JP2008531539A5 - - Google Patents
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- Publication number
- JP2008531539A5 JP2008531539A5 JP2007556671A JP2007556671A JP2008531539A5 JP 2008531539 A5 JP2008531539 A5 JP 2008531539A5 JP 2007556671 A JP2007556671 A JP 2007556671A JP 2007556671 A JP2007556671 A JP 2007556671A JP 2008531539 A5 JP2008531539 A5 JP 2008531539A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- benzisoxazol
- piperidin
- oxy
- pyran
- 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
- -1 carboxy, tetrazolyl Chemical group 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 201000006549 dyspepsia Diseases 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 102000005962 receptors Human genes 0.000 claims 3
- 108020003175 receptors Proteins 0.000 claims 3
- UXIXUNHVTNSKMD-UHFFFAOYSA-N 1-[[4-[[4-(2,2,2-trifluoroethoxy)-1,2-benzoxazol-3-yl]oxymethyl]piperidin-1-yl]methyl]cyclobutane-1-carboxylic acid Chemical compound C1CC(COC=2C3=C(OCC(F)(F)F)C=CC=C3ON=2)CCN1CC1(C(=O)O)CCC1 UXIXUNHVTNSKMD-UHFFFAOYSA-N 0.000 claims 2
- FRHAOXBQUUWPPW-UHFFFAOYSA-N 1-[[4-[[4-(2-methylpropoxy)-1,2-benzoxazol-3-yl]oxymethyl]piperidin-1-yl]methyl]cyclobutane-1-carboxylic acid Chemical compound C1=2C(OCC(C)C)=CC=CC=2ON=C1OCC(CC1)CCN1CC1(C(O)=O)CCC1 FRHAOXBQUUWPPW-UHFFFAOYSA-N 0.000 claims 2
- KNJWDUQVAGKDKN-UHFFFAOYSA-N 2,2-dimethyl-3-[4-[[4-(2,2,2-trifluoroethoxy)-1,2-benzoxazol-3-yl]oxymethyl]piperidin-1-yl]propanoic acid Chemical compound C1CN(CC(C)(C)C(O)=O)CCC1COC1=NOC2=CC=CC(OCC(F)(F)F)=C12 KNJWDUQVAGKDKN-UHFFFAOYSA-N 0.000 claims 2
- FUBDQYLQCKJWAE-UHFFFAOYSA-N 3-[4-[[4-(cyclobutylmethoxy)-1,2-benzoxazol-3-yl]oxymethyl]piperidin-1-yl]-2,2-dimethylpropanoic acid Chemical compound C1CN(CC(C)(C)C(O)=O)CCC1COC1=NOC2=CC=CC(OCC3CCC3)=C12 FUBDQYLQCKJWAE-UHFFFAOYSA-N 0.000 claims 2
- ONQNYJGWMQSMEE-UHFFFAOYSA-N 4-[2-[4-[[4-(2,2,2-trifluoroethoxy)-1,2-benzoxazol-3-yl]oxymethyl]piperidin-1-yl]ethyl]oxane-4-carboxylic acid Chemical compound C1CC(COC=2C3=C(OCC(F)(F)F)C=CC=C3ON=2)CCN1CCC1(C(=O)O)CCOCC1 ONQNYJGWMQSMEE-UHFFFAOYSA-N 0.000 claims 2
- WPIWLBKBCQJDHA-UHFFFAOYSA-N 4-[2-[4-[[4-(2-methylpropoxy)-1,2-benzoxazol-3-yl]oxymethyl]piperidin-1-yl]ethyl]oxane-4-carboxylic acid Chemical compound C1=2C(OCC(C)C)=CC=CC=2ON=C1OCC(CC1)CCN1CCC1(C(O)=O)CCOCC1 WPIWLBKBCQJDHA-UHFFFAOYSA-N 0.000 claims 2
- HSMMHNBGQLGCBY-UHFFFAOYSA-N 4-[[4-[[4-(2,2,2-trifluoroethoxy)-1,2-benzoxazol-3-yl]oxymethyl]piperidin-1-yl]methyl]oxane-4-carboxylic acid Chemical compound C1CC(COC=2C3=C(OCC(F)(F)F)C=CC=C3ON=2)CCN1CC1(C(=O)O)CCOCC1 HSMMHNBGQLGCBY-UHFFFAOYSA-N 0.000 claims 2
- NYKSUAPPIBWVTB-UHFFFAOYSA-N 4-[[4-[[4-(2-methylpropoxy)-1,2-benzoxazol-3-yl]oxymethyl]piperidin-1-yl]methyl]oxane-4-carboxylic acid Chemical compound C1=2C(OCC(C)C)=CC=CC=2ON=C1OCC(CC1)CCN1CC1(C(O)=O)CCOCC1 NYKSUAPPIBWVTB-UHFFFAOYSA-N 0.000 claims 2
