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1. 发明授权

US08664411B2 Tetrahydropyranochromene gamma secretase inhibitors 有权
标题翻译：四氢吡喃色烯γ分泌酶抑制剂
公开(公告)号：US08664411B2
公开(公告)日：2014-03-04
申请号：US12665580
申请日：2008-07-01
申请人： Wen-Lian Wu , Thomas A. Bara , Duane A. Burnett , John W. Clader , Martin S. Domalski , Yan Jin , Hubert B. Josien , Hongmei Li , Xian Liang , Dmitri A. Pissarnitski , Thavalakulamgara K. Sasikumar , Jesse K. Wong , Ruo Xu , Zhiqiang Zhao , Paul McNamara
发明人： Wen-Lian Wu , Thomas A. Bara , Duane A. Burnett , John W. Clader , Martin S. Domalski , Yan Jin , Hubert B. Josien , Hongmei Li , Xian Liang , Dmitri A. Pissarnitski , Thavalakulamgara K. Sasikumar , Jesse K. Wong , Ruo Xu , Zhiqiang Zhao , Paul McNamara
IPC分类号： C07D311/80 , C07D493/04 , A61K31/352
CPC分类号： C07D493/04 , C07D311/78 , C07D407/12
摘要： Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.
摘要翻译：公开了下式的新型γ-分泌酶抑制剂。还公开了抑制γ-分泌酶，治疗神经变性疾病的方法和治疗阿尔茨海默氏病的方法。还公开了在一个反应步骤中使用醛（或酮）和被两个吸电子基团取代的烷基的混合物制备烯烃的方法，并使该混合物与：（a）磺酰卤（例如磺酰氯）和（b）磺酰基酐和碱性胺，或（c）芳基-C（O） - 卤化物和碱式叔胺，或（d）芳基-C（O） - OC（O） - 芳基和碱式叔胺，或（e）杂芳基-C（O） - 卤化物和碱式叔胺，或（f）杂芳基-C（O）-OC（O） - 杂芳基和碱性叔胺。

2. 发明申请

US20110236400A1 TETRAHYDROPYRANOCHROMENE GAMMA SECRETASE INHIBITORS 有权
标题翻译：四氢吡喃葡萄糖消炎酶抑制剂
公开(公告)号：US20110236400A1
公开(公告)日：2011-09-29
申请号：US12665580
申请日：2008-07-01
申请人： Wen-Lian Wu , Thomas A. Bara , Duane A. Burnett , John W. Clader , Martin S. Domalski , Yan Jin , Hubert B. Josien , Hongmei Li , Xian Liang , Dmitri A. Pissarnitski , Thavalakulamgara K. Sasikumar , Jesse K. Wong , Ruo Xu , Zhiqiang Zhao , Paul E. McNamara
发明人： Wen-Lian Wu , Thomas A. Bara , Duane A. Burnett , John W. Clader , Martin S. Domalski , Yan Jin , Hubert B. Josien , Hongmei Li , Xian Liang , Dmitri A. Pissarnitski , Thavalakulamgara K. Sasikumar , Jesse K. Wong , Ruo Xu , Zhiqiang Zhao , Paul E. McNamara
IPC分类号： A61K39/395 , C07D493/04 , C07D311/80 , C07D407/12 , A61K31/35 , A61K31/352 , A61K31/381 , A61P25/28 , A61P29/00 , A61P31/00 , C07C201/12 , C07C67/343
CPC分类号： C07D493/04 , C07D311/78 , C07D407/12
摘要： Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.
摘要翻译：公开了下式的新型γ-分泌酶抑制剂。还公开了抑制γ-分泌酶，治疗神经变性疾病的方法和治疗阿尔茨海默氏病的方法。还公开了在一个反应步骤中使用醛（或酮）和被两个吸电子基团取代的烷基的混合物制备烯烃的方法，并使该混合物与：（a）磺酰卤（例如磺酰氯）和（b）磺酰基酐和碱性胺，或（c）芳基-C（O） - 卤化物和碱式叔胺，或（d）芳基-C（O） - （O） - 芳基和碱式叔胺，或（e）杂芳基-C（O） - 卤化物和碱式叔胺，或（f）杂芳基-C（O）-O-C（O ） - 杂芳基和碱性叔胺。

