Unsaturated acetylene phosphonate derivatives of purines
First Claim
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1. A compound of the formula:
- ##STR24## the stereoisomeric forms and mixtures thereof, tautomeric forms or the pharmaceutically acceptable salts thereof, whereinX1 is H or NH2 ;
X2 is OH or NH2 ;
Z is nothing, CH2, CH2 CH2, or CH2 O;
W is ##STR25## wherein T is nothing, T'"'"' or T", whereinT'"'"' is CH2 CH2, andT" is CH2 OCH2, CH2 OCH(CH2 OH);
R3 and R4 are each independently OH, OR5, OR5 '"'"', or --O--CH(R6)--O--C(O)R5, provided that when one of R3 and R4 is OH the other is not --O--CH(R6)--O--C(O)R5, wherein R5 and R5 '"'"' are each independently C1-15 alkyl or benzyl, and R6 is H or C1-10 alkyl.
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Abstract
Disclosed are novel unsaturated acetylene phosphonate derivatives of certain purines or pyrimidines useful as antiviral agents, methods useful for their preparation and use of these compounds as antiviral agents effective against DNA viruses, retroviruses and viruses involved in tumor formation.
41 Citations
9 Claims
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1. A compound of the formula:
- ##STR24## the stereoisomeric forms and mixtures thereof, tautomeric forms or the pharmaceutically acceptable salts thereof, wherein
X1 is H or NH2 ; X2 is OH or NH2 ; Z is nothing, CH2, CH2 CH2, or CH2 O; W is ##STR25## wherein T is nothing, T'"'"' or T", wherein T'"'"' is CH2 CH2, and T" is CH2 OCH2, CH2 OCH(CH2 OH); R3 and R4 are each independently OH, OR5, OR5 '"'"', or --O--CH(R6)--O--C(O)R5, provided that when one of R3 and R4 is OH the other is not --O--CH(R6)--O--C(O)R5, wherein R5 and R5 '"'"' are each independently C1-15 alkyl or benzyl, and R6 is H or C1-10 alkyl. - View Dependent Claims (2, 3, 4, 5, 6, 7)
- ##STR24## the stereoisomeric forms and mixtures thereof, tautomeric forms or the pharmaceutically acceptable salts thereof, wherein
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8. A method of treating a patient for a viral infection of DNA viruses, retroviruses or viruses involved in tumor formation by administration to a patient of a sufficient amount of the compound according to claim.
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9. A method of preparing a compound of the formula:
- ##STR26## the stereoisomeric forms and mixtures thereof, tautomeric forms or the pharmaceutically acceptable salts thereof, wherein
X1 is H or NH2 ; X2 is OH or NH2 ; Z is nothing, CH2, CH2 CH2, or CH2 O; W is ##STR27## wherein T is nothing, T'"'"' or T", wherein T'"'"' is CH2 CH2, and T" is CH2 OCH2, CH2 OCH(CH2 OH R3 and R4 are each independently OH, OR5, OR5 '"'"', or --O--CH(R6)--O--C(O)R5, provided that when one of R3 or R4 is OH the other is not --O--CH(R6)--O--C(O)R5, wherein R5 and R5 '"'"' are each independently C1-15 alkyl or benzyl, and R6 is H or C1-10 alkyl comprising the steps of deprotecting a compound of the formula;
##STR28## wherein R3 and R4 are OR5, OR5 '"'"' or --O--CH--(R6)--O--C(O)R5 as previously defined and Pg is a protecting group,and is optionally hydrolyzed to provide the compound wherein R3 and R4 are each --OH.
- ##STR26## the stereoisomeric forms and mixtures thereof, tautomeric forms or the pharmaceutically acceptable salts thereof, wherein
Specification
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Current AssigneeAventis Incorporated (Sanofi )
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Original AssigneeMerrell Pharmaceuticals Incorporated (Dow, Inc.)
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InventorsCasara, Patrick, Halazy, Serge, Nave, Jean-Fran.cedilla.ois
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Primary Examiner(s)Shah, Mukund J.
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Assistant Examiner(s)Sripada, Pavanaram K.
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Application NumberUS08/505,168Time in Patent Office1,054 DaysField of Search544/243, 544/244, 544/265, 514/81, 514/262US Class Current514/81CPC Class CodesA61K 31/675 having nitrogen as a ring h...C07F 9/6512 having the nitrogen atoms i...
