DE3585540D1 - Therapeutisch verwendbare zytotoxische konjugate und verfahren zu deren herstellung. - Google Patents

Therapeutisch verwendbare zytotoxische konjugate und verfahren zu deren herstellung.

Info

Publication number
DE3585540D1
DE3585540D1 DE8787202356T DE3585540T DE3585540D1 DE 3585540 D1 DE3585540 D1 DE 3585540D1 DE 8787202356 T DE8787202356 T DE 8787202356T DE 3585540 T DE3585540 T DE 3585540T DE 3585540 D1 DE3585540 D1 DE 3585540D1
Authority
DE
Germany
Prior art keywords
group
functions
formula
originating
proteins
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
DE8787202356T
Other languages
English (en)
Inventor
Franz K Jansen
Pierre Gros
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sanofi SA
Original Assignee
Sanofi SA
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sanofi SA filed Critical Sanofi SA
Application granted granted Critical
Publication of DE3585540D1 publication Critical patent/DE3585540D1/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring 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
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6817—Toxins
    • A61K47/6819—Plant toxins
    • A61K47/6825—Ribosomal inhibitory proteins, i.e. RIP-I or RIP-II, e.g. Pap, gelonin or dianthin
    • 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
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6817—Toxins
    • A61K47/6819—Plant toxins
    • A61K47/6825—Ribosomal inhibitory proteins, i.e. RIP-I or RIP-II, e.g. Pap, gelonin or dianthin
    • A61K47/6827—Ricin A
    • 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
    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
    • 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
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/415—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from plants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Toxicology (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Botany (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)
  • Soft Magnetic Materials (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
DE8787202356T 1984-06-20 1985-06-18 Therapeutisch verwendbare zytotoxische konjugate und verfahren zu deren herstellung. Expired - Fee Related DE3585540D1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR8409703A FR2566271B1 (fr) 1984-06-20 1984-06-20 Nouveaux conjugues cytotoxiques utilisables en therapeutique et procede d'obtention

Publications (1)

Publication Number Publication Date
DE3585540D1 true DE3585540D1 (de) 1992-04-09

Family

ID=9305246

Family Applications (2)

Application Number Title Priority Date Filing Date
DE8585401199T Expired DE3568166D1 (en) 1984-06-20 1985-06-18 Cytotoxic conjugates useful in therapy, and process for obtaining them
DE8787202356T Expired - Fee Related DE3585540D1 (de) 1984-06-20 1985-06-18 Therapeutisch verwendbare zytotoxische konjugate und verfahren zu deren herstellung.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
DE8585401199T Expired DE3568166D1 (en) 1984-06-20 1985-06-18 Cytotoxic conjugates useful in therapy, and process for obtaining them

Country Status (8)

Country Link
US (1) US4980457A (de)
EP (2) EP0169111B1 (de)
JP (1) JPS6112630A (de)
AT (2) ATE40699T1 (de)
CA (1) CA1256796A (de)
DE (2) DE3568166D1 (de)
FR (2) FR2566271B1 (de)
ZA (1) ZA854558B (de)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4837003A (en) * 1984-09-13 1989-06-06 Mallinckrodt, Inc. Radiolabeled antibody fragments
US4659839A (en) * 1984-10-10 1987-04-21 Mallinckrodt, Inc. Coupling agents for radiolabeled antibody fragments
FR2601680B1 (fr) * 1986-07-15 1990-06-29 Sanofi Sa Inhibiteur de la synthese proteique, procede d'isolement, utilisation et compositions pharmaceutiques en contenant
FR2601679B1 (fr) * 1986-07-15 1990-05-25 Sanofi Sa Immunotoxines, procede de preparation et compositions pharmaceutiques en contenant
US4970303A (en) * 1988-02-03 1990-11-13 Xoma Corporation Linking agents and methods
IE62496B1 (en) * 1990-04-19 1995-02-08 Res Dev Foundation Antibody conjugates for treatment of neoplastic disease
EP0489931A4 (en) * 1990-06-29 1993-02-24 Toray Industries, Inc. Immunotoxin complex
AU7863591A (en) * 1990-09-14 1992-04-15 Biogen, Inc. Production of multimeric glycoproteins through chemical coupling
DE4033714C3 (de) * 1990-10-24 1995-09-07 Brahms Diagnostica Gmbh Neues Hapten-Analytikum basierend auf dem Prinzip einer Antigen-Antikörper-Reaktion
JP3093383B2 (ja) * 1990-11-30 2000-10-03 塩野義製薬株式会社 抗体標識のための放射性ヨウ素化合物
HUT65328A (en) * 1991-04-01 1994-05-02 Cortech Process for producing bradykinin antagonists
US5416191A (en) * 1991-04-01 1995-05-16 Cortech, Inc. Bradykinin antagonists
US6777190B1 (en) 1991-04-10 2004-08-17 Biosite, Inc. Crosstalk inhibitors and their uses
AU1772992A (en) * 1991-04-10 1992-11-17 Biosite Diagnostics Incorporated Crosstalk inhibitors and their uses
US5112607A (en) * 1991-06-05 1992-05-12 The United States Of America As Represented By The Secretary Of The Army Potentiation of immunotoxin action by Brefeldin A
CA2070961C (en) * 1991-06-14 2004-12-07 Michael Chorev Thiol-reactive maleimido-based radiolabeling reagents
US5622929A (en) * 1992-01-23 1997-04-22 Bristol-Myers Squibb Company Thioether conjugates
US5965132A (en) 1992-03-05 1999-10-12 Board Of Regents, The University Of Texas System Methods and compositions for targeting the vasculature of solid tumors
US6749853B1 (en) * 1992-03-05 2004-06-15 Board Of Regents, The University Of Texas System Combined methods and compositions for coagulation and tumor treatment
DE19636889A1 (de) * 1996-09-11 1998-03-12 Felix Dr Kratz Antineoplastisch wirkende Transferrin- und Albuminkonjugate zytostatischer Verbindungen aus der Gruppe der Anthrazykline, Alkylantien, Antimetabolite und Cisplatin-Analoga und diese enthaltende Arzneimittel
US6673538B1 (en) 1997-07-25 2004-01-06 The Trustees Of Boston University Methods and compositions for designing vaccines
AU8513798A (en) 1997-07-25 1999-02-16 Trustees Of Boston University Methods and compositions for determining species of bacteria and fungi
US6339626B1 (en) * 1998-03-16 2002-01-15 Ge Medical Systems Global Technology Company, Llc MRI system with fractional decimation of acquired data
IL140700A0 (en) * 1998-07-13 2002-02-10 Univ Texas Cancer treatment methods using therapeutic conjugates that bind to aminophospholipids
US6818213B1 (en) * 1998-07-13 2004-11-16 Board Of Regents, The University Of Texas System Cancer treatment compositions comprising therapeutic conjugates that bind to aminophospholipids
EP1172372B1 (de) * 1999-04-02 2005-08-31 Ajinomoto Co., Inc. Vefahren zur herstellung von peptiduntereinheiten aus polymer-proteinen
US6703020B1 (en) 1999-04-28 2004-03-09 Board Of Regents, The University Of Texas System Antibody conjugate methods for selectively inhibiting VEGF
NZ514918A (en) 1999-04-28 2003-11-28 Univ Texas Compositions and methods for cancer treatment by selectively inhibiting VEGF
ZA200305980B (en) * 2001-02-12 2007-01-31 Res Dev Foundation Modified proteins, designer toxins, and methods of making thereof
IL159894A0 (en) * 2001-07-17 2004-06-20 Res Dev Foundation Therapeutic agents comprising pro-apoptotic proteins
EP1572170A4 (de) * 2002-06-12 2007-02-28 Res Dev Foundation Immunotoxin als therapeutisches mittel und seine verwendungen
CN101132813A (zh) * 2005-02-01 2008-02-27 研究发展基金会 靶向blys受体的blys融合蛋白和用于治疗b细胞增殖性疾病的方法

