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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Oncology (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 |
|---|---|---|---|---|
| EP2109605B1 (en) * | 2006-12-22 | 2013-02-20 | Boehringer Ingelheim International GmbH | 2- [(phenylamino) -pyrimidin-4ylamin0] -cyclopentane carboxamide derivatives and related compounds as inhibitors of kinases of the cell cycle for the treatment of cancer |
| 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. |
| EP2268621A1 (en) * | 2008-03-20 | 2011-01-05 | Boehringer Ingelheim International GmbH | Regioselective preparation of substituted pyrimidines |
| UY31714A (es) * | 2008-03-20 | 2009-11-10 | Boehringer Ingelheim Int | Preparación selectiva de pirimidinas sustituidas |
| 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. |
| MX2011003292A (es) | 2008-09-29 | 2011-04-21 | Boehringer Ingelheim Int | Compuestos antiproliferativos. |
| 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 |
| EP2464633A1 (en) | 2009-08-14 | 2012-06-20 | Boehringer Ingelheim International GmbH | Regioselective preparation of 2-amino-5-trifluoromethylpyrimidine derivatives |
| US8933227B2 (en) | 2009-08-14 | 2015-01-13 | Boehringer Ingelheim International Gmbh | Selective synthesis of functionalized pyrimidines |
| US8466155B2 (en) * | 2009-10-02 | 2013-06-18 | Boehringer Ingelheim International Gmbh | Pyrimidines |
| EP2552907B1 (en) | 2010-03-26 | 2014-10-22 | 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 |
| CN105837519A (zh) | 2010-06-04 | 2016-08-10 | 霍夫曼-拉罗奇有限公司 | 作为lrrk2调节剂的氨基嘧啶衍生物 |
| WO2012059932A1 (en) * | 2010-11-01 | 2012-05-10 | Aurigene Discovery Technologies Limited | 2, 4 -diaminopyrimidine derivatives as protein kinase inhibitors |
| CN103313978B (zh) | 2010-11-10 | 2015-04-15 | 霍夫曼-拉罗奇有限公司 | 作为lrrk2调节剂的吡唑氨基嘧啶衍生物 |
| US8710055B2 (en) | 2010-12-21 | 2014-04-29 | Boehringer Ingelheim International Gmbh | Triazolylphenyl sulfonamides as serine/threonine kinase inhibitors |
| CN105793251B (zh) * | 2013-12-05 | 2018-10-12 | 豪夫迈·罗氏有限公司 | 具有亲电子官能性的杂芳基吡啶酮和氮杂-吡啶酮化合物 |
| RU2016129380A (ru) * | 2013-12-20 | 2018-01-25 | СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | Замещенные диаминопиримидильные соединения, их композиции и способы лечения с их участием |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69933680T2 (de) | 1998-08-29 | 2007-08-23 | Astrazeneca Ab | Pyrimidine verbindungen |
| BRPI9915552B8 (pt) * | 1998-11-10 | 2021-05-25 | Janssen Pharmaceutica Nv | pirimidinas inibidoras da reprodução do hiv |
| 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 |
| PL367130A1 (en) * | 2001-05-29 | 2005-02-21 | Schering Aktiengesellschaft | Cdk inhibiting pyrimidines, production thereof and their use as medicaments |
| DK1534286T3 (da) | 2002-07-29 | 2010-04-26 | Rigel Pharmaceuticals Inc | Fremgangsmåder til behandling eller forebyggelse af autoimmune sygdomme med 2,4-pyrimidindiamin-forbindelser |
| JP4634367B2 (ja) | 2003-02-20 | 2011-02-16 | スミスクライン ビーチャム コーポレーション | ピリミジン化合物 |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| ATE506953T1 (de) * | 2003-08-07 | 2011-05-15 | Rigel Pharmaceuticals Inc | 2,4-pyrimidindiamin-verbindungen und verwendungen als antiproliferative mittel |
| EP1763514A2 (en) * | 2004-05-18 | 2007-03-21 | 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 PE PE2007000569A patent/PE20080068A1/es not_active Application Discontinuation
- 2007-05-11 PE PE2011001452A patent/PE20120006A1/es not_active Application Discontinuation
- 2007-05-11 AR ARP070102041A patent/AR060890A1/es unknown
- 2007-05-11 US US11/747,337 patent/US8623887B2/en active Active
- 2007-05-14 TW TW096117060A patent/TW200815392A/zh unknown
- 2007-05-15 KR KR1020087030445A patent/KR20090018955A/ko not_active Withdrawn
- 2007-05-15 CN CNA2007800176717A patent/CN101443325A/zh active Pending
- 2007-05-15 EP EP07729171A patent/EP2027107B1/de active Active
- 2007-05-15 JP JP2009510448A patent/JP5247681B2/ja active Active
- 2007-05-15 AT AT07729171T patent/ATE545641T1/de active
- 2007-05-15 EP EP11159659A patent/EP2357181A1/de not_active Withdrawn
- 2007-05-15 BR BRPI0712400-7A patent/BRPI0712400A2/pt not_active IP Right Cessation
- 2007-05-15 WO PCT/EP2007/054723 patent/WO2007132010A1/de not_active Ceased
- 2007-05-15 EA EA200802214A patent/EA200802214A1/ru unknown
- 2007-05-15 AU AU2007251553A patent/AU2007251553A1/en not_active Abandoned
- 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 MX MX2008014500A patent/MX2008014500A/es unknown
- 2007-05-15 UA UAA200813829A patent/UA94944C2/ru unknown
-
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 |
|---|---|
| CN101443325A (zh) | 2009-05-27 |
| EP2357181A1 (de) | 2011-08-17 |
| US20090163467A1 (en) | 2009-06-25 |
| CA2647238A1 (en) | 2007-11-22 |
| EP2027107B1 (de) | 2012-02-15 |
| JP5247681B2 (ja) | 2013-07-24 |
| MX2008014500A (es) | 2008-11-27 |
| EA200802214A1 (ru) | 2009-06-30 |
| NZ573506A (en) | 2011-12-22 |
| NO20083845L (no) | 2008-12-11 |
| TW200815392A (en) | 2008-04-01 |
| PE20120006A1 (es) | 2012-02-02 |
| BRPI0712400A2 (pt) | 2012-10-16 |
| AR060890A1 (es) | 2008-07-23 |
| EP2027107A1 (de) | 2009-02-25 |
| UA94944C2 (ru) | 2011-06-25 |
| WO2007132010A1 (de) | 2007-11-22 |
| US8623887B2 (en) | 2014-01-07 |
| ZA200807581B (en) | 2010-05-26 |
| ATE545641T1 (de) | 2012-03-15 |
| ECSP088905A (es) | 2008-12-30 |
| IL195218A0 (en) | 2009-09-22 |
| KR20090018955A (ko) | 2009-02-24 |
| AU2007251553A1 (en) | 2007-11-22 |
| JP2009537485A (ja) | 2009-10-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |