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1. 发明授权

US5648505A Method for the preparation of a novel C-ring precursor for taxoids and novel intermediates 失效
标题翻译：用于制备紫杉类和新型中间体的新型C环前体的方法
公开(公告)号：US5648505A
公开(公告)日：1997-07-15
申请号：US447843
申请日：1995-05-23
申请人： Zhi-Qiang Xia , Esko Karvinen , Ari Koskinen
发明人： Zhi-Qiang Xia , Esko Karvinen , Ari Koskinen
IPC分类号： C07D317/72 , C07D493/10
CPC分类号： C07D317/72 , C07D493/10
摘要： The present invention relates to a process for the preparation of a compound of the formula (VIII) or (IX) useful as precursor for the C-ring in taxanes ##STR1## wherein R' is a C.sub.1 -C.sub.6 -alkyl. The invention further relates to the novel compounds (VIII) and (IX) and to novel intermediates in said process.
摘要翻译：本发明涉及一种制备式（Ⅷ）或（Ⅸ）化合物的方法，其可用作紫杉烷中的C-环的前体，其中R'为 C1-C6-烷基。本发明还涉及新化合物（VIII）和（IX）以及所述方法中的新型中间体。

2. 发明授权

US5498738A Method for the preparation of a novel a-ring precursor for taxoids and novel intermediates 失效
标题翻译：用于制备紫杉类和新型中间体的新型α-环前体的方法
公开(公告)号：US5498738A
公开(公告)日：1996-03-12
申请号：US266557
申请日：1994-06-28
申请人： Esko Karvinen , Ari Koskinen
发明人： Esko Karvinen , Ari Koskinen
IPC分类号： C07C67/14 , C07C67/283 , C07C67/29 , C07C69/007 , C07C69/145 , C07C69/24 , C07D305/14 , C07F7/18 , C07F7/08
CPC分类号： C07F7/1856 , C07C67/14 , C07C67/283 , C07C67/29 , C07C69/007 , C07D305/14
摘要： The present invention a process for the preparation of a compound of the formula (X) useful as precursor for the A-ring in taxanes ##STR1## wherein R' is an ##STR2## in which R" is a linear, branched or cyclic alkyl group of 1 to 10 carbon atoms. The invention further relates to the novel compound (X) and to novel intermediates in said process.
摘要翻译：本发明制备式（X）化合物的方法，其用作紫杉烷中的A环的前体，其中R'是其中R“为直链的，具有1-10个碳原子的支链或环状烷基。本发明还涉及新化合物（X）和所述方法中的新型中间体。

3. 发明授权

US5426228A General method for preparation of sphingosine bases and their analogues 失效
标题翻译：鞘氨醇碱及其类似物的制备方法
公开(公告)号：US5426228A
公开(公告)日：1995-06-20
申请号：US265776
申请日：1994-06-27
申请人： Ari Koskinen , Paivi Koskinen
发明人： Ari Koskinen , Paivi Koskinen
IPC分类号： C07C213/00 , C07C209/68 , C07C209/62
CPC分类号： C07C213/00 , Y02P20/55
摘要： Described herein is a novel method of preparing selectively diastereomers of sphingosine bases and their analogues of general formula (1a) or (1b) ##STR1## where R is an aliphatic or aromatic substituent containing a straight, branched or cyclic chain, which may include one or several heteroatoms as chain members and one or several functional groups as substituents. The method comprises the steps of:a) converting a starting material into an intermediate product in the form of .alpha.,.beta.-unsaturated ketone having the general formula (4a) or (4b) ##STR2## where R is as defined above and PG are any protecting groups compatible with the method,b) reducing said .alpha.,.beta.-unsaturated ketone to an aminoalcohol with DIBAL in toluene to obtain selectively an anti-diastereomer, andc) removing the protecting groups to obtain the free sphingosine base or its analogue according to formula (1a) or (1b).
摘要翻译：本文描述了选择性地制备鞘氨醇碱基的非对映异构体的新方法及其通式（1a）或（1b）的类似物。其中R是含有直链，支链或环状链，其可以包括一个或几个作为链成员的杂原子和一个或几个官能团作为取代基。该方法包括以下步骤：a）将原料转化为具有通式（4a）或（4b）的α，β-不饱和酮形式的中间产物（4a）（4b）其中R如上所定义，PG是与该方法相容的任何保护基团，b）在甲苯中将所述α，β-不饱和酮还原为具有DIBAL的氨基醇，以选择性地获得反非对映异构体，和c）将保护基团除去获得根据式（1a）或（1b）的游离的鞘氨醇碱或其类似物。

4. 发明申请

US20070134757A1 Method for cleaving proteins 审中-公开
标题翻译：切割蛋白的方法
公开(公告)号：US20070134757A1
公开(公告)日：2007-06-14
申请号：US10563826
申请日：2004-07-08
申请人： Markus Linder , Jussi Jantti , Hans Soderlund , Juho Helaja , Ari Koskinen
发明人： Markus Linder , Jussi Jantti , Hans Soderlund , Juho Helaja , Ari Koskinen
IPC分类号： C12P21/06 , C07K14/47
CPC分类号： C07K1/12 , C07K1/1075
摘要： This, invention relates to a method for cleaving proteins or peptides at a specific site. According to the invention an amino acid sequence is constructed at a predetermined cleavage site and the protein or peptide is allowed to react with free metal ions in a buffer. The buffer further comprises a reducing or oxidizing agent for enhancing the cleavage. The amino acids in the amino acid sequence are selected from the group comprising histidine, lysine, tryptophan, arginine, tyrosine, phenylalanine, and cysteine.
摘要翻译：本发明涉及在特定部位切割蛋白质或肽的方法。根据本发明，在预定的切割位点构建氨基酸序列，并使蛋白质或肽与缓冲液中的游离金属离子反应。缓冲剂还包含用于增强裂解的还原或氧化剂。氨基酸序列中的氨基酸选自组氨酸，赖氨酸，色氨酸，精氨酸，酪氨酸，苯丙氨酸和半胱氨酸。

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