公开(公告)号：US20070043069A1

公开(公告)日：2007-02-22

申请号：US11463144

申请日：2006-08-08

Applicant: Alan Birch ,  Andrew Morley ,  Andrew Stocker ,  Paul Whittamore

Inventor： Alan Birch ,  Andrew Morley ,  Andrew Stocker ,  Paul Whittamore

IPC: C07D471/02 ,  A61K31/4745

CPC classification number: C07D495/04

Abstract: Heterocyclic amides of formula (1) wherein: X is N or CH; R4 and R5 together are either —S—C(R6)═C(R7)— or —C(R7)═C(R6)—S—; R6 and R7 are independently selected from, for example hydrogen, halo and C1-4alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof, possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.

Abstract translation: 式（1）的杂环酰胺其中：X是N或CH; R 4和R 5一起是-SC（R 6）-C（R 7） - 或 -C（R 7）C（R 6）-S-; R 6和R 7独立地选自，例如氢，卤素和C 1-4烷基; A是亚苯基或亚杂芳基; n为0,1或2; R 1选自例如卤素，硝基，氰基，羟基，羧基; R 2是氢，羟基或羧基; R 3选自例如氢，羟基，芳基，杂环基和C 1-4烷基（任选被1或2个R 8取代） 组）; R 8选自例如羟基，-COCOOR 9，-C（O）N（R 9）（R 10） ），-NHC（O）R 9，（R 9）（R 10）N - 和-COOR ^{9 ; R 9和R 10选自例如氢，羟基，C 1-4烷基（任选被1或2个R SUP取代 > 13 ）; R 13选自羟基，卤素，三卤代甲基和C 1-4烷氧基; 或其药学上可接受的盐或前药具有糖原磷酸化酶抑制活性，因此在治疗与增加的糖原磷酸化酶活性相关的疾病状态方面具有价值。 描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。}

公开(公告)号：US20050131016A1

公开(公告)日：2005-06-16

申请号：US10506748

申请日：2003-03-04

Applicant: Alan Birch ,  Andrew Morley

Inventor： Alan Birch ,  Andrew Morley

IPC: A61K31/4709 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61P3/04 ,  A61P3/10 ,  A61P7/00 ,  A61P9/10 ,  A61P43/00 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  C07D43/02

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D417/14

Abstract: Heterocyclic amides of formula (1) wherein: is a single or double bond; A is phenylene or heteroarylene; m is 0, 1 or 2; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R4 is independently selected from for example hydrogen, halo, nitro, cyano, hydroxy, C1-4alkyl, and C1-4alkanoyl; R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.

Abstract translation: 式（1）的杂环酰胺其中：是单键或双键; A是亚苯基或亚杂芳基; m为0,1或2; n为0,1或2; R 1选自例如卤素，硝基，氰基，羟基，羧基; R 2是氢，羟基或羧基; R 3选自例如氢，羟基，芳基，杂环基和C 1-4烷基（任选被1或2个R 8取代） 组）; R 4独立地选自例如氢，卤素，硝基，氰基，羟基，C 1-4烷基和C 1-4烷基。 烷酰基; R 8选自例如羟基，-COCOOR 9，-C（O）N（R 9）（R 10） ），-NHC（O）R 9，（R 9）（R 10）N - 和-COOR ^{9 ; R 9和R 10选自例如氢，羟基，C 1-4烷基（任选被1或2个R SUP取代 > 13 ）; R 13选自羟基，卤素，三卤代甲基和C 1-4烷氧基; 或其药学上可接受的盐或前体药物; 具有糖原磷酸化酶抑制活性，因此具有与增加的糖原磷酸化酶活性相关的疾病状态的治疗价值。 描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。}

公开(公告)号：US20080096874A1

公开(公告)日：2008-04-24

申请号：US11792922

申请日：2005-12-09

Applicant: Alan Birch ,  Suzanne Bowker ,  Roger Butlin ,  Craig Donald ,  William Mccoull ,  Thorsten Nowak ,  Alleyn Plowright

Inventor： Alan Birch ,  Suzanne Bowker ,  Roger Butlin ,  Craig Donald ,  William Mccoull ,  Thorsten Nowak ,  Alleyn Plowright

IPC: A61K31/4245 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61P3/04 ,  A61P3/10 ,  C07D271/113 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D271/113 ,  C07D413/12

Abstract: Compounds of formula (I), and salts and pro-drugs thereof: Formula (I) wherein for example R1 is optionally substituted aryl or heteroaryl; Y is a linking group selected from, for example, a direct bond, and a (substituted) alkyl chain; R2 is an optionally substituted aryl, an optionally substituted cycloalkyl or an optionally substituted heterocyclic group; are described. Processes to make such compounds and their use as DGAT inhibitors, for example in the treatment of obesity, are also described.

Abstract translation: 式（I）化合物及其盐和前药：式（I）其中例如R 1为任选取代的芳基或杂芳基; Y是选自例如直接键和（取代的）烷基链的连接基团; R 2是任选取代的芳基，任选取代的环烷基或任选取代的杂环基; 被描述。 还描述了制备这些化合物的方法及其作为DGAT抑制剂的用途，例如用于治疗肥胖症。

公开(公告)号：US20050131015A1

公开(公告)日：2005-06-16

申请号：US10506741

申请日：2003-03-04

Applicant: Alan Birch ,  Andrew Morley ,  Andrew Stocker ,  Paul Whittamore

Inventor： Alan Birch ,  Andrew Morley ,  Andrew Stocker ,  Paul Whittamore

IPC: A61K31/4375 ,  A61K31/4709 ,  A61K31/519 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/10 ,  A61P43/00 ,  C07D495/04 ,  C07D519/00 ,  C07D498/02

CPC classification number: C07D495/04

Abstract: Heterocyclic amides of formula (1) wherein: X is N or CH; R4 and R5 together are either —S—C(R6)═C(R7)— or —C(R7)═C(R6)—S—; R6 and R7 are independently selected from, for example hydrogen, halo and Cl-4alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.

