PE20090944A1 - PIRIMIDINAS BICICLICAS FUSIONADAS COMO INHIBIDORES DE LA VIA Pi3K/AKT - Google Patents
PIRIMIDINAS BICICLICAS FUSIONADAS COMO INHIBIDORES DE LA VIA Pi3K/AKTInfo
- Publication number
- PE20090944A1 PE20090944A1 PE2008001378A PE2008001378A PE20090944A1 PE 20090944 A1 PE20090944 A1 PE 20090944A1 PE 2008001378 A PE2008001378 A PE 2008001378A PE 2008001378 A PE2008001378 A PE 2008001378A PE 20090944 A1 PE20090944 A1 PE 20090944A1
- Authority
- PE
- Peru
- Prior art keywords
- phenyl
- pyrimidine
- methyl
- pi3k
- triazol
- Prior art date
Links
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 title 1
- 108091007960 PI3Ks Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000003230 pyrimidines Chemical class 0.000 title 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- -1 AMINO Chemical class 0.000 abstract 3
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical class C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 abstract 2
- SRNKZYRMFBGSGE-UHFFFAOYSA-N [1,2,4]triazolo[1,5-a]pyrimidine Chemical compound N1=CC=CN2N=CN=C21 SRNKZYRMFBGSGE-UHFFFAOYSA-N 0.000 abstract 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical group [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen(.) Chemical compound [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- INSWZAQOISIYDT-UHFFFAOYSA-N imidazo[1,2-a]pyrimidine Chemical compound C1=CC=NC2=NC=CN21 INSWZAQOISIYDT-UHFFFAOYSA-N 0.000 abstract 1
- 230000037361 pathway Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (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)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
REFERIDA A UN DERIVADO DE PIRIMIDINA DE FORMULA (I), DONDE EL ANILLO B Y LA PIRIMIDINA A LA CUAL ESTA FUSIONADO FORMAN UN SISTEMA DE ANILLOS SELECCIONADOS DE (a), (b) Y (c); R1 ES H, ALQUILO C1-C4, HALOGENO, AMINO, ENTRE OTROS; R3 ES H O ALQUILO C1-C4; R4 ES FENILO O TIENILO; R5 ES H, ALCOXI C1-C4, AMINO, CICLOALQUILO C3-C7, ENTRE OTROS; R6 ES H O ALQUILO C1-C4; R7 ES -W-Y; W ES HETEROARILENO MONOCICLICO DE 5 MIEMBROS QUE COMPRENDE UN ATOMO DE NITROGENO Y OPCIONALMENTE HETEROATOMOS ADICIONALES SELECCIONADOS DE O, N Y S; Y ES FENILO O HETEROARILO MONOCICLICO DE 5 O 6 MIEMBROS QUE COMPRENDE UN ATOMO DE NITROGENO Y OPCIONALMENTE HETEROATOMOS ADICIONALES SELECCIONADOS DE O, N Y S. SON COMPUESTOS PREFERIDOS: 6-FENIL-7-(4-{[4-(3-PIRIDIN-2-IL-1,2,4-TRIAZOL-5-IL)PIPERIDIN-1-IL]METIL}FENIL)IMIDAZO[1,2a]-PIRIMIDINA, 6-FENIL-5-(4-{[4-(5-PIRIDIN-2-IL-1,2,4-TRIAZOL-3-IL)PIPERIDIN-1-IL]METILçFENIL)[1,2,4]TRIAZOLO[1,5a]-PIRIMIDINA, 2-METIL-6-FENIL-5-(4-{[4-(5-PIRIDIN-2-IL-1,2,4-TRIAZOL-3-IL)PIPERIDIN-1-IL]METIL}FENIL)[1,2,4]-TRIAZOLO[1,5-a]PIRIMIDINA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHICIDORES DE LA VIA Pi3K/Akt Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES PROLIFERATIVAS
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN1572MU2007 | 2007-08-14 | ||
| EP07118736A EP2050748A1 (en) | 2007-10-18 | 2007-10-18 | Novel fused pyrimidines |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20090944A1 true PE20090944A1 (es) | 2009-08-09 |
Family
ID=40153211
