Claims
- 1. A compound of the formula (I): ##STR127## wherein A, B, Y and Z are each hydrogen, or the pair (1) A and B and/or the pair (2) Y and Z together represent a direct valence bond between the carbon atoms to which they are attached, thereby forming a double bond therebetween; W is a group of --COR or a group of X; and n is zero or an integer of 1 to 4 when W is the group of --COR; n is an integer of 1 to 3 when W is ghe group of X; R is selected from the group consisting of:
- (1) a group of the formula ##STR128## wherein R.sup.1 is hydrogen or lower alkyl and m is an integer of from 1 to 5;
- (2) a group of the formula ##STR129## wherein k and l are the same or different and each is an integer of from 1 to 5;
- (3) a group of the formula
- --NHCH.sub.2 COOR.sup.2
- wherein R.sup.2 is hydrogen, lower alkyl or aryl;
- (4) a group of the formula ##STR130## wherein p is an integer of from 0 to 5 and R.sup.3 and R.sup.4 are each hydrogen or lower alkyl;
- (5) a group of the formula ##STR131## wherein q is an integer of from 1 to 5, R.sup.5, R.sup.6 and R.sup.7 are each hydrogen or lower alkyl, and X is a halogen;
- (6) a group of the formula ##STR132## wherein r is 2 or 3 and R.sup.8 is lower alkyl; (7) a group of the formula ##STR133## wherein s is 2 or 3, R.sup.9 and R.sup.10 are each lower alkyl and X is a halogen;
- (8) a group of the formula ##STR134## wherein D is a group of the formula --(CH.sub.2).sub.t OH, in which t is an integer of from 0 to 5, a group of the formula ##STR135## wherein u is an integer of from 0 to 5 and R.sup.11 and R.sup.12 are each hydrogen or lower alkyl, or a group of the formula ##STR136## wherein v is an integer of from 0 to 5, R.sup.13, R.sup.14 and R.sup.15 are each lower alkyl and X is a halogen;
- (9) a group of the formula ##STR137## wherein R.sup.16 is hydrogen or lower alkyl and w is an integer of from 1 to 5;
- (10) a group of the formula ##STR138## wherein R.sup.17 is hydrogen or lower alkyl and x is an integer of from 0 to 5; and
- (11) a group of the formula ##STR139## wherein R.sup.18 is hydrogen and y is integer of 1 to 5, X is selected from the group consisting of:
- (1) a group of the formula ##STR140## wherein b is zero or an integer of 1 to 5 and R.sup.31 is a lower alkyl, (2) a group of the formula ##STR141## wherein R.sup.34 is a lower alkyl, (3) a group of the formula ##STR142## (4) a group of the formula
- --CONH--CH.sub.2 CH(OH)CH.sub.2 OH
- or a pharmaceutically acceptable salt thereof.
- 2. A compound as claimed in claim 1 wherein W is the group of --COR.
- 3. A compound as claimed in claim 1 wherein W is X.
- 4. A pharmaceutical composition having antithrombic activity which comprises a therapeutically effective amount of a compound as defined in claim 1, in association with a pharmaceutically acceptable carrier, diluent or vehicle.
- 5. A pharmaceutical composition having anti-PAF activity which comprises a therapeutically effective amount of a compound as claimed in claim 1, in association with a pharmaceutically acceptable carrier, diluent or vehicle.
- 6. A compound having the formula ##STR143## wherein A, B, Y and Z are each hydrogen, or the pair (1) A and B and/or the pair (2) Y and Z together represent a direct valence bond between the carbon atoms to which they are attached, thereby forming a double bond therebetween; n is an integer of 1 to 3; and X is selected from the group consisting of:
- (1) a group of the formula ##STR144## wherein b is zero or an integer of 1 to 5 and R.sup.31 is a lower alkyl, (2) a group of the formula ##STR145## wherein R.sup.34 is a lower alkyl, (3) a group of the formula ##STR146## and (4) CONH--CH.sub.2 CH(OH)CH.sub.2 OH,
- or a pharmaceutically acceptable salt thereof.
- 7. A compound as claimed in claim 6 in which X is ##STR147##
- 8. A compound of the formula: ##STR148## wherein A, B, Y and Z are each hydrogen, or the pair (1) A and B and/or the pair (2) Y and Z together represent a direct valence bond between the carbon atoms to which they are attached, thereby forming a double bond therebetween; n is zero or an integer of 1 to 4; R is selected from the group consisting of:
- (1) a group of the formula
- --NHCH.sub.2 COOR.sup.2
- wherein R.sup.2 is hydrogen, lower alkyl or aryl;
- (2) a group of the formula ##STR149## wherein q is an integer of from 1 to 5, R.sup.5, R.sup.6 and R.sup.7 are each hydrogen or lower alkyl, and X is a halogen;
- (3) a group of the formula ##STR150## wherein r is 2 or 3 and R.sup.8 is lower alkyl; (4) a group of the formula ##STR151## wherein s is 2 or 3, R.sup.9 and R.sup.10 are each lower alkyl and X is a halogen;
- (5) a group of the formula ##STR152## wherein D is a group of the formula --(CH.sub.2).sub.t OH, in which t is an integer of from 0 to 5, a group of the formula ##STR153## wherein u is an integer of from 0 to 5 and R.sup.11 and R.sup.12 are each hydrogen or lower alkyl, or a group of the formula ##STR154## wherein v is an integer of from 0 to 5, R.sup.13, R.sup.14 and R.sup.15 are each lower alkyl and X is a halogen;
- (6) a group of the formula ##STR155## wherein R.sup.16 is hydrogen or lower alkyl and w is an integer of from 1 to 5;
- (7) a group of the formula ##STR156## wherein R.sup.17 is hydrogen or lower alkyl and x is an integer of from 0 to 5; and
- (8) a group of the formula ##STR157## wherein R.sup.18 is hydrogen or lower alkyl and y is an integer of 1 to 5,
- or a pharmaceutically acceptable salt thereof.
