AR077628A1 - Derivados de 6-(morfolin-4-il)-pirimidin-4(3h)-ona, su preparacion y su utilizacion farmaceutica como inhibidores de la fosforilacion de akt(pkb) - Google Patents

Derivados de 6-(morfolin-4-il)-pirimidin-4(3h)-ona, su preparacion y su utilizacion farmaceutica como inhibidores de la fosforilacion de akt(pkb)

Info

Publication number
AR077628A1
AR077628A1 ARP100102348A ARP100102348A AR077628A1 AR 077628 A1 AR077628 A1 AR 077628A1 AR P100102348 A ARP100102348 A AR P100102348A AR P100102348 A ARP100102348 A AR P100102348A AR 077628 A1 AR077628 A1 AR 077628A1
Authority
AR
Argentina
Prior art keywords
alkyl
radicals
alkoxy
radical
hydrogen atom
Prior art date
Application number
ARP100102348A
Other languages
English (en)
Inventor
Fabienne Thompson
Victor Certal
Karl Andreas Karlsson
Frank Halley
Bruno Filoche-Romme
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 FR0903238A external-priority patent/FR2947548B1/fr
Priority claimed from FR0957073A external-priority patent/FR2951170B1/fr
Application filed by Sanofi Aventis filed Critical Sanofi Aventis
Publication of AR077628A1 publication Critical patent/AR077628A1/es

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    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La invencion se refiere a los nuevos productos de la formula (1) Reivindicacion 1: Productos de la formula (1): en la que: Z representa -O-, -NH, N-cicloalquilo, N-alk, o N-fenilo, con alk y fenilo eventualmente sustituidos con uno o varios radicales elegidos entre los átomos de halogeno, y los radicales alquilo, alcoxi, hidroxilo, ciano y fenilo, este mismo eventualmente sustituido con uno o varios radicales elegidos entre los átomos de halogeno y los radicales hidroxilo, alcoxi y alquilo; n representa un numero entero de 0 a 4; R1 representa un átomo de hidrogeno, de halogeno o un radical hidroxilo, alquilo o alcoxi; estando los radicales alquilo y alcoxi eventualmente sustituidos con un grupo NRxRy o con uno o varios átomos de halogeno; bien entendido que R1 puede representar un resto fenilo fusionado con el fenilo que lleva R1 para formar un radical naftilo; R2 y R3 idénticos o diferentes representan un átomo de hidrogeno, un átomo de halogeno o un radical alquilo eventualmente sustituido con uno o varios átomos de halogeno; R4 representa un átomo de hidrogeno; siendo NRxRy de tal modo que Rx representa un átomo de hidrogeno o un radical alquilo y Ry representa un átomo de hidrogeno o un radical alquilo; o bien Rx y Ry forman con el átomo de nitrogeno al que están unidos un radical cíclico que tiene de 3 a 10 eslabones y eventualmente uno o varios de otros heteroátomos elegidos entre O, S, NH y N-alquilo, estando este radical cíclico eventualmente sustituido con uno o varios radicales idénticos o diferentes elegidos entre los átomos de halogeno y los radicales alquilo, hidroxilo, oxo, alcoxi, NH2; N-Halk y N(alk)2; siendo todos los radicales alquilo (alk) y alcoxi anteriores lineales o ramificados y comprendiendo de 1 a 6 átomos de carbono, estando dichos productos de la formula (1) en todas las formas isomeras posibles, racémicas, enantiomeras y diastereoisomeras, así como las sales de adicion con los ácidos minerales y orgánicos o con las bases minerales y orgánicas de dichos productos de la formula (1). Reivindicacion 16: A título de productos industriales nuevos, los intermedios de síntesis de las formulas C, D, F, J y K tales como se han definido en la reivindicacion 4 o 5 anteriormente y se recuerdan a continuacion: en las cuales R1, R2, R3 y Z tienen la definicion indicada en una cualquiera de las reivindicaciones 1 a 2.
ARP100102348A 2009-07-02 2010-07-01 Derivados de 6-(morfolin-4-il)-pirimidin-4(3h)-ona, su preparacion y su utilizacion farmaceutica como inhibidores de la fosforilacion de akt(pkb) AR077628A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FR0903238A FR2947548B1 (fr) 2009-07-02 2009-07-02 Nouveaux derives de 1h-pyrimidin-2-one, leur preparation pharmaceutique comme inhibiteurs de phosphorylation d'akt(pkb)
US24110109P 2009-09-10 2009-09-10
FR0957073A FR2951170B1 (fr) 2009-10-09 2009-10-09 Nouveaux derives de 1h-pyrimidin-2-one, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt(pkb)

