US2004198779A1PendingUtilityA1
Heterocycle substituted diphenyl leukotriene antagonists
Priority: Nov 11, 1999Filed: Jan 28, 2004Published: Oct 7, 2004
Est. expiryNov 11, 2019(expired)· nominal 20-yr term from priority
C07D 277/24C07D 285/10C07D 275/02C07D 307/42C07D 261/08C07D 285/06C07D 207/333C07D 207/08C07D 285/01C07D 233/64C07D 249/06C07D 285/12C07D 333/16C07D 231/12C07D 307/12
49
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Claims
Abstract
The invention relates to novel heterocycle substituted diphenyl leukotriene B 4 (LTB 4 ) antagonists, to compositions containing such compounds, and to methods of using such compounds for treatment of inflammatory diseases.
Claims
exact text as granted — not AI-modified1 - 17 . (canceled)
18 . The compound of claim 1 wherein the R1, R2, R3 and R4 groups for substitution in formula (I) are selected from the following variables coded R01 thru R16
R variables
Combination
R1 group
R2 group
R3 group
R4 group
Code
choice
choice
choice
choice
R01
R1
R2
R3
R4
R02
R1
R2
R3
PG1-R4
R03
R1
R2
PG1-R3
R4
R04
R1
R2
PG1-R3
PG1-R4
R05
R1
PG1-R2
R3
R4
R06
R1
PG1-R2
R3
PG1-R4
R07
R1
PG1-R2
PG1-R3
R4
R08
R1
PG1-R2
PG1-R3
PG1-R4
R09
PG1-R1
R2
R3
R4
R10
PG1-01
R2
R3
PG1-R4
R11
PG1-R1
R2
PG1-R3
R4
R12
PG1-R1
R2
PG1-R3
PG1-R4
R13
PG1-R1
PG1-R2
R3
R4
R14
PG1-R1
PG1-R2
R3
PG1-R4
R15
PG1-R1
PG1-R2
PG1-R3
R4
R16
PG1-R1
PG1-R2
PG1-R3
PG1-R4
and;
the Y1, Y2, and Y3 groups for substitution in formula (I) are selected from the following variables coded Y01 thru Y27:
Y variables combination Y1 group code choice Y2 group choice Y3 group choice Y01 Y1 Y2 Y3 Y02 Y1 Y2 PG1-Y3 Y03 Y1 Y2 PG2-Y3 Y04 Y1 PG1-Y2 Y3 Y05 Y1 PG2-Y2 Y3 Y06 Y1 PG1-Y2 PG1-Y3 Y07 Y1 PG1-Y2 PG2-Y3 Y08 Y1 PG2-Y2 PG1-Y3 Y09 Y1 PG2-Y2 PG2-Y3 Y10 PG1-Y1 Y2 Y3 Y11 PG1-Y1 Y2 PG1-Y3 Y12 PG1-Y1 Y2 PG2-Y3 Y13 PG1-Y1 PG1-Y2 Y3 Y14 PG1-Y1 PG1-Y2 PG1-Y3 Y15 PG1-Y1 PG1-Y2 PG2-Y3 Y16 PG1-Y1 PG2-Y2 Y3 Y17 PG1-Y1 PG2-Y2 PG1-Y3 Y18 PG1-Y1 PG2-Y2 PG2-Y3 Y19 PG2-Y1 Y2 Y3 Y20 PG2-Y1 Y2 PG1-Y3 Y21 PG2-Y1 Y2 PG2-Y3 Y22 PG2-Y1 PG1-Y2 Y3 Y23 PG2-Y1 PG1-Y2 PG1-Y3 Y24 PG2-Y1 PG1-Y2 PG2-Y3 Y25 PG2-Y1 PG2-Y2 Y3 Y26 PG2-Y1 PG2-Y2 PG1-Y3 Y27 PG2-Y1 PG2-Y2 PG2-Y3
and;
the X and Z groups and the n variable for substitution in formula (I) are selected from the following variables coded XZn01 thru XZn24:
XZn variables Z combination X group Group n integer code choice Choice group choice XZn01 X Z n XZn02 X Z PG1-n XZn03 X Z PG2-n XZn04 X PG1-Z n XZn05 X PG2-Z n XZn06 X PG3-Z n XZn07 X PG1-Z PG1-n XZn08 X PG2-Z PG1-n XZn09 X PG3-Z PG1-n XZn10 X PG1-Z PG2-n XZn11 X PG2-Z PG2-n XZn12 X PG3-Z PG2-n XZn13 PG1-X Z n XZn14 PG1-X Z PG1-n XZn15 PG1-X Z PG2-n XZn16 PG1-X PG1-Z n XZn17 PG1-X PG2-Z n XZn18 PG1-X PG3-Z n XZn19 PG2-X PG1-Z PG1-n XZn20 PG2-X PG2-Z PG1-n XZn21 PG2-X PG3-Z PG1-n XZn22 PG2-X PG1-Z PG2-n XZn23 PG2-X PG2-Z PG2-n XZn24 PG2-X PG3-Z PG2-n
19 - 22 . (canceled)
23 . A pharmaceutical composition which comprises a therapeutically effective amount of a compound according to claim 19 and a pharmaceutically acceptable carrier or diluent.
24 . A method for the treatment or prevention of Inflammatory Diseases, which comprises administering to a mammal in need thereof a therapeutically effective amount of a compound according to claim 18 .
25 . A method for in vivo inhibition of leukotriene B 4 in a mammal in need thereof, which comprises administering to said mammal a therapeutically effective amount of a compound according to claim 18 .
26 . The method of claim 25 wherein the route of administration is oral and the dose is about 1 to about 1000 milligrams per day.
27 . The method of claim 25 wherein the route of administration is parenteral and the dose is about 0.1 to about 100 milligrams per day.
28 - 29 . (canceled)Cited by (0)
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