US20040005641A1 - 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
US20040005641A1
US20040005641A1 US10/367,624 US36762403A US2004005641A1 US 20040005641 A1 US20040005641 A1 US 20040005641A1 US 36762403 A US36762403 A US 36762403A US 2004005641 A1 US2004005641 A1 US 2004005641A1
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Prior art keywords
compound
therapeutic agent
mmol
alkyl
cell
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Abandoned
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US10/367,624
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English (en)
Inventor
Michael Burnet
Jan-Hinrich Guse
Gene Kim
Hans-Jurgen Gutke
Albert Beck
Georgia Tsotsou
Irina Droste-Borel
Laurence Barker
Michael Wolff
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Priority to US10/367,624 priority Critical patent/US20040005641A1/en
Assigned to SYMPORE GMBH reassignment SYMPORE GMBH ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: BARKER, LAURENCE, BECK, ALBERT, BURNET, MICHAEL, DROSTE-BOREL, IRINA, GUSE, JAN-HINRICH, GUTKE, HANS-JURGEN, KIM, GENE, TSOTSOU, GEORGIA, WOLFF, MICHAEL
Publication of US20040005641A1 publication Critical patent/US20040005641A1/en
Assigned to SYNOVO GMBH reassignment SYNOVO GMBH ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: SYMPORE GMBH
Assigned to MERCKLE GMBH reassignment MERCKLE GMBH ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: SYNOVO GMBH
Assigned to MERCKLE GMBH reassignment MERCKLE GMBH CORRECTED COVER SHEET TO CORRECT PROPERTY NUMBERS, PREVIOUSLY RECORDED AT REEL/FRAME 017269/0914 (ASSIGNMENT OF ASSIGNOR'S INTEREST) Assignors: SYNOVO GMBH
Assigned to BURNET, DR. MICHAEL reassignment BURNET, DR. MICHAEL ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: MERCKLE GMBH
Priority to US11/895,295 priority patent/US20080145343A1/en
Abandoned legal-status Critical Current

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    • 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)
  • Cell Biology (AREA)
  • Urology & Nephrology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Biotechnology (AREA)
  • Pathology (AREA)
  • Microbiology (AREA)
  • Nanotechnology (AREA)
  • Biochemistry (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Food Science & Technology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Toxicology (AREA)
  • General Physics & Mathematics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Rheumatology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biophysics (AREA)
  • Endocrinology (AREA)
  • Ecology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Medical Informatics (AREA)
  • Genetics & Genomics (AREA)
  • Gastroenterology & Hepatology (AREA)
US10/367,624 2002-02-15 2003-02-14 Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof Abandoned US20040005641A1 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
US10/367,624 US20040005641A1 (en) 2002-02-15 2003-02-14 Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
US11/895,295 US20080145343A1 (en) 2002-02-15 2007-08-23 Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US35758902P 2002-02-15 2002-02-15
US10/367,624 US20040005641A1 (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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US11/895,295 Continuation US20080145343A1 (en) 2002-02-15 2007-08-23 Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof

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US20040005641A1 true US20040005641A1 (en) 2004-01-08

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US10/367,624 Abandoned US20040005641A1 (en) 2002-02-15 2003-02-14 Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
US10/504,786 Abandoned US20060099660A1 (en) 2002-02-15 2003-02-14 Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
US11/895,295 Abandoned US20080145343A1 (en) 2002-02-15 2007-08-23 Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
US12/157,937 Expired - Fee Related US8357506B2 (en) 2002-02-15 2008-06-12 Method of identifying improved conjugates of biologically active compounds

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US10/504,786 Abandoned US20060099660A1 (en) 2002-02-15 2003-02-14 Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
US11/895,295 Abandoned US20080145343A1 (en) 2002-02-15 2007-08-23 Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
US12/157,937 Expired - Fee Related US8357506B2 (en) 2002-02-15 2008-06-12 Method of identifying improved conjugates of biologically active compounds

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US (4) US20040005641A1 (US20040005641A1-20040108-C00016.png)
EP (1) EP1483579A4 (US20040005641A1-20040108-C00016.png)
AU (1) AU2003215245A1 (US20040005641A1-20040108-C00016.png)
HR (1) HRP20040849A2 (US20040005641A1-20040108-C00016.png)
WO (1) WO2003070173A2 (US20040005641A1-20040108-C00016.png)

