PE20080068A1 - Compuestos derivados de pirimidina como inhibidores de la quinasa aurora - Google Patents
Compuestos derivados de pirimidina como inhibidores de la quinasa auroraInfo
- Publication number
- PE20080068A1 PE20080068A1 PE2007000569A PE2007000569A PE20080068A1 PE 20080068 A1 PE20080068 A1 PE 20080068A1 PE 2007000569 A PE2007000569 A PE 2007000569A PE 2007000569 A PE2007000569 A PE 2007000569A PE 20080068 A1 PE20080068 A1 PE 20080068A1
- Authority
- PE
- Peru
- Prior art keywords
- cycloalkyl
- inhibitors
- aryl
- alkyl
- pyrimidine
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 108091000080 Phosphotransferase Proteins 0.000 title 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 239000005441 aurora Substances 0.000 title 1
- 102000020233 phosphotransferase Human genes 0.000 title 1
- 102000003989 Aurora kinases Human genes 0.000 abstract 1
- 108090000433 Aurora kinases Proteins 0.000 abstract 1
- 208000007766 Kaposi sarcoma Diseases 0.000 abstract 1
- -1 PYRIMIDINE DERIVATIVE COMPOUNDS Chemical class 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 206010003246 arthritis Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 208000032839 leukemia Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic 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
- C07D405/02—Heterocyclic 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
- C07D405/12—Heterocyclic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/02—Heterocyclic 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
- C07D401/12—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/14—Heterocyclic 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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic 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
- C07D405/14—Heterocyclic 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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Transplantation (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE PIRIMIDINA DE FORMULA (1) DONDE X ES N O CH; R1 ES CICLOALQUILO(C3-C10) OPCIONALMENTE SUSTITUIDO CON R3 O R4, DONDE R3 ES C(O)Rc, C(O)ORc, S(O)2Rc, ENTRE OTROS, DONDE Rc ES H, ALQUILO(C1-C6), CICLOALQUILO(C3-C10), ARILO(C6-C10), ENTRE OTROS; R4 ES Ra O Rb, DONDE Ra ES ALQUILO(C1-C6), CICLOALQUILO(C3-C10), ARILO(C6-C10), ENTRE OTROS; Rb ES =O, HALOALQUILOXI(C1-C3), OCF3, CN, ENTRE OTROS; R2 ES H, HALOGENO, CN, NO2, ALQUILO(C1-C4), ENTRE OTROS; Rg ES H, ALQUILO(C1-C6), CICLOALQUILO(C3-C8), ARILO(C6-C10), ENTRE OTROS; m ES 0 O 1; n ES DE 0 A 4; p ES DE 0 A 2. SON COMPUESTOS PREFERIDOS: 4-[4-((1R,2S)-2-ISOPROPILCARBAMOIL-CICLOPENTILAMINO)-5-TRIFLUOROMETIL-PIRIMIDIN-2-ILAMINO]-N-METIL-N-(1,2,2,6,6-PENTAMETIL-PIPERIDIN-4-IL)-BENZAMIDA, N-ISOPROPIL-4-[4-((1R,2S)-2-ISOPROPILCARBAMOIL-CICLOPENTILAMINO)-5-TRIFLUOROMETIL-PIRIMIDIN-2-ILAMINO]-N-(1-METIL-PIPERIDIN-4-IL)-BENZAMIDA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA QUINASA AURORA SIENDO UTILES EN EL TRATAMIENTO DE SARCOMA DE KAPOSI, ARTRITIS, LEUCEMIA, PSORIASIS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06113967 | 2006-05-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20080068A1 true PE20080068A1 (es) | 2008-03-17 |
Family
ID=37102115
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2007000569A PE20080068A1 (es) | 2006-05-15 | 2007-05-11 | Compuestos derivados de pirimidina como inhibidores de la quinasa aurora |
| PE2011001452A PE20120006A1 (es) | 2006-05-15 | 2007-05-11 | Compuestos derivados de pirimidina como inhibidores de la quinasa aurora |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2011001452A PE20120006A1 (es) | 2006-05-15 | 2007-05-11 | Compuestos derivados de pirimidina como inhibidores de la quinasa aurora |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US8623887B2 (es) |
| EP (2) | EP2027107B1 (es) |
| JP (1) | JP5247681B2 (es) |
| KR (1) | KR20090018955A (es) |
| CN (1) | CN101443325A (es) |
