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1. 发明授权

US09926337B2 Substituted asymmetric ureas as modulators of ghrelin receptor activity 有权
公开(公告)号：US09926337B2
公开(公告)日：2018-03-27
申请号：US15368362
申请日：2016-12-02
申请人： HELSINN HEALTHCARE SA
发明人： Claudio Giuliano , Silvina Garcia Rubio , Antoine Daina , Angelo Guainazzi , Claudio Pietra
IPC分类号： A61K31/17 , C07C275/26 , C07F7/08 , C07D401/14 , C07D211/58 , C07D401/12 , C07D417/14 , C07D409/14 , C07D239/26 , C07D405/12 , C07D403/12 , C07D471/04 , C07D401/06 , C07D211/60 , C07D211/94 , C07D211/96 , C07D213/00 , C07D241/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07F7/0812 , C07D211/58 , C07D211/60 , C07D211/94 , C07D211/96 , C07D213/00 , C07D239/26 , C07D241/12 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor. The compounds have the general Formula I: or pharmaceutically acceptable salts thereof.

2. 再颁专利

USRE46424E1 Method for producing 3-amidinophenylalanine derivatives 有权
公开(公告)号：USRE46424E1
公开(公告)日：2017-06-06
申请号：US14145892
申请日：2013-12-31
申请人： Wilex AG
发明人： Hugo Ziegler , Peter Wikstroem
IPC分类号： C07D295/00 , C07D213/00 , C07D295/205 , C07D211/60
CPC分类号： C07D295/205 , C07D211/60
摘要： The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (H2 or ammonium formiate formate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.

3. 发明授权

US09546157B2 Asymmetric piperidinyl-substituted ureas as medicines 有权
标题翻译：不对称哌啶基取代脲作为药物
公开(公告)号：US09546157B2
公开(公告)日：2017-01-17
申请号：US14640551
申请日：2015-03-06
申请人： Helsinn Healthcare SA
发明人： Claudio Giuliano , Silvina Garcia Rubio , Antoine Daina , Angelo Guainazzi , Claudio Pietra
IPC分类号： A61K31/4468 , C07D211/58 , C07D295/00 , C07D401/14 , C07D401/12 , C07D417/14 , C07D409/14 , C07D239/26 , C07D405/12 , C07D403/12 , C07D471/04 , C07D401/06 , C07D211/60 , C07D211/94 , C07D211/96 , C07D213/00
CPC分类号： C07F7/0812 , C07D211/58 , C07D211/60 , C07D211/94 , C07D211/96 , C07D213/00 , C07D239/26 , C07D241/12 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor. The compounds have the general Formula I: or pharmaceutically acceptable salts thereof.
摘要翻译：公开了用于预防和/或治疗由生长素释放肽受体病理生理介导的疾病的化合物，组合物和方法。化合物具有通式I或其药学上可接受的盐。

4. 发明授权

US09161537B2 Substituted 4-cyan-3-phenyl-4-(pyridine-3-yl)butanoates, processes for preparation thereof and use thereof as herbicides and plant growth regulators 有权
标题翻译：取代的4-氰基-3-苯基-4-（吡啶-3-基）丁酸酯，其制备方法及其作为除草剂和植物生长调节剂的用途
公开(公告)号：US09161537B2
公开(公告)日：2015-10-20
申请号：US14366099
申请日：2012-12-17
申请人： BAYER INTELLECTUAL PROPERTY GMBH
发明人： Harald Jakobi , Marc Morsin , Hansjörg Dietrich , Elmar Gatzweiler , Isolde Haeuser-Hahn , Ines Heinemann , Christopher Hugh Rosinger
IPC分类号： C07D213/00 , A01N43/40 , C07D405/12 , C07D409/12 , C07D213/57
CPC分类号： A01N43/40 , C07D213/57 , C07D405/12 , C07D409/12
摘要： Compounds of the formula (I) or salts thereof in which R1 and (R2)n are as defined in Claim 1 are suitable as herbicides for the control of harmful plants or as plant growth regulators. The compounds can be prepared by the processes of Claim 7.
摘要翻译：式（I）化合物或其盐，其中R 1和（R 2）n如权利要求1中所定义，它们适合用作控制有害植物或作为植物生长调节剂的除草剂。化合物可以通过权利要求7的方法制备。