3. 发明授权

US07396929B2 Synthesis of 3-amino-4-substituted pyrazole derivatives 失效
标题翻译： 3-氨基-4-取代的吡唑衍生物的合成
公开(公告)号：US07396929B2
公开(公告)日：2008-07-08
申请号：US11448191
申请日：2006-06-07
申请人： Jianshe Kong , Tao Meng , Paul E. McNamara , Xian Liang , Jesse K. Wong
发明人： Jianshe Kong , Tao Meng , Paul E. McNamara , Xian Liang , Jesse K. Wong
IPC分类号： C07D417/02
CPC分类号： C07D231/38
摘要： This application discloses a novel process to synthesize 3-amino-4-substituted pyrazole derivatives, which may be used, for example, as intermediates to prepare compounds having, for example, pharmaceutical utility.
摘要翻译：本申请公开了一种合成3-氨基-4-取代的吡唑衍生物的新方法，其可用于例如制备具有例如药物效用的化合物的中间体。

4. 发明申请

US20060281756A1 Synthesis of 3-amino-4-substituted pyrazole derivatives 失效
标题翻译： 3-氨基-4-取代的吡唑衍生物的合成
公开(公告)号：US20060281756A1
公开(公告)日：2006-12-14
申请号：US11448191
申请日：2006-06-07
申请人： Jianshe Kong , Tao Meng , Paul McNamara , Xian Liang , Jesse Wong
发明人： Jianshe Kong , Tao Meng , Paul McNamara , Xian Liang , Jesse Wong
IPC分类号： A61K31/496 , A61K31/454 , A61K31/4439 , A61K31/427 , A61K31/416 , C07D403/02 , C07D417/02
CPC分类号： C07D231/38
摘要： This application discloses a novel process to synthesize 3-amino-4-substituted pyrazole derivatives, which may be used, for example, as intermediates to prepare compounds having, for example, pharmaceutical utility.
摘要翻译：本申请公开了一种合成3-氨基-4-取代的吡唑衍生物的新方法，其可用于例如制备具有例如药物效用的化合物的中间体。

5. 发明申请

US20120174168A1 Method and Apparatus for Retrieving I Frame 有权
标题翻译：检索I帧的方法和装置
公开(公告)号：US20120174168A1
公开(公告)日：2012-07-05
申请号：US13395243
申请日：2010-04-23
申请人： Xian Liang
发明人： Xian Liang
IPC分类号： H04N21/643 , H04N21/633
CPC分类号： H04N21/2389 , H04N19/48 , H04N19/61 , H04N21/23418 , H04N21/2387 , H04N21/4385 , H04N21/44008 , H04N21/8451 , H04N21/8453 , H04N21/8455
摘要： A method and apparatus for retrieving an I frame are disclosed in the present invention, wherein, the method includes: analyzing transport stream packets in a transport stream one by one, and if it is determined that the current transport stream packet is a video packet and includes a Packet Elementary Stream (PES) header, then making a determination according to data after the PES header in the current transport stream packet to locate initial and/or end locations of the I frame. In the present invention, without parsing syntax elements in H.264, such as a Sequence Parameter Set (SPS), a Picture Parameter Set (PPS), a slice etc., the location of the I frame can be positioned by simply comparing various Transport stream (TS) packets in the TS stream and making a determination.
摘要翻译：本发明公开了一种用于检索I帧的方法和装置，其中，该方法包括：逐个分析传输流中的传输流分组，以及如果确定当前传输流分组是视频分组，包括分组基本流（PES）报头，然后根据当前传输流分组中的PES报头之后的数据进行确定，以定位I帧的初始和/或结束位置。在本发明中，在不解析诸如序列参数集（SPS），图像参数集（PPS），片段等的H.264中的语法元素的情况下，可以通过简单地比较各种传输流（TS）数据包在TS流中并进行确定。

