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1. 发明申请

WO2006014325A3 C-MET MODULATORS AND METHOD OF USE 审中-公开
标题翻译： C-MET调制器及其使用方法
公开(公告)号：WO2006014325A3
公开(公告)日：2007-03-01
申请号：PCT/US2005023364
申请日：2005-07-01
申请人： EXELIXIS INC , BANNEN LYNNE CANNE , CHAN DIVA SZE-MING , DALRYMPLE LISA ESTHER , JAMMALAMADAKA VASU , KHOURY RICHARD GEORGE , LEAHY JAMES WILLIAM , MAC MORRISON B , MANN GRACE , MANN LARRY W , NUSS JOHN M , PARKS JASON JEVIOUS , WANG YONG , XU WEI
发明人： BANNEN LYNNE CANNE , CHAN DIVA SZE-MING , DALRYMPLE LISA ESTHER , JAMMALAMADAKA VASU , KHOURY RICHARD GEORGE , LEAHY JAMES WILLIAM , MAC MORRISON B , MANN GRACE , MANN LARRY W , NUSS JOHN M , PARKS JASON JEVIOUS , WANG YONG , XU WEI
IPC分类号： C07D471/04 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/519 , A61K31/52 , A61K31/522 , A61P35/00 , C07D473/06 , C07D473/16 , C07D473/18 , C07D473/22 , C07D473/24 , C07D473/30 , C07D473/34 , C07D473/38 , C07D473/40 , C07D487/04 , C07D491/04 , C07D495/04
CPC分类号： C07D487/04 , C07D209/52 , C07D471/04 , C07D473/30 , C07D473/32 , C07D493/04 , C07D493/14 , C07D493/20 , C07D498/04
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 appropriately functionalized 5,6-fused bicyclics which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, and flt-3, 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：本发明提供用于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，本发明提供了适当的功能化的5,6融合双链体，其抑制，调节和/或调节与上述细胞活性变化相关的激酶受体，特别是c-Met，KDR和flt-3信号转导途径，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。

2. 发明申请

WO2005030140A3 C-MET MODULATORS AND METHODS OF USE 审中-公开
标题翻译： C-MET调制器和使用方法
公开(公告)号：WO2005030140A3
公开(公告)日：2005-05-19
申请号：PCT/US2004031523
申请日：2004-09-24
申请人： EXELIXIS INC , BANNEN LYNNE CANNE , CHAN DIVA SZE-MING , CHEN JEFF , DALRYMPLE LISA ESTHER , FORSYTH TIMOTHY PATRICK , HUYNH TAI PHAT , JAMMALAMADAKA VASU , KHOURY RICHARD GEORGE , LEAHY JAMES WILLIAM , MAC MORRISON B , MANN GRACE , MANN LARRY W , NUSS JOHN M , PARKS JASON JEVIOUS , TAKEUCHI CRAIG STACY , WANG YONG , XU WEI
发明人： BANNEN LYNNE CANNE , CHAN DIVA SZE-MING , CHEN JEFF , DALRYMPLE LISA ESTHER , FORSYTH TIMOTHY PATRICK , HUYNH TAI PHAT , JAMMALAMADAKA VASU , KHOURY RICHARD GEORGE , LEAHY JAMES WILLIAM , MAC MORRISON B , MANN GRACE , MANN LARRY W , NUSS JOHN M , PARKS JASON JEVIOUS , TAKEUCHI CRAIG STACY , WANG YONG , XU WEI
IPC分类号： A61K20060101 , A61K31/47 , A61K31/535 , C07D215/16 , C07D215/20 , C07D413/00
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
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：本发明提供了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，迁移和化学侵袭的化合物。更具体地说，本发明提供了抑制，调节和/或调节激酶受体，特别是与细胞活性改变有关的c-Met，KDR，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，以及使用它们来治疗激酶依赖性疾病和病症的方法。本发明还提供制备如上所述化合物的方法和含有这些化合物的组合物。