5. 发明授权

US08957214B2 Pest control agent 有权
标题翻译：害虫控制剂
公开(公告)号：US08957214B2
公开(公告)日：2015-02-17
申请号：US13814753
申请日：2011-08-26
申请人： Shinzo Kagabu , Masaaki Mitomi , Shigeki Kitsuda , Ryo Horikoshi , Masahiro Nomura , Yasumichi Onozaki
发明人： Shinzo Kagabu , Masaaki Mitomi , Shigeki Kitsuda , Ryo Horikoshi , Masahiro Nomura , Yasumichi Onozaki
IPC分类号： C07D213/00 , A01N43/40 , C07D211/98 , A01N43/50 , A01N43/78 , A01N47/40 , C07C233/05 , C07C233/12 , C07C261/04 , C07C271/12 , C07C311/09 , C07F9/58 , C07D401/06
CPC分类号： A01N43/40 , A01N37/18 , A01N43/50 , A01N43/54 , A01N43/58 , A01N43/78 , A01N47/02 , A01N47/12 , A01N47/40 , A01N57/32 , C07C233/05 , C07C233/12 , C07C261/04 , C07C271/12 , C07C311/09 , C07D211/98 , C07D213/36 , C07D213/40 , C07D213/42 , C07D213/61 , C07D213/75 , C07D237/08 , C07D277/32 , C07D333/20 , C07D401/06 , C07D401/12 , C07D405/12 , C07D417/12 , C07F9/58
摘要： A compound of formula (Ie′): wherein Ar′, R1, R4e and Y are as defined herein and a method of controlling pests using the compound.
摘要翻译：式（Ie'）的化合物：其中Ar'，R 1，R 4e和Y如本文所定义，以及使用该化合物控制害虫的方法。

6. 发明授权

US08901102B2 Therapeutic substances that modulate genome methylation 有权
公开(公告)号：US08901102B2
公开(公告)日：2014-12-02
申请号：US14165050
申请日：2014-01-27
申请人： Retrotope, Inc.
发明人： Mikhail S. Shchepinov
IPC分类号： C07H19/06 , C07D213/00 , C07H19/073 , C07D405/04
CPC分类号： C07H19/06 , C07D405/04 , C07H19/073
摘要： Compounds containing nucleic acid bases or their precursors modified by enrichment at specific sites with heavy stable isotopes of elements naturally present at those sites in minute amount are useful for the treatment of diseases characterized by altered gene expression and altered pattern of epigenomic control. These compounds, when used as nutrients or in other medicinal application methods, can alter the DNA methylation pattern in a simple way through the well-understood mechanism of kinetic isotope effect (KIE). This effect could also be useful for modifying methylation kinetics in stem cell technology, cloning and as disease therapeutics.

7. 发明授权

US08895782B2 Alkynyl phenyl derivative compounds for treating ophthalmic diseases and disorders 有权
公开(公告)号：US08895782B2
公开(公告)日：2014-11-25
申请号：US14162672
申请日：2014-01-23
申请人： Acucela Inc.
发明人： Ian Leslie Scott , Vladimir Aleksandrovich Kuksa , Mark W. Orme , Thomas Little , Anna Gall , Jennifer Gage , Feng Hong
IPC分类号： C07D213/00 , C07C235/34 , C07C215/42 , C07D335/02 , C07C217/48 , C07C211/27 , C07C215/30 , C07D309/12 , C07C217/64 , C07D213/38
CPC分类号： C07C215/68 , C07C211/27 , C07C211/30 , C07C215/28 , C07C215/30 , C07C215/42 , C07C217/14 , C07C217/48 , C07C217/62 , C07C217/64 , C07C217/72 , C07C235/34 , C07C237/20 , C07C251/40 , C07C255/58 , C07C317/28 , C07C323/25 , C07C323/29 , C07C323/36 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D209/32 , C07D213/14 , C07D213/38 , C07D309/06 , C07D309/10 , C07D309/12 , C07D333/06 , C07D333/16 , C07D335/02
摘要： Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.

