Triptolide analogs for the treatment of autoimmune and inflammatory disorders
AssigneeEmory University
InventorsSusheng Wang, Dennis C. Liotta, James P. Snyder, Hariharan Venkatesan
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Abstract
The present invention provides synthetic methods and compositions for treatment of autoimmune and anti-inflammatory disorders comprising administering an effective amount of a derivative of triptolide alone or in combination or alternation with other anti-autoimmune or anti-inflammatory compounds.
Claims42
A compound of the formula (V):
- or its pharmaceutically acceptable salt thereof, wherein:
- (a) B, D and E are independently O;
- (b) G is OR11, NR11R12 or SR11;
- (c) R1, R2, R3, R4, R5 and R6 are independently hydrogen, alkyl, alkenyl, alkynyl, aryl, alkaryl, arylalkyl;
- a moiety selected from optionally substituted furyl, furanyl, pyridyl, pyrimidyl, thienyl, isothiazolyl, imidazolyl, tetrazolyl, pyrazinyl, benzofuranyl, benzothiophenyl, quinolyl, isoquinolyl, benzothienyl, isobenzofuryl, pyrazolyl, indolyl, isoindolyl, benzimidazolyl, purinyl, carbazolyl, oxazolyl, thiazolyl, isothiazolyl, 1,2,4-thiadiazolyl, isooxazolyl, pyrrolyl, quinazolinyl, cinnolinyl, phthalazinyl, xanthinyl, hypoxanthinyl, thiophene, furan, pyrrole, isopyrrole, pyrazole, and imidazole;
- and
- (d) each R7, R8, R9, R10, R11 and R12 is independently hydrogen, alkyl, alkenyl, alkynyl, aryl, alkaryl, arylalkyl;
- a moiety selected from optionally substituted furyl furanyl, pyridyl, pyrimidyl, thienyl, isothiazolyl, imidazolyl, tetrazolyl, pyrazinyl, benzofuranyl, benzothiophenyl, quinolyl, isoquinolyl, benzothienyl, isobenzofuryl, pyrazolyl, indolyl, isoindolyl, benzimidazolyl, purinyl, carbazolyl, oxazolyl, thiazolyl, isothiazolyl, 1,2,4-thiadiazolyl, isooxazolyl, pyrrolyl, quinazolinyl, cinnolinyl, phthalazinyl, xanthinyl, hypoxanthinyl, thiophene, furan, pyrrole, isopyrrole, pyrazole, and imidazole.
A compound of formula:
- or its pharmaceutically acceptable salt thereof.
A pharmaceutical composition for the treatment of an inflammatory disorder in a host comprising an effective treatment amount of a compound of formula:
- or its pharmaceutically acceptable salt thereof, wherein:
- (a) B, D and E are independently O;
- (b) G is OR11, N11R12 or SR11;
- (c) R1, R2, R3, R4, R5 and R6 are independently hydrogen, alkyl, alkenyl, alkynyl, aryl, alkaryl, arylalkyl;
- a moiety selected from optionally substituted furyl, furanyl, pyridyl, pyrimidyl, thienyl, isothiazolyl, imidazolyl, tetrazolyl, pyrazinyl, benzofuranyl, benzothiophenyl, quinolyl, isoquinolyl, benzothienyl, isobenzofuryl, pyrazolyl, indolyl, isoindolyl, benzimidazolyl, purinyl, carbazolyl, oxazolyl, thiazolyl, isothiazolyl, 1,2,4-thiadiazolyl, isooxazolyl, pyrrolyl, quinazolinyl, cinnolinyl, phthalazinyl, xanthinyl, hypoxanthinyl, thiophene, furan, pyrrole, isopyrrole, pyrazole, and imidazole and
- each R7, R8, R9, R10, R11 and R12 is independently hydrogen, alkyl, alkenyl, alkynyl, aryl, alkaryl, arylalkyl;
- a moiety selected from optionally substituted furyl, furanyl, pyridyl, pyrimidyl, thienyl, isothiazolyl, imidazolyl, tetrazolyl, pyrazinyl, benzofuranyl, benzothiophenyl, quinolyl, isoquinolyl, benzothienyl, isobenzofuryl, pyrazolyl, indolyl, isoindolyl, benzimidazolyl, purinyl, carbazolyl, oxazolyl, thiazolyl, isothiazolyl, 1,2,4-thiadiazolyl, isooxazolyl, pyrrolyl, quinazolinyl cinnolinyl, phthalazinyl, xanthinyl, hypoxanthinyl thiophene, furan, pyrrole, isopyrrole, pyrazole, and imidazole:
- in a pharmaceutically acceptable carrier in combination with other anti-inflammatory agents.
A pharmaceutical composition for the treatment of an inflammatory disorder in a host comprising an effective treatment amount of a compound of formula:
- or its pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier or diluent.
A pharmaceutical composition for the treatment of an inflammatory disorder in a host comprising an effective treatment amount of a compound of formula:
- or a pharmaceutically acceptable salt thereof;
- in a pharmaceutically acceptable carrier, in combination with another anti-inflammatory agent.
The pharmaceutical composition of any one of claims 15 or 38, wherein the host is a human.
Dependencies are inferred from the claim text.