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MX2018004696A - Analogos de epotilona, metodos de sintesis, metodos de tratamiento y conjugados con farmacos de los mismos. - Google Patents

Analogos de epotilona, metodos de sintesis, metodos de tratamiento y conjugados con farmacos de los mismos.

Info

Publication number
MX2018004696A
MX2018004696A MX2018004696A MX2018004696A MX2018004696A MX 2018004696 A MX2018004696 A MX 2018004696A MX 2018004696 A MX2018004696 A MX 2018004696A MX 2018004696 A MX2018004696 A MX 2018004696A MX 2018004696 A MX2018004696 A MX 2018004696A
Authority
MX
Mexico
Prior art keywords
methods
drug conjugates
synthesis
treatment
epothilone analogs
Prior art date
Application number
MX2018004696A
Other languages
English (en)
Inventor
C Nicolaou Kyriacos
Rhoades Derek
Wang Yanping
Totokotsopoulos Sotirios
Original Assignee
Univ Rice William M
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 Univ Rice William M filed Critical Univ Rice William M
Publication of MX2018004696A publication Critical patent/MX2018004696A/es

Links

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/428Thiazoles condensed with carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6835Medicinal 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
    • A61K47/6851Medicinal 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
    • A61K47/6869Medicinal 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 the tumour determinant being from a cell of the reproductive system: ovaria, uterus, testes, prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/06Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08Bridged systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Cell Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

En un aspecto, la presente invención se refiere a análogos de epotilona de la Fórmula (I), en donde las variables son como las aquí definidas. En otro aspecto, la presente invención también se refiere a métodos para la preparación de los compuestos aquí descritos. En otro aspecto, la presente invención se refiere también a composiciones farmacéuticas y a métodos de uso de los compuestos aquí descritos. Adicionalmente, también se proporcionan conjugados de fármacos con porciones de los compuestos que tienen como objetivo células.
MX2018004696A 2015-10-16 2016-10-14 Analogos de epotilona, metodos de sintesis, metodos de tratamiento y conjugados con farmacos de los mismos. MX2018004696A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562242702P 2015-10-16 2015-10-16
PCT/US2016/057093 WO2017066606A1 (en) 2015-10-16 2016-10-14 Epothilone analogs, methods of synthesis, methods of treatment, and drug conjugates thereof

Publications (1)

Publication Number Publication Date
MX2018004696A true MX2018004696A (es) 2018-11-29

Family

ID=58518025

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2018004696A MX2018004696A (es) 2015-10-16 2016-10-14 Analogos de epotilona, metodos de sintesis, metodos de tratamiento y conjugados con farmacos de los mismos.

Country Status (10)

Country Link
US (1) US10874646B2 (es)
EP (1) EP3371176A4 (es)
JP (1) JP2018534283A (es)
CN (1) CN108430996A (es)
AU (1) AU2016340093A1 (es)
BR (1) BR112018007673A2 (es)
CA (1) CA3002027A1 (es)
MA (1) MA43178A (es)
MX (1) MX2018004696A (es)
WO (1) WO2017066606A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL3976588T3 (pl) * 2019-10-18 2023-08-21 Fmc Corporation Sposoby wytwarzania kwasu 5-bromo-2-(3-chloropirydyn-2-ylo)-2h- pirazolo-3-karboksylowego
EP4045487A1 (en) * 2019-10-18 2022-08-24 Fmc Corporation Methods for the preparation of 5-bromo-2-(3-chloro-pyridin-2-yl)-2h-pyrazole-3-carboxylic acid
PL3976589T3 (pl) * 2019-10-18 2023-07-31 Fmc Corporation Sposoby wytwarzania kwasu 5-bromo-2-(3-chloropirydyn-2-ylo)-2H-pirazolo-3-karboksylowego

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6441186B1 (en) 1996-12-13 2002-08-27 The Scripps Research Institute Epothilone analogs
US6380394B1 (en) * 1996-12-13 2002-04-30 The Scripps Research Institute Epothilone analogs
US6399638B1 (en) 1998-04-21 2002-06-04 Bristol-Myers Squibb Company 12,13-modified epothilone derivatives
EP1161430A2 (de) 1999-02-11 2001-12-12 Schering Aktiengesellschaft Epothilon-derivate, verfahren zu deren herstellung und ihre pharmazeutische verwendung
AU772750C (en) 1999-04-30 2005-02-24 Schering Aktiengesellschaft 6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations
AU2006318284A1 (en) 2005-11-22 2007-05-31 The Scripps Research Institute Chemical synthesis of a highly potent epothilone
AR061181A1 (es) * 2006-05-25 2008-08-13 Bristol Myers Squibb Co Compuestos de aziridinil-epotilona
AR062448A1 (es) 2006-05-25 2008-11-12 Endocyte Inc Conjugados de analogos de aziridinil-epotilona y composiciones farmaceuticas que comprenden los mismos
EP1930004A1 (en) * 2006-12-08 2008-06-11 Bayer Schering Pharma Aktiengesellschaft Use of epothilones in the treatment of osteoporosis and related diseases
EP2009114A1 (en) * 2007-06-29 2008-12-31 Bayer Schering Pharma Aktiengesellschaft Methods, kits, and compounds for determining responsiveness to treatment of a pathological disorder by epothilones
CN101519404B (zh) 2008-02-29 2016-01-20 唐莉 15环噻酮衍生物及其制备方法与应用
WO2014096551A1 (en) * 2012-12-21 2014-06-26 Glykos Finland Oy Linker-payload molecule conjugates
US20140323533A1 (en) * 2013-04-29 2014-10-30 Bristol-Myers Squibb Company Combination of anti-ctla4 antibody with tubulin modulating agents for the treatment of proliferative diseases

Also Published As

Publication number Publication date
CN108430996A (zh) 2018-08-21
US10874646B2 (en) 2020-12-29
BR112018007673A2 (pt) 2018-11-06
AU2016340093A1 (en) 2018-05-10
EP3371176A4 (en) 2019-09-04
WO2017066606A1 (en) 2017-04-20
CA3002027A1 (en) 2017-04-20
EP3371176A1 (en) 2018-09-12
JP2018534283A (ja) 2018-11-22
US20190022069A1 (en) 2019-01-24
MA43178A (fr) 2018-09-12

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