Ciba-geigy Corporation

Novartis Corporation

Irmgard Wiesenberg

Martin Missbach

Pier G Ferrini

Leo Widler

Ulrich Feige

The current invention concerns the use of a receptor from the RZR/ROR receptor family or of a functional fragment thereof in a test of a compound for anti-autoimmune, anti-arthritic, anti-tumor, melatonin-like and/or melatonin-antagonistic activity and the production of a receptor ligand complex comprising said receptor or a functional fragment thereof and a ligand of said receptor. Described is also a method for testing compounds for said activity (screening for ligands) and the active compounds identified therewith.

Screening method using the RZR receptor family

Compounds of the formula I ##STR1## in which R.sub.1 is lower alk-2-en-1-yl, lower alk-3-en-2-yl, lower alk-2-yn-1-yl or lower alkyl substituted in the 2,3-position by radicals which can be eliminated to give a double bond, R.sub.2 is hydrogen and R.sub.3 is methyl which is unsubstituted or substituted by radicals which can be eliminated together with hydrogen R.sub.2 to give a double bond or R.sub.2 and R.sub.3 are both hydrogen or lower alkyl or are together methylene and R.sub.4 is a group of the formula Ia, Ib or Ic ##STR2## in which R.sub.5 is hydrogen, lower alkyl, lower alk-2-en-1-yl or lower alk-2-yn-1-yl and R.sub.6 is a group of the formula Id or Ie ##STR3## in which R.sub.1, R.sub.2, R.sub.3 and R.sub.5 are as defined, and their pharmaceutically acceptable salts can be used in a novel manner for the treatment of diseases of the rheumatoid type.

Use of 2-iminothiazolidin-4-one derivatives as novel pharmaceutical

Compounds of formula I ##STR1## wherein X and Y are each independently of the other thio or sulfynyl, R.sub.1 is lower alk-2-en-1-yl, lower alk-3-en-2-yl, lower alk-2--yn-1-yl, or lower alkyl that is substituted in the 2,3-position by radicals that can be eliminated to form a double bond, R.sub.2 is hydrogen and R.sub.3 is unsubstituted methyl or methyl substituted by a radical that can be eliminated together with hydrogen Rhd 2 to form a double bond, or R.sub.2 and R.sub.3 are each hydrogen or lower alkyl or together are methylene, R.sub.4 is free or protected hydroxy, or hydrogen, and R.sub.5 is hydrogen, lower alkyl, lower alk-2-en-1-yl, lower alk-2-yn-1-yl, or lower alkyl that is substituted in the 2,3-position by radicals that can be eliminated to form a double bond, and their pharmaceutically acceptable salts may be used in a novel manner for the treatment of disorders of the rheumatoid type.

Growing community of inventors

Weil am Rhein, Germany

Irmgard Wiesenberg