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1. 发明授权

US5831117A Method of preparing retroviral protease inhibitor intermediates 失效
公开(公告)号：US5831117A
公开(公告)日：1998-11-03
申请号：US376340
申请日：1995-01-20
申请人： John S. Ng , Claire A. Przybyla , Shu-Hong Zhang
发明人： John S. Ng , Claire A. Przybyla , Shu-Hong Zhang
IPC分类号： C07D303/36 , C07C213/10 , C07C215/08 , C07C215/18 , C07C215/26 , C07C215/28 , C07C221/00 , C07C223/02 , C07C255/26 , C07C271/16 , C07C271/20 , C07C271/22 , C07C275/14 , C07C275/24 , C07C309/73 , C07F7/18 , C07C309/01
CPC分类号： C07D207/30 , C07C213/10 , C07C215/18 , C07C215/26 , C07C215/28 , C07C271/20 , C07C275/24 , C07D211/06 , C07D211/26
摘要： Chiral hydroxyethylamine, hydroxyethylurea or hydroxyethylsulfonamide isostere containing retroviral protease and renin inhibitors can be prepared by multi-step syntheses that utilize key chiral amine intermediates. This invention is a cost effective method of obtaining such key chiral amine intermediates enantiomerically, diastereomerically and chemically pure. The method is suitable for large scale (multikilogram) productions. This invention also encompasses organic acid and inorganic acid salts of the amine intermediates.

2. 发明授权

US07189864B2 Method of preparing intermediates useful in synthesis of retroviral protease inhibitors 失效
标题翻译：制备可用于合成逆转录病毒蛋白酶抑制剂的中间体的方法
公开(公告)号：US07189864B2
公开(公告)日：2007-03-13
申请号：US10962746
申请日：2004-10-13
申请人： John S. Ng , Claire A. Przybyla , Richard A. Mueller , Michael L. Vazquez , Daniel P. Getman
发明人： John S. Ng , Claire A. Przybyla , Richard A. Mueller , Michael L. Vazquez , Daniel P. Getman
IPC分类号： C07C221/00 , C07D301/02
CPC分类号： C07K5/06191 , A61K31/17 , A61K31/195 , A61K31/197 , A61K31/216 , A61K31/27 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K38/00 , C04B35/632 , C07B2200/07 , C07C213/00 , C07C213/02 , C07C213/08 , C07C269/06 , C07C271/20 , C07C271/22 , C07C275/14 , C07C275/18 , C07C275/22 , C07C275/24 , C07C275/28 , C07C311/47 , C07C317/44 , C07C317/50 , C07C323/60 , C07C329/06 , C07C335/08 , C07C335/12 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D213/81 , C07D215/48 , C07D215/50 , C07D215/54 , C07D217/26 , C07D235/06 , C07D235/24 , C07D239/38 , C07D241/44 , C07D295/13 , C07D295/15 , C07D303/36 , C07D307/85 , C07D401/12 , C07K5/0207 , C07K5/021 , C07K5/06026 , C07K5/06139 , C07C215/08 , C07C215/28 , C07C271/16
摘要： A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide from a chiral alpha amino aldehyde.
摘要翻译：对于易于大规模制备基于羟基脲的手性HIV蛋白酶抑制剂的中间体描述了合成。该方法包括由手性α氨基醛形成非对映选择性环氧化物。

