WO2005027828A3 - 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
WO2005027828A3
WO2005027828A3 PCT/US2004/026485 US2004026485W WO2005027828A3 WO 2005027828 A3 WO2005027828 A3 WO 2005027828A3 US 2004026485 W US2004026485 W US 2004026485W WO 2005027828 A3 WO2005027828 A3 WO 2005027828A3
Authority
WO
WIPO (PCT)
Prior art keywords
conjugates
formulation
preparation
methods
biologically active
Prior art date
Application number
PCT/US2004/026485
Other languages
French (fr)
Other versions
WO2005027828A2 (en
Inventor
Hans-Jurgen Gutke
Christian Flohr
Albert Beck
Simona Margutti
Mary Eggers
Jan-Hinrich Guse
Moussa Khobzaoui
Michael Burnet
Original Assignee
Synovo Gmbh
Hans-Jurgen Gutke
Christian Flohr
Albert Beck
Simona Margutti
Mary Eggers
Jan-Hinrich Guse
Moussa Khobzaoui
Michael Burnet
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 Synovo Gmbh, Hans-Jurgen Gutke, Christian Flohr, Albert Beck, Simona Margutti, Mary Eggers, Jan-Hinrich Guse, Moussa Khobzaoui, Michael Burnet filed Critical Synovo Gmbh
Publication of WO2005027828A2 publication Critical patent/WO2005027828A2/en
Publication of WO2005027828A3 publication Critical patent/WO2005027828A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • 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
    • 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
    • A61K47/545—Heterocyclic compounds
    • 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
    • A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins

Abstract

This invention features a compound of the following formula: T-(-L-C)m, T is a transportophore, L is a bond or a linker having a molecular weight up to 240 dalton, C is a non-antibiotic therapeutic agent, and m is 1, 2, 3, 4, 5, 6, 7, or 8, in which the transportophore has an immune selectivity ratio of at least 2, the transportophore is covalently bonded to the non-antibiotic therapeutic agent via the bond or the linker, and the compound has an immune selectivity ratio of at least 2.
PCT/US2004/026485 2003-08-20 2004-08-16 Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof WO2005027828A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US10/644,600 2003-08-20
US10/644,600 US20040186063A1 (en) 2002-02-15 2003-08-20 Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof

Publications (2)

Publication Number Publication Date
WO2005027828A2 WO2005027828A2 (en) 2005-03-31
WO2005027828A3 true WO2005027828A3 (en) 2005-07-28

Family

ID=34375730

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2004/026485 WO2005027828A2 (en) 2003-08-20 2004-08-16 Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof

Country Status (2)

Country Link
US (1) US20040186063A1 (en)
WO (1) WO2005027828A2 (en)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004005313A2 (en) * 2002-07-08 2004-01-15 Pliva - Istrazivacki Institut D.O.O. Hybrid molecules of macrolides with steroid/non-steroid anti-inflammatory, antineoplastic and antiviral active molecules
AU2003255851B2 (en) * 2002-07-08 2009-07-23 Glaxosmithkline Istrazivacki Centar Zagreb D.O.O. New compounds, compositions and methods for treatment of inflammatory diseases and conditions
NZ537716A (en) * 2002-07-08 2007-05-31 Glaxosmithkline Zagreb Novel nonsteroidal anti-inflammatory substances, compositions and methods for their use
HRP20030324A2 (en) * 2003-04-24 2005-02-28 Pliva-Istra�iva�ki institut d.o.o. Compounds of antiinflammatory effect
US20060183696A1 (en) * 2004-08-12 2006-08-17 Pliva-Istrazivacki Institut D.O.O. Use of immune cell specific conjugates for treatment of inflammatory diseases of gastrointestinal tract
US20060035845A1 (en) * 2004-08-12 2006-02-16 Pliva-Istrazivacki Institut D.O.O. Use of immune cell specific conjugates for treatment of inflammatory diseases of the gastrointestinal tract
US7767797B1 (en) 2004-09-30 2010-08-03 Synovo Gmbh Macrocyclic compounds and methods of use thereof
AU2006274197A1 (en) * 2005-07-26 2007-02-01 Merckle Gmbh Macrolide conjugates of pyrrolizine and indolizine compounds as inhibitors of 5-lipooxygenase and cyclooxygenase
EP2625185A4 (en) * 2010-10-10 2014-03-26 Synovo Gmbh Anti-inflammatory macrolides
US9289507B2 (en) 2012-05-17 2016-03-22 Extend Biosciences, Inc. Carriers for improved drug delivery
US9789197B2 (en) 2014-10-22 2017-10-17 Extend Biosciences, Inc. RNAi vitamin D conjugates
WO2016065052A1 (en) 2014-10-22 2016-04-28 Extend Biosciences, Inc. Insulin vitamin d conjugates
WO2016065042A1 (en) 2014-10-22 2016-04-28 Extend Biosciences, Inc. Therapeutic vitamin d conjugates

