JP2005526723A5 - - Google Patents
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- Publication number
- JP2005526723A5 JP2005526723A5 JP2003567880A JP2003567880A JP2005526723A5 JP 2005526723 A5 JP2005526723 A5 JP 2005526723A5 JP 2003567880 A JP2003567880 A JP 2003567880A JP 2003567880 A JP2003567880 A JP 2003567880A JP 2005526723 A5 JP2005526723 A5 JP 2005526723A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- alkyl
- phenyl
- carboxamide
- pyrazole
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims 30
- 125000003545 alkoxy group Chemical group 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 18
- -1 aralkoxy Chemical group 0.000 claims 15
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 15
- 125000004076 pyridyl group Chemical group 0.000 claims 11
- 125000003710 aryl alkyl group Chemical group 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- 239000012453 solvate Substances 0.000 claims 9
- 125000003386 piperidinyl group Chemical group 0.000 claims 7
- 125000003373 pyrazinyl group Chemical group 0.000 claims 7
- 125000002541 furyl group Chemical group 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 125000002883 imidazolyl group Chemical group 0.000 claims 6
- 125000000842 isoxazolyl group Chemical group 0.000 claims 6
- 125000002757 morpholinyl group Chemical group 0.000 claims 6
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 6
- 125000002971 oxazolyl group Chemical group 0.000 claims 6
- 125000003226 pyrazolyl group Chemical group 0.000 claims 6
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 6
- 125000000168 pyrrolyl group Chemical group 0.000 claims 6
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 6
- 125000000335 thiazolyl group Chemical group 0.000 claims 6
- 125000001544 thienyl group Chemical group 0.000 claims 6
- 125000001425 triazolyl group Chemical group 0.000 claims 6
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 5
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 5
- 125000001786 isothiazolyl group Chemical group 0.000 claims 5
- 125000004193 piperazinyl group Chemical group 0.000 claims 5
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- ZBNXLNQOZROTKK-UHFFFAOYSA-N 1-(3-chlorophenyl)-n-isoquinolin-5-yl-5-methylpyrazole-3-carboxamide Chemical compound CC1=CC(C(=O)NC=2C3=CC=NC=C3C=CC=2)=NN1C1=CC=CC(Cl)=C1 ZBNXLNQOZROTKK-UHFFFAOYSA-N 0.000 claims 2
- BJIGPOHHQXLJJG-UHFFFAOYSA-N 1-(3-fluorophenyl)-n-isoquinolin-5-yl-5-methylpyrazole-3-carboxamide Chemical compound CC1=CC(C(=O)NC=2C3=CC=NC=C3C=CC=2)=NN1C1=CC=CC(F)=C1 BJIGPOHHQXLJJG-UHFFFAOYSA-N 0.000 claims 2
- JXZCRDUDHXLHSO-UHFFFAOYSA-N 1-[2-chloro-5-(trifluoromethyl)phenyl]-n-isoquinolin-5-yl-5-methylpyrazole-3-carboxamide Chemical compound CC1=CC(C(=O)NC=2C3=CC=NC=C3C=CC=2)=NN1C1=CC(C(F)(F)F)=CC=C1Cl JXZCRDUDHXLHSO-UHFFFAOYSA-N 0.000 claims 2
- HESDFBZNGHRRPM-UHFFFAOYSA-N 5-methyl-n-(3-methylisoquinolin-5-yl)-1-[3-(trifluoromethyl)phenyl]pyrazole-3-carboxamide Chemical compound CC1=CC(C(=O)NC=2C3=CC(C)=NC=C3C=CC=2)=NN1C1=CC=CC(C(F)(F)F)=C1 HESDFBZNGHRRPM-UHFFFAOYSA-N 0.000 claims 2
- FRCOEAAEFSEYPE-UHFFFAOYSA-N 5-methyl-n-quinolin-3-yl-1-[3-(trifluoromethyl)phenyl]pyrazole-3-carboxamide Chemical compound CC1=CC(C(=O)NC=2C=C3C=CC=CC3=NC=2)=NN1C1=CC=CC(C(F)(F)F)=C1 FRCOEAAEFSEYPE-UHFFFAOYSA-N 0.000 claims 2
