摘要:
New imidazoquinoxaline compounds having the general formula ##STR1## wherein R.sup.3 is ##STR2## wherein R' is C.sub.1-6 -alkyl, which may be straight or branched, C.sub.3-7 -cycloalkyl or phenyl; andR.sup.4 is hydrogen or C.sub.1-6 -alkyl; and 5-N-oxides thereof.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and in improving the cognitive function of the brain of mammals.
摘要:
The invention relates to a dealkylation chemical process for preparing imidazoquinoxalines bearing hydrogen substitution in the five position, and to valuable pharm-intermediates of the formula I ##STR1## wherein ##STR2## wherein R' is C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl, phenyl, thienyl, or C.sub.1-3 -alkoxymethyland wherein R.sup.6 and R.sup.7 independently are hydrogen,halogen or CF.sub.3, used in that process. The intermediates also have anticonvulsant and anxiolytic properties.
摘要:
New imidazoquinoxaline 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; and ##STR3## wherein R.sup.5 is hydrogen or halogen. The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and in improving the cognitive function of the brain of mammals.
摘要:
New heterocyclic compounds having the general formula ##STR1## wherein R.sup.3 is ##STR2## CO.sub.2 R' or CONR'R", wherein R' and R" independently are C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl or C.sub.1-6 -alkoxymethyl;--A-- is --C(.dbd.O)--NR'"--, --NR'"--C(.dbd.O)--, or ##STR3## wherein R'" is C.sub.1-6 -alkyl; X is C or N; andR.sup.4 is hydrogen, halogen, CN, C.sub.1-6 -alkyl, C.sub.1-6 -alkynyl, trimethylsilyl-C.sub.1-6 -alkynyl, aryloxy which may be substituted with halogen, aralkoxy, C.sub.3-7 -cycloalkoxy which may be substituted with one or more C.sub.1-6 -alkyl groups, or NR""R'"", wherein R"" and R""' independently are C.sub.1-6 -alkyl or together with the nitrogen atom form a 3-7 membered heterocyclic ring.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 the use of compounds capable of inhibiting the activity of a proton-gated cation channel in the treatment of alleviation of diseases or disorders associated with, or mediated by a drop in extra cellular pH.
摘要:
A compound having the formula or a pharmaceutically acceptable salt thereof wherein R is hydrogen or hydroxy; R1 is hydrogen, alkyl, arylalkyl, (CH2)nOH, or (CH2)nNR7R8; R5 and R6 are each independently hydrogen, halogen, NO2, CN, CF3, SO2NR7R8, PO3R9R10, alkyl, alkenyl, alkynyl, (CH2)nCONR7R8, (CH2)nCO2R10, NHCOR11, A is a ring formed by the following: a-NR12—CHR13—CHR14-b, a-CHR13—CHR14—NR12-b, a-CHR13—NR12—CHR14-b, a-CHR14—CH2—NR12—CHR13-b, a-CHR13—NR12—CH2—CHR14-b, a-CH2—CH2—CHR13—NR12-b, a-NR12—CHR13—CHR12—CH2—CH2-b, a-CH2—CH2—NR12—CH2—CH2-b, a-CH2—CH2—CH2NR12—CH2-b, a-CH2—NR12—CH2—CH2-b a-CH2—CH2—CH2—CH2—NR12-b, a-NR12—CH2—CH2—CH2—CH2-b, The compounds are useful in the treatment of disorders responsive to the blockade of glutamic and aspartic acid receptors.
摘要翻译:具有下式的化合物或其药学上可接受的盐,其中R是氢或羟基; R 1是氢,烷基,芳基烷基,(CH 2)n OH或(CH 2)n NR 7 R 8; R 5和 R 6各自独立地为氢,卤素,NO 2,CN,CF 3,SO 2 NR 7,PO 3 R 9,烷基,烯基,炔基,(CH 2)n CONR 7 R 8 >,(CH 2)n CO 2 R 10,NHCOR 11,A是由以下形成的环:a-NR 12 -CHR 13 -CHR 14 - ,a-CHR 13 - CHR 14 -NR 12 -b,a-CHR 13 -NR 12 -CHR 14 -b,a-CHR 14 -CH 2 -NR 12 -CHR 13 - b,a-CHR 13 -NR 12 -CH 2 -CHR 14 -b,a-CH 2 -CH 2 -CHR 13 -NR 12 -b,-NR a R 12 -CHR -CH 2 -CH 2-b,a-CH 2 -CH 2 -NR 12 -CH 2 -CH 2 -B,a-CH 2 -CH 2 -CH 2 NR 12 -CH 2 -B,a-CH 2 - NR 12 -CH 2 -CH 2 -BA-CH 2 -CH 2 -CH 2 -CH 2 -NR 12 -b,a-NR 12 -CH 2 -CH 2 -CH 2 -CH 2 -B,该化合物可用于治疗 的阻滞谷氨酸和天冬氨酸受体的病症。
摘要:
The present patent application discloses compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof or an oxide thereof wherein R.sub.3 is ##STR2## wherein A, B and D each is CH, or one or two of A, B and D is N and the others are CH;R.sup.11 is phenyl, benzimidazolyl, or monocyclic heteroaryl all of which may be substituted one or more times with substituents selected from alkyl, halogen, CF.sub.3, amino, nitro, cyano, acylamino, alkoxy, acyl, phenyl, and monocyclic heteroaryl, andone of R.sup.6 and R.sup.7 is hydrogen and the other is pyrrolyl which may be substituted one or more times with substituents selected from halohen, alkyl, phenyl, and alkoxy.The compounds are useful for the treatment of various central nervous system disorders such as epilepsy and other convulsive disorders, anxiety, sleep disorders and memory disorders.
摘要:
Novel azacyclic compounds selected from the group consisting of ##STR1## wherein R.sup.1 is H or C.sub.1-6 -alkylR.sup.3 is ##STR2## R" is H or C.sub.1-8 -alkyl or C.sub.1-6 -alkoxy or C.sub.1-4 -alkoxy-C.sub.1-4 -alkyl or aryl, andR.sup.4 is H, C.sub.1-8 -alkyl or Cl;and a salt thereof with a pharmaceutically-acceptable acid.The new compounds are useful in improving the cognitive functions of the forebrain and hippocampus of mammals, and are useful in the treatment of Alzheimer's disease.
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.