摘要:
18-Methyl-19-nor-20-keto steroids of the formula ##STR1## wherein R.sub.1 and R.sub.2 collectively are an oxygen atom, or each is hydrogen, or one of R.sub.1 and R.sub.2 is hydrogen and the other is hydroxy, and R.sub.3 is a ketonic oxygen atom or two hydrogen atoms, possess CNS-depressant activity, especially anesthetic-narcotic activity.
摘要:
D-homo-20-ketopregnanes of the formula ##STR1## wherein R.sub.1 is oxygen, ##STR2## in which R.sub.5 is hydrogen or lower acyl; R.sub.2 is hydrogen or methyl; R.sub.3 is oxygen, ##STR3## or two hydrogen atoms; R.sub.4 is hydrogen, hydroxy or acyloxy; R.sub.6 is hydrogen or methyl; and R.sub.7 is hydrogen, acetyl, hydroxy or lower acyloxy in the .alpha.- or .beta.-position possess CNS-depressant activity, including anesthesia upon parenteral administration, and are produced by hydrogenating the corresponding steroids having double bonded C.sub.5 and/or C.sub.16 carbon atoms.
摘要:
Benzomorphans of the formula ##STR1## wherein R.sub.1 is H, CH.sub.3 or C.sub.2 H.sub.5 ; R.sub.2 is CH.sub.3 or C.sub.2 H.sub.5 and R.sub.3 and R.sub.4, which can be alike or different, each are lower alkyl, and the acid addition salts thereof with physiologically acceptable acids have CNS activity, including analgesic, morphine antagonistic, anti-convulsive, muscle relaxant, sedative and neuroleptic activity.
摘要翻译:其中R 1是H,CH 3或C 2 H 5的式[IMAGE]的苯并吗啡; R2是CH3或C2H5,R3和R4可以相同或不同,各自为低级烷基,其与生理上可接受的酸的酸加成盐具有CNS活性,包括止痛,吗啡拮抗,抗惊厥,肌肉松弛剂,镇静剂 和精神安定药活动。
摘要:
4-(Polyalkoxyphenyl)-2-pyrrolidones of the formula ##STR1## wherein R.sub.1 and R.sub.2 each are hydrocarbon of up to 18 carbon atoms at least one being other than methyl, a heterocyclic ring, or alkyl of 1-5 carbon atoms substituted by halogen, OH, COOH, alkoxy, alkoxycarbonyl or an amino group; R' is H, alkyl, aryl or acyl; and X is O or S; possess neuropsychotropic activity. The compounds wherein X is O can be produced by saponifying and decarboxylating a corresponding 2-pyrrolidone-3-carboxylic acid alkyl ester or cyclizing a corresponding 3-phenyl-4-amino-butyric acid or alkyl ester thereof. The pyrrolidones can be converted to the corresponding thiopyrrolidones by reaction with phosphorous pentasulfide in the presence of base.
摘要:
4-(Polyalkoxyphenyl)-2-pyrrolidones of the formula ##STR1## wherein R.sub.1 and R.sub.2 each are hydrocarbon of up to 18 carbon atoms or alkyl of 1-5 carbon atoms substituted by halogen, OH, COOH, alkoxy, alkoxycarbonyl, carboxamido or amino or collectively are alkylene of 1-3 carbon atoms, R.sub.3 is H or OCH.sub.3, R.sub.4 is H, alkyl, aryl or acyl and X is O or S possess neuropsychotropic activity. The compounds wherein X is O are produced by saponifying and decarboxylating a corresponding 2-pyrrolidone-3-carboxylic acid alkyl ester or cyclizing a corresponding 3-phenyl-4-aminobutyric acid or alkyl ester thereof. The pyrrolidones are converted to corresponding thiopyrrolidones in a conventional manner, e.g., by reaction with phosphorous pentasulfide in the presence of base.
摘要:
Diacylapomorphines of the formula ##STR1## wherein R.sub.1 and R.sub.2 are both acyl of 1-17 carbons are symptomatically effective agents in the treatment of motor disorders of the type associated with a dopamine deficiency of the extrapyramidal system of the central nervous system, e.g. Parkinson's disease. Pharmaceutical compositions containing these compounds as an active ingredient are described, as well as new compunds of the above formula wherein R.sub.1 and R.sub.2 are formyl or acyl of 3-17 carbon atoms.
摘要:
Compounds of general Formula I labeled with .sup.121 I, .sup.122 I, .sup.123 I, .sup.124 I, .sup.125 I, .sup.131 I and .sup.132 I isotopes ##STR1## wherein R.sup.6 is a C.sub.1-6 aliphatic hydrocarbon residue andC.sub.2 -C.sub.3 C.sub.9 -C.sub.10 is a single or a double bond, as well as their acid addition salts,are useful as diagnostic media, e.g., in imaging dopamine and other receptors.