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1. 发明授权

US07906541B2 Process to prepare new substituted 1H-benzo[d]imidazol-2(3H)-ones, new intermediates and their use as BACE 1 inhibitors 失效
标题翻译：制备新的取代的1H-苯并[d]咪唑-2（3H） - 酮，新的中间体及其用作BACE1抑制剂的方法
公开(公告)号：US07906541B2
公开(公告)日：2011-03-15
申请号：US12329739
申请日：2008-12-08
申请人： Christian Roussel , Frederico Andreoli , Nicolas Daniel Pierre Vanthuyne
发明人： Christian Roussel , Frederico Andreoli , Nicolas Daniel Pierre Vanthuyne
IPC分类号： A61K31/4184 , C07D235/26
CPC分类号： C07D235/26
摘要： The invention relates to a new process leading to new substituted 1H-benzo[d]imidazol-2(3H)-ones of formula III and III′, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly as BACE 1 inhibitors in the treatment of Alzheimer disease.
摘要翻译：本发明涉及导致式III和III'的新的取代的1H-苯并[d]咪唑-2（3H） - 酮的新方法，其包含它们的药物组合物和它们作为治疗剂的用途，特别是作为BACE1抑制剂在治疗阿尔茨海默病。

2. 发明申请

US20100120880A1 PROCESS TO PREPARE NEW SUBSITUTED 1H-BENZO[d]IMIDAZOL-2(3H)-ONES, NEW INTERMEDIATES AND THEIR USE AS BACE 1 INHIBITORS 失效
标题翻译：制备新的取代的1H-苯并[d]咪唑烷-2（3H） - 酮，新的中间体及其作为BACE 1抑制剂的方法
公开(公告)号：US20100120880A1
公开(公告)日：2010-05-13
申请号：US12329739
申请日：2008-12-08
申请人： Christian Roussel , Federico Andreoli , Nicolas Daniel Pierre Vanthuyne
发明人： Christian Roussel , Federico Andreoli , Nicolas Daniel Pierre Vanthuyne
IPC分类号： A61K31/4184 , C07D235/04 , A61P25/28
CPC分类号： C07D235/26
摘要： The invention relates to a new process leading to new substituted 1H-benzo[d]imidazol-2(3H)-ones of formula III and III′, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly as BACE 1 inhibitors in the treatment of Alzheimer disease.
摘要翻译：本发明涉及导致式III和III'的新的取代的1H-苯并[d]咪唑-2（3H） - 酮的新方法，其包含它们的药物组合物和它们作为治疗剂的用途，特别是作为BACE1抑制剂在治疗阿尔茨海默病。

3. 发明申请

US20050240059A1 Process for the preparation of primary amines 失效
标题翻译：制备伯胺的方法
公开(公告)号：US20050240059A1
公开(公告)日：2005-10-27
申请号：US10523734
申请日：2003-07-28
申请人： Muriel Serradeil Albalat , Jean-Claude Vallejos , Christian Roussel , Didier Wilhelm
发明人： Muriel Serradeil Albalat , Jean-Claude Vallejos , Christian Roussel , Didier Wilhelm
IPC分类号： C07B57/00 , C07C213/02 , C07C217/40 , C07C217/48 , C07D249/08 , C07D249/14 , C07C29/68
CPC分类号： C07D249/08 , C07C213/02 , C07C217/40 , C07C217/48
摘要： Process for the preparation of primary amines of formula (I): where R3 represents an alkyl, cycloalkyl or aralkyl group, by reaction of a triazolium salt of formula (II): where R1 and R2 represent hydrogen or an alkyl, aralkyl or aryl group, R4 represents an alkyl or aralkyl group or a residue of an organic polymer functionalized by an alkylating group, and A− represents a halogen, alkylsulphonate, arylsulphonate, alkyl sulphate, hydrogensulphate, hemisulphate, perchlorate or hydroxide, with a hydride, in order to obtain an amine of formula (I), which is isolated, if desired, and intermediates.
摘要翻译：用于制备式（I）的伯胺的方法：其中R 3表示烷基，环烷基或芳烷基，通过式（II）的三唑盐反应：其中R 1和R 2表示氢或烷基，芳烷基或芳基 R4表示烷基或芳烷基或由烷基化基团官能化的有机聚合物的残基，并且A表示卤素，烷基磺酸盐，芳基磺酸盐，烷基硫酸盐，硫酸氢盐，半硫酸盐，高氯酸盐或氢氧化物，与氢化物反应，以获得式（I）的胺，如果需要，其分离，并且中间体。

