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1. (WO2012167415) PYRIMIDOPYRIMIDONE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2012/167415 International Application No.: PCT/CN2011/002152
Publication Date: 13.12.2012 International Filing Date: 21.12.2011
IPC:
C07D 487/04 (2006.01) ,A61K 31/519 (2006.01) ,A61K 31/5377 (2006.01) ,A61K 31/551 (2006.01) ,A61K 31/541 (2006.01) ,A61P 35/00 (2006.01) ,A61P 35/02 (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
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
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
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
551
having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
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
54
having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
541
Non-condensed thiazines 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
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:
中国科学院广州生物医药与健康研究院 GUANGZHOU INSTITUTE OF BIOMEDICINE AND HEALTH, CHINESE ACADEMY OF SCIENCES [CN/CN]; 中国广东省广州市 科学城开源大道190号 190 Kai Yuan Avenue, Science Park Guangzhou, Guangdong 510530, CN (AllExceptUS)
丁克 DING, Ke [CN/CN]; CN (UsOnly)
常少华 CHANG, Shaohua [CN/CN]; CN (UsOnly)
徐石林 XU, Shilin [CN/CN]; CN (UsOnly)
张连文 ZHANG, Lianwen [CN/CN]; CN (UsOnly)
涂正超 TU, Zhengchao [CN/CN]; CN (UsOnly)
丁健 DING, Jian [CN/CN]; CN (UsOnly)
耿美玉 GENG, Meiyu [CN/CN]; CN (UsOnly)
陈奕 CHEN, Yi [CN/CN]; CN (UsOnly)
Inventors:
丁克 DING, Ke; CN
常少华 CHANG, Shaohua; CN
徐石林 XU, Shilin; CN
张连文 ZHANG, Lianwen; CN
涂正超 TU, Zhengchao; CN
丁健 DING, Jian; CN
耿美玉 GENG, Meiyu; CN
陈奕 CHEN, Yi; CN
Agent:
广州华进联合专利商标代理有限公司 ADVANCE CHINA I. P. LAW OFFICE; 中国广东省广州市 先烈中路69号918-920室万志香/何冲 WAN, Zhixiang/HE, Chong Suite 918-920, 9/F., Dong Shan Plaza, No.69 Xianlie Central Road Guangzhou, Guangdong 510095, CN
Priority Data:
201110156399.910.06.2011CN
Title (EN) PYRIMIDOPYRIMIDONE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
(FR) DÉRIVÉS DE PYRIMIDOPYRIMIDONE, COMPOSITIONS PHARMACEUTIQUES ET LEURS UTILISATIONS
(ZH) 嘧啶并嘧啶酮类化合物及其药用组合物和应用
Abstract:
(EN) Provided are 7-substituted amino-3, 4-2H-pyrimidine[4,5-d] pyridine-1H-one compounds represented by general formula (I) or (II) and their uses for preparing drugs for treating cancers. Researches have proved that they can inhibit the proliferation of many kinds of tumor cells and target to inhibit epidermal growth factor receptor kinase (EGFR), especially inhibit cancer cells of EGFR (T790M) mutant with single-point mutant or multi-points mutant. Therefore, they can be used as EGFR inhibitors for anti-cancer drugs, and possesses excellent value for uses.
(FR) L'invention concerne des composés d'amino-3,4-2H-pyrimidine[4,5-d]pyridine-1H-one 7-substituée représentés par la formule générale (I) ou (II), et leurs utilisations pour la préparation de médicaments pour le traitement des cancers. Les recherches ont prouvé qu'ils peuvent inhiber la prolifération de nombreux types de cellules tumorales et être ciblés pour inhiber la kinase du récepteur du facteur de croissance épidermique (EGFR), notamment pour inhiber les cellules cancéreuses d'EGFR (T790M) mutantes à mutations ponctuelles ou multiples. Ils peuvent par conséquent être utilisés en tant qu'inhibiteurs d'EGFR pour les médicaments anti-cancer, et possèdent une excellente valeur pour les utilisations.
(ZH) 本发明提供了由通式(Ⅰ)或(Ⅱ)表示7-(取代氨基)-3,4-二氢嘧啶[4,5-d]吡啶-(1氢)-酮类化合物及其在制备治疗肿瘤药物中的应用。经研究证实,它们能过抑制多种肿瘤细胞增殖,可用于靶向抑制表皮生长因子受体激酶(EGFR),尤其有效抑制EGFR(T790M)突变株的单点突变或多点突变癌细胞。因此可作为EGFR抑制剂用于抗癌药物的使用,有较大的应用价值。
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, 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, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (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, ML, MR, NE, SN, TD, TG)
Publication Language: Chinese (ZH)
Filing Language: Chinese (ZH)
Also published as:
CA2838885EP2746283US20140296216AU2011370586