公开(公告)号：US10053417B2

公开(公告)日：2018-08-21

申请号：US15806722

申请日：2017-11-08

申请人： THERAVANCE BIOPHARMA R&D IP, LLC

发明人： Erik Fenster ,  Melissa Fleury ,  Adam D. Hughes

IPC分类号： A61K31/40 ,  A61K31/42 ,  A61K31/44 ,  A61K31/197 ,  A61K31/397 ,  A61K31/5375 ,  C07D205/04 ,  C07D207/09 ,  C07D207/14 ,  C07D213/56 ,  C07C235/34 ,  C07D261/04 ,  C07D295/32 ,  C07C243/38 ,  A61K31/341 ,  A61K31/4409 ,  C07D213/86 ,  C07D213/87 ,  C07C235/80 ,  A61K31/4406 ,  A61K31/192 ,  C07D213/65 ,  A61K45/06 ,  A61K31/495 ,  A61K31/4015 ,  C07D307/68 ,  C07D213/61 ,  C07D211/62 ,  C07D211/60 ,  C07D211/48 ,  C07D211/46 ,  C07D211/42 ,  C07D211/38 ,  C07D211/22 ,  C07C243/32 ,  C07C243/24 ,  C07D493/10 ,  C07D207/16 ,  C07D207/12 ,  C07D207/08 ,  C07D265/30 ,  C07C235/78 ,  C07C235/74 ,  C07C235/20 ,  C07C235/12 ,  C07C233/56 ,  C07D261/02 ,  C07D239/36 ,  C07D405/06 ,  C07D401/04 ,  C07D233/06 ,  C07D309/08 ,  C07C259/04 ,  C07D213/75 ,  C07D491/107

CPC分类号： C07C243/38 ,  A61K31/192 ,  A61K31/197 ,  A61K31/341 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/495 ,  A61K31/5375 ,  A61K45/06 ,  C07C233/56 ,  C07C235/12 ,  C07C235/20 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C235/80 ,  C07C243/24 ,  C07C243/32 ,  C07C259/04 ,  C07C2601/08 ,  C07C2601/16 ,  C07D205/04 ,  C07D207/08 ,  C07D207/09 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D211/22 ,  C07D211/38 ,  C07D211/42 ,  C07D211/46 ,  C07D211/48 ,  C07D211/60 ,  C07D211/62 ,  C07D213/56 ,  C07D213/61 ,  C07D213/65 ,  C07D213/75 ,  C07D213/86 ,  C07D213/87 ,  C07D233/06 ,  C07D239/36 ,  C07D261/02 ,  C07D261/04 ,  C07D265/30 ,  C07D295/32 ,  C07D307/68 ,  C07D309/08 ,  C07D401/04 ,  C07D405/06 ,  C07D491/107 ,  C07D493/10

摘要： In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

公开(公告)号：US10034870B2

公开(公告)日：2018-07-31

申请号：US15591419

申请日：2017-05-10

申请人： THERAVANCE BIOPHARMA R&D IP, LLC

发明人： Lori Jean Patterson ,  Eric L. Stangeland

IPC分类号： A61K31/4465 ,  C07D211/32 ,  C07D211/22

CPC分类号： A61K31/4465 ,  C07D211/22 ,  C07D211/32

摘要： The invention relates to compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

公开(公告)号：US20180201577A1

公开(公告)日：2018-07-19

申请号：US15688185

申请日：2017-08-28

申请人： Global Blood Therapeutics, Inc.

发明人： Qing Xu ,  Zhe Li

IPC分类号： C07D207/08 ,  C07D403/06 ,  C07C271/16 ,  C07D401/06 ,  C07D335/02 ,  C07D333/38 ,  C07D309/28 ,  C07D309/08 ,  C07D279/12 ,  C07D265/30 ,  C07D241/04 ,  C07D213/81 ,  C07D211/78 ,  C07D211/60 ,  C07D211/22 ,  C07D211/16 ,  C07D207/48 ,  C07D207/34 ,  C07D401/12

CPC分类号： C07D207/08 ,  C07C271/16 ,  C07D207/34 ,  C07D207/48 ,  C07D211/16 ,  C07D211/22 ,  C07D211/60 ,  C07D211/78 ,  C07D213/81 ,  C07D241/04 ,  C07D265/30 ,  C07D279/12 ,  C07D309/08 ,  C07D309/28 ,  C07D333/38 ,  C07D335/02 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06

摘要： Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.

公开(公告)号：US10018875B2

公开(公告)日：2018-07-10

申请号：US15002012

申请日：2016-01-20

申请人： Samsung Display Co. Ltd.

