CN103038235B - 取代的咪唑并吡嗪 - Google Patents
取代的咪唑并吡嗪 Download PDFInfo
- Publication number
- CN103038235B CN103038235B CN201180038047.1A CN201180038047A CN103038235B CN 103038235 B CN103038235 B CN 103038235B CN 201180038047 A CN201180038047 A CN 201180038047A CN 103038235 B CN103038235 B CN 103038235B
- Authority
- CN
- China
- Prior art keywords
- base
- alkyl
- imidazo
- amino
- pyrazine
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- 0 CC(C([*@]1C=C(C)C#CC)=*(C)C(*)=C1P)=C Chemical compound CC(C([*@]1C=C(C)C#CC)=*(C)C(*)=C1P)=C 0.000 description 11
- AFCJCACHNAVZRS-UHFFFAOYSA-N FC(CCCNc1nc(Br)c[n]2c1ncc2-c(cc1)ccc1-c1cnc(C2CC2)[nH]1)(F)F Chemical compound FC(CCCNc1nc(Br)c[n]2c1ncc2-c(cc1)ccc1-c1cnc(C2CC2)[nH]1)(F)F AFCJCACHNAVZRS-UHFFFAOYSA-N 0.000 description 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
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10164587.7 | 2010-06-01 | ||
| EP10164587 | 2010-06-01 | ||
| PCT/EP2011/058713 WO2011151259A1 (en) | 2010-06-01 | 2011-05-27 | Substituted imidazopyrazines |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103038235A CN103038235A (zh) | 2013-04-10 |
| CN103038235B true CN103038235B (zh) | 2015-07-29 |
Family
ID=44359555
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201180038047.1A Expired - Fee Related CN103038235B (zh) | 2010-06-01 | 2011-05-27 | 取代的咪唑并吡嗪 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9199999B2 (enExample) |
| EP (1) | EP2576560B1 (enExample) |
| JP (1) | JP5824040B2 (enExample) |
| CN (1) | CN103038235B (enExample) |
| CA (1) | CA2801031A1 (enExample) |
| ES (1) | ES2555261T3 (enExample) |
| WO (1) | WO2011151259A1 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI541243B (zh) | 2010-09-10 | 2016-07-11 | 拜耳知識產權公司 | 經取代咪唑并嗒 |
| CA2821817A1 (en) * | 2010-12-17 | 2012-06-21 | Bayer Intellectual Property Gmbh | Substituted 6-imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders |
| ES2530802T3 (es) * | 2010-12-17 | 2015-03-06 | Bayer Ip Gmbh | Imidazopirazinas 6-tiosustituidas para uso como inhibidores de MPS-1 y TKK en el tratamiento de trastornos hiperproliferativos |
| EP2651945A1 (en) * | 2010-12-17 | 2013-10-23 | Bayer Intellectual Property GmbH | 6-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders |
| JP2013545776A (ja) * | 2010-12-17 | 2013-12-26 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング | 過剰増殖性障害の治療におけるmps−1およびtkk阻害剤として使用するための6置換イミダゾピラジン |
| EP2825540B1 (en) | 2012-03-14 | 2016-09-14 | Bayer Intellectual Property GmbH | Substituted imidazopyridazines |
| WO2014020043A1 (en) | 2012-08-02 | 2014-02-06 | Bayer Pharma Aktiengesellschaft | Combinations for the treatment of cancer |
| WO2014020041A1 (en) | 2012-08-02 | 2014-02-06 | Bayer Pharma Aktiengesellschaft | Combinations for the treatment of cancer |
| AU2013344716B2 (en) | 2012-11-16 | 2018-03-01 | University Health Network | Pyrazolopyrimidine compounds |
| JP6095857B2 (ja) * | 2013-11-15 | 2017-03-15 | ユニバーシティ・ヘルス・ネットワーク | ピラゾロピリミジン化合物 |
| DK3283642T3 (da) | 2015-04-17 | 2024-01-02 | Crossfire Oncology Holding B V | Prognostiske biomarkører til ttk-hæmmerbaseret kemoterapi |
| WO2019245590A1 (en) | 2018-06-18 | 2019-12-26 | Avista Pharma Solutions, Inc. | Chemical compounds |
| US11459331B2 (en) | 2019-01-30 | 2022-10-04 | Avista Pharma Solutions, Inc. | Chemical compounds |
| CA3128346A1 (en) | 2019-01-30 | 2020-08-06 | Avista Pharma Solutions, Inc. | Synthetic process and novel intermediates |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008156614A2 (en) * | 2007-06-14 | 2008-12-24 | Schering Corporation | Imidazopyrazines as protein kinase inhibitors |
| CN101370811A (zh) * | 2005-11-10 | 2009-02-18 | 先灵公司 | 作为蛋白激酶抑制剂的咪唑并吡嗪化合物 |
| CN101589045A (zh) * | 2006-11-08 | 2009-11-25 | 先灵公司 | 作为蛋白质激酶抑制剂的咪唑并吡嗪 |
| JP2010111624A (ja) * | 2008-11-06 | 2010-05-20 | Shionogi & Co Ltd | Ttk阻害作用を有するインダゾール誘導体 |
| WO2011013729A1 (ja) * | 2009-07-30 | 2011-02-03 | オンコセラピー・サイエンス株式会社 | Ttk阻害作用を有する縮合イミダゾール誘導体 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5023252A (en) | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US5011472A (en) | 1988-09-06 | 1991-04-30 | Brown University Research Foundation | Implantable delivery system for biological factors |
| US7576085B2 (en) | 2002-09-23 | 2009-08-18 | Schering Corporation | Imidazopyrazines as cyclin dependent kinase inhibitors |
