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1. 发明授权

US5025027A Cyclic carbamate analogues of (+)-pilocarpine 失效
标题翻译：（+） - 毛果芸香碱的环状氨基甲酸酯类似物
公开(公告)号：US5025027A
公开(公告)日：1991-06-18
申请号：US446486
申请日：1989-12-05
申请人： Henry Rapoport , Per Sauerberg
发明人： Henry Rapoport , Per Sauerberg
IPC分类号： C07D413/06
CPC分类号： C07D413/06
摘要： Pilocarpine analogues are provided having the structure ##STR1## where one of R.sub.1 or R.sub.2 is an alkyl, such as methyl, ethyl, propyl, butyl, and so forth, and the corresponding secondary alkyl groups, an aralkyl, such as benzyl, phenylethyl, phenylpropyl, and the corresponding secondary aralkyl residues, or a cycloalkyl having less than about 12 carbon atoms. R.sub.3 has at least two carbon atoms but less than about 9. These pilocarpine analogues have improved duration of biological activity with respect to pilocarpine. A particularly preferred compound is a muscarinic agonist equipotent with pilocarpine, where R.sub.2 is methyl, and R.sub.3 is ethyl.
摘要翻译：提供具有结构“IMAGE”的毛果芸香碱类似物，其中R 1或R 2中的一个为烷基，例如甲基，乙基，丙基，丁基等，以及相应的仲烷基，芳烷基如苄基，苯乙基，苯基丙基和相应的仲芳烷基或具有小于约12个碳原子的环烷基。 R3具有至少两个碳原子但小于约9.这些毛果芸香碱类似物相对于毛果芸香碱具有改善的生物活性持续时间。特别优选的化合物是与毛果芸香碱等效的毒蕈碱激动剂，其中R2是甲基，R3是乙基。

2. 发明授权

US06514987B1 Frangible compounds for pathogen inactivation 有权
标题翻译：用于病原体灭活的易碎化合物
公开(公告)号：US06514987B1
公开(公告)日：2003-02-04
申请号：US09610652
申请日：2000-07-02
申请人： David Cook , John E. Merritt , Aileen Nerio , Henry Rapoport , Adonis Stassinopoulos , Susan Wollowitz , Jan Matejovic , William A. Denny
发明人： David Cook , John E. Merritt , Aileen Nerio , Henry Rapoport , Adonis Stassinopoulos , Susan Wollowitz , Jan Matejovic , William A. Denny
IPC分类号： A61K3144
CPC分类号： C07D405/12 , A61L2/0082 , A61M1/0209 , B01J20/28 , C07D219/10 , C07D493/04 , C07F9/64
摘要： Compounds and methods for inactivating pathogens in materials are described, including compositions and methods for inactivating pathogens in biological materials such as red blood cell preparations and plasma. The compounds and methods may be used to treat materials intended for in vitro or in vivo use, such as clinical testing or transfusion. The compounds are designed to specifically bind to and react with nucleic acid, and then to degrade to form breakdown products. The degradation reaction is preferably slower than the reaction with nucleic acid.
摘要翻译：描述了用于灭活材料中的病原体的化合物和方法，包括用于灭活生物材料如红细胞制剂和血浆中的病原体的组合物和方法。化合物和方法可以用于治疗用于体外或体内使用的物质，例如临床试验或输血。该化合物被设计成与核酸特异性结合并与其反应，然后降解以形成分解产物。降解反应优选比与核酸的反应更慢。

3. 发明授权

US06420570B1 Psoralen compounds 失效
标题翻译：补骨脂素化合物
公开(公告)号：US06420570B1
公开(公告)日：2002-07-16
申请号：US09767611
申请日：2001-01-22
申请人： Susan Wollowitz , Stephen T. Isaacs , Henry Rapoport , Hans Peter Spielmann
发明人： Susan Wollowitz , Stephen T. Isaacs , Henry Rapoport , Hans Peter Spielmann
IPC分类号： C07D49300
CPC分类号： C07D493/04 , A01N1/0215 , A01N43/90 , A61K31/365 , A61K31/37 , A61K41/0019 , A61K41/0066 , A61L2/0011
摘要： Psoralen compound compositions are synthesized which have substitutions on the 4, 4′, 5′, and 8 positions of the psoralen, which yet permit their binding to nucleic acid of pathogens. Reaction conditions that photoactivate these bound psoralens result in covalent crosslinking to nucleic acid, thereby inactivating the pathogen. Higher psoralen binding levels and lower mutagenicity results in safer, more efficient, and reliable inactivation of pathogens. In addition to the psoralen compositions, the invention contemplates inactivating methods using the new psoralens.
摘要翻译：合成补骨脂素化合物组合物，其在补骨脂素的4,4'，5'和8位上具有取代，其仍然允许它们与病原体的核酸结合。激活这些结合的补骨脂素的反应条件导致与核酸的共价交联，从而使病原体灭活。更高的补骨脂素结合水平和较低的致突变性导致更安全，更有效和可靠的病原体失活。除了补骨脂素组合物之外，本发明考虑使用新的补骨脂素的灭活方法。

4. 发明授权

US6004741A Method for the photoactivation of 4' and 5' primary aminoalkyl psoralens in platelet preparations 失效
标题翻译： 4'和5'伯氨基烷基补骨脂素在血小板制剂中的光活化方法
公开(公告)号：US6004741A
公开(公告)日：1999-12-21
申请号：US957307
申请日：1997-10-23
申请人： Susan Wollowitz , Stephen T. Isaacs , Henry Rapoport , Hans Peter Spielmann , Aileen Nerio
发明人： Susan Wollowitz , Stephen T. Isaacs , Henry Rapoport , Hans Peter Spielmann , Aileen Nerio
IPC分类号： A61K31/37 , A61K41/00 , A61L2/00 , A01N1/02 , C12N7/06
CPC分类号： A61L2/0011 , A01N1/0215 , A01N1/0294 , A61K31/37 , A61K41/0066
摘要： Psoralen compounds are synthesized which have substitutions on the 4, 4', 5', and 8 positions of the psoralen, which permit enhanced binding to nucleic acid of pathogens. Higher psoralen binding levels and lower mutagenicity are described, resulting in safer, more efficient, and reliable inactivation of pathogens in blood products. The invention contemplates inactivation methods using the new psoralens which do not compromise the function of blood products for transfusion. In particular, 4' and 5' primary aminoalkyl psoralens are photoactivated in platelet preparations to inactivate pathogens.
摘要翻译：合成补骨脂素化合物，其在补骨脂素的4,4'，5'和8位上具有取代，其允许增强与病原体核酸的结合。描述了更高的补骨脂素结合水平和较低的致突变性，导致血液制品中病原体的更安全，更有效和可靠的失活。本发明考虑使用新的补骨脂素的灭活方法，其不损害用于输血的血液制品的功能。特别地，4'和5'伯氨基烷基补骨脂素在血小板制剂中被光活化以灭活病原体。

5. 发明授权

US5654443A Compounds for the photo decontamination of pathogens in blood 失效
标题翻译：用于血液中病原体照相去污的化合物
公开(公告)号：US5654443A
公开(公告)日：1997-08-05
申请号：US455955
申请日：1995-05-31
申请人： Susan Wollowitz , Stephen T. Isaacs , Henry Rapoport , Hans Peter Spielmann
发明人： Susan Wollowitz , Stephen T. Isaacs , Henry Rapoport , Hans Peter Spielmann
IPC分类号： A01N1/02 , A61K31/365 , A61K31/37 , A61K35/14 , A61K41/00 , A61L2/00 , C07D493/04
CPC分类号： C07D493/04 , A01N1/0215 , A61K31/365 , A61K31/37 , A61K41/0019 , A61K41/0066 , A61L2/0011
摘要： Psoralen compound compositions are synthesized which have substitutions on the 4, 4', 5', and 8 positions of the psoralen, which yet permit their binding to nucleic acid of pathogens. Reaction conditions that photoactivate these bound psoralens result in covalent crosslinking to nucleic acid, thereby inactivating the pathogen. Higher psoralen binding levels and lower mutagenicity results in safer, more efficient, and reliable inactivation of pathogens. In addition to the psoralen compositions, the invention contemplates inactivating methods using the new psoralens.
摘要翻译：合成补骨脂素化合物组合物，其在补骨脂素的4,4'，5'和8位上具有取代，其仍然允许它们与病原体的核酸结合。激活这些结合的补骨脂素的反应条件导致与核酸的共价交联，从而使病原体灭活。更高的补骨脂素结合水平和较低的致突变性导致更安全，更有效和可靠的病原体失活。除了补骨脂素组合物之外，本发明考虑使用新的补骨脂素的灭活方法。

6. 发明授权

US5593823A Method for inactivating pathogens in blood using photoactivation of 4'-primary amino-substituted psoralens 失效
标题翻译：使用4'-伯氨基取代的补骨脂素的光活化来灭活血液中的病原体的方法
公开(公告)号：US5593823A
公开(公告)日：1997-01-14
申请号：US337987
申请日：1994-11-14
申请人： Susan Wollowitz , Stephen T. Isaacs , Henry Rapoport , Hans P. Spielmann , Aileen Nerio
发明人： Susan Wollowitz , Stephen T. Isaacs , Henry Rapoport , Hans P. Spielmann , Aileen Nerio
IPC分类号： A01N1/02 , A61K31/365 , A61K31/37 , A61K41/00 , A61L2/00 , C07D493/04 , C12N7/06
CPC分类号： C07D493/04 , A01N1/0215 , A01N1/0294 , A61K31/365 , A61K31/37 , A61K41/0019 , A61K41/0066 , A61L2/0011
摘要： Psoralen compounds are synthesized which have substitutions on the 4, 4', 5', and 8 positions of the psoralen, which permit enhanced binding to nucleic acid of pathogens. Higher psoralen binding levels and lower mutagenicity are described, resulting in safer, more efficient, and reliable inactivation of pathogens in blood products. The invention contemplates inactivation methods using the new psoralens which do not compromise the function of blood products for transfusion.
摘要翻译：合成补骨脂素化合物，其在补骨脂素的4,4'，5'和8位上具有取代，其允许增强与病原体核酸的结合。描述了更高的补骨脂素结合水平和较低的致突变性，导致血液制品中病原体的更安全，更有效和可靠的失活。本发明考虑使用新的补骨脂素的灭活方法，其不损害用于输血的血液制品的功能。

7. 发明授权

US5578736A Compounds for the photo-decontamination of pathogens in blood 失效
标题翻译：用于血液中病原体照相去污的化合物
公开(公告)号：US5578736A
公开(公告)日：1996-11-26
申请号：US456205
申请日：1995-05-31
申请人： Susan Wollowitz , Stephen T. Isaacs , Henry Rapoport , Hans P. Spielmann
发明人： Susan Wollowitz , Stephen T. Isaacs , Henry Rapoport , Hans P. Spielmann
IPC分类号： A01N1/02 , A61K31/365 , A61K31/37 , A61K35/14 , A61K41/00 , A61L2/00 , C07D493/04 , C07D493/02
CPC分类号： C07D493/04 , A01N1/0215 , A61K31/365 , A61K31/37 , A61K41/0019 , A61K41/0066 , A61L2/0011
摘要： Psoralen compound compositions are synthesized which have substitutions on the 4, 4', 5', and 8 positions of the psoralen, which yet permit their binding to nucleic acid of pathogens. Reaction conditions that photoactivate these bound psoralens result in covalent crosslinking to nucleic acid, thereby inactivating the pathogen. Higher psoralen binding levels and lower mutagenicity results in safer, more efficient, and reliable inactivation of pathogens. In addition to the psoralen compositions, the invention contemplates inactivating methods using the new psoralens.
摘要翻译：合成补骨脂素化合物组合物，其在补骨脂素的4,4'，5'和8位上具有取代，其仍然允许它们与病原体的核酸结合。激活这些结合的补骨脂素的反应条件导致与核酸的共价交联，从而使病原体灭活。更高的补骨脂素结合水平和较低的致突变性导致更安全，更有效和可靠的病原体失活。除了补骨脂素组合物之外，本发明考虑使用新的补骨脂素的灭活方法。

8. 发明授权

US5322942A Synthesis of optically active lactones from L-aspartic acid and intermediates thereof 失效
标题翻译：从L-天冬氨酸合成光学活性内酯及其中间体
公开(公告)号：US5322942A
公开(公告)日：1994-06-21
申请号：US709373
申请日：1991-06-03
申请人： Henry Rapoport , Jeffrey M. Dener , Lin-hau Zhang
发明人： Henry Rapoport , Jeffrey M. Dener , Lin-hau Zhang
IPC分类号： C07C227/30 , C07C69/612 , C07C69/63 , C07C227/32 , C07C229/24 , C07D233/54 , C07D233/64 , C07D307/33 , C07D405/04 , C07D405/06 , C07D239/20
CPC分类号： C07D233/64 , C07C227/32 , C07C229/24 , C07C69/612 , C07C69/63 , C07D307/33 , C07D405/04 , C07D405/06
摘要： Optically active lactones are described, such as an intermediate lactone having the formula ##STR1## where R and R.sup.2 are each independently alkyl with 1 to 6 carbon atoms, cycloalkyl with 6 to 10 carbon atoms, aryl with 6 to 10 carbon atoms, or arylalkyl with 7 to 19 carbon atoms, R.sup.4 is H or C.sub.1-6 alkyl, and Ar is a homo- or heteroaromatic ring with 5 or 6 ring atoms being optionally substituted by C.sub.1-6 alkyl or alkoxy groups, halogen atoms, cyano or nitro groups. Such optically active, intermediate lactones are prepared from L-aspartic acid, and can be readily converted to (+)-pilocarpine and its analogues by hydrolysis, reduction, and hydrogenation, such as to an optically active lactone having the formula ##STR2## which is (+)-pilocarpine when R is ethyl, R.sup.4 is H, and Ar is 1-methylimidazol-5-yl.
摘要翻译：描述了光学活性内酯，例如具有式VIa的中间体内酯，其中R和R 2各自独立地为具有1至6个碳原子的烷基，具有6至10个碳原子的环烷基，具有6至10个碳原子的芳基，或具有7至19个碳原子的芳基烷基，R 4是H或C 1-6烷基，Ar是具有5或6个环原子的均聚或杂芳环，任选地被C 1-6烷基或烷氧基，卤素原子，氰基或硝基团体这种光学活性的中间体内酯由L-天冬氨酸制备，并且可以通过水解，还原和氢化而容易地转化为（+） - 毛果芸香碱及其类似物，例如具有式VIII的光学活性内酯当R为乙基时，其为（+） - 毛果芸香碱，R4为H，Ar为1-甲基咪唑-5-基。

9. 发明授权

US4124598A Psoralens 失效
标题翻译：补骨脂素
公开(公告)号：US4124598A
公开(公告)日：1978-11-07
申请号：US734031
申请日：1976-10-20
申请人： John E. Hearst , Henry Rapoport , Stephen Isaacs , Che-Kun J. Shen
发明人： John E. Hearst , Henry Rapoport , Stephen Isaacs , Che-Kun J. Shen
IPC分类号： A61K31/35 , A61K31/365 , A61K31/70 , A61K31/7088 , A61K39/00 , A61P17/00 , A61P27/00 , A61P31/12 , A61P43/00 , C07D493/04 , C07H21/00 , C07H21/02 , C07H21/04 , G01N33/53
CPC分类号： C07D493/04 , C07H21/00 , Y10S514/863
摘要： New psoralen compounds have been synthesized. The compounds all include the addition of substituent groups at the 4' position on the basic trioxsalen structure. Specifically, the compounds have the structure: ##STR1## wherein X may be any desired substituent such as halogenated alkyls, alcohols, ethers, aminoalkyls, etc. The new substituted psoralens exhibit high solubility in aqueous solution and low dissociation constants from deoxyribonucleic acid (DNA), as well as a reactivity with ribonucleic acids (RNA). Such psoralen compounds find use in the study of secondary structures of nucleic acids; as inhibitors of RNA replication; in the inactivation of viruses; and in the photo chemotherapy of psoriasis.
摘要翻译：已经合成了新的补骨脂素化合物。化合物全部包括在碱性三氧杂环己烷结构的4'位上添加取代基。具体地，化合物具有以下结构：其中X可以是任何所需的取代基，例如卤代烷基，醇，醚，氨基烷基等。新的取代补骨脂素在水溶液中表现出高溶解度和来自脱氧核糖核酸（DNA）的低解离常数），以及与核糖核酸（RNA）的反应性。这种补骨脂素化合物可用于研究核酸二级结构; 作为RNA复制的抑制剂; 在灭活病毒; 并在银屑病的照片化疗中。

10. 发明授权

US06218100B1 5′-primary aminoalkyl psoralen compositions with platelets 失效
标题翻译：具有血小板的5'-氨基烷基补骨脂素组合物
公开(公告)号：US06218100B1
公开(公告)日：2001-04-17
申请号：US08900032
申请日：1997-07-24
申请人： Susan Wollowitz , Stephen T. Isaacs , Henry Rapoport , Hans Peter Spielmann
发明人： Susan Wollowitz , Stephen T. Isaacs , Henry Rapoport , Hans Peter Spielmann
IPC分类号： A01N102
CPC分类号： C07D493/04 , A01N1/0215 , A61K31/365 , A61K31/37 , A61K41/0019 , A61K41/0066 , A61L2/0011
摘要： Psoralen compounds are synthesized which have substitutions on the 4, 4′, 5′, and 8 positions of the psoralen, which permit enhanced binding to nucleic acid of pathogens. Higher psoralen binding levels and lower mutagenicity are described, resulting in safer, more efficient, and reliable inactivation of pathogens in blood products. The invention contemplates inactivation methods using the new psoralens which do not compromise the function of blood products for transfusion. In particular, use of 5′-primary aminoalkyl psoralens to inactivate pathogens in platelets is disclosed.
摘要翻译：合成补骨脂素化合物，其在补骨脂素的4,4'，5'和8位上具有取代，其允许增强与病原体核酸的结合。描述了更高的补骨脂素结合水平和较低的致突变性，导致血液制品中病原体的更安全，更有效和可靠的失活。本发明考虑使用新的补骨脂素的灭活方法，其不损害用于输血的血液制品的功能。特别地，公开了使用5'-氨基烷基补骨脂素灭活血小板中的病原体。

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