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1.发明授权Method for the synthesis of pharmacologically active compounds and intermediates for such synthesis 失效用于合成药理学活性化合物的方法和用于这种合成的中间体
公开(公告)号：US4777293A
公开(公告)日：1988-10-11
申请号：US753682
申请日：1985-07-10
申请人： Bo R. Lamm
发明人： Bo R. Lamm
IPC分类号： C07D521/00 , C07C67/00 , C07C213/00 , C07C217/32 , C07D295/182 , C07D321/06 , C07C93/06 , C07D209/04 , C07D417/04
CPC分类号： C07D295/182 , C07D321/06 , Y02P20/55
摘要： A process for the preparation of an aryloxypropanolamine of the formulaAr--OCH.sub.2 CH(OH)CH.sub.2 NH--R Iwherein Ar is a carbocyclic or heterocyclic aromatic group and R is an alkyl or substituted alkyl group having 1 to 6 carbon atoms, characterized in subjecting a compound of the formula ##STR1## to oxidative cleavage to a dialdehyde of the formula ##STR2## which is then made subject to reduction, amination, acetal hydrolysis, and, where required, removal of a nitrogen protective group, to the formation of a compound of formula I, or an acid addition salt thereof, a compound of formula II and the preparation thereof from mannitol.
摘要翻译： 一种制备式Ar-OCH 2 CH（OH）CH 2 NH-RI的芳氧基丙醇胺的方法，其中Ar是碳环或杂环芳族基团，R是具有1至6个碳原子的烷基或取代的烷基，其特征在于使化合物 式II的氧化裂解制成式“IMAGE”III的二醛，然后将其还原，胺化，缩醛水解，并且在需要时除去氮保护基团以形成 式I化合物或其酸加成盐，式II化合物及其从甘露醇制备。
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2.发明授权
公开(公告)号：US4544750A
公开(公告)日：1985-10-01
申请号：US526900
申请日：1983-08-26
申请人： Arne E. Brandstrom , Bo R. Lamm
发明人： Arne E. Brandstrom , Bo R. Lamm
IPC分类号： A61K31/44 , C07D213/68 , C07D213/89 , C07D401/12
CPC分类号： C07D213/89 , C07D213/68
摘要： Novel compounds of the formula ##STR1## wherein R is H or CH.sub.3, a process for their preparation, and their use as intermediates in the preparation of pharmaceutically useful compounds, e.g. substituted benzimidazoles containing a pyridine radical, i.a. omeprazole.
摘要翻译： 新颖的式（IMAGE）化合物，其中R是H或CH 3，它们的制备方法，以及它们作为制备药用有用化合物的中间体的用途。 含吡啶基的取代苯并咪唑，例如 奥美拉唑
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3.发明授权Separation of enantiomers of non-steroidal anti-inflammatory drugs and chiral selector therefor 失效分离非甾体抗炎药物和手性选择剂的对映异构体
公开(公告)号：US5387338A
公开(公告)日：1995-02-07
申请号：US89861
申请日：1993-07-09
IPC分类号： C07B57/00 , C07C51/487 , C07C233/65 , C07D307/00 , C07D307/92 , B01D15/08
CPC分类号： C07D307/00 , C07B57/00 , C07C233/65 , C07C51/487 , C07D307/92 , C07C2103/26
摘要： The invention relates to a chiral selector useful in separating underivatized enantiomers of nonsterodial anti-inflammatory agents, particularly naproxen and other arylacetic acid compounds, and relates to a process for achieving such separation utilizing the chiral selector, which is also useful in achieving the enantiomeric separation of amines, alcohol derivatives, epoxides and sulfoxides. The invention is also directed to an apparatus which comprises the chiral selectors.