6. 发明授权

US5914411A Alternate method for acylating 10-deacetylbaccatin III selectively at the C-10 position 失效
标题翻译：在C-10位置选择性地酰化10-脱乙酰基浆果赤霉素III的替代方法
公开(公告)号：US5914411A
公开(公告)日：1999-06-22
申请号：US10285
申请日：1998-01-21
申请人： Nicholas J. Sisti , Jan Zygmunt , Herbert R. Brinkman , Madhavi C. Chander , Xian Liang , James D. McChesney
发明人： Nicholas J. Sisti , Jan Zygmunt , Herbert R. Brinkman , Madhavi C. Chander , Xian Liang , James D. McChesney
IPC分类号： A61K31/337 , A61P35/00 , C07D305/14
CPC分类号： C07D305/14
摘要： A method of acylating 10-deacetylbaccatin III at the C-10 position over the C-7 hydroxy position thereof to produce baccatin IIII is accomplished first by dissolving 10-deacetylbaccatin III in an acceptable ether solvent therefor, such as tetrahydrofuran. A lithium salt, preferably lithium chloride, is added. A trialkylamine base or pyridine is next added, followed by the addition of an acylating agent, such as acetyl chloride. The resulting solution may be quenched, for example with ammonium chloride, to eliminate excess of the acylating agent. The result is baccatin III in solution. This solution may then be diluted with ethyl acetate to form an organic phase and an aqueous phase, with the organic phase being washed and thereafter reduced. Recrystallization and column chromatography may be employed to purify the baccatin III.
摘要翻译：首先通过将10-脱乙酰基浆果赤霉素III溶解在其可接受的醚溶剂如四氢呋喃中来完成在其C-7羟基上的C-10位上酰化10-脱乙酰基浆果赤霉素Ⅲ以产生浆果赤霉素IIII的方法。加入锂盐，优选氯化锂。然后加入三烷基胺碱或吡啶，然后加入酰化剂如乙酰氯。所得溶液可以例如用氯化铵淬灭，以消除过量的酰化剂。结果是溶液中的浆果赤霉素III。然后可以用乙酸乙酯稀释该溶液以形成有机相和水相，同时洗涤有机相，然后还原。可以使用重结晶和柱色谱来纯化浆果赤霉素III。

7. 发明授权

US6066749A Method for conversion of C-2'-O-protected-10-hydroxy taxol to c-2'-O-protected taxol:useful intermediates in paclitaxel synthesis 失效
标题翻译：将C-2'-O-保护的10-羟基紫杉醇转化为c-2'-O保护的紫杉醇的方法：紫杉醇合成中的有用中间体
公开(公告)号：US6066749A
公开(公告)日：2000-05-23
申请号：US71261
申请日：1998-05-01
申请人： Nicholas J. Sisti , Herbert R. Brinkman , James D. McChesney , Madhavi C. Chander , Xian Liang , Jan Zygmunt
发明人： Nicholas J. Sisti , Herbert R. Brinkman , James D. McChesney , Madhavi C. Chander , Xian Liang , Jan Zygmunt
IPC分类号： C07D305/14
CPC分类号： C07D305/14
摘要： A method of acylating C-2' O-protected-10-hydroxy taxol selectively at the C-10 hydroxyl position over the C-7 hydroxy position thereof to produce C-2' O-protected taxol is accomplished first by dissolving C-2' O-protected-10-hydroxy taxol in an acceptable ether solvent therefor, such as tetrahydrofuran, to form a first solution at a first temperature. The first solution is then cooled to a second temperature, and a lithium base, preferably n-butyl lithium, is added to form an intermediate compound having a lithium alkoxide at the C-10 position thereof. An acylating agent, such as acetyl chloride, is then added. The resulting solution may be quenched, for example with ammonium chloride, to eliminate excess of the acylating agent and the lithium base. The result is a solution containing C-2' O-protected taxol. This solution may then be washed, concentrated and purified. The present invention is also directed to C-10 lithium alkoxide intermediate compounds for the production of paclitaxel.
摘要翻译：首先通过将C-2'O-保护的10-羟基紫杉醇溶解在C-10羟基的C- 在其可接受的醚溶剂如四氢呋喃中的O-保护的10-羟基紫杉醇在第一温度下形成第一溶液。然后将第一溶液冷却至第二温度，并加入锂碱，优选正丁基锂以形成其C-10位上具有锂醇盐的中间体化合物。然后加入酰化剂，如乙酰氯。所得溶液可以例如用氯化铵淬灭，以消除过量的酰化剂和锂碱。其结果是含有C-2'O保护的紫杉醇的溶液。然后可以将该溶液洗涤，浓缩并纯化。本发明还涉及用于生产紫杉醇的C-10锂盐中间体化合物。

