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1. 发明授权

US06252085B1 Production of amide derivatives and intermediates therefor 失效
标题翻译：酰胺衍生物及其中间体的生产
公开(公告)号：US06252085B1
公开(公告)日：2001-06-26
申请号：US09580831
申请日：2000-05-30
申请人： Takashi Inaba , Yasuki Yamada
发明人： Takashi Inaba , Yasuki Yamada
IPC分类号： C07D26308
CPC分类号： C07D413/04 , C07C319/14 , C07D217/26 , C07D263/14 , C07D321/06 , C07C323/25 , C07C323/42
摘要： A method for producing an amide derivative of the formula [XV] wherein each-symbol is as defined in the specification, and an enantiomer thereof, a novel intermediate useful for producing said compound and a production method thereof. The production method of the present invention is extremely easy and simple as compared to the conventional methods, and enables effective production of compound [XV] at high yields, which includes compound [XVI] having an HIV protease inhibitory action. In addition, the novel intermediates of the present invention are extremely useful as intermediates for producing not only the aforementioned compound [XVI] but also compounds useful as X-ray contrast media.
摘要翻译：一种制备式[XV]的酰胺衍生物的方法，其中每个符号如说明书中所定义，及其对映异构体，可用于制备所述化合物的新型中间体及其制备方法。本发明的制备方法与常规方法相比非常容易和简单，并且能够以高产率有效生产化合物[XV]，其包括具有HIV蛋白酶抑制作用的化合物[XVI]。此外，本发明的新型中间体作为用于生产上述化合物[XVI]的中间体以及用作X射线造影剂的化合物是非常有用的。

2. 发明授权

US06515135B2 Aminoaryl oxazolidinone N-oxides 失效
公开(公告)号：US06515135B2
公开(公告)日：2003-02-04
申请号：US09988079
申请日：2001-06-28
申请人： Robert C. Gadwood , Bharat V. Kamdar
发明人： Robert C. Gadwood , Bharat V. Kamdar
IPC分类号： C07D26308
CPC分类号： C07D263/20 , C07D413/10 , C07D413/12 , C07D417/10 , C07D491/08 , C07D491/10 , C07D495/08
摘要： The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.

3. 发明授权

US06410741B1 Optically active bisoxazoline compounds, production and use thereof 失效
标题翻译：光学活性的双恶唑啉化合物，其生产和使用
公开(公告)号：US06410741B1
公开(公告)日：2002-06-25
申请号：US09563914
申请日：2000-05-04
申请人： Makoto Itagaki , Gohfu Suzukamo
发明人： Makoto Itagaki , Gohfu Suzukamo
IPC分类号： C07D26308
CPC分类号： C07D263/12 , C07B2200/07 , C07C67/347 , C07C69/743 , C07C233/18
摘要： An optically active bisoxazoline compound of the formula [I]: wherein R1 represents alkyl group, cycloalkyl group, aralkyl group, phenyl group which may be substituted or alkoxy group and two geminal alkyl groups may be joined together to form a cyclic structure; R2 represents alkyl group, cycloalkyl group, aralkyl group, phenyl group which may be substituted; R3 represents hydrogen atom, (C2-C4)alkyl group or cycloalkyl group; and the asterisk * represents an asymmetric carbon atom
摘要翻译：式[I]的光学活性双恶唑啉化合物：其中R 1表示烷基，环烷基，芳烷基，可被取代的苯基或烷氧基和两个偕烷基可以连接在一起形成环状结构; R 2表示烷基，环烷基，芳烷基，可被取代的苯基; R3表示氢原子，（C2-C4）烷基或环烷基; 星号*表示不对称碳原子

4. 发明授权

US06583292B2 Method for the esterification of alcohols and compounds useful therefor as potential anticancer agents 失效
标题翻译：用于酯化醇和作为潜在抗癌剂的化合物的方法
公开(公告)号：US06583292B2
公开(公告)日：2003-06-24
申请号：US10068645
申请日：2002-02-06
申请人： Dennis C. Liotta , Hariharan Venkatesan , Laura Captain , Michael V. Voronkov , James P. Snyder , Marcus A. Schestopol
发明人： Dennis C. Liotta , Hariharan Venkatesan , Laura Captain , Michael V. Voronkov , James P. Snyder , Marcus A. Schestopol
IPC分类号： C07D26308
CPC分类号： C07D263/16 , C07C35/37 , C07C229/34 , C07D263/26 , C07D277/14 , C07D305/14 , C07D413/12
摘要： Described herein is a method for preparing an ester by (a) admixing a compound having the formula I: with a base to form an intermediate, and (b) admixing the intermediate produced in step (a) with a compound composed of an alcohol, an alkoxide, or a combination thereof, wherein steps (a) and (b) are performed in situ.
摘要翻译：本文描述的是通过（a）将具有式I化合物与碱混合以形成中间体的方法，和（b）将步骤（a）中制备的中间体与由醇组成的化合物混合，醇盐或其组合，其中步骤（a）和（b）原位进行。

