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1. 发明申请

US20120209000A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：US20120209000A1
公开(公告)日：2012-08-16
申请号：US13450784
申请日：2012-04-19
申请人： Brian Alvin JOHNS , Yasunori Aoyama , Hiroshi Yoshida , Yoshiyuki Taoda
发明人： Brian Alvin JOHNS , Yasunori Aoyama , Hiroshi Yoshida , Yoshiyuki Taoda
IPC分类号： C07D471/22
CPC分类号： C07D471/14
摘要： The present invention is directed to a compound of the formula: The compound is useful as an intermediate for preparing an HIV drug.
摘要翻译：本发明涉及下式的化合物：该化合物可用作制备HIV药物的中间体。

2. 发明授权

US08183372B2 Substituted 9,11-dioxo-2,3,4a,5,9,11,13,13a-octahydor-1H-pyrido[1,2-a]pyrrolo[1′,2′:3,4]imidazo[1,2-d]pyrazines 有权
标题翻译：取代的9,11-二氧代-2,3,4a，5,9,11,13,13a-八氢-1H-吡啶并[1,2-a]吡咯并[1'，2'：3,4]咪唑并[1 ，2-d]吡嗪
公开(公告)号：US08183372B2
公开(公告)日：2012-05-22
申请号：US13055046
申请日：2009-07-23
申请人： Brian Alvin Johns , Yasunori Aoyama , Hiroshi Yoshida , Yoshiyuki Taoda
发明人： Brian Alvin Johns , Yasunori Aoyama , Hiroshi Yoshida , Yoshiyuki Taoda
IPC分类号： C07D241/36
CPC分类号： C07D471/14
摘要： The present invention is directed to a process for the preparation of a compound of formula 1b which compound is useful as a prodrug of HIV integrase inhibitors and therefore is useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC. The process includes the steps of a) brominating a compound of formula P-7 to form a compound of formula P-8, b) treating a compound of formula P-8 with NaIO4 to form a compound of formula P-9, c) reacting a compound of formula P-9 with [(2R)-pyrrolidinylmethyl]amine of formula to form a compound of formula P-10, d) reacting a compound of formula P-10 with 2, 4-difluorobenzylamine to form a compound of formula P-11, e) treating a compound of P-11 with palladium on carbon and ammonium hydroxide to form a compound of formula 1a, and f) treating a compound of formula 1a with NaOH and ethanol to form a compound of formula 1b. The structures of the above mentioned compounds are disclosed in the specification.
摘要翻译：本发明涉及一种制备式1b化合物的方法，该化合物可用作HIV整合酶抑制剂的前药，因此可用于抑制HIV复制，预防和/或治疗HIV感染，和治疗艾滋病和/或ARC。该方法包括以下步骤：a）将式P-7化合物溴化以形成式P-8的化合物，b）用NaIO 4处理式P-8的化合物以形成式P-9的化合物，c）使式P-9的化合物与式的[（2R） - 吡咯烷基甲基]胺反应形成式P-10的化合物，d）使式P-10的化合物与2,4-二氟苄胺反应，形成化合物式P-11，e）用钯碳和氢氧化铵处理P-11化合物以形成式1a化合物，和f）用NaOH和乙醇处理式1a化合物以形成式1b化合物。上述化合物的结构在说明书中公开。

3. 发明授权

US08217034B2 Chemical compounds 有权
标题翻译：化合物
公开(公告)号：US08217034B2
公开(公告)日：2012-07-10
申请号：US13054633
申请日：2009-07-23
申请人： Brian Alvin Johns , Jason Gordon Weatherhead , Toshikazu Hakogi , Yasunori Aoyama
发明人： Brian Alvin Johns , Jason Gordon Weatherhead , Toshikazu Hakogi , Yasunori Aoyama
IPC分类号： A61K31/535 , C07D498/14
CPC分类号： A61K31/535 , C07D498/14
摘要： The present invention features compounds that are prodrugs of HIIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
摘要翻译：本发明的特征在于作为HIIV整合酶抑制剂的前药的化合物，因此可用于抑制HIV复制，预防和/或治疗HIV感染以及治疗AIDS和/或ARC。