4. 发明授权

US4221722A Process for preparing alkylpyrylium salts 失效
标题翻译：烷基吡喃鎓盐的制备方法
公开(公告)号：US4221722A
公开(公告)日：1980-09-09
申请号：US960610
申请日：1978-11-14
申请人： Michel Arnaud , Christian Roussel
发明人： Michel Arnaud , Christian Roussel
IPC分类号： C07D213/09 , C07D213/14 , C07D213/16 , C07D213/50 , C07D309/34 , C07D213/18
CPC分类号： C07D309/34
摘要： A process for preparing polyalkylpyrylium salts comprising a polyalkylpyrylium cation, wherein the pyrylium nucleus is substituted by 3 to 5 alkyl substituents three of which are situated in the 2-, 4- and 6-position is disclosed which comprises the step of reacting a branched alkane comprising at least one tertiary carbon atom with an acylating agent which is a reactive alkylcarboxylic acid derivative and an alkyl halide in the presence of a Lewis acid catalyst selected from the group consisting of aluminum halides, ferric halides and mixtures thereof.
摘要翻译：一种制备聚烷基吡喃鎓盐的方法，包括聚烷基吡喃鎓阳离子，其中吡喃核被3至5个烷基取代基取代，其中3个位于2-，4-和6-位，其包括使支链烷烃在选自卤化铝，三卤化铁及其混合物的路易斯酸催化剂存在下，包含至少一个叔碳原子与酰化剂反应的烷基羧酸衍生物和烷基卤化物。

5. 发明授权

US07890753B2 Secure mode for processors supporting MMU and interrupts 有权
标题翻译：支持MMU和中断的处理器的安全模式
公开(公告)号：US07890753B2
公开(公告)日：2011-02-15
申请号：US10256642
申请日：2002-09-27
申请人： Franck Dahan , Christian Roussel , Alain Chateau , Peter Cumming
发明人： Franck Dahan , Christian Roussel , Alain Chateau , Peter Cumming
IPC分类号： H04L29/06
CPC分类号： G06F21/556 , G06F9/30047 , G06F9/3802 , G06F9/468 , G06F12/1491 , G06F21/51 , G06F21/52 , G06F21/74 , G06F21/82 , G06F2221/2101 , G06F2221/2105 , G06F2221/2141 , G06F2221/2143 , G06F2221/2149 , G06F2221/2153
摘要： A digital system is provided with a secure mode (3rd level of privilege) built in a non-invasive way on a processor system that includes a processor core, instruction and data caches, a write buffer and a memory management unit. A secure execution mode is thus provided on a platform where the only trusted software is the code stored in ROM. In particular the OS is not trusted, all native applications are not trusted. A secure execution mode is provided that allows virtual addressing when a memory management unit (MMU) is enabled. The secure execution mode allows instruction and data cache to be enabled. A secure execution mode is provided that allows all the system interruptions to be unmasked. The secure mode is entered through a unique entry point. The secure execution mode can be dynamically entered and exited with full hardware assessment of the entry/exit conditions. A specific set of entry conditions is monitored that account for caches, write buffer and MMU being enabled. The structure of the activation sequence code accounts for caches, write buffer and MMU being enabled. The structure of the exit sequences code accounts for caches, write buffer and MMU being enabled. A specific way is provided to manage a safe exit of secure mode under generic interruptions and allows return from interruption through entry point and activation sequence and a proper resuming of the secure execution. A specific way is provided to manage the MMU in secure mode and provide data exchange between secure and non-secure environment.
摘要翻译：在包括处理器核心，指令和数据高速缓存，写入缓冲器和存储器管理单元的处理器系统上，数字系统被提供有以非侵入式方式内置的安全模式（第三级特权）。因此，在唯一可信软件是存储在ROM中的代码的平台上提供安全执行模式。特别是操作系统不受信任，所有本地应用程序都不被信任。提供了一种安全执行模式，当启用存储器管理单元（MMU）时允许虚拟寻址。安全执行模式允许指令和数据高速缓存启用。提供了一种安全执行模式，允许所有系统中断被隐藏。通过唯一的入口点输入安全模式。安全执行模式可以通过进入/退出条件的完整硬件评估来动态输入和退出。监视一个特定的条目条目，这些条目占用缓存，写入缓冲区和MMU被启用。激活序列代码的结构用于缓存，写入缓冲区和MMU被使能。退出序列代码的结构用于缓存，写入缓冲区和MMU被启用。提供了一种具体的方法来管理通用中断下安全模式的安全退出，并允许从中断通过入口点和激活顺序返回，并适当恢复安全执行。提供了以安全模式管理MMU的特定方式，并在安全和非安全环境之间提供数据交换。

