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US4132788A Expired / Lapsed US ⏱️ 0.0 years remaining

Antiarthritic potentiation

Assignee: Janssen Pharmaceuticals Inc
•
Filing: 1977-12-19
•
Granted: 1979-01-02
•
Expires: 1997-12-19
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Abstract

Abstract The anti-inflammatory and antiarthritic properties of 5-aroyl-1-loweralkyl-pyrrole-2-acetic acid derivatives are potentiated by acetaminophen and aspirin.

Inventors

  • 👤 Stewart Wong

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-27 08:27
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/40; A61K31/60

Claims Analysis

Total Claims: 38
Claim 1
Independent Claim 139 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit: (1) from about 0.1 to about 1000 mg of a 5-aroyl-1-loweralkyl-pyrrole-2-acetic acid compound as the primary active agent, said compound being a member selected from the group having the formula: ##STR3## wherein R 3 is a member selected from the group consisting of hydrogen, loweralkyl and chloro, and Ar is a member selected from the group consisting of p-loweralkylphenyl and p-halophenyl, and the non-toxic therapeutically acceptable salts thereof; and (2) a compound selected from the group consisting of from about 150 to about 2000 mg of acetaminophen and from about 150 to about 1000 mg of aspirin as the potentiating agent; wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 2
Dependent Claim 139 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit: (1) from about 0.1 to about 1000 mg of a 5-aroyl-1-loweralkyl-pyrrole-2-acetic acid compound as the primary active agent, said compound being a member selected from the group having the formula: ##STR3## wherein R 3 is a member selected from the group consisting of hydrogen, loweralkyl and chloro, and Ar is a member selected from the group consisting of p-loweralkylphenyl and p-halophenyl, and the non-toxic therapeutically acceptable salts thereof; and (2) a compound selected from the group consisting of from about 150 to about 2000 mg of acetaminophen and from about 150 to about 1000 mg of aspirin as the potentiating agent; wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 3
Dependent Claim 139 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit: (1) from about 0.1 to about 1000 mg of a 5-aroyl-1-loweralkyl-pyrrole-2-acetic acid compound as the primary active agent, said compound being a member selected from the group having the formula: ##STR4## wherein R 3 is a member selected from the group consisting of hydrogen, methyl and chloro; and Ar is a member selected from the group consisting of p-methylphenyl and p-chlorophenyl; and the non-toxic therapeutically acceptable salts thereof; and (2) a compound selected from the group consisting of from about 150 to about 200 mg of acetaminophen and from about 150 to about 1000 mg of aspirin as the potentiating agent; wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 4
Dependent Claim 139 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit: (1) from about 0.1 to about 1000 mg of a 5-aroyl-1-loweralkyl-pyrrole-2-acetic acid compound as the primary active agent, said compound being a member selected from the group having the formula: ##STR4## wherein R 3 is a member selected from the group consisting of hydrogen, methyl and chloro; and Ar is a member selected from the group consisting of p-methylphenyl and p-chlorophenyl; and the non-toxic therapeutically acceptable salts thereof; and (2) a compound selected from the group consisting of from about 150 to about 200 mg of acetaminophen and from about 150 to about 1000 mg of aspirin as the potentiating agent; wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 5
Dependent Claim 15 words
A composition according to claim 2 in which the dosage unit form is a tablet.
Claim 6
Dependent Claim 15 words
A composition according to claim 2 in which the dosage unit form is a capsule.
Claim 7
Dependent Claim 99 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit from about 0.1 to about 1000 mg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary active agent and a compound selected from the group consisting of from about 150 to about 2000 mg of acetaminophen and from about 150 to about 1000 mg of aspirin as the potentiating agent, wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 8
Dependent Claim 99 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit from about 0.1 to about 1000 mg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary active agent and a compound selected from the group consisting of from about 150 to about 2000 mg of acetaminophen and from about 150 to about 1000 mg of aspirin as the potentiating agent, wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 9
