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1. WO2020135210 - SUBSTITUTED ARYL COMPOUND AND PREPARATION METHOD THEREFOR AND USE THEREOF

Publication Number WO/2020/135210
Publication Date 02.07.2020
International Application No. PCT/CN2019/126555
International Filing Date 19.12.2019
IPC
C07D 405/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
14containing three or more hetero rings
C07D 498/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 471/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 451/02 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
451Heterocyclic compounds containing 8-azabicyclo octane, 9-azabicyclo nonane, or 3-oxa-9-azatricyclo nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
02containing not further condensed 8-azabicyclo octane or 3-oxa-9-azatricyclo nonane ring systems, e.g. tropane; Cyclic acetals thereof
A61K 31/444 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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
444containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4545 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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
445Non-condensed piperidines, e.g. piperocaine
4523containing further heterocyclic ring systems
4545containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
CPC
A61K 31/444
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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
444containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
A61K 31/4545
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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
445Non condensed piperidines, e.g. piperocaine
4523containing further heterocyclic ring systems
4545containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/506
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
506not condensed and containing further heterocyclic rings
A61K 31/53
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
53having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 31/5377
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
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
5377not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/5383
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
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
5383ortho- or peri-condensed with heterocyclic ring systems
Applicants
  • 四川科伦博泰生物医药股份有限公司 SICHUAN KELUN-BIOTECH BIOPHARMACEUTICAL CO., LTD. [CN]/[CN]
Inventors
  • 刘金明 LIU, Jinming
  • 何婷 HE, Ting
  • 蔡家强 CAI, Jiaqiang
  • 李晓勇 LI, Xiaoyong
  • 罗小勇 LUO, Xiaoyong
  • 田强 TIAN, Qiang
  • 宋宏梅 SONG, Hongmei
  • 薛彤彤 XUE, Tongtong
  • 王利春 WANG, Lichun
  • 王晶翼 WANG, Jingyi
Agents
  • 中国国际贸易促进委员会专利商标事务所 CCPIT PATENT AND TRADEMARK LAW OFFICE
Priority Data
201811616858.528.12.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) SUBSTITUTED ARYL COMPOUND AND PREPARATION METHOD THEREFOR AND USE THEREOF
(FR) COMPOSÉ ARYLE SUBSTITUÉ, PROCÉDÉ DE PRÉPARATION CORRESPONDANT ET UTILISATION ASSOCIÉE
(ZH) 取代芳基化合物及其制备方法和用途
Abstract
(EN)
Disclosed are a substituted aryl compound or pharmaceutically acceptable salts thereof, a stereoisomer, a polymorphic substance, a solvate, a N-oxide, an isotopically labeled compound, a metabolite or a prodrug and a preparation method therefor and a use thereof, pharmaceutical compositions containing the compound and therapeutic use thereof. The described compound or the pharmaceutical compositions thereof can inhibit the activity of adenosine A2a receptor and can be used for treatment and prevention of diseases related to adenosine A2a receptor, specifically for treatment of tumor.
(FR)
L'invention concerne un composé aryle substitué ou des sels pharmaceutiquement acceptables de celui-ci, un stéréoisomère, une substance polymorphe, un solvate, un N-oxyde, un composé marqué par un isotope, un métabolite ou un promédicament, un procédé de préparation correspondant et une utilisation associée, des compositions pharmaceutiques contenant le composé et une utilisation thérapeutique associée. Le composé selon l'invention ou les compositions pharmaceutiques de celui-ci peuvent inhiber l'activité du récepteur A2a de l'adénosine et peuvent être utilisés pour le traitement et la prévention de maladies associées au récepteur A2a de l'adénosine, en particulier pour le traitement d'une tumeur.
(ZH)
取代芳基化合物或其药学上可接受的盐、立体异构体、多晶型物、溶剂合物、N-氧化物、同位素标记的化合物、代谢物或前药及其制备方法和用途,包含所述化合物的药物组合物以及他们的治疗用途。上述化合物或其药物组合物能够抑制腺苷A2a受体活性,可用于治疗或预防与腺苷A2a受体有关疾病,尤其是用于治疗肿瘤。
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