Solid phase and combinatorial library syntheses of fused 2,4-pyr

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

514318, 544224, 546112, 546138, 548452, 548527, 549 1, 549200, A01N 4340, C07D23700

Patent

active

060253711

ABSTRACT:
The invention provides chemistry libraries containing fused 2,4-pyrimidinediones. The invention also provides methods for the construction of fused 2,4-pyrimidinedione containing libraries. The invention further provides methods for the identification of bioactive, fused 2,4-pyrimidinediones from those libraries.

REFERENCES:
patent: 4521420 (1985-06-01), Maurer et al.
patent: 4631211 (1986-12-01), Houghten
patent: 4835157 (1989-05-01), Press et al.
patent: 5463564 (1995-10-01), Agrafiotis et al.
patent: 5510240 (1996-04-01), Lam et al.
patent: 5549974 (1996-08-01), Holmes
Buckman et al., "Solid-phase synthesis of 1,3-dialkyl quinazoline-2,4-diones" Tetrahedron Lett. (1996) 37:4439-4442.
Bunin et al., "A general and expedient method for the solid-phase synthesis of 1,4-benzodiazepine derivatives" J. Am. Chem. Soc. (1992) 114:10997-10998.
Canonne et al., "Synthesis of chiral 3-substituted 2,4(1H,3H)-quinazolinediones" Heterocycles (1993) 36: 1305-1314.
Cho et al., "An unnatural biopolymer " Science (1993) 261:1303-1305.
Evans et al., "The asymmetric synthesis of .delta.-amino acids. Electrophilic azidation of chiral imide enolates, a practical approach to the synthesis of (R)-and (S)-.delta.-azido carboxylic acids" J. Amer. Chem. Soc. (1990) 112:4011-4030.
Furka et al., "General method for rapid synthesis of multicomponent peptide mixtures" Int. J. Peptide Protein Res. (1991) 37:487-493.
Fodor et al., "Light-directed, spatially addressable parallel chemical synthesis" Science (1991) 251:767-773.
Geysen et al., "Use of peptide synthesis to probe viral antigens for epitopes to a resolution of a single amino acid" Proc. Natl. Acad. Sci. USA (1984) 81:3998-4002.
Gordeev et al., "Approaches to a combinatorial synthesis of heterocycles: Solid phase synthesis of pyridines and pyrido[2,3-d]pyrimidines" Tetrahedron Lett. (1996) 37:4643-4646.
Gordon et al., "Strategy and tactics in combinatorial organic synthesis. Applications to drug discovery" Acc. Chem. Res. (1995) 29:144-154.
Gordon et al., "Reductive alkylation on a solid phase: Synthesis of a piperazinedione combinatorial library" Biorg. Medicinal Chem. Lett. (1995) 5:47-50.
Gordon et al., "Applications of combinatorial technologies to drug discovery. 2. Combinatorial organic synthesis, library screening strategies, and future directions" J. Med. Chem. (1994) 37:1385-1401.
Grant, G.A., ed., Synthetic Peptides. A User's Guide (1992) W.H. Freeman and Co., New York. A title page and table of contents are enclosed herewith.
Greene et al., Protective Groups in Organic Synthesis, 2d Ed., (1991) John Wiley & Sons, Inc., New York. A title page and table of contents are enclosed herewith.
Harper et al., Review of Physiological Chemistry, 16th Ed., (1977) Lange Medical Publications, pp. 21-24.
Hermkens et al., "Solid-phase organic reactions: A review of the recent literature" Tetrahedron (1996) 52:4527-4554.
Houghten, "General method for the rapid solid-phase synthesis of large numbers of peptides: Specificity of antigen-antibody interaction at the level of individual amino acids" Proc. Natl. Acad. Sci. USA, (1985) 82:5131-5135.
Houghten et al., "Generation and use of synthetic peptide combinatorial libraries for basic research and drug discovery" Nature (1991) 354:84-86.
