公开(公告)号：US12098119B2

公开(公告)日：2024-09-24

申请号：US17293917

申请日：2018-05-14

Applicant: Nutshell BioTech (Shanghai) Co., Ltd.

Inventor： Jian Zhang ,  Yinyi Chen ,  Cong Ruan ,  Xiuyan Yang ,  Chengxiang Wang ,  Qiufen Zhang ,  Jialin Shang ,  Xinyuan Xu

IPC: C07C303/38 ,  C07C311/37 ,  C07C311/44

CPC classification number: C07C303/38 ,  C07C311/37 ,  C07C311/44

Abstract: Disclosed by the present invention are an SIRT6 small-molecule allosteric activator and the application thereof and provided is an SIRT6 small-molecule allosteric activator that contains a derivative as shown in formula (1) or a pharmacologically acceptable salt thereof as the active ingredient. The SIRT6 small-molecule allosteric activator designed and synthesized in the present invention has high efficacy and low toxicity, may significantly activate SIRT6 activity during in vitro experiments, and has great importance in the development of pharmaceuticals for relevant diseases.

公开(公告)号：US10071956B2

公开(公告)日：2018-09-11

申请号：US15326379

申请日：2015-07-15

Applicant: SRF Limited

Inventor： Thirupathi Arumugam ,  Mariano Patrick Philips ,  Dilli Babu ,  Maheshwaran Chellaiah ,  Sarathy Iyengar ,  Rajdeep Anand

IPC: C07C303/38 ,  C07C311/48

CPC classification number: C07C303/38 ,  C07C311/48

Abstract: The present invention provides a process for the preparation of dibenzenesulfonimide.

公开(公告)号：US20180251423A1

公开(公告)日：2018-09-06

申请号：US15755356

申请日：2016-11-25

Applicant: CHINA PHARMACEUTICAL UNIVERSITY

Inventor： Qidong YOU ,  Zhengyu JIANG ,  Mengchen LU ,  Zhiyun CHEN ,  Haopeng SUN ,  Xiaojin ZHANG ,  Xiaoke GUO ,  Xiaoli XU

IPC: C07C311/21 ,  C07C303/08 ,  A61P3/10 ,  A61P9/10 ,  A61P11/00 ,  A61P25/16 ,  A61P25/28

CPC classification number: C07C311/21 ,  A61P3/10 ,  A61P9/10 ,  A61P11/00 ,  A61P25/16 ,  A61P25/28 ,  C07C303/08 ,  C07C303/38 ,  C07C311/29 ,  C07C311/46 ,  C07D257/04

Abstract: Compounds of formula (I) having 1-sulfonamido-4-aryloxy as a basic backbone. A preliminary activity test showed that the compounds provide excellent interference of a binding of Nrf2 by Keap1, thereby activating Nrf2. The compounds have a potential anti-inflammatory activity and can be used to treat a plurality of inflammation-associated diseases, including chronic obstructive pulmonary disease (COPD), Alzheimer's disease, Parkinson's disease, atherosclerosis, chronic kidney disease (CKD), diabetes, gastroenteritis, rheumatoid arthritis, and the like.

公开(公告)号：US09861977B2

公开(公告)日：2018-01-09

申请号：US15078209

申请日：2016-03-23

Applicant: NISSAN NORTH AMERICA, INC.

Inventor： Rameshwar Yadav

IPC: H01M8/10 ,  C08G75/30 ,  B01J39/18 ,  C07C311/09 ,  C07C303/38 ,  C07C311/11 ,  C08G61/12 ,  C08F114/26 ,  B01J39/04 ,  B01J39/20 ,  H01M8/0239

CPC classification number: B01J39/20 ,  B01J39/05 ,  B01J41/12 ,  C07C303/38 ,  C07C303/40 ,  C07C311/09 ,  C07C311/11 ,  C08F8/30 ,  C08F8/34 ,  C08F114/26 ,  C08G61/121 ,  C08G2261/1452 ,  C08G2261/334 ,  C08G2261/516 ,  C08G2261/74 ,  H01M8/0239 ,  H01M8/103 ,  H01M8/1032 ,  H01M8/1039 ,  H01M2250/20 ,  Y02T90/32 ,  C07C311/48

Abstract: A multi-acid monomer disclosed herein has the formula wherein R is one or more units of a non-SO2F or non-SO2Cl portion of a polymer precursor in sulfonyl fluoride or sulfonyl chloride form, X is a non-sulfonyl halide group of a multi-sulfonyl halide compound having a minimum of two acid giving groups, and Y is remaining sulfonyl halide groups of the multi-sulfonyl halide compound.

