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1. 发明授权

US06555686B2 Asymmetric synthesis of quinazolin-2-ones useful as HIV reverse transcriptase inhibitors 失效
公开(公告)号：US06555686B2
公开(公告)日：2003-04-29
申请号：US09909731
申请日：2001-07-20
申请人： Rodney L. Parsons , Roberta L. Dorow , Akin H. Davulcu , Joseph M. Fortunak , Gregory D. Harris , Goss S. Kauffman , William A. Nugent , Lilian A. Radesca
发明人： Rodney L. Parsons , Roberta L. Dorow , Akin H. Davulcu , Joseph M. Fortunak , Gregory D. Harris , Goss S. Kauffman , William A. Nugent , Lilian A. Radesca
IPC分类号： C07D23972
CPC分类号： C07D239/80
摘要： This invention relates generally to the asymmetric synthesis of quinazolin-2-ones that are useful as inhibitors of HIV reverse transcriptase. The synthesis is accomplished through the chiral ligand mediated addition of cyclopropylacetylide.

2. 发明授权

US5530124A Method for preparing cyclic ureas and their use for the synthesis of HIV protease inhibitors 失效
标题翻译：制备环脲的方法及其用于合成HIV蛋白酶抑制剂的用途
公开(公告)号：US5530124A
公开(公告)日：1996-06-25
申请号：US269320
申请日：1994-06-30
申请人： Lilian A. Radesca , Gregory D. Harris , Edward K. W. Wat , Robert E. Waltermire
发明人： Lilian A. Radesca , Gregory D. Harris , Edward K. W. Wat , Robert E. Waltermire
IPC分类号： C07C221/00 , C07C223/02 , C07D491/04 , C07D491/056
CPC分类号： C07D491/04 , C07C221/00 , C07C223/02
摘要： This invention provides improved synthetic processes for the preparation of hydroxy-protected cyclic urea compounds of Formula (IX), ##STR1## which are useful as intermediates for the preparation of cyclic urea human immunodeficiency virus (HIV) protease inhibitors, from N-protected aminoaldehydes. The processes of the present invention provide high yields, can be conducted on multikilogram scale, and eliminate the need for chromatographic purification of intermediates or final product.
摘要翻译：本发明提供改进的制备式（IX）的羟基保护的环状脲化合物的合成方法，其可用作从N-保护的氨基醛制备环状尿素人免疫缺陷病毒（HIV）蛋白酶抑制剂的中间体。本发明的方法提供高产率，可以在多千克规模上进行，并且不需要中间体或最终产物的色谱纯化。

