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1. 发明申请

WO2010135429A3 COMPOSITIONS FOR MODULATING A KINASE CASCADE AND MEHTODS OF USE THEREOF 审中-公开
标题翻译：用于调节激酶的组合物及其使用方法
公开(公告)号：WO2010135429A3
公开(公告)日：2011-03-31
申请号：PCT/US2010035408
申请日：2010-05-19
申请人： KINEX PHARMACEUTICALS LLC , CODY JEREMY A , HANGAUER DAVID G JR , ISBESTER PAUL K , PALMER GRANT J , PATRA DEBASIS , SALSBURY JONATHON
发明人： CODY JEREMY A , HANGAUER DAVID G JR , ISBESTER PAUL K , PALMER GRANT J , PATRA DEBASIS , SALSBURY JONATHON
IPC分类号： C07D413/10 , A61K31/5355 , A61P3/04 , A61P35/00 , 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)-?/-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)-?/-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)-iV- 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）-β-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）-β-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的激酶级联，使用本发明的组合物。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（形式A）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. 发明申请

WO2010135429A2 COMPOSITIONS FOR MODULATING A KINASE CASCADE AND MEHTODS OF USE THEREOF 审中-公开
标题翻译：用于调节激酶的组合物及其使用方法
公开(公告)号：WO2010135429A2
公开(公告)日：2010-11-25
申请号：PCT/US2010/035408
申请日：2010-05-19
申请人： KINEX PHARMACEUTICALS, LLC , CODY, Jeremy, A. , HANGAUER, David, G., Jr. , ISBESTER, Paul, K. , PALMER, Grant, J. , PATRA, Debasis , SALSBURY, Jonathon
发明人： CODY, Jeremy, A. , HANGAUER, David, G., Jr. , ISBESTER, Paul, K. , PALMER, Grant, J. , PATRA, Debasis , SALSBURY, Jonathon
IPC分类号： C07D413/10 , C07D413/12 , A61K31/5355 , A61P35/00 , A61P3/04
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)-Λ/-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)-Λ/-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)-iV- 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）-β-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）-β-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的组合物的激酶级联。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（形式A）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。

3. 发明申请

WO2008008273A1 POLYMORPHIC FORM OF FLUORO-7-(2,2,2-TRIFLUOROETHOXY) PHENOXATHIIN-10,10-DIOXIDE 审中-公开
标题翻译：氟代-7-（2,2,2-三氟乙酰）苯氧基-10,10-二氧化物的多晶型
公开(公告)号：WO2008008273A1
公开(公告)日：2008-01-17
申请号：PCT/US2007/015533
申请日：2007-07-05
申请人： CENERX BIOPHARMA, INC. , BROT, Elisabeth C., A. , KEEFE, Daniel, K., Jr. , HANEY, Brian, P. , METCALFE, Nigel , PALMER, Grant, J. , ISBESTER, Paul, K.
发明人： BROT, Elisabeth C., A. , KEEFE, Daniel, K., Jr. , HANEY, Brian, P. , METCALFE, Nigel , PALMER, Grant, J. , ISBESTER, Paul, K.
IPC分类号： C07D327/08 , A61K31/38 , A61P25/00
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。

4. 发明申请

WO2007035629A2 DIPEPTIDYL PEPTIDASE INHIBITORS 审中-公开
标题翻译： DIPEPTIDYL PEPTIDASE抑制剂
公开(公告)号：WO2007035629A2
公开(公告)日：2007-03-29
申请号：PCT/US2006036276
申请日：2006-09-15
申请人： TAKEDA PHARMACEUTICAL , FENG JUN , GWALTNEY STEPHEN L , STAFFORD JEFFREY A , ZHANG ZHIYUAN , ELDER BRUCE J , ISBESTER PAUL K , PALMER GRANT J , SALSBURY JONATHON S , ULYSSE LUCKNER
发明人： FENG JUN , GWALTNEY STEPHEN L , STAFFORD JEFFREY A , ZHANG ZHIYUAN , ELDER BRUCE J , ISBESTER PAUL K , PALMER GRANT J , SALSBURY JONATHON S , ULYSSE LUCKNER
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。

