CA3078579A1 - Pyrimidine tbk/ikk.epsilon. inhibitor compounds and uses thereof - Google Patents

Pyrimidine tbk/ikk.epsilon. inhibitor compounds and uses thereof Download PDF

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Publication number
CA3078579A1
CA3078579A1 CA3078579A CA3078579A CA3078579A1 CA 3078579 A1 CA3078579 A1 CA 3078579A1 CA 3078579 A CA3078579 A CA 3078579A CA 3078579 A CA3078579 A CA 3078579A CA 3078579 A1 CA3078579 A1 CA 3078579A1
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CA
Canada
Prior art keywords
compound
yloxy
methoxy
oxan
amino
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CA3078579A
Other languages
English (en)
French (fr)
Inventor
Srinivasa R. Karra
Yufang Xiao
Brian A. Sherer
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.)
Merck Patent GmbH
Original Assignee
Merck Patent GmbH
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 Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of CA3078579A1 publication Critical patent/CA3078579A1/en
Pending legal-status Critical Current

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Classifications

    • 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • 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
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Emergency Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA3078579A 2017-10-17 2018-10-17 Pyrimidine tbk/ikk.epsilon. inhibitor compounds and uses thereof Pending CA3078579A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762573251P 2017-10-17 2017-10-17
US62/573,251 2017-10-17
PCT/US2018/056190 WO2019079373A1 (en) 2017-10-17 2018-10-17 PYRIMIDINE TBK / IKKε INHIBITORY COMPOUNDS AND USES THEREOF

Publications (1)

Publication Number Publication Date
CA3078579A1 true CA3078579A1 (en) 2019-04-25

Family

ID=64110185

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3078579A Pending CA3078579A1 (en) 2017-10-17 2018-10-17 Pyrimidine tbk/ikk.epsilon. inhibitor compounds and uses thereof

Country Status (14)

Country Link
US (1) US20230019491A1 (enExample)
EP (1) EP3697772A1 (enExample)
JP (1) JP7266592B2 (enExample)
KR (1) KR20200072519A (enExample)
CN (1) CN111247135A (enExample)
AU (1) AU2018352699A1 (enExample)
BR (1) BR112020007466A2 (enExample)
CA (1) CA3078579A1 (enExample)
IL (1) IL273891A (enExample)
MX (1) MX2020003507A (enExample)
RU (1) RU2020115596A (enExample)
SG (1) SG11202003407VA (enExample)
TW (1) TWI802604B (enExample)
WO (1) WO2019079373A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3078583A1 (en) * 2017-10-17 2019-04-25 Merck Patent Gmbh Pyrimidine tbk/ikk.epsilon. inhibitor compounds and uses thereof
JP7359783B2 (ja) 2018-06-05 2023-10-11 クリネティックス ファーマシューティカルズ,インク. メラノコルチンサブタイプ-2受容体(mc2r)アンタゴニストおよびその使用
CN112552280A (zh) * 2019-09-25 2021-03-26 常州强力先端电子材料有限公司 一种高产酸的磺酰亚胺类光产酸剂
JP7657792B2 (ja) * 2019-11-07 2025-04-07 クリネティックス ファーマシューティカルズ,インク. メラノコルチンサブタイプ-2受容体(mc2r)アンタゴニストおよびその使用
PT4077307T (pt) 2019-12-18 2025-06-03 Crinetics Pharmaceuticals Inc Antagonistas do recetor de subtipo 2 da melanocortina (mc2r) à base de piperidina gem-dissubstituída e suas utilizações
JP7651574B2 (ja) 2019-12-23 2025-03-26 クリネティックス ファーマシューティカルズ,インク. スピロ環式ピペリジンメラノコルチンサブタイプ-2受容体(mc2r)アンタゴニストおよびその使用
IL305952A (en) 2021-03-19 2023-11-01 Crinetics Pharmaceuticals Inc Melanocortin subtype 2 receptor (MC2R) antagonist for disease treatment
CN117447407B (zh) * 2023-12-19 2024-06-11 潍坊医学院 一种JAK2抑制剂Pacritinib及其中间体的制备方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2911139A1 (fr) * 2007-01-05 2008-07-11 Sanofi Aventis Sa Nouveaux derives de phenyl-(4-phenyl-pyrimidin-2-yl)amines, leur preparation a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de ikk
ES2535166T3 (es) * 2007-09-04 2015-05-06 The Scripps Research Institute Pirimidinil-aminas sustituidas como inhibidores de proteína-quinasas
CN102791697A (zh) * 2009-10-12 2012-11-21 瑞科西有限公司 作为TBKL和/或IKKε抑制剂的氨基-嘧啶化合物
GB201012105D0 (en) 2010-07-19 2010-09-01 Domainex Ltd Novel pyrimidine compounds
BR112013026202A2 (pt) * 2011-04-12 2017-07-25 Myrexis Inc composições e usos terapêuticos de inibidores quinase epsilon relacionado a ikk e quinase i de ligação a tank
DE102011112978A1 (de) 2011-09-09 2013-03-14 Merck Patent Gmbh Benzonitrilderivate
JP2018524350A (ja) * 2015-06-29 2018-08-30 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung TBK/IKKε阻害剤化合物及びその用途

Also Published As

Publication number Publication date
CN111247135A (zh) 2020-06-05
BR112020007466A2 (pt) 2020-09-24
RU2020115596A (ru) 2021-11-18
JP2020537671A (ja) 2020-12-24
US20230019491A1 (en) 2023-01-19
IL273891A (en) 2020-05-31
AU2018352699A1 (en) 2020-05-28
SG11202003407VA (en) 2020-05-28
WO2019079373A1 (en) 2019-04-25
TWI802604B (zh) 2023-05-21
MX2020003507A (es) 2020-07-22
KR20200072519A (ko) 2020-06-22
TW201922735A (zh) 2019-06-16
JP7266592B2 (ja) 2023-04-28
RU2020115596A3 (enExample) 2021-11-18
EP3697772A1 (en) 2020-08-26

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