The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Apr. 20, 1993

Filed:

Sep. 25, 1991
Applicant:
Inventors:

Wolfgang Frostl, Basel, CH;

Knut A Jaeggi, Basel, CH;

Assignee:

Ciba-Geigy Corporation, Ardsley, NY (US);

Attorneys:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K / ; C07F / ;
U.S. Cl.
CPC ...
514 96 ; 514100 ; 549-5 ; 549-6 ; 549-7 ; 549220 ;
Abstract

Benzoheterocyclylalkylaminoalkanediphosphonic acids of formula I ##STR1## wherein R.sub.1 and R.sub.2, independently of one another, are hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, R.sub.3 is hydrogen or lower alkyl, X and Y, independently of one another, are oxy or thio, alk.sub.1 and alk.sub.2 are identical or different lower alkylene radicals, n is 0 or 1 and m and m', independently of one another, are 0, 1 or 2, the sum of n, m and m' being 1, 2 or 3, and their salts exhibit a pronounced regulatory action on the calcium metabolism of warm-blooded animals. They are prepared, for example, as follows: in a compound of the formula ##STR2## wherein R.sub.1, R.sub.2, n, m, m', X, Y, alk.sub.1 and alk.sub.2 are as defined above, R'.sub.3 is one of the groups R.sub.3 mentioned above or is an amino-protecting group R.sub.0, Z.sub.1 is a functionally modified phosphono group, and Z.sub.2 is a free or functionally modified phosphono group, converting functionally modified phosphono Z.sub.1 and, where appropriate, Z.sub.2 into the free phosphono group, and, if desired, converting a resulting compound into a different compound of formula I, separating a mixture of isomers obtainable in accordance with the process into the components and separating the preferred isomer, and/or converting a free compound obtainable in accordance with the process into a salt or converting a salt obtainable in accordance with the process into the corresponding free compound.


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