JP2005517666A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2005517666A5 JP2005517666A5 JP2003554646A JP2003554646A JP2005517666A5 JP 2005517666 A5 JP2005517666 A5 JP 2005517666A5 JP 2003554646 A JP2003554646 A JP 2003554646A JP 2003554646 A JP2003554646 A JP 2003554646A JP 2005517666 A5 JP2005517666 A5 JP 2005517666A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- general formula
- amino
- methyl
- alkyl
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 20
- -1 C 1 -C 6 - alkoxy Chemical group 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 239000001257 hydrogen Substances 0.000 claims 11
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 11
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 238000000034 method Methods 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 4
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 3
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 230000008569 process Effects 0.000 claims 3
- 125000002861 (C1-C4) alkanoyl group Chemical group 0.000 claims 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 230000008578 acute process Effects 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000001246 bromo group Chemical group Br* 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 230000006020 chronic inflammation Effects 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000004458 methylaminocarbonyl group Chemical group [H]N(C(*)=O)C([H])([H])[H] 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- YNGDWRXWKFWCJY-UHFFFAOYSA-N 1,4-Dihydropyridine Chemical group C1C=CNC=C1 YNGDWRXWKFWCJY-UHFFFAOYSA-N 0.000 claims 1
- 108010028275 Leukocyte Elastase Proteins 0.000 claims 1
- 102000016799 Leukocyte elastase Human genes 0.000 claims 1
- 241001465754 Metazoa Species 0.000 claims 1
- 125000004442 acylamino group Chemical group 0.000 claims 1
- 125000001664 diethylamino group Chemical group [H]C([H])([H])C([H])([H])N(*)C([H])([H])C([H])([H])[H] 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 230000002194 synthesizing effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0130553A GB2383326A (en) | 2001-12-20 | 2001-12-20 | Antiinflammatory dihydropyridines |
| GB0216664A GB2390849A (en) | 2002-07-17 | 2002-07-17 | 3-Acyl-1,4-dihydro-1,4-di(phenyl/azinyl/diazinyl)pyridine derivatives for use as human neutrophil elastase inhibitors |
| PCT/EP2002/013931 WO2003053930A1 (en) | 2001-12-20 | 2002-12-09 | 1,4-dihydro-1,4-diphenylpyridine derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005517666A JP2005517666A (ja) | 2005-06-16 |
| JP2005517666A5 true JP2005517666A5 (enExample) | 2006-02-02 |
| JP4486817B2 JP4486817B2 (ja) | 2010-06-23 |
Family
ID=26246892
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003554646A Expired - Fee Related JP4486817B2 (ja) | 2001-12-20 | 2002-12-09 | 1,4−ジヒドロ−1,4−ジフェニルピリジン誘導体 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US7199136B2 (enExample) |
| EP (1) | EP1458682B1 (enExample) |
| JP (1) | JP4486817B2 (enExample) |
| AU (1) | AU2002361992A1 (enExample) |
| CA (1) | CA2470813A1 (enExample) |
| DE (1) | DE60214428T2 (enExample) |
| ES (1) | ES2271365T3 (enExample) |
| WO (1) | WO2003053930A1 (enExample) |
Families Citing this family (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0219896D0 (en) | 2002-08-27 | 2002-10-02 | Bayer Ag | Dihydropyridine derivatives |
| AU2003255492A1 (en) * | 2002-09-10 | 2004-04-30 | Bayer Healthcare Ag | Heterocyclic derivatives |
| SE0302487D0 (sv) * | 2003-09-18 | 2003-09-18 | Astrazeneca Ab | Novel compounds |
| CA2556463C (en) * | 2004-02-19 | 2012-08-14 | Bayer Healthcare Ag | Dihydropyridinone derivatives |
