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1. 发明授权

US4035352A Preparation of 7-substituted amino-desacetoxycephalosporanic acid compounds 失效
标题翻译： 7-取代氨基 - 脱乙酰氧基头孢烷酸化合物的制备
公开(公告)号：US4035352A
公开(公告)日：1977-07-12
申请号：US575024
申请日：1975-05-06
申请人： Jan Verweij , Hong Sheng Tan , Hermanus Jacobus Kooreman
发明人： Jan Verweij , Hong Sheng Tan , Hermanus Jacobus Kooreman
IPC分类号： C07D499/00 , C07D501/10 , C07D499/32
CPC分类号： C07D501/10 , C07D499/00
摘要： Novel 6-substituted amino-penicillanic acid anhydrides useful in the process for the preparation of 7-substituted amino-desacetoxycephalosporanic derivatives comprising converting a 6-substituted amino-penicillanic acid sulfoxide into an anhydride of a 6-substituted amino-penicillanic acid sulfoxide, heating the said acid anhydride intermediate at a temperature up to at most 160.degree. C in a dry inert organic solvent with an anhydrous acid which is capable of causing ring expansion of the penam ring to a .DELTA..sup.3 -cephem ring, in the presence of a silicon-containing compound capable of (a) removing water formed during the ring enlargement of the penam structure fast enough to prevent water hydrolysis of the acid anhydride moiety present and (b) forming neutral or basic products on hydrolysis, the aforesaid acid being strong enough not to be, or not to a substantial extent to be, silylated under the reaction conditions employed, and hydrolyzing the resulting compound in situ to form the .DELTA..sup.3 -7-substituted amino-desacetoxycephalosporanic acid as such or as a salt, such as alkali metal, alkaline earth metal or amine salt.
摘要翻译：用于制备7-取代氨基 - 脱乙酰氧基头孢烷衍生物的方法中的6-取代氨基 - 青霉烷酸酐包括将6-取代氨基 - 青霉烷酸亚砜转化成6-取代氨基 - 青霉烷酸亚砜的酸酐，加热所述酸酐中间体在干燥的惰性有机溶剂中在至多160℃的温度下与无水酸反应，所述无水酸在硅的存在下能够引起环吡嗪环向DELTA 3-头孢烯环的扩展能够（a）在Penam结构的环扩大期间形成的水快速去除以防止存在的酸酐部分的水解，和（b）在水解时形成中性或碱性产物，上述酸不足够在所使用的反应条件下是或不在很大程度上甲硅烷基化，并原位水解所得化合物以形成DEL TA 3-7取代的氨基 - 脱乙酰氧基头孢烷酸，或作为盐，如碱金属，碱土金属或胺盐。

2. 发明授权

US4046761A Process for preparing cephalosporin derivatives 失效
标题翻译：制备头孢菌素衍生物的方法
公开(公告)号：US4046761A
公开(公告)日：1977-09-06
申请号：US664056
申请日：1976-03-04
申请人： Jan Verweij , Hong Sheng Tan
发明人： Jan Verweij , Hong Sheng Tan
IPC分类号： C07D207/46 , C07D209/48 , C07D501/10 , C07D501/02 , A61K31/545
CPC分类号： C07D209/48 , C07D207/46
摘要： Novel azetidine derivatives of the formula ##STR1## wherein R.sub.1 is an acylamido group, R.sub.2 is selected from the group consisting of ##STR2## wherein R.sub.4, R.sub.5 and R.sub.6 are individually selected from the group consisting of hydrogen, lower alkyl and lower alkenyl, n is 2 or 3 and -- in the case when formula IIB is a phenyl -- this group may carry 1 to 4 substituents selected from the group consisting of halogen, lower alkyl, lower alkenyl and phenyl, and R.sub.3 is lower alkyl optionally substituted with 1 or 2 phenyls which phenyl groups may be substituted with nitro and a process for their preparation and process for the preparation of cephalosporanic acid derivatives using the azetidines of formula I as intermediates.This is a division of Serial No. 547,948, filed Feb. 7, 1975 now Pat. No. 4,007,202.
摘要翻译：新颖的式Ⅰa的氮杂环丁烷衍生物，其中R1是酰氨基，R2选自由下列组成的组：其中R 4，R 5和R 6分别选自氢，低级烷基和低级烯基，n为2或3， - 在式IIB为苯基的情况下，该基团可以携带1至4个选自卤素，低级烷基，低级烯基和苯基的取代基，且R3较低任选被1或2个苯基取代的烷基，该苯基可以被硝基取代，其制备方法和使用式I的氮杂环丁烷作为中间体制备头孢烷酸衍生物的方法。

