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ECSP12011570A - Nuevos derivados de (6-oxo-1,6-dihidro-pirimidin-2-il)-amida, su preparación y su utilización farmacéutica como inhibidores de fosforilación de akt(pkb) - Google Patents

Nuevos derivados de (6-oxo-1,6-dihidro-pirimidin-2-il)-amida, su preparación y su utilización farmacéutica como inhibidores de fosforilación de akt(pkb)

Info

Publication number
ECSP12011570A
ECSP12011570A EC2012011570A ECSP12011570A ECSP12011570A EC SP12011570 A ECSP12011570 A EC SP12011570A EC 2012011570 A EC2012011570 A EC 2012011570A EC SP12011570 A ECSP12011570 A EC SP12011570A EC SP12011570 A ECSP12011570 A EC SP12011570A
Authority
EC
Ecuador
Prior art keywords
pkb
akt
inhibitors
phosphorilation
pirimidin
Prior art date
Application number
EC2012011570A
Other languages
English (en)
Inventor
Jean-Christophe Carry
Franck Halley
Laurent Schio
Victor Certal
Karl Andreas Karlsoon
Fabienne Thompson
Original Assignee
Sanofi Aventis
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 FR0903239A external-priority patent/FR2947547B1/fr
Priority claimed from FR0957070A external-priority patent/FR2951169B1/fr
Application filed by Sanofi Aventis filed Critical Sanofi Aventis
Publication of ECSP12011570A publication Critical patent/ECSP12011570A/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/20Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D239/22Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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 aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La invención se refiere a los nuevos productos de fórmula (I): en la que R1 representa arilo o heteroarilo sustituidos opcionalmente ; R representa H o bien forma con R1 un ciclo de 5 ó 6 eslabones fusionado a un resto arilo o heteroarilo que contiene opcionalmente uno o varios O, S, N, NH y Nalk, estando sustituido opcionalmente ; R2, R3 representan independientemente H, Hal o alquilo sustituido opcionalmente con uno o varios Hal ; R4 representa H; R5 representa un H o alquilo sustituido opcionalmente con uno o varios átomos de halógeno; estando estos productos en todas las formas isómeras y las sales, como medicamentos principalmente como inhibidores de fosforilación de AKT(PKB).
EC2012011570A 2009-07-02 2012-01-03 Nuevos derivados de (6-oxo-1,6-dihidro-pirimidin-2-il)-amida, su preparación y su utilización farmacéutica como inhibidores de fosforilación de akt(pkb) ECSP12011570A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FR0903239A FR2947547B1 (fr) 2009-07-02 2009-07-02 Nouveaux derives de (6-oxo-1,6-dihydro-pyrimidin-2-yl)-amide, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt (pkb)
US24110009P 2009-09-10 2009-09-10
FR0957070A FR2951169B1 (fr) 2009-10-09 2009-10-09 Nouveaux derives de (6-oxo-1,6-dihydro-pyrimidin-2-yl)-amide, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt(pkb)

Publications (1)

Publication Number Publication Date
ECSP12011570A true ECSP12011570A (es) 2012-02-29

Family

ID=42635553

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2012011570A ECSP12011570A (es) 2009-07-02 2012-01-03 Nuevos derivados de (6-oxo-1,6-dihidro-pirimidin-2-il)-amida, su preparación y su utilización farmacéutica como inhibidores de fosforilación de akt(pkb)

Country Status (36)

Country Link
US (2) US8791255B2 (es)
EP (1) EP2448927B1 (es)
JP (1) JP5680638B2 (es)
KR (1) KR20120106714A (es)
CN (1) CN102548970B (es)
AR (1) AR077364A1 (es)
AU (1) AU2010267816B2 (es)
CA (1) CA2767064C (es)
CL (1) CL2012000003A1 (es)
CO (1) CO6480974A2 (es)
CR (1) CR20110703A (es)
DK (1) DK2448927T3 (es)
DO (1) DOP2011000407A (es)
EA (1) EA021088B1 (es)
EC (1) ECSP12011570A (es)
ES (1) ES2464125T3 (es)
HN (1) HN2011003482A (es)
HR (1) HRP20140478T1 (es)
IL (2) IL217295A (es)
MA (1) MA33501B1 (es)
ME (1) ME01885B (es)
MX (1) MX2012000094A (es)
MY (1) MY153042A (es)
NI (1) NI201200002A (es)
NZ (1) NZ597579A (es)
PE (1) PE20120640A1 (es)
PL (1) PL2448927T3 (es)
PT (1) PT2448927E (es)
RS (1) RS53317B (es)
SG (2) SG10201402867TA (es)
SI (1) SI2448927T1 (es)
SM (1) SMT201400084B (es)
TW (1) TWI466883B (es)
UY (1) UY32755A (es)
WO (1) WO2011001114A1 (es)
ZA (1) ZA201200026B (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2969614A1 (fr) * 2010-12-28 2012-06-29 Sanofi Aventis Nouveaux derives de pyrimidinones, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt(pkb)
FR2969610B1 (fr) * 2010-12-28 2013-04-05 Sanofi Aventis Nouveaux derives de (6-oxo-1,6-dihydro-pyrimidin-2-yl)-indolinamide, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt(pkb)
FR2969609B1 (fr) * 2010-12-28 2013-02-08 Sanofi Aventis Nouveaux derives de 6-oxo-dihydro-pyrimidine, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt(pkb)
SI2658844T1 (sl) 2010-12-28 2017-02-28 Sanofi Novi derivati pirimidina, njihova priprava in njihova farmacevtska uporaba kot inhibitorje AKT(PKB) fosforilacije
AU2012214413A1 (en) * 2011-02-11 2013-08-22 Dana-Farber Cancer Institute, Inc. Method of inhibiting hamartoma tumor cells
EP2570127A1 (en) 2011-09-16 2013-03-20 Sanofi Compositions and methods for treating cancer using PI3KB beta inhibitor and MAPK pathway inhibitor, including MEK and RAF inhibitors
EP2968350A1 (en) 2013-03-15 2016-01-20 Sanofi Anti-tumoral composition comprising a pi3kbeta inhibitor and a raf inhibitor, to overcome cancer cells resistance
SG11201507720PA (en) 2013-04-05 2015-10-29 Sanofi Sa Anti-tumoral composition comprising a pi3kbeta-selective inhibitor and a pi3kalpha-selective inhibitor
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WO2020104456A1 (en) 2018-11-20 2020-05-28 Tes Pharma S.R.L INHIBITORS OF α-AMINO-β-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE

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Also Published As

Publication number Publication date
JP2012531464A (ja) 2012-12-10
SG177469A1 (en) 2012-02-28
AU2010267816A1 (en) 2012-02-16
AU2010267816B2 (en) 2015-11-12
IL217295A0 (en) 2012-02-29
SMT201400084B (it) 2014-09-08
HRP20140478T1 (hr) 2014-07-04
UY32755A (es) 2011-01-31
CN102548970A (zh) 2012-07-04
DOP2011000407A (es) 2012-06-15
CA2767064C (fr) 2017-11-07
EA201270111A1 (ru) 2012-07-30
US20120270867A1 (en) 2012-10-25
MY153042A (en) 2014-12-31
ME01885B (me) 2014-12-20
EP2448927B1 (fr) 2014-03-12
NI201200002A (es) 2012-03-30
TWI466883B (zh) 2015-01-01
MA33501B1 (fr) 2012-08-01
US8993565B2 (en) 2015-03-31
CN102548970B (zh) 2015-11-25
JP5680638B2 (ja) 2015-03-04
CO6480974A2 (es) 2012-07-16
PT2448927E (pt) 2014-06-12
NZ597579A (en) 2013-06-28
IL217321A0 (en) 2012-02-29
CL2012000003A1 (es) 2012-08-03
SI2448927T1 (sl) 2014-06-30
TW201103924A (en) 2011-02-01
AR077364A1 (es) 2011-08-24
US20140303156A1 (en) 2014-10-09
US8791255B2 (en) 2014-07-29
ES2464125T3 (es) 2014-05-30
WO2011001114A1 (fr) 2011-01-06
HK1169110A1 (en) 2013-01-18
IL217295A (en) 2015-10-29
EA021088B1 (ru) 2015-04-30
PL2448927T3 (pl) 2014-09-30
KR20120106714A (ko) 2012-09-26
ZA201200026B (en) 2013-03-27
RS53317B (sr) 2014-10-31
MX2012000094A (es) 2012-05-22
PE20120640A1 (es) 2012-06-09
CA2767064A1 (fr) 2011-01-06
SG10201402867TA (en) 2014-08-28
HN2011003482A (es) 2014-11-10
CR20110703A (es) 2012-03-06
DK2448927T3 (da) 2014-06-16
EP2448927A1 (fr) 2012-05-09

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