WO2012101065A3 - Composés de pyrimidine biarylamine et leurs utilisations - Google Patents

Composés de pyrimidine biarylamine et leurs utilisations Download PDF

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Publication number
WO2012101065A3
WO2012101065A3 PCT/EP2012/050909 EP2012050909W WO2012101065A3 WO 2012101065 A3 WO2012101065 A3 WO 2012101065A3 EP 2012050909 W EP2012050909 W EP 2012050909W WO 2012101065 A3 WO2012101065 A3 WO 2012101065A3
Authority
WO
WIPO (PCT)
Prior art keywords
amine compounds
compounds
cdk9
cdk9 inhibitors
biaryl amine
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.)
Ceased
Application number
PCT/EP2012/050909
Other languages
English (en)
Other versions
WO2012101065A2 (fr
Inventor
William R. Antonios-Mccrea
Paul A. Barsanti
Cheng Hu
Xianming Jin
Xiaodong Lin
Eric J. Martin
Yue Pan
Keith B Pfister
Paul A. Renhowe
Martin Sendzik
James Sutton
Lifeng Wan
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.)
Novartis AG
Original Assignee
Novartis AG
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 Novartis AG filed Critical Novartis AG
Publication of WO2012101065A2 publication Critical patent/WO2012101065A2/fr
Publication of WO2012101065A3 publication Critical patent/WO2012101065A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Cette invention concerne un composé de pyrimidine de formule (I) où X ou Y, mais pas les deux, est N, et les sels, énantiomères, stéréoisomères, rotamères, tautomères, diastéréomères, formes deutérées, ou racémates de qualité pharmaceutique de celui-ci. Ces composés inhibent l'activité des CDK9 et sont, donc, utiles à titre d'agents pharmaceutiques. Des méthodes pour traiter une maladie ou une affection médiée par les CDK9 à l'aide des composés de Formule I et de leurs isomères, et des compositions pharmaceutiques contenant les composés selon l'invention sont également décrites.
PCT/EP2012/050909 2011-01-28 2012-01-20 Composés de pyrimidine biarylamine et leurs utilisations Ceased WO2012101065A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161437071P 2011-01-28 2011-01-28
US61/437,071 2011-01-28

Publications (2)

Publication Number Publication Date
WO2012101065A2 WO2012101065A2 (fr) 2012-08-02
WO2012101065A3 true WO2012101065A3 (fr) 2013-01-10

Family

ID=45524558

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2012/050909 Ceased WO2012101065A2 (fr) 2011-01-28 2012-01-20 Composés de pyrimidine biarylamine et leurs utilisations

Country Status (1)

Country Link
WO (1) WO2012101065A2 (fr)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103917527B (zh) 2011-09-16 2017-05-31 拜耳知识产权有限责任公司 二取代的5‑氟‑嘧啶
WO2013059634A1 (fr) 2011-10-20 2013-04-25 The Regents Of The University Of California Utilisation d'inhibiteurs de cdk9 pour réduire la dégradation cartilagineuse
HK1209414A1 (en) 2012-10-18 2016-04-01 Bayer Pharma Aktiengesellschaft 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group
CN105102434A (zh) 2012-10-18 2015-11-25 拜耳药业股份公司 含砜基团的4-(邻)-氟苯基-5-氟嘧啶-2-基胺
TW201418243A (zh) 2012-11-15 2014-05-16 Bayer Pharma AG 含有磺醯亞胺基團之ｎ－（吡啶－２－基）嘧啶－４－胺衍生物
US10300073B2 (en) 2014-10-14 2019-05-28 The Regents Of The University Of California Use of CDK9 and BRD4 inhibitors to inhibit inflammation
CA2964683A1 (fr) 2014-10-16 2016-04-21 Bayer Pharma Aktiengesellschaft Derives de benzofuranyle-pyrimidine fluores contenant un groupe sulfone
JP6847099B2 (ja) 2015-09-29 2021-03-24 バイエル ファーマ アクチエンゲゼルシャフト 新規な大環状スルホンジイミン化合物
ES2819869T3 (es) 2015-10-08 2021-04-19 Bayer Pharma AG Nuevos compuestos macrocíclicos modificados
WO2017060322A2 (fr) 2015-10-10 2017-04-13 Bayer Pharma Aktiengesellschaft Conjugué anticorps-médicament (adc) inhibiteur de ptefb
CA3057891A1 (fr) 2017-03-28 2018-10-04 Bayer Aktiengesellschaft Nouveaux composes macrocycliques inhibiteurs de ptefb
EP3601253B1 (fr) 2017-03-28 2021-09-15 Bayer Aktiengesellschaft Nouveaux composés macrocycliques inhibiteurs de ptefb
US11701347B2 (en) 2018-02-13 2023-07-18 Bayer Aktiengesellschaft Use of 5-fluoro-4-(4-fluoro-2-methoxyphenyl)-N-{4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2-amine for treating diffuse large B-cell lymphoma
SG11202009356RA (en) 2018-03-29 2020-10-29 Takeda Pharmaceuticals Co Heterocyclic compound
IL298219A (en) 2020-05-15 2023-01-01 Algen Biotechnologies Inc Certain chemical compositions and methods of use thereof
TW202329937A (zh) 2021-12-03 2023-08-01 美商英塞特公司 雙環胺ｃｋ１２抑制劑
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors
CA3251059A1 (fr) 2022-05-02 2023-11-09 The Board Of Trustees Of The Leland Stanford Junior University Compositions, systèmes et procédés de modulation d’un gène cible

