公开(公告)号：US20060223800A1

公开(公告)日：2006-10-05

申请号：US11422338

申请日：2006-06-06

申请人： Stephen Garland ,  David Haigh ,  Deidre Mary Hickey ,  John Liddle ,  David Smith ,  Robert Ward ,  Jason Witherington

发明人： Stephen Garland ,  David Haigh ,  Deidre Mary Hickey ,  John Liddle ,  David Smith ,  Robert Ward ,  Jason Witherington

IPC分类号： A61K31/5377 ,  A61K31/496 ,  A61K31/4745 ,  C07D471/02

CPC分类号： C07D471/04 ,  C07D213/85 ,  C07D487/04

摘要： The present invention includes compound of formula (I), or a derivative thereof wherein Y is CH or N; R1 is unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted cycloalkenyl, unsubstituted or substituted aryl, aralkyl wherein the aryl and the alkyl moieties may each independently be unsubstituted or substituted, aralkenyl wherein the aryl, and alkenyl moieties may each independently be unsubstituted or substituted, unsubstituted or substituted heterocyclyl, or heterocyclylalkyl wherein the heterocyclcyl and the alkyl moieties may each inedepently be unsubstituted or substituted; and R2 is unsubstituted aryl or unsubstituted or substituted or substituted heteroaryl. Additionally the present invention inlcudes a process for preparing such a compound, a pharmaceutical composition containing such a compound, and the use of such a compound in medicine.

摘要翻译： 本发明包括式（I）化合物或其衍生物，其中Y为CH或N; R 1是未取代或取代的烷基，未取代或取代的环烷基，未取代或取代的烯基，未取代或取代的环烯基，未取代或取代的芳基，芳烷基，其中芳基和烷基部分各自独立地为未取代或取代的 芳基和烯基部分可以各自独立地是未取代的或取代的，未取代的或取代的杂环基或杂环基烷基，其中杂环基和烷基部分各自是未取代的或取代的; R 2是未取代的芳基或未取代或取代或取代的杂芳基。 另外本发明涉及制备这种化合物的方法，含有这种化合物的药物组合物，以及这种化合物在医药中的用途。

公开(公告)号：US07297792B2

公开(公告)日：2007-11-20

申请号：US11422338

申请日：2006-06-06

申请人： Stephen Garland ,  David Haigh ,  Deidre Mary Bernadette Hickey ,  John Liddle ,  David Glynn Smith ,  Robert William Ward ,  Jason Witherington

发明人： Stephen Garland ,  David Haigh ,  Deidre Mary Bernadette Hickey ,  John Liddle ,  David Glynn Smith ,  Robert William Ward ,  Jason Witherington

IPC分类号： C07D413/00

CPC分类号： C07D471/04 ,  C07D213/85 ,  C07D487/04

摘要： The present invention includes compound of formula (I), or a derivative thereof, wherein Y is CH or N; R1 is unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted cycloalkenyl, unsubstituted or substituted aryl, aralkyl wherein the aryl and the alkyl moieties may each independently be unsubstituted or substituted, aralkenyl wherein the aryl, and alkenyl moieties may each independently be unsubstituted or substituted, unsubstituted or substituted heterocyclyl, or heterocyclylalkyl wherein the heterocyclcyl and the alkyl moieties may each inedepently be unsubstituted or substituted; and R2 is unsubstituted aryl or unsubstituted or substituted or substituted heteroaryl. Additionally the present invention inlcudes a process for preparing such a compound, a pharmaceutical composition containing such a compound, and the use of such a compound in medicine.

摘要翻译： 本发明包括式（I）化合物或其衍生物，其中Y为CH或N; R 1是未取代或取代的烷基，未取代或取代的环烷基，未取代或取代的烯基，未取代或取代的环烯基，未取代或取代的芳基，芳烷基，其中芳基和烷基部分各自独立地为未取代或取代的 芳基和烯基部分可以各自独立地是未取代的或取代的，未取代的或取代的杂环基或杂环基烷基，其中杂环基和烷基部分各自是未取代的或取代的; R 2是未取代的芳基或未取代或取代或取代的杂芳基。 另外本发明涉及制备这种化合物的方法，含有这种化合物的药物组合物，以及这种化合物在医药中的用途。

公开(公告)号：US07109199B2

公开(公告)日：2006-09-19

申请号：US10381292

申请日：2001-09-19

申请人： Stephen Garland ,  David Haigh ,  Deidre Mary Bernadette Hickey ,  John Liddle ,  David Glynn Smith ,  Robert William Ward ,  Jason Witherington

