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1. 发明授权

US09561236B2 Dosing regimen for sedation with CNS 7056 (Remimazolam) 有权
标题翻译：用中枢神经系统7056（雷莫唑仑）镇静剂量给药方案
公开(公告)号：US09561236B2
公开(公告)日：2017-02-07
申请号：US13883935
申请日：2011-11-07
申请人： Karin Wilhelm-Ogunbiyi , Keith Borkett , Gary Stuart Tilbrook , Hugh Wiltshire
发明人： Karin Wilhelm-Ogunbiyi , Keith Borkett , Gary Stuart Tilbrook , Hugh Wiltshire
IPC分类号： A61K31/5517 , A61K31/4468 , A61K45/06
CPC分类号： A61K31/5517 , A61K9/0019 , A61K31/4468 , A61K45/06 , A61K2300/00
摘要： The invention relates to a dosing regimen for sedation with the fast-acting benzodiazepine CNS 7056 in combination with an opioid, in particular fentanyl, whereas CNS 7056 is given in a dose of 2 to 20 mg, preferably between 4 and 9 mg and most preferably between 5 and 8 mg.
摘要翻译：本发明涉及一种用快速作用苯二氮卓CNS 7056与阿片样物质，特别是芬太尼联合镇静的给药方案，而CNS 7056以2至20mg，优选4至9mg的剂量给予，最优选 5至8毫克。

2. 发明申请

US20140080815A1 DOSING REGIMEN FOR SEDATION WITH CNS 7056 (REMIMAZOLAM) 有权
标题翻译：用于与CNS 7056（REMIMAZOLAM）
公开(公告)号：US20140080815A1
公开(公告)日：2014-03-20
申请号：US13883935
申请日：2011-11-07
申请人： Karin Wilhelm-Ogunbiyi , Keith Borkett , Gary Stuart Tilbrook , Hugh Wiltshire
发明人： Karin Wilhelm-Ogunbiyi , Keith Borkett , Gary Stuart Tilbrook , Hugh Wiltshire
IPC分类号： A61K31/5517 , A61K45/06 , A61K31/4468
CPC分类号： A61K31/5517 , A61K9/0019 , A61K31/4468 , A61K45/06 , A61K2300/00
摘要： The invention relates to a dosing regimen for sedation with the fast-acting benzodiazepine CNS 7056 in combination with an opioid, in particular fentanyl, whereas CNS 7056 is given in a dose of 2 to 10 mg, preferably between 4 and 9 mg and most preferably between 5 and 8 mg.
摘要翻译：本发明涉及一种用快速作用苯二氮卓CNS 7056与阿片样物质，特别是芬太尼联合镇静的给药方案，而CNS 7056剂量为2至10mg，优选4至9mg，最优选 5至8毫克。

3. 发明申请

US20150368199A1 PROCESS FOR PREPARING 3-[(4S)-8-BROMO-1-METHYL-6-(2-PYRIDINYL)-4H-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 有权
标题翻译：制备3 - [（4S）-8-溴-1-甲基-6-（2-吡啶基）-4H-咪唑并[1,2-A] [1,4]苯并噻吩并[4-y]]丙酸甲酯的方法 ESTER或其中的苯甲磺酸盐及其用途的化合物
公开(公告)号：US20150368199A1
公开(公告)日：2015-12-24
申请号：US14841899
申请日：2015-09-01
申请人： Gary Stuart Tilbrook , Andreas Schumacher , Rene Emmenegger
发明人： Gary Stuart Tilbrook , Andreas Schumacher , Rene Emmenegger
IPC分类号： C07D213/50
CPC分类号： C07D401/04 , C07D213/40 , C07D213/50 , C07D487/04 , C07F9/65586
摘要： The invention concerns a new process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]-propionic acid methyl ester or 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]propionic acid methyl ester benzene sulfonate (P) which comprises reacting 3-[(S)-7-bromo-2-((R and/or S)-2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]-propionic acid methyl ester of formula (EM) with an oxidizing agent and optionally treating the reaction product under acidic conditions, such as to produce the compound of formula (F) or the compound (P), and new compounds useful as starting material or as intermediate for performing that process.
摘要翻译：本发明涉及一种制备3 - [（4S）-8-溴-1-甲基-6-（2-吡啶基）-4H-咪唑并[1,2-a] [1,4]苯并二氮杂- 吡啶-3-基] - 丙酸甲酯或3 - [（4S）-8-溴-1-甲基-6-（2-吡啶基）-4H-咪唑并〔1,2-a〕〔1,4〕苯并二氮杂-4- 吡啶-2-基]丙酸甲酯苯磺酸盐（P），其包括使3 - [（S）-7-溴-2 - （（R和/或S）-2-羟基 - 丙基氨基） -3H-苯并[e] [1,4]二氮杂-3-基] - 丙酸甲酯与氧化剂反应，并在酸性条件下任选地处理反应产物，例如制备式（F）或化合物（P），以及可用作原料的新化合物或用于进行该方法的中间体。

