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1.发明授权公开(公告)号：US08586768B2
公开(公告)日：2013-11-19
申请号：US12945180
申请日：2010-11-12
IPC分类号： C07D311/58 , C07D311/70 , A61K31/352
CPC分类号： A61K31/352 , C07D311/58 , C07D493/04
摘要： A method of synthesizing rottlerin analogs is described. The synthesis methods described are the first known method of synthesizing rottlerin analogs from commercially-available materials to produce cost effective analogs. Rottlerin analog structures made by the synthesis methods and methods of use for treating a neurological or inflammatory response mediated by protein kinase C (PKC) are further described.
摘要翻译： 描述了合成罗德莱因类似物的方法。 所述的合成方法是从商业可得的材料合成罗腾霉素类似物以制备具有成本效益的类似物的第一种已知方法。 进一步描述通过用于治疗由蛋白激酶C（PKC）介导的神经或炎症反应的合成方法和方法制备的罗特勒林类似物结构。
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公开(公告)号：US5952311A
公开(公告)日：1999-09-14
申请号：US990576
申请日：1997-12-15
IPC分类号： C12N15/09 , A61K31/335 , A61K31/41 , A61K31/425 , A61K38/00 , A61K38/46 , A61K41/00 , A61K45/08 , A61K48/00 , A61P31/12 , C07D277/64 , C07D277/68 , C07D313/06 , C07D417/04 , C07H21/04 , C12N5/10 , C12N9/02 , A01N31/08 , A61K31/495 , C12N15/85
CPC分类号： C07D277/68 , A61K41/0019 , A61K41/0057 , C07D277/64 , C07D313/06 , C07D417/04 , C12N9/0069 , A01K2217/05 , A61K38/00 , A61K48/00 , C12N2799/027
摘要： Disclosed herein are compounds, compositions, and methods to inactivate a virus and destroy tumor cells. The methods involve the addition into the cell of a compound containing a photosensitizing chemical and an energy donating chemical, optionally linked by a chemical tether. Also introduced into the cell are means to chemically activate the energy donating chemical which photoactivates the photosensitizing chemical which then destroys the tumor or virus. The photosensitizing chemical is preferably hypericin, porphyrin, or an analog and the energy donating chemical is preferably luciferin or an analog. Methods for synthesizing the chemicals are also disclosed. Further, the energy donating chemical is activated by an activating chemical. The expression of the activating chemical is regulated so as to target the virus-infected or tumor cells. Regulating the activating chemical is accomplished by a number of methods including construction of an expression plasmid containing a gene encoding the activating chemical under control of a promoter which is transactivated by replication of the virus or transactivated by elevated levels of proteins expressed in tumor cells.
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3.发明授权
公开(公告)号：US4237057A
公开(公告)日：1980-12-02
申请号：US42314
申请日：1979-05-25
申请人： George A. Kraus
发明人： George A. Kraus
IPC分类号： C07D307/58 , C07D493/04
CPC分类号： C07D493/04 , C07D307/58 , Y02P20/55
摘要： An efficient synthesis of quinone pyrano-gamma-lactone antibiotics such as kalafungin and the new compound 9-deoxykalafungin in four basic steps from readily available starting materials. The key step in which all of the carbon atoms present in the target molecule are assembled is the addition of an alkoxy furan to a two position functionally substituted 1,4 naphthoquinone. This is followed by alkylating to provide protecting groups, hydride reduction, removal of the protecting groups, internal cyclization and by oxidative dealkylation to provide practical overall yields of the desired antibiotics.
摘要翻译： 醌类吡喃γ-内酯类抗生素如卡拉芬净和新化合物9-脱氧卡拉芬净在四个基本步骤中有效合成即可得到的起始原料。 存在于靶分子中的所有碳原子组装的关键步骤是将烷氧基呋喃加入到功能取代的1,4萘醌的两位上。 然后烷基化以提供保护基团，氢化物还原，去除保护基团，内部环化和通过氧化脱烷基化，以提供所需抗生素的实际总产率。
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公开(公告)号：US09000209B2
公开(公告)日：2015-04-07
申请号：US14234079
申请日：2012-06-21
申请人： George A. Kraus
发明人： George A. Kraus
IPC分类号： C07C67/313 , C07C51/377 , C07C67/317 , C07C67/343 , C07C51/367
CPC分类号： C07C67/317 , C07C51/367 , C07C51/377 , C07C67/313 , C07C67/343 , C07C2603/66 , C07C2603/86 , C07C69/80 , C07C69/76 , C07C63/04 , C07C63/331 , C07C65/24 , C07C65/21 , C07C63/49 , C07C69/612
摘要： A method of synthesis of para-substituted benzoate esters and acids is provided, wherein the para-substituted regioisomer is obtained substantially free of the meta-substituted impurity, the method comprising contacting a coumalate ester or acid and an unactivated alkene at elevated temperature in the presence of a metal oxidation catalyst and an oxidant. The metal oxidation catalyst can be palladium, such as palladium on carbon, and the oxidant can be the oxygen gas in ambient air. The reaction can be carried out without solvent or in high boiling hydrocarbon solvents such as mesitylene. When the unactivated alkene is a monosubstituted alkene, yields of at least about 50 or 60% of para-substituted ester and acid products, respectively, are obtained, substantially free of the regioisomeric meta-substituted impurity.
