JP2013515031A5 - - Google Patents
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- Publication number
- JP2013515031A5 JP2013515031A5 JP2012545268A JP2012545268A JP2013515031A5 JP 2013515031 A5 JP2013515031 A5 JP 2013515031A5 JP 2012545268 A JP2012545268 A JP 2012545268A JP 2012545268 A JP2012545268 A JP 2012545268A JP 2013515031 A5 JP2013515031 A5 JP 2013515031A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- halo
- alkyloxy
- pyrimidin
- amine
- 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 42
- 125000005843 halogen group Chemical group 0.000 claims 24
- 125000003545 alkoxy group Chemical group 0.000 claims 21
- 125000005214 aminoheteroaryl group Chemical group 0.000 claims 9
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 125000004414 alkyl thio group Chemical group 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- 125000004430 oxygen atom Chemical group O* 0.000 claims 6
- 229920006395 saturated elastomer Polymers 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- -1 1-{[3-chloro-5- (trifluoromethyl) -2-pyridinyl] sulfanyl} ethyl Chemical group 0.000 claims 3
- 125000006164 6-membered heteroaryl group Chemical group 0.000 claims 3
- 206010065390 Inflammatory pain Diseases 0.000 claims 3
- 208000002193 Pain Diseases 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 208000004296 neuralgia Diseases 0.000 claims 3
- 208000021722 neuropathic pain Diseases 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- IVWOENWZBVIUFI-MRVPVSSYSA-N 4-[(1r)-1-(3-methoxypyridin-2-yl)oxyethyl]pyrimidin-2-amine Chemical compound COC1=CC=CN=C1O[C@H](C)C1=CC=NC(N)=N1 IVWOENWZBVIUFI-MRVPVSSYSA-N 0.000 claims 2
- ICFLLTCXXSTBNA-SSDOTTSWSA-N 4-[(1r)-1-[3-(trifluoromethyl)pyridin-2-yl]oxyethyl]pyrimidin-2-amine Chemical compound O([C@H](C)C=1N=C(N)N=CC=1)C1=NC=CC=C1C(F)(F)F ICFLLTCXXSTBNA-SSDOTTSWSA-N 0.000 claims 2
- CWQVTZBWZFEUCZ-ZCFIWIBFSA-N 4-[(1r)-1-[4-(trifluoromethyl)pyrimidin-2-yl]oxyethyl]pyrimidin-2-amine Chemical compound O([C@H](C)C=1N=C(N)N=CC=1)C1=NC=CC(C(F)(F)F)=N1 CWQVTZBWZFEUCZ-ZCFIWIBFSA-N 0.000 claims 2
- BRDFFIWBTPFAGW-UHFFFAOYSA-N 4-[1-[3-(trifluoromethyl)pyridin-2-yl]sulfanylethyl]pyrimidin-2-amine Chemical compound C=1C=NC(N)=NC=1C(C)SC1=NC=CC=C1C(F)(F)F BRDFFIWBTPFAGW-UHFFFAOYSA-N 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 230000002981 neuropathic effect Effects 0.000 claims 2
- LJXQPZWIHJMPQQ-UHFFFAOYSA-N pyrimidin-2-amine Chemical compound NC1=NC=CC=N1 LJXQPZWIHJMPQQ-UHFFFAOYSA-N 0.000 claims 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- YYEYMXDRGTXIIZ-SSDOTTSWSA-N 4-[(1r)-1-(2,4-difluorophenoxy)ethyl]pyrimidin-2-amine Chemical compound O([C@H](C)C=1N=C(N)N=CC=1)C1=CC=C(F)C=C1F YYEYMXDRGTXIIZ-SSDOTTSWSA-N 0.000 claims 1
- OCGVPGIOKVTCBH-SSDOTTSWSA-N 4-[(1r)-1-(2,5-difluorophenoxy)ethyl]pyrimidin-2-amine Chemical compound O([C@H](C)C=1N=C(N)N=CC=1)C1=CC(F)=CC=C1F OCGVPGIOKVTCBH-SSDOTTSWSA-N 0.000 claims 1
- RPQVMJSHJBPMOL-SSDOTTSWSA-N 4-[(1r)-1-(2-chloro-5-fluorophenoxy)ethyl]pyrimidin-2-amine Chemical compound O([C@H](C)C=1N=C(N)N=CC=1)C1=CC(F)=CC=C1Cl RPQVMJSHJBPMOL-SSDOTTSWSA-N 0.000 claims 1
- YIIPERPMWRNKSL-MRVPVSSYSA-N 4-[(1r)-1-(3-fluorophenoxy)ethyl]pyrimidin-2-amine Chemical compound O([C@H](C)C=1N=C(N)N=CC=1)C1=CC=CC(F)=C1 YIIPERPMWRNKSL-MRVPVSSYSA-N 0.000 claims 1
- OCGVPGIOKVTCBH-ZETCQYMHSA-N 4-[(1s)-1-(2,5-difluorophenoxy)ethyl]pyrimidin-2-amine Chemical compound O([C@@H](C)C=1N=C(N)N=CC=1)C1=CC(F)=CC=C1F OCGVPGIOKVTCBH-ZETCQYMHSA-N 0.000 claims 1
- YIIPERPMWRNKSL-QMMMGPOBSA-N 4-[(1s)-1-(3-fluorophenoxy)ethyl]pyrimidin-2-amine Chemical compound O([C@@H](C)C=1N=C(N)N=CC=1)C1=CC=CC(F)=C1 YIIPERPMWRNKSL-QMMMGPOBSA-N 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 239000012752 auxiliary agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US28918209P | 2009-12-22 | 2009-12-22 | |