发明人： Ji Hong Bae ,  Heung Shik Park ,  Keun Chan Oh

IPC分类号： G02F1/1337 ,  G02F1/1341 ,  C07D211/46 ,  C07D211/22 ,  C09K19/54 ,  C09K19/34 ,  C09K19/56 ,  C08G73/10

CPC分类号： G02F1/133711 ,  C07D211/22 ,  C07D211/46 ,  C08G73/1042 ,  C08G73/1078 ,  C09K19/3483 ,  C09K19/54 ,  C09K19/542 ,  C09K19/56 ,  C09K2019/548 ,  G02F1/133707 ,  G02F1/133788 ,  G02F1/1341 ,  G02F2001/133726 ,  G02F2001/133742

摘要： A curved liquid crystal display comprises, a first curved substrate; a second curved substrate facing the first curved substrate; a liquid crystal layer disposed between the first curved substrate and the second curved substrate; a first curved liquid crystal alignment layer disposed between the liquid crystal layer and the first curved substrate and containing a light stabilizer; and a second curved liquid crystal alignment layer disposed between the liquid crystal layer and the second curved substrate.

公开(公告)号：US20170327459A1

公开(公告)日：2017-11-16

申请号：US15600998

申请日：2017-05-22

申请人： THERAVANCE BIOPHARMA R&D IP, LLC

发明人： Erik Fenster ,  Melissa Fleury ,  Adam D. Hughes

IPC分类号： C07C243/38 ,  C07D491/107 ,  A61K31/192 ,  C07D405/06 ,  C07D401/04 ,  C07D309/08 ,  C07D307/68 ,  C07D295/32 ,  C07D265/30 ,  C07D261/04 ,  C07D261/02 ,  C07D239/36 ,  C07D233/06 ,  C07D213/87 ,  C07D213/86 ,  C07D213/75 ,  C07D213/65 ,  C07D213/61 ,  C07D213/56 ,  C07D211/62 ,  C07D211/60 ,  C07D211/48 ,  C07D211/46 ,  C07D211/42 ,  C07D211/38 ,  C07D211/22 ,  C07D207/16 ,  C07D207/14 ,  C07D207/12 ,  C07D207/09 ,  C07D207/08 ,  C07D205/04 ,  C07C259/04 ,  C07C243/32 ,  C07C243/24 ,  C07C235/80 ,  C07C235/78 ,  C07C235/74 ,  C07C235/34 ,  C07C235/20 ,  C07C235/12 ,  C07C233/56 ,  A61K45/06 ,  A61K31/5375 ,  A61K31/495 ,  A61K31/4409 ,  A61K31/4406 ,  A61K31/44 ,  A61K31/42 ,  A61K31/4015 ,  A61K31/40 ,  A61K31/397 ,  A61K31/341 ,  A61K31/197 ,  C07D493/10 ,  C07C2601/16 ,  C07C2601/08

CPC分类号： C07C243/38 ,  A61K31/192 ,  A61K31/197 ,  A61K31/341 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/495 ,  A61K31/5375 ,  A61K45/06 ,  C07C233/56 ,  C07C235/12 ,  C07C235/20 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C235/80 ,  C07C243/24 ,  C07C243/32 ,  C07C259/04 ,  C07C2601/08 ,  C07C2601/16 ,  C07D205/04 ,  C07D207/08 ,  C07D207/09 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D211/22 ,  C07D211/38 ,  C07D211/42 ,  C07D211/46 ,  C07D211/48 ,  C07D211/60 ,  C07D211/62 ,  C07D213/56 ,  C07D213/61 ,  C07D213/65 ,  C07D213/75 ,  C07D213/86 ,  C07D213/87 ,  C07D233/06 ,  C07D239/36 ,  C07D261/02 ,  C07D261/04 ,  C07D265/30 ,  C07D295/32 ,  C07D307/68 ,  C07D309/08 ,  C07D401/04 ,  C07D405/06 ,  C07D491/107 ,  C07D493/10

摘要： In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

公开(公告)号：US09803199B2

公开(公告)日：2017-10-31

申请号：US14903711

申请日：2014-07-07

申请人： DAIICHI SANKYO COMPANY, LIMITED

发明人： Makoto Koizumi ,  Yoshiyuki Onishi ,  Takako Niwa ,  Masakazu Tamura ,  Yuji Kasuya

IPC分类号： C12N15/113 ,  A61K31/7088 ,  A61K31/713 ,  C07C219/16 ,  C07D211/22 ,  C07D211/46 ,  A61K47/48 ,  A61K9/127 ,  C12N15/11 ,  A61K9/10 ,  A61K47/18 ,  A61K47/22 ,  A61K47/28 ,  A61K47/44 ,  A61K48/00

CPC分类号： C12N15/113 ,  A61K9/10 ,  A61K9/127 ,  A61K9/1271 ,  A61K9/1272 ,  A61K31/7088 ,  A61K31/713 ,  A61K47/18 ,  A61K47/22 ,  A61K47/28 ,  A61K47/44 ,  A61K47/543 ,  A61K48/0008 ,  A61K48/005 ,  C07C219/16 ,  C07D211/22 ,  C07D211/46 ,  C12N15/111 ,  C12N2310/14 ,  C12N2320/32

摘要： The present invention provides a compound represented by the formula (Ia) as a novel cationic lipid that forms a lipid particle and also provides a lipid particle comprising the compound. The present invention further provides a nucleic acid lipid particle containing the lipid particle, and a pharmaceutical composition containing the nucleic acid lipid particle as an active ingredient.

