公开(公告)号：US20080009603A1

公开(公告)日：2008-01-10

申请号：US11825293

申请日：2007-07-03

申请人： Victor Gault ,  Finbarr O'Harte ,  Nigel Irwin ,  Peter Flatt

发明人： Victor Gault ,  Finbarr O'Harte ,  Nigel Irwin ,  Peter Flatt

IPC分类号： A61K38/22

CPC分类号： C07K14/575 ,  A61K38/00 ,  Y10T29/4935

摘要： The present invention provides peptide analogues which are antagonists of gastric inhibitory peptide (GIP). The peptides, based on GIP 1-42 include substitutions and/or modifications which have enhanced resistance to degradation by the enzyme dipeptidyl peptidase IV (DPP IV). The invention also provides a process of N terminally modifying GIP and the use of the peptide analogues for treatment of diabetes.

摘要翻译： 本发明提供作为胃抑制肽（GIP）拮抗剂的肽类似物。 基于GIP 1-42的肽包括通过酶二肽基肽酶IV（DPP IV）具有增强的降解抗性的取代和/或修饰。 本发明还提供N末端修饰GIP的方法和肽类似物用于治疗糖尿病的用途。

公开(公告)号：US20070167370A1

公开(公告)日：2007-07-19

申请号：US11713892

申请日：2007-03-05

申请人： Victor Gault ,  Finbarr O'Harte ,  Nigel Irwin ,  Peter Flatt

发明人： Victor Gault ,  Finbarr O'Harte ,  Nigel Irwin ,  Peter Flatt

IPC分类号： A61K38/22

CPC分类号： C07K14/575 ,  A61K38/00 ,  Y10T29/4935

摘要： The present invention provides peptide analogues which are antagonists of gastric inhibitory peptide (GIP). The peptides, based on GIP 1-42 include substitutions and/or modifications which have enhanced resistance to degradation by the enzyme dipeptidyl peptidase IV (DPP IV). The invention also provides a process of N terminally modifying GIP and the use of the peptide analogues for treatment of diabetes.

摘要翻译： 本发明提供作为胃抑制肽（GIP）拮抗剂的肽类似物。 基于GIP 1-42的肽包括通过酶二肽基肽酶IV（DPP IV）具有增强的降解抗性的取代和/或修饰。 本发明还提供N末端修饰GIP的方法和肽类似物用于治疗糖尿病的用途。

公开(公告)号：US20050272652A1

公开(公告)日：2005-12-08

申请号：US11090787

申请日：2005-03-25

申请人： Victor Gault ,  Finbarr O'Harte ,  Nigel Irwin ,  Patrick Harriott ,  Peter Flatt

发明人： Victor Gault ,  Finbarr O'Harte ,  Nigel Irwin ,  Patrick Harriott ,  Peter Flatt

IPC分类号： A61K38/00 ,  A61K38/22 ,  C07K14/575

CPC分类号： C07K14/575 ,  A61K38/00 ,  Y10T29/4935

摘要： The present invention provides peptide analogues which are antagonists of gastric inhibitory peptide (GIP). The peptides, based on GIP 1-42 include substitutions and/or modifications which have enhanced resistance to degradation by the enzyme dipeptidyl peptidase IV (DPP IV). The invention also provides a process of N terminally modifying GIP and the use of the peptide analogues for treatment of diabetes.

摘要翻译： 本发明提供作为胃抑制肽（GIP）拮抗剂的肽类似物。 基于GIP 1-42的肽包括通过酶二肽基肽酶IV（DPP IV）具有增强的降解抗性的取代和/或修饰。 本发明还提供N末端修饰GIP的方法和肽类似物用于治疗糖尿病的用途。

公开(公告)号：US20050277590A1

公开(公告)日：2005-12-15

申请号：US11090825

申请日：2005-03-25

申请人： Finbarr O'Harte ,  Peter Flatt

发明人： Finbarr O'Harte ,  Peter Flatt

IPC分类号： A61K38/00 ,  A61K38/22 ,  A61K38/26 ,  A61P5/48 ,  C07K14/575

CPC分类号： C07K14/575 ,  A61K38/00

摘要： The present invention provides peptides which stimulate the release of insulin. The peptides, based on GIP 1-42 include substitutions and/or modifications which enhance and influence secretion and/or have enhanced resistance to degradation. The invention also provides a process of N terminally modifying GIP and the use of the peptide analogues for treatment of diabetes.

