WO2010120994A3 - Ureidoaryl-and carbamoylaryl-morpholino- pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their synthesis - Google Patents

Ureidoaryl-and carbamoylaryl-morpholino- pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their synthesis 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
Prior art date
Application number
PCT/US2010/031183
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French (fr)
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WO2010120994A2 (en
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/en
Publication of WO2010120994A3 publication Critical patent/WO2010120994A3/en

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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

The invention relates to ureidophenyl-morpholino pyrimidine and guanidinophenyl-morpholino pyrimidine compounds of formula, and to methods for making and using the compounds.
PCT/US2010/031183 2009-04-17 2010-04-15 Ureidoaryl-and carbamoylaryl-morpholino- pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their synthesis WO2010120994A2 (en)

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 (en) 2010-10-21
WO2010120994A3 true WO2010120994A3 (en) 2013-08-01

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PCT/US2010/031183 WO2010120994A2 (en) 2009-04-17 2010-04-15 Ureidoaryl-and carbamoylaryl-morpholino- pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their synthesis

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112707907B (en) * 2019-10-24 2023-05-23 张飞 Purine derivative and intermediate thereof, and application of purine derivative and intermediate thereof in preparation of anti-cancer drugs

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2542536B1 (en) 2010-03-04 2015-01-21 Cellzome Limited Morpholino substituted urea derivatives as mtor inhibitors
US8440662B2 (en) 2010-10-31 2013-05-14 Endo Pharmaceuticals, Inc. Substituted quinazoline and pyrido-pyrimidine derivatives
JP2014510122A (en) * 2011-04-04 2014-04-24 セルゾーム リミテッド Dihydropyrrolopyrimidine derivatives as mTOR inhibitors
US8846656B2 (en) 2011-07-22 2014-09-30 Novartis Ag Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators
EP2758379B1 (en) 2011-09-21 2016-10-19 Cellzome Limited Urea and carbamate derivatives of 2-morpholino-1,3,5-triazine as mTOR inhibitors for the treatment of immunological or proliferative diseases
BR112014007310A2 (en) 2011-09-27 2017-04-04 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as mutant idh inhibitors
AU2012320465B2 (en) 2011-10-07 2016-03-03 Cellzome Limited Morpholino substituted bicyclic pyrimidine urea or carbamate derivatives as mTOR inhibitors
UY34632A (en) 2012-02-24 2013-05-31 Novartis Ag OXAZOLIDIN- 2- ONA COMPOUNDS AND USES OF THE SAME
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 (en) 2013-03-14 2018-01-10 Novartis AG 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
WO2014144169A1 (en) * 2013-03-15 2014-09-18 Epizyme, Inc. Carm1 inhibitors and uses thereof
EP3053926B1 (en) 2013-09-30 2018-08-08 Shanghai Yingli Pharmaceutical Co. Ltd. Fused pyrimidine compound, intermediate, preparation method therefor, and composition and application thereof
EP3059238B1 (en) * 2013-10-16 2020-05-27 Shanghai Yingli Pharmaceutical Co. Ltd. Fused heterocyclic compound, preparation method therefor, pharmaceutical composition, and uses thereof
RU2719422C2 (en) 2014-08-04 2020-04-17 Нуэволюшон А/С Optionally condensed heterocyclyl-substituted pyrimidine derivatives suitable for treating inflammatory, metabolic, oncological and autoimmune diseases
CA3004534C (en) * 2015-11-23 2023-11-07 Council Of Scientific & Industrial Research Fused pyrimidines as isoform selective phosphoinositide-3-kinase-alpha inhibitors and process for preparation thereof
AU2017275657B2 (en) 2016-06-02 2021-08-19 Novartis Ag Potassium channel modulators
CN107793365B (en) * 2016-08-31 2021-08-17 上海微创医疗器械（集团）有限公司 Compound and preparation method and application thereof
SI3571193T1 (en) 2017-01-23 2022-04-29 Cadent Therapeutics, Inc. Potassium channel modulators
CN107721937B (en) * 2017-10-26 2021-02-05 沈阳药科大学 Preparation method and application of compound containing pyrimidone skeleton
CN108358949A (en) * 2018-03-01 2018-08-03 南京法恩化学有限公司 The preparation method of 2,4- of one kind dichloro-thiophenes simultaneously [3,2-D] pyrimidine
CN109824701B (en) * 2019-03-26 2021-08-13 武汉工程大学 Pyridinothiazole compound and preparation method and application thereof
CA3160522A1 (en) 2019-12-20 2021-06-24 Sanne Schroder Glad Compounds active towards nuclear receptors
CA3174176A1 (en) 2020-03-31 2021-10-07 Sanne Schroder Glad Compounds active towards nuclear receptors
MX2022012260A (en) 2020-03-31 2022-11-30 Nuevolution As Compounds active towards nuclear receptors.

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006005914A1 (en) * 2004-07-09 2006-01-19 Astrazeneca Ab 2, 4, 6-trisubstituted pyrimidines as phosphotidylinositol (pi) 3-kinase inhibitors and their use in the treatment of cancer

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006005914A1 (en) * 2004-07-09 2006-01-19 Astrazeneca Ab 2, 4, 6-trisubstituted pyrimidines as phosphotidylinositol (pi) 3-kinase inhibitors and their use in the treatment of cancer

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112707907B (en) * 2019-10-24 2023-05-23 张飞 Purine derivative and intermediate thereof, and application of purine derivative and intermediate thereof in preparation of anti-cancer drugs

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