公开(公告)号：US11919895B2

公开(公告)日：2024-03-05

申请号：US17080247

申请日：2020-10-26

申请人： Saint Louis University

发明人： Daniela Salvemini ,  Christopher K. Arnatt

IPC分类号： C07D471/04 ,  A61P23/00 ,  A61P25/02 ,  C07D217/06 ,  C07D295/135

CPC分类号： C07D471/04 ,  A61P23/00 ,  A61P25/02 ,  C07D217/06 ,  C07D295/135

摘要： Disclosed herein are compositions and methods for treating neuropathic pain in a subject in need thereof. Compositions disclosed herein are GPR183 antagonists. The methods include administering to a subject in need thereof a therapeutically effective amount of a GPR183 antagonist.

公开(公告)号：US20230278971A1

公开(公告)日：2023-09-07

申请号：US18316254

申请日：2023-05-12

申请人： Versitech Limited

发明人： Yi Tsun Richard KAO ,  Peng GAO ,  Xuechen LI ,  Ming LIU

IPC分类号： C07D295/08 ,  A61K9/00 ,  C07D215/58 ,  C07D217/06 ,  A61P31/04

CPC分类号： C07D295/08 ,  A61K9/0095 ,  C07D215/58 ,  C07D217/06 ,  A61P31/04

摘要： Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives, and methods for prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (II):




The present methods include administering to a subject an effective amount of one or more compounds of Formula (II). In one embodiment, said microbial infections are bacterial infections. More specifically, said bacterial infections are staphylococcal infections.

公开(公告)号：US20230233551A1

公开(公告)日：2023-07-27

申请号：US17815256

申请日：2022-07-27

申请人： Novartis Pharmaceuticals Corporation

发明人： Thomas GADEK ,  John BURNIER

IPC分类号： A61K31/4725 ,  C07D217/00 ,  C07D217/02 ,  A61K31/198 ,  A61K31/404 ,  A61K31/4162 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/54 ,  A61K31/541 ,  A61P27/02 ,  A61K31/381 ,  A61K45/06 ,  C07D333/38 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  A61K33/00 ,  A61K33/06 ,  C07D217/20 ,  C07D217/06 ,  A61K31/405 ,  A61K31/495 ,  A61K38/07 ,  A61K38/08 ,  A61K38/12 ,  A61K38/17 ,  G01N33/50 ,  G01N33/68 ,  A61K31/197 ,  A61K31/341 ,  A61K31/352 ,  A61K31/472 ,  C07D401/06 ,  A61K31/275 ,  A61K31/40 ,  A61K31/517 ,  C07C279/28 ,  C07C317/50 ,  C07D207/06 ,  C07D217/26 ,  C07D307/52 ,  C07D413/14 ,  A61K9/00 ,  G01N33/566 ,  A61B3/10 ,  A61B3/14

CPC分类号： A61K31/4725 ,  C07D217/00 ,  C07D217/02 ,  A61K31/198 ,  A61K31/404 ,  A61K31/4162 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/54 ,  A61K31/541 ,  A61P27/02 ,  A61K31/381 ,  A61K45/06 ,  C07D333/38 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  A61K33/00 ,  A61K33/06 ,  C07D217/20 ,  C07D217/06 ,  A61K31/405 ,  A61K31/495 ,  A61K38/07 ,  A61K38/08 ,  A61K38/12 ,  A61K38/1703 ,  G01N33/5011 ,  G01N33/5032 ,  G01N33/6872 ,  A61K31/197 ,  A61K31/341 ,  A61K31/352 ,  A61K31/472 ,  C07D401/06 ,  G01N33/5047 ,  A61K31/275 ,  A61K31/40 ,  A61K31/517 ,  C07C279/28 ,  C07C317/50 ,  C07D207/06 ,  C07D217/26 ,  C07D307/52 ,  C07D413/14 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0048 ,  A61K9/0053 ,  G01N33/566 ,  A61B3/101 ,  A61K9/0051 ,  A61B3/145 ,  G01N2333/70525 ,  G01N2500/02 ,  G01N2500/10 ,  G01N2333/705 ,  G01N2333/70546 ,  G01N2500/20 ,  G01N2500/04 ,  G01N2800/16

摘要： The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.

