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1. 发明申请

WO2014141104A1 3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH 审中-公开
标题翻译： 3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES作为突变体IDH的抑制剂
公开(公告)号：WO2014141104A1
公开(公告)日：2014-09-18
申请号：PCT/IB2014/059695
申请日：2014-03-12
申请人： NOVARTIS AG , CAFERRO, Thomas Raymond , CHEN, Zhuoliang , CHO, Young Shin , COSTALES, Abran Q. , LEVELL, Julian Roy , LIU, Gang , MANNING, James R. , SENDZIK, Martin , SHAFER, Cynthia , SHULTZ, Michael David , SUTTON, James , WANG, Yaping , ZHAO, Qian
发明人： CAFERRO, Thomas Raymond , CHEN, Zhuoliang , CHO, Young Shin , COSTALES, Abran Q. , LEVELL, Julian Roy , LIU, Gang , MANNING, James R. , SENDZIK, Martin , SHAFER, Cynthia , SHULTZ, Michael David , SUTTON, James , WANG, Yaping , ZHAO, Qian
IPC分类号： C07D413/14 , C07D413/04 , C07D417/14 , A61K31/506 , A61P35/00
CPC分类号： C07D413/14 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D413/04 , C07D417/14
摘要： The invention is directed to a formula (I), or a pharmamceutically acceptable salt thereof, wherein R 1 , R 2a , R 2b and R 3 -R 7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.
摘要翻译：本发明涉及式（I）或其药学上可接受的盐，其中R1，R2a，R2b和R3-R7是本文。本发明还涉及含有式（I）化合物的组合物以及这些化合物在抑制具有新形态活性的突变体IDH蛋白质中的用途。本发明还涉及式（I）化合物在治疗与这种突变体IDH蛋白相关的疾病或病症中的用途，包括但不限于细胞增殖病症如癌症。

2. 发明申请

WO2005097791A1 INHIBITORS OF IAP 审中-公开
标题翻译： IAP的抑制剂
公开(公告)号：WO2005097791A1
公开(公告)日：2005-10-20
申请号：PCT/EP2005/003619
申请日：2005-04-06
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , PALERMO, Mark, G. , SHARMA, Sushil, Kumar , STRAUB, Christopher , WANG, Run-Ming , ZAWEL, Leigh , ZHANG, Yanlin , CHEN, Zhuoliang , WANG, Yaping , YANG, Fan , WRONA, Wojciech , LIU, Gang , CHAREST, Mark, G. , HE, Feng
发明人： PALERMO, Mark, G. , SHARMA, Sushil, Kumar , STRAUB, Christopher , WANG, Run-Ming , ZAWEL, Leigh , ZHANG, Yanlin , CHEN, Zhuoliang , WANG, Yaping , YANG, Fan , WRONA, Wojciech , LIU, Gang , CHAREST, Mark, G. , HE, Feng
IPC分类号： C07D471/04
CPC分类号： C07D207/16 , C07D207/06 , C07D207/08 , C07D207/09 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/10 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要： Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).
摘要翻译：抑制Smac蛋白与式（I）的凋亡蛋白抑制剂（IAP）结合的新型化合物。

