Substituted pyrazoles

Details Substituted pyrazoles Substituted pyrazoles

2005-08-30

2005-08-30

Berch, Mark L. (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C514S249000, C514S248000, C514S260100, C514S265100, C514S234200, C540S599000, C540S600000, C544S236000, C544S278000, C544S280000, C544S350000, C544S235000, C544S117000

Reexamination Certificate

active

06936603

ABSTRACT:
Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.

REFERENCES:
patent: 4500525 (1985-02-01), Winters et al.
patent: 5264576 (1993-11-01), Shutske et al.
patent: 5739153 (1998-04-01), Peignier et al.
patent: 5776718 (1998-07-01), Palmer et al.
patent: 5856514 (1999-01-01), Peignier et al.
patent: 5976858 (1999-11-01), Palmer et al.
patent: 6030946 (2000-02-01), Klaus et al.
patent: 6287840 (2001-09-01), Palmer et al.
patent: 0254241 (1988-01-01), None
patent: 382637 (1993-07-01), None
patent: 502788 (1995-04-01), None
patent: 655248 (1999-09-01), None
patent: 1 489 280 (1975-01-01), None
patent: S50-116470 (1974-03-01), None
patent: S52-14765 (1975-07-01), None
patent: WO 94/29276 (1994-12-01), None
patent: WO 95/23222 (1995-08-01), None
patent: WO 96/30353 (1996-10-01), None
patent: WO 97/21439 (1997-06-01), None
patent: WO 97/40066 (1997-10-01), None
patent: WO 9856785 (1998-12-01), None
patent: WO 99/24480 (1999-05-01), None
patent: WO 99/48911 (1999-09-01), None
patent: WO 99/58153 (1999-11-01), None
patent: WO 00/49008 (2000-08-01), None
patent: WO 00/51998 (2000-09-01), None
patent: WO 00/55144 (2000-09-01), None
patent: WO 01/09110 (2001-02-01), None
patent: WO 01/19796 (2001-03-01), None
patent: WO 01/40204 (2001-06-01), None
Palmer, J. T. et al.; “Vinyl Sulfones as Mechanism-Based Cysteine Protease Inhibitors”; J. Med. Chem. (1995) 38(17):3193-3196.
Bromme, D. et al.; “Peptidyl vinyl sulphones: a new class of potent and selective cysteine protease inhibitors”; Biochem. J. (1996) 315:85-89.
McGrath, M.E. et al.: “Crystal structure of human cathepsin S”; Protein Science (1998) 7:1294-1302.
Nerenberg, J. B. et al.; “Design and Synthesis of N-Alkylated Saccharins as Selective a-1A Adrenergic Receptor Antagonists”; Bioorg. Med. Chem. Lett. (1998) 8:2467-2472.
Honey, K. et al.; “Role of Lysosomal Cysteine Proteinases in Antigen Presentation to CD4 T Cells”; Inflammation Research (2001) Sup. 3, vol. 50, p S159 abstr. 10/01.
Li, W. et al.: “Tissue Specific Expression of Cathepsins and Antigen Presentation”; Inflammation Research (2001) Sup 3, vol. 50 p S159 abstr. 10/02.
Magill, C. et al.; “Cysteine Proteases in Antigen Presentation and Models of Inflammation”; Inflammation Research (2001) Sup 3, vol. 50, p S159, abstr. 10/03.
Allen, E.M. et al.; “Reversible Cathepsin S (CATS) Inhibitors Block Invariant Chain Degradation Both In Vitro and In Vivo”; Inflammation Research (2001) Sup 3. vol. 50, p S159, abstr. 10/04.
Podolin, P. L. et al.; “Inhibition if Cathepsin S Blocks Invariant Chain Processing and Antigen-Induced Proliferation in Vitro, and Reduces the Severity of Collagen-Induced Arthritis in Vivo”; Inflammation Research (2001) Sup. 3, vol. 50, p S159, abstr. 10/05.
Spero, D. et al.; “Design and Synthesis of Novel Cathepsin S Inhibitors”; Inflammation Research (2001) Sup. 3, vol. 50, p S206, abstr. 079.
Andronati, S.A. et al.: “Synthesis of 1-[-4-(4-phenyl-1-piperazinyl)butyl]1,2-dihydro-3H-1,4-benzodiazepin-2-ones and 1H-indazoles and their affinity for benzodiazepine receptors”; Chemical Abstracts No. (CAN) 122:314528; (1994) 8:126-131.
Bromme, D, et al.; “High level expression and crystallization of recombinant human cathepsin S”; Protein Science (1996) 5:789-791.
Kirschke, H. et al.; “Cathepsin S”: Handbook of Proteolytic Enzymes; Barrett, A.J.: Rawlings, N.D.: Woessner, J.F., Editors, Academic Press (1998) 621-624.
Nakagawa, T.Y. et al.: “Impaired Invariant Chain Degradation and Antigen Presentation and Diminished Collagen-Induced Arthritis in Cathepsin S Null Mice”: Immunity (1999) 10:207-217.
Riese, R.J. et al.; “Cathepsin S Activity Regulates Antigen Presentation and Immunity”; J.Clin. Invest. (1996) 101(11):2351-2363.
Shi, G.P., et al.; “Cathepsin S Required for Normal MHC Class II Peptide Loading and Germinal Center Development”; Immunity (1999) 10:197-206.
Singh, P., et al.; “Quantitative Structure-Activity Relationship Studies on a New Class of Antihypertensive Agents: Derivatives of 3-Aryl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine”; Quant. Struct.-Act. Relat. (1990) 9:29-32.
Winters, G. et al.; “Synthesis in Vitro [3H]Prazosin Displacement and in Vivo Activity of 3-Aryl-4,5,6,7-tetrahydropyrazolol[4,3-c]pyridines, a New Class of Antihypertensive”; J. Med. Chem. (1985) 28(7):934-940.
Nakatsuka, Masashi et al.: “Preparation of pyrazole derivatives as immunosuppressants”; retreived from STN Database accession No. 130:52417, XP002193692 abstract; Chemical Abstracts Service, Columbus, Ohio, US.
PCT International Search Report PCT/US01/25180 dated Apr. 5, 2002.
PCT Search Report for PCT/US 01/27441 dated Jul. 18, 2002.
Kaoru Saegusa, et al. “Cathepsin S Inhibitor prevents autoantigen presentation and autoimmunity”, Journal of Clinical Investigation, Aug. 2002, vol. 110, No. 3.
Andronati, “Synthesis of 3-aryl-1-[4-phenyl-1-piperazinyl)butyl]indazole derivatives and their affinity to 5-HT1Aserotonin and dopamine D1receptors” Pharmazie 54 (1999) 2, pp. 99-101.

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