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1. 发明申请

US20210155597A1 COMPOSITIONS AND METHODS FOR TREATMENT OF PAIN 有权
公开(公告)号：US20210155597A1
公开(公告)日：2021-05-27
申请号：US17100433
申请日：2020-11-20
申请人： SYNVENTA LLC
发明人： Artour Gomtsian , Anton Bespalov
IPC分类号： C07D279/06 , C07D417/12 , C07D487/10 , C07D231/56 , C07D413/04 , C07D405/12 , C07D401/04 , C07D231/06 , C07D231/12 , C07C279/22 , A61P25/00
摘要： The present disclosure relates to compositions comprising a transient receptor potential vanilloid-1 (TRPV1) antagonist and an alpha-2 adrenoreceptor agonist useful in the treatment of various forms of pain, including chronic pain (CP) syndromes, inflammatory pain and pain associated with neuropathy and other diseases and disease states; and methods of use thereof.

2. 发明申请

US20200317730A1 TARGETED NITROXIDE AGENTS 审中-公开
公开(公告)号：US20200317730A1
公开(公告)日：2020-10-08
申请号：US16689930
申请日：2019-11-20
申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education
发明人： Peter Wipf , Marie-Celine Frantz
IPC分类号： C07K5/08 , A61K31/454 , C07D211/58 , C07D401/12 , A61K47/64 , C07D417/12 , C07C237/16 , C07D209/46 , C07D211/94 , C07D221/22 , C07D209/44 , C07D279/06 , C07D471/08
摘要： Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

3. 发明申请

US20180298054A1 TARGETED NITROXIDE AGENTS 审中-公开
公开(公告)号：US20180298054A1
公开(公告)日：2018-10-18
申请号：US15855598
申请日：2017-12-27
申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education
发明人： Peter Wipf , Marie-Celine Frantz
IPC分类号： C07K5/08 , C07D221/22 , C07D211/94 , C07D209/46 , C07C237/16 , A61K47/64 , A61K31/454 , C07D279/06 , C07D209/44 , C07D417/12 , C07D401/12 , C07D211/58 , C07D471/08
摘要： Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

4. 发明授权

US10051861B2 N-arylamidine-substituted trifluoroethyl sulfide derivatives as acaricides and insecticides 有权
公开(公告)号：US10051861B2
公开(公告)日：2018-08-21
申请号：US15349297
申请日：2016-11-11
申请人： BAYER CROPSCIENCE AG , BAYER INTELLECTUAL PROPERTY GMBH
发明人： Adeline Koehler , Bernd Alig , Angela Becker , Arnd Voerste , Ulrich Goergens , Reiner Fischer , Wahed Ahmed Moradi , Silvia Cerezo-Galvez , Julia Johanna Hahn , Kerstin Ilg , Hans-Georg Schwarz , Takuya Gomibuchi , Masahito Ito , Daiei Yamazaki , Katsuhiko Shibuya , Eiichi Shimojo
IPC分类号： C07D207/22 , C07D207/34 , C07D211/38 , C07D211/72 , C07D211/98 , C07D239/28 , C07D241/24 , C07D263/28 , C07D277/16 , C07D277/18 , C07D277/38 , C07D277/54 , C07D279/06 , C07D285/08 , C07D295/125 , C07D295/13 , C07D305/08 , C07D307/24 , C07D307/68 , C07D331/04 , C07D333/38 , C07D333/48 , C07D401/06 , A01N41/10 , A01N41/12 , A01N43/40 , C07C323/36 , C07C323/44 , C07D213/78 , C07C317/40 , C07C323/41 , C07C335/16 , C07D213/61 , A01N43/08 , A01N43/10 , A01N43/36 , A01N43/60 , A01N43/84 , A01N43/86 , C07C315/02 , C07C317/34 , C07C319/20 , C07C323/45 , C07C319/14
摘要： The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) in which X1, X2, X3, X4, R1, R2, R3, n have the meanings given in the description—to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation.

5. 发明授权

US09890192B2 Targeted nitroxide agents 有权
公开(公告)号：US09890192B2
公开(公告)日：2018-02-13
申请号：US14943965
申请日：2015-11-17
申请人： University of Pittsburgh—of the Commonwealth System of Higher Education
发明人： Peter Wipf , Marie-Celine Frantz
IPC分类号： C07K5/08 , A61K31/454 , C07D211/58 , C07D401/12 , C07D417/12 , C07C237/16 , C07D209/46 , C07D211/94 , C07D221/22 , C07D209/44 , C07D279/06 , C07D471/08 , A61K47/64
CPC分类号： C07K5/08 , A61K31/454 , A61K47/64 , C07C237/16 , C07D209/44 , C07D209/46 , C07D211/58 , C07D211/94 , C07D221/22 , C07D279/06 , C07D401/12 , C07D417/12 , C07D471/08
摘要： Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