8. 发明授权

US08809544B2 Nitrogen-containing heterocyclic compound and method for producing same 有权
标题翻译：含氮杂环化合物及其制造方法
公开(公告)号：US08809544B2
公开(公告)日：2014-08-19
申请号：US14175904
申请日：2014-02-07
申请人： Nippon Soda Co., Ltd.
发明人： Koichi Kutose , Hiroki Inoue , Shiro Tsubokura
IPC分类号： C07D213/00 , C07D213/75 , C07D213/89
CPC分类号： C07D213/89 , C07D213/75
摘要： There are provided a nitrogen-containing heterocyclic compound such as a substituted amino-pyridine-N-oxide compound represented by formula (1), which is useful as a synthetic intermediate for an agrochemical and the like; and a method for producing the nitrogen-containing heterocyclic compound. (In formula (1), R1 and R2 each represents a hydrogen atom or an unsubstituted or substituted alkyl group; R3 represents a hydrogen atom, an unsubstituted or substituted alkylcarbonyl group or the like; R4 represents an unsubstituted or substituted alkylcarbonyl group, an unsubstituted or substituted arylcarbonyl group or the like; A represents a hydroxyl group, a thiol group or the like; m represents any one of integers of 1 to 4; k represents any one of integers of 0 to 3; and k+m≦4.)
摘要翻译：提供了可用作农药等的合成中间体的含氮杂环化合物，例如由式（1）表示的取代的氨基 - 吡啶-N-氧化物化合物; 和含氮杂环化合物的制造方法。（式（1）中，R 1和R 2各自表示氢原子或未取代或取代的烷基; R 3表示氢原子，未取代或取代的烷基羰基等; R 4表示未取代或取代的烷基羰基，未取代的或取代的芳基羰基等; A表示羟基，硫醇基等; m表示1〜4的整数中的任一个; k表示0〜3的整数中的任一个; k + m＆lt; 1l; 4。）

9. 发明授权

US08772500B2 TRPV3 modulators 有权
标题翻译： TRPV3调节剂
公开(公告)号：US08772500B2
公开(公告)日：2014-07-08
申请号：US13658374
申请日：2012-10-23
申请人： AbbVie Inc.
发明人： Erol K. Bayburt , Bruce Clapham , Phil B. Cox , Jerome F. Daanen , Michael J. Dart , Gregory A. Gfesser , Arthur Gomtsyan , Michael E. Kort , Philip R. Kym , Robert G. Schmidt
IPC分类号： C07D213/00 , C07D213/28 , C07D211/74 , C07D421/00 , C07D401/00
CPC分类号： C07D213/38 , A61K31/192 , A61K31/435 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/47 , A61K31/505 , A61K45/06 , C07D213/30 , C07D213/34 , C07D213/72 , C07D215/14 , C07D221/04 , C07D239/26 , C07D311/04 , C07D401/06 , C07D405/06 , C07D405/08 , C07D405/10 , C07D417/08 , A61K2300/00
摘要： Disclosed herein are modulators of TRPV3 of formula (II): wherein G1, X1, X2, X3, X4, X5, G2, Ra, Rb, and u are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
摘要翻译：本文公开了式（II）的TRPV3的调节剂：其中G1，X1，X2，X3，X4，X5，G2，Ra，Rb和u如说明书中所定义。还提出了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和障碍的方法。

10. 发明授权

US08772499B2 TRPV3 modulators 有权
标题翻译： TRPV3调节剂
公开(公告)号：US08772499B2
公开(公告)日：2014-07-08
申请号：US13658355
申请日：2012-10-23
申请人： AbbVie Inc.
发明人： Erol K. Bayburt , Bruce Clapham , Phil B. Cox , Jerome F. Daanen , Michael J. Dart , Gregory A. Gfesser , Arthur Gomtsyan , Michael E. Kort , Philip R. Kym , Robert G. Schmidt , Eric A. Voight
IPC分类号： C07D213/00 , C07D213/28 , C07D211/74 , C07D421/00 , C07D401/00
CPC分类号： C07D213/38 , A61K31/192 , A61K31/435 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/47 , A61K31/505 , A61K45/06 , C07D213/30 , C07D213/34 , C07D213/72 , C07D215/14 , C07D221/04 , C07D239/26 , C07D311/04 , C07D401/06 , C07D405/06 , C07D405/08 , C07D405/10 , C07D417/08 , A61K2300/00
摘要： Disclosed herein are modulators of TRPV3 of Formula (I) wherein p is 1, 2, 3, or 4, and G1, X1, X2, X3, X4, X5, G2, Z1, Ra, Rb, and u are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
摘要翻译：本文公开了式（I）的TRPV3的调节剂，其中p为1,2,3或4，并且G1，X1，X2，X3，X4，X5，G2，Z1，Ra，Rb和u如规格。还提出了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和障碍的方法。

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