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1. 发明申请

US20140294805A1 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：US20140294805A1
公开(公告)日：2014-10-02
申请号：US13820497
申请日：2011-09-02
申请人： Kenneth W. Bair , Timm R. Baumeister , Alexandre J. Buckmelter , Karl H. Clodfelter , Peter Dragovich , Francis Gosselin , Bingsong Han , Jian Lin , Dominic J. Reynolds , Bruce Roth , Chase C. Smith , Zhongguo Wang , Po-Wai Yuen , Xiaozhang Zheng
发明人： Kenneth W. Bair , Timm R. Baumeister , Alexandre J. Buckmelter , Karl H. Clodfelter , Peter Dragovich , Francis Gosselin , Bingsong Han , Jian Lin , Dominic J. Reynolds , Bruce Roth , Chase C. Smith , Zhongguo Wang , Po-Wai Yuen , Xiaozhang Zheng
IPC分类号： C07D495/04 , A61K31/437 , C07D471/04 , C07D487/04 , A61K31/519 , A61K31/55 , C07D491/048 , A61K31/4355 , A61K31/4365 , A61K31/496 , A61K31/5377 , A61K45/06 , A61K31/497
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：

2. 发明申请

US20150104384A1 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：US20150104384A1
公开(公告)日：2015-04-16
申请号：US14382141
申请日：2013-03-01
申请人： Kenneth W. Bair , Timm R. Baumeister , Alexandre J. Buckmelter , Karl H. Clodfelter , Peter Dragovich , Francis Gosselin , Janet Gunzner-Toste , Bingsong Han , Jian Lin , Xiongcai Liu , Dominic J. Reynolds , Chase C. Smith , Zhongguo Wang , Mark Zak , Yamin Zhang , Guiling Zao , Xiaozhang Zheng , Po-Wai Yuen
发明人： Kenneth W. Bair , Timm R. Baumeister , Alexandre J. Buckmelter , Karl H. Clodfelter , Peter Dragovich , Francis Gosselin , Janet Gunzner-Toste , Bingsong Han , Jian Lin , Xiongcai Liu , Dominic J. Reynolds , Chase C. Smith , Zhongguo Wang , Mark Zak , Yamin Zhang , Guiling Zao , Xiaozhang Zheng , Po-Wai Yuen
IPC分类号： C07D519/00 , A61K31/454 , A61K31/5386 , C07D491/048 , A61K31/4545 , A61K45/06 , C07D471/04 , C07D495/04 , A61K31/496 , A61K31/5025 , A61K31/46 , A61K31/551 , C07D487/04 , A61K31/5377
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。

3. 发明授权

US09458172B2 Pyridinyl and pyrimidinyl sulfoxide and sulfone derivatives 有权
标题翻译：吡啶基和嘧啶基亚砜和砜衍生物
公开(公告)号：US09458172B2
公开(公告)日：2016-10-04
申请号：US14382123
申请日：2013-03-01
申请人： Kenneth W Bair , Timm R Baumeister , Peter Dragovich , Francis Gosselin , Po-Wai Yuen , Mark Zak , Xiaozhang Zheng
发明人： Kenneth W Bair , Timm R Baumeister , Peter Dragovich , Francis Gosselin , Po-Wai Yuen , Mark Zak , Xiaozhang Zheng
IPC分类号： C07D498/00 , C07D413/00 , C07D487/00 , C07D401/00 , C07D221/02 , C07D471/02 , A61K31/4965 , A61K31/519 , A61K31/44 , A61K31/47 , C07D495/04 , C07D471/04 , C07D491/048 , A61K45/06 , A61K31/455 , A61K31/706 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , C07D487/04
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。

4. 发明申请

US20150175621A1 PYRIDINYL AND PYRIMIDINYL SULFOXIDE AND SULFONE DERIVATIVES 有权
标题翻译：吡啶并吡啶衍生物和硫代衍生物
公开(公告)号：US20150175621A1
公开(公告)日：2015-06-25
申请号：US14382123
申请日：2013-03-01
申请人： Kenneth W Bair , Timm R Baumeister , Peter Dragovich , Francis Gosselin , Po-Wai Yuen , Mark Zak , Xiaozhang Zheng
发明人： Kenneth W Bair , Timm R Baumeister , Peter Dragovich , Francis Gosselin , Po-Wai Yuen , Mark Zak , Xiaozhang Zheng
IPC分类号： C07D495/04 , A61K31/444 , C07D487/04 , A61K31/519 , A61K45/06 , A61K31/506 , A61K31/4545 , A61K31/5377 , A61K31/496 , C07D471/04 , C07D491/048
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。

