4-Aminoquinoline derivatives

US3933829A · kind A · utility

Assignee

• John Wyeth & Brother Limited · GB

Inventors

• John L. Archibald
• John T. A. Boyle
• John Saunders

Key dates

• Filing date: Aug 22, 1974
• Grant date: Jan 20, 1976
• Expiry date: Aug 22, 1994

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D211/58
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The disclosure describes new 4-aminoquinoline derivatives of general formula ##SPC1## And their acid addition salts, where X is a halogen atom or a trifluoromethyl group, Z is a hydrogen atom or a defined substituent, R is group of the formula EQU --R.sub.3 N--A--NR.sub.1 R.sub.2 (II) EQU --nr.sub.1 n--r.sub.3 (iii a) Or EQU --N N NR.sub.1 R.sub.2 (III b) where A in formula II is a chain of 1 to 5 methylene groups which may be substituted with alkyl, the ring in formula IIIa and IIIb is a piperidine or pyrrolidine ring that may be substituted with alkyl and R.sub.1, R.sub.2 and R.sub.3 represent hydrogen or certain defined substituents. The new 4-aminoquinoline derivatives show anti-hypertensive activity and, in some cases, show one or more of the following activities: anti-malarial activity, anti-inflammatory activity, anti-trichomonal activity and inhibition of blood platelet aggregation. The present invention concerns new 4-aminoquinoline derivatives, a process for their preparation and pharmaceutical compositions containing them. The invention also concerns new intermediates useful for the preparation of the 4-aminoquinoline derivatives. The invention provides new 4-aminoquinol…