Process for preparing peptidyl heterocyclic ketone derivatives

Details Process for preparing peptidyl heterocyclic ketone derivatives Process for preparing peptidyl heterocyclic ketone derivatives

2007-04-17

2007-04-17

Tsang, Cecilia J. (Department: 1654)

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Synthesis of peptides

C530S335000

Reexamination Certificate

active

10902755

ABSTRACT:
The present invention relates to novel processes for the preparation of peptidyl heterocyclic ketones of the general formula (I)wherein all variables are as herein defined. The present invention further relates to novel pharmaceutical salts and processes for their preparation. The peptidyl heterocyclic ketones of formula (I) are potent and selective inhibitors of tryptase, useful for the treatment and prevention of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis.

REFERENCES:
patent: WO 97/48687 (1997-12-01), None
patent: WO 00/44733 (2000-08-01), None
patent: WO 0044733 (2000-08-01), None
Michael J. Costanzo, et al, “Potent, Small-Molecule Inhibitors of Human Mast Cell Tryptase Antiasthmatic Action of a Dipeptide-Based Transition-State Analogue Containing a Benzothiazole Ketone,” J. Med. Chem.; 2003; 46(18) pp. 3865-3876.
Costano, M.J. et al: “Potent, Small-Molecule Inhibitors of Human Mast Cell Tryptase. Antiasthmatic Action of a Dipeptide-Based Transition-State Analogue Containing a Benzothizaole Ketone”, J. Med. Chem. vol. 46, 2003, pp. 3865-3876, XP002314429.
PCT International Search Report, PCT/US2004/025413, Jan. 21, 2005.
Acta Chimica Sinica - Chinese Edition - Huaxue Xuebao, 48 (9), 1990, pp. 931-935.
Bodanszky, Miklos, “Activation and Coupling” Principles of Peptide Synthesis, 1993, pp. 9-61, vol. II, Springer Laboratory, Springer-Verlag, 2ndedition.
T. W. Greene & P.G.M. Wuts, Protective Groups in Organic Synthesis, John Wiley and Sons, 1991.
Protective Groups in Organic Chemistry, Ed. J.F.W. Mcomie, Plenum Press, 1973, pp. 43-93.

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