AR245368A1 - Un procedimiento para la preparacion de un conjugado medicinal citotoxico. - Google Patents

Un procedimiento para la preparacion de un conjugado medicinal citotoxico.

Info

Publication number
AR245368A1
AR245368A1 AR89314592A AR31459289A AR245368A1 AR 245368 A1 AR245368 A1 AR 245368A1 AR 89314592 A AR89314592 A AR 89314592A AR 31459289 A AR31459289 A AR 31459289A AR 245368 A1 AR245368 A1 AR 245368A1
Authority
AR
Argentina
Prior art keywords
formula
link
ancient
carbonyl
alkyl
Prior art date
Application number
AR89314592A
Other languages
English (en)
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Application granted granted Critical
Publication of AR245368A1 publication Critical patent/AR245368A1/es

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/44—Antibodies bound to carriers
    • 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
    • A61K47/6883—Polymer-drug antibody conjugates, e.g. mitomycin-dextran-Ab; DNA-polylysine-antibody complex or conjugate used for therapy
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Biotechnology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

UN PROCEDIMIENTO PARA LA PREPARACION DE UN CONJUGADO MEDICINAL CITOTOXICO DE FORMULA (I), DONDE: AC ES UN ANTICUERPO FISIOLOGICAMENTE ACEPTABLE O FRAGMENTOS DEL MISMO, DICHO ANTICUERPO Y DICHOS FRAGMENTOS CAPACES DE RECONOCER ANTIGENOS ASOCIADOS A UNA CELULA INDESEABLE; M ES UN NUMERO ENTERO DE 1 A 10; Z ES HIDROGENO O ALQUILO; X ES UN ENLACE, ALQUILENO, O AMINO-ALQUILENO; Y ES UN ENLACE, CARBONILO, -O-, CON LA CONDICION DE QUE Y ES CARBONILO, CUANDO X ES AMINOALQUILENO E Y ES UN ENLACE O CARBONILO CUANDO X ES UN ENLACE; AR ES PIRROLILO, M-FENILO O P-FENILO; V ES UN MEDICAMENTOTIPO VINCA DE FORMULA (II), DONDE:R ES H, CH3 O CHO; DONDE R3 ES H Y UNO DE LOS RADICALES R1 Y R2 ES ETILO Y EL OTRO ES H U OH; CUANDO R2 Y R3 SE TOMAN JUNTOS, FORMAN UN ANILLO DE OXIRANO EN CUYO CASO R1 ES ETILO; R4 ES H (ALQUIL)-CO O CLORO (ALQUIL)-CO; OBTENIDO POR HACER REACCIONAR EN CUALQUIER ORDEN COMPATIBLE CON LA FORMACION DEL CONJUGADO DE FORMULA (I), VINCAHIDRAZIDAS DE FORMULA:NH2-NH-V UN ANTICUERPO AB Y UN ALDEHIDO O CETONA DE FORMULA: R5-COXY-AR-COZ PARA FORMAR LOS INTERMEDIARIOS DE FORMULA (IA) (IB), Y LUEGO HACERLOS REACCIONAR CON UN ANTICUERPO AB, RESPECTIVAMENTECON VINCAHIDRAZIDA DE FORMULA (IA), PARA FORMAR LOS COMPUESTOS DE FORMULA (I), SIENDO: R5 UN GRUPO HIDROXI O UN GRUPO CARBOXIACTIVANTE TAL COMO SUCCINIMIDOXI.
AR89314592A 1988-08-08 1989-08-04 Un procedimiento para la preparacion de un conjugado medicinal citotoxico. AR245368A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US07/230,084 US5006652A (en) 1988-08-08 1988-08-08 Intermediates for antibody-vinca drug conjugates

Publications (1)

Publication Number Publication Date
AR245368A1 true AR245368A1 (es) 1994-01-31

Family

ID=22863896

Family Applications (1)

Application Number Title Priority Date Filing Date
AR89314592A AR245368A1 (es) 1988-08-08 1989-08-04 Un procedimiento para la preparacion de un conjugado medicinal citotoxico.

Country Status (15)