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5466681A (en) * 1990-02-23 1995-11-14 Microcarb, Inc. Receptor conjugates for targeting penicillin antibiotics to bacteria
US5928868A (en) * 1996-04-26 1999-07-27 Massachusetts Institute Of Technology Three hybrid screening assay

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3417077A (en) * 1966-05-16 1968-12-17 Lilly Co Eli Erythromycin derivative and process for the preparation thereof
US4375414A (en) * 1971-05-20 1983-03-01 Meir Strahilevitz Immunological methods for removing species from the blood circulatory system and devices therefor
US3884903A (en) * 1973-06-21 1975-05-20 Abbott Lab 4{41 -Deoxy-4{41 -oxoerythromycin B derivatives
YU43116B (en) * 1979-04-02 1989-04-30 Pliva Pharm & Chem Works Process for preparing 11-aza-4-o-cladinosyl-6-o-desosaminyl-15-ethyl-7,13,14-trihydroxy-3,5,7,9,12,14-hexamethyl-oxacyclopentadecane-2-one(11-aza-10-deox
SI8110592A8 (en) * 1981-03-06 1996-06-30 Pliva Pharm & Chem Works Process for preparing of n-methyl-11-aza-10-deoxo-10-dihydroerythromycine a and derivatives thereof
US4474768A (en) * 1982-07-19 1984-10-02 Pfizer Inc. N-Methyl 11-aza-10-deoxo-10-dihydro-erytromycin A, intermediates therefor
JPH0720857B2 (en) * 1988-08-11 1995-03-08 テルモ株式会社 Liposome and its manufacturing method
US5405975A (en) * 1993-03-29 1995-04-11 Molecular Probes, Inc. Fluorescent ion-selective diaryldiaza crown ether conjugates
US5486536A (en) * 1994-08-15 1996-01-23 The Regents Of The University Of Michigan Sulfatides as anti-inflammatory compounds
US5750493A (en) * 1995-08-30 1998-05-12 Raymond F. Schinazi Method to improve the biological and antiviral activity of protease inhibitors
US5827533A (en) * 1997-02-06 1998-10-27 Duke University Liposomes containing active agents aggregated with lipid surfactants
EP0967794B1 (en) * 1998-06-26 2004-06-09 Agilent Technologies, Inc. (a Delaware corporation) Photodiode array
US6043227A (en) * 1998-08-19 2000-03-28 Pfizer Inc. C11 carbamates of macrolide antibacterials
WO2001051061A1 (en) * 2000-01-14 2001-07-19 Intrabiotics Pharmaceuticals, Inc. Derivatives of polyene macrolides and preparation and use thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5466681A (en) * 1990-02-23 1995-11-14 Microcarb, Inc. Receptor conjugates for targeting penicillin antibiotics to bacteria
US5928868A (en) * 1996-04-26 1999-07-27 Massachusetts Institute Of Technology Three hybrid screening assay

Also Published As

Publication number Publication date
US20040186063A1 (en) 2004-09-23
WO2005027828A2 (en) 2005-03-31

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