HUE030373T2 - Eljárás fiziológiásan aktív polipeptid helyspecifikus konjugátumának elõállítására - Google Patents

Eljárás fiziológiásan aktív polipeptid helyspecifikus konjugátumának elõállítására Download PDF

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Publication number
HUE030373T2
HUE030373T2 HUE10753706A HUE10753706A HUE030373T2 HU E030373 T2 HUE030373 T2 HU E030373T2 HU E10753706 A HUE10753706 A HU E10753706A HU E10753706 A HUE10753706 A HU E10753706A HU E030373 T2 HUE030373 T2 HU E030373T2
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HU
Hungary
Prior art keywords
alkohol
conjugate
peg
physiologically active
pegylated
Prior art date
Application number
HUE10753706A
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English (en)
Inventor
Dae Hae Song
Jae Hee Shin
Jae Min Lee
Young Kyung Park
Se Chang Kwon
Gwan Sun Lee
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Hanmi Science Co Ltd
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Publication date
Application filed by Hanmi Science Co Ltd filed Critical Hanmi Science Co Ltd
Publication of HUE030373T2 publication Critical patent/HUE030373T2/hu

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/1072—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups
    • C07K1/1077—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups by covalent attachment of residues other than amino acids or peptide residues, e.g. sugars, polyols, fatty acids
    • 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
    • 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
    • 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
    • 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
    • C07K14/62—Insulins

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Endocrinology (AREA)
  • Toxicology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Analytical Chemistry (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (4)

  1. Ss^ladatísi jgéayjpöíök í. Eljárás lselyspecífífeis, iizlologiásari aktív pölipöpiídtí®sjagátsm előállítására, amely magába« foglaíjiv a kővetkező lépésékek i, fiziológiása« aktív polipeptid kezelése mm. peptídíl pöíaserret olyan ívakelóközegiien, amely táftalmag adóit mennyiségit alkoholt és adóit pH^a vas,;exálial lehetővé teszi a mm psptidíi polimer kötődéséi a MoiögíásiKíi aktív poíipepiíd «élise igéhez és ti) a fiziológiásán akiív ipôilpeptN^tMjugâtum izolálása, és tisztítása az i) lépés reakcíökeverékéböl •.•ioncserélő kromatográtíávál. alkohol alkalmazásával, áhol a fiziológiásán aktív poíipepiid exenciin, inzulin, oxmiOmodiiHn, öiiM, GLP-2, grelin, calciíonln vagy ezek valamely siÉí1^éká,iii^lÍp!Ís.|%}#í· a (t>(IV) képíet kOzöi váít kiválasztva:
    í képlet Ül képlet
    ÍV képiét : ahol;M äikobol etanoí vagy izopropanol, áltól az glköhólgi:: fogatára VGosikoztätya 25¾ íérfögat% mennyiségben van jelen a téakcíóközegiien, ahol az í) lépésben alkalmazott pH /·· 10, amennyiben a fiziológiásán aktív polipeptid exendin, o^lntomöéuiín, GOM, GLP<3 vagyezék valámely s^sipa^kn, és áltól a» i) ÍépÉsbeó alkalmazott pH 4^gantennyiben a fiziológiásán aktív políppfid humán inzulin vagy származéka.
  2. 2. igénypont szerinti eljárás, ahol a neobpeptidii polimer poíléti ián-giikoí.
  3. 3. Az l. tgtksypmp s^nöti e|ÉgSy aboi atotÄldkfe vonatkoztatva az alkohol a reaketéközegben 35-60 térfogat% mennyiségben van jelen.
  4. 4. kz L igénypont szerinti eljárás, ahol a helyspecifikus, fiziológiásán aktív poíipesttid-konlugátum éxertdln-4 konjugáttmt, amelyben PPG kapcsolódik Lys27-hez> c&amp;lcitönin-konjugáium, amelyben PEG kapcsa* lódík az N'terminálishoz, oximoirtotíuiin-konjngátutn, amelyben PEG kapcsolódik lys27-hez vagy Ly§|{Mio&amp; humáninzuiio-konjxtgátum. amelyben PEG kapcsolódik az A láncba« a Gly I N-terminálisához vagy .S-'lMálté« ban i..ys20-hoz, vagy GLP-l vagy Gt.P-2 koniugáHint, amelyben PEG kapcsolódik Lys.?.?-hez vagy Lys?0-hoz
HUE10753706A 2009-03-20 2010-03-18 Eljárás fiziológiásan aktív polipeptid helyspecifikus konjugátumának elõállítására HUE030373T2 (hu)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
KR20090023953 2009-03-20

