PE20220393A1 - Procedimiento novedoso para preparar un conjugado de farmaco de accion prolongada mediante la preparacion de un intermedio - Google Patents

Procedimiento novedoso para preparar un conjugado de farmaco de accion prolongada mediante la preparacion de un intermedio

Info

Publication number
PE20220393A1
PE20220393A1 PE2022000090A PE2022000090A PE20220393A1 PE 20220393 A1 PE20220393 A1 PE 20220393A1 PE 2022000090 A PE2022000090 A PE 2022000090A PE 2022000090 A PE2022000090 A PE 2022000090A PE 20220393 A1 PE20220393 A1 PE 20220393A1
Authority
PE
Peru
Prior art keywords
preparing
coo
formula
drug conjugate
nhco
Prior art date
Application number
PE2022000090A
Other languages
English (en)
Inventor
Cheongbyeol Shin
Dooseo Jang
Ji Hye Moon
Dong Hyun Kim
Ji Eun Lee
Original Assignee
Hanmi Pharm Ind Co Ltd
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 Hanmi Pharm Ind Co Ltd filed Critical Hanmi Pharm Ind Co Ltd
Publication of PE20220393A1 publication Critical patent/PE20220393A1/es

Links

Classifications

    • 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
    • C07K14/575—Hormones
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32—Polymers modified by chemical after-treatment
    • C08G65/321—Polymers modified by chemical after-treatment with inorganic compounds
    • C08G65/325—Polymers modified by chemical after-treatment with inorganic compounds containing nitrogen
    • 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
    • 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
    • A61K47/56—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • 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
    • 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
    • C07K14/575—Hormones
    • C07K14/605—Glucagons
    • 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
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Zoology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Endocrinology (AREA)
  • Genetics & Genomics (AREA)
  • Inorganic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Polymers & Plastics (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

La presente invencion se refiere a un compuesto de Formula 1 o un estereoisomero, un solvato o una sal farmaceuticamente aceptable del mismo: X-L1-(OCH2CH2)nO-L2-R (Formula 1) donde X comprende, en el extremo N, una secuencia bisagra que comprende una secuencia de aminoacidos de la SEQ ID NO: 9 (Pro-Ser-Cys-Pro); L1 es un alquileno C1-C6 de cadena lineal o ramificada; L2 es -a1-CONH-, -a1-NHCO-, -a1-NHCO-a2-, -COO-, -b1-COO-, -COO-b2- o -b1-COO-b2-, en los que a1, a2, b1 y b2 son cada uno independientemente un alquileno C1-C6 de cadena lineal o ramificada; n es de 10 a 2400; y, R es uno cualquiera seleccionado del grupo que consiste en 2,5-dioxopirrolidinilo, 2,5-dioxopirrolilo, aldehido, maleimida, disulfuro de arilo C6-C20, disulfuro de heteroarilo C5-C20, vinil sulfona, tiol, acetamida halogenada, succinimida, carbonato de p-nitrofenilo y tioester. Dicho compuesto de Formula 1 es un farmaco preferentemente un polipeptido fisiologicamente activo el cual es un agonista trigonal de GLP-1/GIP/Glucagon o un analogo del mismo. La invencion tambien se refiere a una composicion para preparar el conjugado del farmaco y un procedimiento de preparacion del mismo.
PE2022000090A 2019-07-18 2019-07-18 Procedimiento novedoso para preparar un conjugado de farmaco de accion prolongada mediante la preparacion de un intermedio PE20220393A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/KR2019/008912 WO2021010532A1 (ko) 2019-07-18 2019-07-18 신규 중간체 제조를 통한 지속형 약물 결합체의 제조 방법

Publications (1)

Publication Number Publication Date
PE20220393A1 true PE20220393A1 (es) 2022-03-18

Family

ID=74210441

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022000090A PE20220393A1 (es) 2019-07-18 2019-07-18 Procedimiento novedoso para preparar un conjugado de farmaco de accion prolongada mediante la preparacion de un intermedio

Country Status (12)

Country Link
US (2) US11717577B2 (es)
EP (1) EP4001303A4 (es)
JP (2) JP7394207B2 (es)
KR (2) KR102478588B1 (es)
CN (1) CN114945587A (es)
AU (1) AU2019457235C1 (es)
BR (1) BR112022000760B1 (es)
CA (1) CA3147883C (es)
MX (1) MX2022000758A (es)
NZ (1) NZ784956A (es)
PE (1) PE20220393A1 (es)
WO (1) WO2021010532A1 (es)

Family Cites Families (19)

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US6096871A (en) 1995-04-14 2000-08-01 Genentech, Inc. Polypeptides altered to contain an epitope from the Fc region of an IgG molecule for increased half-life
DE69731289D1 (de) 1996-03-18 2004-11-25 Univ Texas Immunglobulinähnliche domäne mit erhöhten halbwertszeiten
MY149128A (en) 2005-08-16 2013-07-15 Hanmi Science Co Ltd A method for the mass production of immunoglobulin fc region deleted initial methionine residues
BRPI0710011A2 (pt) 2006-04-14 2011-08-02 Trubion Pharmaceuticals Inc proteìnas de ligação compreendendo articulação de imunoglobulina e regiões fc dotadas de funções efetoras fc alteradas
CA2688275A1 (en) 2007-05-31 2008-12-04 Genmab A/S Stable igg4 antibodies
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CA2792942A1 (en) * 2010-04-09 2011-10-13 Merck Sharp & Dohme Corp. Novel single chemical entities and methods for delivery of oligonucleotides
KR101382593B1 (ko) * 2010-07-21 2014-04-10 한미사이언스 주식회사 신규한 지속형 글루카곤 결합체 및 이를 포함하는 비만 예방 및 치료용 약학적 조성물
UA113626C2 (xx) * 2011-06-02 2017-02-27 Композиція для лікування діабету, що містить кон'югат інсуліну тривалої дії та кон'югат інсулінотропного пептиду тривалої дії
GB201203071D0 (en) * 2012-02-22 2012-04-04 Ucb Pharma Sa Biological products
KR102073748B1 (ko) * 2013-01-31 2020-02-05 한미약품 주식회사 재조합 효모 형질전환체 및 이를 이용하여 면역글로불린 단편을 생산하는 방법
RU2677796C9 (ru) 2013-03-05 2019-03-15 Ханми Фарм. Ко., Лтд. Улучшенный способ получения конъюгата физиологически активного полипептида с высоким выходом
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Also Published As

Publication number Publication date
BR112022000760A2 (pt) 2022-03-15
EP4001303A4 (en) 2023-05-31
US20230248843A1 (en) 2023-08-10
JP7394207B2 (ja) 2023-12-07
AU2019457235B2 (en) 2022-06-16
JP2022532445A (ja) 2022-07-14
CN114945587A (zh) 2022-08-26
US20230103271A2 (en) 2023-03-30
AU2019457235C1 (en) 2022-12-22
KR20210010428A (ko) 2021-01-27
AU2019457235A1 (en) 2022-03-03
US11717577B2 (en) 2023-08-08
KR102478588B1 (ko) 2022-12-16
WO2021010532A1 (ko) 2021-01-21
JP2023182575A (ja) 2023-12-26
KR20220022899A (ko) 2022-02-28
NZ784956A (en) 2023-01-27
US20220257788A1 (en) 2022-08-18
MX2022000758A (es) 2022-02-11
CA3147883C (en) 2024-01-02
CA3147883A1 (en) 2021-01-21
KR102334315B1 (ko) 2021-12-06
BR112022000760B1 (pt) 2024-01-02
EP4001303A1 (en) 2022-05-25

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