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
Links
Classifications
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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
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- 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
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- 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
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.
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)
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) |
CA2828456C (en) * | 2011-03-03 | 2021-05-04 | Zalicus Pharmaceuticals Ltd. | N-benzl-amino-carboxamide inhibitors of the sodium channel |
US9828348B2 (en) | 2013-11-08 | 2017-11-28 | Purdue Pharma L.P. | Benzimidazole derivatives and use thereof |
Family Cites Families (13)
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 |
ATE363471T1 (de) | 2000-01-24 | 2007-06-15 | Astrazeneca Ab | Durch einen morpholinrest substituierte therapeutische verbindungen |
GB0119865D0 (en) | 2001-08-14 | 2001-10-10 | Cancer Res Campaign Tech | DNA-PK inhibitors |
RU2004135554A (ru) * | 2002-05-09 | 2006-01-20 | Цитокинетикс, Инк. (Us) | Пиримидиноны, композиции на их основе и способы их использования |
CA2495661C (en) | 2002-08-16 | 2011-06-14 | Kinacia Pty Ltd. | Inhibition of phosphoinositide 3-kinase beta |
AR053358A1 (es) * | 2005-04-15 | 2007-05-02 | Cancer Rec Tech Ltd | Inhibidores de adn - pk |
JP2008542253A (ja) | 2005-05-26 | 2008-11-27 | クドス ファーマシューティカルズ リミテッド | Dna損傷癌療法に対してatm欠損癌を感作するためのdna−pk阻害の使用 |
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 |
US20100227858A1 (en) | 2007-07-09 | 2010-09-09 | Astrazeneca Ab | Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases |
WO2009007749A2 (en) | 2007-07-09 | 2009-01-15 | Astrazeneca Ab | Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases |
CN101801962A (zh) | 2007-07-09 | 2010-08-11 | 阿斯利康(瑞典)有限公司 | 用于治疗增殖疾病的三取代嘧啶衍生物 |
BRPI0814688A2 (pt) | 2007-07-09 | 2017-06-06 | Astrazeneca Ab | composto, uso de um composto, métodos para produzir um efeito antiproliferativo em um animal de sangue quente, e para tratar doenças, e, composição farmacêutica |
-
2010
- 2010-07-01 WO PCT/FR2010/051376 patent/WO2011001115A1/fr active Application Filing
- 2010-07-01 JP JP2012518121A patent/JP5680639B2/ja not_active Expired - Fee Related
- 2010-07-01 AR ARP100102348A patent/AR077628A1/es unknown
- 2010-07-01 EP EP10742015.0A patent/EP2448932B1/fr active Active
- 2010-07-02 TW TW099121936A patent/TWI477500B/zh not_active IP Right Cessation
- 2010-07-02 UY UY0001032756A patent/UY32756A/es not_active Application Discontinuation
-
2011
- 2011-12-20 US US13/331,199 patent/US8507483B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
WO2011001115A1 (fr) | 2011-01-06 |
EP2448932B1 (fr) | 2014-03-05 |
US8507483B2 (en) | 2013-08-13 |
US20120172360A1 (en) | 2012-07-05 |
JP5680639B2 (ja) | 2015-03-04 |
EP2448932A1 (fr) | 2012-05-09 |
UY32756A (es) | 2011-01-31 |
TWI477500B (zh) | 2015-03-21 |
JP2012531465A (ja) | 2012-12-10 |
TW201103928A (en) | 2011-02-01 |
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