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31.
公开(公告)号:US08889664B2
公开(公告)日:2014-11-18
申请号:US13096942
申请日:2011-04-28
申请人: William Bajjalieh , Lynne Canne Bannen , S. David Brown , Patrick Kearney , Morrison Mac , Charles K. Marlowe , John M. Nuss , Zerom Tesfai , Yong Wang , Wei Xu
发明人: William Bajjalieh , Lynne Canne Bannen , S. David Brown , Patrick Kearney , Morrison Mac , Charles K. Marlowe , John M. Nuss , Zerom Tesfai , Yong Wang , Wei Xu
IPC分类号: C07D403/12 , A61K31/498 , C07D487/04 , C07D241/54 , A61K31/4985 , C07D413/12 , C07D401/12 , A61P35/00 , C07D417/12 , C07D409/12 , C07D241/44
CPC分类号: C07D401/12 , C07D241/44 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , Y02P20/55
摘要: The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.
摘要翻译: 本发明包括与许多恶性肿瘤如卵巢癌,宫颈癌,乳腺癌,结肠癌,直肠癌和成胶质细胞瘤等相关的磷脂酰肌醇3-激酶(PI3K)的小分子抑制剂。 因此,本发明的化合物可用于治疗,预防和/或抑制这些疾病。
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32.
公开(公告)号:US20110207712A1
公开(公告)日:2011-08-25
申请号:US13096942
申请日:2011-04-28
申请人: William Bajjalieh , Lynne Canne Bannen , S. David Brown , Patrick Kearney , Morrison Mac , Charles K. Marlowe , John M. Nuss , Zerom Tesfai , Yong Wang , Wei Xu
发明人: William Bajjalieh , Lynne Canne Bannen , S. David Brown , Patrick Kearney , Morrison Mac , Charles K. Marlowe , John M. Nuss , Zerom Tesfai , Yong Wang , Wei Xu
IPC分类号: C07D403/12 , A61K31/498 , C07D487/04 , C07D241/54 , A61K31/4985 , C07D413/12 , C07D401/12 , A61P35/00
CPC分类号: C07D401/12 , C07D241/44 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , Y02P20/55
摘要: The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.
摘要翻译: 本发明包括与许多恶性肿瘤如卵巢癌,宫颈癌,乳腺癌,结肠癌,直肠癌和成胶质细胞瘤等相关的磷脂酰肌醇3-激酶(PI3K)的小分子抑制剂。 因此,本发明的化合物可用于治疗,预防和/或抑制这些疾病。
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公开(公告)号:US20050227973A1
公开(公告)日:2005-10-13
申请号:US10498338
申请日:2002-12-13
申请人: S. Brown , Lynne Canne-Bannen , Erick Co , Vasu Jammalamadaka , Rickard Khoury , Moon Kim , Donna Le , Amy Tsuhako , Morrison Mac , Shumeye Mamo , John Nuss , Michael Prisbylla , Wei Xu
发明人: S. Brown , Lynne Canne-Bannen , Erick Co , Vasu Jammalamadaka , Rickard Khoury , Moon Kim , Donna Le , Amy Tsuhako , Morrison Mac , Shumeye Mamo , John Nuss , Michael Prisbylla , Wei Xu
IPC分类号: A61K31/40 , A61K31/18 , A61K31/277 , A61K31/405 , A61K31/44 , A61K31/4406 , A61K31/4418 , A61K31/445 , A61K31/4462 , A61K31/4465 , A61K31/4965 , A61K31/506 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P19/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07C303/02 , C07C303/40 , C07C309/87 , C07C311/29 , C07D207/09 , C07D211/34 , C07D213/56 , C07D213/65 , C07D213/70 , C07D233/48 , C07D233/54 , C07D295/13 , C07D295/15 , C07D295/185 , C07D295/215 , C07D311/70 , C07D409/04
CPC分类号: C07D409/04 , C07C311/29 , C07C2601/14 , C07D207/09 , C07D211/34 , C07D213/56 , C07D213/65 , C07D213/70 , C07D233/48 , C07D233/64 , C07D295/13 , C07D295/15 , C07D295/185 , C07D295/215 , C07D311/70
摘要: The present invention provides compounds useful for inhibiting the ADAM-10 protein. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. The invention also provides methods for making bis-aryl ether sulfonyl chorides and ADAM-10 modulators therefrom.