3. 发明授权

US4003894A Preparation of 7-substituted amino-desacetoxycephalosporanic acid compounds 失效
标题翻译： 7-取代氨基 - 脱乙酰氧基头孢烷酸化合物的制备
公开(公告)号：US4003894A
公开(公告)日：1977-01-18
申请号：US574365
申请日：1975-05-05
申请人： Jan Verweij , Hong Sheng Tan , Hermanus Jacobus Kooreman
发明人： Jan Verweij , Hong Sheng Tan , Hermanus Jacobus Kooreman
IPC分类号： C07D501/10
CPC分类号： C07D501/10
摘要： Process for the preparation of 7-substituted amino-desacetoxycephalosporanic derivatives comprising converting a 6-substituted amino-penicillanic acid sulfoxide into an anhydride of a 6-substituted amino-penicillanic acid sulfoxide, heating the said acid anhydride intermediate at a temperature up to at most 160.degree. C in a dry inert organic solvent with an anhydrous acid which is capable of causing ring expansion of the penam ring to a .DELTA..sup.3 -cephem ring, in the presence of a silicon-containing compound capable of (a) removing water formed during the ring enlargement of the penam structure fast enough to prevent water hydrolysis of the acid anhydride moiety present and (b) forming neutral or basic products on hydrolysis, the aforesaid acid being strong enough not to be, or not to a substantial extent to be, silylated under the reaction conditions employed, and hydrolyzing the resulting compound in situ to form the .DELTA..sup.3 -7-substituted amino-desacetoxycephalosporanic acid as such or as a salt, such as alkali metal, alkaline earth metal or amine salt and to the novel sulfoxide acid anhydrides formed therein.
摘要翻译：用于制备7-取代的氨基 - 脱乙酰氧基头孢烷衍生物的方法，包括将6-取代的氨基 - 青霉烷酸亚砜转化为6-取代的氨基 - 青霉烷酸亚砜的酸酐，将所述酸酐中间体加热至多至多 160℃在干燥惰性有机溶剂中与无水酸反应，该无水酸能够在含硅化合物的存在下使Penam环环化为DELTA 3-头孢烯环，所述含硅化合物能够（a）除去在阳离子结构的环扩大足够快以防止存在的酸酐部分的水解，和（b）在水解时形成中性或碱性产物，上述酸足够强，不大或不在很大程度上是在所用的反应条件下甲硅烷基化，并原位水解所得化合物，形成DELTA 3-7-取代的氨基 - 脱乙酰氧基头孢烷酸，或者如盐，如碱金属，碱土金属或胺盐，以及其中形成的新的亚砜酸酐。

4. 发明授权

US4007202A Azetidine derivatives 失效
标题翻译：氮杂环丁烷衍生物
公开(公告)号：US4007202A
公开(公告)日：1977-02-08
申请号：US547948
申请日：1975-02-07
申请人： Jan Verweij , Hong Sheng Tan
发明人： Jan Verweij , Hong Sheng Tan
IPC分类号： C07D205/08 , A61K31/545 , C07D201/02 , C07D205/095 , C07D207/46 , C07D209/48 , C07D401/12 , C07D403/12 , C07D501/08 , C07D501/10 , C07D501/30 , C07D501/60 , C07D207/12
CPC分类号： C07D209/48 , C07D207/46
摘要： Novel azetidine derivatives of the formula ##STR1## wherein R.sub.1 is an acylamido group, R.sub.2 is selected from the group consisting of ##STR2## wherein R.sub.4, R.sub.5 and R.sub.6 are individually selected from the group consisting of hydrogen, lower alkyl and lower alkenyl, n is 2 or 3 and -- in the case when formula IIB is a phenyl - this group may carry one to four substituents selected from the group consisting of halogen, lower alkyl, lower alkenyl and phenyl, and R.sub.3 is lower alkyl optionally substituted with 1 or 2 phenyls which phenyl groups may be substituted with nitro and the dotted lines of formula IIB indicate the optional presence of double bonds and a process for their preparation and process for the preparation of cephalosporanic acid derivatives using the azetidines of formula I as intermediates.
摘要翻译：新颖的式Ⅰa的氮杂环丁烷衍生物，其中R 1是酰氨基，R 2选自其中R 4，R 5和R 6各自独立地选自下列的组合：IIA IIB IIC IID 由氢，低级烷基和低级烯基组成的组，n为2或3， - 在式IIB为苯基的情况下，该基团可以携带一至四个选自以下的取代基：卤素，低级烷基，低级烯基和苯基，R3是任选被1或2个苯基取代的低级烷基，该苯基可以被硝基取代，式IIB的虚线表示双键的任选存在，以及它们的制备方法和制备方法使用式I的氮杂环丁烷的头孢烷酸衍生物作为中间体。