6. 发明授权

US09642363B2 N-arylamidine-substituted trifluoroethyl sulfide derivatives as acaricides and insecticides 有权
公开(公告)号：US09642363B2
公开(公告)日：2017-05-09
申请号：US14366715
申请日：2012-12-12
申请人： BAYER CROPSCIENCE AG , BAYER INTELLECTUAL PROPERTY GMBH
发明人： Adeline Koehler , Bernd Alig , Angela Becker , Arnd Voerste , Ulrich Goergens , Reiner Fischer , Wahed Ahmed Moradi , Silvia Cerezo-Galvez , Julia Johanna Hahn , Kerstin Ilg , Hans-Georg Schwarz , Takuya Gomibuchi , Masahito Ito , Daiei Yamazaki , Katsuhiko Shibuya , Eiichi Shimojo
IPC分类号： C07D207/22 , C07D207/34 , C07D211/38 , C07D211/72 , C07D213/61 , C07D213/78 , C07D239/28 , C07D241/24 , C07D263/28 , C07D277/18 , C07D279/06 , C07D285/08 , C07D295/125 , A01N41/10 , A01N41/12 , A01N43/40 , C07C323/36 , C07C323/44 , C07D331/04 , C07D333/38 , C07D333/48 , C07C317/40 , C07C323/41 , C07C335/16 , C07D305/08 , C07D307/24 , C07D307/68 , A01N43/08 , A01N43/10 , A01N43/36 , A01N43/60 , A01N43/84 , A01N43/86 , C07C315/02 , C07C317/34 , C07C319/20 , C07C323/45
CPC分类号： A01N41/10 , A01N41/12 , A01N43/08 , A01N43/10 , A01N43/36 , A01N43/40 , A01N43/60 , A01N43/84 , A01N43/86 , C07C315/02 , C07C317/34 , C07C317/40 , C07C319/14 , C07C319/20 , C07C323/36 , C07C323/41 , C07C323/44 , C07C323/45 , C07C335/16 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/22 , C07D207/34 , C07D211/38 , C07D211/72 , C07D211/98 , C07D213/61 , C07D213/78 , C07D239/28 , C07D241/24 , C07D263/28 , C07D277/16 , C07D277/18 , C07D277/38 , C07D277/54 , C07D279/06 , C07D285/08 , C07D295/125 , C07D295/13 , C07D305/08 , C07D307/24 , C07D307/68 , C07D331/04 , C07D333/38 , C07D333/48 , C07D401/06
摘要： The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) in which X1, X2, X3, X4, R1, R2, R3, n have the meanings given in the description—to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation.

7. 发明申请

US20160137692A1 TARGETED NITROXIDE AGENTS 有权
公开(公告)号：US20160137692A1
公开(公告)日：2016-05-19
申请号：US14943965
申请日：2015-11-17
申请人： University of Pittsburgh - of the Commonwealth System of Higher Education
发明人： Peter Wipf , Marie-Celine Frantz
IPC分类号： C07K5/08 , C07D471/08 , C07D209/44 , C07D279/06 , C07D211/94
CPC分类号： C07K5/08 , A61K31/454 , A61K47/64 , C07C237/16 , C07D209/44 , C07D209/46 , C07D211/58 , C07D211/94 , C07D221/22 , C07D279/06 , C07D401/12 , C07D417/12 , C07D471/08
摘要： Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

8. 发明申请

US20150329506A1 4,6-DIARYLAMINOTHIAZINES AS BACE1 INHIBITORS AND THEIR USE FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION 有权
标题翻译： 4-DIARYLAMINOTHIAZINES作为BACE1抑制剂及其用于减少β-淀粉样生成的用途
公开(公告)号：US20150329506A1
公开(公告)日：2015-11-19
申请号：US14653025
申请日：2012-12-19
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： Yong-Jin Wu , Jason M. Guernon
IPC分类号： C07D279/06 , C07D417/14 , C07D417/10
CPC分类号： C07D279/06 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14
摘要： Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: (I) wherein R1 and R2 are independently hydrogen, or —CH3; or R1 and R2 can join together in a ring by adding —(CH2)4—; R3 is hydrogen or C1-C3 alkyl; Y and Z are independently a C6-C10-aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4 dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, —C═OC1-4 alkyl, —SO2C1-4 alkyl, and C2-C4 alkynyl; A is selected from the group of phenyl, benzyl, oxazolyl, thiazolyl, isoxazolyl, imidazolyl, pyrazolyl, pyridyl, pyrimidinyl, and pyrazinyl groups which can be further substituted with from 0-3 substituents selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4 dialkylamino, haloC1-4 alkyl, hydroxyC1-6 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is —NHCO—, or is a single bond; and L and Z together can be absent.
摘要翻译：包括其药学上可接受的盐的式（I）化合物在本文中阐述：（I）其中R 1和R 2独立地是氢或-CH 3; 或者R 1和R 2可以通过加入 - （CH 2）4 - R3是氢或C1-C3烷基; Y和Z独立地是C 6 -C 10 - 芳基或5-10元杂环基，其可以进一步被0-3个选自以下的取代基取代：卤素，羟基，氨基，C 1-4烷基氨基，C 1-4二烷基氨基卤代C 1-4烷基，CN，C 1 -C 6烷基或环烷基，C 1 -C 6烷氧基，-C 1 -C 1-4烷基，-SO 2 C 1-4烷基和C 2 -C 4炔基; A选自苯基，苄基，恶唑基，噻唑基，异恶唑基，咪唑基，吡唑基，吡啶基，嘧啶基和吡嗪基，其可以进一步被0-3个选自以下的取代基取代：卤素，羟基，氨基， C 1-4烷基氨基，C 1-4二烷基氨基，卤代C 1-4烷基，羟基C 1-6烷基，CN，C 1 -C 6烷基或环烷基，C 1 -C 6烷氧基和C 2 -C 4炔基; L是-NHCO-，或是单键; 可以不存在L和Z。

