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31. 发明授权

US09981887B1 Synthesis of phenylethynylbenzenes 有权
公开(公告)号：US09981887B1
公开(公告)日：2018-05-29
申请号：US15867009
申请日：2018-01-10
申请人： The United States of America, as represented by the Secretary of the Navy
发明人： Matthew Laskoski , Teddy M. Keller
IPC分类号： C07C2/86 , C07C37/62 , C07C303/28
CPC分类号： C07C2/868 , C07C37/62 , C07C303/28 , C07C2523/44 , C07C2523/72 , C07C2531/22 , C07C2531/24 , C07C39/245 , C07C15/54 , C07C309/66
摘要： A method of: reacting a dihydroxybenzene with bromine to form a bromodihydroxybenzene; reacting the bromodihydroxybenzene with trifluoromethanesulfonyl chloride or trifluoromethanesulfonic anhydride to form a bromotrifluoromethanesulfonatobenzene; and reacting the bromotrifluoromethanesulfonatobenzene with phenylacetylene to form a phenylethynylbenzene.

32. 发明授权

US09458174B2 Inhibitors of the activity of complex (III) of the mitochondrial electron transport chain and use thereof 有权
标题翻译：线粒体电子传递链复合物（III）的活性抑制剂及其用途
公开(公告)号：US09458174B2
公开(公告)日：2016-10-04
申请号：US14401685
申请日：2013-05-23
申请人： STEMERGIE BIOTECHNOLOGY SA
发明人： Virginie Clement-Schatlo , Thomas Fessard , Damien Barbaras , Joana Matos , Erick Carreira
IPC分类号： A61K31/41 , C07D495/10 , C07D213/81 , C07D215/28 , C07C275/42 , C07C39/30 , C07D231/56 , C07C311/08 , C07D235/26 , C07D405/12 , C07C215/50 , C07D249/06 , C07C233/25 , C07D263/32 , C07D263/34 , C07D487/10 , C07C237/38 , C07C237/42 , C07C251/48 , C07D209/42 , C07D305/06 , C07C49/825 , C07D403/12 , C07D223/28 , C07D235/18 , C07C233/33 , C07D261/08 , C07C235/60 , C07C235/62 , C07D263/57 , C07D491/107 , C07C237/40 , C07C237/44 , C07D277/56 , C07D513/10 , C07D305/08 , A01N31/08 , A01N33/10 , A01N35/04 , A01N37/24 , A01N37/40 , A01N37/44 , A01N37/46 , A01N37/50 , A01N43/20 , A01N43/38 , A01N43/40 , A01N43/42 , A01N43/46 , A01N43/52 , A01N43/56 , A01N43/60 , A01N43/647 , A01N43/76 , A01N43/78 , A01N43/80 , A01N43/90 , A01N47/30 , C07C39/24 , C07C43/178 , C07C49/245 , A61K31/137 , A61K31/167 , A61K31/17 , A61K31/18 , A61K31/397 , A61K31/421 , A61K31/44 , A61K31/47 , A61K31/55 , A61K45/06 , C07D223/24
CPC分类号： C07D495/10 , A01N31/08 , A01N33/10 , A01N35/04 , A01N37/24 , A01N37/40 , A01N37/44 , A01N37/46 , A01N37/50 , A01N43/20 , A01N43/38 , A01N43/40 , A01N43/42 , A01N43/46 , A01N43/52 , A01N43/56 , A01N43/60 , A01N43/647 , A01N43/76 , A01N43/78 , A01N43/80 , A01N43/90 , A01N47/30 , A61K31/137 , A61K31/167 , A61K31/17 , A61K31/18 , A61K31/397 , A61K31/421 , A61K31/44 , A61K31/47 , A61K31/55 , A61K45/06 , C07C39/245 , C07C39/30 , C07C43/1787 , C07C49/245 , C07C49/825 , C07C215/50 , C07C233/25 , C07C233/33 , C07C235/60 , C07C235/62 , C07C237/38 , C07C237/40 , C07C237/42 , C07C237/44 , C07C251/48 , C07C275/42 , C07C311/08 , C07C2601/04 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2602/42 , C07C2603/74 , C07D209/42 , C07D213/81 , C07D215/28 , C07D223/24 , C07D223/28 , C07D231/56 , C07D235/18 , C07D235/26 , C07D249/06 , C07D261/08 , C07D263/32 , C07D263/34 , C07D263/57 , C07D277/56 , C07D305/06 , C07D305/08 , C07D403/12 , C07D405/12 , C07D487/10 , C07D491/107 , C07D513/10
摘要： The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumor-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.
摘要翻译：本发明涉及线粒体电子传递链的复合体（III）的活性抑制剂及其在治疗和/或预防呈递肿瘤起始细胞的癌症中的用途。本发明还涉及单独或与其它药物活性剂组合含有所述抑制剂的药物组合物，以及它们作为药物或作为农药的用途，其中其作为线粒体呼吸抑制剂的性质是有益的。