4. 发明授权

US08642588B2 Short-acting benzodiazepine salts and their polymorphic forms 有权
标题翻译：短效苯二氮卓类盐及其多晶型物
公开(公告)号：US08642588B2
公开(公告)日：2014-02-04
申请号：US12373457
申请日：2007-07-10
申请人： Gary Stuart Tilbrook , Louisa Jane Cubitt
发明人： Gary Stuart Tilbrook , Louisa Jane Cubitt
IPC分类号： A61P25/20 , A61K31/55 , C07D401/04
CPC分类号： C07D401/04
摘要： The invention relates to esylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.
摘要翻译：本发明涉及式（I）化合物的盐酸盐：还描述了制备盐的方法及其作为药物的用途，特别是用于镇静或催眠，抗焦虑，肌肉松弛剂或抗惊厥剂的用途。

5. 发明授权

US09193730B2 Short-acting benzodiazepine salts and their polymorphic forms 有权
标题翻译：短效苯二氮卓类盐及其多晶型物
公开(公告)号：US09193730B2
公开(公告)日：2015-11-24
申请号：US12373472
申请日：2007-07-10
申请人： Gary Stuart Tilbrook , Louisa Jane Cubitt
发明人： Gary Stuart Tilbrook , Louisa Jane Cubitt
IPC分类号： C07D401/14 , C07D487/12 , C07D487/04
CPC分类号： C07D487/04 , C07B2200/07 , C07B2200/13 , C07C309/29
摘要： The invention relates to besylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.
摘要翻译：本发明涉及式（I）化合物的苯磺酸盐：制备盐的方法及其作为药物的用途，特别是用于镇静或催眠，抗焦虑，肌肉松弛剂或抗惊厥药物的用途。

6. 发明申请

US20100081647A1 SHORT-ACTING BENZODIAZEPINE SALTS AND THEIR POLYMORPHIC FORMS 有权
标题翻译：短效苯扎林盐及其多形态
公开(公告)号：US20100081647A1
公开(公告)日：2010-04-01
申请号：US12373472
申请日：2007-07-10
申请人： Gary Stuart Tilbrook , Louisa Jane Cubitt
发明人： Gary Stuart Tilbrook , Louisa Jane Cubitt
IPC分类号： A61K31/551 , C07D487/04 , A61P25/18
CPC分类号： C07D487/04 , C07B2200/07 , C07B2200/13 , C07C309/29
摘要： The invention relates to besylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.
摘要翻译：本发明涉及式（I）化合物的苯磺酸盐：制备盐的方法及其作为药物的用途，特别是用于镇静或催眠，抗焦虑，肌肉松弛剂或抗惊厥药物的用途。

