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1. 发明授权

US08309549B2 Compositions for modulating a kinase cascade and methods of use thereof 有权
标题翻译：用于调节激酶级联的组合物及其使用方法
公开(公告)号：US08309549B2
公开(公告)日：2012-11-13
申请号：US13094679
申请日：2011-04-26
申请人： David G. Hangauer, Jr. , Debasis Patra , Jeremy A. Cody , Grant J. Palmer , Paul K. Isbester , Jonathon Salsbury
发明人： David G. Hangauer, Jr. , Debasis Patra , Jeremy A. Cody , Grant J. Palmer , Paul K. Isbester , Jonathon Salsbury
IPC分类号： A61K31/5377 , C07D413/12
CPC分类号： C07D213/56 , A61K31/44 , C07B2200/13 , C07D213/59 , C07D413/12
摘要： The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.
摘要翻译：本发明涉及包含2-（5-（4-（2-吗啉代乙氧基）苯基）吡啶-2-基）-N-苄基乙酰胺及其甲磺酸盐和二盐酸盐的组合物。本发明提供了合成2-（5-（4-（2-吗啉代乙氧基）苯基）吡啶-2-基）-N-苄基乙酰胺及其甲磺酸盐和二盐酸盐的有效方法和调节一种或多种组分的方法使用本发明组合物的激酶级联。本发明还提供2-（5-（4-（2-吗啉代乙氧基）苯基）吡啶-2-基）-N-苄基乙酰胺（A型）的甲磺酸盐的新型多晶型物，其特征在于独特的X射线衍射图和差示扫描量热法，以及独特的晶体结构。

2. 发明授权

US08293739B2 Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof 有权
标题翻译：制备用于调节激酶级联的组合物的方法及其使用方法
公开(公告)号：US08293739B2
公开(公告)日：2012-10-23
申请号：US13094667
申请日：2011-04-26
申请人： David G. Hangauer, Jr. , Daniel Coughlin , Jonathan Gale , Jeremy A. Cody , Debasis Patra , Grant J. Palmer , Paul K. Isbester , Jonathon Salsbury
发明人： David G. Hangauer, Jr. , Daniel Coughlin , Jonathan Gale , Jeremy A. Cody , Debasis Patra , Grant J. Palmer , Paul K. Isbester , Jonathon Salsbury
IPC分类号： A61K31/535
CPC分类号： C07D413/12
摘要： The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. More specifically, the invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy) phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention.
摘要翻译：本发明涉及包含2-（5-（4-（2-吗啉代乙氧基）苯基）吡啶-2-基）-N-苄基乙酰胺及其甲磺酸盐和二盐酸盐的组合物。更具体地说，本发明提供了合成2-（5-（4-（2-吗啉代乙氧基）苯基）吡啶-2-基）-N-苄基乙酰胺及其甲磺酸盐和二盐酸盐的有效方法和调节一种或使用本发明组合物的激酶级联的更多成分。

3. 发明授权

US08288539B2 Dipeptidyl peptidase inhibitors 有权
公开(公告)号：US08288539B2
公开(公告)日：2012-10-16
申请号：US11929482
申请日：2007-10-30
申请人： Jun Feng , Stephen L. Gwaltney , Jeffrey A. Stafford , Zhiyuan Zhang , Bruce J. Elder , Paul K. Isbester , Grant J. Palmer , Jonathon S. Salsbury , Luckner G. Ulysse
发明人： Jun Feng , Stephen L. Gwaltney , Jeffrey A. Stafford , Zhiyuan Zhang , Bruce J. Elder , Paul K. Isbester , Grant J. Palmer , Jonathon S. Salsbury , Luckner G. Ulysse
IPC分类号： C07D239/54 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , A61K31/505 , A61K31/506 , A61P3/10 , A61P19/02 , A61P35/00
CPC分类号： C07D403/04 , C07D239/545 , C07D401/04 , C07D401/14 , C07D403/12 , C07D409/14
摘要： Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C═NR9; and each L, X, R1, R2, and R3 are as defined herein.

4. 发明申请

US20110184178A1 POLYMORPHS OF 5-(3-(ETHYLSULFONYL)PHENYL)-3,8-DIMETHYL-N-(1-METHYLPIPERIDIN-4-YL)-9H-PYRIDO[2,3-B]INDOLE-7-CARBOXAMIDE AND METHODS OF USE THEREFOR 审中-公开
标题翻译： 5-（3-（乙基磺酰基）苯基）-3,8-二甲基-N-（1-甲基哌啶-4-基）-9H-吡啶并[2,3-b]吲哚-7-羧酸的聚合物及其使用方法其他
公开(公告)号：US20110184178A1
公开(公告)日：2011-07-28
申请号：US12988627
申请日：2009-04-14
申请人： Paul Isbester , Bingidimi I. Mobele , Grant J. Palmer , Jonathon S. Salsbury , Luckner Ulysse
发明人： Paul Isbester , Bingidimi I. Mobele , Grant J. Palmer , Jonathon S. Salsbury , Luckner Ulysse
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The invention relates to polymorphic forms of 5-(3-(ethylsulfonyl)phenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9h-pyrido[2,3-b]indole-7-carboxamide (referred to herein as Compound I), which has the formula: The invention also relates to compositions thereof and methods for the preparation of the polymorphs of Compound I, and kits and articles of manufacture of the compositions, and methods of using the compositions to treat various diseases.
摘要翻译：本发明涉及5-（3-（乙基磺酰基）苯基）-3,8-二甲基-N-（1-甲基哌啶-4-基）-9H-吡啶并[2,3-b]吲哚-7-基）其具有下式：本发明还涉及其组合物和制备化合物I的多晶型物的方法，以及组合物的试剂盒和制品，以及使用组合物的方法治疗各种疾病。

5. 发明授权

US07812050B2 Polymorphic form of fluoro-7-(2,2,2-trifluoroethoxy) phenoxathiin-10,10-dioxide 有权
标题翻译：氟-7-（2,2,2-三氟乙氧基）苯氧硫蛋白-10,10-二氧化物的多晶型
公开(公告)号：US07812050B2
公开(公告)日：2010-10-12
申请号：US11773892
申请日：2007-07-05
申请人： Elisabeth C. A. Brot , Daniel K. Keefe, Jr. , Brian P. Haney , Nigel Metcalfe , Grant J. Palmer , Paul K. Isbester
发明人： Elisabeth C. A. Brot , Daniel K. Keefe, Jr. , Brian P. Haney , Nigel Metcalfe , Grant J. Palmer , Paul K. Isbester
IPC分类号： A61K31/39 , C07D327/08
CPC分类号： C07D327/08
摘要： Provided herein is a new form of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathin 10,10-dioxide, which demonstrates higher stability relative to other forms of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin-10,10-dioxide. In particular, this new form affords less dosage critical administration of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathin 10,10-dioxide relative to other forms. The new solid form of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin-10,10-dioxide has been determined and is provided herein. This new solid form of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin-10,10-dioxide can be characterized by any of a number of its properties, including, but not limited to, melting point, differential scanning calorimetry, infrared spectroscopic spectrum or portions thereof, solubility, methods and conditions under which this form is prepared, and/or precipitated from solution, and, when in crystalline form, the crystalline form can be characterized according to the diffraction pattern or portions thereof.
摘要翻译：本文提供了一种新形式的3-氟-7-（2,2,2-三氟乙氧基）吩恶嗪素10,10-二氧化物，其相对于其它形式的3-氟-7-（2,2,2' - 三氟乙氧基）苯氧硫蛋白-10,10-二氧化物。特别地，相对于其它形式，这种新形式对3-氟-7-（2,2,2-三氟乙氧基）吩恶嗪素10,10-二氧化物的剂量临界施用较少。已经确定了新的固体形式的3-氟-7-（2,2,2-三氟乙氧基）苯氧硫杂质-10,10-二氧化物，并在此提供。这种新的固体形式的3-氟-7-（2,2,2-三氟乙氧基）苯氧硫杂-10,10-二氧化物可用其许多特性来表征，包括但不限于熔点差扫描量热法，红外光谱或其部分，溶解度，制备这种形式的方法和条件和/或从溶液中沉淀出来，并且当以结晶形式时，可以根据衍射图案或其部分来表征结晶形式。

6. 发明授权

US07807689B2 Dipeptidyl peptidase inhibitors 有权
标题翻译：二肽基肽酶抑制剂
公开(公告)号：US07807689B2
公开(公告)日：2010-10-05
申请号：US11080992
申请日：2005-03-15
申请人： Zhiyuan Zhang , Bruce J. Elder , Paul K. Isbester , Grant J. Palmer , Luckner G. Ulysse
发明人： Zhiyuan Zhang , Bruce J. Elder , Paul K. Isbester , Grant J. Palmer , Luckner G. Ulysse
IPC分类号： C07D401/04 , A61K31/506 , A61P3/10 , A61P35/00
CPC分类号： C07D403/04 , C07D239/545 , C07D401/04 , C07D401/14 , C07D403/12 , C07D409/14
摘要： The present invention provides a compound of the formula: or stereoisomers or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, articles of manufacture comprising the same, and methods of using the same.
摘要翻译：本发明提供下式的化合物或其立体异构体或其药学上可接受的盐，其药物组合物，包含其的制品及其使用方法。

7. 发明授权

US07781584B2 Dipeptidyl peptidase inhibitors 有权
标题翻译：二肽基肽酶抑制剂
公开(公告)号：US07781584B2
公开(公告)日：2010-08-24
申请号：US11929549
申请日：2007-10-30
申请人： Jun Feng , Stephen L. Gwaltney , Jeffrey A. Stafford , Zhiyuan Zhang , Bruce J. Elder , Paul K. Isbester , Grant J. Palmer , Jonathon S. Salsbury , Luckner G. Ulysse
发明人： Jun Feng , Stephen L. Gwaltney , Jeffrey A. Stafford , Zhiyuan Zhang , Bruce J. Elder , Paul K. Isbester , Grant J. Palmer , Jonathon S. Salsbury , Luckner G. Ulysse
IPC分类号： C07D239/54 , A61K31/505 , A61P19/02
CPC分类号： C07D403/04 , C07D239/545 , C07D401/04 , C07D401/14 , C07D403/12 , C07D409/14
摘要： Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C═NR9; and each L, X, R1, R2, and R3 are as defined herein.
摘要翻译：提供化合物，药物，试剂盒和方法用于DPP-IV和其它S9蛋白酶，其包含包含：其中M为N或CR 4的化合物; Q1和Q2各自独立地选自CO，SO，SO2和C≡NR9; 并且每个L，X，R 1，R 2和R 3如本文所定义。

