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1. 发明申请

WO2007089768A2 4-ARYL-2-AMINO-PYRIMIDINES OR 4-ARYL-2-AMINOALKYL-PYRIMIDINES AS JAK-2 MODULATORS AND METHODS OF USE 审中-公开
标题翻译：作为JAK-2调节剂的4-亚芳基-2-氨基吡啶或4-亚氨基-2-氨基亚氨基嘧啶和使用方法
公开(公告)号：WO2007089768A2
公开(公告)日：2007-08-09
申请号：PCT/US2007/002515
申请日：2007-01-30
申请人： EXELIXIS, INC. , MANN, Grace , AAY, Naing , ARCALAS, Arlyn , BROWN, S. David , CHAN, Wai Ki Vicky , CHEN, Jeff , DU, Hongwang , EPSHTEYN, Sergey , FORSYTH, Timothy , GALAN, Adam A. , HUYNH, Tai Phat , IBRAHIM, Mohamed Abdulkader , JOHNSON, Henry William Beecroft , KANE, Brian , KEARNEY, Patrick , KIM, Byung Gyu , KOLTUN, Elena , LEAHY, James William , LEE, Matthew Sangyup , LEWIS, Gary L. , MEYR, Lisa E. , NOGUCHI, Robin Tammie , PACK, Michael , RIDGWAY, Brian Hugh , SHI, Xian , WOOLFREY, John , ZHOU, Peiwen
发明人： MANN, Grace , AAY, Naing , ARCALAS, Arlyn , BROWN, S. David , CHAN, Wai Ki Vicky , CHEN, Jeff , DU, Hongwang , EPSHTEYN, Sergey , FORSYTH, Timothy , GALAN, Adam A. , HUYNH, Tai Phat , IBRAHIM, Mohamed Abdulkader , JOHNSON, Henry William Beecroft , KANE, Brian , KEARNEY, Patrick , KIM, Byung Gyu , KOLTUN, Elena , LEAHY, James William , LEE, Matthew Sangyup , LEWIS, Gary L. , MEYR, Lisa E. , NOGUCHI, Robin Tammie , PACK, Michael , RIDGWAY, Brian Hugh , SHI, Xian , WOOLFREY, John , ZHOU, Peiwen
IPC分类号： C07D239/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14
CPC分类号： C07D239/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/12 , C07D453/02 , C07D487/04
摘要： This invention relates to certain pyrimidine derivative inhibitors of JAK-2, having Formula (I): wherein D, E, L, Z, R 1 , R 2 , R 25 , and n1 are as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof.
摘要翻译：本发明涉及具有式（I）的JAK-2的某些嘧啶衍生物抑制剂：其中D，E，L，Z，R 1，R 2， SUP＆gt; 25＆gt;和n1如本说明书中所定义，其药学上可接受的盐，其药物组合物及其使用方法。

2. 发明申请

WO2008143759A1 PYRIMIDINONES AS CASEIN KINASE II (CK2) MODULATORS 审中-公开
标题翻译：吡啶二酮作为CASEIN KINASE II（CK2）调节剂
公开(公告)号：WO2008143759A1
公开(公告)日：2008-11-27
申请号：PCT/US2008/005419
申请日：2008-04-24
申请人： EXELIXIS, INC. , KOLTUN, Elena S. , KEARNEY, Patrick , AAY, Naing , ARCALAS, Arlyn , CHAN, Wai Ki Vicky , CURTIS, Jeffry Kimo , DU, Hongwang , HUANG, Ping , KANE, Brian , KIM, Moon Hwan , PACK, Michael , TSUHAKO, Amy L. , XU, Wei , ZAHARIA, Cristiana A. , ZHOU, Peiwen
发明人： KOLTUN, Elena S. , KEARNEY, Patrick , AAY, Naing , ARCALAS, Arlyn , CHAN, Wai Ki Vicky , CURTIS, Jeffry Kimo , DU, Hongwang , HUANG, Ping , KANE, Brian , KIM, Moon Hwan , PACK, Michael , TSUHAKO, Amy L. , XU, Wei , ZAHARIA, Cristiana A. , ZHOU, Peiwen
IPC分类号： C07D403/04 , C07D405/04 , C07D413/04 , C07D417/04 , A61K31/513 , A61P35/00
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 Fomula 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。 Fomula I的化合物是酪蛋白激酶II（CK2）途径的抑制剂。

