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1. 发明申请

WO2012125668A1 TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF 审中-公开
标题翻译： TrkA激酶抑制剂，其组合物及其方法
公开(公告)号：WO2012125668A1
公开(公告)日：2012-09-20
申请号：PCT/US2012/028979
申请日：2012-03-14
申请人： MERCK SHARP & DOHME CORP. , GREEN, Ahren , LI, Yiwei , STACHEL, Shawn
发明人： GREEN, Ahren , LI, Yiwei , STACHEL, Shawn
IPC分类号： A01N43/90
CPC分类号： C07D471/04 , C07D239/94
摘要： The present invention is directed to quinazolinyl and pyridoquinazolinyl compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
摘要翻译：本发明涉及式（I）的喹唑啉基和吡啶并喹啉基化合物，其是原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂，因此可用于治疗疼痛，炎症，癌症，再狭窄，动脉粥样硬化，牛皮癣，血栓形成，与神经生长因子（NGF）受体TrkA的异常活动相关的疾病，障碍，损伤或与异常髓鞘或脱髓鞘相关的疾病或病症相关的功能障碍。

2. 发明申请

WO2012125667A1 TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF 审中-公开
标题翻译： TrkA激酶抑制剂，其组合物及其方法
公开(公告)号：WO2012125667A1
公开(公告)日：2012-09-20
申请号：PCT/US2012/028977
申请日：2012-03-14
申请人： MERCK SHARP & DOHME CORP. , GREEN, Ahren , LI, Yiwei , STACHEL, Shawn
发明人： GREEN, Ahren , LI, Yiwei , STACHEL, Shawn
IPC分类号： C07D249/00
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention is directed to pyridotriazole and benztriazole compounds of formula (I) (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
摘要翻译：本发明涉及作为原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂的式（I）（I）的吡啶并三唑和苯并三唑化合物，因此可用于治疗疼痛，炎症，癌症，再狭窄，动脉粥样硬化，牛皮癣，血栓形成，疾病，障碍，损伤或与脱髓鞘或脱髓鞘相关的功能紊乱或与神经生长因子（NGF）受体TrkA的异常活动相关的疾病或病症。

3. 发明申请

WO2011043954A1 NOVEL TRPA1 ANTAGONISTS 审中-公开
标题翻译：新一代TRPA1 ANTAGONISTS
公开(公告)号：WO2011043954A1
公开(公告)日：2011-04-14
申请号：PCT/US2010/050493
申请日：2010-09-28
申请人： MERCK SHARP & DOHME CORP. , BILODEAU, Mark, T. , EGBERTSON, Melissa , GREEN, Ahren , LI, Yiwei , HARTNETT, John, C.
发明人： BILODEAU, Mark, T. , EGBERTSON, Melissa , GREEN, Ahren , LI, Yiwei , HARTNETT, John, C.
IPC分类号： A61K31/555
CPC分类号： C07C215/20 , A61K31/133 , C07C25/02 , C07C211/34 , C07C215/44 , C07C255/58 , C07C2602/10 , C07D215/38 , C07D215/44 , C07D311/74 , C07D311/76 , C07D405/04 , C07D405/06
摘要： The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function. The present invention further relates to methods and compositions that antagonize both a function of TRPA1 and a function of one or more additional TRP channels.
摘要翻译：本发明涉及调节至少一种TRP家族成员的组合物和方法。具体地说，本发明涉及新型TRPA1拮抗剂及其用于治疗慢性炎性和神经性疼痛等疼痛的用途。可以调节一种或多种TRPA1功能的化合物在许多方面是有用的，包括但不限于维持钙稳态; 维持钠稳态; 调节细胞内钙含量; 调节膜极化（膜电位）; 调节阳离子水平; 和/或治疗或预防与钙稳态相关的疾病，病症或病症，钠稳态，钙或钠血管平衡，或膜极化/超极化（包括低钠和过度兴奋性）和/或治疗或预防与疾病，病症或病症相关与TRPA1表达或功能调节或失调。本发明还涉及拮抗TRPA1的功能和一种或多种另外的TRP通道的功能的方法和组合物。

4. 发明申请

WO2008137609A1 5-LIPOXYGENASE-ACTIVATING PROTEIN (FLAP) INHIBITORS 审中-公开
标题翻译： 5-脂氧合酶激活蛋白（FLAP）抑制剂
公开(公告)号：WO2008137609A1
公开(公告)日：2008-11-13
申请号：PCT/US2008/062310
申请日：2008-05-01
申请人： AMIRA PHARMACEUTICALS, INC. , HUTCHINSON, John, Howard , PRASIT, Petpiboon, Peppi , STEARNS, Brian, Andrew , EVANS, Jillian, F. , MORAN, Mark , LI, Yiwei , WANG, Bowei , TRUONG, Yen, Pham , ROPPE, Jeffrey, Roger , SCOTT, Jill, Melissa , ZUNIC, Jasmine, Eleanor , ARRUDA, Jeannie, M. , SEIDERS, Thomas, Jon , STOCK, Nicholas, Simon , HADDACH, Mustapha
发明人： HUTCHINSON, John, Howard , PRASIT, Petpiboon, Peppi , STEARNS, Brian, Andrew , EVANS, Jillian, F. , MORAN, Mark , LI, Yiwei , WANG, Bowei , TRUONG, Yen, Pham , ROPPE, Jeffrey, Roger , SCOTT, Jill, Melissa , ZUNIC, Jasmine, Eleanor , ARRUDA, Jeannie, M. , SEIDERS, Thomas, Jon , STOCK, Nicholas, Simon , HADDACH, Mustapha
IPC分类号： C07D209/26 , C07D209/04
CPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.
摘要翻译：本文描述了含有调节5-脂氧合酶活化蛋白（FLAP）活性的化合物和药物组合物。本文还描述了单独使用这种FLAP调节剂并与其他化合物组合使用以治疗呼吸系统疾病，心血管疾病和其他白三烯依赖性或白三烯介导的病症或疾病的方法。

5. 发明申请

WO2007056021A3 5-LIPOXYGENASE-ACTIVATING PROTEIN (FLAP) INHIBITORS 审中-公开
公开(公告)号：WO2007056021A3
公开(公告)日：2007-07-12
申请号：PCT/US2006042690
申请日：2006-10-30
申请人： AMIRA PHARMACEUTICALS INC , HUTCHINSON JOHN H , PRASIT PETPIBOON PEPPI , MORAN MARK , EVANS JILLIAN F , STEARNS BRIAN ANDREW , ROPPE JEFFREY ROGER , LI YIWEI , ZUNIC JASMINE ELEANOR , ARRUDA JEANNIE M , STOCK NICHOLAS SIMON , HADDACH MUSTAPHA
发明人： HUTCHINSON JOHN H , PRASIT PETPIBOON PEPPI , MORAN MARK , EVANS JILLIAN F , STEARNS BRIAN ANDREW , ROPPE JEFFREY ROGER , LI YIWEI , ZUNIC JASMINE ELEANOR , ARRUDA JEANNIE M , STOCK NICHOLAS SIMON , HADDACH MUSTAPHA
IPC分类号： C07D209/00 , A61K31/415
CPC分类号： C07D401/14 , C07D401/12 , C07D403/10 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.

6. 发明申请

WO2006135627A2 INHIBITORS OF AKT ACTIVITY 审中-公开
标题翻译： AKT活动的抑制剂
公开(公告)号：WO2006135627A2
公开(公告)日：2006-12-21
申请号：PCT/US2006/022079
申请日：2006-06-07
申请人： MERCK & CO., INC. , ARMSTRONG, Donna, J. , HU, Essa, H. , KELLY, Michael, J. III , LAYTON, Mark, E. , LI, Yiwei , LIANG, Jun , RODZINAK, Kevin, J. , ROSSI, Michael, A. , SANDERSON, Philip, E. , WANG, Jiabing
发明人： ARMSTRONG, Donna, J. , HU, Essa, H. , KELLY, Michael, J. III , LAYTON, Mark, E. , LI, Yiwei , LIANG, Jun , RODZINAK, Kevin, J. , ROSSI, Michael, A. , SANDERSON, Philip, E. , WANG, Jiabing
IPC分类号： A61K31/397
CPC分类号： C07D471/14 , C07D487/14
摘要： The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译：本发明提供抑制Akt活性的取代的萘啶化合物。特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。

7. 发明申请

WO2006065601A8 INHIBITORS OF AKT ACTIVITY 审中-公开
标题翻译： AKT活动的抑制剂
公开(公告)号：WO2006065601A8
公开(公告)日：2006-10-19
申请号：PCT/US2005044294
申请日：2005-12-09
申请人： MERCK & CO INC , ARRUDA JEANNIE M , CAMPBELL BRIAN T , COSFORD NICHOLAS D P , HOFFMAN JACOB M , HU ESSA H , LAYTON MARK E , LI YIWEI , LIANG JUN , RODZINAK KEVIN J , SIU TONY , STEARNS BRIAN A , TEHRANI LIDA R
发明人： ARRUDA JEANNIE M , CAMPBELL BRIAN T , COSFORD NICHOLAS D P , HOFFMAN JACOB M , HU ESSA H , LAYTON MARK E , LI YIWEI , LIANG JUN , RODZINAK KEVIN J , SIU TONY , STEARNS BRIAN A , TEHRANI LIDA R
IPC分类号： A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention is directed to compounds which contain substituted naphthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on.
摘要翻译：本发明涉及含有抑制Akt（丝氨酸/苏氨酸蛋白激酶）活性的取代萘啶的化合物。本发明还涉及含有本发明化合物的治疗组合物和治疗癌症的方法，包括施用本发明化合物。与PCT公开WO2003 / 086394中报道的其它萘啶类相比，这些取代的萘啶具有意想不到的有利性质，这种意想不到的有利性质可包括增加的细胞效力/溶解度，更大的选择性，增强的药代动力学性质，缺乏目标活性等。

8. 发明申请

WO2006065601A2 INHIBITORS OF AKT ACTIVITY 审中-公开
标题翻译： AKT活性抑制剂
公开(公告)号：WO2006065601A2
公开(公告)日：2006-06-22
申请号：PCT/US2005/044294
申请日：2005-12-09
申请人： MERCK & CO., INC. , ARRUDA, Jeannie, M. , CAMPBELL, Brian, T. , COSFORD, Nicholas, D. P. , HOFFMAN, Jacob, M. , HU, Essa, H. , LAYTON, Mark, E. , LI, Yiwei , LIANG, Jun , RODZINAK, Kevin, J. , SIU, Tony , STEARNS, Brian, A. , TEHRANI, Lida, R.
发明人： ARRUDA, Jeannie, M. , CAMPBELL, Brian, T. , COSFORD, Nicholas, D. P. , HOFFMAN, Jacob, M. , HU, Essa, H. , LAYTON, Mark, E. , LI, Yiwei , LIANG, Jun , RODZINAK, Kevin, J. , SIU, Tony , STEARNS, Brian, A. , TEHRANI, Lida, R.
IPC分类号： A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention is directed to compounds which contain substituted naphthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on.
摘要翻译：本发明涉及含有抑制丝氨酸/苏氨酸蛋白激酶Akt活性的取代萘啶的化合物。本发明还涉及含有本发明化合物的化学治疗组合物和用于治疗癌症的方法，其包括施用本发明的化合物。与PCT公开WO2003 / 086394中报道的其他萘啶相比，这些取代的萘啶具有出乎意料的有利性质，这种意想不到的有利性质可包括增加的细胞效力/溶解度，更高的选择性，增强的药代动力学性质，缺乏脱靶活性等。 p>

9. 发明申请

WO2006036395A3 INHIBITORS OF AKT ACTIVITY 审中-公开
标题翻译： AKT活动的抑制剂
公开(公告)号：WO2006036395A3
公开(公告)日：2007-12-21
申请号：PCT/US2005029941
申请日：2005-08-19
申请人： MERCK & CO INC , BILODEAU MARK T , COSFORD NICHOLAS D P , HARTNETT JOHN C , LIANG JUN , MANLEY PETER J , NEILSON LOU ANNE , SIU TONY , WU ZHICAI , LI YIWEI
发明人： BILODEAU MARK T , COSFORD NICHOLAS D P , HARTNETT JOHN C , LIANG JUN , MANLEY PETER J , NEILSON LOU ANNE , SIU TONY , WU ZHICAI , LI YIWEI
IPC分类号： A61K31/519 , A61K31/397 , C07D225/04 , C07D403/14 , C07D471/14 , C07D487/14
CPC分类号： C07D471/04
摘要： The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
摘要翻译：本发明涉及含有抑制Akt（丝氨酸/苏氨酸蛋白激酶）活性的取代的5-去氮萘啶部分的化合物。本发明还涉及含有本发明化合物的治疗组合物和治疗癌症的方法，包括施用本发明化合物。

10. 发明申请

WO2007056220A2 5-LIPOXYGENASE-ACTIVATING PROTEIN (FLAP) INHIBITORS 审中-公开
公开(公告)号：WO2007056220A2
公开(公告)日：2007-05-18
申请号：PCT/US2006/043095
申请日：2006-11-03
申请人： AMIRA PHARMACEUTICALS, INC. , HUTCHINSON, John, H. , PRASIT, Petpiboon, Peppi , MORAN, Mark , EVANS, Jillian, F. , LI, Yiwei , ZUNIC, Jasmine, Eleanor , HADDACH, Mustapha , STOCK, Nicholas, Simon
发明人： HUTCHINSON, John, H. , PRASIT, Petpiboon, Peppi , MORAN, Mark , EVANS, Jillian, F. , LI, Yiwei , ZUNIC, Jasmine, Eleanor , HADDACH, Mustapha , STOCK, Nicholas, Simon
IPC分类号： A61K31/501 , A61K31/497 , A61K31/4439 , A61K31/427 , C07D417/02 , C07D403/02
CPC分类号： C07D401/10 , C07D401/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.

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