5. 发明授权

US06441188B1 Aminoaryl oxazolidinone N-oxides 失效
标题翻译：氨基芳基恶唑烷酮N-氧化物
公开(公告)号：US06441188B1
公开(公告)日：2002-08-27
申请号：US09988078
申请日：2001-06-28
申请人： Robert C. Gadwood , Bharat V. Kamdar
发明人： Robert C. Gadwood , Bharat V. Kamdar
IPC分类号： C07D26308
CPC分类号： C07D263/20 , C07D413/10 , C07D413/12 , C07D417/10 , C07D491/08 , C07D491/10 , C07D495/08
摘要： The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.
摘要翻译：本发明提供式I的氨基芳基恶唑烷酮N-氧化物化合物，其中变量如本文所定义。这些化合物是非常水溶性的，其可用于制备这些化合物的药物制剂。它们也在体内快速转化回母体胺，使得它们可用作母体胺的前药。它们对许多人类和兽医病原体有效，包括革兰氏阳性好氧细菌，如多重耐药葡萄球菌，链球菌和肠球菌，以及厌氧生物，如拟杆菌属。和梭菌属（Clostridia spp。）物种和耐酸生物，如结核分枝杆菌，鸟分枝杆菌和分枝杆菌，以及生物体如支原体属（Mycoplasma spp）。

6. 发明授权

US06794516B2 Synthesis of clasto-lactacystin &bgr;-lactone and analogs thereof 有权
标题翻译：合成乳链球蛋白β-内酯及其类似物
公开(公告)号：US06794516B2
公开(公告)日：2004-09-21
申请号：US10360459
申请日：2003-02-07
申请人： François Soucy , Louis Plamondon , Mark Behnke , William Roush
发明人： François Soucy , Louis Plamondon , Mark Behnke , William Roush
IPC分类号： C07D26308
CPC分类号： C07D263/16 , C07B2200/07 , C07C69/675 , C07C231/14 , C07C235/80 , C07C237/06 , C07C247/04 , C07D207/28 , C07D491/04 , C07C233/83
摘要： The present invention is directed to an improved synthesis of clasto-lactacystin-&bgr;-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-&bgr;-lactones, and analogs thereof and their use as proteosome inhibitors.
摘要翻译：本发明涉及与现有技术中描述的合成相比，以更少的步骤和更大的总产率进行的乳链球菌 - 乳胞素-β-内酯及其类似物的改进合成。合成途径依赖于恶唑啉中间体的新立体有择合成和甲酰胺向恶唑啉的独特立体选择性加成。还描述了新的clasto-lactacystin-β-内酯及其类似物及其作为蛋白质体抑制剂的用途。

7. 发明授权

US06472534B2 Methods for the preparation of intermediates in the synthesis of HIV-protease inhibitors 失效
标题翻译：在合成HIV-蛋白酶抑制剂中制备中间体的方法
公开(公告)号：US06472534B2
公开(公告)日：2002-10-29
申请号：US09986146
申请日：2001-11-07
申请人： Bennett C. Borer , Scott E. Zook , Juliette K. Busse
发明人： Bennett C. Borer , Scott E. Zook , Juliette K. Busse
IPC分类号： C07D26308
CPC分类号： C07D263/14 , C07D307/22 , C07D413/06 , Y02P20/55
摘要： Methods for the preparation of chemical intermediates in the synthesis of HIV-protease inhibitors related to and including nelfinavir mesylate are disclosed. The method of this invention comprises converting tetrohydran derivatives into oxazolines to provide key reaction intermediates for the preparation of nelfinavir. Also disclosed is a method for the preparation of a chiral amino alcohol from an epoxy-tetrahydrofuran.
摘要翻译：公开了在与奈非那韦甲磺酸盐相关的HIV-蛋白酶抑制剂的合成中制备化学中间体的方法。本发明的方法包括将四氢化茚衍生物转化为恶唑啉以提供制备奈非那韦的关键反应中间体。还公开了一种由环氧 - 四氢呋喃制备手性氨基醇的方法。

8. 发明授权

US06437145B1 Method of producing oxazolidinones, the use thereof and oxazolidinones 失效
标题翻译：生产恶唑烷酮的方法，其用途和恶唑烷酮
公开(公告)号：US06437145B1
公开(公告)日：2002-08-20
申请号：US09542278
申请日：2000-04-04
申请人： Karlheinz Drauz , Günter Knaup , Stefan Retzow
发明人： Karlheinz Drauz , Günter Knaup , Stefan Retzow
IPC分类号： C07D26308
CPC分类号： C07D263/18 , C07C231/14 , C07C237/22
摘要： The invention concerns a method of producing oxazolidinones of formula (I), wherein R1-R5 have the meanings given in the description, by reacting cyclical anhydrides of formula (II) with carbonyl compounds of general formula (III) at temperatures between ambient temperature and approximately 150° C. The invention also concerns the production of the cyclical anhydrides of formula (II) by reacting N-protected aminodicarboxylic acids of formula (IV) with a dehydrating agent in situ. The invention further concerns the use of oxazolidinones of formula (I) for the &agr;-selective production of esters of formula (V) and amides of general formula (VII).
摘要翻译：本发明涉及一种制备式（I）的恶唑烷酮的方法，其中R1-R5具有本说明书中给出的含义，通式（II）的环状酸酐与通式（III）的羰基化合物在环境温度和本发明还涉及式（II）的环状酸酐通过将式（Ⅳ）的N-保护的氨基二羧酸与脱水剂原位反应来生产。本发明还涉及式（I）的恶唑烷酮在通式（Ⅴ）的酯和通式（Ⅶ）的酰胺的α-选择性生产中的应用。

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