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL47372A (en) * 1975-05-27 1979-10-31 Yeda Res & Dev Fab'dimers bound to daunomycin or adriamycin,their preparation and pharmaceutical compositions containing same
FR2437213A1 (fr) * 1978-09-28 1980-04-25 Cm Ind Produits cytotoxiques formes par liaison covalente de la chaine a de la ricine avec un anticorps et leur procede de preparation
JPS5616418A (en) * 1979-07-20 1981-02-17 Teijin Ltd Antitumor protein complex and its preparation
FR2466252A2 (fr) * 1979-10-03 1981-04-10 Clin Midy Nouveaux produits ayant notamment des proprietes anticancereuses a base de chaine a de la ricine et d'une proteine
JPS5686121A (en) * 1979-12-14 1981-07-13 Teijin Ltd Antitumor proten complex and its preparation
EP0044167A3 (de) * 1980-07-14 1982-04-21 The Regents Of The University Of California Durch einen Antikörper gerichtetes zytotoxisches Mittel
JPS5764617A (en) * 1980-10-08 1982-04-19 Teijin Ltd Cytotoxic proteinic complex and its preparation
JPS57106625A (en) * 1980-12-22 1982-07-02 Teijin Ltd Cytotoxic protein complex and its preparation
JPS5843926A (ja) * 1981-09-08 1983-03-14 Suntory Ltd 選択性制癌剤
FR2516794B1 (fr) * 1981-11-20 1985-10-25 Sanofi Sa Nouveaux medicaments anticancereux pour le traitement des leucemies t constitues de la chaine a de la ricine et d'un anticorps monoclonal specifique
US4670563A (en) * 1984-06-20 1987-06-02 Sanofi Imidazolides as intermediates for the synthesis of cytotoxic conjugates
FR2577135B1 (fr) * 1985-02-13 1989-12-15 Sanofi Sa Immunotoxines a longue duree d'action comportant un constituant glycopeptidique inactivant les ribosomes modifie sur ses motifs polysaccharidiques

Also Published As

Publication number Publication date
ZA854558B (en) 1986-02-26
FR2566271A1 (fr) 1985-12-27
EP0169111B1 (de) 1989-02-08
US4980457A (en) 1990-12-25
EP0269188A2 (de) 1988-06-01
FR2606413A1 (fr) 1988-05-13
ATE40699T1 (de) 1989-02-15
FR2606413B1 (fr) 1989-07-28
EP0169111A1 (de) 1986-01-22
EP0269188B1 (de) 1992-03-04
JPS6112630A (ja) 1986-01-21
EP0269188A3 (en) 1988-08-31
ATE73139T1 (de) 1992-03-15
CA1256796A (en) 1989-07-04
DE3568166D1 (en) 1989-03-16
FR2566271B1 (fr) 1986-11-07

Similar Documents

Publication Publication Date Title
DE3585540D1 (de) Therapeutisch verwendbare zytotoxische konjugate und verfahren zu deren herstellung.
US8293888B2 (en) Sialic acid derivatives
JP5795040B2 (ja) タンパク質の誘導体化及び結合のための活性化シアル酸誘導体
AU659427B2 (en) Site-specific conjugation of immunoglobulins and detectable labels
JPS6121227B2 (de)
JPS63238100A (ja) 抗体複合体の製造方法
JP5197009B2 (ja) シアル酸誘導体
KR880001299A (ko) 면역독소, 그의 제조방법 및 그를 함유하는 약학 조성물
US20170001956A1 (en) Hydrocarbyl carboxybetaine and method for preventing hofmann elimination in alkaline environment
US5104976A (en) Ribosome-inactivating glycoproteins, modified by oxidation of their osidic units and formation of a schiff's base and in-vivo prolonged action immunotoxins containing such a glycoprotein
KR930003333B1 (ko) 탄수화물 단위가 변형된 리보솜을 비활성화시키는 당단백질 성분을 함유하는 지속-작용성 면역독소의 제조방법
WO1999008996A1 (en) Method of reducing a schiff base
WO1999001469A1 (en) A method for attaching polyethylene glycol to macromolecules
JPH0625143B2 (ja) イミダゾリド
EP0261225B1 (de) Lektinkomplex, sowie verfahren und sonde zu dessen herstellung
JPH0149299B2 (de)
WO1987004171A1 (en) Process for preparing antibody complex
Meikle et al. Preparation of polysaccharide-enzyme conjugates for competitive binding assays
JPH0149298B2 (de)
CS256456B1 (cs) Silanová činidla obsahující chemicky vázané komplexonové seskupení
JPH029564B2 (de)

Legal Events

Date Code Title Description
8380 Miscellaneous part iii

Free format text: DER PATENTINHABER LAUTET RICHTIG: ELF SANOFI, PARIS, FR

8328 Change in the person/name/address of the agent

Free format text: BEETZ, R., DIPL.-ING. DR.-ING. TIMPE, W., DR.-ING. SIEGFRIED, J., DIPL.-ING. SCHMITT-FUMIAN, W., PROF. DIPL.-CHEM. DR.RER.NAT. MAYR, C., DIPL.-PHYS.DR.RER.NAT., PAT.-ANWAELTE, 8000 MUENCHEN

8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee