Basf Aktiengesellschaft

Richter Gedeon Vegyeszeti Gyar Rt

Egis Gyogyszergyar

Richter Gedeon Vegyeszeti Gmbh

Berta Knoll

Jozsef Knoll

Lujza E Petocz

Attila Mandi

Edit Berenyi Nee Poldermann

Janos Nagy

Marton Fekete

Istvan Gyertyan

Istvan Gacsalyi

Huba Kalasz

Katalin Budai Nee Simonyi

Julia Timar

Ildiko Niklya

Gabriella Zsila

Zsuzsa Furts

Gabriella Zsilla

Katain Budainee Simonyi

Ne Simonyi Budai

Edit Berenyi Ne Poldermann

Sandor Harmath

The 3-amino-4-ethylthio-quinoline of the Formula I ##STR1## and pharmaceutically acceptable acid addition salts thereof possess useful therapeutical properties. They exhibit a potent and highly selective anxiolytic and narcosis potentiating effect and are devoid of sedative and anti-convulsive effect. Consequently, the invention relates to pharmaceutical compositions comprising the compound of Formula I or a salt thereof as active agent. The invention also relates to a new and improved process for the preparation of the compound of Formula I.

Pharmaceutical compositions

The new compounds of the general Formula I ##STR1## (wherein R.sub.1 stands for C.sub.1-5 alkyl, C.sub.2-5 alkenyl, C.sub.2-5 alkinyl, C.sub.3-7 cycloalkyl or optionally substituted phenyl-(C.sub.1-4 alkyl);

Quinoline thioethers

The invention relates to new thiazolo[4,5-c]quinoline derivatives of the general Formula I ##STR1## and acid addition salts thereof, a process for the preparation of the same and pharmaceutical compositions comprising the said compounds. The substituent definition of the general Formula I is as follows:

Thiazolo/4,5-c/quinolines as major tranquilizers

The selective appetite-regulating substances satietin and satietin-D had up to the present been prepared from human or animal blood serum or plasma by ultrafiltration, gel chromatography, treatment with trichloroacetic acid, affinity chromatography and optionally treatment with a proteolytic enzyme. According to the invention, satietin and satietin-D are obtained in a purified form by using immunoabsorption. Being glycoproteins, both satietin and satietin-D form antibodies (antisatietin and antisatietin-D, respectively) in the living organism and can be isolated from the blood and bound to a gel column. For the preparation of satietin and satietin-D, respectively, the human or animal blood plasma or serum is subjected to ultrafiltration and the ultrafiltrate, containing in addition to satietin and satietin-D other constituents with a molecular weight below 50000 daltons, is contacted with the gel column. The antibody bound to the gel column forms with satietin or satietin-D, respectively, an immunocomplex remaining on the column while the other constituents of the ultrafiltrate can be eluted by a buffer. Then, the immunocomplex is cleaved, whereby satietin or satietin-D, respectively, can be eluted in a purified form from the column. The column containing the antibody may repeatedly be used.

Purified appetite-regulating substances of biological orgin, their

It has been found that 2-methyl-thiazolo[4,5-c]quinoline and pharmaceutically acceptable acid addition salts and hydrates thereof possess valuable central nervous depressive properties being different from those of benzodiazepines. The invention relates to pharmaceutical compositions comprising as active ingredient 2-methyl-thiazolo[4,5-c]quinoline of the Formula I ##STR1## or a pharmaceutically acceptable acid addition salt or hydrate thereof.

Pharmaceutical compositions of 2-methyl-thiazolo[4,5-c]quinoline

The invention involves isolating a food intake suppressant by subjecting blood serum to ultrafiltration transmitting up to a molecular weight of 30,000 daltons, partially evaporating the filtrate, removing the insoluble part from the concentrate obtained, adding trichloroacetic acid up to a concentration of 5 to 25 weight/volume percent to the liquid phase at a temperature of 0.degree. to 10.degree. C., removing the proteins precipitated, subjecting the obtained solution to chromatography on a gel with a void volume below a molecular weight of 4000 daltons, eluting with a solution of pH 6.0 to 7.0, concentrating the biologically active fractions, chromatographing again on a gel with a void volume below a molecular weight of 4000 daltons, fractionating by elution with water, lyophilizing the active fractions, dissolving the lyophilized fractions in a buffer of pH 8.1 to 8.2, adding trypsin and chymotrypsin to the solution in a substantially identical amount of 0.01 to 0.2 by weight as calculated for the total weight of the lyophilized product, subjecting the mixture to digestion at a temperature of 36.degree. C. to 39.degree. C., preferably with occasionally shaking from 20 to 30 hours, adding after the first 5 hours trypsin and chymotrypsin in a substantially half amount as calculated for the original enzyme quantity and continuing the digestion, then adding trichloroacetic acid to the reaction mixture up to a concentration of 4 to 6 weight/volume percent at a temperature between 0.degree. and 10.degree. C., keeping the mixture at a temperature between -15.degree. C. and 5.degree. C. for 1 to 24 hours, removing the insoluble part, subjecting the reaction mixture to chromatography on a gel with a void volume below a molecular weight of 4000 daltons, fractionating by elution with water and lyophilizing the biologically active fractions.

Process for the preparation of a new-type active substance selectively

Described is the method of preparing satietin, a peptide separated from plasma or serum and possessing the effect of inhibiting food intake. Also described is the product satietin.

Process for the production of an andrexogenic substance having specific

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Budapest, Hungary

Berta Knoll