AMIDINE DERIVATIVES WITH SPASMOLYTIC,PSYCHOSTIMULANT AND ANOREXIGENIC PROPERTIES

• Main Authors: ILDIKO KOSA, ZOLTAN ECSERY, JOZSEF KNOLL
• Format: Patent
• Language: English
• Published: 16.05.1972
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

1,238,693. Amidine derivatives. CHINOIN GYOGYSZER ES VEGYESZETI TERMEKEK GYARA. RT. 8 July, 1968 [11 July, 1967], No. 32556/68. Heading C2C. Novel compounds of Formula I and pharmaceutically acceptable salts thereof wherein R 1 , R 2 and R 3 are each H; allyl optionally substituted by halogen, OH, carboxy, amino, mono- or di-alkylamine, acylamino, acetoxy, alkoxy, aryl optionally substituted as defined below or heterocyclic groups; aryl optionally substituted by halogen, OH, COOH, alkoxy, acylamino, acyloxy, alkyl or substituted alkyl as defined above; or are heterocyclic optionally substituted; R 4 and R 5 are each H, NO 2 , OH, alkoxy, halogen, amino or acylamino, are prepared by reaction of a compound of Formula II wherein X is -O- attached to Y which with Z is and an amine HN(R 2 )R 3 or by reaction of a compound of Formula II wherein X is OH and Y and Z are H, and a compound of formula R 3 N=C(R 1 )B, where B is a reactive group. Pharmaceutical compositions in conventional forms for oral, rectal and parenteral administration and having psychostimulant, anorexigenic and spasmolytic action as well as being useful in treating epilepsy comprise an above novel compound on salt and a carrier diluent or excipient.