Hutchins et al., "A general method for the solid phase synthesis of ureas" Tetrahedron Lett. (1994) 35:4055-4058.
Lam et al., "A new type of synthetic peptide library for identifying ligand-binding activity" Nature (1991) 354:82-84.
Lowe, III et al., "Structure-activity relationship of quinazolinedione inhibitors of calcium-independent phosphodiesterase" J. Med. Chem. (1991) 34:624-628.
Maillard et al., "Derives de la (3H) quinazolinone-4-doues de proprietes anti-inflammatoires. III. Derives de la 1H-3H-quinazoline-dione-2,4 et produits voisins" Fr. Chim. Ther. (1968) 3:100-105.
Merrifield, "Solid phase peptide synthesis. I. The synthesis of a tetrapeptide" J. Am. Chem. Soc. (1963) 85:2149-2154.
Mignani et al., "New indole derivatives as potent and selective serotonin uptake inhibitors" Bioorg. Med. Chem. Lett. (1993) 3:1913-1918.
Montginoul et al., "Activites analgesiques, anticonvulsivantes et anti-inflammatoires de 1H, 3H-quinazolinediones-2,4" Ann. Pharm. Franc. (1988) 46:223-232.
Murphy et al., "Combinatorial organic synthesis of highly functionalized pyrrolidines: Identification of a potent angiotensin converting enzyme inhibitor from a mercaptoacyl proline library" J. Am. Chem. Soc. (1995) 117:7029-7030.
Rich et al., "Preparation of a new o-nitrobenzyl resin for solid-phase synthesis of tert-butyloxycarbonyl-protected peptide acids" J. Am. Chem. Soc. (1975) 97:1575-1579.
Roth et al., Pharmaceutical Chemistry, Volume 1: Drug Synthesis (1988) John Wiley & Sons, Inc., New York, pp. 326-329.
Simon et al., "Peptoids: A modular approach to drug discovery" Proc. Natl. Acad. Sci. USA (1992) 89:9367-9371.
Smith et al., "An efficient solid phase synthetic route to 1,3-disubstituted 2,4(1H,3H)-quinazolinediones suitable for combinatorial synthesis" Bioorg. Med. Chem. Lett. (1996) 6:1483-1486.
Wang et al., "Solid phase synthesis of protected peptides via photolytic cleavage of the .alpha.-methylphenacy ester anchoring linkage" J. Org. Chem. (1976) 41:3258-3261.
Williams, Synthesis of Optically Active .alpha.-Amino Acids, (1989) Pergamon Press. A title page and table of contents are enclosed herewith.
Williams et al., "Asymmetric synthesis of monosubstituted and .alpha., .alpha.-disubstituted .alpha.-amino acids via diastereoselective glycine enolate alkylations" J. Amer. Chem. Soc. (1991) 113:9276-9286.
Canonne, P., "Synthesis of chiral 3-substituted 2,4(1H,3H)-Quinazolinediones" Meterocycles (1993) 36(6):1305-1314.
Gouilleux et al., "Solid Phase Synthesis of Chiral 3-substituted Quinazoline-2,4-diones" Tetrahedron Letters (1996) 37(39):7031-7034.
Malamas et al., "Quinazolineacetic Acids and Related Analogues as Aldose Reductase Inhibitors" J. Med. Chem. (1991) 34(4):1492-1503.
Ogawa et al., "Preparation of thienopyrimidinediones as aldose reductase inhibitors" Chemical Abstracts (1991) 114: 756, Abstract no. 10235e.
Smith et al., Bioorganic & Medicinal Chemistry Letters., vol. 6., No. 13., pp. 1483-1486., 1996.
Patel et al., Mol. Diversity Comb. Chem: Lib. Drug Discovery, Conf., pp. 58-69., 1996.
Gordeev et al., Tetrahedron Letters., vol. 37., No. 27., pp. 4643-4646., 1996.

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Solid phase and combinatorial library syntheses of fused 2,4-pyr does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Solid phase and combinatorial library syntheses of fused 2,4-pyr, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Solid phase and combinatorial library syntheses of fused 2,4-pyr will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-1906191

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.