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公开(公告)号：US06531589B1
公开(公告)日：2003-03-11
申请号：US08598320
申请日：1996-02-08
申请人： Radhakrishnan P. Iyer , Theresa Devlin , Ivan Habus , Dong Yu , Sudhir Agrawal , Nan-Hui Ho
发明人： Radhakrishnan P. Iyer , Theresa Devlin , Ivan Habus , Dong Yu , Sudhir Agrawal , Nan-Hui Ho
IPC分类号： C07H2100
摘要： The invention provides new methods for synthesizing oligonucleotides that allow for deprotection of the oligonucleotides under more mild conditions than existing methods. The invention further provides a nucleoside base protecting group that is stable under oligonucleotide synthesis conditions, but which can be removed under more mild conditions than existing protecting groups, as well as nucleoside synthons having such base protecting groups.
摘要翻译： 本发明提供了合成寡核苷酸的新方法，其允许在比现有方法更温和的条件下对寡核苷酸进行脱保护。 本发明还提供了在寡核苷酸合成条件下稳定但可在比现有保护基更温和的条件下除去的核苷碱保护基，以及具有这种碱保护基的核苷合成子。
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2.发明授权Synthesis of oligonucleotides containing alkylphosphonate internucleoside linkages 失效含有烷基膦酸酯核苷间键的寡核苷酸的合成
公开(公告)号：US5962674A
公开(公告)日：1999-10-05
申请号：US606915
申请日：1996-02-26
申请人： Radhakrishnan P. Iyer , Theresa Devlin , Ivan Habus , Dong Yu , Sudhir Agrawal
发明人： Radhakrishnan P. Iyer , Theresa Devlin , Ivan Habus , Dong Yu , Sudhir Agrawal
摘要： The invention provides new reagents and an improved process for synthesizing oligonucleotides that contain methylphosphonate internucleoside linkages. The reagents and process utilize a nucleoside base protecting group that is stable under oligonucleotide synthesis conditions, but which can be removed under more mild conditions than existing protecting groups.
摘要翻译： 本发明提供新的试剂和用于合成含有甲基膦酸核苷间键的寡核苷酸的改进方法。 试剂和方法利用在寡核苷酸合成条件下稳定的核苷碱基保护基，但可以在比现有保护基更温和的条件下除去。
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3.发明授权Process for making oligonucleotides containing o- and s- methylphosphotriester internucleoside linkages 失效制备含有O-和S-甲基磷酸核苷间核苷键的寡核苷酸的方法
公开(公告)号：US5955599A
公开(公告)日：1999-09-21
申请号：US570390
申请日：1995-12-11
申请人： Radhakrishnan P. Iyer , Theresa Devlin , Ivan Habus , Dong Yu , Sudhir Agrawal
发明人： Radhakrishnan P. Iyer , Theresa Devlin , Ivan Habus , Dong Yu , Sudhir Agrawal
摘要： The invention provides oligonucleotides containing methyl phosphotriester linkages and processes for making and methods for using such oligonucleotides.
摘要翻译： 本发明提供了含有甲基磷酸三酯键的寡核苷酸及其制备方法和使用这些寡核苷酸的方法。
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4.发明授权Primary phosphoramidate internucleoside linkages and oligonucleotides containing the same 失效初级氨基磷酸核苷间核苷键和含有其的寡核苷酸
公开(公告)号：US6140482A
公开(公告)日：2000-10-31
申请号：US519318
申请日：1995-08-25
申请人： Radhakrishnan P. Iyer , Theresa Devlin , Ivan Habus , Dong Yu , Sudhir Agrawal
发明人： Radhakrishnan P. Iyer , Theresa Devlin , Ivan Habus , Dong Yu , Sudhir Agrawal
摘要： The invention provides new primary phosphoramidate internucleoside linkages that are less sterically constrained than existing phosphoramidate linkages, as well as oligonucleotides containing such linkages and processes for making and methods for using such oligonucleotides.
摘要翻译： 本发明提供了比现有氨基磷酸酯键更少的空间限制的新的初级氨基磷酸酯核苷间键，以及含有这种连接的寡核苷酸和制备方法以及使用这种寡核苷酸的方法。
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5.发明授权5-pentenoyl moiety as a nucleoside-amino protecting group, 4-pentenoyl-protected nucleotide synthons, and related oligonucleotide syntheses 失效5-戊烯酰基部分作为核苷 - 氨基保护基，4-戊烯酰基保护的核苷酸合成子和相关的寡核苷酸合成
公开(公告)号：US5614622A
公开(公告)日：1997-03-25
申请号：US518921
申请日：1995-08-24
申请人： Radhakrishnan P. Iyer , Theresa Devlin , Ivan Habus , Dong Yu , Sudhir Agrawal
发明人： Radhakrishnan P. Iyer , Theresa Devlin , Ivan Habus , Dong Yu , Sudhir Agrawal
摘要： The invention provides new methods for synthesizing oligonucleotides that allow for deprotection of the oligonucleotide under more mild conditions than existing methods. The invention further provides a nucleoside base protective group that is stable under oligonucleotide synthesis conditions, but which can be removed under more mild conditions than existing protective groups, as well as nucleoside synthons having such base protective groups.
摘要翻译： 本发明提供了合成寡核苷酸的新方法，其允许寡核苷酸在比现有方法更温和的条件下脱保护。 本发明还提供了在寡核苷酸合成条件下稳定但可在比现有保护基更温和的条件下除去的核苷碱基保护基以及具有这种碱性保护基的核苷合成子。
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公开(公告)号：US4853416A
公开(公告)日：1989-08-01
申请号：US185463
申请日：1988-04-25
IPC分类号： A61K9/00 , A61K9/08 , A61K31/155 , A61K47/04 , A61P33/02 , C07C257/18
CPC分类号： A61K9/0078 , A61K31/155
摘要： A pharmaceutical composition comprising an aqueous solution of pentamidine or a pharmaceutically acceptable salt thereof, the solution having a pH of less than 4.5. The pH of the solution is preferably less than 4.0, more preferably less than 3.5, and especially less than 3.0.Also disclosed is a method for the prophylactic or remedial treatment of pneumo-cystis carinii pneumonia, which method comprises administration by inhalation to a patient having or being susceptible to that condition of a therapeutically effective quantity of an aqueous solution of pentamidine, or a pharmaceutically acceptable salt thereof, the solution having a pH of less than 4.5.
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