Combinatorial libraries of substrate-bound cyclic organic compou

Details Combinatorial libraries of substrate-bound cyclic organic compou Combinatorial libraries of substrate-bound cyclic organic compou

1995-06-07

1999-09-28

Achutamurthy, Ponnathapura

Chemistry: analytical and immunological testing

Involving an insoluble carrier for immobilizing immunochemicals

436531, 530330, 530333, 530334, 435 71, G01N 33543, G01N 33545, G01N 3353, A61K 3806

Patent

active

059587920

ABSTRACT:
The invention relates to libraries of cyclic organic compounds and method of producing and assaying such libraries. According to the invention, each cyclic organic compound is constructed from a starting material in the form of a solid surface derivatized with a starting resin. Compounds are reacted with the resin to add or to form a cyclic group. The reactions are preferable carried out using a split resin procedure so that different compounds can be reacted with a plurality of subamounts so as to increase the size of the library. For example, compounds are reacted with a solid support bound starting resin to obtain a compound which includes an aldehyde functional group wherein the aldehyde compound or compounds reacted with it have substituents which are varied such that a mixture of products is obtained. The invention further relates to methods of producing combinatorial libraries of cyclic organic compounds from substrate bound compounds by cleaving the compounds from the support after synthesizing is completed and to assaying libraries of such compounds.

REFERENCES:
patent: 3634364 (1972-01-01), Greenbelt et al.
patent: 4833092 (1989-05-01), Geysen
patent: 5010175 (1991-04-01), Rutter et al.
patent: 5066716 (1991-11-01), Robey et al.
patent: 5143854 (1992-09-01), Pirrung et al.
patent: 5182366 (1993-01-01), Huebner et al.
patent: 5194392 (1993-03-01), Geysen
patent: 5225533 (1993-07-01), Rutter et al.
patent: 5252296 (1993-10-01), Zuckermann et al.
patent: 5266684 (1993-11-01), Rutter et al.
patent: 5288514 (1994-02-01), Ellman
Simon, Reyna et al., " Peptoids: A Modular Approach to Drug Discovery" Proc. Nat.l Acad. Sci. USA (1992) vol. 89:9367-9371.
Zuckerman, Ronald et al., " Efficient Method for the Preparation of Synthesis", Chemtracts-Macromolecular Chemistry (1993) vol.4:80-83.
Marcincin, Anton et al., "Studium Adheznych Vlastnosti N-Substituovanych Polyamidov.ll. Adhezna Praca N-Alkoxymetyl-Poly-Kaprolaktamu Kniektorym Polymerom", Plasty Kauc (1975) vol.12:101-104.
Kasica, H. et al., " Electrical Conductivity of N-Substituted Polyamides", Journal of Polymer Science Part A-1 vol.6:1615-1623.
Cosani A. et al., " N-Substituted Poly ( -amino acids). 1. Synthesis and Characterization of Poly (N-methyl-y-mehtyl L-Glutamate) and Poly ( N-methyl-Y-ethyl L-glutamate) .sup.1 ", Macromolecules (1978) vol.11 No.5;1041-1045.
Bunin, Barry A. and Ellman Jonathan A., "A General and Expedient Method for the Solid-Phase Synthesis of 1,4-Benzodiazephine Derivatives", J.Am.Chem.Soc. (Oct. 1992) vol.114:10997-10998.
Bunin, Barry A. et al., "The Combinatorial Synthesis and Chemical and Biological Evaluation of a 1,4-Benzodiazephine Library", Proc.Natl.Acad.Sci. USA (May. 1994) vol.91:4708-4712.
Chen, Chixu, et al., "`Analogous` Organic Synthesis of Small-Compound Libraries: Validation of Combinatorial Chemistry in Small-Molecule Synthesis," J. Am. Chem. Soc., (1994) vol. 116, pp. 2661-2662.
Deshpande, Milind S., "Formation of Carbon-Carbon Bond on Solid Support: Application of the Stille Reaction", Tetrahedron Lett. (1994) vol.35, No.31:5613-5614.
Dower W.J. and Fodor, S.P.A., "Chapter 28. The Search for Molecular Diversity (II): Recombinant and Synthetic Randomized Peptide Libraries", Annu.Rep.Med.Chem. (1991) vol.26:271-280.
Furka, A., et al. "General Method for Rapid Synthesis of Multicomponent Peptide Mixtures", Int.J.Peptides Protein Res. (1991) vol.37:487-493.
Furka, A., et al., "Cornucopia of Peptides by Synthesis", Dept. Org. Chem,
Hobbs-DeWitt, Sheila, et al., "`Diversomers`: An Approach to Nonpeptide, Nonoligomeric Chemical Diversity", Proc.Natl.Acad.Sci. USA (Aug. 1993) vol.90:6909-6913.
Houghten et al., "Generation and Use of Synthetic Peptide Combinational Libraries for Basic Research and Drug Discovery", Nature (1991) vol.354:84-86.
Kates S.A. et al., "Automated Allyl Cleavage for Continuous-Flow Synthesis of Cyclic and Branched Peptides" Anal.Biochem. (1993) vol.212:303-310.
Robey et al., "Automated Synthesis of N-Bromoacetyl-Modified Peptides for the Preparation of Synthetic Peptide Polymers, Peptide-Protein Conjugates, and Cyclic Peptides", Analytical Biochemistry (1989) vol.177:373-377.
Robey, F.A. et al. "Synthesis, Analyses and Uses of Site-Specific Bromoacetyl-Derivatized Synthetic Peptides: Starting Materials for Countless New Cyclic Peptides, Peptomers and Peptide Conjugates", Chimica Oggi (1992) 27-31.
Stewart, J.M. and Young, J.D., "Solid Phase Peptide Synthesis", (2nd ed.), Pierce, Rockford, Il (1984) 30-31.
Zuckermann, R.N. et al., "Design Construction and Application of Fully Automated Equimolar Peptide Mixture Synthesizer", Intl.J.Peptide Protein Res., (1992) vol.40:497-506.
Desai et al. Drug development and Research., vol. 33., pp. 174-188., 1994.
Gordon et al ., Journal of Medicinal Chemistry., vol. 37., No. 10. May 13, 1994.
Zuckermann et al., J. Am. Chem. Soc., vol. 114., pp. 10646-10647., 1992.

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