4. 发明授权

US08580967B2 Methyl 3-(benzyloxy)-1-(2,2-dihydroxyethyl)-4-oxo-1,4-dihydropyridine-2-carboxylate and processes for the preparation thereof 有权
标题翻译： 3-（苄氧基）-1-（2,2-二羟乙基）-4-氧代-1,4-二氢吡啶-2-羧酸甲酯及其制备方法
公开(公告)号：US08580967B2
公开(公告)日：2013-11-12
申请号：US13054847
申请日：2009-07-23
申请人： Brian Alvin Johns , Jason Gordon Weatherhead , Toshikazu Hakogi , Yasunori Aoyama
发明人： Brian Alvin Johns , Jason Gordon Weatherhead , Toshikazu Hakogi , Yasunori Aoyama
IPC分类号： C07D213/79
CPC分类号： A61K31/675 , A61K31/4985 , A61K31/5377 , C07D211/86 , C07D309/40 , C07D498/14 , C07F9/65583
摘要： The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the delivery of compounds for the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC. For example, the present invention includes methyl 3-(benzyloxy)-1-(2,2-dihydroxyethyl)-4-oxo-1,4-dihydropyridine-2 -carboxylate of the formula P-8: and processes for the preparation thereof.
摘要翻译：本发明的特征在于作为HIV整合酶抑制剂的前药的化合物，因此可用于递送用于抑制HIV复制，预防和/或治疗HIV感染以及治疗AIDS和/或ARC的化合物。例如，本发明包括式P-8的3-（苄氧基）-1-（2,2-二羟乙基）-4-氧代-1,4-二氢吡啶-2-羧酸甲酯：及其制备方法。

5. 发明申请

US20110183940A1 CHEMICAL COMPOUNDS 有权
标题翻译：化学化合物
公开(公告)号：US20110183940A1
公开(公告)日：2011-07-28
申请号：US13054847
申请日：2009-07-23
申请人： Brian Alvin Johns , Jason Gordon Weatherhead , Toshikazu Hakogi , Yasunori Aoyama
发明人： Brian Alvin Johns , Jason Gordon Weatherhead , Toshikazu Hakogi , Yasunori Aoyama
IPC分类号： A61K31/675 , C07D491/147 , A61K31/4985 , C07D413/14 , A61K31/5377 , C07D315/00 , C07D213/803 , A61P31/18
CPC分类号： A61K31/675 , A61K31/4985 , A61K31/5377 , C07D211/86 , C07D309/40 , C07D498/14 , C07F9/65583
摘要： The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the delivery of compounds for the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
摘要翻译：本发明的特征在于作为HIV整合酶抑制剂的前药的化合物，因此可用于递送用于抑制HIV复制，预防和/或治疗HIV感染以及治疗AIDS和/或ARC的化合物。

6. 发明申请

US20110190236A1 CHEMICAL COMPOUNDS 有权
标题翻译：化学化合物
公开(公告)号：US20110190236A1
公开(公告)日：2011-08-04
申请号：US13054633
申请日：2009-07-23
申请人： Brian Alvin Johns , Jason Gordon Weatherhead , Toshikazu Hakogi , Yasunori Aoyama
发明人： Brian Alvin Johns , Jason Gordon Weatherhead , Toshikazu Hakogi , Yasunori Aoyama
IPC分类号： A61K31/675 , C07D498/14 , A61K31/5365 , A61P31/12 , A61P31/18
CPC分类号： A61K31/535 , C07D498/14
摘要： The present invention features compounds that are prodrugs of HIIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
摘要翻译：本发明的特征在于作为HIIV整合酶抑制剂的前药的化合物，因此可用于抑制HIV复制，预防和/或治疗HIV感染以及治疗AIDS和/或ARC。

7. 发明申请

US20110245516A1 MALTOL ETHER PROCESSES AND INTERMEDIATES 有权
标题翻译： MALTOL过程和中间件
公开(公告)号：US20110245516A1
公开(公告)日：2011-10-06
申请号：US13133481
申请日：2009-12-08
申请人： Yasunori Aoyama
发明人： Yasunori Aoyama
IPC分类号： C07D309/40
CPC分类号： C07D309/38
摘要： Novel processes and intermediates are provided according to the general reaction scheme: Formula I, II, III, IV (I), (II), (III), (IV) utilizing a ruthenium catalyst in an oxidative cleavage of the triene 4 whereby an aldehyde may be produced and optionally taken on to a carboxylic acid 5: Formula V (V)
摘要翻译：根据通用反应方案提供新的方法和中间体：在三烯4的氧化裂解中使用钌催化剂的式I，II，III，IV（I），（II），（III），（IV）可以制备醛，并任选地加入到羧酸5中：式V（V）

