Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
515 words
A compound of the formula: wherein: R 1 is H , halogen, C 1 -C 8 alkyl, C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, -CF 3 , -OR 2 , -SR 2 , -NR 2 R 2 , -CHO, -COOR 2 , -(C=O)R 2 , -C(OH)R 2 R 2 , -CN, -NO 2 , substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, or substituted or unsubstituted phenethyl; R 2 is H, C 1 -C 8 alkyl, C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, -CF 3 , substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, or substituted or unsubstituted phenethyl; R 3 is -(A) m -(CR 2 =CR 2 ) p -(CR 2 R 2 ) m -Q; R 4 is H, halogen, -NO 2 , -CN, -OR 2 , -SR 2 , NR 2 R 2 , or C 1 -C 8 alkyl; R 5 is -(CH 2 ) s -C-(CH 2 ) s -R 7 ; R 6 R 6 is H or C 1 -C 4 alkyl; R7 is A) a monocyclic or bicyclic heterocyclic radical containing from 3 to 12 nuclear carbon atoms and 1 or 2 nuclear heteroatoms selected from N and S with at least one being N, and with each ring in the heterocyclic radical being formed of 5 or 6 atoms, or B) the radical W - R 8 ; R 8 contains up to 21 carbon atoms and is (1) a hydrocarbon radical or (2) an acyl radical of an organic acyclic or monocyclic carboxylic acid containing not more than 1 heteroatom in the ring; R 9 is -OR 10 , -SR 10 , or NR 10 R 10 ; R 10 is H, C 1 -C 6 alkyl, -(C=O)R 11 , unsubstituted phenyl or unsubstituted benzyl; R 11 is H, C 1 -C 8 alkyl, C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, -CF 3 , or unsubstituted phenyl, benzyl, or phenethyl; m is 0-8; n is 1 or 2; p is 0-2; s is 0-3; A is -CR 2 R 4 -, or =C=O ; Q is -COOR 2 , tetrazole, -COOR 5 , -COCH 2 OH, -CONHSO 2 R 11 , -CH 20 H, - CN , -CONR 10 R 10 , -NHSO 2 R 11 (but only when the sum of m and p in R 3 is greater than 0), or if Q is COOH and R 3 contains an R 4 which is -OH, -SH, or -NHR 2 then Q and R 4 and the carbons through which they are attached may form a heterocyclic ring with loss of water; W is O, S, or NH; X is O, S, -SO, -SO 2 , or - NR 2 ; Y is -(CR 2 =CR 2 ) n -, -(C=C) n -, -CR 2 R 2- X-, or -X-CR 2 R 2 -; with the proviso that when R 4 is on the carbon adjacent to X it is not OH, S H , or NHR 2 ; and the pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
515 words
A compound of the formula: wherein: R 1 is H , halogen, C 1 -C 8 alkyl, C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, -CF 3 , -OR 2 , -SR 2 , -NR 2 R 2 , -CHO, -COOR 2 , -(C=O)R 2 , -C(OH)R 2 R 2 , -CN, -NO 2 , substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, or substituted or unsubstituted phenethyl; R 2 is H, C 1 -C 8 alkyl, C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, -CF 3 , substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, or substituted or unsubstituted phenethyl; R 3 is -(A) m -(CR 2 =CR 2 ) p -(CR 2 R 2 ) m -Q; R 4 is H, halogen, -NO 2 , -CN, -OR 2 , -SR 2 , NR 2 R 2 , or C 1 -C 8 alkyl; R 5 is -(CH 2 ) s -C-(CH 2 ) s -R 7 ; R 6 R 6 is H or C 1 -C 4 alkyl; R7 is A) a monocyclic or bicyclic heterocyclic radical containing from 3 to 12 nuclear carbon atoms and 1 or 2 nuclear heteroatoms selected from N and S with at least one being N, and with each ring in the heterocyclic radical being formed of 5 or 6 atoms, or B) the radical W - R 8 ; R 8 contains up to 21 carbon atoms and is (1) a hydrocarbon radical or (2) an acyl radical of an organic acyclic or monocyclic carboxylic acid containing not more than 1 heteroatom in the ring; R 9 is -OR 10 , -SR 10 , or NR 10 R 10 ; R 10 is H, C 1 -C 6 alkyl, -(C=O)R 11 , unsubstituted phenyl or unsubstituted benzyl; R 11 is H, C 1 -C 8 alkyl, C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, -CF 3 , or unsubstituted phenyl, benzyl, or phenethyl; m is 0-8; n is 1 or 2; p is 0-2; s is 0-3; A is -CR 2 R 4 -, or =C=O ; Q is -COOR 2 , tetrazole, -COOR 5 , -COCH 2 OH, -CONHSO 2 R 11 , -CH 20 H, - CN , -CONR 10 R 10 , -NHSO 2 R 11 (but only when the sum of m and p in R 3 is greater than 0), or if Q is COOH and R 3 contains an R 4 which is -OH, -SH, or -NHR 2 then Q and R 4 and the carbons through which they are attached may form a heterocyclic ring with loss of water; W is O, S, or NH; X is O, S, -SO, -SO 2 , or - NR 2 ; Y is -(CR 2 =CR 2 ) n -, -(C=C) n -, -CR 2 R 2- X-, or -X-CR 2 R 2 -; with the proviso that when R 4 is on the carbon adjacent to X it is not OH, S H , or NHR 2 ; and the pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
118 words
A compound of Claim 1 of the Formula Ia: wherein: R 1 is H, halogen, C 1 -C 8 alkyl, C 2 -C 8 2 alkenyl, C 2 -C 8 alkynyl, -CF 3 , -OR 2 , - SR 2 , - NR 2 R 2 , - CHO , - COOR 2 , -(C=O)R 2 , -C(OH)R 2 R 2 , -CN, -NO 2 , substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, or substituted or unsubstituted phenethyl; Y is -(CR 2 =CR 2 ) n - or -(C=C) n -: R to R 11 , m, n, p, s, A, Q, W, and X are as defined in Claim 1; and the pharmaceutically acceptable salts thereof.
Claim 4
Dependent Claim
65 words
A compound of Claim 1 of the Formula Ib: wherein: R 1 is H, halogen, CH 3 , -CF 3 , or SCF 3 ; R 2 is H, C 1 -C 3 alkyl, C 2 -C 3 alkenyl, or R to R 11 , m, p, s, A, Q, W, and X are as defined in Claim 1; and the pharmaceutically acceptable salts thereof.
Claim 5
Dependent Claim
64 words
A compound of Claim 1 of the Formula Ic: wherein: R 1 is H, halogen, CH 3 , C 2 -C 3 alkenyl, R 2 is H, C 1 -C 3 alkyl, C 2 -C 3 alkenyl, or R 3 to R 11 , m, p, s, A, Q, W, and X are as defined in Claim 1; and the pharmaceutically acceptable salts thereof.
Claim 6
Dependent Claim
12 words
A compound of Claim 1 which is a compound of Formula E:
Claim 7
Dependent Claim
33 words
A compound of Claim 1 which is a compound of Formula F: wherein: R 1 is 5-Cl; 6-Cl; 7-Cl; 6-Br; 7-Br; 7-CF 3 ; 5-CF 3 ; 7-F; 6,7-diCl; 5,6-diCl, 6-Me; or 6-F.
Claim 8
Dependent Claim
19 words
A compound of Claim 1 of Formula G: wherein XR 3 is NHCOCOOEt or OCH 2 CO 2 Me.
Claim 9
Dependent Claim
34 words
A compound of Claim 1 which is: (E)-4-(3-(2-(quinolin-2-yl)-1-methylethenyl)phenoxy)-butyric acid; 4-(3-(2-(7-bromoquinolin-2-yl)ethynyl)phenoxy)butanoic acid sodium salt; Methyl (D,L) 2-(3-(2-(7-bromoquinolin-2-yl)ethynyl)-phenoxy)propanoate; (D,L) 2-(3-(2-(7-bromoquinolin-2-yl)ethynyl)phenoxyl- propanoic acid sodium salt; (Z)-(D,L)-2-(3-(2-(7-chloroquinolin-2-yl)-1-methylethenyl)phenoxy)propanoic acid sodium salt; (E)-(D,L)-2-(3-(2-(7-chloroquinolin-2-yl)-1-methylethenyl)phenoxy)propanoic acid sodium salt; 2-(3-(7-bromoquinolin-2-ylmethoxy)phenoxy)propanoic acid; or 5-(1-(3-(2-(7-chloroquinolin-2-yl)cyclopropyl)-phenoxy)ethyl)-1H-tetrazole.
Claim 10
Dependent Claim
28 words
A pharmaceutical composition useful in antagonizing leukotriene action in mammals comprising a compound as claimed in any one of Claims 1 to 8 and a pharmaceutically acceptable carrier.
Claim 11
Dependent Claim
82 words
A composition as claimed in Claim 10 additionally comprising an effective amount of at least one further active ingredient that is a non-steroidal anti-inflammatory drug; a peripheral analgesic agent; a cyclooxygenase inhibitor; a leukotriene antagonist; a leukotriene inhibitor; an H 2 -receptor antagonist; an antihistaminic agent; a prostaglandin antagonist; or a thromboxane antagonist; where the weight ratio of the compound claimed in any one of Claims 1 to 8 to the total amount of further active ingredient(s) ranges from 1000:1 to 1:1000.
Claim 12
Dependent Claim
41 words
A compound as claimed in any one of Claims 1 to 8 or a composition as claimed in Claim 9 or 10, for use in preventing the synthesis, the action, or the release of SRS-A and leukotriene D 4 in mammals.