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008001378A PE20090944A1 (es) | 2007-08-14 | 2008-08-14 | PIRIMIDINAS BICICLICAS FUSIONADAS COMO INHIBIDORES DE LA VIA Pi3K/AKT |
Country Status (37)
| Country | Link |
|---|---|
| US (2) | US7776864B2 (es) |
| EP (1) | EP2188291B1 (es) |
| JP (1) | JP5344637B2 (es) |
| KR (1) | KR20100053556A (es) |
| CN (1) | CN101778851B (es) |
| AR (1) | AR067945A1 (es) |
| AU (1) | AU2008288392B2 (es) |
| BR (1) | BRPI0815207A2 (es) |
| CA (1) | CA2694058C (es) |
| CL (1) | CL2008002398A1 (es) |
| CO (1) | CO6260077A2 (es) |
| CR (1) | CR11270A (es) |
| CY (1) | CY1113486T1 (es) |
| DK (1) | DK2188291T3 (es) |
| DO (1) | DOP2010000058A (es) |
| EA (1) | EA020996B1 (es) |
| EC (1) | ECSP109964A (es) |
| ES (1) | ES2396177T3 (es) |
| HN (1) | HN2010000313A (es) |
| HR (1) | HRP20121022T1 (es) |
| IL (1) | IL203163A (es) |
| MA (1) | MA31608B1 (es) |
| MX (1) | MX2010001746A (es) |
| MY (1) | MY169738A (es) |
| NZ (1) | NZ583267A (es) |
| PA (1) | PA8793201A1 (es) |
| PE (1) | PE20090944A1 (es) |
| PL (1) | PL2188291T3 (es) |
| PT (1) | PT2188291E (es) |
| RS (1) | RS52559B (es) |
| SI (1) | SI2188291T1 (es) |
| SV (1) | SV2010003483A (es) |
| TN (1) | TN2010000070A1 (es) |
| TW (1) | TWI439272B (es) |
| UA (1) | UA99735C2 (es) |
| UY (1) | UY31293A1 (es) |
| WO (1) | WO2009021992A2 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA97257C2 (en) * | 2006-10-19 | 2012-01-25 | Такеда Фармасьютикал Компани Лимитед | Indole derivatives |
| UY31293A1 (es) | 2007-08-14 | 2009-03-31 | Pirimidinas biciclicas fusionadas | |
| JP5599783B2 (ja) | 2008-05-30 | 2014-10-01 | アムジエン・インコーポレーテツド | Ｐｉ３キナーゼの阻害薬 |
| KR20110114663A (ko) * | 2009-02-13 | 2011-10-19 | 바이엘 파마 악티엔게젤샤프트 | 융합된 피리미딘 |
| EP2396331B1 (en) * | 2009-02-13 | 2013-10-16 | Bayer Intellectual Property GmbH | Fused pyrimidines as akt inhibitors |
| WO2010114780A1 (en) | 2009-04-01 | 2010-10-07 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| WO2010125799A1 (ja) | 2009-04-27 | 2010-11-04 | 塩野義製薬株式会社 | Pi3k阻害活性を有するウレア誘導体 |
| US20130184273A1 (en) * | 2010-07-13 | 2013-07-18 | Bayer Intellectual Property Gmbh | Bicyclic pyrimidines |
| ES2539257T3 (es) | 2010-07-28 | 2015-06-29 | Bayer Intellectual Property Gmbh | Imidazo[1,2-b]piridazinas sustituidas |
| EA024890B1 (ru) | 2011-04-07 | 2016-10-31 | Байер Интеллектчуал Проперти Гмбх | Имидазопиридазины в качестве ингибиторов akt киназы |
| RU2644769C2 (ru) | 2013-01-23 | 2018-02-14 | Астразенека Аб | Химические соединения |
| US20140274685A1 (en) | 2013-03-15 | 2014-09-18 | Bayer Cropscience Lp | Compositions, additives, and methods for mitigating or controlling seed dust |
| UA121297C2 (uk) * | 2013-03-15 | 2020-05-12 | Байєр Кропсайєнс Лп | Композиції, добавки та способи зменшення або контролювання пилу насіння |
| WO2019055750A1 (en) | 2017-09-15 | 2019-03-21 | Aduro Biotech, Inc. | PYRAZOLOPYRIMIDINONE COMPOUNDS AND USES THEREOF |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004502691A (ja) | 2000-06-30 | 2004-01-29 | ワイス | 抗癌薬としての置換トリアゾロピリミジン |
| US7449488B2 (en) * | 2002-06-04 | 2008-11-11 | Schering Corporation | Pyrazolopyrimidines as protein kinase inhibitors |
