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1. 发明授权

US08034787B2 Enzyme-cleavable prodrug compounds 有权
标题翻译：可酶切的前药化合物
公开(公告)号：US08034787B2
公开(公告)日：2011-10-11
申请号：US12228636
申请日：2008-08-14
申请人： Vincent Dubois , Ann Marie Fernandez , Sanjeev Gangwar , Evan Lewis , Thomas J. Lobl , Matthew H. Nieder , Lesley B. Pickford , Andre Trouet , Geoffrey T. Yarranton
发明人： Vincent Dubois , Ann Marie Fernandez , Sanjeev Gangwar , Evan Lewis , Thomas J. Lobl , Matthew H. Nieder , Lesley B. Pickford , Andre Trouet , Geoffrey T. Yarranton
IPC分类号： A61K38/06 , A61P35/00 , C07K16/28
CPC分类号： A61K47/65
摘要： The prodrug of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by the enzyme Thimet oligopeptidase, or TOP. Also disclosed are methods of designing prodrugs by utilizing TOP-cleavable sequences within the conjugate and methods of treating patients with prodrugs of the invention.
摘要翻译：本发明的前药是治疗剂的修饰形式，并且包含治疗剂，寡肽，稳定基团和任选的连接基团。前药可通过Thimet寡肽酶或TOP切割。还公开了通过利用缀合物内的TOP-可切割序列和用本发明的前药治疗患者的方法来设计前药的方法。

2. 发明申请

US20090110753A1 Enzyme-cleavable prodrug compounds 有权
公开(公告)号：US20090110753A1
公开(公告)日：2009-04-30
申请号：US12228636
申请日：2008-08-14
申请人： Vincent Dubois , Anne Marie Fernandez , Sanjeev Gangwar , Evan Lewis , Thomas J. Lobl , Matthew H. Nieder , Lesley B. Pickford , Andre Trouet , Geoffrey T. Yarranton
发明人： Vincent Dubois , Anne Marie Fernandez , Sanjeev Gangwar , Evan Lewis , Thomas J. Lobl , Matthew H. Nieder , Lesley B. Pickford , Andre Trouet , Geoffrey T. Yarranton
IPC分类号： A61K33/24 , A61K47/42 , A61K31/437 , A61K31/357 , A61K31/4985 , A61K31/337 , A61K31/704 , A61K31/4353 , A61K31/282 , A61P35/00 , A61K47/48 , A61K38/13 , A61K31/47 , A61K31/407 , A61K31/506 , A61K31/662 , A61K31/513 , A61K31/522 , A61K31/675 , A61K31/7052
CPC分类号： A61K47/65
摘要： The prodrug of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by the enzyme Thimet oligopeptidase, or TOP. Also disclosed are methods of designing prodrugs by utilizing TOP-cleavable sequences within the conjugate and methods of treating patients with prodrugs of the invention.

3. 发明授权

US07425541B2 Enzyme-cleavable prodrug compounds 有权
标题翻译：可酶切的前药化合物
公开(公告)号：US07425541B2
公开(公告)日：2008-09-16
申请号：US09879442
申请日：2001-06-11
申请人： Vincent Dubois , Ann Marie Fernandez , Sanjeev Gangwar , Evan Lewis , Thomas J. Lobl , Matthew H. Nieder , Lesley B. Pickford , Andre Trouet , Geoffrey Yarranton
发明人： Vincent Dubois , Ann Marie Fernandez , Sanjeev Gangwar , Evan Lewis , Thomas J. Lobl , Matthew H. Nieder , Lesley B. Pickford , Andre Trouet , Geoffrey Yarranton
IPC分类号： A61K38/07 , A61K38/08 , A61K38/10 , A61K38/16 , C07K7/08 , C07K7/04 , C07K5/10 , C07K1/00
CPC分类号： A61K47/65
摘要： The prodrug of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by the enzyme Thimet oligopeptidase, or TOP. Also disclosed are methods of designing prodrugs by utilizing TOP-cleavable sequences within the conjugate and methods of treating patients with prodrugs of the invention.
摘要翻译：本发明的前药是治疗剂的修饰形式，并且包含治疗剂，寡肽，稳定基团和任选的连接基团。前药可通过Thimet寡肽酶或TOP切割。还公开了通过利用缀合物内的TOP-可切割序列和用本发明的前药治疗患者的方法来设计前药的方法。

4. 发明申请

US20130303465A1 Cylodextrin Complexation Methods for Formulating Peptide Proteasome Inhibitors 审中-公开
公开(公告)号：US20130303465A1
公开(公告)日：2013-11-14
申请号：US13614599
申请日：2012-09-13
申请人： Evan Lewis , Peter Shwonek , Sean Dalziel , Mouhannad Jumaa
发明人： Evan Lewis , Peter Shwonek , Sean Dalziel , Mouhannad Jumaa
IPC分类号： A61K38/07 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/00 , A61P1/04 , A61P17/06 , A61P3/10
CPC分类号： B82Y5/00 , A61K38/00 , A61K47/6951
摘要： This disclosure provides methods for formulating compositions comprising one or more peptide proteasome inhibitors and a cyclodextrin, particularly a substituted cyclodextrin. Such methods substantially increase the solubility and stability of these proteasome inhibitors and facilitate both their manufacture and administration.

