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1.
公开(公告)号:US5198568A
公开(公告)日:1993-03-30
申请号:US756950
申请日:1991-09-09
申请人: Charles M. Zepp , Stephen A. Wald , David R. Dodds
发明人: Charles M. Zepp , Stephen A. Wald , David R. Dodds
IPC分类号: B01J19/24 , C07C219/10 , C07C305/04 , C07C305/10 , C07C309/65 , C07C309/66 , C07C327/32 , C07F9/09 , C12N11/02 , C12P1/00 , C12P7/40 , C12P41/00
CPC分类号: C12P41/005 , B01J19/2475 , C07C219/10 , C07C305/04 , C07C305/10 , C07C309/65 , C07C309/66 , C07C327/32 , C07F9/091 , C12N11/02 , C12P1/00 , C12P41/00 , C12P7/40 , B01J2219/00159 , B01J2219/00162 , B01J2219/00177
摘要: This invention relates to novel compositions of matter which are esters with enhanced water solubility, for use in aqueous enzymatic resolution reactions of racemic mixtures of these esters for producing the separate chiral isomers of the racemic mixture. The invention also relates to novel methods for preparing these esters. The importance of the production of the separate chiral isomers of the racemic mixtures resides in the isolation of the isomers which frequently have different biological activities. Of particular significance regarding the water soluble esters of this invention is that they are derivatized with groups which enhance their aqueous solubility and their reactivity with enzymatic resolving methods which are mediated in an aqueous environment.
摘要翻译: 本发明涉及物质的新型组合物,其是具有增强的水溶性的酯,用于这些酯的外消旋混合物的水性酶拆分反应中用于产生外消旋混合物的分离的手性异构体。 本发明还涉及制备这些酯的新方法。 外消旋混合物的分离手性异构体的生产的重要性在于分离经常具有不同生物活性的异构体。 对于本发明的水溶性酯具有特别意义的是它们用增强其水溶性的基团和它们与在水性环境中介导的酶拆分方法的反应性的基团衍生化。
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公开(公告)号:US5077217A
公开(公告)日:1991-12-31
申请号:US178743
申请日:1988-04-07
IPC分类号: B01J19/24 , C07C219/10 , C07C305/04 , C07C305/10 , C07C309/65 , C07C309/66 , C07C327/32 , C07F9/09 , C12M1/40 , C12N11/02 , C12N11/08 , C12P1/00 , C12P7/40 , C12P7/64 , C12P13/06 , C12P17/12 , C12P41/00
CPC分类号: C12N11/02 , B01J19/2475 , C07C219/10 , C07C305/04 , C07C305/10 , C07C309/65 , C07C309/66 , C07C327/32 , C07F9/091 , C12M21/18 , C12M25/02 , C12M29/04 , C12M29/16 , C12N11/08 , C12P1/00 , C12P41/00 , C12P41/005 , C12P7/40 , B01J2219/00159 , B01J2219/00162 , B01J2219/00177
摘要: This invention relates to novel methods for facilitating the enzymatic resolution of racemic mixtures of esters, which are derivatized with groups which enhance the esters' aqueous solubility, in an extractive member reactor where the enzyme is placed alternatively either (1) in the aqueous phase, (2) in association with the membrane, or (3) in the aqueous phase and in association with the membrane, wherein the aqueous ester phase is contacted with one side of the membrane, and where an organic extractive phase is contacted with the other side of the membrane, wherein the extractive phase serves to remove the resolving reaction product. Of particular significance regarding this invention is its use of water soluble esters that are derivatized with groups which enhance their aqueous solubility and their reactivity with enzymatic resolving methods which are mediated in an aqueous environment. Novel methods were utilized to prepare these esters, for use in this invention's methods for enzymatically resolving the racemic mixtures of the esters, to produce the separate chiral isomers of the racemic mixture. The importance of the resolution of the separate chiral isomers of the racemic mixtures resides in the isolation of the isomers which frequently have different biological activities.
摘要翻译: 本发明涉及用于促进酯的外消旋混合物的酶拆分的新方法,其在提取成分反应器中被提取酯水溶性的基团衍生化,其中酶在水相中置换为(1) (2)与膜结合,或(3)在水相中并与膜结合,其中酯水相与膜的一侧接触,并且其中有机萃取相与另一侧接触 的膜,其中萃取相用于除去拆分的反应产物。 对于本发明具有特别意义的是其使用水溶性酯,其用增强其水溶性的基团衍生化,并且它们与在水性环境中介导的酶拆分方法的反应性。 使用新的方法制备这些酯,用于本发明的用于酶拆分酯的外消旋混合物的方法,以产生外消旋混合物的分离的手性异构体。 拆分外消旋混合物的单独手性异构体的重要性在于分离经常具有不同生物活性的异构体。
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公开(公告)号:US5057427A
公开(公告)日:1991-10-15
申请号:US178950
申请日:1988-04-07
IPC分类号: C07C219/10 , C07C305/04 , C07C305/10 , C07C309/65 , C07C309/66 , C07C327/32 , C07F9/09 , C12N11/02 , C12P1/00 , C12P7/40 , C12P41/00
CPC分类号: C12P41/005 , C07C219/10 , C07C305/04 , C07C305/10 , C07C309/65 , C07C309/66 , C07C327/32 , C07F9/091 , C12N11/02 , C12P1/00 , C12P41/00 , C12P7/40
摘要: This invention relates to a novel method of effecting aqueous enzymatic and homogeneous resolutions of racemic esters which exhibit enhanced aqueous solubility. The preferred embodiment of this invention relates to the resolutions which are effected by placing the enzyme and racemic esters in an aqueous phase wherein one of the ester enantiomers is preferentially and stereospecifically de-esterified to effect the resolution of the initial racemic mixture. In another embodiment of this invention, the resolutions are effected by placing the enzyme and racemic esters in an aqueous phase, and contacting this aqueous phase with an organic phase. The preferential and stereospecific de-esterification of one of the ester enantiomers is effected, and the chiral acid product of the de-esterification reaction is extracted into the organic phase.
摘要翻译: 本发明涉及一种影响水性溶解度提高的外消旋酯的水性酶和均相分辨率的新方法。 本发明的优选实施方案涉及通过将酶和外消旋酯置于水相中进行的分辨率,其中酯对映异构体之一优先立体特异性脱酯化以实现初始外消旋混合物的拆分。 在本发明的另一个实施方案中,通过将酶和外消旋酯置于水相中并使该水相与有机相接触来实现分辨率。 实现酯对映异构体之一的优先和立体特异性去酯化,将脱酯反应的手性酸产物萃取到有机相中。
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4.
公开(公告)号:US5196568A
公开(公告)日:1993-03-23
申请号:US178735
申请日:1988-04-07
申请人: Charles M. Zepp , Stephen A. Wald , David R. Dodds
发明人: Charles M. Zepp , Stephen A. Wald , David R. Dodds
IPC分类号: B01J19/24 , C07C219/10 , C07C305/04 , C07C305/10 , C07C309/65 , C07C309/66 , C07C327/32 , C07F9/09 , C12N11/02 , C12P1/00 , C12P7/40 , C12P41/00
CPC分类号: C12P41/005 , B01J19/2475 , C07C219/10 , C07C305/04 , C07C305/10 , C07C309/65 , C07C309/66 , C07C327/32 , C07F9/091 , C12N11/02 , C12P1/00 , C12P41/00 , C12P7/40 , B01J2219/00159 , B01J2219/00162 , B01J2219/00177
摘要: This invention relates to novel compositions of matter which are esters with enhanced water solubility, for use in aqueous enzymatic resolution reactions of racemic mixtures of these esters for producing the separate chiral isomers of the racemic mixture. The invention also relates to novel methods for preparing these esters. The importance of the production of the separate chiral isomers of the racemic mixtures resides in the isolation of the isomers which frequently have different biological activities. Of particular significance regarding the water soluble esters of this invention is that they are derivatized with groups which enhance their aqueous solubility and their reactivity with enzymatic resolving methods which are mediated in an aqueous environment. In addition, the importance of these compounds resides in their being useful in novel methods for facilitating the enzymatic resolution reactions of racemic mixtures of esters, which are derivatized with groups which enhance the esters' aqueous solubility, in 1) a homogeneous aqueous reaction system where an extractive phase is not present, 2) a multiphase dispersion extractive reaction where an extractive phase is present, and 3) an extractive membrane reactor where the enzyme is placed alternatively either (a) in the aqueous phase, (b) in association with the membrane, or (c) in the aqueous phase and in association with the membrane, wherein the aqueous ester phase is contacted with one side of the membrane, and where an organic extractive phase is contacted with the other side of the membrane, wherein the extractive phase serves to remove the resolving reaction product.