6. 发明授权

US07237081B2 Secure mode for processors supporting interrupts 有权
标题翻译：支持中断的处理器的安全模式
公开(公告)号：US07237081B2
公开(公告)日：2007-06-26
申请号：US10256523
申请日：2002-09-27
申请人： Franck Dahan , Christian Roussel , Alain Chateau , Peter Cumming
发明人： Franck Dahan , Christian Roussel , Alain Chateau , Peter Cumming
IPC分类号： G06F12/14 , G06F11/30 , G06F12/00 , H04L9/32 , H04L9/00
CPC分类号： G06F21/556 , G06F9/30047 , G06F9/3802 , G06F9/468 , G06F12/1491 , G06F21/51 , G06F21/52 , G06F21/74 , G06F21/82 , G06F2221/2101 , G06F2221/2105 , G06F2221/2141 , G06F2221/2143 , G06F2221/2149 , G06F2221/2153
摘要： A digital system is provided with a secure mode (3rd level of privilege) built in a non-invasive way on a processor system that includes a processor core, instruction and data caches, a write buffer and a memory management unit. A secure execution mode is thus provided on a platform where the only trusted software is the code stored in ROM. In particular the OS is not trusted, all native applications are not trusted. A secure execution mode is provided that allows virtual addressing when a memory management unit (MMU) is enabled. The secure execution mode allows instruction and data cache to be enabled. A secure execution mode is provided that allows all the system interruptions to be unmasked. The secure mode is entered through a unique entry point. The secure execution mode can be dynamically entered and exited with full hardware assessment of the entry/exit conditions. A specific set of entry conditions is monitored that account for caches, write buffer and MMU being enabled. The structure of the activation sequence code accounts for caches, write buffer and MMU being enabled. The structure of the exit sequences code accounts for caches, write buffer and MMU being enabled. A specific way is provided to manage a safe exit of secure mode under generic interruptions and allows return from interruption through entry point and activation sequence and a proper resuming of the secure execution. A specific way is provided to manage the MMU in secure mode and provide data exchange between secure and non-secure environment.
摘要翻译：在包括处理器核心，指令和数据高速缓冲存储器，写入缓冲器和写入缓冲器的处理器系统中，数字系统被提供有以非侵入式方式构建的安全模式（3级的特权级别）内存管理单元。因此，在唯一可信软件是存储在ROM中的代码的平台上提供安全执行模式。特别是操作系统不受信任，所有本地应用程序都不被信任。提供了一种安全执行模式，当启用存储器管理单元（MMU）时允许虚拟寻址。安全执行模式允许指令和数据高速缓存启用。提供了一种安全执行模式，允许所有系统中断被隐藏。通过唯一的入口点输入安全模式。安全执行模式可以通过进入/退出条件的完整硬件评估来动态输入和退出。监视一个特定的条目条目，这些条目占用缓存，写入缓冲区和MMU被启用。激活序列代码的结构用于缓存，写入缓冲区和MMU被使能。退出序列代码的结构用于缓存，写入缓冲区和MMU被启用。提供了一种具体的方法来管理通用中断下安全模式的安全退出，并允许从中断通过入口点和激活顺序返回，并适当恢复安全执行。提供了以安全模式管理MMU的特定方式，并在安全和非安全环境之间提供数据交换。