- QKBBWAFNMUOVAZ-UHFFFAOYSA-N 5-methyl-n-quinolin-5-yl-1-[3-(trifluoromethyl)phenyl]pyrazole-3-carboxamide Chemical compound CC1=CC(C(=O)NC=2C3=CC=CN=C3C=CC=2)=NN1C1=CC=CC(C(F)(F)F)=C1 QKBBWAFNMUOVAZ-UHFFFAOYSA-N 0.000 claims 2
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 2
- RNFRFPSSWGWDKI-UHFFFAOYSA-N benzoquinuclidine Chemical group C12=CC=CC=C2N2CCC1CC2 RNFRFPSSWGWDKI-UHFFFAOYSA-N 0.000 claims 2
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- WEKSTRYBSSDRRD-UHFFFAOYSA-N n-[1-acetyl-3-[(dimethylamino)methyl]-3,4-dihydro-2h-quinolin-7-yl]-4-phenylbenzamide Chemical compound C=1C=C2CC(CN(C)C)CN(C(C)=O)C2=CC=1NC(=O)C(C=C1)=CC=C1C1=CC=CC=C1 WEKSTRYBSSDRRD-UHFFFAOYSA-N 0.000 claims 2
- RLUXNAPFXSKUES-UHFFFAOYSA-N n-[3-[(dimethylamino)methyl]-1,2,3,4-tetrahydroquinolin-7-yl]-4-phenylbenzamide Chemical compound C=1C=C2CC(CN(C)C)CNC2=CC=1NC(=O)C(C=C1)=CC=C1C1=CC=CC=C1 RLUXNAPFXSKUES-UHFFFAOYSA-N 0.000 claims 2
- XIROUHIROZWIGD-UHFFFAOYSA-N n-[3-[(dimethylamino)methyl]-1-formyl-3,4-dihydro-2h-quinolin-7-yl]-4-phenylbenzamide Chemical compound C=1C=C2CC(CN(C)C)CN(C=O)C2=CC=1NC(=O)C(C=C1)=CC=C1C1=CC=CC=C1 XIROUHIROZWIGD-UHFFFAOYSA-N 0.000 claims 2
- OXKVEIRVLVYRGP-UHFFFAOYSA-N n-[3-[(dimethylamino)methyl]-1-methylsulfonyl-3,4-dihydro-2h-quinolin-7-yl]-4-phenylbenzamide Chemical compound C=1C=C2CC(CN(C)C)CN(S(C)(=O)=O)C2=CC=1NC(=O)C(C=C1)=CC=C1C1=CC=CC=C1 OXKVEIRVLVYRGP-UHFFFAOYSA-N 0.000 claims 2
- ULGJQTZESNGVFR-UHFFFAOYSA-N n-isoquinolin-5-yl-1-(3-methoxyphenyl)-5-methylpyrazole-3-carboxamide Chemical compound COC1=CC=CC(N2C(=CC(=N2)C(=O)NC=2C3=CC=NC=C3C=CC=2)C)=C1 ULGJQTZESNGVFR-UHFFFAOYSA-N 0.000 claims 2
- CPNKPIYIMJJWTI-UHFFFAOYSA-N n-isoquinolin-5-yl-5-methyl-1-[3-(trifluoromethyl)phenyl]pyrazole-3-carboxamide Chemical compound CC1=CC(C(=O)NC=2C3=CC=NC=C3C=CC=2)=NN1C1=CC=CC(C(F)(F)F)=C1 CPNKPIYIMJJWTI-UHFFFAOYSA-N 0.000 claims 2
- DZXOOWSJLLMRJJ-UHFFFAOYSA-N 5-amino-n-isoquinolin-5-yl-1-[3-(trifluoromethyl)phenyl]pyrazole-3-carboxamide Chemical compound NC1=CC(C(=O)NC=2C3=CC=NC=C3C=CC=2)=NN1C1=CC=CC(C(F)(F)F)=C1 DZXOOWSJLLMRJJ-UHFFFAOYSA-N 0.000 claims 1
- BUZFNXOUWRSUBK-UHFFFAOYSA-N 5-methyl-n-quinolin-8-yl-1-[3-(trifluoromethyl)phenyl]pyrazole-3-carboxamide Chemical compound CC1=CC(C(=O)NC=2C3=NC=CC=C3C=CC=2)=NN1C1=CC=CC(C(F)(F)F)=C1 BUZFNXOUWRSUBK-UHFFFAOYSA-N 0.000 claims 1
- 230000008485 antagonism Effects 0.000 claims 1
- 230000009286 beneficial effect Effects 0.000 claims 1
- 150000003857 carboxamides Chemical class 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- SJDMUMDEWSBHIX-UHFFFAOYSA-N n-[3-[2-(diethylamino)ethyl]-4-methyl-2-oxo-1h-quinolin-7-yl]-4-phenylpiperazine-1-carboxamide Chemical compound C1=C2NC(=O)C(CCN(CC)CC)=C(C)C2=CC=C1NC(=O)N(CC1)CCN1C1=CC=CC=C1 SJDMUMDEWSBHIX-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
Applications Claiming Priority (8)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0203673A GB0203673D0 (en) | 2002-02-15 | 2002-02-15 | Novel compounds |
| GB0203680A GB0203680D0 (en) | 2002-02-15 | 2002-02-15 | Novel compounds |
| GB0203677A GB0203677D0 (en) | 2002-02-15 | 2002-02-15 | Novel compounds |
