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US 6,271,402 B1Granted
HIV integrase inhibitors
AssigneeMerck & Co., Inc.
InventorsSheo Bux Singh, Deborah L. Zink, Daria Jean Hazuda, Peter J. Felock, Anne W. Dombrowski
Life of this patent
Estimating the term…
Abstract
Compound of formula I: wherein the R groups are as defined by the specification. The compounds are useful in the inhibition of HIV integrase, the treatment of infection of HIV and treatment of AIDS.
Claims12
A compound of the formula I
- wherein:
- “a” is selected from a single bond or a double bond;
- R1 is selected from:
- (a) —OH,
- (b) —OC(O)CH3,
- (c) —OC(O)CH2C(CH3)(OH)CH2CO2H,
- (d) —OC(O)CH2C(CH3)(OH)CH2CO2CH3,
- (e) —OC(O)(CH2)2CO2H,
- (f) —OC(O)(CH2)2CO2CH3,
- (g) —OC(O)(CH2)2CONHOH,
- (h) —OCH2OCH3,
- (i) —OC(O)C6H5,
- (j) —OC(O)CH2NH—C(O)OC(CH3)3,
- (k) —OSO2CH3,
- (l) —OC(O)CH2NH2, and
- (m) —OC(O)—(CH2)15—OH;
- R2 is selected from:
- (a) —OH,
- (b) —OC(O)CH3,
- (c) ═O,
- (d) —OC(O)(CH2)2CO2H,
- (e) —OC(O)(CH2)2CO2CH3,
- (f) —OC(O)(CH2)2CONHOH,
- (g) —OCH2OCH3,
- (h) —OC(O)C6H5,
- (i) —OC(O)CH2NHC(O)OC(CH3)3,
- (j) —OSO2CH3,
- (k) —OSO2OH, and
- (l) —OC(O)CH2NH2;
- or R1 and R2 are joined to form:
- R3 is selected from:
- (a) —OH, and
- (b) —OC(O)CH3;
- R4 is selected from:
- (a) —OH, and
- (b) —OC(O)CH3;
- R5 and R6 are independently selected from:
- (a) —H, and
- (b) —OH,
- or together form:
- (c) ═CH2, or
- (d) —CH2O—;
- R7 is selected from:
- (a) H, and
- (b) OH;
- or a pharmaceutically acceptable salt thereof;
- provided that:
- when
- R1 is —OH, —OC(O)—(CH2)15—OH, —OC(O)(CH2)2CO2H, or —OC(O)CH3, and
- R2 is —OH, —OSO2OH, —OC(O)CH3, or —OC(O)(CH2)2CO2H, and
- R3 is —OH or —OC(O)CH3, and
- R4 is —OH or —OC(O)CH3,
- then
- R5 and R6 do not together form
- (a) ═CH2, or
- (b) —CH2O—.
53 more elements
A compound selected from:
A composition comprising a therapeutically effective amount of compound of structural formula I:
- wherein:
- “a” is selected from a single bond or a double bond;
- R1 is selected from:
- (a) —OH,
- (b) —OC(O)CH3,
- (c) —OC(O)CH2C(CH3)(OH)CH2CO2H,
- (d) —OC(O)CH2C(CH3)(OH)CH2CO2CH3,
- (e) —OC(O)(CH2)2CO2H,
- (f) —OC(O)(CH2)2CO2CH3,
- (g) —OC(O)(CH2)2CONHOH,
- (h) —OCH2OCH3,
- (i) —OC(O)C6H5,
- (j) —OC(O)CH2NH—C(O)OC(CH3)3,
- (k) —OSO2CH3,
- (l) —OC(O)CH2NH2,
- (m) —OC(O)—(CH2)15—OH, and
- (n) H;
- R2 is selected from:
- (a) —OH,
- (b) —OC(O)CH3,
- (c) ═O,
- (d) —OC(O)(CH2)2CO2H,
- (e) —OC(O)(CH2)2CO2CH3,
- (f) —OC(O)(CH2)2CONHOH,
- (g) —OCH2OCH3,
- (h) —OC(O)C6H5,
- (i) —OC(O)CH2NHC(O)OC(CH3)3,
- (j) —OSO2CH3,
- (k) —OSO2OH, and
- (l) —OC(O)CH2NH2;
- or R1 and R2 are joined to form:
- R3 is selected from:
- (a) —H,
- (b) —OH, and
- (c) —OC(O)CH3;
- R4 is selected from:
- (a) —H,
- (b) —OH, and
- (c) —OC(O)CH3;
- R5 and R6 are independently selected from:
- (a) —H,
- (b) —OH, and
- (c) —CH3,
- or together form:
- (c) ═CH2, or
- (d) —CH2O—;
- R7 is selected from:
- (a) H, and
- (b) OH;
- or a pharmaceutically acceptable salt thereof;
- in combination with a therapeutically effective amount of an AIDS treatment agent selected from:
- (a) an AIDS antiviral agent,
- (b) an immunomodulator, and
- (c) an anti-infective agent, and
- a pharmaceutically acceptable carrier.
52 more elements
Dependencies are inferred from the claim text.