CA2887435A1 - Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors - Google Patents

Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors Download PDF

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Publication number
CA2887435A1
CA2887435A1 CA 2887435 CA2887435A CA2887435A1 CA 2887435 A1 CA2887435 A1 CA 2887435A1 CA 2887435 CA2887435 CA 2887435 CA 2887435 A CA2887435 A CA 2887435A CA 2887435 A1 CA2887435 A1 CA 2887435A1
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CA
Canada
Prior art keywords
alkyl
hydrogen
polyhaloalkyl
independently selected
monohaloalkyl
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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.)
Abandoned
Application number
CA 2887435
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English (en)
French (fr)
Inventor
Hariprasad Vankayalapati
Venkataswamy SORNA
Steven L. Warner
David J. Bearss
Sunil Sharma
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.)
University of Utah Research Foundation Inc
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University of Utah Research Foundation Inc
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Publication date
Application filed by University of Utah Research Foundation Inc filed Critical University of Utah Research Foundation Inc
Publication of CA2887435A1 publication Critical patent/CA2887435A1/en
Abandoned legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epidemiology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA 2887435 2012-10-04 2013-10-04 Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors Abandoned CA2887435A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261709519P 2012-10-04 2012-10-04
US61/709,519 2012-10-04
PCT/US2013/063549 WO2014055928A2 (en) 2012-10-04 2013-10-04 Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors

Publications (1)

Publication Number Publication Date
CA2887435A1 true CA2887435A1 (en) 2014-04-10

Family

ID=50435582

Family Applications (1)

Application Number Title Priority Date Filing Date
CA 2887435 Abandoned CA2887435A1 (en) 2012-10-04 2013-10-04 Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors

Country Status (7)

Country Link
US (2) US9828376B2 (enExample)
EP (2) EP2903972B1 (enExample)
JP (1) JP6401169B2 (enExample)
KR (1) KR102194611B1 (enExample)
CN (1) CN104822664B (enExample)
CA (1) CA2887435A1 (enExample)
WO (1) WO2014055928A2 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2694486B1 (en) 2011-04-01 2018-01-10 University of Utah Research Foundation Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors
JP6313772B2 (ja) 2012-10-04 2018-04-18 ユニヴァーシティー オブ ユタ リサーチ ファウンデーション チロシン受容体キナーゼｂｔｋ阻害剤である置換ｎ−（３−（ピリミジン−４−イル）フェニル）アクリルアミド類似体
KR102194611B1 (ko) * 2012-10-04 2020-12-23 유니버시티 오브 유타 리서치 파운데이션 티로신 수용체 키나아제 btk 억제제로서 치환된 n-(3-(피리미딘-4-일)페닐)아크릴아미드 유사체
US9512084B2 (en) 2013-11-29 2016-12-06 Novartis Ag Amino pyrimidine derivatives
CN105712998B (zh) * 2014-12-05 2019-12-13 上海润诺生物科技有限公司 氮杂吲哚类衍生物、其制备方法及其在医药上的应用
CA3108065C (en) 2018-07-31 2025-10-07 Loxo Oncology, Inc. SPRAY-DRIED DISPERSIONS, FORMULATIONS AND POLYMORPHIES OF (S)-5-AMINO-3-(4-((5-FLUORO-2-METHOXYBENZAMIDO)METHYL)PHENYL)(1,1,1-TRIFLUOROPROPANE-2-YL)-1H-PYRAZOLE-4-CARBOXAMIDE
US12157730B2 (en) 2019-03-19 2024-12-03 Voronoi Inc. Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component
JP7109013B2 (ja) 2019-03-19 2022-07-29 ボロノイ インコーポレイテッド ヘテロアリール誘導体、ヘテロアリール誘導体の生成方法、およびヘテロアリール誘導体を有効成分として含む医薬組成物
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
IL296921B1 (en) * 2020-04-15 2026-08-01 Pyramid Biosciences Inc Methods for preparing receptor tyrosine kinase inhibitors
WO2022236255A2 (en) * 2021-05-03 2022-11-10 Nuvation Bio Inc. Heterocyclic compounds as kinase inhibitors
US20250171462A1 (en) * 2022-03-02 2025-05-29 Nico Therapeutics, Inc. Compounds, compositions, and methods

