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1. 发明授权

US07579481B2 Method of making imidazole-2-ones and 2-thiones 有权
标题翻译：制备咪唑-2-酮和2-噻吩的方法
公开(公告)号：US07579481B2
公开(公告)日：2009-08-25
申请号：US11467292
申请日：2006-08-25
申请人： Michael E. Garst , Lloyd Dolby , Shervin Esfandiari
发明人： Michael E. Garst , Lloyd Dolby , Shervin Esfandiari
IPC分类号： A61K31/4166 , C07D233/32
CPC分类号： C07D233/84 , C07D233/70
摘要： A method of 4-substituted imidazole-2-ones and thiones which comprises reacting a methylene urea or methylene thiourea wherein said methylene is substituted with the 4-subsituent and a cyano or alkycarboxylate group to provide said 4-substituted imidazole 2-one or thione.
摘要翻译：一种4-取代咪唑-2-酮和硫杂的方法，其包括使亚甲基脲或亚甲基硫脲与4-取代基和氰基或烷基羧酸酯基团取代的亚甲基硫脲反应，以提供所述4-取代的咪唑-2-酮或硫酮。

2. 发明授权

US07880017B2 Process for the synthesis of imidazoles 有权
标题翻译：合成咪唑的方法
公开(公告)号：US07880017B2
公开(公告)日：2011-02-01
申请号：US11744564
申请日：2007-05-04
申请人： Lloyd J. Dolby , Shervin Esfandiari , Michael E. Garst
发明人： Lloyd J. Dolby , Shervin Esfandiari , Michael E. Garst
IPC分类号： C07D233/66
CPC分类号： C07F7/0814
摘要： The present invention provides a process for the preparation of imidazoles by reacting a cyano compound with a silylalkylisocyanide compound. Such imidazoles are useful pharmacologically-active compounds and/or intermediates for the preparation of pharmacologically-active compounds.
摘要翻译：本发明提供通过使氰基化合物与甲硅烷基烷基异氰化合物反应制备咪唑的方法。这样的咪唑是用于制备药理学活性化合物的有用的药理学活性化合物和/或中间体。

3. 发明授权

US07919630B2 Synthesis of imidazole 2-thiones via thiohydantoins 有权
标题翻译：通过硫代乙内酰脲合成咪唑2-硫杂
公开(公告)号：US07919630B2
公开(公告)日：2011-04-05
申请号：US11468187
申请日：2006-08-29
申请人： Michael E. Garst , Lloyd J. Dolby , Shervin Esfandiari , Alfred A. Avey, Jr. , Vivian Rose MacKenzie , Charles David Muchmore
发明人： Michael E. Garst , Lloyd J. Dolby , Shervin Esfandiari , Alfred A. Avey, Jr. , Vivian Rose MacKenzie , Charles David Muchmore
IPC分类号： C07D233/84 , C07D233/86
CPC分类号： C07D233/84
摘要： The present invention provides a method of making an imidazole 2-thione which comprises the step(s) of reducing a thiohydantoin to said imidazole-2-thione.
摘要翻译：本发明提供一种制备咪唑2-硫酮的方法，其包括将硫代乙内酰脲还原为所述咪唑-2-硫酮的步骤。

4. 发明授权

US5675019A Process for making piloloctam and derivatives thereof 失效
标题翻译：吡罗克定及其衍生物的制备方法
公开(公告)号：US5675019A
公开(公告)日：1997-10-07
申请号：US685897
申请日：1996-07-18
申请人： Lloyd J. Dolby , Nestor A. Fedoruk , Shervin Esfandiari , Michael E. Garst
发明人： Lloyd J. Dolby , Nestor A. Fedoruk , Shervin Esfandiari , Michael E. Garst
IPC分类号： C07D207/26 , C07D207/267
CPC分类号： C07D207/26
摘要： A process of preparing lactam derivatives of pilocarpine is disclosed. The process involves condensation of a dihydroxybutene and alkyl orthoester to form a lactone intermediate which is oxidized to trans-pilopic acid. This lactone ring is reacted with a benzylamine and the benzyl group removed with a novel dissolving metal reduction mixture to yield the key intermediate IV ##STR1## which can be elaborated to pilolactam through a known sequence of steps.
摘要翻译：公开了制备毛果芸香碱内酰胺衍生物的方法。该方法涉及二羟基丁烯和烷基原酸酯的缩合形成内酯中间体，其被氧化成反式吡啶酸。该内酯环与苄胺反应，并用新的溶解金属还原混合物除去苄基，得到关键的中间体式IV，其可以通过已知的步骤顺序制备成吡咯酰胺。

