N-linked ureas and carbamates of heterocyclic thioesters

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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548533, A61K 3140, C07D20706

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active

059359897

ABSTRACT:
This invention relates to neurotrophic low molecular weight, small molecule N-linked ureas and carbamates 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.

REFERENCES:
patent: 4310461 (1982-01-01), Krapcho et al.
patent: 4390695 (1983-06-01), Krapcho et al.
patent: 4578474 (1986-03-01), Krapcho et al.
patent: 4593102 (1986-06-01), Shanklin
patent: 4596819 (1986-06-01), Nicolaides et al.
patent: 4886813 (1989-12-01), Nakamura et al.
patent: 5001142 (1991-03-01), Trybulski et al.
patent: 5192773 (1993-03-01), Armistead et al.
patent: 5276207 (1994-01-01), Schneider et al.
patent: 5330993 (1994-07-01), Armistead et al.
patent: 5385918 (1995-01-01), Connell et al.
patent: 5541191 (1996-07-01), Skotnicki et al.
patent: 5585397 (1996-12-01), Tung et al.
Yamishita, Dennis S. et al., "Design, Synthesis and Evolution of Dual Domain FKBP Ligands," Bioorg. Med. Chem. Lett., 1994, 4(2), 325-328.
Luengo, Juan I. et al., "Synthesis and Structure-Activity Relationships of Macrocyclic FKBP Ligands," Bioorg. Med. Chem. Lett., 1994 4(2), 321-324.
Holt, Dennis A. et al., "Structure-Activity Studies of Synthetic FKBP Ligands as Peptidyl-Prolyl Isomerase Inhibitors," Bioorg. Med. Chem. Lett., 1994, 4(2), 315-320.
Birkenshaw, Timothy N. et al., "Synthetic FKBP12 Ligands. Design and Synthesis of Pyranose Replacements," Bioorg. Med. Chem. Lett., 1994, 4(21), 2501-2506.
Holt, Dennis A. et al., "Design, Synthesis, and Kinetic Evaluation of High-Affinity FKBP Ligands and the X-ray Crystal Structure of Their Complexes with FKBP12," J. Am. Chem. Soc., 1993, 115, 9925-9938.
Wang, Gary T. et al., "Synthesis and FKBP Binding of Small Molecule Mimics of the Tricarbonyl Region of FK506," Biorg. Med. Chem. Lett., 1994, 4(9), 1161-1166.
Boulmedais, Ali et al., "Stereochimie de la reduction electrochimique d'a-cetoamides optiquement actives II. Electroreduction de benzoylflormamides derives de la S(-)-proline," Bull. Soc. Chim. Fr., 1988, 9(2), 185-191.
Dragovitch, Peter S. et al. "Structure-Based Design of Novel, Urea-Containing FKBP12 Inhibitors," J. Med. Chem., 1996, 39, 1872-1884.
Teague, Simon J. et al., "Synthesis and Study of a Non Macrocyclic FK506 Derivative," Bioorg. Med. Chem. Lett., 1994, 4(13), 1581-1584.
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.
Schreiber, Stuart L., "Chemistry and Biology of the Immunophilins and Their Immunosuppressive Ligands," Science, 1991, 251, 282-287.

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