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1. 发明授权

US10913728B2 O-substituted hydroxamic acids 有权
公开(公告)号：US10913728B2
公开(公告)日：2021-02-09
申请号：US16321378
申请日：2017-07-27
申请人： The Johns Hopkins University , John P. Toscano , Saghar Nourian , Daryl A. Guthrie
发明人： John P. Toscano , Saghar Nourian , Daryl A. Guthrie
IPC分类号： C07D311/56 , C07D239/62 , C07D231/28 , A61P9/10
摘要： O-substituted hydroxamic acids with carbon-based leaving groups as HNO donors are disclosed. Pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions also are disclosed.

2. 发明申请

US20200024246A1 POGOSTONE DERIVATIVES AND METHODS OF USING THE SAME 审中-公开
公开(公告)号：US20200024246A1
公开(公告)日：2020-01-23
申请号：US16518550
申请日：2019-07-22
申请人： Hamyard Associates LLC
发明人： George A. Kraus , Joel R. Coats , Edmund J. Norris
IPC分类号： C07D309/38 , C07D493/04 , C07D215/20 , C07C49/788 , C07C49/248 , C07D311/56 , C07D407/06 , C07C49/203 , C07D233/96 , C07D413/06 , A01N43/80 , A01N43/50 , A01N43/16 , A01N31/16 , A01N43/28
摘要： Described are novel derivatives of pogostone and methods of using the same.

3. 发明申请

US20180362489A1 COMPOSITION AND RODENTICIDAL BAIT COMPRISING FLOCOUMAFEN, AND PROCESS FOR CONTROLLING TARGET RODENT PESTS 审中-公开
公开(公告)号：US20180362489A1
公开(公告)日：2018-12-20
申请号：US16061115
申请日：2016-12-06
申请人： LIPHATECH , INSTITUT ENSEIGNEMENT SUPERIEUR ET RECHERCHE EN ALIMENTATION SANTE ANIMALE SCIENCES AGRONOMIQUES E
发明人： Hervé CARUEL , Etienne BENOIT , Isabelle FOUREL , Virginie LATTARD
IPC分类号： C07D311/56 , A01N43/16 , A01N25/00
摘要： Disclosed is a composition including flocoumafen and an amount of a configurational stereoisomer of flocoumafen, named enantiomer E4, such that the ratio of this amount to the amount of flocoumafen in the composition is less than 10%, the enantiomer E4 being present with the exclusion of a racemic mixture, the enantiomer E4 having, by chromatographic analysis of flocoumafen, a retention time t4 having a value such that t1

4. 发明申请

US20180362488A1 STEREOISOMER OF FLOCOUMAFEN, COMPOSITION AND RODENTICIDE BAIT COMPRISING SAME, AND METHOD FOR CONTROLLING TARGET RODENT PESTS 审中-公开
公开(公告)号：US20180362488A1
公开(公告)日：2018-12-20
申请号：US16061092
申请日：2016-12-06
申请人： LIPHATECH , INSTITUT ENSEIGNEMENT SUPERIEUR ET RECHERCHE EN ALIMENTATION SANTE ANIMALE SCIENCES AGRONOMIQUES
发明人： Hervé CARUEL , Etienne BENOIT , Isabelle FOUREL , Virginie LATTARD
IPC分类号： C07D311/56 , A01N43/16 , A01N25/00
摘要： Disclosed is a configurational stereoisomer, referred to as enantiomer E2, of flocoumafen, the enantiomer E2 having, as determined by the chromatographic analysis of a flocoumafen composition including four configurational stereoisomers of flocoumafen, carried out under conditions described hereinafter, a retention time t2 with a value such that t1

5. 发明申请

US20150274755A1 COMPOUND DIVERSIFICATION USING LATE STAGE FUNCTIONALIZATION 审中-公开
标题翻译：使用最后阶段功能化的化合物多样化
公开(公告)号：US20150274755A1
公开(公告)日：2015-10-01
申请号：US14431134
申请日：2013-09-20
申请人： Shane W. KRSKA , Petr VACHAL , Christopher J. WELCH , Graham F. SMITH , MERCK SHARP & DOHME CORP.
发明人： Shane W. Krska , Petr Vachal , Christopher J. Welch , Graham F. Smith
IPC分类号： C07F5/02 , C07D311/56
CPC分类号： C07C17/10 , C07C17/013 , C07D311/56 , C07F5/025 , C40B40/04 , C40B50/08
摘要： The present invention relates to methods for generating limited chemical diversity for biologically relevant lead molecules by late state functionalization, separation, and post-functionalization modification. The methods optionally include one or more screening steps. Traditional drug development has relied on the synthesis of individual compounds or the generation of large chemical libraries, but these methods have generally been fairly inefficient in obtaining drug products.
摘要翻译：本发明涉及通过后期官能化，分离和后官能化修饰产生生物相关铅分子的有限化学多样性的方法。方法可选地包括一个或多个筛选步骤。传统药物开发依赖于单个化合物的合成或大量化学文库的产生，但这些方法在获得药物产品方面通常相当低效。

