PE20181025A1 - Inhibidores de ezh2 - Google Patents

Inhibidores de ezh2

Info

Publication number
PE20181025A1
PE20181025A1 PE2018000313A PE2018000313A PE20181025A1 PE 20181025 A1 PE20181025 A1 PE 20181025A1 PE 2018000313 A PE2018000313 A PE 2018000313A PE 2018000313 A PE2018000313 A PE 2018000313A PE 20181025 A1 PE20181025 A1 PE 20181025A1
Authority
PE
Peru
Prior art keywords
methyl
compounds
cyclohexyl
ethyl
refers
Prior art date
Application number
PE2018000313A
Other languages
English (en)
Inventor
Esteban Dominguez
Deqi Guo
Mary Margaret Mader
Anh-Quan Hannah Nguyen
Prado Miriam Filadelfa Del
Michael Enrico Richett
Michael John Rodriguez
Yvonne Yee Mai Yip
Kuo-Long Yu
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of PE20181025A1 publication Critical patent/PE20181025A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/28Compounds containing heavy metals
    • A61K31/282Platinum compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • A61K33/24Heavy metals; Compounds thereof
    • A61K33/243Platinum; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Inorganic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Epoxy Compounds (AREA)

Abstract

Se refiere a compuestos que inhiben la actividad de la histona lisina metiltransferasa, potenciador del homologo de Zeste 2 (EZH2), donde: X es -CH2- o -CH2-CH2-; Y' es -NR4R5, -CH(CH3)-ciclohexil-4-il-N-metil-N-metoxietilo, entre otros; R4 es ciclohex-4-il sustituido con N-metil-N-metoxietilamino, N-metil-N-ciclopropilamino, entre otros; R5 es metilo o etilo; R6 es metilo o cloro. Tambien se refiere a una composicion y a una combinacion que comprende a dichos compuestos. Un compuesto preferido es 5-[(4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)metil]-2-{(1R)-1-[4-(3-metoxiazetidin-1-il)ciclohexil]etil}-3-metil-5,6,7,8-tetrahidro-4H-tieno[3,2-c]azepin-4-ona. Dichos compuestos son utiles para el tratamiento del cancer tales como cancer de ovario, gastrico, colorrectal, entre otros
PE2018000313A 2015-08-27 2016-08-22 Inhibidores de ezh2 PE20181025A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP15382433 2015-08-27
EP15382615 2015-12-11

Publications (1)

Publication Number Publication Date
PE20181025A1 true PE20181025A1 (es) 2018-06-27

Family

ID=56801893

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2018000313A PE20181025A1 (es) 2015-08-27 2016-08-22 Inhibidores de ezh2

Country Status (31)

Country Link
US (1) US9718838B2 (es)
EP (1) EP3341379B1 (es)
JP (1) JP6704040B2 (es)
KR (1) KR20180030704A (es)
CN (1) CN107922434B (es)
AU (1) AU2016313541A1 (es)
BR (1) BR112018003108A2 (es)
CA (1) CA2994428A1 (es)
CO (1) CO2018002033A2 (es)
CR (1) CR20180104A (es)
CY (1) CY1122364T1 (es)
DK (1) DK3341379T3 (es)
DO (1) DOP2018000058A (es)
EC (1) ECSP18014798A (es)
ES (1) ES2756603T3 (es)
HR (1) HRP20192101T1 (es)
HU (1) HUE047630T2 (es)
IL (1) IL257061A (es)
LT (1) LT3341379T (es)
MD (1) MD3341379T2 (es)
ME (1) ME03650B (es)
MX (1) MX2018002484A (es)
PE (1) PE20181025A1 (es)
PH (1) PH12018500423A1 (es)
PL (1) PL3341379T3 (es)
PT (1) PT3341379T (es)
RS (1) RS59615B1 (es)
SI (1) SI3341379T1 (es)
TN (1) TN2018000058A1 (es)
TW (1) TW201718598A (es)
WO (1) WO2017035060A1 (es)

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Also Published As

Publication number Publication date
CR20180104A (es) 2018-04-24
KR20180030704A (ko) 2018-03-23
DOP2018000058A (es) 2018-03-30
AU2016313541A1 (en) 2018-02-15
ECSP18014798A (es) 2018-04-30
CA2994428A1 (en) 2017-03-02
BR112018003108A2 (pt) 2018-09-25
MX2018002484A (es) 2018-06-15
IL257061A (en) 2018-03-29
RS59615B1 (sr) 2020-01-31
JP6704040B2 (ja) 2020-06-03
CN107922434A (zh) 2018-04-17
DK3341379T3 (da) 2019-12-02
WO2017035060A1 (en) 2017-03-02
ME03650B (me) 2020-07-20
PH12018500423A1 (en) 2018-08-29
US9718838B2 (en) 2017-08-01
JP2018530527A (ja) 2018-10-18
HUE047630T2 (hu) 2021-12-28
PL3341379T3 (pl) 2020-05-18
EP3341379B1 (en) 2019-10-09
CO2018002033A2 (es) 2018-05-21
ES2756603T3 (es) 2020-04-27
TN2018000058A1 (en) 2019-07-08
CY1122364T1 (el) 2021-01-27
LT3341379T (lt) 2019-12-10
SI3341379T1 (sl) 2019-11-29
TW201718598A (zh) 2017-06-01
US20170066780A1 (en) 2017-03-09
HRP20192101T1 (hr) 2020-02-21
EP3341379A1 (en) 2018-07-04
MD3341379T2 (ro) 2020-01-31
PT3341379T (pt) 2019-12-16
CN107922434B (zh) 2020-06-19

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