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1. 发明申请

US20080032972A1 Pyridopyrazines and derivatives thereof as alk and c-Met inhibitors 有权
标题翻译：吡啶并吡嗪及其衍生物为alk和c-Met抑制剂
公开(公告)号：US20080032972A1
公开(公告)日：2008-02-07
申请号：US11799066
申请日：2007-04-30
申请人： Bruce Dorsey , Karen Milkiewicz , Douglas Pippin , Jay Theroff , Ted Underiner , Linda Weinberg , Craig Zificsak
发明人： Bruce Dorsey , Karen Milkiewicz , Douglas Pippin , Jay Theroff , Ted Underiner , Linda Weinberg , Craig Zificsak
IPC分类号： A61K31/4985 , A61K31/5375 , A61P43/00 , C07D413/14 , C07D487/04
CPC分类号： C07D471/04
摘要： The present invention provides a compound of Formula I or a pharmaceutically acceptable salt form thereof, wherein A, L1, R1, R2, R3, R4, R5, R6, and X are as defined herein. The compounds of Formula I have ALK and/or c-Met inhibitory activity, and may be used to treat ALK- or c-Met-mediated disorders or conditions.
摘要翻译：本发明提供式I化合物或其药学上可接受的盐形式，其中A 1，L 1，R 1，R 2， R 3，R 4，R 5，R 6和X如本文所定义。式I化合物具有ALK和/或c-Met抑制活性，可用于治疗ALK-或c-Met介导的病症或病症。

2. 发明申请

US20090221555A1 FUSED BICYCLIC DERIVATIVES OF 2,4-DIAMINOPYRIMIDINE AS ALK AND c-MET INHIBITORS 有权
标题翻译： 2,4-二氨基嘧啶作为ALK和c-MET抑制剂的熔融双相衍生物
公开(公告)号：US20090221555A1
公开(公告)日：2009-09-03
申请号：US12162851
申请日：2007-10-23
申请人： Gulzar Ahmed , Adolph Bohnstedt , Henry Joseph Breslin , Jason Burke , Matthew A. Curry , James L. Diebold , Bruce Dorsey , Benjamin J. Dugan , Daming Feng , Diane E. Gingrich , Tao Guo , Koc-Kan Ho , Keith S. Learn , Joseph G. Lisko , Rong-qiang Liu , Eugen Mesaros , Karen Milkiewicz , Gregory R. Ott , Jonathan Parrish , Jay P. Theroff , Tho V. Thieu , Rabindranath Tripathy , Theodore L. Underiner , Jason C. Wagner , Linda Weinberg , Gregory J. Wells , Ming You , Craig A. Zificsak
发明人： Gulzar Ahmed , Adolph Bohnstedt , Henry Joseph Breslin , Jason Burke , Matthew A. Curry , James L. Diebold , Bruce Dorsey , Benjamin J. Dugan , Daming Feng , Diane E. Gingrich , Tao Guo , Koc-Kan Ho , Keith S. Learn , Joseph G. Lisko , Rong-qiang Liu , Eugen Mesaros , Karen Milkiewicz , Gregory R. Ott , Jonathan Parrish , Jay P. Theroff , Tho V. Thieu , Rabindranath Tripathy , Theodore L. Underiner , Jason C. Wagner , Linda Weinberg , Gregory J. Wells , Ming You , Craig A. Zificsak
IPC分类号： A61K31/55 , C07D239/02 , A61K31/505 , C07D403/00 , C07D413/14 , A61K31/5377 , C07D413/00 , C07D403/14
CPC分类号： C07D239/48 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.
摘要翻译：本发明提供式I或II化合物或其药学上可接受的盐形式，其中R1，R2，R3，R4，R5，A1，A2，A3，A4和A5如本文所定义。式I或II的化合物具有ALK和/或c-Met抑制活性，并且可用于治疗增殖性疾病。