3. 发明申请

WO2011101409A1 PYRROLOPYRIMIDINE COMPOUNDS AS INHIBITORS OF CDK4/6 审中-公开
标题翻译：作为CDK4 / 6的抑制剂的吡咯烷酮化合物
公开(公告)号：WO2011101409A1
公开(公告)日：2011-08-25
申请号：PCT/EP2011/052353
申请日：2011-02-17
申请人： NOVARTIS AG , BRAIN, Christopher, Thomas , CHO, Young Shin , GIRALDES, John, William , LAGU, Bharat , LEVELL, Julian , LUZZIO, Michael , PEREZ, Lawrence, Blas , WANG, Yaping , YANG, Fan
发明人： BRAIN, Christopher, Thomas , CHO, Young Shin , GIRALDES, John, William , LAGU, Bharat , LEVELL, Julian , LUZZIO, Michael , PEREZ, Lawrence, Blas , WANG, Yaping , YANG, Fan
IPC分类号： C07D487/04 , C07B59/00 , A61K31/519 , A61P35/00 , C07D519/00
CPC分类号： C07D487/04 , C07D471/08 , C07D471/10 , C07D487/08 , C07D487/10 , C07D498/08 , C07D498/10 , C07D498/20 , C07D519/00
摘要： The invention is directed to novel pyrrolopyrimidine compounds of formula (I) wherein R 1 , R 2Y , R 4 , R 8 - R 11 , A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译：本发明涉及式（I）的新颖吡咯并嘧啶化合物，其中R 1，R 2 Y，R 4，R 8 -R 11，A和L在本文中定义，并包括其盐，包括其药学上可接受的盐。本发明的化合物是CDK4 / 6抑制剂，可用于治疗由CDK4 / 6介导的疾病和病症，如癌症，包括外套细胞淋巴瘤，脂肪肉瘤，非小细胞肺癌，黑素瘤，鳞状细胞食管癌癌症和乳腺癌。本发明还涉及包含本发明化合物的药物组合物。本发明还涉及抑制CDK4 / 6活性的方法以及使用本发明化合物或包含本发明化合物的药物组合物治疗与之相关的病症。

4. 发明申请

WO2010125402A1 IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES 审中-公开
标题翻译：咪唑衍生物及其作为细胞周期调节因子的调节剂
公开(公告)号：WO2010125402A1
公开(公告)日：2010-11-04
申请号：PCT/GB2010/050725
申请日：2010-04-30
申请人： NOVARTIS AG , ASTEX THERAPEUTICS LIMITED , HOWARD, Steven , MORTENSON, Paul Neil , HISCOCK, Steven Douglas , WOOLFORD, Alison Jo-Anne , WOODHEAD, Andrew James , CHESSARI, Gianni , O'REILLY, Marc , CONGREVE, Miles Stuart , DAGOSTIN, Claudio , CHO, Young Shin , YANG, Fan , CHEN, Christine Hiu-Tung , BRAIN, Christopher Thomas , LAGU, Bharat , WANG, Yaping , KIM, Sunkyu , GRIALDES, John , LUZZIO, Michael Joseph , PEREZ, Lawrence Blas
发明人： HOWARD, Steven , MORTENSON, Paul Neil , HISCOCK, Steven Douglas , WOOLFORD, Alison Jo-Anne , WOODHEAD, Andrew James , CHESSARI, Gianni , O'REILLY, Marc , CONGREVE, Miles Stuart , DAGOSTIN, Claudio , CHO, Young Shin , YANG, Fan , CHEN, Christine Hiu-Tung , BRAIN, Christopher Thomas , LAGU, Bharat , WANG, Yaping , KIM, Sunkyu , GRIALDES, John , LUZZIO, Michael Joseph , PEREZ, Lawrence Blas
IPC分类号： C07D233/22 , C07D235/12 , C07D401/06 , C07D401/10 , C07D401/14 , C07D409/10 , C07D409/14 , C07D413/14 , C07D417/10 , A61K31/4164 , A61K31/4178 , A61P35/00
CPC分类号： C07D471/04 , C07D233/22 , C07D233/24 , C07D235/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D487/04 , C07D519/00
摘要： The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N + -O - or CR 3 ; Y is N, N + -O - or CR 3a ; R 1 and R 2 are independently selected from hydrogen and various substituents as defined in the claims; or R 1 and R 2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R 3 is selected from hydrogen and various substituents; and R 3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.
摘要翻译：本发明提供式（I）化合物及其盐，互变异构体，溶剂化物和N-氧化物; 其中Q是CH或N; X是N，N + -O-或CR 3; Y是N，N + -O-或CR3a; R 1和R 2独立地选自氢和权利要求中定义的各种取代基; 或R 1和R 2与它们所连接的原子一起连接以形成任选取代的4至7个成员的碳环或杂环芳族或非芳族环; R3选自氢和各种取代基; 并且R 3a选自氢和权利要求中定义的各种取代基。还提供含有式（I）化合物，制备化合物的方法和化合物的医疗用途的药物组合物。式（I）化合物具有作为CDK激酶抑制剂的活性，并且可用于治疗尤其是增殖性疾病如癌症。

5. 发明申请

WO2006133147A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2006133147A2
公开(公告)日：2006-12-14
申请号：PCT/US2006/021850
申请日：2006-06-06
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , CHEN, Zhuoliang , PALERMO, Mark, G. , SHARMA, Sushil, K. , SMITH, Troy , STRAUB, Christopher, S. , WANG, Run-Ming, D. , WANG, Yaping , ZAWEL, Leigh
发明人： CHEN, Zhuoliang , PALERMO, Mark, G. , SHARMA, Sushil, K. , SMITH, Troy , STRAUB, Christopher, S. , WANG, Run-Ming, D. , WANG, Yaping , ZAWEL, Leigh
IPC分类号： C07K5/02 , C07K5/06 , C07K5/08 , A61K38/05 , A61K38/06 , A61P35/00
CPC分类号： C07K5/0808 , C07D213/56 , C07D223/10 , C07D223/16 , C07D471/04 , C07D487/04 , C07D487/06 , C07D513/04 , C07K5/06026 , C07K5/06191 , C07K5/0806 , C07K5/0827 , C07K5/1008
摘要： The present disclosure relates to XIAP inhibitor compounds of the formula (I)
摘要翻译：本公开涉及式（I）的XIAP抑制剂化合物，

6. 发明公开

EP1313705A1 GEM-SUBSTITUTED ALPHA V BETA 3 INTEGRIN ANTAGONISTS 审中-公开
标题翻译：偕取代的α-V BETA 3整联蛋白拮抗剂
公开(公告)号：EP1313705A1
公开(公告)日：2003-05-28
申请号：EP01968257.4
申请日：2001-08-29
申请人： Pharmacia Corporation , Khanna, Ish Kumar , Yu, Yi , Fun-Lu, Hwang , Chandrakumar, Nizal S. , Huff, Renee M. , Russell, Mark A. , Boys, Mark L. , Schretzman, Lori A. , Chen, Barbara B. , Desai, Bipinchandra N. , Nagarajan, Srinivasan Raj , Gasiecki, Alan F. , Penning, Thomas D. , Rogers, Thomas , Wendt, John Adam , Khilevich, Albert , Wang, Yaping
发明人： KHANNA, Ish, Kumar , YU, Yi , FUN-LU, Hwang , CHANDRAKUMAR, Nizal, S. , HUFF, Renee, M. , RUSSELL, Mark, A. , BOYS, Mark, L. , SCHRETZMAN, Lori, A. , CHEN, Barbara, B. , DESAI, Bipinchandra, N. , NAGARAJAN, Srinivasan, Raj , GASIECKI, Alan, F. , PENNING, Thomas, D. , ROGERS, Thomas , WENDT, John, Adam , KHILEVICH, Albert , WANG, Yaping , DEVADAS, Balekudra
IPC分类号： C07D213/74 , C07D401/12 , C07D213/73 , C07D471/04 , A61K31/4427 , A61K31/553 , A61P35/00 , A61P31/00
CPC分类号： C07D213/73 , C07D213/74 , C07D401/12 , C07D471/04
摘要： The present invention relates to a class of compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of Formula (I), and methods of selectively inhibiting or antagonizing the αvβ3 and/or the αvβ5 integrin.

7. 发明申请

WO2004058254A1 HETEROARYLALKANOIC ACIDS AS INTEGRIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为INTEGRIN受体拮抗剂的异氟烷酸
公开(公告)号：WO2004058254A1
公开(公告)日：2004-07-15
申请号：PCT/US2003/040898
申请日：2003-12-22
申请人： PHARMACIA CORPORATION , BOYS, Mark, L. , SCHRETZMAN, Lori, A. , TOLLEFSON, Michael, B. , CHANDRAKUMAR, Nizal, S. , KHANNA, Ish, K. , NGUYEN, Maria , DOWNS, Victoria , MOHLER, Scott, B. , GESICKI, Glen, J. , PENNING, Thomas, D. , CHEN, Barbara, B. , WANG, Yaping , KHILEVICH, Albert , DESAI, Bipinchandra, N. , YU, Yi , WENDT, John, A. , STENMARK, Heather , WU, Lisa , HUFF, Renee, M. , NAGARAJAN, Srinivasan, R. , DEVADAS, Balekudru , LU, Hwang-Fun , RUSSELL, Mark , SPANGLER, Dale, P. , PARIKH, Mihir, D. , CLARE, Michael
发明人： BOYS, Mark, L. , SCHRETZMAN, Lori, A. , TOLLEFSON, Michael, B. , CHANDRAKUMAR, Nizal, S. , KHANNA, Ish, K. , NGUYEN, Maria , DOWNS, Victoria , MOHLER, Scott, B. , GESICKI, Glen, J. , PENNING, Thomas, D. , CHEN, Barbara, B. , WANG, Yaping , KHILEVICH, Albert , DESAI, Bipinchandra, N. , YU, Yi , WENDT, John, A. , STENMARK, Heather , WU, Lisa , HUFF, Renee, M. , NAGARAJAN, Srinivasan, R. , DEVADAS, Balekudru , LU, Hwang-Fun , RUSSELL, Mark , SPANGLER, Dale, P. , PARIKH, Mihir, D. , CLARE, Michael
IPC分类号： A61K31/4245
CPC分类号： A61K31/4245 , A61K31/4745
摘要： The present invention relates to pharmaceutical compositions comprising compounds of the Formula I, or a pharmaceutically acceptable salt thereof, and methods of selectively inhibiting or antagonizing the ανβ3 and/or the ανβ5 integrin without significantly inhibiting the ανβ6 integrin.
摘要翻译：本发明涉及包含式I化合物或其药学上可接受的盐的药物组合物，以及在不显着抑制alphaneta 6整联蛋白的情况下选择性地抑制或拮抗氨化疟原虫3和/或囟化α5整联蛋白的方法。

8. 发明申请

WO2007017522A1 FERROCENE-DIPHOSPHINE LIGANDS 审中-公开
标题翻译：糠醛 - 双胍配体
公开(公告)号：WO2007017522A1
公开(公告)日：2007-02-15
申请号：PCT/EP2006/065196
申请日：2006-08-10
申请人： SOLVIAS AG , WEISSENSTEINER, Walter , WANG, Yaping , SPINDLER, Felix , PUGIN, Benoît , FENG, Xiangdong
发明人： WEISSENSTEINER, Walter , WANG, Yaping , SPINDLER, Felix , PUGIN, Benoît , FENG, Xiangdong
IPC分类号： C07F17/02 , C07F19/00 , C07B31/00 , B01J31/00
CPC分类号： C07F17/02
摘要： Compounds of the formula (I) in the form of racemates, mixtures of stereoisomers or optically pure stereoisomers, formula (I), where X 1 and X 2 are each, independently of one another, a secondary phosphino group; R 1 is a halogen atom or a substituent bound via a C atom, N atom, S atom, Si atom, a P(O) group or a P(S) group to the cyclopentadienyl ring; R 2 is C 1 -C 4 -alkyl or phenyl; m is from 1 to 3 and n is 0 or from 1 to 5, are ligands for complexes of transition metals as enantioselective and homogeneous catalysts. As a result of the substitution, the conversion, the stereoselectivity and/or the configuration of the adduct formed can be influenced and optimization of catalysts can be made possible in this way.
摘要翻译：外消旋物形式的式（I）化合物，立体异构体的混合物或光学纯立体异构体式（I），其中X 1和X 2各自独立地为一个二次膦基; R 1是通过C原子，N原子，S原子，Si原子，P（O）基或P（S）键连接到环戊二烯基环上的卤素原子或取代基; R 2是C 1 -C 4 - 烷基或苯基; m为1至3，n为0或1至5，为过渡金属络合物作为对映选择性和均相催化剂的配体。作为取代的结果，可以影响形成的加合物的转化率，立体选择性和/或构型，并且可以以这种方式使催化剂的优化成为可能。