3. 发明申请

WO2008133955A1 6-PHENYLPYRIMIDINONES AS PIM MODULATORS 审中-公开
标题翻译： 6-苯基嘧啶酮作为PIM调节剂
公开(公告)号：WO2008133955A1
公开(公告)日：2008-11-06
申请号：PCT/US2008/005309
申请日：2008-04-25
申请人： EXELIXIS, INC. , KOLTUN, Elena S. , TSUHAKO, Amy L. , AAY, Naing , BROWN, S. David , CHAN, Wai Ki Vicky , DU, Hongwang , HUANG, Ping , KANE, Brian , KEARNEY, Patrick , KIM, Moon Hwan , PACK, Michael , XU, Wei , ZHOU, Peiwen
发明人： KOLTUN, Elena S. , TSUHAKO, Amy L. , AAY, Naing , BROWN, S. David , CHAN, Wai Ki Vicky , DU, Hongwang , HUANG, Ping , KANE, Brian , KEARNEY, Patrick , KIM, Moon Hwan , PACK, Michael , XU, Wei , ZHOU, Peiwen
IPC分类号： C07D239/36 , C07D403/12 , C07D413/04 , C07D409/04 , C07D407/12 , C07D409/12 , A61K31/513 , A61P35/00 , C07D213/64
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, R 1 , R 2 , R 11 and R 12 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 本说明书中的定义如下：＆lt; 11＆gt;和＆lt; 12＆gt; 其药物组合物; 及其使用方法。

4. 发明申请

WO2010091164A1 INHIBITORS OF GLUCOSYLCERAMIDE SYNTHASE 审中-公开
标题翻译：葡萄球菌素合成酶抑制剂
公开(公告)号：WO2010091164A1
公开(公告)日：2010-08-12
申请号：PCT/US2010/023168
申请日：2010-02-04
申请人： EXELIXIS, INC. , AAY, Naing , AOYAMA, Ron, G. , ARCALAS, Arlyn , CHAN, Wai Ki, Vicky , DU, Hongwang , KEARNEY, Patrick , KOLTUN, Elena, S. , NACHTIGALL, Jason, August , PACK, Michael , RICHARDS, Steven, James
发明人： AAY, Naing , AOYAMA, Ron, G. , ARCALAS, Arlyn , CHAN, Wai Ki, Vicky , DU, Hongwang , KEARNEY, Patrick , KOLTUN, Elena, S. , NACHTIGALL, Jason, August , PACK, Michael , RICHARDS, Steven, James
IPC分类号： C07C233/55 , C07D205/04 , C07D207/09 , C07D207/14 , C07D209/18 , C07D211/56 , C07D211/58 , C07D213/56 , C07D403/06 , C07D295/185 , C07D233/64 , C07D319/16 , C07D453/02 , C07D487/04 , A61K31/495
CPC分类号： C07C237/22 , C07C2601/02 , C07C2601/14 , C07D205/04 , C07D207/09 , C07D207/14 , C07D209/18 , C07D211/56 , C07D211/58 , C07D213/56 , C07D233/64 , C07D295/185 , C07D319/16 , C07D403/06 , C07D453/02 , C07D487/04
摘要： The present invention comprises glucosylceramide synthase (GCS) modulators of following structural formula (I); wherein R1, A, L, R2, R3, and m are defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof, and methods of making said compounds. The invention further comprises compositions comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which GCS is a mediator or is implicated. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases in which GCS is a mediator or is implicated.
摘要翻译：本发明包括以下结构式（I）的葡萄糖神经酰胺合成酶（GCS）调节剂; 其中R1，A，L，R2，R3和m如本文所定义，以及它们的N-氧化物及其药学上可接受的盐，以及制备所述化合物的方法。本发明进一步包括含有化合物，N-氧化物和/或其药学上可接受的盐的组合物。本发明还包括使用化合物和组合物来治疗其中GCS是介质或涉及的疾病。本发明还包括在药物中和用于制备药物中的用途，特别是用于治疗其中GCS是介质或涉及的疾病。

