2.
    发明专利
    未知

    公开(公告)号:NO323233B1

    公开(公告)日:2007-02-05

    申请号:NO20013709

    申请日:2001-07-27

    Abstract: 1-(3,5-bis-(Trifluoromethyl)-benzoyl)-2-(1H-indol-3-ylmethyl)-4-((5-am inomethyl-2H-1,2,3-triazol-4-yl)-methyl)-piperazines (I) are new. Triazole derivatives of formula (I) and their acid addition salts are new. R1 = H or alkyl; R2 = alkyl; dialkylaminoalkyl, alkoxycarbonylalkyl; 5-6 membered cycloalkyl (or its heterocyclic analog) optionally substituted by 1 or 2 alkyl; phenylalkyl (or its heterocyclic analog), optionally substituted in the ring by 1 or 2 of halo, alkyl and/or alkoxy and optionally substituted in the alkyl chain by 1 or 2 of alkyl or spiro-4-5C alkylene; or phenylalkoxy, optionally substituted in the ring by 1 or 2 of halo, alkyl and/or alkoxy; R3 = alkyl; alkoxycarbonylalkyl; or 5-6 membered cycloalkyl (or its heterocyclic analog) optionally substituted by 1 or 2 alkyl; or NR2R3 = cyclic amino of formula (a); or a pyrrolidine ring substituted by a 4C alkylene chain bonded to two adjacent C; A = N, O, CH2 or CH; n = 1-3; R4 = H, alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl or dialkylaminoalkyl; phenylalkyl (or its heterocyclic analog), optionally substituted in the ring by 1 or 2 of halo, alkyl and/or alkoxy and optionally substituted in the alkyl chain by 1 or 2 alkyl; 5-6 membered cycloalkyl (or its heterocyclic analog); or 5-6 membered cycloalkyl-alkyl (or its heterocyclic analog) ; R5 = H, alkyl or alkoxyalkyl; or R4 + R5 = spiro-ethylenedioxy, 3-4C alkylene bonded to two adjacent C or a fused benzene ring; all alkyl moieties are lower, i.e. have 1-4C. Independent claims are included for: (i) the preparation of (I); and (ii) new azide intermediates of formula (IV).

    6.
    发明专利
    未知

    公开(公告)号:PT1176144E

    公开(公告)日:2003-11-28

    申请号:PT01117433

    申请日:2001-07-19

    Abstract: 1-(3,5-bis-(Trifluoromethyl)-benzoyl)-2-(1H-indol-3-ylmethyl)-4-((5-am inomethyl-2H-1,2,3-triazol-4-yl)-methyl)-piperazines (I) are new. Triazole derivatives of formula (I) and their acid addition salts are new. R1 = H or alkyl; R2 = alkyl; dialkylaminoalkyl, alkoxycarbonylalkyl; 5-6 membered cycloalkyl (or its heterocyclic analog) optionally substituted by 1 or 2 alkyl; phenylalkyl (or its heterocyclic analog), optionally substituted in the ring by 1 or 2 of halo, alkyl and/or alkoxy and optionally substituted in the alkyl chain by 1 or 2 of alkyl or spiro-4-5C alkylene; or phenylalkoxy, optionally substituted in the ring by 1 or 2 of halo, alkyl and/or alkoxy; R3 = alkyl; alkoxycarbonylalkyl; or 5-6 membered cycloalkyl (or its heterocyclic analog) optionally substituted by 1 or 2 alkyl; or NR2R3 = cyclic amino of formula (a); or a pyrrolidine ring substituted by a 4C alkylene chain bonded to two adjacent C; A = N, O, CH2 or CH; n = 1-3; R4 = H, alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl or dialkylaminoalkyl; phenylalkyl (or its heterocyclic analog), optionally substituted in the ring by 1 or 2 of halo, alkyl and/or alkoxy and optionally substituted in the alkyl chain by 1 or 2 alkyl; 5-6 membered cycloalkyl (or its heterocyclic analog); or 5-6 membered cycloalkyl-alkyl (or its heterocyclic analog) ; R5 = H, alkyl or alkoxyalkyl; or R4 + R5 = spiro-ethylenedioxy, 3-4C alkylene bonded to two adjacent C or a fused benzene ring; all alkyl moieties are lower, i.e. have 1-4C. Independent claims are included for: (i) the preparation of (I); and (ii) new azide intermediates of formula (IV).

    DERIVATIVES OF N-TRIAZOLYLMETHYLPIPERAZINE AS NEUROKININE RECEPTOR-ANTAGONISTS, PREPARATION THEREOF AND MEDICAMENTS

    公开(公告)号:SK7572001A3

    公开(公告)日:2002-02-05

    申请号:SK7572001

    申请日:2001-06-01

    Abstract: 1-(3,5-bis-(Trifluoromethyl)-benzoyl)-2-(1H-indol-3-ylmethyl)-4-((5-am inomethyl-2H-1,2,3-triazol-4-yl)-methyl)-piperazines (I) are new. Triazole derivatives of formula (I) and their acid addition salts are new. R1 = H or alkyl; R2 = alkyl; dialkylaminoalkyl, alkoxycarbonylalkyl; 5-6 membered cycloalkyl (or its heterocyclic analog) optionally substituted by 1 or 2 alkyl; phenylalkyl (or its heterocyclic analog), optionally substituted in the ring by 1 or 2 of halo, alkyl and/or alkoxy and optionally substituted in the alkyl chain by 1 or 2 of alkyl or spiro-4-5C alkylene; or phenylalkoxy, optionally substituted in the ring by 1 or 2 of halo, alkyl and/or alkoxy; R3 = alkyl; alkoxycarbonylalkyl; or 5-6 membered cycloalkyl (or its heterocyclic analog) optionally substituted by 1 or 2 alkyl; or NR2R3 = cyclic amino of formula (a); or a pyrrolidine ring substituted by a 4C alkylene chain bonded to two adjacent C; A = N, O, CH2 or CH; n = 1-3; R4 = H, alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl or dialkylaminoalkyl; phenylalkyl (or its heterocyclic analog), optionally substituted in the ring by 1 or 2 of halo, alkyl and/or alkoxy and optionally substituted in the alkyl chain by 1 or 2 alkyl; 5-6 membered cycloalkyl (or its heterocyclic analog); or 5-6 membered cycloalkyl-alkyl (or its heterocyclic analog) ; R5 = H, alkyl or alkoxyalkyl; or R4 + R5 = spiro-ethylenedioxy, 3-4C alkylene bonded to two adjacent C or a fused benzene ring; all alkyl moieties are lower, i.e. have 1-4C. Independent claims are included for: (i) the preparation of (I); and (ii) new azide intermediates of formula (IV).

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