CO2017000363A2 - Inhibidores de la desmetilasa-1 específica de la lisina (lsd-1) derivados del [(5-carbonil)-1h-pirrol-3-il]-benzonitrilo o [(4-carbonil)imidazol-2-il]-benzonitrilo - Google Patents

Inhibidores de la desmetilasa-1 específica de la lisina (lsd-1) derivados del [(5-carbonil)-1h-pirrol-3-il]-benzonitrilo o [(4-carbonil)imidazol-2-il]-benzonitrilo

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Publication number
CO2017000363A2
CO2017000363A2 CONC2017/0000363A CO2017000363A CO2017000363A2 CO 2017000363 A2 CO2017000363 A2 CO 2017000363A2 CO 2017000363 A CO2017000363 A CO 2017000363A CO 2017000363 A2 CO2017000363 A2 CO 2017000363A2
Authority
CO
Colombia
Prior art keywords
benzonitrile
carbonyl
cancer
lysine
lsd
Prior art date
Application number
CONC2017/0000363A
Other languages
English (en)
Inventor
Toufike Kanouni
James Marvin Veal
Jeffrey Alan Stafford
Young K Chen
Zhe Nie
Original Assignee
Celgene Quanticel Res Inc
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 Celgene Quanticel Res Inc filed Critical Celgene Quanticel Res Inc
Publication of CO2017000363A2 publication Critical patent/CO2017000363A2/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/10Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)

Abstract

La presente invención se refiere en general a composiciones y métodos para tratar cáncer y enfermedad neoplásica. En este documento se proporcionan compuestos derivados heterocíclicos sustituidos y composiciones farmacéuticas que comprenden dichos compuestos. Los compuestos en cuestión y composiciones son útiles para la inhibición de la desmetilasa-1 específica de la lisina. Además, los compuestos en cuestión y composiciones son útiles para el tratamiento de cáncer, tales como cáncer de próstata, cáncer de mama, cáncer de vejiga, cáncer de pulmón y/o melanoma y similares.
CONC2017/0000363A 2014-07-03 2017-01-16 Inhibidores de la desmetilasa-1 específica de la lisina (lsd-1) derivados del [(5-carbonil)-1h-pirrol-3-il]-benzonitrilo o [(4-carbonil)imidazol-2-il]-benzonitrilo CO2017000363A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462020758P 2014-07-03 2014-07-03
PCT/US2015/038661 WO2016004105A1 (en) 2014-07-03 2015-06-30 Inhibitors of lysine specific demethylase-1

Publications (1)

Publication Number Publication Date
CO2017000363A2 true CO2017000363A2 (es) 2017-04-10

Family

ID=55019933

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2017/0000363A CO2017000363A2 (es) 2014-07-03 2017-01-16 Inhibidores de la desmetilasa-1 específica de la lisina (lsd-1) derivados del [(5-carbonil)-1h-pirrol-3-il]-benzonitrilo o [(4-carbonil)imidazol-2-il]-benzonitrilo

Country Status (18)

Country Link
US (3) US10414750B2 (es)
EP (1) EP3164509B1 (es)
JP (2) JP6525422B2 (es)
KR (1) KR102450671B1 (es)
CN (1) CN106604997B (es)
AU (1) AU2015284197B2 (es)
BR (1) BR112017000042B1 (es)
CA (1) CA2954060A1 (es)
CL (1) CL2016003423A1 (es)
CO (1) CO2017000363A2 (es)
EA (1) EA201790082A1 (es)
EC (1) ECSP17006776A (es)
ES (1) ES2905280T3 (es)
IL (1) IL249876B (es)
MX (1) MX2017000170A (es)
SG (1) SG11201700007YA (es)
WO (1) WO2016004105A1 (es)
ZA (1) ZA201700072B (es)

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RS64423B1 (sr) * 2014-07-03 2023-09-29 Celgene Quanticel Research Inc Inhibitori lizin specifične demetilaze-1
EP3307909A1 (en) 2015-06-12 2018-04-18 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
WO2017013061A1 (en) 2015-07-17 2017-01-26 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
IL261721B (en) 2016-03-15 2022-07-01 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of solid tumors
US11034991B2 (en) 2016-03-16 2021-06-15 Oryzon Genomics S.A. Methods to determine KDM1A target engagement and chemoprobes useful therefor
US10150754B2 (en) 2016-04-19 2018-12-11 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
EP3535420A1 (en) 2016-11-03 2019-09-11 Oryzon Genomics, S.A. Biomarkers for determining responsiveness to lsd1 inhibitors
CN110996949A (zh) 2017-08-03 2020-04-10 奥瑞泽恩基因组学股份有限公司 用于治疗行为改变的方法
AR112900A1 (es) * 2017-09-13 2019-12-26 Hanmi Pharm Ind Co Ltd Compuesto derivado de pirazol y uso de este
JP7535797B2 (ja) 2019-03-20 2024-08-19 オリソン ヘノミクス,ソシエダ アノニマ 化合物バフィデムスタット(vafidemstat)などkdm1a阻害剤を使用した注意欠陥多動性障害の処置方法
CN113613653A (zh) 2019-03-20 2021-11-05 奥莱松基因组股份有限公司 治疗边缘型人格障碍的方法
WO2021004610A1 (en) 2019-07-05 2021-01-14 Oryzon Genomics, S.A. Biomarkers and methods for personalized treatment of small cell lung cancer using kdm1a inhibitors
TW202304416A (zh) 2021-04-08 2023-02-01 西班牙商奧萊松基因組股份有限公司 用於治療骨髓癌的lsd1抑制劑的組合
WO2023217784A1 (en) 2022-05-09 2023-11-16 Oryzon Genomics, S.A. Methods of treating nf1-mutant tumors using lsd1 inhibitors
WO2023217758A1 (en) 2022-05-09 2023-11-16 Oryzon Genomics, S.A. Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors
WO2024110649A1 (en) 2022-11-24 2024-05-30 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors and menin inhibitors for treating cancer

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US20190194161A1 (en) 2019-06-27
US10414750B2 (en) 2019-09-17
US10626103B2 (en) 2020-04-21
EP3164509B1 (en) 2021-12-29
MX2017000170A (es) 2017-05-01
JP6833896B2 (ja) 2021-02-24
EA201790082A1 (ru) 2017-08-31
SG11201700007YA (en) 2017-01-27
IL249876A0 (en) 2017-03-30
WO2016004105A1 (en) 2016-01-07
ZA201700072B (en) 2018-04-25
EP3164509A4 (en) 2018-02-28
US20180265491A1 (en) 2018-09-20
BR112017000042B1 (pt) 2021-11-03
CN106604997A (zh) 2017-04-26
KR102450671B1 (ko) 2022-10-04
AU2015284197B2 (en) 2021-07-22
CN106604997B (zh) 2021-02-19
ECSP17006776A (es) 2017-03-31
IL249876B (en) 2020-06-30
US20190194162A1 (en) 2019-06-27
US10626104B2 (en) 2020-04-21
JP6525422B2 (ja) 2019-06-05
JP2017521407A (ja) 2017-08-03
KR20170027822A (ko) 2017-03-10
BR112017000042A2 (pt) 2018-07-17
ES2905280T3 (es) 2022-04-07
AU2015284197A1 (en) 2017-02-02
CA2954060A1 (en) 2016-01-07
JP2019172676A (ja) 2019-10-10
EP3164509A1 (en) 2017-05-10
CL2016003423A1 (es) 2017-11-10

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