公开(公告)号：US20190016715A1

公开(公告)日：2019-01-17

申请号：US15950683

申请日：2018-04-11

申请人： Sanford-Burnham Medical Research Institute

发明人： Nicholas David Peter COSFORD ,  Dhanya RAVEENDRA-PANICKAR ,  Douglas J. SHEFFLER

IPC分类号： C07D417/14 ,  C07D231/12 ,  C07D403/12 ,  C07D263/32 ,  C07D277/26 ,  C07D307/38 ,  C07D333/24 ,  C07D401/14 ,  C07D405/10 ,  C07D409/02 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/10 ,  A61K31/505 ,  A61K31/506 ,  C07D233/64 ,  C07D285/08 ,  C07D277/20 ,  C07D249/08 ,  C07D417/04 ,  C07D217/06 ,  A61K31/433 ,  A61K31/427 ,  A61K31/426 ,  A61K31/4196 ,  C07D277/30 ,  C07D275/02 ,  C07D271/06 ,  C07D243/12 ,  C07D409/04 ,  C07D239/26 ,  C07D405/04 ,  C07D403/10 ,  C07D401/12 ,  C07D401/10 ,  C07D401/04 ,  C07D233/54 ,  C07D261/08

CPC分类号： C07D243/14 ,  A61K31/4196 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/505 ,  A61K31/506 ,  A61P25/00 ,  C07D217/06 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D239/26 ,  C07D243/12 ,  C07D249/08 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D275/02 ,  C07D277/20 ,  C07D277/26 ,  C07D277/30 ,  C07D285/08 ,  C07D307/38 ,  C07D333/24 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D405/10 ,  C07D409/02 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14

摘要： Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.

公开(公告)号：US10005792B2

公开(公告)日：2018-06-26

申请号：US15508074

申请日：2015-09-03

申请人： CTXT PTY LTD

发明人： Ylva Elisabet Bergman ,  Romina Lessene ,  Danny Ganame ,  Richard Charles Foitzik ,  Benjamin Joseph Morrow ,  Michelle Ang Camerino ,  Scott Raymond Walker ,  H. Rachel Lagiakos ,  John Feutrill ,  Paul Anthony Stupple

IPC分类号： C07D207/12 ,  C07D209/44 ,  C07D211/22 ,  C07D211/46 ,  C07D211/58 ,  C07D211/76 ,  C07D213/81 ,  C07D213/82 ,  C07D217/06 ,  C07D217/12 ,  C07D231/14 ,  C07D231/20 ,  C07D231/56 ,  C07D235/08 ,  C07D271/08 ,  C07D271/10 ,  C07D261/18 ,  C07D277/56 ,  C07D277/68 ,  C07D265/30 ,  C07D265/34 ,  C07D401/04 ,  C07D401/12 ,  C07D413/04 ,  C07D451/02 ,  C07D451/14 ,  C07D491/08 ,  C07D491/107 ,  C07C233/78 ,  C07C235/42 ,  C07C235/60 ,  C07D295/192

CPC分类号： C07D491/107 ,  C07C233/78 ,  C07C235/42 ,  C07C235/50 ,  C07C235/60 ,  C07C311/08 ,  C07C2602/06 ,  C07C2602/08 ,  C07C2602/10 ,  C07D205/04 ,  C07D207/12 ,  C07D209/44 ,  C07D211/22 ,  C07D211/46 ,  C07D211/58 ,  C07D211/76 ,  C07D213/81 ,  C07D213/82 ,  C07D217/06 ,  C07D231/12 ,  C07D231/14 ,  C07D231/20 ,  C07D231/56 ,  C07D235/08 ,  C07D261/18 ,  C07D265/30 ,  C07D265/34 ,  C07D271/08 ,  C07D271/10 ,  C07D277/56 ,  C07D277/68 ,  C07D295/185 ,  C07D295/192 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/04 ,  C07D451/02 ,  C07D451/14 ,  C07D491/08

