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1. 发明授权

US11040937B2 Amide derivative 有权
公开(公告)号：US11040937B2
公开(公告)日：2021-06-22
申请号：US15121687
申请日：2015-02-27
申请人： TOHOKU UNIVERSITY , NATIONAL UNIVERSITY CORPORATION GUNMA UNIVERSITY , FUSO PHARMACEUTICAL INDUSTRIES, LTD.
发明人： Haruhisa Kikuchi , Yoshiteru Oshima , Toshio Hattori , Yuzuru Kubohara , Osamu Yamada , Jing Zhang , Yoshihisa Matsushita , Shinya Kida
IPC分类号： C07C235/50 , C07C235/48 , C07C233/36 , C07C233/78 , C07C233/62 , C07D309/08 , C07D471/04 , C07D213/81 , C07C235/60 , C07C237/22 , C07C237/42 , C07D209/14 , C07C237/34 , A61K31/437 , A61K31/4045 , A61K31/4409 , A61K31/445 , A61K31/40 , A61K31/351 , A61K31/167 , A61K31/381 , A61K31/397 , A61K31/166 , A61K31/165 , C07D205/04 , C07D207/16 , C07D211/60 , C07D333/38
摘要： The present invention provides a useful medicament for the treatment and/or prophylaxis of a disease associated with the enhancement of OPN production including cancer, which comprises a compound of formula: wherein R1, R2, R3, R4, R5, R6, R7, m, n, p, X, and Y are as defined in the specification, a pharmaceutically acceptable salt thereof.

2. 发明授权

US10745350B2 Compounds and pharmaceutical composition associated with ubiquitination-proteasome system 有权
公开(公告)号：US10745350B2
公开(公告)日：2020-08-18
申请号：US15748827
申请日：2016-07-30
申请人： CALGENT BIOTECHNOLOGY CO., LTD.
发明人： Yun Yen , Jing-ping Liou , Shiow-lin Pan
IPC分类号： A61K31/122 , A61K31/40 , A61K31/166 , A61K31/70 , C07D207/04 , A61K45/06 , A61P35/00 , C07D295/135 , C07D295/13 , C07C311/29 , C07C237/34 , C07D213/40 , C07C225/30 , C07C255/58 , C07D209/08 , C07D209/44 , C07D215/38 , C07D215/40 , A61K33/24 , A61K31/7048 , C07C235/54 , A61P25/14 , A61P25/28 , A61P3/10 , C07C237/48
摘要： The invention relates to new compounds with low cytotoxicity for blocking ubiquitination-proteasome system in diseases. Accordingly, these compounds can be used in treatment of treating disorders including, but not limited to, cancers, neurodegenerative diseases, inflammatory disorders and autoimmune disorders and metabolic disorders.

3. 发明申请

US20170107174A1 COMPOUNDS, PHARMACEUTICAL COMPOSITION AND THEIR USE IN TREATING NEURODEGENERATIVE DISEASES 审中-公开
公开(公告)号：US20170107174A1
公开(公告)日：2017-04-20
申请号：US15317742
申请日：2015-06-15
申请人： UNIVERSITE DE LILLE 2 DROIT ET SANTE , CENTER HOSPITALIER REGIONAL ET UNIVERSITARE DE LILLE (CHRU)
发明人： Patricia Melnyk , Patrick Vermersch , Pascal Carato , Bénédicte Oxombre-Vanteghem , Hélène Zephir , Marion Donnier-Marechal
IPC分类号： C07C233/78 , C07D209/44 , C07C235/50 , C07C211/29 , C07C255/57 , C07C237/10 , C07C255/60 , C07C311/37 , A61K49/00 , C07C237/34
CPC分类号： C07C233/78 , A61K49/00 , C07C211/27 , C07C211/29 , C07C235/50 , C07C237/10 , C07C237/20 , C07C237/34 , C07C255/57 , C07C255/60 , C07C311/37 , C07D209/08 , C07D209/44
摘要： The present invention is directed to novel compounds of Formula (I), pharmaceutically acceptable salts or solvates thereof, and their use.