6. 发明申请

US20130143957A1 POLYMORPHIC FORMS OF WARFARIN POTASSIUM AND PREPARATIONS THEREOF 失效
标题翻译：多形态多糖形式及其制备方法
公开(公告)号：US20130143957A1
公开(公告)日：2013-06-06
申请号：US13699293
申请日：2011-05-20
申请人： Prabhudas Bodhuri , Gamini Weeratunga , Keshava K.S. Murthy
发明人： Prabhudas Bodhuri , Gamini Weeratunga , Keshava K.S. Murthy
IPC分类号： A61K31/365 , C07D311/56 , C07D311/06
CPC分类号： C07D311/56
摘要： There is provided crystalline solvate forms of Warfarin potassium, termed APO-I and APO-II, and processes for making APO-I and APO-II. APO-I and APO-II are polymorphic solvate forms of Warfarin potassium.
摘要翻译：提供了称为APO-1和APO-II的华法林钾的结晶溶剂化物形式，以及制备APO-1和APO-II的方法。 APO-I和APO-II是华法林钾的多晶型溶剂合物形式。

7. 发明授权

US07932405B2 Halogenated ester derivatives of coumarins for the treatment of coagulation disorders 有权
标题翻译：香豆素的卤代酯衍生物用于治疗凝血障碍
公开(公告)号：US07932405B2
公开(公告)日：2011-04-26
申请号：US12268109
申请日：2008-11-10
申请人： Pascal Druzgala , Cyrus Becker
发明人： Pascal Druzgala , Cyrus Becker
IPC分类号： C07D311/56 , A61K31/352
CPC分类号： C07D311/56
摘要： The subject invention provides anticoagulant compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R3, n and Ar are as defined herein. The compounds of the subject invention can be used to treat at-risk populations thereby bringing relief of symptoms, improving the quality of life, preventing acute and long-term complications, reducing mortality and treating accompanying disorders. The invention further comprises pharmaceutical compositions comprising the compounds and salts of the invention, as well as methods of using the compounds, salts, and compositions of the invention.
摘要翻译：本发明提供了式I的抗凝血剂化合物及其药学上可接受的盐，其中R 1，R 3，n和Ar如本文所定义。本发明的化合物可用于治疗危险人群，从而缓解症状，改善生活质量，预防急性和长期并发症，降低死亡率和治疗伴随的疾病。本发明还包括包含本发明化合物和盐的药物组合物，以及使用本发明化合物，盐和组合物的方法。

8. 发明申请

US20050143588A1 Production of isoflavone derivatives 审中-公开
标题翻译：异黄酮衍生物的生产
公开(公告)号：US20050143588A1
公开(公告)日：2005-06-30
申请号：US10851270
申请日：2004-05-20
申请人： Andrew Heaton , Naresh Kumar
发明人： Andrew Heaton , Naresh Kumar
IPC分类号： C07B61/00 , C07D311/36 , C07D311/38 , C07D311/56 , C07D311/58 , C07D311/74
CPC分类号： C07D311/56 , C07D311/36 , C07D311/38
摘要： Methods for the hydrogenation of isoflavones are described which provide access to workable quantities of isoflavan-4-ols, isoflav-3-enes, and isoflavans. The isoflavone derivatives can be obtained in high purity and in near quantitative yields whilst employing pharmaceutically acceptable reagents and solvents.
摘要翻译：描述了异黄酮氢化方法，其提供了可使用量的异黄烷-4-醇，异氟烷-3-烯和异构体。异黄酮衍生物可以以高纯度和接近定量的产率获得，同时使用药学上可接受的试剂和溶剂。

