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1. 发明授权

US5599973A GABA and L-glutamic acid analogs for antiseizure treatment 失效
标题翻译： GABA和L-谷氨酸类似物用于抗发病治疗
公开(公告)号：US5599973A
公开(公告)日：1997-02-04
申请号：US420580
申请日：1995-04-12
申请人： Richard B. Silverman , Ryszard Andruszkiewicz , Po-Wai Yuen , Denis M. Sobieray , Lloyd C. Franklin , Mark A. Schwindt
发明人： Richard B. Silverman , Ryszard Andruszkiewicz , Po-Wai Yuen , Denis M. Sobieray , Lloyd C. Franklin , Mark A. Schwindt
IPC分类号： A61K31/197 , C07C69/34 , C07C69/675 , C07C229/08 , C07C229/24 , C07C229/28 , C07C229/34 , C07C247/12 , C07C309/73 , C07D263/22 , C07D263/26 , G11B20/14 , G11B27/30 , C07C229/00
CPC分类号： A61K31/197 , C07C229/08 , C07C229/24 , C07C229/28 , C07C229/34 , C07C247/12 , C07C309/73 , C07C69/34 , C07C69/675 , C07D263/22 , C07D263/26 , G11B20/1426 , G11B27/3027 , C07C2101/14
摘要： A compound of the formula ##STR1## wherein R.sub.1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R.sub.2 is hydrogen or methyl; and R.sub.3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.
摘要翻译：式Ⅰ化合物，其中R1是具有1至6个碳原子的直链或支链烷基，苯基或具有3至6个碳原子的环烷基; R2是氢或甲基; 并且R 3是氢，甲基或羧基; 其用于治疗癫痫发作。公开了用于制备化合物的方法。还公开了在合成化合物期间制备的中间体。

2. 发明授权

US5563175A GABA and L-glutamic acid analogs for antiseizure treatment 失效
标题翻译： GABA和L-谷氨酸类似物用于抗发病治疗
公开(公告)号：US5563175A
公开(公告)日：1996-10-08
申请号：US420575
申请日：1995-04-12
申请人： Richard B. Silverman , Ryszard Andruszkiewicz , Po-Wai Yuen , Denis M. Sobieray , Lloyd C. Franklin , Mark A. Schwindt
发明人： Richard B. Silverman , Ryszard Andruszkiewicz , Po-Wai Yuen , Denis M. Sobieray , Lloyd C. Franklin , Mark A. Schwindt
IPC分类号： A61K31/197 , C07C69/34 , C07C69/675 , C07C229/08 , C07C229/24 , C07C229/28 , C07C229/34 , C07C247/12 , C07C309/73 , C07D263/22 , C07D263/26 , G11B20/14 , G11B27/30 , A61K31/195
CPC分类号： A61K31/197 , C07C229/08 , C07C229/24 , C07C229/28 , C07C229/34 , C07C247/12 , C07C309/73 , C07C69/34 , C07C69/675 , C07D263/22 , C07D263/26 , G11B20/1426 , G11B27/3027 , C07C2101/14
摘要： A compound of the formula ##STR1## wherein R.sub.1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R.sub.2 is hydrogen or methyl; and R.sub.3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.
摘要翻译：式Ⅰ化合物，其中R1是具有1至6个碳原子的直链或支链烷基，苯基或具有3至6个碳原子的环烷基; R2是氢或甲基; 并且R 3是氢，甲基或羧基; 其用于治疗癫痫发作。公开了用于制备化合物的方法。还公开了在合成化合物期间制备的中间体。

3. 发明授权

US5608090A GABA and L-glutamic acid analogs for antiseizure treatment 失效
公开(公告)号：US5608090A
公开(公告)日：1997-03-04
申请号：US420577
申请日：1995-04-12
申请人： Richard B. Silverman , Ryszard Andruszkiewicz , Po-Wai Yuen , Denis M. Sobieray , Lloyd C. Franklin , Mark A. Schwindt
发明人： Richard B. Silverman , Ryszard Andruszkiewicz , Po-Wai Yuen , Denis M. Sobieray , Lloyd C. Franklin , Mark A. Schwindt
IPC分类号： A61K31/197 , C07C69/34 , C07C69/675 , C07C229/08 , C07C229/24 , C07C229/28 , C07C229/34 , C07C247/12 , C07C309/73 , C07D263/22 , C07D263/26 , G11B20/14 , G11B27/30 , C07C247/00
CPC分类号： A61K31/197 , C07C229/08 , C07C229/24 , C07C229/28 , C07C229/34 , C07C247/12 , C07C309/73 , C07C69/34 , C07C69/675 , C07D263/22 , C07D263/26 , G11B20/1426 , G11B27/3027 , C07C2101/14
摘要： A compound of the formula ##STR1## wherein R.sub.1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R.sub.2 is hydrogen or methyl; and R.sub.3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.

