Tetraphosphonate bicyclic trisanhydrides
First Claim
Patent Images
1. A compound having the following structure:
-
wherein each of R1, R2, R3, and R4 is independently H, OH or F;
X is O, S, mono- or di-halomethylene, or NR wherein R is H or alkyl, or CH2;
Y is OH, SH or F; and
each of W1 and W2 is independently H, OH, ═
O, OR, SH, SR, NH2, NHR or NR2, wherein R is C1-C5 alkyl and n is an integer from 1 to 5.
4 Assignments
0 Petitions
Accused Products
Abstract
Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biolologically active compounds, and the compounds which may be synthesized from such intermediates.
8 Citations
28 Claims
-
1. A compound having the following structure:
-
wherein each of R1, R2, R3, and R4 is independently H, OH or F;
X is O, S, mono- or di-halomethylene, or NR wherein R is H or alkyl, or CH2;
Y is OH, SH or F; and
each of W1 and W2 is independently H, OH, ═
O, OR, SH, SR, NH2, NHR or NR2, wherein R is C1-C5 alkyl and n is an integer from 1 to 5.- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28)
P1-(2′
,3′
-O-isopropylideneadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)methylenebis(phosphonate),P1-(2′
,3′
-O-isopropylideneadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-(2′
,3′
-O-isopropylideneadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-(2′
,3′
-O-isopropylideneadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-(2′
,3′
-O-isopropylideneadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylocta-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-(3′
-O-acetyl-2′
-fluoro-2′
-deoxyadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-(3′
-O-acetyl-2′
-fluoro-2′
-deoxyadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-(3′
-O-acetyl-2′
-fluoro-2′
-deoxyadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-(3′
-O-acetyl-2′
-fluoro-2′
-deoxyadenosin-5′
-yl)-P2-(7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-(3′
-O-acetyl-2′
-fluoro-2′
-deoxyadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-(2′
-O-acetyl-3′
-fluoro-3′
-deoxyadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-(2′
-O-acetyl-3′
-fluoro-3′
-deoxyadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-(2′
-O-acetyl-3′
-fluoro-3′
-deoxyadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-(2′
-O-acetyl-3′
-fluoro-3′
-deoxyadenosin-5′
-yl)-P2-(7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-(2′
-O-acetyl-3′
-fluoro-3′
-deoxyadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-O-acetyl-2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-O-acetyl-2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2-ene-5′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-O-acetyl-2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-O-acetyl-2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2-ene-7′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-O-acetyl-2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl) adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-ene-8′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-O-acetyl-3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2-ene-4′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-O-acetyl-3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2-ene-5′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-O-acetyl-3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-O-acetyl-3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-O-acetyl-3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-(2′
,3′
-O-isopropylideneguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-(2′
,3′
-O-isopropylideneguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-(2′
,3′
-O-isopropylideneguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-(2′
,3′
-O-isopropylideneguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-(2′
,3′
-O-isopropylideneguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-(3′
-O-acetyl-2′
-fluoro-2′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)lmethylenebis(phosphonate),P1-(3′
-O-acetyl-2′
-fluoro-2′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-(3′
-O-acetyl-2′
-fluoro-2′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-(3′
-O-acetyl-2′
-fluoro-2′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-(3′
-O-acetyl-2′
-fluoro-2′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-(2′
-O-acetyl-3′
-fluoro-3′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-(2′
-O-acetyl-3′
-fluoro-3′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-(2′
-O-acetyl-3′
-fluoro-3′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-(2′
-O-acetyl-3′
-fluoro-3′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-(2′
-O-acetyl-3′
-fluoro-3′
-deoxyguanosin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-O-acetyl-2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl) guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-O-acetyl-2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl) guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-O-acetyl-2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl) guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-O-acetyl-2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl) guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-O-acetyl-2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl) guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-O-acetyl-3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-O-acetyl-3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-O-acetyl-3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-O-acetyl-3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-O-acetyl-3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4′
-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-(2′
,3′
-O-isopropylideneinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-(2′
,3′
-O-isopropylideneinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-(2′
,3′
-O-isopropylideneinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-(2′
,3′
-O-isopropylideneinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-(2′
,3′
-O-isopropylideneinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-(3′
-O-acetyl-2′
-fluoro-2′
-deoxyinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-(3′
-O-acetyl-2′
-fluoro-2′
-deoxyinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-(3′
-O-acetyl-2′
-fluoro-2′
-deoxyinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-(3′
-O-acetyl-2′
-fluoro-2′
-deoxyinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-(3′
-O-acetyl-2′
-fluoro-2′
-deoxyinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-(2′
-O-acetyl-3′
-fluoro-3′
-deoxyinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-(2′
-O-acetyl-3′
-fluoro-3′
-deoxyinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-(2′
-O-acetyl-3′
-fluoro-3′
-deoxyinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-(2′
-O-acetyl-3′
-fluoro-3′
-deoxyinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-(2′
-O-acetyl-3′
-fluoro-3′
-deoxyinosin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-O-acetyl-2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-O-acetyl-2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-O-acetyl-2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-O-acetyl-2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-O-acetyl-2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-O-acetyl-3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-nmethoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-O-acetyl-3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-O-acetyl-3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-O-acetyl-3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate), andP1-[9-(2′
-O-acetyl-3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate).
