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Details for Patent: 5,840,746

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Details for Patent: 5,840,746

Title: Use of inhibitors of cyclooxygenase in the treatment of neurodegenerative diseases
Abstract:The present invention provides a method of treating a neurodegenerative disease and in particular Alzheimers disease which comprises administering to a human in need thereof a therapeutically effective amount of a non-steroid COX-II inhibitor. Although a wide range of COX-II inhibitors may be employed but it is preferred to employ compounds of the Formula I: ##STR1##
Inventor(s): Ducharme; Yves (Montreal, CA), Gauthier; Jacques Yves (Laval, CA), Prasit; Petpiboon (Kirkland, CA), Leblanc; Yves (Kirkland, CA), Wang; Zhaoyin (Pierrefonds, CA), Leger; Serge (Dollard Des Ormeaux, CA), Therien; Michel (Dollard Des Ormeaux, CA)
Assignee: Merck Frosst Canada, Inc. (Kirkland, CA)
Filing Date:Sep 05, 1997
Application Number:08/926,291
Claims:1. A method of treating Alzheimer's disease in a human which comprises administering to said human an effective amount of a non-steroidal COX-2 inhibitor, wherein said non-steroidal COX-2 inhibitor will bind at least 100 times as well to COX-2 as to COX-1.

2. A method according to claim 1 wherein the administration is oral administration.

3. A method according to claim 2 wherein the non-steroidal COX-2 inhibitor is within a tablet or capsule.

4. A method according to claim 3 wherein said COX-2 inhibitor is selected from:

(a) 3-(4-(Aminosulfonyl)phenyl)-2-(4-fluorophenyl)-5-(2-hydroxy-2-propyl)thiop hene,

(b) 3-(4-(Aminosulfonyl)phenyl)-2-(4-fluorophenyl)thiophene,

(c) 3-(4-(Aminosulfonyl)phenyl)-2-(4-fluorophenyl)-5-(2-propyl)thiophene,

(d) 3-(4-(Aminosulfonyl)phenyl)-2-cyclohexylthiophene,

(e) 5-(4-Carboxyphenyl)-4-(4-(methylsulfonyl)phenyl) thiophene-2-carboxylic acid,

(f) 4-(4-Fluorophenyl)-2-methyl-5-(4-(methylsulfonyl)phenyl)thiazole,

(g) 2-(4-Fluorophenyl)-3-(4-(methylsulfonyl)phenyl)-2-cyclopenten-1-one

(h) 4-(4-(Methylsulfonyl)phenyl)-5-(4-fluorophenyl)-isothiazole,

(i) 3-(4-Fluorophenyl)-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone,

(j) 3-(4-Fluorophenyl)-4-(4-(aminosulfonyl)phenyl)-2-(5H)-furanone,

(k) 3-(4-Fluorophenyl)-4-(4-(methylsulfonyl)phenyl) furan,

(l) 5,5-Dimethyl-3-(4-fluorophenyl)-4-(4-methylsulfonyl) phenyl)-2-(5H)-furanone,

(m) 2-(4-(Aminosulfonyl)phenyl)-3-(4-fluorophenyl) thiophene,

(n) 3-(4-(Trifluoroacetylaminosulfonyl)phenyl)-2-(4-fluorophenyl)thiophene,

(o) 3-(3-Fluorophenyl)-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone,

(p) 5,5-Dimethyl-3-(3-fluorophenyl)-4-(4-methylsulfonyl) phenyl)-2-(5H)-furanone,

(q) 5,5-Dimethyl-3-(3-chlorophenyl)-4-(4-methylsulfonyl) phenyl)-2-(5H)-furanone,

(r) 3-(3,4-Difluorophenyl)-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone,

(s) 3-(3,4-Dichlorophenyl)-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone,

(t) 5,5-Dimethyl-3-(3,4-difluorophenyl)-4-(4-methylsulfonyl)phenyl)-2-(5H)-fur anone,

(u) 5,5-Dimethyl-3-(3,4-dichlorophenyl)-4-(4-methylsulfonyl)phenyl)-2-(5H)-fur anone,

(v) 5,5-Dimethyl-3-(4-chlorophenyl)-4-(4-methylsulfonyl)phenyl)-2-(5H)-furanon e,

(w) 3-(2-Naphthyl)-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone,

(x) 5,5-Dimethyl-3-(2-naphthyl)-4-(4-(methylsulfonyl) phenyl)-2-(5H)-furanone, and

(y) 3-phenyl-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone.

5. A method of treating dementia associated with Alzheimer's disease in a human which comprises administering to said human an effective amount of a non-steroidal COX-2 inhibitor, wherein said non-steroidal COX-2 inhibitor will bind at least 100 times as well to COX-2 as to COX-1.

