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Triptolide analogs for the treatment of autoimmune and inflammatory disorders

  • US 6,777,441 B2
  • Filed: 10/02/2001
  • Issued: 08/17/2004
  • Est. Priority Date: 10/02/2000
  • Status: Expired due to Term
First Claim
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1. A compound of the formula (V):

  • embedded imageor 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.

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