公开(公告)号：US12084425B2

公开(公告)日：2024-09-10

申请号：US17295843

申请日：2019-10-12

Applicant: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD. ,  SHANGHAI AOBO PHARMTECH, INC., LTD.

Inventor： Wei Xu ,  Xi Chen ,  Hong Gu

IPC: C07D307/87

CPC classification number: C07D307/87 ,  C07B2200/13

Abstract: Provided herein is a method for preparing an Escitalopram bis-hydroxynaphtoate ((S)-(+)-1-(3-(-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydro-5-cyanisob enzofuranone) crystal form A. Said method is ecofriendly and non pollutive, and the obtained Escitalopram bis-hydroxynaphtoate crystal form A is highly pure and easy to reproduce.

公开(公告)号：US20240294465A1

公开(公告)日：2024-09-05

申请号：US18567733

申请日：2022-06-09

Applicant: HELMHOLTZ ZENTRUM MUNCHEN - DEUTSCHES FORSCHUNGSZENTRUM FUR GESUNDHEIT UND UMWELT

Inventor： Gerald BURGSTALLER ,  Michael GERCKENS ,  Oliver PLETTENBURG ,  Ali YILDIRIM ,  Ma HUILONG

IPC: C07C235/38 ,  A61K31/167 ,  A61K31/245 ,  A61K31/343 ,  A61K31/353 ,  A61K31/357 ,  A61K31/36 ,  A61K31/37 ,  A61K31/396 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/4245 ,  A61K31/44 ,  A61K31/4402 ,  C07C317/32 ,  C07C325/02 ,  C07D209/08 ,  C07D213/643 ,  C07D213/75 ,  C07D229/02 ,  C07D231/20 ,  C07D235/08 ,  C07D249/04 ,  C07D271/12 ,  C07D307/81 ,  C07D307/87 ,  C07D311/20 ,  C07D311/58 ,  C07D317/60 ,  C07D319/18 ,  G01N33/50 ,  G01N33/58

CPC classification number: C07C235/38 ,  A61K31/167 ,  A61K31/245 ,  A61K31/343 ,  A61K31/353 ,  A61K31/357 ,  A61K31/36 ,  A61K31/37 ,  A61K31/396 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/4245 ,  A61K31/44 ,  A61K31/4402 ,  C07C317/32 ,  C07C325/02 ,  C07D209/08 ,  C07D213/643 ,  C07D213/75 ,  C07D229/02 ,  C07D231/20 ,  C07D235/08 ,  C07D249/04 ,  C07D271/12 ,  C07D307/81 ,  C07D307/87 ,  C07D311/20 ,  C07D311/58 ,  C07D317/60 ,  C07D319/18 ,  G01N33/5044 ,  G01N33/582 ,  C07C2601/02

Abstract: The present invention relates to new cinnamic add amides which may be used for treatment of fibrosis and neoplasia and to cinnamic acid amides for use in the treatment of fibrosis, neoplasia, arthrolithiasis, familiar mediterranean fever and pericarditis. Further, the invention relates to a pharmaceutical composition comprising said cinnamic acid amides and to a screening essay for identifying compounds suitable for the treatment of fibrosis.

公开(公告)号：US11897858B2

公开(公告)日：2024-02-13

申请号：US17866513

申请日：2022-07-17

Applicant: Mark Hasleton

Inventor： Anton Frenkel ,  Raeann Ruiyun

IPC: C07D307/87

CPC classification number: C07D307/87 ,  C07B2200/13

Abstract: The present disclosure relates to a new salt of escitalopram and its solid state forms, processes for the preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

公开(公告)号：US10374167B2

公开(公告)日：2019-08-06

申请号：US15036311

申请日：2014-10-20

Applicant: Merck Patent GmbH

Inventor： Philipp Stoessel ,  Amir Hossain Parham ,  Christof Pflumm ,  Anja Jatsch

IPC: H01L51/00 ,  H01L51/50 ,  C07D209/86 ,  C07D219/14 ,  C07D307/87 ,  C07D471/04 ,  C07D487/04 ,  C07D491/107 ,  C09K11/06 ,  H01L51/56

Abstract: The present invention relates to novel compounds according to formula (I) having a six-membered ring structure substituted with electron donor, electron acceptor and sterically demanding groups. Said compound is suited for use in organic electronic devices, particularly in organic electroluminescent devices (OLEDs). Formula (I) wherein Q1 and Q2 are independently of each other selected from the group consisting of N, CRA, CRD, and CRS; Z1 and Z2 are independently of each other selected from the group consisting of N, CRA and CRD; RA is a group with −M-effect; RD is a group with +M-effect; and RS is a sterically demanding group, with the provision that the compound of general formula (I) comprises at least one group CRA and at least one group CRD.

