Small molecule inhibitors of rotamase enzyme activity

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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Reexamination Certificate

active

07960570

ABSTRACT:
This invention relates to neurotrophic compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.

REFERENCES:
patent: 3795738 (1974-03-01), Plotnikoff
patent: 3810884 (1974-05-01), Gold
patent: 3917840 (1975-11-01), Gold
patent: 4070361 (1978-01-01), Petrillo, Jr.
patent: 4128653 (1978-12-01), Cushman et al.
patent: 4310461 (1982-01-01), Krapcho et al.
patent: 4321269 (1982-03-01), Wareing
patent: 4374829 (1983-02-01), Harris et al.
patent: 4390695 (1983-06-01), Krapcho et al.
patent: 4431644 (1984-02-01), Smith et al.
patent: 4472380 (1984-09-01), Harris et al.
patent: 4501901 (1985-02-01), Thottathil et al.
patent: 4507292 (1985-03-01), Heywang et al.
patent: 4531964 (1985-07-01), Shimano et al.
patent: 4574079 (1986-03-01), Gavras et al.
patent: 4578474 (1986-03-01), Krapcho et al.
patent: 4593102 (1986-06-01), Shanklin, Jr.
patent: 4604402 (1986-08-01), Godfry, Jr. et al.
patent: 4649147 (1987-03-01), Mueller et al.
patent: 4708954 (1987-11-01), Ienaga et al.
patent: 4762821 (1988-08-01), Nestor
patent: 4766110 (1988-08-01), Ryan et al.
patent: 4808573 (1989-02-01), Gold et al.
patent: 4818749 (1989-04-01), Gold et al.
patent: 4912231 (1990-03-01), Kronenthal et al.
patent: 5002963 (1991-03-01), De Luca et al.
patent: 5147877 (1992-09-01), Goulet
patent: 5192773 (1993-03-01), Armistead et al.
patent: 5204338 (1993-04-01), Baader et al.
patent: 5252579 (1993-10-01), Skotnicki et al.
patent: 5294603 (1994-03-01), Rinehart
patent: 5319098 (1994-06-01), Burbaum et al.
patent: 5330993 (1994-07-01), Armistead et al.
patent: 5348944 (1994-09-01), Gold et al.
patent: 5359138 (1994-10-01), Takeuchi et al.
patent: 5385918 (1995-01-01), Connell et al.
patent: 5414083 (1995-05-01), Hacki et al.
patent: 5424454 (1995-06-01), Burbaum et al.
patent: 5447915 (1995-09-01), Schreiber et al.
patent: 5516797 (1996-05-01), Armistead et al.
patent: 5543423 (1996-08-01), Zelle et al.
patent: 5589499 (1996-12-01), Weth
patent: 5614547 (1997-03-01), Hamilton et al.
patent: 5620971 (1997-04-01), Armistead et al.
patent: 5622970 (1997-04-01), Armistead et al.
patent: 5661167 (1997-08-01), Peet et al.
patent: 5696135 (1997-12-01), Steiner et al.
patent: 5721256 (1998-02-01), Hamilton et al.
patent: 5726184 (1998-03-01), Zelle
patent: 5780484 (1998-07-01), Zelle et al.
patent: 5786378 (1998-07-01), Hamilton et al.
patent: 5795908 (1998-08-01), Hamilton et al.
patent: 5798355 (1998-08-01), Steiner et al.
patent: 5801187 (1998-09-01), Li et al.
patent: 5801197 (1998-09-01), Steiner et al.
patent: 5811434 (1998-09-01), Zelle et al.
patent: 5840736 (1998-11-01), Zelle et al.
patent: 6037370 (2000-03-01), Armistead
patent: 6124328 (2000-09-01), Armistead
patent: 7153883 (2006-12-01), Hamilton et al.
patent: 2008/0076817 (2008-03-01), Hamilton et al.
patent: 3508251 (1986-09-01), None
patent: 3931051 (1990-03-01), None
patent: 4015255 (1991-11-01), None
patent: 12401 (1980-06-01), None
patent: 48159 (1982-03-01), None
patent: 50800 (1982-05-01), None
patent: 73143 (1983-03-01), None
patent: 88350 (1983-09-01), None
patent: 196841 (1986-10-01), None
patent: 260118 (1988-03-01), None
patent: 333174 (1989-09-01), None
patent: 352000 (1990-01-01), None
patent: 378318 (1990-07-01), None
patent: 405994 (1991-01-01), None
patent: 419049 (1991-03-01), None
patent: 468339 (1992-01-01), None
patent: 564924 (1993-10-01), None
patent: 572365 (1993-12-01), None
patent: 652229 (1995-05-01), None
patent: 2247456 (1992-03-01), None
patent: 4149166 (1992-05-01), None
patent: 5178824 (1993-07-01), None
patent: 8809789 (1988-12-01), None
patent: 9012805 (1990-11-01), None
patent: 9104985 (1991-04-01), None
patent: 9113088 (1991-09-01), None
patent: 9200278 (1992-01-01), None
patent: 9203472 (1992-03-01), None
patent: 9204370 (1992-03-01), None
