Guanidinoalkyl-1,1-bisphosphonic acid derivatives, process for t

Details Guanidinoalkyl-1,1-bisphosphonic acid derivatives, process for t Guanidinoalkyl-1,1-bisphosphonic acid derivatives, process for t

1992-12-10

1994-03-15

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Phosphorus containing other than solely as part of an...

514 80, 548113, 558157, 558158, 558159, 562 13, A61K 3166, A61K 31675, C07F 940, C07F 938, C07F 96506

Patent

active

052946088

ABSTRACT:
The invention describes tautomeric compounds of the formula Ia, Ib or Ic ##STR1## and/or their physiologically tolerable salts, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are a hydrogen atom, substituted (C.sub.1 -C.sub.7)-alkyl, (C.sub.3 -C.sub.10)-cycloalkyl, substituted phenyl or (C.sub.1 -C.sub.4)-alkylphenyl, R.sup.2 is substituted phosphoric acid, R.sup.2 and R.sup.3, R.sup.2 and R.sup.5 or R.sup.4 and R.sup.5 form a monocyclic 5- to 7-membered saturated or unsaturated heterocyclic ring which is mono- or polysubstituted, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are a hydrogen atom or (C.sub.1 -C.sub.5)-alkyl, X is a hydrogen atom, hydroxyl or halogen, l and n are an integer from 0 to 7, m is an integer from 0 to 2, and the sum of the numbers l, m and n is less than or equal to 10, a process for the preparation of the compounds of the formula Ia, Ib or Ic, pharmaceuticals and their use for the prophylaxis or treatment of osteoporosis.

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patent: 5039669 (1991-08-01), Isomura et al.
Organische Phosphorverbindungen 75, Herstellung und Eigenschaften von Aminomethylendiphosphinaten und -diphosphonaten, RR.sup.1 NCH [P(O)R.sup.2 (OR.sup.3)].sub.2 und Derivaten: Ludwig Maier; Phosphorus and Sulfur 11:311-322 (1981).
The Synthesis of Stereochemically Pure Peptide Derivatives by the Phythaloyl Method, John C. Sheehan et al.; Am. Soc.; 74:3822-3825 (1951).
Amino Acids, V. Phthalyl Derivatives; John H. Billman et al.; Am. Soc.; 70:1473-1474 (1948).
Rechersches dans la serie des diuretiques sulfamides; A. Lespagnol et al.; Bull. Soc. Fra.; pp. 800-804; (1965).

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