Abstract:
The invention relates to a group of hydronopol derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these novel hydronopol derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved. The invention relates to compounds of the general formula (1) wherein the symbols have the meanings as given in the description.
Abstract:
The invention relates to compounds of general formula (I), wherein the meaning of R1, R2, R3, R4, R5 and R6 is given in a description, to a method for producing said compounds and to intermediate products thereof. Drugs containing the inventive compounds of formula (1) are also disclosed. I
Abstract:
The invention relates to a group of hydronopol derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these novel hydronopol derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved. The invention relates to compounds of the general formula (1) wherein the symbols have the meanings as given in the description.
Abstract:
The invention relates to a group of hydronopol derivatives which are agonist s on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these novel hydronopol derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved. The invention relates to compounds of the general formula (1) wherein the symbols have the meanings as given in the descriptio n.
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).
Abstract:
7-Alkyl-3-(substituted phenyl)-9,9-(dialkyl or alkylene)-3,7-diazabicyclo (3.3.1) nonane derivatives (I) are new. Diazabicyclononane derivatives of formula (I) and their acid addition salts are new. R1 = 1-6C alkyl or 4-7C cycloalkylalkyl; R2, R3 = 1-4C alkyl; or R2 + R3 = 3-6C alkylene; and R4 = phenyl (monosubstituted in the ortho- or para-position by NO2, CN or 2-5C alkanoyl) or 2,4-dinitrophenyl. An Independent claim is also included for the preparation of (I).
Abstract:
The use of 4-chloro-5-((4,5-dihydro-1H-imidazol-2-yl)- amino)-6-methoxypyrimidine of formula (I) or its acid addn. salts is claimed for the prepn. of pharmaceutical compsns. for the treatment of hyperglycaemia. Also claimed in the prepn. of such as compsn. by converting an antihyperglycaemically active amt. of (I) or its salt into a suitable dosage form, in combination with conventional auxiliaries.
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).
Abstract:
The use of 4-chloro-5-((4,5-dihydro-1H-imidazol-2-yl)- amino)-6-methoxypyrimidine of formula (I) or its acid addn. salts is claimed for the prepn. of pharmaceutical compsns. for the treatment of hyperglycaemia. Also claimed in the prepn. of such as compsn. by converting an antihyperglycaemically active amt. of (I) or its salt into a suitable dosage form, in combination with conventional auxiliaries.