| EP09180321.3 | 2009-12-22 | ||
| US61/289,182 | 2009-12-22 | ||
| EP09180321 | 2009-12-22 | ||
| PCT/EP2010/070213 WO2011076723A1 (en) | 2009-12-22 | 2010-12-20 | Amino-heteroaryl derivatives as hcn blockers |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013515031A JP2013515031A (ja) | 2013-05-02 |
| JP2013515031A5 true JP2013515031A5 (https=) | 2013-09-26 |
| JP5728024B2 JP5728024B2 (ja) | 2015-06-03 |
Family
ID=42045216
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012545268A Expired - Fee Related JP5728024B2 (ja) | 2009-12-22 | 2010-12-20 | Ｈｃｎ遮断薬としてのアミノ−ヘテロアリール誘導体 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8952001B2 (https=) |
| EP (1) | EP2516397B1 (https=) |
| JP (1) | JP5728024B2 (https=) |
| KR (1) | KR20120095481A (https=) |
| CN (1) | CN102884048B (https=) |
| AR (1) | AR079543A1 (https=) |
| AU (1) | AU2010335231C1 (https=) |
| BR (1) | BR112012015170A8 (https=) |
| CA (1) | CA2783209C (https=) |
| MX (1) | MX2012007426A (https=) |
| RU (1) | RU2549546C2 (https=) |
| WO (1) | WO2011076723A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5917503B2 (ja) * | 2011-05-19 | 2016-05-18 | 株式会社東芝 | モリブデン造粒粉の製造方法 |
| WO2013030665A1 (en) | 2011-09-02 | 2013-03-07 | Purdue Pharma L.P. | Pyrimidines as sodium channel blockers |
| US9133131B2 (en) | 2011-11-15 | 2015-09-15 | Purdue Pharma L.P. | Pyrimidine diol amides as sodium channel blockers |
| RU2014150494A (ru) * | 2012-05-30 | 2016-07-20 | Ф. Хоффманн-Ля Рош Аг | Пирролидиногетероциклы |
| CN106588803A (zh) * | 2016-11-16 | 2017-04-26 | 西南科技大学 | 一种制备5‑乙酰基异噁唑的新方法 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4606757A (en) * | 1982-12-23 | 1986-08-19 | The Dow Chemical Company | Diphenoxymethylpyridines having herbicidal properties |
| KR100197583B1 (ko) | 1997-02-04 | 1999-06-15 | 이민화 | 환자용모니터를 구비한 초음파진단장치 |
| AU2001272421A1 (en) | 2000-05-24 | 2001-12-03 | Akzo Nobel N.V. | Full length human hcn1 ih channel subunit and variants |
| JP4228700B2 (ja) * | 2001-04-10 | 2009-02-25 | 日本新薬株式会社 | 慢性関節リウマチの治療剤 |
| US6980419B2 (en) | 2003-03-12 | 2005-12-27 | Zonare Medical Systems, Inc. | Portable ultrasound unit and docking station |
| CN101023374A (zh) | 2004-09-17 | 2007-08-22 | 皇家飞利浦电子股份有限公司 | 无线超声系统显示器 |
| US20070135437A1 (en) * | 2005-03-04 | 2007-06-14 | Alsgen, Inc. | Modulation of neurodegenerative diseases |
| DK2848610T3 (da) * | 2006-11-15 | 2017-11-06 | Ym Biosciences Australia Pty | Hæmmere af kinaseaktivitet |
| WO2009077608A1 (en) * | 2007-12-19 | 2009-06-25 | Palau Pharma, S. A. | 2 -aminopyrimidine derivatives as histamine h4 antagonists |
| NZ720282A (en) * | 2008-02-28 | 2017-12-22 | Vertex Pharma | Heteroaryl derivatives as cftr modulators |
| TW201022233A (en) | 2008-11-04 | 2010-06-16 | Organon Nv | (Pyrrolidin-2-yl)phenyl derivatives |
-
2010
- 2010-12-20 US US13/518,427 patent/US8952001B2/en active Active
- 2010-12-20 WO PCT/EP2010/070213 patent/WO2011076723A1/en not_active Ceased
- 2010-12-20 JP JP2012545268A patent/JP5728024B2/ja not_active Expired - Fee Related
- 2010-12-20 BR BR112012015170A patent/BR112012015170A8/pt not_active Application Discontinuation
- 2010-12-20 CA CA2783209A patent/CA2783209C/en not_active Expired - Fee Related
- 2010-12-20 CN CN201080064520.9A patent/CN102884048B/zh not_active Expired - Fee Related
- 2010-12-20 RU RU2012131279/04A patent/RU2549546C2/ru not_active IP Right Cessation
- 2010-12-20 MX MX2012007426A patent/MX2012007426A/es active IP Right Grant
- 2010-12-20 AR ARP100104763A patent/AR079543A1/es unknown
- 2010-12-20 EP EP10795690.6A patent/EP2516397B1/en not_active Not-in-force
- 2010-12-20 KR KR1020127019218A patent/KR20120095481A/ko not_active Withdrawn
- 2010-12-20 AU AU2010335231A patent/AU2010335231C1/en not_active Ceased
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