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US4442099A Expired / Lapsed US ⏱️ 0.0 years remaining

Leukotriene analogues

Assignee: RESEARCH Corp A NOT-FOR-PROFIT CORP OF NY
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Filing: 1981-11-27
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Granted: 1984-04-10
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Expires: 2001-11-27
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Abstract

Abstract A compound of the formula ##STR1## wherein n is an integer from 2 to 4; m is an integer from 3 to 5; R is OM, OR 1 or NR 2 R 3 where M is a pharmaceutically acceptable cation; R 1 , R 2 and R 3 are the same or different and selected from the group consisting of hydrogen, C 1 -C 12 branched, unbranched or cyclic alkyl, aryl and aralkyl; or R 2 and R 3 taken together form a group of the formula ##STR2## can be used as an inhibitor of the lipoxygenase pathway of the arachidonic acid cascade in animals.

Inventors

  • 👤 Kyriacos C. Nicolaou
  • 👤 Nicos A. Petasis
  • 👤 Steven P. Seitz

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-07 21:33
CPC Classifications
C; C07; C07D; C07D295/00; C07D295/16; C07D295/18; C07D295/182; C07D295/185; A; A61; A61P; A61P11/00; A61P37/00; A61P37/08; C07C; C07C57/00; C07C57/26; C07F; C07F7/00; C07F7/02; C07F7/08; C07F7/18; C07F7/1804; C07F9/00; C07F9/02; C07F9/28; C07F9/38; C07F9/40; C07F9/4003; C07F9/4015

Claims Analysis

Total Claims: 22
Claim 1
Independent Claim 103 words
A compound of the formula ##STR11## wherein n is an integer from 2 to 4; m is an integer from 3 to 5; R is OM, OR 1 or NR 2 R 3 where M is a pharmaceutically acceptable cation; R 1 , R 2 and R 3 are the same or different and selected from the group consisting of: hydrogen; C 1 -C 12 branched, unbranched or cyclic alkyl; phenyl, lower-alkyl substituted phenyl, halo-substituted phenyl and combinations thereof; and benzyl, lower alkyl substituted benzyl, and halo-substituted benzyl; or R 2 and R 3 taken together form a group of the formula: ##STR12##
Claim 2
Dependent Claim 103 words
A compound of the formula ##STR11## wherein n is an integer from 2 to 4; m is an integer from 3 to 5; R is OM, OR 1 or NR 2 R 3 where M is a pharmaceutically acceptable cation; R 1 , R 2 and R 3 are the same or different and selected from the group consisting of: hydrogen; C 1 -C 12 branched, unbranched or cyclic alkyl; phenyl, lower-alkyl substituted phenyl, halo-substituted phenyl and combinations thereof; and benzyl, lower alkyl substituted benzyl, and halo-substituted benzyl; or R 2 and R 3 taken together form a group of the formula: ##STR12##
Claim 3
Dependent Claim 9 words
The compound of claim 1 wherein m is 4.
Claim 4
Dependent Claim 9 words
The compound of claim 1 wherein n is 3.
Claim 5
Dependent Claim 9 words
The compound of claim 1 wherein R is OM.
Claim 6
Dependent Claim 11 words
The compound of claim 1 wherein R is OR 1 .
Claim 7
Dependent Claim 12 words
The compound of claim 4 wherein M is an alkali metal cation.
Claim 8
Dependent Claim 15 words
The compound of claim 5 wherein R 1 is hydrogen or a lower alkyl group.
Claim 9
Dependent Claim 10 words
The compound of claim 7 wherein R 1 is methyl.
Claim 10
Dependent Claim 16 words
The compound of claim 1 which is ##STR13## wherein R 1 is hydrogen or lower alkyl.
Claim 11
Dependent Claim 117 words
A pharmaceutical composition comprising an amount sufficient to inhibit the lipoxygenase pathway of arachidonic acid metabolism of a compound of the formula: ##STR14## wherein n is an integer from 2 to 4; n is an integer from 3 to 5; R is OM, OR 1 or NR 2 R 3 where M is a pharmaceutically acceptable cation; R 1 , R 2 and R 3 are the same or different and selected from the group consisting of: hydrogen; phenyl, lower-alkyl substituted phenyl, halo-substituted phenyl and combinations thereof; and benzyl, lower alkyl substituted benzyl and halo-substituted benzyl; or R 2 and R 3 taken together form a group of the formula: ##STR15## together with an inert pharmaceutical carrier.
Claim 12
Dependent Claim 117 words
A pharmaceutical composition comprising an amount sufficient to inhibit the lipoxygenase pathway of arachidonic acid metabolism of a compound of the formula: ##STR14## wherein n is an integer from 2 to 4; n is an integer from 3 to 5; R is OM, OR 1 or NR 2 R 3 where M is a pharmaceutically acceptable cation; R 1 , R 2 and R 3 are the same or different and selected from the group consisting of: hydrogen; phenyl, lower-alkyl substituted phenyl, halo-substituted phenyl and combinations thereof; and benzyl, lower alkyl substituted benzyl and halo-substituted benzyl; or R 2 and R 3 taken together form a group of the formula: ##STR15## together with an inert pharmaceutical carrier.
Claim 13
Dependent Claim 9 words
The composition of claim 10 wherein m is 4.
Claim 14
Dependent Claim 9 words
The composition of claim 10 wherein n is 3.
Claim 15
Dependent Claim 9 words
The composition of claim 10 wherein R is OM.
Claim 16
Dependent Claim 11 words
The compositon of claim 11 wherein R is OR 1 .
Claim 17
Dependent Claim 11 words
The composition of claim 13 wherein M is alkali metal cation.
Claim 18
Dependent Claim 15 words
The composition of claim 14 wherein R 1 is hydrogen or a lower alkyl group.
Claim 19
Dependent Claim 10 words
The composition of claim 16 wherein R 1 is methyl.
Claim 20
Dependent Claim 18 words
The composition of claim 10 wherein the compound is ##STR16## wherein R 1 is hydrogen or lower alkyl.
Claim 21
Dependent Claim 11 words
The composition of claim 10 wherein said carrier is an aerosol.
Claim 22
Independent Claim 46 words
A method of inhibiting the lipoxygenase pathway of the arachidonic acid cascade in a warm blooded animal which comrpises administering to said animal a lipoxygenase pathway inhibiting amount of a compound as in any of claims 1, 2, 3, 4, 5, 6, 7, 8 or 9.

References Cited (Backward Citations)

US3671558A Cited
US3737450A Cited
US4001428A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1987-04-10 1987-10-10 1988-04-10 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1991-04-10 1991-10-10 1992-04-10 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1995-04-10 1995-10-10 1996-04-10 $7700.00 Window Closed / Lapsed

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