WO2004012735A3 - New effector conjugates, process for their production and their pharmaceutical use - Google Patents

New effector conjugates, process for their production and their pharmaceutical use Download PDF

Info

Publication number
WO2004012735A3
WO2004012735A3 PCT/EP2003/008483 EP0308483W WO2004012735A3 WO 2004012735 A3 WO2004012735 A3 WO 2004012735A3 EP 0308483 W EP0308483 W EP 0308483W WO 2004012735 A3 WO2004012735 A3 WO 2004012735A3
Authority
WO
WIPO (PCT)
Prior art keywords
production
pharmaceutical use
conjugates
new effector
effector conjugates
Prior art date
Application number
PCT/EP2003/008483
Other languages
French (fr)
Other versions
WO2004012735A2 (en
Inventor
Markus Berger
Gerhard Siemeister
Ulrich Klar
Joerg Willuda
Andreas Menrad
Klaus Bosslet
Original Assignee
Schering Ag
Markus Berger
Gerhard Siemeister
Ulrich Klar
Joerg Willuda
Andreas Menrad
Klaus Bosslet
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/en
Priority claimed from DE10305098A external-priority patent/DE10305098A1/en
Priority to AU2003253365A priority Critical patent/AU2003253365A1/en
Priority to EP03743752A priority patent/EP1524979A2/en
Priority to JP2005506073A priority patent/JP2006505627A/en
Priority to YUP-2005/0082A priority patent/RS20050082A/en
Priority to IL16603903A priority patent/IL166039A0/en
Priority to MXPA05001282A priority patent/MXPA05001282A/en
Application filed by Schering Ag, Markus Berger, Gerhard Siemeister, Ulrich Klar, Joerg Willuda, Andreas Menrad, Klaus Bosslet filed Critical Schering Ag
Priority to CA002492437A priority patent/CA2492437A1/en
Priority to NZ537870A priority patent/NZ537870A/en
Priority to EA200500223A priority patent/EA200500223A1/en
Priority to BR0313043-6A priority patent/BR0313043A/en
Publication of WO2004012735A2 publication Critical patent/WO2004012735A2/en
Publication of WO2004012735A3 publication Critical patent/WO2004012735A3/en
Priority to IS7708A priority patent/IS7708A/en
Priority to NO20051038A priority patent/NO20051038L/en
Priority to HR20050186A priority patent/HRP20050186A2/en

Links

Classifications

    • 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

Landscapes

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

Abstract

Conjugates of epothilones and epothilone derivatives (as effectors) with suitable biomolecules (as recognition units) are described. Their production is carried out by the effectors being reacted with suitable linkers, and the compounds that are produced are conjugated to the recognition units. The pharmaceutical use of the conjugates for treating proliferative or angiogenesis-associated processes is described.
PCT/EP2003/008483 2002-07-31 2003-07-31 New effector conjugates, process for their production and their pharmaceutical use WO2004012735A2 (en)

Priority Applications (13)

Application Number Priority Date Filing Date Title
EA200500223A EA200500223A1 (en) 2002-07-31 2003-07-31 NEW CONJUGATES - EFFECTORS, METHOD OF THEIR PRODUCTION AND THEIR PHARMACEUTICAL APPLICATION
BR0313043-6A BR0313043A (en) 2002-07-31 2003-07-31 Effector conjugates, process for their production and pharmaceutical use
CA002492437A CA2492437A1 (en) 2002-07-31 2003-07-31 New effector conjugates, process for their production and their pharmaceutical use
JP2005506073A JP2006505627A (en) 2002-07-31 2003-07-31 Novel effector conjugates, methods for their production and their pharmaceutical use
YUP-2005/0082A RS20050082A (en) 2002-07-31 2003-07-31 New efector conjugates,process for their production and their pharmaceutical use
IL16603903A IL166039A0 (en) 2002-07-31 2003-07-31 New effector conjugates process for their production and their pharmaceutical use
MXPA05001282A MXPA05001282A (en) 2002-07-31 2003-07-31 New effector conjugates, process for their production and their pharmaceutical use.
AU2003253365A AU2003253365A1 (en) 2002-07-31 2003-07-31 New effector conjugates, process for their production and their pharmaceutical use
EP03743752A EP1524979A2 (en) 2002-07-31 2003-07-31 New effector conjugates, process for their production and their pharmaceutical use
NZ537870A NZ537870A (en) 2002-07-31 2003-07-31 New effector conjugates, process for their production and their pharmaceutical use
IS7708A IS7708A (en) 2002-07-31 2005-02-23 Steering molecule links, their synthesis and pharmacological use
HR20050186A HRP20050186A2 (en) 2002-07-31 2005-02-25 New effector conjugates, process for their production and their pharmaceutical use
NO20051038A NO20051038L (en) 2002-07-31 2005-02-25 New effector conjugates, processes for their preparation, and their pharmaceutical use