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GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
GB9924862D0 (en) 1999-10-20 1999-12-22 Celltech Therapeutics Ltd Chemical compounds
EP1648875A1 (en) * 2003-07-30 2006-04-26 Cyclacel Limited 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors
CA2561311A1 (en) 2004-04-09 2005-10-27 Merck & Co., Inc. Inhibitors of akt activity
US8133900B2 (en) 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
WO2007053452A1 (en) 2005-11-01 2007-05-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
EA200870217A1 (ru) * 2006-01-30 2009-02-27 Экселиксис, Инк. 4-арил-2-аминопиримидины или 4-арил-2-аминоалкилпиримидины в качестве модуляторов jak-2 и содержащие их фармацевтические композиции
CA2686378C (en) 2007-05-04 2012-07-24 Irm Llc Pyrimidine derivatives and compositions as c-kit and pdgfr kinase inhibitors
EP2200436B1 (en) 2007-09-04 2015-01-21 The Scripps Research Institute Substituted pyrimidinyl-amines as protein kinase inhibitors
US8338439B2 (en) * 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
AU2009262068C1 (en) * 2008-06-27 2015-07-02 Celgene Car Llc Heteroaryl compounds and uses thereof
US8426428B2 (en) 2008-12-05 2013-04-23 Principia Biopharma, Inc. EGFR kinase knockdown via electrophilically enhanced inhibitors
PL2389372T3 (pl) 2009-01-23 2016-02-29 Rigel Pharmaceuticals Inc Kompozycje i sposoby hamowania szlaku JAK
SG172857A1 (en) 2009-02-09 2011-08-29 Supergen Inc Pyrrolopyrimidinyl axl kinase inhibitors
KR101705158B1 (ko) * 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
US7741330B1 (en) 2009-10-12 2010-06-22 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase
EP2694486B1 (en) 2011-04-01 2018-01-10 University of Utah Research Foundation Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors
EP3628665B1 (en) 2011-04-01 2022-11-02 University of Utah Research Foundation Substituted n-phenylpyrimidin-2-amine analogs as inhibitors of the axl kinase
EP2788000B1 (en) 2011-12-06 2018-05-30 Merck Sharp & Dohme Corp. Pyrrolopyrimidines as janus kinase inhibitors
KR102194611B1 (ko) 2012-10-04 2020-12-23 유니버시티 오브 유타 리서치 파운데이션 티로신 수용체 키나아제 btk 억제제로서 치환된 n-(3-(피리미딘-4-일)페닐)아크릴아미드 유사체
JP6313772B2 (ja) 2012-10-04 2018-04-18 ユニヴァーシティー オブ ユタ リサーチ ファウンデーション チロシン受容体キナーゼｂｔｋ阻害剤である置換ｎ−（３−（ピリミジン−４−イル）フェニル）アクリルアミド類似体

Also Published As

Publication number Publication date
KR102194611B1 (ko) 2020-12-23
US20150252048A1 (en) 2015-09-10
EP2903972A2 (en) 2015-08-12
EP2903972B1 (en) 2019-12-04
WO2014055928A2 (en) 2014-04-10
WO2014055928A3 (en) 2014-06-26
KR20150067759A (ko) 2015-06-18
EP2903972A4 (en) 2016-04-06
CN104822664B (zh) 2017-01-18
CN104822664A (zh) 2015-08-05
HK1213243A1 (en) 2016-06-30
US9828376B2 (en) 2017-11-28
EP3680238A1 (en) 2020-07-15
US20180134719A1 (en) 2018-05-17
JP2015532304A (ja) 2015-11-09
JP6401169B2 (ja) 2018-10-03

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Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20191001

FZDE Discontinued

Effective date: 20220509