CN102686580B - 用作酪蛋白激酶抑制剂的咪唑衍生物 - Google Patents
用作酪蛋白激酶抑制剂的咪唑衍生物 Download PDFInfo
- Publication number
- CN102686580B CN102686580B CN201080059759.7A CN201080059759A CN102686580B CN 102686580 B CN102686580 B CN 102686580B CN 201080059759 A CN201080059759 A CN 201080059759A CN 102686580 B CN102686580 B CN 102686580B
- Authority
- CN
- China
- Prior art keywords
- imidazol
- fluorophenyl
- amine
- pyrimidin
- piperidin
- 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)(C)OC(N(C1)CC1[n]1c(-c2nc(*)ccc2)c(-c(cc2)ccc2F)nc1)=O Chemical compound CC(C)(C)OC(N(C1)CC1[n]1c(-c2nc(*)ccc2)c(-c(cc2)ccc2F)nc1)=O 0.000 description 2
- KYIONJZKLFZCFB-WMDMUMDLSA-N CC(CN(C1)CC1[n]1c(-c2nc(N)ncc2)c(-c(cc2)ccc2F)nc1)/N=C\CCN Chemical compound CC(CN(C1)CC1[n]1c(-c2nc(N)ncc2)c(-c(cc2)ccc2F)nc1)/N=C\CCN KYIONJZKLFZCFB-WMDMUMDLSA-N 0.000 description 1
- DEBZZOLMKVPGDM-UHFFFAOYSA-N Fc(cc1)ccc1-c1c(-c2ncncc2)[n](C2CCNCC2)cn1 Chemical compound Fc(cc1)ccc1-c1c(-c2ncncc2)[n](C2CCNCC2)cn1 DEBZZOLMKVPGDM-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- C07D403/14—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 three or more hetero rings
-
- 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
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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
- C07D401/14—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
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Anesthesiology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25550609P | 2009-10-28 | 2009-10-28 | |
| US61/255,506 | 2009-10-28 | ||
| PCT/IB2010/054749 WO2011051858A1 (en) | 2009-10-28 | 2010-10-20 | Imidazole derivatives as casein kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102686580A CN102686580A (zh) | 2012-09-19 |
| CN102686580B true CN102686580B (zh) | 2014-09-10 |
Family
ID=43301770
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080059759.7A Expired - Fee Related CN102686580B (zh) | 2009-10-28 | 2010-10-20 | 用作酪蛋白激酶抑制剂的咪唑衍生物 |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US8518944B2 (2) |
| EP (1) | EP2493876B1 (2) |
| JP (1) | JP5784620B2 (2) |
| KR (1) | KR101421852B1 (2) |
| CN (1) | CN102686580B (2) |
| AR (1) | AR078797A1 (2) |
| AU (1) | AU2010311035B2 (2) |
| CA (1) | CA2777632C (2) |
| DK (1) | DK2493876T3 (2) |
| ES (1) | ES2460065T3 (2) |
| HR (1) | HRP20140252T1 (2) |
| IL (1) | IL219190A0 (2) |
| IN (1) | IN2012DN03182A (2) |
| MX (1) | MX2012004997A (2) |
| PL (1) | PL2493876T3 (2) |
| PT (1) | PT2493876E (2) |
| RS (1) | RS53246B (2) |
| SI (1) | SI2493876T1 (2) |
| TW (1) | TW201125864A (2) |
| UY (1) | UY32977A (2) |
| WO (1) | WO2011051858A1 (2) |
| ZA (1) | ZA201202776B (2) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2094836B1 (en) | 2006-11-15 | 2016-06-08 | Massachusetts Eye & Ear Infirmary | Generation of inner ear cells |
| LT3181133T (lt) * | 2010-12-20 | 2019-09-25 | Pfizer Inc. | Nauji kondensuoti piridino junginiai, kaip kazeino kinazės inhibitoriai |
| CA2883896C (en) | 2012-09-07 | 2023-03-07 | Massachusetts Eye & Ear Infirmary | Treating hearing loss |
| JP6267231B2 (ja) | 2012-12-21 | 2018-01-24 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | カゼインキナーゼ１δ／ε阻害剤としての新規な置換イミダゾール |
| EP3006438A4 (en) | 2013-05-30 | 2017-01-18 | Sumitomo Dainippon Pharma Co., Ltd. | Cyclic aminomethyl pyrimidine derivative |