公开(公告)号：US20190071405A1

公开(公告)日：2019-03-07

申请号：US16181864

申请日：2018-11-06

Applicant: AUTIFONY THERAPEUTICS LIMITED

Inventor： Agostino Marasco ,  Giuseppe Alvaro ,  Anne Dècor ,  Dieter Hamprecht ,  Paolo Dambruoso ,  Simona Tommasi

IPC: C07D249/12 ,  C07C255/37 ,  C07C43/225 ,  C07C255/46 ,  C07C43/313 ,  C07D307/87 ,  C07D401/04 ,  C07D311/96 ,  C07D311/76 ,  C07D311/04 ,  C07D307/94 ,  C07D405/14 ,  C07C255/48 ,  C07C43/29

Abstract: Compounds of formula (I) are of use in the modulation of Kv3.1, Kv.3.2 and Kv3.3 channels and have utility in the treatment or prevention of related disorders.

公开(公告)号：US09713602B1

公开(公告)日：2017-07-25

申请号：US15071184

申请日：2016-03-15

Applicant: National Sun Yat-sen University

Inventor： Chia-Chen Wang ,  Wei-Ren Chen

IPC: C07D307/87 ,  C07D307/77 ,  C07D493/04 ,  A61K31/343 ,  A61K31/663

CPC classification number: A61K31/343 ,  A61K31/365 ,  A61K31/6615 ,  A61K31/663 ,  A61K2300/00

Abstract: The present invention relates to a method for increasing the oxygen release efficiency of a hemoglobin-based blood substitute by using a phthalide compound, comprising the steps of: administering to a subject in need thereof the phthalide compound or co-administering to the subject in need thereof the phthalide compound along with the hemoglobin-based blood substitute, wherein the phthalide compound has an effect of increasing the oxygen release efficiency of the hemoglobin-based blood substitute, wherein the hemoglobin-based blood substitute can be fetal hemoglobin (HbF) or other Hb variants retaining two native α subunits. The phthalide compound is used to substitute for or cooperate with 2,3-BPG, to play a role of a 2,3-BPG substitute, to act on the hemoglobin-based blood substitute to effectively substitute the function of normal hemoglobin in releasing oxygen to tissue cells, in order to maintain the cellular oxygenation level within a normal range.

公开(公告)号：US09700563B2

公开(公告)日：2017-07-11

申请号：US15135433

申请日：2016-04-21

Applicant: Dennis Michael Godek ,  Harry Ralph Howard

Inventor： Dennis Michael Godek ,  Harry Ralph Howard

IPC: A61K31/5377 ,  A61K31/4025 ,  A61K31/4178 ,  A61K31/343 ,  C07D405/06 ,  C07D405/04 ,  C07D307/87

CPC classification number: A61K31/5377 ,  A61K31/343 ,  A61K31/4025 ,  A61K31/4178 ,  C07D307/87 ,  C07D405/04 ,  C07D405/06

Abstract: The invention is directed to a method of treatment for chronic pain, the method comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20160301016A1

公开(公告)日：2016-10-13

申请号：US15036311

申请日：2014-10-20

Applicant: MERCK PATENT GMBH

Inventor： Philipp STOESSEL ,  Amir Hossain PARHAM ,  Christof PFLUMM ,  Anja JATSCH

IPC: H01L51/00 ,  C07D209/86 ,  C07D487/04 ,  C07D219/14 ,  C07D491/107 ,  C07D471/04 ,  C09K11/06 ,  C07D307/87

CPC classification number: H01L51/0072 ,  C07D209/86 ,  C07D219/14 ,  C07D307/87 ,  C07D471/04 ,  C07D487/04 ,  C07D491/107 ,  C09K11/06 ,  C09K2211/1007 ,  C09K2211/1011 ,  C09K2211/1014 ,  C09K2211/1029 ,  C09K2211/1033 ,  C09K2211/1044 ,  C09K2211/1088 ,  H01L51/005 ,  H01L51/0052 ,  H01L51/0058 ,  H01L51/006 ,  H01L51/0061 ,  H01L51/0071 ,  H01L51/0073 ,  H01L51/5012 ,  H01L51/5024 ,  H01L51/5076 ,  H01L51/5092 ,  H01L51/5096 ,  H01L51/56 ,  Y02E10/549 ,  Y02P70/521

