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1. 发明授权

US06313312B1 3-Azabicyclo[3.1.0]hexane derivatives useful in therapy 失效
标题翻译：可用于治疗的3-氮杂双环[3.1.0]己烷衍生物
公开(公告)号：US06313312B1
公开(公告)日：2001-11-06
申请号：US09467871
申请日：1999-12-20
申请人： Bernard Joseph Banks , Robert James Crook , Stephen Paul Gibson , Graham Lunn , Alan John Pettman
发明人： Bernard Joseph Banks , Robert James Crook , Stephen Paul Gibson , Graham Lunn , Alan John Pettman
IPC分类号： C07D20952
CPC分类号： C07D401/04 , C07D209/52 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/06 , C07D409/06 , C07D409/10 , C07D413/12 , C07D417/06
摘要： Compounds of formula (I), their salts and prodrugs thereof, where the substituents are as defined herein are disclosed as opiate binding agents useful in the treatment of opiate-mediated conditions. Also described are processes for making such substances.
摘要翻译：公开了其中取代基如本文所定义的式（I）化合物及其盐和前药，其用作阿片剂结合剂，其用于治疗阿片剂介导的病症。还描述了制备这些物质的方法。

2. 发明授权

US07049444B2 3-azabicyclo[3.1.0]hexane derivatives useful in therapy 失效
公开(公告)号：US07049444B2
公开(公告)日：2006-05-23
申请号：US10214658
申请日：2002-08-07
申请人： Bernard Joseph Banks , Robert James Crook , Stephen Paul Gibson , Graham Lunn , Alan John Pettman
发明人： Bernard Joseph Banks , Robert James Crook , Stephen Paul Gibson , Graham Lunn , Alan John Pettman
IPC分类号： C07D209/52
CPC分类号： C07D401/04 , C07D209/52 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/06 , C07D409/06 , C07D409/10 , C07D413/12 , C07D417/06
摘要： Compounds of formula (I), their salts and prodrugs thereof, where the substituents are as defined herein are disclosed as opiate binding agents useful in the treatment of opiate-mediated conditions. Also described are processes for making such substances.

3. 发明授权

US06737430B2 Mutual prodrug of amlodipine and atorvastatin 失效
标题翻译：氨氯地平和阿托伐他汀的前药
公开(公告)号：US06737430B2
公开(公告)日：2004-05-18
申请号：US10000985
申请日：2001-10-31
申请人： Robert James Crook , Alan John Pettman
发明人： Robert James Crook , Alan John Pettman
IPC分类号： A61K314439
CPC分类号： C07D401/12 , A61K31/4422 , A61K31/4439 , A61K2300/00
摘要： The present invention relates to a mutual prodrug of amlodipine and atorvastatin, pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions thereof and the use of said prodrug and its salts in the manufacture of medicaments for the treatment of atherosclerosis, angina pectoris, combined hypertension and hyperlipidaemia and the management of cardiac risk.
摘要翻译：本发明涉及氨氯地平和阿托伐他汀的互用前药，其药学上可接受的酸加成盐，其药物组合物以及所述前药及其盐在制备用于治疗动脉粥样硬化，心绞痛，联合高血压和高脂血症的药物中的用途和心脏风险的管理。

4. 发明授权

US07026479B2 Process for the production of quinazolines 失效
标题翻译：喹唑啉生产工艺
公开(公告)号：US07026479B2
公开(公告)日：2006-04-11
申请号：US10199755
申请日：2002-07-19
申请人： Lee Terence Boulton , Robert James Crook , Alan John Pettman , Robert Walton
发明人： Lee Terence Boulton , Robert James Crook , Alan John Pettman , Robert Walton
IPC分类号： C07D239/70 , C07D237/02
CPC分类号： C07D401/04 , C07D213/57
摘要： The invention provides a process for the production of a compound of formula (A), or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, and R4 are as defined herein.
摘要翻译：本发明提供了制备式（A）化合物或其药学上可接受的盐或溶剂合物的方法，其中R 1，R 2，R 2， > 3 ，而R 4 4如本文所定义。

