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US 2006/0040931 A1Published application
Benzomorpholine derivatives
AssigneeToray Industries, Inc.
InventorsMichihiro Ohno, Ryoji Hayashi, Masafumi Isogaya, Hiroshi Ueda
Life of this patent
Estimating the term…
Abstract
This invention relates to benzomorpholine derivatives typified by a compound represented by general formula (VIII) or pharmaceutically acceptable salts thereof and platelet aggregation inhibitors comprising the same. The compounds of the present invention have a strong inhibitory effect of platelet aggregation, so that they are effective for treating and preventing diseases in which thrombus is involved.
Claims13
A benzomorpholine derivative or pharmaceutically acceptable salt thereof represented by formula i,
- wherein
- A is C2-4 alkylene, c24 alkenylene, or c24 alkynylene,
- R1 is:
- (1) unsubstituted aryl or heteroaryl, or aryl or heteroaryl substituted with one or a plurality of substituents independently selected from the following group,
- a) C1-5 alkyl, b) C1-5 alkoxy c) C3-8 cycloalkyl, d) C1-5 haloalkyl, e) phenyl, f) phenoxy, g) hydroxyl, h) C1-5 hydroxyalkyl, i) C1-5 haloalkyloxy, j) mercapto, k) C1-5 alkylthio, 1) C1-5 haloalkylthio, m) halogen, n) cyano, o) nitro, p) amino, q) C1-5 alkylamino, r) C2-10 dialkylamino, s) acyl, t) carboxyl, u) C2-6 alkyloxycarbonyl, v) mesyl, w) trifluoromethanesulfonyl, and x) tosyl;
- or
- (2) unsubstituted C1-5 alkyl, C3-8 cycloalkyl, C2-10 alkenyl, C4-10 cycloalkenyl, or C2-10 alkynyl, or C1-5 alkyl, C3-8 cycloalkyl, C2-10 alkenyl, C4-10 cycloalkenyl, or C2-10 alkynyl substituted with one or a plurality of substituents independently selected from the following group,
- a) phenyl, b) hydroxyl, c) C1-5 alkyl, d) C3-8 cycloalkyl, e) C1-5 haloalkyl, and f) halogen;
- R2 is unsubstituted aryl or heteroaryl, or aryl or heteroaryl substituted with one or a plurality of substituents independently selected from the following group,
- a) C1-5 alkyl, b) C1-5 alkoxy, c) C3-8 cycloalkyl, d) C1-5 haloalkyl, e) phenyl, f) phenoxy, g) hydroxyl, h) C1-5 hydroxyalkyl, i) C1-5 haloalkyloxy, j) mercapto, k) C1-5 alkylthio, 1) C1-5 haloalkylthio, m) halogen, n) cyano, o) nitro, p) amino, q) C1-5 alkylamino, r) C2-10 dialkylamino, s) acyl, t) carboxyl, u) C2-6 alkyloxycarbonyl, v) mesyl, w) trifluoromethanesulfonyl, and x) tosyl;
- R3 is hydrogen, halogen, C1-5 alkyl, or C1-5 alkoxy;
- R4 is —X— (CH2)n-COOR5, and X is —O—, —S—, or —CH2—;
- R5 is hydrogen or C1-5 alkyl;
- and n is an integer that is 1, 2, or 3.
11 more elements
12-16. (canceled)
A pharmaceutical composition comprising:
- a pharmaceutically acceptable carrier;
- and
- a benzomorpholine derivative or pharmaceutically acceptable salt thereof represented by formula I,
- wherein
- A is C2-4 alkylene, C2-4 alkenylene, or C2-4 alkynylene,
- R1 is:
- (1) unsubstituted aryl or heteroaryl, or aryl or heteroaryl substituted with one or a plurality of substituents independently selected from the following group,
- a) C1-5 alkyl, b) C s5 alkoxy c) C3-8 cycloalkyl, d) C1-5 haloalkyl, e) phenyl, f) phenoxy, g) hydroxyl, h) C1-5 hydroxyalkyl, i) C1-5 haloalkyloxy, j) mercapto, k) C1-5 alkylthio, 1) C1-5 haloalkylthio, m) halogen, n) cyano, o) nitro, p) amino, q) C1-5 alkylamino, r) C2-10 dialkylamino, s) acyl, t) carboxyl, u) C2-6 alkyloxycarbonyl, v) mesyl, w) trifluoromethanesulfonyl, and x) tosyl;
- or
- (2) unsubstituted C1-5 alkyl, C3-8 cycloalkyl, C2-10 alkenyl, C4-10 cycloalkenyl, or C2-10 alkynyl, or C1-5 alkyl, C3-8 cycloalkyl, C2-10 alkenyl, C4-10 cycloalkenyl, or C2-10 alkynyl substituted with one or a plurality of substituents independently selected from the following group,
- a) phenyl, b) hydroxyl, c) C1-5 alkyl, d) C3-8 cycloalkyl, e) C1-5 haloalkyl, and f) halogen;
- R2 is unsubstituted aryl or heteroaryl, or aryl or heteroaryl substituted with one or a plurality of substituents independently selected from the following group,
- a) C1-5 alkyl, b) C1-5 alkoxy, c) C3-8 cycloalkyl, d) C1-5 haloalkyl, e) phenyl, f) phenoxy, g) hydroxyl, h) C1-5 hydroxyalkyl, i) C1-5 haloalkyloxy, j) mercapto, k) C1-5 alkylthio, l) C1-5 haloalkylthio, m) halogen, n) cyano, o) nitro, p) amino, q) C1-5 alkylamino, r) C2-10 dialkylamino, s) acyl, t) carboxyl, u) C2-6 alkyloxycarbonyl, v) mesyl, w) trifluoromethanesulfonyl, and x) tosyl;
- R3 is hydrogen, halogen, C1-5 alkyl, or C1-5 alkoxy;
- R4 is —X— (CH2)n-COOR5, and X is —O—, —S—, or —CH2—;
- R5 is hydrogen or C1-5 alkyl;
- and n is an integer that is 1, 2, or 3.
14 more elements
Dependencies are inferred from the claim text.