7. 发明授权

US09156842B2 Process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-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 有权
标题翻译：制备3 - [（4S）-8-溴-1-甲基-6-（2-吡啶基）-4H-咪唑并[1,2-A] [1,4]苯并二氮杂-4-YL]丙酸甲酯酯或其苯磺酸盐，以及可用于该方法的化合物
公开(公告)号：US09156842B2
公开(公告)日：2015-10-13
申请号：US13496742
申请日：2010-09-15
申请人： Gary Stuart Tilbrook , Andreas Schumacher , René Emmenegger
发明人： Gary Stuart Tilbrook , Andreas Schumacher , René Emmenegger
IPC分类号： C07D487/04 , C07D213/40 , C07D401/04 , C07F9/6558
CPC分类号： C07D401/04 , C07D213/40 , C07D213/50 , C07D487/04 , C07F9/65586
摘要： The invention concerns a new process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]-propionic acid methyl ester or 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]propionic acid methyl ester benzene sulfonate (P) which comprises reacting 3-[(S)-7-bromo-2-((R and/or S)-2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]-propionic acid methyl ester of formula (EM) with an oxidizing agent and optionally treating the reaction product under acidic conditions, such as to produce the compound of formula (F) or the compound (P), and new compounds useful as starting material or as intermediate for performing that process.
摘要翻译：本发明涉及一种制备3 - [（4S）-8-溴-1-甲基-6-（2-吡啶基）-4H-咪唑并[1,2-a] [1,4]苯并二氮杂- 吡啶-3-基] - 丙酸甲酯或3 - [（4S）-8-溴-1-甲基-6-（2-吡啶基）-4H-咪唑并〔1,2-a〕〔1,4〕苯并二氮杂-4- 吡啶-2-基]丙酸甲酯苯磺酸盐（P），其包括使3 - [（S）-7-溴-2 - （（R和/或S）-2-羟基 - 丙基氨基） -3H-苯并[e] [1,4]二氮杂-3-基] - 丙酸甲酯与氧化剂反应，并在酸性条件下任选地处理反应产物，例如制备式（F）或化合物（P），以及可用作原料的新化合物或用于进行该方法的中间体。

8. 发明授权

US06448273B1 Orally active iron (III) chelators 有权
标题翻译：口服活性铁（III）螯合剂
公开(公告)号：US06448273B1
公开(公告)日：2002-09-10
申请号：US09451112
申请日：1999-11-30
申请人： Robert Charles Hider , Gary Stuart Tilbrook , Zudong Liu
发明人： Robert Charles Hider , Gary Stuart Tilbrook , Zudong Liu
IPC分类号： A61K314412
CPC分类号： C07D213/69 , C07D213/81 , C07D309/40 , C07D417/06 , C07D493/04
摘要： A compound of formula I wherein R is hydrogen or a group that is removed by metabolism in vivo to provide the free hydroxy compound, R1 is an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by a hydroxy group or a carboxylic acid ester, sulpho acid ester or a C1-6 alkoxy, C6-aryloxy or C7-10aralkoxy ether thereof, and R3 is selected from hydrogen and C1-6 alkyl; characterized in that R2 is selected from groups (i) —CONH—R5 (ii)—CR6R6OR7 (iii) —CONHCOR5 and (iv) —CON(CnH2n+1)2 R4 is selected from hydrogen, C1-6 alkyl and a group as described for R2; R5 is selected from hydrogen and optionally hydroxy, alkoxy, aryloxy or aralkoxy substituted C1-13 alkyl, aryl and C7-13 alkyl R6 is independently selected from hydrogen and C1-13 alkyl, R7 is selected from hydrogen, C1-13 alkyl, aryl and C7-13 aralkyl or a pharmaceutically acceptable salt of any such compound and CnH2n+1 is C1-6alkyl with the proviso that the compound is not one of 1-ethyl-2-(1′-hydroxyethyl)-3-hydroxypyridin-4-one and 1-methyl-2-hydroxymethyl-3-hydroxypyridoin-4-one.
摘要翻译：式I化合物，其中R是氢或通过体内代谢除去以提供游离羟基化合物的基团，R 1是脂族烃基或被羟基或羧酸酯取代的脂族烃基，磺酸酯或 C 1-6烷氧基，C 6芳氧基或C 7-10芳烷氧基醚，R 3选自氢和C 1-6烷基;其特征在于R 2选自（ⅰ）-CONH-R5（ⅱ）-CR6R6OR7（ⅲ） - CONHCOR 5和（iv）-CON（C n H 2n + 1）2 R 4选自氢，C 1-6烷基和如对R 2所述的基团; R 5选自氢和任选的羟基，烷氧基，芳氧基或芳烷氧基取代的C 1-13烷基，芳基和C7-13烷基R6独立地选自氢和C1-13烷基，R7选自氢，C1-13烷基，芳基和C7-13芳烷基或任何这样的化合物的药学上可接受的盐，C n H 2n + 1是C 1-6烷基，条件是该化合物不是1-乙基-2-（1'-羟乙基）-3-羟基吡啶-4中的一种 - 酮和1-甲基-2-羟甲基-3-羟基吡啶-4-酮。