公开(公告)号：US20170210912A1

公开(公告)日：2017-07-27

申请号：US15329408

申请日：2015-07-29

Applicant: MITSUBISHI MATERIALS CORPORATION ,  Mitsubishi Materials Electronic Chemicals Co., Ltd.

Inventor： Masato Fujita ,  Masakazu Uotani ,  Takeshi Kamiya ,  Tsunetoshi Honda ,  Daisuke Takano

IPC: C09D5/16 ,  B01D17/02 ,  C09D7/00 ,  C07C229/12 ,  C07C227/16 ,  C07C233/05 ,  C07C231/02 ,  C07C311/05 ,  C07C303/38 ,  C07C309/13 ,  C07C303/02 ,  C07D211/38 ,  C07D265/30 ,  C07D207/10 ,  C07D241/04 ,  C02F1/40

CPC classification number: C09D5/1625 ,  B01D17/02 ,  C02F1/40 ,  C07C227/06 ,  C07C227/08 ,  C07C227/16 ,  C07C227/18 ,  C07C229/06 ,  C07C229/12 ,  C07C231/02 ,  C07C231/12 ,  C07C233/05 ,  C07C233/08 ,  C07C303/02 ,  C07C303/22 ,  C07C303/38 ,  C07C303/40 ,  C07C309/04 ,  C07C309/13 ,  C07C309/29 ,  C07C311/03 ,  C07C311/05 ,  C07D207/10 ,  C07D211/38 ,  C07D241/04 ,  C07D265/30 ,  C08K5/17 ,  C08L101/00 ,  C09D5/16 ,  C09D7/20 ,  C09D7/40 ,  C09D201/00 ,  C09K3/00 ,  Y02W10/37

Abstract: The hydrophilic oil repellent includes one or more types of nitrogen-containing fluorine-based compounds. The nitrogen-containing fluorine-based compound includes any one hydrophilicity imparting group selected from the group consisting of anion type hydrophilicity imparting groups, cation type hydrophilicity imparting groups, and amphoteric type hydrophilicity imparting groups in the molecule.

公开(公告)号：US20160200730A1

公开(公告)日：2016-07-14

申请号：US15075033

申请日：2016-03-18

Applicant: Wei He

Inventor： Wei He

IPC: C07D487/04

CPC classification number: A61K31/519 ,  C07C303/38 ,  C07C311/08 ,  C07D487/04 ,  C07D519/00 ,  C07F5/025 ,  C07F5/04

Abstract: Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.

Abstract translation: 本文描述了一系列新的多氟取代的吡唑并嘧啶化合物或其盐。 这些化合物是Bruton的酪氨酸激酶（BTK）抑制剂。 这些化合物可具有更好的BTK抑制选择性和药代动力学性质。 本文公开了这些化合物的合成方法。 本文公开了多氟取代的二苯甲酮和取代的苯氧基苯的新型合成方法。 还公开了包含本文所述的BTK抑制剂的药物组合物。 本发明还涉及包含本文所述的化合物作为活性成分的药物制剂。 本发明还包括通过施用BTK抑制剂及其制剂来治疗和抑制自身免疫性疾病，超敏反应性疾病，炎性疾病和癌症的治疗方法。

公开(公告)号：US20140200362A1

公开(公告)日：2014-07-17

申请号：US14153878

申请日：2014-01-13

Applicant: Hoffmann-La Roche Inc.

Inventor： Jiang Zhu

IPC: C07C303/40

CPC classification number: C07C303/40 ,  C07C303/38 ,  C07C311/46 ,  C07C311/39

Abstract: The present invention provides a novel method for preparing compounds N-(4-nitro-2-sulfamoyl-phenyl)-malonamic acid methyl ester and N-(4-amino-2-sulfamoyl-phenyl)-malonamic acid methyl ester, which are novel intermediates for preparing a key intermediate N-(4-methanesulfonylamino-2-sulfamoyl-phenyl)-malonamic acid methyl ester, for the preparation of N-(3-{(1R,2S,7R,8S)-3-[(4-fluorophenyl)methyl]-6-hydroxy-4-oxo-3-azatricyclo [6.2.1.02,7]undec-5-en-5-yl}-1,1-dioxo-1,4-dihydro-1λ6,2,4-benzothiadiazin-7-yl)methanesulfonamide, also known commercially as Setrobuvir, a compound useful in treating hepatitis C.

