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תולדות n – אוקסיד ו/או די –n – אוקסיד של מייצבי/מאפנני קולטן דופאמין המציגות פרופילים משופרים של תופעות לוואי של הלב וכלי הדם
专利权人:
IVAX INTERNATIONAL GMBH;NSAB FILIAL AF NEUROSEARCH SWEDEN AB SVERIGE
发明人:
申请号:
IL20140109
公开号:
IL201401A
申请日:
2009.10.11
申请国别(地区):
IL
年份:
2015
代理人:
摘要:
A compound having the general formula wherein A is selected from the group consisting of to the formation of a compound of the general formula (1) and a compound of the general formula (2) respectively, and pharmaceutically acceptable salts thereof, wherein R1 is a member selected from the group consisting of CF3, OSO2CF3, OSO2CH3, SOR4, SO2R4, COR4, CN, OR4, NO2, CONHR4, 3-thiophene, 2-thiophene, 3-furane, 2-furane, F, Cl, Br and I, wherein R4 is as defined below; R2 is a member selected from the group consisting of H, F, Cl, Br, I, CN, CF3, CH3, OCH3, OH, NH2, SOmCF3, O(CH2)mCF3, SO2N(R4)2, CH═NOR4, COCOOR4, COCOON(R4)2, (C1-C8)alkyl, (C3-C8)cykloalkyl, CH2OR4, CH2(R4)2, NR4SO2CF3, NO2, at phenyl at positions 2, 4, 5 or 6, wherein x and R4 are as defined below; R3 is a member selected from the group consisting of hydrogen, CF3, CH2CF3, (C1-C8)alkyl, (C3-C8)cykloalkyl, (C4-C9)cycloalkylmethyl, (C2-C8)alkenyl, (C2-C8)alkynyl, 3,3,3-tri-fluoropropyl, 4,4,4-trifluorobutyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, phenylethyl, 2-thiopheneethyl and 3-thiopheneethyl; R4 is a member selected from the group consisting of hydrogen, CF3, CH2CF3, (C1-C8)alkyl, (C3-C8)cycloalkyl, (C4-C9)cycloalkylmethyl, (C2-C8)alkenyl, (C2-C8)alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, 2-tetrahydrofurane and 3-tetrahydrofurane; X is selected from the group consisting of N and sp3-hybridized C; Y is selected from the group consisting of O and, when R3 represents H, OH; Z is selected from the group consisting of H and OH when X is sp3-hybridized C or Z represents O or an electronic lone-pair when X is N; the dashed line represents a bond when X is sp2-hybridized C or is absent when X is N; m is an integer 1 or 2; n is an integer 1-3; provided that when n in Formula 1 is 2, R1 is SO2CH3 and R2 is H R3 does not represent n-propyl. The invention also relates to a pharmaceutical preparation containing said compound, the use of said compound for the manufacture of a pharmaceutical com
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