公开(公告)号：US07253198B2

公开(公告)日：2007-08-07

申请号：US10536303

申请日：2003-12-03

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

发明人： 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分类号： C07D275/03 ,  C07D207/12 ,  A61K31/425 ,  A61K31/4015

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

摘要： 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.

摘要翻译： 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

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

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

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

CPC分类号： C07D207/267 ,  C07D211/76 ,  C07D223/10 ,  C07D263/22

摘要： 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.

摘要翻译： 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：US06753172B1

公开(公告)日：2004-06-22

申请号：US09292411

申请日：1999-04-15

申请人： David John Payne ,  Peter Henry Milner ,  Stewart Campbell Pearson ,  John Timothy Lonsdale

发明人： David John Payne ,  Peter Henry Milner ,  Stewart Campbell Pearson ,  John Timothy Lonsdale

IPC分类号： C12N900

CPC分类号： C12N9/001 ,  A61K39/00 ,  C07K14/31 ,  G01N33/56938

摘要： Prokayrotic FABI polypeptides and DNA (RNA) encoding such FABI and a procedure for such polypeptides by recombinant techniques is disclosed. Also disclosed are methods for utilizing such FABI for the treatment of infection, such as bacterial infections. Antagonists against such FABI and their use as a therapeutic to treat infections, such asstaphylococcal infections are also disclosed. Also disclosed are diagnostic assays for detecting diseases related to the presence of FABI nucleic acid sequences and the polypeptides in a host. Also disclosed are diagnostic assays for detecting polynucleotides encoding FABI and for detecting the polypeptide in a host.

摘要翻译： 公开了Prokayrotic FABI多肽和编码这种FABI的DNA（RNA）和通过重组技术的这种多肽的程序。 还公开了利用这种FABI来治疗感染的方法，例如细菌感染。 还公开了抗这种FABI的拮抗剂及其作为治疗感染治疗感染的用途，例如葡萄球菌感染。 还公开了用于检测与宿主中FABI核酸序列和多肽的存在相关的疾病的诊断测定法。 还公开了用于检测编码FABI的多核苷酸并用于检测宿主中的多肽的诊断测定。

公开(公告)号：US06432670B1

公开(公告)日：2002-08-13

申请号：US09292412

申请日：1999-04-15

申请人： David John Payne ,  Peter Henry Milner ,  Stewart Campbell Pearson ,  John Timothy Lonsdale

发明人： David John Payne ,  Peter Henry Milner ,  Stewart Campbell Pearson ,  John Timothy Lonsdale

IPC分类号： C07H2104

CPC分类号： C12N9/001 ,  A61K39/00 ,  C07K14/31 ,  G01N33/56938

摘要： Prokayrotic FAB I polypeptides and DNA (RNA) encoding such FAB I and a procedure for producing such polypeptides by recombinant techniques is disclosed. Also disclosed are methods for utilizing such FAB I for the treatment of infection, such as bacterial infections. Antagonists against such FAB I and their use as a therapeutic to treat infections, such asstaphylococcal infections are also disclosed. Also disclosed are diagnostic assays for detecting diseases related to the presence of FAB I nucleic acid sequences and the polypeptides in a host. Also disclosed are diagnostic assays for detecting polynucleotides encoding FAB I and for detecting the polypeptide in a host.

摘要翻译： 公开了Prokayrotic FAB I多肽和编码这种FAB I的DNA（RNA）和通过重组技术产生此类多肽的方法。 还公开了利用这种FAB I来治疗感染的方法，例如细菌感染。 还公开了抗这种FAB I的拮抗剂及其作为治疗性感染治疗如葡萄球菌感染的用途。 还公开了用于检测与宿主中FAB I核酸序列和多肽的存在相关的疾病的诊断测定。 还公开了用于检测编码FAB I的多核苷酸并用于检测宿主中的多肽的诊断测定。

公开(公告)号：US20080318933A1

公开(公告)日：2008-12-25

申请号：US11576070

申请日：2005-10-05

申请人： Mahmood Ahmed ,  Christopher Norbert Johnson ,  Neil Derek Miller ,  Peter Henry Milner ,  Dean Andrew Rivers ,  David R Witty

发明人： Mahmood Ahmed ,  Christopher Norbert Johnson ,  Neil Derek Miller ,  Peter Henry Milner ,  Dean Andrew Rivers ,  David R Witty

IPC分类号： A61K31/55 ,  C07D401/04 ,  A61K31/454 ,  A61P3/00 ,  A61P25/00 ,  C07D403/04 ,  A61K31/403

CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D417/14

摘要： The present invention relates to novel indole derivatives such as compounds of the formula (I): which possess antagonist potency at the 5-HT6 receptor and the use of such compounds or pharmaceutically acceptable salts or solvates thereof in the treatment of Alzheimer's disease and other CNS disorders.

摘要翻译： 本发明涉及新的吲哚衍生物，例如式（I）的化合物：其具有5-HT 6受体的拮抗剂效力，以及这些化合物或其药学上可接受的盐或溶剂化物在治疗阿尔茨海默病和其它CNS中的用途 疾病

公开(公告)号：US07160905B2

公开(公告)日：2007-01-09

申请号：US10496334

申请日：2002-11-29

申请人： Andrew Faller ,  Peter Henry Milner ,  John Gerard Ward

发明人： Andrew Faller ,  Peter Henry Milner ,  John Gerard Ward

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

CPC分类号： C07D207/27 ,  C07C317/42 ,  C07C317/46 ,  C07C2602/42 ,  C07D213/81 ,  C07D333/38

摘要： 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.

摘要翻译： 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：US06995254B1

公开(公告)日：2006-02-07

申请号：US08790043

申请日：1997-01-28

申请人： David John Payne ,  Peter Henry Milner ,  Stewart Campbell Pearson ,  John Timothy Lonsdale

发明人： David John Payne ,  Peter Henry Milner ,  Stewart Campbell Pearson ,  John Timothy Lonsdale

IPC分类号： C07H21/00 ,  C12N15/31 ,  C12N15/53

CPC分类号： C12N9/001 ,  A61K39/00 ,  C07K14/31 ,  G01N33/56938

摘要： Prokayrotic FAB I polypeptides and DNA (RNA) encoding such FAB I and a procedure for producing such polypeptides by recombinant techniques is disclosed. Also disclosed are methods for utilizing such FAB I for the treatment of infection, such as bacterial infections. Antagonists against such FAB I and their use as a therapeutic to treat infections, such as staphylococcal infections are also disclosed. Also disclosed are diagnostic assays for detecting diseases related to the presence of FAB I nucleic acid sequences and the polypeptides in a host. Also disclosed are diagnostic assays for detecting polynucleotides encoding FAB I and for detecting the polypeptide in a host.

摘要翻译： 公开了Prokayrotic FAB I多肽和编码这种FAB I的DNA（RNA）和通过重组技术产生此类多肽的方法。 还公开了利用这种FAB I来治疗感染的方法，例如细菌感染。 针对这种FAB I的拮抗剂及其作为治疗性感染治疗如葡萄球菌感染的用途也被公开。 还公开了用于检测与宿主中FAB I核酸序列和多肽的存在相关的疾病的诊断测定。 还公开了用于检测编码FAB I的多核苷酸并用于检测宿主中的多肽的诊断测定。

公开(公告)号：US06458779B1

公开(公告)日：2002-10-01

申请号：US09701946

申请日：2001-04-05

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

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

IPC分类号： A61K31545

CPC分类号： 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

摘要： 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.

摘要翻译： 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。