9. 发明授权

US06897220B2 Inhibitors of histone deacetylase 有权
标题翻译：组蛋白脱乙酰酶抑制剂
公开(公告)号：US06897220B2
公开(公告)日：2005-05-24
申请号：US10358556
申请日：2003-02-04
申请人： Daniel Delorme , Zhihong Zhou
发明人： Daniel Delorme , Zhihong Zhou
IPC分类号： A61K31/4015 , A61K31/445 , A61K31/495 , A61K31/513 , A61K31/53 , A61K31/537 , A61P35/00 , C07C233/44 , C07C233/80 , C07C235/38 , C07C235/42 , C07C235/56 , C07C235/84 , C07C237/20 , C07C237/22 , C07C237/40 , C07C237/42 , C07C255/58 , C07C255/59 , C07C275/34 , C07C275/36 , C07C311/42 , C07C323/32 , C07C323/36 , C07C323/44 , C07C323/60 , C07C381/00 , C07D213/30 , C07D213/74 , C07D233/54 , C07D239/91 , C07D251/18 , C07D251/52 , C07D251/54 , C07D263/14 , C07D263/24 , C07D265/36 , C07D271/06 , C07D277/42 , C07D277/74 , C07D277/82 , C07D295/155 , C07D307/12 , C07D307/28 , C07D311/56 , C07D311/58 , C07D333/36 , C07D333/38 , C07D401/04 , C07D401/12 , C07D403/04 , C07D409/12 , C07D473/40 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D521/00 , C07F7/08 , C07D239/42 , A61K31/506
CPC分类号： C07D401/04 , A61K31/4015 , A61K31/445 , A61K31/495 , A61K31/513 , A61K31/53 , A61K31/537 , C07C233/44 , C07C233/80 , C07C235/38 , C07C235/42 , C07C235/56 , C07C235/84 , C07C237/20 , C07C237/22 , C07C237/40 , C07C237/42 , C07C255/58 , C07C255/59 , C07C275/34 , C07C275/36 , C07C311/42 , C07C323/32 , C07C323/36 , C07C323/44 , C07C323/60 , C07C381/00 , C07D213/30 , C07D213/74 , C07D231/12 , C07D233/56 , C07D233/64 , C07D239/91 , C07D249/08 , C07D251/18 , C07D251/52 , C07D251/54 , C07D263/14 , C07D263/24 , C07D265/36 , C07D271/06 , C07D277/42 , C07D277/74 , C07D277/82 , C07D295/155 , C07D307/12 , C07D307/28 , C07D311/56 , C07D311/58 , C07D333/36 , C07D333/38 , C07D401/12 , C07D403/04 , C07D409/12 , C07D473/40 , C07D487/04 , C07D495/04 , C07D513/04 , C07F7/081 , C07F7/0812
摘要： The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
摘要翻译：本发明涉及抑制组蛋白脱乙酰酶。本发明提供了抑制组蛋白脱乙酰酶酶活性的化合物和方法。本发明还提供了治疗细胞增殖性疾病和病症的组合物和方法。

10. 发明授权

US5686631A Asymmetric synthesis of R and S warfarin and its analogs 失效
标题翻译： R和S华法林及其类似物的不对称合成
公开(公告)号：US5686631A
公开(公告)日：1997-11-11
申请号：US678211
申请日：1996-07-11
申请人： Hui-Yin Li , Andrea Jane Robinson
发明人： Hui-Yin Li , Andrea Jane Robinson
IPC分类号： C07D20060101 , C07D311/56 , C07D311/02
CPC分类号： C07D311/56
摘要： The present invention provides a novel process for making compounds of formula 2a or 2b or pharmaceutically acceptable salts thereof, ##STR1## wherein R1 is selected from the group consisting of phenyl and phenyl substituted with at least one group selected from NO.sub.2 and halogen; R.sub.2 is H; R.sub.3 is selected from the group consisting of C.sub.1-4 alkyl, phenyl, and benzyl; and, R.sub.4 is selected from the group consisting of H and halogen; which comprises the steps of: a) oxidizing a racemate of formula 2 or a salt thereof to form a dehydro-compound of formula 3, ##STR2## wherein R.sub.5 is selected from the group consisting of H, CH.sub.3, benzyl, C.sub.2-8 acyl Na, Li and K; and, b) asymmetrically hydrogenating a compound of formula 3 in the presence of a chiral phosphine catalyst to form a compound of formula 2a or 2b.
摘要翻译：本发明提供制备式2a或2b化合物或其药学上可接受的盐的新方法，其中R 1选自苯基和至少被取代的苯基一个选自NO2和卤素的基团; R2为H; R 3选自C 1-4烷基，苯基和苄基; 并且R 4选自H和卤素; 其包括以下步骤：a）氧化式2的外消旋物或其盐以形成式3的脱氢化合物，其中H，CH 3，苄基，C 2-8酰基Na，Li和K ; 和b）在手性膦催化剂的存在下不对称地氢化式3的化合物以形成式2a或2b的化合物。

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