公开(公告)号：US20240287009A1

公开(公告)日：2024-08-29

申请号：US18411304

申请日：2024-01-12

申请人： Infineum International Limited

发明人： Evan A. HAIDASZ ,  Robert A. Clarkson ,  Michael A. Collins ,  BENJAMIN G. N. CHAPPELL

IPC分类号： C07D295/03 ,  C07C211/21 ,  C07C211/27 ,  C07C211/45 ,  C07C217/08 ,  C07C217/40 ,  C07C217/76 ,  C07D209/08 ,  C07D217/04 ,  C07D295/033 ,  C07D295/195 ,  C08F36/14

CPC分类号： C07D295/03 ,  C07C211/21 ,  C07C211/27 ,  C07C211/45 ,  C07C217/08 ,  C07C217/40 ,  C07C217/76 ,  C07D209/08 ,  C07D217/04 ,  C07D295/033 ,  C07D295/195 ,  C08F36/14

摘要： Disclosed herein are addition-polymerizable monomer composition including an amine-derivatized alpha-methyl styrene (ADAMS) monomer according to structure (I) and/or an aminated conjugated aliphatic methylated polyene (ACAMP) monomer according to structure (II):




with k, R1, R2, R3, and R4 defined herein. Difunctional monomers of these types with two polymerizable loci and/or two amine loci are also disclosed herein. Further disclosed herein are methods for making such compositions.

公开(公告)号：US20240199535A1

公开(公告)日：2024-06-20

申请号：US18554365

申请日：2022-04-08

申请人： IMMUNIC AG

发明人： Christian GEGE ,  Hella KOHLHOF ,  Andreas MÜHLER ,  Daniel VITT

IPC分类号： C07C233/75 ,  A61K31/16 ,  A61K31/167 ,  A61K31/341 ,  A61K31/381 ,  A61K31/426 ,  A61K31/437 ,  A61K31/44 ,  A61K31/472 ,  A61K31/5375 ,  A61P31/14 ,  C07C233/74 ,  C07D213/68 ,  C07D213/73 ,  C07D217/04 ,  C07D265/30 ,  C07D277/34 ,  C07D307/30 ,  C07D333/40 ,  C07D471/04

CPC分类号： C07C233/75 ,  A61K31/16 ,  A61K31/167 ,  A61K31/341 ,  A61K31/381 ,  A61K31/426 ,  A61K31/437 ,  A61K31/44 ,  A61K31/472 ,  A61K31/5375 ,  A61P31/14 ,  C07C233/74 ,  C07D213/68 ,  C07D213/73 ,  C07D217/04 ,  C07D265/30 ,  C07D277/34 ,  C07D307/30 ,  C07D333/40 ,  C07D471/04

摘要： The invention relates to novel deuterated compounds of Formula (I)




and their use as medicaments.

公开(公告)号：US20240174615A1

公开(公告)日：2024-05-30

申请号：US18377670

申请日：2023-10-06

申请人： Revolution Medicines, Inc.

发明人： Steven G. BALLMER ,  Xiaojun HUANG ,  Shaoling LI

IPC分类号： C07D217/04 ,  C07D487/04 ,  C07D498/18 ,  C07D519/00

CPC分类号： C07D217/04 ,  C07D487/04 ,  C07D498/18 ,  C07D519/00

摘要： The present disclosure relates to novel methods for preparing rapamycin analog compounds, as well as to related intermediates useful in such methods.

公开(公告)号：US11760764B2

公开(公告)日：2023-09-19

申请号：US17303089

申请日：2021-05-19

申请人： Aligos Therapeutics, Inc.

发明人： Tongfei Wu ,  Pierre Jean-Marie Bernard Raboisson ,  Antitsa Dimitrova Stoycheva ,  Francois Gonzalvez ,  Jerome Deval ,  Cheng Liu

IPC分类号： C07D519/00 ,  C07C229/16 ,  C07C215/14 ,  C07D233/36 ,  C07D207/267 ,  C07D295/135 ,  C07D217/02 ,  C07D209/44 ,  C07C211/42 ,  C07D205/12 ,  C07D491/107 ,  C07D217/04 ,  C07D401/14 ,  C07D471/04 ,  C07C233/36

