WO2012059873A3 - Anti-diabetic compounds - Google Patents

Anti-diabetic compounds Download PDF

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Publication number
WO2012059873A3
WO2012059873A3 PCT/IB2011/054874 IB2011054874W WO2012059873A3 WO 2012059873 A3 WO2012059873 A3 WO 2012059873A3 IB 2011054874 W IB2011054874 W IB 2011054874W WO 2012059873 A3 WO2012059873 A3 WO 2012059873A3
Authority
WO
WIPO (PCT)
Prior art keywords
linker
covalently attached
fgf21
diabetic compounds
compounds
Prior art date
Application number
PCT/IB2011/054874
Other languages
French (fr)
Other versions
WO2012059873A2 (en
Inventor
Tetsuya Ishino
Moorthy Sitharamaiah Suriyanarayana Palanki
Bernard Norman Violand
Tapan Kanti Das
Tamara Shafer Hodge
Nancy Jane Levin
Erin Kristen Parsons
Original Assignee
Covx Technologies Ireland, Ltd.
Pfizer Inc.
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45401106&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2012059873(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority to RU2013118441/15A priority Critical patent/RU2013118441A/en
Priority to AU2011324886A priority patent/AU2011324886A1/en
Priority to JP2013537240A priority patent/JP2014500248A/en
Priority to SG2013033378A priority patent/SG190082A1/en
Priority to BR112013011172A priority patent/BR112013011172A2/en
Priority to CA2815967A priority patent/CA2815967A1/en
Priority to MX2013005075A priority patent/MX2013005075A/en
Application filed by Covx Technologies Ireland, Ltd., Pfizer Inc. filed Critical Covx Technologies Ireland, Ltd.
Priority to KR1020137014378A priority patent/KR20130086623A/en
Priority to EP11799823.7A priority patent/EP2635309A2/en
Priority to CN2011800641240A priority patent/CN103282055A/en
Publication of WO2012059873A2 publication Critical patent/WO2012059873A2/en
Publication of WO2012059873A3 publication Critical patent/WO2012059873A3/en
Priority to IL225895A priority patent/IL225895A0/en
Priority to ZA2013/03657A priority patent/ZA201303657B/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/40—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6815—Enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/475—Growth factors; Growth regulators
    • C07K14/50—Fibroblast growth factor [FGF]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide
    • C07K2319/30—Non-immunoglobulin-derived peptide or protein having an immunoglobulin constant or Fc region, or a fragment thereof, attached thereto
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide
    • C07K2319/31—Fusion polypeptide fusions, other than Fc, for prolonged plasma life, e.g. albumin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide
    • C07K2319/70—Fusion polypeptide containing domain for protein-protein interaction
    • C07K2319/74—Fusion polypeptide containing domain for protein-protein interaction containing a fusion for binding to a cell surface receptor
    • C07K2319/75—Fusion polypeptide containing domain for protein-protein interaction containing a fusion for binding to a cell surface receptor containing a fusion for activation of a cell surface receptor, e.g. thrombopoeitin, NPY and other peptide hormones

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Toxicology (AREA)
  • Zoology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)

Abstract

The present invention provides a FGF21 molecule covalently attached to the combining site of an antibody via a linker, wherein the linker is covalently attached to the side chain of a linking residue within FGF21. Various uses of the compounds are provided, including methods to prevent or treat diabetes or diabetes-related conditions.
PCT/IB2011/054874 2010-11-05 2011-11-02 Anti-diabetic compounds WO2012059873A2 (en)

Priority Applications (12)