发明人： Stephen Garland ,  David Haigh ,  Deidre Mary Bernadette Hickey ,  John Liddle ,  David Glynn Smith ,  Robert William Ward ,  Jason Witherington

IPC分类号： C07D487/04 ,  C07D471/04 ,  A61K31/4162 ,  A61P3/10

CPC分类号： C07D471/04 ,  C07D213/85 ,  C07D487/04

摘要： The present invention includes compound of formula (I), or a derivative thereof, wherein Y is CH or N; R1 is unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted cycloalkenyl, unsubstituted or substituted aryl, aralkyl wherein the aryl and the alkyl moieties may each independently be unsubstituted or substituted, aralkenyl wherein the aryl, and alkenyl moieties may each independently be unsubstituted or substituted, unsubstituted or substituted heterocyclyl, or heterocyclylalkyl wherein the heterocyclyl and the alkyl moieties may each independently be unsubstituted or substituted; and R2 is unsubstituted aryl or unsubstituted or substituted or substituted heteroaryl. Additionally the present invention includes a process for preparing such a compound, a pharmaceutical composition containing such a compound, and the use of such a compound in medicine.

摘要翻译： 本发明包括式（I）化合物或其衍生物，其中Y为CH或N; R 1是未取代或取代的烷基，未取代或取代的环烷基，未取代或取代的烯基，未取代或取代的环烯基，未取代或取代的芳基，芳烷基，其中芳基和烷基部分各自独立地为未取代或取代的 芳基和烯基部分可各自独立地为未取代或取代的未取代或取代的杂环基或杂环基烷基，其中杂环基和烷基部分各自独立地为未取代或取代的; R 2是未取代的芳基或未取代或取代或取代的杂芳基。 另外本发明包括制备这种化合物的方法，含有这种化合物的药物组合物，以及这种化合物在医药中的用途。

公开(公告)号：US07348339B2

公开(公告)日：2008-03-25

申请号：US10508760

申请日：2003-03-21

申请人： Nicholas Bailey ,  Mark James Bamford ,  Haifeng Cui ,  Stephen Garland ,  Krista B Goodman ,  Mark A Hilfiker ,  Dennis Lee ,  Terence Aaron Panchal ,  Robert A Stavenger ,  David Matthew Wilson ,  Jason Witherington

发明人： Nicholas Bailey ,  Mark James Bamford ,  Haifeng Cui ,  Stephen Garland ,  Krista B Goodman ,  Mark A Hilfiker ,  Dennis Lee ,  Terence Aaron Panchal ,  Robert A Stavenger ,  David Matthew Wilson ,  Jason Witherington

IPC分类号： A61K31/44 ,  A01N43/42 ,  C07D265/30 ,  C07D295/00 ,  C07D498/02

CPC分类号： C07D471/04

摘要： A compound of the formula and physiologically acceptable salts and or N-oxides thereof wherein, X1 is N or CR3; X2 is N or CR4; X3 is N or CR5; X4 is N or CR6. with the proviso that at least one but not more than two of X1, X2, X3 and X4 represents N. R1 is a 5-, or 6-membered heterocyclic group selected from group a, b, c or d wherein X5 is a group selected from N or CR7 and X6 is a group selected from O, S or NR8; X7 and X8 which may be the same or different is a group selected from N or CR9; X9 is a group selected from O, S or NR8 and X10 is N or CR10; X11, X12 and X13 may be the same or different and selected from a group N or CR11; processes for their preparation, pharmaceutical compositions containing them and their use in medicine.

摘要翻译： 下式的化合物及其生理上可接受的盐和/或其N-氧化物，其中X 1是N或CR 3; X 2是N或CR 4; X 3是N或CR 5; X 4是N或CR 6。 条件是X 1，X 2，X 3和X 4中的至少一个但不多于两个， SUB>表示N. R 1是选自a，b，c或d的5-或6-元杂环基，其中X 5是选自 N或CR 7和X 6是选自O，S或NR 8的基团; X 7和X 8可以相同或不同，是选自N或CR 9的基团。 X 9是选自O，S或NR 8和X 10的基团是N或CR 10; X 11，X 12和X 13可以相同或不同，并且选自N或C 11 ; 其制备方法，含有它们的药物组合物及其在医药中的用途。

公开(公告)号：US20050153978A1

公开(公告)日：2005-07-14

申请号：US10508592

申请日：2003-03-21

申请人： Michael Alberti ,  Stephen Garland ,  David Jung ,  James Veal ,  Jason Witherington