3. 发明申请

WO2005117909A3 KINASE MODULATORS AND METHODS OF USE 审中-公开
标题翻译：激酶调节剂及其使用方法
公开(公告)号：WO2005117909A3
公开(公告)日：2006-04-27
申请号：PCT/US2005013860
申请日：2005-04-22
申请人： EXELIXIS INC , ANAND NEEL K , BLAZEY CHARLES M , BOWLES OWEN JOSEPH , BUSSENIUS JOERG , CANNE BANNEN LYNNE , CHAN DIVA SZE-MING , CHEN BAILI , CO ERICK WANG , COSTANZO SIMONA , DEFINA STEVEN CHARLES , DUBENKO LARISA , FRANZINI MAURIZIO , HUANG PING , JAMMALAMADAKA VASU , KHOURY RICHARD GEORGE , KIM MOON HWAN , KLEIN RHETT RONALD , LE DONNA TRA , MAC MORRISON B , NUSS JOHN M , PARKS JASON JEVIOUS , RICE KENNETH D , TSANG TSZE H , TSUHAKO AMY LEW , WANG YONG , XU WEI
发明人： ANAND NEEL K , BLAZEY CHARLES M , BOWLES OWEN JOSEPH , BUSSENIUS JOERG , CANNE BANNEN LYNNE , CHAN DIVA SZE-MING , CHEN BAILI , CO ERICK WANG , COSTANZO SIMONA , DEFINA STEVEN CHARLES , DUBENKO LARISA , FRANZINI MAURIZIO , HUANG PING , JAMMALAMADAKA VASU , KHOURY RICHARD GEORGE , KIM MOON HWAN , KLEIN RHETT RONALD , LE DONNA TRA , MAC MORRISON B , NUSS JOHN M , PARKS JASON JEVIOUS , RICE KENNETH D , TSANG TSZE H , TSUHAKO AMY LEW , WANG YONG , XU WEI
IPC分类号： A61K31/7076 , C07D487/04 , A61K31/496
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of the Formula (I) and (II) wherein R, R 21 , R 25 -R 33 , m, n, X 21 -X 23 , and Q 1 are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly p70S6 and/or Akt kinases. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.
摘要翻译：本发明涉及式（I）和（II）的化合物，其中R 1，R 21，R 23，R 33，m ，n，X 21 -X 23和Q 1在本文中定义。该化合物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。本发明的化合物抑制，调节和/或调节激酶，特别是p70S6和/或Akt激酶。使用和制备化合物及其药物组合物以治疗激酶依赖性疾病和病症的方法也是本发明的一个方面。

4. 发明申请

WO2006025979A2 MODULATORS OF NUCLEAR RECEPTORS 审中-公开
标题翻译：核受体调节剂
公开(公告)号：WO2006025979A2
公开(公告)日：2006-03-09
申请号：PCT/US2005026353
申请日：2005-07-24
申请人： EXELIXIS INC , BAYNE CHRISTOPHER D , JOHNSON ALAN T , LU SHAO-PO , MOHAN RAJU , NYMAN MICHAEL C , SCHWEIGER EDWIN J , STEVENS WILLIAM C JR , WANG HAIXIA , XIE YINONG , BANNEN LYNNE CANNE , CHAN DIVA SZE-MING , HUANG PING , JAMMALAMADAKA VASU , KHOURY RICHARD G , MAC MORRISON B , PARKS JASON JEVIOUS , WANG YONG , XU WEI
发明人： BAYNE CHRISTOPHER D , JOHNSON ALAN T , LU SHAO-PO , MOHAN RAJU , NYMAN MICHAEL C , SCHWEIGER EDWIN J , STEVENS WILLIAM C JR , WANG HAIXIA , XIE YINONG , BANNEN LYNNE CANNE , CHAN DIVA SZE-MING , HUANG PING , JAMMALAMADAKA VASU , KHOURY RICHARD G , MAC MORRISON B , PARKS JASON JEVIOUS , WANG YONG , XU WEI
IPC分类号： A61K31/4439 , C07D213/85 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/12
CPC分类号： C07D401/12 , C07D213/84 , C07D213/85 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/12
摘要： Compounds of the invention, such as compounds of formula (I), where n, m, A, R1, R2, R3, R4 and R5 are defined herein, are useful as modulators of the activity of liver X receptors. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
摘要翻译：本发明的化合物，例如其中n，m，A，R 1，R 2，R 3，R 4和R 5如本文所定义的式（I）化合物可用作肝X受体活性的调节剂。还公开了含有该化合物的药物组合物和使用该化合物的方法。