| JP4825194B2 (ja) * | 2004-02-26 | 2011-11-30 | バイエル・シェーリング・ファルマ・アクチェンゲゼルシャフト | 1,4−ジアリール−ジヒドロピリミジン−2−オン化合物およびヒト好中球エラスターゼ阻害剤としてのそれらの使用 |
| EP1730121B1 (en) | 2004-02-26 | 2013-08-07 | Bayer Intellectual Property GmbH | 1,4-diaryl-dihydropyrimidin-2-ones and their use as human neutrophil elastase inhibitors |
| GB0516313D0 (en) | 2005-08-08 | 2005-09-14 | Argenta Discovery Ltd | Azole derivatives and their uses |
| US7994211B2 (en) | 2005-08-08 | 2011-08-09 | Argenta Discovery Limited | Bicyclo[2.2.1]hept-7-ylamine derivatives and their uses |
| DE102007019690A1 (de) | 2007-04-26 | 2008-10-30 | Bayer Healthcare Ag | Verwendung von cyclisch substituierten Furopyrimidin-Derivaten zur Behandlung der pulmonalen arteriellen Hypertonie |
| DE102007019691A1 (de) | 2007-04-26 | 2008-10-30 | Bayer Healthcare Ag | Verwendung von acyclisch substituierten Furopyrimidin-Derivaten zur Behandlung der pulmonalen arteriellen Hypertonie |
| DE102007027800A1 (de) | 2007-06-16 | 2008-12-18 | Bayer Healthcare Ag | Substituierte bicyclische Heteroaryl-Verbindungen und ihre Verwendung |
| DE102007027799A1 (de) | 2007-06-16 | 2008-12-18 | Bayer Healthcare Ag | Substituierte Furopyrimidine und ihre Verwendung |
| DE102007051762A1 (de) | 2007-10-30 | 2009-05-07 | Bayer Healthcare Ag | Substituierte Pyrrolotriazine und ihre Verwendung |
| DE102007054786A1 (de) | 2007-11-16 | 2009-05-20 | Bayer Healthcare Ag | Trisubstituierte Furopyrimidine und ihre Verwendung |
| PT2229358E (pt) | 2007-12-14 | 2011-06-29 | Pulmagen Therapeutics Asthma Ltd | Indoles e sua utilização terapêutica |
| DE102008007400A1 (de) | 2008-02-04 | 2009-08-06 | Bayer Healthcare Ag | Substituierte Furane und ihre Verwendung |
| DE102009004197A1 (de) * | 2009-01-09 | 2010-07-15 | Bayer Schering Pharma Aktiengesellschaft | Heterocyclisch anellierte Diaryldihydropyrimidin-Derivate und ihre Verwendung |
| AU2010215261A1 (en) | 2009-02-17 | 2011-09-08 | Chiesi Farmaceutici S.P.A. | Triazolopyridine derivatives as p38 MAP kinase inhibitors |
| GB0902648D0 (en) | 2009-02-17 | 2009-04-01 | Argenta Discovery Ltd | Pharmaceutical compounds and compositions |
| GB0918922D0 (en) | 2009-10-28 | 2009-12-16 | Vantia Ltd | Aminopyridine derivatives |
| GB0918924D0 (en) | 2009-10-28 | 2009-12-16 | Vantia Ltd | Azaindole derivatives |
| GB0918923D0 (en) | 2009-10-28 | 2009-12-16 | Vantia Ltd | Aminothiazole derivatives |
| GB201009731D0 (en) | 2010-06-10 | 2010-07-21 | Pulmagen Therapeutics Inflamma | Kinase inhibitors |
| CN103974953B (zh) | 2011-12-09 | 2016-06-29 | 奇斯药制品公司 | 激酶抑制剂 |
| CN103987708B (zh) | 2011-12-09 | 2016-06-22 | 奇斯药制品公司 | 4-羟基-1,2,3,4-四氢萘-1-基脲的衍生物及其在呼吸道疾病治疗中的用途 |
| CN105968110B (zh) | 2011-12-09 | 2018-04-27 | 奇斯药制品公司 | 激酶抑制剂 |
| US20140221335A1 (en) | 2013-02-06 | 2014-08-07 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| US9115093B2 (en) | 2013-03-04 | 2015-08-25 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| WO2014195402A1 (en) | 2013-06-06 | 2014-12-11 | Chiesi Farmaceutici S.P.A. | Kinase inhibitors |
| US9440930B2 (en) | 2014-07-31 | 2016-09-13 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| US9657015B2 (en) | 2014-07-31 | 2017-05-23 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| US9290457B2 (en) * | 2014-07-31 | 2016-03-22 | Boehringer Ingelheim International Gmbh | Substituted dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| US9475779B2 (en) | 2014-07-31 | 2016-10-25 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| US9458113B2 (en) | 2014-07-31 | 2016-10-04 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| US9958484B2 (en) * | 2015-07-08 | 2018-05-01 | Qualcomm Incorporated | Apparatus and method for measuring load current by applying compensated gain to voltage derived from drain-to-source voltage of power gating device |