- OSVYROXPCDNADU-UHFFFAOYSA-N 4-[[4-[[4-(cyclobutylmethoxy)-1,2-benzoxazol-3-yl]oxymethyl]piperidin-1-yl]methyl]oxane-4-carboxylic acid Chemical compound C1CC(COC=2C3=C(OCC4CCC4)C=CC=C3ON=2)CCN1CC1(C(=O)O)CCOCC1 OSVYROXPCDNADU-UHFFFAOYSA-N 0.000 claims 2
- PHUXSWIUZWOCPN-UHFFFAOYSA-N 4-[[4-[[[4-(2-methylpropoxy)-1,2-benzoxazol-3-yl]amino]methyl]piperidin-1-yl]methyl]oxane-4-carboxylic acid Chemical compound C1=2C(OCC(C)C)=CC=CC=2ON=C1NCC(CC1)CCN1CC1(C(O)=O)CCOCC1 PHUXSWIUZWOCPN-UHFFFAOYSA-N 0.000 claims 2
- LRVGHUMNFQGPKK-KESTWPANSA-N C1=2C(OCC(C)C)=CC=CC=2ON=C1OCC(CC1)CCN1C[C@H]1CC[C@H](C(O)=O)CC1 Chemical compound C1=2C(OCC(C)C)=CC=CC=2ON=C1OCC(CC1)CCN1C[C@H]1CC[C@H](C(O)=O)CC1 LRVGHUMNFQGPKK-KESTWPANSA-N 0.000 claims 2
- LCODUFIYGGWHBR-JCNLHEQBSA-N C1C[C@@H](C(=O)O)CC[C@@H]1CN1CCC(COC=2C3=C(OCC(F)(F)F)C=CC=C3ON=2)CC1 Chemical compound C1C[C@@H](C(=O)O)CC[C@@H]1CN1CCC(COC=2C3=C(OCC(F)(F)F)C=CC=C3ON=2)CC1 LCODUFIYGGWHBR-JCNLHEQBSA-N 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000004850 cyclobutylmethyl group Chemical group C1(CCC1)C* 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 125000004205 trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- XTFIVUDBNACUBN-UHFFFAOYSA-N 1,3,5-trinitro-1,3,5-triazinane Chemical compound [O-][N+](=O)N1CN([N+]([O-])=O)CN([N+]([O-])=O)C1 XTFIVUDBNACUBN-UHFFFAOYSA-N 0.000 claims 1
- LOBORLIRYMJWGF-UHFFFAOYSA-N 2,2-difluoro-3-[4-[[4-(2,2,2-trifluoroethoxy)-1,2-benzoxazol-3-yl]oxymethyl]piperidin-1-yl]propanoic acid Chemical compound C1CN(CC(F)(F)C(=O)O)CCC1COC1=NOC2=CC=CC(OCC(F)(F)F)=C12 LOBORLIRYMJWGF-UHFFFAOYSA-N 0.000 claims 1
- IUDMCGWMTLGWSD-UHFFFAOYSA-N 4-[[4-[2-[[4-(2,2,2-trifluoroethoxy)-1,2-benzoxazol-3-yl]oxy]ethyl]piperidin-1-yl]methyl]oxane-4-carboxylic acid Chemical compound C1CC(CCOC=2C3=C(OCC(F)(F)F)C=CC=C3ON=2)CCN1CC1(C(=O)O)CCOCC1 IUDMCGWMTLGWSD-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 206010010774 Constipation Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 206010028813 Nausea Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 206010030216 Oesophagitis Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 206010047700 Vomiting Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 206010003119 arrhythmia Diseases 0.000 claims 1
- 208000015114 central nervous system disease Diseases 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 125000004851 cyclopentylmethyl group Chemical group C1(CCCC1)C* 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000006881 esophagitis Diseases 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 230000030135 gastric motility Effects 0.000 claims 1
- 208000029493 gastroesophageal disease Diseases 0.000 claims 1
