Process for the manufacture of novel substituted...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/547 (2006.01) A61K 31/41 (2006.01) C07F 9/6506 (2006.01) C07F 9/6524 (2006.01) C07F 9/653 (2006.01) C07F 9/6539 (2006.01) C07F 9/6541 (2006.01)

Patent

CA 1324383

Process for the manufacture of novel substituted aminomethanediphosphonic acids Abstract Heteroarylaminomethanediphosphonic acids of the formula Image (I) in which R1 represents an optionally benzo- or cyclohexeno-fused 5-membered heteroaryl radical that contains, as hetero atom(s), either from 2 to 4 N-atoms or 1 or 2 N-atoms as well as 1 O-atom or S-atom and that is unsubstituted or is substituted by lower alkyl; by phenyl that is unsubstituted or is substituted by lower alkyl, lower alkoxy and/or by halogen; by lower alkoxy; by hydroxy; by di-lower alkylamino; by lower alkylthio and/or by halogen; and R2 represents hydrogen or lower alkyl, and their salts, have a regulatory action on the calcium metabolism and can be used as active ingredients in medicaments for the treatment of illnesses that can be attributed to disorders of the calcium metabolism. They are manufactured, for example, as follows: in a compound of the formula Image (II) in which X1 represents a functionally modified phosphono group X and X2 represents phosphono or similarly represents a functionally modified phosphono group X, the group(s) X is(are) converted into free phosphono.

552085

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