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СОЕДИНЕНИЯ ДИОКСИН- И ОКСАЗИН[2,3-D]ПИРИМИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ ФОСФОИНОЗИТИД-3-КИНАЗЫ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ
专利权人:
Ф. ХОФФМАНН-ЛЯ РОШ АГ (CH)
发明人:
ХИЛД Роберт Эндрю (GB),МАКЛИН Невиль Джэймс (GB)
申请号:
RU2015108410
公开号:
RU2015108410A
申请日:
2013.08.29
申请国别(地区):
RU
年份:
2016
代理人:
摘要:
1. A compound of formula Ia: and stereoisomers, geometric isomers, tautomers and pharmaceutically acceptable salts of said compound, wherein R independently selected from H, = O, S-alkyl, S-alkenyl, S-alkynyl and C-Skarbotsiklila, wherein said alkyl and carbocyclyl optionally substituted with one or more groups independently selected from F, Cl, Br, I, -CH, -CHCH, CH (CH), -CHCH (CH), -CHCH, -CHCN, -CN, -CF, - CHOH, -SON, -CONH, -CONH (CH), -CON (CH), -NO, -NH, -NHCH, -N (CH), -NHCOCH, -OH, = O, -OCH, -OCHCH, -OCH (CH), -SH, -NHC (= O) NHCH, -NHC (= O) NHCHCH), -NHC (= O) NHCH (CH), -NHS (O) CH, -N (CH) C (= O) OC (CH), -S (O) CH, benzyl, benzyloxy, cyclopropyl, mo Folin, morpholinomethyl and 4-methylpiperazin-1-yl or a group of the group R or Robrazuyut spiro group, a 3-6-membered carbocyclic or heterocyclic ring Rvybirayut Sarila from C-C-C-and Sgeterotsiklila Cgeteroarila, each of which is optionally substituted by one or more groups independently selected from F, Cl, Br, I, -CH, -CHCH, CH (CH), -CHCH (CH), -CHCH, -CHCN, -CN, -CF, -CHOH, -SON, -CONH, -CONH (CH), - CON (CH), -NO, -NH, -NHCH, -N (CH), -NHCOCH, -OH, -OCH, -OCHCH, -OCH (CH), -SH, -NHC (= O) NHCH, - NHC (= O) NHCHCH, -NHC (= O) NHCH (CH), -NHS (O) CH, -N (CH) C (= O) OC (CH), -S (O) CH, benzyl, benzyloxy , morpholinyl, morpholinomethyl and 4-methylpiperazin-1-yl 2. A compound according to claim 1, characterized in that are independently selected from H, -CH, -CHCH, -C (CH), -CHOH, -SNSNON, -C (CH) OH -SNOSN, -CN, -CHF,. - CHFi -CF.3. A compound according to Claim. 1, characterized in that are independently selected from H, -SNi tsiklopropila.4. A compound according to Claim. 1, characterized in that are independently selected from H, -CH, -C (CH), -CHOH, -CF, -CHF and tsiklopropila.5. A compound according to claim. 4, wherein each R is -SN.6. A compound according to Claim. 1, characterized in that the two Robrazuyut = O or tsiklopropil.7. A compound according to claim 1, characterized in that R is phe
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