Publications (1)

Publication Number Publication Date
AR077628A1 true AR077628A1 (es) 2011-09-14

Family

ID=42646247

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100102348A AR077628A1 (es) 2009-07-02 2010-07-01 Derivados de 6-(morfolin-4-il)-pirimidin-4(3h)-ona, su preparacion y su utilizacion farmaceutica como inhibidores de la fosforilacion de akt(pkb)

Country Status (7)

Country Link
US (1) US8507483B2 (es)
EP (1) EP2448932B1 (es)
JP (1) JP5680639B2 (es)
AR (1) AR077628A1 (es)
TW (1) TWI477500B (es)
UY (1) UY32756A (es)
WO (1) WO2011001115A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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)
ES2786298T3 (es) 2011-03-03 2020-10-09 Zalicus Pharmaceuticals Ltd Inhibidores de benzimidazol del canal de sodio
US9828348B2 (en) 2013-11-08 2017-11-28 Purdue Pharma L.P. Benzimidazole derivatives and use thereof

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6096753A (en) * 1996-12-05 2000-08-01 Amgen Inc. Substituted pyrimidinone and pyridone compounds and methods of use
PT1257537E (pt) 2000-01-24 2007-08-03 Astrazeneca Ab Compostos terapêuticos morfolino-substituídos.
GB0119865D0 (en) * 2001-08-14 2001-10-10 Cancer Res Campaign Tech DNA-PK inhibitors
CA2485148A1 (en) * 2002-05-09 2003-11-20 Cytokinetics, Inc. Pyrimidinone compounds, compositions and methods
US7598377B2 (en) 2002-08-16 2009-10-06 Astrazeneca Ab Inhibition of phosphoinositide 3-kinase β
AR054438A1 (es) 2005-04-15 2007-06-27 Kudos Pharm Ltd Inhibidores de adn -pk
EP1895997A2 (en) 2005-05-26 2008-03-12 Kudos Pharmaceuticals Ltd Use of dna-pk inhibition to sensitise atm deficient cancers to dna-damaging cancer therapies
WO2008064244A2 (en) 2006-11-20 2008-05-29 The Trustees Of Columbia University In The City Of New York Phosphoinositide modulation for the treatment of neurodegenerative diseases
WO2008148074A2 (en) 2007-05-24 2008-12-04 Research Foundation Of State University Of New York Inhibitors of mtor and methods of treatment using same
CA2692725A1 (en) 2007-07-09 2009-01-15 Astrazeneca Ab Compound - 946
EP2178866A2 (en) 2007-07-09 2010-04-28 AstraZeneca AB Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
EA018708B1 (ru) 2007-07-09 2013-10-30 Астразенека Аб ПРОИЗВОДНЫЕ МОРФОЛИНОПИРИМИДИНА, ИСПОЛЬЗУЕМЫЕ ПРИ ЗАБОЛЕВАНИЯХ, СВЯЗАННЫХ С mTOR КИНАЗОЙ И/ИЛИ PI3K
AU2008273889B2 (en) 2007-07-09 2012-03-08 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases

Also Published As

Publication number Publication date
US8507483B2 (en) 2013-08-13
JP2012531465A (ja) 2012-12-10
US20120172360A1 (en) 2012-07-05
EP2448932A1 (fr) 2012-05-09
TW201103928A (en) 2011-02-01
JP5680639B2 (ja) 2015-03-04
EP2448932B1 (fr) 2014-03-05
TWI477500B (zh) 2015-03-21
WO2011001115A1 (fr) 2011-01-06
UY32756A (es) 2011-01-31

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