Claims
- 1. A pharmaceutical composition having anti-atherosclerotic activity by reducing tissue lipids and favorably altering plasma lipids, which comprises as active ingredient an antiatherosclerotically effective amount of a diphosphonate ester compound of the formula ##STR53## wherein X is H or OH; m is zero or 1, R is CH.sub.3 or C.sub.2 H.sub.5 but when m is zero and X is OH then R is only CH.sub.3 ; and A is selected from the group consisting of ##STR54## where n is an integer from 1 to 6 and Y is H, CH.sub.3, OCH.sub.3 or halogen, A being other than ##STR55## when m is zero, and a pharmaceutically acceptable excipient.
- 2. A composition according to claim 1, in which said compound is of the formula ##STR56## where R and A are as defined in claim 1.
- 3. A composition according to claim 1, in which said compound is of the formula ##STR57## where R and A are as defined in claim 1.
- 4. A composition according to claim 1, in which said compound is of the formula ##STR58## where R and A are as defined in claim 1.
- 5. A composition according to claim 1 in which Y is H or a chlorine atom in para position.
- 6. A composition according to claim 1, in which said compound is tetramethyl 2,2-dimethyl 2-(p-chlorophenoxy) ethane 1-hydroxy-1,1-diphosphonate.
- 7. A composition according to claim 1, in which said compound is tetramethyl 1-[4(4'-chlorobenzoyl)phenyl]-methane 1-hydroxy 1,1-diphosphonate.
- 8. A composition according to claim 1, in which said compound is dimethyl .alpha.(dimethoxyphosphinyl)p-chlorobenzyl phosphate.
- 9. A composition according to claim 1, in which said compound is dimethyl .alpha.(dimethoxyphosphinyl)p-fluorobenzyl phosphate.
- 10. A composition according to claim 1, in which said compound is dimethyl [1(dimethoxyphosphinyl) 2,2-dimethyl 2-phenyl]-ethyl phosphate.
- 11. A composition according to claim 1, in which said compound is dimethyl [1(dimethoxyphosphinyl) 2,2-dimethyl 2(p-chlorophenyl)] ethyl phosphate.
- 12. A composition according to claim 1, in which said compound is dimethyl [.alpha.-(dimethoxyphosphinyl) 4-(4'-chlorobenzoyl)] benzyl phosphate.
Priority Claims (2)
Number |
Date |
Country |
Kind |
794992 |
Feb 1979 |
GBX |
|
7933157 |
Sep 1979 |
GBX |
|
Parent Case Info
The present application is a continuation-in-part of application Ser. No. 114,423, filed Jan. 22, 1980, now U.S. Pat. No. 4,309,364.
US Referenced Citations (6)
Foreign Referenced Citations (4)
Number |
Date |
Country |
1394386 |
Apr 1964 |
FRX |
8441M |
Jun 1971 |
FRX |
777718 |
Jun 1957 |
GBX |
1026366 |
Apr 1966 |
GBX |
Non-Patent Literature Citations (3)
Entry |
Pudovik et al., Index Chemicus, vol. 28; Issue 216; 1968. |
Nicholson et al., J. Org. Chem., vol. 36; No. 24; 1971, pp. 3843-3845. |
Kosolapoff et al., Organic Phosphorus Compounds, vol. 7, Wiley Interscience, New York, 1976, pp. 267, 269 and 270. |
Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
114423 |
Jan 1980 |
|