4. 发明申请

US20080161564A1 Aromatic sulfonated ketals 审中-公开
标题翻译：芳香磺化缩酮
公开(公告)号：US20080161564A1
公开(公告)日：2008-07-03
申请号：US12004204
申请日：2007-12-20
申请人： Mark A. Schwindt , Robert J. Topping , Charles E. Tucker
发明人： Mark A. Schwindt , Robert J. Topping , Charles E. Tucker
IPC分类号： C07D241/10
CPC分类号： C07D319/08 , C07D241/20
摘要： The present invention advantageously provides ketal functional compounds that can be strong electrophiles under conditions compatible with ketal groups, are stable, crystalline solids at room temperature, and are much safer to handle than ketal iodides. The present invention accomplishes by incorporating aromatic sulfonyl moieties into ketal functional materials. The compounds are useful starting materials or intermediates in the synthesis of more complex organic molecules.
摘要翻译：本发明有利地提供缩酮官能化合物，其在与缩酮基团相容的条件下可以是强亲电体，在室温下是稳定的，结晶固体，并且比酮碘化物更安全。本发明通过将芳香族磺酰部分引入缩酮功能材料来实现。这些化合物是合成更复杂有机分子的有用起始原料或中间体。

5. 发明授权

US07439222B2 Process and systems for peptide synthesis 有权
标题翻译：肽合成的方法和系统
公开(公告)号：US07439222B2
公开(公告)日：2008-10-21
申请号：US11021952
申请日：2004-12-23
申请人： Martin R. Guinn , Lewis M. Hodges , David A. Johnston , Hendrick Moorlag , Mark A. Schwindt
发明人： Martin R. Guinn , Lewis M. Hodges , David A. Johnston , Hendrick Moorlag , Mark A. Schwindt
IPC分类号： A01N37/18 , A61K38/00
CPC分类号： C07K1/04 , C07K1/026 , Y02P20/55
摘要： The invention provides methods of synthesizing peptides, involving the steps of providing a composition including a peptide fragment, wherein the peptide fragment has at least one amino acid residue and includes a base-sensitive, N-terminal protecting group; removing the base-sensitive, N-terminal protecting group from the peptide fragment using a deprotection reagent that includes a base, whereby an N-terminal functionality on the peptide fragment is deprotected; removing the base from the composition to provide a residual base content of more than 100 ppm; causing a reactive peptide fragment having a reactive C-terminus and a base-sensitive N-terminal protecting group to react with the deprotected N-terminal functionality of the peptide fragment under conditions such that the reactive peptide fragment is added to the peptide fragment; and optionally repeating the deprotection and coupling steps until a desired peptide is obtained. Also provided are methods of synthesizing peptides, wherein base is removed from the composition to a point where the composition would provide a positive chloranil test. Also provided are methods of synthesizing peptides, wherein coupling is performed in basic reaction mixtures.
摘要翻译：本发明提供了合成肽的方法，包括提供包含肽片段的组合物的步骤，其中肽片段具有至少一个氨基酸残基并且包括碱敏感的N-末端保护基; 使用包含碱的去保护试剂从肽片段中除去碱敏感的N-末端保护基，从而将肽片段上的N-末端官能团去保护; 从组合物中除去碱以提供大于100ppm的残留碱含量; 使得具有反应性C末端和碱敏感性N末端保护基团的反应性肽片段与肽片段的去保护的N末端官能团反应，使得将反应性肽片段加入到肽片段中; 并任选地重复脱保护和偶联步骤，直至获得所需的肽。还提供了合成肽的方法，其中将碱从组合物中除去至组合物将提供正氯醌测试的程度。还提供了合成肽的方法，其中在碱性反应混合物中进行偶联。

6. 发明授权

US06743927B2 Synthesis of 3,6-dialkyl-5,6-dihydro-4-hydroxy-pyran-2-one 有权
公开(公告)号：US06743927B2
公开(公告)日：2004-06-01
申请号：US10364547
申请日：2003-02-10
申请人： Michael P. Fleming , Yeun-Kwei Han , Lewis M. Hodges , David A. Johnston , Roger P. Micheli , Kurt Puentener , Chris R. Roberts , Michelangelo Scalone , Mark A. Schwindt , Robert J. Topping
发明人： Michael P. Fleming , Yeun-Kwei Han , Lewis M. Hodges , David A. Johnston , Roger P. Micheli , Kurt Puentener , Chris R. Roberts , Michelangelo Scalone , Mark A. Schwindt , Robert J. Topping
IPC分类号： C07D30932
CPC分类号： C07F3/02 , C07B2200/07 , C07C67/30 , C07C67/31 , C07D305/12 , C07D309/32 , C07C69/716 , C07C69/675
摘要： The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&dgr;-lactone.