9. 发明申请

US20120330007A1 PROCESS FOR PREPARING 3-[(4S)-8-BROMO-1-METHYL-6-(2-PYRIDINYL)-4H-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 有权
标题翻译：制备3 - [（4S）-8-溴-1-甲基-6-（2-吡啶基）-4H-咪唑并[1,2-A] [1,4]苯并噻吩-4-基]丙酸甲酯的方法 ESTER或其中的苯甲磺酸盐及其用途的化合物
公开(公告)号：US20120330007A1
公开(公告)日：2012-12-27
申请号：US13496742
申请日：2010-09-15
申请人： Gary Stuart Tilbrook , Andreas Schumacher , René Emmengger
发明人： Gary Stuart Tilbrook , Andreas Schumacher , René Emmengger
IPC分类号： C07D487/06 , C07D211/70
CPC分类号： C07D401/04 , C07D213/40 , C07D213/50 , C07D487/04 , C07F9/65586
摘要： The invention concerns a new process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]-propionic acid methyl ester or 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]propionic acid methyl ester benzene sulfonate (P) which comprises reacting 3-[(S)-7-bromo-2-((R and/or S)-2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]-propionic acid methyl ester of formula (EM) with an oxidizing agent and optionally treating the reaction product under acidic conditions, such as to produce the compound of formula (F) or the compound (P), and new compounds useful as starting material or as intermediate for performing that process.
摘要翻译：本发明涉及一种制备3 - [（4S）-8-溴-1-甲基-6-（2-吡啶基）-4H-咪唑并[1,2-a] [1,4]苯并二氮杂- 吡啶-3-基] - 丙酸甲酯或3 - [（4S）-8-溴-1-甲基-6-（2-吡啶基）-4H-咪唑并〔1,2-a〕〔1,4〕苯并二氮杂-4- 吡啶-2-基]丙酸甲酯苯磺酸盐（P），其包括使3 - [（S）-7-溴-2 - （（R和/或S）-2-羟基 - 丙基氨基） -3H-苯并[e] [1,4]二氮杂-3-基] - 丙酸甲酯与氧化剂反应，并在酸性条件下任选地处理反应产物，例如制备式（F）或化合物（P），以及可用作原料的新化合物或用于进行该方法的中间体。

10. 发明申请

US20100075955A1 SHORT-ACTING BENZODIAZEPINE SALTS AND THEIR POLYMORPHIC FORMS 有权
标题翻译：短效苯扎林盐及其多形态
公开(公告)号：US20100075955A1
公开(公告)日：2010-03-25
申请号：US12373457
申请日：2007-07-10
申请人： Gary Stuart Tilbrook , Louisa Jane Cubitt
发明人： Gary Stuart Tilbrook , Louisa Jane Cubitt
IPC分类号： A61K31/5517 , C07D487/04 , A61P25/00
CPC分类号： C07D401/04
摘要： The invention relates to esylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.
摘要翻译：本发明涉及式（I）化合物的盐酸盐：还描述了制备盐的方法及其作为药物的用途，特别是用于镇静或催眠，抗焦虑，肌肉松弛剂或抗惊厥剂的用途。

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