Abstract: The new compound vincane of the formula ##STR1## is prepared by the reduction or reductive dehydratation, respectively, a compound of the formula ##STR2## wherein A.about.B represents the group --CH.dbd.CH-- or ##STR3## i.e. of vincamenine or of vincanol.
Type:
Grant
Filed:
July 6, 1977
Date of Patent:
August 7, 1979
Assignee:
Richter Gedeon Vegyeszeti Gyar RT
Inventors:
Otto Clauder, Arpad Kiraly, Jozsef Kokosi, Egon Karpati, Laszlo Szporny
Abstract: The invention relates to novel piperazine derivatives having the formula (I), ##STR1## wherein R.sub.1 represents a C.sub.1-5 alkyl group having optionally a phenyl, trimethoxyphenyl, phenoxy, methoxy-cyclohexyl or heptamethyleneimino substituent on the terminal carbon atom, allyl group, a phenyl group having optionally one or more halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trihalomethyl or allyl substituent(s), or a C.sub.2-5 alkoxycarbonyl group,R.sub.2 represents hydrogen or a C.sub.1-4 alkyl group, andR.sub.3 represents furyl group, 9-xanthenyl group or a C.sub.5-6 cycloalkyl group having a C.sub.1-4 alkoxy substituent,Or acid addition salts or quaternary salts thereof.The invention also relates to pharmaceutical compositions containing the above compounds, furthermore to a process for the preparation of the novel compounds and pharmaceutical compositions.The novel compounds according to the invention possess anti-arrhythmic and coronary dilatating effects.
Type:
Grant
Filed:
December 12, 1977
Date of Patent:
February 20, 1979
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt.
Inventors:
Karoly Felfoldi, Jozsef Apjok, Mihaly Bartok, Jozsef Czombos, Arpad Molnar, Ferenc Noteisz, Egon Karpati, Laszlo Szporny
Abstract: A compound of the formula (I) ##STR1## wherein X stands for a hydrogen atom, an optionally substituted aliphatic or aromatic sulfonyloxy group, a thiocyanato group, an azido group or an amino group optionally mono- or disubstituted by aliphatic, cycloaliphatic, aromatic or araliphatic hydrocarbon groups, acyl, alkyloxycarbonyl, cycloalkyloxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl, aminocarboimido groups or the substituents of the said amino group may form with the nitrogen atom thereof a five-, six- or seven-membered saturated or unsaturated heterocyclic ring optionally containing a further nitrogen, oxygen or sulfur hetero atom, and a quaternary salt or acid addition salt thereof. The compounds are useful in the treatment of arteriosclerosis and high blood pressure.
Type:
Grant
Filed:
August 30, 1976
Date of Patent:
October 17, 1978
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt.
Inventors:
Otto Clauder, Jozsef Kokosi, Laszlo Szporny, Egon Karpati
Abstract: A compound of the formula (I) ##STR1## wherein X is a halogen,Z.sub.1 and Z.sub.2 are both hydrogen, orZ.sub.1 is hydroxy and Z.sub.2 is chlorine, orZ.sub.1 and Z.sub.2 together stand for an .alpha.-epoxy group.
Abstract: 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.
Abstract: A fluid is introduced into a bed of a material to be fluidized along the bottom surface thereof at a pulsating velocity which is by an order of magnitude greater than the velocity of fluidization.Such method can be carried out in a fluidization apparatus having a per se known distributor the orifices of which are overlapped by reeds which vibrate when a pressure fluid is introduced into a bed above the distributor.
Abstract: Apovincaminol ester of formula ##STR1## wherein R is an alkylcarbonyl group having 3 to 12 carbon atoms, or a pharmaceutically acceptable acid addition salt thereof.
Type:
Grant
Filed:
July 7, 1976
Date of Patent:
August 22, 1978
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt.
Inventors:
Csaba Lorincz, Maria Bolyos, Kalman Szasz, Laszlo Szporny, Egon Karpati, Eva Palosi
Abstract: A process for the preparation of L-aspartyl-(O-sulfato-L-tyrosyl)-L-methionyl-glycyl-L-tryptophyl-L-methion yl-L-aspartyl-L-phenylalanine amide, which comprises treating the protected octapeptide amide of the general formula (II) ##STR1## wherein X is BOC, Cbz or Ddz,Y is O.sup.t Bu, OBzl or OH andW is O.sup.t Bu, OBzl or OH,in the presence of an ether with an excess of the complex compound of sulfur trioxide and a tertiary amine containing at least one alkyl group, converting the obtained sulfate ester of the protected octapeptide amide into an alkali metal salt and simultaneously removing the formyl group from the tryptophan unit by reacting the sulfate ester with an alkali metal hydroxide, and then splitting off the remaining protective groups by acidolysis.