-
-
3. The compound of claim 1, wherein the compound is selected from the group consisting of:
-
P1-(adenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methylphthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-(adenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7?-yl)]methylenebis(phosphonate),P1-(adenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2-ene-8′
-yl)]methylenebis(phosphonate),P1-(2′
-fluoro-2′
-deoxyadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]-methylenebis(phosphonate),P1-(2′
-fluoro-2′
-deoxyadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]-methylenebis(phosphonate),P1-(2′
-fluoro-2′
-deoxyadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2-ene-6′
-yl)]methylenebis(phosphonate),P1-(2′
-fluoro-2′
-deoxyadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]-methylenebis(phosphonate),P1-(2′
-fluoro-2′
-deoxyadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]-methylenebis(phosphonate),P1-(3′
-fluoro-3′
-deoxyadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]-methylenebis(phosphonate),P1-(3′
-fluoro-3′
-deoxyadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]-methylenebis(phosphonate),P1-(3′
-fluoro-3′
-deoxyadenosin-5′
-yl)-P2-[-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]-methylenebis(phosphonate),P1-(3′
-fluoro-3′
-deoxyadenosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]-methylenebis(phosphonate),P1-(3′
-fluoro-3′
-deoxyadenosin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]-methylenebis(phosphonate),P1-[9-(2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl] P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)lmethylenebis(phosphonate),P1-[9-(2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)adenin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-(guanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-(guanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-(guanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-(guanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-(guanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2-ene-8′
-yl)]methylenebis(phosphonate),P1-(2′
-fluoro-2′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]-methylenebis(phosphonate),P1-(2′
-fluoro-2′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-(2′
-fluoro-2′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2-ene-6′
-yl)]methylenebis(phosphonate),P1-(2′
-fluoro-2′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-(2′
-fluoro-2′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-(3′
-fluoro-3′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-(3′
-fluoro-3′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-(3′
-fluoro-3′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-(3′
-fluoro-3′
-deoxyguanosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-(3′
-fluoro-3′
-deoxyguanosin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)guanin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-(inosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-(inosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-(inosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-(inosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-(inosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2-ene-8′
-yl)]methylenebis(phosphonate),P1-(2′
-fluoro-2′
-deoxyinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-(2′
-fluoro-2′
-deoxyinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-(2′
-fluoro-2′
-deoxyinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2-ene-6′
-yl)]methylenebis(phosphonate),P1-(2′
-fluoro-2′
-deoxyinosin-5′
-yl)-P2-[mycophenol-6-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-(2′
-fluoro-2′
-deoxyinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-(3′
-fluoro-3′
-deoxyinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-(3′
-fluoro-3′
-deoxyinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-(3′
-fluoro-3′
-deoxyinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-(3′
-fluoro-3′
-deoxyinosin-5′
-yl)-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-(3′
-fluoro-3′
-deoxyinosin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)-hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)-hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate),P1-[9-(2′
-fluoro-2′
-deoxy-β
-D-arabinofuranosyl)-hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methylphthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)-hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylbut-2′
-ene-4′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)-hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylpent-2′
-ene-5′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)-hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhex-2′
-ene-6′
-yl)]methylenebis(phosphonate),P1-[9-(3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)-hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methylhept-2′
-ene-7′
-yl)]methylenebis(phosphonate), andP1-[9-(3′
-fluoro-3′
-deoxy-β
-D-arabinofuranosyl)-hypoxanthin-5′
-yl]-P2-[7-hydroxy-5-methoxy-4-methyl-phthalan-1-on-6-yl-(3′
-methyloct-2′
-ene-8′
-yl)]methylenebis(phosphonate).