发明人： Michael Alberti ,  Stephen Garland ,  David Jung ,  James Veal ,  Jason Witherington

IPC分类号： A61K31/4184 ,  A61K31/4245 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61P1/04 ,  A61P3/10 ,  A61P9/00 ,  A61P11/06 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P43/00 ,  C07D403/04 ,  C07D413/04 ,  C07D413/14 ,  C07D471/06 ,  A61K31/4439 ,  A61K31/4709 ,  C07D43/14

CPC分类号： C07D403/04 ,  A61K31/4184 ,  C07D413/04 ,  C07D413/14 ,  C07D471/06

摘要： A method of treating an Msk-1 and/or ROCK(1 and 2) mediated disease or condition in a mammal comprising administration of an effective amount of a compounds of the formula (I) and physiologically acceptable salts thereof wherein, R1 is a 5, or 6 membered heterocyclic group selected from group a, b, c or d wherein X1 is a group selected from N or CR7 and X2 is a group selected from O, S or NR8; X3 and X4 which may be the same or different is a group selected from N or CR7; X5 is a group selected from O, S or NR8 and X6 is N or CR7; X7, X8 and X9 may be the same or different and selected from a group N or CR7, pharmaceutical compositions, novel compounds and processes for their preparation.

摘要翻译： 一种在哺乳动物中治疗Msk-1和/或ROCK（1和2）介导的疾病或病症的方法，包括施用有效量的式（I）化合物及其生理学上可接受的盐，其中R 1， 1是选自组a，b，c或d的5或6元杂环基团，其中X 1是选自N或CR 7的基团。 并且X 2是选自O，S或NR 8的基团。 X 3和X 4可以相同或不同，是选自N或CR 7的基团。 X 5是选自O，S或NR 8和X 6的基团是N或CR 7; X 7，X 8和X 9可以相同或不同，并且选自N或C 7 ，药物组合物，新化合物及其制备方法。

公开(公告)号：US20050197328A1

公开(公告)日：2005-09-08

申请号：US10508760

申请日：2003-03-21

申请人： Nicholas Bailey ,  Mark Bamford ,  Haifeng Cui ,  Stephen Garland ,  Krista Goodman ,  Mark Hilfiker ,  Dennis Lee ,  Terence Panchal ,  Robert Stavenger ,  David Wilson ,  Jason Witherington

发明人： Nicholas Bailey ,  Mark Bamford ,  Haifeng Cui ,  Stephen Garland ,  Krista Goodman ,  Mark Hilfiker ,  Dennis Lee ,  Terence Panchal ,  Robert Stavenger ,  David Wilson ,  Jason Witherington

IPC分类号： C07D473/36 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/52 ,  A61K31/5377 ,  A61P1/04 ,  A61P11/06 ,  A61P19/10 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D471/04 ,  A61K31/551 ,  A61K31/498 ,  A61K31/503 ,  C07D473/14 ,  C07D487/02

CPC分类号： C07D471/04

摘要： A compound of the formula and physiologically acceptable salts and or N-oxides thereof wherein, X1 is N or CR3; X2 is N or CR4; X3 is N or CR5; X4 is N or CR6. with the proviso that at least one but not more than two of X1, X2, X3 and X4 represents N. R1 is a 5-, or 6-membered heterocyclic group selected from group a, b, c or d wherein X5 is a group selected from N or CR7 and X6 is a group selected from O, S or NR8; X7 and X8 which may be the same or different is a group selected from N or CR9; X9 is a group selected from O, S or NR8 and X10 is N or CR10; X11, X12 and X13 may be the same or different and selected from a group N or CR11; processes for their preparation, pharmaceutical compositions containing them and their use in medicine.

摘要翻译： 下式的化合物及其生理上可接受的盐和/或其N-氧化物，其中X 1是N或CR 3; X 2是N或CR 4; X 3是N或CR 5; X 4是N或CR 6。 条件是X 1，X 2，X 3和X 4中的至少一个但不多于两个， SUB>表示N. R 1是选自a，b，c或d的5-或6-元杂环基，其中X 5是选自 N或CR 7和X 6是选自O，S或NR 8的基团; 可以相同或不同的是选自N或CR 9的基团;其中X 1和X 3可以相同或不同。 X 9是选自O，S或NR 8和X 10的基团是N或CR 10; X 11，X 12和X 13可以相同或不同，选自基团N或CR 13， 11 其制备方法，含有它们的药物组合物及其在医药中的用途。