| WO2004096131A2 (en) | 2003-04-24 | 2004-11-11 | Merck & Co., Inc. | Inhibitors of akt activity |
| EP1737843B1 (en) * | 2004-04-09 | 2011-02-23 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| TW200618800A (en) * | 2004-08-03 | 2006-06-16 | Uriach Y Compania S A J | Heterocyclic compounds |
| AU2005290081B2 (en) * | 2004-08-23 | 2010-12-02 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
| WO2006065601A2 (en) | 2004-12-15 | 2006-06-22 | Merck & Co., Inc. | Inhibitors of akt activity |
| US7994172B2 (en) * | 2004-12-28 | 2011-08-09 | Exelixis, Inc. | [1H-pyrazolo[3, 4-D]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (P70s6k, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases |
| AU2006216998B2 (en) | 2005-02-14 | 2010-12-23 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
| AU2006258124B8 (en) | 2005-06-10 | 2010-01-07 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
| UY31293A1 (es) | 2007-08-14 | 2009-03-31 | Pirimidinas biciclicas fusionadas | |
| KR20110114663A (ko) * | 2009-02-13 | 2011-10-19 | 바이엘 파마 악티엔게젤샤프트 | 융합된 피리미딘 |
-
2008
- 2008-08-14 UY UY31293A patent/UY31293A1/es not_active Application Discontinuation
- 2008-08-14 KR KR1020107003246A patent/KR20100053556A/ko not_active Abandoned
- 2008-08-14 EP EP08787224A patent/EP2188291B1/en active Active
- 2008-08-14 CL CL2008002398A patent/CL2008002398A1/es unknown
- 2008-08-14 JP JP2010520586A patent/JP5344637B2/ja not_active Expired - Fee Related
- 2008-08-14 DK DK08787224.8T patent/DK2188291T3/da active
- 2008-08-14 NZ NZ583267A patent/NZ583267A/en not_active IP Right Cessation
- 2008-08-14 RS RS20120556A patent/RS52559B/sr unknown
- 2008-08-14 PE PE2008001378A patent/PE20090944A1/es not_active Application Discontinuation
- 2008-08-14 WO PCT/EP2008/060690 patent/WO2009021992A2/en not_active Ceased
- 2008-08-14 MX MX2010001746A patent/MX2010001746A/es active IP Right Grant
- 2008-08-14 ES ES08787224T patent/ES2396177T3/es active Active
- 2008-08-14 PA PA20088793201A patent/PA8793201A1/es unknown
- 2008-08-14 CN CN2008801031086A patent/CN101778851B/zh not_active Expired - Fee Related
- 2008-08-14 SI SI200830848T patent/SI2188291T1/sl unknown
- 2008-08-14 PT PT87872248T patent/PT2188291E/pt unknown
- 2008-08-14 US US12/191,703 patent/US7776864B2/en not_active Expired - Fee Related
- 2008-08-14 TW TW097131066A patent/TWI439272B/zh not_active IP Right Cessation
- 2008-08-14 BR BRPI0815207A patent/BRPI0815207A2/pt not_active IP Right Cessation
- 2008-08-14 AU AU2008288392A patent/AU2008288392B2/en not_active Ceased
- 2008-08-14 UA UAA201002746A patent/UA99735C2/uk unknown
- 2008-08-14 MY MYPI2010000150A patent/MY169738A/en unknown
- 2008-08-14 HR HRP20121022AT patent/HRP20121022T1/hr unknown
- 2008-08-14 EA EA201000298A patent/EA020996B1/ru not_active IP Right Cessation
- 2008-08-14 CA CA2694058A patent/CA2694058C/en not_active Expired - Fee Related
- 2008-08-14 PL PL08787224T patent/PL2188291T3/pl unknown
- 2008-08-15 AR ARP080103562A patent/AR067945A1/es unknown
-
2010
- 2010-01-06 IL IL203163A patent/IL203163A/en not_active IP Right Cessation