摘要翻译： 提供了一种合成对位取代的苯甲酸酯和酸的方法，其中基本上不含间位取代的杂质获得对位取代的区域异构体，该方法包括在高温下使香豆酸酯或酸与未活化的烯烃接触 存在金属氧化催化剂和氧化剂。 金属氧化催化剂可以是钯，例如钯碳，氧化剂可以是环境空气中的氧气。 该反应可以在没有溶剂的情况下进行，也可以在高沸点烃溶剂例如均三甲苯中进行。 当未活化的烯烃是单取代的烯烃时，分别获得至少约50或60％的对位取代的酯和酸产物的产率，基本上不含区域异构间位取代的杂质。
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公开(公告)号：US08415489B2
公开(公告)日：2013-04-09
申请号：US13292812
申请日：2011-11-09
申请人： George A. Kraus , Yi Yuan
发明人： George A. Kraus , Yi Yuan
IPC分类号： C07D407/14
CPC分类号： C07D493/18
摘要： The invention provides compounds that are A-type procyanidins. The compounds can be prepared by reacting flavylium salts with catechins or analogs thereof, for example, under anhydrous conditions in alcohol.
摘要翻译： 本发明提供了A型原花青素的化合物。 这些化合物可以通过使黄烷基盐与儿茶素或其类似物反应，例如在无水条件下在醇中反应来制备。
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公开(公告)号：US20120059175A1
公开(公告)日：2012-03-08
申请号：US13292812
申请日：2011-11-09
申请人： George A. Kraus , Yi Yuan
发明人： George A. Kraus , Yi Yuan
IPC分类号： C07D493/16 , C07D493/06
CPC分类号： C07D493/18
摘要： The invention provides compounds that are A-type procyanidins. The compounds can be prepared by reacting flavylium salts with catechins or analogs thereof, for example, under anhydrous conditions in alcohol.
摘要翻译： 本发明提供了A型原花青素的化合物。 这些化合物可以通过使黄烷基盐与儿茶素或其类似物反应，例如在无水条件下在醇中反应来制备。
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公开(公告)号：US4965267A
公开(公告)日：1990-10-23
申请号：US395992
申请日：1989-08-21
IPC分类号： A01N43/90 , C07D493/04
CPC分类号： C07D493/04 , A01N43/90
摘要： A new pyranoquinone and use thereof as an anticoccidial agent.
摘要翻译： 一种新的吡喃醌，其用作抗球虫剂。
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8.发明授权
公开(公告)号：US4214092A
公开(公告)日：1980-07-22
申请号：US13519
申请日：1979-02-21
申请人： George A. Kraus
发明人： George A. Kraus
IPC分类号： C07D307/58 , C07D333/32 , C07D333/16 , C07D307/12
CPC分类号： C07D333/32 , C07D307/58
摘要： A method of preparing acyloxy furans and thiophenes from butenolides comprising reacting a pre-selected butenolide with an acylating agent in the presence of a base to provide an acyloxy furan intermediate, which in turn undergoes rearrangement in the presence of Lewis Acids by cleavage of a carbon-oxygen bond, and addition of the cleaved moiety to the furan ring forming a carbon-carbon bond on the ring. The result is a heretofore unknown group of lactone type compounds which are biologically active, in and of themselves, and in addition offer use as versatile synthesis intermediates to achieve, by conventional synthesis methods heretofore unavailable compounds.
摘要翻译： 一种从丁烯内酯制备酰氧基呋喃和噻吩的方法，包括在碱的存在下使预选的丁烯酸酯与酰化剂反应，得到酰氧基呋喃中间体，其又在路易斯酸存在下通过裂解碳进行重排 - 氧键，并将切割的部分加入到在环上形成碳 - 碳键的呋喃环上。 结果是迄今为止未知的内酯类化合物组，其本身具有生物活性，并且另外提供作为多功能合成中间体的用途，通过迄今为止不可得的化合物的常规合成方法来实现。
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公开(公告)号：US07615649B2
公开(公告)日：2009-11-10
申请号：US11275756
申请日：2006-01-26
申请人： George A. Kraus , Yi Yuan
发明人： George A. Kraus , Yi Yuan
IPC分类号： C07D493/18 , C07D493/08
CPC分类号： C07D493/18
摘要： A method for preparing A-type procyanidins is provided by reacting flavylium salts with catechins and analogs thereof, under anhydrous conditions in alcohol.
摘要翻译： 通过在无水条件下在醇中将黄烷鎓盐与儿茶素类及其类似物反应来提供A型原花青素的方法。
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公开(公告)号：US07183432B2
公开(公告)日：2007-02-27
申请号：US11092333
申请日：2005-03-29
申请人： George A. Kraus , Jaehoon Bae
发明人： George A. Kraus , Jaehoon Bae
IPC分类号： C07C233/09
CPC分类号： C07C233/09
摘要： A method of synthesizing diacetylenic amides is described. The key steps of the invention include the reaction of an aldehyde with the monoanion of a diacetylene and the reductive removal of a propargylic alcohol. The invention offers the first known method of synthesizing diacetylenic amides that are naturally isolated from Echinacea through a direct and flexible route.
摘要翻译： 描述了合成二炔酰胺的方法。 本发明的关键步骤包括醛与二乙炔的单阴离子的反应以及炔丙醇的还原性除去。 本发明提供了通过直接和柔性的途径合成天然分离自紫锥菊的二乙酰基酰胺的第一已知方法。
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