AR110598A1 - PROPHARMS OF ACTIVE CYTOTOX PRINCIPLES WITH ENZYMATICALLY SCINDIBLE GROUPS - Google Patents

PROPHARMS OF ACTIVE CYTOTOX PRINCIPLES WITH ENZYMATICALLY SCINDIBLE GROUPS

Info

Publication number
AR110598A1
AR110598A1 ARP170100719A ARP170100719A AR110598A1 AR 110598 A1 AR110598 A1 AR 110598A1 AR P170100719 A ARP170100719 A AR P170100719A AR P170100719 A ARP170100719 A AR P170100719A AR 110598 A1 AR110598 A1 AR 110598A1
Authority
AR
Argentina
Prior art keywords
groups
active
scindible
propharms
cytotox
Prior art date
Application number
ARP170100719A
Other languages
Spanish (es)
Inventor
Berndt Sandra Dr
Sommer Anette Dr
Simone Greven
Mahlert Christoph Dr
Terjung Carsten Dr
Dietz Lisa Dr
Stelte-Ludwig Beatrix Dr
Wagner Sarah Dr
Leo Marx
Rebstock Anne Dr
- Dr Lerchen Hans-Georg Sophie
Original Assignee
Bayer Pharma 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
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of AR110598A1 publication Critical patent/AR110598A1/en

Links

Classifications

    • 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
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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
    • 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
    • A61K47/6845—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 cytokine, e.g. growth factors, VEGF, TNF, a lymphokine or an interferon
    • 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
    • A61K47/6849—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 receptor, a cell surface antigen or a cell surface determinant

Abstract

Profármacos o bien conjugados de la fórmula general (1), en los que se enmascaran los principios activos citotóxicos tales como, por ejemplo, inhibidores de la proteína del huso de la quinesina con grupos escindibles por legumaína y así liberan el principio activo, así como al uso de estos profármacos o conjugados para el tratamiento y/o la prevención de enfermedades, así como al uso de estos profármacos o bien conjugados para la preparación de medicamentos para el tratamiento y/o la prevención de enfermedades, en especial de enfermedades hiperproliferativas y/o angiogénicas tales como, por ejemplo, enfermedades cancerosas. Composición farmacéutica.Prodrugs or conjugates of the general formula (1), in which the cytotoxic active ingredients are masked such as, for example, inhibitors of the kinesin spindle protein with groups cleavable by legumaine and thus release the active principle, as well as to the use of these prodrugs or conjugates for the treatment and / or prevention of diseases, as well as to the use of these prodrugs or conjugates for the preparation of medicaments for the treatment and / or prevention of diseases, especially hyperproliferative diseases and / or angiogenic such as, for example, cancerous diseases. Pharmaceutical composition

ARP170100719A 2016-03-24 2017-03-23 PROPHARMS OF ACTIVE CYTOTOX PRINCIPLES WITH ENZYMATICALLY SCINDIBLE GROUPS AR110598A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP16162400 2016-03-24

Publications (1)

Publication Number Publication Date
AR110598A1 true AR110598A1 (en) 2019-04-17

Family

ID=55650218

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP170100719A AR110598A1 (en) 2016-03-24 2017-03-23 PROPHARMS OF ACTIVE CYTOTOX PRINCIPLES WITH ENZYMATICALLY SCINDIBLE GROUPS

Country Status (1)

Country Link
AR (1) AR110598A1 (en)

Similar Documents

Publication Publication Date Title
UY37168A (en) PROPHARMS OF ACTIVE CYTOTOX PRINCIPLES WITH ENZYMATICALLY SCINDIBLE GROUPS
CL2020000501A1 (en) Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp1) inhibitors and their uses.
CR20190318A (en) Benzooxazole derivatives as immunomodulators
SV2018005687A (en) DIHYDROIMIDAZOPIRAZINONA DERIVATIVES USED IN CANCER TREATMENT
SV2017005461A (en) BENZAMIDS REPLACED WITH 1,3-TIAZOL-2-ILO
BR112018015273A2 (en) benzimidazole derivatives as ror-gamma modulators
AR110419A1 (en) PROPHARMS OF ACTIVE CYTOTOX PRINCIPLES WITH ENZYMATICALLY SCINDIBLE GROUPS
ECSP18073366A (en) INDOLINE DERIVATIVES SUBSTITUTE AS INHIBITORS OF DENGUE VIRAL REPLICATION
ECSP18073293A (en) INDOLINE DERIVATIVES SUBSTITUTE AS INHIBITORS OF DENGUE VIRAL REPLICATION
SV2018005750A (en) DERIVATIVES OF INDOL COMPOUNDS REPLACED AS INHIBITORS OF THE VIRIC REPLICATION OF DENGUE
BR112013018920A2 (en) nanoparticle compositions, formulations thereof and their uses
ECSP109935A (en) PYRIMIDINE MORFOLINE DERIVATIVES USED IN DISEASES RELATED TO MTOR QUINASA AND / OR PI3K
CL2020000747A1 (en) Niraparib formulations.
BR112012021086A2 (en) pharmaceutical compositions of spiro-oxindole compound for topical administration and their use as therapeutic agents
AR096892A1 (en) A PHARMACEUTICAL COMBINATION FOR THE TREATMENT OF MELANOMA
UY38228A (en) TRIAZOLOPYRIMIDINE COMPOUNDS AND THEIR USE IN THE TREATMENT OF CANCER
ECSP14013275A (en) DERIVATIVES OF ESTRA-1,3,5 (10), 16-TETRAEN-3-CARBOXAMIDE, PROCEDURES FOR THEIR PREPARATION, PHARMACEUTICAL PREPARATIONS THAT CONTAIN THEM, AS WELL AS THEIR USE FOR THE PREPARATION OF MEDICINES
BR112015019412A8 (en) bace1 inhibitors, their uses, and pharmaceutical composition
CL2021001388A1 (en) Useful compounds in hiv therapy
BR112017006113A8 (en) Auristatin uses, pharmaceutical compositions, dosage forms for cancer treatment and kits.
CY1120602T1 (en) [1,2,4] TRIAZOLO [4,3-B] PYRIDAZINES FOR USE IN THE TREATMENT OF MULTIPLATERIC DISEASES
CU20200008A7 (en) SUBSTITUTE DIHYDROOXADIAZINONE COMPOUNDS USEFUL IN THE TREATMENT OF HYPERPROLIFERATIVE DISEASES, METHODS FOR PREPARING SUCH COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
ECSP19066134A (en) IMIDAZO [4,5-c] QUINOLIN-2-ONA DEUTERATED COMPOUNDS AND THEIR USE IN THE TREATMENT OF CANCER
PE20151607A1 (en) ORGANIC COMPOUND FORMULATIONS
BR112019007863A2 (en) innovative naphthyridinone derivatives and their use in the treatment of arrhythmia

Legal Events

Date Code Title Description
FB Suspension of granting procedure