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
DE10234975A DE10234975A1 (en) 2002-07-31 2002-07-31 New effector conjugates of epithilones useful to treat e.g. diseases associated with proliferative processes, neurodegenerative diseases, multiple sclerosis, Alzheimer's disease and rheumatoid arthritis
DE10234975.4 2002-07-31
DE10305098A DE10305098A1 (en) 2003-02-07 2003-02-07 New effector conjugates of epithilones useful to treat e.g. diseases associated with proliferative processes, neurodegenerative diseases, multiple sclerosis, Alzheimer's disease and rheumatoid arthritis
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 WO2004012735A2 (en) 2004-02-12
WO2004012735A3 true WO2004012735A3 (en) 2004-05-27

Family

ID=31498923

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2003/008483 WO2004012735A2 (en) 2002-07-31 2003-07-31 New effector conjugates, process for their production and their pharmaceutical use

Country Status (16)

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

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9138484B2 (en) 2007-06-25 2015-09-22 Endocyte, Inc. Conjugates containing hydrophilic spacer linkers
US9187521B2 (en) 2007-10-25 2015-11-17 Endocyte, Inc. Tubulysins and processes for preparing
US9505747B2 (en) 2012-03-29 2016-11-29 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
US9550734B2 (en) 2004-07-23 2017-01-24 Endocyte, Inc. Bivalent linkers and conjugates thereof
US9555139B2 (en) 2007-03-14 2017-01-31 Endocyte, Inc. Binding ligand linked drug delivery conjugates of tubulysins

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SK11452001A3 (en) * 1999-02-11 2002-04-04 Schering Aktiengesellschaft Epothilon derivatives, method for the production and the use thereof as pharmaceuticals
WO2004018478A2 (en) 2002-08-23 2004-03-04 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US7649006B2 (en) 2002-08-23 2010-01-19 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
GB0221312D0 (en) 2002-09-13 2002-10-23 Novartis Ag Organic compounds
JP2006510626A (en) * 2002-12-05 2006-03-30 シエーリング アクチエンゲゼルシャフト Epothilone analogs for site-specific delivery in the treatment of proliferative diseases
DE10256982A1 (en) 2002-12-05 2004-06-24 Schering Ag New epithilone derivatives are useful for the treatment of diseases associated with proliferative diseases e.g. tumor diseases, inflammatory diseases and neurodegenerative diseases
JP2007519681A (en) * 2004-01-30 2007-07-19 バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト Novel effector complexes, methods for producing them and their pharmaceutical use
US7541330B2 (en) 2004-06-15 2009-06-02 Kosan Biosciences Incorporated Conjugates with reduced adverse systemic effects
PE20080102A1 (en) * 2006-05-25 2008-02-11 Bristol Myers Squibb Co AZIRIDINYL-EPOTILONE CONJUGATES AND PHARMACEUTICAL COMPOSITIONS INCLUDING THE SAME
PE20080316A1 (en) 2006-05-25 2008-04-10 Bristol Myers Squibb Co AZIRIDINYL-EPOTILONE COMPOUNDS
WO2008147941A1 (en) 2007-05-25 2008-12-04 Bristol-Myers Squibb Company Processes for making epothilone compounds and analogs
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
IT1401451B1 (en) * 2010-06-10 2013-07-26 Chemi Spa NEW PROCESS OF PREPARATION OF 2-HYDROXY-4-PHENYL-3,4-DIHYDRO-2H-CHROMEN-6-IL-METHANOL E (R) -2- [3- (DIISOPROPYLAMINOUS) -1-PHENYLPROPYL] -4- ( hydroxymethyl) Phenol.
US10080805B2 (en) 2012-02-24 2018-09-25 Purdue Research Foundation Cholecystokinin B receptor targeting for imaging and therapy
EA201590622A1 (en) 2012-10-16 2015-10-30 Эндосайт, Инк. CONJUGATES FOR DELIVERY OF MEDICINES CONTAINING NOT MEETING IN THE NATURE OF AMINO ACID AND METHODS OF APPLICATION
IL266112B1 (en) * 2016-10-17 2024-03-01 Pfizer Anti-edb antibodies and antibody-drug conjugates
KR102377416B1 (en) * 2017-06-30 2022-03-21 엘지디스플레이 주식회사 Display Device

