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1. 发明申请

WO02085848A8 SYNTHESIS OF PANCRATISTATIN PRODRUGS 审中-公开
标题翻译：人参皂苷前体的合成
公开(公告)号：WO02085848A8
公开(公告)日：2003-05-30
申请号：PCT/US0211964
申请日：2002-04-17
申请人： UNIV ARIZONA STATE , PETIT GEORGE R , ORR BRIAN , DUCKI SYLVIE
发明人： PETIT GEORGE R , ORR BRIAN , DUCKI SYLVIE
IPC分类号： A61P31/14 , A61P35/00 , C07D453/04 , C07D491/04 , C07F9/6561 , C07D471/00
CPC分类号： C07F9/6561 , Y02P20/55
摘要： A new and efficient synthesis of the (+)-pancratistatin phosphate prodrug 2a has been accomplished. Selective protection (tetraacetate 4) of (+)-pancratistatin (1a) was followed by phosphorylation (to 5) with dibenzyl chlorophosphite (prepared in situ from dibenzyl phosphite). Cleavage of the acetate (with sodium methoxide) and benzyl (by hydrogenolysis) protecting groups followed by concomitant reaction with two equivalents of sodium methoxide afforded good yield of disodium (+)-pancratistatin phosphate (2a). Further increases in yields of the prodrug (2a) were realized by avoiding heat in the final purification steps. Fourteen (2b-o) additional metal and ammonium derived phosphate prodrugs were also synthesized.
摘要翻译：（+） - pancratistatin磷酸酯前药2a的新的和有效的合成已经完成。（+） - pancratistatin（1a）的选择性保护（四乙酸酯4）之后，用二苄基氯亚磷酸酯（由二苄基亚磷酸酯原位制备）磷酸化（至5）。乙酸酯（含有甲醇钠）和苄基（通过氢解）保护基团的裂解随后与2当量的甲醇钠反应提供了良好收率的（+） - pancratistatin-磷酸二钠（2a）。前药（2a）的收率进一步增加是通过避免最终纯化步骤中的加热来实现的。还合成了十四个（2b-o）另外的金属和铵衍生的磷酸酯前药。

2. 发明申请

WO02085848A2 SYNTHESIS OF PANCRATISTATIN PRODRUGS 审中-公开
标题翻译： PANCRATISTATIN PRODRUGS的合成
公开(公告)号：WO02085848A2
公开(公告)日：2002-10-31
申请号：PCT/US0211964
申请日：2002-04-17
申请人： UNIV ARIZONA STATE , PETIT GEORGE R , ORR BRIAN , DUCKI SYLVIE
发明人： PETIT GEORGE R , ORR BRIAN , DUCKI SYLVIE
IPC分类号： A61P31/14 , A61P35/00 , C07D453/04 , C07D491/04 , C07F9/6561 , C07D
CPC分类号： C07F9/6561 , Y02P20/55
摘要： A new and efficient synthesis of the (+)-pancratistatin phosphate prodrug 2a has been accomplished. Selective protection (tetraacetate 4) of (+)-pancratistatin (1a) was followed by phosphorylation (to 5) with dibenzyl chlorophosphite (prepared in situ from dibenzyl phosphite). Cleavage of the acetate (with sodium methoxide) and benzyl (by hydrogenolysis) protecting groups followed by concomitant reaction with two equivalents of sodium methoxide afforded good yield of disodium (+)-pancratistatin phosphate (2a). Further increases in yields of the prodrug (2a) were realized by avoiding heat in the final purification steps. Fourteen (2b-o) additional metal and ammonium derived phosphate prodrugs were also synthesized.
摘要翻译：已经完成了（+） - 泛磷酸肌苷酸前药2a的新的和有效的合成。（+） - pancratistatin（1a）的选择性保护（四乙酸酯4），随后用二氯亚磷酸二苄基酯（由二亚磷酸酯原位制备）进行磷酸化（至5）。乙酸盐（用甲醇钠）和苄基（通过氢解）保护基团裂解，随后与两当量甲醇钠同时反应，得到良好的二钠（+） - 磷酸二钙（2a）的产率。通过在最终纯化步骤中避免热量来实现前药（2a）的产率的进一步提高。还合成了十四（2b-o）个额外的金属和铵衍生的磷酸酯前药。

3. 发明申请

WO2007106371A2 METHOD AND APPARATUS FOR AUTOMATICALLY CREATING MUSICAL COMPOSITIONS 审中-公开
标题翻译：用于自动创建音乐组合物的方法和装置
公开(公告)号：WO2007106371A2
公开(公告)日：2007-09-20
申请号：PCT/US2007005967
申请日：2007-03-08
申请人： SONY CORP , MADISON MEDIA SOFTWARE INC , ORR BRIAN
发明人： ORR BRIAN
IPC分类号： G10H7/00 , A63H5/00 , G04B13/00
CPC分类号： G10H1/0025 , G10H2210/111 , G10H2210/125 , G10H2240/081 , G10H2240/085 , G10H2240/131
摘要： A music generation engine automatically generates musical compositions by accessing musical sections and corresponding properties including similarity factors that provide a quantified indication of the similarity of musical sections to one another (e.g., a percentage of similarity). A sequential relationship of the musical sections is then determined according to an algorithmic process that uses the similarity factors to assess the desirability of the sequential relationship. The algorithmically created musical composition may then be stored, such as by rendering the composition as an audio file or by storing a library file that refers to the musical sections. The created musical composition may include layers respectively having different audio elements such that the created musical composition has a first dimension along a timeline and a second dimension that provides a depth based upon the presence of different audio elements. The presence and absence of audio elements along the timeline can be based upon the value of an intensity parameter, which may be an intensity envelope that is predetermined or automatically generated based upon user specifications.
摘要翻译：音乐生成引擎通过访问音乐部分和相应的属性来自动生成音乐作品，包括提供音乐部分彼此的相似性的量化指示（例如，相似度的百分比）的相似性因素。然后根据使用相似性因子来评估顺序关系的可取性的算法过程来确定音乐部分的顺序关系。然后可以存储算法创建的音乐作品，例如通过将作品呈现为音频文件或通过存储引用音乐片段的库文件来存储。所创建的音乐作品可以包括分别具有不同音频元素的层，使得所创建的音乐作品具有沿着时间线的第一维度，以及基于不同音频元素的存在来提供深度的第二维度。沿着时间线的音频元素的存在和不存在可以基于强度参数的值，强度参数可以是基于用户规格预定或自动生成的强度包络。

4. 发明申请

WO2011037854A2 METHODS FOR PRODUCING HYDROCODONE, HYDROMORPHONE OR A DERIVATIVE THEREOF 审中-公开
标题翻译：生产氢可酮，氢吗啡酮或其衍生物的方法
公开(公告)号：WO2011037854A2
公开(公告)日：2011-03-31
申请号：PCT/US2010049454
申请日：2010-09-20
申请人： MALLINCKRODT INC , ORR BRIAN , DUMMITT WILLIAM E
发明人： ORR BRIAN , DUMMITT WILLIAM E
IPC分类号： C07D489/02
CPC分类号： C07D489/02
摘要： The present disclosure generally relates to methods for producing opioid derivatives. More particularly, the present disclosure relates to the preparation of hydromorphone, hydrocodone, or a derivative thereof, by means of a non-catalytic hydrogenation reaction of thebaine, oripavine or a derivative thereof, respectively, using a hydrazide reagent, followed by hydrolysis of the hydrogenated intermediate at a low temperature and for a short period of time. Additionally, the present disclosure relates to a composition comprising the desired hydromorphone, hydrocodone, or a derivative thereof, in combination with a 6-beta compound that is structurally related thereto.
摘要翻译：本公开总体涉及用于生产阿片样衍生物的方法。更具体地说，本公开内容涉及通过蒂巴因，东罂粟碱或其衍生物分别使用酰肼试剂的非催化氢化反应，然后水解该氢化酮酮，氢可酮或其衍生物来制备氢吗啡酮，氢可酮或其衍生物氢化中间体在低温下短时间。此外，本公开涉及包含期望的氢吗啡酮，氢可酮或其衍生物以及与其结构相关的6-β化合物的组合物。

5. 发明申请

WO2012037309A3 IMPROVED PROCESS FOR THE PREPARATION OF SUFENTANIL BASE AND RELATED COMPOUNDS 审中-公开
标题翻译：改进的苏芬太尼碱及其相关化合物的制备方法
公开(公告)号：WO2012037309A3
公开(公告)日：2012-05-10
申请号：PCT/US2011051695
申请日：2011-09-15
申请人： MALLINCKRODT LLC , ORR BRIAN , HAAR JR JOSEPH , KLEMM GEORGE H , TOMAZI KEITH G
发明人： ORR BRIAN , HAAR JR JOSEPH , KLEMM GEORGE H , TOMAZI KEITH G
IPC分类号： C07D409/06
CPC分类号： C07D409/06
摘要： The present disclosure generally related to an improved process for the preparation of various piperidine derivatives. More particularly, the present disclosure related to an improved process for preparing sufentanil base (1) and related compounds, which advantageously utilizes more cost effective and/or less hazardous reagents, including a dispersion comprising between about 50% and about 70% by weight (based on the total weight of the dispersion) of an alkali metal hydride, such as sodium hydride, as well as eliminates the need for expensive and/or time consuming purification techniques.
摘要翻译：本公开总体上涉及制备各种哌啶衍生物的改进方法。更具体地说，本公开涉及用于制备舒芬太尼碱（1）和相关化合物的改进方法，其有利地使用更具成本效益和/或危害更小的试剂，包括含有约50重量％至约70重量％基于分散体的总重量）的碱金属氢化物如氢化钠，并且消除了对昂贵和/或耗时的纯化技术的需要。

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