摘要翻译: 本发明提供了可用于抑制ADAM-10蛋白质的化合物。 这些化合物可用于体外研究ADAM-10(及其抑制)在生物过程中的作用。 本发明还包括药物组合物,其包含一种或多种本发明的ADAM-10抑制剂与药学上可接受的载体的组合。 这样的组合物可用于治疗癌症,关节炎和与血管发生相关的疾病。 相应地,本发明还包括治疗癌症,关节炎和与血管生成有关的疾病形式的方法,其中ADAM-10起关键作用。 本发明还提供从其制备双芳基醚磺酰氯和ADAM-10调节剂的方法。
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公开(公告)号:US20060199820A1
公开(公告)日:2006-09-07
申请号:US10518110
申请日:2003-06-11
申请人: Lynne Bannen , Erick Co , Vasu Jammalamadaka , John Nuss , Moon Hwan Kim , Donna Le , Amy Lew , Morrison Mac , Shumeye Mamo , Richard Khoury , Zhaoyang Wen , Wei Xu
发明人: Lynne Bannen , Erick Co , Vasu Jammalamadaka , John Nuss , Moon Hwan Kim , Donna Le , Amy Lew , Morrison Mac , Shumeye Mamo , Richard Khoury , Zhaoyang Wen , Wei Xu
IPC分类号: A61K31/5377 , A61K31/497 , A61K31/496 , A61K31/495 , C07D413/02 , C07D403/02
CPC分类号: C07D241/04 , C07C309/87 , C07D213/70 , C07D401/06 , C07D401/12 , C07D403/06 , C07D413/06
摘要: The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.
摘要翻译: 本发明提供了用于抑制ADAM-10蛋白质的化合物,具有选择性对MMP-1。 这些化合物可用于体外研究ADAM-10(及其抑制)在生物过程中的作用。 本发明还包括药物组合物,其包含一种或多种本发明的ADAM-10抑制剂与药学上可接受的载体的组合。 这样的组合物可用于治疗癌症,关节炎和与血管发生相关的疾病。 相应地,本发明还包括治疗癌症,关节炎和与血管生成有关的疾病形式的方法,其中ADAM-10起关键作用。
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公开(公告)号:US20080161305A1
公开(公告)日:2008-07-03
申请号:US11910720
申请日:2006-04-06
IPC分类号: A61K31/5377 , C07D413/12 , C12Q1/48 , C12N5/06
CPC分类号: C07D215/233
摘要: The present invention provides compounds, which have activity for modulating protein kinase enzymatic activity and are potentially useful for modulating cellular activities such as, e.g., proliferation, differentiation, programmed cell death, migration and chemoinvasion. The present invention also provides compositions containing such compounds, and methods for producing and using such compounds and compositions.
摘要翻译: 本发明提供具有调节蛋白激酶酶活性的活性并且可能用于调节细胞活性例如增殖,分化,程序性细胞死亡,迁移和化学侵蚀的化合物。 本发明还提供含有这些化合物的组合物,以及制备和使用这些化合物和组合物的方法。
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公开(公告)号:US20060122171A1
公开(公告)日:2006-06-08
申请号:US10533555
申请日:2003-11-14
申请人: Wei Xu , Lynne Canne Bannen , Samuel Brown , Erick Co , John Nuss , Moon Kim , Rhett Klein , Donna Lee , Amy Tsuhako , Morrison Mac , Jason Parks , Zhaoyang Wen , Wei Cheng
发明人: Wei Xu , Lynne Canne Bannen , Samuel Brown , Erick Co , John Nuss , Moon Kim , Rhett Klein , Donna Lee , Amy Tsuhako , Morrison Mac , Jason Parks , Zhaoyang Wen , Wei Cheng
IPC分类号: A61K31/55 , A61K31/454 , C07D403/14
CPC分类号: C07D403/14 , C07D401/14 , C07D413/14 , C07D451/04
摘要: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides oxindole derivatives which inhibit, regulate and/or modulate kinase receptor, particularly VEGF receptor 2 (Flk-1/KDR), FGFR1, and PDGFR (alpha and beta), signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.
