公开(公告)号：US20240174626A1

公开(公告)日：2024-05-30

申请号：US18548366

申请日：2022-02-21

Applicant: COMPAGNIE GENERALE DES ETABLISSEMENTS MICHELIN

Inventor： Milan FEDURCO ,  Marco RIBEZZO

IPC: C07D277/14 ,  C08G18/10 ,  C08G18/38 ,  C08G63/685 ,  C08G63/688 ,  C08G69/42

CPC classification number: C07D277/14 ,  C08G18/10 ,  C08G18/3857 ,  C08G63/685 ,  C08G63/688 ,  C08G69/42

Abstract: Monomers which contain a 4-thiazolidinone unit connected to a benzene nucleus and which contain two functions selected from hydroxyl and carboxyl are provided. A process for synthesizing them and to the use of them in the synthesis of polycondensates such as polyamides, polyesters and polyurethanes is also provided. Due to the monomers according to the disclosure, 2-mercaptopropionic acid is not used in the synthesis of polycondensates containing 4-thiazolidinone units.

公开(公告)号：US20190315683A1

公开(公告)日：2019-10-17

申请号：US16443793

申请日：2019-06-17

Applicant: Promentis Pharmaceuticals, Inc.

Inventor： Michael Neary ,  James Nieman ,  Steven Tanis ,  Daniel Lawton ,  Garry Smith

IPC: C07C327/34 ,  C07C323/60 ,  C07D277/14 ,  C07C327/26 ,  C07D277/08 ,  C07C327/32 ,  C07C329/06 ,  C07C323/59 ,  C07C323/58 ,  C07C323/57 ,  C07D241/08 ,  C07D327/04

Abstract: Novel substituted N-acetyl-L-cysteine (NAC) derivatives and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction.

公开(公告)号：US10071958B2

公开(公告)日：2018-09-11

申请号：US14888576

申请日：2014-05-01

Applicant: API Corporation

Inventor： Yuuki Asuma ,  Hisatoshi Uehara ,  Tomoko Maeda ,  Yasuyo Saito ,  Ryoma Miyake ,  Hiroshi Kawabata

IPC: C07C319/06 ,  C07C323/52 ,  C07C323/58 ,  C07D277/14 ,  C07C319/02 ,  C12P13/12 ,  C07C319/14 ,  C07C319/20 ,  C07C323/60

CPC classification number: C07C319/06 ,  C07C319/02 ,  C07C319/14 ,  C07C319/20 ,  C07C323/52 ,  C07C323/58 ,  C07C323/60 ,  C07D277/14 ,  C12P13/12 ,  C07C323/12 ,  C07C323/03

Abstract: According to the present invention, it becomes possible to perform a process for converting into an α-substituted cysteine represented by general formula (1) or a salt thereof at low cost and on an industrial scale by employing a process that is routed through a compound represented by general formula (3) to a compound represented by general formula (6). Particularly, by employing a process that is routed through a compound represented by general formula (7-2), it becomes possible to detach a tert-butyl protection group in a simple manner and to produce the compound represented by general formula (1) with high purity. Furthermore, by employing a process that is routed through tert-butylthiomethanol or a process that is routed through a compound represented by general formula (9), it becomes possible to produce a compound represented by general formula (2) without generating bischloromethylether that is an oncogenic substance. In the production of an α-substituted-D-cysteine or a salt thereof, it becomes possible to perform a process for converting the compound represented by general formula (2) into a compound represented by general formula (3S) in one step by allowing an enzyme or the like to act on the compound represented by general formula (2).

