WO2004012735A2 - Nouveaux conjugues d'effecteurs, procedes permettant de les produire et utilisation pharmaceutique de ceux-ci - Google Patents

Nouveaux conjugues d'effecteurs, procedes permettant de les produire et utilisation pharmaceutique de ceux-ci Download PDF

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Publication number
WO2004012735A2
WO2004012735A2 PCT/EP2003/008483 EP0308483W WO2004012735A2 WO 2004012735 A2 WO2004012735 A2 WO 2004012735A2 EP 0308483 W EP0308483 W EP 0308483W WO 2004012735 A2 WO2004012735 A2 WO 2004012735A2
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WO
WIPO (PCT)
Prior art keywords
dione
dihydroxy
tetramethyl
methyl
oxacyclohexadec
Prior art date
Application number
PCT/EP2003/008483
Other languages
English (en)
Other versions
WO2004012735A3 (fr
Inventor
Markus Berger
Gerhard Siemeister
Ulrich Klar
Jörg WILLUDA
Andreas Menrad
Klaus Bosslet
Original Assignee
Schering Ag
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
Priority claimed from DE10234975A external-priority patent/DE10234975A1/de
Priority claimed from DE10305098A external-priority patent/DE10305098A1/de
Priority to JP2005506073A priority Critical patent/JP2006505627A/ja
Priority to AU2003253365A priority patent/AU2003253365A1/en
Priority to BR0313043-6A priority patent/BR0313043A/pt
Priority to EP03743752A priority patent/EP1524979A2/fr
Priority to CA002492437A priority patent/CA2492437A1/fr
Priority to IL16603903A priority patent/IL166039A0/xx
Application filed by Schering Ag filed Critical Schering Ag
Priority to YUP-2005/0082A priority patent/RS20050082A/sr
Priority to MXPA05001282A priority patent/MXPA05001282A/es
Priority to NZ537870A priority patent/NZ537870A/en
Priority to EA200500223A priority patent/EA200500223A1/ru
Publication of WO2004012735A2 publication Critical patent/WO2004012735A2/fr
Publication of WO2004012735A3 publication Critical patent/WO2004012735A3/fr
Priority to IS7708A priority patent/IS7708A/is
Priority to NO20051038A priority patent/NO20051038L/no
Priority to HR20050186A priority patent/HRP20050186A2/hr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6807—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug or compound being a sugar, nucleoside, nucleotide, nucleic acid, e.g. RNA antisense
    • A61K47/6809—Antibiotics, e.g. antitumor antibiotics anthracyclins, adriamycin, doxorubicin or daunomycin
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/36—Oxygen or sulfur atoms
    • C07D207/40—2,5-Pyrrolidine-diones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Cell Biology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Biochemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)

Abstract

L'invention concerne des conjugués d'épothilones et des dérivés d'épothilone (en tant qu'effecteurs) avec des biomolécules adéquates (en tant qu'unités de reconnaissance). Le procédé de production consiste à faire réagir les effecteurs avec des lieurs appropriés ; les composés qui sont produits étant conjugués avec les unités de reconnaissance. La présente invention concerne également l'utilisation pharmaceutique de ces conjugués pour traiter des troubles prolifératifs ou associés à l'angiogenèse.
PCT/EP2003/008483 2002-07-31 2003-07-31 Nouveaux conjugues d'effecteurs, procedes permettant de les produire et utilisation pharmaceutique de ceux-ci WO2004012735A2 (fr)

Priority Applications (13)

Application Number Priority Date Filing Date Title
NZ537870A NZ537870A (en) 2002-07-31 2003-07-31 New effector conjugates, process for their production and their pharmaceutical use
EA200500223A EA200500223A1 (ru) 2002-07-31 2003-07-31 Новые конъюгаты - эффекторы, способ их получения и их фармацевтическое применение
YUP-2005/0082A RS20050082A (en) 2002-07-31 2003-07-31 New efector conjugates,process for their production and their pharmaceutical use
BR0313043-6A BR0313043A (pt) 2002-07-31 2003-07-31 Conjugados efetores, processo para sua produção e seu uso farmacêutico
EP03743752A EP1524979A2 (fr) 2002-07-31 2003-07-31 Nouveaux conjugues d'effecteurs, procedes permettant de les produire et utilisation pharmaceutique de ceux-ci
CA002492437A CA2492437A1 (fr) 2002-07-31 2003-07-31 Nouveaux conjugues d'effecteurs, procedes permettant de les produire et utilisation pharmaceutique de ceux-ci
IL16603903A IL166039A0 (en) 2002-07-31 2003-07-31 New effector conjugates process for their production and their pharmaceutical use
JP2005506073A JP2006505627A (ja) 2002-07-31 2003-07-31 新規エフェクター接合体、それらの生成方法及びそれらの医薬使用
AU2003253365A AU2003253365A1 (en) 2002-07-31 2003-07-31 New effector conjugates, process for their production and their pharmaceutical use
MXPA05001282A MXPA05001282A (es) 2002-07-31 2003-07-31 Conjugados efectores nuevos, procedimiento para su produccion y su uso farmaceutico.
IS7708A IS7708A (is) 2002-07-31 2005-02-23 Tenglar fyrir stýrisameindir, efnasmíði þeirra oglyfjafræðileg notkun
HR20050186A HRP20050186A2 (en) 2002-07-31 2005-02-25 New effector conjugates, process for their production and their pharmaceutical use
NO20051038A NO20051038L (no) 2002-07-31 2005-02-25 Nye effektorkonjugater, fremgangsmate for deres fremstilling, og deres farmasoytiske bruk