7. 发明授权

US06858749B2 Synthesis of 3,6-dialkyl-5,6-dihydro-4-hydroxy-pyran-2-one 有权
标题翻译： 3,6-二烷基-5,6-二氢-4-羟基 - 吡喃-2-酮的合成
公开(公告)号：US06858749B2
公开(公告)日：2005-02-22
申请号：US10364536
申请日：2003-02-10
申请人： Michael P. Fleming , Yeun-Kwei Han , Lewis M. Hodges , David A. Johnston , Roger P. Micheli , Kurt Puentener , Chris R. Roberts , Michelangelo Scalone , Mark A. Schwindt , Robert J. Topping
发明人： Michael P. Fleming , Yeun-Kwei Han , Lewis M. Hodges , David A. Johnston , Roger P. Micheli , Kurt Puentener , Chris R. Roberts , Michelangelo Scalone , Mark A. Schwindt , Robert J. Topping
IPC分类号： C07B61/00 , C07C67/30 , C07C67/31 , C07D305/12 , C07D309/32 , C07F3/02 , C07C69/66
CPC分类号： C07F3/02 , C07B2200/07 , C07C67/30 , C07C67/31 , C07D305/12 , C07D309/32 , C07C69/716 , C07C69/675
摘要： The present invention relates to a novel process for producing a δ-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-δ-lactone.
摘要翻译：本发明涉及用于制备下式的δ-内酯的新方法：使用下式的酰卤：其中R 1，R 2，R 3和X在本文中描述，以及新颖的中间体。特别地，本发明涉及对映选择性地制备（R） - 内酯的方法。

8. 发明授权

US06545165B1 Synthesis of 3,6-dialkyl-5,6-dihydro-4-hydroxy-pyran-2-one 有权
标题翻译： 3,6-二烷基-5,6-二氢-4-羟基 - 吡喃-2-酮的合成
公开(公告)号：US06545165B1
公开(公告)日：2003-04-08
申请号：US09668834
申请日：2000-09-22
申请人： Michael P. Fleming , Yeun-Kwei Han , Lewis M. Hodges , David A. Johnston , Roger P. Micheli , Kurt Puentener , Chris R. Roberts , Michelangelo Scalone , Mark A. Schwindt , Robert J. Topping
发明人： Michael P. Fleming , Yeun-Kwei Han , Lewis M. Hodges , David A. Johnston , Roger P. Micheli , Kurt Puentener , Chris R. Roberts , Michelangelo Scalone , Mark A. Schwindt , Robert J. Topping
IPC分类号： C07D30932
CPC分类号： C07F3/02 , C07B2200/07 , C07C67/30 , C07C67/31 , C07D305/12 , C07D309/32 , C07C69/716 , C07C69/675
摘要： The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&dgr;-lactone.
摘要翻译：本发明涉及用于制备下式的δ-内酯的新方法：使用下式的酰卤：其中R1，R2 R3和X如本文所述，以及新的中间体。特别地，本发明涉及对映选择性地制备（R） - 内酯的方法。

9. 发明授权

US06818789B2 Synthesis of 3,6-dialkyl-5,6-dihydro-4-hydroxy-pyran-2-one 有权
标题翻译： 3,6-二烷基-5,6-二氢-4-羟基 - 吡喃-2-酮的合成
公开(公告)号：US06818789B2
公开(公告)日：2004-11-16
申请号：US10364692
申请日：2003-02-10
申请人： Michael P. Fleming , Yeun-Kwei Han , Lewis M. Hodges , David A. Johnston , Roger P. Micheli , Kurt Puentener , Chris R. Roberts , Michelangelo Scalone , Mark A. Schwindt , Robert J. Topping
发明人： Michael P. Fleming , Yeun-Kwei Han , Lewis M. Hodges , David A. Johnston , Roger P. Micheli , Kurt Puentener , Chris R. Roberts , Michelangelo Scalone , Mark A. Schwindt , Robert J. Topping
IPC分类号： C07C6966
CPC分类号： C07F3/02 , C07B2200/07 , C07C67/30 , C07C67/31 , C07D305/12 , C07D309/32 , C07C69/716 , C07C69/675
摘要： The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&dgr;-lactone.
摘要翻译：本发明涉及用于制备下式的δ-内酯的新方法：使用下式的酰卤：其中R 1，R 2，R 3和X在本文中描述，以及新颖的中间体。特别地，本发明涉及对映选择性地制备（R） - 内酯的方法。

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