3. 发明授权

US06218534B1 Preparation of asymmetric cyclic ureas through a monoacylated diamine intermediate 有权
标题翻译：通过单酰化二胺中间体制备不对称环脲
公开(公告)号：US06218534B1
公开(公告)日：2001-04-17
申请号：US09166507
申请日：1998-10-05
申请人： Benjamin R. P. Stone , Luigi Anzalone , Joseph M. Fortunak , Gregory D. Harris , Ioannis I. Valvis , Robert E. Waltermire
发明人： Benjamin R. P. Stone , Luigi Anzalone , Joseph M. Fortunak , Gregory D. Harris , Ioannis I. Valvis , Robert E. Waltermire
IPC分类号： C07D40310
CPC分类号： C07D491/04 , C07D243/04 , C07D317/14
摘要： A process for the preparation of asymmetric cyclic ureas of Formula (VI) starting from the diamine of Formula (I). In the process, a compound of Formual (I), wherein G is a group selected from —C(—CH2CH2CH2CH2CH2—)—, —C(CH2CH3)2—, —C(CH3)(CH2CH3)—, —C(CH2CH2CH2CH3)2—, —C(CH3)(CH2CH(CH3)CH3)—, —CH(phenyl)—, —CH2—, —C(CH3)2—, and —C(OCH3)(CH2CH2CH3)—, is selectively monoacylated with an acylating agent to give an asymmetric monoacylated diamine, 2) the asymmetric monoacylated diamine is contacted with an aldehdye and a reducing agent to form a monoalkylated monoacylated diamine, 3) the monoalkylated monoacylated diamine is contacted with a strong base to form a monoalkylated de-acylated diamine, 4) the monoalkylated de-acylated diamine is contacted with 3-cyano-4-fluoro-benzaldehyde and a reducing agent to form a dialkylated diamine, and 5) the dialkylated diamine is contacted with phosgene in the presence of a base to form a compound of Formula (VI). The invention allows for scalable preparation of a wide variety of asymmetrical cyclic ureas useful as HIV protease inhibitors for the treatment of HIV infection.
摘要翻译：从式（I）的二胺开始制备式（VI）的不对称环脲的方法。在该方法中，式（I）的化合物，其中G是选自-C（-CH 2 CH 2 CH 2 CH 2 CH 2 - ） - ， - C（CH 2 CH 3）2 - ， - C（CH 3）（CH 2 CH 3） - ， - C（CH 2 CH 2 CH 2 CH 3 ） - ， - C（CH 3）（CH 2 CH（CH 3）CH 3） - ， - CH（苯基） - ， - CH 2 - ， - C（CH 3）2 - 和-C（OCH 3）（CH 2 CH 2 CH 3）用酰化剂单酰化以产生不对称的单酰化二胺，2）不对称单酰化二胺与醛缩二乙醇和还原剂接触以形成单烷基化单酰化二胺，3）单烷基化单酰化二胺与强碱接触以形成单烷基化去酰化二胺，4）使单烷基化的脱酰基二胺与3-氰基-4-氟 - 苯甲醛和还原剂接触以形成二烷基化二胺，和5）二烷基化二胺在光气存在下与光气接触碱形成式（VI）的化合物。本发明允许可扩展地制备用作治疗HIV感染的HIV蛋白酶抑制剂的各种不对称环脲。

4. 发明授权

US06452000B2 Preparation of asymmetric cyclic ureas through a monoacylated diamine intermediate 有权
标题翻译：通过单酰化二胺中间体制备不对称环脲
公开(公告)号：US06452000B2
公开(公告)日：2002-09-17
申请号：US09801137
申请日：2001-03-07
申请人： Benjamin R. P. Stone , Luigi Anzalone , Joseph M. Fortunak , Gregory D. Harris , Ioannis I. Valvis , Robert E. Waltermire
发明人： Benjamin R. P. Stone , Luigi Anzalone , Joseph M. Fortunak , Gregory D. Harris , Ioannis I. Valvis , Robert E. Waltermire
IPC分类号： C07D31772
CPC分类号： C07D491/04 , C07D243/04 , C07D317/14
摘要： The present invention concerns an improved process for the preparation of asymmetric cyclic ureas as well as intermediates in the preparation of asymmetric cyclic ureas. In the process, a diamine of formula (I-a) is selectively monoacylated to give an asymmetric monoacylated diamine which can be converted into asymmetric intermediates. The asymmetric intermediates can be further alkylated, cyclized, and/or modified to give compounds which are useful as HIV protease inhibitors for the treatment of HIV infection. The invention allows for scalable preparation of a wide variety of asymmetrical cyclic ureas.
摘要翻译：本发明涉及制备不对称环脲的改进方法以及制备不对称环脲的中间体。在该方法中，式（I-a）的二胺选择性单酰化，得到不对称单酰化二胺，其可以转化为不对称中间体。不对称中间体可以进一步烷基化，环化和/或修饰，得到可用作HIV蛋白酶抑制剂用于治疗HIV感染的化合物。本发明允许可扩展地制备各种不对称的环状尿素。