Type:
Grant
Filed:
April 28, 1977
Date of Patent:
July 25, 1978
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt.
Inventors:
Botond Penke, Lajos Balaspiri, Peter Pallai, Kalman Kovacs, Vince Varro, Janos Lonovics, Laszlo Varga, Gyorgy Dobo, Geza Ivanyi, Lajos Kovacs, Miklos Low, Judit Low, nee Kaloczy
Abstract: Curare-type salts of the formula ##STR1## WHEREIN Ac is an alkyl carbonyl group containing 1 to 4 carbon atoms in the alkyl moiety and one ofR.sub.1 and R.sub.2, is a methylene group and the other is a group of the formula >N-R.sub.2 wherein R.sub.2 is an alkyl group containing 1 to 3 carbon atoms,A is halogen andR.sub.3 is an alkyl group containing 1 to 4 carbon atoms, or an alkyl group; andA process for the preparation thereof are disclosed.
Type:
Grant
Filed:
July 28, 1976
Date of Patent:
July 18, 1978
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt.
Inventors:
Zoltan Tuba, Maria Marsai, Katalin Biro, Laszlo Szporny, Egon Karpati, Szaboles Szeberenyi
Abstract: 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.
Abstract: Racemic and optically active 1-alkyl-1,2,3,4,6,7,12,12b-octahydro-indolo[2,3-a]quinolizines of vasodilatory and haemodynamic effect are disclosed.
Type:
Grant
Filed:
June 23, 1976
Date of Patent:
May 16, 1978
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt.
Inventors:
Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Egon Karpati, Laszlo Szporny
Abstract: The invention is directed to a new substituted derivative of .alpha.-ethylnyl-benzophenone, namely, the 3-iodo-.alpha.-ethynyl-benzhydrol which has high antifungal activity.
Abstract: A process is disclosed for the separation and recovery of vinblastine and leurosine from a mixture of diindole alkaloids obtained by extraction of the plant, Vinca rosea L.
Abstract: .alpha.-ethynyl-benzhydrols, namely 2,5-dimethyl-.alpha.-ethynyl and 4-n-butyl-.alpha.-ethynyl benzhydrol, are made by reacting the starting benzophenone with acetylene in a solvent delivering no protons, in the presence of an alkali metal tertiary alcoholate, preferably potassium-ter.-butylate or potassium-tert.-amylate.
Abstract: A heart and vasotropic pharmaceutical of the formula: ##STR1## wherein R represents a hydrogen atom or an acyl group, preferably a C.sub.1-15 alkylcarbonyl, C.sub.2-6 alkenylcarbonyl, or a phenyl- (C.sub.1-5)-alkylcarbonyl group or a benzoyl group optionally substituted with halogen, trihalomethyl, C.sub.1-4 or nitroAnd pharmaceutically acceptable acid addition and quaternary salts thereof.
Type:
Grant
Filed:
June 9, 1976
Date of Patent:
December 27, 1977
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt.
Inventors:
Csaba Lorincz, Kalman Szasz, Maria Bolyos, Karola Jovanovics, Laszlo Szporny, Egon Karpati, Eva Palosi
Abstract: 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.
Type:
Grant
Filed:
December 10, 1976
Date of Patent:
December 20, 1977
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt.
Inventors:
Erzsebet Mago nee Karacsony, Jozsef Borsi, Endre Csanyi, Katalin Pik, Lajos Wolf
Abstract: New compounds of the general formula (I), ##STR1## wherein R.sub.1 and R.sub.2 each stand for a saturated or unsaturated, straight-chained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, orR.sub.1 and R.sub.2 together with the adjacent nitrogen atom may form an optionally substituted heterocyclic group optionally containing a further oxygen or nitrogen hetero atom,But if R.sub.1 stands for methyl, R.sub.2 may only stand for a group other than methyl, are prepared by reacting a compound of the general formula ##STR2## wherein X stands for halogen, with a secondary amine of the general formula (III),r.sub.1 --nh--r.sub.2 (iii)wherein R.sub.1 and R.sub.2 each have the same meanings as defined above.The new compounds of the general formula (I), as well as their pharmaceutical acceptable acid addition salts or quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess antipyretic activity.