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Phenylacetate anti-inflammatory composition

Assignee: Procter and Gamble Co
•
Filing: 1979-10-22
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Granted: 1981-08-04
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Expires: 1999-10-22
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Abstract

Abstract The anti-inflammatory activity of fenoprofen, ketoprofen, MK-830 and other phenylacetic acid-based anti-inflammatory drugs is enhanced by administration thereof in conjunction with a phosphonate compound such as EHDP or Cl2MDP.

Inventors

  • 👤 Lawrence Flora
  • 👤 Marion D. Francis

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-27 11:08
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/66

Claims Analysis

Total Claims: 21
Claim 1
Independent Claim 172 words
An anti-inflammatory composition, comprising: (1) from about 10 mg to about 500 mg of a phenylacetic acid-based compound selected from the group consisting of fenoprofen, ketoprofen, MK-830 having the formula ##STR5## and pharmaceutically-acceptable salts and esters thereof; and (2) from about 50 mg. to about 250 mg. of an organophosphonate compound selected from the group consisting of geminal organophosphonates of the formula ##STR6## or pharmaceutically acceptable salts thereof, wherein n is an integer from 1 to about 10; R 3 is selected from the group consisting of H, --CH 2 OH, C 1 -C 20 alkyl or cycloalkyl, C 2 -C 20 alkenyl, aryl, phenylethyl, benzyl, halogen, amino, substituted amino, --CH 2 COOH, --CH 2 PO 3 H 2 , --CH(PO 3 H 2 ) (OH) or --CH 2 CH(PO 3 H 2 ) 2 ; and R 4 is selected from the group consisting of H, lower alkyl, amino, benzyl, halogen, --OH, --CH 2 COOH, --CH 2 PO 3 H 2 or --CH 2 CH 2 PO 3 H 2 .
Claim 2
Dependent Claim 172 words
An anti-inflammatory composition, comprising: (1) from about 10 mg to about 500 mg of a phenylacetic acid-based compound selected from the group consisting of fenoprofen, ketoprofen, MK-830 having the formula ##STR5## and pharmaceutically-acceptable salts and esters thereof; and (2) from about 50 mg. to about 250 mg. of an organophosphonate compound selected from the group consisting of geminal organophosphonates of the formula ##STR6## or pharmaceutically acceptable salts thereof, wherein n is an integer from 1 to about 10; R 3 is selected from the group consisting of H, --CH 2 OH, C 1 -C 20 alkyl or cycloalkyl, C 2 -C 20 alkenyl, aryl, phenylethyl, benzyl, halogen, amino, substituted amino, --CH 2 COOH, --CH 2 PO 3 H 2 , --CH(PO 3 H 2 ) (OH) or --CH 2 CH(PO 3 H 2 ) 2 ; and R 4 is selected from the group consisting of H, lower alkyl, amino, benzyl, halogen, --OH, --CH 2 COOH, --CH 2 PO 3 H 2 or --CH 2 CH 2 PO 3 H 2 .
Claim 3
Dependent Claim 32 words
A composition according to claim 1 wherein the organophosphonate compound is a member selected from the group consisting of ethane-1-hydroxy-1,1-diphosphonic acid, dichloromethanediphosphonic acid, methanediphosphonic acid, and the pharmaceutically-acceptable salts and esters thereof.
Claim 4
Dependent Claim 41 words
A composition according to claim 1, comprising a safe and effective amount of a member selected from the group consisting of fenoprofen, ketoprofen, and MK-830, and a safe and effective amount of dichloromethanediphosphonic acid, or the pharmaceutically-acceptable salts or esters thereof.
Claim 5
Dependent Claim 48 words
A composition according to claim 3 in unit dosage form, comprising: from about 10 mg to about 500 mg of a member selected from the group consisting of fenoprofen and ketoprofen; and from about 50 mg to about 250 mg of dichloromethanediphosphonic acid, or a pharmaceutically-acceptable salt thereof.
Claim 6
Dependent Claim 39 words
A composition according to claim 1, comprising a safe and effective amount of a member selected from the group consisting of fenoprofen, ketoprofen, and MK-830, and a safe and effective amount of ethane-1-hydroxy-1,1-diphosphonic acid, or the pharmaceutically-acceptable salts thereof.
Claim 7
Dependent Claim 48 words
A composition according to claim 5 in unit dosage form comprising: from about 10 mg to about 500 mg of a member selected from the group consisting of fenoprofen and ketoprofen; and from about 50 mg to about 250 mg of ethane-1-hydroxy-1,1-diphosphonic acid, or the pharmaceutically-acceptable salts thereof.
Claim 8
Dependent Claim 39 words
A composition according to claim 1 comprising a safe and effective amount of a member selected from the group consisting of fenoprofen, ketoprofen, and MK-830, and a safe and effective amount of methanediphosphonic acid, or the pharmaceutically-acceptable salts thereof.
Claim 9
Dependent Claim 48 words
A composition according to claim 7 in unit dosage form, comprising: from about 10 mg to about 500 mg of a member selected from the group consisting of fenoprofen and ketoprofen; and from about 50 mg to about 250 mg of methanediphosphonic acid, or a pharmaceutically-acceptable salt thereof.
