公开(公告)号：US20090181939A1

公开(公告)日：2009-07-16

申请号：US12407021

申请日：2009-03-19

Applicant: James Edward Paul Davidson ,  Jonathan Mark Bentley ,  Claire Elizabeth Dawson ,  Kerry Harrison ,  Howard Langham Mansell ,  Alan Leslie Pither ,  Robert Mark Pratt ,  Jonathan Richard Anthony Roffey ,  Victoria Jane Ruston

Inventor： James Edward Paul Davidson ,  Jonathan Mark Bentley ,  Claire Elizabeth Dawson ,  Kerry Harrison ,  Howard Langham Mansell ,  Alan Leslie Pither ,  Robert Mark Pratt ,  Jonathan Richard Anthony Roffey ,  Victoria Jane Ruston

IPC: A61K31/551 ,  C07D403/02 ,  A61K31/397 ,  C07D205/04

CPC classification number: C07D401/12 ,  C07D205/04 ,  C07D211/46 ,  C07D403/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12

Abstract: Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB1 receptors, such as obesity, wherein: R1 is aryl or heteroaryl; R2 is alkyl, aryl or heteroaryl; R3 is alkyl, aryl, heteroaryl, NR9R10, OR15, or NR16C(O)R17; Y is C═O, C═S, SO2, or (CR7R8)p; m=1 or 2; n=1 or 2; and p=1, 2, 3 or 4, R7 to R17 being as defined in the specification; wherein if —Y—R3 is C(O)NH(alkyl) then: R1 and/or R2 is selected from heteroaryl; and/or m and/or n is 2; and/or R11 and/or R12 is lower alkyl, or a pharmaceutically acceptable salt or prodrug thereof.

Abstract translation: 式（I）化合物及其在治疗中的用途，特别是用于治疗由CB1受体介导的障碍，例如肥胖症，其中：R1是芳基或杂芳基; R2是烷基，芳基或杂芳基; R3是烷基，芳基，杂芳基，NR9R10，OR15或NR16C（O）R17; Y是C-O，C-S，SO2或（CR7R8）p; m = 1或2; n = 1或2; 和p = 1,2,3或4，R7至R17如说明书中所定义; 其中如果-Y-R 3是C（O）NH（烷基），那么：R 1和/或R 2选自杂芳基; 和/或m和/或n为2; 和/或R 11和/或R 12是低级烷基，或其药学上可接受的盐或前药。

公开(公告)号：US07504522B2

公开(公告)日：2009-03-17

申请号：US10552575

申请日：2004-04-29

Applicant: James Edward Paul Davidson ,  Claire Elizabeth Dawson ,  Kerry Harrison ,  Howard Langham Mansell ,  Robert Mark Pratt ,  Sukhjit Sohal ,  Victoria Jane Ruston

Inventor： James Edward Paul Davidson ,  Claire Elizabeth Dawson ,  Kerry Harrison ,  Howard Langham Mansell ,  Robert Mark Pratt ,  Sukhjit Sohal ,  Victoria Jane Ruston

IPC: C07D205/00 ,  A61K31/397

CPC classification number: C07D405/12 ,  C07D205/04 ,  C07D409/12

Abstract: Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB1 receptors such as obesity: Formula (I) wherein: R1 and R2 are independently selected from aryl; and R3 is hydrogen or alkyl; or a pharmaceutically acceptable salt or prodrug thereof, wherein at least one of R1 and R2 has a non-hydrogen substituent in the ortho-position(s) thereof relative to the point of attachment to the [—CH—O—] group.

Abstract translation: 式（I）化合物及其在治疗中的用途，特别是用于治疗由CB1受体介导的障碍如肥胖症：式（I）其中：R 1和R 2独立地选自芳基; 并且R 3是氢或烷基; 或其药学上可接受的盐或前药，其中R 1和R 2中的至少一个在其邻位相对于[-CH-O-]基团的连接点具有非氢取代基。