patent: 9216501 (1992-10-01), None
patent: 9218478 (1992-10-01), None
patent: 9219593 (1992-11-01), None
patent: 9219745 (1992-11-01), None
patent: 9221313 (1992-12-01), None
patent: 9307269 (1993-04-01), None
patent: 9313066 (1993-07-01), None
patent: 9323548 (1993-11-01), None
patent: 9325546 (1993-12-01), None
patent: 9405639 (1994-03-01), None
patent: 9407858 (1994-04-01), None
patent: 9413629 (1994-06-01), None
patent: 9512572 (1995-05-01), None
patent: 9524385 (1995-09-01), None
patent: 9526337 (1995-10-01), None
patent: 9535308 (1995-12-01), None
patent: 9535367 (1995-12-01), None
patent: 9606097 (1996-02-01), None
patent: 9615101 (1996-05-01), None
patent: 9617816 (1996-06-01), None
patent: 9633184 (1996-10-01), None
patent: 9636630 (1996-11-01), None
patent: 9641609 (1996-12-01), None
patent: 9207782 (1993-04-01), None
Ando, Takao et al., “Formation of Crossed Phenzine from the Reactions between Tetra-p-anisyl- and Tetra-p-tolyl-hydrazines in Liquid Sulphur Dioxide,” Chem. Comm., S. Chem. Comm., 1975, 989.
Andrus, Merrit B., Structure-based design of an acyclic ligand that bridges FKBP12 and calcineurin, J. Am. Chem. Soc., 1993, 115(2), 10420-1.
Armistead, D.M. et al., “Design, synthesis and structure of non-macrocyclic inhibitors of FKBP12, the major binding protin for the immunosuppressant FK506,” Acta Crystallogr. 1995, D5I (4), 522-8.
Askin, D. et al., “Chemistry of FK-506: benzilic acid rearrangement of the tricarbonyl system,” Tetrahedron Lett., 1989,30(6), 671-4.
Askin, D. et al., “Effecient Degradation of FK-506 to a versatile synthetic intermediate,” J. Org. Chem., 1990, 55(20), 5451-4.
Baader, Ekkehard et al., “Inhibition of prolyl 4-hydroxylase by oxalyl amino acid derivatives in vitro, in isolated microsomes and in embryonic chicken tissues,” Biochem. J., 1994, 300(2), 525-30.
Baumann, K. et al., “Synthesis and oxidative cleavage of the major equilibrium products of ascomycin and Fk 506,” Tetrahedron Lett., 1995, 26(13), 2231-4.
Bender, D., et al., “Periodate oxidation of α-keto γ-lactams. Enol oxidation and β-lactam formation. Mechanism of periodate hydroxylation reactions,” J. Org. Chem., 1978, 43(17), 3354-62.
Birkenshaw, Timothy N. etal. “Synthetic FKBP12 Ligands. Design and Synthesis of Pyranose Replacements,” Bioorganic & Medicinal Chemistry Letters, 1994, vol. 4, No. 21, pp. 2501-2506.
Blaschke et al., Chemical abstracts, 1974. 85, 78405k.
Boulmedais, Au et al., “Stereochemistry of Electrochernical Reduction of Optically Active a-ketoamides. II. Electroreduction of benzoylformamides derived from S-(−)-proline,” Bull. Soc. Chim. Fr., 1989, (2), 185-91.(French).
Bycroft, Bame W., and Lee Grahame R., “Efficient asymmetric synthesis of γ-amino from γ-keto acids and ammonia with conservation of the chiral reagent,” J. Chem. Soc., 1975, 24, 988-9.
Caffrey, Moya V. et al. “Synthesis and Evaluation of Dual Domain Macrocyclic FKBP12 Ligands,” Bioorganic & Medicinal Chemistry Letters, 1994, vol. 4, No. 21, pp. 2507-2510.
Cameron, Andrew et al., “Immunophilin FK506 binding protein associated with inositol 1,4,5-tnphosphate receptor modulates calcium flux,” Proc. Natl. Acad. Sci. USA, 1995, 92, 1784-1 788.
Caufield, Craig E. and Musser, John H., Annual Reports in Medicinal Chemistry, Johns (Ed.). Academic Press, Inc., Chapter 21, 195-204,1989.
Chakaraborty, Tushar K., “Studies towards the development of cyclic peptide-based analogs of macrolide immunosuppressants,” Pure Appl. Chem., 1996, 68(3), 565-568.
Chakraborty, TK et al., “Design and Synthesis of a rapamycin-based high affinity binding FKBP12 ligand,” Chem. Biol., 1995, 2(3), 157-61.
Coleman, R., and Danishefsky, S., “Degradation and manipulations of the immunosuppressant FK506: preparation of potential synthetic Intermediates,” Heterocycles, 1989, 28(1), 157-61.
Colombo, L. et al., “Enantiosetective synthesis of secondary alcohols in the pressence of chiral ligands,

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