| WO2015119579A1 (en) | 2014-02-07 | 2015-08-13 | Agency For Science, Technology And Research | 2,4,5-tri-substituted azole-based casein kinase 1 inhibitors as inducers for cardiomyogenesis |
| WO2016022776A2 (en) | 2014-08-06 | 2016-02-11 | Massachusetts Eye And Ear Infirmary | Increasing atoh1 life to drive sensorineural hair cell differentiantion |
| CN107847480B (zh) | 2015-03-23 | 2021-06-25 | 墨尔本大学 | 呼吸性疾病的治疗 |
| WO2017096233A1 (en) | 2015-12-04 | 2017-06-08 | Massachusetts Eye And Ear Infirmary | Treatment of hearing loss by inhibition of casein kinase 1 |
| CN109219439B (zh) | 2016-01-29 | 2022-09-20 | 马萨诸塞眼科耳科诊所 | 内耳支持细胞的扩增和分化及其使用方法 |
| PT3619204T (pt) * | 2017-05-03 | 2025-10-29 | Tianli Biotech Pty Ltd | Compostos para o tratamento de doenças respiratórias |
| US10973820B2 (en) | 2017-12-13 | 2021-04-13 | Facio Intellectual Property B.V. | Compounds for treatment of diseases related to DUX4 expression |
| MX2021002652A (es) * | 2018-09-09 | 2021-09-23 | Qanatpharma Ag | Uso de inhibidores de caseina-cinasa 1 para el tratamiento de enfermedades vasculares. |
| JP7575099B2 (ja) * | 2018-11-07 | 2024-10-29 | ティアンリ バイオテック プロプライエタリ リミテッド | 呼吸器疾患の処理のための新規な化合物 |
| TW202112368A (zh) | 2019-06-13 | 2021-04-01 | 荷蘭商法西歐知識產權股份有限公司 | 用於治療有關dux4表現之疾病的抑制劑組合 |
| CN115335057A (zh) * | 2020-03-27 | 2022-11-11 | 北京原基华毅生物科技有限公司 | 抑制酪蛋白激酶的方法 |
| EP4126878A4 (en) * | 2020-03-27 | 2024-07-10 | Gritscience Biopharmaceuticals Co., Ltd. | COMPOUNDS AS CASEIN KINASE INHIBITORS |
| AR122711A1 (es) * | 2020-06-25 | 2022-09-28 | Alchemedicine Inc | COMPUESTO HETEROCÍCLICO COMO INHIBIDOR DE CASEÍNA QUINASA 1d Y/O QUINASA 5 TIPO RECEPTOR DE ACTIVINA |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6096739A (en) * | 1996-03-25 | 2000-08-01 | Smithkline Beecham Corporation | Treatment for CNS injuries |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1992012154A1 (en) * | 1990-12-31 | 1992-07-23 | Fujisawa Pharmaceutical Co., Ltd. | Imidazotriazine derivatives |
| IL110296A (en) * | 1993-07-16 | 1999-12-31 | Smithkline Beecham Corp | Imidazole compounds process for their preparation and pharmaceutical compositions containing them |
| US6239279B1 (en) | 1998-12-16 | 2001-05-29 | Smithkline Beecham Corporation | Synthesis for 4-aryl-5-pyrimidine imidazole substituted derivatives |
| GB0108770D0 (en) * | 2001-04-06 | 2001-05-30 | Eisai London Res Lab Ltd | Inhibitors |
| IL159416A0 (en) * | 2001-06-18 | 2004-06-01 | Univ Rockefeller | Regulation of neuronal function through metabotropic glutamate receptor signaling pathways |
| DE602004020685D1 (de) * | 2003-12-11 | 2009-05-28 | Aventis Pharma Inc | Substituierte 1h-pyrroloä3,2-b, 3,2-c und 2,3-cüpyridin-2-carbonsäureamide und verwandte analoga als inhibitoren von caseinkinase-i-epsilon |
| JO2629B1 (en) * | 2004-08-19 | 2012-06-24 | افينتيس فارما سوتيكالز انك | Branched carboxylic acid amides containing thienobirol, carboxylic acid amides containing pyrolithiazole, and the like as kinase inhibitors casein epsilon |
| BRPI0514397A (pt) * | 2004-08-19 | 2008-06-10 | Aventis Pharma Inc | derivados de 3-ariltioindol-2-carboxamida e análogos destes como inibidores de caseìna cinase iépsilon |
| CA2626789A1 (en) * | 2005-10-21 | 2007-04-26 | Exelixis, Inc. | Pyrimidinones as casein kinase ii (ck2) modulators |