7. 发明授权

US07220883B2 Process for the preparation of primary amines 失效
标题翻译：制备伯胺的方法
公开(公告)号：US07220883B2
公开(公告)日：2007-05-22
申请号：US10523734
申请日：2003-07-28
申请人： Muriel Serradeil Albalat , Jean-Claude Vallejos , Christian Roussel , Didier Wilhelm
发明人： Muriel Serradeil Albalat , Jean-Claude Vallejos , Christian Roussel , Didier Wilhelm
IPC分类号： C07C209/42 , C07D249/08 , C07D249/14
CPC分类号： C07D249/08 , C07C213/02 , C07C217/40 , C07C217/48
摘要： Process for the preparation of primary amines of formula (I): where R3 represents an alkyl, cycloalkyl or aralkyl group, by reaction of a triazolium salt of formula (II): where R1 and R2 represent hydrogen or an alkyl, aralkyl or aryl group, R4 represents an alkyl or aralkyl group or a residue of an organic polymer functionalized by an alkylating group, and A− represents a halogen, alkylsulphonate, arylsulphonate, alkyl sulphate, hydrogensulphate, hemisulphate, perchlorate or hydroxide, with a hydride, in order to obtain an amine of formula (I), which is isolated, if desired, and intermediates.
摘要翻译：用于制备式（I）的伯胺的方法：其中R 3表示烷基，环烷基或芳烷基，通过式（II）的三唑盐反应：其中R 1和R 2表示氢或烷基，芳烷基或芳基 R4表示烷基或芳烷基或由烷基化基团官能化的有机聚合物的残基，并且A表示卤素，烷基磺酸盐，芳基磺酸盐，烷基硫酸盐，硫酸氢盐，半硫酸盐，高氯酸盐或氢氧化物，与氢化物反应，以获得式（I）的胺，如果需要，其分离，并且中间体。

8. 发明授权

US07012138B1 Chiral polysaccharide esters, one of the methods for preparing them and their uses for obtaining optically enriched acids or for chiral chromatography 失效
标题翻译：手性多糖酯，其制备方法之一及其用于获得光学富集酸或用于手性色谱法的用途
公开(公告)号：US07012138B1
公开(公告)日：2006-03-14
申请号：US10239405
申请日：1999-12-02
申请人： Christian Roussel , Brice Bonnet , Innocenzo De Riggi , Cristina Suteu
发明人： Christian Roussel , Brice Bonnet , Innocenzo De Riggi , Cristina Suteu
IPC分类号： C08B33/00 , C08B35/00
CPC分类号： C08B3/10 , A61K31/715 , A61K31/717 , A61K31/724 , C07B57/00 , C08B3/16 , C08B3/24 , C08B33/02 , C08B37/0012
摘要： The present invention relates to chiral esters of polysaccharides, preferably of cellulose, amylose, β-cyclodextrin or amylopectin, obtained by reacting, in basic medium, polysaccharides (polyhydroxylated compounds) with racemic or enriched acid chlorides bearing a hydrogen and an aromatic group on their a carbon.This acid precursor (I) may be α-phenylpropionic acid, ibuprofen, ketoprofen or naproxen and, more generally, any acid derivative which may lead to a reactive form of ketene type.These novel asymmetric esters of polyhydroxylated compounds may be used as means of chiral enrichment, as medicinal systems with sustained and controlled release of enriched chiral active principles, these active principles consisting of the acyl parts of the esters grafted onto the hydroxyls (or even onto the amines) of the polyhydroxylated compounds, or alternatively as chiral stationary phases (CSPs).The invention is also directed toward a process for preparing these esters, to a chiral enrichment process and to the enrichment means, the medicinal systems and the CSPs targeted above.
摘要翻译：本发明涉及多糖，优选纤维素，直链淀粉，β-环糊精或支链淀粉的手性酯，其通过在碱性介质中使多糖（多羟基化合物）与含有氢和芳族基团的外消旋或富含酰基氯反应而获得一个碳。该酸前体（I）可以是α-苯基丙酸，布洛芬，酮洛芬或萘普生，更一般地，可以导致乙烯酮型反应形式的任何酸衍生物。这些新型的多羟基化合物的不对称酯可用作手性富集的手段，作为具有持续和受控释放的富含手性活性成分的药物体系，这些活性成分由接枝到羟基上的酯的酰基部分胺），或者作为手性固定相（CSP）。本发明还涉及制备这些酯，手性富集方法和富集装置，上述目标药物系统和CSP的方法。