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995009853A1 (fr) * 1993-10-01 1995-04-13 Ciba-Geigy Ag Derives pyridine pharmacologiquement actifs ainsi que leurs procedes de preparation
WO2001093682A1 (fr) * 2000-06-08 2001-12-13 Syngenta Participations Ag Derives de n-phenyl-4-(4-pyridyl)-2-pyrimidine-amine
WO2008079933A2 (fr) * 2006-12-22 2008-07-03 Novartis Ag Composés organiques et leurs utilisations
WO2008148889A1 (fr) * 2007-06-08 2008-12-11 Bayer Cropscience Sa Derives heterocyclyl-pyrimidinyl-amino fongicides
WO2009061761A2 (fr) * 2007-11-06 2009-05-14 E. I. Du Pont De Nemours And Company Amines fongicides

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
WO2004078163A2 (fr) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Compositions pharmaceutiques a base d'un co-cristal
JP4867350B2 (ja) 2003-12-19 2012-02-01 宇部興産株式会社 ４−置換−４−シアノテトラヒドロピラン化合物の製法

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995009853A1 (fr) * 1993-10-01 1995-04-13 Ciba-Geigy Ag Derives pyridine pharmacologiquement actifs ainsi que leurs procedes de preparation
WO2001093682A1 (fr) * 2000-06-08 2001-12-13 Syngenta Participations Ag Derives de n-phenyl-4-(4-pyridyl)-2-pyrimidine-amine
WO2008079933A2 (fr) * 2006-12-22 2008-07-03 Novartis Ag Composés organiques et leurs utilisations
WO2008148889A1 (fr) * 2007-06-08 2008-12-11 Bayer Cropscience Sa Derives heterocyclyl-pyrimidinyl-amino fongicides
WO2009061761A2 (fr) * 2007-11-06 2009-05-14 E. I. Du Pont De Nemours And Company Amines fongicides

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
CHRISTIAN PILLONEL: "Evaluation of phenylaminopyrimidines as antifungal protein kinase inhibitors", PEST MANAGEMENT SCIENCE, WILEY & SONS, BOGNOR REGIS; GB, vol. 61, 13 June 2005 (2005-06-13), pages 1069 - 1076, XP002429106, ISSN: 1526-498X, DOI: 10.1002/PS.1080 *
KUO G-H ET AL: "Synthesis and Identification of [1,3,5]Triazine-pyridine Biheteroaryl as a Novel Series of Potent Cyclin-Dependent Kinase Inhibitors", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 48, no. 14, 27 May 2005 (2005-05-27), pages 4535 - 4546, XP002468199, ISSN: 0022-2623, DOI: 10.1021/JM040214H *
MCINTYRE ET AL.: "Pyridazine based inhibitors of p38 MAPK", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 12, 2002, pages 689 - 692, XP002675476 *
STANETTY ET AL.: "Novel and efficient access to phenylamino-pyrimidine type protein kinase C inhibitors utilizing a negishi cross-coupling strategy", J. ORG. CHEM., vol. 70, 2005, pages 5215 - 5220, XP002675475 *

Also Published As

Publication number Publication date
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