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1. 发明申请

US20070203136A1 TRIAZOLOPYRIDAZINES AS KINASE MODULATORS 有权
标题翻译：三唑吡啶作为激酶调节剂
公开(公告)号：US20070203136A1
公开(公告)日：2007-08-30
申请号：US11612020
申请日：2006-12-18
申请人： Tianbao Lu , Richard Alexander , Richard Connors , Maxwell Cummings , Robert Galemmo , Heather Rae Hufnagel , Dana Johnson , Ehab Khalil , Kristi Leonard , Thomas Markotan , Anna Maroney , Jan Sechler , Jeremy Travins , Robert Tuman
发明人： Tianbao Lu , Richard Alexander , Richard Connors , Maxwell Cummings , Robert Galemmo , Heather Rae Hufnagel , Dana Johnson , Ehab Khalil , Kristi Leonard , Thomas Markotan , Anna Maroney , Jan Sechler , Jeremy Travins , Robert Tuman
IPC分类号： A61K31/503 , A61K31/5377 , C07D487/04
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要翻译：本发明涉及式I的三唑并哒嗪化合物：其中R 1，R 5，R 6，R 7， >，R 8和A如本文所定义，使用这些化合物作为蛋白质酪氨酸激酶调节剂，特别是c-Met的抑制剂，以及这些化合物用于降低或抑制激酶活性的用途 c-Met在细胞或受试者中的调节，并调节细胞或受试者中的c-Met表达，以及这些化合物在受试者中预防或治疗细胞增殖性疾病和/或与c-Met有关的障碍的用途。本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

2. 发明申请

US20070066610A1 Acylhydrazones as kinase modulators 有权
标题翻译：酰腙作为激酶调节剂
公开(公告)号：US20070066610A1
公开(公告)日：2007-03-22
申请号：US11377077
申请日：2006-03-16
申请人： Kristi Leonard , Tianbao Lu , Robert Tuman , Dana Johnson , Anna Maroney , Jan Sechler , Richard Connors , Richard Alexander , Maxwell Cummings , Robert Galemmo , Thomas Markotan
发明人： Kristi Leonard , Tianbao Lu , Robert Tuman , Dana Johnson , Anna Maroney , Jan Sechler , Richard Connors , Richard Alexander , Maxwell Cummings , Robert Galemmo , Thomas Markotan
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/404 , C07D413/14 , C07D405/14
CPC分类号： C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12
摘要： The invention is directed to acylhydrazones compounds of Formula I: where R1, R2 and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要翻译：本发明涉及式I的酰腙化合物：其中R 1，R 2和A如本文所定义，使用这些化合物作为蛋白质酪氨酸激酶调节剂，特别是 c-Met的抑制剂以及这些化合物在细胞或受试者中降低或抑制c-Met的激酶活性并调节细胞或受试者中的c-Met表达的用途，以及这些化合物用于预防或在受试者中治疗与c-Met相关的细胞增殖性疾病和/或障碍。本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

3. 发明申请

US20070142305A1 N-substituted tricyclic 1-aminopyrazoles as inhibitors for the treatment of cell proliferative disorders 有权
标题翻译： N-取代的三环1-氨基吡唑作为治疗细胞增殖性疾病的抑制剂
公开(公告)号：US20070142305A1
公开(公告)日：2007-06-21
申请号：US11657912
申请日：2007-01-25
申请人： Chih Ho , Bengt Brunmark , Stuart Emanuel , Robert Galemmo , Dana Johnson , Donald Ludovici , Umar Maharoof , Jay Mei , Jan Sechler , Eric Strobel , Robert Tuman , Hwa Yen
发明人： Chih Ho , Bengt Brunmark , Stuart Emanuel , Robert Galemmo , Dana Johnson , Donald Ludovici , Umar Maharoof , Jay Mei , Jan Sechler , Eric Strobel , Robert Tuman , Hwa Yen
IPC分类号： A61K31/7052 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4439 , A61K31/4162 , C07D413/02 , C07D403/02
CPC分类号： C07F9/65038 , C07D231/54 , C07D231/56 , C07D233/64 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D491/04 , C07D495/04
摘要： The invention is directed to N-substituted tricyclic 3-AMINOPYRAZOLE derivatives, which are useful as inhibitors of platelet-derived growth factor receptor (PDGF-R) kinase, and methods for the preparation of said derivatives. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as tumors and other cell. proliferative disorders.
摘要翻译：本发明涉及可用作血小板衍生生长因子受体（PDGF-R）激酶抑制剂的N-取代三环3-氨基吡唑衍生物，以及制备所述衍生物的方法。本发明还涉及包含本发明化合物的药物组合物和用于治疗诸如肿瘤和其它细胞的病症的方法。增生性疾病

4. 发明申请

US20050130910A1 Immobilized N-substituted tricyclic 3-aminopyrazoles for the identification of biomolecular targets 审中-公开
标题翻译：固定的N-取代三环3-氨基吡唑，用于鉴定生物分子靶标
公开(公告)号：US20050130910A1
公开(公告)日：2005-06-16
申请号：US10986500
申请日：2004-11-10
申请人： Chih Ho , Robert Galemmo , Dana Johnson , Jay Mei , Stanley Belkowski , Richard Connors
发明人： Chih Ho , Robert Galemmo , Dana Johnson , Jay Mei , Stanley Belkowski , Richard Connors
IPC分类号： A61K31/4162 , A61K31/422 , A61K31/427 , A61K31/7056 , C07D231/54 , C07D231/56 , C07D401/12 , C07D403/12 , C07D413/02 , C07D417/02 , C07D495/04 , C07H17/00 , G01N33/543 , G01N33/574
CPC分类号： C07D403/12 , C04B35/632 , C07D231/54 , C07D231/56 , C07D401/12 , C07D495/04 , G01N33/574 , G01N2333/71 , G01N2500/00
摘要： The present invention relates to immobilized N-substituted tricyclic 3-aminopyrazole compounds of Formula 1 as tools for the identification of bimolecular targets in cells of therapeutic significance, profiling the selectivity of compounds, prediction of possible related toxicities and exploration of mechanisms of action in biological systems for therapeutic indications related to compounds. These agents can be used to identify biomolecules with the potential to interact with the immobilized reagent. The identified biomolecule may be then be used as a therapeutic target, serve as a marker of drug action, or alternatively describe an untoward or toxic potential of the immobilized agent.
摘要翻译：本发明涉及式1的固定化N-取代三环3-氨基吡唑化合物，作为用于鉴定细胞中双分子靶标的具有治疗意义的工具，分析化合物的选择性，预测可能的相关毒性和探索生物学作用机制与化合物相关的治疗适应症系统。这些试剂可用于鉴定具有与固定化试剂相互作用的潜力的生物分子。所鉴定的生物分子然后可以用作治疗靶，用作药物作用的标记，或者替代地描述固定化剂的不利或有毒的潜力。

5. 发明申请

US20070149572A1 METHOD OF INHIBITING FLT3 KINASE 有权
标题翻译：抑制FLT3激酶的方法
公开(公告)号：US20070149572A1
公开(公告)日：2007-06-28
申请号：US11550077
申请日：2006-10-17
申请人： Shelley Ballentine , Christian Baumann , Jinsheng Chen , Carl Illig , Sanath Meegalla , M. Rudolph , Robert Tuman , Mark Wall , Kenneth Wilson , Dana Johnson
发明人： Shelley Ballentine , Christian Baumann , Jinsheng Chen , Carl Illig , Sanath Meegalla , M. Rudolph , Robert Tuman , Mark Wall , Kenneth Wilson , Dana Johnson
IPC分类号： A61K31/454
CPC分类号： A61K31/4439 , A61K31/454 , A61K31/497 , A61K31/5355 , Y10S514/908
摘要： A method of reducing or inhibiting kinase activity of FLT3 in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 using a ompound of the present invention: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要翻译：一种减少或抑制细胞或受试者中FLT3的激酶活性的方法，以及使用本发明的方法使用这些化合物在受试者中预防或治疗细胞增殖性疾病和/或与FLT3相关的病症：或其溶剂合物，水合物，互变异构体或其药学上可接受的盐。本发明还涉及治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

6. 发明申请

US20070004660A1 Synergistic Modulation of Flt3 Kinase Using Alkylquinolines and Alkylquinazolines 审中-公开
标题翻译：使用烷基喹啉和烷基喹唑啉协同调节Flt3激酶
公开(公告)号：US20070004660A1
公开(公告)日：2007-01-04
申请号：US11422395
申请日：2006-06-06
申请人： Christian Baumann , Michael Gaul , Dana Johnson , Robert Tuman
发明人： Christian Baumann , Michael Gaul , Dana Johnson , Robert Tuman
IPC分类号： A61K48/00 , A61K31/541 , A61K31/5377 , A61K31/517 , A61K31/496
CPC分类号： A61K31/4709 , A61K31/00 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , A61K2300/00
摘要： The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from alkylquinoline and alkylquinazoline compounds of Formula I′: where R1, R2, R3, Z, G, Q and X are as defined herein. Included within the present invention is both prophylactic and therapeutic methods for treating a subject at risk of (or susceptible to) developing a cell proliferative disorder or a disorder related to FLT3.
摘要翻译：本发明涉及抑制FLT3酪氨酸激酶活性或在细胞或受试者中表达或降低FLT3激酶活性或表达的方法，其包括施用法呢基转移酶抑制剂和FLT3激酶抑制剂，其选自烷基喹啉和式I的烷基喹唑啉化合物 '：其中R 1，R 2，R 3，Z，G，Q和X如本文所定义。本发明包括预防和治疗方法，用于治疗患有（或易于）发展为与FLT3相关的细胞增殖性疾病或紊乱的风险的受试者。

7. 发明申请

US20060281772A1 ALKYLQUINOLINE AND ALKYLQUINAZOLINE KINASE MODULATORS 有权
标题翻译：烷基胆碱和碱性氨基酸激酶调节剂
公开(公告)号：US20060281772A1
公开(公告)日：2006-12-14
申请号：US11422349
申请日：2006-06-06
申请人： Nand Baindur , Michael Gaul , Kevin Kreutter , Christian Baumann , Alexander Kim , Guozhang Xu , Robert Tuman , Dana Johnson
发明人： Nand Baindur , Michael Gaul , Kevin Kreutter , Christian Baumann , Alexander Kim , Guozhang Xu , Robert Tuman , Dana Johnson
IPC分类号： A61K31/517 , A61K31/4709 , C07D403/04 , C07D401/04
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula I: wherein R1, R2, R3, B, Z, G, Q and X are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of FLT3 and/or c-kit and/or TrkB, the use of such compounds to reduce or inhibit kinase activity of FLT3 and/or c-kit and/or TrkB in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 and/or c-kit and/or TrkB. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要翻译：本发明涉及式I的烷基喹啉和烷基喹唑啉化合物：其中R 1，R 2，R 3，B，Z，G， Q和X如本文所定义，使用这些化合物如蛋白酪氨酸激酶调节剂，特别是FLT3和/或c-kit和/或TrkB的抑制剂，使用这些化合物来降低或抑制FLT3和/或 c-kit和/或TrkB，以及这些化合物在受试者中用于预防或治疗细胞增殖性疾病和/或与FLT3和/或c-kit和/或TrkB相关的疾病的用途。本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

8. 发明申请

US20060281788A1 SYNERGISTIC MODULATION OF FLT3 KINASE USING A FLT3 INHIBITOR AND A FARNESYL TRANSFERASE INHIBITOR 审中-公开
公开(公告)号：US20060281788A1
公开(公告)日：2006-12-14
申请号：US11422413
申请日：2006-06-06
申请人： Christian Baumann , Michael Gaul , Dana Johnson , Robert Tuman
发明人： Christian Baumann , Michael Gaul , Dana Johnson , Robert Tuman
IPC分类号： A61K31/454 , A61K48/00
CPC分类号： A61K45/06 , A61K31/4427 , A61K31/454 , A61K2300/00
摘要： The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from compounds of Formula I′: Included within the present invention is both prophylactic and therapeutic methods for treating a subject at risk of (or susceptible to) developing a cell proliferative disorder or a disorder related to FLT3.

9. 发明申请

US20070015207A1 Triazolopyrimidine derivatives 有权
标题翻译：三唑并嘧啶衍生物
公开(公告)号：US20070015207A1
公开(公告)日：2007-01-18
申请号：US11329642
申请日：2006-01-11
申请人： Donald Ludovici , Richard Connors , Steven Coats , Li Liu , Bart De Corte , Dana Johnson , Mark Schulz
发明人： Donald Ludovici , Richard Connors , Steven Coats , Li Liu , Bart De Corte , Dana Johnson , Mark Schulz
IPC分类号： G01N33/53 , C07H21/04 , C12P21/06 , C12N5/06 , C07D487/02 , C07K16/40 , C12N9/12
CPC分类号： C07K14/4738 , C07D487/04 , C12N9/1205 , C12Q1/485 , G01N2500/02
摘要： The invention relates to the discovery of triazolopyrimidine derivatives of formula (I), which have been found to exhibit inhibitory activity against the serine-tyrosine and tyrosine kinases.
摘要翻译：本发明涉及已发现对丝氨酸 - 酪氨酸和酪氨酸激酶具有抑制活性的式（I）三唑并嘧啶衍生物的发现。

10. 发明申请

US20140114231A1 Formulations and Compositions of Hydrophobic Extracts of Skin Tree 审中-公开
标题翻译：皮肤疏水提取物的配方和组成
公开(公告)号：US20140114231A1
公开(公告)日：2014-04-24
申请号：US13656705
申请日：2012-10-20
申请人： Bertha Rostro , Mehdie Kohanloo , Dana Johnson , Candace Johnson
发明人： Bertha Rostro , Mehdie Kohanloo , Dana Johnson , Candace Johnson
IPC分类号： A61N5/06 , A61K36/48
CPC分类号： A61N5/062 , A61K36/48
摘要： This patent discloses formulations, compositions, and process method and device, of hydrophobic extracts and biomass of Skin Tree, also called Mimosa tenuiflora, also called Mimosa cabrera, also called Mimosa hostilis, also called Jurema, also called Tepezcohuite, and apparatus used for cell repair, and the regeneration and rejuvenation of glabrous skin and hair bearing skin. The formulations and compositions herein disclosed, alone and when used with apparatus described, i.e. in combination, will serve to modulate cell repair and block inflammatory processes, infection and disease, reversing skin aging, thereby restoring normal cell and skin conditions, coloration, homeostasis, youth, vitality, and firmness. Still other applications include biomass, biofuel processing methods, applications to biodiesel, gasoline, jet fuel, terpene fuel production, cellulose fuels, kerogens, crude oils, light sweet crude oil productions, refinery operations, viscosity modification, and refining, and deepwater oil exploration, crude oil desalting, fuels, biofuels, and fuel additives, refinery additives, or chemical modifiers, viscosity modifiers, and crude oil desalting.
摘要翻译：该专利公开了皮肤树的疏水性提取物和生物质的也称为含羞草（Mimosa tenuiflora）的制剂，组合物和方法和装置，也称为含羞草cabrera，也称为含羞草（Mimosa hostilis），也称为Jurema，也称为Tepezcohuite，以及用于细胞的装置修复，无毛皮肤和头发皮肤的再生和恢复。本文公开的制剂和组合物，当与所述的装置组合使用时，将用于调节细胞修复和阻断炎症过程，感染和疾病，逆转皮肤老化，从而恢复正常的细胞和皮肤状况，着色，体内平衡，青春，活力和坚定。还有其他应用包括生物质，生物燃料加工方法，生物柴油，汽油，喷气燃料，萜烯燃料生产，纤维素燃料，焦油，原油，轻质原油生产，炼油作业，粘度改性和精炼以及深水油勘探的应用原油脱盐，燃料，生物燃料和燃料添加剂，炼油添加剂或化学改性剂，粘度调节剂和原油脱盐。

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