6. A method according to claim 5 wherein the administration is oral administration.

7. A method according to claim 6 wherein the non-steroidal COX-2 inhibitor is within a tablet or capsule.

8. A method according to claim 7 wherein the COX-2 inhibitor is selected from:

(a) 3-(4-(Aminosulfonyl)phenyl)-2-(4-fluorophenyl)-5-(2-hydroxy-2-propyl)thiop hene,

(b) 3-(4-(Aminosulfonyl)phenyl)-2-(4-fluorophenyl)thiophene,

(c) 3-(4-(Aminosulfonyl)phenyl)-2-(4-fluorophenyl)-5-(2-propyl)thiophene,

(d) 3-(4-(Aminosulfonyl)phenyl)-2-cyclohexylthiophene,

(e) 5-(4-Carboxyphenyl)-4-(4-(methylsulfonyl)phenyl) thiophene-2-carboxylic acid,

(f) 4-(4-Fluorophenyl)-2-methyl-5-(4-(methylsulfonyl)phenyl)thiazole,

(g) 2-(4-Fluorophenyl)-3-(4-(methylsulfonyl)phenyl)-2-cyclopenten-1-one

(h) 4-(4-(Methylsulfonyl)phenyl)-5-(4-fluorophenyl)-isothiazole,

(i) 3-(4-Fluorophenyl)-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone,

(j) 3-(4-Fluorophenyl)-4-(4-(aminosulfonyl)phenyl)-2-(5H)-furanone,

(k) 3-(4-Fluorophenyl)-4-(4-(methylsulfonyl)phenyl) furan,

(l) 5,5-Dimethyl-3-(4-fluorophenyl)-4-(4-methylsulfonyl) phenyl)-2-(5H)-furanone,

(m) 2-(4-(Aminosulfonyl)phenyl)-3-(4-fluorophenyl) thiophene,

(n) 3-(4-(Trifluoroacetylaminosulfonyl)phenyl)-2-(4-fluorophenyl)thiophene,

(o) 3-(3-Fluorophenyl)-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone,

(p) 5,5-Dimethyl-3-(3-fluorophenyl)-4-(4-methylsulfonyl) phenyl)-2-(5H)-furanone,

(q) 5,5-Dimethyl-3-(3-chlorophenyl)-4-(4-methylsulfonyl) phenyl)-2-(5H)-furanone,

(r) 3-(3,4-Difluorophenyl)-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone,

(s) 3-(3,4-Dichlorophenyl)-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone,

(t) 5,5-Dimethyl-3-(3,4-difluorophenyl)-4-(4-methylsulfonyl)phenyl)-2-(5H)-fur anone,

(u) 5,5-Dimethyl-3-(3,4-dichlorophenyl)-4-(4-methylsulfonyl)phenyl)-2-(5H)-fur anone,

(v) 5,5-Dimethyl-3-(4-chlorophenyl)-4-(4-methylsulfonyl)phenyl)-2-(5H)-furanon e,

(w) 3-(2-Naphyhyl)-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone,

(x) 5,5-Dimethyl-3-(2-naphyhyl)-4-(4-(methylsulfonyl) phenyl)-2-(5H)-furanone, and

(y) 3-phenyl-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone.

9. A method according to claim 1 wherein the COX-2 inhibitor is of formula I ##STR222## or pharmacetically acceptable salts thereof wherein: X--Y--Z-- is selected from the group consisting of --C(O)--O--CR.sup.5 (R.sup.5')-- when side b is a double bond, and sides a and c are single bonds; and

R.sup.1 is selected from the group consisting of

(a) S(O).sub.2 CH.sub.3,

(b) S(O).sub.2 NH.sub.2,

R.sup.2 is selected from the group consisting of

(a) C.sub.1-6 alkyl,

(b) C.sub.3, C.sub.4, C.sub.5, C.sub.6, and C.sub.7, cycloalkyl,

(c) heteroaryl

(d) mono- or di-substituted phenyl wherein the substituent is selected from the group consisting of

(1) hydrogen,

(2) halo,

(3) C.sub.1-6 alkoxy,

(4) C.sub.1-6 alkylthio,

(5) CN,

(6) CF.sub.3,

(7) C.sub.1-6 alkyl,

(8) N.sub.3,

(9) --CO.sub.2 H,

(10) --CO.sub.2 --C.sub.1-4 alkyl,

(11) --C(R.sup.5)(R.sup.6)--OH,

(12) --C(R.sup.5)(R.sup.6)--O--C.sub.1-4 alkyl, and

(13) --C.sub.1-6 alkyl-CO.sub.2 --R.sup.5 ;

R.sup.5, R.sup.5' and R.sup.6 are each independently selected from the group consisting of

(a) hydrogen,

(b) C.sub.1-6 alkyl,

or R.sup.5 and R.sup.6 together with the carbon to which they are attached form a saturated monocyclic carbon ring of 3, 4, 5, 6 or 7 atoms.
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