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1. 发明授权

US06194139B1 Methods for photodecontamination of pathogens in blood 有权
标题翻译：血液中病原体的光电净化方法
公开(公告)号：US06194139B1
公开(公告)日：2001-02-27
申请号：US09407814
申请日：1999-09-28
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： 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.
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。

2. 发明授权

US6093831A N-trityl and N-phenylfluorenyl carboxyanhydrides of amino acids 失效
标题翻译：氨基酸的N-三苯甲基和N-苯基芴基羧酸酐
公开(公告)号：US6093831A
公开(公告)日：2000-07-25
申请号：US258469
申请日：1999-02-26
申请人： Henry Rapoport , Tae Bo Sim
发明人： Henry Rapoport , Tae Bo Sim
IPC分类号： C07D263/44
CPC分类号： C07D263/44
摘要： Amino acids are derivatized for use in peptide synthesis by conversion to N-carboxyanhydrides that are N-proected by either a trityl or a phenylfluorenyl group.
摘要翻译：氨基酸通过转化成由三苯甲基或苯基芴基进行N-检测的N-羧酸酐而被衍生化用于肽合成。

3. 发明授权

US6004742A Method for inactivation of pathogens in platelets using 4' and 5' primary amino-substituted psoralens 失效
标题翻译：使用4'和5'伯氨基取代的补骨脂素使血小板中的病原体失活的方法
公开(公告)号：US6004742A
公开(公告)日：1999-12-21
申请号：US962903
申请日：1997-11-03
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： A61K31/37 , A61K41/00 , A61L2/00 , A01N1/02 , C12N7/06
CPC分类号： A61K41/0066 , A01N1/0215 , A01N1/0294 , A61K31/37 , A61L2/0011 , A61L2/0088
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 add 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 compounds with primary aminoalkyl substitutions on the 4' or 5' positions of psoralen are used to inactivate pathogens in blood products such as platelets.
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的核酸添加结合。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。特别是在补骨脂素的4'或5'位上具有伯氨基烷基取代的化合物用于灭活血液制品如血小板中的病原体。

4. 发明授权

US5712085A 5'-(4-amino-2-oxa)butye-4,4', 8-trinethylpsoralen in synthetic medium 失效
标题翻译： 5' - （4-氨基-2-氧杂）丁基-4,4'，8-三乙基肌醇在合成培养基
公开(公告)号：US5712085A
公开(公告)日：1998-01-27
申请号：US465148
申请日：1995-06-05
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： A01N1/02 , A61K31/365 , A61K31/37 , A61K41/00 , A61L2/00 , C07D493/04 , C07D493/00
CPC分类号： C07D493/04 , A01N1/02 , A01N1/0205 , 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. Also disclosed are compositions comprising 4' or 5'-primary amino substituted psoralens in a synthetic media.
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。还公开了在合成培养基中包含4'或5'-主要氨基取代的补骨脂素的组合物。

5. 发明授权

US5625079A Synthesizing psoralen compounds useful as intermediates 失效
标题翻译：合成补骨脂素化合物可用作中间体
公开(公告)号：US5625079A
公开(公告)日：1997-04-29
申请号：US462377
申请日：1995-06-05
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 , C07D493/00
CPC分类号： C07D493/04 , A01N1/02 , A01N1/0205 , A61K31/365 , A61K31/37 , A61K41/0019 , A61K41/0066 , A61L2/0011
摘要： Synthesis of 4,8-dialkyl-4'-bromomethyl-5'-methylpsoralen and 4,8-dialkyl-5'-bromomethyl-4'-methylpsoralen compounds useful as intermediates.
摘要翻译：用作中间体的4,8-二烷基-4'-溴甲基-5'-甲基睾丸激素和4,8-二烷基-5'-溴甲基-4'-甲基脯氨酸化合物的合成。

6. 发明授权

US5585503A Compounds for the photodecontamination of pathogens in blood 失效
公开(公告)号：US5585503A
公开(公告)日：1996-12-17
申请号：US455053
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 , C07D493/00
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.