8. 发明申请

US20090275750A1 DIPEPTIDYL PEPTIDASE INHIBITORS 有权
标题翻译： DIPEPTIDYL PEPTIDASE抑制剂
公开(公告)号：US20090275750A1
公开(公告)日：2009-11-05
申请号：US12066769
申请日：2006-09-15
申请人： Jun Feng , Stephen L. Gwaltney , Jeffrey A. Stafford , Zhiyuan Zhang , Paul R. Brodluahrer , Bruce Elder , Paul Isbester , Richard S. Fornicola , Philip B. Kisanga , Bingidimi I. Mobele , Grant J. Palmer , Maxwell M. Reeve , Jonathon S. Salsbury , Luckner Ulysse , Sripathy Venkatraman
发明人： Jun Feng , Stephen L. Gwaltney , Jeffrey A. Stafford , Zhiyuan Zhang , Paul R. Brodluahrer , Bruce Elder , Paul Isbester , Richard S. Fornicola , Philip B. Kisanga , Bingidimi I. Mobele , Grant J. Palmer , Maxwell M. Reeve , Jonathon S. Salsbury , Luckner Ulysse , Sripathy Venkatraman
IPC分类号： C07D403/04 , C07D401/04
CPC分类号： C07D239/553 , C07D239/545 , C07D401/04 , C07D401/14 , C07D403/12 , C07D409/14
摘要： Methods of making compounds of the formula (I) wherein the variables are as defined herein. Also, methods of making compounds that may be used to inhibit dipeptidyl peptidase.
摘要翻译：制备式（I）化合物的方法，其中变量如本文所定义。另外，制备可用于抑制二肽基肽酶的化合物的方法。

9. 发明申请

US20080177064A1 DIPEPTIDYL PEPTIDASE INHIBITORS 有权
公开(公告)号：US20080177064A1
公开(公告)日：2008-07-24
申请号：US11928944
申请日：2007-10-30
申请人： Jun Feng , Stephen L. Gwaltney , Jeffrey A. Stafford , Zhiyuan Zhang , Bruce J. Elder , Paul K. Isbester , Grant J. Palmer , Jonathon S. Salsbury , Luckner G. Ulysse
发明人： Jun Feng , Stephen L. Gwaltney , Jeffrey A. Stafford , Zhiyuan Zhang , Bruce J. Elder , Paul K. Isbester , Grant J. Palmer , Jonathon S. Salsbury , Luckner G. Ulysse
IPC分类号： C07D223/02 , C07D239/24
CPC分类号： C07D403/04 , C07D239/545 , C07D401/04 , C07D401/14 , C07D403/12 , C07D409/14
摘要： Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C═NR9; and each L, X, R1, R2, and R3 are as defined herein.

10. 发明申请

US20110201612A1 Compositions for Modulating a Kinase Cascade and Methods of Use Thereof 有权
标题翻译：用于调节激酶级联的组合物及其使用方法
公开(公告)号：US20110201612A1
公开(公告)日：2011-08-18
申请号：US13094679
申请日：2011-04-26
申请人： David G. Hangauer, JR. , Debasis Patra , Jeremy A. Cody , Grant J. Palmer , Paul K. Isbester , Jonathon Salsbury
发明人： David G. Hangauer, JR. , Debasis Patra , Jeremy A. Cody , Grant J. Palmer , Paul K. Isbester , Jonathon Salsbury
IPC分类号： A61K31/5377 , C07D413/12 , A61P19/00 , A61P35/00 , A61P9/00 , A61P3/00 , A61P27/00 , A61P25/04
CPC分类号： C07D213/56 , A61K31/44 , C07B2200/13 , C07D213/59 , C07D413/12
摘要： The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.
摘要翻译：本发明涉及包含2-（5-（4-（2-吗啉代乙氧基）苯基）吡啶-2-基）-N-苄基乙酰胺及其甲磺酸盐和二盐酸盐的组合物。本发明提供了合成2-（5-（4-（2-吗啉代乙氧基）苯基）吡啶-2-基）-N-苄基乙酰胺及其甲磺酸盐和二盐酸盐的有效方法和调节一种或多种组分的方法使用本发明组合物的激酶级联。本发明还提供2-（5-（4-（2-吗啉代乙氧基）苯基）吡啶-2-基）-N-苄基乙酰胺（A型）的甲磺酸盐的新型多晶型物，其特征在于独特的X射线衍射图和差示扫描量热法，以及独特的晶体结构。

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