| TW201720828A (zh) | 2015-11-23 | 2017-06-16 | 赫孚孟拉羅股份公司 | 治療性化合物及組合物以及其使用方法 |
| EP3394058B1 (en) | 2015-12-23 | 2020-10-14 | Chiesi Farmaceutici S.p.A. | N-[3-(3-{4-[[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl} -ureido)-phenyl]-methanesulfonamide derivatives and their use as p38 mapk inhibitors |
| EP3394060A1 (en) | 2015-12-23 | 2018-10-31 | Chiesi Farmaceutici S.p.A. | 1-(3-tert-butyl-2h-pyrazol-5-yl or 5-tert-butyl-isoxaol-3-yl)-3-(4-([1,2,4]triazolo[4,3-a]pyridin-6-yloxy)-1,2,3,4-tetrahydro-naphthalenyl) urea derivatives and their use as p38 mapk inhibitors |
| EP3394059B1 (en) | 2015-12-23 | 2020-11-25 | Chiesi Farmaceutici S.p.A. | 1-(3-tert-butyl-phenyl)-3-(4-([1,2,4]triazolo[4,3-a]pyridin-6-yloxy)-1,2,3,4-tetrahydro- naphthalen-1-yl)-urea derivatives and their use as p38 mapk inhibitors |
| WO2017191098A1 (en) | 2016-05-05 | 2017-11-09 | F. Hoffmann-La Roche Ag | Pyrazole derivatives, compositions and therapeutic use thereof |
| CN109890817B (zh) | 2016-09-06 | 2022-06-17 | 豪夫迈·罗氏有限公司 | 8-(氮杂环丁烷-1-基)-[1,2,4]三唑并[1,5-a]吡啶基化合物、其组合物和应用方法 |
| CN110114343B (zh) | 2016-12-29 | 2022-09-06 | 豪夫迈·罗氏有限公司 | 吡唑并嘧啶化合物及其使用方法 |
| WO2018166993A2 (en) | 2017-03-14 | 2018-09-20 | F. Hoffmann-La Roche Ag | Pyrazolochlorophenyl compounds, compositions and methods of use thereof |
| CN110678467B (zh) | 2017-05-22 | 2023-06-13 | 豪夫迈·罗氏有限公司 | 治疗化合物和组合物及其使用方法 |
| BR112019024322A2 (pt) | 2017-05-22 | 2020-06-16 | F. Hoffmann-La Roche Ag | Compostos e composições terapêuticos e métodos de uso dos mesmos |
| US10364245B2 (en) | 2017-06-07 | 2019-07-30 | Chiesi Farmaceutici S.P.A. | Kinase inhibitors |
| CN111587250A (zh) | 2018-01-15 | 2020-08-25 | 豪夫迈·罗氏有限公司 | 作为jak抑制剂的吡唑并嘧啶化合物 |
| JP2020015705A (ja) * | 2018-07-27 | 2020-01-30 | 住友化学株式会社 | アニリン化合物の製造方法 |
| MA56518A (fr) | 2019-06-18 | 2022-04-27 | Hoffmann La Roche | Inhibiteurs de sulfone pyrazolopyrimidine de jak kinases et leurs utilisations |
| TW202115069A (zh) | 2019-06-18 | 2021-04-16 | 瑞士商赫孚孟拉羅股份公司 | Jak激酶之經四唑取代之吡唑并嘧啶抑制劑及其用途 |
| JP7716993B2 (ja) | 2019-06-18 | 2025-08-01 | エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト | Jakキナーゼのピラゾロピリミジンアリールエーテル阻害剤及びその使用 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2753946A1 (de) * | 1977-12-03 | 1979-06-13 | Bayer Ag | 1-n-aryl-1,4-dihydropyridine und ihre verwendung als arzneimittel |
| DE3222367A1 (de) | 1982-06-15 | 1983-12-15 | Bayer Ag, 5090 Leverkusen | Verwendung von 1,4-dihydropyridinen in antiarteriosklerotika und deren herstellung |
| DE4011695A1 (de) * | 1990-04-11 | 1991-10-17 | Bayer Ag | Verwendung von n-alkylierten 1,4-dihydropyridindicarbonsaeureestern als arzneimittel, neue verbindungen und verfahren zu ihrer herstellung |
| DE4328884A1 (de) | 1993-08-27 | 1995-03-02 | Bayer Ag | Verwendung von N-alkylierten 1,4-Dihydropyridincarbonsäureestern als Arzneimittel |
| JP3337829B2 (ja) * | 1994-07-29 | 2002-10-28 | 日研化学株式会社 | 1,4−ジヒドロピリジン化合物 |
-
2002
- 2002-12-09 AU AU2002361992A patent/AU2002361992A1/en not_active Abandoned
- 2002-12-09 WO PCT/EP2002/013931 patent/WO2003053930A1/en not_active Ceased
- 2002-12-09 DE DE60214428T patent/DE60214428T2/de not_active Expired - Lifetime
- 2002-12-09 ES ES02796589T patent/ES2271365T3/es not_active Expired - Lifetime
- 2002-12-09 EP EP02796589A patent/EP1458682B1/en not_active Expired - Lifetime
- 2002-12-09 US US10/498,967 patent/US7199136B2/en not_active Expired - Fee Related
- 2002-12-09 CA CA002470813A patent/CA2470813A1/en not_active Abandoned
- 2002-12-09 JP JP2003554646A patent/JP4486817B2/ja not_active Expired - Fee Related