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US20040014685A1 (en) * 2002-07-08 2004-01-22 Pliva Pharmaceutical Industry, Incorporated Compounds, compositions and methods for treatment of inflammatory diseases and conditions
US20040077612A1 (en) * 2002-07-08 2004-04-22 Pliva Dd Novel compounds, compositions as carriers for steroid/nonsteroid anti-inflammatory; antienoplastic and antiviral active molecules
US20040097434A1 (en) * 2002-07-08 2004-05-20 Pliva Pharmaceutical Industry, Incorporated Novel nonsteroidal anti-inflammatory substances, compositions and methods for their use
US20050080003A1 (en) * 2003-04-24 2005-04-14 Mladen Mercep Compounds with anti-inflammatory activity
US20050129619A1 (en) * 2003-12-10 2005-06-16 Board Of Regents, The University Of Texas System N2S2 chelate-targeting ligand conjugates
US20090093014A1 (en) * 2002-02-15 2009-04-09 Dr. Michael Burnet Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
US20090221697A1 (en) * 2005-07-26 2009-09-03 Merckle Gmbh Macrolide conjugates of pyrrolizine and indolizine compounds as inhibitors of 5-lipooxygenase and cyclooxygenase

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EP1482957A4 (en) * 2002-02-15 2006-07-19 Merckle Gmbh ANTIBIOTIC CONJUGATES
WO2003070174A2 (en) * 2002-02-15 2003-08-28 Sympore Gmbh Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
TW200420573A (en) 2002-09-26 2004-10-16 Rib X Pharmaceuticals Inc Bifunctional heterocyclic compounds and methods of making and using same
PL1635835T3 (pl) * 2003-06-13 2010-06-30 Novartis Ag Pochodne 2-aminopirymidyny jako inhibitory kinazy RAF
CN102816194A (zh) 2004-02-27 2012-12-12 瑞伯-X医药品有限公司 大环化合物以及其制作和使用方法
BRPI0514254A (pt) * 2004-08-12 2008-06-03 Glaxosmithkline Zagreb uso de conjugados célula-especìficos para o tratamento de doenças inflamatórias do trato gastrintestinal
US7767797B1 (en) 2004-09-30 2010-08-03 Synovo Gmbh Macrocyclic compounds and methods of use thereof
GB2427360A (en) 2005-06-22 2006-12-27 Complex Biosystems Gmbh Aliphatic prodrug linker
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
CN101619085B (zh) * 2009-08-11 2015-04-22 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
US9895449B2 (en) 2010-05-25 2018-02-20 Syndevrx, Inc. Polymer-conjugated MetAP2 inhibitors, and therapeutic methods of use thereof
US9320805B2 (en) 2010-05-25 2016-04-26 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
CN105431426A (zh) 2013-04-10 2016-03-23 新德发制药有限公司 Metap2抑制剂和治疗肥胖症的方法
CN104710488B (zh) * 2015-03-11 2017-09-15 江南大学 一种泰拉霉素的半抗原和完全抗原的合成方法
US9969722B2 (en) 2015-12-10 2018-05-15 Syndevrx, Inc. Fumagillol derivatives and polymorphs thereof
CA3008960A1 (en) 2016-01-11 2017-07-20 Syndevrx, Inc. Treatment for tumors driven by metabolic dysfunction
CA3117666A1 (en) 2018-10-26 2020-04-30 Syndevrx, Inc. Biomarkers of metap2 inhibitors and applications thereof
CN114025759A (zh) 2019-04-18 2022-02-08 阿祖拉眼科有限公司 用于治疗眼病的化合物和方法
JP2023546453A (ja) * 2020-10-21 2023-11-02 アズーラ オフサルミックス エルティーディー． 眼障害を処置するための化合物および方法
US11459351B1 (en) * 2021-04-05 2022-10-04 Azura Ophthalmics Ltd. Compounds and methods for the treatment of ocular disorders

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US4834973A (en) * 1971-05-20 1989-05-30 Meir Strahilevitz Immunological methods for treating mammals
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US8357506B2 (en) 2002-02-15 2013-01-22 Michael Burnet Method of identifying improved conjugates of biologically active compounds
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