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1. 发明申请

WO2010139967A8 DIHYDROINDOLE AND TETRAHYDROISOQUINOLINE DERIVATIVES USEFUL AS POTASSIUM CHANNEL INHIBITORS 审中-公开
标题翻译：用作钾通道抑制剂的二氢吲哚和四氢喹啉衍生物
公开(公告)号：WO2010139967A8
公开(公告)日：2011-12-22
申请号：PCT/GB2010001123
申请日：2010-06-04
申请人： XENTION LTD , HAMLYN RICHARD JOHN , MADGE DAVID , MULLA MUSHTAQ , HARTZOULAKIS BASIL , JONES SIMON MARK , JOHN DEREK EDWARD
发明人： HAMLYN RICHARD JOHN , MADGE DAVID , MULLA MUSHTAQ , HARTZOULAKIS BASIL , JONES SIMON MARK , JOHN DEREK EDWARD
IPC分类号： C07D401/12 , A61K31/4155 , A61K31/4178 , A61K31/47 , A61P9/00 , A61P17/00 , C07D403/12
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 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 hydrogen, 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 and R6 for each occurrence is optionally substituted alkyl; R7 and R8 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 = 0, 1, 2 or 3; o = 0, 1 or 2 with the proviso that when o = 0, n is 1, 2 or 3 and when o = 1, 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独立地选自由CH 2，CH（R 5）或C（R 5）（R 6）组成的组。 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; R 3选自氢，卤素，羟基，烷氧基，芳氧基，任选取代的烷基，任选取代的氨基，任选取代的氨基磺酰基或腈; R 4选自氢，任选取代的烷基，任选取代的环烷基，任选取代的杂环烷基，任选取代的酰基，任选取代的磺酰基，任选取代的氨磺酰基，任选取代的芳基，任选取代的芳烷基和任选取代的杂芳基; R5和R6每次出现是任选取代的烷基; R 7和R 8相同或不同，各自表示氢，任选取代的烷基，任选取代的环烷基，任选取代的芳烷基，任选取代的芳基或任选取代的杂芳基; 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。

2. 发明申请

WO0128537A3 BISSULFONAMIDE DERIVATIVES AS ENZYME INHIBITORS 审中-公开
标题翻译：双酚A衍生物作为酶抑制剂
公开(公告)号：WO0128537A3
公开(公告)日：2001-06-14
申请号：PCT/GB0003944
申请日：2000-10-13
申请人： ARROW THERAPEUTICS LTD , MADGE DAVID , WISHART GRANT , DOLMAN MARK , MAUNDER PETER
发明人： MADGE DAVID , WISHART GRANT , DOLMAN MARK , MAUNDER PETER
IPC分类号： C07D239/74 , A01N41/06 , A61K31/145 , A61K31/18 , A61K31/381 , A61K31/422 , A61K31/425 , A61K31/426 , A61K31/4436 , A61K31/517 , A61L2/18 , A61P31/04 , A61P31/10 , A61P33/06 , A61P43/00 , C07C311/13 , C07C311/21 , C07C311/29 , C07C311/46 , C07C317/14 , C07D333/34 , C07D409/04 , C07D413/04 , C07D417/04
CPC分类号： A61K31/18 , C07C311/13 , C07C311/21 , C07C311/29 , C07C311/46 , C07C317/14
摘要： Bissulfonamide derivatives of formula (I) are capable of inhibiting: a) the biosynthesis of aromatic amino acids via the shikimate pathway and b) the catabolism of quinic acid, wherein: Ar is an aryl or heteroaryl group; R1 and R2 are the same or different and each represent hydrogen or alkyl or R1 and R2 together form a C1-C3 alkylene group, -CO- or -CS-; and R3 and R4 are the same or different and each represent -alkyl-aryl, -alkyl-heteroaryl, -alkenyl-aryl, -alkenyl-heteroaryl, -alkynyl-aryl-alkynyl-heterorayl, aryl or heteroaryl.
摘要翻译：式（I）的双磺酰胺衍生物能够抑制：a）通过莽草酸通路生物合成芳族氨基酸，和b）奎尼酸的分解代谢，其中：Ar是芳基或杂芳基; R 1和R 2相同或不同，各自表示氢或烷基，或者R 1和R 2一起形成C 1 -C 3亚烷基-CO-或-CS-; 并且R 3和R 4相同或不同，并且各自表示 - 烷基 - 芳基， - 烷基 - 杂芳基 - - 烯基 - 芳基， - 烯基 - 杂芳基 - - 炔基 - 芳基 - 炔基 - 杂芳基，芳基或杂芳基。

3. 发明专利

AU2012338570A1 Thieno- and furo - pyrimidines and pyridines, useful as potassium channel inhibitors 未知
公开(公告)号：AU2012338570A1
公开(公告)日：2014-07-03
申请号：AU2012338570
申请日：2012-11-15
申请人： XENTION LTD
发明人： MADGE DAVID , CHAN FIONA , JOHN DEREK EDWARD , EDWARDS SIMON D , BLUNT RICHARD , HARTZOULAKIS BASIL , BROWN LINDSAY
IPC分类号： C07D491/048 , A61K31/4365 , A61K31/519 , A61P9/06 , C07D495/04
摘要： The present invention provides compounds of formula (I): (Formula (I); wherein A, R

4. 发明专利

CA2855346A1 THIENO- AND FURO - PYRIMIDINES AND PYRIDINES, USEFUL AS POTASSIUM CHANNEL INHIBITORS 未知
公开(公告)号：CA2855346A1
公开(公告)日：2013-05-23
申请号：CA2855346
申请日：2012-11-15
申请人： XENTION LTD
发明人： MADGE DAVID , CHAN FIONA , JOHN DEREK EDWARD , EDWARDS SIMON D , BLUNT RICHARD , HARTZOULAKIS BASIL , BROWN LINDSAY
IPC分类号： C07D491/048 , A61K31/4365 , A61K31/519 , A61P9/06 , C07D495/04
摘要： The present invention provides compounds of formula (I): (Formula (I); wherein A, R1, R2, R3 I, V, X, and Z are defined herein, which are potassium channel inhibitors. The invention further provides pharmaceutical compositions comprising the compounds of formula (I) and their use in therapy, in particular in treatment of diseases or conditions that are mediated by Kir3.1 and/or Kir3.4 or any heteromultimers thereof, or that require inhibition of Kir3.1 and/or Kir3.4 or any heteromultimers thereof.

5. 发明专利

ZA201403503B THIENO- AND FURO - PYRIMIDINES AND PYRIDINES, USEFUL AS POTASSIUM CHANNEL INHIBITORS 未知
公开(公告)号：ZA201403503B
公开(公告)日：2016-09-28
申请号：ZA201403503
申请日：2014-05-14
申请人： XENTION LTD
发明人： HARTZOULAKIS BASIL , EDWARDS SIMON D , CHAN FIONA , BROWN LINDSAY , BLUNT RICHARD , JOHN DEREK EDWARD , MADGE DAVID

6. 发明专利

IN1183MUN2014A THIENO AND FURO PYRIMIDINES AND PYRIDINES USEFUL AS POTASSIUM CHANNEL INHIBITORS 未知
公开(公告)号：IN1183MUN2014A
公开(公告)日：2015-07-03
申请号：IN1183MUN2014
申请日：2014-06-12
申请人： XENTION LTD
发明人： MADGE DAVID , CHAN FIONA , JOHN DEREK EDWARD , EDWARDS SIMON D , BLUNT RICHARD , HARTZOULAKIS BASIL , BROWN LINDSAY
IPC分类号： C07D491/048 , A61K31/519 , C07D495/04
摘要： The present invention provides compounds of formula (I): (Formula (I); wherein A R R R V X and Z are defined herein which are potassium channel inhibitors. The invention further provides pharmaceutical compositions comprising the compounds of formula (I) and their use in therapy in particular in treatment of diseases or conditions that are mediated by K3.1 and/or K3.4 or any heteromultimers thereof or that require inhibition of K3.1 and/or K3.4 or any heteromultimers thereof.

7. 发明专利

NZ626199A Thieno- and furo - pyrimidines and pyridines, useful as potassium channel inhibitors 未知
公开(公告)号：NZ626199A
公开(公告)日：2015-04-24
申请号：NZ62619912
申请日：2012-11-15
申请人： XENTION LTD
发明人： MADGE DAVID , CHAN FIONA , JOHN DEREK EDWARD , EDWARDS SIMON D , BLUNT RICHARD , HARTZOULAKIS BASIL , BROWN LINDSAY
IPC分类号： C07D491/048 , A61K31/4365 , A61K31/519 , A61P9/06 , C07D495/04
摘要： Disclosed herein are thieno and furo pyridine and pyrimidine compounds of formula (I) wherein R3 is N(RaRb)J where Ra and Rb form a ring with the nitrogen to which they are attached and the remainder of the substituents are as are defined herein. The compounds are potassium channel inhibitors intended for use in treatment of diseases or conditions that are mediated by KI3.1 and/or Kir3.4 or any heteromultimers thereof, or that require inhibition of Kir3.1 and/or Kir3.4 or any heteromultimers thereof such as cardiovascular diseases. Also disclosed are pharmaceutical compositions comprising the compounds of formula (I).

8. 发明专利

MX2014005935A TIENO- Y FURO-PIRIMIDINAS Y PIRIDINAS, UTILES COMO INHIBIDORES DEL CANAL DE POTASIO. 未知
公开(公告)号：MX2014005935A
公开(公告)日：2014-09-04
申请号：MX2014005935
申请日：2012-11-15
申请人： XENTION LTD
发明人： HARTZOULAKIS BASIL , JOHN DEREK EDWARD , MADGE DAVID , CHAN FIONA , EDWARDS SIMON D , BLUNT RICHARD , BROWN LINDSAY
IPC分类号： C07D491/048 , A61K31/4365 , A61K31/519 , A61P9/06 , C07D495/04
摘要： Compuestos de fórmula (I): (ver Fórmula) donde A, R1, R2, R3I, V, X y Z son como se los define en la presente, que son inhibidores de los canales de potasio. Composiciones farmacéuticas que comprenden compuestos de fórmula (I). Su uso en la terapia, particularmente en el tratamiento de enfermedades o afecciones que son mediadas por Kir3.1, por Kir3.4 y/o por cualquier heteromultímero de éstos, o bien de enfermedades o afecciones que pueden combatirse a través de la inhibición de Kir3.1, de Kir3.4 y/o de cualquier heteromultímero de éstos.

9. 发明专利

AT542824T 未知
公开(公告)号：AT542824T
公开(公告)日：2012-02-15
申请号：AT06820463
申请日：2006-12-08
申请人： XENTION LTD
发明人： FORD JOHN , MADGE DAVID , PAYNE HELEN , KNIGHT JAMIE
IPC分类号： C07D495/04 , A61K31/38

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