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CATECHOL-O-METHYL TRANSFERASE INHIBITORS AND THEIR APPLICATION FOR THE TREATMENT OF PSYCHOTIC DISORDERS
专利权人:
МЕРК ШАРП ЭНД ДОМЭ КОРП. (US)
发明人:
УОЛКЕНБЕРГ Скотт (US),БЭРРОУ Джеймс К. (US),ХАРРИСОН Скотт Т. (US),ТРОТТЕР Б. Уэсли (US),НАНДА Каусик К. (US),МЭНЛИ Питер Дж. (US),ЧЖАО Чжицзянь (US)
申请号:
RU2012142180/04
公开号:
RU2012142180A
申请日:
2011.02.28
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
1. The compound of structural formula I: including its tautomers or pharmaceutically acceptable salts and individual enantiomers and diastereomers, where: Y represents hydrogen, CN, C-alkynyl, (CH) C-heterocyclyl, (CH) C-aryl, and these alkynyl , heterocyclyl and aryl are optionally substituted with 1-3 R groups; X, X and R are independently hydrogen, halogen, CN, C-alkyl, C-alkynyl, (CH) C-aryl, (CH) C-heterocyclyl alkyl, heterocyclyl and aryl are optionally substituted with 1-3 R groups; R is H, OH, C-alkyl, N (CH), (CH) C-cycloalkyl, (CH) C-heterocyclyl, (CH) C-aryl, wherein said aryl and heterocyclyl are optionally substituted with 1-3 R groups; R is C-alkyl, halogen, hydroxyl, C1-6 alkynyl, (CH) CF, OCHF, OCF, C-cycloalkyl, NRC (O ) R, C (O) N (R), C (R) OR, C (O) R, NO, CN, N (R), (CH) C (O) OR, SOR, NHSOR, OR, (CH ) C-heterocyclyl, C (O) (CH) C-heterocyclyl, (CH) C-aryl or C (O) (CH) C-aryl, wherein said alkyl, alkynyl, cycloalkyl, heterocyclyl and aryl are optionally substituted 1 -3 R groups: R is C-alkyl, halogen, CHF, OCHF, -O-, N (R), CHOH, (CH) C-aryl, (CH) C-heterocyclyl, OR, C-cycloalkyl, (CH ) CF, or CN; and n is an integer from 0 to 5.2. The compound according to claim 1, where Y is (CH) C-aryl selected from the group consisting of phenyl and naphthyl, wherein said phenyl and naphthyl are optionally substituted with 1-3 R.3 groups. The compound of claim 1, wherein Y is (CH) C-heterocyclyl selected from the group consisting of quinolinyl, isoquinolinyl, thiazolyl, triazolyl, pyrrolyl, pyrrolidinyl, pyrazolyl, imidazolyl, and pyrimidinyl, each of which is optionally substituted with 1 -3 groups R.4. The compound according to claim 1, where Y is C-alkynyl, optionally substituted with 1-3 R.5 groups. The compound according to claim 1, where R represents, n1. Соединение структурной формулы I:включая его таутомеры или фармацевтически приемлемые соли и индивидуальные энантиомеры и диастереомеры, где:Y представляет собой водород, CN, C-алкинил, (CH)C-гетеро
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