| GB0209032A GB0209032D0 (en) | 2002-04-19 | 2002-04-19 | Novel compounds |
| GB0209003A GB0209003D0 (en) | 2002-04-19 | 2002-04-19 | Novel compounds |
| GB0209035A GB0209035D0 (en) | 2002-04-19 | 2002-04-19 | Novel compounds |
| GB0221318A GB0221318D0 (en) | 2002-09-13 | 2002-09-13 | Novel compounds |
| PCT/GB2003/000608 WO2003068749A1 (en) | 2002-02-15 | 2003-02-13 | Vanilloid receptor modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005526723A JP2005526723A (ja) | 2005-09-08 |
| JP2005526723A5 true JP2005526723A5 (enExample) | 2006-03-09 |
Family
ID=27739514
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003567880A Pending JP2005526723A (ja) | 2002-02-15 | 2003-02-13 | バニロイド受容体モジュレーター |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US7538121B2 (enExample) |
| EP (2) | EP2033953A1 (enExample) |
| JP (1) | JP2005526723A (enExample) |
| AR (1) | AR038420A1 (enExample) |
| AT (1) | ATE416168T1 (enExample) |
| AU (1) | AU2003245773A1 (enExample) |
| DE (1) | DE60325025D1 (enExample) |
| ES (1) | ES2316777T3 (enExample) |
| TW (1) | TW200403223A (enExample) |
| WO (1) | WO2003068749A1 (enExample) |
Families Citing this family (96)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE465993T1 (de) | 2002-02-01 | 2010-05-15 | Euro Celtique Sa | 2-piperazinpyridine für die schmerzbehandlung |
| US6974818B2 (en) | 2002-03-01 | 2005-12-13 | Euro-Celtique S.A. | 1,2,5-thiadiazol-3-YL-piperazine therapeutic agents useful for treating pain |
| WO2003097586A1 (en) | 2002-05-17 | 2003-11-27 | Janssen Pharmaceutica N.V. | Aminotetralin-derived urea modulators of vanilloid vr1 receptor |
| BR0312322A (pt) | 2002-06-28 | 2005-04-12 | Euro Celtique Sa | Compostos, composições, métodos para o tratamento da dor em um animal, da incontinência urinária em um animal, de uma úlcera em um animal, de sìndrome de intestino irritável em um animal, da doença inflamatória do intestino em um animal, métodos para a inibição da função de vr1 em uma célula, kits e métodos para a preparação de uma composição |
| US7262194B2 (en) | 2002-07-26 | 2007-08-28 | Euro-Celtique S.A. | Therapeutic agents useful for treating pain |
| GB0221157D0 (en) * | 2002-09-12 | 2002-10-23 | Glaxo Group Ltd | Novel treatment |
| US7157462B2 (en) | 2002-09-24 | 2007-01-02 | Euro-Celtique S.A. | Therapeutic agents useful for treating pain |
| GB0226724D0 (en) * | 2002-11-15 | 2002-12-24 | Merck Sharp & Dohme | Therapeutic agents |
| JP4422034B2 (ja) * | 2002-12-06 | 2010-02-24 | バイエル・ヘルスケア・アクチェンゲゼルシャフト | テトラヒドロ−ナフタレン誘導体 |
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- 2003-02-13 AU AU2003245773A patent/AU2003245773A1/en not_active Abandoned
- 2003-02-13 EP EP03739564A patent/EP1480954B1/en not_active Expired - Lifetime
- 2003-02-13 DE DE60325025T patent/DE60325025D1/de not_active Expired - Lifetime
- 2003-02-13 ES ES03739564T patent/ES2316777T3/es not_active Expired - Lifetime
- 2003-02-13 AR ARP030100474A patent/AR038420A1/es unknown
- 2003-02-13 WO PCT/GB2003/000608 patent/WO2003068749A1/en not_active Ceased
- 2003-02-13 AT AT03739564T patent/ATE416168T1/de not_active IP Right Cessation
- 2003-02-13 US US10/503,648 patent/US7538121B2/en not_active Expired - Fee Related
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