5. 发明申请

WO2010091104A1 GLUCOSYLCERAMIDE SYNTHASE INHIBITORS 审中-公开
标题翻译： GLUCOSYLCERAMIDE SYNTHASE抑制剂
公开(公告)号：WO2010091104A1
公开(公告)日：2010-08-12
申请号：PCT/US2010/023080
申请日：2010-02-03
申请人： EXELIXIS, INC. , CHAN, Wai, Ki, Vicky , DU, Hongwang , KEARNEY, Patrick , KOLTUN, Elena, S. , NACHTIGALL, Jason, August , NOSON, Kevin , PACK, Michael , RICHARDS, Steven, James
发明人： CHAN, Wai, Ki, Vicky , DU, Hongwang , KEARNEY, Patrick , KOLTUN, Elena, S. , NACHTIGALL, Jason, August , NOSON, Kevin , PACK, Michael
IPC分类号： C07D401/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D471/04 , C07D487/04 , C07D213/643 , A61K31/44 , A61K31/496 , A61P3/00 , A61P35/00
CPC分类号： C07D213/643 , C07D401/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D471/04 , C07D487/04
摘要： The present invention comprises glucosylceramide synthase (GCS) inhibitors of structural formula (I), and pharmaceutically acceptable salts thereof, wherein R 1 , E, A, L, X 1 , Q, R 4 , R 5 , m and n, are as defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which GCS is a mediator or is implicated. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases in which GCS is a mediator or is implicated.
摘要翻译：本发明包括结构式（I）的葡萄糖神经酰胺合成酶（GCS）抑制剂及其药学上可接受的盐，其中R 1，E，A，L，X 1，Q，R 4，R 5，m和n如本文所定义，以及它们的N-氧化物及其药学上可接受的盐。本发明还包括包含化合物，N-氧化物和/或其药学上可接受的盐的组合物。本发明还包括使用化合物和组合物来治疗其中GCS是介质或涉及的疾病。本发明还包括在药物中和用于制备药物中的用途，特别是用于治疗其中GCS是介质或涉及的疾病。

6. 发明申请

WO2010138487A1 BENZOXAZEPINES AS INHIBITORS OF PI3K/m TOR AND METHODS OF THEIR USE AND MANUFACTURE 审中-公开
标题翻译：苯并噻唑作为PI3K / m TOR的抑制剂及其使用和制造方法
公开(公告)号：WO2010138487A1
公开(公告)日：2010-12-02
申请号：PCT/US2010/036032
申请日：2010-05-25
申请人： EXELIXIS, INC. , AAY, Naing , ARCALAS, Arlyn , BOWLES, Owen, Joseph , BUSSENIUS, Joerg , CURTIS, Jeffry, Kimo , DEFINA, Steven, Charles , DUBENKO, Larisa , HARRIS, Jason, R. , JACKSON-UGUETO, Eileen, E. , MANALO, Jean-Claire, Limun , KIM, Angie, Inyoung , PACK, Michael , PETO, Csaba, J. , RICE, Kenneth, D. , TSANG, Tsze, H.
发明人： AAY, Naing , ARCALAS, Arlyn , BOWLES, Owen, Joseph , BUSSENIUS, Joerg , CURTIS, Jeffry, Kimo , DEFINA, Steven, Charles , DUBENKO, Larisa , HARRIS, Jason, R. , JACKSON-UGUETO, Eileen, E. , MANALO, Jean-Claire, Limun , KIM, Angie, Inyoung , PACK, Michael , PETO, Csaba, J. , RICE, Kenneth, D. , TSANG, Tsze, H.
IPC分类号： C07D413/04 , C07D413/14 , C07D417/14 , C07D451/02 , C07D471/10 , C07D487/04 , C07D487/08 , A61K31/553 , A61P35/00
CPC分类号： C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： The invention is directed to Compounds of Formula (I): the invention provides compounds that inhibit, regulate, and/or modulate P13K and/or mTOR that are useful in the treatment of hyperproliferative diseases, such as cancer, in mammals. This invention also provides methods of making the compound methods of using such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds. For example, cancer in which activity against PI3fC-alph mTOR, or both contributes to its pathology and/or symptomatology include breast cancer mantle cell lymphoma, renal cell carcinoma, acute myelogenous leukemia, chronic myelogenous leukemia, NPM/ALK- transformed anaplastic large cell lymphoma, diffu large B cell lymphoma, rhabdomyosarcoma, ovarian cancer, endometrial cancer, cervic cancer, non small cell lung carcinoma, small cell lung carcinoma, adenocarcinoma, col cancer, rectal cancer, gastric carcinoma, hepatocellular carcinoma, melanoma, pancreat cancer, prostate carcinoma, thyroid carcinoma, anaplastic large cell lymphoma, hemangiom glioblastoma, or head and neck cancer.
摘要翻译：本发明涉及式（I）的化合物：本发明提供抑制，调节和/或调节P13K和/或mTOR的化合物，其可用于治疗哺乳动物中过度增殖性疾病如癌症。本发明还提供了使用这些化合物在哺乳动物，特别是人类中过度增殖性疾病的治疗方法和含有这些化合物的药物组合物的方法。例如，其中针对PI3fC-alph mTOR或其两者都有助于其病理学和/或症状学的活性的癌症包括乳腺癌套细胞淋巴瘤，肾细胞癌，急性骨髓性白血病，慢性骨髓性白血病，NPM / ALK转化的变应性大细胞淋巴瘤，弥漫性大B细胞淋巴瘤，横纹肌肉瘤，卵巢癌，子宫内膜癌，宫颈癌，非小细胞肺癌，小细胞肺癌，腺癌，胆囊癌，直肠癌，胃癌，肝细胞癌，黑素瘤，胰腺癌，前列腺癌，甲状腺癌，间变性大细胞淋巴瘤，血管瘤胶质母细胞瘤或头颈癌。

7. 发明申请

WO2010138490A1 BENZOXAZEPINES AS INHIBITORS OF MTOR AND METHODS OF THEIR USE AND MANUFACTURE 审中-公开
标题翻译：苯并噻唑作为MTOR的抑制剂及其使用和制造方法
公开(公告)号：WO2010138490A1
公开(公告)日：2010-12-02
申请号：PCT/US2010/036038
申请日：2010-05-25
申请人： EXELIXIS, INC. , AAY, Naing , BLAZEY, Charles, M. , BOWLES, Owen, Joseph , BUSSENIUS, Joerg , CURTIS, Jeffry, Kimo , DEFINA, Steven, Charles , DUBENKO, Larisa , HARRIS, Jason, R. , JACKSON-UGUETO, Eileen, E. , KIM, Angie, Inyoung , MANALO, Jean-claire, Limun , PACK, Michael , PETO, Csaba, J. , RICE, Kenneth, D. , TSANG, Tsze, H. , WANG, Longcheng
发明人： AAY, Naing , BLAZEY, Charles, M. , BOWLES, Owen, Joseph , BUSSENIUS, Joerg , CURTIS, Jeffry, Kimo , DEFINA, Steven, Charles , DUBENKO, Larisa , HARRIS, Jason, R. , JACKSON-UGUETO, Eileen, E. , KIM, Angie, Inyoung , MANALO, Jean-claire, Limun , PACK, Michael , PETO, Csaba, J. , RICE, Kenneth, D. , TSANG, Tsze, H. , WANG, Longcheng
IPC分类号： C07D413/04 , C07D413/14 , C07D417/14 , C07D471/08 , C07D487/08 , C07D519/00 , A61K31/553 , A61P35/00
CPC分类号： C07D413/04 , C07D413/14 , C07D417/14 , C07D451/02 , C07D451/04 , C07D451/06 , C07D453/06 , C07D487/08
摘要： The invention is directed to inhibitors of mTOR and pharmaceutically acceptable salts or solvates thereof, as well as methods of using them. The inhibitors are generally of structural formula wherein the combination of R 1 and R 2 are as defined herein, and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及mTOR及其药学上可接受的盐或溶剂化物的抑制剂，以及使用它们的方法。抑制剂通常具有结构式，其中R1和R2的组合如本文所定义，及其药学上可接受的盐。

8. 发明申请

WO2002061073A2 HIGH THROUGHPUT GENETIC SCREENING OF LIPID AND CHOLESTEROL PROCESSING USING FLUORESCENT COMPOUNDS 审中-公开
标题翻译：使用荧光化合物进行脂肪和胆固醇加工的高通量遗传筛选
公开(公告)号：WO2002061073A2
公开(公告)日：2002-08-08
申请号：PCT/US2002/002766
申请日：2002-01-30
申请人： THOMAS JEFFERSON UNIVERSITY , FARBER, Steven , PACK, Michael
发明人： FARBER, Steven , PACK, Michael
IPC分类号： C12N15/00
CPC分类号： G01N33/5088 , A01K2217/05 , A01K2227/40 , A01K2267/03 , A01K2267/0362 , C12N15/8509
摘要： The present invention utilizes fluorescent lipids, particularly quenched phospholipid or cholesterol analogues, to facilitate screening for phenotypes representing perturbations of lipid processing; screening for genetic mutations that lead to disorders of phospholipid and/or cholesterol metabolism; and screening of compounds designed to treat disorders of phospholipid and/or cholesterol metabolism. The present invention is a mutant fish containing a metabolic defect affecting phospholipid and cholesterol processing. The mutant fish is useful for studying phospholipid and cholesterol metabolism and for screening compounds designed to treat disorders of phospholipid and/or cholesterol metabolism.
摘要翻译：本发明利用荧光脂质，特别是淬灭的磷脂或胆固醇类似物，以便于筛选代表脂质加工扰动的表型; 筛选导致磷脂和/或胆固醇代谢紊乱的遗传突变; 以及筛选旨在治疗磷脂和/或胆固醇代谢紊乱的化合物。本发明是含有影响磷脂和胆固醇加工的代谢缺陷的突变鱼。突变鱼可用于研究磷脂和胆固醇代谢，并用于筛选旨在治疗磷脂和/或胆固醇代谢紊乱的化合物。

9. 发明申请

WO2007075753A2 HIGH THROUGH-PUT METHOD OF SCREENING COMPOUNDS FOR PHARMACOLOGICAL ACTIVITY 审中-公开
标题翻译：用于药物活性的筛选化合物的高通量方法
公开(公告)号：WO2007075753A2
公开(公告)日：2007-07-05
申请号：PCT/US2006/048542
申请日：2006-12-19
申请人： THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA , PACK, Michael
发明人： PACK, Michael
IPC分类号： A01K67/027 , A61K49/00
CPC分类号： A61K49/0008 , A61K49/0021 , A61K49/0052 , A61K49/0089
摘要： Provided is a method for high through-put screening for physiologic alterations in an altered teleost displaying a phenotype that is characteristic of the alteration and different from a wild-type, unaltered, matched teleost, comprising the steps of contacting the teleost displaying a genetically-inherited or chemically-induced phenotype with at least one test compound for a sufficient time and under suitable conditions to induce a response in the teleost indicative of pharmacological activity of the compound, and detecting and comparing the response with that of a matched, untreated, control, wherein a change in the teleost signal that is different from that of the control, indicates an altered phenotype and pharmacological activity of the at least one test compound. Further provided are the compounds identified by this method, the zebrafish having an altered phenotype resulting from treatment in accordance with these methods, and kits for facilitating the high through-put screening methods.
摘要翻译：本发明提供了一种显示表现型变异和不同于野生型未改变的匹配硬骨转基因的表型的改变的硬骨鱼的生物学改变的高通量筛选方法，包括以下步骤：遗传的或化学诱导的表型与至少一种测试化合物足够的时间和在合适的条件下诱导指示化合物的药理学活性的硬骨中的反应，以及检测和比较匹配的未处理的对照的响应其中所述硬骨架信号与所述对照不同的改变指示所述至少一种测试化合物的改变的表型和药理学活性。进一步提供的是通过该方法鉴定的化合物，斑马鱼具有根据这些方法的治疗产生的改变的表型，以及用于促进高通量筛选方法的试剂盒。

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