5. 发明授权

US07598394B2 Process for the synthesis of imidazoles 有权
标题翻译：合成咪唑的方法
公开(公告)号：US07598394B2
公开(公告)日：2009-10-06
申请号：US11623693
申请日：2007-01-16
申请人： Lloyd J. Dolby , Shervin Esfandiari , Michael E. Garst
发明人： Lloyd J. Dolby , Shervin Esfandiari , Michael E. Garst
IPC分类号： C07D233/66 , A61K31/4174
CPC分类号： C07D233/56 , C07D233/64 , C07D401/04 , C07D409/04
摘要： The present invention provides a process for the preparation of imidazoles by reacting a cyano compound with a silylalkylisocyanide compound. Such imidazoles are useful pharmacologically-active compounds and/or intermediates for the preparation of pharmacologically-active compounds.
摘要翻译：本发明提供通过使氰基化合物与甲硅烷基烷基异氰化合物反应制备咪唑的方法。这样的咪唑是用于制备药理学活性化合物的有用的药理学活性化合物和/或中间体。

6. 发明授权

US07183305B2 Process for the synthesis of imidazoles 有权
标题翻译：合成咪唑的方法
公开(公告)号：US07183305B2
公开(公告)日：2007-02-27
申请号：US10706474
申请日：2003-11-11
申请人： Lloyd J. Dolby , Shervin Esfandiari , Michael E. Garst
发明人： Lloyd J. Dolby , Shervin Esfandiari , Michael E. Garst
IPC分类号： A61K31/4164 , C07D233/64
CPC分类号： C07D233/56 , C07D233/64 , C07D401/04 , C07D409/04
摘要： The present invention provides a process for the preparation of imidazoles by reacting a cyano compound with a silylalkylisocyanide compound. Such imidazoles are useful pharmacologically-active compounds and/or intermediates for the preparation of pharmacologically-active compounds.
摘要翻译：本发明提供通过使氰基化合物与甲硅烷基烷基异氰化合物反应制备咪唑的方法。这样的咪唑是用于制备药理学活性化合物的有用的药理学活性化合物和/或中间体。

7. 发明授权

US5675038A Lithium and amine dissolving metal reduction 失效
标题翻译：锂和胺溶解金属还原
公开(公告)号：US5675038A
公开(公告)日：1997-10-07
申请号：US685902
申请日：1996-07-18
申请人： Lloyd J. Dolby , Nestor A. Fedoruk , Shervin Esfandiari , Natalie C. Chamberlain , Michael E. Garst
发明人： Lloyd J. Dolby , Nestor A. Fedoruk , Shervin Esfandiari , Natalie C. Chamberlain , Michael E. Garst
IPC分类号： C07B31/00 , C07C5/11 , C07C13/48 , C07C29/132 , C07C31/137 , C07C41/18 , C07C41/20 , C07C43/188 , C07C45/41 , C07C45/62 , C07C47/32 , C07C209/40 , C07C209/44 , C07C209/48 , C07C209/50 , C07C209/52 , C07C211/07 , C07C211/17 , C07C211/35 , C07C211/48 , C07C231/08 , C07C231/12 , C07C233/05 , C07C319/02 , C07C319/06 , C07C321/26 , C07D233/06 , C07D233/10 , C07D403/06 , C07C291/00
CPC分类号： C07C5/11 , C07B31/00 , C07C209/40 , C07C209/48 , C07C209/50 , C07C209/52 , C07C231/08 , C07C231/12 , C07C29/132 , C07C319/02 , C07C319/06 , C07C41/18 , C07C45/41 , C07C45/62 , C07D233/06 , C07D233/10 , C07C2101/16 , C07C2102/10 , C07C2103/74
摘要： The invention is directed to a process for reducing or reductively cleaving an organic compound susceptible to dissolving metal reduction comprising exposing the organic compound to a solution of lithium in a polyamine including at least two amino groups, selected from the group consisting of primary and secondary amino groups and mixtures thereof, e.g. ethylenediamine and R--NH.sub.2, optionally containing a lower alkyl alcohol, wherein R is chosen from the group consisting of ethyl, propyl, and butyl, including all straight and branched chain isomers thereof, for a time sufficient to effect reduction.
摘要翻译：本发明涉及减少或还原性裂解易溶解金属还原的有机化合物的方法，其包括将有机化合物暴露于含有至少两个氨基的多胺中的锂溶液，所述多胺选自伯和仲氨基基团及其混合物，例如乙二胺和R-NH 2，任选地含有低级烷基醇，其中R选自乙基，丙基和丁基，包括其所有直链和支链异构体在足以实现还原的时间。

