HENNEQUIN LAURENT FRANþOIS ANDRE,PLE PATRICK,STOKES ELAINE SOPHIE ELIZABETH,MCKERRECHER DARREN
申请号：
CZ20012889
公开号：
CZ303692B6
申请日:
2000.02.08
申请国别(地区):
CZ
年份:
2013
代理人:
摘要：
Chinazolinový derivát obecného vzorce II, kde kruh C prestavuje chinolyl, naftyl, benzodioxolyl, indazolyl, benzothiazolyl, dihydroindenyl, chromenyl, benzoxazinyl, dihydrobenzoxazinyl, indolyl, chinazolinyl, benzimidazolyl, tetrahydrochinolyl, karbazolyl, dihydroindolyl nebo 1H-pyrrolo[2,3-b]pyridyl. Chinazolinové deriváty podle vynálezu inhibují úcinky VEGF a tím snizují angiogenezi a/nebo propustnost cév u teplokrevných zivocichu. Popisuje se zpusob prípravy derivátu vzorce II, farmacetuické prostredky je obsahující a pouzití derivátu pro prípravu léku s antiangiogenními úcinky a/nebo s úcinky na snízení propustnosti cév nebo s protirakovinovými úcinky pro pouzití pri lécbe rady stavu, vcetne rakoviny a revmatické artritidy.In the present invention, there is disclosed a quinazoline derivative of the general formula II in which the ring C represents quinolyl, naphthyl, benzodioxolyl, indazolyl, benzothiazolyl, dihydroindenyl, chromenyl, benzoxazinyl, dihydrobenzoxazinyl, indolyl, quinazolinyl, benzimidazolyl, tetrahydroquinolyl, carbazolyl, dihydroindolyl or 1H-pyrrolo[2,3-b]pyridyl. The quinazoline derivatives of the present invention inhibit the effects of VEGF reducing thus angiogenesis and/or vascular permeability effect in warm-blooded animals. There is also disclosed a process for preparing the derivatives of the general formula II, pharmaceutical compositions in which they are comprised as well as the use of the derivatives in the preparation of medicaments exhibiting antiangiogenic activity and vascular permeability reducing effects or antineoplastic activity for use in the treatment of a number of disease states including cancer and rheumatoid arthritis.