Application Number Priority Date Filing Date Title
CN2011800641240A CN103282055A (en) 2010-11-05 2011-11-02 Anti-diabetic compounds
MX2013005075A MX2013005075A (en) 2010-11-05 2011-11-02 Anti-diabetic compounds.
JP2013537240A JP2014500248A (en) 2010-11-05 2011-11-02 Anti-diabetic compounds
SG2013033378A SG190082A1 (en) 2010-11-05 2011-11-02 Anti-diabetic compounds
BR112013011172A BR112013011172A2 (en) 2010-11-05 2011-11-02 antidiabetic compounds
CA2815967A CA2815967A1 (en) 2010-11-05 2011-11-02 Anti-diabetic compounds
KR1020137014378A KR20130086623A (en) 2010-11-05 2011-11-02 Anti-diabetic compounds
RU2013118441/15A RU2013118441A (en) 2010-11-05 2011-11-02 ANTI-DIABETIC COMPOUNDS
AU2011324886A AU2011324886A1 (en) 2010-11-05 2011-11-02 Anti-diabetic compounds
EP11799823.7A EP2635309A2 (en) 2010-11-05 2011-11-02 Anti-diabetic compounds
IL225895A IL225895A0 (en) 2010-11-05 2013-04-22 Anti-diabetic compounds
ZA2013/03657A ZA201303657B (en) 2010-11-05 2013-05-20 Anti-diabetic compounds

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US41071510P 2010-11-05 2010-11-05
US61/410,715 2010-11-05

Publications (2)

Publication Number Publication Date
WO2012059873A2 WO2012059873A2 (en) 2012-05-10
WO2012059873A3 true WO2012059873A3 (en) 2012-06-28

Family

ID=45401106

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2011/054874 WO2012059873A2 (en) 2010-11-05 2011-11-02 Anti-diabetic compounds

Country Status (18)

Country Link
US (1) US8722622B2 (en)
EP (1) EP2635309A2 (en)
JP (1) JP2014500248A (en)
KR (1) KR20130086623A (en)
CN (1) CN103282055A (en)
AR (1) AR083786A1 (en)
AU (1) AU2011324886A1 (en)
BR (1) BR112013011172A2 (en)
CA (1) CA2815967A1 (en)
CO (1) CO6741158A2 (en)
IL (1) IL225895A0 (en)
MX (1) MX2013005075A (en)
PE (1) PE20140260A1 (en)
RU (1) RU2013118441A (en)
SG (1) SG190082A1 (en)
TW (1) TW201233685A (en)
WO (1) WO2012059873A2 (en)
ZA (1) ZA201303657B (en)

Families Citing this family (12)

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Publication number Priority date Publication date Assignee Title
US9574002B2 (en) 2011-06-06 2017-02-21 Amgen Inc. Human antigen binding proteins that bind to a complex comprising β-Klotho and an FGF receptor
EP3125921B1 (en) 2014-03-11 2020-07-08 Novartis AG Fgf21 variants for use in treating hiv-haart induced partial lipodystrophy
US10328131B2 (en) 2014-03-13 2019-06-25 Dana-Farber Cancer Institute, Inc. Compositions and methods for regulating pancreatic beta cell function using adipsin
MY198629A (en) 2014-07-24 2023-09-11 Genentech Inc Methods of conjugating an agent to a thiol moiety in a protein that contains at least one trisulfide bond
US11638745B2 (en) 2015-05-20 2023-05-02 University of Pittsburgh—Of the Commonwealth Cvctom of Hierher Education Method to improve neurologic outcomes in temperature managed patients
RU2752530C2 (en) 2015-08-03 2021-07-29 Новартис Аг Methods for treating fgf21-related disorders
US10899844B2 (en) 2017-02-08 2021-01-26 Novartis Ag FGF21 mimetic antibodies and uses thereof
WO2020010117A2 (en) 2018-07-03 2020-01-09 Bristol-Myers Squibb Company Fgf21 formulations
EP3863672A4 (en) * 2018-10-11 2022-06-29 The Scripps Research Institute Antibody compounds with reactive arginine and related antibody drug conjugates
AR122359A1 (en) * 2020-01-08 2022-09-07 Bristol Myers Squibb Co FGF-21 CONJUGATE FORMULATIONS
CN113728013B (en) 2020-01-11 2022-06-14 北京质肽生物医药科技有限公司 Conjugates of fusion proteins of GLP-1 and FGF21
CA3217236A1 (en) * 2021-04-30 2022-11-03 Innovent Biologics (Suzhou) Co. Ltd. Oxm3 storage agent, oxm3 preparation, and preparation method

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