摘要翻译： 本发明涉及可用于分离非甾体抗炎剂，特别是萘普生和其它芳基乙酸化合物的未衍生化对映异构体的手性选择剂，涉及使用手性选择剂实现这种分离的方法，其也可用于实现对映异构体分离 的胺，醇衍生物，环氧化物和亚砜。 本发明还涉及一种包括手性选择器的装置。
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4.发明授权Separation of enantiomers of non-steroidal anti-inflammatory drugs and chiral selector therefor 失效分离非甾体抗炎药物和手性选择剂的对映异构体
公开(公告)号：US5256293A
公开(公告)日：1993-10-26
申请号：US847449
申请日：1992-03-09
IPC分类号： C07B57/00 , C07C51/487 , C07C233/65 , C07D307/00 , C07D307/92 , B01D15/08
CPC分类号： C07D307/00 , C07B57/00 , C07C233/65 , C07C51/487 , C07D307/92 , C07C2103/26
摘要： The invention relates to a chiral selector useful in separating underivatized enantiomers of nonsterodial anti-inflammatory agents, particularly naproxen and other arylacetic acid compounds, and relates to a process for achieving such separation utilizing the chiral selector, which is also useful in achieving the enantiomeric separation of amines, alcohol derivatives, epoxides and sulfoxides. The invention is also directed to an apparatus which comprises the chiral selectors.
摘要翻译： 本发明涉及可用于分离非甾体抗炎剂，特别是萘普生和其它芳基乙酸化合物的未衍生化对映异构体的手性选择剂，涉及使用手性选择剂实现这种分离的方法，其也可用于实现对映异构体分离 的胺，醇衍生物，环氧化物和亚砜。 本发明还涉及一种包括手性选择器的装置。
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5.发明授权
公开(公告)号：US5484530A
公开(公告)日：1996-01-16
申请号：US321200
申请日：1994-10-11
IPC分类号： C07B57/00 , C07C51/487 , C07C233/65 , C07D307/00 , C07D307/92 , B01D15/08
CPC分类号： C07D307/00 , C07B57/00 , C07C233/65 , C07C51/487 , C07D307/92 , C07C2103/26
摘要： The invention relates to a chiral selector useful in separating underivatized enantiomers of nonsterodial anti-inflammatory agents, particularly naproxen and other arylacetic acid compounds, and relates to a process for achieving such separation utilizing the chiral selector, which is also useful in achieving the enantiomeric separation of amines, alcohol derivatives, epoxides and sulfoxides. The invention is also directed to an apparatus which comprises the chiral selectors.
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6.发明授权Stereoisomers of benzonitrile derivatives, useful as cardiac arrhythmiac agents 失效苯并噻唑衍生物的立体异构体，有用的作为心脏抗坏血酸剂
公开(公告)号：US5055490A
公开(公告)日：1991-10-08
申请号：US539852
申请日：1990-06-18
IPC分类号： A61K31/275 , A61K31/10 , A61K31/13 , A61P9/06 , C07C205/30 , C07C205/34 , C07C315/04 , C07C317/00 , C07C317/02 , C07C317/28
CPC分类号： C07C317/28
摘要： 4-[3-[ethyl[3-((R*)-propylsulfinyl)propyl]amino]-2(R)-hydroxypropoxy]-benzonitrile,4-[3-[ethyl[3-((S*)-propylsulfinyl)propyl]amino]-2(R)-hydroxypropoxy]-benzonitrile,4-[3-[ethyl[3-((R*)-propylsulfinyl)propyl]amino]-2(S)-hydroxypropoxy]-benzonitrile,4-[3-[ethyl[3-[((S*)-propylsulfinyl)propyl]amino]-2(S)-hydroxypropoxy]-benzonitrile andpharmaceutically acceptable salt thereof, processes for their preparation, as well as the use of said compounds for the preparation of medicaments with action against cardiac arrhythmias.
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公开(公告)号：US4620008A
公开(公告)日：1986-10-28
申请号：US697396
申请日：1985-02-01
申请人： Arne E. Brandstrom , Bo R. Lamm
发明人： Arne E. Brandstrom , Bo R. Lamm
IPC分类号： A61K31/44 , C07D213/68 , C07D213/89 , C07D401/12
CPC分类号： C07D213/89 , C07D213/68
摘要： Novel compounds of the formula ##STR1## wherein R is H or CH.sub.3, a process for their preparation, and their use as intermediates in the preparation of pharmaceutically useful compounds, e.g. substituted benzimidazoles containing a pyridine radical, i.a. omeprazole.
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