5. 发明授权

US5072008A Manufacture of lactol derivatives 失效
标题翻译： LACTOL衍生物的制造
公开(公告)号：US5072008A
公开(公告)日：1991-12-10
申请号：US365699
申请日：1989-06-14
申请人： Gregory D. Harris
发明人： Gregory D. Harris
IPC分类号： C07D307/30 , C07C45/59 , C07C47/27 , C07C47/273 , C07C47/277 , C07C59/48 , C07C205/44 , C07D307/20 , C07D307/33
CPC分类号： C07D307/20 , C07C201/12 , C07C45/59 , C07C47/27 , C07C47/273 , C07C47/277
摘要： The invention concerns a novel process for the stereospecific manufacture of novel hydroxymethyl lactols of the formula I by a one step reduction of a corresponding lactone carboxylic ester of the formula II (many of which esters are novel) using a reducing agent such as diisobutylaluminium hydride at about ambient temperature. The lactols of formula I are intermediates for the production of pharmacologically active 1,3-dioxane alkenoic acids useful in the treatment of certain cardiovascular and pulmonary medical conditions. Certain of the esters of formula II are novel and are also included in the invention.

6. 发明授权

US4789789A Event distribution and combination system 失效
标题翻译：事件分配和组合系统
公开(公告)号：US4789789A
公开(公告)日：1988-12-06
申请号：US830596
申请日：1986-02-17
申请人： Michael D. Kersenbrock , David A. Lowry , Gregory D. Harris , Michael D. Henry , Francis D. Kohlmeier
发明人： Michael D. Kersenbrock , David A. Lowry , Gregory D. Harris , Michael D. Henry , Francis D. Kohlmeier
IPC分类号： G06F13/14 , G05B19/02 , G05B19/045 , H02J1/00
CPC分类号： G05B19/045 , Y02P80/15 , Y10T307/461 , Y10T307/477
摘要： An apparatus for generating trigger signals responsive to a selected pattern of event detection signals, the apparatus comprising an interim function bus, programmable means to selectively energize conductors of the interim function bus on detection of the selected event detection signal pattern, and programmable means to generate the trigger signal on detection of a selected pattern of interim function bus signals. The generating means are programmed for pattern recognition by binary data appearing on control lines from a shift register, the shift register being loaded by serial data from external control circuits. The apparatus also includes provisions for synchronizing the generation of signal patterns on the interim function bus to a system clock, and for synchronizing the generation of trigger signals to clocks associated with triggerable devices.
摘要翻译：一种用于响应于所选择的事件检测信号模式产生触发信号的装置，所述装置包括临时功能总线，用于在检测所选择的事件检测信号模式时选择性地激励临时功能总线的导体的可编程装置，以及可编程装置，触发信号检测到所选择的临时功能总线信号模式。生成装置被编程为通过出现在来自移位寄存器的控制线上的二进制数据进行模式识别，移位寄存器由来自外部控制电路的串行数据加载。该装置还包括用于将临时功能总线上的信号模式的产生同步到系统时钟的规定，并且用于将触发信号的产生与与可触发装置相关联的时钟同步。

7. 发明授权

US5169974A Process for manufacturing aryloxyaldehydes 失效
标题翻译：制备芳氧醛的方法
公开(公告)号：US5169974A
公开(公告)日：1992-12-08
申请号：US424615
申请日：1989-10-20
申请人： Gregory D. Harris , Stanley A. Lee
发明人： Gregory D. Harris , Stanley A. Lee
IPC分类号： C07C45/43 , C07C45/58 , C07C45/64 , C07C47/198 , C07C47/277 , C07C255/54 , C07C319/14 , C07C323/22
CPC分类号： C07C323/22 , C07C255/54 , C07C319/14 , C07C45/43 , C07C45/58 , C07C47/277
摘要： The invention concerns a novel process for the manufacture of various aryloxyaliphatic aldehydes and related arylthio analogues, which are useful as chemical intermediates. The process involves reacting a dihalogenohydroxyalkane of the formula: HO.C(R.sup.2).sub.2.CHX.sub.2 wherein R.sup.2 is alkyl and X is chloro or bromo with a phenol or thiophenol in the presence of base and is applicable to large scale use.
摘要翻译：本发明涉及用于制备各种芳氧脂肪醛和相关芳硫基类似物的新方法，其可用作化学中间体。该方法包括在碱存在下使下式HO.C（R2）2.CHX2的二卤代羟基烷烃与苯酚或苯硫酚反应，其中R2为烷基，X为氯或溴，并适用于大规模应用。