4. 发明申请

US20150166470A1 7-DISUBSTITUTED-PHENYL TETRACYCLINE DERIVATIVES 审中-公开
标题翻译： 7-取代的苯基四环素衍生物
公开(公告)号：US20150166470A1
公开(公告)日：2015-06-18
申请号：US14403616
申请日：2013-05-30
申请人： Paratek Pharmaceuticals, Inc.
发明人： Todd Bowser , Paul Abato
IPC分类号： C07C237/34
CPC分类号： C07C237/34 , C07C2603/46
摘要： 7-Disubstituted-phenyl tetracycline compounds are disclosed herein. Also disclosed is a method for treatment or prevention of spinal muscular atrophy using the 7-disubstituted-phenyl tetracycline compounds. This invention also relates to a method for treating or preventing a subject having spinal muscular atrophy. The method includes administering to the subject an effective amount of a tetracycline compound of formula (1), such that the spinal muscular atrophy is treated or prevented. Advantageously, the tetracycline compounds used in this method of the invention have one or more of the following characteristics: 1) potency in modulating mRNA splicing, 2) potency in modulating SMN protein levels, 3) central nervous system (CNS) and/pr brain penetration, 4) decreased phototoxic properties and 5) decreased antibacterial properties.
摘要翻译： 7-二取代 - 苯基四环素化合物在本文中公开。还公开了使用7-二取代 - 苯基四环素化合物治疗或预防脊髓性肌肉萎缩的方法。本发明还涉及治疗或预防具有脊髓性肌肉萎缩的受试者的方法。该方法包括向受试者施用有效量的式（1）的四环素化合物，使得治疗或预防脊髓性肌萎缩。有利地，本发明方法中使用的四环素化合物具有一个或多个以下特征：1）调节mRNA剪接的效力，2）调节SMN蛋白水平的效力，3）中枢神经系统（CNS）和/ 渗透，4）光毒性降低，5）降低抗菌性能。

5. 发明申请

US20150038705A1 METHODS OF USE COMPRISING A BIOCIDAL POLYAMINE 有权
标题翻译：使用生物聚氨酯的方法
公开(公告)号：US20150038705A1
公开(公告)日：2015-02-05
申请号：US14507431
申请日：2014-10-06
申请人： Curza Global, LLC , University of Utah Research Foundation
发明人： DUSTIN WILLIAMS , RYAN LOOPER , SUJEEVINI JEYAPALINA , TRAVIS HAUSSENER , PAUL R. SEBAHAR , HARI KANNA REDDY
IPC分类号： C07D333/20 , A01N33/04 , C07C211/11 , C07C211/14 , C07C217/54 , A01N33/10 , C07C225/12 , A01N37/06 , C07C237/34 , A01N37/18 , C07D317/58 , A01N43/30 , C07D295/135 , A01N43/84 , A01N43/10 , C07C211/09
CPC分类号： A01N43/84 , A01N33/00 , A01N33/02 , A01N33/04 , A01N33/10 , A01N37/06 , A01N37/18 , A01N37/20 , A01N37/30 , A01N43/10 , A01N43/30 , A01N43/40 , A01N47/12 , A61K31/135 , A61K31/137 , A61K31/166 , A61K31/325 , A61K31/357 , A61K31/381 , A61K31/4418 , A61K31/5375 , A61L12/14 , A61L12/147 , C07C211/01 , C07C211/09 , C07C211/11 , C07C211/14 , C07C211/27 , C07C217/54 , C07C217/58 , C07C225/12 , C07C233/78 , C07C237/34 , C07C271/20 , C07D213/38 , C07D213/64 , C07D295/135 , C07D317/46 , C07D317/58 , C07D333/20 , C09D5/1625
摘要： Compounds, compositions, and methods comprising a polyamine compound are described, which may be used to kill, disperse, treat, reduce biofilms, and/or inhibit or substantially prevent biofilm formation. In certain aspects, the present invention relates to compounds, compositions, and methods comprising polyamine compounds that have antimicrobial or dispersing activity against a variety of bacterial strains capable of forming biofilms.
摘要翻译：描述了包含多胺化合物的化合物，组合物和方法，其可用于杀死，分散，治疗，减少生物膜和/或抑制或基本上防止生物膜形成。在某些方面，本发明涉及包含对能够形成生物膜的各种细菌菌株具有抗微生物或分散活性的多胺化合物的化合物，组合物和方法。

