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US5650489A Expired / Lapsed US ⏱️ 0.0 years remaining

Random bio-oligomer library, a method of synthesis thereof, and a method of use thereof

Assignee: Aventis Pharmaceuticals Inc
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Filing: 1991-06-19
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Granted: 1997-07-22
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Expires: 2011-06-19
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Abstract

Abstract The instant invention provides a library of bio-oligomers of defined size and known composition, in which the library contains all of the possible sequences of the bio-oligomers, and a method of synthesis thereof. The bio-oligomers of the library may be peptides, nucleic acids, or a combination of the foregoing. The instant invention also provides methods to identify bio-oligomers from a library that demonstrate desired characteristics such as binding, bioactivity and catalytic activity. Thus the instant invention provides a unique and powerful method to identify a useful bio-oligomer sequences from a library more quickly than current state-of-the-art technology allows. Effector molecules for use in treatment or diagnosis of disease are also provided.

Inventors

  • 👤 Kit Sang Lam
  • 👤 Sydney E. Salmon

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 22:37
CPC Classifications
C; C12; C12N; C12N15/00; C12N15/09; C12N15/10; C12N15/1034; C12N15/1075; C12Q; C12Q1/00; C07; C07K; C07K1/00; C07K1/04; C07K1/047; C07K14/00; C07K14/435; C07K14/665; C07K14/70; C07K14/82; C07K16/00; C07K16/18; C07K16/26; C07K16/32; C12N15/1062; A; A61; A61K; A61K38/00; A61K39/00; B; B01; B01J; B01J2219/00; B01J2219/00274; B01J2219/00583; B01J2219/00585; B01J2219/0059; B01J2219/00592; B01J2219/0068; B01J2219/00702; B01J2219/00718; B01J2219/0072; B01J2219/00722; B01J2219/00725; B01J2219/00729; C07K2317/00; C07K2317/30; C07K2317/34; C07K2317/90; C07K2317/92; C40; C40B; C40B40/00; C40B40/04; C40B40/06; C40B40/10; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55; Y10; Y10S; Y10S530/00; Y10S530/806; Y10S530/81; Y10S530/812; Y10S530/815; Y10S530/817

Claims Analysis

Total Claims: 13
Claim 1
Independent Claim 184 words
A library comprising a multiplicity of solid phase supports, wherein a single peptide species is attached to each solid phase support, and in which the library is prepared by a method comprising repeating k times, wherein k is at least three, the steps of: (i) providing at least two aliquots of a solid phase support said supports having an N reactive site; (ii) separately introducing a species of subunit of the peptides to each of the aliquots of solid phase supports such that a different subunit is introduced into each aliquot, said subunit having an N-blocking group and at least one of said subunits having a protecting group or a plurality of protecting groups; (iii) completely covalently coupling the subunit to substantially all the reactive sites of the solid phase support; (iv) thoroughly mixing and removing the N-blocking groups of the aliquots of the solid phase supports whereby an N reactive site is provided; and after repeating steps ii through (iv) k times, a final step of removing any protecting groups such that the deprotected peptides remain covalently attached to the solid phase supports.
Claim 2
Dependent Claim 184 words
A library comprising a multiplicity of solid phase supports, wherein a single peptide species is attached to each solid phase support, and in which the library is prepared by a method comprising repeating k times, wherein k is at least three, the steps of: (i) providing at least two aliquots of a solid phase support said supports having an N reactive site; (ii) separately introducing a species of subunit of the peptides to each of the aliquots of solid phase supports such that a different subunit is introduced into each aliquot, said subunit having an N-blocking group and at least one of said subunits having a protecting group or a plurality of protecting groups; (iii) completely covalently coupling the subunit to substantially all the reactive sites of the solid phase support; (iv) thoroughly mixing and removing the N-blocking groups of the aliquots of the solid phase supports whereby an N reactive site is provided; and after repeating steps ii through (iv) k times, a final step of removing any protecting groups such that the deprotected peptides remain covalently attached to the solid phase supports.
Claim 3
Dependent Claim 26 words
The library of claim 1 in which the subunits are selected from the group consisting of glycine, L-amino acids, D-amino acids, non-classical amino acids and peptidomimetics.
Claim 4
Dependent Claim 51 words
The library of claim 1 in which each peptide species includes at least two amino acids capable of intra-peptide cross-linking and the library of peptides has been treated so as to crosslink the amino acids capable of crosslinking in each peptide to form a constrained, cyclized or rigidized intra-molecular crosslinked peptide.
Claim 5
Dependent Claim 31 words
The library of claim 1 in which the solid phase support is selected from the group consisting of polystyrene resin, polyamide resin, polystyrene resin grafted with polyethylene glycol and polydimethylacrylamide resin.
Claim 6
Dependent Claim 14 words
The library of claim 4 in which the solid phase support is polydimethylacrylamide resin.
Claim 7
Dependent Claim 17 words
The library of claim 4 in which the solid phase support is polystyrene grafted with polyethylene glycol.
Claim 8
Dependent Claim 27 words
The library of claim 1 in which the solid phase support of step (i) comprises a linker by means of which the peptides can be attached covalently.
Claim 9
Dependent Claim 27 words
The library of claim 7 in which the linker is selected from the group consisting of aminobutyric acid, aminocaproic acid, 7-aminoheptanoic acid, ethylene glycol, and 8-aminocaprylic acid.
Claim 10
Dependent Claim 38 words
The library of claim 1 in which the method of preparing the library comprises a further step after step (iii) of assessing the completeness of coupling of the subunit to the solid phase support in each separate aliquot.
Claim 11
Dependent Claim 11 words
The library of claim 1 comprising at least about 8000 species.
Claim 12
Dependent Claim 11 words
The library of claim 10 comprising at least about 500,000 species.
Claim 13
Dependent Claim 11 words
The library of claim 11 comprising at least about 2,500,000 species.

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Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 2000-07-21 2001-01-20 2001-07-22 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 2004-07-21 2005-01-20 2005-07-22 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2008-07-21 2009-01-20 2009-07-22 $7700.00 Window Closed / Lapsed

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