5. 发明授权

US6117433A Use of compositions comprising stabilized biologically effective compounds 失效
标题翻译：使用包含稳定的生物有效化合物的组合物
公开(公告)号：US6117433A
公开(公告)日：2000-09-12
申请号：US930685
申请日：1998-04-28
申请人： Luppo Edens , Hong Sheng Tan , Johannes Wilhelmus Jacobus Lambers
发明人： Luppo Edens , Hong Sheng Tan , Johannes Wilhelmus Jacobus Lambers
IPC分类号： A61K8/02 , A61K8/34 , A61K8/35 , A61K8/66 , A61K9/08 , A61K9/10 , A61K31/70 , A61K38/46 , A61K38/48 , A61K47/10 , A61Q5/02 , B05B11/00 , A61K9/14
CPC分类号： A61K9/10 , A61K9/08 , B05B11/3084
摘要： A dual chambered dispensing system allows for application of an aqueous composition containing a biologically effective compound which is adequately stabilized. The system separately contains the stabilized biologically effective compound composition in one chamber and an aqueous basic composition in the other. Both compositions are simultaneously delivered from the dispensing system, whereupon the compositions are mixed to result in a final composition suitable for direct application.
摘要翻译： PCT No.PCT / EP97 / 00507 Sec。 371日期：1998年4月8日 102（e）日期1998年4月8日PCT 1997年1月31日PCT PCT。第WO97 / 27841号公报日期1997年8月7日双室分配系统允许施加含有适当稳定的生物有效化合物的含水组合物。该系统在一个室中分开含有稳定的生物有效的化合物组合物，另一个含有碱性组合物。两种组合物同时从分配系统递送，于是组合物被混合以产生适于直接施用的最终组合物。

6. 发明授权

US06369036B1 Antifungal composition 失效
标题翻译：抗真菌组合物
公开(公告)号：US06369036B1
公开(公告)日：2002-04-09
申请号：US09069534
申请日：1998-04-30
申请人： Ferdinand Theodorus Van Rijn , Jacobus Stark , Hong Sheng Tan , Willem Johan Van Zoest , Nicolaas Cornelis Barendse
发明人： Ferdinand Theodorus Van Rijn , Jacobus Stark , Hong Sheng Tan , Willem Johan Van Zoest , Nicolaas Cornelis Barendse
IPC分类号： A61K3170
CPC分类号： C12Q1/18 , A01N25/02 , A01N43/90 , A01N63/02 , A23C19/11 , A23C19/16 , A23C19/163 , A23L3/34635 , A61K31/70 , C07H17/08 , G01N33/56961 , A01N25/08 , A01N25/04 , A01N2300/00
摘要： The present invention provides a method of preparing an improved antifungal composition containing an antifungal compound of the polyene type such as natamycin wherein the antifungal compound is incorporated into the composition in a form which shows an enhanced activity, e.g. in the form of a solution and/or being in a modified polymorphic form.
摘要翻译：本发明提供一种制备改进的抗真菌组合物的方法，所述抗真菌组合物含有多烯类抗真菌化合物，例如那他霉素，其中抗真菌化合物以显示增强活性的形式，例如，以溶液的形式和/或处于修饰的多晶形式。

