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21. 发明授权

US5565585A Azido diacetal propane derivatives 失效
标题翻译：叠氮二缩醛丙烷衍生物
公开(公告)号：US5565585A
公开(公告)日：1996-10-15
申请号：US225225
申请日：1994-04-08
申请人： Chi-Huey Wong , Richard L. Pederson , Yi-Fong Wang
发明人： Chi-Huey Wong , Richard L. Pederson , Yi-Fong Wang
IPC分类号： C07C45/89 , C07C247/04 , C07F9/02 , C07C211/00
CPC分类号： C07C247/04 , C07C45/89
摘要： A new and practical method for synthesizing heterocyclic polyhydroxylated alkaloids using enzymatic aldol condensation and catalytic intramolecular reductive amination is disclosed.
摘要翻译：公开了一种使用酶促醛缩醇缩合和催化分子内还原胺化合成杂环多羟基化生物碱的新型实用方法。

22. 发明授权

US07045543B2 Covalent conjugates of biologically-active compounds with amino acids and amino acid derivatives for targeting to physiologically-protected sites 失效
公开(公告)号：US07045543B2
公开(公告)日：2006-05-16
申请号：US09993976
申请日：2001-11-05
申请人： Milton B. Yatvin , Richard L. Pederson
发明人： Milton B. Yatvin , Richard L. Pederson
IPC分类号： A01N43/38 , A01N37/18 , A61K31/405 , A61K31/40 , A61K38/00
CPC分类号： A61K47/542
摘要： This invention herein describes a method of facilitating the entry of drugs into cells and tissues at physiologically protected sites at pharmacokinetically useful levels and also a method of targeting drugs to physiologically protected sites in vivo. Also provided are drug conjugates with an amino acid or derivative thereof for facilitating such targeted drug delivery. The conjugates and methods of this invention provide an advance over other drug targeting methods known in the prior art, because the invention provides drug concentrations in such physiologically protected sites that can reach therapeutically-effective levels after administration of systemic levels much lower than are currently administered to achieve a therapeutic dose. This technology is appropriate for use with psychotropic, neurotropic, neurological, antibiotic, antibacterial, antimycotic, antiviral, antiproliferative or antineoplastic drugs, agents and conjugates, for rapid and efficient introduction of such agents across, e.g., the blood-brain barrier. Further, the invention provides means for retention and prolonged enzymatic release of such drugs, agents and conjugates comprising the conjugates of the invention, in the brain and central nervous system and other physiologically-protected sites.

23. 发明授权

US06664257B2 Anti-mycobacterial compounds 失效
公开(公告)号：US06664257B2
公开(公告)日：2003-12-16
申请号：US09993974
申请日：2001-11-05
申请人： Milton B. Yatvin , Richard L. Pederson
发明人： Milton B. Yatvin , Richard L. Pederson
IPC分类号： A61K3150
CPC分类号： C07D241/24 , A61K31/4965
摘要： This invention provides compositions of matter, pharmaceutical compounds, methods of synthesizing such compounds and methods for using such compounds to treat animals infected with a pathogenic mycobacterium. The invention specifically provides compositions and pharmaceutical compositions thereof for the treatment of tuberculosis and other Mycobacterium-caused diseases.

24. 发明授权

US5916983A Biologically active compounds by catalytic olefin metathesis 失效
标题翻译：通过催化烯烃复分解生物活性化合物
公开(公告)号：US5916983A
公开(公告)日：1999-06-29
申请号：US863872
申请日：1997-05-27
申请人： Richard L. Pederson , Robert H. Grubbs
发明人： Richard L. Pederson , Robert H. Grubbs
IPC分类号： C07C6/04 , C07C17/26 , C07C17/266 , C07C29/09 , C07C67/293 , C07C69/007 , C08F4/72 , C07C29/12 , C08F4/80 , C07F14/00
CPC分类号： C07C69/007 , C07C17/2632 , C07C17/266 , C07C29/095 , C07C6/04 , C07C67/11 , C07C67/26 , C07C67/293 , C07B2200/09 , C07C2531/24
摘要： Biologically active compounds such as pheromones and precursors thereof are produced by catalyzed cross metathesis of dissimilar terminal olefins or of a cyclodiene and a terminal olefin.
摘要翻译：通过异种末端烯烃或环二烯和末端烯烃的催化交叉复分解产生生物活性化合物如信息素及其前体。

25. 发明授权

US07507854B2 Impurity reduction in Olefin metathesis reactions 失效
标题翻译：烯烃复分解反应的杂质减少
公开(公告)号：US07507854B2
公开(公告)日：2009-03-24
申请号：US10924743
申请日：2004-08-23
申请人： Choon Woo Lee , Soon Hyeok Hong , Daniel P. Sanders , Robert H. Grubbs , Richard L. Pederson
发明人： Choon Woo Lee , Soon Hyeok Hong , Daniel P. Sanders , Robert H. Grubbs , Richard L. Pederson
IPC分类号： C07C69/52
CPC分类号： C07D303/04 , C07C6/04 , C07C67/293 , C07C2531/24 , C07D207/20 , C07C69/007 , C07C69/145 , C07C69/533
摘要： The present invention relates to the use of isomerization inhibitors in olefin metathesis reactions. The inhibitors are low molecular weight organic acids such as formic acid, acetic acid, benzoic acid, and the like.
摘要翻译：本发明涉及异构化抑制剂在烯烃复分解反应中的用途。抑制剂是低分子量有机酸，例如甲酸，乙酸，苯甲酸等。

26. 发明授权

US5143831A Fructose 1,6-diphosphate aldolase catalyzed steroselective synthesis of sugars 失效
标题翻译：果糖1,6-二磷酸醛缩酶催化立体选择性合成糖
公开(公告)号：US5143831A
公开(公告)日：1992-09-01
申请号：US238756
申请日：1988-08-30
申请人： Chi-Huey Wong , John R. Durrwachter , Richard L. Pederson
发明人： Chi-Huey Wong , John R. Durrwachter , Richard L. Pederson
IPC分类号： C07H5/04 , C07H7/02 , C07H11/00 , C07H13/04 , C12P19/26 , C12P41/00
CPC分类号： C07H13/04 , C07H11/00 , C07H5/04 , C07H7/02 , C12P19/26 , C12P41/00
摘要： A method for preparing optically pure N-containing sugars is disclosed wherein an optically impure chiral aldehyde acceptor is enzymatically condensed with dihydroxyacetone phosphate or dihydroxyacetone with a catalytic amount of inorganic arsenate in the presence of an aldolase to form an N-containing sugar.
摘要翻译：公开了一种用于制备光学纯的含N糖的方法，其中光学上不纯的手性醛受体在醛缩酶存在下用催化量的无机砷酸盐与二羟基丙酮磷酸酯或二羟基丙酮进行酶学缩合以形成含N的糖。

27. 发明授权

US06676972B2 Covalent microparticle-drug conjugates for biological targeting 失效
公开(公告)号：US06676972B2
公开(公告)日：2004-01-13
申请号：US10237846
申请日：2002-09-09
申请人： Michael J. Meredith , Milton B. Yatvin , Richard L. Pederson
发明人： Michael J. Meredith , Milton B. Yatvin , Richard L. Pederson
IPC分类号： A61K914
CPC分类号： A61K9/167 , Y10S977/906 , Y10S977/907
摘要： This invention provides reagents and methods for specifically delivering antibiotic, antimicrobial and antiviral compounds, drugs and agents to phagocytic mammalian cells. The invention also relates to specific delivery to and uptake of such compounds by phagocytic cells. The invention specifically relates to reagents and methods for facilitating the entry of antibiotic, antimicrobial and antiviral compounds, drugs and agents into phagocytic cells. The invention specifically provides compositions of matter and pharmaceutical embodiments of such compositions comprising such antibiotic, antimicrobial or antiviral compounds, drugs and agents conjugated to, impregnated with or coated onto particulate carriers generally termed microparticles. In particular embodiments, the antibiotic, antimicrobial and antiviral compounds, drugs and agents are covalently linked to a microparticle via a specifically-degradable linker molecule which is the target of a microorganism-specific protein having enzymatic activity. Also provided are porous microparticles impregnated with antibiotic, antimicrobial or antiviral compounds, drugs and agents wherein the surface or outside extent of the microparticle is covered with a degradable coating that is specifically degraded within an infected phagocytic mammalian cell. Also provided are nonporous microparticles coated with antibiotic, antimicrobial or antiviral compounds, drugs and agents and further coated wherein the surface or outside extent of the microparticle is covered with a degradable coating that is specifically degraded within an infected phagocytic mammalian cell. Thus, the invention provides cell targeting of drugs wherein the targeted drug is only released in cells infected with a particular microorganism. Methods of inhibiting, attenuating, arresting, combating and overcoming microbial infection of phagocytic mammalian cells in vivo and in vitro, especially cells infected with tuberculosis-causing and other Mycobacterium species microorganisms, are also provided.

28. 发明授权

US06215019B1 Synthesis of 5-decenyl acetate and other pheromone components 有权
标题翻译：乙酸5-癸烯和其他信息素组分的合成
公开(公告)号：US06215019B1
公开(公告)日：2001-04-10
申请号：US09387486
申请日：1999-09-01
申请人： Richard L. Pederson , Robert H. Grubbs
发明人： Richard L. Pederson , Robert H. Grubbs
IPC分类号： C07C6702
CPC分类号： C07C67/293 , C07C69/007 , C07C69/145
摘要： The present invention relates to syntheses of 5-decenyl acetate, the major component in Peach Twig Borer pheromone, and other pheromone components. The syntheses entails few reaction steps, use commercially available starting materials, and have relatively short process times. A preferred embodiment of the syntheses involves self-metathesizing 1-hexene in the presence of Grubbs' catalyst, [(PCy3)2Cl2]Ru═CHPh. The resulting 5-decene is then reacted with an alcohol or acetate protected hexene under vacuum to yield 5-decenyl acetate. These syntheses produce good yields without the need for expensive or sophisticated equipment.
摘要翻译：本发明涉及乙酸5-癸烯酯的合成，其是Peach Twig Borer信息素中的主要成分和其他信息素成分。合成的反应步骤很少，使用市售的原料，加工时间相对较短。合成的一个优选实施方案涉及在Grubbs催化剂[（PCy 3）2 Cl 2] Ru = CHPh存在下对1-己烯进行自转化。然后将所得的5-癸烯在真空下与醇或乙酸酯保护的己烯反应，得到乙酸5-癸酯。这些合成产生良好的产率，而不需要昂贵或复杂的设备。

29. 发明授权

US5329025A 3-azido compound 失效
标题翻译： 3-叠氮基化合物
公开(公告)号：US5329025A
公开(公告)日：1994-07-12
申请号：US862157
申请日：1992-04-02
申请人： Chi-Huey Wong , Richard L. Pederson , Yi-Fong Wang
发明人： Chi-Huey Wong , Richard L. Pederson , Yi-Fong Wang
IPC分类号： C07C45/89 , C07C247/04 , C07C247/02 , C07C205/05 , C07C207/00 , C07C247/00
CPC分类号： C07C247/04 , C07C45/89
摘要： A new and practical method for synthesizing heterocyclic polyhydroxylated alkaloids using enzymatic aldol condensation and catalytic intramolecular reductive amination is disclosed.
摘要翻译：公开了一种使用酶促醛缩醇缩合和催化分子内还原胺化合成杂环多羟基化生物碱的新型实用方法。

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