WO2013024282A3 - Inhibitor or down- regulator of the expression of one or both of tbk1 ikk-epsilon for use in the treatment of pi3kinase dependent cancer - Google Patents

Inhibitor or down- regulator of the expression of one or both of tbk1 ikk-epsilon for use in the treatment of pi3kinase dependent cancer Download PDF

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Publication number
WO2013024282A3
WO2013024282A3 PCT/GB2012/051978 GB2012051978W WO2013024282A3 WO 2013024282 A3 WO2013024282 A3 WO 2013024282A3 GB 2012051978 W GB2012051978 W GB 2012051978W WO 2013024282 A3 WO2013024282 A3 WO 2013024282A3
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WO
WIPO (PCT)
Prior art keywords
tbk1
regulator
inhibitor
expression
pi3kinase
Prior art date
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PCT/GB2012/051978
Other languages
French (fr)
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WO2013024282A2 (en
Inventor
Gary Newton
Trevor Perrior
Alan Ashworth
Christopher James LORD
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Domainex Limited
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Publication of WO2013024282A2 publication Critical patent/WO2013024282A2/en
Publication of WO2013024282A3 publication Critical patent/WO2013024282A3/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/713—Double-stranded nucleic acids or oligonucleotides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Abstract

The invention provides a compound that is an inhibitor of one or both of TBK1 and IKKε, or a down-regulator of the expression of one or both of TBK1 and IKKε, for use in a method of treating a cancer that is dependent on the PI3kinase pathway. The invention further provides a method of treating cancer in an individual in whom the cancer is dependent on the PI3kinase pathway, comprising administering to the individual a compound that is an inhibitor of one or both of TBK1 and IKKε, or a down-regulator of the expression of one or both of TBK1 and IKKε.
PCT/GB2012/051978 2011-08-15 2012-08-14 Compounds and their uses WO2013024282A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1114051.4A GB201114051D0 (en) 2011-08-15 2011-08-15 Compounds and their uses
GB1114051.4 2011-08-15

Publications (2)

Publication Number Publication Date
WO2013024282A2 WO2013024282A2 (en) 2013-02-21
WO2013024282A3 true WO2013024282A3 (en) 2013-05-16

Family

ID=44764528

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB2012/051978 WO2013024282A2 (en) 2011-08-15 2012-08-14 Compounds and their uses

Country Status (2)

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GB (1) GB201114051D0 (en)
WO (1) WO2013024282A2 (en)

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ES2951688T3 (en) 2011-02-28 2023-10-24 Epizyme Inc 6,5-Substituted Fused Bicyclic Heteroaryl Compounds
SG10201704095UA (en) 2012-04-24 2017-06-29 Vertex Pharma Dna-pk inhibitors
GB201303109D0 (en) * 2013-02-21 2013-04-10 Domainex Ltd Novel pyrimidine compounds
TR201901886T4 (en) 2013-03-12 2019-03-21 Vertex Pharma DNA-PK inhibitors.
WO2014151630A2 (en) 2013-03-15 2014-09-25 Irm Llc Compounds and compositions for the treatment of parasitic diseases
US9186361B2 (en) 2013-03-15 2015-11-17 Novartis Ag Compounds and compositions for the treatment of parasitic diseases
US9296754B2 (en) 2013-03-15 2016-03-29 Novartis Ag Compounds and compositions for the treatment of parasitic diseases
US9206188B2 (en) 2013-04-18 2015-12-08 Arrien Pharmaceuticals Llc Substituted pyrrolo[2,3-b]pyridines as ITK and JAK inhibitors
CA2953747A1 (en) 2013-06-28 2014-12-31 Auckland Uniservices Limited Amino acid and peptide conjugates and conjugation process
PL3057953T3 (en) 2013-10-17 2019-01-31 Vertex Pharmaceuticals Incorporated Co-crystals of (s)-n-methyl-8-(1-((2'-methyl-[4,5'-bipyrimidin]-6-yl)amino)propan-2-yl)quinoline-4-carboxamide and deuterated derivatives thereof as dna-pk inhibitors
PT3083627T (en) 2013-12-19 2018-11-30 Novartis Ag [1,2,4]triazolo[1,5-a]pyrimidine derivatives as protozoan proteasome inhibitors for the treatment of parasitic diseases such as leishmaniasis
JP2017503026A (en) 2014-01-15 2017-01-26 サントル ナシオナル ドゥ ラ ルシェルシュ シアンティフィーク（セーエヌエールエス） Water-soluble 4-azapodophyllotoxin analog
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
CN106715419A (en) 2014-09-26 2017-05-24 吉利德科学公司 Aminotriazine derivatives useful as TANK-binding kinase inhibitor compounds
US10253062B2 (en) 2014-12-23 2019-04-09 Margaret Anne Brimble Amino acid and peptide conjugates and uses thereof
BR112017002594A2 (en) 2015-12-17 2017-12-19 Gilead Sciences Inc tank binding kinase inhibitor compounds
US10894784B2 (en) 2015-12-18 2021-01-19 Bayer Pharma Aktiengesellschaft Heteroarylbenzimidazole compounds
KR20180128915A (en) 2016-02-26 2018-12-04 오클랜드 유니서비시즈 리미티드 Amino acid and peptide conjugates and methods of conjugation
WO2017207534A1 (en) 2016-06-03 2017-12-07 Bayer Pharma Aktiengesellschaft Substituted heteroarylbenzimidazole compounds
DE102016113714A1 (en) 2016-07-26 2018-02-01 Rosa Karl Transfection procedure with non-viral gene delivery systems
TW201815418A (en) 2016-09-27 2018-05-01 Vertex Pharma Method for treating cancer using a combination of DNA-damaging agents and DNA-PK inhibitors
GB201702947D0 (en) 2017-02-23 2017-04-12 Domainex Ltd Novel compounds
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GB201114051D0 (en) 2011-09-28
WO2013024282A2 (en) 2013-02-21

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