Substituted 4-phenylaminothiazoles, their process of preparation and the pharmaceutical compositions containing them

US5880135A · kind A · utility

Assignee

• Sanofi · FR

Inventors

• Danielle Gully · Saubens, FR
• Pierre Roger · Limoges, FR
• Camille G. Wermuth · Strasbourg, FR

Key dates

• Filing date: Dec 22, 1997
• Grant date: Mar 9, 1999
• Expiry date: Dec 22, 2017

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D277/42
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A compound, as well as its stereoisomers and addition salts, possssing antagonist activity with respect to corticotropin releasing hormone (CRF) has the formula: ##STR1## in which R.sub.1, and R.sub.21 which are identical or different, are independently selected from a halogen atom; a (C.sub.1 -C.sub.5)hydroxyalkyl radical; a (C.sub.1 -C.sub.5)alkyl; a (C.sub.7 -C.sub.10)aralkyl; a (C.sub.1 -C.sub.5)alkoxy; a trifluoromethyl; a nitro; a nitrile; an --SR group in which R is selected from hydrogen, a (C.sub.1 -C.sub.5)alkyl radical and a (C.sub.7 -C.sub.10)aralkyl radical; an --S--CO--R group in which R is selected from a (C.sub.1 -C.sub.5)alkyl radical and an aralkyl radical in which the aryl part is (C.sub.6 -C.sub.8) and the alkyl part is (C.sub.1 -C.sub.4); a --COOR' group in which R' is selected from hydrogen and a (C.sub.1 -C.sub.5)alkyl; a --CONR--R'R" group with R' and R" as defined above for R'; an --NR'R" group with R' and R" as defined above for R'; a --CONRaRb or --NRaRb group in which Ra and Rb constitute, with the nitrogen atom to which they are bonded, a 5- to 7-membered heterocycle; and an --NHCO--NR'R" group with R' and R" as defined above for R'; R.sub.3 represents …