JP2007513094A5 - - Google Patents
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- Publication number
- JP2007513094A5 JP2007513094A5 JP2006541751A JP2006541751A JP2007513094A5 JP 2007513094 A5 JP2007513094 A5 JP 2007513094A5 JP 2006541751 A JP2006541751 A JP 2006541751A JP 2006541751 A JP2006541751 A JP 2006541751A JP 2007513094 A5 JP2007513094 A5 JP 2007513094A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- hetaryl
- benzimidazol
- pyrazin
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 63
- 229910052799 carbon Inorganic materials 0.000 claims 21
- 125000003118 aryl group Chemical group 0.000 claims 14
- 201000010099 disease Diseases 0.000 claims 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 13
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 10
- 239000000203 mixture Substances 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 125000002877 alkyl aryl group Chemical group 0.000 claims 4
- 125000004429 atom Chemical group 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- -1 hydrate Substances 0.000 claims 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 4
- 239000000651 prodrug Substances 0.000 claims 4
- 229940002612 prodrug Drugs 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 206010061218 Inflammation Diseases 0.000 claims 3
- 150000001721 carbon Chemical class 0.000 claims 3
- 208000015181 infectious disease Diseases 0.000 claims 3
- 230000004054 inflammatory process Effects 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 206010003645 Atopy Diseases 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 101001004391 Drosophila melanogaster Protein jim lovell Proteins 0.000 claims 2
- 101000844245 Homo sapiens Non-receptor tyrosine-protein kinase TYK2 Proteins 0.000 claims 2
- 101000997835 Homo sapiens Tyrosine-protein kinase JAK1 Proteins 0.000 claims 2
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 claims 2
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 claims 2
- 206010020751 Hypersensitivity Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 102100032028 Non-receptor tyrosine-protein kinase TYK2 Human genes 0.000 claims 2
- 208000025747 Rheumatic disease Diseases 0.000 claims 2
- 102100033438 Tyrosine-protein kinase JAK1 Human genes 0.000 claims 2
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims 2
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 claims 2
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims 2
- 208000026935 allergic disease Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 230000009610 hypersensitivity Effects 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 230000003612 virological effect Effects 0.000 claims 2
- LYAYTYZBNIDHGD-UHFFFAOYSA-N 1-[6-(3,4-dihydro-1h-isoquinolin-2-yl)pyrazin-2-yl]benzimidazole-5-carbonitrile Chemical compound C1CC2=CC=CC=C2CN1C1=NC(N2C3=CC=C(C=C3N=C2)C#N)=CN=C1 LYAYTYZBNIDHGD-UHFFFAOYSA-N 0.000 claims 1
- GRCXICUDDSRJES-UHFFFAOYSA-N 1-[6-[1-(3-fluorophenyl)ethylamino]pyrazin-2-yl]benzimidazole-5-carboxamide Chemical compound C=1N=CC(N2C3=CC=C(C=C3N=C2)C(N)=O)=NC=1NC(C)C1=CC=CC(F)=C1 GRCXICUDDSRJES-UHFFFAOYSA-N 0.000 claims 1
- HMEBYGNNEPEWQH-ZDUSSCGKSA-N 1-[6-[[(1s)-1-phenylethyl]amino]pyrazin-2-yl]benzimidazol-5-amine Chemical compound C1([C@@H](NC=2N=C(C=NC=2)N2C3=CC=C(N)C=C3N=C2)C)=CC=CC=C1 HMEBYGNNEPEWQH-ZDUSSCGKSA-N 0.000 claims 1
- YKVFWHHWJJTRQP-INIZCTEOSA-N 2,2-dimethyl-n-[3-[6-[[(1s)-1-phenylethyl]amino]pyrazin-2-yl]benzimidazol-5-yl]propanamide Chemical compound C1([C@@H](NC=2N=C(C=NC=2)N2C3=CC(NC(=O)C(C)(C)C)=CC=C3N=C2)C)=CC=CC=C1 YKVFWHHWJJTRQP-INIZCTEOSA-N 0.000 claims 1
- VBWJEZDFZIHWIK-UHFFFAOYSA-N 3-[6-(3,4-dihydro-1h-isoquinolin-2-yl)pyrazin-2-yl]benzimidazole-5-carbonitrile Chemical compound C1CC2=CC=CC=C2CN1C1=NC(N2C=NC3=CC=C(C=C32)C#N)=CN=C1 VBWJEZDFZIHWIK-UHFFFAOYSA-N 0.000 claims 1
- IESZHLQBGAQXSR-UHFFFAOYSA-N 3-[6-[1-(3-fluorophenyl)ethylamino]pyrazin-2-yl]benzimidazole-5-carbonitrile Chemical compound C=1N=CC(N2C3=CC(=CC=C3N=C2)C#N)=NC=1NC(C)C1=CC=CC(F)=C1 IESZHLQBGAQXSR-UHFFFAOYSA-N 0.000 claims 1
- JHKRBMBABQNEAP-UHFFFAOYSA-N 3-[6-[1-(3-fluorophenyl)ethylamino]pyrazin-2-yl]benzimidazole-5-carboxamide Chemical compound C=1N=CC(N2C3=CC(=CC=C3N=C2)C(N)=O)=NC=1NC(C)C1=CC=CC(F)=C1 JHKRBMBABQNEAP-UHFFFAOYSA-N 0.000 claims 1
- YIJNMNSHUNMBKK-SFHVURJKSA-N 3-[6-[[(1s)-1,2,3,4-tetrahydronaphthalen-1-yl]amino]pyrazin-2-yl]benzimidazole-5-carbonitrile Chemical compound C1CCC2=CC=CC=C2[C@H]1NC1=NC(N2C=NC3=CC=C(C=C32)C#N)=CN=C1 YIJNMNSHUNMBKK-SFHVURJKSA-N 0.000 claims 1
- LYXMUFYMDITEBX-ZDUSSCGKSA-N 3-[6-[[(1s)-1-phenylethyl]amino]pyrazin-2-yl]benzimidazol-5-amine Chemical compound C1([C@@H](NC=2N=C(C=NC=2)N2C3=CC(N)=CC=C3N=C2)C)=CC=CC=C1 LYXMUFYMDITEBX-ZDUSSCGKSA-N 0.000 claims 1
- CYOIRCQXBZKWDU-CQSZACIVSA-N 6-(benzimidazol-1-yl)-n-[(1r)-1-phenylethyl]pyrazin-2-amine Chemical compound C1([C@H](NC=2N=C(C=NC=2)N2C3=CC=CC=C3N=C2)C)=CC=CC=C1 CYOIRCQXBZKWDU-CQSZACIVSA-N 0.000 claims 1
- CYOIRCQXBZKWDU-AWEZNQCLSA-N 6-(benzimidazol-1-yl)-n-[(1s)-1-phenylethyl]pyrazin-2-amine Chemical compound C1([C@@H](NC=2N=C(C=NC=2)N2C3=CC=CC=C3N=C2)C)=CC=CC=C1 CYOIRCQXBZKWDU-AWEZNQCLSA-N 0.000 claims 1
- IIEVOFLNCFEHRU-UHFFFAOYSA-N 6-(benzimidazol-1-yl)-n-benzylpyrazin-2-amine Chemical compound C=1N=CC(N2C3=CC=CC=C3N=C2)=NC=1NCC1=CC=CC=C1 IIEVOFLNCFEHRU-UHFFFAOYSA-N 0.000 claims 1
- 102000042838 JAK family Human genes 0.000 claims 1
- 108091082332 JAK family Proteins 0.000 claims 1
- RWKKYDUIYRVASH-UHFFFAOYSA-N [1-[6-[1-(4-fluorophenyl)ethylamino]pyrazin-2-yl]benzimidazol-5-yl]methanol Chemical compound C=1N=CC(N2C3=CC=C(CO)C=C3N=C2)=NC=1NC(C)C1=CC=C(F)C=C1 RWKKYDUIYRVASH-UHFFFAOYSA-N 0.000 claims 1
- PFPLICQLPSWUOP-UHFFFAOYSA-N [3-[6-[1-(4-fluorophenyl)ethylamino]pyrazin-2-yl]benzimidazol-5-yl]methanol Chemical compound C=1N=CC(N2C3=CC(CO)=CC=C3N=C2)=NC=1NC(C)C1=CC=C(F)C=C1 PFPLICQLPSWUOP-UHFFFAOYSA-N 0.000 claims 1
- AVEOXLDCNLUDJO-UHFFFAOYSA-N n-[1-(4-fluorophenyl)ethyl]-6-[6-[(4-methylpiperazin-1-yl)methyl]benzimidazol-1-yl]pyrazin-2-amine Chemical compound C=1C=C(F)C=CC=1C(C)NC(N=1)=CN=CC=1N(C1=C2)C=NC1=CC=C2CN1CCN(C)CC1 AVEOXLDCNLUDJO-UHFFFAOYSA-N 0.000 claims 1
- BOSNHXOQHRBDCM-AWEZNQCLSA-N n-[1-[6-[[(1s)-1-phenylethyl]amino]pyrazin-2-yl]benzimidazol-5-yl]acetamide Chemical compound C1([C@@H](NC=2N=C(C=NC=2)N2C3=CC=C(NC(C)=O)C=C3N=C2)C)=CC=CC=C1 BOSNHXOQHRBDCM-AWEZNQCLSA-N 0.000 claims 1
