Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives
Patent
1998-06-29
2000-10-24
Peselev, Elli
Organic compounds -- part of the class 532-570 series
Organic compounds
Carbohydrates or derivatives
536 72, 536 172, 536 175, 536 176, 536 179, 536 181, 549385, 549387, 549388, 549510, 549511, C07H 1708, C07D30500, C07D31100
Patent
active
061369616
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention is in the field of biologically active compounds.
2. Discussion of the Background
The prior art is replete with examples of chemically, microbially, or enzymatically synthesizing compounds with biological activity. The goal of these efforts is the discovery of new and improved pharmaceutical compounds.
The discovery of new pharmaceutical compounds is for the most part a trial and error process. So many diverse factors constitute an effective pharmaceutical compound that it is extremely difficult to reduce the discovery process to a systematic approach. Typically, thousands of organic compounds must be isolated from biological sources or chemically synthesized and tested before a pharmaceutical compound is found.
Synthesizing and testing new compounds for biological activity, which is the first step in identifying a new synthetic drug, is a time consuming and expensive undertaking. Typically, compounds must by synthesized, purified, tested and quantitatively compared to other compounds in order to identify active compounds or identify compounds with optimal activity. The synthesis of new compounds is accomplished for the most part using standard chemical methods. Such methods provide for the synthesis of virtually any type of organic compound; however, because chemical reactions are non-specific, these syntheses require numerous steps and multiple purifications before a final compound is produced and ready for testing.
New biological and chemical approaches have recently been developed which provide for the synthesis and screening of large libraries of small peptides and oligonucleotides. These methods provide for the synthesis of a broad range of chemical compounds and provide the means to potentially identify biologically active compounds. The chemistries for synthesizing such large numbers of these natural and non-naturally occurring polymeric compounds is complicated, but manageable because each compound is synthesized with the same set of chemical protocols, the difference being the random order in which amino acids or nucleotides are introduced into the reaction sequence.
The prior art is replete with examples showing enzymatic conversion of non-physiological substances under many conditions. solvents vs. water is reversed. Journal of the American Chemical Society 108 2767-2768, 1986. PEG-modified thermolysin in peptide synthesis catalyzed in organic solvents. Biotechnology Letters 10 (2) 101-106, 1988. endonucleases by specificity relaxation in the presence of organic solvents. Ann. N.Y. Acad. Sci. 542 255-265, 1988. acid ester in an organic media with chymotrypsin modified by a bio-imprinting procedure. Biotechnology Letters 12 (3) 161-166, 1990. stereoselectivity and substrate selectivity of bio-imprinted .alpha.-chymotrypsin in anhydrous organic media. Journal of the American Chemical Society 113 (24) 9366-9368, 1991. Organic solvent changes the chymotrypsin specificity with respect to nucleophiles. FEBS Letters 307 (3) 309-312, 1992. enzyme catalysis and specificity by water-soluble additives. Ann. New York Acad. Sci. (Enzyme Eng. XI, D. S. Clark, D. A. Estell, eds) 672 329-335, 1992. Gaertner, H.. Organic reactions catalyzed by modified enzymes. 1. Alteration of the substrate specificity of a-chymotrypsin by the modification process. Journal of Molecular Catalysis 71 (2) 261-278, 1992. in organic solvents: medium effect on substrate specificity. Enzyme and Microbial Technology 14 (10) 842-847, 1992. and substrate chemistries, J. Org. Chem. 58 (12) 3238-3244, 1993. media is strongly solvent dependent. Biocatalysis 8 (1) 3-19, 1993. specificity of an enzyme. JACS 115 (5) 1629-1631, 1993. Changed/Tailored of enzyme enantioselectivity by the reaction medium. Journal of the American Chemical Society 110 (21) 7236-7237, 1988. enantioselectivity? Journal of the American Chemical Society 113 (8) 3166-3171, 1991. prediction. Pure and Applied Chemistry 64 (8) 1129-1134, 1992. of racemic carboxylic acids via the lipase-catalyzed irrevers
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Greenwald
Clark Douglas S.
Dordick Jonathan S.
Khmelnitsky Yuri L.
Michels Peter C.
EnzyMed, Inc.
Peselev Elli
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