8. 发明授权

US07930940B2 Ultrasonic transducer 有权
标题翻译：超声波换能器
公开(公告)号：US07930940B2
公开(公告)日：2011-04-26
申请号：US12007767
申请日：2008-01-15
申请人： Akira Onodera , Yasunori Aoyama
发明人： Akira Onodera , Yasunori Aoyama
IPC分类号： G01N29/00
CPC分类号： G01N29/28 , G01N29/043 , G01N29/223 , G01N29/34 , G01N2291/044 , G01N2291/101
摘要： An ultrasonic transducer incorporated into an ultrasonic inspection apparatus for examining existence of defect in a sample dipped in water comprises a transducer main part having an oscillator which projects an ultrasonic wave to the sample, receives the reflected wave from the sample and outputs the received reflected wave as an echo signal, a transmitter substrate producing a drive pulse for emitting the ultrasonic wave to the oscillator, a receiver substrate for amplifying the echo signal, a housing for containing therein both substrates electrically connected, and connecting member for electrically connecting between a signal input/output terminal and the side of the oscillator in the transducer main part, wherein, when a maximum operational frequency of the ultrasonic wave emitted from the oscillator is referred to as fmax [MHz], the connecting member is set at a length of 100/fmax [cm] or less. Even if the sample to be examined is small, a desirable defect inspection can be achieved at an excellent examination accuracy.
摘要翻译：包含在超声波检查装置中的用于检查浸入水中的样品中存在缺陷的超声波换能器包括具有将超声波投射到样品的振荡器的换能器主体，从样品接收反射波并输出接收到的反射波作为回波信号，产生用于向振荡器发射超声波的驱动脉冲的发射器基板，用于放大回波信号的接收器基板，用于容纳其中两个基板电连接的壳体和用于电连接信号输入 /输出端子和振荡器主体中的振荡器侧，其中当从振荡器发射的超声波的最大工作频率被称为fmax [MHz]时，连接构件被设置为100 / fmax [cm]以下。即使被检查样本小，也可以以良好的检查精度实现期望的缺陷检查。

9. 发明申请

US20080282805A1 Ultrasonic transducer 有权
标题翻译：超声波换能器
公开(公告)号：US20080282805A1
公开(公告)日：2008-11-20
申请号：US12007767
申请日：2008-01-15
申请人： Akira Onodera , Yasunori Aoyama
发明人： Akira Onodera , Yasunori Aoyama
IPC分类号： G01N29/00
CPC分类号： G01N29/28 , G01N29/043 , G01N29/223 , G01N29/34 , G01N2291/044 , G01N2291/101
摘要： An ultrasonic transducer incorporated into an ultrasonic inspection apparatus for examining existence of defect in a sample dipped in water comprises a transducer main part having an oscillator which projects an ultrasonic wave to the sample, receives the reflected wave from the sample and outputs the received reflected wave as an echo signal, a transmitter substrate producing a drive pulse for emitting the ultrasonic wave to the oscillator, a receiver substrate for amplifying the echo signal, a housing for containing therein both substrates electrically connected, and connecting member for electrically connecting between a signal input/output terminal and the side of the oscillator in the transducer main part, wherein, when a maximum operational frequency of the ultrasonic wave emitted from the oscillator is referred to as fmax [MHz], the connecting member is set at a length of 100/fmax [cm] or less. Even if the sample to be examined is small, a desirable defect inspection can be achieved at an excellent examination accuracy.
摘要翻译：包含在超声波检查装置中的用于检查浸入水中的样品中存在缺陷的超声波换能器包括具有将超声波投射到样品的振荡器的换能器主体，从样品接收反射波并输出接收到的反射波作为回波信号，产生用于向振荡器发射超声波的驱动脉冲的发射器基板，用于放大回波信号的接收器基板，用于容纳其中两个基板电连接的壳体和用于电连接信号输入 /输出端子和振荡器主体中的振荡器侧，其中当从振荡器发射的超声波的最大工作频率被称为fmax [MHz]时，连接构件被设置为100 / fmax [cm]以下。即使被检查样本小，也可以以良好的检查精度实现期望的缺陷检查。

10. 发明授权

US08710249B2 Maltol ether processes and intermediates 有权
标题翻译：麦芽酚醚工艺和中间体
公开(公告)号：US08710249B2
公开(公告)日：2014-04-29
申请号：US13133481
申请日：2009-12-08
申请人： Yasunori Aoyama
发明人： Yasunori Aoyama
IPC分类号： C07D309/40
CPC分类号： C07D309/38
摘要： Novel processes and intermediates are provided according to the general reaction scheme: Formula I, II, III, IV (I), (II), (III), (IV) utilizing a ruthenium catalyst in an oxidative cleavage of the triene 4 whereby an aldehyde may be produced and optionally taken on to a carboxylic acid 5: Formula V (V)
摘要翻译：根据通用反应方案提供新的方法和中间体：在三烯4的氧化裂解中使用钌催化剂的式I，II，III，IV（I），（II），（III），（IV）可以制备醛，并任选地加入到羧酸5中：式V（V）

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