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1. (WO2013152683) BICYCLE SUBSTITUTED PYRAZOLONEAZO DERIVATIVES AND PREPARATION METHOD AND USE THEREOF
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2013/152683 International Application No.: PCT/CN2013/073550
Publication Date: 17.10.2013 International Filing Date: 01.04.2013
IPC:
C07D 231/48 (2006.01) ,C07D 405/12 (2006.01) ,C07D 403/12 (2006.01) ,C07D 417/12 (2006.01) ,A61K 31/4152 (2006.01) ,A61K 31/4155 (2006.01) ,A61K 31/427 (2006.01) ,A61P 7/00 (2006.01) ,A61P 7/06 (2006.01) ,A61P 7/04 (2006.01) ,A61P 35/02 (2006.01) ,C12N 5/078 (2010.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
231
Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02
not condensed with other rings
10
having two or three double bonds between ring members or between ring members and non-ring members
14
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
44
Oxygen and nitrogen or sulfur and nitrogen atoms
46
Oxygen atom in position 3 or 5 and nitrogen atom in position 4
48
with hydrocarbon radicals attached to said nitrogen atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
415
1,2-Diazoles
4152
having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
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
415
1,2-Diazoles
4155
not condensed and 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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425
Thiazoles
427
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
7
Drugs for disorders of the blood or the extracellular fluid
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
06
Antianaemics
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
04
Antihaemorrhagics; Procoagulants; Haemostatatic agents; Antifibrinolytic 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
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
N
MICRO-ORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICRO-ORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
5
Undifferentiated human, animal or plant cells, e.g. cell lines; Tissues; Cultivation or maintenance thereof; Culture media therefor
07
Animal cells or tissues
071
Vertebrate cells or tissues, e.g. human cells or tissues
078
Cells from blood or from the immune system
Applicants:
齐鲁制药有限公司 QILU PHARMACEUTICAL CO., LTD. [CN/CN]; 中国山东省济南市 高新区新泺大街317号 No. 317, Xinluo Street, High Technical Zone Jinan, Shandong 250100, CN
Inventors:
范传文 FAN, Chuanwen; CN
张龙 ZHANG, Long; CN
周豪杰 ZHOU, Haojie; CN
赵洪令 ZHAO, Hongling; CN
杨莹莹 YANG, Yingying; CN
Agent:
中国国际贸易促进委员会专利商标事务所 CCPIT PATENT AND TRADEMARK LAW OFFICE; 中国北京市 西城区阜成门外大街2号万通新世界广场8层 8th Floor, Vantone New World Plaza 2 Fuchengmenwai Street, Xicheng District Beijing 100037, CN
Priority Data:
201210103270.611.04.2012CN
Title (EN) BICYCLE SUBSTITUTED PYRAZOLONEAZO DERIVATIVES AND PREPARATION METHOD AND USE THEREOF
(FR) DÉRIVÉS PYRAZOLONEAZO BICYCLIQUES SUBSTITUÉS, LEUR PROCÉDÉ DE PRÉPARATION ET UTILISATION
(ZH) 双环取代吡唑酮偶氮类衍生物、其制备方法及用途
Abstract:
(EN) The present invention is in the medical and chemical field, and relates to a class of bicycle substituted pyrazoloneazo derivatives, the preparation method and a pharmaceutical composition and use thereof. In particular, the present invention relates to a compound shown as formula (I) and a pharmaceutically acceptable salt and solvate thereof. The present invention also relates to the preparation method of the compound of formula (I), a pharmaceutical composition comprising same and the use thereof in preparing medicine. The compound of formula (I) of the present invention is an effective TPO agonist and a good drug for treating thrombocytopenia.
(FR) La présente invention se situe dans le domaine médical et chimique, et elle concerne une classe de dérivés pyrazoloneazo bicycliques substitués, leur procédé de préparation, une composition pharmaceutique et leur utilisation. En particulier, la présente invention concerne un composé représenté par la formule I et l'un de ses sels et solvates pharmaceutiquement acceptables. La présente invention concerne également le procédé de préparation du composé de formule (I), une composition pharmaceutique renfermant ce dernier et son utilisation dans la préparation d'un médicament. Le composé de formule I de la présente invention est un agoniste efficace de la TPO et un bon médicament pour le traitement de la thrombocytopénie.
(ZH) 本发明属于医药化工领域,涉及一类双环取代吡唑酮偶氮类衍生物、其制备方法、其药物组合物和用途。具体地说,本发明涉及式I所示化合物或其药学上可接受的盐或溶剂合物。本发明还涉及式I化合物的制备方法,包括它的药物组合物以及它们的制药用途。本发明的式I化合物是有效的TPO激动剂,是良好的治疗血小板减少症药物。
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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, 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, PA, 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 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, ML, MR, NE, SN, TD, TG)
Publication Language: Chinese (ZH)
Filing Language: Chinese (ZH)