BLEhJNI Dzheffri (US),БЛЭЙНИ Джеффри (US),GIBBONS Pol A. (US),ГИББОНС Пол А. (US),KhANAN Ehmili (US),ХАНАН Эмили (US),LISSIKATOS Dzhozef P. (US),ЛИССИКАТОС Джозеф П. (US),MAGNUSON Stiven R. (US),МАГНУ,BLEHJNI DZHEFFRI,БЛЭЙНИ Джеффри,GIBBONS POL A.,ГИББОНС Пол А.,KHANAN EHMILI,ХАНАН Эмили,LISSIKATOS DZHOZEF P.,ЛИССИКАТОС Джозеф П.,MAGNUSON STIVEN R.,МАГНУСОН Стивен Р.,PASTOR RICHARD,ПАСТОР Ричард,RO
申请号：
RU2011121876/04
公开号：
RU0002539568C2
申请日:
2009.11.02
申请国别(地区):
RU
年份:
2015
代理人:
摘要：
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to novel compounds of formula Ia, their stereoisomers or pharmaceutically acceptable salts, inhibiting JAK kinase activity. Compounds can be applied in treatment of inflammatory diseases, such as rheumatoid arthritis, psoriasis, contact dermatitis, in treatment of autoimmune diseases, such as lupus, multiple sclerosis, neurodegenerative diseases, such as Alzheimer's disease, etc. In formula Ia R1 represents H； R2 represents -OR4, -NR3R4- or -NR3S(O)2R4； R3 represents H or C1-C6alkyl, where said alkyl is optionally substituted with ORa； R4 represents H, C1-C6alkyl, -(C0-C5alkyl)(C3-C6cycloalkyl), -(C0-C5alkyl)(C4-C5heteroaryl), where heteroaryl contains 1-2 nitrogen atoms as heteroatoms, or -(C0-C5alkyl)(C6aryl), where said alkyl is optionally substituted with group R8 and said aryl, cycloalkyl and heteroaryl are optionally substituted with group R9； or R3 and R4, taken together with nitrogen atom, which they are bound to, form C3heterocyclyl, containing 1 nitrogen atom as heteroatom, optionally substituted with group R13； Z represents -NR5R6； R5 represents H； R6 represents H, C1-C10alkyl, -(C0-C5alkyl)(C4-C5heterocyclyl), where heterocyclyl contains oxygen atom as heteroatom, -(C0-C5alkyl)(C3-C8cycloalkyl), -(C0-C5alkyl)(C3-C5heteroaryl), where heteroaryl contains 1 nitrogen atom or 1 oxygen atom or contains 2 atoms, selected fromoxygen, nitrogen and sulphur, as heteroatoms, -(C0-C5alkyl)(C6aryl), where said alkyl is optionally substituted with group R10, and said aryl, cycloalkyl, heteroaryl and heterocyclyl are optionally substituted with group R11； R7 represents H； R8 and R10 each independently represents halogen or ORa； R9 independently represents -CN, -CF3, halogen, -C(O)ORa, -C(O)NRaRb, -(C0-C5alkyl)NRaRb, -(C0-C5alkyl)ORa, -(C0-C5alkyl)SRa, -O[C(Ra)2]1-3O-, C1-C3alkyl, optionally substituted with F, -(C0-C5alkyl)(C3-C6cycloalkyl), optionally substituted with group oxo or F, -(C0-C5alkyl)C3-C6heteroc
