ECSP055626A - NEW CONJUGATES OF EFFECTORS, PROCEDURES FOR PREPARATION AND PHARMACEUTICAL USE - Google Patents

NEW CONJUGATES OF EFFECTORS, PROCEDURES FOR PREPARATION AND PHARMACEUTICAL USE

Info

Publication number
ECSP055626A
ECSP055626A EC2005005626A ECSP055626A ECSP055626A EC SP055626 A ECSP055626 A EC SP055626A EC 2005005626 A EC2005005626 A EC 2005005626A EC SP055626 A ECSP055626 A EC SP055626A EC SP055626 A ECSP055626 A EC SP055626A
Authority
EC
Ecuador
Prior art keywords
effectors
pharmaceutical use
procedures
preparation
conjugates
Prior art date
Application number
EC2005005626A
Other languages
Spanish (es)
Inventor
Markus Berger
Gerhard Siemeister
Ulrich Klar
Joerg 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/en
Priority claimed from DE10305098A external-priority patent/DE10305098A1/en
Application filed by Schering Ag filed Critical Schering Ag
Publication of ECSP055626A publication Critical patent/ECSP055626A/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

Abstract

Se describen conjugados de epotilonas y derivados de epotilonas como efectores con biomoléculas adecuadas (como unidades de reconocimiento. Su producción se lleva a cabo haciendo reaccionar los efectores con ligadores adecuados y los compuestos que son producidos se conjugan con las unidades de reconocimiento. Se describe el uso farmacéutico de los conjugados para el tratamiento de procesos neurodegenerativos o asociados con la angiogénesis.Conjugates of epothilones and derivatives of epothilones are described as effectors with suitable biomolecules (as recognition units. Their production is carried out by reacting the effectors with suitable linkers and the compounds that are produced are conjugated with the recognition units. Pharmaceutical use of conjugates for the treatment of neurodegenerative processes or associated with angiogenesis.

EC2005005626A 2002-07-31 2005-02-24 NEW CONJUGATES OF EFFECTORS, PROCEDURES FOR PREPARATION AND PHARMACEUTICAL USE ECSP055626A (en)

Applications Claiming Priority (3)

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
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
US45167303P 2003-03-05 2003-03-05

Publications (1)

Publication Number Publication Date
ECSP055626A true ECSP055626A (en) 2005-04-18

Family

ID=31498923

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2005005626A ECSP055626A (en) 2002-07-31 2005-02-24 NEW CONJUGATES OF EFFECTORS, PROCEDURES FOR PREPARATION AND 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)

Families Citing this family (22)

* 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
US7649006B2 (en) 2002-08-23 2010-01-19 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
JP4791183B2 (en) 2002-08-23 2011-10-12 スローン−ケッタリング インスティトュート フォア キャンサー リサーチ Synthesis and use of epothilone, its intermediates and analogues
GB0221312D0 (en) 2002-09-13 2002-10-23 Novartis Ag Organic compounds
EP1581218A1 (en) * 2002-12-05 2005-10-05 Schering AG 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
WO2005074901A2 (en) * 2004-01-30 2005-08-18 Schering Ag New effector conjugates, process for their production and their pharmaceutical use
US7541330B2 (en) 2004-06-15 2009-06-02 Kosan Biosciences Incorporated Conjugates with reduced adverse systemic effects
JP5149620B2 (en) 2004-07-23 2013-02-20 エンドサイト，インコーポレイテッド Bivalent linker and conjugate thereof
AR061181A1 (en) 2006-05-25 2008-08-13 Bristol Myers Squibb Co AZIRIDINIL-EPOTILONE COMPOUNDS
PE20080102A1 (en) * 2006-05-25 2008-02-11 Bristol Myers Squibb Co AZIRIDINYL-EPOTILONE CONJUGATES AND PHARMACEUTICAL COMPOSITIONS INCLUDING THE SAME
NZ599239A (en) 2007-03-14 2013-10-25 Endocyte Inc Binding ligand linked drug delivery conjugates of tubulysins
WO2008147941A1 (en) 2007-05-25 2008-12-04 Bristol-Myers Squibb Company Processes for making epothilone compounds and analogs
WO2009002993A1 (en) 2007-06-25 2008-12-31 Endocyte, Inc. Conjugates containing hydrophilic spacer linkers
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
US9187521B2 (en) 2007-10-25 2015-11-17 Endocyte, Inc. Tubulysins and processes for preparing
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
US20140080175A1 (en) 2012-03-29 2014-03-20 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
IN2015DN04147A (en) 2012-10-16 2015-10-16 Endocyte Inc
KR102338660B1 (en) * 2016-10-17 2021-12-10 화이자 인코포레이티드 Anti-EDB Antibodies and Antibody-Drug Conjugates
KR102377416B1 (en) * 2017-06-30 2022-03-21 엘지디스플레이 주식회사 Display Device

Family Cites Families (10)

* Cited by examiner, † Cited by third party
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DK130984A (en) * 1983-03-07 1984-09-08 Smithkline Beckman Corp Leukotriene antagonists
IL107400A0 (en) * 1992-11-10 1994-01-25 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
CA2404938C (en) * 2000-04-28 2011-11-01 Kosan Biosciences, Inc. Production of polyketides
US6441213B1 (en) * 2000-05-18 2002-08-27 National Starch And Chemical Investment Holding Corporation Adhesion promoters containing silane, carbamate or urea, and donor or acceptor functionality
US20020045609A1 (en) * 2000-05-26 2002-04-18 Gary Ashley 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
GB0116143D0 (en) * 2001-07-02 2001-08-22 Amersham Pharm Biotech Uk Ltd Chemical capture reagent

Also Published As

Publication number Publication date
CA2492437A1 (en) 2004-02-12
WO2004012735A2 (en) 2004-02-12
EP1524979A2 (en) 2005-04-27
KR20050026033A (en) 2005-03-14
NZ537870A (en) 2007-03-30
MXPA05001282A (en) 2005-04-28
IL166039A0 (en) 2006-01-15
BR0313043A (en) 2005-06-14
CO5700741A2 (en) 2006-11-30
AU2003253365A1 (en) 2004-02-23
JP2006505627A (en) 2006-02-16
WO2004012735A3 (en) 2004-05-27
HRP20050186A2 (en) 2005-10-31
PL374528A1 (en) 2005-10-31
NO20051038L (en) 2005-04-06
IS7708A (en) 2005-02-23

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