公开(公告)号：US20180251424A1

公开(公告)日：2018-09-06

申请号：US15978489

申请日：2018-05-14

Applicant: API Corporation

Inventor： Yuuki Asuma ,  Hisatoshi Uehara ,  Tomoko Maeda ,  Yasuyo Saito ,  Ryoma Miyake ,  Hiroshi Kawabata

IPC: C07C319/06 ,  C07C323/60 ,  C07C323/52 ,  C07C323/58 ,  C07C319/20 ,  C07C319/14 ,  C12P13/12 ,  C07D277/14 ,  C07C319/02 ,  C07C323/12 ,  C07C323/03

CPC classification number: C07C319/06 ,  C07C319/02 ,  C07C319/14 ,  C07C319/20 ,  C07C323/52 ,  C07C323/58 ,  C07C323/60 ,  C07D277/14 ,  C12P13/12 ,  C07C323/12 ,  C07C323/03

Abstract: According to the present invention, it becomes possible to perform a process for converting into an α-substituted cysteine represented by general formula (1) or a salt thereof at low cost and on an industrial scale by employing a process that is routed through a compound represented by general formula (3) to a compound represented by general formula (6). Particularly, by employing a process that is routed through a compound represented by general formula (7-2), it becomes possible to detach a tert-butyl protection group in a simple manner and to produce the compound represented by general formula (1) with high purity. Furthermore, by employing a process that is routed through tert-butylthiomethanol or a process that is routed through a compound represented by general formula (9), it becomes possible to produce a compound represented by general formula (2) without generating bischloromethylether that is an oncogenic substance. In the production of an α-substituted-D-cysteine or a salt thereof, it becomes possible to perform a process for converting the compound represented by general formula (2) into a compound represented by general formula (3S) in one step by allowing an enzyme or the like to act on the compound represented by general formula (2).

公开(公告)号：US20170253569A1

公开(公告)日：2017-09-07

申请号：US15449406

申请日：2017-03-03

Applicant: National Health Research Institutes

Inventor： Shau-Hua Ueng ,  Shiu-Hwa Yeh ,  Shu-Yu Lin ,  Chuan Shih

IPC: C07D277/14 ,  C07D417/10 ,  A61K31/427 ,  C07D417/12 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  C07H17/02 ,  A61K31/7056 ,  C07D417/04 ,  C07D277/54 ,  C07D249/08 ,  A61K31/433 ,  C07D417/14 ,  A61K31/497 ,  A61K31/506 ,  A61K31/402 ,  C07D207/27 ,  A61K45/06 ,  A61K31/426

CPC classification number: C07D277/14 ,  A61K31/402 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/485 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P29/00 ,  C07D207/27 ,  C07D249/08 ,  C07D277/54 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07H17/02 ,  A61K2300/00

Abstract: A pharmaceutical composition containing a compound of Formula (I) for treating an opioid receptor-associated condition. Also disclosed is a method for treating an opioid receptor-associated condition using such a compound. Further disclosed are two sets of thiazolidinone compounds of formula (I): (i) compounds each having an enantiomeric excess greater than 90% and (ii) compounds each being substituted with deuterium.

公开(公告)号：US09376408B2

公开(公告)日：2016-06-28

申请号：US14653437

申请日：2013-12-17

Applicant: Merck Sharp & Dohme Corp.

Inventor： Pengcheng Patrick Shao ,  Revathi Reddy Katipally

IPC: C07D277/14 ,  A61K31/426 ,  C07D417/06 ,  A61K31/4439 ,  C07D417/14 ,  A61K31/444 ,  A61K45/06 ,  C07D417/10

CPC classification number: C07D277/14 ,  A61K31/426 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D417/06 ,  C07D417/10 ,  C07D417/14

Abstract: Thiazolidinone compounds, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.

Abstract translation: 噻唑烷酮化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。

公开(公告)号：US20160081987A1

公开(公告)日：2016-03-24

申请号：US14391785

申请日：2012-07-30

Applicant: Daniel Lawton ,  Michael Neary ,  James A. Nieman

Inventor： Daniel Lawton ,  Michael Neary ,  James A. Nieman

IPC: A61K31/426 ,  C07D277/14 ,  A61K45/06 ,  C07D241/08 ,  A61K31/198 ,  C07D267/10 ,  C07K5/062

CPC classification number: A61K31/426 ,  A61K31/198 ,  A61K45/06 ,  C07D241/08 ,  C07D267/10 ,  C07D277/14 ,  C07K5/0606

Abstract: Novel cysteine prodrugs and their use in the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of the Central Nervous System (CNS), including but not limited to schizophrenia, drug craving, drug addiction, bipolar disorder, anxiety, depression, Parkinson's disease, Alzheimer's disease, cognitive dysfunction, multiple sclerosis, Amyotrophic lateral sclerosis (ALS), ischemic stroke, HIV dementia, and Huntington's disease.

