New heterocyclic substd. piperazine derivs

Pyrrolidinyl-, piperidinyl- and hexamethyleneimino-substd. piperazine derivs. (I) and their tautomers, stereoisomers (including mixtures) and salts are new. Ra = 3-pyrrolidinyl, 3- or 4-piperidinyl or 3- or 4- hexamethyleneiminyl opt. monosubstd. by 1-5C alkyl or aryl-1-3C alkyl (opt. monosubstd. on...

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Hauptverfasser: GUTH, BRIAN., 88447 WARTHAUSEN, DE, HIMMELSBACH, FRANK. DR., 88441 MITTELBIBERACH, DE, LINZ, GUENTER. DR., 88441 MITTELBIBERACH, DE, PIEPER, HELMUT. DR., 88400 BIBERACH, DE, WEISENBERGER, JOHANNES. DR., 88400 BIBERACH, DE, AUSTEL, VOLKHARD, .. DR., 88400 BIBERACH, DE
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Sprache:eng ; ger
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Zusammenfassung:Pyrrolidinyl-, piperidinyl- and hexamethyleneimino-substd. piperazine derivs. (I) and their tautomers, stereoisomers (including mixtures) and salts are new. Ra = 3-pyrrolidinyl, 3- or 4-piperidinyl or 3- or 4- hexamethyleneiminyl opt. monosubstd. by 1-5C alkyl or aryl-1-3C alkyl (opt. monosubstd. on or in alkyl part by COOH, 1-3C alkoxycarbonyl, CONH2, CONH(1-3C alkyl), CON(1-3C alkyl)2, vinyl or ethynyl); or, when this substit. is not on a C atom alpha to N, by OH, 1-3C alkoxy, NH2, NH(1-3C alkyl) or N(1-3C alkyl)2; or 1-6C alkanoyl; benzoyl; allyloxycarbonyl; 1-5C alkoxycarbonyl; or phenyl-1-3C alkoxycarbonyl; Rb, Rc = H; 1-5C alkyl; aryl; or aryl-1-5C alkyl; or together with the ethylene bridge between them form o-phenylene; and the piperazinylene gp. in (I) can contain 1 or 2 CO gps. in place of 1 or 2 CH2 gps.; Y1 = -A1-; -CO-; -CO-CO-; -A1-CO-; -CO-A1-; -SO2-A2-; -A2-SO2-; -CO-A1-CO-; -CO-NR1-CO-; -CO-NR1-A2-; -CO-NR1-A2-CO-; -CO-A2-NR1-CO-; -CO-A2-O-; or -CO-A2-NR1; R1 = H; 1-5C alkyl; aryl; or aryl-1-3C alkyl; A1 = 1-5C n-alkylene opt. monosubstd. by 1-5C alkyl, cyclohexyl-1-3C alkyl, aryl, aryl-1-3C alkyl or, when not alpha to a N atom, R1O; A2 = 1-4C n-alkylene opt. monosubstd. by 1-5C alkyl, aryl or aryl-1-3C alkyl; Y2= phenylene; cyclohexylene; pyridinylene; 3- or 4- piperidinylene or 1,4-piperazinylene opt. contg. 1 CO gp. in place of 1 CH2 gp. adjacent to a N atom, and in the case of 4-piperidinylene opt. 4-substd. by R1O (N, O or O,O acetal or N, O or N,N bond must not be formed in linkage with Y1 or Y3); 1,4-ketopiperazinylene opt. monosubstd. alpha to CO gp. by 1-5C alkyl (opt. substd. by phenyl, R1O-phenyl, 1-3C alkoxycarbonyl or COOH); -NR1-B- linked to Y1 via the N atom; or -O-B- linked to Y1 via the O atom; B = phenylene; cyclohexylene; pyridinylene; or piperidinylene linked via the 3- or 4-position with the NR1 or O of Y2 and opt contg. 1 CO gp. in place of 1 CH2 gp. adjacent to a N atom; Y3 = -CO-; -A2-CO-; -CH2-CH(NHR2)-CO-; -NR2-A3-CO-; -CH2-NR2-A3-CO-; -O-A3-CO-; -CO-A3-CO-; or -CO-NR1-A3-CO-; A3 = 1-3C n-alkylene opt. monosubstd. by 1-5C alkyl, aryl, pyridyl or aryl-1-3C alkyl; R2 = H; 1-5C alkyl; aryl-1-3C alkyl; aryl; 1-5C alkoxycarbonyl; 1-5C alkylsulphonyl; aryl-1-3C alkylsulphonyl or arylsulphonyl; formyl opt. monosubstd. by 1-4C alkyl, aryl or aryl-1-3C alkyl; and -A2-CO-, -NR2-A3-CO- and -O-A3-CO- are linked with Y2 via A2, NR2 and O, respectively, and -NR2-A3-CO-, -CH2-NR2-A3-CO- and -O-A3-CO- cannot be linked with a N at