- 2010-02-12 SV SV2010003483A patent/SV2010003483A/es unknown
- 2010-02-12 TN TNP2010000070A patent/TN2010000070A1/fr unknown
- 2010-02-12 CO CO10015919A patent/CO6260077A2/es active IP Right Grant
- 2010-02-12 CR CR11270A patent/CR11270A/es unknown
- 2010-02-12 DO DO2010000058A patent/DOP2010000058A/es unknown
- 2010-02-12 EC EC2010009964A patent/ECSP109964A/es unknown
- 2010-02-12 HN HN2010000313A patent/HN2010000313A/es unknown
- 2010-02-12 MA MA32617A patent/MA31608B1/fr unknown
- 2010-03-25 US US12/731,880 patent/US8614218B2/en not_active Expired - Fee Related
-
2012
- 2012-12-13 CY CY20121101220T patent/CY1113486T1/el unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PE20120534A1 (es) | PIRIMIDINAS FUSIONADAS COMO INHIBIDORES DE Akt | |
| PE20090596A1 (es) | Imidazoles biciclicos fusionados | |
| PE20091833A1 (es) | Derivados heterociclicos espiro biciclicos o heterociclicos biciclicos, puenteados, de pirazolo [1,5-a]pirimidinas como inhibidores de quinasas raf y metodos para su preparacion | |
| PE20140390A1 (es) | Derivados de imidazo[1,2-b]piridazina e imidazo[4,5-b]piridina como inhibidores de jak | |
| PE20080315A1 (es) | DERIVADOS DE PIRAZOLO-[3,4-d]-PIRIMIDINAS COMO INHIBIDORES DE CINASA PI-3 | |
| PE20090370A1 (es) | Derivados de heterociclo fusionado como inhibidores de quinasa | |
| PE20151249A1 (es) | Derivados de pirazolopirimidina como inhibidores de jak quinasas | |
| PE20110560A1 (es) | NUEVOS DERIVADOS DE TRIAZOLO[4,3-a]PIRIDINA, SU PROCEDIMIENTO DE PREPARACION, SU APLICACION COMO MEDICAMENTOS, COMPOSICIONES FARMACEUTICAS Y NUEVA UTILIZACION PARTICULARMENTE COMO INHIBIDORES DE MET | |
| PE20141557A1 (es) | Derivado de pirazoloquinolina | |
| PE20170189A1 (es) | Nuevos derivados de pirazolo pirimidina y su uso como inhibidores de malt1 | |
| PE20110545A1 (es) | Compuestos de triazolopiridina como inhibidores de jak | |
| PE20091211A1 (es) | Derivados de pirazolopirimidina como moduladores de pde9a | |
| PE20110411A1 (es) | Imidazopiridazinacarbonitrilos como inhibidores de quinasa | |
| PE20110995A1 (es) | DERIVADOS DE PIRROLO[3,4-e]PIRIMIDINA COMO INHIBIDORES DE PDE1 | |
| HRP20191268T1 (hr) | Derivati tieno[2,3-c]pirol-4-ona kao inhibitori erk | |
| PE20080548A1 (es) | Derivados de [4,5']bipirimidinil-6,4'-diamina como inhibidores de cinasa de proteina | |
| EA201170771A1 (ru) | Органические соединения | |
| PE20090492A1 (es) | Compuestos heterociclos como inhibidores de cinasa de fosfatidil-inositol-3 | |
| PE20120107A1 (es) | Inhibidores de proteina cinasa | |
| PE20081612A1 (es) | Analogos de las pterinas | |
| PE20091116A1 (es) | Derivados de piridina y pirazina como inhibidores de tirosina quinasas | |
| PE20110944A1 (es) | DERIVADOS DE PIRAZOLO[3,4-d]PIRIMIDINA COMO INHIBIDORES PDE1 | |
| PE20170666A1 (es) | 2-(morfolin-4-il)-1,7-naftiridinas | |
| PE20091083A1 (es) | Moduladores tieno- y furo- pirimidina del receptor de histamina h4 | |
| MX2009010728A (es) | Compuestos de imidazo[1,2-a]piridina como inhibidores de la tirosina-cinasa repectora. |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |