公开(公告)号：US06235753B1

公开(公告)日：2001-05-22

申请号：US09180547

申请日：1999-01-21

Applicant: Stuart Bailey ,  Andrew Faller ,  David Glynn Smith ,  Derek Richard Buckle

Inventor： Stuart Bailey ,  Andrew Faller ,  David Glynn Smith ,  Derek Richard Buckle

IPC: C07C25904

CPC classification number: C07D333/54 ,  C07C259/06 ,  C07D277/64 ,  C07D307/80 ,  C07D333/60

Abstract: Inhibitors of the Production of s-CD23 and the secretion of TNF are provided.

Abstract translation: 提供了s-CD23的产生抑制剂和TNF的分泌

公开(公告)号：US06242467B1

公开(公告)日：2001-06-05

申请号：US09381405

申请日：1999-09-17

Applicant: Andrew Faller

Inventor： Andrew Faller

IPC: A61K3144

CPC classification number: C07D409/04 ,  C07C311/19 ,  C07C311/29

Abstract: Compounds of formula (I) wherein R is hydroxy, hydrogen, alkenyl, alkynyl or aryl, and R1 is aryl or heteroaryl, are useful in the treatment and prophylaxis of conditions mediated by CD23 or TNF.

Abstract translation: 其中R为羟基，氢，烯基，炔基或芳基，R 1为芳基或杂芳基的式（I）化合物可用于治疗和预防由CD23或TNF介导的病症。

公开(公告)号：US07253198B2

公开(公告)日：2007-08-07

申请号：US10536303

申请日：2003-12-03

Applicant: Emmanuel H Demont ,  Andrew Faller ,  David Timothy MacPherson ,  Peter Henry Milner ,  Alan Naylor ,  Sally Redshaw ,  Steven James Stanway ,  David R Vesey ,  Daryl S Walter

Inventor： Emmanuel H Demont ,  Andrew Faller ,  David Timothy MacPherson ,  Peter Henry Milner ,  Alan Naylor ,  Sally Redshaw ,  Steven James Stanway ,  David R Vesey ,  Daryl S Walter

IPC: C07D275/03 ,  C07D207/12 ,  A61K31/425 ,  A61K31/4015

CPC classification number: C07D207/267 ,  C07D211/76 ,  C07D275/02 ,  C07D279/02 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

Abstract: The present invention relates to novel hydroxyethylamine compounds having Asp2 (β-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.

Abstract translation: 本发明涉及具有Asp2（β-分泌酶，BACE1或Memapsin）抑制活性的新型羟乙基胺化合物，其制备方法，含有它们的组合物及其用于治疗以β-淀粉样蛋白升高或β- 淀粉样沉积物，特别是阿尔茨海默氏病。

公开(公告)号：US06992103B2

公开(公告)日：2006-01-31

申请号：US10496269

申请日：2002-11-29

Applicant: Andrew Faller ,  David Timothy MacPherson ,  Peter Henry Milner ,  Steven James Stanway ,  Leontine Saskia Trouw

Inventor： Andrew Faller ,  David Timothy MacPherson ,  Peter Henry Milner ,  Steven James Stanway ,  Leontine Saskia Trouw

IPC: A61K31/4015 ,  A61K31/4166 ,  A61K31/4439 ,  C07D207/24 ,  C07D223/10

CPC classification number: C07D207/267 ,  C07D211/76 ,  C07D223/10 ,  C07D263/22

Abstract: The present invention relates to novel hydroxyethylene compounds having Asp2 (β-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.

Abstract translation: 本发明涉及具有Asp2（β-分泌酶，BACE1或Memapsin）抑制活性的新型羟基亚乙基化合物，其制备方法，含有它们的组合物及其用于治疗以β-淀粉样蛋白升高或β- 淀粉样沉积物，特别是阿尔茨海默氏病。

公开(公告)号：US20060025459A1

公开(公告)日：2006-02-02

申请号：US10536303

申请日：2003-12-03

Applicant: Emmanuel Demont ,  Andrew Faller ,  David Macpherson ,  Peter Milner ,  Alan Naylor ,  Sally Redshaw ,  Steven Stanway ,  David Vesey ,  Daryl Walter

Inventor： Emmanuel Demont ,  Andrew Faller ,  David Macpherson ,  Peter Milner ,  Alan Naylor ,  Sally Redshaw ,  Steven Stanway ,  David Vesey ,  Daryl Walter

IPC: A61K31/425 ,  A61K31/4025 ,  A61K31/4015 ,  C07D417/02 ,  C07D403/02

CPC classification number: C07D207/267 ,  C07D211/76 ,  C07D275/02 ,  C07D279/02 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

Abstract: The present invention relates to novel hydroxyethylamine compounds having Asp2 (β-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.

Abstract translation: 本发明涉及具有Asp2（β-分泌酶，BACE1或Memapsin）抑制活性的新型羟乙基胺化合物，其制备方法，含有它们的组合物及其用于治疗以β-淀粉样蛋白升高或β- 淀粉样沉积物，特别是阿尔茨海默氏病。

公开(公告)号：US20050038028A1

公开(公告)日：2005-02-17

申请号：US10496334

申请日：2002-11-29

Applicant: Andrew Faller ,  Peter Milner ,  John Ward

Inventor： Andrew Faller ,  Peter Milner ,  John Ward

IPC: C07D333/40 ,  A61K31/166 ,  A61K31/381 ,  A61K31/402 ,  A61K31/44 ,  A61P25/28 ,  A61P43/00 ,  C07C315/02 ,  C07C317/42 ,  C07C317/44 ,  C07C317/46 ,  C07D207/26 ,  C07D207/27 ,  C07D213/81 ,  C07D333/38 ,  C07D277/18 ,  A61K31/165 ,  A61K31/50 ,  C07D213/56

CPC classification number: C07D207/27 ,  C07C317/42 ,  C07C317/46 ,  C07C2602/42 ,  C07D213/81 ,  C07D333/38

Abstract: The present invention relates to hydroxyethylene compounds of formula (I), in which Ra represents a group of formula (a) or (b) where R1 represents —SO2R5, W1 represents CO or SO2, and the other variables are as defined in the claims, having Asp2 (β-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, compositions containing them, and their use in the treatment of diseases characterised by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease. Formula (I):

Abstract translation: 本发明涉及式（I）的羟基亚乙基化合物，其中R 5'表示式（a）或（b）的基团，其中R 1表示-SO 2 R 5，W 1表示CO或SO 2，以及 其他变量如权利要求中所定义，具有Asp2（β-分泌酶，BACE1或突变蛋白）抑制活性，其制备方法，含有它们的组合物及其在治疗特征在于升高的β-淀粉样蛋白水平或β的疾病中的用途 淀粉样蛋白沉积物，特别是阿尔茨海默氏病。 式（I）：

公开(公告)号：US07160905B2

公开(公告)日：2007-01-09

申请号：US10496334

申请日：2002-11-29

Applicant: Andrew Faller ,  Peter Henry Milner ,  John Gerard Ward

Inventor： Andrew Faller ,  Peter Henry Milner ,  John Gerard Ward

IPC: A61K31/44 ,  A61K31/41 ,  C07D211/72 ,  C07D333/12 ,  C07D207/40

CPC classification number: C07D207/27 ,  C07C317/42 ,  C07C317/46 ,  C07C2602/42 ,  C07D213/81 ,  C07D333/38

Abstract: The present invention relates to novel hydroxyethylene compounds having Asp2 (β-secretase. BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.

Abstract translation: 本发明涉及具有Asp2（β-分泌酶，BACE1或Memapsin）抑制活性的新型羟基亚乙基化合物，其制备方法，含有它们的组合物及其用于治疗以β-淀粉样蛋白升高或β- 淀粉样沉积物，特别是阿尔茨海默氏病。

公开(公告)号：US20050085520A1

公开(公告)日：2005-04-21

申请号：US10496269

申请日：2002-11-29

Applicant: Andrew Faller ,  David Macpherson ,  Peter Milner ,  Steven Stanway ,  Leontine Trouw

Inventor： Andrew Faller ,  David Macpherson ,  Peter Milner ,  Steven Stanway ,  Leontine Trouw

IPC: A61K31/402 ,  A61K31/4025 ,  A61K31/421 ,  A61K31/4439 ,  A61K31/451 ,  A61K31/55 ,  A61P9/00 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D207/26 ,  C07D207/267 ,  C07D207/27 ,  C07D211/76 ,  C07D223/10 ,  C07D263/20 ,  C07D263/22 ,  C07D401/04 ,  A61K31/426 ,  A61K31/4164

CPC classification number: C07D207/267 ,  C07D211/76 ,  C07D223/10 ,  C07D263/22

Abstract: The present invention relates to novel hydroxyethylene compounds having Asp2 (β-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.

Abstract translation: 本发明涉及具有Asp2（β-分泌酶，BACE1或Memapsin）抑制活性的新型羟基亚乙基化合物，其制备方法，含有它们的组合物及其用于治疗以β-淀粉样蛋白升高或β- 淀粉样沉积物，特别是阿尔茨海默氏病。

公开(公告)号：US06673965B1

公开(公告)日：2004-01-06

申请号：US10111209

申请日：2002-07-16

Applicant: John Gerard Ward ,  Andrew Faller

Inventor： John Gerard Ward ,  Andrew Faller

IPC: C07C25904

CPC classification number: C07C259/06 ,  A61K31/165 ,  C07C237/22

Abstract: A compound of formula (I) wherein: R isopropyl; n is 0; R1 is naphthylmethyl; R2 is t-butyl; and R3 is methyl; is useful in the treatment of disorders mediated by s-CD23.

Abstract translation: 式（I）的化合物，其中：R异丙基; n为0; R 1为萘基甲基; R 2为叔丁基; 和R 3是甲基;可用于治疗由s-CD23介导的病症。

公开(公告)号：US06458779B1

公开(公告)日：2002-10-01

申请号：US09701946

申请日：2001-04-05

Applicant: Andrew Faller ,  David Timothy MacPherson ,  Peter Henry Milner ,  Jayshree Mistry ,  John Gerald Ward

Inventor： Andrew Faller ,  David Timothy MacPherson ,  Peter Henry Milner ,  Jayshree Mistry ,  John Gerald Ward

IPC: A61K31545

CPC classification number: C07D207/404 ,  C07C237/22 ,  C07C259/06 ,  C07C323/60 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/10 ,  C07D215/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D271/06 ,  C07D277/24 ,  C07D311/58 ,  C07D333/54 ,  C07D333/60

Abstract: Compounds of Formula (1) wherein: R is methyl substituted by one to three groups from alkyl, aryl, alkenyl, and alkynyl; n is ) or 1; R1 is arylmethyl or heterocyclylmethyl; R2 is alkyl, alkenyl, cycloalkyl or cycloalkenyl; and R3 is hydrogen, alkyl, alkenyl, alkynyl or aryl; are useful in the treatment of disorders mediated y s-CD23.

Abstract translation: 式（1）的化合物，其中：R是被烷基，芳基，烯基和炔基一至三个基团取代的甲基; n是）或1; R1是芳基甲基或杂环基甲基; R2是烷基，烯基，环烷基或环烯基; R3是氢，烷基，烯基，炔基或芳基; 可用于治疗介导的s-CD23的病症。