33. 发明申请

US20150148301A1 INHIBITORS OF THE ACTIVITY OF COMPLEX (III) OF THE MITOCHONDRIAL ELECTRON TRANSPORT CHAIN AND USE THEREOF 有权
标题翻译：咪唑电子传输链复合物（III）的活性抑制剂及其用途
公开(公告)号：US20150148301A1
公开(公告)日：2015-05-28
申请号：US14401685
申请日：2013-05-23
申请人： STEMERGIE BIOTECHNOLOGY SA
发明人： Virginie Clement-Schatlo , Thomas Fessard , Damien Barbaras , Joana Matos , Erick Carreira
IPC分类号： C07D495/10 , A61K31/167 , A61K45/06 , C07D213/81 , A61K31/44 , C07D215/28 , A61K31/47 , C07C311/08 , A61K31/18 , C07C275/42 , A61K31/17 , C07C215/50 , A61K31/137 , C07D263/34 , A61K31/421 , C07D223/24 , A61K31/55 , A61K31/397 , C07C237/44
CPC分类号： C07D495/10 , A01N31/08 , A01N33/10 , A01N35/04 , A01N37/24 , A01N37/40 , A01N37/44 , A01N37/46 , A01N37/50 , A01N43/20 , A01N43/38 , A01N43/40 , A01N43/42 , A01N43/46 , A01N43/52 , A01N43/56 , A01N43/60 , A01N43/647 , A01N43/76 , A01N43/78 , A01N43/80 , A01N43/90 , A01N47/30 , A61K31/137 , A61K31/167 , A61K31/17 , A61K31/18 , A61K31/397 , A61K31/421 , A61K31/44 , A61K31/47 , A61K31/55 , A61K45/06 , C07C39/245 , C07C39/30 , C07C43/1787 , C07C49/245 , C07C49/825 , C07C215/50 , C07C233/25 , C07C233/33 , C07C235/60 , C07C235/62 , C07C237/38 , C07C237/40 , C07C237/42 , C07C237/44 , C07C251/48 , C07C275/42 , C07C311/08 , C07C2601/04 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2602/42 , C07C2603/74 , C07D209/42 , C07D213/81 , C07D215/28 , C07D223/24 , C07D223/28 , C07D231/56 , C07D235/18 , C07D235/26 , C07D249/06 , C07D261/08 , C07D263/32 , C07D263/34 , C07D263/57 , C07D277/56 , C07D305/06 , C07D305/08 , C07D403/12 , C07D405/12 , C07D487/10 , C07D491/107 , C07D513/10
摘要： The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.
摘要翻译：本发明涉及线粒体电子传递链的复合体（III）的活性抑制剂及其在治疗和/或预防呈递肿瘤起始细胞的癌症中的用途。本发明还涉及单独或与其它药物活性剂组合含有所述抑制剂的药物组合物，以及它们作为药物或作为其作为线粒体呼吸抑制剂的性质有益的农药的用途。

34. 发明申请

US20140066497A1 TREATMENT OF IMMUNE DYSREGULATION USING CANNABINOID DERIVATIVES 有权
标题翻译：使用CANNABINOID衍生物治疗免疫调节
公开(公告)号：US20140066497A1
公开(公告)日：2014-03-06
申请号：US14010729
申请日：2013-08-27
申请人： Immugen Pharmaceuticals, Inc.
发明人： Craig TRAVIS
IPC分类号： A61K31/352
CPC分类号： A61K31/352 , A61K31/05 , A61K31/09 , A61K31/353 , C07C39/08 , C07C39/10 , C07C39/19 , C07C39/245 , C07C43/23 , C07F9/12
摘要： This invention discloses cannabinoid derivatives and pharmaceutical uses thereof.
摘要翻译：本发明公开了大麻素衍生物及其药物用途。

