Claims
- 1. A compound of Formula (I),
- 2. The compound of claim 1 wherein A is phenyl or substituted phenyl.
- 3. The compound of claim 2 wherein -R2-R3- is
- 4. The compound of claim 2 wherein a is a double bond.
- 5. The compound of claim 4 wherein R′ is -Bp-G-Eq-W or phenyl independently substituted with one or more groups selected from alkyl, substituted alkyl, alkoxy, nitro, amino,
- 6. The compound of claim 5 wherein
(a) p is 0 and q is 1; (b) G is phenyl or substituted phenyl; (c) E is NHCO; and (d) W is phenyl or substituted phenyl.
- 7. The compound of claim 6 wherein R5 is —CONZ1Z2 wherein Z1 and Z2 are as claimed in claim 1.
- 8. The compound of claim 2 wherein R5 is —CONZ1Z2 wherein Z1 and Z2 are as claimed in claim 1.
- 9. The compound of claim 2 wherein X is selected from CH2, CHOH, and C═O.
- 10. The compound of claim 9 wherein -R2-R3- is
- 11. The compound of claim 10 wherein
R1 is H; R4 is H; R5 is H; R′is substituted phenyl or -Bp-G-Eq-W wherein
(a) W is phenyl or substituted phenyl; (b) E is NHCO; and (c) p is 0.
- 12. The compound of claim 2 wherein n is 1 or 2.
- 13. The compound of claim 12 wherein n is 1 and a is a double bond.
- 14. The compound of claim 1 which is (S)-4-(2-fluorophenylbenzoyl-4-aminobenzoyl)-3′-(2-(N,N-dimethylaminoethylaminocarbonyl))-4-aza-[6,4]-spiro-[5,6]-benzoundec-2′-ene.
- 15. The compound of claim 1 which is (R)-4-(2-fluorophenylbenzoyl-4-aminobenzoyl)-3′-(2-(N,N-dimethylaminoethylaminocarbonyl))-4-aza-[6,4]-spiro-[5,6]-benzoundec-2′-ene.
- 16. The compound of claim 1, which is (S)-4-(2-phenylbenzoyl-4-aminobenzoyl)-3′-(2-(N,N-dimethylaminoethylaminocarbonyl))-4-aza-[6,4]-spiro-[5,6]-benzoundec-2′-ene.
- 17. The compound of claim 1 which is (R)-4-(2-phenylbenzoyl-4-aminobenzoyl)-3′-(2-(N,N-dimethylaminoethylaminocarbonyl))-4-aza-[6,4]-spiro-[5,6]-benzoundec-2′-ene.
- 18. The compound of claim 1 which is 4-[3-methoxy-4-(3-hydroxymethylpyrrol-1-yl)benzoyl]-3′-[2-(N,N-dimethylamino)ethylcarboxamido]-4-aza-[6,4]-spiro-[5,6]-benzoundec-2′-ene.
- 19. A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier.
- 20. A method of treating a subject suffering from a condition associated with vasopressin receptor activity, which comprises administering to the subject a therapeutically effective amount of the compound of Formula I as defined in claim 1.
- 21. A method of inhibiting in a subject the onset of a condition associated with vasopressin receptor activity, which comprises administering to the subject a prophylactically effective dose of a compound of Formula I as defined in claim 1.
- 22. The method of claim 19 or 20 wherein said condition is selected from inner ear disorders, hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, water retention, aggression, obsessive-compulsive disorders, dysmenorrhea, nephrotic syndrome, and central nervous injuries.
- 23. The method of claim 21 wherein said condition is congestive heart failure or cardiac insufficiency.
- 24. A process for making a pharmaceutical composition comprising mixing any of the compounds according to claim 1 and a pharmaceutically acceptable carrier.
- 25. An intermediate of a formula selected from
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This application claims priority from U.S. Ser. No. 60/216,220, filed Jul. 5, 2000.
Provisional Applications (1)
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Number |
Date |
Country |
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60216220 |
Jul 2000 |
US |