5. 发明申请

WO2011140268A2 DUAL MODE HEMODIALYSIS MACHINE 审中-公开
标题翻译：双模式HEMODIALYSIS MACHINE
公开(公告)号：WO2011140268A2
公开(公告)日：2011-11-10
申请号：PCT/US2011/035252
申请日：2011-05-04
申请人： C-TECH BIOMEDICAL, INC. , PALMER, Grant
发明人： PALMER, Grant
IPC分类号： A61M1/14 , A61M1/34 , A61M1/10
CPC分类号： A61M1/1696 , A61M1/1656 , A61M1/1668 , A61M1/287 , A61M1/3646
摘要： A compact portable dual mode hemodialysis machine system is provided. The system includes a sorbent dialysis module with a sorbent cartridge that purifies a dialysate fluid that flows therethrough, where the sorbent dialysis module returns the purified dialysate fluid from the sorbent cartridge to an inlet of a dialyzer. The system also includes a single-pass dialysis module with an acetate pump, a bicarbonate pump and a mixing chamber, where the acetate and bicarbonate pumps flow acetate and bicarbonate mixtures, respectively, into the mixing chamber. The single-pass dialysis module receives a desired amount of water from a reverse osmosis device, the single-pass dialysis module operated to direct used dialysate from the dialyzer to a drain. The machine system can be operated to replace the sorbent cartridge with the single-pass dialysis module to switch the operation of the dual mode hemodialysis machine system from a sorbent dialysis mode to a single-pass dialysis mode
摘要翻译：提供了一种紧凑型便携式双模式血液透析机系统。该系统包括具有吸附剂盒的吸附剂透析模块，其用于净化流过其中的透析液，其中吸附剂透析模块将纯化的透析液从吸附剂盒返回到透析器的入口。该系统还包括具有乙酸泵，碳酸氢盐泵和混合室的单程透析模块，其中乙酸盐和碳酸氢盐泵将乙酸盐和碳酸氢盐混合物分别流入混合室。单次透析模块从反渗透装置接收所需量的水，所述单次透析模块操作以将透析液直接从透析器引导至排水管。可以操作机器系统以用单程透析模块代替吸附剂盒，以将双模式血液透析机系统的操作从吸附剂透析模式切换到单次透析模式

6. 发明申请

WO2009129259A3 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
公开(公告)号：WO2009129259A3
公开(公告)日：2009-10-22
申请号：PCT/US2009/040556
申请日：2009-04-14
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , ISBESTER, Paul , PALMER, Grant, J. , MOBELE, Bingidimi, I. , SALSBURY, Jonathon, S. , ULYSEE, Luckner
发明人： ISBESTER, Paul , PALMER, Grant, J. , MOBELE, Bingidimi, I. , SALSBURY, Jonathon, S. , ULYSEE, Luckner
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00 , A61P25/00
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: (A). 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.

7. 发明申请

WO2008089436A2 CRYSTALLINE FORMS OF HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译：结晶形式的HISTONE脱乙酰酶抑制剂
公开(公告)号：WO2008089436A2
公开(公告)日：2008-07-24
申请号：PCT/US2008/051481
申请日：2008-01-18
申请人： TAKEDA SAN DIEGO, INC. , HAYES, Patrick D. , ISBESTER, Paul , MOBELE, Bingidimi I. , PALMER, Grant , SALSBURY, Jonathon S. , SUN, Xufeng , ULYSSE, Luckner
发明人： HAYES, Patrick D. , ISBESTER, Paul , MOBELE, Bingidimi I. , PALMER, Grant , SALSBURY, Jonathon S. , SUN, Xufeng , ULYSSE, Luckner
CPC分类号： C07D231/56 , C07D231/14
摘要： The application is related to polymorphs and salts of compounds having the formulae: Compound (I) N-(2-Aminophenyl)-4-((5,6-dimethoxy-2H-indazol-2-yl)methyl)benzamide Compound (II) 4-((6-Acetamido-2H-indazol-2-yl)methyl)-N-(2-aminophenyl)benzamide Compound (III) 1-(4-(2-Aminophenylcarbamoyl)benzyl)-N-ethyl-1H-pyrazole-4-carboxamide Also provided are novel 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：化合物（I）N-（2-氨基苯基）-4 - （（5,6-二甲氧基-2H-吲唑-2-基）嘧啶-4-基）甲基）苯甲酰胺化合物（III）1-（4-（2-氨基苯基氨基甲酰基）苄基）-N-乙基-1H-吡唑-4-甲酰胺还提供了用于制备化合物（I）的多晶型物的新方法，以及该组合物的试剂盒和制品以及使用该组合物处理各种疾病。

8. 发明申请

WO2008089436A3 CRYSTALLINE FORMS OF HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译： HISTONE脱乙酰酶抑制剂的结晶形式
公开(公告)号：WO2008089436A3
公开(公告)日：2008-12-24
申请号：PCT/US2008051481
申请日：2008-01-18
申请人： TAKEDA SAN DIEGO INC , HAYES PATRICK D , ISBESTER PAUL , MOBELE BINGIDIMI I , PALMER GRANT , SALSBURY JONATHON S , SUN XUFENG , ULYSSE LUCKNER
发明人： HAYES PATRICK D , ISBESTER PAUL , MOBELE BINGIDIMI I , PALMER GRANT , SALSBURY JONATHON S , SUN XUFENG , ULYSSE LUCKNER
IPC分类号： C07D231/14 , A61K31/415 , A61K31/416 , A61P35/00 , C07D231/56
CPC分类号： C07D231/56 , C07D231/14
摘要： The application is related to polymorphs and salts of compounds having the formulae: Compound (I) N-(2-Aminophenyl)-4-((5,6-dimethoxy-2H-indazol-2-yl)methyl)benzamide Compound (II) 4-((6-Acetamido-2H-indazol-2-yl)methyl)-N-(2-aminophenyl)benzamide Compound (III) 1-(4-(2-Aminophenylcarbamoyl)benzyl)-N-ethyl-1H-pyrazole-4-carboxamide Also provided are novel 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：本申请涉及具有下列化学式的化合物的多晶型物和盐：化合物（I）N-（2-氨基苯基）-4 - （（5,6-二甲氧基-2H-吲唑-2-基）甲基）苯甲酰胺化合物（II ）4 - （（6-乙酰氨基-2H-吲唑-2-基）甲基）-N-（2-氨基苯基）苯甲酰胺化合物（III）1-（4-（2-氨基苯基氨基甲酰基）苄基）-N-乙基-1H- 吡唑-4-甲酰胺还提供了制备化合物（I）的多晶型物的新方法，以及组合物的试剂盒和制品，以及使用该组合物治疗各种疾病的方法。

9. 发明申请

WO2007017740A1 SALTS AND POLYMORPHS OF A VERGF-R INHIBITOR 审中-公开
标题翻译： VERGF-R抑制剂的SALTS和POLYMORPHS
公开(公告)号：WO2007017740A1
公开(公告)日：2007-02-15
申请号：PCT/IB2006/002171
申请日：2006-07-27
申请人： PFIZER INC. , LI, Yi , LIU, Jia , SISTLA, Anand , ELDER, Bruce, Joseph , HONG, Yufeng , ISBESTER, Paul, Kenneth , PALMER, Grant, Jackson , SALSBURY, Jonathan, Stuart , ULYSSE, Luckner, Gerard
发明人： LI, Yi , LIU, Jia , SISTLA, Anand , ELDER, Bruce, Joseph , HONG, Yufeng , ISBESTER, Paul, Kenneth , PALMER, Grant, Jackson , SALSBURY, Jonathan, Stuart , ULYSSE, Luckner, Gerard
IPC分类号： C07D405/12 , C07D413/14 , A61P35/00 , A61K31/4709
CPC分类号： C07D413/14 , C07D405/12
摘要： The invention relates to salts and free base forms of N,2-dimethyl-6-[7-(2- morpholinoethoxy)quinolin-4-yloxy]benzofuran-3-carboxamide. The invention further relates to pharmaceutical compositions of these salts and free base forms and methods of treating disorders such as cancer using such compositions.
摘要翻译：本发明涉及N，2-二甲基-6- [7-（2-吗啉代乙氧基）喹啉-4-基氧基]苯并呋喃-3-甲酰胺的盐和游离碱形式。本发明进一步涉及这些盐和游离碱形式的药物组合物以及使用这种组合物治疗疾病如癌症的方法。

10. 发明申请

WO2010135429A8 COMPOSITIONS FOR MODULATING A KINASE CASCADE AND METHODS OF USE THEREOF 审中-公开
标题翻译：用于调节激酶的组合物及其使用方法
公开(公告)号：WO2010135429A8
公开(公告)日：2011-06-03
申请号：PCT/US2010035408
申请日：2010-05-19
申请人： KINEX PHARMACEUTICALS LLC , CODY JEREMY A , HANGAUER DAVID G JR , ISBESTER PAUL K , PALMER GRANT J , PATRA DEBASIS , SALSBURY JONATHON
发明人： CODY JEREMY A , HANGAUER DAVID G JR , ISBESTER PAUL K , PALMER GRANT J , PATRA DEBASIS , SALSBURY JONATHON
IPC分类号： C07D413/10 , A61K31/5355 , A61P3/04 , A61P35/00 , 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)-?/-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)-?/-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)-iV- 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）-β-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）-β-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的激酶级联，使用本发明的组合物。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（形式A）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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