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公开(公告)号：US08227622B2
公开(公告)日：2012-07-24
申请号：US12830577
申请日：2010-07-06
申请人： Debra Ainge , Eric Merifield , Colin Thomson , Michael Butters , Ravi Ramakrishnan , Ravi Naidu Rayapati , Parhalad Ray Sharma
发明人： Debra Ainge , Eric Merifield , Colin Thomson , Michael Butters , Ravi Ramakrishnan , Ravi Naidu Rayapati , Parhalad Ray Sharma
IPC分类号： C07D209/30 , C07D209/12
CPC分类号： C07D209/40 , C07D209/30 , C07D209/32
摘要： The invention relates to compounds of formula (X), and salts thereof, and their use as intermediates in improved manufacturing processes for the synthesis of pharmaceutical compound (I): X is ═O, ═N—OH or ═N—OC(O)Me; Y is hydrogen, PhS- or p-chlorophenylsulfanyl; Z is hydrogen or —CH2COOR1 wherein R1 is selected from hydrogen, optionally substituted hydrocarbyl and optionally substituted heterocyclyl.
摘要翻译： 本发明涉及式（X）化合物及其盐，以及它们在制备药物化合物（I）的合成制造方法中作为中间体的用途：X是= O，= N-OH或= N-OC（O ）我; Y是氢，Ph-或对氯苯硫基; Z是氢或-CH 2 COOR 1，其中R 1选自氢，任选取代的烃基和任选取代的杂环基。
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公开(公告)号：US08034932B2
公开(公告)日：2011-10-11
申请号：US11793418
申请日：2005-12-22
IPC分类号： C07D239/36 , C07D239/42
CPC分类号： C07D239/36 , C07D239/42
摘要： A process for formation of a compound of formula (I) or a pharmaceutically acceptable salt thereof, (A chemical formula should be inserted here—please see paper copy enclosed herewith) I via a Heck reaction is described. Intermediates useful in the process and processes for making said intermediates are also described.
摘要翻译： 描述了通过Heck反应形成式（I）化合物或其药学上可接受的盐的方法（应在此插入化学式，请参见随附的I）。 还描述了用于制备所述中间体的方法和方法中的中间体。
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公开(公告)号：US20110046394A1
公开(公告)日：2011-02-24
申请号：US12830577
申请日：2010-07-06
申请人： Debra Ainge , Eric Merifield , Colin Thomson , Michael Butters , Ravi Ramakrishnan , Ravi Naidu Rayapati , Parhalad Ray Sharma
发明人： Debra Ainge , Eric Merifield , Colin Thomson , Michael Butters , Ravi Ramakrishnan , Ravi Naidu Rayapati , Parhalad Ray Sharma
IPC分类号： C07D209/30 , C07D209/24
CPC分类号： C07D209/40 , C07D209/30 , C07D209/32
摘要： The invention relates to compounds of formula (X), and salts thereof, and their use as intermediates in improved manufacturing processes for the synthesis of pharmaceutical compound (I): X is ═O, ═N—OH or ═N—OC(O)Me; Y is hydrogen, PhS- or p-chlorophenylsulfanyl; Z is hydrogen or —CH2COOR1 wherein R1 is selected from hydrogen, optionally substituted hydrocarbyl and optionally substituted heterocyclyl.
摘要翻译： 本发明涉及式（X）化合物及其盐，以及它们在制备药物化合物（I）的合成制造方法中作为中间体的用途：X是= O，= N-OH或= N-OC（O ）我; Y是氢，Ph-或对氯苯硫基; Z是氢或-CH 2 COOR 1，其中R 1选自氢，任选取代的烃基和任选取代的杂环基。
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公开(公告)号：US20090043097A1
公开(公告)日：2009-02-12
申请号：US12121228
申请日：2008-05-15
IPC分类号： C07D513/04
CPC分类号： C07D497/04 , C07D513/04
摘要： A method for the preparation of a compound of formula (1) or a pharmaceutically acceptable salt or solvate thereof; from a compound of the formula: (IV); wherein L represents a leaving group.
摘要翻译： 一种制备式（1）化合物或其药学上可接受的盐或溶剂合物的方法; 由式（IV）表示的化合物： 其中L表示离去基团。
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5.发明申请公开(公告)号：US20050272747A1
公开(公告)日：2005-12-08
申请号：US11120739
申请日：2005-05-02
申请人： Michael Butters , Alan Pettman
发明人： Michael Butters , Alan Pettman
IPC分类号： A61K31/506 , C07D43/02
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.
