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1. 发明申请

WO2013127267A1 PYRIDINYL AND PYRIMIDINYL SULFOXIDE AND SULFONE DERIVATIVES 审中-公开
标题翻译：吡啶并吡啶并吡啶衍生物及其衍生物
公开(公告)号：WO2013127267A1
公开(公告)日：2013-09-06
申请号：PCT/CN2013/000214
申请日：2013-03-01
申请人： GENENTECH, INC. , FORMA TM, LLC , BAIR, Kenneth W. , BAUMEISTER, Timm R. , DRAGOVICH, Peter , GOSSELIN, Francis , YUEN, Po-Wai , ZAK, Mark , ZHENG, Xiaozhang
发明人： BAIR, Kenneth W. , BAUMEISTER, Timm R. , DRAGOVICH, Peter , GOSSELIN, Francis , YUEN, Po-Wai , ZAK, Mark , ZHENG, Xiaozhang
IPC分类号： C07D471/04 , C07D491/048 , C07D497/04 , A61K31/4355 , A61K31/437 , A61P3/10 , A61P9/10 , A61P35/00 , A61P29/00
CPC分类号： C07D471/04 , A61K31/444 , A61K31/4545 , A61K31/455 , A61K31/496 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/706 , A61K45/06 , C07D487/04 , C07D491/048 , C07D495/04 , A61K2300/00
摘要： Disclosed are certain pyridinyl and pyrimidinyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds and methods of treatment using such compounds.
摘要翻译：公开了某些吡啶基和嘧啶基亚砜和砜化合物，包含这些化合物的药物组合物和使用这些化合物的治疗方法。

2. 发明申请

WO2012031197A1 NOVEL COMPOUNDS AND COMPOSITIONS FOR THE INHIBITION OF NAMPT 审中-公开
标题翻译：新型化合物和组合物抑制NAMPT
公开(公告)号：WO2012031197A1
公开(公告)日：2012-03-08
申请号：PCT/US2011/050321
申请日：2011-09-02
申请人： FORMA THERAPEUTICS, INC. , GENENTECH, INC. , BAIR, Kenneth, W. , BAUMEISTER, Timm , BUCKMELTER, Alexandre, J. , CLODFELTER, Karl, H. , DRAGOVICH, Peter , GOSSELIN, Francis , HAN, Bingsong , LIN, Jian , REYNOLDS, Dominic J. , ROTH, Bruce , SMITH, Chase, C. , WANG, Zhongguo , YUEN, Po-Wai , ZHENG, Xiaozhang
发明人： BAIR, Kenneth, W. , BAUMEISTER, Timm , BUCKMELTER, Alexandre, J. , CLODFELTER, Karl, H. , DRAGOVICH, Peter , GOSSELIN, Francis , HAN, Bingsong , LIN, Jian , REYNOLDS, Dominic J. , ROTH, Bruce , SMITH, Chase, C. , WANG, Zhongguo , YUEN, Po-Wai , ZHENG, Xiaozhang
IPC分类号： C07D471/04 , C07D491/04 , C07D495/04 , A61K31/437 , A61P35/00
CPC分类号： A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/496 , A61K31/497 , A61K31/519 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04
摘要： The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below:
摘要翻译：本发明涉及抑制NAMPT，其合成，应用和解毒剂的化合物和组合物。本发明的说明性化合物如下所示：

3. 发明申请

WO2009158308A1 SYNTHESIS OF CHIRAL AMINES 审中-公开
标题翻译：合成氨基酸
公开(公告)号：WO2009158308A1
公开(公告)日：2009-12-30
申请号：PCT/US2009/048129
申请日：2009-06-22
申请人： MERCK FROSST CANADA LTD. , O'SHEA, Paul , GOSSELIN, Francis , MCWILLIAMS, James, C.
发明人： O'SHEA, Paul , GOSSELIN, Francis , MCWILLIAMS, James, C.
IPC分类号： C07B43/04 , C07B53/00
CPC分类号： C07B53/00 , C07B43/04
摘要： The instant invention involves the enantioselective hydrogenation of isomeric N-H imines (N-unsubstituted) using a transition metal based catalyst modified with a chiral phosphine derivative to produce enantiomerically enriched chiral amines.
摘要翻译：本发明涉及使用用手性膦衍生物改性的过渡金属基催化剂对异构N-H亚胺（N-未取代的）进行对映选择性氢化以产生对映体富集的手性胺。

4. 发明申请

WO2015073739A1 PROCESSES FOR THE PREPARATION OF PYRIMIDINYLCYCLOPENTANE COMPOUNDS 审中-公开
标题翻译：制备吡咯烷酮类化合物的方法
公开(公告)号：WO2015073739A1
公开(公告)日：2015-05-21
申请号：PCT/US2014/065567
申请日：2014-11-13
申请人： F. HOFFMANN-LA ROCHE AG , GENENTECH, INC. , IDING, Hans , REENTS, Reinhard , SCALONE, Michelangelo , GOSSELIN, Francis
发明人： IDING, Hans , REENTS, Reinhard , SCALONE, Michelangelo , GOSSELIN, Francis
IPC分类号： C07D239/70 , A61K31/517
CPC分类号： C07D239/70 , C07B2200/07 , C07C269/06 , C07C271/22 , C12P17/165
摘要： The present invention relates to a process for the preparation of a compound of formula (I), wherein R 1 is as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.
摘要翻译：本发明涉及制备式（I）化合物的方法，其中R1如本文所定义，其可用作制备活性药物化合物的中间体。