- KPECUUQAZILQNR-AWEZNQCLSA-N n-[1-[6-[[(1s)-1-phenylethyl]amino]pyrazin-2-yl]benzimidazol-5-yl]methanesulfonamide Chemical compound C1([C@@H](NC=2N=C(C=NC=2)N2C3=CC=C(NS(C)(=O)=O)C=C3N=C2)C)=CC=CC=C1 KPECUUQAZILQNR-AWEZNQCLSA-N 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 0 CC[C@](CC*C1=C*/C=C/C([n]2c3ccccc3nc2)=*CC1)c1ccccc1 Chemical compound CC[C@](CC*C1=C*/C=C/C([n]2c3ccccc3nc2)=*CC1)c1ccccc1 0.000 description 3
- UOMJXONAQYKUCS-UHFFFAOYSA-N C(CC1=NC(c2ccncc2)=CC=C=C1)C1c2ccccc2N=C1 Chemical compound C(CC1=NC(c2ccncc2)=CC=C=C1)C1c2ccccc2N=C1 UOMJXONAQYKUCS-UHFFFAOYSA-N 0.000 description 1
- BLGLGPUUQBKOCN-UHFFFAOYSA-N COc(cc(cc1)-c2cncc(CC3C=Nc4ccccc4C3)n2)c1O Chemical compound COc(cc(cc1)-c2cncc(CC3C=Nc4ccccc4C3)n2)c1O BLGLGPUUQBKOCN-UHFFFAOYSA-N 0.000 description 1
- HSAZFZPMRIUKSD-UHFFFAOYSA-N CS(CCCc(cc1)ccc1-c1cncc(-[n]2c3ccccc3nc2)n1)(=O)=O Chemical compound CS(CCCc(cc1)ccc1-c1cncc(-[n]2c3ccccc3nc2)n1)(=O)=O HSAZFZPMRIUKSD-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2003906686A AU2003906686A0 (en) | 2003-12-03 | Azole-based kinase inhibitors | |
| AU2003906686 | 2003-12-03 | ||
| AU2004902060A AU2004902060A0 (en) | 2004-04-20 | Azole-based kinase inhibitors (2) | |
| AU2004902060 | 2004-04-20 | ||
| PCT/AU2004/001690 WO2005054230A1 (en) | 2003-12-03 | 2004-12-03 | Azole-based kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2007513094A JP2007513094A (ja) | 2007-05-24 |
| JP2007513094A5 true JP2007513094A5 (https=) | 2007-11-15 |
| JP4808628B2 JP4808628B2 (ja) | 2011-11-02 |
Family
ID=34654577
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006541751A Expired - Fee Related JP4808628B2 (ja) | 2003-12-03 | 2004-12-03 | アゾール系キナーゼ阻害剤 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US7737143B2 (https=) |
| EP (1) | EP1689739B1 (https=) |
| JP (1) | JP4808628B2 (https=) |
| KR (1) | KR101211514B1 (https=) |
| BR (1) | BRPI0417345A (https=) |
| CA (1) | CA2545425C (https=) |
| ES (1) | ES2578254T3 (https=) |
| GB (1) | GB2423083B (https=) |
| IL (1) | IL175568A (https=) |
| NZ (1) | NZ545694A (https=) |
| PT (1) | PT1689739T (https=) |
| WO (1) | WO2005054230A1 (https=) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2561831A1 (en) | 2004-04-13 | 2005-12-22 | Icagen, Inc. | Polycyclic pyrazines as potassium ion channel modulators |
| AU2007227210A1 (en) | 2006-03-20 | 2007-09-27 | Synta Pharmaceuticals Corp. | Benzoimidazolyl-parazine compounds for inflammation and immune-related uses |
| JP2010505794A (ja) * | 2006-10-03 | 2010-02-25 | ノイロサーチ アクティーゼルスカブ | カリウムチャネル調節剤として有用なインダゾリル誘導体 |
| DE602007011793D1 (de) * | 2006-10-18 | 2011-02-17 | Pfizer Prod Inc | Biaryl-ether-harnstoffverbindungen |
| US8131527B1 (en) | 2006-12-22 | 2012-03-06 | Astex Therapeutics Ltd. | FGFR pharmacophore compounds |
| US8513276B2 (en) | 2006-12-22 | 2013-08-20 | Astex Therapeutics Limited | Imidazo[1,2-a]pyridine compounds for use in treating cancer |
| HRP20150642T1 (hr) | 2006-12-22 | 2015-08-14 | Astex Therapeutics Limited | BICIKLIÄŚKE HETEROCIKLIÄŚKE TVARI KAO INHIBITORI FGFR-a |
| JP5140154B2 (ja) | 2007-06-27 | 2013-02-06 | アストラゼネカ・アクチエボラーグ | ピラジノン誘導体および肺疾患の処置におけるそれらの使用 |
| GB0720038D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New compounds |
| GB0720041D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New Compounds |
