RU2018112257A - Оптимизация растворимости иммуносвязывающих средств - Google Patents

Оптимизация растворимости иммуносвязывающих средств Download PDF

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RU2018112257A
RU2018112257A RU2018112257A RU2018112257A RU2018112257A RU 2018112257 A RU2018112257 A RU 2018112257A RU 2018112257 A RU2018112257 A RU 2018112257A RU 2018112257 A RU2018112257 A RU 2018112257A RU 2018112257 A RU2018112257 A RU 2018112257A
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amino acid
heavy chain
acid position
immunobinding agent
serine
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RU2018112257A
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Леонардо БОРРАС
Дэвид УРЕХ
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ИЭсБиЭйТЕК, ЭН АЛЬКОН БАЙОМЕДИКАЛ РИСЕРЧ ЮНИТ ЭлЭлСи
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/24Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
    • C07K16/241Tumor Necrosis Factors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/22Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against growth factors ; against growth regulators
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/50Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/56Immunoglobulins specific features characterized by immunoglobulin fragments variable (Fv) region, i.e. VH and/or VL
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/50Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/56Immunoglobulins specific features characterized by immunoglobulin fragments variable (Fv) region, i.e. VH and/or VL
    • C07K2317/567Framework region [FR]
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/50Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/56Immunoglobulins specific features characterized by immunoglobulin fragments variable (Fv) region, i.e. VH and/or VL
    • C07K2317/569Single domain, e.g. dAb, sdAb, VHH, VNAR or nanobody®
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/60Immunoglobulins specific features characterized by non-natural combinations of immunoglobulin fragments
    • C07K2317/62Immunoglobulins specific features characterized by non-natural combinations of immunoglobulin fragments comprising only variable region components
    • C07K2317/622Single chain antibody (scFv)
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/90Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
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    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/90Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
    • C07K2317/94Stability, e.g. half-life, pH, temperature or enzyme-resistance

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (AREA)
  • Mycology (AREA)
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  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Saccharide Compounds (AREA)

Claims (14)

1. Иммуносвязывающее средство, содержащее следующие повышающие растворимость мотивы в аминокислотных положениях 12, 103 и 144 тяжелой цепи (Система нумерации AHo):
(a) серин (S) в аминокислотном положении 12 тяжелой цепи;
(b) серин (S) в аминокислотном положении 103 тяжелой цепи; и
(c) серин (S) в аминокислотном положении 144 тяжелой цепи;
где иммуносвязывающее средство содержит вариабельную область тяжелой цепи или ее фрагмент.
2. Иммуносвязывающее средство по п. 1, дополнительно содержащее
(a) аспарагиновую кислоту (D) в аминокислотном положении 31 легкой цепи;
(b) глютаминовую кислоту (E) в аминокислотном положении 83 легкой цепи;
(c) аргинин (R) в аминокислотном положении 43 тяжелой цепи;
(d) лейцин (L) в аминокислотном положении 67 тяжелой цепи; и/или
(e) аланин (A) в аминокислотном положении 78 тяжелой цепи.
3. Иммуносвязывающее средство по п. 1 или 2, которое представляет собой scFv антитело, полноразмерный иммуноглобулин, Fab фрагмент, Dab или вариабельную область тяжелой цепи, содержащую единственный вариабельный домен или два константных домена.
4. Иммуносвязывающее средство по п. 3, где иммуносвязывающее средство специфически связывается с TNFα человека или VEGF человека.
5. Композиция, содержащая, иммуносвязывающее средство по п. 1 и фармацевтически приемлемый носитель.
RU2018112257A 2008-06-25 2018-04-05 Оптимизация растворимости иммуносвязывающих средств RU2018112257A (ru)

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US7569208P 2008-06-25 2008-06-25
US61/075,692 2008-06-25

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RU2011102548/10A RU2514658C2 (ru) 2008-06-25 2009-06-25 Оптимизация растворимости иммуносвязывающих средств
RU2014104577A RU2653441C2 (ru) 2008-06-25 2014-02-10 Оптимизация растворимости иммуносвязывающих средств
RU2018112257A RU2018112257A (ru) 2008-06-25 2018-04-05 Оптимизация растворимости иммуносвязывающих средств

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RU2014104577A RU2653441C2 (ru) 2008-06-25 2014-02-10 Оптимизация растворимости иммуносвязывающих средств

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EP (2) EP3241843B1 (ru)
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KR (2) KR101650165B1 (ru)
CN (2) CN102076715B (ru)
AU (1) AU2009264566B2 (ru)
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CY1124644T1 (el) 2022-07-22
KR101790567B1 (ko) 2017-10-26
CN102076715B (zh) 2018-06-19
US20170096482A1 (en) 2017-04-06
WO2009155725A1 (en) 2009-12-30
ES2629345T3 (es) 2017-08-08
PT3241843T (pt) 2021-09-10
JP2011525496A (ja) 2011-09-22
SI3241843T1 (sl) 2021-11-30
EP2307455B1 (en) 2017-03-22
CA2728829A1 (en) 2009-12-30
DK3241843T3 (da) 2021-09-06
US20110268728A1 (en) 2011-11-03
US20190169284A1 (en) 2019-06-06
JP5745720B2 (ja) 2015-07-08
LT3241843T (lt) 2021-09-27
KR101650165B1 (ko) 2016-08-22
PL2307455T3 (pl) 2017-09-29
RU2014104577A (ru) 2015-08-20
US10221237B2 (en) 2019-03-05
CN105418763A (zh) 2016-03-23
EP3241843A1 (en) 2017-11-08
MX346024B (es) 2017-03-02
PL3241843T3 (pl) 2021-12-27
BRPI0914666A2 (pt) 2015-10-20
RU2514658C2 (ru) 2014-04-27
JP2016128517A (ja) 2016-07-14
SI2307455T1 (sl) 2017-07-31
CN102076715A (zh) 2011-05-25
EP2307455A1 (en) 2011-04-13
PT2307455T (pt) 2017-07-03
HUE034827T2 (en) 2018-03-28
CA2728829C (en) 2018-01-02
RU2653441C2 (ru) 2018-05-08
US11046757B2 (en) 2021-06-29
KR20110022714A (ko) 2011-03-07
LT2307455T (lt) 2017-06-26
ZA201008595B (en) 2012-02-29
EP3241843B1 (en) 2021-07-28
HRP20211356T1 (hr) 2021-11-26
HUE056090T2 (hu) 2022-01-28
DK2307455T3 (en) 2017-07-10
US9556265B2 (en) 2017-01-31
CY1119626T1 (el) 2018-04-04
AU2009264566A1 (en) 2009-12-30
RU2011102548A (ru) 2012-07-27
AU2009264566B2 (en) 2014-05-08
HRP20171250T1 (hr) 2017-10-20
ES2884117T3 (es) 2021-12-10
JP2014111667A (ja) 2014-06-19
MX2011000074A (es) 2011-02-24
KR20160083129A (ko) 2016-07-11

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