公开(公告)号：US20150307464A1

公开(公告)日：2015-10-29

申请号：US14653437

申请日：2013-12-17

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Pengcheng Patrick Shao ,  Revathi Reddy Katipally

IPC: C07D277/14 ,  C07D417/06 ,  A61K45/06 ,  C07D417/14 ,  A61K31/444 ,  A61K31/426 ,  A61K31/4439

CPC classification number: C07D277/14 ,  A61K31/426 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D417/06 ,  C07D417/10 ,  C07D417/14

Abstract: Thiazolidinone compounds, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.

Abstract translation: 噻唑烷酮化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。

公开(公告)号：US08916712B2

公开(公告)日：2014-12-23

申请号：US14174669

申请日：2014-02-06

Applicant: Anne S. Martin ,  Board of Trustees of the University of Arkansas

Inventor： Alexei G. Basnakian ,  Richard B. Walker ,  John R. J. Sorenson

IPC: C07F3/06 ,  C07C323/58 ,  C07C323/25 ,  C07D207/16 ,  C07D277/06 ,  C07C323/59 ,  C07D277/14

CPC classification number: C07F3/06 ,  C07C323/25 ,  C07C323/58 ,  C07C323/59 ,  C07D207/16 ,  C07D277/06 ,  C07D277/14

Abstract: The present invention provides compositions and methods for cytoprotection. In particular, it provides zinc chelate compositions comprising at least one zinc ion and at least one aminothiol ligand.

Abstract translation: 本发明提供了用于细胞保护的组合物和方法。 特别地，其提供包含至少一种锌离子和至少一种氨基硫醇配体的锌螯合物组合物。

公开(公告)号：US20120088759A1

公开(公告)日：2012-04-12

申请号：US13319774

申请日：2010-05-11

Applicant: Hamed Aissaoui ,  Christoph Boss ,  Christine Brotschi ,  Markus Gude ,  John Gatfield ,  Romain Siegrist ,  Thierry Sifferlen ,  Jodi T. Williams

Inventor： Hamed Aissaoui ,  Christoph Boss ,  Christine Brotschi ,  Markus Gude ,  John Gatfield ,  Romain Siegrist ,  Thierry Sifferlen ,  Jodi T. Williams

IPC: A61K31/54 ,  C07D277/34 ,  C07D417/12 ,  A61K31/506 ,  A61K31/4439 ,  A61K31/426 ,  A61K31/498 ,  A61P25/22 ,  A61P25/00 ,  C07D417/10 ,  C07D417/04 ,  C07D279/06 ,  A61K31/501 ,  A61K31/427 ,  A61K31/4709 ,  A61K31/541 ,  A61P25/20 ,  A61P25/18 ,  C07D277/14

CPC classification number: C07D277/14 ,  C07D417/04

Abstract: The present invention relates to thiazolidin-4-one and [1,3]-thiazinan-4-one compounds of formula (I) wherein X, Y, R3 and R4 are as described in the description, or pharmaceutically acceptable salts thereof, for the prevention or treatment of diseases related to the orexin system. The present invention also relates to novel thiazolidin-4-one compounds of formula (II) and their use as pharmaceuticals, pharmaceutical compositions containing one or more compounds of formula (II), and especially their use as orexin receptor antagonists.

Abstract translation: 本发明涉及式（I）的噻唑烷-4-酮和[1,3]噻嗪-4-酮化合物，其中X，Y，R 3和R 4如说明书中所述或其药学上可接受的盐，用于 预防或治疗与食欲素系统有关的疾病。 本发明还涉及式（II）的新型噻唑烷-4-酮化合物及其作为药物的用途，含有一种或多种式（II）化合物的药物组合物，特别是其作为食欲素受体拮抗剂的用途。