摘要翻译: 本发明涉及物质的新型组合物,其是具有增强的水溶性的酯,用于这些酯的外消旋混合物的水性酶拆分反应中用于产生外消旋混合物的分离的手性异构体。 本发明还涉及制备这些酯的新方法。 外消旋混合物的分离手性异构体的生产的重要性在于分离经常具有不同生物活性的异构体。 对于本发明的水溶性酯具有特别意义的是它们用增强其水溶性的基团和它们与在水性环境中介导的酶拆分方法的反应性的基团衍生化。 此外,这些化合物的重要性在于它们可用于促进酯的外消旋混合物的酶拆分反应的新方法,其通过增强酯的水溶性的基团衍生化,在1)均匀的水反应体系中,其中 萃取相不存在,2)存在萃取相的多相分散萃取反应,和3)提取膜反应器,其中酶在(a)在水相中交替放置,(b)与 膜或(c)在水相中并与膜结合,其中酯水相与膜的一侧接触,并且其中有机萃取相与膜的另一侧接触,其中提取物 相用于除去分解反应产物。
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公开(公告)号:US06627646B2
公开(公告)日:2003-09-30
申请号:US09907556
申请日:2001-07-17
申请人: Roger P. Bakale , Chris Senanayake , Yaping Hong , Kostas Saranteas , Martin P. Redmon , Stephen A. Wald
发明人: Roger P. Bakale , Chris Senanayake , Yaping Hong , Kostas Saranteas , Martin P. Redmon , Stephen A. Wald
IPC分类号: A61K31445
CPC分类号: C07D401/12
摘要: Polymorphic crystalline forms of the antihistaminic drug norasternizole are disclosed. Processes for the production of the preferred polymorph are also disclosed.
摘要翻译: 公开了抗组胺药物诺拉非尼唑的多晶型形式。 还公开了制备优选多晶型物的方法。
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公开(公告)号:US4164400A
公开(公告)日:1979-08-14
申请号:US752884
申请日:1976-12-21
申请人: Stephen A. Wald
发明人: Stephen A. Wald
CPC分类号: B01D46/04 , B01D39/083 , B01D39/086 , B01D39/1623 , B01D2239/0464 , B01D2239/0627 , B01D2275/10 , B01D2279/55
摘要: There is provided a filter wherein the filtering means has a non-woven needled textile filter fabric with an overall bulk density of at least 6 pounds per cubic foot and bulk density gradient such that the bulk density at the face surface of the fabric is greater than the bulk density at the back surface of the fabric. In conjunction with that bulk density gradient is a filtering gradient such that the fineness of filtration at the face surface is greater than the fineness of filtration at the back surface. The filter may be in any convenient form, such as the bag of an air conveyor filter or a vacuum cleaner filter.
摘要翻译: 提供了一种过滤器,其中过滤装置具有非织造针织织物过滤织物,其整体体积密度至少为6磅/立方英尺,体积密度梯度使织物表面的体积密度大于 织物背面的体积密度。 结合该堆积密度梯度是过滤梯度,使得在表面处的过滤细度大于后表面的过滤细度。 过滤器可以是任何方便的形式,例如空气输送机过滤器的袋子或真空吸尘器过滤器。
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公开(公告)号:US06268533B1
公开(公告)日:2001-07-31
申请号:US09493042
申请日:2000-01-27
申请人: Yun Gao , Robert Hett , Kevin Q. Fang , Stephen A. Wald , Chris Hugh Senanayake
发明人: Yun Gao , Robert Hett , Kevin Q. Fang , Stephen A. Wald , Chris Hugh Senanayake
IPC分类号: C07C21752
CPC分类号: C07C205/37 , A61K9/0073 , A61K9/0075 , A61K9/0078 , A61K9/008 , C07C205/45 , C07C217/86 , C07C233/25 , C07C233/43
摘要: A method is disclosed for the preparation of optically pure isomers of formoterol by the reaction of an optically pure 4-benzyloxy-3-formamidostyrene oxide with an optically pure 4-methoxy-&agr;-methyl-N-(phenylmethyl)benzeneethanamine followed by debenzylation. Useful intermediates in the process are also disclosed, as are the novel L-tartrate salt of R,R-formoterol and pharmaceutical compositions thereof.
