Hoechst Aktiengesellschaft

University Patents, Inc.

Michael Leineweber

Ernold Granzer

Alfred Puhler

Klaus-Dieter Kampe

Gerhard Rackur

Eugen Uhlmann

Marvin H Caruthers

Wolfgang Wohlleben

Yitzhak Stabinsky

Joachim Engels

Norbert Krass

Wolfgang Ulmer

Axel Hoffmann

Hans Georg Boger

Moshe Leitner

Wolfgang Wolleben

Hans G B Oger

Manfred Huttinger

Soluble salts of 4-amino-2-(4,4-dimethylimidazolidin-2-on-1-yl)pyrimidine-5-carboxylic acid N-methyl-N-(3-trifluoromethylphenyl)amide, a process for the preparation thereof, the use thereof as pharmaceuticals and starting materials. Salts, which are soluble and freely soluble in water, of 4-amino-2-(4,4-dimethylimidazolidin-2-on-1-yl)pyrimidine-5-carboxylic acid N-methyl-N-(3-trifluoromethylphenyl)-amide and a process for the preparation thereof are described. The compounds are suitable for the treatment of lipid metabolism disorders which are beneficially influenced by stimulation of the hepatic LDL receptor. Also described are the compounds of the formula IV ##STR1## and the salts thereof.

Soluble salts of 4-amino-2-(4,4-dimethylimidazolidin-2-on-1-yl)

The present invention relates to tertiary 4-amino-2-ureidopyrimidine-5-carboxamides of formula I: ##STR1## in which R.sup.1 is (C.sub.1 -C.sub.8)-alkyl wherein one or more H are replaced by F; R.sup.2 is selected from the group consisting of F, Cl, Br, H, --O--(C.sub.1 -C.sub.8)-alkyl and (C.sub.1 -C.sub.8)-alkyl, wherein one or more of the H of the alkyls can be replaced by F; R.sup.3 is selected from the group consisting of F, Cl, Br, H, --O--(C.sub.1 -C.sub.4)-alkyl and (C.sub.1 -C.sub.4)-alkyl, wherein one or more of the H of the alkyl can be replaced by F; R.sup.4 is CF.sub.3 or OCF.sub.3 ; and their physiologically tolerable salts. Process for preparing the compounds of formula I are also described. The compounds are suitable for the treatment of disorders of lipid metabolism.

Compounds for treating disorders of lipid metabolism and their

Compounds of the formula I ##STR1## in which R.sup.1 to R.sup.6 have the stated meanings, and the readily water-soluble salts of these compounds, and a process for the preparation thereof are described. The compounds are suitable for the treatment of lipid metabolism disorders which are beneficially influenced by a stimulation of the hepatic LDL receptor. Also described are compounds of the formula II ##STR2## and the salts thereof.

Pyrimidines

Partial sequences of human-.gamma.-interferon, comprising aminoacid sequences 5 to 127, 1 to 127 and 5 to 146, having biological activity. These partial sequences can be obtained by a genetic engineering process, for which purpose the appropriate DNA sequences are chemically synthesized. The DNA sequences are incorporated in hybrid plasmids, and the latter are introduced into host organisms and their expression is induced there. The biologically active polypeptides are suitable, as is human-.gamma.-interferon, for medicaments.

Preparation of polypeptides having human .gamma.-interferon activity

DNA sequences encoding for novel human lymphoblastoid-leukocyte hybrid interferons. Methods of making nucleotide sequences comprising ribosome binding sites, promoter regions, and segments of human lymphoblastoid and leukocyte interferons are described. DNA sequences for hybrid interferons are cloned and expressed in plasmid vectors. Transformed microorganisms and novel lymphoblastoid-leukocyte polypeptide interferons having biological or immunological activity are disclosed.

Hybrid lymphoblastoid-leukocyte human interferons

The plasmid p SVH 1, which is obtained from Streptomyces venezuelae DSM 40755 and which has a molecular weight of 8.4 megadaltons, a contour length of 4.1 .mu.m and a molecular size of 12.6 kilobases, and its use for the construction of a vector and for cloning foreign DNA in suitable host organisms.

Plasmid P SVH 1 and its use

The new streptomyces plasmid p SG 2, having a molecular weight of 9.2 megadaltons, a contour length of 4.58 .mu.m and a molecular length of about 13.8 kilobases, is described, together with its preparation from a culture of 'Streptomyces ghanaensis' ATCC 14 672.

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Frankfurt am Main, Germany

Michael Leineweber