5. 发明申请

WO2006025979A9 MODULATORS OF NUCLEAR RECEPTORS 审中-公开
公开(公告)号：WO2006025979A9
公开(公告)日：2006-04-20
申请号：PCT/US2005026353
申请日：2005-07-24
申请人： EXELIXIS INC , BAYNE CHRISTOPHER D , JOHNSON ALAN T , LU SHAO-PO , MOHAN RAJU , NYMAN MICHAEL C , SCHWEIGER EDWIN J , STEVENS WILLIAM C JR , WANG HAIXIA , XIE YINONG , BANNEN LYNNE CANNE , CHAN DIVA SZE-MING , HUANG PING , JAMMALAMADAKA VASU , KHOURY RICHARD G , MAC MORRISON B , PARKS JASON JEVIOUS , WANG YONG , XU WEI
发明人： BAYNE CHRISTOPHER D , JOHNSON ALAN T , LU SHAO-PO , MOHAN RAJU , NYMAN MICHAEL C , SCHWEIGER EDWIN J , STEVENS WILLIAM C JR , WANG HAIXIA , XIE YINONG , BANNEN LYNNE CANNE , CHAN DIVA SZE-MING , HUANG PING , JAMMALAMADAKA VASU , KHOURY RICHARD G , MAC MORRISON B , PARKS JASON JEVIOUS , WANG YONG , XU WEI
IPC分类号： A61K31/4439 , C07D213/85 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/12
CPC分类号： C07D401/12 , C07D213/84 , C07D213/85 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/12
摘要： Compounds of the invention, such as compounds of formula (I), where n, m, A, R1, R2, R3, R4 and R5 are defined herein, are useful as modulators of the activity of liver X receptors. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

6. 发明申请

WO2010003133A3 CDK MODULATORS 审中-公开
标题翻译： CDK调制器
公开(公告)号：WO2010003133A3
公开(公告)日：2010-03-18
申请号：PCT/US2009049637
申请日：2009-07-02
申请人： EXELIXIS INC , BAHCECI SULEYMAN , CHAN BRYAN , CHAN DIVA SZE-MING , CHEN JEFF , FORSYTH TIMOTHY PATRICK , FRANZINI MAURIZIO , JAMMALAMADAKA VASU , JEONG JOON WON , JONES LISA RENEE , KELLEY RYAN MICHAEL , KIM MOON HWAN , LEAHY JAMES W , MAC MORRISON B , NOGUCHI ROBIN TAMMIE , RAO PALLAVI , RIDGWAY BRIAN HUGH , XU WEI , WANG YONG
发明人： BAHCECI SULEYMAN , CHAN BRYAN , CHAN DIVA SZE-MING , CHEN JEFF , FORSYTH TIMOTHY PATRICK , FRANZINI MAURIZIO , JAMMALAMADAKA VASU , JEONG JOON WON , JONES LISA RENEE , KELLEY RYAN MICHAEL , KIM MOON HWAN , LEAHY JAMES W , MAC MORRISON B , NOGUCHI ROBIN TAMMIE , RAO PALLAVI , RIDGWAY BRIAN HUGH , XU WEI , WANG YONG
IPC分类号： A61K31/437 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/5383 , A61K31/55 , A61P35/00 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/107 , C07D498/04 , C07D498/14
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： A compound according to Formula I : or a pharmaceutically-acceptable salt thereof, wherein R1, R3, A, B and D are as defined in the specification; pharmaceutical compositions thereof, and methods of use thereof.
摘要翻译：根据式I的化合物或其药学上可接受的盐，其中R1，R3，A，B和D如说明书中所定义; 其药物组合物及其使用方法。

