CA2090860A1 - Synthesis of equimolar multiple oligomer mixtures, especially of oligopeptide mixtures - Google Patents

Synthesis of equimolar multiple oligomer mixtures, especially of oligopeptide mixtures

Info

Publication number
CA2090860A1
CA2090860A1 CA002090860A CA2090860A CA2090860A1 CA 2090860 A1 CA2090860 A1 CA 2090860A1 CA 002090860 A CA002090860 A CA 002090860A CA 2090860 A CA2090860 A CA 2090860A CA 2090860 A1 CA2090860 A1 CA 2090860A1
Authority
CA
Canada
Prior art keywords
synthesis
mixtures
equimolar
amino acid
disclosed
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
CA002090860A
Other languages
French (fr)
Other versions
CA2090860C (en
Inventor
Richard A. Houghten
Julio H. Cuervo
Clemencia Pinilla
Jon R. Appel, Jr.
Silvie Blondelle
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
ITEREX PHARMACEUTICALS LP
Original Assignee
Richard A. Houghten
Julio H. Cuervo
Clemencia Pinilla
Jon R. Appel, Jr.
Silvie Blondelle
Iterex Pharmaceuticals Ltd. Partnership
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Richard A. Houghten, Julio H. Cuervo, Clemencia Pinilla, Jon R. Appel, Jr., Silvie Blondelle, Iterex Pharmaceuticals Ltd. Partnership filed Critical Richard A. Houghten
Publication of CA2090860A1 publication Critical patent/CA2090860A1/en
Application granted granted Critical
Publication of CA2090860C publication Critical patent/CA2090860C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J19/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J19/0046—Sequential or parallel reactions, e.g. for the synthesis of polypeptides or polynucleotides; Apparatus and devices for combinatorial chemistry or for making molecular arrays
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/04—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length on carriers
    • C07K1/047—Simultaneous synthesis of different peptide species; Peptide libraries
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00274—Sequential or parallel reactions; Apparatus and devices for combinatorial chemistry or for making arrays; Chemical library technology
    • B01J2219/00277—Apparatus
    • B01J2219/00279—Features relating to reactor vessels
    • B01J2219/00281—Individual reactor vessels
    • B01J2219/00295—Individual reactor vessels the reactor vessels having pervious side walls
    • B01J2219/00297—"Tea bags"
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00274—Sequential or parallel reactions; Apparatus and devices for combinatorial chemistry or for making arrays; Chemical library technology
    • B01J2219/00277—Apparatus
    • B01J2219/00457—Dispensing or evacuation of the solid phase support
    • B01J2219/00459—Beads
    • B01J2219/00461—Beads and reaction vessel together
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00274—Sequential or parallel reactions; Apparatus and devices for combinatorial chemistry or for making arrays; Chemical library technology
    • B01J2219/00277—Apparatus
    • B01J2219/00497—Features relating to the solid phase supports
    • B01J2219/005—Beads
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00274—Sequential or parallel reactions; Apparatus and devices for combinatorial chemistry or for making arrays; Chemical library technology
    • B01J2219/00583—Features relative to the processes being carried out
    • B01J2219/00585—Parallel processes
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00274—Sequential or parallel reactions; Apparatus and devices for combinatorial chemistry or for making arrays; Chemical library technology
    • B01J2219/00583—Features relative to the processes being carried out
    • B01J2219/0059—Sequential processes
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00274—Sequential or parallel reactions; Apparatus and devices for combinatorial chemistry or for making arrays; Chemical library technology
    • B01J2219/00583—Features relative to the processes being carried out
    • B01J2219/00592—Split-and-pool, mix-and-divide processes
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00274—Sequential or parallel reactions; Apparatus and devices for combinatorial chemistry or for making arrays; Chemical library technology
    • B01J2219/00583—Features relative to the processes being carried out
    • B01J2219/00596—Solid-phase processes
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00274—Sequential or parallel reactions; Apparatus and devices for combinatorial chemistry or for making arrays; Chemical library technology
    • B01J2219/00718—Type of compounds synthesised
    • B01J2219/0072—Organic compounds
    • B01J2219/00725—Peptides
    • C—CHEMISTRY; METALLURGY
    • C40—COMBINATORIAL TECHNOLOGY
    • C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B40/00—Libraries per se, e.g. arrays, mixtures
    • C40B40/04—Libraries containing only organic compounds
    • C40B40/10—Libraries containing peptides or polypeptides, or derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C40—COMBINATORIAL TECHNOLOGY
    • C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B60/00—Apparatus specially adapted for use in combinatorial chemistry or with libraries
    • C40B60/14—Apparatus specially adapted for use in combinatorial chemistry or with libraries for creating libraries

Abstract

A process for the synthesis of a complex mixture pool of solid support-coupled monomeric repeating unit compounds such as amino acid derivatives is disclosed in which the mixture pool contains an equimolar representation of reacted monomeric re-peating unit compounds coupled. Also disclosed is a process for the stepwise synthesis of a complex mixture of coupled or free, unsupported oligomers such as oligopeptides. A set of self-solubilizing, unsupported mixed oligopeptides having one or more predetermined amino acid residues at one or more of the same, predetermined positions in the oligopeptide chain in which the set contains equimolar amounts of a plurality of different amino acid residues, preferably at least six different residues, at one or more of the same predetermined positions of the oligopeptide chain is also disclosed, as are methods of making and using the same.
CA002090860A 1990-11-21 1991-11-20 Synthesis of equimolar multiple oligomer mixtures, especially of oligopeptide mixtures Expired - Fee Related CA2090860C (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US61702390A 1990-11-21 1990-11-21
US617,023 1990-11-21
US70165891A 1991-05-16 1991-05-16
US701,658 1991-05-16
US79755191A 1991-11-19 1991-11-19
US07/797,551 1991-11-19
PCT/US1991/008694 WO1992009300A1 (en) 1990-11-21 1991-11-20 Synthesis of equimolar multiple oligomer mixtures, especially of oligopeptide mixtures

Publications (2)

Publication Number Publication Date
CA2090860A1 true CA2090860A1 (en) 1992-05-22
CA2090860C CA2090860C (en) 2003-09-16

Family

ID=27417190

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002090860A Expired - Fee Related CA2090860C (en) 1990-11-21 1991-11-20 Synthesis of equimolar multiple oligomer mixtures, especially of oligopeptide mixtures

Country Status (11)

Country Link
US (2) US5556762A (en)
EP (1) EP0558671B1 (en)
JP (1) JP3523252B2 (en)
AT (1) ATE176239T1 (en)
AU (1) AU668347B2 (en)
CA (1) CA2090860C (en)
DE (1) DE69130831T2 (en)
DK (1) DK0558671T3 (en)
ES (1) ES2129442T3 (en)
GR (1) GR3030061T3 (en)
WO (1) WO1992009300A1 (en)

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