JP2007513171A5 - - Google Patents
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- Publication number
- JP2007513171A5 JP2007513171A5 JP2006542754A JP2006542754A JP2007513171A5 JP 2007513171 A5 JP2007513171 A5 JP 2007513171A5 JP 2006542754 A JP2006542754 A JP 2006542754A JP 2006542754 A JP2006542754 A JP 2006542754A JP 2007513171 A5 JP2007513171 A5 JP 2007513171A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- benzodiazepine
- ethyl
- alkyl
- methyl
- 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
- 210000000981 Epithelium Anatomy 0.000 claims description 5
- 150000001875 compounds Chemical class 0.000 claims 25
- 239000000203 mixture Substances 0.000 claims 23
- 239000011780 sodium chloride Substances 0.000 claims 15
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 13
- 230000000875 corresponding Effects 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 200000000018 inflammatory disease Diseases 0.000 claims 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- RUJBDQSFYCKFAA-UHFFFAOYSA-N Tofisopam Chemical compound N=1N=C(C)C(CC)C2=CC(OC)=C(OC)C=C2C=1C1=CC=C(OC)C(OC)=C1 RUJBDQSFYCKFAA-UHFFFAOYSA-N 0.000 claims 2
- 125000003310 benzodiazepinyl group Chemical group N1N=C(C=CC2=C1C=CC=C2)* 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 2
- -1 salt compound Chemical class 0.000 claims 2
- 230000001225 therapeutic Effects 0.000 claims 2
- RUJBDQSFYCKFAA-HNNXBMFYSA-N (5R)-1-(3,4-dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5H-2,3-benzodiazepine Chemical compound C1([C@H](C(=NN=2)C)CC)=CC(OC)=C(OC)C=C1C=2C1=CC=C(OC)C(OC)=C1 RUJBDQSFYCKFAA-HNNXBMFYSA-N 0.000 claims 1
- SHRHVSNRULCERG-AWEZNQCLSA-N (5R)-1-(3,4-dimethoxyphenyl)-5-ethyl-7-methoxy-4-methyl-5H-2,3-benzodiazepin-8-ol Chemical compound C1([C@H](C(=NN=2)C)CC)=CC(OC)=C(O)C=C1C=2C1=CC=C(OC)C(OC)=C1 SHRHVSNRULCERG-AWEZNQCLSA-N 0.000 claims 1
- SHRHVSNRULCERG-UHFFFAOYSA-N 1-(3,4-dimethoxyphenyl)-5-ethyl-7-methoxy-4-methyl-5H-2,3-benzodiazepin-8-ol Chemical compound N=1N=C(C)C(CC)C2=CC(OC)=C(O)C=C2C=1C1=CC=C(OC)C(OC)=C1 SHRHVSNRULCERG-UHFFFAOYSA-N 0.000 claims 1
- ROGBMOMCGNYQGY-UHFFFAOYSA-N 1-(3,4-dimethoxyphenyl)-5-ethyl-8-methoxy-4-methyl-2,5-dihydro-2,3-benzodiazepin-7-one Chemical compound N1N=C(C)C(CC)C2=CC(=O)C(OC)=CC2=C1C1=CC=C(OC)C(OC)=C1 ROGBMOMCGNYQGY-UHFFFAOYSA-N 0.000 claims 1
- 125000003762 3,4-dimethoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C(OC([H])([H])[H])C([H])=C1* 0.000 claims 1
- DZXRAZFRRZSDCL-UHFFFAOYSA-N 4-(5-ethyl-7,8-dimethoxy-4-methyl-2,5-dihydro-2,3-benzodiazepin-1-ylidene)-2-methoxycyclohexa-2,5-dien-1-one Chemical compound N1N=C(C)C(CC)C2=CC(OC)=C(OC)C=C2C1=C1C=CC(=O)C(OC)=C1 DZXRAZFRRZSDCL-UHFFFAOYSA-N 0.000 claims 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 1
- FLOQWEXJOIQDKK-UHFFFAOYSA-N 5-(5-ethyl-7,8-dimethoxy-4-methyl-5H-2,3-benzodiazepin-1-yl)-2-methoxyphenol Chemical compound N=1N=C(C)C(CC)C2=CC(OC)=C(OC)C=C2C=1C1=CC=C(OC)C(O)=C1 FLOQWEXJOIQDKK-UHFFFAOYSA-N 0.000 claims 1
