DZHORZH DON M.,VAN LU,LI BITSIN',EHRIKSSON ANNA M.,EHNSELL GREHKHEM K.,ДЖОРЖ Дон М.,ВАН Лу,LI BITSIN,ЛИ Бицинь,ЭРИКССОН Анна М.,ЭНСЕЛЛ Грэхем К.
申请号:
RU2010116182
公开号:
RU2481332C2
申请日:
2008.09.25
申请国别(地区):
RU
年份:
2013
代理人:
摘要:
FIELD: medicine, pharmaceutics.SUBSTANCE: present invention refers to new compounds of formula (I)or to its stereoisomers, or to a pharmaceutically acceptable salt, wherein Rrepresents H or (C-C)alkyl; Ris specified in an optionally substituted group consisting of -(CH)-aryl, -CH(CH)-aryl, -(CH)-arylaryl, -(CH)-arylheteroaryl, -(CH)-(C-C) cycloalkyl, -(CH)-heteroaryl, -(CH)-heterocyclyl and -(C-C) cycloalkylaryl; or Rand Rtaken together with a nitrogen atom form 2,3-dihydro-1H-isoindolyl, decahydroisoquinolinyl, optionally substituted piperidinyl or optionally substituted pyrrolidinyl; Y is specified in an an optionally substituted group consisting of 5,6,7,8-tetrahydro[1,6]naphthyridinyl, -NH-(CH)-heterocyclyl, wherein NH is attached to carbonyl, and -heterocyclylaryl, wherein heterocyclyl is attached to carbonyl; and n is equal to 0, 1 or 2; wherein each heterocyclyl represents an independent non-aromatic ring system containing 3 to 12 ring atoms, and at least one ring atom specified in a group consisting of nitrogen, oxygen and sulphur; wherein each heteroaryl represents an independent non-aromatic ring system containing 3 to 12 ring atoms and at least one ring atom specified in a group consisting of nitrogen, oxygen and sulphur; and wherein the optional substitutes are independently specified in a group consisting of C-C-alkyl, C-C-alkoxy, halogen, CN, CF, OCF, NH, NH(CH), N(CH), hydroxy, cyclohexyl, phenyl, pyrrolidinyl, -C(O)-piperidinyl, -N(H)-C(O)-C-C-alkyl and N(H)-S(O)-C-C-alkyl. The invention also describes a pharmaceutical composition having chemokine receptor antagonist activity and a method of treating such diseases, such as rheumatoid arthritis, psoriasis, lupus, etc.EFFECT: there are prepared and described new chemical compounds that can be used as chemokine receptor antagonists and, as such, may be used in treating certain pathological conditions and diseases, particularly inflammatory pathological conditions and diseases and proliferative disorders