TN2011000657A1 - NOVEL (6-OXO-1,6-DIHYDRO-PYRIMIDIN-2-YL) -AMIDE DERIVATIVES, THEIR PREPARATION AND THEIR PHARMACEUTICAL USE AS AKT PHOSPHORYLATION INHIBITORS (PKB) - Google Patents

NOVEL (6-OXO-1,6-DIHYDRO-PYRIMIDIN-2-YL) -AMIDE DERIVATIVES, THEIR PREPARATION AND THEIR PHARMACEUTICAL USE AS AKT PHOSPHORYLATION INHIBITORS (PKB)

Info

Publication number
TN2011000657A1
TN2011000657A1 TNP2011000657A TN2011000657A TN2011000657A1 TN 2011000657 A1 TN2011000657 A1 TN 2011000657A1 TN P2011000657 A TNP2011000657 A TN P2011000657A TN 2011000657 A TN2011000657 A TN 2011000657A TN 2011000657 A1 TN2011000657 A1 TN 2011000657A1
Authority
TN
Tunisia
Prior art keywords
pkb
novel
pyrimidin
dihydro
oxo
Prior art date
Application number
TNP2011000657A
Other languages
French (fr)
Inventor
Jean-Christophe Carry
Victor Certal
Frank Halley
Karl Andreas Karlsson
Laurent Schio
Fabienne Thompson
Original Assignee
Sanofi Sa
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
Priority claimed from PCT/FR2010/051375 external-priority patent/WO2011001114A1/en
Application filed by Sanofi Sa filed Critical Sanofi Sa
Publication of TN2011000657A1 publication Critical patent/TN2011000657A1/en

Links

Classifications

    • 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
    • C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon 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
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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

L'invention concerne les nouveaux produits de formule (I): dans laquelle R1 représente aryle ou hétéroaryle éventuellement substitués; R représente H ou bien forme avec R1 un cycle à 5 ou 6 chaînons fusionné à un reste aryle ou hétéroaryle renfermant éventuellement un ou plusieurs O, S, N, NH et Nalk, étant éventuellement substitué; R2, R3 représentent indépendamment H, Hal ou alkyle éventuellement substitué par un ou plusieurs Hal; R4 représente H; R5 représente un H ou alkyle éventuellement substitué par un ou plusieurs atomes d'halogène; ces produits étant sous toutes les formes isomères et les sels, à titre de médicaments notamment comme inhibiteurs de phosphorylation d'AKT(PKB).The invention relates to novel products of formula (I): wherein R 1 represents optionally substituted aryl or heteroaryl; R represents H or forms with R1 a 5- or 6-membered ring fused to an aryl or heteroaryl residue optionally containing one or more O, S, N, NH and Nalk, being optionally substituted; R2, R3 independently represent H, Hal or alkyl optionally substituted with one or more Hal; R4 is H; R5 represents an H or alkyl optionally substituted with one or more halogen atoms; these products being in all isomeric forms and salts, as medicaments in particular as inhibitors of phosphorylation of AKT (PKB).

TNP2011000657A 2009-07-02 2011-12-22 NOVEL (6-OXO-1,6-DIHYDRO-PYRIMIDIN-2-YL) -AMIDE DERIVATIVES, THEIR PREPARATION AND THEIR PHARMACEUTICAL USE AS AKT PHOSPHORYLATION INHIBITORS (PKB) TN2011000657A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR0903239A FR2947547B1 (en) 2009-07-02 2009-07-02 NOVEL (6-OXO-1,6-DIHYDRO-PYRIMIDIN-2-YL) -AMIDE DERIVATIVES, THEIR PREPARATION AND THEIR PHARMACEUTICAL USE AS AKT PHOSPHORYLATION INHIBITORS (PKB)
PCT/FR2010/051375 WO2011001114A1 (en) 2009-07-02 2010-07-01 Novel (6-oxo-1, 6-dihydro-pyrimidin-2-yl)-amide derivatives, preparation thereof, and pharmaceutical use thereof as akt(pkb) phosphorylation inhibitors

Publications (1)

Publication Number Publication Date
TN2011000657A1 true TN2011000657A1 (en) 2013-05-24

Family

ID=41611847

Family Applications (1)

Application Number Title Priority Date Filing Date
TNP2011000657A TN2011000657A1 (en) 2009-07-02 2011-12-22 NOVEL (6-OXO-1,6-DIHYDRO-PYRIMIDIN-2-YL) -AMIDE DERIVATIVES, THEIR PREPARATION AND THEIR PHARMACEUTICAL USE AS AKT PHOSPHORYLATION INHIBITORS (PKB)

Country Status (5)

Country Link
BR (1) BRPI1015913A2 (en)
CR (1) CR20120071A (en)
FR (1) FR2947547B1 (en)
TN (1) TN2011000657A1 (en)
UA (1) UA107357C2 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111393374A (en) * 2020-05-08 2020-07-10 张建蒙 Oxo-dihydropyridazine derivative and application thereof in antitumor drugs

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009007749A2 (en) * 2007-07-09 2009-01-15 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases

Also Published As

Publication number Publication date
FR2947547B1 (en) 2012-05-18
BRPI1015913A2 (en) 2020-08-18
UA107357C2 (en) 2014-12-25
FR2947547A1 (en) 2011-01-07
CR20120071A (en) 2012-11-01

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