摘要： A compound of formula (1a), (1b) or (1c) wherein: n is 1 or 2; RN is H or Me; R1 is optionally one or more halo or methyl groups; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d (if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R3a and R3b are independently selected from H and Me; R4a is selected from OH, —NH2, —C(═O)NH2, and —CH2OH; R4b is either H or Me; R5 is either H or Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl.

公开(公告)号：US20180003702A1

公开(公告)日：2018-01-04

申请号：US15244135

申请日：2016-08-23

申请人： SENOMYX, INC.

发明人： Xiaodong LI ,  Lena LUUKKONEN ,  Hong XU

IPC分类号： G01N33/543 ,  A23L27/00 ,  A23L27/20 ,  G01N33/566 ,  G01N33/50 ,  C07F9/655 ,  C07D405/12 ,  C07D317/68 ,  C07D307/84 ,  C07C275/34 ,  C07C275/30 ,  C07C235/54 ,  C07C233/65 ,  A61K47/24 ,  A61K47/22 ,  A61K8/55 ,  A61K8/49 ,  A23L2/56 ,  G01N33/74

CPC分类号： G01N33/543 ,  A23L2/56 ,  A23L27/202 ,  A23L27/203 ,  A23L27/2054 ,  A23L27/88 ,  A23V2002/00 ,  A61K8/4973 ,  A61K8/55 ,  A61K47/22 ,  A61K47/24 ,  C07C233/65 ,  C07C235/54 ,  C07C275/30 ,  C07C275/34 ,  C07D209/08 ,  C07D209/42 ,  C07D213/40 ,  C07D213/81 ,  C07D213/85 ,  C07D215/48 ,  C07D217/06 ,  C07D231/14 ,  C07D261/18 ,  C07D263/56 ,  C07D271/12 ,  C07D275/03 ,  C07D277/64 ,  C07D285/135 ,  C07D307/52 ,  C07D307/68 ,  C07D307/79 ,  C07D307/82 ,  C07D307/84 ,  C07D317/68 ,  C07D333/24 ,  C07D333/38 ,  C07D401/04 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07F9/65517 ,  G01N33/5041 ,  G01N33/566 ,  G01N33/74 ,  G01N2333/726

摘要： The invention relates to compounds that specifically bind a T1R1/T1R3 or T1R2/T1R3 receptor or fragments or sub-units thereof. The present invention also relates to the use of hetero-oligomeric and chimeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging.

公开(公告)号：US20170334847A1

公开(公告)日：2017-11-23

申请号：US15602693

申请日：2017-05-23

申请人： Incyte Corporation ,  Incyte Holdings Corporation

发明人： Wenqing Yao ,  Jincong Zhuo ,  Meizhong Xu ,  Colin Zhang ,  Brian W. Metcalf ,  Chunhong He ,  Ding-Quan Qian

IPC分类号： C07D207/06 ,  A61K31/407 ,  C07D495/04 ,  C07D493/10 ,  C07D491/20 ,  C07D491/107 ,  C07D491/10 ,  C07D487/10 ,  C07D487/08 ,  C07D487/04 ,  C07D471/10 ,  C07D471/04 ,  C07D417/04 ,  C07D413/14 ,  C07D413/10 ,  C07D405/14 ,  C07D405/04 ,  C07D403/04 ,  C07D401/14 ,  C07D401/10 ,  C07D401/06 ,  C07D401/04 ,  C07D333/34 ,  C07D295/185 ,  C07D221/20 ,  C07D217/26 ,  C07D217/06 ,  C07D213/38 ,  C07D211/70 ,  C07D211/66 ,  C07D211/64 ,  C07D211/58 ,  C07D211/52 ,  C07D211/48 ,  C07D211/46 ,  C07D211/34 ,  C07D211/22 ,  C07D211/18 ,  C07D211/16 ,  C07D209/70 ,  C07D209/62 ,  C07D209/52 ,  C07D209/44 ,  C07D209/42 ,  C07D209/08 ,  C07D207/27 ,  C07D207/16 ,  C07D207/14 ,  C07D207/12 ,  C07D207/10 ,  C07D207/08 ,  A61K31/4439 ,  C07D498/20 ,  C07D513/10

