Claims
- 1. A compound of formula I:
- 2. The compound of claim 1 wherein the detectable group is aryl or Het, optionally substituted with one or more substituents independently selected from —COORb, —S(O)nNRbRb, halo, cyano, nitro, aryl, heterocycle, (C1-C10)alkoxy, (C2-C6)alkenyl, —C(═O)NRbRb, —OC(═O)NRbRb, —NRbRb, or —S(O)nRb, where each Rb is independently hydrogen, (C1-C10)alkyl, or (C1-C10)alkanoyl.
- 3. The compound of claim 2 wherein aryl or Het is phenyl, indenyl, naphthyl, anthracenyl, or anthranil, which aryl or Het is optionally substituted with one or more substituents independently selected from —COORb, —S(O)nNRbRb, halo, cyano, nitro, aryl, heterocycle, (C2-C6)alkenyl, —C(═O)NRbRb, —OC(═O)NRbRb, —NRbRb, or —S(O)nRb, where each Rb is independently hydrogen, (C1-C10)alkyl, or (C1-C10)alkanoyl.
- 4. The compound of claim 1 wherein R1 is substituted phenyl.
- 5. The compound of claim 1 wherein R1 is phenyl substituted with —COORb.
- 6. The compound of claim 1 wherein R1 is 2-methoxycarboxy phenyl.
- 7. The compound of claim 1 wherein R1 is substituted naphthyl.
- 8. The compound of claim 1 wherein R1 is naphthyl substituted with a —S(O)nNRbRb.
- 9. The compound of claim 1 wherein R1 is naphthyl substituted at the 5-position with a —S(O)nNRbRb substituent.
- 10. The compound of claim 1 wherein R1 is 5-N,N′—dimethylaminosulfonyl naphthy-1-yl.
- 11. The compound of claim 1 wherein R2 is OH.
- 12. The compound of claim 1 wherein R2 is (C1-C10)alkanoyloxy.
- 13. The compound of claim 1 wherein R2 is —O—P(═O)(—ORa)2.
- 14. The compound of claim 1 wherein R2 is —O—P(═O)(—ORa)—O—P(═O)(—ORa)2.
- 15. The compound of claim 1 wherein R2 is —CH2—O—P(═O)(—ORa)2.
- 16. The compound of claim 1 wherein R2 is —CH2—O—P(═O)(—ORa)—O—P(═O)(—ORa)2.
- 17. The compound of claim 1 wherein R2 is —CH2—P(═O)(—ORa)2.
- 18. The compound of claim 1 wherein R2 is —CH{—P(═O)(—ORa)2}2.
- 19. The compound of claim 1 wherein R2 is —CH2—P(═O)(—ORa)—O—P(═O)(—ORa)2.
- 20. The compound of claim 1 wherein R2 is —CH═CH{—P(═O)(—ORa)2}.
- 21. The compound of claim 1 wherein R2 is —CH═C {—P(═O)(—ORa)2}2.
- 22. The compound of claim 1 wherein Ra is hydrogen.
- 23. The compound of claim 1 wherein Ra is —C(═O)—CH3.
- 24. The compound of claim 1 wherein Ra is —CH3.
- 25. The compound of claim 1 wherein Ra is —CH2—O—(C1-C6)alkanoyl.
- 26. The compound of claim 2 wherein Rb is hydrogen.
- 27. The compound of claim 2 wherein Rb is —CH3.
- 28. The compound of claim 1 wherein n is 1.
- 29. The compound of claim 1 wherein n is 2.
- 30. The compound of claim 1 wherein n is 3.
- 31. The compound of claim 1 wherein X is —O—.
- 32. The compound of claim 1 wherein X is —S—.
- 33. A pharmaceutical composition comprising a compound as described in claim 1 and a pharmaceutically acceptable diluent or carrier.
- 34. A method of treating cancer, comprising administering to a mammal afflicted with cancer, an amount of a compound as described in claim 1 effective to treat said cancer.
- 35. A method of inhibiting a prenylation transferase enzyme or synthase enzyme comprising contacting the enzyme with an effective amount of a compound as described in claim 1.
- 36. A method of accessing the metabolic status of an enzyme comprising:
contacting the enzyme with an effective amount of a mixture of a farnesol analog compound and a geraniol or geranylgeraniol analog compound as described in claim 1; and measuring the relative ratio of farnesylation to geranylgeranylation of the famesol and the geraniol or geranylgeraniol analog compounds accomplished by the enzyme.
- 37. A compound as described in claim 1 for use in medical therapy or diagnosis.
- 38. The compound of claim 37 wherein the therapy or diagnosis is treating cancer.
- 39. The use of a compound as described in claim 1 for the manufacture of a medicament useful for the treatment of cancer.
- 40. The use of a compound as described in claim 1 for the manufacture of a medicament useful for inhibiting prenylation transferase enzymes in a mammal.
- 41. A protein conjugate comprising a protein linked to a fluorescent fragment of a compound of claim 1.
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application is a divisional under 37 C.F.R. 1.53(b) of U.S. patent application Ser. No. 10/116,737 filed Apr. 3, 2002, which claimed priority under 35 U.S.C. 119(e) to U.S. Provisional Patent Application Serial No. 60/281,170, filed Apr. 3, 2001, which applications are incorporated by reference and made a part hereof.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60281170 |
Apr 2001 |
US |
Divisions (1)
|
Number |
Date |
Country |
Parent |
10116737 |
Apr 2002 |
US |
Child |
10780391 |
Feb 2004 |
US |