Dependent Claim 99 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit from about 0.1 to about 1000 mg of a member selected from the group consisting of 5-p-chlorobenzoyl-1,4-dimethyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary active agent and a compound selected from the group consisting of from about 150 to about 2000 mg of acetaminophen and from about 150 to about 1000 mg of aspirin as the potentiating agent, wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 10
Dependent Claim 99 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit from about 0.1 to about 1000 mg of a member selected from the group consisting of 5-p-chlorobenzoyl-1,4-dimethyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary active agent and a compound selected from the group consisting of from about 150 to about 2000 mg of acetaminophen and from about 150 to about 1000 mg of aspirin as the potentiating agent, wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 11
Dependent Claim 99 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit from about 0.2 to about 500 mg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary active agent and a compound selected from the group consisting of from about 325 to about 1000 mg of acetaminophen and from about 325 to about 500 mg of aspirin as the potentiating agent, wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 12
Dependent Claim 99 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit from about 0.2 to about 500 mg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary active agent and a compound selected from the group consisting of from about 325 to about 1000 mg of acetaminophen and from about 325 to about 500 mg of aspirin as the potentiating agent, wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 13
Dependent Claim 99 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit from about 0.2 to about 500 mg of a member selected from the group consisting of 5-p-chlorobenzoyl-1,4-dimethyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary active agent and a compound selected from the group consisting of from about 325 to about 1000 mg of acetaminophen and from about 325 to about 500 mg of aspirin as the potentiating agent, wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 14
Dependent Claim 99 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit from about 0.2 to about 500 mg of a member selected from the group consisting of 5-p-chlorobenzoyl-1,4-dimethyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary active agent and a compound selected from the group consisting of from about 325 to about 1000 mg of acetaminophen and from about 325 to about 500 mg of aspirin as the potentiating agent, wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 15
Dependent Claim 81 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit from about 2.5 to about 1000 mg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary active agent and from about 150 to about 2000 mg of acetaminophen as the potentiating agent, wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 16
Dependent Claim 81 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit from about 2.5 to about 1000 mg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary active agent and from about 150 to about 2000 mg of acetaminophen as the potentiating agent, wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 17
Dependent Claim 81 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit from about 2.5 to about 1000 mg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary active agent and from about 150 to about 1000 mg of aspirin as the potentiating agent, wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 18
Dependent Claim 81 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit from about 2.5 to about 1000 mg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary active agent and from about 150 to about 1000 mg of aspirin as the potentiating agent, wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 19
Dependent Claim 81 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit from about 5.0 to about 500 mg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary active agent and from about 325 to about 1000 mg of acetaminophen as the potentiating agent, wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 20
Dependent Claim 81 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit from about 5.0 to about 500 mg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary active agent and from about 325 to about 1000 mg of acetaminophen as the potentiating agent, wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 21
Dependent Claim 81 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit from about 5.0 to about 500 mg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary active agent and from about 325 to about 500 mg of aspirin as the potentiating agent, wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 22
Dependent Claim 81 words