5. 发明申请

US20080193988A1 Process for the Preparation of Sulfonamide Derivatives 审中-公开
标题翻译：磺酰胺衍生物的制备方法
公开(公告)号：US20080193988A1
公开(公告)日：2008-08-14
申请号：US11995988
申请日：2006-07-10
申请人： Iain Robert Gladwell , Pieter David De Koning , Ian Brian Moses , Alan John Pettman , Nicholas Murray Thomson
发明人： Iain Robert Gladwell , Pieter David De Koning , Ian Brian Moses , Alan John Pettman , Nicholas Murray Thomson
IPC分类号： C12P7/62 , C07C319/00 , C07D303/08
CPC分类号： C07C311/48 , C07C51/367 , C07C237/20 , C07C303/40 , C07D303/36 , C07F7/1804 , C12P7/62 , Y02P20/55 , C07C59/42 , C07C311/08
摘要： The invention relates to a process for the preparation of compounds of formula (I) wherein Q1 is a group selected from formulae (II) & (III) and a group *-NR6-Q2-A or, if appropriate, their pharmaceutically acceptable salts and/or isomers, tautomers, solvates or isotopic variations thereof, as well as intermediates used in said process.
摘要翻译：本发明涉及式（I）化合物的制备方法，其中Q 1是选自式（II）和（III）和基团-NR 6的基团，或其合适的药学上可接受的盐和/或异构体，互变异构体，溶剂合物或同位素变体，以及所述方法中使用的中间体。

6. 发明申请

US20090306384A1 Process for the Production of Benzopyran-2-ol Derivatives 有权
标题翻译：苯并吡喃-2-醇衍生物的制备方法
公开(公告)号：US20090306384A1
公开(公告)日：2009-12-10
申请号：US12302228
申请日：2007-05-21
申请人： Jens Bertil Ahman , Barry Richard Dillon , Alan John Pettman
发明人： Jens Bertil Ahman , Barry Richard Dillon , Alan John Pettman
IPC分类号： C07D409/14 , C07D311/06 , C07C215/30 , C07C229/34
CPC分类号： C07D311/20 , C07C45/69 , C07C213/02 , C07D311/58 , C07C47/27 , C07C215/54 , C07C219/28
摘要： The invention provides a process for producing a compound of formula (I), wherein Y is selected from the group consisting of CH3, CH2OH, CH2CH2OH, CH2Br and Br; comprising the steps of: (i) reacting a compound of formula (II), wherein OX represents hydroxy or O−M+, in which M+ is a cation selected from Li+, Na+ and K+, and Y is as defined above; with trans-cinnamaldehyde (III), in the presence of a secondary amine compound; then (ii) treating the product of the preceding step with acid to afford the compound of formula (I). The above process may also be used in the production of tolterodine and fesoterodine, which are useful in the treatment of overactive bladder.
摘要翻译：本发明提供了制备式（I）化合物的方法，其中Y选自CH 3，CH 2 OH，CH 2 CH 2 OH，CH 2 Br和Br; 包括以下步骤：（i）使式（II）化合物其中OX表示羟基或O-M +，其中M +是选自Li +，Na +和K +的阳离子，Y如上定义; 在仲胺化合物的存在下反式肉桂醛（III）; 然后（ii）用酸处理前述步骤的产物，得到式（I）化合物。上述方法也可用于生产托特罗定和非索罗定，其可用于治疗膀胱过动症。

7. 发明授权

US06586594B1 Preparation of triazoles by organometallic addition to ketones and intermediates therefor 失效
标题翻译：通过有机金属加成酮和其中间体制备三唑
公开(公告)号：US06586594B1
公开(公告)日：2003-07-01
申请号：US09011346
申请日：1998-02-04
申请人： Michael Butters , Alan John Pettman , Julie Ann Harrison
发明人： Michael Butters , Alan John Pettman , Julie Ann Harrison
IPC分类号： C07D40310
CPC分类号： C07D239/30 , C07D239/34 , C07D239/36 , C07D403/06
摘要： A process for the preparation of a compound of the formula: or an acid addition or base salt thereof, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and trifluoromethyl; R1 is C1-C6 alkyl; and “Het” is pyrimidinyl optionally substituted by 1 to 3 substituents each independently selected from C1-C4 alkyl, C1-C4 alkoxy, halo, oxo, benzyl and benzyloxy, comprising reacting a compound of the formula: with a compound of the formula wherein X is chloro, bromo or iodo, the reaction taking place in the presence of zinc; at least one of iodine or a Lewis acid; and an aprotic organic solvent: optionally further reacting the resulting compound with an acid or base to form the corresponding acid addition or base salt thereof.
摘要翻译：一种制备下式化合物或其酸加成盐或碱盐的方法，其中R为任选被1-3个各自独立地选自卤素和三氟甲基的取代基取代的苯基; R1是C1-C6烷基; 和“Het”是任选被1至3个独立地选自C 1 -C 4烷基，C 1 -C 4烷氧基，卤素，氧代，苄基和苄氧基的取代基取代的嘧啶基，包括使下式化合物与式是氯，溴或碘，反应发生在锌的存在下; 碘或路易斯酸中的至少一种; 和非质子有机溶剂：任选地使所得化合物与酸或碱进一步反应以形成相应的酸加成盐或碱盐。