6. 发明申请

US20120004310A1 NON-PEPTIDE BDNF NEUROTROPHIN MIMETICS 审中-公开
标题翻译：非肽BDNF神经营养因子
公开(公告)号：US20120004310A1
公开(公告)日：2012-01-05
申请号：US13117537
申请日：2011-05-27
申请人： Frank M. LONGO , Stephen M. Massa , Sandeep Gupta
发明人： Frank M. LONGO , Stephen M. Massa , Sandeep Gupta
IPC分类号： A61K31/166 , C07C33/26 , C07C33/30 , C07C43/23 , C07C237/34 , C07C233/78 , C07C215/68 , C07D211/42 , C07D295/135 , C07D215/20 , A61K31/047 , A61K31/09 , A61P25/28 , A61P25/00 , A61P25/08 , A61P25/16 , A61P9/10 , A61P25/24 , A61P3/00 , A61P3/04 , A61P29/00 , A61P35/00 , C12N5/071 , C12N5/0793 , C07C327/48
CPC分类号： C07C33/30 , A61K31/136 , C07C33/26 , C07C33/46 , C07C43/2055 , C07C43/23 , C07C211/53 , C07C215/16 , C07C215/68 , C07C215/70 , C07C215/74 , C07C233/78 , C07C237/34 , C07C237/42 , C07C327/48 , C07C2601/14 , C07D211/42 , C07D215/14 , C07D215/20 , C07D295/135 , C07D401/10
摘要： Methods and compounds for treating neurological and other disorders are provided. Included is the administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for a TrkB receptor molecule.
摘要翻译：提供了治疗神经系统疾病和其他疾病的方法和化合物。包括向有需要的受试者施用有效量的对TrkB受体分子具有结合和/或调节特异性的化合物。

7. 发明申请

US20090018116A1 Therapeutic Compounds 审中-公开
标题翻译：治疗化合物
公开(公告)号：US20090018116A1
公开(公告)日：2009-01-15
申请号：US11569295
申请日：2005-05-20
申请人： Shujuan Jin , Ziping Liu , Claire Milburn , Miroslaw Tomaszewski , Christopher Walpole , Zhong-Yong Wei , Hua Yang
发明人： Shujuan Jin , Ziping Liu , Claire Milburn , Miroslaw Tomaszewski , Christopher Walpole , Zhong-Yong Wei , Hua Yang
IPC分类号： A61K31/55 , A61K31/40 , C07D207/09 , C07C237/34 , A61P1/00 , A61P35/00 , A61K31/166 , C07D223/04
CPC分类号： C07C237/42 , C07C237/44 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2601/18 , C07D207/09 , C07D211/26 , C07D215/48 , C07D217/16 , C07D237/28 , C07D265/30 , C07D295/13 , C07D295/192 , C07D295/32 , C07D307/79 , C07D309/14 , C07D317/46 , C07D319/08 , C07D319/12 , C07D321/10 , C07D413/06 , C07D471/08
摘要： Compounds of formula I or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, R4 and n are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
摘要翻译：式I化合物或其药学上可接受的盐：其中R1，R2，R3，R4和n如本说明书中所定义，以及包括该化合物的盐和药物组合物的制备。它们可用于治疗，特别是治疗疼痛。

8. 发明申请

US20060286567A1 Salicylamide-lanthanide complexes for use as luminescent markers 有权
公开(公告)号：US20060286567A1
公开(公告)日：2006-12-21
申请号：US11347881
申请日：2006-02-06
申请人： Kenneth Raymond , Stephane Petoud , Seth Cohen , Jide Xu
发明人： Kenneth Raymond , Stephane Petoud , Seth Cohen , Jide Xu
IPC分类号： C12Q1/68 , C07F5/00 , C12M1/34 , A61K31/28 , C07C237/34
CPC分类号： C12Q1/37 , C07C235/60 , C07C235/84 , C07C237/34 , C09K11/06 , C09K2211/1007 , C09K2211/182 , G01N33/582 , G01N2458/40 , Y10S436/80
摘要： The present invention provides luminescent lanthanide metal chelates comprising a metal ion of the lanthanide series and a complexing agent comprising at least one salicylamidyl moiety. Also provided are probes incorporating the salicylamidyl ligands of the invention and methods utilizing the ligands of the invention and probes comprising the ligands of the invention.

