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1. (WO2019024876) FORMYLPYRIDINE DERIVATIVE HAVING FGFR4 INHIBITORY ACTIVITY, PREPARATION METHOD THEREFOR AND USE THEREOF
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2019/024876 International Application No.: PCT/CN2018/098078
Publication Date: 07.02.2019 International Filing Date: 01.08.2018
IPC:
C07D 213/75 (2006.01) ,C07D 213/04 (2006.01) ,C07D 401/14 (2006.01) ,C07D 401/12 (2006.01) ,A61K 31/444 (2006.01) ,A61K 31/506 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60
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
72
Nitrogen atoms
75
Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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
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
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
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
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
444
containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
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
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
上海和誉生物医药科技有限公司 ABBISKO THERAPEUTICS CO., LTD. [CN/CN]; 中国上海市 浦东新区中国(上海)自由贸易试验区蔡伦路780号721室 Room 721, No. 780 Cailun Road, China (Shanghai) Pilot Free Trade Zone, Pudong New Area Shanghai 201203, CN
Inventors:
邓海兵 DENG, Haibing; CN
杨飞 YANG, Fei; CN
喻红平 YU, Hongping; CN
陈椎 CHEN, Zhui; CN
徐耀昌 XU, Yaochang; 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 106, Building No. 1, Universal High-Tech Plaza 958 Zhen Bei Road, Putuo District Shanghai 200333, CN
Priority Data:
201710661244.804.08.2017CN
Title (EN) FORMYLPYRIDINE DERIVATIVE HAVING FGFR4 INHIBITORY ACTIVITY, PREPARATION METHOD THEREFOR AND USE THEREOF
(FR) DÉRIVÉ DE FORMYLPYRIDINE AYANT UNE ACTIVITÉ INHIBITRICE DE FGFR4, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
(ZH) 一种具有FGFR4抑制活性的醛基吡啶衍生物、其制备方法和应用
Abstract:
(EN) The present invention relates to formylpyridine derivatives having FGFR4 inhibitory activities, a preparation method therefor and use thereof, the formylpyridine derivatives having a structure of formula (I), the definition of each substituent in the formula being as described in the description and claims. The series of compounds of the present invention have very strong inhibitory effects on FGFR4 kinases, have very high selectivity, and can be widely used in the preparation of medicaments for treating cancers, particularly prostate cancer, liver cancer, pancreatic cancer, esophageal cancer, stomach cancer, lung cancer, breast cancer, ovarian cancer, colon cancer, skin cancer, neuroglioblastoma or rhabdomyosarcoma, and prospectively will be further developed to become a new generation of FGFR4 inhibitors.
(FR) La présente invention concerne des dérivés de formylpyridine ayant des activités inhibitrices de FGFR4, leur procédé de préparation et leur utilisation, les dérivés formylpyridine ayant une structure de formule (I), la définition de chaque substituant dans la formule étant telle que décrite dans la description et les revendications. La série de composés selon la présente invention possède un effet inhibiteur très puissant sur les kinases FGFR4, ainsi qu'une sélectivité très élevée, et peut être largement utilisée dans la préparation de médicaments destinés au traitement de cancers, en particulier le cancer de la prostate, le cancer du foie, le cancer du pancréas, le cancer de l'œsophage, le cancer de l'estomac, le cancer du poumon, le cancer du sein, le cancer de l'ovaire, le cancer du côlon, le cancer de la peau, le neuroglioblastome ou le rhabdomyosarcome, et est censé être développé de manière prospective en une nouvelle génération d'inhibiteurs de FGFR4.
(ZH) 本发明涉及一种具有FGFR4抑制活性的醛基吡啶衍生物、其制备方法和应用,所述甲酰基吡啶衍生物具有式(I)结构,式中各取代基的定义如说明书和权利要求书所述。本发明系列化合物对FGFR4激酶具有很强的抑制作用,并具有非常高的选择性,可广泛应用于制备治疗癌症特别是前列腺癌、肝癌、胰腺癌、食管癌、胃癌、肺癌、乳腺癌、卵巢癌、结肠癌、皮肤癌、神经胶质母细胞瘤或横纹肌肉瘤的药物,有望开发成新一代FGFR4抑制剂。
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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)