5. 发明申请

WO2013127266A1 AMIDO-BENZYL SULFONE AND SULFOXIDE DERIVATIVES 审中-公开
标题翻译： AMIDO-苄基硫醚和硫代衍生物
公开(公告)号：WO2013127266A1
公开(公告)日：2013-09-06
申请号：PCT/CN2013/000213
申请日：2013-03-01
申请人： GENENTECH, INC. , FORMA TM, LLC , BAIR, Kenneth W. , BAUMEISTER, Timm R. , BUCKMELTER, Alexandre J. , CLODFELTER, Karl H. , DRAGOVICH, Peter , GOSSELIN, Francis , GUNZNER-TOSTE, Janet , HAN, Bingsong , LIN, Jian , LIU, Xiongcai , REYNOLDS, Dominic J. , SMITH, Chase C. , WANG, Zhongguo , ZAK, Mark , ZHANG, Yamin , ZHAO, Guiling , ZHENG, Xiaozhang , YUEN, Po-Wai
发明人： BAIR, Kenneth W. , BAUMEISTER, Timm R. , BUCKMELTER, Alexandre J. , CLODFELTER, Karl H. , DRAGOVICH, Peter , GOSSELIN, Francis , GUNZNER-TOSTE, Janet , HAN, Bingsong , LIN, Jian , LIU, Xiongcai , REYNOLDS, Dominic J. , SMITH, Chase C. , WANG, Zhongguo , ZAK, Mark , ZHANG, Yamin , ZHAO, Guiling , ZHENG, Xiaozhang , YUEN, Po-Wai
IPC分类号： C07D471/04 , C07D491/04 , C07D495/04 , A61K31/437 , A61P35/00
CPC分类号： C07D519/00 , A61K31/454 , A61K31/4545 , A61K31/46 , A61K31/496 , A61K31/5025 , A61K31/5377 , A61K31/5386 , A61K31/551 , A61K45/06 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04
摘要： The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
摘要翻译：本发明涉及某些酰氨基 - 苄基亚砜和砜化合物，包含这些化合物的药物组合物和使用这些化合物的治疗方法。

6. 发明申请

WO2012030683A2 NOVEL SINGLE CHEMICAL ENTITIES AND METHODS FOR DELIVERY OF OLIGONUCLEOTIDES 审中-公开
标题翻译：新型单一化学实验和交付寡糖的方法
公开(公告)号：WO2012030683A2
公开(公告)日：2012-03-08
申请号：PCT/US2011/049479
申请日：2011-08-29
申请人： MERCK SHARP & DOHME CORP. , COLLETTI, Steven, L. , GOSSELIN, Francis , JADHAV, Vasant, R. , SHAW, Anthony, W. , TELLERS, David, M. , TUCKER, Thomas, J. , YUAN, Yu , ZEWGE, Daniel
发明人： COLLETTI, Steven, L. , GOSSELIN, Francis , JADHAV, Vasant, R. , SHAW, Anthony, W. , TELLERS, David, M. , TUCKER, Thomas, J. , YUAN, Yu , ZEWGE, Daniel
IPC分类号： C12P21/06
CPC分类号： C12N15/113 , A61K47/64 , C12N15/111 , C12N15/87 , C12N2310/14 , C12N2310/3513 , C12N2310/3515 , C12N2320/32

7. 发明申请

WO2009042098A1 CHROMENONE DERIVATIVES AND THEIR USE FOR LEUKOTRIENE BIOSYNTHESIS INHIBITION 审中-公开
标题翻译：氯苯酮衍生物及其用于紫杉醇生物合成抑制剂
公开(公告)号：WO2009042098A1
公开(公告)日：2009-04-02
申请号：PCT/US2008/010987
申请日：2008-09-23
申请人： MERCK & CO., INC. , GOSSELIN, Francis , VYDRA, Vicky
发明人： GOSSELIN, Francis , VYDRA, Vicky
IPC分类号： C07D413/12 , A61K31/4245 , A61P19/02
CPC分类号： C07D413/12
摘要： This invention provides novel salt and crystalline forms thereof of (-) 4-(4-fluorophenyl)-7-[({5-[1-hydroxy-1-(trifluoromethyl)propyl]-1,3,4-oxadiazol-2-yl}-amino)-methyl]-2H-chromen-2-one. The compounds are 5-LO inhibitors and are useful for treatment of conditions such as asthma, allergic rhinitis, COPD, and atherosclerosis.
摘要翻译：本发明提供了（ - ）4-（4-氟苯基）-7 - [（{5- [1-羟基-1-（三氟甲基）丙基] -1,3,4-恶二唑-2 基} - 氨基） - 甲基] -2H-吡喃-2-酮。该化合物是5-LO抑制剂，可用于治疗诸如哮喘，过敏性鼻炎，COPD和动脉粥样硬化的病症。

8. 发明申请

WO2011090965A1 NOVEL CATIONIC LIPIDS FOR OLIGONUCLEOTIDE DELIVERY 审中-公开
标题翻译：用于交付寡糖的新型阳离子脂肪
公开(公告)号：WO2011090965A1
公开(公告)日：2011-07-28
申请号：PCT/US2011/021619
申请日：2011-01-19
申请人： MERCK SHARP & DOHME CORP. , ZEWGE, Daniel , GOSSELIN, Francis
发明人： ZEWGE, Daniel , GOSSELIN, Francis
IPC分类号： A61K9/127 , C07C211/00
CPC分类号： C12N15/113 , C07C217/40 , C07C217/52 , C07C2601/02 , C07D207/08 , C07D207/12 , C07D209/48 , C07D211/22 , C07D211/44 , C07D211/46 , C07D295/088 , C07H21/02 , C12N15/1137 , C12N2310/14 , C12N2310/141 , C12N2310/321 , C12N2330/30
摘要： The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a catiomc lipid scaffold that is susceptible to hydrolytic instability that may translate into reduced liver residence times and reduced hepatocellular toxicity. The present invention employs acetals and ketals to provide a low pH sensitive chemical handle for degradation.
摘要翻译：本发明提供了可以与其它脂质组分如胆固醇和PEG-脂质组合使用以与寡核苷酸形成脂质纳米颗粒的新型阳离子脂质。本发明的目的是提供易于水解不稳定性的潜在脂质支架，其可能转化为减少的肝停留时间和降低的肝细胞毒性。本发明使用缩醛和缩酮来提供用于降解的低pH敏感化学手柄。

9. 发明申请

WO2009140125A2 DEPROTECTION OF SYNTHETIC OLIGONUCLEOTIDES USING AQUEOUS ETHANOLAMINE 审中-公开
标题翻译：使用水性乙酰胺对合成寡核苷酸的保护
公开(公告)号：WO2009140125A2
公开(公告)日：2009-11-19
申请号：PCT/US2009/043064
申请日：2009-05-07
申请人： MERCK & CO., INC. , GOSSELIN, Francis , GOWANI, Amran
发明人： GOSSELIN, Francis , GOWANI, Amran
IPC分类号： C07H21/04
CPC分类号： C07H1/00 , C07H21/00 , Y02P20/55
摘要： This invention concerns an efficient and safer (easy to handle and environmentally less hazardous) protocol for cleavage and deprotection of synthetic oligonucleotides utilizing ethanolamine. Specifically, the present invention features a method for 1) the removal of amide protecting groups from nucleobases and 2) cleavage of the synthetic oligonucleotides from their solid support allowing the isolation and subsequent purification of said oligonucleotides.
摘要翻译：本发明涉及使用乙醇胺的合成寡核苷酸的切割和脱保护的有效和安全（易于处理和环境更少的危害）方案。具体地，本发明的特征在于一种方法，用于1）从核碱基中除去酰胺保护基团，和2）将合成寡核苷酸从其固体支持物切割出来，从而分离和随后纯化所述寡核苷酸。

10. 发明申请

WO1997002468A1 MARINE NAVIGATION DEVICE 审中-公开
标题翻译：海上导航装置
公开(公告)号：WO1997002468A1
公开(公告)日：1997-01-23
申请号：PCT/FR1996001016
申请日：1996-07-02
申请人： GOSSELIN, Francis , LELOUP, Frédéric
IPC分类号： G01C21/20
CPC分类号： G01C21/20 , B63B49/00 , G09B29/10 , G09B29/106
摘要： A device for determining a position on a navigational chart on the basis of GPS data, comprising a rapid orientation and positioning assembly having two discs arranged one on top of the other and used as a protractor and a reader, respectively, said discs being pivotably joined together in the middle by a pointing means (24) and two positioning rules. The upper rule is also used for orientation and both rules have a central longitudinal aperture (4, 5) while the edges of the rules include a projection enabling each rule to slide freely along a respective mortised recess in each disc. The upper rule is provided with a double longitudinal scale. Said device is particularly useful as an aid for work on navigational charts.
摘要翻译：一种用于基于GPS数据确定导航图上的位置的装置，包括具有分别彼此排列并分别用作量角器和读取器的两个盘的快速取向和定位组件，所述盘可枢转地连接一起在中间由一个指向手段（24）和两个定位规则。上限也用于取向，并且两个规则都具有中心纵向孔（4,5），而规则的边缘包括使每个规则沿着每个盘中的相应的被迫凹槽自由滑动的突起。上面的规则提供了双重纵向尺度。所述装置特别有助于在导航图上工作。

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