WO2010120994A3 - Composés d'uréido-aryl-pyrimidine et de carbamoylaryl-morpholino-pyrimidine, leur utilisation comme inhibiteurs de la kinase mtor et de la kinase pi-3, et leur synthèse - Google Patents

Composés d'uréido-aryl-pyrimidine et de carbamoylaryl-morpholino-pyrimidine, leur utilisation comme inhibiteurs de la kinase mtor et de la kinase pi-3, et leur synthèse Download PDF

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Publication number
WO2010120994A3
WO2010120994A3 PCT/US2010/031183 US2010031183W WO2010120994A3 WO 2010120994 A3 WO2010120994 A3 WO 2010120994A3 US 2010031183 W US2010031183 W US 2010031183W WO 2010120994 A3 WO2010120994 A3 WO 2010120994A3
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WIPO (PCT)
Prior art keywords
kinase
morpholino
ureidoaryl
carbamoylaryl
synthesis
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PCT/US2010/031183
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English (en)
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WO2010120994A2 (fr
Inventor
Jeroen Cunera Verheijen
Arie Zask
Semiramis Ayral-Kaloustian
Christoph Martin Dehnhardt
Nan Zhang
Aranapakam Mudumbai Venkatesan
Thai Hiep Nguyen
Kevin Joseph Curran
Joshua Aaron Kaplan
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Wyeth Llc
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Publication of WO2010120994A2 publication Critical patent/WO2010120994A2/fr
Publication of WO2010120994A3 publication Critical patent/WO2010120994A3/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems
    • 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
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/04—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 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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/12—Heterocyclic 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 three hetero rings
    • C07D491/14—Ortho-condensed systems
    • C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom

Abstract

La présente invention concerne des composés d'uréido-phényl-morpholino pyrimidine et de guanidinophényl-morpholino pyrimidine de formule, et des procédés permettant de fabriquer les composés.
PCT/US2010/031183 2009-04-17 2010-04-15 Composés d'uréido-aryl-pyrimidine et de carbamoylaryl-morpholino-pyrimidine, leur utilisation comme inhibiteurs de la kinase mtor et de la kinase pi-3, et leur synthèse WO2010120994A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US17032809P 2009-04-17 2009-04-17
US61/170,328 2009-04-17

Publications (2)

Publication Number Publication Date
WO2010120994A2 WO2010120994A2 (fr) 2010-10-21
WO2010120994A3 true WO2010120994A3 (fr) 2013-08-01

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PCT/US2010/031183 WO2010120994A2 (fr) 2009-04-17 2010-04-15 Composés d'uréido-aryl-pyrimidine et de carbamoylaryl-morpholino-pyrimidine, leur utilisation comme inhibiteurs de la kinase mtor et de la kinase pi-3, et leur synthèse

Country Status (1)

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WO (1) WO2010120994A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112707907B (zh) * 2019-10-24 2023-05-23 张飞 嘌呤衍生物及其中间体与制备抗癌症药物的应用

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EP2542536B1 (fr) 2010-03-04 2015-01-21 Cellzome Limited Dérivés d'urée à substitution morpholino en tant qu'inhibiteurs mTOR
US8440662B2 (en) 2010-10-31 2013-05-14 Endo Pharmaceuticals, Inc. Substituted quinazoline and pyrido-pyrimidine derivatives
JP2014510122A (ja) * 2011-04-04 2014-04-24 セルゾーム リミテッド ｍＴＯＲ阻害剤としてのジヒドロピロロピリミジン誘導体
US8846656B2 (en) 2011-07-22 2014-09-30 Novartis Ag Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators
EP2758379B1 (fr) 2011-09-21 2016-10-19 Cellzome Limited Dérivés d'urée et de carbamate de 2-morpholino-1,3,5-triazine en tant qu'inhibiteurs de mTOR pour le traitement de maladies immunologiques ou proliferatives
BR112014007310A2 (pt) 2011-09-27 2017-04-04 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inibidores de idh mutante
AU2012320465B2 (en) 2011-10-07 2016-03-03 Cellzome Limited Morpholino substituted bicyclic pyrimidine urea or carbamate derivatives as mTOR inhibitors
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
US9499561B2 (en) 2012-04-10 2016-11-22 Shanghai Yingli Pharmaceutical Co., Ltd. Fused pyrimidine compound, and preparation method, intermediate, composition, and uses thereof
US9296733B2 (en) 2012-11-12 2016-03-29 Novartis Ag Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases
EP2970240B1 (fr) 2013-03-14 2018-01-10 Novartis AG 3-pyrimidin-4-yl-oxazolidin-2-ones comme inhibiteurs d'idh mutante
WO2014144169A1 (fr) * 2013-03-15 2014-09-18 Epizyme, Inc. Inhibiteurs de carm1 et leurs utilisations
EP3053926B1 (fr) 2013-09-30 2018-08-08 Shanghai Yingli Pharmaceutical Co. Ltd. Composé de pyrimidine condensée, intermédiaire, procédé de préparation s'y rapportant et composition et application correspondantes
EP3059238B1 (fr) * 2013-10-16 2020-05-27 Shanghai Yingli Pharmaceutical Co. Ltd. Composé hétérocyclique condensé, son procédé de préparation, composition pharmaceutique et leurs utilisations
RU2719422C2 (ru) 2014-08-04 2020-04-17 Нуэволюшон А/С Необязательно конденсированные гетероциклил-замещенные производные пиримидина, пригодные для лечения воспалительных, метаболических, онкологических и аутоиммунных заболеваний
CA3004534C (fr) * 2015-11-23 2023-11-07 Council Of Scientific & Industrial Research Pyrimidines fusionnees utilisees comme inhibiteurs de la phosphoinositide 3-kinase alpha selectifs d'une isoforme et leur procede de preparation
AU2017275657B2 (en) 2016-06-02 2021-08-19 Novartis Ag Potassium channel modulators
CN107793365B (zh) * 2016-08-31 2021-08-17 上海微创医疗器械（集团）有限公司 一种化合物及其制备方法和用途
SI3571193T1 (sl) 2017-01-23 2022-04-29 Cadent Therapeutics, Inc. Modulatorji kalijevega kanalčka
CN107721937B (zh) * 2017-10-26 2021-02-05 沈阳药科大学 含有嘧啶酮骨架的化合物的制备方法和用途
CN108358949A (zh) * 2018-03-01 2018-08-03 南京法恩化学有限公司 一种2，4-二氯噻吩并[3，2-d]嘧啶的制备方法
CN109824701B (zh) * 2019-03-26 2021-08-13 武汉工程大学 一种吡啶并噻唑类化合物及其制备方法和应用
CA3160522A1 (fr) 2019-12-20 2021-06-24 Sanne Schroder Glad Composes actifs vis-a-vis des recepteurs nucleaires
CA3174176A1 (fr) 2020-03-31 2021-10-07 Sanne Schroder Glad Composes actifs vis-a-vis des recepteurs nucleaires
MX2022012260A (es) 2020-03-31 2022-11-30 Nuevolution As Compuestos activos frente a receptores nucleares.

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WO2006005914A1 (fr) * 2004-07-09 2006-01-19 Astrazeneca Ab Pyrimidines a substitution triple aux positions 2, 4, 6 utilises en tant qu'inhibiteurs de phosphotidylinositol (pi) 3-kinase et utilisations de celles-ci pour traiter un cancer

Patent Citations (1)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112707907B (zh) * 2019-10-24 2023-05-23 张飞 嘌呤衍生物及其中间体与制备抗癌症药物的应用

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