Phosphosuccinic acid derivatives, processes for the production t

Details Phosphosuccinic acid derivatives, processes for the production t Phosphosuccinic acid derivatives, processes for the production t

1995-12-18

1997-11-04

Haley, Jacqueline

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

562 24, A61K 3166, A61K 3119, C07C 5510

Patent

active

056839944

DESCRIPTION:

BRIEF SUMMARY
This is a National Stage application of PCT/EP94/09180 filed Jun. 17, 1994 and published as WO 95/00522 on Jan. 5, 1995
The present invention concerns new phosphonosuccinic acid derivatives, processes for the production thereof as well as pharmaceutical agents containing these substances.
It has been found that phosphonosuccinic acid derivatives of the present invention exhibit an excellent action on calcium metabolism and thus are suitable for treating disturbances of calcium metabolism. They can above all be used when bone formation and bone degradation are disturbed, i.e. they are suitable for treating diseases of the skeletal system such as e.g. osteoporosis, Morbus Paget, Morbus Bechterew and others.
Due to these properties they can also be used in urolithiasis therapy and for the prevention of heterotopic ossification. Furthermore they form the basis for treating rheumatoid arthritis, osteoarthritis and degenerative arthrosis through their influence on calcium metabolism.
The present invention concerns compounds of the general formula I, ##STR2## in which R.sup.1, R.sup.2 can be, independently of each other hydrogen, lower alkyl, cycloalkyl or arylmethyl, or one of the groups OR.sup.6 or NR.sup.7 R.sup.8 or, together with the atoms to which they are bound, can form a five- to seven-membered carbocyclic ring or a heterocyclic ring containing one to two heteroatoms, arylalkyl, bicyclic aryl, biaryl or a group of formulae a) or b) or, together with R.sup.4 and the carbon atom to which it is bound, forms a five- to seven-membered carbocyclic or heterocyclic ring which can be substituted if desired, ##STR3## R.sup.6 denotes hydrogen, lower alkyl or arylmethyl, R.sup.7, R.sup.8 denote, independently of each other, hydrogen or lower alkyl or, together with the nitrogen atom to which they are bound, form a five- to six-membered heterocyclic ring, cycloalkenyl, monocyclic or bicyclic aryl, biaryl, alkylene chain with 2-6 carbon atoms, wherein in the case that hydrogen, R.sup.5 may not be hydrogen, hydroxy, methoxy, c.sub.1 -C.sub.3 alkyl or aryl, or NR.sup.7 R.sup.8 alk may not be a valency dash.
Phosphonosuccinic acid derivatives of formula I have already been described in DE-A-23 60 797 in which R.sup.3 denotes hydrogen or C.sub.1 -C.sub.3 alkyl, R.sup.4 denotes hydrogen and R.sup.5 denotes hydrogen or C.sub.1 -C.sub.3 alkyl for influencing the deposition and dissolution of sparingly soluble calcium salts.
Additional compounds of formula I are described in the following chemical abstracts without information on a possible use as pharmaceutical agents: .dbd.OCH.sub.3 in CA, 105(5):42932.times. and CA, 104(1):5939. may be substituted in CA 115(23):255757 n and CA106 (21):176504 p.
Lower alkyl should in all cases denote a straight-chained or branched C.sub.1 -C.sub.6 alkyl group such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, pentyl or hexyl, in particular methyl, ethyl, propyl, isobutyl and pentyl.
Lower alkenyl denotes unsaturated residues with 3-6 carbon atoms such as e.g. allyl, but-2-enyl, hexy-2,4-dienyl, above all allyl.
Cycloalkyl denotes a 3-7-membered ring which may be substituted if desired such as a cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl ring, in particular a cyclopropyl, cyclopentyl and cyclohexyl ring. These cycloalkyl residues can be substituted once or twice by C.sub.1 -C.sub.6 alkyl groups, preferably a methyl, ethyl or isopropyl group as well as by hydroxy, methoxy, benzyloxy, amino, methylamino, dimethylamino, benzylamino groups or by chlorine or bromine.
Cycloalkenyl denotes a cyclopentenyl, cyclohexenyl or cycloheptenyl ring which may be substituted if desired. These rings can be substituted once or twice by a C.sub.1 -C.sub.6 alkyl group preferably a methyl, ethyl or isopropyl group as well as by chlorine, bromine or hydroxy, methoxy, benzyloxy, amino, methylamino, dimethylamino or benzyl-amino groups.
If the residues R.sup.3 and R.sup.4 together with the carbon atoms to which they are bound form a carbocyclic or heterocyclic ring, this is a saturated o

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