- 208000021302 gastroesophageal reflux disease Diseases 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000008693 nausea Effects 0.000 claims 1
- 230000000144 pharmacologic effect Effects 0.000 claims 1
- 201000002859 sleep apnea Diseases 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US65665305P | 2005-02-25 | 2005-02-25 | |
| US60/656,653 | 2005-02-25 | ||
| US71597705P | 2005-09-09 | 2005-09-09 | |
| US60/715,977 | 2005-09-09 | ||
| PCT/IB2006/000313 WO2006090224A1 (en) | 2005-02-25 | 2006-02-15 | Benzisoxazole derivatives |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012051657A Division JP5509236B2 (ja) | 2005-02-25 | 2012-03-08 | ベンズイソキサゾール誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008531539A JP2008531539A (ja) | 2008-08-14 |
| JP2008531539A5 true JP2008531539A5 (https=) | 2009-03-19 |
| JP4970290B2 JP4970290B2 (ja) | 2012-07-04 |
Family
ID=36101715
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007556671A Expired - Lifetime JP4970290B2 (ja) | 2005-02-25 | 2006-02-15 | ベンズイソキサゾール誘導体 |
| JP2012051657A Expired - Lifetime JP5509236B2 (ja) | 2005-02-25 | 2012-03-08 | ベンズイソキサゾール誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012051657A Expired - Lifetime JP5509236B2 (ja) | 2005-02-25 | 2012-03-08 | ベンズイソキサゾール誘導体 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US8816090B2 (https=) |
| EP (1) | EP1856114B1 (https=) |
| JP (2) | JP4970290B2 (https=) |
| CA (1) | CA2598516C (https=) |
| DK (1) | DK1856114T3 (https=) |
| ES (1) | ES2523459T3 (https=) |
| WO (1) | WO2006090224A1 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0525068D0 (en) | 2005-12-08 | 2006-01-18 | Novartis Ag | Organic compounds |
| JP5540099B2 (ja) | 2009-09-14 | 2014-07-02 | スベン ライフ サイエンシズ リミティド | ５−ｈｔ４受容体リガンドとしての１，２−ジヒドロ−２−オキソキノリン化合物 |
| CA2788656A1 (en) * | 2010-02-16 | 2011-08-25 | Pfizer Inc. | (r)-4-((4-((4-(tetrahydrofuran-3-yloxy)benzo[d]isoxazol-3-yloxy)methyl)piperidin-1-yl)methyl)tetrahydro-2h-pyran-4-ol, a partial agonist of 5-ht4 receptors |
| BR112013020641B1 (pt) | 2011-02-25 | 2021-11-03 | Yuhan Corporation | Composto, composição farmacêutica, processos para a preparação de composto e respectivo uso ou de seu sal farmaceuticamente aceitável |
| JP6051431B2 (ja) * | 2011-03-23 | 2016-12-27 | ラクオリア創薬株式会社 | 消化管運動促進剤として機能する５−ｈｔ４受容体作動物質 |
| WO2012157288A1 (en) | 2011-05-18 | 2012-11-22 | Raqualia Pharma Inc. | Polymorph form of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2h-pyran-4-carboxylic acid |
| PT2758394E (pt) | 2011-09-19 | 2015-04-22 | Suven Life Sciences Ltd | Compostos heteroarilo como ligandos de recetores 5-ht4 |
| BR112015011392A2 (pt) * | 2012-11-21 | 2017-07-11 | Raqualia Pharma Inc | formas polimórficas de ácidos, processo de preparação, composição farmacêutica e uso das mesmas |
