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公开(公告)号：US5668168A
公开(公告)日：1997-09-16
申请号：US470102
申请日：1995-06-06
申请人： Thien V. Truong , Donald E. Bierer , Jeffrey M. Dener , Richard Hector , Michael S. Tempesta , Bernard Loev , Wu Yang , Masato Koreeda
发明人： Thien V. Truong , Donald E. Bierer , Jeffrey M. Dener , Richard Hector , Michael S. Tempesta , Bernard Loev , Wu Yang , Masato Koreeda
IPC分类号： A61K9/12 , A61K31/38 , A61K31/385 , A61P31/04 , A61P31/10 , C07C323/14 , C07C323/16 , C07D339/04 , C07D339/08 , C07C321/06
CPC分类号： C07C323/14 , A61K31/385 , C07D339/04 , C07D339/08
摘要： This invention pertains to a novel group of 1,2-dithiin compounds useful as antiinfective agents, and a novel synthetic process to produce the same. The compounds are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans or Aspergillus fumigatus.
摘要翻译： 本发明涉及可用作抗感染剂的新型1,2-二硫素化合物组合物及其制备方法。 这些化合物特别有效地治疗真菌感染，特别是由白色念珠菌，新型隐球菌或烟曲霉引起的真菌感染。
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公开(公告)号：US5556875A
公开(公告)日：1996-09-17
申请号：US110917
申请日：1995-08-24
申请人： Thien V. Truong , Donald E. Bierer , Jeffrey M. Dener , Richard Hector , Michael S. Tempesta , Bernard Loev , Wu Yang , Masato Koreeda
发明人： Thien V. Truong , Donald E. Bierer , Jeffrey M. Dener , Richard Hector , Michael S. Tempesta , Bernard Loev , Wu Yang , Masato Koreeda
IPC分类号： A61K9/12 , A61K31/38 , A61K31/385 , A61P31/04 , A61P31/10 , C07C323/14 , C07C323/16 , C07D339/04 , C07D339/08
CPC分类号： C07C323/14 , A61K31/385 , C07D339/04 , C07D339/08
摘要： This invention pertains to a novel group of 1,2-dithiin compounds useful as antiinfective agents, and a novel synthetic process to produce the same. The compounds are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans or Aspergillus fumigatus.
摘要翻译： 本发明涉及可用作抗感染剂的新型1,2-二硫素化合物组合物及其制备方法。 这些化合物特别有效地治疗真菌感染，特别是由白色念珠菌，新型隐球菌或烟曲霉引起的真菌感染。
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3.发明授权Process for the preparation of mono- and bis(phosphocholine) derivatives which have antifungal activity 失效具有抗真菌活性的单和双（磷酸胆碱）衍生物的制备方法
公开(公告)号：US5811568A
公开(公告)日：1998-09-22
申请号：US234483
申请日：1994-04-28
IPC分类号： A01N57/14 , A01N57/16 , A61K31/66 , A61K31/70 , A61K31/7028 , A61K36/18 , A61K47/24 , A61P31/04 , A61P31/10 , C07F9/09 , C07F9/10 , C07F9/655 , C07G3/00 , C07H15/04 , C07H15/18 , C07F9/02
CPC分类号： A01N57/14 , A01N57/16 , A61K31/685 , A61K31/688 , A61K31/70 , A61K47/24 , C07F9/093 , C07F9/10 , C07H15/04 , C07H15/18
摘要： This invention pertains to a synthetic process for obtaining a unique phosphocholine derivative which has been isolated from the leaves of the plant Irbachia alata, identified to be 1,22-bis�2-(trimethylammonium)ethylphosphatyl! docosane is disclosed. Also disclosed is a synthetic process for obtaining a novel class of mono- and bis(phosphocholine) derivatives which are useful as antiinfective agents. The compounds are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans, and Aspergillus fumigatus.
摘要翻译： 本发明涉及一种用于获得已鉴定为1,22-双[2-（三甲基铵）乙基磷酰基]二十二烷的植物Irbachia alata的叶分离的独特的磷酸胆碱衍生物的合成方法。 还公开了一种用于获得可用作抗感染剂的新型单 - 和双（磷酸胆碱）衍生物的合成方法。 这些化合物特别有效地治疗真菌感染，特别是由白色念珠菌，新型隐球菌和烟曲霉引起的真菌感染。
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4.发明授权Preparation of symmetrical and unsymmetrical 3,6-disubstituted-1,2-dithiins having antifungal activity 失效具有抗真菌活性的对称和不对称3,6-二取代-1,2-二硫辛的制备
公开(公告)号：US5583235A
公开(公告)日：1996-12-10
申请号：US212096
申请日：1994-03-11
IPC分类号： C07D339/08 , C07D409/06 , C07D409/12 , C07D409/14 , C07D521/00 , C07F7/18
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D339/08 , C07D409/06 , C07D409/12 , C07D409/14 , C07F7/1856
摘要： The present invention provides an improved procedure for the preparation of 3,6-disubstituted-1,2-dithiin derivatives, especially unsymmetrical 1,2-dithiins. In addition, the process offers significant process, scaleup, and safety advantages over the previously reported synthetic processes. The compounds synthesized by this new process and described herein are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans, Aspergillus fumigatus, Trichophyton rubrum, Candida parapsilosis, Candida tropicalis, or Candida krusei.
摘要翻译： 本发明提供了制备3,6-二取代-1,2-二硫素衍生物，特别是不对称1,2-二硫辛烷的改进方法。 此外，该方法比以前报道的合成方法提供了重要的过程，放大和安全优势。 通过这种新方法合成并在本文中描述的化合物在治疗真菌感染，特别是由白色念珠菌，新型隐球酵母，烟曲霉，红色毛癣菌，热带假丝酵母，热带假丝酵母或克罗斯假丝酵母引起的真菌感染中特别有效。
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5.发明授权N-aryl and N-heteroarylamide and urea derivatives as inhibitors of acyl coenzyme A: cholesterol acyl transferase (ACAT) 失效N-芳基和N-杂芳基酰胺和脲衍生物作为酰基辅酶A的抑制剂：胆固醇酰基转移酶（ACAT）
公开(公告)号：US5656634A
公开(公告)日：1997-08-12
申请号：US251075
申请日：1994-05-31
IPC分类号： C07C233/25 , C07C233/58 , C07C233/59 , C07C233/60 , C07C235/24 , C07C275/34 , C07C317/44 , C07C323/52 , C07C323/60 , C07D213/73 , A61K31/44 , C07D213/38 , C07D239/42
CPC分类号： C07D213/73 , C07C233/25 , C07C233/58 , C07C233/59 , C07C233/60 , C07C235/24 , C07C275/34 , C07C317/44 , C07C323/52 , C07C323/60 , C07C2101/16 , C07C2102/08 , C07C2102/10 , C07C2102/42 , C07C2102/44
摘要： Compounds of the formula ##STR1## the pharmaceutically acceptable salts thereof, wherein Q and R.sup.1 are as defined below, and novel carboxylic acid and acid halide intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.
摘要翻译： 下式的化合物其中Q和R 1如下所定义，其中药学上可接受的盐，以及用于合成这些化合物的新的羧酸和酰卤中间体。 式I化合物是酰基辅酶A：胆固醇酰基转移酶（ACAT）的抑制剂，可用作降血脂和抗动脉粥样硬化剂。
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