8. 发明授权

US07294716B2 Process for preparing isomerically pure prodrugs of proton pump inhibitors 失效
标题翻译：制备质子泵抑制剂的异构纯的前体药物的方法
公开(公告)号：US07294716B2
公开(公告)日：2007-11-13
申请号：US10891317
申请日：2004-07-13
申请人： Michael E. Garst , Lloyd Jay Dolby , Shervin Esfandiari , Vivian Rose MacKenzie , Alfred Arthur Avey, Jr. , David Charles Muchmore , Geoffrey Kenneth Cooper , Thomas C. Malone
发明人： Michael E. Garst , Lloyd Jay Dolby , Shervin Esfandiari , Vivian Rose MacKenzie , Alfred Arthur Avey, Jr. , David Charles Muchmore , Geoffrey Kenneth Cooper , Thomas C. Malone
IPC分类号： C07D401/12 , C07D401/14 , C07D409/14
CPC分类号： C07D401/12 , C04B35/632
摘要： Synthetic methods for preparing isomerically pure N-arylsulfonyl derivatives of proton pump inhibitors which include a substituted benzimidazole nucleus are shown by the synthetic schemes and experimental description.
摘要翻译：通过合成方案和实验描述显示了用于制备包含取代的苯并咪唑核的质子泵抑制剂异构纯的N-芳基磺酰基衍生物的合成方法。

9. 发明授权

US07115748B2 Method of making imidazole-2-thiones 有权
公开(公告)号：US07115748B2
公开(公告)日：2006-10-03
申请号：US11007454
申请日：2004-12-07
申请人： Michael E. Garst , Lloyd Jay Dolby , Shervin Esfandiari , Alfred Arthur Avey, Jr.
发明人： Michael E. Garst , Lloyd Jay Dolby , Shervin Esfandiari , Alfred Arthur Avey, Jr.
IPC分类号： C07D233/42
CPC分类号： C07D233/42 , C07D405/04 , C07D409/04
摘要： The present invention provides a method of making an imidazole-2-thione which comprises the steps of reacting a vicinal diamine with a compound having a thiocarbonyl moiety and oxidizing the resulting reaction product to obtain said imidazole-2-thione.

10. 发明授权

US5418234A Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives 失效
标题翻译：使用（2-咪唑啉-2-基氨基）喹喔啉衍生物的方法
公开(公告)号：US5418234A
公开(公告)日：1995-05-23
申请号：US298494
申请日：1994-08-30
申请人： Charles Gluchowski , Michael E. Garst , James A. Burke , Larry A. Wheeler , Michael E. Garst
发明人： Charles Gluchowski , Michael E. Garst , James A. Burke , Larry A. Wheeler , Michael E. Garst
IPC分类号： A61K31/495 , C07D403/12 , A61K31/50
CPC分类号： C07D403/12 , A61K31/495 , Y10S514/816 , Y10S514/854 , Y10S514/93
摘要： A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.4 are independently selected from the group consisting of H and alkyl radicals having 1 to 4 carbon atoms; the R.sub.2 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the R.sub.3 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the 2-imidazolin-2-ylamino group may be in any of the 5-, 6, 7- or 8-positions of the quinoxaline nucleus; and R.sub.5, R.sub.6 and R.sub.7 each is located in one of the remaining 5-, 6-, 7- or 8-positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals having 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain and reduction in or prevention of at least one effect of ischemia.
摘要翻译：治疗哺乳动物的方法包括向哺乳动物施用有效量以在哺乳动物中提供所需治疗效果，所述化合物选自下列化合物：具有下式的那些化合物：其药学上可接受的酸加成盐及其混合物，其中R 1和R 4独立地选自H和具有1至4个碳原子的烷基; R 2独立地选自H或具有1至4个碳原子的烷基，或者一起是氧代; R 3独立地选自H或具有1至4个碳原子的烷基，或者一起是氧代; 2-咪唑啉-2-基氨基可以在喹喔啉核的5-，6-或7-位中的任一个中; 并且R5，R6和R7各自位于喹喔啉核的剩余的5-，6-，7-或8-位中的一个，并且独立地选自Cl，Br，H和具有1至 3个碳原子。当向哺乳动物施用时，这些化合物提供期望的治疗效果，例如减少外周疼痛和减少或预防至少一种局部缺血的作用。

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