9. 发明授权

US07120771B2 Secure mode for processors supporting MMU 有权
标题翻译：支持MMU的处理器的安全模式
公开(公告)号：US07120771B2
公开(公告)日：2006-10-10
申请号：US10256596
申请日：2002-09-27
申请人： Franck Dahan , Christian Roussel , Alain Chateau , Peter Cumming
发明人： Franck Dahan , Christian Roussel , Alain Chateau , Peter Cumming
IPC分类号： G06F12/00
CPC分类号： G06F21/556 , G06F9/30047 , G06F9/3802 , G06F9/468 , G06F12/1491 , G06F21/51 , G06F21/52 , G06F21/74 , G06F21/82 , G06F2221/2101 , G06F2221/2105 , G06F2221/2141 , G06F2221/2143 , G06F2221/2149 , G06F2221/2153
摘要： A digital system is provided with a secure mode (3rd level of privilege) built in a non-invasive way on a processor system that includes a processor core, instruction and data caches, a write buffer and a memory management unit. A secure execution mode is thus provided on a platform where the only trusted software is the code stored in ROM. In particular the OS is not trusted, all native applications are not trusted. A secure execution mode is provided that allows virtual addressing when a memory management unit (MMU) is enabled. The secure execution mode allows instruction and data cache to be enabled. A secure execution mode is provided that allows all the system interruptions to be unmasked. The secure mode is entered through a unique entry point. The secure execution mode can be dynamically entered and exited with full hardware assessment of the entry/exit conditions. A specific set of entry conditions is monitored that account for caches, write buffer and MMU being enabled. The structure of the activation sequence code accounts for caches, write buffer and MMU being enabled. The structure of the exit sequences code accounts for caches, write buffer and MMU being enabled. A specific way is provided to manage a safe exit of secure mode under generic interruptions and allows return from interruption through entry point and activation sequence and a proper resuming of the secure execution. A specific way is provided to manage the MMU in secure mode and provide data exchange between secure and non-secure environment.
摘要翻译：在包括处理器核心，指令和数据高速缓冲存储器，写入缓冲器和写入缓冲器的处理器系统中，数字系统被提供有以非侵入式方式构建的安全模式（3级的特权级别）内存管理单元。因此，在唯一可信软件是存储在ROM中的代码的平台上提供安全执行模式。特别是操作系统不受信任，所有本地应用程序都不被信任。提供了一种安全执行模式，当启用存储器管理单元（MMU）时允许虚拟寻址。安全执行模式允许指令和数据高速缓存启用。提供了一种安全执行模式，允许所有系统中断被隐藏。通过唯一的入口点输入安全模式。安全执行模式可以通过进入/退出条件的完整硬件评估来动态输入和退出。监视一个特定的条目条目，这些条目占用缓存，写入缓冲区和MMU被启用。激活序列代码的结构用于缓存，写入缓冲区和MMU被使能。退出序列代码的结构用于缓存，写入缓冲区和MMU被启用。提供了一种具体的方法来管理通用中断下安全模式的安全退出，并允许从中断通过入口点和激活顺序返回，并适当恢复安全执行。提供了以安全模式管理MMU的特定方式，并在安全和非安全环境之间提供数据交换。

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