-
-
4. The compound of claim 1, wherein X is CH2.
-
5. The compound of claim 1, wherein X is dihalomethylene.
-
6. The compound of claim 1, wherein W1 is NH2, NRH, or NR2.
-
7. The compound of claim 1, wherein W2 is H.
-
8. The compound of claim 1, wherein W2 is NH2, NRH, or NR2.
-
9. The compound of claim 1, wherein R1 and R2 are OH, and R3 and R4 are H.
-
10. The compound of claim 1, wherein Y is OH.
-
11. The compound of claim 1, wherein n is 1.
-
12. The compound of claim 1, wherein n is 3.
-
13. The compound of claim 1, wherein X is CH2, and W1 and W2 are NH2, NRH, or NR2, and W2 is H.
-
14. The compound of claim 1, wherein X is CH2, and W1 and W2 are NH2, NRH, or NR2, and W2 is H.
-
15. The compound of claim 1, wherein X is dihalomethylene, W1 and W2 are NH2, NRH, or NR2, and W2 is H.
-
16. The compound of claim 1, wherein X is dihalomethylene, and W1 and W2 are NH2, NRH, or NR2.
-
17. The compound of claim 1, wherein X is CH2, R1 and R2 are OH, and R3 and R4 are H.
-
18. The compound of claim 1, wherein X is dihalomethylene, R1 and R2 are OH, and R3 and R4 are H.
-
19. The compound of claim 1, wherein X is CH2, W1 is NH2, NRH, or NR2, W2 is H, and n is 1.
-
20. The compound of claim 1, wherein X is CH2, W1 and W2 are NH2, NRH, or NR2, and n is 1.
-
21. The compound of claim 1, wherein X dihalomethylene, W1 is NH2, NRH, or NR2, W2 is H, and n is 1.
-
22. The compound of claim 1, wherein X is dihalomethylene, W1 and W2 are NH2, NRH, or NR2, and n is 1.
-
23. The compound of claim 1, wherein X is CH2, W1 and W2 are NH2, NRH, or NR, and n is 3.
-
24. The compound of claim 1, wherein X is CH2, R1 and R2 are OH, and R3 and R4 are H, and n is 1.
-
25. The compound of claim 1, wherein dihalomethylene, R1 and R2 are OH, and R3 and R4 are H, and n is 1.
-
26. The compound of claim 1, wherein X is CH2, R1 and R2 are OH, and R3 and R4 are H, and n is 3.
-
27. The compound of claim 1, which is P1-(Adenosin-5’
- -yl)-P2-(mycophenol-5’
-yl) methylenebis(phosphonate).
- -yl)-P2-(mycophenol-5’
-
28. The compound of claim 1, which is P1-(Adenosin-5’
- yl)-P2-[7-hydroxy-5-methoxy-4methyphtalan-1-on-6yl-(3’
-methylhex-2’
-ene-6’
-yl)]methylenebis-(phosphonate).
- yl)-P2-[7-hydroxy-5-methoxy-4methyphtalan-1-on-6yl-(3’
Specification
-
- Resources
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Current AssigneePharmasset Incorporated (Gilead Sciences Inc.)
-
Original AssigneePharmasset Incorporated (Gilead Sciences Inc.)
-
InventorsPankiewicz, Krzysztof W., Watanabe, Kyoichi A., Lesiak, Krystyna
-
Primary Examiner(s)Trinh, Ba K.
-
Application NumberUS08/949,180Time in Patent Office1,516 DaysField of Search536/26.3, 536/26.2, 536/26.23, 536/26.24, 536/26.72, 536/26.74, 536/27.21, 536/27.3, 536/27.6, 536/27.7, 536/28.53, 536/29.2, 544/276, 544/277, 544/265, 558/87, 558/155US Class Current536/26.3CPC Class CodesA61P 35/02 specific for leukemiaA61P 43/00 Drugs for specific purposes...C07F 9/2495 containing the structure P(...C07F 9/3235 Esters of poly(thio)phosphi...C07F 9/4025 Esters of poly(thio)phospho...C07F 9/4423 Amides of poly (thio)phosph...C07F 9/657172 the ring phosphorus atom an...C07F 9/657181 the ring phosphorus atom an...C07F 9/6581 having phosphorus and nitro...C07H 19/10 with the saccharide radical...C07H 19/20 with the saccharide radical...C07H 19/207 the phosphoric or polyphosp...
