Claims
- 1. A methylenediphosphonic acid derivative of the formula: ##STR32## wherein: R.sub.1 represents C.sub.5 -C.sub.7 cycloalkyl, phenyl unsubstituted or monosubstituted or polysubstituted by a member selected from amongst halogen, C.sub.1 -C.sub.6 alkyl or trifluoromethyl; or pyridyl
- Alk denotes linear or branched C.sub.1 -C.sub.6 alkylene;
- R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl or --CONH.sub.2 ;
- R.sub.3 represents hydrogen, C.sub.1 -C.sub.6 alkyl, benzyl or phenyl unsubstituted or substituted by a member selected from amongst chlorine or methyl;
- R.sub.2 and R.sub.3, taken together, represent (CH.sub.2).sub.m, in which m is 4 or 5; and
- n is 0, 1 or 2;
- and salts thereof with pharmaceutically acceptable inorganic or organic bases.
- 2. A methylenediphosphonic acid derivative according to claim 1, wherein R.sub.1 is p-chlorophenyl, Alk is (CH.sub.2).sub.3, R.sub.2 is H and R.sub.3 is benzyl.
- 3. A methylenediphosphonic acid derivative of the formula: ##STR33## wherein: R.sub.1 represents C.sub.1 -C.sub.6 alkyl;
- Alk denotes linear or branched C.sub.1 -C.sub.6 alkylene;
- R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl or --CONH.sub.2 ;
- R.sub.3 represents hydrogen, C.sub.1 -C.sub.6 alkyl, benzyl or phenyl unsubstituted or substituted by a member selected from amongst chlorine or methyl;
- R.sub.2 and R.sub.3, taken together, represents (CH.sub.2).sub.m, in which m is 4 or 5; and
- n is 1;
- and salts thereof with pharmaceutically acceptable inorganic or organic bases.
- 4. A method for the treatment of rheumatism or rheumatoid polyarthritis which comprises administering to an animal in need thereof an antirheumatic effective amount of methylenediphosphonic acid derivative of the formula: ##STR34## wherein: R.sub.1 represents C.sub.1 -C.sub.6 alkyl or C.sub.5 -C.sub.7 cycloalkyl; or R.sub.1 represents phenyl unsubstituted or monosubstituted or polysubstituted by halogen, C.sub.1 -C.sub.6 alkyl or trifluoromethyl, or pyridal;
- Alk denotes linear or branched C.sub.1 -C.sub.6 alkylene;
- R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl or --CONH.sub.2 ;
- R.sub.3 represents hydrogen, C.sub.1 -C.sub.6 alkyl, benzyl or phenyl unsubstituted or substituted by a member selected from amongst chlorine or methyl;
- R.sub.2 and R.sub.3, taken together, represents (CH.sub.2).sub.m, in which m is 4 or 5; and
- n is 0, 1 or 2;
- and salts thereof with pharmaceutically acceptable inorganic or organic bases.
- 5. A pharmaceutical composition having an antirheumatic action, which comprises, as the active ingredient, a methylenediphosphonic acid derivative of the formula: ##STR35## wherein: R.sub.1 represents C.sub.5 -C.sub.7 cycloalkyl, phenyl unsubstituted or monosubstituted or polysubstituted by halogen, C.sub.1 -C.sub.6 alkyl or trifluoromethyl, or pyridyl;
- Alk denotes linear or branched C.sub.1 -C.sub.6 alkylene;
- R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl or --CONH.sub.2 ;
- R.sub.3 represents hydrogen, C.sub.1 -C.sub.6 alkyl, benzyl or phenyl unsubstituted or substituted by a member selected from amongst chlorine or methyl;
- R.sub.2 and R.sub.3, taken together, represents (CH.sub.2).sub.m, in which m is 4 or 5; and
- n is 0, 1 or 2;
- or one of the pharmaceutically acceptable salts of the said derivative with organic or inorganic bases, in association with a pharmaceutically acceptable vehicle.
- 6. A composition as claimed in claim 5, having 10 to 500 mg of active ingredient.
- 7. A pharmaceutical composition having an antirheumatic action, which comprises as the active ingredient, and effective amount of a methylenediphosphonic acid derivative of the formula: ##STR36## wherein: R.sub.1 represents C.sub.1 -C.sub.6 alkyl;
- Alk denotes linear or branched C.sub.1 -C.sub.6 alkylene;
- R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl or --CONH.sub.2 ;
- R.sub.3 represents hydrogen, C.sub.1 -C.sub.6 alkyl, benzyl or phenyl unsubstituted or substituted by a member selected from amongst chlorine or methyl;
- R.sub.2 and R.sub.3, taken together, represents (CH.sub.2).sub.m, in which m is 4 or 5; and
- n is 1;
- or one of the pharmaceutically acceptable salts of the said derivative with organic or inorganic bases; in association with a pharmaceutically acceptable vehicle.
- 8. A composition as claimed in claim 7, having 10 to 500 mg of active ingredient.
Priority Claims (1)
Number |
Date |
Country |
Kind |
8401214 |
Jan 1984 |
FRX |
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Parent Case Info
This application is a continuation of application Ser. No. 919,571, filed Oct. 15, 1986, abandoned, which in turn is a continuation of application Ser. No. 691,893, filed Jan. 16, 1985, now abandoned.
US Referenced Citations (4)
Number |
Name |
Date |
Kind |
3846420 |
Wollmann et al. |
Nov 1974 |
|
3962432 |
Schmidt-Dunker |
Jun 1976 |
|
4006182 |
Ploger et al. |
Feb 1977 |
|
4100167 |
Selvarajan et al. |
Jul 1978 |
|
Foreign Referenced Citations (3)
Number |
Date |
Country |
0015370 |
Sep 1980 |
EPX |
0098567 |
Jan 1984 |
EPX |
2754821 |
Jun 1979 |
DEX |
Continuations (2)
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Number |
Date |
Country |
Parent |
919571 |
Oct 1986 |
|
Parent |
691893 |
Jan 1985 |
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