- FLOQWEXJOIQDKK-AWEZNQCLSA-N 5-[(5R)-5-ethyl-7,8-dimethoxy-4-methyl-5H-2,3-benzodiazepin-1-yl]-2-methoxyphenol Chemical compound C1([C@H](C(=NN=2)C)CC)=CC(OC)=C(OC)C=C1C=2C1=CC=C(OC)C(O)=C1 FLOQWEXJOIQDKK-AWEZNQCLSA-N 0.000 claims 1
- JAFXCRKJKQGETD-UHFFFAOYSA-N 5-ethyl-1-(3-hydroxy-4-methoxyphenyl)-8-methoxy-4-methyl-2,5-dihydro-2,3-benzodiazepin-7-one Chemical compound N1N=C(C)C(CC)C2=CC(=O)C(OC)=CC2=C1C1=CC=C(OC)C(O)=C1 JAFXCRKJKQGETD-UHFFFAOYSA-N 0.000 claims 1
- LNIVKKQAVRCPTL-UHFFFAOYSA-N 5-ethyl-1-(4-hydroxy-3-methoxyphenyl)-8-methoxy-4-methyl-2,5-dihydro-2,3-benzodiazepin-7-one Chemical compound N1N=C(C)C(CC)C2=CC(=O)C(OC)=CC2=C1C1=CC=C(O)C(OC)=C1 LNIVKKQAVRCPTL-UHFFFAOYSA-N 0.000 claims 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- MVJUBSLMLVQYTD-ZDUSSCGKSA-N C1([C@H](C(=NN=2)C)CC)=CC(O)=C(OC)C=C1C=2C1=CC=C(O)C(OC)=C1 Chemical compound C1([C@H](C(=NN=2)C)CC)=CC(O)=C(OC)C=C1C=2C1=CC=C(O)C(OC)=C1 MVJUBSLMLVQYTD-ZDUSSCGKSA-N 0.000 claims 1
- MWBAHRRFJNAKHK-ZDUSSCGKSA-N C1([C@H](C(=NN=2)C)CC)=CC(O)=C(OC)C=C1C=2C1=CC=C(OC)C(O)=C1 Chemical compound C1([C@H](C(=NN=2)C)CC)=CC(O)=C(OC)C=C1C=2C1=CC=C(OC)C(O)=C1 MWBAHRRFJNAKHK-ZDUSSCGKSA-N 0.000 claims 1
- DFPIIEOUMLCAGE-AWEZNQCLSA-N C1([C@H](C(=NN=2)C)CC)=CC(O)=C(OC)C=C1C=2C1=CC=C(OC)C(OC)=C1 Chemical compound C1([C@H](C(=NN=2)C)CC)=CC(O)=C(OC)C=C1C=2C1=CC=C(OC)C(OC)=C1 DFPIIEOUMLCAGE-AWEZNQCLSA-N 0.000 claims 1
- OQTUSGBCCKOANW-AWEZNQCLSA-N C1([C@H](C(=NN=2)C)CC)=CC(OC)=C(OC)C=C1C=2C1=CC=C(O)C(OC)=C1 Chemical compound C1([C@H](C(=NN=2)C)CC)=CC(OC)=C(OC)C=C1C=2C1=CC=C(O)C(OC)=C1 OQTUSGBCCKOANW-AWEZNQCLSA-N 0.000 claims 1
- 208000008665 Gastrointestinal Disease Diseases 0.000 claims 1
- 208000006641 Skin Disease Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 201000002146 gastrointestinal system disease Diseases 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 description 3
- 230000004054 inflammatory process Effects 0.000 description 3
- 241001465754 Metazoa Species 0.000 description 2
- 230000001154 acute Effects 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 0 *C1C(*)=NN=C(c2ccccc2)c2c1cc(*)c(*)c2 Chemical compound *C1C(*)=NN=C(c2ccccc2)c2c1cc(*)c(*)c2 0.000 description 1
- 210000001072 Colon Anatomy 0.000 description 1
- 229960000633 Dextran Sulfate Drugs 0.000 description 1
- 206010012735 Diarrhoea Diseases 0.000 description 1
- 206010018836 Haematochezia Diseases 0.000 description 1
- 210000004698 Lymphocytes Anatomy 0.000 description 1
- 210000004400 Mucous Membrane Anatomy 0.000 description 1
- 210000000440 Neutrophils Anatomy 0.000 description 1
- 210000004011 Plasma Cells Anatomy 0.000 description 1
- 230000001066 destructive Effects 0.000 description 1
- 201000008286 diarrhea Diseases 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 235000020188 drinking water Nutrition 0.000 description 1
- 239000003651 drinking water Substances 0.000 description 1
- 230000003628 erosive Effects 0.000 description 1
- 235000020680 filtered tap water Nutrition 0.000 description 1
