公开(公告)号：US20050112713A1

公开(公告)日：2005-05-26

申请号：US10888524

申请日：2004-07-09

Applicant: Walter DeWolf ,  David Payne ,  Peter Milner ,  Stewart Pearson ,  John Lonsdale

Inventor： Walter DeWolf ,  David Payne ,  Peter Milner ,  Stewart Pearson ,  John Lonsdale

IPC: A61K38/00 ,  A61K39/00 ,  C07K14/31 ,  C12N9/02 ,  G01N33/569 ,  C12Q1/48 ,  C12Q1/26

CPC classification number: C12N9/001 ,  A61K38/00 ,  A61K39/00 ,  C07K14/31 ,  G01N33/56938

Abstract: 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.

Abstract translation: 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：US20050070475A1

公开(公告)日：2005-03-31

申请号：US10950010

申请日：2004-09-24

Applicant: Dominique Bridon ,  Robert Dufresne ,  Nissab Boudjellab ,  Martin Robitaille ,  Peter Milner

Inventor： Dominique Bridon ,  Robert Dufresne ,  Nissab Boudjellab ,  Martin Robitaille ,  Peter Milner

IPC: A61K38/00 ,  A61P31/12 ,  A61P31/16 ,  A61P31/18 ,  C07K14/00 ,  C07K14/155 ,  C07K14/16 ,  A61K38/17 ,  C07K14/47

CPC classification number: C07K14/005 ,  A61K38/00 ,  C12N2740/16122

Abstract: Peptides exhibiting anti-viral and anti-fusogenic activity are modified to provide greater stability and improved half-life in vivo. The selected peptides include fusion inhibitors DP178 and DP107 and related peptides and analogs thereof. The modified peptides are capable of forming covalent bonds with one or more blood components, preferably a mobile blood component.

Abstract translation: 展示抗病毒和抗融合活性的肽被修饰以提供更大的稳定性和改善的体内半衰期。 所选择的肽包括融合抑制剂DP178和DP107及其相关肽及其类似物。 修饰的肽能够与一种或多种血液成分，优选移动血液成分形成共价键。

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：US20240115535A1

公开(公告)日：2024-04-11

申请号：US18275972

申请日：2022-02-07

Applicant: Peter MILNER ,  Mikhail Sergeevich SHCHEPINOV ,  Retrotope, Inc.

Inventor： Peter Milner ,  Mikhail Sergeevich Shchepinov

IPC: A61K31/201 ,  A61P25/28 ,  G01N33/50 ,  G01N33/555

CPC classification number: A61K31/201 ,  A61P25/28 ,  G01N33/5044 ,  G01N33/555

Abstract: Disclosed are methods for inhibiting the progression of neurodegenerative disease. The methods include administering to a patient suffering from such a disease a composition comprising deuterated arachidonic acid or an ester thereof.

公开(公告)号：US20240091188A1

公开(公告)日：2024-03-21

申请号：US18275965

申请日：2022-02-04

Applicant: Peter MILNER ,  Mikhail Sergeevich SHCHEPINOV ,  Retrotope, Inc.

Inventor： Peter Milner ,  Mikhail Sergeevich Shchepinov

IPC: A61K31/202 ,  A61K31/232 ,  A61P25/28

CPC classification number: A61K31/202 ,  A61K31/232 ,  A61P25/28

Abstract: Disclosed are methods or dosing protocols for administering deuterated arachidonic acid or a prodrug thereof to a patient in order to accelerate the time required to achieve of a therapeutic concentration of 13,13-D2-arachidonic acid in vivo.

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：US20050075379A1

公开(公告)日：2005-04-07

申请号：US10759617

申请日：2004-01-16

Applicant: Pascal Druzgala ,  Peter Milner ,  Jurg Pfister

Inventor： Pascal Druzgala ,  Peter Milner ,  Jurg Pfister

IPC: C07D261/12 ,  C07D277/20 ,  C07D277/34 ,  C07D311/70 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07J3/00 ,  A61K31/426

CPC classification number: C07D277/20 ,  C07D261/12 ,  C07D277/34 ,  C07D311/70 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07J3/00 ,  Y10S514/824 ,  Y10S514/866

Abstract: The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.

Abstract translation: 本发明提供了可用于治疗II型糖尿病的药物化合物。 这些化合物是有利的，因为它们容易被代谢药物解毒体系代谢。 特别地，提供了被设计为在化合物的结构内包含酯的噻唑烷二酮类似物。 本发明还涉及治疗疾病如糖尿病的方法，其包括施用包含化合物的治疗有效组合物，所述化合物被设计为由血清或细胞内水解酶和酯酶代谢。 还教导了含酯的噻唑烷二酮类似物的药物组合物。