8. 发明授权

US6048990A Method for selective acylation of C-2'-O-protected-10-hydroxy-taxol at the C-10 position 失效
标题翻译：在C-10位置选择性酰化C-2'-O-保护的10-羟基 - 紫杉醇的方法
公开(公告)号：US6048990A
公开(公告)日：2000-04-11
申请号：US71258
申请日：1998-05-01
申请人： Xian Liang , Jan Zygmunt , Nicholas J. Sisti , Madhavi C. Chander , Herbert R. Brinkman , James D. McChesney
发明人： Xian Liang , Jan Zygmunt , Nicholas J. Sisti , Madhavi C. Chander , Herbert R. Brinkman , James D. McChesney
IPC分类号： C07D305/14
CPC分类号： C07D305/14
摘要： A method of acylating C-2' O-protected-10-hydroxy taxol selectively at the C-10 hydroxyl position over the C-7 hydroxy position thereof to produce C-2' O-protected taxol is accomplished first by dissolving C-2' O-protected-10-hydroxy taxol in an acceptable ether solvent therefor, such as tetrahydrofuran. A lithium salt, preferably lithium chloride, is added. A trialkylamine base or pyridine is next added, followed by the addition of an acylating agent, such as acetyl chloride. The resulting solution may be quenched, for example with ammonium chloride, to eliminate excess of the acylating agent. This solution may then be diluted with ethyl acetate to form an organic phase and an aqueous phase, with the organic phase being washed and thereafter reduced. Recrystallization and column chromatography may be employed to purify the C-2' O-protected taxol.
摘要翻译：首先通过将C-2'O-保护的10-羟基紫杉醇溶解在C-10羟基的C- 'O-保护的10-羟基紫杉醇在其可接受的醚溶剂中，例如四氢呋喃。加入锂盐，优选氯化锂。然后加入三烷基胺碱或吡啶，然后加入酰化剂如乙酰氯。所得溶液可以例如用氯化铵淬灭，以消除过量的酰化剂。然后可以用乙酸乙酯稀释该溶液以形成有机相和水相，同时洗涤有机相，然后还原。可以使用重结晶和柱色谱来纯化C-2'O保护的紫杉醇。

9. 发明授权

US5773461A 7-deoxy-6-substituted paclitaxels 失效
标题翻译： 7-脱氧-6-取代紫杉醇
公开(公告)号：US5773461A
公开(公告)日：1998-06-30
申请号：US868758
申请日：1997-06-04
申请人： Mark D. Wittman , Thomas J. Altstadt , John F. Kadow , David G. I. Kingston , Xian Liang
发明人： Mark D. Wittman , Thomas J. Altstadt , John F. Kadow , David G. I. Kingston , Xian Liang
IPC分类号： A61K31/00 , A61K31/335 , A61K31/337 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61P35/00 , C07D305/14 , C07D407/12
CPC分类号： C07D407/12 , C07D305/14
摘要： The present invention concerns novel paclitaxel derivatives, their use as antitumor agents, and pharmaceutical formulations.
摘要翻译：本发明涉及新型紫杉醇衍生物，其用作抗肿瘤剂和药物制剂。

10. 发明授权

US09215482B2 Method and apparatus for retrieving I frame 有权
标题翻译：检索I帧的方法和装置
公开(公告)号：US09215482B2
公开(公告)日：2015-12-15
申请号：US13395243
申请日：2010-04-23
申请人： Xian Liang
发明人： Xian Liang
IPC分类号： H04N21/44 , H04N21/234 , H04N21/2387 , H04N21/845 , H04N21/2389 , H04N21/4385 , H04N19/61 , H04N19/48
CPC分类号： H04N21/2389 , H04N19/48 , H04N19/61 , H04N21/23418 , H04N21/2387 , H04N21/4385 , H04N21/44008 , H04N21/8451 , H04N21/8453 , H04N21/8455
摘要： A method and apparatus for retrieving an I frame are disclosed in the present invention, wherein, the method includes: analyzing transport stream packets in a transport stream one by one, and if it is determined that the current transport stream packet is a video packet and includes a Packet Elementary Stream (PES) header, then making a determination according to data after the PES header in the current transport stream packet to locate initial and/or end locations of the I frame. In the present invention, without parsing syntax elements in H.264, such as a Sequence Parameter Set (SPS), a Picture Parameter Set (PPS), a slice etc., the location of the I frame can be positioned by simply comparing various Transport stream (TS) packets in the TS stream and making a determination.
摘要翻译：本发明公开了一种用于检索I帧的方法和装置，其中，该方法包括：逐个分析传输流中的传输流分组，以及如果确定当前传输流分组是视频分组，包括分组基本流（PES）报头，然后根据当前传输流分组中的PES报头之后的数据进行确定，以定位I帧的初始和/或结束位置。在本发明中，在不解析诸如序列参数集（SPS），图像参数集（PPS），片段等的H.264中的语法元素的情况下，可以通过简单地比较各种传输流（TS）数据包在TS流中并进行确定。

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