8. 发明授权

US08067594B2 Process for the production of benzopyran-2-ol derivatives 有权
标题翻译：苯并吡喃-2-醇衍生物的制备方法
公开(公告)号：US08067594B2
公开(公告)日：2011-11-29
申请号：US12302228
申请日：2007-05-21
申请人： Jens Bertil Ahman , Barry Richard Dillon , Alan John Pettman
发明人： Jens Bertil Ahman , Barry Richard Dillon , Alan John Pettman
IPC分类号： C07D311/20 , C07D311/58 , C07C215/54 , C07C213/02 , C07C219/28
CPC分类号： C07D311/20 , C07C45/69 , C07C213/02 , C07D311/58 , C07C47/27 , C07C215/54 , C07C219/28
摘要： The invention provides a process for producing a compound of formula (I), wherein Y is selected from the group consisting of CH3, CH2OH, CH2CH2OH, CH2Br and Br; comprising the steps of: (i) reacting a compound of formula (II), wherein OX represents hydroxy or O−M+, in which M+ is a cation selected from Li+, Na+ and K+, and Y is as defined above; with trans-cinnamaldehyde (III), in the presence of a secondary amine compound; then (ii) treating the product of the preceding step with acid to afford the compound of formula (I). The above process may also be used in the production of tolterodine and fesoterodine, which are useful in the treatment of overactive bladder.
摘要翻译：本发明提供了制备式（I）化合物的方法，其中Y选自CH 3，CH 2 OH，CH 2 CH 2 OH，CH 2 Br和Br; 包括以下步骤：（i）使式（II）化合物其中OX表示羟基或O-M +，其中M +是选自Li +，Na +和K +的阳离子，Y如上定义; 在仲胺化合物的存在下反式肉桂醛（III）; 然后（ii）用酸处理前述步骤的产物，得到式（I）化合物。上述方法也可用于生产托特罗定和非索罗定，其可用于治疗膀胱过动症。

9. 发明授权

US07193083B2 Preparation of triazoles by organometallic addition to ketones and intermediates therefor 失效
标题翻译：通过有机金属加成酮和其中间体制备三唑
公开(公告)号：US07193083B2
公开(公告)日：2007-03-20
申请号：US11120739
申请日：2005-05-02
申请人： Michael Butters , Alan John Pettman
发明人： Michael Butters , Alan John Pettman
IPC分类号： C07D403/10
CPC分类号： C07D403/06
摘要： The invention provides a process for the preparation of a compound of the formula: or an acid addition or base salt thereof, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and trifluoromethyl; R1 is C1–C6 alkyl; and “Het” is pyrimidinyl optionally substituted by 1 to 3 substituents each independently selected from C1–C4 alkyl, C1–C4 alkoxy, halo, oxo, benzyl and benzyloxy, comprising reaction of a compound of the formula: wherein R is as previously defined for a compound of the formula (I), with a compound of the formula: wherein R1 and “Het” are as previously defined for a compound of the formula (I) and X is chloro, bromo or iodo, in the presence of zinc, iodine and/or a Lewis acid and an aprotic organic solvent: said process being optionally followed by conversion of the compound of the formula (I) to an acid addition or base salt thereof.
摘要翻译：本发明提供了一种制备下式化合物或其酸加成盐或碱盐的方法，其中R是任选被1-3个各自独立地选自卤素和三氟甲基的取代基取代的苯基; R 1是C 1 -C 6烷基; R 1是C 1 -C 6烷基; “Het”是任选被1至3个独立地选自C 1 -C 4烷基，C 1 -C 3烷基的取代基取代的嘧啶基，包括下式化合物与式（I）化合物反应：其中R如前面定义的式（I）化合物与下式化合物反应：其中 R 1和/或Het如先前对于式（I）化合物所定义，X是氯，溴或碘，在锌，碘和/或路易斯酸和非质子有机溶剂：所述方法任选地随后将式（I）化合物转化为其酸加成盐或碱盐。

10. 发明授权

US07018818B2 Intermediates in the preparation of therapeutic fused bicyclic amino acids 失效
标题翻译：中间体制备治疗性融合双环氨基酸
公开(公告)号：US07018818B2
公开(公告)日：2006-03-28
申请号：US10677836
申请日：2003-10-02
申请人： Iain Robert Gladwell , Alan John Pettman
发明人： Iain Robert Gladwell , Alan John Pettman
IPC分类号： C12P7/44 , C12P7/62 , C07C57/26
CPC分类号： C07C69/608 , C07B2200/07 , C07C51/353 , C07C53/136 , C07C57/26 , C07C67/343 , C07C2602/20 , Y02P20/55
摘要： The invention presents compounds of formula (I), where R represents H or a suitable carboxylic acid protecting group, which are intermediates in the preparation of therapeutic fused bicyclic amino acids.
摘要翻译：本发明提供式（I）化合物，其中R表示H或合适的羧酸保护基，其是制备治疗性稠合双环氨基酸的中间体。

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