摘要翻译： 本发明提供刺激胰岛素释放的肽。 基于GIP 1-42的肽包括增强和影响分泌和/或具有增强的降解抗性的取代和/或修饰。 本发明还提供N末端修饰GIP的方法和肽类似物用于治疗糖尿病的用途。

公开(公告)号：US5430188A

公开(公告)日：1995-07-04

申请号：US168034

申请日：1993-12-15

申请人： Rolf Bader ,  Peter Flatt ,  Paul Radimerski

发明人： Rolf Bader ,  Peter Flatt ,  Paul Radimerski

IPC分类号： B01J27/02 ,  A01N33/00 ,  C07B61/00 ,  C07C209/26 ,  C07C211/00 ,  C07C211/46 ,  C07C213/02 ,  C07C213/08 ,  C07C217/08 ,  C07C217/76 ,  C07C231/00 ,  C07C231/02 ,  C07C233/18 ,  C07C231/08

CPC分类号： C07C231/02 ,  C07C209/26 ,  C07C213/02

摘要： A process for the preparation of 2-alkyl-6-methyl-N(1'-methoxy-2'-propyl)-aniline by catalytic reductive alkylation wherein at least one mole equivalent of methoxyacetone is reacted with one mole equivalent of 2-alkyl-6-methyl-aniline in a liquid medium without an additional solvent, in the presence of a platinized carbon catalyst and hydrogen and in the presence of an acid cocatalyst under a hydrogen pressure of between 2.times.10.sup.5 and 1.times.10.sup.6 Pa at a temperature between 20.degree. and 80.degree. C., characterized in that the reaction mixture contains water from the beginning of the reaction and after the hydrogenation, base is added, the reaction mixture is filtered to separate the catalyst and the title compound recovered from the filtrate. The process is particularly useful for the preparation of N-substituted chloracetanilide herbicides.

摘要翻译： 通过催化还原烷基化制备2-烷基-6-甲基-N（1'-甲氧基-2'-丙基） - 苯胺的方法，其中至少一摩尔当量的甲氧基丙酮与1摩尔当量的2-烷基 -6-甲基 - 苯胺在没有另外的溶剂的液体介质中，在镀铂的碳催化剂和氢的存在下，在酸性助催化剂存在下，在2×10 5和1×10 6 Pa之间的氢气压力下，在20〜 其特征在于，反应混合物从反应开始起含有水，加氢后加入碱，将反应混合物过滤分离出催化剂和从滤液中回收的标题化合物。 该方法特别适用于制备N-取代的氯乙酰苯胺除草剂。

公开(公告)号：US20060121532A1

公开(公告)日：2006-06-08

申请号：US10528537

申请日：2003-09-19

申请人： Aine McKillop ,  Finbarr O'Harte ,  Peter Flatt

发明人： Aine McKillop ,  Finbarr O'Harte ,  Peter Flatt

IPC分类号： G01N33/53 ,  C12Q1/54

CPC分类号： G01N33/6893 ,  G01N33/74 ,  G01N2333/62 ,  G01N2400/02 ,  G01N2800/042

摘要： One of the major pathophysiological consequences of long term elevation of plasma glucose in diabetes is an increase in the non-enzymatic glycation of proteins. Contrary to expectations the present inventors have determined that individuals with well controlled short duration diabetes have particularly high concentrations of glycated insulin which decrease with increased disease severity and duration of diabetes. Further, a small proportion of apparently normal healthy individuals exhibit high glycated insulin levels in line with expected incidence of diabetes in the population. Methods of predicting the onset of diabetes and for monitoring the progression of diabetes by measuring the concentration of Glycated Insulin and the progression of diabetes are disclosed.

摘要翻译： 糖尿病血浆葡萄糖长期升高的主要病理生理后果之一是蛋白质的非酶促糖化作用的增加。 与预期相反，本发明人已经确定，具有良好控制的短期糖尿病的个体具有特别高浓度的糖化胰岛素，其随着疾病严重性和糖尿病持续时间的增加而降低。 此外，一小部分明显正常的健康个体表现出高糖化胰岛素水平，符合人群糖尿病预期发病率。 公开了通过测量糖化胰岛素的浓度和糖尿病进展来预测糖尿病发病和监测糖尿病进展的方法。