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
DE10234975A DE10234975A1 (de) 2002-07-31 2002-07-31 Neue Effektor-Konjugate, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung
DE10234975.4 2002-07-31
DE10305098A DE10305098A1 (de) 2003-02-07 2003-02-07 Neue Effektor-Konjugate, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung
DE10305098.1 2003-02-07
US45167303P 2003-03-05 2003-03-05
US60/451,673 2003-03-05

Publications (2)

Publication Number Publication Date
WO2004012735A2 true WO2004012735A2 (fr) 2004-02-12
WO2004012735A3 WO2004012735A3 (fr) 2004-05-27

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2003/008483 WO2004012735A2 (fr) 2002-07-31 2003-07-31 Nouveaux conjugues d'effecteurs, procedes permettant de les produire et utilisation pharmaceutique de ceux-ci

Country Status (16)

Country Link
EP (1) EP1524979A2 (fr)
JP (1) JP2006505627A (fr)
KR (1) KR20050026033A (fr)
AU (1) AU2003253365A1 (fr)
BR (1) BR0313043A (fr)
CA (1) CA2492437A1 (fr)
CO (1) CO5700741A2 (fr)
EC (1) ECSP055626A (fr)
HR (1) HRP20050186A2 (fr)
IL (1) IL166039A0 (fr)
IS (1) IS7708A (fr)
MX (1) MXPA05001282A (fr)
NO (1) NO20051038L (fr)
NZ (1) NZ537870A (fr)
PL (1) PL374528A1 (fr)
WO (1) WO2004012735A2 (fr)

Cited By (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004024735A2 (fr) * 2002-09-13 2004-03-25 Novartis Ag Nouvelle technique de preparation de derives d'epothilone, nouveaux derives de l'epothilone et nouveaux produits intermediaires utilises dans cette technique et dans les procedes de preparation de ces derives
WO2004050089A1 (fr) * 2002-12-05 2004-06-17 Schering Ag Analogues d'epothilone permettant l'administration specifique d'un site dans le traitement de maladies proliferatives
WO2005074901A2 (fr) * 2004-01-30 2005-08-18 Schering Ag Nouveaux conjugues d'effecteurs, leurs procedes de production et leur utilisation pharmaceutique
US7001916B1 (en) * 1999-02-11 2006-02-21 Schering, Ag Epothilon derivatives, method for the production and the use thereof as pharmaceuticals
WO2007140298A1 (fr) * 2006-05-25 2007-12-06 Bristol-Myers Squibb Company Conjugués d'analogues d'aziridinyl-épothilone et compositions pharmaceutiques les incluant
US7541330B2 (en) 2004-06-15 2009-06-02 Kosan Biosciences Incorporated Conjugates with reduced adverse systemic effects
US7605136B2 (en) 2002-12-05 2009-10-20 Bayer Schering Pharma Ag Effector conjugates, methods for their preparation and their pharmaceutical use
US7759374B2 (en) 2002-08-23 2010-07-20 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
US7872145B2 (en) 2006-05-25 2011-01-18 Bristol-Mysers Squibb Company Aziridinyl-epothilone compounds
US7875638B2 (en) 2002-08-23 2011-01-25 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US8143415B2 (en) 2007-05-25 2012-03-27 Bristol-Myers Squibb Company Processes for making epothilone compounds and analogs
US20130079532A1 (en) * 2010-06-10 2013-03-28 Chemi S.P.A. Process for the preparation of 2-hydroxy-4-phenyl-3,4-dihydro-2h-chromen-6-yl-methanol and (r)-feso-deacyl
US9090563B2 (en) 2004-07-23 2015-07-28 Endocyte, Inc. Bivalent linkers and conjugates thereof
US9662402B2 (en) 2012-10-16 2017-05-30 Endocyte, Inc. Drug delivery conjugates containing unnatural amino acids and methods for using
US9745341B2 (en) 2007-10-25 2017-08-29 Endocyte, Inc. Tubulysins and processes for preparing
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
WO2018073680A1 (fr) * 2016-10-17 2018-04-26 Pfizer Inc. Anticorps anti-edb et conjugués anticorps-médicament
US10080805B2 (en) 2012-02-24 2018-09-25 Purdue Research Foundation Cholecystokinin B receptor targeting for imaging and therapy
US10738086B2 (en) 2007-06-25 2020-08-11 Endocyte Inc. Conjugates containing hydrophilic spacer linkers