- 230000004927 fusion Effects 0.000 description 1
- 231100001045 histological change Toxicity 0.000 description 1
- 230000036732 histological change Effects 0.000 description 1
- 230000002390 hyperplastic Effects 0.000 description 1
- 238000001764 infiltration Methods 0.000 description 1
- 210000004877 mucosa Anatomy 0.000 description 1
- 231100000915 pathological change Toxicity 0.000 description 1
- 230000036285 pathological change Effects 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 238000004904 shortening Methods 0.000 description 1
- KEAYESYHFKHZAL-UHFFFAOYSA-N sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 235000020679 tap water Nutrition 0.000 description 1
- 239000008399 tap water Substances 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/US2003/038643 WO2004050080A1 (en) | 2002-12-03 | 2003-12-03 | Treatment of inflammatory disorders with 2,3-benzodiazepines |
| US10/727,940 US20040138209A1 (en) | 2002-12-03 | 2003-12-03 | Treatment of inflammatory disorders with 2,3- benzodiazepines |
| PCT/US2004/040403 WO2005056017A1 (en) | 2003-12-03 | 2004-12-03 | Treatment of inflammatory disorders of the epithelium with low dose 2,3-benzodiazepines |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007513171A JP2007513171A (ja) | 2007-05-24 |
| JP2007513171A5 true JP2007513171A5 (no) | 2008-01-31 |
Family
ID=34680839
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006542754A Pending JP2007513171A (ja) | 2003-12-03 | 2004-12-03 | ２，３−ベンゾジアゼピン低投与量による上皮の炎症性疾患の治療 |
Country Status (4)
| Country | Link |
|---|---|
| EP (1) | EP1689408A4 (no) |
| JP (1) | JP2007513171A (no) |
| CA (1) | CA2548038A1 (no) |
| WO (1) | WO2005056017A1 (no) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6638928B1 (en) * | 2002-12-03 | 2003-10-28 | Vela Pharmaceuticals, Inc. | Treatment of irritable bowel syndrome and nonulcer dyspepsia with substituted 2,3-benzodiazepines |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1124556T3 (da) * | 1998-10-27 | 2004-10-11 | Vela Pharmaceuticals Inc | Anvendelse af optisk rent (R)-tofisopam til behandling og forebyggelse af angstsygdomme |
| US6080736A (en) * | 1999-10-27 | 2000-06-27 | Janus Pharmaceuticals, Inc. | Methods and compositions for treating and preventing anxiety and anxiety disorders using optically pure (R) tofisopam |
| FR2824065A1 (fr) * | 2001-04-26 | 2002-10-31 | Neuro3D | Composes inhibiteurs des phosphodiesterases des nucleotides cycliques, preparation et utilisations |
| US6864251B2 (en) * | 2002-12-03 | 2005-03-08 | Vela Pharmaceuticals, Inc. | Treatment of LTB4-mediated inflammatory disorders with optically-pure (R)-2,3-benzodiazepines |
-
2004
- 2004-12-03 WO PCT/US2004/040403 patent/WO2005056017A1/en active Application Filing
- 2004-12-03 CA CA002548038A patent/CA2548038A1/en not_active Abandoned
- 2004-12-03 EP EP04812836A patent/EP1689408A4/en not_active Withdrawn
- 2004-12-03 JP JP2006542754A patent/JP2007513171A/ja active Pending
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