9. 发明申请

WO2012171396A1 INTEGRATED MODULE INTEGRATING AMOLED DISPLAY WITH SOLAR PANEL AND ELECTRONIC DEVICE APPLYING SUCH INTEGRATED MODULE 审中-公开
标题翻译：集成模块集成嵌入式显示器与太阳能电池板和应用这种集成模块的电子设备
公开(公告)号：WO2012171396A1
公开(公告)日：2012-12-20
申请号：PCT/CN2012/073475
申请日：2012-04-01
申请人： WANG, Yaping , DING, Rong
发明人： WANG, Yaping , DING, Rong
IPC分类号： H01L27/32
CPC分类号： H01L27/3227 , H01L31/04 , Y02E10/50
摘要： An integrated module integrating an AMOLED display with a solar panel and an electronic device applying such integrated module are provided. The integrated module comprises a transparent AMOLED display portion, a solar cell portion and a shared transparent substrate. The electronic device further comprises a power management portion for managing and distributing the electrical power from the integrated module, a main battery of the electronic device or an external power supply of the electronic device. In the integrated module and the electronic device applying such integrated module, the solar cell portion and the AMOLED display portion share the same substrate, thereby reducing the whole thickness and the size of the electronic device. The AMOLED display portion has self-emissive characteristic and can not be affected by the solar cell portion, thereby ensuring the whole display quality.
摘要翻译：提供了一个将AMOLED显示屏与太阳能电池板集成在一起的集成模块以及应用这种集成模块的电子设备。集成模块包括透明AMOLED显示部分，太阳能电池部分和共享透明基板。电子设备还包括用于管理和分配来自集成模块的电力，电子设备的主电池或电子设备的外部电源的电力管理部分。在集成模块和应用这种集成模块的电子设备中，太阳能电池部分和AMOLED显示部分共享相同的基板，从而减小了电子设备的整体厚度和尺寸。 AMOLED显示部分具有自发射特性，不受太阳能电池部分的影响，从而确保整个显示质量。

10. 发明申请

WO2006081807A2 VERFAHREN ZUR HERSTELLUNG VON LOSARTAN 审中-公开
标题翻译：用于生产氯沙坦
公开(公告)号：WO2006081807A2
公开(公告)日：2006-08-10
申请号：PCT/DE2006/000164
申请日：2006-02-02
申请人： RATIOPHARM GMBH , WANG, Yaping , LI, Yonggang , LI, Yulin , ZHENG, Guojun , LI, Yi
发明人： WANG, Yaping , LI, Yonggang , LI, Yulin , ZHENG, Guojun , LI, Yi
IPC分类号： C07D233/54 , C07D403/10 , C07D257/04 , C07C251/08
CPC分类号： C07C257/14 , C07D233/64 , C07D257/04 , C07D403/10 , Y02P20/55
摘要： Die vorliegende Erfindung betrifft ein neues Verfahren zur Herstellung von Losartan, ein Imidazolderivat mit dem chemischen Namen 2-n-Butyl-4-chloro-5-hydroxymethyl-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-]methyl}imidazol sowie pharmakologisch wirksamer Salze hiervon. Weiterhin betrifft die Erfindung neue Zwischenprodukte, die zur Herstellung von Losartan geeignet sind sowie neue Verfahren zur Herstellung von Zwischenverbindungen, die zur Herstellung von Losartan geeignet sind. Ein Aspekt der Erfindung ist ein Verfahren zur Herstellung einer Verbindung der allgemeinen Formel (I), die bei einer erfindungsgemäßen Darstellung von Losartan als Zwischenstufe entstehen kann.
摘要翻译：本发明涉及一种新的方法用于制备氯沙坦，化学名为2-正丁基-4-氯-5-羟甲基-1-咪唑衍生物 - {[2“ - （1H-四唑-5-基）联苯 4-]甲基}咪唑及其药理学活性的盐。此外，本发明提供新的中间体，其适合用于生产氯沙坦，并且其适合于氯沙坦的制备涉及中间体化合物的制备的新方法。本发明的一个方面是一种用于制备通式（I），其可在氯沙坦的本发明的制剂产生作为中间体的化合物的方法。

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