Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-12-22
2000-09-19
Richter, Johann
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514354, 514365, 514372, 514374, 514378, 514396, 514406, 514407, 514415, 514419, 546249, 546290, 546298, 546301, 546313, 546314, 548200, 548206, 548214, 548215, 548236, 548240, 548248, 5483351, 5483451, 5483421, 5483731, 5483741, 5483761, A61K 31435, A61K 3140, C07D21196, C07D21389
Patent
active
061212733
ABSTRACT:
This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.
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Holt, Dennis A. et al., "Structure-Activity Studies of Synthetic FKBP Ligands as Peptidyl-Prolyl Isomerase Inhibitors," Biorg. Med. Chem. Lett., 1994, 4(2) 315-320.
Holt, Dennis A. et al., "Design Synthesis, and Kinetic Evaluation of High-Affinity FKBP Ligands and the X-ray Crystal Structures of Their Complexes with FKBP12," J. Am. Chem. Soc., 1993, 115, 9925-9938.
Schreiber, Stuart L., "Chemistry and Biology of the Immunophilins and Their Immunosuppresive Ligands," Science, 1991, 251, 282-287.
Dumont, Francis J. et al., "The Immunosuppressive and Toxic Effects of FK-506 are Mechanistically Related: Pharmacology of a Novel Antagonist of FK-506 and Rapamycin," J. Exp. Med., 1992, 176, 751-760.
Hamilton Gregory S.
Huang Wei
Li Jai-He
GPI NIL Holdings, Inc
Juneau Todd L.
Nath Gary M.
Oswecki Jane C.
Richter Johann
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