9. 发明授权

US06872852B2 Polyamine analogues as cytotoxic agents 失效
标题翻译：多胺类似物作为细胞毒性剂
公开(公告)号：US06872852B2
公开(公告)日：2005-03-29
申请号：US10239521
申请日：2001-03-23
申请人： Mark R. Burns
发明人： Mark R. Burns
IPC分类号： C07D233/84 , A61K31/136 , A61K31/137 , A61K31/16 , A61K31/18 , A61K31/27 , A61K31/275 , A61K31/343 , A61K31/36 , A61K31/381 , A61K31/405 , A61K31/4164 , A61K31/427 , A61K31/433 , A61K31/444 , A61K31/4709 , A61K31/506 , A61K45/06 , A61P35/00 , A61P43/00 , C07C211/13 , C07C211/14 , C07C211/27 , C07C211/29 , C07C211/30 , C07C211/31 , C07C211/49 , C07C211/50 , C07C211/54 , C07C217/08 , C07C217/14 , C07C217/40 , C07C217/58 , C07C223/02 , C07C233/10 , C07C233/11 , C07C233/37 , C07C233/40 , C07C233/62 , C07C237/10 , C07C237/12 , C07C237/34 , C07C245/24 , C07C247/16 , C07C255/58 , C07C279/12 , C07C291/02 , C07C311/19 , C07C311/39 , C07C317/44 , C07D207/16 , C07D209/14 , C07D209/18 , C07D213/36 , C07D213/38 , C07D213/73 , C07D215/12 , C07D215/42 , C07D233/42 , C07D277/28 , C07D285/10 , C07D285/14 , C07D307/91 , C07D317/58 , C07D333/20 , C07D333/34 , C07D409/04 , C07D409/14 , C07C211/09 , A61K31/135
CPC分类号： C07D213/73 , A61K45/06 , C07C211/27 , C07C211/29 , C07C211/30 , C07C211/31 , C07C211/49 , C07C211/50 , C07C211/54 , C07C217/40 , C07C217/58 , C07C223/02 , C07C233/37 , C07C233/40 , C07C233/62 , C07C237/10 , C07C247/16 , C07C255/58 , C07C279/12 , C07C291/02 , C07C311/19 , C07C311/39 , C07C317/44 , C07C2601/02 , C07C2603/18 , C07C2603/24 , C07C2603/50 , C07C2603/74 , C07D207/16 , C07D209/18 , C07D213/38 , C07D215/42 , C07D233/42 , C07D277/28 , C07D285/10 , C07D307/91 , C07D333/20 , C07D333/34 , C07D409/14
摘要： Cytotoxic polyamine analogues are provided that are useful for treating diseases where it is desired to inhibit cell growth and/or proliferation, for example cancer and post-angioplasty injury.
摘要翻译：提供了细胞毒性多胺类似物，其可用于治疗期望抑制细胞生长和/或增殖的疾病，例如癌症和血管成形术后损伤。

10. 发明申请

US20030153788A1 Epoxycarboxamide compound, azide compound, and amino alcohol compound, and process for preparing alpha-keto amide compound using them 失效
标题翻译：环氧甲酰胺化合物，叠氮化合物和氨基醇化合物，以及使用它们制备α-酮酰胺化合物的方法
公开(公告)号：US20030153788A1
公开(公告)日：2003-08-14
申请号：US10331702
申请日：2002-12-30
申请人： Seikagaku Corporation
发明人： Nobuo Kobayashi , Tsuneo Koji , Takashi Fujita , Tomofumi Nishimura , Akihiko Hosoda
IPC分类号： C07C237/34 , C07C237/04 , C07C247/04 , C07C247/06 , C07D303/36
CPC分类号： C07D295/215 , C07C231/12 , C07C231/16 , C07C237/22 , C07C247/12 , C07C271/22 , C07C2601/14 , C07D207/16 , C07D295/18 , C07D303/46 , C07D303/48 , C07D317/66 , C07D405/12 , C07D407/12 , C07D413/12
摘要： The present invention is to provide manufacturing intermediates which can be led to useful null-ketoamide compounds having protease-inhibiting activity extremely economically and stereoselectively, and to provide epoxycarboxamide compounds, azide compounds and amino alcohol compounds represented by the following formulae: 1 wherein R1 and R2 each represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R3 represents alkyl group, alkenyl group, aromatic hydrocarbon group, heterocyclic group, R6nullOnull or R7nullN(R8)null; where R6 represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R7 and R8 each represents hydrogen atom, alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group, and, R4 and R5 represent the same groups as R7 and R8, respectively, and R4 and R5 optionally form a ring together; and X represents nullOnull or nullN(R9)null, where R9 represents hydrogen atom or alkyl group, and X optionally forms a ring together with R4 or R5, and processes for preparing null-keto amide compound using the same.
摘要翻译：本发明提供制造中间体，其可以经济地和立体选择性地被引入具有蛋白酶抑制活性的有用的α-酮酰胺化合物，并提供由下式表示的环氧羧酰胺化合物，叠氮化合物和氨基醇化合物：其中R1和R2 各自表示烷基，烯基，芳族烃基或杂环基; R3代表烷基，烯基，芳族烃基，杂环基，R6-O-或R7-N（R8） - ; 其中R 6表示烷基，烯基，芳族烃基或杂环基; R 7和R 8各自表示氢原子，烷基，烯基，芳族烃基或杂环基，R 4和R 5分别表示与R 7和R 8相同的基团，R 4和R 5任选地形成环; 并且X表示-O-或-N（R 9） - ，其中R 9表示氢原子或烷基，X任选地与R 4或R 5一起形成环，以及使用其制备α-酮酰胺化合物的方法。

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