7. 发明授权

US3962277A Acetidine derivatives 失效
标题翻译：维生素D衍生物
公开(公告)号：US3962277A
公开(公告)日：1976-06-08
申请号：US619843
申请日：1975-10-06
申请人： Jan Verwey , Hong Sheng Tan
发明人： Jan Verwey , Hong Sheng Tan
IPC分类号： C07D209/34 , C07D501/10
CPC分类号： C07D501/10
摘要： A new azetidine derivative of the formula: ##EQU1## wherein R.sub.1 represents a penicillin- or cephalosporin-amido group, R.sub.2 represents one of the groups of the following formulae: ##EQU2## wherein R.sub.4, R.sub.5 and R.sub.6 are the same or different and each represents a hydrogen atom or a lower alkyl or alkenyl group, n represents 2 or 3 and - in case formula IIB represents a phenyl group - this group may carry one to four further substituents selected from the group consisting of halogen atoms and lower alkyl, lower alkenyl and phenyl groups,R.sub.3 represents an amino group of the formula ##EQU3## wherein R.sub.7 represents a hydrogen atom or a lower alkyl group and R.sub.8 represents a lower alkyl group, orR.sub.3 represents a N,N'-disubstituted hydrazino group wherein the substituents are lower alkyl groups, e.g. the N,N'-diisopropylhydrazino group, orR.sub.3 represents the group --OR.sub.9, wherein R.sub.9 represents a hydrogen atom, a lower alkyl group, which group may be substituted by 1 to 3 halogen atoms or by 1 or 2 phenyl groups, werein the phenyl groups may be substituted by a methoxy or a nitro group, or R.sub.9 represents a phenacyl group or a salt-forming cation,And corresponding azetidine derivatives of formula I wherein the double bond in the propenyl side chain has been shifted from the 2- to the 1-position, which are versatile intermediates in the process of preparing cephalosporanic and penicillanic derivative.

8. 发明授权

US5821233A Antifungal composition 失效
标题翻译：抗真菌组合物
公开(公告)号：US5821233A
公开(公告)日：1998-10-13
申请号：US446782
申请日：1995-05-26
申请人： Ferdinand Theodorus Van Rijn , Jacobus Stark , Hong Sheng Tan , Willem Johan Van Zoest , Nicolaas Cornelis Barendse
发明人： Ferdinand Theodorus Van Rijn , Jacobus Stark , Hong Sheng Tan , Willem Johan Van Zoest , Nicolaas Cornelis Barendse
IPC分类号： A01N25/02 , A01N43/90 , A01N63/02 , A23C19/11 , A23C19/16 , A23L3/3463 , A23L3/3562 , C07H17/08 , C12Q1/18 , G01N33/569 , A61K31/70
CPC分类号： C12Q1/18 , A01N25/02 , A01N43/90 , A01N63/02 , A23C19/11 , A23C19/16 , A23C19/163 , A23L3/34635 , A61K31/70 , C07H17/08 , G01N33/56961
摘要： Novel compositions that comprise solvates, salts, or other modified crystalline forms of polyene-type antifungal compounds are provided. Representative of such compositions are formulations that comprise the novel cystalline substances .delta.-natamycin and .gamma.-natamycin. Additionally, there are provided methods of preparing or storing such compositions, and also methods of use whereby an enhanced rate of release of antifungal compound, in a pharmaceutical or food products application is achieved.
摘要翻译： PCT No.PCT / EP94 / 03245 Sec。 371日期：1995年5月26日 102（e）日期1995年5月26日PCT 1994年9月28日PCT公布。 WO95 / 08918 PCT公开日期1995年4月6日提供了包含多烯型抗真菌化合物的溶剂合物，盐或其它改性结晶形式的新型组合物。这种组合物的代表是包含新型结晶物质δ-纳他霉素和γ-霉素的制剂。另外，提供了制备或储存这种组合物的方法，以及使用方法，从而实现了药物或食品应用中抗真菌化合物释放速率的提高。

9. 发明授权

US5747078A Longterm antimicrobial activity obtained by sustained release of hydrogen peroxide 失效
标题翻译：通过持续释放过氧化氢获得的长期抗菌活性
公开(公告)号：US5747078A
公开(公告)日：1998-05-05
申请号：US375563
申请日：1995-01-13
申请人： Sylvia Josefine De Jong , Ben Rudolf De Haan , Hong Sheng Tan
发明人： Sylvia Josefine De Jong , Ben Rudolf De Haan , Hong Sheng Tan
IPC分类号： A23L3/3571 , A23L3/358 , C12N11/02 , C12N11/04 , A23C19/00
CPC分类号： A23L3/3571 , A23L3/358 , C12N11/02 , C12N11/04
摘要： Methods for long-term preservation of food products using a lactoperoxidase system. Long-term preservation is achieved by controlled generation of hydrogen peroxide as a substrate for the lactoperoxidase system. Controlled production of hydrogen peroxide is achieved by generating the hydrogen peroxide enzymatically form a system wherein the substrate for the enzyme generating the hydrogen peroxide is immobilized or is generated in situ from a precursor.
摘要翻译：使用乳过氧化物酶系统长期保存食品的方法。通过控制产生过氧化氢作为乳过氧化物酶系统的底物来实现长期保存。过氧化氢的控制生产通过产生过氧化氢酶化形成系统来实现，其中产生过氧化氢的酶的底物被固定化或者由前体原位产生。

