Richter Gedeon Vegyeszeti Gyar Rt

Csaba Lorincz

Kalman Szasz

Laszlo Szporny

Egon Karpati

Karola Jovanovics

Gyorgy Fekete

Lajos Dancsi

Eszter Dezseri

Eva Palosi

Csaba Szantay

Lajos Szabo

Tibor Keve

Janos Galambos

Bela Zsadon

Arpad Kiraly

Lilla Forgach

Maria Zajer Nee Balazs

Bela Rosdy

Gyongyver Kiraly Nee Soos

Bela Szarvady

Maria Bolyos

Bela Stefko

Lajos Kisfaludy

Erik Bogsch

Katalin Nogradi

Lajos Kovacs

Antal Gimesi

Istvan Gebhardt

Sandor Eckhardt

Katalin Honty

Janos Sugar

Gyorgy Dobo

Zsuzsa Relle Nee Somfai

Jozsef Tamas

Aron Szollosy

Zsuzsanna Foldesi Nee Szasz

Eva Lorincz Nee Csapo

The invention relates to the new 17,18-dehydro-apovincaminol-3',4',5'-trimethoxy-benzoate of formula (I) ##STR1## and acid addition salts thereof. According to another aspect of the invention there is provided a process for the preparation of these new compounds. Still another aspect of the invention is a pharmaceutical composition for treating psoriasis.

Polycyclic compounds containing a double bond in the D-ring

The present invention relates to the compounds of the Formulae 1a and 1b and pharmaceutically acceptable acid addition salts thereof. The new 9-nitro-apovincaminol-3',4',5'-trimethoxybenzoate of the Formula 1a ##STR1## and the 11-nitro-apovincaminol-3',4',5'-trimethoxy-benzoate of the Formula 1b ##STR2## and pharmaceutically acceptable acid addition salts thereof can be prepared by nitrating the apovincaminol-3',4',5'-trimethoxy-benzoate of the Formula 11, ##STR3## if desired separating the mixture of the compounds of the Formulae 1a and 1b thus obtained into its components, if desired converting a compound of the Formula 1a or 1b thus obtained into pharmaceutically acceptable acid addition salts thereof. The new compounds of the present invention can be used in therapy in the treatment of psoriasis.

Nitro-substituted polycyclic derivatives useful in the treatment of

A herbicidal composition capable of preventing weed growth of potatoes or soybean plants consists of a triazene or an aromatic nitro compound together with an inorganic salt, especially sodium bisulfate or potassium bisulfate which reduced the quantity of the organic herbicide below that usually required to obtain a corresponding herbicidal effect and hence prevents phytotoxic damage. The composition contains 0.1:1 to 15:1 parts by weight of the inorganic compound to the organic compound and is applied in an amount of 0.1 to 30 kg of the composition per hectare.

Plant-protective and pest-control agent

A mixture of minor diindole alkaloids from Vinca-containing vinblastine and 4-deacetoxy-vinblastine vines, are separated by subjecting the mixture to a deacetylation to correct the vinblastine to deacetyl-vinblastine prior to chromatographic separation of said mixture in a single stage.

Process for separating pharmaceutically active diindole alkaloids

A process for the preparation of alkaloids of the leurosine type having the formula I ##STR1## and the acid addition salts thereof. In the formula I R is hydrogen or methyl. The compounds prepared according to the invention are known compounds showing cytostatic activity.

Process for the preparation of alkaloids of the leurosine type

Tumor inhibiting alkaloids are recovered from Vinca Rosea L. by a method which comprises extracting the dried leaves with a solvent selected from the group consisting of an alkanol having 1 to 5 carbon atoms, a mixture of an alkanol having 1 to 5 carbon atoms and a dilute, aqueous solution, benzene and benzene homologs; subsequently purifying the alkaloid extract obtained by a phase-change method between immiscible solvents, precipitating the main amount of dimeric alkaloids in form of their sulphuric acid addition salts, isolating leurosine, vincistine, vinblastine, desacetoxy-vinblastine, N-desmethyl-vinblastine and desacetyl-vinblastine from the salt mixture obtained, and then completing the separation and isolation of the remaining alkaloids by separation and isolation by adjusting the pH-value of the mother liquor, after precipitation and removal of the salt mixture, to 5.5 to 10, extracting the solution with a water-immiscible organic solvent and separating vindoline, catharantine, 3',4' -anhydrovinblastine and leurosine from the extract by chromatography, extracting vindoline in the pH-range of 2.5 to 3.5 and catharantine 3',4'-anhydrovinblastine and leurosine in the pH-range of 5 to 6 with benzene or a benzene homologue, from the mother liquor obtained when isolating the salt mixture, and separating a mixture of leurosine and 3',4'-anhydrovinblastine by crystallization, epoxidizing this mixture with an oxygen source, or separating the mixture into its components by chromatography, and subsequently epoxidizing the 3',4'-anhydrovinblastine component to leurosine, and isolating catharantine remaining from the mother liquor obtained when separating the crystalline mixture, or separating the extract containing catharantine, 3',4'-anhydrovinblastine and leurosine into its components by chromatography.

Process for the isolation of alkaloid components from the plant Vinca

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.

(-)-Apovincaminol lauric acid ester and cerebral vasodilatory

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.

Process for the preparation of diindole alkaloids or of the acid

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 nitro And pharmaceutically acceptable acid addition and quaternary salts thereof.

Eburnamenine derivatives

Vasodilatory eburnamine-type alkaloid esters of the formula (I) ##STR1## and salts and quaternary derivatives thereof, wherein X.about.Y REPRESENTS A =CH=CH- or ##STR2## R represents a C.sub.1-6 alkoxycarbonyl group optionally substituted with a hydroxy group or with a halogen atom, further an alkenyloxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl group or an acylated primary alcohol group, especially apovincaninic acid ethyl ester, have been prepared by various methods of esterification.

Alkaloid esters

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Budapest, Hungary

Csaba Lorincz