摘要:
The invention relates to new 8.beta.-hydrazinomethyl-ergoline derivatives of the general formula (I), ##STR1## wherein x y stands for a ##STR2## or ##STR3## group, R stands for hydrogen or methyl group, andR.sub.1 stands for hydrogen, a lower acyl group, a di-(lower-alkylaminocarbonyl group, a group of the general formula (VI), ##STR4## wherein Z.sub.1, Z.sub.2 and Z.sub.3 each represent hydrogen, halogen or a trifluoromethyl group, or a group of the general formula (VII), ##STR5## wherein Y represents a lower alkyl group, allyl group or phenyl group, and acid addition salts thereof. These compounds possess valuable antiserotonine, antidepressant and hypotensive effects, furthermore they can be applied as starting substances in the preparation of other biologically active ergoline derivatives.The new compounds of the general formula (I) are prepared according to the invention by reacting the respective 6-methyl-8.beta.-mesyloxymethyl or -tosyloxymethyl-ergoline derivatives with dry hydrazine. In order to obtain the N-substituted hydrazinomethyl compounds, the N-unsubstituted derivatives are reacted with an acylating agent or with an isothiocyanate.
摘要:
New compounds of the general formula (I) ##STR1## wherein R stands for hydrogen or methyl group,x y stands for a group of the formula ##STR2## and R.sub.1 stands for a group of the formula (III), (IV) or (V) ##STR3## wherein n is an integer from 4 to 10, ARE PREPARED BY ACYLATING A COMPOUND OF THE GENERAL FORMULA (II), ##STR4## wherein R and x y each have the same meanings as defined above, and R.sub.2 stands for a group of the formula (VI), (VII) or (VIII), ##STR5## with a C.sub.6-12 carboxylic acid or a C.sub.6-12 carboxylic acid halide. The new compounds of the general formula (I) and their acid addition salts can be used as antidepressants and antiserotonine agents with prolonged effects.
摘要:
The invention relates to new substituted dihydropyridine derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.6 are as defined herein after, the racemic and optically active variants as well as mixtures thereof, furthermore the acid addition salts of these compounds, pharmaceutical compositions containing the same and a process for the preparation thereof.The compounds of the general formula (I) can be advantageously applied for the treatment of pathologically severe hypertensions, their toxicity is low and they possess an advantageous therapeutic index.
摘要:
New 5H-2,3-benzodiazepine derivatives of the formula ##STR1## wherein R is phenyl having a trifluoromethyl or halogen substituent,R.sup.1 is methyl,R.sup.2 is hydrogen,R.sup.3 is methoxy and R.sup.4 is methoxy, and the pharmaceutically acceptable acid addition salts thereof, are potent tranquilizers.
摘要:
9,10-Dihydrolysergic acid-(3'-/pyrrolid-2"-on-1'-yl/-propyl)-amide, 1-methyl-9,10-dihydrolysergic acid-(thiazoline-2'-yl)-amide and lysergic acid-(3'-allyloxy-2'-oxy-propyl)-amide and their pharmaceutically acceptable acid addition salts possess antihypertensive and antiserotonin effect and exert an action on the central nervous system.
摘要:
New acylated 2-aminothiazole derivatives of the general formula (I), ##SPC1##whereinR.sup.1 stands for phenyl group or a pyridyl group,R.sup.2 stands for hydrogen or lower alkyl,R.sup.3 stands for hydrogen, a lower alkyl group or benzyl group, andR.sup.4 and R.sup.5 each represent hydrogen, a C.sub.1-8 alkyl group, allyl group, a hydroxyalkyl group, a C.sub.3-6 cycloalkyl group, .beta.-dimethylaminoethyl group, .beta.-diethylaminoethyl group, benzyl group, 2-furylmethyl group, or a phenyl group having optionally a halogen, methyl, methoxy or trifluoromethyl substituent, orR.sup.4 and R.sup.5 may form, together with the adjacent nitrogen atom, a 5 to 8 membered polymethyleneimino group, morpholino group, piperazino group, N-methylpiperazino group or N-phenylpiperazino group, the compounds of formula I are anticholinergics.
摘要:
The invention relates to new 1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-3,4-dihydro-5H-2,3-benzodiazepi ne of formula (1), optically active isomers and acid addition salts thereof as well as to pharmaceutical compositions containing these compounds. ##STR1## The new compounds of formula (I) can be prepared by reducing 1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine of formula (II) with an inorganic or organic-inorganic and/or complex metal hydride and, if desired, separating the optically active forms of the compound of formula (I) thus-obtained and, if desired, converting the base or bases into acid addition salts or converting the salts into the free bases(s). ##STR2## The new compound of formula (I) possesses significant central nervous effects and can advantageously be used in the therapy.
摘要:
The invention relates to a novel compound of the formula ##STR1## and the pharmaceuticlly acceptable acid addition salts thereof, wherein R stands for a hydrogen atom or methyl group, x y designates a ##STR2## Q is a hydrogen atom or a benzyloxycarbonyl- or N-tert.-butyloxycarbonyl protective group, and R.sub.1 is the side chain of a natural .alpha.-amino acid selected from the group consisting of Arg--, Tryp-13 , Phe--, Ser--, Leu--, Val--, Meth--, Tyr--, His-- or Prol---side-chain.The compounds according to the invention possess antiserotonin and hypotensive effects and act upon the central nervous system.
摘要:
New compounds of the formula ##STR1## wherein R is hydrogen or methyl group,X y is a group of the formula ##STR2## and N IS AN INTEGER OF FROM 4 TO 10, ARE PREPARED BY ACYLATING THE APPROPRIATE LYSERGIC ACID-(3'-ALLYLOXY-2'-OXY-PROPYL)-AMIDE COMPOUNDS WITH CARBOXYLIC ACIDS OF 6 TO 12 CARBON ATOMS OR WITH THEIR REACTIVE DERIVATIVES. If desired, the new compounds can be converted into their pharmaceutically acceptable acid addition salts.The above compounds possess prolonged antidepressive activities.