An oral pharmaceutical composition in dosage unit form suitable for inhibiting inflammation and osteogenic degeneration comprising per dosage unit from about 5.0 to about 500 mg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary active agent and from about 325 to about 500 mg of aspirin as the potentiating agent, wherein said primary and said potentiating agents are in admixture with a pharmaceutically acceptable carrier suitable for oral use.
Claim 23
Independent Claim 123 words
A method of inhibiting inflammation and osteogenic degeneration which comprises orally administering to an arthritic patient a pharmaceutical composition sufficient to provide from about 0.001 to 100 mg/kg of body weight of a 5-aroyl-1-loweralkylpyrrole-2-acetic acid compounds as the primary inflammation and osteogenic degeneration inhibiting agent, said compound being a member selected from the group having the formula: ##STR5## wherein R 3 is a member selected from the group consisting of hydrogen, loweralkyl and chloro, and Ar is a member selected from the group consisting of p-loweralkylphenyl and p-halophenyl, and the non-toxic therapeutically acceptable salts thereof; and from about 50 to 800 mg/kg of body weight of acetaminophen or from about 50 to 300 mg/kg of body weight of aspirin as the potentiating agent.
Claim 24
Independent Claim 123 words
A method of inhibiting inflammation and osteogenic degeneration which comprises orally administering to an arthritic patient a pharmaceutical composition sufficient to provide from about 0.001 to 100 mg/kg of body weight of a 5-aroyl-1-loweralkylpyrrole-2-acetic acid compounds as the primary inflammation and osteogenic degeneration inhibiting agent, said compound being a member selected from the group having the formula: ##STR5## wherein R 3 is a member selected from the group consisting of hydrogen, loweralkyl and chloro, and Ar is a member selected from the group consisting of p-loweralkylphenyl and p-halophenyl, and the non-toxic therapeutically acceptable salts thereof; and from about 50 to 800 mg/kg of body weight of acetaminophen or from about 50 to 300 mg/kg of body weight of aspirin as the potentiating agent.
Claim 25
Independent Claim 123 words
A method of inhibiting inflammation and osteogenic degeneration which comprises orally administering to an arthritic patient a pharmaceutical composition sufficient to provide from about 0.001 to 100 mg/kg of body weight of a 5-aroyl-1-loweralkylpyrrole-2-acetic acid compound as the primary inflammation and osteogenic degeneration inhibiting agent, said compound being a member selected from the group having the formula: ##STR6## wherein R 3 is a member selected from the group consisting of hydrogen, methyl and chloro, and Ar is a member selected from the group consisting of p-methylphenyl and p-chlorophenyl, and the non-toxic therapeutically acceptable salts thereof; and from about 50 to 800 mg/kg of body weight of acetaminophen or from about 50 to 300 mg/kg of body weight of aspirin as the potentiating agent.
Claim 26
Independent Claim 123 words
A method of inhibiting inflammation and osteogenic degeneration which comprises orally administering to an arthritic patient a pharmaceutical composition sufficient to provide from about 0.001 to 100 mg/kg of body weight of a 5-aroyl-1-loweralkylpyrrole-2-acetic acid compound as the primary inflammation and osteogenic degeneration inhibiting agent, said compound being a member selected from the group having the formula: ##STR6## wherein R 3 is a member selected from the group consisting of hydrogen, methyl and chloro, and Ar is a member selected from the group consisting of p-methylphenyl and p-chlorophenyl, and the non-toxic therapeutically acceptable salts thereof; and from about 50 to 800 mg/kg of body weight of acetaminophen or from about 50 to 300 mg/kg of body weight of aspirin as the potentiating agent.
Claim 27
Independent Claim 123 words
A method of inhibiting inflammation and osteogenic degeneration which comprises orally administering to an arthritic patient a pharmaceutical composition sufficient to provide from about 0.01 to 50 mg/kg of body weight of a 5-aroyl-1-loweralkylpyrrole-2-acetic acid compound as the primary inflammation and osteogenic degeneration inhibiting agent, said compound being a member selected from the group having the formula: ##STR7## wherein R 3 is a member selected from the group consisting of hydrogen, methyl and chloro, and Ar is a member selected from the group consisting of p-methylphenyl and p-chlorophenyl, and the non-toxic therapeutically acceptable salts thereof; and from about 100 to 400 mg/kg of body weight of acetaminophen or from about 100 to 150 mg/kg of body weight of aspirin as the potentiating agent.
Claim 28
Independent Claim 123 words
