WO2019043457 MUTANT FGF-21 PEPTIDE CONJUGATES AND USES THEREOF

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Publication Number WO/2019/043457

Publication Date 07.03.2019

International Application No. PCT/IB2018/001112

International Filing Date 04.09.2018

IPC

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CPC

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Applicants

89BIO LTD. [IL]/[IL]

Inventors

KOPEC, Karla, K.
LIU, Patrick, Mengyuan

Priority Data

62/553,970

04.09.2017

Publication Language English (en)

Filing Language English (EN)

Designated States

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Title

(EN) MUTANT FGF-21 PEPTIDE CONJUGATES AND USES THEREOF

(FR) CONJUGUÉS DE PEPTIDE FGF-21 MUTANT ET LEURS UTILISATIONS

Abstract

(EN) The present invention relates to a mutant Fibroblast Growth Factor-21 (FGF-21) peptide conjugate comprising a PEG moiety attached to a mutant FGF-21 peptide via a glycosyl linker and uses thereof. Further provided is a method for producing the mutant FGF-21 peptide conjugate and a pharmaceutical composition and container comprising said mutant FGF-21 peptide conjugate.

(FR) La présente invention concerne un conjugué de peptide de facteur de croissance des fibroblastes 21 (FGF-21) mutant comprenant un fragment PEG lié à un peptide FGF-21 mutant par l'intermédiaire d'un lieur glycosylique et ses utilisations. L'invention concerne en outre un procédé de production du conjugué de peptide FGF-21 mutant et une composition pharmaceutique et un récipient comprenant ledit conjugué de peptide FGF-21 mutant.

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38	Medicinal preparations containing peptides
16	Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
17	from animals; from humans
18	Growth factors; Growth regulators

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3	Drugs for disorders of the metabolism
08	for glucose homeostasis
10	for hyperglycaemia, e.g. antidiabetics

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9	Drugs for disorders of the cardiovascular system
10	for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17	Drugs for dermatological disorders

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17	Drugs for dermatological disorders
02	for treating wounds, ulcers, burns, scars, keloids, or the like

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1. WO2019043457 - MUTANT FGF-21 PEPTIDE CONJUGATES AND USES THEREOF

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
K	PEPTIDES
14	Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435	from animals; from humans
475	Growth factors; Growth regulators
50	Fibroblast growth factor (FGF)

C	CHEMISTRY; METALLURGY
12	BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
P	FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
21	Preparation of peptides or proteins

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47	Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50	the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51	the non-active ingredient being a modifying agent
54	the modifying agent being an organic compound
549	Sugars, nucleosides, nucleotides or nucleic acids

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47	Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50	the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51	the non-active ingredient being a modifying agent
56	the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
59	obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
60	the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47	Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50	the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51	the non-active ingredient being a modifying agent
54	the modifying agent being an organic compound
549	Sugars, nucleosides, nucleotides or nucleic acids

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47	Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50	the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51	the non-active ingredient being a modifying agent
56	the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
59	obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
60	the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol