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PICOLINAMIDE AND PYRIMIDINE-4-CARBOXAMIDE COMPOUNDS, METHOD OF OBTAINING THEREOF AND THEREOF-CONTAINING PHARMACEUTICAL COMPOSITION
专利权人:
LTD.;SK KEMIKALZ KO.
发明人:
RIU Dze Kho (KR),РИУ Дзе Хо (KR),KIM Shin Ae (KR),КИМ Шин Ае (KR),RIU Keun Kho (KR),РИУ Кеун Хо (KR),KIM Dzae Sun (KR),КИМ Дзае Сун (KR),KIM Nam Kho (KR),КИМ Нам Хо (KR),KhAN Khie Jang (KR),ХАН Хие Ян,RIU DZE KHO,РИУ Дзе Хо,KIM SHIN AE,КИМ Шин Ае,RIU KEUN KHO,РИУ Кеун Хо,KIM DZAE SUN,КИМ Дзае Сун,KIM NAM KHO,КИМ Нам Хо,KHAN KHIE JANG,ХАН Хие Янг,KIM JONG KHIUK,КИМ Йонг Хиук,JOUN VON-NO,ЙОУН Вон-Но
申请号:
RU2012152639/04
公开号:
RU0002566827C2
申请日:
2011.05.04
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
FIELD: medicine, pharmaceutics.SUBSTANCE: in formula 1 X represents N or CR, and Y represents N or CH on condition that X and Y are not simultaneously carbon; Z represents N or CH; R1 and R2 represent independently hydrogen, (C3-C10)cycloalkyl, norbornyl, adamantyl or noradamantyl, or R1 and R2 can be bound with each other together with nitrogen atoms, to which they are bound, with the formation of (C5-C10) saturated or unsaturated heterocycle or condensed heterocycle, on condition that R1 and R2 are not simultaneously hydrogen; L represents a single bond, -CO-, -SO2-, -(CR21R22)-(CH2)c- (c represents an integer number 0-5), , -CO(CR21R22)d- (d represents an integer number 1-6), (C3-C10)cycloalkylene, (C6-C20)arylene or 5-6-membered heteroarylene, including one or two heteroatoms, selected from N; R21 and R22 represent independently hydrogen or (C1-C10)alkyl, R represents hydrogen or hydroxyl; R4 and R5 independently represent hydrogen or (C1-C10)alkyl, or R4 and R5, bound together form a 6-membered unsaturated carbocycle; R6 and R7 represent independently hydrogen, (C1-C10)alkyl or halogen; R31-R38, R41-R43 and R46 represent independently hydrogen or (C1-C10)alkyl; and m and n independently represent an integer number 0-3 on condition that m+n represent an integer number 2 or larger. Values of radical R3 and additional substituents of cyclic groups R1-R3, L are given in the invention formula. The invention also relates to pharmaceutical composition, containing the said compounds, and to the 11β-HSD1 inhibitor..EFFECT: invention relates to amide compounds of structural formula 1, which possess inhibiting activity with respect to 11β-HSD1 enzyme.9 cl, 24 tbl, 296 exИзобретение относится к амидным соединениям структурной формулы 1, которые обладают ингибирующей активностью в отношении 11β-HSD1 фермента. В формуле 1 X представляет N или CR, и Y представляет N или СН при условии, что X и Y не являются в одно и то же время углеродом; Z представляет N или СН; R1 и R2 пр
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