CA3041643A1 - 2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of dhodh - Google Patents

2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of dhodh Download PDF

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Publication number
CA3041643A1
CA3041643A1 CA3041643A CA3041643A CA3041643A1 CA 3041643 A1 CA3041643 A1 CA 3041643A1 CA 3041643 A CA3041643 A CA 3041643A CA 3041643 A CA3041643 A CA 3041643A CA 3041643 A1 CA3041643 A1 CA 3041643A1
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Prior art keywords
group
alkyl
fluoro
oxo
dihydro
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Pending
Application number
CA3041643A
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English (en)
French (fr)
Inventor
Stefan Nikolaus Gradl
Duy Nguyen
Knut Eis
Judith Gunther
Timo Stellfeld
Andreas Janzer
Sven Christian
Thomas Mueller
Sherif El Sheikh
Han Jie Zhou
Changjia ZHAO
David Brian Sykes
Steven James Ferrara
Kery LIU
Michael Krober
Claudia MERZ
Michael Niehues
Martina Schafer
Katja Zimmermann
Carl Friedrich Nising
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer AG
Bayer Pharma AG
General Hospital Corp
Broad Institute Inc
Harvard University
Original Assignee
Bayer AG
Bayer Pharma AG
General Hospital Corp
Broad Institute Inc
Harvard University
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Application filed by Bayer AG, Bayer Pharma AG, General Hospital Corp, Broad Institute Inc, Harvard University filed Critical Bayer AG
Publication of CA3041643A1 publication Critical patent/CA3041643A1/en
Pending legal-status Critical Current

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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
    • C07D401/12Heterocyclic 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
    • 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
    • A61K31/41961,2,4-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/101,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D249/12Oxygen or sulfur 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
    • 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
    • C07D405/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
CA3041643A 2016-10-27 2017-10-25 2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of dhodh Pending CA3041643A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CNPCT/CN2016/103643 2016-10-27
CNPCT/CN2016/103643 2016-10-27
US201762569296P 2017-10-06 2017-10-06
US62569296 2017-10-06
PCT/EP2017/077252 WO2018077923A1 (en) 2016-10-27 2017-10-25 2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of dhodh

Publications (1)

Publication Number Publication Date
CA3041643A1 true CA3041643A1 (en) 2018-05-03

Family

ID=60164720

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Application Number Title Priority Date Filing Date
CA3041643A Pending CA3041643A1 (en) 2016-10-27 2017-10-25 2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of dhodh

Country Status (26)

Country Link
US (4) US10815215B2 (enExample)
EP (1) EP3532468B1 (enExample)
JP (1) JP7084389B2 (enExample)
KR (1) KR20190084954A (enExample)
CN (2) CN110023302B (enExample)
AU (1) AU2017351688B2 (enExample)
BR (1) BR112019008458A2 (enExample)
CA (1) CA3041643A1 (enExample)
CL (1) CL2019001160A1 (enExample)
CO (1) CO2019004137A2 (enExample)
CR (1) CR20190212A (enExample)
CU (1) CU24572B1 (enExample)
DO (1) DOP2019000110A (enExample)
EC (1) ECSP19030002A (enExample)
GE (1) GEP20217248B (enExample)
IL (1) IL266214B (enExample)
JO (1) JOP20190094A1 (enExample)
MX (1) MX382665B (enExample)
NI (1) NI201900041A (enExample)
PE (1) PE20191005A1 (enExample)
PH (1) PH12019500932A1 (enExample)
TN (1) TN2019000136A1 (enExample)
TW (1) TW201827414A (enExample)
UA (1) UA123688C2 (enExample)
UY (1) UY37461A (enExample)
WO (1) WO2018077923A1 (enExample)

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JP7126556B2 (ja) 2018-09-28 2022-08-26 富士フイルム株式会社 シタラビンを含む抗腫瘍剤、シタラビンと併用される抗腫瘍効果増強剤、抗腫瘍用キット、およびシタラビンと併用される抗腫瘍剤
EP3898597A1 (en) 2018-12-21 2021-10-27 Les Laboratoires Servier SAS Crystalline and salt forms of an organic compound and pharmaceutical compositions thereof
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CN114222732B (zh) * 2019-10-28 2023-04-04 南京明德新药研发有限公司 一种尿酸促排剂及其合成方法和其在医药上的应用
JP2023513496A (ja) * 2020-02-04 2023-03-31 ヤンセン バイオテツク,インコーポレーテツド ジヒドロオロト酸デヒドロゲナーゼ阻害剤としての複素環式化合物
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JP7084389B2 (ja) 2022-06-14
NI201900041A (es) 2019-06-11
MX2019005009A (es) 2019-08-12
TN2019000136A1 (en) 2020-10-05
CN115557907B (zh) 2024-12-06
PE20191005A1 (es) 2019-07-15
PH12019500932A1 (en) 2020-01-20
EP3532468B1 (en) 2022-03-23
US11130745B2 (en) 2021-09-28
TW201827414A (zh) 2018-08-01
US20230365524A1 (en) 2023-11-16
WO2018077923A1 (en) 2018-05-03
US12486248B2 (en) 2025-12-02
CN110023302A (zh) 2019-07-16
IL266214A (en) 2019-06-30
CU24572B1 (es) 2022-01-13
DOP2019000110A (es) 2019-05-31
CU20190045A7 (es) 2019-12-03
ECSP19030002A (es) 2019-05-31
KR20190084954A (ko) 2019-07-17
EP3532468A1 (en) 2019-09-04
US20200377472A1 (en) 2020-12-03
BR112019008458A2 (pt) 2019-07-09
JP2019533694A (ja) 2019-11-21
CN115557907A (zh) 2023-01-03
GEP20217248B (en) 2021-04-26
JOP20190094A1 (ar) 2019-04-25
CR20190212A (es) 2019-06-24
US20210188805A9 (en) 2021-06-24
US20200123129A1 (en) 2020-04-23
US10815215B2 (en) 2020-10-27
US20220135536A1 (en) 2022-05-05
IL266214B (en) 2021-10-31
CL2019001160A1 (es) 2019-09-13
US11713304B2 (en) 2023-08-01
UA123688C2 (uk) 2021-05-12
UY37461A (es) 2018-05-31
CO2019004137A2 (es) 2019-05-10
MX382665B (es) 2025-03-13
CN110023302B (zh) 2022-07-26
AU2017351688B2 (en) 2022-02-03
AU2017351688A1 (en) 2019-04-11

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