| TW200413378A (en) | 2002-09-23 | 2004-08-01 | Schering Corp | Novel imidazopyrazines as cyclin dependent kinase inhibitors |
| US7157460B2 (en) | 2003-02-20 | 2007-01-02 | Sugen Inc. | Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors |
| US7186832B2 (en) | 2003-02-20 | 2007-03-06 | Sugen Inc. | Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors |
| EP1945216A1 (en) | 2005-11-10 | 2008-07-23 | Schering Corporation | Methods for inhibiting protein kinases |
| US7893058B2 (en) | 2006-05-15 | 2011-02-22 | Janssen Pharmaceutica Nv | Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases |
| WO2007145921A1 (en) | 2006-06-06 | 2007-12-21 | Schering Corporation | Imidazopyrazines as protein kinase inhibitors |
| US20090175852A1 (en) | 2006-06-06 | 2009-07-09 | Schering Corporation | Imidazopyrazines as protein kinase inhibitors |
| US20100144743A1 (en) | 2006-09-05 | 2010-06-10 | Board Of Regents, The University Of Texas System | Compositions and methods for inhibition of tyrosine kinases |
| CA2662677C (en) | 2006-09-05 | 2016-05-31 | Emory University | Kinase inhibitors for preventing or treating pathogen infection and method of use thereof |
| CA2672960A1 (en) | 2006-12-20 | 2008-07-10 | Schering Corporation | Novel jnk inhibitors |
| AU2008282885A1 (en) | 2007-07-31 | 2009-02-05 | Schering Corporation | Anti-mitotic agent and aurora kinase inhibitor combination as anti-cancer treatment |
| GB0716292D0 (en) | 2007-08-21 | 2007-09-26 | Biofocus Dpi Ltd | Imidazopyrazine compounds |
| WO2009097233A1 (en) | 2008-01-28 | 2009-08-06 | Schering Corporation | Imidazopyrazines as protein kinase inhibitors |
| GB0822981D0 (en) * | 2008-12-17 | 2009-01-21 | Summit Corp Plc | Compounds for treatment of duchenne muscular dystrophy |
| WO2010124826A1 (en) | 2009-04-29 | 2010-11-04 | Bayer Schering Pharma Aktiengesellschaft | Substituted imidazoquinoxalines |
| CA2772790C (en) | 2009-09-04 | 2017-06-27 | Benjamin Bader | Substituted aminoquinoxalines as tyrosine threonine kinase inhibitors |
| US8575177B2 (en) * | 2009-12-04 | 2013-11-05 | Senhwa Biosciences, Inc. | Pyrazolopyrimidines and related heterocycles as CK2 inhibitors |
-
2011
- 2011-05-27 ES ES11725886.3T patent/ES2555261T3/es active Active
- 2011-05-27 US US13/700,956 patent/US9199999B2/en not_active Expired - Fee Related
- 2011-05-27 CA CA2801031A patent/CA2801031A1/en not_active Abandoned
- 2011-05-27 JP JP2013512850A patent/JP5824040B2/ja not_active Expired - Fee Related
- 2011-05-27 CN CN201180038047.1A patent/CN103038235B/zh not_active Expired - Fee Related
- 2011-05-27 WO PCT/EP2011/058713 patent/WO2011151259A1/en not_active Ceased
- 2011-05-27 EP EP11725886.3A patent/EP2576560B1/en active Active
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101370811A (zh) * | 2005-11-10 | 2009-02-18 | 先灵公司 | 作为蛋白激酶抑制剂的咪唑并吡嗪化合物 |
| CN101589045A (zh) * | 2006-11-08 | 2009-11-25 | 先灵公司 | 作为蛋白质激酶抑制剂的咪唑并吡嗪 |
| WO2008156614A2 (en) * | 2007-06-14 | 2008-12-24 | Schering Corporation | Imidazopyrazines as protein kinase inhibitors |
| JP2010111624A (ja) * | 2008-11-06 | 2010-05-20 | Shionogi & Co Ltd | Ttk阻害作用を有するインダゾール誘導体 |
| WO2011013729A1 (ja) * | 2009-07-30 | 2011-02-03 | オンコセラピー・サイエンス株式会社 | Ttk阻害作用を有する縮合イミダゾール誘導体 |
Non-Patent Citations (1)
| Title |
|---|
| Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as a2/a3 subtype selective GABAA agonists for the treatment of anxiety;Simon C. Goodacre,等;《Bioorganic & Medicinal Chemistry Letters》;20051227;第16卷(第6期);第1582–1585,参见全文 * |
Also Published As
| Publication number | Publication date |
|---|---|
| HK1179249A1 (en) | 2013-09-27 |
| ES2555261T3 (es) | 2015-12-30 |
| JP5824040B2 (ja) | 2015-11-25 |
| US9199999B2 (en) | 2015-12-01 |
| US20130210815A1 (en) | 2013-08-15 |
| EP2576560B1 (en) | 2015-09-30 |
| CN103038235A (zh) | 2013-04-10 |
| JP2013528610A (ja) | 2013-07-11 |
| EP2576560A1 (en) | 2013-04-10 |
| WO2011151259A1 (en) | 2011-12-08 |
| CA2801031A1 (en) | 2011-12-08 |
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| CN103038235B (zh) | 取代的咪唑并吡嗪 | |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| REG | Reference to a national code |
Ref country code: HK Ref legal event code: DE Ref document number: 1179249 Country of ref document: HK |
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| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20150729 Termination date: 20180527 |