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0121350A2 (en) * 1983-03-07 1984-10-10 Smithkline Beckman Corporation Substituted unsaturated mercaptocarboxylic acids and derivatives as leukotriene antagonists
WO1994011021A1 (en) * 1992-11-10 1994-05-26 Cortech, Inc. Bradykinin antagonists
US5942555A (en) * 1996-03-21 1999-08-24 Surmodics, Inc. Photoactivatable chain transfer agents and semi-telechelic photoactivatable polymers prepared therefrom
WO2001064650A2 (en) * 2000-03-01 2001-09-07 Sloan-Kettering Institute For Cancer Research Center Synthesis of epothilones, intermediates thereto and analogues thereof
WO2001083800A2 (en) * 2000-04-28 2001-11-08 Kosan Biosciences, Inc. Heterologous production of polyketides
EP1156053A2 (en) * 2000-05-18 2001-11-21 National Starch and Chemical Investment Holding Corporation Adhesion promoters which are silanes comprising carbamate- or urea-groups, and a group with donor or acceptor functionality
WO2001092255A2 (en) * 2000-05-26 2001-12-06 Kosan Biosciences, Inc. Epothilone derivatives and methods for making and using the same
DE10041221A1 (en) * 2000-08-22 2002-03-14 Deutsches Krebsforsch Process for the preparation of water-soluble saccharide conjugates and saccharide mimetics by the Diels-Alder reaction and their use as therapeutics or diagnostics
US20020058286A1 (en) * 1999-02-24 2002-05-16 Danishefsky Samuel J. Synthesis of epothilones, intermediates thereto and analogues thereof
WO2003005026A2 (en) * 2001-07-02 2003-01-16 Amersham Biosciences Uk Limited Chemical capture reagent

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0121350A2 (en) * 1983-03-07 1984-10-10 Smithkline Beckman Corporation Substituted unsaturated mercaptocarboxylic acids and derivatives as leukotriene antagonists
WO1994011021A1 (en) * 1992-11-10 1994-05-26 Cortech, Inc. Bradykinin antagonists
US5942555A (en) * 1996-03-21 1999-08-24 Surmodics, Inc. Photoactivatable chain transfer agents and semi-telechelic photoactivatable polymers prepared therefrom
US20020058286A1 (en) * 1999-02-24 2002-05-16 Danishefsky Samuel J. Synthesis of epothilones, intermediates thereto and analogues thereof
WO2001064650A2 (en) * 2000-03-01 2001-09-07 Sloan-Kettering Institute For Cancer Research Center Synthesis of epothilones, intermediates thereto and analogues thereof
WO2001083800A2 (en) * 2000-04-28 2001-11-08 Kosan Biosciences, Inc. Heterologous production of polyketides
EP1156053A2 (en) * 2000-05-18 2001-11-21 National Starch and Chemical Investment Holding Corporation Adhesion promoters which are silanes comprising carbamate- or urea-groups, and a group with donor or acceptor functionality
WO2001092255A2 (en) * 2000-05-26 2001-12-06 Kosan Biosciences, Inc. Epothilone derivatives and methods for making and using the same
DE10041221A1 (en) * 2000-08-22 2002-03-14 Deutsches Krebsforsch Process for the preparation of water-soluble saccharide conjugates and saccharide mimetics by the Diels-Alder reaction and their use as therapeutics or diagnostics
WO2003005026A2 (en) * 2001-07-02 2003-01-16 Amersham Biosciences Uk Limited Chemical capture reagent

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
BERSUKER I B ET AL: "Improved electron-conformational method of pharmacophore identification and bioactivity prediction. Application to angiotensin converting enzyme inhibitors.", JOURNAL OF CHEMICAL INFORMATION AND COMPUTER SCIENCES. 2000 NOV-DEC, vol. 40, no. 6, November 2000 (2000-11-01), pages 1363 - 1376, XP002274169, ISSN: 0095-2338 *
KALGUTKAR A S ET AL: "Inactivation of prostaglandin endoperoxide synthase (PGHS) by N-(substituted)maleimides.", ADVANCES IN EXPERIMENTAL MEDICINE AND BIOLOGY. 1997, vol. 407, 1997, pages 79 - 85, XP009027572, ISSN: 0065-2598 *
REGHUNADHAN NAIR C P ET AL: "Free radical copolymerisation of N-(4-hydroxy phenyl) maleimide with vinyl monomers: Solvent and penultimate-unit effects", EUROPEAN POLYMER JOURNAL, PERGAMON PRESS LTD. OXFORD, GB, vol. 35, no. 10, 28 July 1999 (1999-07-28), pages 1829 - 1840, XP004179475, ISSN: 0014-3057 *
WANG LAI-XI ET AL: "Carbohydrate-centered maleimide cluster as a new type of templates for multivalent peptide assembling: Synthesis of multivalent HIV-1 gp41 peptides.", BIOORGANIC AND MEDICINAL CHEMISTRY, vol. 11, no. 1, 2 January 2003 (2003-01-02), &, pages 159 - 166, XP002274170, ISSN: 0968-0896 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9550734B2 (en) 2004-07-23 2017-01-24 Endocyte, Inc. Bivalent linkers and conjugates thereof
US9555139B2 (en) 2007-03-14 2017-01-31 Endocyte, Inc. Binding ligand linked drug delivery conjugates of tubulysins
US9138484B2 (en) 2007-06-25 2015-09-22 Endocyte, Inc. Conjugates containing hydrophilic spacer linkers
US9187521B2 (en) 2007-10-25 2015-11-17 Endocyte, Inc. Tubulysins and processes for preparing
US9505747B2 (en) 2012-03-29 2016-11-29 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof

Also Published As

Publication number Publication date
IS7708A (en) 2005-02-23
CO5700741A2 (en) 2006-11-30
JP2006505627A (en) 2006-02-16
WO2004012735A2 (en) 2004-02-12
HRP20050186A2 (en) 2005-10-31
IL166039A0 (en) 2006-01-15
MXPA05001282A (en) 2005-04-28
NZ537870A (en) 2007-03-30
ECSP055626A (en) 2005-04-18
AU2003253365A1 (en) 2004-02-23
KR20050026033A (en) 2005-03-14
NO20051038L (en) 2005-04-06
CA2492437A1 (en) 2004-02-12
BR0313043A (en) 2005-06-14
EP1524979A2 (en) 2005-04-27
PL374528A1 (en) 2005-10-31

