IP Library Granted Patent US 8,163,718
Granted Patent B2
US 8,163,718 · App. 12/388,789 · Granted Apr 24, 2012

Nucleoside analogues containing phosphonate or phosphonamide groups

Assignee: Gilead Sciences, Inc.
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Quick Facts
Patent No.
US 8,163,718
App. No.
12/388,789
Granted
Apr 24, 2012
Kind
B2
Abstract

Novel compounds having structure ( 1 ) wherein Z, is N or CH to form a purine, Y, R 1 , R 2′ and R 2 are defined in the specification, are provided for use in the treatment of tumors and the prophylaxis or treatment of viral infections.

Claims (15)

1. A compound having structure (4)

wherein each R a independently is C 1 -C 4 alkyl, or benzyl, each R b independently is C 1 -C 4 alkyl, R 10 is C 1 -C 8 alkyl, or C 2 -C 8 alkenyl, or C 2 -C 8 alkynyl, wherein C 1 -C 8 alkyl is optionally substituted by one C 1 -C 4 alkoxy group or pharmaceutically acceptable salt or enriched optical isomer thereof.

2. A compound having structure (5)

wherein each R b independently is C 1 -C 4 alkyl, or benzyl, R 10 is C 1 -C 4 alkyl; or a pharmaceutically acceptable salt or enriched optical isomer thereof.

3. A compound having structure (7):

wherein

each R c independently is C 1 -C 4 alkyl that is substituted by one C 1 -C 4 alkyl-O—C(O)—O-group; R 10 is C 1 -C 4 alkyl; or a pharmaceutically acceptable salt or an enriched optical isomer thereof.

4. A compound selected from the group consisting of:

or a pharmaceutically acceptable salt, or enriched optical isomer thereof.

5. A pharmaceutical composition comprising a therapeutically effective amount of the compound according to claim 1 and a carrier.

6. A pharmaceutical composition comprising a therapeutically effective amount of the compound according to claim 2 and a carrier.

7. A pharmaceutical composition comprising a therapeutically effective amount of the compound according to claim 3 and a carrier.

8. A pharmaceutical composition comprising a therapeutically effective amount of the compound according to claim 4 and a carrier.

9. A pharmaceutical composition comprising a therapeutically effective amount of the compound according to claim 3 and a second therapeutic agent selected from an anti-viral agent or an anti-tumor/cancer agent.

10. A pharmaceutical composition comprising a therapeutically effective amount of the compound according to claim 4 and a second therapeutic agent selected from an anti-viral agent or an anti-tumor/cancer agent.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 21, 2009
From: BIRKUS, GABRIEL; RAY, ADRIAN S.; TUMAS, DANIEL B.; WATKINS, WILLIAM J.
To: GILEAD SCIENCES, INC.
Reel/Frame 022718/0941 →
Continuity (2)
Provisional Application 61030148 · Feb 20, 2008
Related Publication 20090232768A1 · Sep 17, 2009