公开(公告)号：US08258138B2

公开(公告)日：2012-09-04

申请号：US12550805

申请日：2009-08-31

申请人： Derek Edward John ,  Mushtaq Mulla ,  Richard John Hamlyn ,  Simon Mark Jones ,  Derek Roland Pollard ,  Basil Hartzoulakis ,  Helen Payne ,  David Madge ,  John Ford

发明人： Derek Edward John ,  Mushtaq Mulla ,  Richard John Hamlyn ,  Simon Mark Jones ,  Derek Roland Pollard ,  Basil Hartzoulakis ,  Helen Payne ,  David Madge ,  John Ford

IPC分类号： A61K31/41 ,  C07D207/00

CPC分类号： C07D295/18 ,  C07D207/12 ,  C07D211/10 ,  C07D211/16 ,  C07D211/22 ,  C07D211/48 ,  C07D211/52 ,  C07D217/20 ,  C07D231/18 ,  C07D233/84 ,  C07D241/04 ,  C07D265/30 ,  C07D277/36 ,  C07D307/64 ,  C07D311/58 ,  C07D333/34

摘要： The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives wherein R1, R2, R3, X1, and A are defined herein. The compounds are useful as potassium ion channel inhibitors.

摘要翻译： 本发明提供式（I）化合物或其盐或药学上可接受的衍生物，其中R 1，R 2，R 3，X 1和A如本文所定义。 该化合物可用作钾离子通道抑制剂。

公开(公告)号：US08372840B2

公开(公告)日：2013-02-12

申请号：US12550830

申请日：2009-08-31

申请人： Richard John Hamlyn ,  Mushtaq Mulla ,  Derek Edward John ,  Simon Mark Jones ,  Basil Hartzoulakis ,  David Madge ,  John Ford

发明人： Richard John Hamlyn ,  Mushtaq Mulla ,  Derek Edward John ,  Simon Mark Jones ,  Basil Hartzoulakis ,  David Madge ,  John Ford

IPC分类号： A61K31/41 ,  C07D207/00

CPC分类号： C07C311/21 ,  C07D207/27 ,  C07D213/71 ,  C07D231/18 ,  C07D233/84 ,  C07D233/90 ,  C07D295/135 ,  C07D403/12 ,  C07D413/12

摘要： The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof, wherein R1, R2, R3, R4, R5, X1, and j are defined herein. The compounds are useful as potassium ion channel inhibitors.

摘要翻译： 本发明提供式（I）化合物或其盐或药学上可接受的衍生物，其中R1，R2，R3，R4，R5，X1和j如本文所定义。 该化合物可用作钾离子通道抑制剂。

公开(公告)号：US20100087438A1

公开(公告)日：2010-04-08

申请号：US12550830

申请日：2009-08-31

申请人： Richard John HAMLYN ,  Mushtaq Mulla ,  Derek Edward John ,  Simon Mark Jones ,  Basil Hartzoulakis ,  David Madge ,  John Ford

发明人： Richard John HAMLYN ,  Mushtaq Mulla ,  Derek Edward John ,  Simon Mark Jones ,  Basil Hartzoulakis ,  David Madge ,  John Ford

IPC分类号： A61K31/4166 ,  C07D233/54 ,  C07D265/30 ,  A61K31/5375 ,  A61P9/06 ,  A61P37/00

CPC分类号： C07C311/21 ,  C07D207/27 ,  C07D213/71 ,  C07D231/18 ,  C07D233/84 ,  C07D233/90 ,  C07D295/135 ,  C07D403/12 ,  C07D413/12

摘要： The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof, wherein R1, R2, R3, R4, R5, X1, and j are defined herein. The compounds are useful as potassium ion channel inhibitors.

摘要翻译： 本发明提供式（I）化合物或其盐或药学上可接受的衍生物，其中R1，R2，R3，R4，R5，X1和j如本文所定义。 该化合物可用作钾离子通道抑制剂。

公开(公告)号：US08399481B2

公开(公告)日：2013-03-19

申请号：US12794493

申请日：2010-06-04

申请人： Richard John Hamlyn ,  David Madge ,  Mushtaq Mulla ,  Basil Hartzoulakis ,  Simon Mark Jones ,  Derek Edward John ,  Oliver Gareth Dugdale

发明人： Richard John Hamlyn ,  David Madge ,  Mushtaq Mulla ,  Basil Hartzoulakis ,  Simon Mark Jones ,  Derek Edward John ,  Oliver Gareth Dugdale

IPC分类号： C07D217/24 ,  A61K31/4725

CPC分类号： C07D209/46 ,  C07D217/24 ,  C07D401/12 ,  C07D403/12

摘要： A compound of formula (I) Or its salts or pharmaceutically acceptable derivatives thereof wherein; A represents a chemical moiety with the general formula (II): X is selected from a group consisting of CH2, C(═O), CH(R5), C(R5)(R6) or C(R5)(R6)CH2; R1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl; R2 is selected from the group consisting of optionally substituted aryl or optionally substituted heteroaryl or NR7R8; R3 R4 R5 R6 R7 and R8 are as defined herein; and n=1 or 2 is provided. Pharmaceutical compositions comprising the compounds are also provided. The compounds are useful in treating various conditions including arrhythmia.

摘要翻译： 式（I）化合物或其盐或药学上可接受的衍生物，其中： A表示具有通式（II）的化学部分：X选自CH 2，C（= O），CH（R 5），C（R 5）（R 6）或C（R 5）（R 6）CH 2 ; R 1选自任选取代的芳基烷基和任选取代的杂芳基烷基; R 2选自任选取代的芳基或任选取代的杂芳基或NR 7 R 8; R3 R4 R5 R6 R7和R8如本文所定义; 并且提供n = 1或2。 还提供了包含该化合物的药物组合物。 该化合物可用于治疗各种病症，包括心律失常。

公开(公告)号：US08426442B2

公开(公告)日：2013-04-23

申请号：US12794499

申请日：2010-06-04

申请人： Richard John Hamlyn ,  Mushtaq Mulla ,  David Madge ,  Basil Hartzoulakis ,  Simon Mark Jones ,  Derek Edward John ,  Oliver Gareth Dugdale

发明人： Richard John Hamlyn ,  Mushtaq Mulla ,  David Madge ,  Basil Hartzoulakis ,  Simon Mark Jones ,  Derek Edward John ,  Oliver Gareth Dugdale

IPC分类号： C07D401/12 ,  A61K31/47

CPC分类号： C07D401/12 ,  C07D403/12

摘要： A compound of formula (I): Or its salts or pharmaceutically acceptable derivatives thereof wherein: A represents a chemical moiety with the general formula (II): X and Y are independently selected from a group consisting of CH2, CH(R5) or C(R5)(R6); R1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl; R2 is selected from the group consisting of optionally substituted aryl or optionally substituted heteroaryl or NR7R8; R3 R4 R5 R6 R7 and R8 are as defined herein, n=0, 1, 2 or 3; o=0, 1 or 2, with the proviso that when o=0, then n is 1, 2 or 3 and when o=1, then n is 1 or 2 is provided. Pharmaceutical compositions comprising the compounds are also provided. These compounds are useful in the treatment of various disorders including arrhythmia.

摘要翻译： 式（I）化合物或其盐或其药学上可接受的衍生物其中：A表示具有通式（II）的化学部分：X和Y独立地选自CH 2，CH（R 5）或C （R5）（R6）; R 1选自任选取代的芳基烷基和任选取代的杂芳基烷基; R 2选自任选取代的芳基或任选取代的杂芳基或NR 7 R 8; R3 R4 R5 R6 R7和R8如本文所定义，n = 0,1,2或3; o = 0,1或2，条件是当o = 0时，n为1,2或3，当o = 1时，n为1或2。 还提供了包含该化合物的药物组合物。 这些化合物可用于治疗各种疾病，包括心律失常。

公开(公告)号：US20100087428A1

公开(公告)日：2010-04-08

申请号：US12550860

申请日：2009-08-31

申请人： Mushtaq Mulla ,  Derek Edward John ,  Richard John Hamlyn ,  Sasha Louise Garrett ,  Basil Hartzoulakis ,  David Madge ,  John Ford

发明人： Mushtaq Mulla ,  Derek Edward John ,  Richard John Hamlyn ,  Sasha Louise Garrett ,  Basil Hartzoulakis ,  David Madge ,  John Ford

IPC分类号： A61K31/415 ,  C07D231/04 ,  C07D233/66 ,  C07D213/62 ,  C07D265/36 ,  A61K31/4164 ,  A61K31/44 ,  A61K31/538 ,  A61P19/02 ,  A61P17/06 ,  A61P37/00

CPC分类号： C07C311/21 ,  C07C311/46 ,  C07C317/32 ,  C07C317/40 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D207/12 ,  C07D209/08 ,  C07D211/16 ,  C07D211/34 ,  C07D211/44 ,  C07D213/36 ,  C07D213/40 ,  C07D213/71 ,  C07D231/12 ,  C07D231/18 ,  C07D231/56 ,  C07D233/61 ,  C07D233/64 ,  C07D233/84 ,  C07D265/30 ,  C07D265/36 ,  C07D271/08 ,  C07D277/28 ,  C07D277/36 ,  C07D277/46 ,  C07D285/12 ,  C07D285/135 ,  C07D307/79 ,  C07D311/70 ,  C07D317/62 ,  C07D319/18 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