35. 发明授权

US07956222B2 Methods for producing dibromofluorobenzene derivatives 失效
标题翻译：二溴氟苯衍生物的制备方法
公开(公告)号：US07956222B2
公开(公告)日：2011-06-07
申请号：US11573882
申请日：2005-07-27
申请人： Seiji Yoshikawa
发明人： Seiji Yoshikawa
IPC分类号： C07C41/22
CPC分类号： C07C41/16 , C07C37/56 , C07C39/245 , C07C41/22 , C07C43/225 , C07C45/562 , C07C47/565
摘要： Methods of the present invention for producing dibromofluorobenzene derivatives (compounds II) comprise Step 1, in which compounds (I) having the following general formula (I): (wherein, R1 and R2 each independently represent a C1-6 alkyl group) are reacted in a solvent with a brominating reagent.
摘要翻译：用于制备二溴氟苯衍生物（化合物II）的方法包括步骤1，其中具有以下通式（I）的化合物（I）：（其中，R 1和R 2各自独立地表示C 1-6烷基）反应在具有溴化试剂的溶剂中。

36. 发明申请

US20100286451A1 Process for producing 1,2-dialkoxy-3-fluorobenzene 失效
标题翻译： 1,2-二烷氧基-3-氟苯的制备方法
公开(公告)号：US20100286451A1
公开(公告)日：2010-11-11
申请号：US12805138
申请日：2010-07-14
申请人： Mingjian Qiu , Wei Zhang , Zhaohui Chen , Chunshan Zhang , Yali Zhang
发明人： Mingjian Qiu , Wei Zhang , Zhaohui Chen , Chunshan Zhang , Yali Zhang
IPC分类号： C07C41/01 , C07C43/23
CPC分类号： C07C41/16 , C07C37/00 , C07C37/02 , C07C41/01 , C07C41/26 , C07C43/23 , C07C39/27 , C07C43/225 , C07C39/245
摘要： The present invention relates to a process for producing a 2-fluoro-6-halophenol as an intermediate; a process for producing a 2-alkoxy-3-fluorophenol and further a 1,2-dialkoxy-3-fluorobenzene from the 2-fluoro-6-halophenol; a second process for producing a 1,2-dialkoxy-3-fluorobenzene from the 2-fluoro-6-halophenol; and a 2-alkoxy-3-fluorophenol. The 2-fluoro-6-halophenol can be obtained using a 2-fluorophenol as a starting material and through a sulfonation reaction, a halogenation reaction, and a deprotection reaction. The 2-fluoro-6-halophenol is alkyl-etherified, and subsequently the halogen atom is converted into a hydroxyl group to obtain the 2-alkoxy-3-fluorophenol, which is further alkyl-etherified to thereby obtain the 1,2-dialkoxy-3-fluorobenzene. Alternatively, a 1,2-dialkoxy-3-fluorobenzene is also obtained by converting the halogen atom of the 2-fluoro-6-halophenol into a hydroxyl group to thereby form 3-fluorocatechol and subsequently alkyl-etherifying two hydroxyl groups thereof. The processes of the invention realize low production costs and high process yields, and thus are suitable for industrial production of a 1,2-dialkoxy-3-fluorobenzene.
摘要翻译：本发明涉及作为中间体的2-氟-6-卤代苯酚的制造方法。从2-氟-6-卤苯酚制备2-烷氧基-3-氟苯酚和1,2-二烷氧基-3-氟苯的方法; 从2-氟-6-卤代苯酚制备1,2-二烷氧基-3-氟苯的第二种方法; 和2-烷氧基-3-氟苯酚。 2-氟-6-卤代苯酚可以使用2-氟苯酚作为原料，通过磺化反应，卤化反应和脱保护反应得到。 2-氟-6-卤代苯酚被烷基醚化，随后将卤素原子转化为羟基，得到2-烷氧基-3-氟苯酚，进一步进行烷基醚化，从而得到1,2-二烷氧基 -3-氟苯。或者，也可以通过将2-氟-6-卤代苯酚的卤素原子转化为羟基，从而形成3-氟邻苯二酚，然后将其两个羟基烷基醚化，得到1,2-二烷氧基-3-氟苯。本发明的方法实现了低生产成本和高工艺产率，因此适用于1,2-二烷氧基-3-氟苯的工业生产。