8. 发明授权

US5510495A Process for the isolation and purification of ester functionalized imidazole intermediates by selective hydrolysis 失效
标题翻译：通过选择性水解分离和纯化酯官能化咪唑中间体的方法
公开(公告)号：US5510495A
公开(公告)日：1996-04-23
申请号：US307441
申请日：1994-09-19
申请人： Gregory D. Harris
发明人： Gregory D. Harris
IPC分类号： C07D233/90 , C07D403/10 , C07D233/68
CPC分类号： C07D403/10 , C07D233/90
摘要： A method for isolating and purifying an ester functionalized imidazole compound, useful as an angiotensin (II) antagonist or as a key intermediate therefor, from a mixture of it with its regioisomer in a solvent, by treatment with an alkali metal hydroxide to achieve the regioselective hydrolysis of the undesired regioisomeric ester.
摘要翻译：通过用碱金属氢氧化物处理来分离和纯化可用作血管紧张素（II）拮抗剂或其作为关键中间体的酯官能化咪唑化合物与其区域异构体在溶剂中的混合物的方法，以实现区域选择性不期望的区域异构酯的水解。

9. 发明授权

US5519143A Process for the isolation and purification of an imidazole stereoisomer from a mixture of stereoisomers by selective precipitation 失效
标题翻译：通过选择性沉淀从立体异构体的混合物中分离和纯化咪唑立体异构体的方法
公开(公告)号：US5519143A
公开(公告)日：1996-05-21
申请号：US360248
申请日：1994-09-19
申请人： Gregory D. Harris
发明人： Gregory D. Harris
IPC分类号： C07D233/54 , C07D233/68 , C07D233/90 , C07D403/10 , C07D233/66 , C07D401/10
CPC分类号： C07D233/64 , C07D233/90 , C07D403/10
摘要： A method for the isolation and purification of an imidazole compound, useful as an angiotensin II receptor inhibitor compound or as a key intermediate therefor, from a mixture of it with its regioisomer in a solvent by treament of the mixture with a strong acid to effect selective precipitation of the desired regioisomeric imidazole salt.
摘要翻译：一种用于分离和纯化可用作血管紧张素II受体抑制剂化合物或其作为关键中间体的咪唑化合物的方法，其混合物与其区域异构体在溶剂中的混合物通过混合物与强酸的混合物来实现选择性所需的区域异构咪唑盐的沉淀。

10. 发明授权

US5492905A 1-bolizazepin-2,5-diones 失效
标题翻译：治疗组合物
公开(公告)号：US5492905A
公开(公告)日：1996-02-20
申请号：US74907
申请日：1993-06-10
申请人： Gregory D. Harris , Marc J. Chapdelaine , Paul F. Jackson
发明人： Gregory D. Harris , Marc J. Chapdelaine , Paul F. Jackson
IPC分类号： A61K31/55 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/28 , C07D223/16 , C07D401/04 , C07D403/04 , C07D403/12
CPC分类号： C07D223/16 , A61K31/55 , C07D401/04 , C07D403/04 , C07D403/12
摘要： Benz[b]azepine compounds, pharmaceutical compositions containing them and methods for the treatment of neurological disorders utilizing them.
摘要翻译：苯并[b]吖庚因化合物，含有它们的药物组合物和用于治疗利用它们的神经障碍的方法。

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