-
公开(公告)号:US20050070475A1
公开(公告)日:2005-03-31
申请号:US10950010
申请日:2004-09-24
IPC分类号: A61K38/00 , A61P31/12 , A61P31/16 , A61P31/18 , C07K14/00 , C07K14/155 , C07K14/16 , A61K38/17 , C07K14/47
CPC分类号: C07K14/005 , A61K38/00 , C12N2740/16122
摘要: 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.
摘要翻译: 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:US20050176643A1
公开(公告)日:2005-08-11
申请号:US11067556
申请日:2005-02-25
申请人: Dominique Bridon , Roger Leger , Xicai Huang , Karen Thibaudeau , Martin Robitaille , Peter Milner
发明人: Dominique Bridon , Roger Leger , Xicai Huang , Karen Thibaudeau , Martin Robitaille , Peter Milner
CPC分类号: C07K14/57545 , A61K38/00 , C07K19/00 , C07K2319/01
摘要: The present invention relates to a compound comprising a PYY peptide or a functional derivative thereof, which is coupled to a reactive group. Such a reactive group is capable of reacting on a blood component so as to form a stable covalent bond therewith. The present invention also relates to a conjugate comprising such a compound which is covalently bonded to a blood component. Moreover, the invention also relates to a method of enhancing, in a patient, the anti-obesity activity of a PYY peptide or functional derivative thereof.
摘要翻译: 本发明涉及包含与反应性基团偶联的PYY肽或其功能性衍生物的化合物。 这样的反应性基团能够对血液成分进行反应,与其形成稳定的共价键。 本发明还涉及包含共价键合到血液成分上的化合物的缀合物。 此外,本发明还涉及在患者中增强PYY肽或其功能性衍生物的抗肥胖活性的方法。
-
公开(公告)号:US20050187159A1
公开(公告)日:2005-08-25
申请号:US11066697
申请日:2005-02-25
申请人: Dominique Bridon , Alan Ezrin , Peter Milner , Darren Holmes , Karen Thibaudeau
发明人: Dominique Bridon , Alan Ezrin , Peter Milner , Darren Holmes , Karen Thibaudeau
CPC分类号: C07K19/00
摘要: A method for protecting a peptide from peptidase activity in vivo, the peptide being composed of between 2 and 50 amino acids and having a C-terminus and an N-terminus and a C-terminus amino acid and an N-terminus amino acid is described. In the first step of the method, the peptide is modified by attaching a reactive group to the C-terminus amino acid, to the N-terminus amino acid, or to an amino acid located between the N-terminus and the C-terminus, such that the modified peptide is capable of forming a covalent bond in vivo with a reactive functionality on a blood component. In the next step, a covalent bond is formed between the reactive group and a reactive functionality on a blood component to form a peptide-blood component conjugate, thereby protecting said peptide from peptidase activity. The final step of the method involves the analyzing of the stability of the peptide-blood component conjugate to assess the protection of the peptide from peptidase activity.
-
公开(公告)号:US20060082891A1
公开(公告)日:2006-04-20
申请号:US10501273
申请日:2003-01-10
申请人: Peter Milner , Kirsten Milner
发明人: Peter Milner , Kirsten Milner
CPC分类号: B60J1/02
摘要: A glazing element (12) for an opening defined by opaque boundaries (13) has an edge region (E) shaped to divert light passing through it in a sense such as to enlarge the field of view through the opening. For this purpose the bounding surfaces (33, 34) of the element (12) diverge towards the edge thereof in the edge region (E). The same effect can be achieved by an element (25) adhered to or otherwise held in position to the surface of the element (12) in the edge region (E).
摘要翻译: 用于由不透明边界(13)限定的开口的玻璃元件(12)具有形状成使透过它的光偏转的边缘区域(E),从而通过开口扩大视场。 为此,元件(12)的边界表面(33,34)在边缘区域(E)中朝向其边缘发散。 通过附接到边缘区域(E)中的元件(12)的表面上或以其他方式保持在适当位置的元件(25)可以实现相同的效果。
-
公开(公告)号:US20060247227A1
公开(公告)日:2006-11-02
申请号:US10564931
申请日:2004-07-16
申请人: James Bailey , Gordon Bruton , Anthony Huxley , Peter Milner , Barry Orlek
发明人: James Bailey , Gordon Bruton , Anthony Huxley , Peter Milner , Barry Orlek
IPC分类号: A61K31/55 , A61K31/454 , C07D403/02 , C07D401/02
CPC分类号: C07D401/14 , C07D211/46 , C07D413/14
摘要: The present invention relates to novel piperidine ether derivatives having affinity for the histamine H3 receptor processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.
摘要翻译: 本发明涉及对组胺H3受体制备方法具有亲和力的新型哌啶醚衍生物,含有它们的组合物及其在治疗神经和精神疾病中的用途。
-
6.