37. 发明申请

US20100222436A1 REDOX-ACTIVE THERAPEUTICS FOR TREATMENT OF MITOCHONDRIAL DISEASES AND OTHER CONDITIONS AND MODULATION OF ENERGY BIOMARKERS 审中-公开
标题翻译：用于治疗麻醉病毒及其他条件的REDOX活性治疗剂和能量生物标志物的调节
公开(公告)号：US20100222436A1
公开(公告)日：2010-09-02
申请号：US12777179
申请日：2010-05-10
申请人： Guy M. Miller , Sidney M. Hecht
发明人： Guy M. Miller , Sidney M. Hecht
IPC分类号： A61K31/122 , A61P3/10 , A61P25/00 , A61P35/00
CPC分类号： C07C37/07 , A61K31/355 , C07C39/08 , C07C39/19 , C07C39/24 , C07C39/245 , C07C46/00 , C07C46/02 , C07C46/08 , C07C50/02 , C07C50/06 , C07C50/28 , C07C50/24 , C07C39/11 , C07C39/04
摘要： Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, stroke (MELAS), or Kearns-Sayre Syndrome (KSS) are disclosed, as well as compounds useful in the methods of the invention, such as alpha-tocopherol quinone. Methods and compounds useful in treating other disorders are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.
摘要翻译：公开了治疗或抑制线粒体疾病如弗里德里希共济失调（FRDA），莱伯氏遗传性视神经病变（LHON），线粒体肌病，脑病，乳酸脱落症，中风（MELAS）或Kearns-Sayre综合征（KSS）的方法，以及可用于本发明方法的化合物，例如α-生育酚醌。还公开了可用于治疗其它疾病的方法和化合物。还公开了可用于评估受试者的代谢状态和治疗功效的能量生物标志物。还公开了调节，归一化或增强能量生物标志物的方法以及可用于这些方法的化合物。

38. 发明申请

US20080045753A1 Methods For Producing Dibromofluorobenzene Derivatives 失效
标题翻译：生产二溴氟苯衍生物的方法
公开(公告)号：US20080045753A1
公开(公告)日：2008-02-21
申请号：US11573882
申请日：2005-07-27
申请人： Seiji Yoshikawa
发明人： Seiji Yoshikawa
IPC分类号： C07C39/08 , C07C41/22
CPC分类号： C07C41/16 , C07C37/56 , C07C39/245 , C07C41/22 , C07C43/225 , C07C45/562 , C07C47/565
摘要： Disclosed is a method for producing a dibromofluorobenzene derivative (compound II) comprising a step 1 wherein a compound (I) represented by the general formula (I) below is reacted with a brominating agent in a solvent. (I) (II) (In the formulae, R1 and R2 independently represent a C1-6 alkyl group.)
摘要翻译：公开了一种制备二溴氟苯衍生物（化合物II）的方法，其包括步骤1，其中由下述通式（I）表示的化合物（I）与溴化剂在溶剂中反应。（I）（II）（式中，R 1和R 2独立地表示C 1-6烷基。）

39. 发明申请

US20040030197A1 Process for the synthesis of phenols from arenes 有权
公开(公告)号：US20040030197A1
公开(公告)日：2004-02-12
申请号：US10620122
申请日：2003-07-15
申请人： Board of Trustees of Michigan State University
发明人： Robert E. Maleczka JR. , Milton R. Smith III , Daniel Holmes , Feng Shi
IPC分类号： C07C037/00
CPC分类号： C07D213/68 , C07B41/02 , C07C37/50 , C07C41/26 , C07C67/31 , C07C213/00 , C07C69/88 , C07C69/92 , C07C215/76 , C07C39/27 , C07C43/23 , C07C39/28 , C07C39/245 , C07C39/32 , C07C39/07 , C07C39/24 , C07C39/30 , C07C69/84
摘要： A process to synthesize substituted phenols such as those of the general formula RRnullRnullAr(OH) wherein R, Rnull, and Rnull are each independently hydrogen or any group which does not interfere in the process for synthesizing the substituted phenol including, but not limited to, halo, alkyl, alkoxy, carboxylic ester, amine, amide; and Ar is any variety of aryl or hetroaryl by means of oxidation of substituted arylboronic esters is described. In particular, a metal-catalyzed CnullH activation/borylation reaction is described, which when followed by direct oxidation in a single or separate reaction vessel affords phenols without the need for any intermediate manipulations. More particularly, a process wherein Ir-catalyzed borylation of arenes using pinacolborane (HBPin) followed by oxidation of the intermediate arylboronic ester by OXONE is described.

40. 发明申请

US20030158191A1 Cannabinol derivatives 失效
标题翻译：大麻酚衍生物
公开(公告)号：US20030158191A1
公开(公告)日：2003-08-21
申请号：US10328242
申请日：2002-12-22
发明人： Craig R. Travis
IPC分类号： A61K031/5377 , A61K031/473 , A61K031/382 , A61K031/353 , C07D417/02 , C07D413/02
CPC分类号： A61K31/352 , A61K31/05 , A61K31/09 , A61K31/353 , C07C39/08 , C07C39/10 , C07C39/19 , C07C39/245 , C07C43/23 , C07F9/12
摘要： The invention provides cannabinol derivatives and pharmaceutical preparations thereof.
摘要翻译：本发明提供大麻酚衍生物及其药物制剂

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