WO2003070173A2 - Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof - Google Patents

Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof Download PDF

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Publication number
WO2003070173A2
WO2003070173A2 PCT/US2003/004596 US0304596W WO03070173A2 WO 2003070173 A2 WO2003070173 A2 WO 2003070173A2 US 0304596 W US0304596 W US 0304596W WO 03070173 A2 WO03070173 A2 WO 03070173A2
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WO
WIPO (PCT)
Prior art keywords
compound
therapeutic agent
mmol
alkyl
cell
Prior art date
Application number
PCT/US2003/004596
Other languages
English (en)
French (fr)
Other versions
WO2003070173A3 (en
Inventor
Michael Burnet
Jan-Hinrich Guse
Gene Kim
Albert Beck
Georgia Tsotsou
Irina Droste-Borel
Laurence Barker
Michael Wolff
Hans-Jurgen Gutke
Original Assignee
Sympore Gmbh
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 Sympore Gmbh filed Critical Sympore Gmbh
Priority to US10/504,786 priority Critical patent/US20060099660A1/en
Priority to EP03711061A priority patent/EP1483579A4/en
Priority to AU2003215245A priority patent/AU2003215245A1/en
Publication of WO2003070173A2 publication Critical patent/WO2003070173A2/en
Publication of WO2003070173A3 publication Critical patent/WO2003070173A3/en
Priority to HR20040849A priority patent/HRP20040849A2/xx
Priority to US12/157,937 priority patent/US8357506B2/en

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Classifications

    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • 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
    • A61K47/54—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 compound
    • A61K47/55—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 compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • A61K47/552—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 compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds one of the codrug's components being an antibiotic
    • 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
    • A61K47/54—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 compound
    • A61K47/555—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 compound pre-targeting systems involving an organic compound, other than a peptide, protein or antibody, for targeting specific cells
    • A61K47/556—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 compound pre-targeting systems involving an organic compound, other than a peptide, protein or antibody, for targeting specific cells enzyme catalyzed therapeutic agent [ECTA]
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/66—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 a protein, peptide or polyamino acid the modifying agent being a pre-targeting system involving a peptide or protein for targeting specific cells
    • A61K47/67—Enzyme prodrug therapy, e.g. gene directed enzyme drug therapy [GDEPT] or VDEPT
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/0004—Screening or testing of compounds for diagnosis of disorders, assessment of conditions, e.g. renal clearance, gastric emptying, testing for diabetes, allergy, rheuma, pancreas functions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/5044—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics involving specific cell types
    • G01N33/5047—Cells of the immune system
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5094—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for blood cell populations

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Cell Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Biotechnology (AREA)
  • Pathology (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Nanotechnology (AREA)
  • Toxicology (AREA)
  • Food Science & Technology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • General Engineering & Computer Science (AREA)
  • Ecology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Endocrinology (AREA)
  • Medical Informatics (AREA)
  • Crystallography & Structural Chemistry (AREA)
PCT/US2003/004596 2002-02-15 2003-02-14 Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof WO2003070173A2 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
US10/504,786 US20060099660A1 (en) 2002-02-15 2003-02-14 Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
EP03711061A EP1483579A4 (en) 2002-02-15 2003-02-14 CONJUGATES OF BIOLOGICALLY ACTIVE COMPOUNDS, METHODS FOR THE PREPARATION AND USE OF CONJUGATES, FORMULATION AND PHARMACEUTICAL APPLICATIONS OBTAINED FROM SUCH CONJUGATES
AU2003215245A AU2003215245A1 (en) 2002-02-15 2003-02-14 Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
HR20040849A HRP20040849A2 (en) 2002-02-15 2004-09-15 Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
US12/157,937 US8357506B2 (en) 2002-02-15 2008-06-12 Method of identifying improved conjugates of biologically active compounds

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US35758902P 2002-02-15 2002-02-15
US60/357,589 2002-02-15

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US10504786 A-371-Of-International 2003-02-14
US12/157,937 Continuation US8357506B2 (en) 2002-02-15 2008-06-12 Method of identifying improved conjugates of biologically active compounds

Publications (2)

Publication Number Publication Date
WO2003070173A2 true WO2003070173A2 (en) 2003-08-28
WO2003070173A3 WO2003070173A3 (en) 2003-12-04

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PCT/US2003/004596 WO2003070173A2 (en) 2002-02-15 2003-02-14 Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof

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US (4) US20060099660A1 (US20040005641A1-20040108-C00030.png)
EP (1) EP1483579A4 (US20040005641A1-20040108-C00030.png)
AU (1) AU2003215245A1 (US20040005641A1-20040108-C00030.png)
HR (1) HRP20040849A2 (US20040005641A1-20040108-C00030.png)
WO (1) WO2003070173A2 (US20040005641A1-20040108-C00030.png)

Cited By (14)

