Methylenebisphosphonic acid derivatives

US5442101A · kind A · utility

Assignee

• Leiras Oy · FI

Inventors

• Hannu Hanhijarvi · Turku, FI
• Heikki Nupponen · Kangasala, FI
• Jouko Vepsalainen · Tampere, FI
• Esko Pohjala · Tampere, FI

Key dates

• Filing date: Oct 20, 1993
• Grant date: Aug 15, 1995
• Expiry date: Oct 20, 2013

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07F9/4423
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to novel methylenebisphosphonic acid ester amide derivatives of general formula (I), in which formula W.sup.1, W.sup.2, W.sup.3 and W.sup.4 are independently the group OR.sup.1 or the group NR.sup.2 R.sup.3 wherein R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen or straight or branched, optionally unsaturated C.sub.1 -C.sub.22 -alkyl, optionally substituted, optionally unsaturated C.sub.3 -C.sub.10 -cycloalkyl, aryl, aralkyl or silyl SiR.sub.3, or the groups R.sup.2 and R.sup.3 form together with the adjacent nitrogen atom a 3 to 10-membered saturated, partly saturated or aromatic heterocyclic ring, wherein in addition to the nitrogen atom, there may be one or two heteroatoms from the group N, O and S, provided that in formula (I) at least one of the groups W.sup.1, W.sup.2, W.sup.3 and W.sup.4 is hydroxy and at least one of the groups W.sup.1, W.sup.2, W.sup.3 and W.sup.4 is amino group NR.sup.2 R.sup.3, Q.sup.1 and Q.sup.2 are independently hydrogen, fluorine, chlorine, bromine or iodine, including the stereoisomers, such as the geometrical isomers and the optically active isomers, of the compounds, as well as the pharmacologically acceptable salts o…