JP2010526051A5 - - Google Patents
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- Publication number
- JP2010526051A5 JP2010526051A5 JP2010504894A JP2010504894A JP2010526051A5 JP 2010526051 A5 JP2010526051 A5 JP 2010526051A5 JP 2010504894 A JP2010504894 A JP 2010504894A JP 2010504894 A JP2010504894 A JP 2010504894A JP 2010526051 A5 JP2010526051 A5 JP 2010526051A5
- Authority
- JP
- Japan
- Prior art keywords
- pyrazin
- carboxamide
- phenyl
- amino
- trifluoromethoxy
- 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.)
- Withdrawn
Links
- 150000003839 salts Chemical class 0.000 claims 9
- 239000012453 solvate Substances 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 5
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- CEJKMICKPLFCPJ-UHFFFAOYSA-N n-[6-amino-5-[2-(trifluoromethoxy)phenyl]pyrazin-2-yl]-2-ethylpyrazole-3-carboxamide Chemical compound CCN1N=CC=C1C(=O)NC1=CN=C(C=2C(=CC=CC=2)OC(F)(F)F)C(N)=N1 CEJKMICKPLFCPJ-UHFFFAOYSA-N 0.000 claims 1
- UGHAYWPBUHQJNK-UHFFFAOYSA-N n-[6-amino-5-[2-(trifluoromethoxy)phenyl]pyrazin-2-yl]-2-propan-2-ylpyrazole-3-carboxamide Chemical compound CC(C)N1N=CC=C1C(=O)NC1=CN=C(C=2C(=CC=CC=2)OC(F)(F)F)C(N)=N1 UGHAYWPBUHQJNK-UHFFFAOYSA-N 0.000 claims 1
- IYGNIHHQJIPWBL-UHFFFAOYSA-N n-[6-amino-5-[2-(trifluoromethoxy)phenyl]pyrazin-2-yl]-3-(methoxymethyl)-1,2-oxazole-4-carboxamide Chemical compound COCC1=NOC=C1C(=O)NC1=CN=C(C=2C(=CC=CC=2)OC(F)(F)F)C(N)=N1 IYGNIHHQJIPWBL-UHFFFAOYSA-N 0.000 claims 1
- FPEVBIZIYIUURP-UHFFFAOYSA-N n-[6-amino-5-[2-(trifluoromethoxy)phenyl]pyrazin-2-yl]-3-methyl-1,2-oxazole-4-carboxamide Chemical compound CC1=NOC=C1C(=O)NC1=CN=C(C=2C(=CC=CC=2)OC(F)(F)F)C(N)=N1 FPEVBIZIYIUURP-UHFFFAOYSA-N 0.000 claims 1
- SZHKZPFWVWUNQO-UHFFFAOYSA-N n-[6-amino-5-[2-(trifluoromethoxy)phenyl]pyrazin-2-yl]-5-(methoxymethyl)-1,2-oxazole-4-carboxamide Chemical compound O1N=CC(C(=O)NC=2N=C(N)C(=NC=2)C=2C(=CC=CC=2)OC(F)(F)F)=C1COC SZHKZPFWVWUNQO-UHFFFAOYSA-N 0.000 claims 1
- KXUMBZHAWOLSKD-UHFFFAOYSA-N n-[6-amino-5-[2-(trifluoromethyl)phenyl]pyrazin-2-yl]-3-methyl-1,2-oxazole-4-carboxamide Chemical compound CC1=NOC=C1C(=O)NC1=CN=C(C=2C(=CC=CC=2)C(F)(F)F)C(N)=N1 KXUMBZHAWOLSKD-UHFFFAOYSA-N 0.000 claims 1
- UTHRQYLTFYBSPN-UHFFFAOYSA-N n-[6-amino-5-[5-chloro-2-(trifluoromethoxy)phenyl]pyrazin-2-yl]-2-methylpyrazole-3-carboxamide Chemical compound CN1N=CC=C1C(=O)NC1=CN=C(C=2C(=CC=C(Cl)C=2)OC(F)(F)F)C(N)=N1 UTHRQYLTFYBSPN-UHFFFAOYSA-N 0.000 claims 1
- HYQNDXAIULPCIX-UHFFFAOYSA-N n-[6-amino-5-[5-chloro-2-(trifluoromethoxy)phenyl]pyrazin-2-yl]-3-methyl-1,2-oxazole-4-carboxamide Chemical compound CC1=NOC=C1C(=O)NC1=CN=C(C=2C(=CC=C(Cl)C=2)OC(F)(F)F)C(N)=N1 HYQNDXAIULPCIX-UHFFFAOYSA-N 0.000 claims 1
- MXASHBCILUYQJY-UHFFFAOYSA-N n-[6-amino-5-[5-ethoxy-2-(trifluoromethoxy)phenyl]pyrazin-2-yl]-2-methylpyrazole-3-carboxamide Chemical compound CCOC1=CC=C(OC(F)(F)F)C(C=2C(=NC(NC(=O)C=3N(N=CC=3)C)=CN=2)N)=C1 MXASHBCILUYQJY-UHFFFAOYSA-N 0.000 claims 1
- MIPDTACEPTYIGK-UHFFFAOYSA-N n-[6-amino-5-[5-ethoxy-2-(trifluoromethoxy)phenyl]pyrazin-2-yl]-3-methyl-1,2-oxazole-4-carboxamide Chemical compound CCOC1=CC=C(OC(F)(F)F)C(C=2C(=NC(NC(=O)C=3C(=NOC=3)C)=CN=2)N)=C1 MIPDTACEPTYIGK-UHFFFAOYSA-N 0.000 claims 1
- HZAGYNWZXLPKOA-UHFFFAOYSA-N n-[6-amino-5-[5-fluoro-2-(trifluoromethoxy)phenyl]pyrazin-2-yl]-2-methylpyrazole-3-carboxamide Chemical compound CN1N=CC=C1C(=O)NC1=CN=C(C=2C(=CC=C(F)C=2)OC(F)(F)F)C(N)=N1 HZAGYNWZXLPKOA-UHFFFAOYSA-N 0.000 claims 1
- KVGZRUOOUZTLJL-UHFFFAOYSA-N n-[6-amino-5-[5-fluoro-2-(trifluoromethoxy)phenyl]pyrazin-2-yl]-3-methyl-1,2-oxazole-4-carboxamide Chemical compound CC1=NOC=C1C(=O)NC1=CN=C(C=2C(=CC=C(F)C=2)OC(F)(F)F)C(N)=N1 KVGZRUOOUZTLJL-UHFFFAOYSA-N 0.000 claims 1
- CKJKRXIOOOTHOP-UHFFFAOYSA-N n-[6-amino-5-[5-fluoro-2-(trifluoromethyl)phenyl]pyrazin-2-yl]-3-(trifluoromethyl)-1,2-oxazole-4-carboxamide Chemical compound C=1N=C(C=2C(=CC=C(F)C=2)C(F)(F)F)C(N)=NC=1NC(=O)C1=CON=C1C(F)(F)F CKJKRXIOOOTHOP-UHFFFAOYSA-N 0.000 claims 1
- VNTCPWFJAZYNKF-UHFFFAOYSA-N n-[6-amino-5-[5-fluoro-2-(trifluoromethyl)phenyl]pyrazin-2-yl]-3-methyl-1,2-oxazole-4-carboxamide Chemical compound CC1=NOC=C1C(=O)NC1=CN=C(C=2C(=CC=C(F)C=2)C(F)(F)F)C(N)=N1 VNTCPWFJAZYNKF-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91575207P | 2007-05-03 | 2007-05-03 | |
| US95753207P | 2007-08-23 | 2007-08-23 | |
| PCT/IB2008/001062 WO2008135830A1 (en) | 2007-05-03 | 2008-04-21 | N- [6-amino-s- (phenyl) pyrazin-2-yl] -isoxazole-4-carboxamide derivatives and related compounds as nav1.8 channel modulators for the treatment of pain |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010526051A JP2010526051A (ja) | 2010-07-29 |
| JP2010526051A5 true JP2010526051A5 (enExample) | 2011-06-02 |
Family
ID=39739527
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010504894A Withdrawn JP2010526051A (ja) | 2007-05-03 | 2008-04-21 | 疼痛を治療するためのｎａｖ１．８チャネルモジュレーターとしてのｎ−［６−アミノ−５−（フェニル）ピラジン−２−イル］−イソオキサゾール−４−カルボキサミド誘導体および関連化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20100227872A1 (enExample) |
| EP (1) | EP2155727A1 (enExample) |
| JP (1) | JP2010526051A (enExample) |
| CA (1) | CA2685952C (enExample) |
| WO (1) | WO2008135830A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20100007956A (ko) | 2007-05-03 | 2010-01-22 | 화이자 리미티드 | 나트륨 채널 조절제로서의 2-피리딘 카복스아마이드 유도체 |
| US9079878B2 (en) * | 2011-10-26 | 2015-07-14 | Pfizer Limited | (4-phenylimidazol-2-yl) ethylamine derivatives useful as sodium channel modulators |
| WO2013114250A1 (en) | 2012-02-03 | 2013-08-08 | Pfizer Inc. | Benziimidazole and imidazopyridine derivatives as sodium channel modulators |
| CN115703719B (zh) * | 2021-08-03 | 2024-04-30 | 联化科技股份有限公司 | 一种溴化肟类化合物的制备方法 |
| CA3256486A1 (en) | 2022-04-25 | 2023-11-02 | Siteone Therapeutics Inc | Bicyclic Na V1.8 Heterocyclic Amide Inhibitors for Pain Management |
| WO2025160286A1 (en) | 2024-01-24 | 2025-07-31 | Siteone Therapeutics, Inc. | 2-aryl cycloalkyl and heterocycloalkyl inhibitors of nav1.8 for the treatment of pain |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MA26473A1 (fr) * | 1997-03-01 | 2004-12-20 | Glaxo Group Ltd | Composes pharmacologiquement actifs. |
| EP1802580A2 (en) * | 2004-07-23 | 2007-07-04 | Pfizer, Inc. | Pyridine derivatives |
| NL2000284C2 (nl) * | 2005-11-04 | 2007-09-28 | Pfizer Ltd | Pyrazine-derivaten. |
-
2008
- 2008-04-21 US US12/598,308 patent/US20100227872A1/en not_active Abandoned
- 2008-04-21 EP EP08737568A patent/EP2155727A1/en not_active Withdrawn
- 2008-04-21 JP JP2010504894A patent/JP2010526051A/ja not_active Withdrawn
- 2008-04-21 CA CA2685952A patent/CA2685952C/en not_active Expired - Fee Related
- 2008-04-21 WO PCT/IB2008/001062 patent/WO2008135830A1/en not_active Ceased