07C211/50 ,  C07C317/34 ,  C07C217/58 ,  C07C217/76 ,  C07C219/06 ,  C07D241/44 ,  C07C229/14 ,  C07D487/04 ,  C07C235/48 ,  C07C251/76 ,  A61K31/137 ,  A61K31/351 ,  A61K31/495 ,  A61K31/519 ,  A61K31/15 ,  A61K31/498 ,  A61K45/06 ,  C07C249/16 ,  C07D309/32 ,  C07D475/08 ,  C12N5/09 ,  A61K31/216

摘要： A method for treating a p62-mediated disease (e.g., multiple myeloma) in a subject, the method comprising administering to the subject a therapeutically effective amount of at least one p62-ZZ inhibitor compound.

公开(公告)号：US20190359554A1

公开(公告)日：2019-11-28

申请号：US16472386

申请日：2017-12-20

申请人： Novartis AG

发明人： Florian Karl KLEINBECK-RINIKER ,  Tobias KAPFERER ,  Hongyong KIM ,  Jie KU ,  Kurt LAUMEN ,  Yunzhong LI ,  Wei PENG ,  Thomas RUCH ,  Thierry SCHLAMA ,  Yao YANG

IPC分类号： C07C227/06 ,  C07C229/36 ,  C12P41/00

摘要： The invention relates to a new enantioselective process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone.

公开(公告)号：US20190241498A1

公开(公告)日：2019-08-08

申请号：US16125574

申请日：2018-09-07

申请人： Cole Research & Design, LLC

发明人： Mahmoud A. ElSohly ,  Waseem Gul ,  Jeptha N. Cole

IPC分类号： C07C69/42 ,  A61P17/02 ,  C07C229/36 ,  C07C67/08 ,  C07C69/40 ,  C07C229/08

CPC分类号： C07C69/42 ,  A61P17/02 ,  C07C67/08 ,  C07C69/40 ,  C07C229/08 ,  C07C229/36

摘要： A resveratrol ester has the following structure: R1, R2 and R3 are H or Each R4 is independently a carbon chain of 2 to 4 carbon atoms comprising a terminal carboxylic acid moiety, a carbon chain of 1 to 5 carbon atoms comprising an amine moiety, or R5 is a carbon chain of 3 or 4 carbon atoms having a terminal carboxylic acid moiety. At least one of R1, R2 and R3 is Salts of resveratrol esters are also included.

公开(公告)号：US10344045B2

公开(公告)日：2019-07-09

申请号：US15570771

申请日：2016-05-19

申请人： OUT AND OUT CHEMISTRY S.P.R.L.

发明人： Vincent Luc Antoine Tadino ,  Guillaume André René Villeret

IPC分类号： C07H5/02 ,  C07H1/06 ,  C07B59/00 ,  C07D207/46 ,  B01J19/24 ,  B01J41/00 ,  C01D3/02 ,  C07C39/40 ,  C07C53/18 ,  C07C215/40 ,  C07C229/36 ,  C07D233/91 ,  C07H19/06

摘要： A method of performing a plurality of synthesis processes of preparing a radiopharmaceutical in series includes carrying out a first synthesis run including the steps of: a) providing water containing fluorine-18; b) trapping the fluorine-18 from the water provided in step a) on an anion exchange material; c) eluting the trapped fluorine-18 from the anion exchange material to a reaction vessel of first radiopharmaceutical synthesis cassette; d) preparing a radiopharmaceutical incorporating the eluted fluorine-18 using the first radiopharmaceutical synthesis cassette; where steps a)-d) are repeated in at least one subsequent run using another radiopharmaceutical synthesis cassette; and where the method includes a reconditioning step of the anion exchange material between two consecutive runs. A device for performing this method and a cassette for use in the device are also disclosed.

公开(公告)号：US20190127315A1

公开(公告)日：2019-05-02

申请号：US16094279

申请日：2017-04-05

申请人： AMINOLOGICS CO., LTD.

发明人： IL-Suk BYUN ,  Chul-Hwan YOO ,  Won-Sup KIM

IPC分类号： C07C227/32 ,  C07C229/36 ,  C07C69/86

摘要： A method of preparing D-4,4′-biphenylalanine alkyl ester or L-4,4′-biphenylalanine alkyl ester by subjecting DL-4,4′-biphenylalanine alkyl ester to optical resolution using chiral diaroyl tartaric acid as an optical resolving agent is provided.