Processing

Please wait...

Settings

Settings

Goto Application

1. WO2020182188 - SUBSTITUTED HETEROARYL COMPOUND, COMPOSITION OF SAME, AND USES THEREOF

Publication Number WO/2020/182188
Publication Date 17.09.2020
International Application No. PCT/CN2020/078990
International Filing Date 12.03.2020
IPC
C07D 487/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/519 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 37/02 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
CPC
A61K 31/519
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 37/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants
  • 习峰 XI, Feng [CN]/[CN]
Inventors
  • 习宁 XI, Ning
Priority Data
201910186757.713.03.2019CN
202010157262.409.03.2020CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) SUBSTITUTED HETEROARYL COMPOUND, COMPOSITION OF SAME, AND USES THEREOF
(FR) COMPOSÉ HÉTÉROARYLE SUBSTITUÉ, COMPOSITION CORRESPONDANTE ET UTILISATIONS ASSOCIÉES
(ZH) 取代的杂芳基化合物及其组合物和用途
Abstract
(EN)
Related to the field of pharmaceutics, specifically related to a substituted heteroaryl compound as represented by formula (I), or a stereoisomer, tautomer, nitrogen oxide, solvate, metabolite or pharmaceutically acceptable sale of same, a pharmaceutical composition comprising the compound, and uses of the compound and of the pharmaceutical composition thereof in preparing a medicament for treating proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancer, or other diseases in mammals. The compound provided exhibits great inhibiting activity and optimized kinase selectivity with respect to a target kinase. In addition, the compound provided also has excellent transmembrane properties, exhibits excellent pharmacokinetic properties in an animal body; therefore, the compound provided has great development prospects.
(FR)
La présente invention se rapporte au domaine des produits pharmaceutiques et concerne en particulier un composé hétéroaryle substitué tel que représenté par la formule (I), ou un stéréoisomère, un tautomère, un oxyde d'azote, un solvate, un métabolite ou un sel pharmaceutiquement acceptable de celui-ci, une composition pharmaceutique comprenant le composé, et des utilisations du composé et de la composition pharmaceutique correspondante dans la préparation d'un médicament pour le traitement de maladies prolifératives, de maladies auto-immunes, de maladies allergiques, de maladies inflammatoires, du rejet de greffe, du cancer ou d'autres maladies chez des mammifères. Le composé selon l'invention présente une activité inhibitrice élevée et une sélectivité de kinase optimisée par rapport à une kinase cible. De plus, le composé selon l'invention présente également d'excellentes propriétés transmembranaires, présente d'excellentes propriétés pharmacocinétiques chez un animal ; par conséquent, le composé selon l'invention présente de grandes perspectives de développement.
(ZH)
属于药物领域,具体涉及如式(I)所示的取代的杂芳基化合物、或其立体异构体、互变异构体、氮氧化物、溶剂化物、代谢产物或药学上可接受的盐,和包含所述化合物的药物组合物以及使用所述化合物及其药物组合物在制备治疗哺乳动物的增殖性疾病、自身免疫性疾病、过敏性疾病、炎性疾病、移植排斥、癌症或其他疾病的药物中的用途。提供的化合物对目标激酶显示出优异的抑制活性和优化的激酶选择性。此外,提供的化合物还具有优良的透膜性质,在动物体内显示出优良的药代动力学性质,因此,提供的化合物具有非常好的开发前景。
Latest bibliographic data on file with the International Bureau