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1. WO1990012874 - CYSTEINE ADDED VARIANTS OF POLYPEPTIDES AND CHEMICAL MODIFICATIONS THEREOF

Publication Number WO/1990/012874
Publication Date 01.11.1990
International Application No. PCT/US1990/002144
International Filing Date 19.04.1990
Chapter 2 Demand Filed 19.11.1990
IPC
A61K 38/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61K 47/48 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
48the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
C07K 14/505 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
475Growth factors; Growth regulators
505Erythropoietin (EPO)
C07K 14/535 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
52Cytokines; Lymphokines; Interferons
53Colony-stimulating factor (CSF)
535Granulocyte CSF; Granulocyte-macrophage CSF
C07K 14/54 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
52Cytokines; Lymphokines; Interferons
54Interleukins (IL)
CPC
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61K 47/60
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
56the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
59obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
60the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61P 7/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
A61P 7/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
06Antianaemics
C07K 14/505
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
475Growth factors; Growth regulators
505Erythropoietin [EPO]
C07K 14/535
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
52Cytokines; Lymphokines; Interferons
53Colony-stimulating factor [CSF]
535Granulocyte CSF; Granulocyte-macrophage CSF
Applicants
  • GENETICS INSTITUTE, INC. [US]/[US]
Inventors
  • SHAW, Gray
  • VELDMAN, Geertruida
  • WOOTERS, Joseph
Agents
  • CSERR, Luann
Priority Data
341,99021.04.1989US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) CYSTEINE ADDED VARIANTS OF POLYPEPTIDES AND CHEMICAL MODIFICATIONS THEREOF
(FR) VARIANTES DE POLYPEPTIDES PAR ADDITION DE CYSTEINE, ET LEURS MODIFICATIONS CHIMIQUES
Abstract
(EN)
Cysteine added variants ('CAVs') of polypeptides are provided having one or more cysteine residues substituted for selected naturally occurring amino acid residues, or inserted into the polypeptide sequence, and preferably being further modified by deletion of certain N-terminal amino acids. Such CAVs may be additionally modified by the coupling of sulfhydryl reactive compounds to the introduced cysteine residue(s) without loss of bioactivity to produce selected homogeneously modified IL-3, G-CSF or EPO and improved pharmaceutical compositions containing the same.
(FR)
Des variantes à addition de cystéine (''CAVs'') de polypeptides ont un ou plusieurs restes de cystéine qui remplacent des restes d'acides aminés naturels, ou qui sont introduits dans la séquence du polypeptide, et sont de préférence modifiées par suppression de certains acides aminés à terminaison N. De telles variantes à addition de cystéine peuvent être à nouveau modifiées par couplage de composés réactifs sulfhydryles au reste (aux restes) de cystéine introduit(s) sans perte de bioactivité afin de produire IL-3, G-CSF ou EPO sélectionnés et modifiés de manière homogène. L'invention concerne également des compositions pharmaceutiques améliorées contenant lesdites variantes.
Also published as
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