| CN105164119B (zh) | 2013-03-20 | 2017-12-08 | 苏文生命科学有限公司 | 作为5‑ht4受体激动剂的5‑氨基‑喹啉‑8‑甲酰胺衍生物 |
| MX368017B (es) | 2013-12-16 | 2019-09-13 | Suven Life Sciences Ltd | Compuestos de indazol como agonistas del receptor de 5-ht4. |
| US9833447B2 (en) * | 2014-05-16 | 2017-12-05 | Raqualia Pharma Inc. | 5-HT4 receptor agonist for gastroparesis |
| CA2944982C (en) * | 2014-05-20 | 2022-06-07 | Raqualia Pharma Inc. | Benzisoxazole derivative salt |
| SG11201706501VA (en) | 2015-02-13 | 2017-09-28 | Suven Life Sciences Ltd | AMIDE COMPOUNDS AS 5-HT<sb>4</sb> RECEPTOR AGONISTS |
| WO2026003716A1 (en) | 2024-06-27 | 2026-01-02 | Pfizer Inc. | Process for preparing n-(6-((1h-pyrazol-1-yl)methyl)-4-methoxybenzo[d]isoxazol- 3-yl)-2-methoxybenzenesulfonamide |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4352811A (en) * | 1981-11-12 | 1982-10-05 | Hoechst-Roussel Pharmaceuticals Inc. | 3-(1-Substituted-4-piperidyl)-1,2-benzisoxazoles |
| FR2654104B1 (fr) * | 1989-11-07 | 1992-01-03 | Adir | Nouveaux derives du 1,2-benzisoxazole, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent. |
| FR2674855B1 (fr) * | 1991-04-03 | 1994-01-14 | Synthelabo | Derives de piperidine, leur preparation et leur application en therapeutique. |
| EP0602242A4 (en) * | 1991-08-22 | 1994-06-29 | Yoshitomi Pharmaceutical | Benzisoxazole compound and use thereof. |
| JPH05320160A (ja) * | 1991-08-22 | 1993-12-03 | Yoshitomi Pharmaceut Ind Ltd | ベンゾイソオキサゾール化合物 |
| JPH0641125A (ja) * | 1992-03-26 | 1994-02-15 | Yoshitomi Pharmaceut Ind Ltd | ベンゾイソオキサゾール化合物およびその用途 |
| EP0873990A1 (en) * | 1995-09-22 | 1998-10-28 | Yoshitomi Pharmaceutical Industries, Ltd. | Benzoic acid compounds and medicinal use thereof |
| FR2749304B1 (fr) * | 1996-06-04 | 1998-06-26 | Adir | Nouveaux derives du 3-(piperid-4-yl)1,2-benzisoxazole et du 3-(piperazin-4-yl)1,2-benzisoxazole, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent |
| JP4627882B2 (ja) * | 1998-02-09 | 2011-02-09 | デユフアー・インターナシヨナル・リサーチ・ベー・ブイ | Ｄ４−アンタゴニスト活性を有するベンズイソキサゾール誘導体 |
-
2006
- 2006-02-15 CA CA2598516A patent/CA2598516C/en not_active Expired - Lifetime
- 2006-02-15 DK DK06710393.7T patent/DK1856114T3/en active
- 2006-02-15 WO PCT/IB2006/000313 patent/WO2006090224A1/en not_active Ceased
- 2006-02-15 US US11/814,588 patent/US8816090B2/en not_active Expired - Lifetime
- 2006-02-15 EP EP06710393.7A patent/EP1856114B1/en not_active Expired - Lifetime
- 2006-02-15 ES ES06710393.7T patent/ES2523459T3/es not_active Expired - Lifetime
- 2006-02-15 JP JP2007556671A patent/JP4970290B2/ja not_active Expired - Lifetime
-
2012
- 2012-03-08 JP JP2012051657A patent/JP5509236B2/ja not_active Expired - Lifetime
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