3. 发明授权

US5583238A Method for making intermediates useful in synthesis of retroviral protease inhibitors 失效
标题翻译：制备可用于合成逆转录病毒蛋白酶抑制剂的中间体的方法
公开(公告)号：US5583238A
公开(公告)日：1996-12-10
申请号：US290976
申请日：1994-12-16
申请人： John S. Ng , Claire A. Przybyla , Richard A. Mueller , Michael L. Vazquez , Daniel P. Getman
发明人： John S. Ng , Claire A. Przybyla , Richard A. Mueller , Michael L. Vazquez , Daniel P. Getman
IPC分类号： A61K31/17 , A61K31/195 , A61K31/197 , A61K31/216 , A61K31/27 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K38/00 , C07C213/00 , C07C213/02 , C07C213/08 , C07C215/28 , C07C269/06 , C07C271/16 , C07C271/20 , C07C271/22 , C07C275/14 , C07C275/18 , C07C275/22 , C07C275/24 , C07C275/28 , C07C311/47 , C07C317/44 , C07C317/50 , C07C323/60 , C07C329/06 , C07C335/08 , C07C335/12 , C07D213/81 , C07D215/48 , C07D215/50 , C07D215/54 , C07D217/26 , C07D235/06 , C07D235/24 , C07D239/38 , C07D241/44 , C07D295/13 , C07D295/15 , C07D303/36 , C07D307/85 , C07D401/12 , C07K5/02 , C07K5/06 , C07K5/078 , C07D301/00 , C07D209/48
CPC分类号： C07K5/06191 , A61K31/17 , A61K31/195 , A61K31/197 , A61K31/216 , A61K31/27 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , C07C213/00 , C07C213/02 , C07C213/08 , C07C269/06 , C07C271/20 , C07C271/22 , C07C275/14 , C07C275/18 , C07C275/22 , C07C275/24 , C07C275/28 , C07C311/47 , C07C317/44 , C07C317/50 , C07C323/60 , C07C329/06 , C07C335/08 , C07C335/12 , C07D213/81 , C07D215/48 , C07D215/50 , C07D215/54 , C07D217/26 , C07D235/06 , C07D235/24 , C07D239/38 , C07D241/44 , C07D295/13 , C07D295/15 , C07D303/36 , C07D307/85 , C07D401/12 , C07K5/0207 , C07K5/021 , C07K5/06026 , C07K5/06139 , A61K38/00 , C07B2200/07 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide from a chiral alpha amino aldehyde.
摘要翻译： PCT No.PCT / US93 / 04804 Sec。 371日期1994年12月16日第 102（e）日期1994年12月16日PCT提交1993年5月24日PCT公布。第WO93 / 23388号公报日期：1993年11月25日对于易于大规模制备基于羟乙基脲的手性HIV蛋白酶抑制剂的中间体的描述。该方法包括由手性α氨基醛形成非对映选择性环氧化物。

4. 发明授权

US5648511A Method for making intermediates useful in the synthesis of retroviral protease inhibitors 失效
标题翻译：制备可用于合成逆转录病毒蛋白酶抑制剂的中间体的方法
公开(公告)号：US5648511A
公开(公告)日：1997-07-15
申请号：US452187
申请日：1995-05-25
申请人： John S. Ng , Claire A. Przybyla , Richard A. Mueller , Michael L. Vazquez , Daniel P. Getman , John J. Freskos , Gary A. DeCrescenzo , Deborah E. Bertenshaw , Robert M. Heintz , Suhong Zhang , Chin Liu , Scott A. Laneman
发明人： John S. Ng , Claire A. Przybyla , Richard A. Mueller , Michael L. Vazquez , Daniel P. Getman , John J. Freskos , Gary A. DeCrescenzo , Deborah E. Bertenshaw , Robert M. Heintz , Suhong Zhang , Chin Liu , Scott A. Laneman
IPC分类号： A61K31/17 , A61K31/195 , A61K31/197 , A61K31/27 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K38/00 , C07C213/00 , C07C213/02 , C07C213/08 , C07C215/28 , C07C269/04 , C07C269/06 , C07C271/16 , C07F7/18 , C07K5/078 , C07D253/00
CPC分类号： C07C269/06 , A61K31/17 , A61K31/195 , A61K31/197 , A61K31/27 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , C07C213/00 , C07C213/02 , C07C213/08 , C07C269/04 , C07F7/188 , C07K5/06139 , A61K38/00 , C07B2200/07
摘要： A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide or cyanohydrin from a chiral alpha amino aldehyde.
摘要翻译：对于易于大规模制备基于羟基脲的手性HIV蛋白酶抑制剂的中间体描述了合成。该方法包括由手性α氨基醛形成非对映选择性环氧化物或羟腈。