| AR (1) | AR060890A1 (es) |
| AT (1) | ATE545641T1 (es) |
| AU (1) | AU2007251553A1 (es) |
| BR (1) | BRPI0712400A2 (es) |
| CA (1) | CA2647238A1 (es) |
| EA (1) | EA200802214A1 (es) |
| EC (1) | ECSP088905A (es) |
| IL (1) | IL195218A0 (es) |
| MX (1) | MX2008014500A (es) |
| NO (1) | NO20083845L (es) |
| NZ (1) | NZ573506A (es) |
| PE (2) | PE20080068A1 (es) |
| TW (1) | TW200815392A (es) |
| UA (1) | UA94944C2 (es) |
| WO (1) | WO2007132010A1 (es) |
| ZA (1) | ZA200807581B (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20100144706A1 (en) * | 2006-12-22 | 2010-06-10 | Boehringer Ingelheim International Gmbh | Compounds |
| CL2008001943A1 (es) | 2007-07-02 | 2009-09-11 | Boehringer Ingelheim Int | Compuestos derivados de fenil-triazol, inhibidores de enzimas de señales especificas que participan del control de la proliferacion celular; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar cancer, infecciones, enfermedades inflamatorias y autoinmunes. |
| CA2718858A1 (en) * | 2008-03-20 | 2009-09-24 | Boehringer Ingelheim International Gmbh | Selective synthesis of substituted pyrimidines |
| CL2009000600A1 (es) * | 2008-03-20 | 2010-05-07 | Bayer Cropscience Ag | Uso de compuestos de diaminopirimidina como agentes fitosanitarios; compuestos de diaminopirimidina; su procedimiento de preparacion; agente que los contiene; procedimiento para la preparacion de dicho agente; y procedimiento para combatir plagas de animales y/u hongos dañinos patogenos de plantas. |
| UY31714A (es) * | 2008-03-20 | 2009-11-10 | Boehringer Ingelheim Int | Preparación selectiva de pirimidinas sustituidas |
| PE20110294A1 (es) | 2008-09-29 | 2011-05-26 | Boehringer Ingelheim Int | Compuestos heterociclicos como inhibidores de enzimas de senal especifica |
| US20110071158A1 (en) * | 2009-03-18 | 2011-03-24 | Boehringer Ingelheim International Gmbh | New compounds |
| US8410126B2 (en) * | 2009-05-29 | 2013-04-02 | Boehringer Ingelheim International Gmbh | Pyrimidine inhibitors of PKTK2 |
| US8933227B2 (en) * | 2009-08-14 | 2015-01-13 | Boehringer Ingelheim International Gmbh | Selective synthesis of functionalized pyrimidines |
| US8729265B2 (en) | 2009-08-14 | 2014-05-20 | Boehringer Ingelheim International Gmbh | Regioselective preparation of 2-amino-5-trifluoromethylpyrimidine derivatives |
| US8466155B2 (en) | 2009-10-02 | 2013-06-18 | Boehringer Ingelheim International Gmbh | Pyrimidines |
| US8865703B2 (en) | 2010-03-26 | 2014-10-21 | Boehringer Ingelheim International Gmbh | Pyridyltriazoles |
| US20120107304A1 (en) * | 2010-04-27 | 2012-05-03 | Boehringer Ingelheim International Gmbh | Combination therapy in treatment of oncological and fibrotic diseases |
| JP5713367B2 (ja) | 2010-06-04 | 2015-05-07 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Lrrk2モジュレーターとしてのアミノピリミジン誘導体 |
| WO2012059932A1 (en) * | 2010-11-01 | 2012-05-10 | Aurigene Discovery Technologies Limited | 2, 4 -diaminopyrimidine derivatives as protein kinase inhibitors |
| BR112013011600B1 (pt) | 2010-11-10 | 2022-01-11 | Genentech, Inc | Derivados de pirazol aminopirimidina, seu uso e composição que os compreende |
| US8710055B2 (en) | 2010-12-21 | 2014-04-29 | Boehringer Ingelheim International Gmbh | Triazolylphenyl sulfonamides as serine/threonine kinase inhibitors |
| JP6275846B2 (ja) * | 2013-12-05 | 2018-02-07 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | 求電子性官能基を有するヘテロアリールピリドン及びアザ−ピリドン化合物 |
| EP3736268A1 (en) * | 2013-12-20 | 2020-11-11 | Signal Pharmaceuticals, LLC | Process for the preparation of substituted diaminopyrimidyl compounds |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE342892T1 (de) | 1998-08-29 | 2006-11-15 | Astrazeneca Ab | Pyrimidine verbindungen |
| KR100658489B1 (ko) | 1998-11-10 | 2006-12-18 | 얀센 파마슈티카 엔.브이. | Hiv 복제를 억제하는 피리미딘 |
| GB9828511D0 (en) | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
