Reverse-turn mimetics and compositions and methods related...

Details Reverse-turn mimetics and compositions and methods related... Reverse-turn mimetics and compositions and methods related...

2005-07-06

2008-08-05

Kifle, Bruck (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C514S249000, C514S387000

Reexamination Certificate

active

07407952

ABSTRACT:
Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having the following structure are disclosed:wherein A, R1, R2, R2aand R3are as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents as well as inhibitors of central nervous disorders. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.

REFERENCES:
patent: 5440013 (1995-08-01), Kahn
patent: 5545568 (1996-08-01), Ellman
patent: 5929237 (1999-07-01), Kahn
patent: 6013458 (2000-01-01), Kahn et al.
patent: 6184223 (2001-02-01), Kahn et al.
patent: 6294525 (2001-09-01), Stasiak et al.
patent: 6413963 (2002-07-01), Kahn et al.
patent: 6440955 (2002-08-01), Stasiak et al.
patent: 6943157 (2005-09-01), Nagula et al.
patent: WO 94/03494 (1994-02-01), None
patent: WO 97/15557 (1997-05-01), None
patent: WO 98/49168 (1998-11-01), None
patent: WO 01/00210 (2001-01-01), None
patent: WO 01/16135 (2001-03-01), None
Abignente et al., “Research on heterocyclic compounds XVI. 2-Methylimidazo[1,2-a]pyrazine-3-carboxylic acids,”Chemical Abstracts Database, Accession No. 103:87841, 1985.
Barrow and Sun, “Spiroquinazoline, a novel substance P inhibitor with a new carbon skeleton, isolated fromAspergillus flavipes,” Chemical Abstracts Databse, Accession No. 121:129499, 1994.
Cutler et al., “Cinereain: a novel metabolite with plant growth regulating properties fromBotrytis cinerea,” Chemical Abstracts Database, Accession No. 109:165645, 1988.
Dennin et al., “Synthesis of derivatives of pyrazino[1,2-a]pyrimidin-4-ones,”Chemical Abstracts Database, Accession No. 114:164135, 1991.
Faehnle and Rothe, “Syntheses and reactions of peptide cyclols,”Chemical Abstracts Database, Accession No. 102:7061, 1985.
Gatta et al., “New [f]-fused xanthines: synthesis of 1,3-dipropyl-1H, 3H-pyrazino, pyrido, pyrimido and pyrrolo [2,1-f]purine-2, 4-diones,”Chemical Abstracts Database:121:57444, 1994.
Hackh's Chemical Dictionary, Grant, Julius (ed.), pp. 332, 532 and 656, 1994.
Kadam et al., “Fermentative manufacture of multiple drug resistance-attenuating ardeemins,”Chemical Abstracts Marpat Database, Accession No. 121:7435, 1994.
Kappe and Kappe, “Cross-conjugated and pseudo-cross-conjugated mesomeric betaines. XVIII. Bicyclic mesoionic pyrimidines with cardiovascular activity,”Chemical Abstracts Database, Accession No. 116:83634, 1992.
Lam et al., “A new type of synthetic peptide library for identifying ligand-binding activity,”Nature354:82-84, 1991.
Lucente et al., “Synthesis and x-ray crystal structure of a tripeptidic cyclol,”Chemical Abstracts Database, Accession No. 96:69410, 1982.
Lucente et al., “Cyclization of Activated N-Benzyloxycarbonyl-Tripeptides,”Tetrahedron Letters, No. 11, pp. 1009-1012, 1978.
Numata et al., “Structures of cytotoxic substances and new quinazoline derivatives produced by a fungus from a salt water fish,”Chemical Abstracts Database, Accession No. 116:210833, 1992.
Okawara et al., “Preparation and hydrogenolysis of fused piperazines by reaction of diamine and triamine derivatives with benzil. Applications to the synthesis of terminal N-monoprotected triamines,”Chemical Abstracts Database, Accession No. 117:191810, 1992.
Okawara et al., “Simple preparation of terminal N-monoprotected triamines using fused piperazines,”Chemical Abstracts Database, Accession No. 114:101300, 1991.
Penn et al., “Biosynthesis of glyantrypine byAspergillus clavatus,” Chemical Abstracts Database, Accession No. 117:44249, 1992.
Penn et al., “Glyantrypine, a novel anthranillic acid-containing metabolite ofAspergillus clavatus,” Chemical Abstracts Database, Accession No. 117:127875, 1992.
Pinnen et al., “Cyclization under mild conditions of anthraniloyl and N-Methylanthraniloyl dipeptides,”Chemical Abstracts Database, Accession No. 110:76029, 1989.
Pinnen et al., “Ten-membered cyclotripeptides: influence of the ring-flexibility on intramolecular reactions,”Chemical Abstracts Database, Accession No. 102:132448, 1985.
Rothe et al., “Cyclol formation during tripeptide cyclizations. Synthesis of a secondary cyclotripeptide, cyclo-(D-Phe-L-Pro-L-Pro),”Chemical Abstracts Database, Accession No. 97:56231, 1982.
Rothe et al., “Secondary all-L-cyclotripeptides,”Chemical Abstracts Database, Accession No. 103:215766, 1985.
Sauter et al., “Novel basically substituted pyrimidines and benzothienopyrimidines,”Chemical Abstracts Database, Accession No. 87:84931, 1977.
Tanaka and Narita, “Syntheses of pyrido[2,3-b]pyrazine derivatives,”Chemical Abstracts Database, Accession No. 84:31002, 1976.
Vojkovsky et al., “Solid Phase Synthesis of Heterocycles Containing an 1-Acyl-3-oxopiperazine Skeleton,”J. Org. Chem., 63:3162-3163, 1998.

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