A method of inhibiting inflammation and osteogenic degeneration which comprises orally administering to an arthritic patient a pharmaceutical composition sufficient to provide from about 0.01 to 50 mg/kg of body weight of a 5-aroyl-1-loweralkylpyrrole-2-acetic acid compound as the primary inflammation and osteogenic degeneration inhibiting agent, said compound being a member selected from the group having the formula: ##STR7## wherein R 3 is a member selected from the group consisting of hydrogen, methyl and chloro, and Ar is a member selected from the group consisting of p-methylphenyl and p-chlorophenyl, and the non-toxic therapeutically acceptable salts thereof; and from about 100 to 400 mg/kg of body weight of acetaminophen or from about 100 to 150 mg/kg of body weight of aspirin as the potentiating agent.
Claim 29
Dependent Claim 12 words
The method of claim 15 wherein said primary agent is 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid.
Claim 30
Dependent Claim 12 words
The method of claim 15 wherein said primary agent is 5-p-chlorobenzoyl-1,4-dimethyl-pyrrole-2-acetic acid.
Claim 31
Independent Claim 70 words
A method of inhibiting inflammation and osteogenic degeneration which comprises orally administering to an arthritic patient a pharmaceutical composition sufficient to provide from about 1.0 to 100 mg/kg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary inflammation and osteogenic degeneration inhibiting agent and from about 50 to 800 mg/kg of body weight of acetaminophen as the potentiating agent.
Claim 32
Independent Claim 70 words
A method of inhibiting inflammation and osteogenic degeneration which comprises orally administering to an arthritic patient a pharmaceutical composition sufficient to provide from about 1.0 to 100 mg/kg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary inflammation and osteogenic degeneration inhibiting agent and from about 50 to 800 mg/kg of body weight of acetaminophen as the potentiating agent.
Claim 33
Independent Claim 70 words
A method of inhibiting inflammation and osteogenic degeneration which comprises orally administering to an arthritic patient a pharmaceutical composition sufficient to provide from about 2.0 to 50 mg/kg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary inflammation and osteogenic degeneration inhibiting agent and from about 100 to 400 mg/kg of body weight of acetaminophen as the potentiating agent.
Claim 34
Independent Claim 70 words
A method of inhibiting inflammation and osteogenic degeneration which comprises orally administering to an arthritic patient a pharmaceutical composition sufficient to provide from about 2.0 to 50 mg/kg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary inflammation and osteogenic degeneration inhibiting agent and from about 100 to 400 mg/kg of body weight of acetaminophen as the potentiating agent.
Claim 35
Independent Claim 70 words
A method of inhibiting inflammation and osteogenic degeneration which comprises orally administering to an arthritic patient a pharmaceutical composition sufficient to provide from about 1.0 to 100 mg/kg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary inflammation and osteogenic degeneration inhibiting agent and from about 50 to 300 mg/kg of body weight of aspirin as the potentiating agent.
Claim 36
Independent Claim 70 words
A method of inhibiting inflammation and osteogenic degeneration which comprises orally administering to an arthritic patient a pharmaceutical composition sufficient to provide from about 1.0 to 100 mg/kg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary inflammation and osteogenic degeneration inhibiting agent and from about 50 to 300 mg/kg of body weight of aspirin as the potentiating agent.
Claim 37
Independent Claim 70 words
A method of inhibiting inflammation and osteogenic degeneration which comprises orally administering to an arthritic patient a pharmaceutical composition sufficient to provide from about 2.0 to 50 mg/kg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary inflammation and osteogenic degeneration inhibiting agent and from about 100 to 150 mg/kg of body weight of aspirin as the potentiating agent.
Claim 38
Independent Claim 70 words
A method of inhibiting inflammation and osteogenic degeneration which comprises orally administering to an arthritic patient a pharmaceutical composition sufficient to provide from about 2.0 to 50 mg/kg of a member selected from the group consisting of 1-methyl-5-p-toluoyl-pyrrole-2-acetic acid and the alkali metal salts thereof as the primary inflammation and osteogenic degeneration inhibiting agent and from about 100 to 150 mg/kg of body weight of aspirin as the potentiating agent.

References Cited (Backward Citations)

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USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1982-01-01 1982-07-03 1983-01-02 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1986-01-01 1986-07-03 1987-01-02 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1990-01-01 1990-07-03 1991-01-02 $7700.00 Window Closed / Lapsed

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