| GB0007371D0 (en) | 2000-03-28 | 2000-05-17 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0016877D0 (en) | 2000-07-11 | 2000-08-30 | Astrazeneca Ab | Chemical compounds |
| RS94703A (sr) | 2001-05-29 | 2007-02-05 | Schering Aktiengesellschaft, | Cdk-inhibirajući pirimidini, njihovo dobijanje i primena kao sredstva za lečenje |
| MXPA05001096A (es) | 2002-07-29 | 2005-11-23 | Rigel Pharmaceuticals Inc | Metodos para tratamiento o prevencion de enfermedades autoinmunes con compuestos de 2,4-diamino-pirimidina. |
| ATE433447T1 (de) | 2003-02-20 | 2009-06-15 | Smithkline Beecham Corp | Pyrimiidinverbindungen |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| US20050113398A1 (en) * | 2003-08-07 | 2005-05-26 | Ankush Argade | 2,4-pyrimidinediamine compounds and uses as anti-proliferative agents |
| WO2005118544A2 (en) * | 2004-05-18 | 2005-12-15 | Rigel Pharmaceuticals, Inc. | Cycloalkyl substituted pyrimidinediamine compounds and their uses |
| EP1598343A1 (de) | 2004-05-19 | 2005-11-23 | Boehringer Ingelheim International GmbH | 2-Arylaminopyrimidine als PLK Inhibitoren |
| US7521457B2 (en) | 2004-08-20 | 2009-04-21 | Boehringer Ingelheim International Gmbh | Pyrimidines as PLK inhibitors |
| US20070032514A1 (en) | 2005-07-01 | 2007-02-08 | Zahn Stephan K | 2,4-diamino-pyrimidines as aurora inhibitors |
-
2007
- 2007-05-11 AR ARP070102041A patent/AR060890A1/es unknown
- 2007-05-11 US US11/747,337 patent/US8623887B2/en active Active
- 2007-05-11 PE PE2007000569A patent/PE20080068A1/es not_active Application Discontinuation
- 2007-05-11 PE PE2011001452A patent/PE20120006A1/es not_active Application Discontinuation
- 2007-05-14 TW TW096117060A patent/TW200815392A/zh unknown
- 2007-05-15 MX MX2008014500A patent/MX2008014500A/es unknown
- 2007-05-15 KR KR1020087030445A patent/KR20090018955A/ko not_active Withdrawn
- 2007-05-15 BR BRPI0712400-7A patent/BRPI0712400A2/pt not_active IP Right Cessation
- 2007-05-15 CN CNA2007800176717A patent/CN101443325A/zh active Pending
- 2007-05-15 UA UAA200813829A patent/UA94944C2/ru unknown
- 2007-05-15 JP JP2009510448A patent/JP5247681B2/ja active Active
- 2007-05-15 EP EP07729171A patent/EP2027107B1/de active Active
- 2007-05-15 WO PCT/EP2007/054723 patent/WO2007132010A1/de not_active Ceased
- 2007-05-15 NZ NZ573506A patent/NZ573506A/en not_active IP Right Cessation
- 2007-05-15 CA CA002647238A patent/CA2647238A1/en not_active Abandoned
- 2007-05-15 EA EA200802214A patent/EA200802214A1/ru unknown
- 2007-05-15 AT AT07729171T patent/ATE545641T1/de active
- 2007-05-15 EP EP11159659A patent/EP2357181A1/de not_active Withdrawn
- 2007-05-15 AU AU2007251553A patent/AU2007251553A1/en not_active Abandoned
-
2008
- 2008-09-03 ZA ZA200807581A patent/ZA200807581B/xx unknown
- 2008-09-05 NO NO20083845A patent/NO20083845L/no not_active Application Discontinuation
- 2008-11-11 IL IL195218A patent/IL195218A0/en unknown
- 2008-11-21 EC EC2008008905A patent/ECSP088905A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| BRPI0712400A2 (pt) | 2012-10-16 |
| PE20120006A1 (es) | 2012-02-02 |
| KR20090018955A (ko) | 2009-02-24 |
| NO20083845L (no) | 2008-12-11 |
| EP2027107A1 (de) | 2009-02-25 |
| AR060890A1 (es) | 2008-07-23 |
| ZA200807581B (en) | 2010-05-26 |
| ECSP088905A (es) | 2008-12-30 |
| WO2007132010A1 (de) | 2007-11-22 |
| EP2357181A1 (de) | 2011-08-17 |
| TW200815392A (en) | 2008-04-01 |
| EP2027107B1 (de) | 2012-02-15 |
| CN101443325A (zh) | 2009-05-27 |
| EA200802214A1 (ru) | 2009-06-30 |
| UA94944C2 (ru) | 2011-06-25 |
| US8623887B2 (en) | 2014-01-07 |
| AU2007251553A1 (en) | 2007-11-22 |
| NZ573506A (en) | 2011-12-22 |
| ATE545641T1 (de) | 2012-03-15 |
| JP5247681B2 (ja) | 2013-07-24 |
| MX2008014500A (es) | 2008-11-27 |
| JP2009537485A (ja) | 2009-10-29 |
| CA2647238A1 (en) | 2007-11-22 |
| IL195218A0 (en) | 2009-09-22 |
| US20090163467A1 (en) | 2009-06-25 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |