Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2005-01-04
2005-01-04
Travers, Russell (Department: 1617)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S210030, C514S414000, C514S422000, C514S424000, C514S428000, C514S439000, C514S441000, C514S443000, C514S464000, C514S465000, C514S466000
Reexamination Certificate
active
06838477
ABSTRACT:
Described herein are compounds related to lactacystin and lactacystin β-lactone, pharmaceutical compositions containing the compounds, and methods of use.
REFERENCES:
patent: 5340736 (1994-08-01), Goldberg
patent: 5453502 (1995-09-01), Aikins et al.
patent: 6335358 (2002-01-01), Fenteany et al.
Pages of Calbiochem® catalog for Clasto-Lactacystin β-Lactone (cat. No. 426102) and Synthetic Lactacystin (cat. no. 426100), as printed on Jun. 8, 2003.
Penrose and McBride, Proteasome-Mediated Degradation of the Papillomavirus E2-TA Protein Is Regulated by Phosphorylation and Can Modulate Viral Genome Copy Number,J. Virology74(13): 6031-6038 (Jul. 2000).
Speranza et al., Inhibition of Proteasome Activity Strongly Affects Kiwifruit Pollen Germination. Involvement of the Ubituitin/Proteasome Pathway as major Regulator,Plant Physiology126: 1150-1161 (Jul. 2001).
Jeffers et al., Degradation of the Met Tyrosine Kinase Receptor by the Ubiquitin-Proteasome Pathway,Molecular and Cellular Biology17(2): 799-808 (Feb. 1997).
Haruta et al., A Rapamycin-Sensitive Pathway Down-Regulates Insulin Signaling via Phosphorylation and Proteasomal Degradation of Insulin Receptor Substrate-1,Molecular Endocrinology14(6): 783-794 2000.
Hamada et al., Stereoselective Total Synthesis of AI-77-B, a Gastroprotective Substance fromBacillus pumilus, J. American Chemical Society 111:1524-1525, 1989.
Thottathil et al., Conversion of L-Pyroglutamic Acid to 4-Alkyl-Substituted L-Prolines. The Synthesis of trans-4-Cyclohexyl-L-Proline, J. Organic Chemistry 51:3140-3143, 1986.
Britta-Mareen Traeckner et al., A Proteasome Inhibitor Prevents Activation of NF-KB and Stabilizes a Newly Phosphorylated Form of IKB-a That is Still Bound to NF-KB,The EMBO Journal 13(22):5433-5441, 1994.
Chida et al., Total Synthesis of (+)-Lactacystin from D-Glucose,J. Chem. Soc./Chem. Comm., p. 793-794, 1995.
Corey et al., Total Synthesis of Lactacystin,J. Am. Chem. Soc. 114:10677-10678, 1992.
Corey et al., “Studies on the Total Synthesis of Lactacystin, an Improved Aidol Coupling . . . ” Tetraahedron Letters 34(44):6977-6980, 1993.
Corey et al., An Enantioselective Synthesis of (6R)-Lactacystin,Tetrahedron Lett. 34:6969-6972, 1993.
Corey et al., Synthesis of (6R,7S)-Lactacystin and 6-Deoxylactacystin from a Common Intermediate,Tetrahedron Lett. 34:6973-6976, 1993.
Corey et al., Total Synthesis of Lactacystin: An Enantioselective Synthesis of (6R)-Lactacystin: Total Synthesis of (+)-Lactacystin, . . . ,Chemtracts-Organic Chemistry, pp. 266-272, 1994.
Djaballah et al., Use of Serine-protease Inhibitors as Probes for the Different Proteolytic Activities of the Rat Liver Multicatalytic Proteinase Complex,Europ. J. Biochem. 209:629-634, 1992.
Fenteany et al., A β-Lactone related to Lactacystin Induces Neurite Outgrowth in a Neuroblastoma Cell Line and Inhibits Cell . . . ,Proc. Natl. Acad. Sci. USA 91:3358-3362, 1994.
Fenteany et al., Inhibition of Proteasome Activities and Subunit-Specific Amino-Terminal Threonine Modification by Lactacystin,Science 268:726-731, 1995.
Figueiredo-Pereira et al., A New Inhibitor of the Chymotrypsin-Like Activity of the Multicatalytic Proteinase Complex (20S Proteasome) . . . ,J. of Neurochemistry 63(4):1578-1581, 1994.
Figueiredo-Pereira et al., Comparison of the Effect of Calpain Inhibitors on Two Extralysosomal Proteinases: The Multicatalytic Proteinase Complex and m-Calpain,J. of Neurochemistry 62(5):1989-1994, 1994.
Mason et al., Proteasomes: the Changing Face of Proteolysis,Chemistry&Biology 1:197-199, 1994.
Goldberg et al., U.S. patent application Ser. No. 08/210,381, filed Mar. 18, 1994.
Nakagawa et al., Biosynthesis of Lactacystin. Origin of the Carbons and Stereospecific NMR Assignment of the Two Diastereotopic Methyl Groups,Tetrahedron Lett. 35(28):5009-5012, 1994.
Orlowski et al., Evidence for the Presence of Five Distinct Proteolytic Components in the Pituitary Multicatalytic Proteinase Complex . . . ,Biochemistry 32:1563-1572, 1993.
Palombella et al., The Ubiquitin-Proteasome Pathway is Required for Processing the NF-κB1 Precursor Protein and the Activation of NF-κB,Cell 78:773-785, 1994.
Peters, J., Proteasomes: Protein Degradation Machines of the Cell,TIBS, pp. 377-382, 1994.
Savroy et al., Reaction of Proteasomes with Peptidylchloromethanes and Peptidyldiazomethanes,Biochem. J. 296:601-605, 1993.
Standaert et al., Abstract,Academic Development Program Symposium, Merck Research Laboratories, Oct., 1993, Rahway, New Jersey.
Standaert et al., Poster Session,Merck Research Laboratories Academic Development Symposium, Oct. 11, 1993, Rahway, New Jersey.
Sunazuka et al., Total Synthesis of (+)-Lactacystin, the First Non-Protein Neurotrophic Factor,J. Amer. Chem Soc. 115:5302, 1993.
Tsubuki et al., Purification and Characterization of a Z-Leu-Leu-Leu-MCA Degrading Protease Expected to Regulate Neurite Formation: . . . ,Biochem. &Biophys. Res. Comm. 196(3):1195-1201, 1993.
Uno et al., Total Synthesis (+)-Lactacystin from (R)-Glutamate,J. Am. Chem. Soc. 116:2139-2140, 1994.
Vinitsky et al., Inhibition of the Chymotrypsin-like Activity of the Pituitary Multicatalytic Proteinase Complex,Biochemistry 31:9421-9428, 1992.
Vinitsky et al., Inhibition of the Proteolytic Activity of the Multicatalytic Proteinase Complex (Proteasome) by Substrate-related Peptidyl Aldehydes,J. of Biol. Chem. 269(47):29860-29866, 1994.
Fenteany Gabriel
Jamison Timothy F.
Schreiber Stuart L.
Standaert Robert F.
Hale and Dorr LLP
President and Fellows of Harvard College
Travers Russell
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