6. 发明授权

US06335441B1 5&bgr;-cyano-substituted steroid compounds 失效
标题翻译： 5β-氰基取代的类固醇化合物
公开(公告)号：US06335441B1
公开(公告)日：2002-01-01
申请号：US09583158
申请日：2000-05-30
申请人： John S. Ng , Chin Liu , Dennis K. Anderson , Jon P. Lawson , Bernhard Erb , Joseph Wieczorek , Sastry A. Kunda , Leo J. Letendre , Mark J. Pozzo , Yuen-Lung L. Sing , Edward E. Yonan
发明人： John S. Ng , Chin Liu , Dennis K. Anderson , Jon P. Lawson , Bernhard Erb , Joseph Wieczorek , Sastry A. Kunda , Leo J. Letendre , Mark J. Pozzo , Yuen-Lung L. Sing , Edward E. Yonan
IPC分类号： C07J5300
CPC分类号： C07J71/00 , C07J21/00 , C07J21/003 , C07J31/006 , C07J53/00 , C07J53/002 , C07J71/0015 , C12P33/005 , C12P33/10 , C12Q1/02
摘要： Novel 5&bgr;-cyano steroid compounds including compounds of Formula VII: wherein A—A, B—B, R3, R8 and R9 are as defined in the specification.
摘要翻译：包括式VII化合物的新型5β-氰基类固醇化合物：其中A-A，B-B，R 3，R 8和R 9如说明书中所定义。

7. 发明授权

US5104990A Process for the preparation of 3-aryl-3-aminoalkyl-2,6-dioxohexahydropyridines 失效
标题翻译：制备3-芳基-3-氨基甲酰基-2,6-二氧代甲基吡啶的方法
公开(公告)号：US5104990A
公开(公告)日：1992-04-14
申请号：US486027
申请日：1990-02-27
申请人： John H. Dygos , Kathleen T. McLaughlin , John S. Ng , Kalidas Paul
发明人： John H. Dygos , Kathleen T. McLaughlin , John S. Ng , Kalidas Paul
IPC分类号： C07D211/88 , C07D401/04
CPC分类号： C07D211/88
摘要： Disclosed is a process for the preparation of 3-aryl-3-aminoalkyl-2,6-dioxohexahydropridines and particularly the compounds 3-[3-(dimethylamino)propyl]-3-(3-methoxyphenyl)-4, 4-dimethyl-2,6-piperidinedione, monohydrochloride, which is useful as an antidepressant.the process of the present invention comprises the condensation of a sterically hindered nitrile with a sterically hindered .alpha., .beta.-unsaturated diester to produce a nitrile diester. These compounds can then undergo acid catalyzed cyclization and decarboalkoxylation in a one step process to provide the desired 3-aryl-3-aminoalkyl-2,6-dioxohexahydropyridine.

8. 发明授权

US5013864A Process for preparation of .alpha.-alkoxy acetic acids and their salts 失效
标题翻译： α-烷氧基乙酸及其盐的制备方法
公开(公告)号：US5013864A
公开(公告)日：1991-05-07
申请号：US447766
申请日：1989-12-08
申请人： Arthur L. Campbell , Richard A. Mueller , John S. Ng , Richard A. Partis
发明人： Arthur L. Campbell , Richard A. Mueller , John S. Ng , Richard A. Partis
IPC分类号： C07C51/367 , C07C59/125 , C07C59/13 , C07C59/66 , C07C319/20 , C07C323/12 , C07C323/20
CPC分类号： C07C323/20 , C07C51/367
摘要： A process for producing an .alpha.-alkoxy acetic acids and salts thereof which comprises reacting an alcohol of the formula R--OH wherein R is alkyl, substituted alkyl, or cycloalkyl, or cycloalkyl alkyl with a base in an aprotic organic solvent to give an alkoxide followed by removal of the organic solvent and reaction of the alkoxide with a salt of a monohaloacetic acid in a polar aprotic solvent such as DMSO to give the corresponding alkoxyacetate salt which then may be recovered or may optionally be converted to the corresponding acid by contacting the alkoxy acetate salt with an acid.