Abstract: The present invention relates to novel compounds according to formula (I) having a six-membered ring structure substituted with electron donor, electron acceptor and sterically demanding groups. Said compound is suited for use in organic electronic devices, particularly in organic electroluminescent devices (OLEDs). Formula (I) wherein Q1 and Q2 are independently of each other selected from the group consisting of N, CRA, CRD, and CRS; Z1 and Z2 are independently of each other selected from the group consisting of N, CRA and CRD; RA is a group with −M-effect; RD is a group with +M-effect; and RS is a sterically demanding group, with the provision that the compound of general formula (I) comprises at least one group CRA and at least one group CRD.

公开(公告)号：US09289366B2

公开(公告)日：2016-03-22

申请号：US14465993

申请日：2014-08-22

Applicant: International Flavors & Fragrances Inc.

Inventor： Benjamin Amorelli ,  Edward Mark Arruda ,  Robert P. Belko ,  Tingwei Cai ,  Adam P. Closson ,  Nicole L. Giffin ,  Gary J. Mertz ,  Michael G. Monteleone

IPC: A61K8/00 ,  A61K8/49 ,  C11B9/00 ,  C11D3/50 ,  A61K8/36 ,  A61K8/33 ,  A61Q5/02 ,  A61Q19/10 ,  A61Q11/00 ,  C07D307/87 ,  C07C47/21 ,  C07D307/83 ,  C07C69/96 ,  C07C43/162 ,  C07C69/75 ,  C07C69/60 ,  C07C49/385 ,  C07C49/587

CPC classification number: C07C69/75 ,  A61K8/33 ,  A61K8/36 ,  A61K8/37 ,  A61K8/498 ,  A61Q5/00 ,  A61Q5/02 ,  A61Q11/00 ,  A61Q13/00 ,  A61Q15/00 ,  A61Q19/00 ,  A61Q19/10 ,  C07C43/162 ,  C07C47/21 ,  C07C49/385 ,  C07C49/587 ,  C07C69/60 ,  C07C69/96 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07C2602/42 ,  C07D307/83 ,  C07D307/87 ,  C11B9/0015 ,  C11B9/0019 ,  C11B9/0034 ,  C11B9/0038 ,  C11B9/0076 ,  C11D3/2072 ,  C11D3/50

Abstract: The present invention relates to novel compounds and their use as fragrance materials.

Abstract translation: 本发明涉及新型化合物及其作为香料的用途。

公开(公告)号：US09249128B2

公开(公告)日：2016-02-02

申请号：US13881884

申请日：2011-10-21

Applicant: Benjamin Cravatt ,  Daniel Nomura ,  Jae W. Chang

Inventor： Benjamin Cravatt ,  Daniel Nomura ,  Jae W. Chang

IPC: C07C69/017 ,  C07D409/12 ,  C07C271/44 ,  C07C271/46 ,  C07C271/48 ,  C07D207/327 ,  C07D307/86 ,  C07D317/16 ,  C07D403/12 ,  C07D405/12 ,  C07D207/337 ,  C07D307/87 ,  C07D333/24

CPC classification number: C07D409/12 ,  C07C69/017 ,  C07C271/44 ,  C07C271/46 ,  C07C271/48 ,  C07D207/327 ,  C07D207/337 ,  C07D307/86 ,  C07D307/87 ,  C07D317/16 ,  C07D333/24 ,  C07D403/12 ,  C07D405/12

Abstract: Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar IC50 values. An exemplary compound of the invention was shown to be an effective inhibitor of prostate cancer pathogenesis. Other inhibitory compounds of the invention comprising fluorophore groups are shown to be effective in spatial and temporal localization of the serine hydrolase in cells and tissues.

Abstract translation: 丝氨酸水解酶涉及诸如癌症，中枢神经系统疾病，心血管疾病，肥胖症和代谢紊乱等病症。 在蛋白质组文库中表达的许多丝氨酸水解酶在体内是未知的功能。 通过文库与文库筛选鉴定的化合物可用于治疗与特异性丝氨酸水解酶KIAA1363（也称为AADACL1）相关的病症。 制备KIAA1363抑制剂文库，将候选化合物鉴定为具有亚微米IC50值的有效抑制剂。 本发明的示例性化合物被证明是前列腺癌发病机制的有效抑制剂。 显示包含荧光团基团的本发明的其它抑制化合物在丝氨酸水解酶在细胞和组织中的空间和时间定位方面是有效的。