JP2009542787A5 - - Google Patents
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- Publication number
- JP2009542787A5 JP2009542787A5 JP2009518957A JP2009518957A JP2009542787A5 JP 2009542787 A5 JP2009542787 A5 JP 2009542787A5 JP 2009518957 A JP2009518957 A JP 2009518957A JP 2009518957 A JP2009518957 A JP 2009518957A JP 2009542787 A5 JP2009542787 A5 JP 2009542787A5
- Authority
- JP
- Japan
- Prior art keywords
- salt
- salt according
- subject
- composition
- esylate
- 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
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- 150000003839 salts Chemical class 0.000 claims description 40
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical class CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 claims description 20
- 238000000034 method Methods 0.000 claims description 19
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 14
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 12
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims description 12
- 238000004519 manufacturing process Methods 0.000 claims description 12
- 239000000203 mixture Substances 0.000 claims description 12
- 150000001875 compounds Chemical class 0.000 claims description 11
- 239000003814 drug Substances 0.000 claims description 10
- 239000012458 free base Substances 0.000 claims description 8
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 8
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 6
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 6
- 230000000147 hypnotic effect Effects 0.000 claims description 6
- 239000002244 precipitate Substances 0.000 claims description 6
- 239000002904 solvent Substances 0.000 claims description 6
- 206010039897 Sedation Diseases 0.000 claims description 5
- 230000000949 anxiolytic effect Effects 0.000 claims description 5
- 230000036280 sedation Effects 0.000 claims description 5
- 206010010904 Convulsion Diseases 0.000 claims description 4
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims description 4
- 206010021118 Hypotonia Diseases 0.000 claims description 4
- 230000036461 convulsion Effects 0.000 claims description 4
- 230000036640 muscle relaxation Effects 0.000 claims description 4
- 230000002921 anti-spasmodic effect Effects 0.000 claims description 3
- 239000002249 anxiolytic agent Substances 0.000 claims description 3
- 239000000812 cholinergic antagonist Substances 0.000 claims description 3
- 239000013078 crystal Substances 0.000 claims description 3
- 239000003158 myorelaxant agent Substances 0.000 claims description 3
- -1 MtBE Chemical compound 0.000 claims description 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 claims description 2
- 239000012296 anti-solvent Substances 0.000 claims description 2
- 239000006184 cosolvent Substances 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- WBJINCZRORDGAQ-UHFFFAOYSA-N formic acid ethyl ester Natural products CCOC=O WBJINCZRORDGAQ-UHFFFAOYSA-N 0.000 claims description 2
- JMMWKPVZQRWMSS-UHFFFAOYSA-N isopropanol acetate Natural products CC(C)OC(C)=O JMMWKPVZQRWMSS-UHFFFAOYSA-N 0.000 claims description 2
- 229940011051 isopropyl acetate Drugs 0.000 claims description 2
- GWYFCOCPABKNJV-UHFFFAOYSA-N isovaleric acid Chemical compound CC(C)CC(O)=O GWYFCOCPABKNJV-UHFFFAOYSA-N 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 239000000243 solution Substances 0.000 claims 4
- 230000001773 anti-convulsant effect Effects 0.000 claims 1
- 239000001961 anticonvulsive agent Substances 0.000 claims 1
- 229960003965 antiepileptics Drugs 0.000 claims 1
- 239000007864 aqueous solution Substances 0.000 claims 1
- 238000001704 evaporation Methods 0.000 claims 1
- 239000005554 hypnotics and sedatives Substances 0.000 claims 1
- CYHWMBVXXDIZNZ-KRWDZBQOSA-N Cc1cnc2[n]1-c(ccc(Br)c1)c1C(c1ncccc1)=N[C@H]2CCC(OC)=O Chemical compound Cc1cnc2[n]1-c(ccc(Br)c1)c1C(c1ncccc1)=N[C@H]2CCC(OC)=O CYHWMBVXXDIZNZ-KRWDZBQOSA-N 0.000 description 2
- 208000019901 Anxiety disease Diseases 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000000932 sedative agent Substances 0.000 description 1
- 230000001624 sedative effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0613693.1 | 2006-07-10 | ||
| GBGB0613693.1A GB0613693D0 (en) | 2006-07-10 | 2006-07-10 | Benzodiazepine salts (3) |