Claim 10
Dependent Claim 15 words
A composition according to claim 1 or 4 wherein the phenylacetic acid-based compound is fenoprofen.
Claim 11
Independent Claim 194 words
A method for treating or preventing pain and inflammation in animal tissues, comprising administering to an animal in need of such treatment: (1) from about 50 mg to about 6000 mg per day of a phenylacetic acid-based compound selected from the group consisting of fenoprofen, ketoprofen, MK-830 having the formula ##STR7## and pharmaceutically-acceptable salts and esters thereof; and (2) from about 200 mg to about 2000 mg per day of an organophosphonate compound selected from the group consisting of geminal organophosphonates of the formula ##STR8## or pharmaceutically acceptable salts thereof, wherein n is an integer from 1 to about 10; R 3 is selected from the group consisting of H, --CH 2 OH, C 1 -C 20 alkyl or cycloalkyl, C 2 -C 20 alkenyl, aryl, phenylethyl, benzyl, halogen, amino, substituted amino, --CH 2 COOH, --CH 2 PO 3 H 2 , --CH(PO 3 H 2 ) (OH) or --CH 2 CH(PO 3 H 2 ) 2 ; and R 4 is selected from the group consisting of H, lower alkyl, amino, benzyl, halogen, --OH, --CH 2 COOH, --CH 2 PO 3 H 2 or --CH 2 CH 2 PO 3 H 2 .
Claim 12
Independent Claim 194 words
A method for treating or preventing pain and inflammation in animal tissues, comprising administering to an animal in need of such treatment: (1) from about 50 mg to about 6000 mg per day of a phenylacetic acid-based compound selected from the group consisting of fenoprofen, ketoprofen, MK-830 having the formula ##STR7## and pharmaceutically-acceptable salts and esters thereof; and (2) from about 200 mg to about 2000 mg per day of an organophosphonate compound selected from the group consisting of geminal organophosphonates of the formula ##STR8## or pharmaceutically acceptable salts thereof, wherein n is an integer from 1 to about 10; R 3 is selected from the group consisting of H, --CH 2 OH, C 1 -C 20 alkyl or cycloalkyl, C 2 -C 20 alkenyl, aryl, phenylethyl, benzyl, halogen, amino, substituted amino, --CH 2 COOH, --CH 2 PO 3 H 2 , --CH(PO 3 H 2 ) (OH) or --CH 2 CH(PO 3 H 2 ) 2 ; and R 4 is selected from the group consisting of H, lower alkyl, amino, benzyl, halogen, --OH, --CH 2 COOH, --CH 2 PO 3 H 2 or --CH 2 CH 2 PO 3 H 2 .
Claim 13
Dependent Claim 32 words
A method according to claim 10 wherein the organophosphonate compound is a member selected from the group consisting of ethane-1-hydroxy-1,1-diphosphonic acid, dichloromethanediphosphonic acid, methanediphosphonic acid, and the pharmaceutically-acceptable salts and esters thereof.
Claim 14
Dependent Claim 12 words
A method according to claim 10 wherein the animal is a human.
Claim 15
Dependent Claim 33 words
A method according to claim 12 which employs a safe and effective amount of fenoprofen or ketoprofen and a safe and effective amount of dichloromethanediphosphonic acid, or the pharmaceutically-acceptable salts or esters thereof.
Claim 16
Dependent Claim 41 words
A method according to claim 13 which employs: from about 50 mg to about 6000 mg of fenoprofen or ketoprofen per day; and from about 200 mg to about 2000 mg of dichloromethanediphosphonic acid, or a pharmaceutically-acceptable salt thereof, per day.
Claim 17
Dependent Claim 33 words
A method according to claim 12 which employs a safe and effective amount of fenoprofen or ketoprofen and a safe and effective amount of ethane-1-hydroxy-1,1-diphosphonic acid, or the pharmaceutically-acceptable salts or esters thereof.
Claim 18
Dependent Claim 41 words
A method according to claim 15 which employs: from about 50 mg to about 6000 mg of fenoprofen or ketoprofen per day; and from about 200 mg to about 2000 mg of ethane-1-hydroxy-1,1-diphosphonic acid, or a pharmaceutically-acceptable salt thereof, per day.
Claim 19
Dependent Claim 33 words
A method according to claim 12 which employs a safe and effective amount of fenoprofen or ketoprofen and a safe and effective amount of methanediphosphonic acid, or the pharmaceutically-acceptable salts or esters thereof.
Claim 20
Dependent Claim 41 words
A method according to claim 17 which employs: from about 50 mg to about 6000 mg of fenoprofen or ketoprofen per day; and from about 200 mg to about 2000 mg of methanediphosphonic acid, or a pharmacutically-acceptable salt thereof, per day.
Claim 21
Dependent Claim 16 words
A method according to claim 10 or 14 which employs fenoprofen as the phenylacetic acid-based compound.

References Cited (Backward Citations)

US3553314A Cited
US3584125A Cited
US3553315A Cited
US3584124A Cited
US3678164A Cited
US3641246A Cited
US3662066A Cited
US3683080A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1984-08-03 1985-02-02 1985-08-04 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1988-08-03 1989-02-02 1989-08-04 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1992-08-03 1993-02-02 1993-08-04 $7700.00 Window Closed / Lapsed

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