Similar Documents

Publication Publication Date Title
WO2004012735A3 (en) New effector conjugates, process for their production and their pharmaceutical use
WO2005074901A3 (en) New effector conjugates, process for their production and their pharmaceutical use
RS20050082A (en) New efector conjugates,process for their production and their pharmaceutical use
WO2003000699A8 (en) Substituted 1-oxa-2,8-diaza-spiro[4,5]dec-2-ene derivatives as medicaments for the treatment of pain
WO2003008431A1 (en) Process for producing sugar chain asparagine derivative
AU2003242083A1 (en) Complex of organic medicines and beta-cyclodextrin derivatives and its preparing process
EP1726299A3 (en) Cores and microcapsules suitable for parenteral administration as well as process for their manufacture
WO2005062977A3 (en) Prostate cancer specific internalizing human antibodies
WO2008003155A3 (en) Methods to prepare penta-1,4-dien-3-ones and substituted cyclohexanones and derivatives with antitumoral and antiparasitic properties, the compounds and their uses
CA2474510A1 (en) Fused tricyclic heterocycles useful for treating hyper-proliferative disorders
HK1070350A1 (en) Protected 3.5-dihydroxy-2.2-dimethyl-valeronitriles for the synthesis of epothilones and derivatives and method for the production and use thereof
WO2003026563A3 (en) Conjugated anti-psychotic drugs and uses thereof
WO2002076438A3 (en) Flt-1 ligands and their uses in the treatment of diseases regulatable by angiogenesis
WO2004111047A3 (en) Cycloalkanepyrrolopyridines as dp receptor antagonists
AU2003903242A0 (en) Process for the treatment of wood
TW200603215A (en) Apparatus for manufacturing substrate
AU7280300A (en) Porous organic polymer shaped bodies
AU2000273123A1 (en) Composition for manufacturing formed article comprising starch, pulverized plantfiber or organic fertilizer obtained by treating garbage as main material, meth od for producing the same, method for manufacturing formed article using the same, and formed article and method for use
AU2003228202A1 (en) Process for the production of nanoparticles, wherein low mechanical and sonic energies are used simultaneously
TW200510323A (en) Process for the preparation of nonpeptide substituted spirobenzoazepine derivatives
AU2002358768A1 (en) Organic dispersions of surface-modified nanoparticles, method for the production and use thereof
WO2004037167A3 (en) Methods of treating dry eye disease with lantibiotics
AU2003240042A1 (en) A process for the biological treatment of ammonium-rich aqueous media
WO2005021541A3 (en) Process for the production of polymorphs of rosiglitazone maleate
NO20051794D0 (en) Process for the preparation of epothilone derivatives, and novel intermediates for the process, and processes for the preparation of such

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: P-2005/0082

Country of ref document: YU

AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NI NO NZ OM PG PH PL PT RO RU SC SD SE SG SK SL SY TJ TM TN TR TT TZ UA UG US UZ VC VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LU MC NL PT RO SE SI SK TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
WWE Wipo information: entry into national phase

Ref document number: 2003743752

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: 38/DELNP/2005

Country of ref document: IN

WWE Wipo information: entry into national phase

Ref document number: 2492437

Country of ref document: CA

WWE Wipo information: entry into national phase

Ref document number: 537870

Country of ref document: NZ

WWE Wipo information: entry into national phase

Ref document number: 2005506073

Country of ref document: JP

WWE Wipo information: entry into national phase

Ref document number: 20038181118

Country of ref document: CN

Ref document number: 1-2005-500185

Country of ref document: PH

Ref document number: 1020057001569

Country of ref document: KR

WWE Wipo information: entry into national phase

Ref document number: PA/a/2005/001282

Country of ref document: MX

Ref document number: 2003253365

Country of ref document: AU

Ref document number: 374528

Country of ref document: PL

WWE Wipo information: entry into national phase

Ref document number: CR2005-007674

Country of ref document: CR

WWE Wipo information: entry into national phase

Ref document number: 200500223

Country of ref document: EA

WWE Wipo information: entry into national phase

Ref document number: 2005/01648

Country of ref document: ZA

Ref document number: 05017568

Country of ref document: CO

Ref document number: 200501648

Country of ref document: ZA

WWE Wipo information: entry into national phase

Ref document number: P20050186A

Country of ref document: HR

WWP Wipo information: published in national office

Ref document number: 1020057001569

Country of ref document: KR

WWP Wipo information: published in national office

Ref document number: 2003743752

Country of ref document: EP