7. 发明授权

US5399719A Compounds for the photodecontamination of pathogens in blood 失效
公开(公告)号：US5399719A
公开(公告)日：1995-03-21
申请号：US83459
申请日：1993-06-28
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 , C07D493/00
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.

8. 发明授权

US5173482A Immunosuppressive analogues and derivatives of succinylacetone 失效
标题翻译：琥珀酰丙酮的免疫抑制类似物和衍生物
公开(公告)号：US5173482A
公开(公告)日：1992-12-22
申请号：US624078
申请日：1990-12-06
申请人： Danute E. Nitecki , Margaret Moreland , Lois Aldwin , Corey H. Levenson , Irwin Braude , David F. Mark , Henry Rapoport
发明人： Danute E. Nitecki , Margaret Moreland , Lois Aldwin , Corey H. Levenson , Irwin Braude , David F. Mark , Henry Rapoport
IPC分类号： A61K31/12 , A61K31/16 , A61K31/19 , A61K31/22 , A61K31/23 , A61K31/41
CPC分类号： A61K31/22 , A61K31/12 , A61K31/16 , A61K31/19 , A61K31/23 , A61K31/41
摘要： Succinylacetone derived or related medicaments and methods of synthesis of the same are shown wherein the medicaments consists of succinylacetonyl-proline-PEG, succinylacetonyl-NH-PEG, or compounds that have the formula: ##STR1## and that have immunosuppressive activity both in vivo and in vitro based on their activities in cellular immunologic assays and adjuvant induced arthritis in rats, respectively.
摘要翻译：所示的琥珀酰丙酮衍生物或相关药物及其合成方法，其中药物由琥珀酰丙酰基 - 脯氨酸-PEG，琥珀酰乙酰基-NH- PEG或具有下式的化合物组成：其中n = 1-6。基于它们在细胞免疫测定中的活性和大鼠中的佐剂诱导的关节炎的活性，分别在体内和体外具有免疫抑制活性。

9. 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。

10. 发明授权

US4618710A Preparation of optically active ketones 失效
标题翻译：光学活性酮的制备
公开(公告)号：US4618710A
公开(公告)日：1986-10-21
申请号：US417771
申请日：1982-09-13
申请人： Henry Rapoport , Thomas F. Buckley, III
发明人： Henry Rapoport , Thomas F. Buckley, III
IPC分类号： C07C271/06 , C07C307/02 , C07C311/00 , C07C125/065 , C07C125/067 , C07C143/74 , C07C143/78
CPC分类号： C07C307/02 , C07C271/06 , C07C311/00
摘要： An optically active alpha-amino acid derivative having the formula: ##STR1## wherein: X is OH, Cl, Br, I, or OCOR.sub.3 ;Y is a radical selected to stabilize the alpha carbon atom of the alpha-amino acid derivative sufficiently to prevent significant change in symmetry thereof during replacement of X with an alkyl, aryl, alkenyl, alkynyl, alkaryl, aralkyl, alkenaryl or alkynaryl radical, or such radical having one or more chemical constituents thereon; andR.sub.1 and R.sub.2 are different from one another and are each hydrogen or an alkyl, aryl, alkenyl, alkynyl, alkaryl, aralkyl, alkenaryl, or alkynaryl radical, or such radical having one or more non-protic chemical constituents thereon is conventionally synthesized from the corresponding alpha-amino acid. The ##STR2## portion of the above derivative is converted to a ketone functionality without racemization.
摘要翻译：具有下式的光学活性α-氨基酸衍生物：其中：X是OH，Cl，Br，I或OCOR3; Y是选择的基团，以充分稳定α-氨基酸衍生物的α碳原子，以防止在用烷基，芳基，烯基，炔基，烷芳基，芳烷基，烯芳基或炔烃基取代X时其对称性的显着变化，或这种基团在其上具有一种或多种化学成分; 并且R 1和R 2彼此不同，并且各自为氢或烷基，芳基，烯基，炔基，烷芳基，芳烷基，烯芳基或炔烃基，或者其上具有一个或多个非质子化学成分的基团通常由相应的α-氨基酸。上述衍生物的部分转化为酮官能团而不外消旋化。

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