3. 发明授权

US08148391B2 Fused bicyclic derivatives of 2,4-diaminopyrimidine as ALK and c-Met inhibitors 有权
标题翻译： 2,4-二氨基嘧啶作为ALK和c-Met抑制剂的稠合双环衍生物
公开(公告)号：US08148391B2
公开(公告)日：2012-04-03
申请号：US12162851
申请日：2007-10-23
申请人： Gulzar Ahmed , Henry Joseph Breslin , Jason Burke , Matthew A. Curry , James L. Diebold , Bruce Dorsey , Benjamin J. Dugan , Daming Feng , Diane E. Gingrich , Tao Guo , Keith S. Learn , Joseph G. Lisko , Rong-Qiang Liu , Eugen Florin Mesaros , Karen Milkiewicz , Gregory R. Ott , Jay P. Theroff , Tho V. Thieu , Rabindranath Tripathy , Theodore L. Underiner , Gregory J. Wells , Craig A. Zificsak
发明人： Gulzar Ahmed , Henry Joseph Breslin , Jason Burke , Matthew A. Curry , James L. Diebold , Bruce Dorsey , Benjamin J. Dugan , Daming Feng , Diane E. Gingrich , Tao Guo , Keith S. Learn , Joseph G. Lisko , Rong-Qiang Liu , Eugen Florin Mesaros , Karen Milkiewicz , Gregory R. Ott , Jay P. Theroff , Tho V. Thieu , Rabindranath Tripathy , Theodore L. Underiner , Gregory J. Wells , Craig A. Zificsak
IPC分类号： A61K31/505 , C07D239/02
CPC分类号： C07D239/48 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.
摘要翻译：本发明提供式I或II化合物或其药学上可接受的盐形式，其中R1，R2，R3，R4，R5，A1，A2，A3，A4和A5如本文所定义。式I或II的化合物具有ALK和/或c-Met抑制活性，并且可用于治疗增殖性疾病。

4. 发明申请

US20120165519A1 Fused Bicyclic Derivatives of 2,4-Diaminopyrimidine as ALK and c-MET Inhibitors 有权
标题翻译： 2,4-二氨基嘧啶的双酚衍生物作为ALK和c-MET抑制剂
公开(公告)号：US20120165519A1
公开(公告)日：2012-06-28
申请号：US13413322
申请日：2012-03-06
申请人： Gulzar Ahmed , Henry Joseph Breslin , Jason Burke , Matthew A. Curry , James L. Diebold , Bruce Dorsey , Benjamin J. Dugan , Daming Feng , Diane E. Gingrich , Tao Guo , Keith S. Learn , Joseph G. Lisko , Rong-qiang Liu , Eugen Mesaros , Karen Milkiewicz , Gregory R. Ott , Jay P. Theroff , Tho V. Thieu , Rabindranath Tripathy , Theodore L. Underiner , Gregory J. Wells , Craig A. Zificsak
发明人： Gulzar Ahmed , Henry Joseph Breslin , Jason Burke , Matthew A. Curry , James L. Diebold , Bruce Dorsey , Benjamin J. Dugan , Daming Feng , Diane E. Gingrich , Tao Guo , Keith S. Learn , Joseph G. Lisko , Rong-qiang Liu , Eugen Mesaros , Karen Milkiewicz , Gregory R. Ott , Jay P. Theroff , Tho V. Thieu , Rabindranath Tripathy , Theodore L. Underiner , Gregory J. Wells , Craig A. Zificsak
IPC分类号： C07D403/14 , C07D498/04 , C07D413/12 , C07D409/14 , C07D405/12 , C07D417/14 , C07D401/14 , C07D405/14 , C07D403/12 , C07D413/14
CPC分类号： C07D239/48 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.
摘要翻译：本发明提供式I或II化合物或其药学上可接受的盐形式，其中R1，R2，R3，R4，R5，A1，A2，A3，A4和A5如本文所定义。式I或II的化合物具有ALK和/或c-Met抑制活性，并且可用于治疗增殖性疾病。

5. 发明申请

US20060199809A1 Factor Xa compounds 有权
标题翻译：因子Xa化合物
公开(公告)号：US20060199809A1
公开(公告)日：2006-09-07
申请号：US11257208
申请日：2005-10-24
申请人： Tianbao Lu , Tho Thieu , Yu-Kai Lee , Daniel Parks , Thomas Markotan , Wenxi Pan , Karen Milkiewicz , Mark Player
发明人： Tianbao Lu , Tho Thieu , Yu-Kai Lee , Daniel Parks , Thomas Markotan , Wenxi Pan , Karen Milkiewicz , Mark Player
IPC分类号： A61K31/54 , A61K31/5377 , A61K31/519 , C07D487/02
CPC分类号： C07D413/14 , C07D231/56 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D409/14 , C07D413/04 , C07D417/10
摘要： The present invention is directed to novel compounds of Formula I: and forms and pharmaceutical compositions thereof, and the use thereof as inhibitors of Factor Xa.
摘要翻译：本发明涉及式I的新型化合物及其形式和药物组合物，以及其作为因子Xa抑制剂的用途。

6. 发明申请

US20060030544A1 Protein kinase and phosphatase inhibitors and methods for designing them 有权
公开(公告)号：US20060030544A1
公开(公告)日：2006-02-09
申请号：US11206115
申请日：2005-10-07
申请人： David Hangauer , Moustafa El-Araby , Karen Milkiewicz
发明人： David Hangauer , Moustafa El-Araby , Karen Milkiewicz
IPC分类号： A61K31/405 , A61K31/675 , C07F9/547 , C07D209/12
CPC分类号： C07D209/42 , A61K31/404 , A61K31/47
摘要： The present invention provides a method for identifying inhibitors of protein kinases and/or protein phosphatases. Methods are also provided for inhibiting protein kinase and/or protein phosphatase activity. Specific non-peptide protein tyrosine kinase and/or protein phosphatase inhibitors are provided. The protein kinase or protein phosphatase inhibitors of the present invention may be used to treat a number of conditions in patients, including cancer, psoriasis, arthrosclerosis, immune system activity, Type II diabetes, and obesity.

7. 发明申请

US20060235007A1 Substituted 1,4-diazepines and uses thereof 审中-公开
标题翻译：取代的1,4-二氮杂及其用途
公开(公告)号：US20060235007A1
公开(公告)日：2006-10-19
申请号：US11452861
申请日：2006-06-14
申请人： Tianbao Lu , Karen Milkiewicz , Pierre Raboisson , Maxwell Cummings , Raul Calvo , Daniel Parks , Louis LaFrance , Juan Marugan Sanchez , Joan Gushue , Kristi Leonard
发明人： Tianbao Lu , Karen Milkiewicz , Pierre Raboisson , Maxwell Cummings , Raul Calvo , Daniel Parks , Louis LaFrance , Juan Marugan Sanchez , Joan Gushue , Kristi Leonard
IPC分类号： A61K31/5513 , C07D403/02 , C07D413/02 , C07D243/18
CPC分类号： C07D243/14
摘要： The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: R1, R2, R9, R10, Ra, Rd and M are defined herein; X is a bivalent radical of: an alkane, a cycloalkane, an optionally-substituted arene, an optionally-substituted heteroarene, an optionally-substituted arylalkane or an optionally-substituted heteroarylalkane; and R3 is —CO2Rd, —CO2M, —OH, —NHRd, —SO2Rd, —NHCONHRd, optionally-substituted amidino or optionally-substituted guanidino; or R3—X— is hydrogen or an electron pair; R4 is oxygen or —NR9R10; R5 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; and R6, R7 and R8 are independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkylalkyl, aralkyl or heteroarylalkyl, each of which is optionally substituted; or R6 and R7, together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted 1 to 3 times with Ra.
摘要翻译：本发明涉及新的1,4-二氮杂，其药物组合物及其作为HDM2-p53相互作用抑制剂的用途。化合物具有式I：或其溶剂合物，水合物或其药学上可接受的盐; 其中：R 1，R 2，R 9，R 10，R SUP， >，R d和M在本文中定义; X是二价基团：烷烃，环烷烃，任选取代的芳烃，任选取代的杂芳烃，任选取代的芳基烷烃或任选取代的杂芳基烷烃; 和R 3是-CO 2 R 2，-CO 2 M，-OH，-NHR 0 任选取代的脒基或任选取代的胍基;其中R 1，R 2，R 3，R 4，或R 3 -X-是氢或电子对; R 4是氧或-NR 9 R 10; R 5是环烷基，芳基，杂芳基，环烷基烷基，芳烷基，杂芳基烷基或饱和或部分不饱和的杂环，其各自任选被取代; R 6和R 8独立地是氢，烷基，环烷基，芳基，杂芳基，饱和或部分不饱和的杂环，环烷基烷基，芳烷基或杂芳基烷基，其各自任选被取代; 或R 6和R 7与它们所连接的碳原子一起形成3-至7-元碳环，任选地被R 1取代1至3倍， SUP> a 。

8. 发明申请

US20060189511A1 Method for cytoprotection through mdm2 and hdm2 inhibition 审中-公开
标题翻译：通过mdm2和hdm2抑制细胞保护的方法
公开(公告)号：US20060189511A1
公开(公告)日：2006-08-24
申请号：US10514338
申请日：2003-05-13
申请人： Holly Koblish , Carl Manthey , Christopher Molly , Tianbao Lu , Daniel Parks , Louis Lafrance , Karen Milkiewicz , Theodore Carver , Bruce Grasberger
发明人： Holly Koblish , Carl Manthey , Christopher Molly , Tianbao Lu , Daniel Parks , Louis Lafrance , Karen Milkiewicz , Theodore Carver , Bruce Grasberger
IPC分类号： A61K38/17 , A01N1/02
CPC分类号： A61K31/5513
摘要： The present invention is directed to a method of protecting one or more cells from programmed cytotoxic cell death by contacting the cells with a cytoprotective amount of an MDM2 and/or HDM2 inhibitor. The cytoprotective amount of inhibitor is typically used as a pulsed administration. Useful inhibitors include a class of 1,4-benzodiazepines, which act as inhibitors of MDM2-p53 interactions. The method of the invention can be employed as an adjunct to chemotherapy or radiation therapy. In addition, the methods of the invention can be employed to treat a disease or condition that involves excessive cell death.
摘要翻译：本发明涉及通过使细胞与细胞保护剂量的MDM2和/或HDM2抑制剂接触来保护一种或多种细胞免受程序性细胞毒性细胞死亡的方法。抑制剂的细胞保护量通常用作脉冲给药。有用的抑制剂包括一类1,4-苯二氮卓类，其作为MDM2-p53相互作用的抑制剂。本发明的方法可以用作化疗或放射治疗的辅助物质。此外，本发明的方法可用于治疗涉及过度细胞死亡的疾病或病症。

9. 发明申请

US20060148792A1 Substituted 1,4-benzodiazepines and uses thereof 审中-公开
标题翻译：取代的1,4-苯并二氮杂及其用途
公开(公告)号：US20060148792A1
公开(公告)日：2006-07-06
申请号：US11371964
申请日：2006-03-09
申请人： Tianbao Lu , Louis LaFrance , Daniel Parks , Karen Milkiewicz , Raul Calvo , Maxwell Cummings , Alexander Kim , Bruce Grasberger , Theodore Carver
发明人： Tianbao Lu , Louis LaFrance , Daniel Parks , Karen Milkiewicz , Raul Calvo , Maxwell Cummings , Alexander Kim , Bruce Grasberger , Theodore Carver
IPC分类号： A61K31/551 , C07D243/12 , C07D243/18
CPC分类号： C07D401/04 , C07D243/14 , C07D403/10 , C07D405/04 , C07D409/04
摘要： The present invention is directed to novel 1,4-benzodiazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: X and Y are independently —C(O)—, —CH2— or —C(S)—; R1, R2, R3, R4, R7, R8, Rb, Rc, Rd and M arm defined herein; R5 is hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, optionally substituted heteroaralkyl, carboxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, aminocarbonyl, aminocarbonylalkyl, alkylaminocarbonyl or alkylaminocarbonylalkyl; R6 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; R9 is cycloalkyl: aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkyl(alkyl), aralkyl or heteroarylalkyl, each of which is optionally substituted; and R10 is —(CH2)n—CO2Rb, —(CH2)m—CO2M, —(CH2)i—OH or —(CH2)j—CONRcRd n is 0-8, m is 0-8, i is 1-8 and j is 0-8.
摘要翻译：本发明涉及新的1,4-苯二氮卓类药物，其药物组合物及其作为HDM2-p53相互作用抑制剂的用途。化合物具有式I：或其溶剂合物，水合物或其药学上可接受的盐; 其中：X和Y独立地为-C（O） - ， - CH 2 - 或-C（S） - ; R 1，R 2，R 3，R 4，R 7， R 8，R b，R c，R d，R d和M臂; R 5是氢，烷基，环烷基，任选取代的芳基，任选取代的杂芳基，任选取代的芳烷基，任选取代的杂芳烷基，羧基烷基，烷氧基羰基，烷氧基羰基烷基，氨基羰基，氨基羰基烷基，烷基氨基羰基或烷基氨基羰基烷基; R 6是环烷基，芳基，杂芳基，环烷基烷基，芳烷基，杂芳基烷基或饱和或部分不饱和的杂环，其各自任选被取代; R 9是环烷基：芳基，杂芳基，饱和或部分不饱和的杂环，环烷基（烷基），芳烷基或杂芳基烷基，其各自任选被取代; 和R 10是 - （CH 2）n - - - - - - （CH 2）n - ， - （CH 2）2 - ， - M 2 - ， - （CH 2） -OH或 - （CH 2 CH 2）n -CONR C n R n为0-8 ，m为0-8，i为1-8，j为0-8。

10. 发明申请

US20060089401A1 Kinase inhibitors 有权
标题翻译：激酶抑制剂
公开(公告)号：US20060089401A1
公开(公告)日：2006-04-27
申请号：US11261858
申请日：2005-10-27
申请人： David Hangauer , Thomas Marsilje , Karen Milkiewicz
发明人： David Hangauer , Thomas Marsilje , Karen Milkiewicz
IPC分类号： A61K31/405 , A61K31/165 , C07C235/66
CPC分类号： C12Q1/485 , G01N2500/04
摘要： The present invention provides a method for identifying inhibitors of protein kinases. Methods are also provided for inhibiting protein kinase activity. Specific non-peptide protein tyrosine kinase inhibitors are provided. The protein kinases produced using the method of the present invention may be used to treat a number of conditions in patients, including cancer, psoriasis, atherosclerosis, or immune system activity.
摘要翻译：本发明提供了鉴定蛋白激酶抑制剂的方法。还提供了用于抑制蛋白激酶活性的方法。提供了特异性的非肽蛋白酪氨酸激酶抑制剂。使用本发明的方法产生的蛋白激酶可用于治疗患者的许多病症，包括癌症，牛皮癣，动脉粥样硬化或免疫系统活性。

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