CPC分类号： C07D519/00 ,  C07C211/42 ,  C07C215/14 ,  C07C229/16 ,  C07C233/36 ,  C07D205/12 ,  C07D207/267 ,  C07D209/44 ,  C07D217/02 ,  C07D217/04 ,  C07D295/135 ,  C07D401/14 ,  C07D471/04 ,  C07D491/107 ,  C07C2602/08

摘要： The present disclosure related to compounds that can be useful as inhibitors of PD-1, PD-L1 or the PD-1/PD-L1 interaction. Also disclosed herein are pharmaceutical compositions of that can include a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and uses of or methods of using a compound of Formula (I), or a pharmaceutically acceptable salt thereof, for the treatment of PD-L1 related diseases including but not limited to liver diseases, cancer, hepatocellular carcinoma, viral diseases, or hepatitis B.

公开(公告)号：US20230150929A1

公开(公告)日：2023-05-18

申请号：US17912485

申请日：2021-03-17

申请人： The Board of Regents of The University of Texas System

发明人： Jia Zhou ,  Stephen Yarwood ,  Pingyuan Wang ,  Urszula Luchowska-Stanska ,  Boy van Basten

IPC分类号： C07C311/51 ,  C07D215/20 ,  C07D215/22 ,  C07D239/78 ,  C07D217/04 ,  C07D487/04 ,  C07D213/74 ,  C07D209/04 ,  C07D231/56 ,  C07D213/61 ,  C07D231/12 ,  C07D307/38

CPC分类号： C07C311/51 ,  C07D209/04 ,  C07D213/61 ,  C07D213/74 ,  C07D215/20 ,  C07D215/22 ,  C07D217/04 ,  C07D231/12 ,  C07D231/56 ,  C07D239/78 ,  C07D307/38 ,  C07D487/04 ,  C07C2602/10

摘要： The invention relates generally to novel EPAC1 activators, such as Formula I and II and the preparation thereof as well as the use of EPAC1 activators disclosed herein as to selectively activate EPAC1 in cells.

公开(公告)号：US20180346486A1

公开(公告)日：2018-12-06

申请号：US16002007

申请日：2018-06-07

申请人： CADILA HEALTHCARE LIMITED

发明人： Ranjit C. DESAI ,  Brijeshkumar SRIVASTAVA

IPC分类号： C07D513/04 ,  C07F3/00 ,  A61K31/40 ,  C07D209/44 ,  C07D295/096 ,  C07D491/048 ,  C07D207/06 ,  C07D209/12 ,  C07D498/04 ,  C07D495/04 ,  C07D207/20 ,  C07D207/08 ,  C07D491/04 ,  C07D487/04 ,  C07D471/04 ,  C07D217/04 ,  C07D215/20 ,  C07D215/06 ,  A61K31/519 ,  A61K31/4985 ,  A61K31/472 ,  A61K31/47 ,  A61K31/439 ,  A61K31/437 ,  A61K31/4365 ,  A61K31/4162 ,  A61K31/407 ,  A61K31/404 ,  C07D491/08 ,  A61K31/496 ,  A61K31/4453 ,  A61K31/4375 ,  A61K31/435 ,  C07D209/08

CPC分类号： C07D513/04 ,  A61K31/40 ,  A61K31/404 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/435 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/439 ,  A61K31/4453 ,  A61K31/47 ,  A61K31/472 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/519 ,  C07D207/06 ,  C07D207/08 ,  C07D207/20 ,  C07D209/08 ,  C07D209/12 ,  C07D209/44 ,  C07D215/06 ,  C07D215/20 ,  C07D217/04 ,  C07D295/096 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D491/08 ,  C07D495/04 ,  C07D498/04 ,  C07F3/00

摘要： The present invention relates to a compound (3S)-3-(4-((3-(6-Oxa-3-azabicyclo [3.1.1]heptan-3-ylmethyl)benzyl)oxy)phenyl)hex-4-ynoic acid methods for use of this and other compounds.

公开(公告)号：US20180230083A1

公开(公告)日：2018-08-16

申请号：US15952031

申请日：2018-04-12

申请人： Auspex Pharmaceuticals, Inc.

发明人： Chengzhi Zhang

IPC分类号： C07C231/12 ,  C07C231/02 ,  C07B59/00

CPC分类号： C07C231/12 ,  C07B59/001 ,  C07B59/002 ,  C07B2200/05 ,  C07C221/00 ,  C07C231/02 ,  C07D217/04 ,  C07D455/06 ,  C07C233/18 ,  C07C223/02

摘要： The present invention relates to new methods of manufacturing benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), and intermediates thereof.