9. 发明授权

US07238507B2 Aspergillus ochraceus 11 alpha hydroxylase and oxidoreductase 失效
标题翻译：曲霉曲霉11α羟化酶和氧化还原酶
公开(公告)号：US07238507B2
公开(公告)日：2007-07-03
申请号：US10900856
申请日：2004-07-28
申请人： Suzanne L. Bolten , Robert A. Clayton , Alan M. Easton , Leslie C. Engel , Dean M. Messing , John S. Ng , Beverly Reitz , Mark C. Walker , Ping T. Wang
发明人： Suzanne L. Bolten , Robert A. Clayton , Alan M. Easton , Leslie C. Engel , Dean M. Messing , John S. Ng , Beverly Reitz , Mark C. Walker , Ping T. Wang
IPC分类号： C12N9/02
CPC分类号： C12N9/0083 , C07K14/38 , C07K16/40 , C12N1/14 , C12N3/00 , C12N9/0004 , C12N2799/026 , C12P33/10
摘要： The present invention relates to a novel cytochrome P450-like enzyme (Aspergillus ochraceus 11 alpha hydroxylase) and an oxidoreductase (Aspergillus ochraceus oxidoreductase) isolated from cDNA library generated from the mRNA of Aspergillus ochraceus spores. When the cDNA encoding the 11 alpha hydroxylase was co-expressed in Spodoptera frugiperda (Sf-9) insect cells with the cDNA encoding human oxidoreductase as an electron donor, it successfully catalyzed the conversion of the steroid substrate 4-androstene-3,17-dione (AD) to 11 alpha-hydroxy-AD as determined by HPLC analysis. The invention also relates to nucleic acid molecules associated with or derived from these cDNAs including complements, homologues and fragments thereof, and methods of using these nucleic acid molecules, to generate, for example, polypeptides and fragments thereof. The invention also relates to the generation of antibodies that recognizes the A. ochraceus 11 alpha hydroxylase and oxidoreductase and methods of using these antibodies to detect the presence of these native and recombinant polypeptides within unmodified and transformed host cells, respectively. The invention also provides methods of expressing the Aspergillus 11 alpha hydroxylase gene separately, or in combination with human or Aspergillus oxidoreductase, in heterologous host cells, to facilitate the bioconversion of steroid substrates to their 11 alpha hydroxy-counterparts.
摘要翻译：本发明涉及从赭曲霉孢子的mRNA产生的cDNA文库中分离的新型细胞色素P450样酶（赭曲霉11α羟化酶）和氧化还原酶（赭曲霉氧化还原酶）。当编码11α羟化酶的cDNA在草地贪夜蛾（Sf-9）昆虫细胞中以编码人氧化还原酶的cDNA作为电子给体共同表达时，其成功地催化类固醇底物4-雄甾烯-3,17- （AD）至11α-羟基-AD，通过HPLC分析测定。本发明还涉及与这些cDNA相关或衍生的核酸分子，包括其互补序列，同系物和片段，以及使用这些核酸分子的方法，以产生例如其多肽及其片段。本发明还涉及识别赭曲霉11α羟化酶和氧化还原酶的抗体的产生以及使用这些抗体分别在未修饰和转化的宿主细胞中检测这些天然和重组多肽的存在的方法。本发明还提供在异源宿主细胞中单独或与人或曲霉属氧化还原酶组合表达曲霉11α羟化酶基因的方法，以促进类固醇底物对其11α羟基对应物的生物转化。

10. 发明授权

US06630587B2 Processes for preparation of 9,11-epoxy steroids and intermediates useful therein 失效
标题翻译：制备9,11-环氧类固醇及其中有用的中间体的方法
公开(公告)号：US06630587B2
公开(公告)日：2003-10-07
申请号：US09923977
申请日：2001-08-07
申请人： John S. Ng , Ping T. Wang , Julio A. Baez , Chin Liu , Dennis K. Anderson , Jon P. Lawson , Bernhard Erb , Joseph Wieczorek , Gennaro Mucciariello , Fortunato Vanzanella , Sastry A. Kunda , Leo J. Letendre , Mark J. Pozzo , Yuen-Lung L. Sing , Edward E. Yonan
发明人： John S. Ng , Ping T. Wang , Julio A. Baez , Chin Liu , Dennis K. Anderson , Jon P. Lawson , Bernhard Erb , Joseph Wieczorek , Gennaro Mucciariello , Fortunato Vanzanella , Sastry A. Kunda , Leo J. Letendre , Mark J. Pozzo , Yuen-Lung L. Sing , Edward E. Yonan
IPC分类号： C07J900
CPC分类号： C07J71/00 , C07J21/00 , C07J21/003 , C07J31/006 , C07J53/00 , C07J53/002 , C07J71/0015 , C12P33/005 , C12P33/10 , C12Q1/02
摘要： Novel 9&agr;-hydroxy steroid compounds, including compounds of Formula IX wherein —A—A—, —B—B—, R1, R3, R8 and R9 are as defined in the specification.
摘要翻译：新的9-羟基类固醇化合物，包括式IX的化合物，其中-A-A-，-B-B-，R 1，R 3，R 8和R 9如说明书中所定义。

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