摘要： The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein; X1 is selected from a group consisting of CH2, C(═O), C(═NH), NC(═O), R1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl R2 is selected from the group consisting of optionally substituted alkyl, optionally substituted aryl or heteroaryl or NR24R25 R3 is selected from the group consisting of hydrogen, halogen, hydroxyl, alkoxy, aryloxy, optionally substituted alkyl, optionally substituted amino, optionally substituted amino sulfonyl or nitrile; R4 is selected from the group consisting of optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted acyl, optionally substituted sulfonyl, optionally substituted sulfamoyl, optionally substituted aryl, optionally substituted arylalkyl, and optionally substituted heteroaryl R5 may be hydrogen, an optionally substituted alkyl, preferably CH3 or, NR4R5 may form an optionally substituted saturated or partially saturated 4-7 membered ring with the general formula (II). Wherein; X2 is C(═O), CH2, CH(R6) or C(R6)(R6), X3 is CH2, CH(R7), C(R7)(R7), NH, N(R8), O or S Each R6 independently represents optionally substituted amino, optionally substituted amino carbonyl, hydroxyl, optionally substituted acyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalky, optionally substituted aryl or optionally substituted heteroaryl; Each R7 independently represents optionally substituted amino, optionally substituted amino carbonyl, hydroxyl, optionally substituted acyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalky, optionally substituted aryl or optionally substituted hetero aryl R8 is optionally substituted acyl, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl; R24 and R25 are the same or different and each represents hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl, n=1 or 2 m=1, 2 or 3 With the proviso that when X1 is C═O and R5 is H then R4 is not: Or Or Where R4a, R5a and R6a are each independently H, C1-6alkyl, aryl, heteroaryl, cycloalkyl, or aryl-C1-6alkyl; R10a is H or C1-6alkyl; and R11a is C1-6alkyl or aryl-C1-6alkyl and when X1 is C═O or CH2 and R5 is H then R4 is not: Where q is 0 to 5, R3b is H, OH or alkoxy and R4b is NH2, phenyl or a C3-10 heterocycle. The compounds are useful as potassium ion channel inhibitors.

公开(公告)号：US08673901B2

公开(公告)日：2014-03-18

申请号：US12550860

申请日：2009-08-31

申请人： Mushtaq Mulla ,  Derek Edward John ,  Richard John Hamlyn ,  Sasha Louise Garrett ,  Basil Hartzoulakis ,  David Madge ,  John Ford

发明人： Mushtaq Mulla ,  Derek Edward John ,  Richard John Hamlyn ,  Sasha Louise Garrett ,  Basil Hartzoulakis ,  David Madge ,  John Ford

IPC分类号： C07C311/21 ,  C07D205/04 ,  C07D211/08 ,  A61K31/18

CPC分类号： C07C311/21 ,  C07C311/46 ,  C07C317/32 ,  C07C317/40 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D207/12 ,  C07D209/08 ,  C07D211/16 ,  C07D211/34 ,  C07D211/44 ,  C07D213/36 ,  C07D213/40 ,  C07D213/71 ,  C07D231/12 ,  C07D231/18 ,  C07D231/56 ,  C07D233/61 ,  C07D233/64 ,  C07D233/84 ,  C07D265/30 ,  C07D265/36 ,  C07D271/08 ,  C07D277/28 ,  C07D277/36 ,  C07D277/46 ,  C07D285/12 ,  C07D285/135 ,  C07D307/79 ,  C07D311/70 ,  C07D317/62 ,  C07D319/18 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

摘要： The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein X1, R1, R2, R3, R4, and R5 are defined as set forth in the specification. The compounds are useful as potassium ion channel inhibitors.

摘要翻译： 本发明提供式（I）化合物或其盐或其药学上可接受的衍生物，其中X1，R1，R2，R3，R4和R5如说明书所述定义。 该化合物可用作钾离子通道抑制剂。

公开(公告)号：US20140206703A1

公开(公告)日：2014-07-24

申请号：US14008776

申请日：2012-03-29

申请人： John Ford ,  Derek Edward John

发明人： John Ford ,  Derek Edward John

IPC分类号： C07D495/04

CPC分类号： C07D495/04

摘要： The present invention relates to thienopyrimidine compounds which are potassium channel inhibitors. Pharmaceutical compositions comprising the compounds and their use in the treatment of arrhythmia are also described.

摘要翻译： 本发明涉及作为钾通道抑制剂的噻吩并嘧啶化合物。 还描述了包含该化合物的药物组合物及其在治疗心律失常中的用途。

公开(公告)号：US09249155B2

公开(公告)日：2016-02-02

申请号：US14008776

申请日：2012-03-29

申请人： John Ford ,  Derek Edward John

发明人： John Ford ,  Derek Edward John

IPC分类号： C07D495/04

CPC分类号： C07D495/04

摘要： The present invention relates to thienopyrimidine compounds which are potassium channel inhibitors. Pharmaceutical compositions comprising the compounds and their use in the treatment of arrhythmia are also described.

摘要翻译： 本发明涉及作为钾通道抑制剂的噻吩并嘧啶化合物。 还描述了包含该化合物的药物组合物及其在治疗心律失常中的用途。