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公开(公告)号：US06645979B2
公开(公告)日：2003-11-11
申请号：US10005587
申请日：2001-10-29
申请人： Anne Bruckner , Michael Butters , Paul Vincent Fish , Michael Paul Fitzgerald , Julie Ann Macrae , Trevor Jack Newbury , Richard Anthony Storey
发明人： Anne Bruckner , Michael Butters , Paul Vincent Fish , Michael Paul Fitzgerald , Julie Ann Macrae , Trevor Jack Newbury , Richard Anthony Storey
IPC分类号： A01N4342
CPC分类号： C07D217/22
摘要： The invention described herein relates to a process for the preparation of (7-(3-carboxyphenyl)-4-chloroisoquinolin-1-yl)guanidine (I), intermediates thereto and new forms and formulations thereof, including the zwitterion monohydrate of (I), suitable for pharmaceutical use.
摘要翻译： 本文所述的本发明涉及制备（7-（3-羧基苯基）-4-氯异喹啉-1-基）胍（I）的方法，其中间体及其新形式和制剂，包括（I ），适合制药用途。
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公开(公告)号：US08076481B2
公开(公告)日：2011-12-13
申请号：US12705711
申请日：2010-02-15
申请人： Michael Butters , Jeffrey Crabb , Philip Hopes , Bharti Patel
发明人： Michael Butters , Jeffrey Crabb , Philip Hopes , Bharti Patel
IPC分类号： C07D241/02
CPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14
摘要： A process for preparing pharmaceutically active compounds of formula (I) or a salt thereof wherein R1, n, m, R3, R6, X1, X2, X3 and X4 are as defined in the specification, is described. Novel intermediates are also described and claimed.
摘要翻译： 描述了制备式（I）的药学活性化合物或其盐的方法，其中R 1，n，m，R 3，R 6，X 1，X 2，X 3和X 4如说明书中所定义。 新的中间体也被描述和要求保护。
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公开(公告)号：US20100210841A1
公开(公告)日：2010-08-19
申请号：US12705711
申请日：2010-02-15
申请人： Michael Butters , Jeffrey Crabb , Philip Hopes , Bharti Patel
发明人： Michael Butters , Jeffrey Crabb , Philip Hopes , Bharti Patel
IPC分类号： C07D403/06 , C07D403/14
CPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14
摘要： A process for preparing pharmaceutically active compounds of formula (I) or a salt thereof wherein R1, n, m, R3, R6, X1, X2, X3 and X4 are as defined in the specification, is described. Novel intermediates are also described and claimed.
摘要翻译： 描述了制备式（I）的药学活性化合物或其盐的方法，其中R 1，n，m，R 3，R 6，X 1，X 2，X 3和X 4如说明书中所定义。 新的中间体也被描述和要求保护。
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公开(公告)号：US20080207903A1
公开(公告)日：2008-08-28
申请号：US11793418
申请日：2005-12-22
IPC分类号： C07D239/24
CPC分类号： C07D239/36 , C07D239/42
摘要： A process for formation of a compound of formula (I) or a pharmaceutically acceptable salt thereof, (A chemical formula should be inserted here—please see paper copy enclosed herewith) I via a Heck reaction is described. Intermediates useful in the process and processes for making said intermediates are also described.
摘要翻译： 描述了通过Heck反应形成式（I）化合物或其药学上可接受的盐的方法（应在此插入化学式，请参见随附的I）。 还描述了用于制备所述中间体的方法和方法中的中间体。
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10.发明授权公开(公告)号：US07307174B2
公开(公告)日：2007-12-11
申请号：US10528612
申请日：2003-09-29
申请人： Michael Butters , Paul Schofield , Andrew Stocker
发明人： Michael Butters , Paul Schofield , Andrew Stocker
IPC分类号： C07D495/04
CPC分类号： C07D495/04 , C07D333/36 , Y02P20/55
摘要： Novel Process and Intermediates. A process for preparing a compound of formula (I) where R4 and R5 are as defined in the specification; and R6 is hydrogen or a protecting group, which process comprises cyclisation of a compound of formula (II) where R4 and R5 and R6 are as defined in relation to formula (I), and R7 is nitrogen protecting group, and removing the group R7, and thereafter if desired, removing any protecting group R6. Novel intermediates and the use of these in the formation of pharmaceutical compounds is also described and claimed
摘要翻译： 新工艺和中间体。 制备其中R 4和R 5的式（I）化合物的方法如说明书中所定义; 和R 6是氢或保护基，该方法包括式（II）化合物的环化，其中R 4和R 5和R 5和 R 6如关于式（I）所定义，R 7为氮保护基，除去基团R 7，和 此后如果需要，除去任何保护基团R 6。 还描述和要求保护新型中间体及其在药物化合物形成中的用途
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