公开(公告)号:US20060047000A1
公开(公告)日:2006-03-02
申请号:US11167925
申请日:2005-06-27
申请人: Pascal Druzgala , Peter Milner , Jurg Pfister
发明人: Pascal Druzgala , Peter Milner , Jurg Pfister
IPC分类号: A61K31/426 , A61K31/42 , A61K31/198 , A61K31/192
CPC分类号: C07D417/06 , C07D401/04 , C07D413/04 , C07J3/005 , C07J9/00
摘要: 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.
-
公开(公告)号:US20070142164A1
公开(公告)日:2007-06-21
申请号:US10579183
申请日:2004-11-11
申请人: Peter Milner
发明人: Peter Milner
IPC分类号: F16H15/38
CPC分类号: F16H15/52
摘要: A continuously variable transmission device has planetary members (23) in rolling contact with radially inner and outer races (12, 14; 36, 37) each comprising axially spaced relatively axially movable parts, and control means (18) for determining the axial separation of the parts (12, 14) of one of the two races, in which the planetary members (23) are connected for drive transmission to an input or output member (30) of the transmission device by connection means which allows the radial position of the planets to vary in response to variation in the axial separation of the parts (12, 14) of the said one of the two races (37), and in which the generatrix of the curved surface (70, 71) of at least one of the races (37) and/or planetary members (23) is non-circular.
摘要翻译: 一种无级变速传动装置具有与径向内径和外径(12,14; 36,37)滚动接触的行星构件(23),每个径向内和外座圈(12,14; 36,37)均包括轴向间隔开的相对轴向可移动部件,以及控制装置(18),用于确定 两个座圈中的一个的部分(12,14),其中行星构件(23)被连接以通过连接装置通过连接装置驱动传动到传动装置的输入或输出构件(30),所述连接装置允许 行星根据两个座圈(37)中的一个的部件(12,14)的轴向间隔的变化而变化,并且其中曲面(70,71)的母线中的至少一个 种族(37)和/或行星构件(23)是非圆形的。
-
公开(公告)号:US20050037997A9
公开(公告)日:2005-02-17
申请号:US10251522
申请日:2002-09-20
申请人: Pascal Druzgala , Peter Milner , Jurg Pfister
发明人: Pascal Druzgala , Peter Milner , Jurg Pfister
IPC分类号: A61P3/10 , C07D261/12 , C07D277/20 , C07D277/34 , C07D311/70 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07J3/00 , C07J1/00 , A61K31/58 , A61K31/69 , C07J17/00 , C07J43/00
CPC分类号: C07D277/20 , C07D261/12 , C07D277/34 , C07D311/70 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07J3/00 , Y10S514/866
摘要: 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.
-
公开(公告)号:US6087375A
公开(公告)日:2000-07-11
申请号:US330744
申请日:1999-06-11
申请人: Dominique P. Bridon , Alan Ezrin , Peter Milner
发明人: Dominique P. Bridon , Alan Ezrin , Peter Milner
IPC分类号: C12N5/06 , A61K38/00 , A61K47/48 , A61P7/02 , C07K5/068 , C07K14/765 , C07K16/18 , C07D215/04 , A61K31/4709 , C07D215/06
CPC分类号: A61K47/48007 , A61K47/48238 , A61K47/48384
摘要: Novel compounds comprising chemically reactive intermediates which can react with available reactive functionalities on blood components to form covalent linkages, where the resulting covalently-bound conjugates are found to have thrombin inhibition activity are provided. Specifically, the thrombin inhibitor compounds of the present invention are derivatives of the known thrombin inhibitor argatroban, which can be covalently linked to chemically reactive functionalities on various blood components. The conjugated thrombin inhibitors thereby have extended lifetimes in the bloodstream, as compared to the unconjugated parent drug, and are, therefore, capable of maintaining thrombin inhibitory activity for extended periods of time as compared to the unconjugated parent drug. Also provided herein are methods for inhibiting thrombin activity in vivo comprising administering to the bloodstream of a mammalian host the novel compounds of the present invention.
摘要翻译: 提供了包含化学反应中间体的新型化合物,其可与血液成分上的可用反应性官能团反应以形成共价键,其中发现所得的共价结合的缀合物具有凝血酶抑制活性。 具体地,本发明的凝血酶抑制剂化合物是已知的凝血酶抑制剂阿加曲班的衍生物,其可以与各种血液成分上的化学反应性官能团共价连接。 与未缀合的母体药物相比,缀合的凝血酶抑制剂在血液中的寿命延长,因此与未缀合的母体药物相比,能够延长凝血酶抑制活性。 本文还提供用于抑制体内凝血酶活性的方法,包括向哺乳动物宿主的血流施用本发明的新化合物。
-
公开(公告)号:US20240115535A1
公开(公告)日:2024-04-11
申请号:US18275972
申请日:2022-02-07
IPC分类号: A61K31/201 , A61P25/28 , G01N33/50 , G01N33/555
CPC分类号: A61K31/201 , A61P25/28 , G01N33/5044 , G01N33/555
摘要: 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.
-
-
-
-
-
-
-
-
-