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ599239A (en) 2007-03-14 2013-10-25 Endocyte Inc Binding ligand linked drug delivery conjugates of tubulysins
US20140080175A1 (en) 2012-03-29 2014-03-20 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
KR102377416B1 (ko) * 2017-06-30 2022-03-21 엘지디스플레이 주식회사 표시장치

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EP0121350A2 (fr) * 1983-03-07 1984-10-10 Smithkline Beckman Corporation Acides mercaptocarboxyliques insaturés substitués et dérivés comme antagonistes de leukotriène
WO1994011021A1 (fr) * 1992-11-10 1994-05-26 Cortech, Inc. Antagoniste de bradykinine
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WO2001064650A2 (fr) * 2000-03-01 2001-09-07 Sloan-Kettering Institute For Cancer Research Center Synthese d'epothilones, de leurs produits intermediaires et de leurs analogues
WO2001083800A2 (fr) * 2000-04-28 2001-11-08 Kosan Biosciences, Inc. Production de polyketides
EP1156053A2 (fr) * 2000-05-18 2001-11-21 National Starch and Chemical Investment Holding Corporation Silanes avec des groupements carbamates ou uréa, et des groupements avec une fonctionnalité de donneur ou accepteur
WO2001092255A2 (fr) * 2000-05-26 2001-12-06 Kosan Biosciences, Inc. Derives d'epothilone, procedes de production et methodes d'utilisation
DE10041221A1 (de) * 2000-08-22 2002-03-14 Deutsches Krebsforsch Verfahren zur Herstellung von wasserlöslichen Saccharidkonjugaten und Saccharidmimetika durch Diels-Alder-Reaktion und ihre Verwendung als Therapeutika oder Diagnostika
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EP0121350A2 (fr) * 1983-03-07 1984-10-10 Smithkline Beckman Corporation Acides mercaptocarboxyliques insaturés substitués et dérivés comme antagonistes de leukotriène
WO1994011021A1 (fr) * 1992-11-10 1994-05-26 Cortech, Inc. Antagoniste de bradykinine
US5942555A (en) * 1996-03-21 1999-08-24 Surmodics, Inc. Photoactivatable chain transfer agents and semi-telechelic photoactivatable polymers prepared therefrom
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WO2001064650A2 (fr) * 2000-03-01 2001-09-07 Sloan-Kettering Institute For Cancer Research Center Synthese d'epothilones, de leurs produits intermediaires et de leurs analogues
WO2001083800A2 (fr) * 2000-04-28 2001-11-08 Kosan Biosciences, Inc. Production de polyketides
EP1156053A2 (fr) * 2000-05-18 2001-11-21 National Starch and Chemical Investment Holding Corporation Silanes avec des groupements carbamates ou uréa, et des groupements avec une fonctionnalité de donneur ou accepteur
WO2001092255A2 (fr) * 2000-05-26 2001-12-06 Kosan Biosciences, Inc. Derives d'epothilone, procedes de production et methodes d'utilisation
DE10041221A1 (de) * 2000-08-22 2002-03-14 Deutsches Krebsforsch Verfahren zur Herstellung von wasserlöslichen Saccharidkonjugaten und Saccharidmimetika durch Diels-Alder-Reaktion und ihre Verwendung als Therapeutika oder Diagnostika
WO2003005026A2 (fr) * 2001-07-02 2003-01-16 Amersham Biosciences Uk Limited Reactif chimique de capture

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US8513429B2 (en) 2002-08-23 2013-08-20 Sloan-Kettering Insitute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
US8110590B2 (en) 2002-08-23 2012-02-07 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
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US7759374B2 (en) 2002-08-23 2010-07-20 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
WO2004024735A2 (fr) * 2002-09-13 2004-03-25 Novartis Ag Nouvelle technique de preparation de derives d'epothilone, nouveaux derives de l'epothilone et nouveaux produits intermediaires utilises dans cette technique et dans les procedes de preparation de ces derives
WO2004024735A3 (fr) * 2002-09-13 2004-07-22 Novartis Ag Nouvelle technique de preparation de derives d'epothilone, nouveaux derives de l'epothilone et nouveaux produits intermediaires utilises dans cette technique et dans les procedes de preparation de ces derives
US7470792B2 (en) 2002-09-13 2008-12-30 Novartis Ag Process for the preparation of epothilone derivatives, new epothilone derivatives as well as new intermediate products for the process and the methods of preparing same
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EP1524979A2 (fr) 2005-04-27
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NZ537870A (en) 2007-03-30
MXPA05001282A (es) 2005-04-28
IL166039A0 (en) 2006-01-15
BR0313043A (pt) 2005-06-14
CO5700741A2 (es) 2006-11-30
AU2003253365A1 (en) 2004-02-23
JP2006505627A (ja) 2006-02-16
WO2004012735A3 (fr) 2004-05-27
HRP20050186A2 (en) 2005-10-31
ECSP055626A (es) 2005-04-18
PL374528A1 (en) 2005-10-31
NO20051038L (no) 2005-04-06
IS7708A (is) 2005-02-23

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