Nucleoside Phosphonate Analogs

• US 20110071101A1
• Filed: 04/09/2008
• Published: 03/24/2011
• Est. Priority Date: 04/25/2003
• Status: Abandoned Application

• Current Assignee: Adrian S. Ray, Aesop Cho, Alan X. Huang, Choung U. Kim, Christopher P. Lee, Constantine G. Boojamra, David A. Oare, James M. Chen, Lee S. Chong, Maria Fardis, Sundaramoorthi Swaminathan, Thorsten Kirschberg, Vidya K. Prasad, William J. Watkins, Xiaowu Chen
• Original Assignee: Adrian S. Ray, Aesop Cho, Alan X. Huang, Choung U. Kim, Christopher P. Lee, Constantine G. Boojamra, David A. Oare, James M. Chen, Lee S. Chong, Maria Fardis, Sundaramoorthi Swaminathan, Thorsten Kirschberg, Vidya K. Prasad, William J. Watkins, Xiaowu Chen
• Inventors: Watkins, William J., Prasad, Vidya K., Lee, Christopher P., Chen, Xiaowu, Swaminathan, Sundaramoorthi, Kirschberg, Thorsten, Chen, James M., Huang, Alan X., Oare, David A., Cho, Aesop, Fardis, Maria, Chong, Lee S., Kim, Choung U., Boojamra, Constantine G., Ray, Adrian S.
• Application Number:
  US12/100,314
• Publication Number:
  US 20110071101A1
• Time in Patent Office: Days
• US Class Current: 514/52
• CPC Class Codes: C07F 9/65586 at least one of the hetero rings does not contain nitrogen as ring hetero atom
• CPC Class Codes: C07F 9/6561 containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
• CPC Class Codes: C07F 9/65616 containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
• CPC Class Codes: C07H 19/056 Triazole or tetrazole radicals
• CPC Class Codes: C07H 19/06 Pyrimidine radicals
• CPC Class Codes: C07H 19/14 Pyrrolo-pyrimidine radicals
• CPC Class Codes: C07H 19/173 with 2-deoxyribosyl as the saccharide radical
• CPC Class Codes: C07H 7/04 Carbocyclic radicals

Abstract

The invention is related to phosphorus substituted nucleoside compounds and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Claims

1. A conjugate comprising a nucleoside linked to one or more phosphonate groups;

or a pharmaceutically acceptable salt or solvate thereof.

2. The conjugate of claim 1, or a pharmaceutically acceptable salt or solvate thereof, that is a compound of Formula 240:

3. The conjugate of claim 2, or a pharmaceutically acceptable salt or solvate thereof, which has the formula:

)

[DRUG]-(A⁰)_nn

wherein;

DRUG is a compound of formula 240; and

nn is 1, 2, or 3.

4. The conjugate of claim 2 which has any one of formulae 18 and 19:

28. The conjugate of claim 2 wherein each A³ is of the formula:

29. The conjugate of claim 2 wherein each A³ is of the formula:

30. The conjugate of claim 2 wherein each A³ is of the formula:

31. The conjugate of claim 2 wherein each A³ is of the formula:

32. The conjugate of claim 2 wherein each A³ is of the formula:

57. The conjugate of claim 2 wherein each A³ is of the formula:

58. The conjugate of claim 2 wherein each A³ is of the formula:

59. The conjugate of claim 2 wherein each A³ is of the formula:

60. The conjugate of claim 2 wherein each A³ is of the formula:

61. The conjugate of claim 2 wherein each A³ is of the formula:

62. The conjugate of claim 2 wherein each A³ is of the formula:

63. The conjugate of claim 3 wherein A⁰ is of the formula:

107. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a conjugate, or a pharmaceutically acceptable salt or solvate thereof, as described in claim 2.

108. A unit dosage form comprising a conjugate as described in claim 2, or a pharmaceutically acceptable salt or solvate thereof;

and a pharmaceutically acceptable excipient.

5-27. -27. (canceled)

33-56. -56. (canceled)

64-106. -106. (canceled)

109-114. -114. (canceled)