摘要:
A compound having the formula ##STR1## wherein R.sup.1 is C.sub.1-6 -alkyl which may be branched or cyclic;R.sup.2 is C.sub.1-6 -alkyl which may be branched or cyclic; or wherein R.sup.1 and R.sup.2 together represent --(CH.sub.2).sub.n --, wherein n is 3, 4, 5.and a method of treating disorders of a mammal, including a human, responsive to the blockade of glutamic and aspartic acid receptors, with the same.
摘要:
A method of treatment with compounds having the formula ##STR1## R.sup.1 is hydrogen, C.sub.1-6 -alkyl which may be branched, C.sub.3-7 -cycloalkyl, benzyl, phenyl which may be substituted, acyl, hydroxy, C.sub.1-6 -alkoxy, CH.sub.2 CO.sub.2 R' wherein R' is hydrogen or C.sub.1-6 -alkyl which may be branched, CH.sub.2 CN, CH.sub.2 CONR.sup.IV R.sup.V wherein R.sup.IV and R.sup.V independently are hydrogen or C.sub.1-6 -alkyl, or CH.sub.2 C(.dbd.NOH)NH.sub.2 ; R.sup.2 is hydrogen, benzyl, C.sub.1-6 -alkyl which may be branched, or C.sub.3-7 -cycloalkyl; R.sup.4, R.sup.5, R.sup.6, R.sup.7 independently are hydrogen, C.sub.1-6 -alkyl which may be branched, phenyl, halogen, C.sub.1-6 -alkoxy, NO.sub.2, CN, CF.sub.3, OCF.sub.3, or SO.sub.2 NR"R'" wherein R" and R'" independently are hydrogen, aralkoxy, aralkyl, or C.sub.1-6 -alkyl; or R.sup.6 and R.sup.7 together form an additional 4 to 7 membered ring which may be aromatic or partial saturated and which may be substituted with halogen, NO.sub.2, CF.sub.3, CN, OCF.sub.3, SO.sub.2 NR" R"' wherein R" and R"' independently are hydrogen, aralkoxy, aralkyl, or C.sub.1-6 -alkyl, and R.sup.4 and R.sup.5 have the meanings set forth above, are disclosed, as well as pharmaceutical compositions thereof. Certain of the compounds are novel.The compounds and pharmaceutical compositions containing the compounds are useful in the treatment of central nervous system disorders and especially conditions sensitive to excitatory amino acids.
摘要:
New heterocyclic derivatives having the general formula: ##STR1## wherein X is ##STR2## or CO.sub.2 R' wherein R' is C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl, or C.sub.1-3 -alkoxymethyl, and--A-- is --(CH.sub.2).sub.n --Y--(CH.sub.2).sub.m --,wherein n and m are 0 or 1 and --Y-- is --O--, --S--, --CH.sub.2 --, or --NR"--, wherein R" is hydrogen or C.sub.1-6 -alkyl.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and nootropics and in human and animal health as anthelmintics, ecto- and endoparasiticides, insecticides and acaricides.
摘要:
New heterocyclic derivatives havingy the general formula: ##STR1## wherein ##STR2## wherein R' is C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl, or C.sub.1-3 -alkoxymethyl, and--A-- is --(CH.sub.2).sub.n --Y--(CH.sub.2).sub.m --,wherein n and m are O or 1 and --Y-- is --O--, --S--, --CH.sub.2 --, or --NR"--, wherein R" is hydrogen or C.sub.1-6 -alkyl.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and nootropics and in human and animal health as anthelmintics, ecto- and endoparasiticides, insecticides and acaricides.
摘要:
New heterocyclic compounds having the general formula ##STR1## wherein ##STR2## wherein R' is C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl or C.sub.1-6 -alkoxymethyl;R.sup.4 is C.sub.1-6 -alkyl;--S-- is ##STR3## and wherein R.sup.5 and R.sup.6 independently are hydrogen, C.sub.1-6 -alkyl, or aryl.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and in improving the cognitive function of the brain of mammals.
摘要:
Piperidine compounds having the formula ##STR1## wherein R.sup.1 is hydrogen, (C.sub.1-6 -alkoxyaryl)alkyl, diphenylmethozy-C.sub.1-6 -alkyl, C.sub.1-8 -alkyl, C.sub.4-10 -cycloalkylalkyl, phenoxy-C.sub.1-8 -alkyl, or C.sub.1-6 -alkoxy-C.sub.1-6 -alkyl; andR is ##STR2## or CH.dbd.NOR' wherein R' is C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl, C.sub.1-6 -alkoxy-C.sub.1-6 -alkyl, aryl-C.sub.0-6 -alkyl, which may optionally be substituted with one or more halogen and (.sub.1-5 -alkoxy, thienyl, or C.sub.4-7 -cycloalkylalkyl.The novel compounds are useful for the treatment of pain conditions and as neuroleptics.
摘要:
New heterocyclic compounds having the general formula ##STR1## wherein X is ##STR2## wherein R.sup.1 is C.sub.1-6 -alkyl, Cphd 3-7-cycloalkyl, phenyl, thienyl, or C.sub.1-3 -alkoxymethyl,R.sup.6 and R.sup.7 independently are hydrogen or halogen, and--A--is --N(R")--C(O)--, --N(R")--CH.sub.2 --, or ##STR3## wherein R" is hydrogen, C.sub.3.differential. -cycloalkyl, or C.sub.1-6 -alkyl The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and nootropics.
摘要:
The invention relates to a hydrochloride salt of (1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-[(methyloxy)methyl]-8-azabicyclo[3.2.1]octane, uses of the salt as a medicament in the treatment inter alia of disorders of the central nervous system and pharmaceutical compositions and dosage forms comprising the salt.
摘要:
This invention relates to novel 1,5,7-trisubstituted benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex.
摘要:
The present invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for inducing and maintaining anesthesia, sedation and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.