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1. WO2021042411 - AKR1C3 INHIBITOR OR PHARMACEUTICALLY ACCEPTABLE SALT OF SAME, PREPARATION METHOD FOR SAME, AND USES THEREOF

Publication Number WO/2021/042411
Publication Date 11.03.2021
International Application No. PCT/CN2019/105880
International Filing Date 16.09.2019
IPC
C07C 59/64 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
59Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O-metal, -CHO, keto, ether, groups, groups, or groups
40Unsaturated compounds
58containing ether groups, groups, groups, or groups
64containing six-membered aromatic rings
C07C 59/52 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
59Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O-metal, -CHO, keto, ether, groups, groups, or groups
40Unsaturated compounds
42containing hydroxy or O-metal groups
52a hydroxy or O-metal group being bound to a carbon atom of a six-membered aromatic ring
C07C 57/58 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
57Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
52containing halogen
58containing six-membered aromatic rings
C07C 63/72 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
63Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings
68containing halogen
72Polycyclic acids
C07C 51/353 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
51Preparation of carboxylic acids or their salts, halides, or anhydrides
347by reactions not involving formation of carboxyl groups
353by isomerisation; by change of size of the carbon skeleton
C07C 51/363 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
51Preparation of carboxylic acids or their salts, halides, or anhydrides
347by reactions not involving formation of carboxyl groups
363by introduction of halogen; by substitution of halogen atoms by other halogen atoms
CPC
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07C 205/56
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
205Compounds containing nitro groups bound to a carbon skeleton
49the carbon skeleton being further substituted by carboxyl groups
56having nitro groups bound to carbon atoms of six-membered aromatic rings and carboxyl groups bound to acyclic carbon atoms of the carbon skeleton
C07C 255/57
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
255Carboxylic acid nitriles
49having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
57containing cyano groups and carboxyl groups, other than cyano groups, bound to the carbon skeleton
C07C 2601/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
2601Systems containing only non-condensed rings
02with a three-membered ring
C07C 323/62
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
323Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
50containing thio groups and carboxyl groups bound to the same carbon skeleton
62having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
C07C 57/58
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
57Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
52containing halogen
58containing six-membered aromatic rings
Applicants
  • 中国药科大学 CHINA PHARMACEUTICAL UNIVERSITY [CN]/[CN]
Inventors
  • 孙昊鹏 SUN, Haopeng
  • 何思雨 HE, Siyu
  • 刘阳 LIU, Yang
  • 郭青龙 GUO, Qinglong
  • 冯锋 FENG, Feng
  • 赵丽 ZHAO, Li
Agents
  • 南京苏高专利商标事务所(普通合伙) NANJING SUGAO PATENT AND TRADEMARK FIRM (ORDINARY PARTNERSHIP)
Priority Data
201910845469.806.09.2019CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) AKR1C3 INHIBITOR OR PHARMACEUTICALLY ACCEPTABLE SALT OF SAME, PREPARATION METHOD FOR SAME, AND USES THEREOF
(FR) INHIBITEUR DE AKR1C3 OU UN SEL PHARMACEUTIQUEMENT ACCEPTABLE DE CELUI-CI, PROCÉDÉ DE PRÉPARATION CORRESPONDANT ET UTILISATIONS ASSOCIÉES
(ZH) AKR1C3抑制剂或其可药用的盐、其制备方法及用途
Abstract
(EN)
Disclosed are an AKR1C3 inhibitor or a pharmaceutically acceptable salt of same, a preparation method for same, and uses thereof. A structural optimization is performed with a nonsteroidal anti-inflammatory medicament, flurbiprofen, serving as a lead compound. Disclosed are the biphenyl AKR1C3 inhibitor as represented by formula (I) and the preparation method therefor. As proven in target activity tests, the compound of the present invention is provided with an activity for significantly inhibiting AKR1C3, can be further developed into a medicament for treating or preventing diseases by inhibiting aldehyde ketone reductase AKR1C3, and lays a molecular foundation for studies on mechanisms related to tumor resistance.
(FR)
L'invention concerne un inhibiteur d'AKR1C3 ou un sel pharmaceutiquement acceptable de celui-ci, un procédé de préparation correspondant et des utilisations associées. Une optimisation structurale est réalisée avec un médicament anti-inflammatoire non stéroïdien, du flurbiprofène, servant de composé tête de série. L'invention concerne un inhibiteur de biphényl AKR1C3 représenté par la formule (I) et un procédé de préparation correspondant. Des tests d'activité cible prouvent que le composé selon la présente invention est doté d'une activité pour inhiber de manière significative AKR1C3, peut en outre être développé en un médicament pour le traitement ou la prévention de maladies par inhibition de l'aldéhyde cétone réductase AKR1C3, et présente une base moléculaire pour des études sur des mécanismes liés à la résistance tumorale.
(ZH)
本发明公开了AKR1C3抑制剂或其可药用的盐、其制备方法及用途,以非甾体抗炎药氟比洛芬作为先导化合物进行结构的优化,公开了如 (I) 的联苯类AKR1C3抑制剂及其制备方法,靶标活性测试证明,本发明的化合物具有可明显抑制AKR1C3的活性,可作为进一步开发为通过抑制醛酮还原酶AKR1C3来治疗和/或预防疾病的药物,为肿瘤耐药相关机制学研究奠定分子基础。
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