UY32756A - Nuevos derivados de 1h-pirimidin-2-ona, su preparacion y su utilizacion farmaceutica como inhibidores de la fos-forilacion de akt (pkb) - Google Patents
Nuevos derivados de 1h-pirimidin-2-ona, su preparacion y su utilizacion farmaceutica como inhibidores de la fos-forilacion de akt (pkb)Info
- Publication number
- UY32756A UY32756A UY0001032756A UY32756A UY32756A UY 32756 A UY32756 A UY 32756A UY 0001032756 A UY0001032756 A UY 0001032756A UY 32756 A UY32756 A UY 32756A UY 32756 A UY32756 A UY 32756A
- Authority
- UY
- Uruguay
- Prior art keywords
- pkb
- akt
- inhibitors
- forilation
- pirimidin
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 230000026731 phosphorylation Effects 0.000 abstract 1
- 238000006366 phosphorylation reaction Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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
-
- 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
Landscapes
- 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)
- Gastroenterology & Hepatology (AREA)
- Neurosurgery (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Pulmonology (AREA)
- Reproductive Health (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La invención se refiere a los nuevos productos de fórmula (I): en la que: Z representa -O-, -NH, Ncicloalquilo, Nalk o N-fenilo eventualmente sustituidos; n representa O a 4; R1 representa H, Hal, hidroxilo, alquilo o alcoxi; estando los radicales alquilo y alcoxi eventualmente sustituidos; pudiendo representar R1 un resto fenilo fusionado con el fenilo que lleva R1 para formar naftilo; R2 y R3 representan H. Hal o alquilo eventualmente sustituido con uno o varios átomos de halógeno; R4 representa H; estando estos productos bajo todas las formas isómeras y las sales, a título de medicamentos principalmente como inhibidotes de la fosforilación de AKT (PKB).
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 |
|---|---|
| UY32756A true UY32756A (es) | 2011-01-31 |
Family
ID=42646247
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UY0001032756A UY32756A (es) | 2009-07-02 | 2010-07-02 | Nuevos derivados de 1h-pirimidin-2-ona, su preparacion y su utilizacion farmaceutica como inhibidores de la fos-forilacion 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) |
| EP3009427B1 (en) | 2011-03-03 | 2019-12-18 | Zalicus Pharmaceuticals Ltd. | Benzimidazole 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 |
| CN1891699A (zh) | 2000-01-24 | 2007-01-10 | 基纳西亚股份有限公司 | 用于治疗的吗啉代基取代的化合物 |
| GB0119865D0 (en) * | 2001-08-14 | 2001-10-10 | Cancer Res Campaign Tech | DNA-PK inhibitors |
| KR20050036911A (ko) * | 2002-05-09 | 2005-04-20 | 싸이토키네틱스, 인코포레이티드 | 화합물들, 방법 및 조성물 |
| JP4646626B2 (ja) | 2002-08-16 | 2011-03-09 | アストラゼネカ アクチボラグ | ホスホイノシチド3−キナーゼβの阻害 |
| AR053358A1 (es) | 2005-04-15 | 2007-05-02 | Cancer Rec Tech 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 |
| EP2074118A2 (en) | 2007-07-09 | 2009-07-01 | AstraZeneca AB | Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases |
| AU2008273892A1 (en) | 2007-07-09 | 2009-01-15 | Astrazeneca Ab | Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases |
| JP2010533159A (ja) | 2007-07-09 | 2010-10-21 | アストラゼネカ アクチボラグ | 化合物947 |
| ATE554075T1 (de) | 2007-07-09 | 2012-05-15 | Astrazeneca Ab | Bei mit mtor-kinase und/oder pi3k in zusammenhang stehenden krankheiten angewendete morpholinopyrimidinderivate |
-
2010
- 2010-07-01 WO PCT/FR2010/051376 patent/WO2011001115A1/fr not_active Ceased
- 2010-07-01 JP JP2012518121A patent/JP5680639B2/ja not_active Expired - Fee Related
- 2010-07-01 EP EP10742015.0A patent/EP2448932B1/fr active Active
- 2010-07-01 AR ARP100102348A patent/AR077628A1/es unknown
- 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 |
|---|---|
| AR077628A1 (es) | 2011-09-14 |
| EP2448932A1 (fr) | 2012-05-09 |
| JP5680639B2 (ja) | 2015-03-04 |
| WO2011001115A1 (fr) | 2011-01-06 |
| US8507483B2 (en) | 2013-08-13 |
| US20120172360A1 (en) | 2012-07-05 |
| TW201103928A (en) | 2011-02-01 |
| TWI477500B (zh) | 2015-03-21 |
| EP2448932B1 (fr) | 2014-03-05 |
| JP2012531465A (ja) | 2012-12-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 109 | Application deemed to be withdrawn |
Effective date: 20190211 |