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EP1482957A1 (en) * 2002-02-15 2004-12-08 Sympore GmbH Antibiotic conjugates
EP1483277A2 (en) * 2002-02-15 2004-12-08 Sympore GmbH Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
WO2004110452A1 (en) * 2003-06-13 2004-12-23 Novartis Ag 2-aminopyrimidine derivatives as raf kinase inhibitors
WO2006018698A2 (en) * 2004-08-12 2006-02-23 Glaxosmithkline Istrazivacki Centar Zagreb D.O.O. Use of cell-specific conjugates for treatment of inflammatory diseases of the gastrointestinal tract
US7091187B2 (en) 2002-07-08 2006-08-15 Pliva-Istrazivacki Institut D.O.O. Compounds, compositions and methods for treatment of inflammatory diseases and conditions
US7091196B2 (en) 2002-09-26 2006-08-15 Rib-X Pharmaceuticals, Inc. Bifunctional heterocyclic compounds and methods of making and using same
US7109176B2 (en) 2002-07-08 2006-09-19 Pliva-Istrazivacki Institut D.O.O. Nonsteroidal anti-inflammatory substances, compositions and methods for their use
WO2006136586A2 (en) * 2005-06-22 2006-12-28 Complex Biosystems Gmbh N, n-bis- (2-hydroxyethyl) glycine amide as linker in polymer conjugated prodrugs
US7157433B2 (en) 2002-07-08 2007-01-02 Glaxosmithkline Istrazivacki Centar Zagreb Compounds, compositions as carriers for steroid/nonsteroid anti-inflammatory; antienoplastic and antiviral active molecules
WO2007093840A2 (en) * 2006-02-15 2007-08-23 Glaxosmithkline Istrazivacki Centar Zagreb D.O.O. Use of cell-specific conjugates for treatment of inflammatory diseases of the gastrointestinal tract
CN101619085A (zh) * 2009-08-11 2010-01-06 沈阳药科大学 红霉素衍生物及其作为肿瘤细胞增殖抑制剂的用途
US7767797B1 (en) 2004-09-30 2010-08-03 Synovo Gmbh Macrocyclic compounds and methods of use thereof
US8202843B2 (en) 2004-02-27 2012-06-19 Rib-X Pharmaceuticals, Inc. Macrocyclic compounds and methods of making and using the same
CN104710488A (zh) * 2015-03-11 2015-06-17 江南大学 一种泰拉霉素的半抗原和完全抗原的合成方法

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EP1483579A4 (en) * 2002-02-15 2006-07-12 Merckle Gmbh CONJUGATES OF BIOLOGICALLY ACTIVE COMPOUNDS, METHODS FOR THE PREPARATION AND USE OF CONJUGATES, FORMULATION AND PHARMACEUTICAL APPLICATIONS OBTAINED FROM SUCH CONJUGATES
HRP20030324A2 (en) * 2003-04-24 2005-02-28 Pliva-Istra�iva�ki institut d.o.o. Compounds of antiinflammatory effect
US9050378B2 (en) * 2003-12-10 2015-06-09 Board Of Regents, The University Of Texas System N2S2 chelate-targeting ligand conjugates
WO2007012464A1 (en) * 2005-07-26 2007-02-01 Merckle Gmbh Macrolide conjugates of pyrrolizine and indolizine compounds as inhibitors of 5-lipooxygenase and cyclooxygenase
US9895449B2 (en) 2010-05-25 2018-02-20 Syndevrx, Inc. Polymer-conjugated MetAP2 inhibitors, and therapeutic methods of use thereof
WO2011150022A2 (en) 2010-05-25 2011-12-01 Syndevrx, Inc. Polymer-conjugated metap2 inhibitors, and therapeutic methods of use thereof
US20130137831A1 (en) * 2010-05-25 2013-05-30 John S. Petersen Optimized drug conjugates
DK2984085T3 (da) 2013-04-10 2019-10-21 Syndevrx Inc Modificerede eller polymerkonjugerede fumagillol metap2-hæmmere til anvendelse i behandling af fedme
KR20180093995A (ko) 2015-12-10 2018-08-22 신데브알엑스, 인크. 푸마길롤 유도체 및 그의 다형체
US10646463B2 (en) 2016-01-11 2020-05-12 Syndevrx, Inc. Treatment for tumors driven by metabolic dysfunction
CN113453721A (zh) 2018-10-26 2021-09-28 辛德弗雷克斯公司 Metap2抑制剂的生物标志物及其应用
KR20220003555A (ko) 2019-04-18 2022-01-10 아주라 오프탈믹스 엘티디 안구 장애의 치료를 위한 화합물 및 방법
WO2022084738A2 (en) * 2020-10-21 2022-04-28 Azura Ophthalmics Ltd. Compounds and methods for the treatment of ocular disorders
US11459351B1 (en) * 2021-04-05 2022-10-04 Azura Ophthalmics Ltd. Compounds and methods for the treatment of ocular disorders

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Cited By (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1483277A2 (en) * 2002-02-15 2004-12-08 Sympore GmbH Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
US7579324B2 (en) 2002-02-15 2009-08-25 C-A-I-R Biosciences Gmbh Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
EP1482957A4 (en) * 2002-02-15 2006-07-19 Merckle Gmbh ANTIBIOTIC CONJUGATES
EP1482957A1 (en) * 2002-02-15 2004-12-08 Sympore GmbH Antibiotic conjugates
EP1483277A4 (en) * 2002-02-15 2007-10-03 Merckle Gmbh CONJUGATES OF BIOLOGICALLY ACTIVE COMPOUNDS, METHODS OF PREPARATION AND USE, AND FORMULATION AND PHARMACEUTICAL APPLICATIONS
US7157433B2 (en) 2002-07-08 2007-01-02 Glaxosmithkline Istrazivacki Centar Zagreb Compounds, compositions as carriers for steroid/nonsteroid anti-inflammatory; antienoplastic and antiviral active molecules
US7091187B2 (en) 2002-07-08 2006-08-15 Pliva-Istrazivacki Institut D.O.O. Compounds, compositions and methods for treatment of inflammatory diseases and conditions
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US20090093014A1 (en) 2009-04-09
US20060099660A1 (en) 2006-05-11
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