Abstract translation: 本发明提供了制备化合物N-（4-硝基-2-氨磺酰基 - 苯基） - 丙酰甲酸甲酯和N-（4-氨基-2-氨磺酰基 - 苯基） - 丙酰甲酸甲酯的新方法，它们是 用于制备N-（3 - {（1R，2S，7R，8S）-3 - [（1R，2R）-3-甲氧基苯基） - 丙酰胺酸甲酯的关键中间体N-（4-甲磺酰氨基-2-氨磺酰基 - 苯基） 4-氟苯基）甲基] -6-羟基-4-氧代-3-氮杂三环[6.2.1.02,7]十一碳-5-烯-5-基} -1,1-二氧代-1,4-二氢-1λ6， 2,4-苯并噻二嗪-7-基）甲磺酰胺，也称为Setrobuvir，一种可用于治疗丙型肝炎的化合物。

公开(公告)号：US08685616B2

公开(公告)日：2014-04-01

申请号：US12997132

申请日：2009-06-10

Applicant: Kenneth E. Gonsalves ,  Mingxing Wang

Inventor： Kenneth E. Gonsalves ,  Mingxing Wang

IPC: G03F7/004 ,  C07C303/38 ,  G03F7/039

CPC classification number: G03F7/027 ,  C07C303/38 ,  C07C309/65 ,  C07C309/73 ,  C07C309/75 ,  C07C311/48 ,  C07C381/12 ,  C07C2602/42 ,  C07D333/46 ,  G03F7/0045 ,  G03F7/0046 ,  G03F7/039 ,  G03F7/0397 ,  Y10S430/106 ,  Y10S430/12 ,  Y10S430/122 ,  Y10S430/123

Abstract: The present invention provides photoacid generators for use in chemically amplified resists and lithographic processes using the same.

Abstract translation: 本发明提供用于化学放大抗蚀剂的光酸产生剂和使用其的光刻法。

公开(公告)号：US08513443B2

公开(公告)日：2013-08-20

申请号：US13386519

申请日：2010-07-10

Applicant: Andreas Maderna ,  Jean-Michel Vernier

Inventor： Andreas Maderna ,  Jean-Michel Vernier

IPC: C07D317/10

CPC classification number: C07C303/38 ,  C07C317/18 ,  C07C2601/02 ,  C07D317/18 ,  C07D317/26 ,  C07C311/28

Abstract: The present invention relates to the preparation of (R)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide and (S)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.

Abstract translation: 本发明涉及制备（R）-N-（3,4-二氟-2-（2-氟-4-碘苯基氨基）-6-甲氧基苯基）-1-（2,3-二羟基丙基）环丙烷-1 - 磺酰胺和（S）-N-（3,4-二氟-2-（2-氟-4-碘苯基氨基）-6-甲氧基苯基）-1-（2,3-二羟丙基）环丙烷-1-磺酰胺。

公开(公告)号：US20130172295A1

公开(公告)日：2013-07-04

申请号：US13779188

申请日：2013-02-27

Applicant: Gilead Sciences, Inc.

Inventor： Kenneth R. Crawford ,  Eric D. Dowdy ,  Arnold Gutierrez ,  Richard P. Polniaszek ,  Richard Hung Chiu Yu

IPC: C07F9/6561 ,  A61K31/665 ,  C07C311/29 ,  C07D493/04 ,  C07C51/41

CPC classification number: C07F9/6561 ,  A61K31/665 ,  C07C51/412 ,  C07C253/30 ,  C07C303/38 ,  C07C303/40 ,  C07C311/29 ,  C07D493/04 ,  C07F9/4006 ,  C07F9/4075 ,  C07F9/4084 ,  C07C255/60

Abstract: A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed

Abstract translation: 因此公开了用于制备抗病毒HIV蛋白酶抑制剂化合物的双呋喃中间体的合成方法