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1. (WO2018121228) COMPOUND HAVING AXL INHIBITORY ACTIVITY, PREPARATION METHOD THEREFOR AND USE THEREOF
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Pub. No.: WO/2018/121228 International Application No.: PCT/CN2017/115380
Publication Date: 05.07.2018 International Filing Date: 11.12.2017
IPC:
C07D 487/04 (2006.01) ,C07F 7/08 (2006.01) ,C07F 7/10 (2006.01) ,A61K 31/519 (2006.01) ,A61K 31/695 (2006.01) ,A61K 31/55 (2006.01) ,A61K 31/5377 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
7
Compounds containing elements of the 4th Group of the Periodic System
02
Silicon compounds
08
Compounds having one or more C-Si linkages
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
7
Compounds containing elements of the 4th Group of the Periodic System
02
Silicon compounds
08
Compounds having one or more C-Si linkages
10
containing nitrogen
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
695
Silicon compounds
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
55
having seven-membered rings, e.g. azelastine, pentylenetetrazole
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
535
having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5375
1,4-Oxazines, e.g. morpholine
5377
not condensed and containing further heterocyclic rings, e.g. timolol
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
中国科学院上海药物研究所 SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES [CN/CN]; 中国上海市 浦东张江祖冲之路555号 555 Zu Chong Zhi Road, Zhang Jiang, Pudong Shanghai 201203, CN
Inventors:
段文虎 DUAN, Wenhu; CN
耿美玉 GENG, Meiyu; CN
王蔚 WANG, Wei; CN
丁健 DING, Jian; CN
艾菁 AI, Jing; CN
许丹丹 XU, Dandan; CN
彭霞 PENG, Xia; CN
曹素芬 CAO, Sufen; CN
季寅淳 JI, Yinchun; CN
Agent:
上海一平知识产权代理有限公司 XU & PARTNERS, LLC.; 中国上海市 普陀区真北路958号天地科技广场1号楼106室 Room No.106, Building No.1, Universal High-Tech Plaza, 958 Zhen Bei Road, Putuo District Shanghai 200333, CN
Priority Data:
201611237355.828.12.2016CN
Title (EN) COMPOUND HAVING AXL INHIBITORY ACTIVITY, PREPARATION METHOD THEREFOR AND USE THEREOF
(FR) COMPOSÉ AYANT UNE ACTIVITÉ INHIBITRICE D'AXL, SA MÉTHODE DE PRÉPARATION ET SON UTILISATION
(ZH) 一种具有AXL抑制活性的化合物及其制备和应用
Abstract:
(EN) The present invention relates to a compound having AXL inhibitory activities, a preparation method therefor and use thereof. In particular, disclosed is a compound of a structure as represented by formula (I), each group and substituent thereof are as defined in the description. Further disclosed is a preparation method of the described compound and use thereof as a protein tyrosine kinase inhibitor, in particular as an AXL inhibitor, in medicaments for the treatment of cancer-related diseases.
(FR) La présente invention concerne un composé ayant des activités inhibitrices d'AXL, sa méthode de préparation et son utilisation. En particulier, l'invention concerne un composé de structure telle que représentée par la formule (I), chaque groupe et son substituant étant tels que définis dans la description. L'invention concerne en outre une méthode de préparation du composé décrit et son utilisation en tant qu'inhibiteur d'une protéine tyrosine kinase, en particulier en tant qu'inhibiteur d'AXL, dans des médicaments pour le traitement de maladies associées au cancer.
(ZH) 本发明涉及一种具有AXL抑制活性的化合物及其制备和应用。具体地,本发明公开了式(I)所示结构的化合物,其中各基团和取代基如说明书中所定义。本发明还公开了上述化合物的制备方法及其作为蛋白酪氨酸激酶抑制剂,特别是作为AXL抑制剂,在治疗癌症相关疾病的药物中的用途。
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
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)