摘要翻译: 公开了通过光学纯的4-苄氧基-3-甲酰氨基苯乙烯氧化物与光学纯的4-甲氧基-α-甲基-N-(苯基甲基)苯乙胺的反应,然后脱苄基反应制备福莫特罗的光学纯异构体的方法。 还公开了该方法中有用的中间体,以及R,R-福莫特罗的新型L-酒石酸盐及其药物组合物。
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公开(公告)号:US4257791A
公开(公告)日:1981-03-24
申请号:US65529
申请日:1979-08-10
申请人: Stephen A. Wald
发明人: Stephen A. Wald
CPC分类号: B01D46/0001 , B01D39/083 , B01D39/086 , B01D39/1623 , B01D46/0075 , B01D46/04 , B01D46/10 , B01D46/2411 , B01D2239/04 , B01D2239/0464 , B01D2239/0654 , B01D2239/1291 , B01D2275/10 , B01D2279/55 , B01D2279/60
摘要: There is provided a filter wherein the filtering means has a non-woven needled textile filter fabric with an overall bulk density of at least 6 pounds per cubic foot and bulk density gradient such that the bulk density at the face surface of the fabric is greater than the bulk density at the back surface of the fabric. In conjunction with that bulk density gradient is a filtering gradient such that the fineness of filtration at the back face surface is greater than the fineness of filtration at the surface. The filter may be in any convenient form, such as the bag of an air conveyor filter or a vacuum cleaner filter.
摘要翻译: 提供了一种过滤器,其中过滤装置具有非织造针织织物过滤织物,其整体体积密度至少为6磅/立方英尺,体积密度梯度使织物表面的体积密度大于 织物背面的体积密度。 结合该堆积密度梯度是过滤梯度,使得背面表面的过滤细度大于表面处的过滤细度。 过滤器可以是任何方便的形式,例如空气输送机过滤器的袋子或真空吸尘器过滤器。
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公开(公告)号:US6040344A
公开(公告)日:2000-03-21
申请号:US83010
申请日:1998-05-21
申请人: Yun Gao , Robert Hett , Kevin Q. Fang , Stephen A. Wald , Martin P. Redmon , Chris Hugh Senanayake
发明人: Yun Gao , Robert Hett , Kevin Q. Fang , Stephen A. Wald , Martin P. Redmon , Chris Hugh Senanayake
IPC分类号: B01J23/42 , A61K9/00 , A61K9/10 , A61K9/14 , A61K9/20 , A61K9/48 , A61K31/167 , A61P11/08 , A61P43/00 , C07B61/00 , C07C205/37 , C07C205/45 , C07C213/02 , C07C217/60 , C07C217/86 , C07C231/18 , C07C233/25 , C07C233/43 , A61K31/16 , C07C233/03
CPC分类号: C07C205/37 , C07C205/45 , C07C217/86 , C07C233/25 , C07C233/43 , A61K9/0073 , A61K9/0075 , A61K9/0078 , A61K9/008
摘要: A method is disclosed for the preparation of optically pure isomers of formoterol by the reaction of an optically pure 4-benzyloxy-3-formamidostyrene oxide with an optically pure 4-methoxy-.alpha.-methyl-N-(phenylmethyl)benzeneethanamine followed by debenzylation. Useful intermediates in the process are also disclosed, as are the novel L-tartrate salt of R,R-formoterol and pharmaceutical compositions thereof.
摘要翻译: 公开了通过光学纯的4-苄氧基-3-甲酰氨基苯乙烯氧化物与光学纯的4-甲氧基-α-甲基-N-(苯基甲基)苯乙胺的反应,然后脱苄基化制备福莫特罗的光学纯异构体的方法。 还公开了该方法中有用的中间体,以及R,R-福莫特罗的新型L-酒石酸盐及其药物组合物。
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公开(公告)号:US4350727A
公开(公告)日:1982-09-21
申请号:US306533
申请日:1981-09-28
申请人: Stephen A. Wald , Robert W. Carter
发明人: Stephen A. Wald , Robert W. Carter
CPC分类号: D06M17/00 , A41D31/02 , B32B5/06 , Y10T428/24033 , Y10T428/24331 , Y10T428/24992 , Y10T442/494
摘要: A textile composite is provided which comprises a non-woven textile fabric, composed of textile fibers needled together into a network of coherently entangled fibers and having an overall bulk density of between 4 and 20 lbs. per cubic foot, and a knitted textile fabric, having a weight of between 1 and 8 ozs. per square yard, bound to the needled fabric. The binding of the fabrics is such that at least one tensile property of the composite is greater than the sum of that same property of the non-woven and knitted fabrics. That same property is measurable at an extension which is the same or less than the extension at failure of the composite.
摘要翻译: 提供了一种纺织复合材料,其包括无纺织物,其由纺织纤维组成,所述纤维针织在一起成为相干缠结纤维的网络,并且具有4至20磅的总体积密度。 每立方英尺,以及重量为1至8盎司的针织纺织品。 每平方码,绑在针织面料上。 织物的结合使得复合材料的至少一个拉伸性能大于无纺布和针织织物的相同性质的总和。 相同的属性可以在扩展时可测量,该扩展与复合材料失效时的扩展相同或更小。
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