10. 发明授权

US3966738A Azetidine derivatives 失效
标题翻译：氮杂环丁烷衍生物
公开(公告)号：US3966738A
公开(公告)日：1976-06-29
申请号：US440725
申请日：1974-02-08
申请人： Jan Verwey , Hong Sheng Tan
发明人： Jan Verwey , Hong Sheng Tan
IPC分类号： C07D205/08 , C07D205/095 , C07D401/12 , C07D403/12 , C07D499/04 , C07D501/08 , C07D501/10 , C07F7/18 , C07D207/24
CPC分类号： C07D501/10 , C07D205/095 , C07F7/1896
摘要： New azetidine derivatives of the formula: ##EQU1## wherein R.sub.1 represents a penicillin- or cephalosporin-amido group, R.sub.2 represents one of the groups of the following formulae: ##EQU2## wherein R.sub.4, R.sub.5 and R.sub.6 are the same or different and each represents a hydrogen atom or a lower alkyl or alkenyl group, n represents 2 or 3 and - in case formula IIB represents a phenyl group - this group may carry one to four further substituents selected from the group consisting of halogen atoms and lower alkyl, lower alkenyl and phenyl groups, R.sub.3 represents an amino group of the formula ##EQU3## wherein R.sub.7 represents a hydrogen atom or a lower alkyl group and R.sub.8 represents a lower alkyl group, or R.sub.3 represents a N,N'-disubstituted hydrazino group wherein the substituents are lower alkyl groups, e.g. the N,N'-diisopropylhydrazino group, or R.sub.3 represents the group -OR.sub.9, wherein R.sub.9 represents a hydrogen atom, a lower alkyl group, which group may be substituted by 1 to 3 halogen atoms or by 1 or 2 phenyl groups, wherein the phenyl groups may be substituted by a methoxy or a nitro group, or R.sub.9 represents a phenacyl group or a salt-forming cation, and corresponding azetidine derivatives of formula 1 wherein the double bond in the propenyl side chain has been shifted from the 2- to the 1-position, which are versatile intermediates in the process of preparing cephalosporanic and penicillanic derivatives.
摘要翻译：新的氮杂环丁烷衍生物，其结构式如下：其中R1代表青霉素或头孢菌素 - 酰氨基，其中R1代表青霉素或头孢菌素 - 酰氨基，其中R1代表青霉素或头孢菌素 - 酰胺基，其中R1代表青霉素或头孢菌素 - 酰胺基， R 2表示以下基团之一：R4 C R4R6 R4OR6 | ANGLE || | PARALLEL | | -CC || | PARALLEL | -C- | PARALLEL -CN- -CCN- | -CC | | | ANGLE | | R5 C R5 R5 n IIA IIB IIC IID其中R4，R5和R6相同或不同，各自表示氢原子或低级烷基或烯基，n表示2或3，并且 - 在式IIB表示苯基的情况下，该基团可以携带一至四个选自卤素原子和低级烷基，低级烯基和苯基的取代基，R3表示式R7-ANGLE R8的氨基，其中R7表示氢原子或低级烷基基团，R 8表示低级烷基，或R 3表示N，N'-二取代肼基取代基是低级烷基，例如 N，N'-二异丙基肼基或R 3表示-OR 9基团，其中R 9表示氢原子，低级烷基，该基团可被1至3个卤素原子取代或被1或2个苯基取代，其中苯基可以被甲氧基或硝基取代，或R9表示苯甲酰基或成盐阳离子，以及相应的式1的氮杂环丁烷衍生物，其中丙烯基侧链中的双键已经从2-位移到 1位，它是制备头孢菌素和青霉烷衍生物过程中的多功能中间体。

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