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1. CN102076695 - Imidazoquinazoline derivatives as anagrelide analogues for the treatment of myeloprolific diseases and thrombotic diseases

Office
China
Application Number 200980125158.9
Application Date 13.05.2009
Publication Number 102076695
Publication Date 25.05.2011
Publication Kind A
IPC
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/519
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 7/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
CPC
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61P 7/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
A61P 7/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
A61P 9/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
Applicants Shire LLC
夏尔有限责任公司
Inventors Golding Bernard
伯纳德·戈尔丁
Franklin Richard
理查德·富兰克林
Macleod Angus
安格斯·马克莱奥德
Agents wang dazuo hong xin
北京英赛嘉华知识产权代理有限责任公司 11204
北京英赛嘉华知识产权代理有限责任公司 11204
Priority Data 0808944.3 16.05.2008 GB
Title
(EN) Imidazoquinazoline derivatives as anagrelide analogues for the treatment of myeloprolific diseases and thrombotic diseases
(ZH) 用于治疗骨髓增生疾病和血栓性疾病的作为阿那格雷类似物的咪唑并喹唑啉衍生物
Abstract
(EN) This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1, and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.
(ZH)

本发明涉及发现选择性血小板减少剂阿那格雷的取代的类似物,其具有降低的心血管副作用潜在性,因此应该在骨髓增生性疾病的治疗中带来改善的患者顺应性和安全性。更具体地,本发明涉及某些咪唑并喹唑啉衍生物,其具有下面示出的通式,其中取代基具有权利要求1中所定义的含义,并且所述衍生物具有在人中作为血小板减少剂的功用。本发明的化合物通过抑制巨核细胞生成、并因此抑制血小板的形成而发挥作用。