公开(公告)号：US09969723B2

公开(公告)日：2018-05-15

申请号：US14872745

申请日：2015-10-01

申请人： HYUNDAI PHARM CO., LTD

发明人： Jin Yang ,  Jin Woong Kim ,  Han Kyu Lee ,  Jae Hyun Kim ,  Chang Mo Son ,  kyu hwan Lee ,  Hyung-Ho Choi ,  daehoon Kim ,  Tae-Young Ha ,  Jaekeol Rhee

IPC分类号： A61K31/497 ,  C07D413/04 ,  C07D213/85 ,  C07D215/06 ,  C07D217/04 ,  C07D221/20 ,  C07D317/72 ,  C07D239/42 ,  C07D271/07 ,  C07D277/82 ,  C07D209/44 ,  C07D211/14 ,  C07D295/073 ,  C07D295/096 ,  C07C51/367 ,  C07C51/373 ,  C07C59/72 ,  C07C59/90 ,  C07D207/06 ,  C07D211/70 ,  C07D213/74 ,  C07D215/04 ,  C07D217/24 ,  C07D239/28 ,  C07D295/155

CPC分类号： C07D413/04 ,  C07C51/367 ,  C07C51/373 ,  C07C59/72 ,  C07C59/90 ,  C07D207/06 ,  C07D209/44 ,  C07D211/14 ,  C07D211/70 ,  C07D213/74 ,  C07D213/85 ,  C07D215/04 ,  C07D215/06 ,  C07D217/04 ,  C07D217/24 ,  C07D221/20 ,  C07D239/28 ,  C07D239/42 ,  C07D271/07 ,  C07D277/82 ,  C07D295/073 ,  C07D295/096 ,  C07D295/155 ,  C07D317/72

摘要： The present invention relates to a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient for the prevention and treatment of metabolic disease. The novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention has excellent activities of activating GPR40 protein and promoting insulin secretion accordingly but has no toxicity when co-administered with other drugs. That is, the novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention can be co-administered with other drugs and can promote the activation of GPR40 protein significantly, so that the composition comprising the same as an active ingredient can be efficiently used as a pharmaceutical composition for the prevention and treatment of metabolic disease such as obesity, type I diabetes, type II diabetes, incompatible glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, and syndrome X, etc.

公开(公告)号：US09890123B2

公开(公告)日：2018-02-13

申请号：US15178174

申请日：2016-06-09

申请人： Aerie Pharmaceuticals, Inc.

发明人： Mitchell A. deLong ,  Susan M. Royalty ,  Jill Marie Sturdivant ,  Geoffrey Richard Heintzelman

IPC分类号： C07D401/12 ,  C07D217/04 ,  A61K31/47 ,  C07D217/02 ,  C07D215/38 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

CPC分类号： C07D217/02 ,  C07D215/38 ,  C07D217/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： 6-Amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, obesity and glaucoma are also provided.

公开(公告)号：US20180022696A1

公开(公告)日：2018-01-25

申请号：US15550839

申请日：2016-02-11

申请人： LATVIAN INSTITUTE OF ORGANIC SYNTHESIS

发明人： Aigars JIRGENSONS ,  Einars LOZA ,  Michael CHARLTON ,  Paul William FINN ,  Lluis RIBAS DE POUPLANA ,  Adelaide SAINT-LÉGER

IPC分类号： C07C311/51 ,  C07D213/71 ,  C07D217/04 ,  C07D239/42 ,  C07D311/04 ,  C07D239/48 ,  C07D239/47 ,  C07D215/06 ,  C07D217/26

CPC分类号： C07C311/51 ,  C07C2601/02 ,  C07D213/71 ,  C07D215/06 ,  C07D215/36 ,  C07D217/04 ,  C07D217/22 ,  C07D217/26 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D251/22 ,  C07D311/04 ,  C07D311/20 ,  C07D487/04

摘要： The present invention relates to novel N-acyl-diarysulfonamides acting as inhibitors of bacterial aminoacyl-tRNA synthetase. These can be used as medicines or as constituent of medicines for the treatment of bacterial infections.