MX2017009145A - Dimeros de benzodiazepina, conjugados de estos, y sus metodos de preparacion y uso. - Google Patents

Dimeros de benzodiazepina, conjugados de estos, y sus metodos de preparacion y uso.

Info

Publication number
MX2017009145A
MX2017009145A MX2017009145A MX2017009145A MX2017009145A MX 2017009145 A MX2017009145 A MX 2017009145A MX 2017009145 A MX2017009145 A MX 2017009145A MX 2017009145 A MX2017009145 A MX 2017009145A MX 2017009145 A MX2017009145 A MX 2017009145A
Authority
MX
Mexico
Prior art keywords
conjugates
making
methods
benzodiazepine dimers
dimers
Prior art date
Application number
MX2017009145A
Other languages
English (en)
Inventor
Gangwar Sanjeev
S Chowdari Naidu
Zhang Yong
N Huynh Tram
M Mcdonald Ivar
M Borzilleri Robert
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of MX2017009145A publication Critical patent/MX2017009145A/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
    • 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
    • A61K47/6843—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 material from animals or humans
    • 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
    • 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
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/30—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/70—Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
    • C07K2317/76—Antagonist effect on antigen, e.g. neutralization or inhibition of binding

Abstract

Dímeros de benzodiazepina que tienen una estructura representada por (ver Fórmula) en donde R1 es (ver Fórmulas) en donde las variables en las Fórmulas (I), (la) y (Ib) son como se definen en la solicitud. Estos dímeros son útiles como agentes antineoplásicos, en especial, cuando se usan en un conjugado anticuerpo-fármaco (ADC, por sus siglas en Inglés).
MX2017009145A 2015-01-14 2016-01-13 Dimeros de benzodiazepina, conjugados de estos, y sus metodos de preparacion y uso. MX2017009145A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562103157P 2015-01-14 2015-01-14
US201562215928P 2015-09-09 2015-09-09
PCT/US2016/013136 WO2016115191A1 (en) 2015-01-14 2016-01-13 Benzodiazepine dimers, conjugates thereof, and methods of making and using

Publications (1)

Publication Number Publication Date
MX2017009145A true MX2017009145A (es) 2017-11-22

Family

ID=55305072

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2017009145A MX2017009145A (es) 2015-01-14 2016-01-13 Dimeros de benzodiazepina, conjugados de estos, y sus metodos de preparacion y uso.

Country Status (19)

Country Link
US (4) US9527871B2 (es)
EP (1) EP3245213B1 (es)
JP (1) JP6498773B2 (es)
KR (1) KR20170102980A (es)
CN (1) CN107428780B (es)
AU (1) AU2016206798A1 (es)
BR (1) BR112017014599A2 (es)
CA (1) CA2973354A1 (es)
CL (1) CL2017001824A1 (es)
CO (1) CO2017008078A2 (es)
EA (1) EA201791550A1 (es)
ES (1) ES2783624T3 (es)
IL (1) IL253402A0 (es)
MX (1) MX2017009145A (es)
PE (1) PE20171184A1 (es)
SG (1) SG11201705646XA (es)
TW (1) TW201632531A (es)
WO (1) WO2016115191A1 (es)
ZA (1) ZA201704738B (es)

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Also Published As

Publication number Publication date
EP3245213A1 (en) 2017-11-22
US10112975B2 (en) 2018-10-30
EP3245213B1 (en) 2020-03-04
US9676794B2 (en) 2017-06-13
US9822144B2 (en) 2017-11-21
CA2973354A1 (en) 2016-07-21
US9527871B2 (en) 2016-12-27
KR20170102980A (ko) 2017-09-12
SG11201705646XA (en) 2017-08-30
JP2018503639A (ja) 2018-02-08
CN107428780B (zh) 2020-09-04
PE20171184A1 (es) 2017-08-22
TW201632531A (zh) 2016-09-16
CN107428780A (zh) 2017-12-01
JP6498773B2 (ja) 2019-04-10
CL2017001824A1 (es) 2018-02-09
IL253402A0 (en) 2017-09-28
CO2017008078A2 (es) 2017-11-10
ZA201704738B (en) 2019-02-27
AU2016206798A1 (en) 2017-08-31
US20180079781A1 (en) 2018-03-22
WO2016115191A1 (en) 2016-07-21
US20170073357A1 (en) 2017-03-16
ES2783624T3 (es) 2020-09-17
BR112017014599A2 (pt) 2018-01-16
US20160200742A1 (en) 2016-07-14
EA201791550A1 (ru) 2017-11-30
US20170233436A1 (en) 2017-08-17

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