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1. (WO2018137610) SUBSTITUTED 1-(ISOXAZOLE-3-YL)-3-(3-FLUORINE-4-PHENYL)UREA DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USE THEREOF
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Pub. No.: WO/2018/137610 International Application No.: PCT/CN2018/073793
Publication Date: 02.08.2018 International Filing Date: 23.01.2018
IPC:
C07D 471/04 (2006.01) ,C07D 413/12 (2006.01) ,C07D 401/14 (2006.01) ,C07D 215/22 (2006.01) ,C07D 491/056 (2006.01) ,A61K 31/519 (2006.01) ,A61K 31/435 (2006.01) ,A61K 31/506 (2006.01) ,A61K 31/517 (2006.01) ,A61P 35/04 (2006.01) ,A61P 37/02 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic 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
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
20
Oxygen atoms
22
attached in position 2 or 4
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
056
with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
517
ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
04
specific for metastasis
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37
Drugs for immunological or allergic disorders
02
Immunomodulators
Applicants:
四川大学 SICHUAN UNIVERSITY [CN/CN]; 中国四川省成都市 一环路南一段24号 No.24 South Section 1, Yihuan Road Chengdu, Sichuan 610065, CN
Inventors:
杨胜勇 YANG, Shengyong; CN
李琳丽 LI, Linli; CN
Agent:
成都君合集专利代理事务所(普通合伙) CHENGDU JUNHEJI PATENT OFFICE (ORDINARY PARTNERSHIP); 中国四川省成都市 天府大道北段1480号高新孵化园8栋2单元(德商国际A座)1001 Room 1001, Unit 2, Building 8, High-tech Incubation Park No.1480, the Northern Section of Tianfu Avenue. Chengdu, Sichuan 610000, CN
Priority Data:
201710060144.X24.01.2017CN
Title (EN) SUBSTITUTED 1-(ISOXAZOLE-3-YL)-3-(3-FLUORINE-4-PHENYL)UREA DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USE THEREOF
(FR) DÉRIVÉ D'URÉE DE 1-(ISOXAZOLE-3-YL)-3-(3-FLUOR-4-PHÉNYL) SUBSTITUÉ, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
(ZH) 取代的1-(异恶唑-3-基)-3-(3-氟-4-苯基)脲衍生物及其制备方法和用途
Abstract:
(EN) A substituted 1-(isoxazole-3-yl)-3-(3-fluorine-4-phenyl)urea derivative, and a preparation method therefor and a use thereof, relating to the technical field of organic synthesis of medicines. A substituted 1-(isoxazole-3-yl)-3-(3-fluorine-4-phenyl)urea derivative is provided, and the structural formula thereof is as represented by formula (I). Also provided is a preparation method for the substituted 1-( isoxazole-3-yl)-3-(3- fluorine-4-phenyl)urea derivative, and a use in preparing an FMS-fins-like tyrosine kinase 3 inhibitor. The present invention provides a novel effective choice for preparation of kinase inhibitors, preparation of medicines for treating autoimmune diseases, and preparation of angiogenesis inhibitors and antitumor medicines in the art, and has a very good application prospect.
(FR) La présente invention se rapporte au domaine technique de la synthèse organique de médicaments, et concerne un dérivé d'urée de 1-(isoxazole-3-yl)-3-(3-fluor-4-phényl) substitué, son procédé de préparation et son utilisation. L'invention concerne un dérivé d'urée de 1-(isoxazole-3-yl)-3-(3-fluor-4-phényl) substitué, et sa formule structurale est telle que représentée par la formule (I). L'invention concerne également un procédé de préparation du dérivé d'urée de 1-(isoxazole-3-yl)-3-(3-fluor-4-phényl) substitué, et une utilisation dans la préparation d'un inhibiteur de tyrosine kinase 3 de type FMS-fins. La présente invention concerne un nouveau choix efficace pour la préparation d'inhibiteurs de kinase, la préparation de médicaments pour le traitement de maladies auto-immunes, et la préparation d'inhibiteurs d'angiogenèse et de médicaments anti-tumoraux dans l'état de la technique, et présente ainsi une très bonne perspective d'application.
(ZH) 一种取代的1-(异恶唑-3-基)-3-(3-氟-4-苯基)脲衍生物及其制备方法和用途,属于有机合成药物技术领域。包括提供了一种取代的1-(异恶唑-3-基)-3-(3-氟-4-苯基)脲衍生物,其结构式如式Ⅰ所示。还提供了上述取代的1-(异恶唑-3-基)-3-(3-氟-4-苯基)脲衍生物的制备方法,及其在制备FMS-样酪氨酸激酶3抑制剂的用途。为本领域中的激酶抑制剂的制备、抗自身免疫性疾病药物的制备、新生血管生成抑制剂和抗肿瘤药物的制备提供了新的有效选择,具有很好的应用前景。
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African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Chinese (ZH)
Filing Language: Chinese (ZH)