CO5580794A2 - CHEMICALLY MODIFIED HUMAN GROWTH HORMONE CONJUGATES - Google Patents

CHEMICALLY MODIFIED HUMAN GROWTH HORMONE CONJUGATES

Info

Publication number
CO5580794A2
CO5580794A2 CO04046633A CO04046633A CO5580794A2 CO 5580794 A2 CO5580794 A2 CO 5580794A2 CO 04046633 A CO04046633 A CO 04046633A CO 04046633 A CO04046633 A CO 04046633A CO 5580794 A2 CO5580794 A2 CO 5580794A2
Authority
CO
Colombia
Prior art keywords
conjugate
poly
amino acid
ethylene glycol
molecule
Prior art date
Application number
CO04046633A
Other languages
Spanish (es)
Inventor
F Finn Roy
Liao Wei
R Siegel Ned
Original Assignee
Pharmacia Corp
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 Pharmacia Corp filed Critical Pharmacia Corp
Publication of CO5580794A2 publication Critical patent/CO5580794A2/en

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
    • C07K14/61—Growth hormone [GH], i.e. somatotropin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/27—Growth hormone [GH], i.e. somatotropin
    • 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
    • A61K47/56—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH

Landscapes

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

Abstract

1.- Un conjugado que comprende al menos una molécula polimérica hidrosoluble unida covalentemente a al menos un resto aminoacídico de un polipéptido de hormona de crecimiento humana (hGH) biológicamente activo o una variante agonista de la misma.2.- El conjugado de la reivindicación 1, en el que dicho polipéptido de hGH comprende la secuencia de aminoácidos de la SEC ID N°:1.3.- El conjugado de la reivindicación 1 ó 2, en el que dicho polímero es una molécula de poli(óxido de etileno).4.- El conjugado de la reivindicación 3, en el que dicha molécula de poli(óxido de etileno) es una molécula de poli(etilenglicol).5.- El conjugado de la reivindicación 4, en el que el poli(etilenglicol) está unido a un resto aminoacídico que tiene uno o más grupos amino libres, uno o más grupos carboxilo libres o uno o más grupos sulfhidrilo libres.6.- El conjugado de la reivindicación 5, formado usando un poli(etilenglicol) activado.7.- El conjugado de la reivindicación 6, en el que dicho poli(etilenglicol) activado comprende un grupo funcional.8.- El conjugado de la reivindicación 7, en el que dicha unión se realiza en un aminoácido que tiene un grupo amino libre.9.- El conjugado de la reivindicación 8, en el que dicho grupo funcional se selecciona entre el grupo compuesto por: carbonatos, carbonil imidazol, ésteres activos de ácidos carboxílicos azlactonas, imidationas cíclicas, isocianatos o isotiocianatos, imidatos y aldehídos.10.- El conjugado de la reivindicación 9, en el que dicho grupo funcional es un carbonato o carbonil imidazol.1. A conjugate comprising at least one water-soluble polymer molecule covalently linked to at least one amino acid residue of a biologically active human growth hormone (hGH) polypeptide or an agonist variant thereof. 2. The conjugate of the claim 1, wherein said hGH polypeptide comprises the amino acid sequence of SEQ ID NO: 1.3.- The conjugate of claim 1 or 2, wherein said polymer is a poly (ethylene oxide) molecule .4 .- The conjugate of claim 3, wherein said poly (ethylene oxide) molecule is a poly (ethylene glycol) molecule .5.- The conjugate of claim 4, wherein the poly (ethylene glycol) is attached to an amino acid residue having one or more free amino groups, one or more free carboxyl groups or one or more free sulfhydryl groups. 6. The conjugate of claim 5, formed using an activated poly (ethylene glycol). conjugate of claim 6, in the that said activated poly (ethylene glycol) comprises a functional group.8.- The conjugate of claim 7, wherein said binding is performed on an amino acid having a free amino group.9.- The conjugate of claim 8, in wherein said functional group is selected from the group consisting of: carbonates, carbonyl imidazole, active esters of azlactone carboxylic acids, cyclic imidations, isocyanates or isothiocyanates, imidates and aldehydes. 10. The conjugate of claim 9, wherein said Functional group is a carbonate or carbonyl imidazole.

CO04046633A 2001-11-20 2004-05-20 CHEMICALLY MODIFIED HUMAN GROWTH HORMONE CONJUGATES CO5580794A2 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US33190701P 2001-11-20 2001-11-20

Publications (1)

Publication Number Publication Date
CO5580794A2 true CO5580794A2 (en) 2005-11-30

Family

ID=23295870

Family Applications (1)

Application Number Title Priority Date Filing Date
CO04046633A CO5580794A2 (en) 2001-11-20 2004-05-20 CHEMICALLY MODIFIED HUMAN GROWTH HORMONE CONJUGATES

Country Status (25)

Country Link
EP (1) EP1453859A2 (en)
JP (2) JP2005525302A (en)
KR (2) KR20070072924A (en)
CN (1) CN1608079A (en)
AP (1) AP2004003050A0 (en)
AU (1) AU2002356990A1 (en)
BR (1) BR0214451A (en)
CA (1) CA2467731A1 (en)
CO (1) CO5580794A2 (en)
EA (2) EA008505B1 (en)
EC (1) ECSP045114A (en)
GE (1) GEP20063860B (en)
HR (1) HRP20040448A2 (en)
HU (1) HUP0500997A2 (en)
IL (1) IL162031A0 (en)
IS (1) IS7268A (en)
MA (1) MA27544A1 (en)
MX (1) MXPA04004809A (en)
NO (1) NO20042182L (en)
OA (1) OA13063A (en)
PL (1) PL374354A1 (en)
RS (1) RS53104A (en)
TN (1) TNSN04090A1 (en)
WO (1) WO2003044056A2 (en)
ZA (1) ZA200403907B (en)

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Also Published As

Publication number Publication date
CA2467731A1 (en) 2003-05-30
ZA200403907B (en) 2007-12-27
EA200700431A1 (en) 2008-02-28
HUP0500997A2 (en) 2007-11-28
OA13063A (en) 2006-11-10
AU2002356990A1 (en) 2003-06-10
ECSP045114A (en) 2004-07-23
EA200400565A1 (en) 2005-06-30
HRP20040448A2 (en) 2006-02-28
KR20050044858A (en) 2005-05-13
EA008505B1 (en) 2007-06-29
NO20042182L (en) 2004-08-11
PL374354A1 (en) 2005-10-17
WO2003044056A2 (en) 2003-05-30
MXPA04004809A (en) 2004-08-11
MA27544A1 (en) 2005-10-03
RS53104A (en) 2006-10-27
BR0214451A (en) 2006-05-30
TNSN04090A1 (en) 2006-06-01
CN1608079A (en) 2005-04-20
EP1453859A2 (en) 2004-09-08
WO2003044056A3 (en) 2003-08-21
GEP20063860B (en) 2006-06-26
KR20070072924A (en) 2007-07-06
JP2005525302A (en) 2005-08-25
JP2006321808A (en) 2006-11-30
AP2004003050A0 (en) 2004-06-30
IS7268A (en) 2004-05-17
IL162031A0 (en) 2005-11-20

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