5. 发明申请

US20130116419A1 POST-SYNTHETIC CHEMICAL MODIFICATION OF RNA AT THE 2'-POSITION OF THE RIBOSE RING VIA "CLICK" CHEMISTRY 审中-公开
标题翻译：通过“点击”化学方法在RIBOSE环的2位上的RNA的后合成化学修饰
公开(公告)号：US20130116419A1
公开(公告)日：2013-05-09
申请号：US13574136
申请日：2011-01-19
申请人： Daniel Zewge , Francis Gosselin
发明人： Daniel Zewge , Francis Gosselin
IPC分类号： C07H21/02
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： This invention relates to the post-synthetic chemical modification of RNA at the 2′-position on the ribose ring via a copper catalyzed Huisgen cycloaddition (“click” chemistry: Kolb, Sharpless Drug Discovery Today 2003, 8, 1128). The invention 1) avoids complex, tedious multi-step syntheses of each desired modified ribonucleoside; 2) allows diverse chemical modifications using high-fidelity chemistry that is completely orthogonal to commonly used alkylamino, carboxylate and disulfide linker reactivities; 3) allows introduction of functional groups that are incompatible with modern automated solid-phase synthesis of RNA and subsequent cleavage-deprotection steps; 4) allows introduction of functional groups useful as targeting ligands; and 5) enables high-throughput structure-activity relationship studies on chemically modified RNA in 96-well format.
摘要翻译：本发明涉及通过铜催化的Huisgen环加成在核糖环上2'-位的RNA的后合成化学修饰（“点击”化学：Kolb，Sharpless Drug Discovery Today 2003,8,1128）。本发明1）避免每种所需修饰的核糖核苷的复杂繁琐的多步合成; 2）允许使用与常用的烷基氨基，羧酸酯和二硫化物连接体反应性完全正交的高保真化学的不同化学修饰; 3）允许引入与现代自动化固相合成RNA和随后的切割 - 脱保护步骤不相容的官能团; 4）允许引入可用作靶向配体的官能团; 和5）能够进行96孔形式的化学修饰RNA的高通量结构 - 活性关系研究。

6. 发明申请

US20060052642A1 Synthesis of alpha fluoroalkyl amines 失效
公开(公告)号：US20060052642A1
公开(公告)日：2006-03-09
申请号：US11221279
申请日：2005-09-07
申请人： Paul O'Shea , Francis Gosselin
发明人： Paul O'Shea , Francis Gosselin
IPC分类号： C07C209/24
CPC分类号： C07C209/52 , C07B2200/07 , C07C213/00 , C07C319/20 , C07C211/29 , C07C211/30 , C07C211/31 , C07C217/48 , C07C323/32
摘要： This invention describes the reaction of an alpha fluoroalkyl ketone with a bis(trialkylsilyl)amide to give a stable N-trialkylsilyl imine. Treatment of the N-trialkylsilyl imine with an alcohol leads to solvolysis of the trialkylsilyl group and yields a stable mixture of an aminal and an imine in high yield. Catalytic reduction of this mixture, or of the individual components, in the presence of a chiral catalyst leads to a fluoroalkyl amine with high enantioselectivity and high yield.

7. 发明授权

US08273913B2 Amidation process for the preparation of cathepsin K inhibitors 有权
标题翻译：用于制备组织蛋白酶K抑制剂的酰胺化方法
公开(公告)号：US08273913B2
公开(公告)日：2012-09-25
申请号：US12593695
申请日：2008-03-31
申请人： Paul O'Shea , Francis Gosselin
发明人： Paul O'Shea , Francis Gosselin
IPC分类号： C07C255/46
CPC分类号： C07C315/04 , C07C2601/02 , C07C317/32
摘要： This invention describes an amidation process whereby amino acids of the Formulae IIA or IIB can be activated and treated with an amine in the presence of a base to yield amides of the Formula (I), without loss of optical purity.
摘要翻译：本发明描述了酰胺化方法，其中式IIA或IIB的氨基酸可以在碱的存在下用胺活化和处理，得到式（I）的酰胺，而不损失光学纯度。

8. 发明授权

US07154005B2 Synthesis of alpha fluoroalkyl amines 失效
标题翻译： α-氟烷基胺的合成
公开(公告)号：US07154005B2
公开(公告)日：2006-12-26
申请号：US11221279
申请日：2005-09-07
申请人： Paul O'Shea , Francis Gosselin
发明人： Paul O'Shea , Francis Gosselin
IPC分类号： C07C209/66
CPC分类号： C07C209/52 , C07B2200/07 , C07C213/00 , C07C319/20 , C07C211/29 , C07C211/30 , C07C211/31 , C07C217/48 , C07C323/32
摘要： This invention describes the reaction of an alpha fluoroalkyl ketone with a bis(trialkylsilyl)amide to give a stable N-trialkylsilyl imine. Treatment of the N-trialkylsilyl imine with an alcohol leads to solvolysis of the trialkylsilyl group and yields a stable mixture of an aminal and an imine in high yield. Catalytic reduction of this mixture, or of the individual components, in the presence of a chiral catalyst leads to a fluoroalkyl amine with high enantioselectivity and high yield.
摘要翻译：本发明描述了α-氟烷基酮与双（三烷基甲硅烷基）酰胺的反应，得到稳定的N-三烷基甲硅烷基亚胺。用醇处理N-三烷基甲硅烷基胺导致三烷基甲硅烷基的溶剂解，并以高产率得到稳定的亚胺和亚胺的混合物。在手性催化剂的存在下，该混合物或各组分的催化还原导致具有高对映选择性和高收率的氟烷基胺。

9. 发明授权

US5983509A Marine navigation device 失效
标题翻译：海洋导航装置
公开(公告)号：US5983509A
公开(公告)日：1999-11-16
申请号：US981703
申请日：1998-01-05
申请人： Francis Gosselin , Frederic Leloup
发明人： Francis Gosselin , Frederic Leloup
IPC分类号： G01C21/20 , G09B29/10 , B43L5/00 , A47B27/00 , B43L7/10
CPC分类号： G01C21/20 , B63B49/00 , G09B29/10 , G09B29/106
摘要： Device for positioning and orienting a boat on a navigational chart by data supplied by a communication via satellite (Global Positioning system), more commonly designated G.P.S., comprising two superposed disks, one serving as lower protractor (D1) provided with a North mark, the other as upper reader (D2), connected in their rotation center by an eyelet (24), two positioning rulers (R1, R2) punched by a longitudinal central aperture (4,5) and present on their edges a tenon which allows them to slide freely, each one in a mortised slide provided on each disk. During the positioning on the chart, the two disks are blocked (D1, D2) one against the other, the lower disk (D1) such as its North mark are placed in direction of the chart, the two rulers (R1, R2) are blocked perpendicularly one towards the other but with free slide. The disks are unlocked (D1, D2) during the orientation, and the upper disk (D2) can pivot with the upper niler (R2) which is used as orientation ruler. For locking, the upper disk (D2) carries an immobilization device, such as a thread case (20) and a blocking screw (21), that cooperate with the hole (16) on the lower disk (D1)
摘要翻译： PCT No.PCT / FR96 / 01016 Sec。 371日期：1998年1月5日 102（e）1998年1月5日PCT PCT 1996年7月2日PCT公布。出版物WO97 / 02468 日期1997年1月23日通过卫星通信（全球定位系统）提供的数据在导航图上定位和定向船舶的设备（全球定位系统），更常用的指定GPS，包括两个叠加的盘，一个作为提供的低量角器（D1）另一个作为上部读取器（D2），通过孔眼（24）在其旋转中心连接，由纵向中心孔（4,5）刺穿并且在其边缘上存在的两个定位尺（R1，R2）榫头允许他们自由滑动，每一个在每个磁盘上提供的踩踏滑块。在图表上的定位过程中，两个磁盘（D1，D2）彼此阻塞，下方的磁盘（D1）如其标记位于图表方向，两个标尺（R1，R2）分别为垂直方向一个朝向另一个方向，但是可以自由滑动。在取向时，盘被解锁（D1，D2），上盘（D2）可以用作定向尺的上部刀具（R2）枢转。为了锁定，上盘（D2）承载与下盘（D1）上的孔（16）配合的固定装置，例如螺纹套（20）和阻塞螺钉（21）

10. 发明授权

US5069714A Segregation-free metallurgical powder blends using polyvinyl pyrrolidone binder 失效
标题翻译：使用聚乙烯吡咯烷酮粘合剂的无SEEGEGATION-FREE冶金粉末
公开(公告)号：US5069714A
公开(公告)日：1991-12-03
申请号：US466664
申请日：1990-01-17
申请人： Francis Gosselin
发明人： Francis Gosselin
IPC分类号： B22F1/00 , B22F3/22
CPC分类号： B22F1/0059 , B22F3/22 , B22F2998/00
摘要： An improved metallurgical powder composition of a ferrous powder and at least one of an alloying powder, a lubricant or other additive. Lining, dusting and/or segregation of the composition is prevented by use of a polyvinyl pyrrolidone binding agent.
摘要翻译：一种改进的含铁粉末的冶金粉末组合物和合金粉末，润滑剂或其它添加剂中的至少一种。通过使用聚乙烯吡咯烷酮粘合剂可防止组合物的衬里，粉尘和/或偏析。

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