9. 发明申请

US20140315898A1 N-ARYLAMIDINE-SUBSTITUTED TRIFLUOROETHYL SULFIDE DERIVATIVES AS ACARICIDES AND INSECTICIDES 有权
标题翻译：作为丙种球菌和杀虫剂的N-亚磺酰胺取代的三氟乙醇硫代衍生物
公开(公告)号：US20140315898A1
公开(公告)日：2014-10-23
申请号：US14366715
申请日：2012-12-12
申请人： BAYER CROPSCIENCE AG , BAYER INTELLECTUAL PROPERTY GMBH
发明人： Adeline Koehler , Bernd Alig , Angela Becker , Arnd Voerste , Ulrich Goergens , Reiner Fischer , Wahed Ahmed Moradi , Silvia Cerezo-Galvez , Julia Johanna Hahn , Kerstin Ilg , Hans-Georg Schwarz , Takuya Gomibuchi , Masahito Ito , Daiei Yamazaki , Katsuhiko Shibuya , Eiichi Shimojo
IPC分类号： A01N41/10 , C07C315/02 , C07D333/38 , A01N43/10 , C07D207/34 , A01N43/36 , C07D307/68 , A01N43/08 , C07D213/78 , A01N43/40 , C07C323/45 , A01N43/84 , C07C319/20 , C07D241/24 , A01N43/60 , C07D279/06 , A01N43/86 , C07C317/34
CPC分类号： A01N41/10 , A01N41/12 , A01N43/08 , A01N43/10 , A01N43/36 , A01N43/40 , A01N43/60 , A01N43/84 , A01N43/86 , C07C315/02 , C07C317/34 , C07C317/40 , C07C319/14 , C07C319/20 , C07C323/36 , C07C323/41 , C07C323/44 , C07C323/45 , C07C335/16 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/22 , C07D207/34 , C07D211/38 , C07D211/72 , C07D211/98 , C07D213/61 , C07D213/78 , C07D239/28 , C07D241/24 , C07D263/28 , C07D277/16 , C07D277/18 , C07D277/38 , C07D277/54 , C07D279/06 , C07D285/08 , C07D295/125 , C07D295/13 , C07D305/08 , C07D307/24 , C07D307/68 , C07D331/04 , C07D333/38 , C07D333/48 , C07D401/06
摘要： The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) in which X1, X2, X3, X4, R1, R2, R3, n have the meanings given in the description—to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation
摘要翻译：本发明涉及式（I）的新型N-芳基酰胺取代的三氟乙基硫醚衍生物，其中X 1，X 2，X 3，X 4，R 1，R 2，R 3，n具有本说明书中给出的含义 - 用作杀螨剂以及用于控制动物害虫的杀虫剂及其制备方法和中间体

10. 发明申请

US20100120754A1 IDENTIFICATION AND USE OF SMALL MOLECULES TO MODULATE TRANSCRIPTION FACTOR FUNCTION AND TO TREAT TRANSCRIPTION FACTOR ASSOCIATED DISEASES 审中-公开
标题翻译：鉴定和使用小分子调节转录因子功能和治疗转录因子相关疾病
公开(公告)号：US20100120754A1
公开(公告)日：2010-05-13
申请号：US12436685
申请日：2009-05-06
申请人： Peter Oettgen , Alan Rigby , Towia Libermann
发明人： Peter Oettgen , Alan Rigby , Towia Libermann
IPC分类号： A61K31/54 , C40B30/02 , A61K31/36 , A61K31/522 , A61K31/17 , A61K31/13 , C07D279/06 , C07D473/00 , C07D317/44 , C07C273/00 , C07C211/00
CPC分类号： G16C20/60 , G16B35/00
摘要： The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor.
摘要翻译：本发明涉及鉴定能够调节转录因子功能的小分子候选试剂的方法，使得该目标蛋白质下游的靶转录因子和/或蛋白质的功能/表达包括使用计算机高通量筛选小分子文库通过独特的转录因子和/或在药效基团内定义的DNA描述符来选择性鉴定其靶向和破坏转录因子-DNA界面的能力的候选小分子/试剂的对接，然后测试/评价上述鉴定的候选试剂通过一种或多种体外测定来调节转录因子功能的能力，包括表达该靶蛋白和/或靶转录因子下游的蛋白质。

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