| PCT/GB2007/002583 WO2008007081A1 (en) | 2006-07-10 | 2007-07-10 | Short-acting benzodiazepine salts and their polymorphic forms |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009542787A JP2009542787A (ja) | 2009-12-03 |
| JP2009542787A5 true JP2009542787A5 (https=) | 2011-08-04 |
| JP5394238B2 JP5394238B2 (ja) | 2014-01-22 |
Family
ID=36926778
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009518957A Active JP5394238B2 (ja) | 2006-07-10 | 2007-07-10 | 短時間作用型ベンゾジアゼピンの塩およびその多型形態 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US8642588B2 (https=) |
| EP (1) | EP2089378B1 (https=) |
| JP (1) | JP5394238B2 (https=) |
| AT (1) | ATE461927T1 (https=) |
| CA (1) | CA2657369C (https=) |
| DE (1) | DE602007005515D1 (https=) |
| ES (1) | ES2343444T3 (https=) |
| GB (1) | GB0613693D0 (https=) |
| WO (1) | WO2008007081A1 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2657347C (en) | 2006-07-10 | 2014-11-18 | Paion Uk Limited | Short-acting benzodiazepine salts and their polymorphic forms |
| EP2305647A1 (en) | 2009-09-18 | 2011-04-06 | PAION UK Limited | Process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4 H-imidazo[1,2-a][1,4]benzodiazepine-4-yl] propionic acid methyl ester or the benzene sulfonate salt thereof, and compounds useful in that process |
| EP2450039A1 (en) * | 2010-11-08 | 2012-05-09 | PAION UK Ltd. | Dosing regimen for sedation with CNS 7056 (Remimazolam) |
| CN102964349A (zh) * | 2011-08-31 | 2013-03-13 | 江苏恒瑞医药股份有限公司 | 苯并二氮杂*衍生物的托西酸盐及其多晶型、它们的制备方法和用途 |
| NZ702063A (en) * | 2012-05-22 | 2016-11-25 | Paion Uk Ltd | Compositions comprising short-acting benzodiazepines |
| UA116452C2 (uk) | 2012-08-31 | 2018-03-26 | ПАЙОН ЮКей ЛІМІТЕД | Режим дозування седативного засобу |
| AR094963A1 (es) | 2013-03-04 | 2015-09-09 | Ono Pharmaceutical Co | Reacción de oxidación excelente en el índice de conversión |
| CN103232454A (zh) * | 2013-05-05 | 2013-08-07 | 王元青 | 治疗精神疾病的药物 |
| CN104146970A (zh) * | 2013-05-05 | 2014-11-19 | 王元青 | 治疗精神疾病的冻干粉针剂 |
| CN103230595B (zh) * | 2013-05-05 | 2014-10-08 | 李友香 | 治疗精神疾病的组合物 |
| CN103202815B (zh) * | 2013-05-05 | 2014-09-24 | 李友香 | 治疗精神疾病的注射剂 |
| CN105130996B (zh) * | 2015-08-07 | 2017-05-03 | 成都倍特药业有限公司 | 苯并二氮杂*衍生物的1,5‑萘二磺酸盐及晶型和它们的制备方法 |
| EP3442539B1 (en) | 2016-04-14 | 2025-04-09 | Paion UK Limited | Orally inhaled and nasal benzodiazepines |
| CN108503644B (zh) | 2016-12-09 | 2019-06-14 | 成都倍特药业有限公司 | 一种苯并二氮杂*衍生物的氢溴酸盐及其制备方法和用途 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3933794A (en) | 1971-08-04 | 1976-01-20 | The Upjohn Company | 2-(2-Alkynylamino)-3H-1,4-benzodiazepines |
| US4724237A (en) | 1984-06-26 | 1988-02-09 | Merck & Co., Inc. | 2-substituted-aminomethyl-1,4-benzodiazepines |
| US5019583A (en) | 1989-02-15 | 1991-05-28 | Glaxo Inc. | N-phenyl-N-(4-piperidinyl)amides useful as analgesics |
| AU678503B2 (en) | 1993-09-24 | 1997-05-29 | Takeda Chemical Industries Ltd. | Condensed heterocyclic compounds and their use as squalene synthetase inhibitors |
| CA2143246C (en) | 1994-03-16 | 2000-08-22 | Thierry Godel | Imidazodiazepines |
| US5834464A (en) | 1994-11-18 | 1998-11-10 | Merck & Co., Inc. | Imidazolinobenzodiazepines |
| PT801651E (pt) | 1995-01-06 | 2001-12-28 | Hoffmann La Roche | Hidroximetil-imidazodiazepinas e seus esteres |
| AU4382896A (en) | 1995-02-02 | 1996-08-21 | F. Hoffmann-La Roche Ag | Acetylimidazobenzodiazepines |
| US7160880B1 (en) | 1999-05-14 | 2007-01-09 | Cenes Limited | Short-acting benzodiazepines |
| GB9911152D0 (en) * | 1999-05-14 | 1999-07-14 | Glaxo Group Ltd | Short-acting benzodiazepines |
| SI21850A (sl) * | 2004-07-28 | 2006-02-28 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Soli olanzapina in njihova pretvorba v prosto bazo olanzapina |
| CA2657347C (en) | 2006-07-10 | 2014-11-18 | Paion Uk Limited | Short-acting benzodiazepine salts and their polymorphic forms |
-
2006
- 2006-07-10 GB GBGB0613693.1A patent/GB0613693D0/en not_active Ceased
-
2007
- 2007-07-10 ES ES07733519T patent/ES2343444T3/es active Active
- 2007-07-10 CA CA2657369A patent/CA2657369C/en active Active
- 2007-07-10 AT AT07733519T patent/ATE461927T1/de active
- 2007-07-10 US US12/373,457 patent/US8642588B2/en active Active
- 2007-07-10 EP EP07733519A patent/EP2089378B1/en active Active
- 2007-07-10 DE DE602007005515T patent/DE602007005515D1/de active Active
- 2007-07-10 WO PCT/GB2007/002583 patent/WO2008007081A1/en not_active Ceased
- 2007-07-10 JP JP2009518957A patent/JP5394238B2/ja active Active
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