Abstract translation: 式（1）的杂环酰胺其中：X是N或CH; R 4和R 5一起是-SC（R 6）-C（R 7） - 或 -C（R 7）C（R 6）-S-; R 6和R 7独立地选自，例如氢，卤素和C 1-4烷基; A是亚苯基或亚杂芳基; n为0,1或2; R 1选自例如卤素，硝基，氰基，羟基，羧基; R 2是氢，羟基或羧基; R 3选自例如氢，羟基，芳基，杂环基和C 1-4烷基（任选被1或2个R 8取代） 组）; R 8选自例如羟基，-COCOOR 9，-C（O）N（R 9）（R 10） ），-NHC（O）R 9，（R 9）（R 10）N - 和-COOR ^{9 ; R 9和R 10选自例如氢，羟基，C 1-4烷基（任选被1或2个R SUP取代 > 13 ）; R 13选自羟基，卤素，三卤代甲基和C 1-4烷氧基; 或其药学上可接受的盐或前体药物; 具有糖原磷酸化酶抑制活性，因此具有与增加的糖原磷酸化酶活性相关的疾病状态的治疗价值。 描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。}

公开(公告)号：US20060211760A1

公开(公告)日：2006-09-21

申请号：US10566068

申请日：2004-08-04

Applicant: Alan Birch ,  Stuart Bennett ,  Linda Godfrey ,  Iain Simpson ,  Paul Whittamore

Inventor： Alan Birch ,  Stuart Bennett ,  Linda Godfrey ,  Iain Simpson ,  Paul Whittamore

IPC: C07D209/42 ,  A61K31/405

CPC classification number: C07D209/42

Abstract: A compound of the formula (1) or a pharmaceutically-acceptable salt wherein, for example, A is phenylene or heteroarylene; Y is selected from —C(O)R2, —C(O)OR2, —C(O)NR2R3, -(1-4C)alkyl [optionally substituted]-(2-4C)alkenyl, —SO2NR2R3, and —S(O)cR2 (wherein c is 0, 1 or 2); compounds which possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.

Abstract translation: 式（1）的化合物或其药学上可接受的盐，其中例如A是亚苯基或亚杂芳基; 其中Y选自-C（O）R 2，-C（O）OR 2，-C（O）NR 2 R 2， （1-4C）烷基[任选取代的] - （2-4C）烯基，-SO 2 NR 2 R 3和-S（O）C R 2（其中c是0,1或2）; 具有糖原磷酸化酶抑制活性的化合物，因此具有与增加的糖原磷酸化酶活性相关的疾病状态的治疗价值。 描述了制备含有它们的化合物和药物组合物的方法。

公开(公告)号：US20080009512A1

公开(公告)日：2008-01-10

申请号：US11569943

申请日：2005-06-14

Applicant: Alan Birch ,  Paul Kemmitt ,  Nathaniel Martin ,  Richard Ward

Inventor： Alan Birch ,  Paul Kemmitt ,  Nathaniel Martin ,  Richard Ward

IPC: A61K31/47 ,  A61K31/4375 ,  A61P3/10 ,  C07D215/60 ,  C07D471/04

CPC classification number: C07D215/38 ,  C07D215/60 ,  C07D471/04

Abstract: Compound of formula (I) or a pharmaceutically-acceptable salt thereof, formula (I) wherein Ar is optionally substituted phenyl; R1 is selected from: formula a) or b) (wherein is a single or double bond); R5, R6, R7 and R8 are for or alkyl; R4 is selected from hydrogen, (3-4C)cycloalkyl and optionally substituted (1-4C)alkyl; R10 is for example selected from hydrogen, (1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, hydroxy(1-4C)alkyl, (1-4C)alkoxy, aryl(1-4C)alkyl; Y is carbon and Ring A is optionally substituted phenylene; or each Y may independently be carbon or nitrogen and Ring A is optionally substituted 5- or 6-membered, heteroarylene ring; R11 is selected from hydrogen and optionally substituted phenyl; p is independently at each occurrence 0, 1 or 2; are described. Processes for making such compounds and their use as DPP-IV inhibitors in the treatment of diabetes are also described.

Abstract translation: 式（I）化合物或其药学上可接受的盐，式（I）其中Ar是任选取代的苯基; R 1选自：式a）或b）（其中是单键或双键）; R 5，R 6，R 7和R 8是用于或烷基的; R 4选自氢，（3-4C）环烷基和任选取代的（1-4C）烷基; R 1是例如选自氢，（1-4C）烷基，（3-6C）环烷基（1-4C）烷基，羟基（1-4C）烷基，（1-4C）烷氧基 ，芳基（1-4C）烷基; Y是碳，环A是任选取代的亚苯基; 或每个Y可以独立地为碳或氮，并且环A为任选取代的5或6元杂亚芳环; R 11选自氢和任选取代的苯基; p在每次出现时独立地为0,1或2; 被描述。 还描述了制备这些化合物的方法及其作为DPP-IV抑制剂在治疗糖尿病中的用途。