- 9. A compound as claimed in claim 8 in which R is ##STR158##
- 10. A compound as claimed in claim 8 in which R is ##STR159##
- 11. A compound as claimed in claim 8 in which R is ##STR160##
- 12. A compound of the formula ##STR161## wherein n is an integer of 1 to 4; p is an integer of from 0 to 5 and R.sup.3 and R.sup.4 are each hydrogen or lower alkyl, or a pharmaceutically acceptable salt thereof.
- 13. A compound of the formula ##STR162## wherein n is an integer of 1 to 4; and R is selected from the group consisting of:
- (1) a group of the formula ##STR163## wherein R.sup.1 is hydrogen or lower alkyl and m is an integer of from 1 to 5, and
- (2) a group of the formula ##STR164## wherein k and l are the same or different and each is an integer of from 1 to 5,
- or a pharmaceutically acceptable salt thereof.
- 14. A compound of the formula ##STR165## wherein n is an integer of 1 to 4, or a pharmaceutically acceptable salt thereof.
- 15. A compound having the formula: ##STR166## wherein A, B, Y and Z are each hydrogen, or the pair (1) A and B and/or the pair (2) Y and Z together represent a direct valence bond between the carbon atoms to which they are attached, thereby forming a double bond therebetween; n is zero or an integer of 1 to 4; R.sup.1 and R.sup.2 is hydrogen, lower alkyl or aryl; or a pharmaceutically acceptable salt thereof.
- 16. A compound having the formula: ##STR167## wherein A, B, Y and Z are each hydrogen, or the pair (a) A and B and/or the pair (2) Y and Z together represent a direct valence bond between the carbon atoms to which they are attached, thereby forming a double bond therebetween; n is zero or an integer of 1 to 4; q is an integer of 1 to 5; R.sup.5, R.sup.6 and R.sup.7 each is hydrogen or lower alkyl, and X is halogen,, or a pharmaceutically acceptable salt thereof.
- 17. A compound having the formula ##STR168## wherein A, B, Y and Z are each hydrogen, of the pair (1) A and B and/or the pair (2) Y and Z together represent a direct valence bond between the carbon atoms to which they are attached, thereby forming a double bond therebetween; n is zero or is an integer of 1 to 4; s is 2 or 3; R.sup.9 and R R.sup.10 each is lower alkyl, and X is halogen, or a pharmaceutically acceptable salt thereof.
- 18. A compound having the formula: ##STR169## wherein A, B, Y and Z are each hydrogen, or the pair (1) A and B and/or the pair (2) Y and Z together represent a direct valence bond between the carbon atoms to which they are attached, thereby forming a double bond therebetween; n is zero or an integer of 1 to 4; and w is an integer of 1 to 5, or a pharmaceutically acceptable salt thereof.
- 19. A compound having the formula: ##STR170## wherein A, B, Y and Z are each hydrogen, or the pair (1) A and B and/or the pair (2) Y and Z together represent a direct valence bond between the carbon atoms to which they are attached, thereby forming a double bond therebetween; n is zero or an integer of 1 to 4; R.sup.18 is hydrogen or lower alkyl and y is an integer of 1 to 5, or a pharmaceutically acceptable salt thereof.
- 20. The compound according to claim 15 in which each of the pair A, B and the pair X, Y together represent a direct valence bond between the carbon atoms to which they are attached, thereby forming a double bond therebetween.
- 21. The compound according to claim 20 in which n is 3.
- 22. The compound according to claim 16 in which each of the pair, A, B and the pair X, Y together represent a direct valence bond between the carbon atoms to which they are attached, thereby forming a double bond therebetween.
- 23. The compound according to claim 22 in which n is 3.
- 24. The compound according to claim 17 in which each of the pair A, B and the pair X, Y together represent a direct valence bond between the carbon atoms to which they are attached, thereby forming a double bond therebetween.
- 25. The compound according to claim 24 in which n is 3.
- 26. The compound according to claim 18 in which each of the pair, A, B and the pair X, Y together represent a direct valence bond between the carbon atoms to which they are attached, thereby forming a double bond therebetween.
- 27. The compound according to claim 26 in which n is 3.
- 28. The compound according to claim 19 in which each of the pair A, B and the pair X, Y together represent a direct valence bond between the carbon atoms to which they are attached, thereby forming a double bond therebetween.
- 29. The compound according to claim 28 in which n is 3.
- 30. The compound according to claim 6 in which each of the pair A, B and the pair X, Y together represent a direct valence bond between the carbon atoms to which they are attached, thereby forming a double bond therebetween.
- 31. The compound according to claim 30 in which n is 3.
- 32. The compound according to claim 8 in which each of the pair A, B and the pair X, Y together represent a direct valence bond between the carbon atoms to which they are attached, thereby forming a double bond therebetween.
- 33. The compound according to claim 32 in which n is 3.
Priority Claims (1)
Number |
Date |
Country |
Kind |
57-208678 |
Nov 1982 |
JPX |
|
Parent Case Info
This is a continuation of application Ser. No. 885,321, filed July 14, 1986, now U.S. Pat. No. 4,742,058, which is a continuation of Ser. No. 554,423, filed Nov. 23, 1983, now abandoned.
US Referenced Citations (5)
Continuations (2)
|
Number |
Date |
Country |
Parent |
885321 |
Jul 1986 |
|
Parent |
554423 |
Nov 1983 |
|