公开(公告)号：US20170226072A1

公开(公告)日：2017-08-10

申请号：US15494789

申请日：2017-04-24

申请人： University of Kentucky Research Foundation

发明人： Peter A. CROOKS ,  Linda P. DWOSKIN ,  John CULVER ,  Justin R. NICKELL ,  Guangrong ZHENG

IPC分类号： C07D295/096 ,  C07D295/073 ,  C07D211/22 ,  C07D211/18 ,  C07D211/14 ,  C07D295/03

CPC分类号： C07D295/096 ,  C07D211/08 ,  C07D211/14 ,  C07D211/18 ,  C07D211/22 ,  C07D295/02 ,  C07D295/03 ,  C07D295/073

摘要： The present invention is directed to 1,4-disubstituted piperidines, 1,4-disubstituted piperazines, 1,4-disubstituted diazepanes, and 1,3-disubstituted pyrrolidine compounds and their use.

公开(公告)号：US20170197977A9

公开(公告)日：2017-07-13

申请号：US14241019

申请日：2012-08-27

申请人： COGNITION THERAPEUTICS, INC.

发明人： Susan M. Catalano ,  Gilbert Rishton ,  Nicholas J. Izzo

IPC分类号： C07D491/107 ,  C07D295/096 ,  C07D211/22 ,  C07C217/62 ,  C07D209/44

CPC分类号： C07D491/107 ,  C07B2200/07 ,  C07C211/28 ,  C07C211/29 ,  C07C215/54 ,  C07C217/58 ,  C07C217/62 ,  C07C235/60 ,  C07C317/32 ,  C07C2601/10 ,  C07C2602/10 ,  C07D209/44 ,  C07D211/14 ,  C07D211/22 ,  C07D295/08 ,  C07D295/096 ,  C07D319/18 ,  C07D491/10

摘要： This invention relates to novel diarylamino compounds that bind to the sigma-2 receptor, to pharmaceutical compositions comprising such compounds, and to methods for inhibiting or restoring synapse loss in neuronal cells, modulating a membrane trafficking change in neuronal cells, and treating cognitive decline and neurodegenerative diseases and disorders therewith.

公开(公告)号：US09643940B2

公开(公告)日：2017-05-09

申请号：US14424215

申请日：2013-08-30

申请人： ONO PHARMACEUTICAL CO., LTD.

发明人： Kousuke Tani ,  Akihiro Kinoshita ,  Keisuke Hanada ,  Yoshiyuki Aratani ,  Takahiro Nekado ,  Atsushi Shimabukuro

IPC分类号： C07D277/56 ,  A61K47/40 ,  C07D277/20 ,  C07D211/22 ,  A61K31/426 ,  C08B37/16 ,  C08L5/16

CPC分类号： C07D277/56 ,  A61K31/426 ,  A61K47/40 ,  C07B2200/13 ,  C07D211/22 ,  C07D277/20 ,  C08B37/0015 ,  C08L5/16

摘要： A compound that can be a therapeutic agent for underactive bladder which has low risk of side effects and can be administered orally is provided. Furthermore, a crystal which is advantageous in view of the stability, long-term storage, handleability, easiness of the drug preparation or the like as a drug substance of medicaments is provided. Since a salt of 2-[(2-{(1R,5R)-2-oxo-5-[(1E,4S)-7,8,8-trifluoro-4-hydroxy-4-methyl-1,7-octadien-1-yl]cyclopentyl}ethyl)thio]-1,3-thiazole-4-carboxylic acid or a diastereomeric mixture thereof and 4-piperidinemethanol is a chemically very stable crystal, it can be stored for a long time, and is very useful as a drug substance of medicaments.

公开(公告)号：US20170107208A1

公开(公告)日：2017-04-20

申请号：US15128829

申请日：2015-03-24

申请人： THE UNIVERSITY OF LIVERPOOL

发明人： Jianliang XIAO ,  Jianjun WU

IPC分类号： C07D409/04 ,  C07D211/22 ,  C07D211/18 ,  C07D401/04 ,  C07D211/32 ,  C07D211/26 ,  C07D405/04 ,  C07D211/34 ,  C07D211/14 ,  C07D211/28

CPC分类号： C07D409/04 ,  C07B2200/13 ,  C07D211/02 ,  C07D211/14 ,  C07D211/18 ,  C07D211/22 ,  C07D211/26 ,  C07D211/28 ,  C07D211/32 ,  C07D211/34 ,  C07D401/04 ,  C07D405/04

摘要： The present invention relates to a process for preparing substituted piperidine compounds and especially chiral substituted piperidine compounds. The process involves reacting a substituted pyridinium ion with an amine as defined herein, in the presence of a hydrogen donor, a catalysts and a suitable solvent.