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US4309364A Expired / Lapsed US ⏱️ 0.0 years remaining

Diphosphonates

Assignee: Symphar SA
•
Filing: 1980-01-22
•
Granted: 1982-01-05
•
Expires: 2000-01-22
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Abstract

Abstract This invention relates to new diphosphonate compounds of formula (I) ##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 --CO--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. These compounds possess remarkable activity as hypoglycemic and/or antiatherogenic agents, and are usable in pharmaceutical compositions to alter lipoprotein profiles in favor of high density lipoproteins and to clear cholesterol from various tissues.

Inventors

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

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-01 15:24
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: 12
Claim 1
Independent Claim 50 words
Diphosphonate methyl esters represented by general formula (I) ##STR44## where X is H or OH, R is CH 3 , m is zero or 1, and A is selected from the group comprising ##STR45## where n is integer from 1 to 6 and Y is H, CH 3 or Cl.
Claim 2
Dependent Claim 50 words
Diphosphonate methyl esters represented by general formula (I) ##STR44## where X is H or OH, R is CH 3 , m is zero or 1, and A is selected from the group comprising ##STR45## where n is integer from 1 to 6 and Y is H, CH 3 or Cl.
Claim 3
Dependent Claim 21 words
Hydroxydiphosphonate methyl esters of formula (Ia) according to claim 1, ##STR46## where R, and A are as defined in claim 1.
Claim 4
Dependent Claim 21 words
Phosphonophosphate methyl esters of formula (Ib) according to claim 1, ##STR47## where R, and A are as defined in claim 1.
Claim 5
Dependent Claim 21 words
Diphosphonate methyl esters of formula (Ic) according to claim 1 ##STR48## where R, and A are as defined in claim 1.
Claim 6
Dependent Claim 8 words
Tetramethyl 1(p-chlorophenyl)methane 1-hydroxy 1-1-diphosphonate according to claim 1.
Claim 7
Dependent Claim 8 words
Tetramethyl 2,2-dimethyl 2-(p-chlorophenoxy)ethane 1-hydroxy-1,1-diphosphonate according to claim 1.
Claim 8
Dependent Claim 8 words
Tetramethyl 1-[4(4'-chlorobenzoyl)phenyl]-methane 1-hydroxy 1,1-diphosphonate according to claim 1.
Claim 9
Dependent Claim 6 words
Dimethyl 1[(dimethoxyphosphinyl)p-chlorobenzyl]phosphate according to claim 1.
Claim 10
Dependent Claim 9 words
Dimethyl [1(dimethoxyphosphinyl) 2,2-dimethyl 2-phenyl]-ethyl phosphate according to claim 1.
Claim 11
Dependent Claim 9 words
Dimethyl [1(dimethoxyphosphinyl)2,2-dimethyl 2(p-chlorophenyl] ethyl phosphate according to claim 1.
Claim 12
Dependent Claim 7 words
Tetramethyl 4-phenylbutylidene, 1,1-diphosphonate according to claim 1.

References Cited (Backward Citations)

US2848475A Cited
FR1394386A Cited
US3299123A Cited
US3471406A Cited
US3463835A Cited
FR8441M Cited
US4067971A Cited
US4137309A Cited
US4113861A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1985-01-04 1985-07-06 1986-01-05 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1989-01-04 1989-07-06 1990-01-05 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1993-01-04 1993-07-06 1994-01-05 $7700.00 Window Closed / Lapsed

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