| US20090275529A1 (en) * | 2008-05-05 | 2009-11-05 | Reiss Allison B | Method for improving cardiovascular risk profile of cox inhibitors |
| GB0810902D0 (en) | 2008-06-13 | 2008-07-23 | Astex Therapeutics Ltd | New compounds |
| CN102131389A (zh) | 2008-06-20 | 2011-07-20 | 健泰科生物技术公司 | 三唑并吡啶jak抑制剂化合物和方法 |
| WO2009155565A1 (en) | 2008-06-20 | 2009-12-23 | Genentech, Inc. | Triazolopyridine jak inhibitor compounds and methods |
| AR073711A1 (es) | 2008-10-01 | 2010-11-24 | Astrazeneca Ab | Derivados de isoquinolina |
| GB0906472D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| GB0906470D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| MX2013010513A (es) * | 2011-03-16 | 2013-10-07 | Hoffmann La Roche | Compuestos de alcohol 6,5-heterociclil-propargilico y usos de los mismos. |
| ES2675720T3 (es) * | 2013-01-10 | 2018-07-12 | Pulmokine, Inc. | Inhibidores de quinasa no selectivos |
| US9925184B2 (en) | 2013-10-11 | 2018-03-27 | Pulmokine, Inc. | Spray-dry formulations |
| US11352328B2 (en) | 2016-07-12 | 2022-06-07 | Arisan Therapeutics Inc. | Heterocyclic compounds for the treatment of arenavirus |
| CA3041679A1 (en) | 2016-10-27 | 2018-05-03 | Lawrence S. ZISMAN | Combination therapy for treating pulmonary hypertension |
| US11024307B2 (en) | 2018-02-08 | 2021-06-01 | Computime Ltd. | Method and apparatus to provide comprehensive smart assistant services |
| US12419865B2 (en) | 2018-12-06 | 2025-09-23 | Arisan Therapeutics Inc. | Compounds for the treatment of arenavirus infection |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2701281B2 (ja) * | 1988-01-22 | 1998-01-21 | 吉富製薬株式会社 | ピラゾロピリジン化合物 |
| EP1169038B9 (en) | 1999-04-15 | 2013-07-10 | Bristol-Myers Squibb Company | Cyclic protein tyrosine kinase inhibitors |
| WO2001000213A1 (en) * | 1999-06-30 | 2001-01-04 | Merck & Co., Inc. | Src kinase inhibitor compounds |
| US20040102455A1 (en) * | 2001-01-30 | 2004-05-27 | Burns Christopher John | Method of inhibiting kinases |
| WO2003099811A1 (en) | 2002-05-23 | 2003-12-04 | Cytopia Pty Ltd | Kinase inhibitors |
| AUPS251402A0 (en) * | 2002-05-23 | 2002-06-13 | Cytopia Pty Ltd | Kinase inhibitors |
| DK1704145T3 (da) * | 2004-01-12 | 2012-09-24 | Ym Biosciences Australia Pty | Selektive kinaseinhibitorer |
-
2004
- 2004-12-03 NZ NZ545694A patent/NZ545694A/en not_active IP Right Cessation
- 2004-12-03 WO PCT/AU2004/001690 patent/WO2005054230A1/en not_active Ceased
- 2004-12-03 JP JP2006541751A patent/JP4808628B2/ja not_active Expired - Fee Related
- 2004-12-03 EP EP04801112.6A patent/EP1689739B1/en not_active Expired - Lifetime
- 2004-12-03 ES ES04801112.6T patent/ES2578254T3/es not_active Expired - Lifetime
- 2004-12-03 CA CA2545425A patent/CA2545425C/en not_active Expired - Fee Related
- 2004-12-03 GB GB0611894A patent/GB2423083B/en not_active Expired - Lifetime
- 2004-12-03 BR BRPI0417345-7A patent/BRPI0417345A/pt not_active IP Right Cessation
- 2004-12-03 PT PT48011126T patent/PT1689739T/pt unknown
- 2004-12-03 US US10/581,412 patent/US7737143B2/en active Active
-
2006
- 2006-05-11 IL IL175568A patent/IL175568A/en not_active IP Right Cessation
- 2006-06-02 KR KR1020067010931A patent/KR101211514B1/ko not_active Expired - Fee Related
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