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ИНГИБИТОРЫ КАТЕХОЛ-О-МЕТИЛТРАНСФЕРАЗЫ И ИХ ПРИМЕНЕНИЕ В ЛЕЧЕНИИ ПСИХИЧЕСКИХ РАССТРОЙСТВ
专利权人:
МЕРК ШАРП ЭНД ДОМЭ КОРП. (US)
发明人:
УОЛКЕНБЕРГ Скотт (US),ХАРРИСОН Скотт Т. (US),БЭРРОУ Джеймс К. (US),ЧЖАО Чжицзянь (US),МЕЛАМЕД Джеффри (US),КЕТТ Натан (US),ЗАРТМАН Эми (US)
申请号:
RU2012142171/04
公开号:
RU2012142171A
申请日:
2011.02.28
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
1. A compound of structural formula I and II: including its tautomers or pharmaceutically acceptable salts and individual enantiomers and diastereomers, wherein: A is hydrogen or C1-6 alkyl, wherein said alkyl is optionally substituted with 1 to 3 halogen, OH or Oalkyl groups, X is hydrogen, OH , halogen, C1-6 alkyl, OC-alkyl, NRR, (CH2) C2-C4ary, (CH2) C3-heterocyclyl, wherein said alkyl, aryl and heterocyclyl are optionally substituted with 1 to 3 R groups R3 is (CH2) C4ary or (CH2) C5-heterocyclyl wherein said aryl and heterocyclyl is optionally substituted with 1 to 3 R groups R and R are independently (CH) Caryl, wherein said aryl and heterocyclyl are optionally substituted with 1 to 3 R groups R and R together with the nitrogen atom to which they are attached form 5 to 10 membered ring which is optionally substituted with 1 to 3 halogen, OH, C2-6 alkenyl, (CH) C-heterocyclyl or (CH 2) -Caryl R 1 is C 1-6 alkyl, halogen, hydroxyl, C2-6 alkynyl, (CH) CF, OCHF, OCF, C cycloalkyl, O (CH 2) C 2 -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, NH (CH) C heterocyclyl, (CH (C1-C6) -Charyl, O (CH2) C4ary or O (CH2) C-heterocyclyl, wherein said alkyl, alkynyl, cycloalkyl, heterocyclyl and aryl are optionally substituted with 1 to 3 R groups R3 is C1-6 alkyl, OC1 alkyl, halogen, CHF, OCHF, N (R), CHOH, S (O) NRR, (CH) Caryl, (CH) C heterocyclyl, C (O) (CH) C heterocyclyl, NH (CH) C heterocyclyl, C (O) NHC cycloalkyl, OR, Cycloalkyl, (CH ) CF or CN, wherein said heterocyclyl is optionally substituted 1 or several C1-6 alkyl and n is 0-5.2. A compound according to claim 1, wherein R 1 is phenyl or pyridyl, both optionally substituted with 1 to 3 R 3 groups. The compound according to claim 2, where R 1 is optionally substituted phenyl. A compound according to claim 2, wherein R & lt 1 & gt is optionally substituted &
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