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Relevant academic research and scientific papers

Heterocyclic analgesic compounds and methods of use thereof

One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.

Heterocyclic analgesic compounds and methods of use thereof

One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.

Heterocyclic analgesic compounds and methods of use thereof

One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.

Piperazine and piperidine compounds

The invention relates to a group of new piperazine and piperidine compounds having interesting pharmacological properties. It has been found that compounds of formula (a) wherein A represents a heterocyclic group of 5-7 ring atoms wherein 1-3 heteroatoms from the group O, N and S are present; R1is hydrogen or fluoro; R2is C1-4-alkyl, C1-4-alkoxy or an oxo group, and p is 0, 1 or 2; Z represents carbon or nitrogen, and the dotted line is a single bond when Z is nitrogen, and a single or double bond when Z is carbon; R3and R4independently are hydrogen or C1-4-alkyl; n has the value 1 or 2; R5is halogen, hydroxy, C1-4-alkoxy or C1-4-alkyl, and q is 0, 1, 2 or 3; Y is phenyl, furanyl or thienyl, which groups may be substituted with 1-3 substituents of the group hydroxy, halogen, C1-4-alkoxy, C1-4-alkyl, cyano, aminocarbonyl, mono- or di-C1-4-alkylaminocarbonyl; and salts thereof show high affinity for both the dopamine D2and serotonin 5-HT1Areceptors.

Acylamino-substituted hetrazepines

A hetrazepine of the formula given below and a pharmaceutical composition comprising a therapeutically effective amount of the hetrazepine and a pharmaceutically acceptable inert carrier are disclosed and are useful in treating disease in a warm-blooded animal induced by endogenously formed PAF; STR1 wherein the substituents are defined herein.

Hetrazepine compounds which have useful pharmaceutical utility

The invention relates to new hetrazepines of general formula STR1 wherein A, Z, n, X, Y, R 1, R 2, R 3 and R 4 have the meanings given in the specification.The new compounds are intended for use in treating pathological conditions and diseases in which PAF (platelet activating factor) is implicated.

Aryl-fused and hetaryl-fused-2,4-diazepine and 2,4-diazocine antiarrhythmic agents

Aryl-fused- and hetaryl-fused-2,4-diazepines of formula XXXVI, benzodiazocines of formula XXX, benzodiazepines of formula II STR1 δ-aminoamides of formula III and aryldimethanamines of formula XXXVII STR2 wherein A is an aryl or hetaryl ring; R1 is hydrogen, alkyl, aryl or hetaryl; R2 is hydrogen, alkyl, substituted alkyl, or aryl; R3 is alkyl, aryl, aralkyl or heteroatom substituted alkyl or aralkyl; R4 is hydrogen or alkyl; R5 is hydrogen, alkyl, aryl or hetaryl; R6 is hydrogen, alkyl, alkoxy, halogen or a fused benzene ring; R9 is hydrogen, alkyl, or substituted alkyl; and R10 is hydrogen, alkyl, or substituted alkyl. The invention further relates to processes for the preparation of, pharmaceutical compositions containing, and methods of treating cardiac arrhythmia with the compounds of formulas XXXVI, XXX, II, III, and XXXVII.

Thieno-traizolo-1,4-diazepino-2-carboxylic acid amides

The invention relates to new thieno-traizolo-1,4-diazepino-2-carboxylic acid amides of formula I STR1 wherein R 1 represents hydrogen, a C 1 -C 4 straight-chained or branched alkyl which can optionally be substituted by halogen, preferably Cl or Br, or by hydroxy, cyclopropyl, C 1 -C 3 alkoxy, preferably methoxy, or halogen, preferably chlorine or bromine;R 2 and R 3, each independently, represent hydrogen, a C 1 -C 4 straight-chained or branched alkyl, C 1 -C 4 hydroxyalkyl or the two groups R 2 and R 3 together with the nitrogen atom represent a 5-, 6- or 7-membered ring which optionally contains a nitrogen, oxygen or sulfur atom as a further heteroatom, the second nitrogen atom optionally being substituted by a C 1 -C 4 alkyl, preferably a methyl group;R 4 represents alpha-pyridyl or a phenyl in which the phenyl ring can be substituted preferably in the 2-position, by methyl, halogen, preferably chlorine or bromine, nitro or trifluoromethyl;n represents one of the numbers 0, 1, 2, 3, 4, 5, 6, 7 or 8; and novel intermediates therefor.The compounds of formula I are useful in the treatment of pathological conditions and diseases in which platelet activating factor is implicated.