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1. 发明申请

US20180194740A1 DEOXYURIDINE TRIPHOSPHATASE INHIBITORS CONTAINING AMINO SULFONYL LINKAGE 审中-公开
公开(公告)号：US20180194740A1
公开(公告)日：2018-07-12
申请号：US15740787
申请日：2016-07-07
申请人： University of Southern California , CV6 Therapeutics (NI) Limited
发明人： Robert D. Ladner , Mark Spyvee , Pravin S. Shirude
IPC分类号： C07D241/08 , C07D239/22 , C07D233/74 , C07D213/74 , C07D211/88 , C07D207/416 , A61P35/02
CPC分类号： C07D241/08 , A61P35/02 , C07D207/40 , C07D207/416 , C07D211/88 , C07D213/74 , C07D233/74 , C07D239/22
摘要： Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.

2. 发明申请

US20180186737A1 HYDANTOIN CONTAINING DEOXYURIDINE TRIPHOSPHATASE INHIBITORS 审中-公开
公开(公告)号：US20180186737A1
公开(公告)日：2018-07-05
申请号：US15741202
申请日：2016-07-07
申请人： CV6 Therapeutics (NI) Limited
发明人： Mark Spyvee , Pravin S. Shirude
IPC分类号： C07D207/40 , A61P35/00 , C07D401/12 , C07D403/12 , C07D405/12 , C07D487/04
CPC分类号： C07D233/74 , A61K31/4015 , A61P35/00 , C07D207/36 , C07D207/40 , C07D207/404 , C07D211/88 , C07D233/46 , C07D239/22 , C07D241/08 , C07D249/12 , C07D251/10 , C07D263/44 , C07D277/34 , C07D401/12 , C07D403/12 , C07D405/12 , C07D487/04 , C07F9/6506
摘要： Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.

3. 发明申请

US20170291876A1 ASYMMETRICALLY CATALYZED SYNTHESIS METHOD OF NITROPYRAZOLE AMIDE COMPOUND 审中-公开
公开(公告)号：US20170291876A1
公开(公告)日：2017-10-12
申请号：US15511243
申请日：2015-06-12
申请人： Zhejiang Jiuzhou Pharmaceutical Co., Ltd.
发明人： Xiaoming FENG , Qian YAO , Xiaohua LIU , Lili LIN , Yuheng ZHANG
IPC分类号： C07D231/12 , C07C201/12
CPC分类号： C07D211/88 , C07C201/12 , C07C205/53 , C07D207/267 , C07D231/12 , C07D231/16 , C07D405/06 , C07D409/06
摘要： A synthesis method of γ-nitropyrazole amide compound through asymmetrical catalyzing technique is provided, a nitroalkane and an α,β-unsaturated pyrazole amide are applied as the raw material, a complex formed by a chiral amine oxide with a rare earth metal compound is served as the catalyst, a 4 Å molecular sieve is served as an additive, the γ-nitropyrazole amide compound can be obtained with a yield more than 99% and enantiomeric excess more than 99% ee. The catalytic system not only has the advantages of simple operation, mild reaction conditions, requiring no acid/base additives, convenient product purification, high yield and enatioselectivity, compliance with green atomic economy, and promising prospects for industrial application, but also allows the obtained γ-nitropyrazole amide compound to undergo some simple chemical conversions to produce some molecules having physiological activities.

4. 发明申请

US20170137382A1 QUATERNARY HETEROATOM CONTAINING COMPOUNDS 审中-公开
公开(公告)号：US20170137382A1
公开(公告)日：2017-05-18
申请号：US15366590
申请日：2016-12-01
申请人： California Institute of Technology
发明人： Brian M. Stoltz , Scott C Virgil , David E. White , Taiga Yurino , Yiyang Liu , Douglas C. Behenna , Douglas Duquette , Christian Eidamshaus
IPC分类号： C07D211/78 , C07D207/277 , C07D207/27 , C07D265/32 , C07D211/90 , C07D211/76 , C07D211/96 , C07D223/10
CPC分类号： C07D211/78 , C07D207/06 , C07D207/08 , C07D207/10 , C07D207/16 , C07D207/26 , C07D207/263 , C07D207/267 , C07D207/27 , C07D207/273 , C07D207/277 , C07D207/46 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/34 , C07D211/38 , C07D211/60 , C07D211/76 , C07D211/88 , C07D211/90 , C07D211/94 , C07D211/96 , C07D223/04 , C07D223/10 , C07D241/04 , C07D241/08 , C07D241/52 , C07D265/30 , C07D265/32 , C07D309/04 , C07D309/30
摘要： The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): comprising treating a compound of Formula (I): with a transition metal catalyst and under alkylation conditions as valence and stability permit.

5. 发明申请

US20160039788A1 DEOXYURIDINE TRIPHOSPHATASE INHIBITORS 有权
标题翻译：脱氧胆碱磷酸酯酶抑制剂
公开(公告)号：US20160039788A1
公开(公告)日：2016-02-11
申请号：US14759386
申请日：2014-01-03
申请人： UNIVERSITY OF SOUTHERN CALIFORNIA
发明人： Robert D. Ladner , Bruno Giethlen
IPC分类号： C07D401/06 , C07D277/34 , C07D239/54 , C07D471/04 , C07D498/04 , C07D211/88 , C07D401/12
CPC分类号： C07D401/06 , C07D211/88 , C07D215/26 , C07D231/56 , C07D239/54 , C07D265/18 , C07D277/34 , C07D277/36 , C07D401/12 , C07D403/06 , C07D471/04 , C07D498/04
摘要： Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
摘要翻译：本文提供了dUTP酶抑制剂，包含这些化合物的组合物和使用这些化合物和组合物的方法。

6. 发明申请

US20150299124A1 SYNTHESIS OF UV ABSORBING COMPOUNDS 审中-公开
标题翻译：紫外吸收化合物的合成
公开(公告)号：US20150299124A1
公开(公告)日：2015-10-22
申请号：US14647610
申请日：2013-11-27
申请人： CORAL SUNSCREEN PTY LTD
发明人： MARK YORK , JOHN RYAN
IPC分类号： C07D211/88 , C07D211/74 , C07D211/86 , C07D211/70
CPC分类号： C07D211/88 , C07D211/70 , C07D211/74 , C07D211/86
摘要： A method of synthesis is provided to obtain a range of UV absorbing compounds. The method broadly involves (a) the reduction of a glutarimide or its reaction with a carbon nucleophile; (b) when step (a) is a reduction, exposing the product of step (a) to an acidic environment to form a cyclic amide; (c) reducing the product of step (a) or step (b) to form a corresponding enamine; and subjecting the enamine product of step (c) to an acylation.
摘要翻译：提供合成方法以获得一系列的UV吸收化合物。该方法广泛涉及（a）戊二酰亚胺的还原或其与碳亲核试剂的反应; （b）当步骤（a）为还原时，将步骤（a）的产物暴露于酸性环境以形成环状酰胺; （c）减少步骤（a）或步骤（b）的产物以形成相应的烯胺; 并使步骤（c）的烯胺产物进行酰化。

7. 发明申请

US20150157616A1 Novel Dihydropyridin-2(1H)-One Compounds as S-Nitrosoglutathione Reductase Inhibitors and Neurokinin-3 Receptor Antagonists 有权
标题翻译：新型二氢吡啶-2（1H） - S-亚硝基谷胱甘肽还原酶抑制剂和神经激肽-3受体拮抗剂的化合物
公开(公告)号：US20150157616A1
公开(公告)日：2015-06-11
申请号：US14598202
申请日：2015-01-15
申请人： N30 Pharmaceuticals, Inc.
发明人： Xicheng Sun , Jian Qiu
IPC分类号： A61K31/4412 , A61K31/4439 , A61K31/4436 , A61K31/444
CPC分类号： A61K31/4412 , A61K31/4436 , A61K31/4439 , A61K31/444 , C07D211/86 , C07D211/88 , C07D401/04 , C07D401/14 , C07D409/04 , C07D409/14
摘要： The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
摘要翻译：本发明涉及可用作S-亚硝基谷胱甘肽还原酶（GSNOR）抑制剂和/或神经激肽-3（NK3）受体拮抗剂的新型二氢吡啶-2（1H） - 酮化合物，包含这些化合物的药物组合物，以及制备和使用一样。