Publications (1)

Publication Number Publication Date
HUE030373T2 true HUE030373T2 (hu) 2017-05-29

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HUE10753706A HUE030373T2 (hu) 2009-03-20 2010-03-18 Eljárás fiziológiásan aktív polipeptid helyspecifikus konjugátumának elõállítására

Country Status (25)

Country Link
US (1) US8895281B2 (hu)
EP (1) EP2408800B1 (hu)
JP (2) JP5759976B2 (hu)
KR (1) KR101164453B1 (hu)
CN (1) CN102369209B (hu)
AR (1) AR075913A1 (hu)
AU (1) AU2010225523B2 (hu)
BR (1) BRPI1013626B8 (hu)
CA (1) CA2755395C (hu)
DK (1) DK2408800T3 (hu)
ES (1) ES2587397T3 (hu)
HK (1) HK1163120A1 (hu)
HR (1) HRP20161055T1 (hu)
HU (1) HUE030373T2 (hu)
IL (1) IL215165A (hu)
MX (1) MX2011009803A (hu)
MY (1) MY150536A (hu)
NZ (1) NZ595848A (hu)
PL (1) PL2408800T3 (hu)
PT (1) PT2408800T (hu)
RU (1) RU2495881C2 (hu)
SG (1) SG174320A1 (hu)
TW (1) TWI472342B (hu)
WO (1) WO2010107256A2 (hu)
ZA (1) ZA201107658B (hu)

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KR101895047B1 (ko) * 2011-12-30 2018-09-06 한미사이언스 주식회사 면역글로불린 단편을 이용한 위치 특이적 글루카곤 유사 펩타이드-2 약물 결합체
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KR101968344B1 (ko) * 2012-07-25 2019-04-12 한미약품 주식회사 옥신토모듈린 유도체를 포함하는 고지혈증 치료용 조성물
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AR096891A1 (es) 2013-07-12 2016-02-03 Hanmi Pharm Ind Co Ltd Conjugado de monómero polipéptido biológicamente activo y conjugado de fragmento fc de inmunoglobulina, que muestra aclaramiento mediado por receptor reducido, y el método para la preparación del mismo
CN103804483A (zh) * 2014-03-13 2014-05-21 中国人民解放军第四军医大学 Orexin-A聚乙二醇化修饰物及其制备方法
KR20150140177A (ko) * 2014-06-05 2015-12-15 한미약품 주식회사 단백질 및 펩타이드의 면역원성을 감소시키는 방법
TWI802396B (zh) 2014-09-16 2023-05-11 南韓商韓美藥品股份有限公司 長效glp-1/高血糖素受體雙促效劑治療非酒精性脂肝疾病之用途
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RU2011142332A (ru) 2013-04-27
HK1163120A1 (en) 2012-09-07
TW201036640A (en) 2010-10-16
CA2755395C (en) 2015-02-24
CN102369209A (zh) 2012-03-07
JP2012520873A (ja) 2012-09-10
CN102369209B (zh) 2015-06-10
WO2010107256A3 (en) 2011-03-17
CA2755395A1 (en) 2010-09-23
BRPI1013626A2 (pt) 2016-04-19
PT2408800T (pt) 2016-08-23
KR20100105494A (ko) 2010-09-29
US20120003712A1 (en) 2012-01-05
JP5759976B2 (ja) 2015-08-05
BRPI1013626B1 (pt) 2021-05-11
AR075913A1 (es) 2011-05-04
SG174320A1 (en) 2011-10-28
TWI472342B (zh) 2015-02-11
ES2587397T3 (es) 2016-10-24
MX2011009803A (es) 2011-09-30
ZA201107658B (en) 2012-12-27
KR101164453B1 (ko) 2012-07-11
IL215165A (en) 2016-11-30
EP2408800A2 (en) 2012-01-25
JP2015127330A (ja) 2015-07-09
PL2408800T3 (pl) 2016-11-30
BRPI1013626B8 (pt) 2021-05-25
RU2495881C2 (ru) 2013-10-20
AU2010225523B2 (en) 2012-05-24
NZ595848A (en) 2014-04-30
AU2010225523A1 (en) 2011-11-10
EP2408800B1 (en) 2016-05-25
EP2408800A4 (en) 2012-12-05
US8895281B2 (en) 2014-11-25
WO2010107256A2 (en) 2010-09-23
DK2408800T3 (en) 2016-08-29
HRP20161055T1 (hr) 2016-11-04
IL215165A0 (en) 2011-12-29
MY150536A (en) 2014-01-30

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