5. 发明申请

US20060088471A1 Compounds for enzyme inhibition 审中-公开
标题翻译：用于酶抑制的化合物
公开(公告)号：US20060088471A1
公开(公告)日：2006-04-27
申请号：US11254541
申请日：2005-10-19
申请人： Mark Bennett , Tonia Buchholz , Susan Demo , Guy Laidig , Evan Lewis , Mark Smyth
发明人： Mark Bennett , Tonia Buchholz , Susan Demo , Guy Laidig , Evan Lewis , Mark Smyth
IPC分类号： A61K51/00 , C07K16/46 , C07K5/04 , C07K5/06
CPC分类号： C07K5/0812 , C07K1/13 , C07K5/06165 , C07K5/0806 , C07K5/0808 , C07K5/1016 , C12Q1/34 , C12Q1/37 , G01N33/573 , G01N2333/976 , G01N2500/00
摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus, such as a detectable label. Along with therapeutic utilities, these peptide based compounds can be used in assays useful for screening, monitoring, diagnostic and/or dosing purposes.
摘要翻译：包括含杂原子的三元环的基于肽的化合物有效地选择性地抑制N末端亲核试剂（Ntn）水解酶的比活性。具有多种活性的那些Ntn的活性可被所描述的化合物差别地抑制。例如，本发明化合物可以选择性地抑制20S蛋白酶体的胰凝乳蛋白酶样和PGPH活性。基于肽的化合物包括至少三种肽单元，环氧化物或氮丙啶，并且在N末端官能化，例如可检测标记。与治疗用途一起，这些基于肽的化合物可用于用于筛选，监测，诊断和/或给药目的的测定中。

6. 发明申请

US20130303482A1 Cylodextrin Complexation Methods for Formulating Peptide Proteasome Inhibitors 审中-公开
标题翻译：用于配制肽蛋白酶体抑制剂的环糊精复合方法
公开(公告)号：US20130303482A1
公开(公告)日：2013-11-14
申请号：US13614829
申请日：2012-09-13
申请人： Evan Lewis , Peter Shwonek , Sean Dalziel , Mouhannad Jumaa
发明人： Evan Lewis , Peter Shwonek , Sean Dalziel , Mouhannad Jumaa
IPC分类号： A61K31/724 , A61P35/00
CPC分类号： B82Y5/00 , A61K38/00 , A61K47/6951
摘要： This disclosure provides methods for formulating compositions comprising one or more peptide proteasome inhibitors and a cyclodextrin, particularly a substituted cyclodextrin. Such methods substantially increase the solubility and stability of these proteasome inhibitors and facilitate both their manufacture and administration.
摘要翻译：本公开提供了用于配制包含一种或多种肽蛋白酶体抑制剂和环糊精，特别是取代的环糊精的组合物的方法。这些方法大大提高了这些蛋白酶体抑制剂的溶解度和稳定性，并促进了它们的制备和给药。

7. 发明申请

US20070261840A1 Exit window milling assembly with improved restraining force 有权
标题翻译：出口窗铣削组件具有改进的约束力
公开(公告)号：US20070261840A1
公开(公告)日：2007-11-15
申请号：US11434358
申请日：2006-05-15
申请人： Calvin Stowe , Evan Lewis , Mohan Soni , Daniel Hart
发明人： Calvin Stowe , Evan Lewis , Mohan Soni , Daniel Hart
IPC分类号： E21B23/03
CPC分类号： E21B29/06
摘要： An assembly for milling a window in a tubular features a layout that keeps a restorative force normal to the whipstock slope acting on the window mill to help it track the whipstock ramp long enough for making an exit at the desired location. A string mill assembly is made long enough to allow such a restorative force to be created on the window mill as it advances down the ramp. The bearing or cutting structures on the string mill are positioned with respect to the window mill so that either the top of the string mill or at least the first bearing structure above the window mill presents at the top of the window as the window mill arrives at the position where it is desired that it make an exit. The lower bearing structure of the string mill also preferably has a rounded profile to facilitate its entrance on to the whipstock ramp without getting in a bind on the tubular wall adjacent the top of the window.
摘要翻译：用于铣削管道中的窗口的组件具有一种布局，其将恢复力保持垂直于作用在窗玻璃上的造斜斜坡，以帮助其跟踪造斜斜坡，足以使其在所需位置处出口。弦碾机组件被制成足够长的时间，以允许在窗碾机上沿着斜坡进入时产生这样的修复力。串磨机上的轴承或切割结构相对于窗口磨机定位，使得当研磨机到达时，弦磨机的顶部或窗玻璃上方的至少第一轴承结构呈现在窗口的顶部希望它退出的位置。串磨机的下轴承结构也优选具有圆形轮廓，以便于其进入造斜坡坡道而不会在邻近窗口顶部的管状壁上结合。

8. 发明申请

US20060128611A1 Composition for enzyme inhibition 有权
标题翻译：用于酶抑制的组合物
公开(公告)号：US20060128611A1
公开(公告)日：2006-06-15
申请号：US11299265
申请日：2005-12-07
申请人： Evan Lewis , Mark Ho , Fabiana Fonseca
发明人： Evan Lewis , Mark Ho , Fabiana Fonseca
IPC分类号： A61K38/14 , A61K31/724 , A61K38/05
CPC分类号： A61K31/336 , A61K9/0019 , A61K9/19 , A61K31/396 , A61K31/724 , A61K38/14 , A61K47/40 , C07K5/0812 , Y02A50/412 , A61K2300/00
摘要： Compositions comprising one or more practically insoluble proteasome inhibitors and a cyclodextrin, particularly a substituted cyclodextrin, substantially increase the solubility of these proteasome inhibitors and facilitate their administration. Such compositions optionally comprise a buffer. Methods of treatment using such compositions are also disclosed.
摘要翻译：包含一种或多种实际上不溶的蛋白酶体抑制剂和环糊精，特别是取代的环糊精的组合物显着增加了这些蛋白酶体抑制剂的溶解性并促进了它们的给药。这种组合物任选地包含缓冲剂。还公开了使用这种组合物的治疗方法。

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