Country Link
US (1) US5006652A (es)
EP (1) EP0354728A3 (es)
JP (1) JPH02131499A (es)
KR (1) KR900002804A (es)
CN (1) CN1040205A (es)
AR (1) AR245368A1 (es)
AU (1) AU619329B2 (es)
DK (1) DK382989A (es)
HU (1) HU206377B (es)
IL (1) IL91182A0 (es)
MX (1) MX164971B (es)
NZ (1) NZ230200A (es)
PH (1) PH27351A (es)
PT (1) PT91372A (es)
ZA (1) ZA895908B (es)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5776093A (en) 1985-07-05 1998-07-07 Immunomedics, Inc. Method for imaging and treating organs and tissues
AU633867B2 (en) * 1989-02-02 1993-02-11 Eli Lilly And Company Delivery of cytotoxic agents
US5272253A (en) * 1991-07-01 1993-12-21 Eli Lilly And Company Cluster conjugates of drugs with antibodies
GR1001459B (el) * 1992-10-08 1993-12-30 Lilly Co Eli Σύμπλεγμα συζυγών φαρμάκων με αντισώματα.
ES2049656B1 (es) * 1992-10-08 1994-11-16 Lilly Co Eli Grupos de conjugados de farmacos con anticuerpos.
US5773001A (en) * 1994-06-03 1998-06-30 American Cyanamid Company Conjugates of methyltrithio antitumor agents and intermediates for their synthesis
US20030119724A1 (en) * 1995-11-22 2003-06-26 Ts`O Paul O.P. Ligands to enhance cellular uptake of biomolecules
AU2002217980A1 (en) 2000-12-01 2002-06-11 Cell Works Inc. Conjugates of glycosylated/galactosylated peptide
EP1389209B1 (en) * 2001-04-24 2009-04-08 Purdue Research Foundation Folate mimetics and folate-receptor binding conjugates thereof
JP4814520B2 (ja) * 2002-05-15 2011-11-16 エンドサイト，インコーポレイテッド ビタミン−マイトマイシン結合体
EP2517729A3 (en) 2003-01-27 2013-01-02 Endocyte, Inc. Vitamin receptor binding drug delivery conjugates
EP1789391B1 (en) * 2004-07-23 2017-06-28 Endocyte, Inc. Bivalent linkers and conjugates thereof
WO2006101845A2 (en) * 2005-03-16 2006-09-28 Endocyte, Inc. Synthesis and purification of pteroic acid and conjugates thereof
JP2009504783A (ja) * 2005-08-19 2009-02-05 エンドサイト，インコーポレイテッド ビンカアルカロイド、類似体および誘導体のリガンド結合体
CN103893778A (zh) * 2005-08-19 2014-07-02 恩多塞特公司 多药物配体缀合物
WO2008101231A2 (en) * 2007-02-16 2008-08-21 Endocyte, Inc. Methods and compositions for treating and diagnosing kidney disease
EP2139523B1 (en) * 2007-03-14 2014-10-22 Endocyte, Inc. Conjugates of folate and tubulysin for targeted drug delivery
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
BRPI0812970A2 (pt) * 2007-06-25 2019-09-24 Endocyte Inc conjugados contendo espaçadores hidrofílicos
AU2008316835B2 (en) 2007-10-25 2015-07-16 Endocyte, Inc. Tubulysins and processes for preparing
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
MX2015004757A (es) 2012-10-16 2015-07-17 Endocyte Inc Conjugados de suministro de farmacos que contienen aminoacidos no naturales y metodo para usarlos.
SG11201507619PA (en) 2013-03-15 2015-10-29 Ct For Drug Res And Dev Cytotoxic and anti-mitotic compounds, and methods of using the same
WO2015095953A1 (en) 2013-12-27 2015-07-02 The Centre For Drug Research And Development Sulfonamide-containing linkage systems for drug conjugates
CN107001415B (zh) 2014-09-17 2021-06-18 酵活有限公司 细胞毒性和抗有丝分裂化合物、及其使用方法

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4203898A (en) * 1977-08-29 1980-05-20 Eli Lilly And Company Amide derivatives of VLB, leurosidine, leurocristine and related dimeric alkaloids
FI820020L (fi) * 1981-01-12 1982-07-13 Lilly Industries Ltd Immunoglobulinkonjugater
US4631190A (en) * 1981-06-26 1986-12-23 Shen Wei C Acidity-sensitive spacer molecule to control the release of pharmaceuticals from molecular carriers
CA1203164A (en) * 1982-03-09 1986-04-15 Thomas J. Mckearn Antibody conjugates
US4671958A (en) * 1982-03-09 1987-06-09 Cytogen Corporation Antibody conjugates for the delivery of compounds to target sites
EP0121388B1 (en) * 1983-03-30 1990-06-13 Lilly Industries Limited Immunoglobulin conjugates
HUT34212A (en) * 1983-04-29 1985-02-28 Omnichem Sa Process for the production of new vindblastin conjugates
LU86157A1 (fr) * 1985-11-12 1987-06-26 Omnichem Sa Nouveau procede de fabrication de conjugues de la vinblastine et de ses derives
US4675400A (en) * 1985-06-17 1987-06-23 Eli Lilly And Company Bifunctional derivatives of 4-desacetyl indole-dihydroindole alkaloids
EP0232693A3 (fr) * 1985-12-16 1988-04-06 La Region Wallonne Conjugués de la vinblastine et de ses dérivés, procédé pour leur préparation et compositions pharmaceutiques les contenant
GB8610551D0 (en) * 1986-04-30 1986-06-04 Hoffmann La Roche Polypeptide & protein derivatives
IL82579A0 (en) * 1986-05-27 1987-11-30 Lilly Co Eli Immunoglobulin conjugates
US4997913A (en) * 1986-06-30 1991-03-05 Oncogen pH-sensitive immunoconjugates and methods for their use in tumor therapy
FR2610198B1 (fr) * 1987-02-03 1990-06-15 Ire Celltarg Sa Conjugues d'hydrazide d'alcaloide de vinca lie a une immunoglobuline, procede de preparation et compositions pharmaceutiques en comprenant
IL89043A0 (en) * 1988-01-27 1989-08-15 Lilly Co Eli Antibody conjugates

Also Published As

Publication number Publication date
AU3933989A (en) 1990-02-08
EP0354728A3 (en) 1991-04-10
HU206377B (en) 1992-10-28
JPH02131499A (ja) 1990-05-21
IL91182A0 (en) 1990-03-19
US5006652A (en) 1991-04-09
DK382989A (da) 1990-02-09
HUT50488A (en) 1990-02-28
PH27351A (en) 1993-06-21
MX164971B (es) 1992-10-09
EP0354728A2 (en) 1990-02-14
NZ230200A (en) 1991-11-26
KR900002804A (ko) 1990-03-23
ZA895908B (en) 1991-04-24
CN1040205A (zh) 1990-03-07
AU619329B2 (en) 1992-01-23
PT91372A (pt) 1990-03-08
DK382989D0 (da) 1989-08-04

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