7. 发明申请

WO2007044729A3 N- (3-AMINO-QUINOXALIN-2-YL) -SULFONAMIDE DERIVATIVES AND THEIR USE AS PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS 审中-公开
标题翻译： N-（3-氨基 - 喹喔啉-2-基） - 磺酰胺衍生物及其作为磷酸二氢吲哚-3-激酶抑制剂的用途
公开(公告)号：WO2007044729A3
公开(公告)日：2007-08-09
申请号：PCT/US2006039574
申请日：2006-10-09
申请人： EXELIXIS INC , BAJJALIEH WILLIAM , BANNEN LYNNE CANNE , BROWN S DAVID , KEARNEY PATRICK , MAC MORRISON , MARLOWE CHARLES K , NUSS JOHN M , TESFAI ZEROM , WANG YONG , XU WEI
发明人： BAJJALIEH WILLIAM , BANNEN LYNNE CANNE , BROWN S DAVID , KEARNEY PATRICK , MAC MORRISON , MARLOWE CHARLES K , NUSS JOHN M , TESFAI ZEROM , WANG YONG , XU WEI
IPC分类号： C07D241/44 , A61K31/498 , A61K31/4985 , A61P35/00 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
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。

8. 发明申请

WO2007089510A3 METHODS FOR DEHYDRATION OF SUGARS 审中-公开
标题翻译：蔗糖脱水方法
公开(公告)号：WO2007089510A3
公开(公告)日：2008-01-17
申请号：PCT/US2007001945
申请日：2007-01-24
申请人： BATTELLE MEMORIAL INSTITUTE , HOLLADAY JOHNATHAN E , HU JIANLI , ZHANG XINJIE , WANG YONG
发明人： HOLLADAY JOHNATHAN E , HU JIANLI , ZHANG XINJIE , WANG YONG
IPC分类号： C07D493/04 , C07H1/00 , C07H3/10 , C08G63/672
CPC分类号： C07D493/04
摘要： The invention includes a method of dehydration of a sugar using a dehydration catalyst and a co-catalyst within a reactor. A sugar is introduced and H 2 is flowed through the reactor at a pressure of less than or equal to about 300 psig to convert at least some of the sugar into an anhydrosugar product. The invention includes a process for producing isosorbide. A starting material comprising sorbitol is flowed into a reactor. H 2 is counter flowed through the reactor. The starting material is exposed to a catalyst in the presence of a co- catalyst which comprises at least one metal. The exposing is conducted at a hydrogen pressure of less than or equal to 300 psig within the reactor and the hydrogen removes at least some of any water present during the exposing and inhibits formation of colored byproducts.
摘要翻译：本发明包括使用反应器内的脱水催化剂和助催化剂使糖脱水的方法。引入糖，并且H 2 O 2以小于或等于约300psig的压力流过反应器，以将至少一些糖转化为脱水糖产物。本发明包括制备异山梨醇的方法。将含有山梨醇的原料流入反应器。 H 2反向流过反应器。在包含至少一种金属的助催化剂的存在下，将原料暴露于催化剂。暴露在反应器内在小于或等于300psig的氢气压力下进行，并且氢去除暴露期间存在的任何水中的至少一些，并且抑制着色副产物的形成。

9. 发明申请

WO2006086733A3 PROCESS FOR PREPARING MAYTANSINOID ANTIBODY CONJUGATES 审中-公开
标题翻译：制备MAYTANSINOID抗体结合物的方法
公开(公告)号：WO2006086733A3
公开(公告)日：2007-06-07
申请号：PCT/US2006004937
申请日：2006-02-10
申请人： IMMUNOGEN INC , CHARI RAVI , ZHANG WEI , MESHULAM DEBORAH H , DAI YONG , WANG YONG , AMPHLETT GODFREY W
发明人： CHARI RAVI , ZHANG WEI , MESHULAM DEBORAH H , DAI YONG , WANG YONG , AMPHLETT GODFREY W
IPC分类号： A61K47/48
CPC分类号： C07K16/2803 , A61K47/642 , A61K47/644 , A61K47/6803 , A61K47/6849 , A61K47/6851
摘要： The invention provides a process for preparing a conjugate comprising a cell binding agent chemically coupled to a drug. The process comprises covalently attaching a linker to a cell binding agent, which then is conjugated to a drug, as well as purification and holding steps, and optionally a tangential flow filtration (TFF) step.
摘要翻译：本发明提供了制备包含与药物化学偶联的细胞结合剂的缀合物的方法。该方法包括将接头共价连接到细胞结合剂上，然后与药物缀合，以及纯化和保持步骤，以及任选的切向流过滤（TFF）步骤。

10. 发明申请

WO2005075606B1 FISCHER-TROPSCH SYNTHESIS USING MICROCHANNEL TECHNOLOGY AND NOVEL CATALYST AND MICROCHANNEL REACTOR 审中-公开
标题翻译：使用微通道技术和新型催化剂和微通道反应器的FISCHER-TROPSCH合成
公开(公告)号：WO2005075606B1
公开(公告)日：2005-11-17
申请号：PCT/US2004042065
申请日：2004-12-15
申请人： VELOCYS INC , WANG YONG , TONKOVICH ANNA LEE , MAZANEC TERRY , DALY FRANCIS P , VANDERWIEL DAVE , HU JIANLI , CAO CHUNSHE , KIBBY CHARLES , LI XIAOHONG , BRISCOE MICHAEL D , GANO NATHAN , CHIN YA-HUEI
发明人： WANG YONG , TONKOVICH ANNA LEE , MAZANEC TERRY , DALY FRANCIS P , VANDERWIEL DAVE , HU JIANLI , CAO CHUNSHE , KIBBY CHARLES , LI XIAOHONG , BRISCOE MICHAEL D , GANO NATHAN , CHIN YA-HUEI
IPC分类号： B01J19/00 , B01J19/24 , B01J21/04 , B01J23/75 , B01J23/889 , B01J23/89 , B01J35/10 , B01J37/02 , C10G2/00
CPC分类号： C10G2/332 , B01J19/0093 , B01J21/04 , B01J23/75 , B01J23/8896 , B01J23/8913 , B01J35/0066 , B01J35/1019 , B01J35/1038 , B01J35/1042 , B01J37/0205 , B01J2219/00783 , B01J2219/00822 , B01J2219/00824 , B01J2219/00826 , B01J2219/00831 , B01J2219/00835 , B01J2219/00844 , B01J2219/0086 , B01J2219/00873 , C10G2/341 , C10G2300/301 , C10G2300/4018 , C10G2300/4025 , C10G2300/70 , C10G2400/04 , C10G2400/10 , Y02P20/582
摘要： The disclosed invention relates to a process for converting a reactant composition comprising H2 and Co to a product comprising at least one aliphatic hydrocarbon having at least about 5 carbon atoms, the process comprising: flowing the reactant composition through a microchannel reactor in contact with a Fischer-Tropsch catalyst to convert the reactant composition to the product, the microchannel reactor comprising a plurality of process microchannels containing the catalyst; transferring heat from the process microchannels to a heat exchanger; and removing the product from the microchannel reactor; the process producing at least about 0.5 gram of aliphatic hydrocarbon having at least about 5 carbon atoms per gram of catalyst per hour; the selectivity to methane in the product being less than about 25%. The disclosed invention also relates to a supported catalyst comprising Co, and a microchannel reactor comprising at least one process microchannel and at least one adjacent heat exchange zone.
摘要翻译：所公开的发明涉及将包含H 2和Co的反应物组合物转化成包含至少一种具有至少约5个碳原子的脂族烃的产物的方法，该方法包括：使反应物组合物流过与Fischer接触的微通道反应器 - 催化剂将反应物组合物转化成产物，微通道反应器包含多个含有催化剂的工艺微通道; 将热量从工艺微通道传递到热交换器; 并从微通道反应器中除去产物; 该方法每小时产生至少约0.5克具有至少约5个碳原子的每克催化剂的脂族烃; 产品中甲烷的选择性小于约25％。所公开的发明还涉及包含Co的载体催化剂和包含至少一个工艺微通道和至少一个相邻的热交换区的微通道反应器。

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