摘要翻译: 本发明提供调节蛋白激酶酶活性以调节细胞活性如增殖,分化,程序性细胞死亡,迁移和化学侵蚀的化合物。 更具体地,本发明提供抑制,调节和/或调节激酶受体,特别是VEGF受体2(Flk-1 / KDR),FGFR1和PDGFR(α和β)的信号转导途径的羟吲哚衍生物,其与细胞的变化相关 如上所述的活性,含有这些化合物的组合物,以及使用它们治疗激酶依赖性疾病和病症的方法。
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公开(公告)号:US20070244116A1
公开(公告)日:2007-10-18
申请号:US11753503
申请日:2007-05-24
申请人: LYNNE BANNEN , Diva Chan , Jeff Chen , Lisa Dalrymple , Timothy Forsyth , Tai Huynh , Vasu Jammalamadaka , Richard Khoury , James Leahy , Morrison Mac , Grace Mann , Larry Mann , John Nuss , Jason Parks , Craig Takeuchi , Yong Wang , Wei Xu
发明人: LYNNE BANNEN , Diva Chan , Jeff Chen , Lisa Dalrymple , Timothy Forsyth , Tai Huynh , Vasu Jammalamadaka , Richard Khoury , James Leahy , Morrison Mac , Grace Mann , Larry Mann , John Nuss , Jason Parks , Craig Takeuchi , Yong Wang , Wei Xu
IPC分类号: A61K31/47 , A61K31/16 , A61K31/517 , C07C229/40 , C07D215/22 , C07D239/94 , C07D413/12 , C07D239/88 , C07C233/59 , A61K31/5355 , A61K31/196
CPC分类号: C07D215/233 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/5377 , C07D215/22 , C07D215/36 , C07D215/38 , C07D215/46 , C07D239/88 , C07D239/94 , C07D295/15 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C12Q1/485 , G01N2500/04 , Y02A50/393
摘要: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
摘要翻译: 本发明提供调节蛋白激酶酶活性以调节细胞活性如增殖,分化,程序性细胞死亡,迁移和化学侵蚀的化合物。 更具体地,本发明提供抑制,调节和/或调节与细胞活性变化相关的激酶受体,特别是c-Met,KDF,c-Kit,flt-3和flt-4信号转导途径的喹唑啉和喹啉 如上所述,含有这些化合物的组合物,及其用于治疗激酶依赖性疾病和病症的方法。 本发明还提供了制备上述化合物的方法和含有这些化合物的组合物。
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公开(公告)号:US20070054928A1
公开(公告)日:2007-03-08
申请号:US11586751
申请日:2006-10-26
申请人: Lynne Bannen , Diva Chan , Jeff Chen , Lisa Dalrymple , Timothy Forsyth , Tai Huynh , Vasu Jammalamadaka , Richard Khoury , James Leahy , Morrison Mac , Grace Mann , Larry Mann , John Nuss , Jason Parks , Craig Takeuchi , Yong Wang , Wei Xu
发明人: Lynne Bannen , Diva Chan , Jeff Chen , Lisa Dalrymple , Timothy Forsyth , Tai Huynh , Vasu Jammalamadaka , Richard Khoury , James Leahy , Morrison Mac , Grace Mann , Larry Mann , John Nuss , Jason Parks , Craig Takeuchi , Yong Wang , Wei Xu
IPC分类号: A61K31/517 , A61K31/4709 , C07D403/02 , C07D401/02
CPC分类号: C07D215/233 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/5377 , C07D215/22 , C07D215/36 , C07D215/38 , C07D215/46 , C07D239/88 , C07D239/94 , C07D295/15 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C12Q1/485 , G01N2500/04 , Y02A50/393
摘要: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
摘要翻译: 本发明提供调节蛋白激酶酶活性以调节细胞活性如增殖,分化,程序性细胞死亡,迁移和化学侵蚀的化合物。 更具体地,本发明提供抑制,调节和/或调节激酶受体,特别是c-Met,KDR,c-Kit,flt-3和flt-4,与细胞活性变化相关的信号转导途径的喹啉和喹啉 含有这些化合物的组合物,以及使用它们治疗激酶依赖性疾病和病症的方法。 本发明还提供了制备上述化合物的方法和含有这些化合物的组合物。
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公开(公告)号:US08324231B2
公开(公告)日:2012-12-04
申请号:US12597271
申请日:2008-04-24
申请人: Elena S. Koltun , Patrick Kearney , Naing Aay , Arlyn Arcalas , Wai Ki Vicky Chan , Jeffry Kimo Curtis , Hongwang Du , Ping Huang , Brian Kane , Moon Hwan Kim , Michael Pack , Amy L. Tsuhako , Wei Xu , Cristiana A. Zaharia , Peiwen Zhou
发明人: Elena S. Koltun , Patrick Kearney , Naing Aay , Arlyn Arcalas , Wai Ki Vicky Chan , Jeffry Kimo Curtis , Hongwang Du , Ping Huang , Brian Kane , Moon Hwan Kim , Michael Pack , Amy L. Tsuhako , Wei Xu , Cristiana A. Zaharia , Peiwen Zhou
IPC分类号: A01N43/54 , A61K31/505
CPC分类号: C07D405/04 , C07D403/04 , C07D413/04 , C07D417/04
摘要: A compound having Formula I: or a pharmaceutically acceptable salt thereof, wherein X, R, R and R are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof. The compounds of Formula I are inhibitors of Casein kinase II (CK2) pathways.
摘要翻译: 具有式I的化合物或其药学上可接受的盐,其中X,R,R和R如说明书中所定义; 其药物组合物; 及其使用方法。 式I的化合物是酪蛋白激酶II(CK2)途径的抑制剂。
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公开(公告)号:US20100135954A1
公开(公告)日:2010-06-03
申请号:US12597275
申请日:2008-04-25
申请人: Amy L. Tsuhako , Naing Aay , S. David Brown , Wai Ki Vicky Chan , Hongwang Du , Ping Huang , Brian Kane , Patrick Kearney , Moon Hwan Kim , Elena S. Koltun , Michael Pack , Wei Xu , Peiwen Zhou
发明人: Amy L. Tsuhako , Naing Aay , S. David Brown , Wai Ki Vicky Chan , Hongwang Du , Ping Huang , Brian Kane , Patrick Kearney , Moon Hwan Kim , Elena S. Koltun , Michael Pack , Wei Xu , Peiwen Zhou
IPC分类号: A61K38/20 , A61K38/21 , A61K31/567 , A61K31/5377 , A61K31/496 , A61K31/506 , C07D413/02 , C07D403/10 , C07D401/10 , A61P35/00
CPC分类号: C07D213/64 , C07D239/36 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/04 , C07D409/12 , C07D413/04
摘要: A compound having Formula I or II (Formula I) or (Formula II), or a pharmaceutically acceptable salt thereof, wherein X, Z, R1, R2, R11 and R12 are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
摘要翻译: 具有式I或II(式I)或(式II)的化合物或其药学上可接受的盐,其中X,Z,R 1,R 2,R 11和R 12如说明书中所定义; 其药物组合物; 及其使用方法。
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