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Anti-inflammatory composition

Assignee: Merck and Co Inc
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Filing: 1981-12-21
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Granted: 1983-04-12
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Expires: 2001-12-21
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Abstract

Abstract A pharmaceutical composition containing an interphenylene 9-thia-11-oxo-12-aza prostanoic acid type renal vasodilator and a non-steroidal anti-inflammatory agent and its use are disclosed.

Inventors

  • 👤 Edward H. Blaine

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 22:02
CPC Classifications
C; C07; C07D; C07D277/00; C07D277/02; C07D277/08; C07D277/12; C07D277/14; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/41; A61K31/425

Claims Analysis

Total Claims: 7
Claim 1
Independent Claim 227 words
A pharmaceutical composition useful for treating inflammation containing (i) a renal vasodilator compound of the formula ##STR5## wherein R is carboxy, a carboxy salt, a carboxy ester of the formula COOR 5 wherein R 5 is C 1-10 alkyl,, or CONHR 6 wherein R 6 is amino or methylsulfonyl; A is a p-phenylene or a m-phenylene or substituted phenylene derivative in which one or two of the phenylene hydrogens is replaced by a methyl or a halo substituent; n is 3 or 4; m is 0, 1, or 2; R 1 is hydrogen, deuterium, or methyl; Z is alkylene or unsaturated alkylene having from 2-3 carbon atoms; R 2 is hydrogen or lower alkanoyl; R 3 is hydrogen or straight chain C 1-3 alkyl; and R 4 is lower straight chain or branched alkyl having from 3-7 carbon atoms, an unsaturated alkyl having from 3-7 carbon atoms, or a substituted lower alkyl selected from polyfluoro alkyl of from 3-7 carbon atoms and lower alkoxy methylene; or R 3 and R 4 taken together with the carbon atom connecting R 3 and R 4 is a cyclic substituent selected from a bridged or unbridged alicyclic ring of from 5-9 carbon atoms or a heterocyclic ring containing sulfur or oxygen and from 5-7 ring-forming carbon atoms. and (ii) inclomethacin wherein the weight ratio i:ii ranges from 1.7:1 to 1:26.
Claim 2
Dependent Claim 227 words
A pharmaceutical composition useful for treating inflammation containing (i) a renal vasodilator compound of the formula ##STR5## wherein R is carboxy, a carboxy salt, a carboxy ester of the formula COOR 5 wherein R 5 is C 1-10 alkyl,, or CONHR 6 wherein R 6 is amino or methylsulfonyl; A is a p-phenylene or a m-phenylene or substituted phenylene derivative in which one or two of the phenylene hydrogens is replaced by a methyl or a halo substituent; n is 3 or 4; m is 0, 1, or 2; R 1 is hydrogen, deuterium, or methyl; Z is alkylene or unsaturated alkylene having from 2-3 carbon atoms; R 2 is hydrogen or lower alkanoyl; R 3 is hydrogen or straight chain C 1-3 alkyl; and R 4 is lower straight chain or branched alkyl having from 3-7 carbon atoms, an unsaturated alkyl having from 3-7 carbon atoms, or a substituted lower alkyl selected from polyfluoro alkyl of from 3-7 carbon atoms and lower alkoxy methylene; or R 3 and R 4 taken together with the carbon atom connecting R 3 and R 4 is a cyclic substituent selected from a bridged or unbridged alicyclic ring of from 5-9 carbon atoms or a heterocyclic ring containing sulfur or oxygen and from 5-7 ring-forming carbon atoms. and (ii) inclomethacin wherein the weight ratio i:ii ranges from 1.7:1 to 1:26.
Claim 3
Dependent Claim 127 words
The composition of claim 1 wherein said (i) compound has the formula ##STR6## wherein X is chlorine or methyl r is 0, 1, or 2; n is 3 or 4; R 1 is hydrogen, deuterium, or methyl; Z is ethylene, trimethylene, cis or trans-propylene, or propynylene; R 3 is hydrogen or lower alkyl of 1-3 carbon atoms; and R 4 is 4-pentenyl, 5,5,5-trifluoropentyl, or lower straight or branched chain alkyl of 3-7 carbon atoms or ##STR7## wherein X is chlorine or methyl r is 0, 1, or 2; n is 3 or 4; m is 0, 1, or 2; R 1 is hydrogen, deuterium, or methyl Z is ethylene, trimethylene, propenylene, or propynylene; y is 0, 2, or 3; and W is polymethylene of 2-6 carbon atoms.
Claim 4
Dependent Claim 12 words
The composition of claim 2 wherein said (i) compound is 4-[3-[3-(3-hydroxyoctyl)-4-oxo-2-thiazolidinyl]propyl]benzoic acid.
Claim 5
Dependent Claim 12 words
The composition of claim 2 wherein said (i) compound is 4-[3-[3-(2-(1-hydroxycyclohexyl)-ethyl]-4-oxo-2-thiazolidinyl]propyl]benzoic acid.
Claim 6
Dependent Claim 13 words
The composition of claim 4 wherein said (i) compound is the (+) enantiomer.
Claim 7
Dependent Claim 19 words
A method of treating inflammation in a human which comprises administering to said human a composition of claim 1.

References Cited (Backward Citations)

US3161654A Cited
US3647858A Cited
US3654349A Cited
US4225609A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1986-04-11 1986-10-11 1987-04-12 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1990-04-11 1990-10-11 1991-04-12 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1994-04-11 1994-10-11 1995-04-12 $7700.00 Window Closed / Lapsed

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