CPC分类号： C07D207/06 ,  A61K31/407 ,  A61K31/4439 ,  C07D207/08 ,  C07D207/10 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D207/27 ,  C07D209/08 ,  C07D209/42 ,  C07D209/44 ,  C07D209/52 ,  C07D209/62 ,  C07D209/70 ,  C07D211/16 ,  C07D211/18 ,  C07D211/22 ,  C07D211/34 ,  C07D211/46 ,  C07D211/48 ,  C07D211/52 ,  C07D211/58 ,  C07D211/64 ,  C07D211/66 ,  C07D211/70 ,  C07D213/38 ,  C07D217/06 ,  C07D217/26 ,  C07D221/20 ,  C07D295/185 ,  C07D333/34 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/10 ,  C07D491/107 ,  C07D491/20 ,  C07D493/10 ,  C07D495/04 ,  C07D498/20 ,  C07D513/10

摘要： The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

公开(公告)号：US20170304292A1

公开(公告)日：2017-10-26

申请号：US15517795

申请日：2015-10-06

申请人： UCB Biopharma SPRL

发明人： Anne VALADE ,  Eric JNOFF ,  Ali ATES ,  Pierre BURSSENS ,  David SKOLC ,  Zara SANDS ,  Benoit MATHIEU

IPC分类号： A61K31/4725 ,  C07D403/06 ,  C07D401/06 ,  C07D413/04 ,  C07D217/06

CPC分类号： A61K31/4725 ,  C07D217/06 ,  C07D401/06 ,  C07D403/06 ,  C07D413/04

摘要： The present invention relates to tetrahydroisoquinoline derivatives according to formula (I), which are Positive Allosteric Modulators of D1 and accordingly of benefit as pharmaceutical agents for the treatment of diseases in which D1 receptors play a role.

公开(公告)号：US20170273966A1

公开(公告)日：2017-09-28

申请号：US15508557

申请日：2015-08-31

申请人： Merck Sharp & Dohme Corp.

发明人： Jason Imbriglio ,  Clare London ,  Zhijian Lu ,  James Tata ,  Yusheng Xiong ,  Ming You ,  Hyewon Youm

IPC分类号： A61K31/47 ,  C07C13/04 ,  A61K31/16 ,  C07D217/06

CPC分类号： A61K31/47 ,  A61K31/16 ,  C07C13/04 ,  C07D217/06 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

摘要： The present invention relates to a compound represented by formula I:and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardio renal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.

公开(公告)号：US20170029375A1

公开(公告)日：2017-02-02

申请号：US15038754

申请日：2014-12-04

申请人： Conopco, Inc., d/b/a UNILEVER

发明人： Bijan HARICHIAN ,  Jose Guillermo ROSA

IPC分类号： C07D211/16

CPC分类号： C07D211/16 ,  C07C231/02 ,  C07C2603/74 ,  C07D205/02 ,  C07D207/06 ,  C07D211/62 ,  C07D215/08 ,  C07D217/06 ,  C07D295/185 ,  C07C233/58

摘要： An effective process of making adamantanamide, which process is fast, does not the use of organic solvents or labor-intensive isolation or purification of the product, by removal of organic solvent or by-products, and has improved yield and purity.

摘要翻译： 制造金刚烷胺的有效方法，该方法快速，不通过去除有机溶剂或副产物而使用有机溶剂或劳动密集型的产物分离或纯化，并且具有提高的产率和纯度。