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1. (WO2015043364) BENZOXAZOLEOXAZINE KETONE COMPOUND AS BLOOD COAGULATION FACTOR XA INHIBITOR
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2015/043364 International Application No.: PCT/CN2014/085844
Publication Date: 02.04.2015 International Filing Date: 03.09.2014
IPC:
C07D 519/00 (2006.01) ,C07D 498/14 (2006.01) ,C07D 513/04 (2006.01) ,A61K 31/5383 (2006.01) ,A61K 31/553 (2006.01) ,A61K 31/5386 (2006.01) ,A61K 31/541 (2006.01) ,A61K 31/542 (2006.01) ,A61P 7/02 (2006.01) ,A61P 9/10 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
519
Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/ or C07D455/257
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
12
in which the condensed system contains three hetero rings
14
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
513
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/, C07D477/232
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
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
55
having seven-membered rings, e.g. azelastine, pentylenetetrazole
553
having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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
5386
spiro-condensed or forming part of bridged 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
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
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
542
ortho- or peri-condensed with heterocyclic ring systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7
Drugs for disorders of the blood or the extracellular fluid
02
Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
10
for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Applicants:
华北制药集团新药研究开发有限责任公司 NORTH CHINA PHARMACEUTICAL NEW DRUG R & D CO., LTD. [CN/CN]; 中国河北省石家庄市 和平东路388号 388 HePing Dong Road Shijiazhuang, Hebei 050015, CN
Inventors:
高任龙 GAO, Renlong; CN
丁照中 DING, Charles Z.; CN
赖光华 LAI, Kwong Wah; CN
陈曙辉 CHEN, Shuihui; CN
颜小兵 YAN, Xiaobing; CN
段宝玲 DUAN, Baoling; CN
朱秀良 ZHU, Xiuliang; CN
路新华 LU, Xinhua; CN
胡军平 HU, Junping; CN
Agent:
北京戈程知识产权代理有限公司 GE CHENG & CO., LTD.; 中国北京市 东城区东长安街1号东方广场东三办公楼19层 Level 19, Tower E3, The Towers, Oriental Plaza No.1, East Chang An Avenue, Dongcheng District Beijing 100738, CN
Priority Data:
201310456006.529.09.2013CN
Title (EN) BENZOXAZOLEOXAZINE KETONE COMPOUND AS BLOOD COAGULATION FACTOR XA INHIBITOR
(FR) COMPOSÉ DE BENZOXAZOLÉOXAZINE CÉTONE COMME INHIBITEUR DU FACTEUR DE COAGULATION SANGUINE XA
(ZH) 作为凝血因子Xa抑制剂的苯并恶唑并恶嗪酮类化合物
Abstract:
(EN) The present invention relates to a novel compound of formula (I), or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof, wherein R1 represents a substituted or unsubstituted aryl or heteroaryl; R2 represents an optionally substituted 3-9 membered carbocyclic or heterocyclic ring, etc.; R3 represents H, etc.; A is selected from O, NH, N-CH3, S, SO, SO2 and CH2; and X, Y and Z are independently selected from CH, C-Br, C-Cl, C-F, C-I and N, respectively. The compound of the invention can be used as an anticoagulant for treating and preventing thrombotic disorders. The present invention meets the real needs for a selective and potent inhibitor of coagulation Xa by providing a potent inhibitor of blood coagulation factor Xa.
(FR) La présente invention concerne un nouveau composé de formule (I), ou son solvat, hydrate, tautomère ou sel pharmaceutiquement acceptable, où R1 représente un groupe aryle ou hétéroaryle substitué ou non substitué; R2 représente un anneau carbocyclique ou hétérocyclique à 3-9 chaînons facultativement substitué, etc.; R3 représente H, etc.; A est choisi parmi O, NH, N-CH3, S, SO, SO2 et CH2; et X, Y et Z sont choisis indépendamment parmi CH, C-Br, C-Cl, C-F, C-I et N, respectivement. Le composé de l'invention peut être utilisé comme anticoagulant pour traiter et prévenir les troubles thrombotiques. La présente invention répond aux besoins réels en inhibiteur puissant et sélectif du facteur de coagulation Xa en proposant un inhibiteur puissant du facteur de coagulation sanguine Xa.
(ZH) 本发明涉及新的式(I)化合物或其溶剂化物、水合物、互变异构体、或药学上可接受的盐,其中R1代表被取代或未被取代的芳基或杂芳基;R2代表任选被取代的3-9元碳环或杂环等;R3代表H等;A选自O、NH、N-CH3、S、SO、SO2和CH2;X、Y和Z分别独立地选自CH、C-Br、C-Cl、C-F、C-I和N。本发明的化合物可以作为治疗和预防血栓异常疾病的抗凝剂,本发明通过提供凝血因子Xa的强力抑制剂以满足针对凝血Xa的选择性和强力抑制剂的现实需求。
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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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, 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, 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)