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Therapeutic process with diphosphonate compounds

Assignee: Symphar SA
•
Filing: 1980-11-18
•
Granted: 1983-02-01
•
Expires: 2000-11-18
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Abstract

Abstract A method of increasing the quantity of circulating high density lipoproteins and clearing cholesterol from certain tissues, comprising administering to a human an effective amount of a compound of the formula ##STR1## where X is H, OH, ##STR2## or NH 2 ; R and R' identical or different are H, CH 3 or C 2 H 5 ; m is zero or 1; and A is selected from the group comprising (CH 3 ) 3 C--, Y--C 6 H 4 --, Y--C 6 H 4 --O--C(CH 3 ) 2 --, Y--C 6 H 4 --C(CH 3 ) 2 --, Y--C 6 H 4 --C(O)--C 6 H 4 --, Y--C 6 H 4 --(CH 2 ) n -- and Y--C 6 H 4 --O--(CH 2 ) n --, where n is an integer from 1 to 6 and Y is H, CH 3 , OCH 3 or Cl. The present invention is a division of our copending application Ser. No. 114,423, filed Jan. 22, 1980, now U.S. Pat. No. 4,309,364.

Inventors

  • 👤 Craig L. Bentzen
  • 👤 Lan Nguyen Mong
  • 👤 Eric Niesor

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-08 11:45
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/38; C07F9/40; C07F9/4003; C07F9/4056; A; A61; A61K; A61K31/00; A61K31/66; C07F9/3804; C07F9/3808; C07F9/3839; C07F9/3882; C07F9/4006; C07F9/4025

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 110 words
A method of increasing the quantity of circulating high density lipoproteins and clearing cholesterol from various tissues, in humans, comprising administering to a human an amount effective to increase the quantity of circulating high density lipoproteins and to clear cholesterol from various tissues, of a diphosphonate compound of ##STR32## where X is H, OH, ##STR33## or NH 2 ; R and R' identical or different are H, CH 3 or C 2 H 5 ; m is zero or 1; and A is selected from the group consisting of ##STR34## where n is an integer from 1 to 6 and Y is H, CH 3 , OCH 3 or Cl.
Claim 2
Independent Claim 110 words
A method of increasing the quantity of circulating high density lipoproteins and clearing cholesterol from various tissues, in humans, comprising administering to a human an amount effective to increase the quantity of circulating high density lipoproteins and to clear cholesterol from various tissues, of a diphosphonate compound of ##STR32## where X is H, OH, ##STR33## or NH 2 ; R and R' identical or different are H, CH 3 or C 2 H 5 ; m is zero or 1; and A is selected from the group consisting of ##STR34## where n is an integer from 1 to 6 and Y is H, CH 3 , OCH 3 or Cl.
Claim 3
Dependent Claim 26 words
A method according to claim 1, in which said compound is of formula (Ia) ##STR35## where R, R' and A are as defined in claim 1.
Claim 4
Dependent Claim 26 words
A method according to claim 1, in which said compound is of formula (Ib) ##STR36## where R, R' and A are as defined in claim 1.
Claim 5
Dependent Claim 26 words
A method according to claim 1, in which said compound is of formula (Ic) ##STR37## where R, R' and A are as defined in claim 1.
Claim 6
Dependent Claim 18 words
A method according to claim 1 in which Y is H or a chlorine atom in para position.
Claim 7
Dependent Claim 15 words
A method according to claim 1, in which said compound is tetramethyl 1(p-chlorophenyl)methane 1-hydroxy 1-1-diphosphonate.
Claim 8
Dependent Claim 15 words
A method according to claim 1, in which said compound is tetramethyl 2-2-dimethyl 2-(p-chlorophenoxy)ethane 1-hydroxy-1,1-diphosphonate.
Claim 9
Dependent Claim 15 words
A method according to claim 1, in which said compound is tetramethyl 1-[4(4'-chlorobenzoyl)phenyl]-methane 1-hydroxy 1,1-diphosphonate.
Claim 10
Dependent Claim 13 words
A method according to claim 1, in which said compound is dimethyl 1[(dimethoxyphosphinyl)p-chlorobenzyl]-phosphate.
Claim 11
Dependent Claim 16 words
A method according to claim 1, in which said compound is dimethyl [1(dimethoxyphosphinyl) 2,2-dimethyl 2-phenyl]-ethyl phosphate.
Claim 12
Dependent Claim 15 words
A method according to claim 1, in which said compound is dimethyl [1(dimethoxyphosphinyl)2,2-dimethyl 2(p-chlorophenyl]ethyl phosphate.
Claim 13
Dependent Claim 14 words
A method according to claim 1, in which said compound is tetraethyl 4-phenylbutylidene 1,1-diphosphonate.
Claim 14
Dependent Claim 14 words
A method according to claim 1, in which said compound is 4-phenylbutylidene 1,1-diphosphonic acid.
Claim 15
Dependent Claim 14 words
A method according to claim 1, in which said compound is tetramethyl 4-phenylbutylidene 1,1-diphosphonate.

References Cited (Backward Citations)

US2848475A Cited
US3299123A Cited
US3471406A Cited
US4067971A Cited
US4237165A Cited
US4113862A Cited
US4309364A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1986-01-31 1986-08-02 1987-02-01 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1990-01-31 1990-08-02 1991-02-01 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1994-01-31 1994-08-02 1995-02-01 $7700.00 Window Closed / Lapsed

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