Claims
- 1. A compound of the formula ##STR4## in which n is 1 or 2 and m is 0 or 1; R is hydrogen, C.sub.1 -C.sub.4 alkyl, benzyl, or phenyl;
- Z is hydrogen or halo;
- X.sub.2, X.sub.3, X.sub.4, and X.sub.5 are independently selected from the group consisting of hydrogen, halo, trifluoromethyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkylthio, and --NR.sub.2 R.sub.3, in which R.sub.2 and R.sub.3 are independently hydrogen, C.sub.1 -C.sub.4 alkyl, benzyl, or phenyl, or R.sub.2 and R.sub.3 taken together with the nitrogen atom to which they are bonded form a 5- or 6-membered ring; or
- X.sub.r and X.sub.r+1, in which r is 2, 3, or 4, taken together form a divalent C.sub.3 -C.sub.5 alkylene group or methylenedioxy; provided at least one of X.sub.2, X.sub.3, X.sub.4, and X.sub.5 is NR.sub.2 R.sub.3 in which R.sub.2 and R.sub.3 taken together with the nitrogen atom to which they are bonded form a 6-membered ring; and
- Y.sub.5 and Y.sub.6 are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halo, and trifluoromethyl; and pharmaceutically acceptable salts thereof.
- 2. A compound of claim 1, in which Z is hydrogen.
- 3. A compound of claim 2, in which m is 0 and n is 2.
- 4. A compound of claim 3, in which Y.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, or halo, and Y.sub.6 is hydrogen.
- 5. A compound of claim 4, in which Y.sub.5 is halo, methoxy, or methyl.
- 6. A compound of claim 4, in which at least two of X.sub.2 X.sub.3 X.sub.4 and X.sub.5 are hydrogen.
- 7. A compound of claim 1, in which m is 0 and n is 2.
- 8. A compound of claim 1, in which Y.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, or halo, and Y.sub.6 is hydrogen.
- 9. A compound of claim 1, in which at least two of X.sub.2 X.sub.3 X.sub.4 and X.sub.5 are hydrogen.
- 10. A compound of claim 6, in which X.sub.2, X.sub.4, and X.sub.5 are hydrogen.
- 11. A compound of claim 1, in which Z is halo.
- 12. A compound of claim 12, in which Z is chloro.
- 13. A compound of claim 12, in which m is 0 and n is 2.
- 14. A compound of claim 13, in which Y.sub.5 is chloro or bromo.
- 15. A compound of claim 1, in which m is 1 and R is selected from the group consisting of methyl, benzyl, and phenyl.
- 16. A compound of claim 15, in which n is 1.
- 17. A compound of claim 16, in which Y.sub.5 is hydrogen or bromo and Y.sub.6 is hydrogen.
- 18. A compound of claim 6, in which X.sub.3 is C.sub.1 -C.sub.6 alkyl.
- 19. A compound of claim 6, in which X.sub.3 is C.sub.1 -C.sub.6 alkoxy.
- 20. A method for inhibiting interaction of cholecystokinin with its receptors in a mammal and thereby antagonizing the influence of endogenous cholecystokinin, which comprises administering to said mammal a compound of claim 1 in an amount effective to antagonize the influence of cholecystokinin in said mammal.
- 21. A pharmaceutical formulation comprising, as the active ingredient, an effective amount of a compound of claim 1, and a pharmaceutically acceptable carrier, excipient, or diluent therefor.
Parent Case Info
This application is a division of application Ser. No. 07/581,943, filed Sep. 13, 1990, now U.S. Pat. No. 5,075,313.
Non-Patent Literature Citations (5)
Entry |
Varma et al., Indian J. Chem. 18B, 275-277 (1979). |
Agarwal et al., Acta Pharm. Jugosl. 32, 37-44 (1982). |
Agarwal et al., J. Chem. Soc. Pak. 6, 89-94 (1984). |
Gupta et al., Indian J. Chem. 26B, 1197-1199 (1987). |
Boltze, et al., Chem. Abstr. 63: 4289 d (1965), abstracting Arzneim. Forsch. 13, 688-701 (1963). |
Divisions (1)
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Number |
Date |
Country |
Parent |
581943 |
Sep 1990 |
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