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1. (WO2019061791) COMPOUND REPRESENTED BY FORMULA I AND USE THEREOF
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2019/061791 International Application No.: PCT/CN2017/113619
Publication Date: 04.04.2019 International Filing Date: 29.11.2017
IPC:
C07D 491/052 (2006.01) ,C07D 493/04 (2006.01) ,C07D 498/04 (2006.01) ,A61K 31/407 (2006.01) ,A61K 31/436 (2006.01) ,A61K 31/357 (2006.01) ,A61K 31/5383 (2006.01) ,A61K 31/4188 (2006.01) ,A61K 45/06 (2006.01) ,A61P 35/00 (2006.01) ,A61P 35/02 (2006.01)
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
044
with only one oxygen atom as ring hetero atom in the oxygen-containing ring
052
the oxygen-containing ring being six-membered
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
493
Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
498
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
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
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
407
condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
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
4353
ortho- or peri-condensed with heterocyclic ring systems
436
the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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
335
having oxygen as the only ring hetero atom, e.g. fungichromin
357
having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
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
5383
ortho- or peri-condensed with heterocyclic ring systems
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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4164
1,3-Diazoles
4188
condensed with heterocyclic ring systems, e.g. biotin, sorbinil
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45
Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06
Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
02
specific for leukemia
Applicants:
清华大学 TSINGHUA UNIVERSITY [CN/CN]; 中国北京市 海淀区清华园 Qinghuayuan, Haidian District Beijing 100084, CN
Inventors:
黄子为 HUANG, Ziwei; CN
方雄 FANG, Xiong; CN
张汇钧 ZHANG, Huijun; CN
徐岩 XU, Yan; CN
安静 AN, Jing; CN
Agent:
北京清亦华知识产权代理事务所(普通合伙) TSINGYIHUA INTELLECTUAL PROPERTY LLC; 中国北京市 海淀区清华园清华大学照澜院商业楼301室 Room 301 Trade Building Zhaolanyuan, Tsinghua University Qinghuayuan, Haidian District Beijing 100084, CN
Priority Data:
201710885075.626.09.2017CN
Title (EN) COMPOUND REPRESENTED BY FORMULA I AND USE THEREOF
(FR) COMPOSÉ REPRÉSENTÉ PAR LA FORMULE I ET SON UTILISATION
(ZH) 式I所示化合物及其应用
Abstract:
(EN) Disclosed in the invention are a compound and a use thereof. The compound is a compound represented by formula I or a stereoscopic isomer, a racemate, an oxynitride, a hydrate, a metabolite, a pharmaceutically acceptable salt or prodrug of the compound represented by formula I, wherein R1, R2 and R3 are each independently -H, -OCH3, -F, Cl, -Br; X is -CN or -COOCH2CH3; and A is a linear fused ring or an angular fused ring. The compound represented by formula I is simple in structure and easy to prepare, relative to a pilot tubulin inhibitor mHA11, the compound is more efficient and less toxic and can effectively inhibit the normal functions of tumor cell tubulin, induce tumor cell apoptosis, and at the same time target and interfere with tumor angiogenesis.
(FR) L'invention concerne un composé et son utilisation. Le composé est un composé représenté par la Formule I ou un isomère stéréoscopique, un racémate, un oxynitrure, un hydrate, un métabolite, un sel ou promédicament pharmaceutiquement acceptable du composé représenté par la Formule I, dans laquelle R1, R2 et R3 sont chacun indépendamment -H, -OCH3, -F, Cl, -Br; X est -CN ou -COOCH2CH3; et A est un cycle fusionné linéaire ou un cycle fusionné angulaire. Le composé représenté par la Formule I est de structure simple et facile à préparer, par rapport à un inhibiteur de tubuline pilote mHA11, le composé est plus efficace et moins toxique et peut inhiber efficacement les fonctions normales de la tubuline de cellules tumorales, induire l'apoptose des cellules tumorales et, en même temps, cibler et interférer avec l'angiogenèse tumorale.
(ZH) 本发明公开了化合物及其应用。其中该化合物为式I所示化合物或式I所示化合物的立体异构体、消旋体、氮氧化物、水合物、代谢产物、药学上可接受的盐或前药,其中,R1, R2、R3 各自独立地为-H、-OCH3、-F、Cl、-Br; X 为-CN或-COOCH2CH3; A 为线型稠合环或角型稠合环。本发明的式I所示的化合物结构简洁且易于制备,相对于先导微管蛋白抑制剂 mHA11, 此类化合物更加高效低毒,能够高效地抑制肿瘤细胞的微管蛋白的正常功能,诱导肿瘤细胞凋亡,并能够同时靶向干扰肿瘤血管生成。
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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)