| EP2308866A1 (de) * | 2009-10-09 | 2011-04-13 | Bayer CropScience AG | Phenylpyri(mi)dinylpyrazole und ihre Verwendung als Fungizide |
| LT3181133T (lt) * | 2010-12-20 | 2019-09-25 | Pfizer Inc. | Nauji kondensuoti piridino junginiai, kaip kazeino kinazės inhibitoriai |
-
2010
- 2010-10-20 SI SI201030539T patent/SI2493876T1/sl unknown
- 2010-10-20 CA CA2777632A patent/CA2777632C/en not_active Expired - Fee Related
- 2010-10-20 KR KR1020127013537A patent/KR101421852B1/ko not_active Expired - Fee Related
- 2010-10-20 CN CN201080059759.7A patent/CN102686580B/zh not_active Expired - Fee Related
- 2010-10-20 ES ES10774282.7T patent/ES2460065T3/es active Active
- 2010-10-20 AU AU2010311035A patent/AU2010311035B2/en not_active Ceased
- 2010-10-20 JP JP2012535977A patent/JP5784620B2/ja active Active
- 2010-10-20 RS RS20140157A patent/RS53246B/sr unknown
- 2010-10-20 MX MX2012004997A patent/MX2012004997A/es active IP Right Grant
- 2010-10-20 PL PL10774282T patent/PL2493876T3/pl unknown
- 2010-10-20 WO PCT/IB2010/054749 patent/WO2011051858A1/en not_active Ceased
- 2010-10-20 EP EP10774282.7A patent/EP2493876B1/en active Active
- 2010-10-20 IN IN3182DEN2012 patent/IN2012DN03182A/en unknown
- 2010-10-20 HR HRP20140252AT patent/HRP20140252T1/hr unknown
- 2010-10-20 DK DK10774282.7T patent/DK2493876T3/en active
- 2010-10-20 PT PT107742827T patent/PT2493876E/pt unknown
- 2010-10-25 TW TW099136328A patent/TW201125864A/zh unknown
- 2010-10-25 US US12/911,030 patent/US8518944B2/en active Active
- 2010-10-27 UY UY0001032977A patent/UY32977A/es not_active Application Discontinuation
- 2010-10-28 AR ARP100103948A patent/AR078797A1/es not_active Application Discontinuation
-
2012
- 2012-04-15 IL IL219190A patent/IL219190A0/en unknown
- 2012-04-16 ZA ZA2012/02776A patent/ZA201202776B/en unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6096739A (en) * | 1996-03-25 | 2000-08-01 | Smithkline Beecham Corporation | Treatment for CNS injuries |
Non-Patent Citations (1)
| Title |
|---|
| Pyrimidinylimidazole Inhibitors of p38: Cyclic N-1 Imidazole Substituents Enhance p38 Kinase Inhibition and Oral Activity;Jerry L. Adams et al.;《Bioorganic & Medicinal Chemistry Letters》;20011231;第11卷;2867–2870 * |
Also Published As
| Publication number | Publication date |
|---|---|
| AR078797A1 (es) | 2011-12-07 |
| US8518944B2 (en) | 2013-08-27 |
| AU2010311035B2 (en) | 2013-05-16 |
| JP5784620B2 (ja) | 2015-09-24 |
| US20110098272A1 (en) | 2011-04-28 |
| PT2493876E (pt) | 2014-03-20 |
| PL2493876T3 (pl) | 2014-06-30 |
| HRP20140252T1 (hr) | 2014-04-25 |
| KR20120088759A (ko) | 2012-08-08 |
| EP2493876B1 (en) | 2014-02-12 |
| CA2777632C (en) | 2014-02-25 |
| WO2011051858A1 (en) | 2011-05-05 |
| KR101421852B1 (ko) | 2014-07-22 |
| EP2493876A1 (en) | 2012-09-05 |
| UY32977A (es) | 2011-05-31 |
| TW201125864A (en) | 2011-08-01 |
| MX2012004997A (es) | 2012-06-12 |
| ES2460065T3 (es) | 2014-05-13 |
| ZA201202776B (en) | 2013-06-26 |
| RS53246B (sr) | 2014-08-29 |
| DK2493876T3 (en) | 2014-03-10 |
| CA2777632A1 (en) | 2011-05-05 |
| IN2012DN03182A (2) | 2015-09-25 |
| JP2013509392A (ja) | 2013-03-14 |
| IL219190A0 (en) | 2012-06-28 |
| HK1171220A1 (en) | 2013-03-22 |
| AU2010311035A1 (en) | 2012-05-03 |
| CN102686580A (zh) | 2012-09-19 |
| SI2493876T1 (sl) | 2014-04-30 |
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