8. 发明授权

US08981128B2 Process for producing compounds comprising nitrile functions 有权
标题翻译：用于生产包含腈功能的化合物的方法
公开(公告)号：US08981128B2
公开(公告)日：2015-03-17
申请号：US14131453
申请日：2012-07-05
申请人： Philippe Marion , Roland Jacquot
发明人： Philippe Marion , Roland Jacquot
IPC分类号： C07D307/68 , C07D211/02 , C07D211/88 , C07D307/24 , C07D307/54
CPC分类号： C07D307/68 , C07D211/02 , C07D211/88 , C07D307/24 , C07D307/54
摘要： The present invention relates to the production of compounds comprising nitrile functions and of cyclic imide compounds. It relates more particularly to the production of compounds comprising nitrile functions from compounds comprising carboxylic functions, advantageously of natural and renewable origin, and from 2-methylglutaronitrile (MGN) or a mixture N of dinitriles comprising 2-methylglutaronitrile (MGN), 2-ethylsuccinonitrile (ESN) and adiponitrile (AdN).
摘要翻译：本发明涉及生产包含腈官能团和环状酰亚胺化合物的化合物。更具体地说，涉及包含腈功能的化合物的化合物的生产，所述化合物包含有机天然和可再生的羧基官能团，以及2-甲基戊二腈（MGN）或包含2-甲基戊二腈（MGN），2-乙基琥珀腈（ESN）和己二腈（AdN）。

9. 发明授权

US08586571B2 Heterocyclic compound 有权
标题翻译：杂环化合物
公开(公告)号：US08586571B2
公开(公告)日：2013-11-19
申请号：US12738486
申请日：2008-10-17
申请人： Shizuo Kasai , Tomohiro Kaku , Masahiro Kamaura
发明人： Shizuo Kasai , Tomohiro Kaku , Masahiro Kamaura
IPC分类号： C07D205/04 , C07D205/08 , C07D205/00 , C07D211/22 , C07D211/44 , C07D211/46 , C07D211/78 , C07D211/88 , C07D413/10 , C07D413/12 , C07D413/06 , C07D417/06 , C07D417/08 , C07D417/10 , C07D471/04 , C07D495/04 , C07D513/04 , C07D401/06 , A61K31/4427 , A61K31/397 , A61K31/445 , A61K31/40 , A61P3/10
CPC分类号： C07D417/04 , C07D205/04 , C07D207/08 , C07D207/12 , C07D211/22 , C07D211/44 , C07D211/46 , C07D211/78 , C07D211/88 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D413/04 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/08 , C07D417/10 , C07D471/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.
摘要翻译：本发明涉及其中每个符号如说明书中所定义的。本发明的化合物具有优异的RBP4降低作用，可用作预防或治疗由增加的RBP4介导的疾病和病症的药物。

10. 发明授权

US07514454B2 Piperidin-2,6-dione pamoate salts and their use for the treatment of stress-related affective disorders 失效
标题翻译：哌啶-2,6-二酮双羟萘酸盐及其用于治疗压力相关情感障碍的用途
公开(公告)号：US07514454B2
公开(公告)日：2009-04-07
申请号：US10524693
申请日：2003-08-18
申请人： Camille Georges Wermuth
发明人： Camille Georges Wermuth
IPC分类号： A61K31/451 , C07D211/88
CPC分类号： C07D211/88
摘要： Novel pamoate salts of certain 3-phenyl-3-dimethylaminoalkyl-4,4-dimethylpiperidin-2,6-diones and pharmacologically acceptable solvates thereof are devoid of the weight loss and hepatocyte changes in the rat which limited to marginally effective levels the permitted clinical doses of the corresponding hydrochlorides in the treatment or prophylaxis of stress-related affective disorders such as anxiety, depression, migraine and sleep apnoea. The preferred pamoate salts are 3(3,5-dimethoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione pamoate and, especially, 3(3-methoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione pamoate.
摘要翻译：某些3-苯基-3-二甲基氨基烷基-4,4-二甲基哌啶-2,6-二酮的新型双羟萘酸盐及其药理学上可接受的溶剂合物没有大鼠的体重减轻和肝细胞变化，其限于允许的临床上的边缘有效水平治疗或预防应激相关情感障碍如焦虑，抑郁，偏头痛和睡眠呼吸暂停的剂量相应的盐酸盐。优选的双羟萘酸盐是3（3,5-二甲氧基苯基）-3-（3-二甲基氨基丙基）-4,4-二甲基哌啶-2,6-二酮双羟萘酸盐，特别是3（3-甲氧基苯基）-3-（3- 二甲基氨基丙基）-4,4-二甲基哌啶-2,6-二酮双羟萘酸。

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