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PE20040747A1 - Nuevos conjugados de efectores y procedimientos para su preparacion - Google Patents

Nuevos conjugados de efectores y procedimientos para su preparacion

Info

Publication number
PE20040747A1
PE20040747A1 PE2003000756A PE2003000756A PE20040747A1 PE 20040747 A1 PE20040747 A1 PE 20040747A1 PE 2003000756 A PE2003000756 A PE 2003000756A PE 2003000756 A PE2003000756 A PE 2003000756A PE 20040747 A1 PE20040747 A1 PE 20040747A1
Authority
PE
Peru
Prior art keywords
aryl
alkyl
methyl
effectors
procedures
Prior art date
Application number
PE2003000756A
Other languages
English (en)
Inventor
Ulrich Klar
Gerhard Siemeister
Markus Berger
Klaus Bosslet
Jorg Willuda
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
Application filed by Schering Ag filed Critical Schering Ag
Publication of PE20040747A1 publication Critical patent/PE20040747A1/es

Links

Classifications

    • 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
    • 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
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Cell Biology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I DONDE R1a Y R1b SON CADA UNO H, ALQUILO C1-C10, ARILO, ARALQUILO, ENTRE OTROS; R2a Y R2b SON CADA UNO H, ALQUILO C1-C10, ARILO, ENTRE OTROS; R3 ES H, ALQUILO C1-C10, ARILO, ARALQUILO; R4a Y R4b SON CADA UNO H, ALQUILO C1-C10, ARILO, ENTRE OTROS; R5 ES H, ARILO, CO2H, CO2ALQUILO, ENTRE OTROS; R6 Y R7 SON CADA UNO H, O JUNTOS FORMAN UN ENLACE ADICIONAL O UN GRUPO NH, ENTRE OTROS; G ES O, CH2; D-E ES UN GRUPO CH2-CH2, CH=CH, CH(OH), ENTRE OTROS; W ES C(=X)R8, RADICAL AROMATICO, HETEROAROMATICO BI O TRICICLICO; L3 ES H, O-L4 ENTRE OTROS; Z ES O, ENTRE OTROS; L1, L2, L4 SON CADA UNO H, C(=O)CL, C(=S)CL, ENTRE OTROS; R8 ES H, ALQUILO C1-C10, ARILO, ENTRE OTROS; A-Y ES O-C(=O), O-CH2, CH2-C(=O), ENTRE OTROS; X ES O, ALQUILENDIOXI C2-C10, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (4S,7R,8S,9S,13Z,16S(E))-4,8-DIHIDROXI-5,5,7,9,13-PENTAMETIL-16-[1-METIL-2-(2-METIL-TIAZOL-4-IL)-VINIL]-OXACICLOHEXADEC-13-EN-2,6-DIONA Y (1S,3S(E),7S,10R,11S,12S,16R)-7,11-DIHIDROXI-8,8,10,12,16-PENTAMETIL-3-[1-METIL-2-(2-METIL-TIAZOL-4-IL)-VINIL]-4,17-DIOXA-BICICLO[14.1.0]HEPTADECAN-5,9-DIONA; ENTRE OTROS. DICHOS COMPUESTOS SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES ASOCIADAS A PROCESOS PROLIFERATIVOS
PE2003000756A 2002-07-31 2003-07-31 Nuevos conjugados de efectores y procedimientos para su preparacion PE20040747A1 (es)

Applications Claiming Priority (2)

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
DE10305098A DE10305098A1 (de) 2003-02-07 2003-02-07 Neue Effektor-Konjugate, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung

Publications (1)

Publication Number Publication Date
PE20040747A1 true PE20040747A1 (es) 2004-12-11

Family

ID=38812801

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2003000756A PE20040747A1 (es) 2002-07-31 2003-07-31 Nuevos conjugados de efectores y procedimientos para su preparacion

Country Status (7)

Country Link
US (3) US7129254B2 (es)
AR (1) AR040956A1 (es)
EA (1) EA200500223A1 (es)
PE (1) PE20040747A1 (es)
RS (1) RS20050082A (es)
TW (1) TW200404065A (es)
UY (1) UY27915A1 (es)

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US20030176663A1 (en) * 1998-05-11 2003-09-18 Eidgenossische Technische Hochscule Specific binding molecules for scintigraphy
CA2400622A1 (en) * 2000-02-24 2001-08-30 Eidgenossische Technische Hochschule Zurich Antibody specific for the ed-b domain of fibronectin, conjugates comprising said antibody, and their use for the detection and treatment of angiogenesis
CN1246333C (zh) * 2000-09-07 2006-03-22 舍林股份公司 EDb－纤粘连蛋白结构域(II)的受体
DE102004004787A1 (de) * 2004-01-30 2005-08-18 Schering Ag Neue Effektor-Konjugate, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung
US7541330B2 (en) * 2004-06-15 2009-06-02 Kosan Biosciences Incorporated Conjugates with reduced adverse systemic effects
US20090074711A1 (en) * 2006-09-07 2009-03-19 University Of Southhampton Human therapies using chimeric agonistic anti-human cd40 antibody
NZ583931A (en) 2007-08-17 2012-06-29 Purdue Research Foundation Psma binding ligand-linker conjugates and methods for using
US8253725B2 (en) * 2007-12-28 2012-08-28 St. Jude Medical, Atrial Fibrillation Division, Inc. Method and system for generating surface models of geometric structures
US9951324B2 (en) 2010-02-25 2018-04-24 Purdue Research Foundation PSMA binding ligand-linker conjugates and methods for using
EP3875082A1 (en) 2012-11-15 2021-09-08 Endocyte, Inc. Conjugates for treating diseases caused by psma expressing cells
EP2934596A1 (en) * 2012-12-21 2015-10-28 Glykos Finland Oy Linker-payload molecule conjugates
TN2016000137A1 (en) 2013-10-18 2017-10-06 Deutsches Krebsforsch Labeled inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer.
ES3013992T3 (en) 2013-11-14 2025-04-16 Endocyte Inc Compounds for positron emission tomography
US10973920B2 (en) 2014-06-30 2021-04-13 Glykos Finland Oy Saccharide derivative of a toxic payload and antibody conjugates thereof
HUE052460T2 (hu) 2014-09-12 2021-04-28 Genentech Inc Anti-HER2 antitestek és immunkonjugátumok
US10188759B2 (en) 2015-01-07 2019-01-29 Endocyte, Inc. Conjugates for imaging
MA43345A (fr) 2015-10-02 2018-08-08 Hoffmann La Roche Conjugués anticorps-médicaments de pyrrolobenzodiazépine et méthodes d'utilisation
WO2019204335A1 (en) 2018-04-17 2019-10-24 Endocyte, Inc. Methods of treating cancer
EP3972627A4 (en) 2019-05-20 2023-06-21 Endocyte, Inc. Methods for preparing psma conjugates

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Also Published As

Publication number Publication date
US20080166362A1 (en) 2008-07-10
US7335775B2 (en) 2008-02-26
US20070088060A1 (en) 2007-04-19
AR040956A1 (es) 2005-04-27
US7129254B2 (en) 2006-10-31
TW200404065A (en) 2004-03-16
US20050026971A1 (en) 2005-02-03
UY27915A1 (es) 2004-02-27
EA200500223A1 (ru) 2005-08-25
RS20050082A (sr) 2007-09-21

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