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1. 发明授权

US4372973A 16-Amino-postaglandin derivatives, their acid addition salts, and a process for the preparation thereof 失效
标题翻译： 16-氨基 - Postaglandin衍生物及其酸加成盐及其制备方法
公开(公告)号：US4372973A
公开(公告)日：1983-02-08
申请号：US332840
申请日：1981-12-21
申请人： Gabor Ambrus , Eva Toth-Sarudy , Gyorgy Cseh , Istvan Barta , Gyula Horvath
发明人： Gabor Ambrus , Eva Toth-Sarudy , Gyorgy Cseh , Istvan Barta , Gyula Horvath
IPC分类号： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C12P31/00 , C07C177/00
CPC分类号： C12P31/00 , C07C405/0041 , Y02P20/55
摘要： The invention relates to new 16-amino-prostaglandin derivatives of general formula I, ##STR1## wherein C-15 and C-16 may have either S or R configuration, Z stands for a hydrogen atom or a lower alkyl group, and their acid addition salts. These compounds can be prepared by removing the ester group and the p-nitrocarbobenzyloxy protective group of a 9.alpha., 11.alpha., 15-trihydroxy-16-p-nitrobenzyloxycarbonylamido-5-cis,13-trans-prostadienoic acid derivative of general formula XII--wherein C-15 and C-16 may have either S or R configuration and Z stands for a lower alkyl group--in an optional sequence with the limitation that in those compounds of general formula I where Z stands for a lower alkyl group solely the p-nitrocarbobenzyloxy group is removed, and the resulting product of general formula I is optionally converted with an organic or inorganic acid into a salt.The new prostaglandin derivatives of the invention have valuable therapeutical properties, and can be applied as abortive or oxytocic agents.
摘要翻译：本发明涉及通式I的新的16-氨基前列腺素衍生物，其中C-15和C-16可以具有S或R构型，Z代表氢原子或低级烷基，它们的酸加成盐。这些化合物可以通过除去通式9的9α，11α，15-三羟基-16-对硝基苄氧基羰基酰胺基-5-顺式，13-反式 - 前列腺烯酸衍生物的酯基和对硝基苄氧基保护基来制备 XII-其中C-15和C-16可以具有S或R构型，Z表示低级烷基 - 在任选的序列中，限制在通式I的那些化合物中，其中Z仅代表低级烷基除去对硝基羰基苄氧基，将所得的通式I的产物任选地用有机或无机酸转化成盐。本发明的新型前列腺素衍生物具有有价值的治疗性质，可用作流产或催产素。

2. 发明授权

US4418205A 16-Amino-18,19,20-trinor-prostaglandin derivatives, and acid addition salts 失效
标题翻译： 16-氨基-18,19,20-三肽前列腺素衍生物和酸加成盐
公开(公告)号：US4418205A
公开(公告)日：1983-11-29
申请号：US329039
申请日：1981-12-09
申请人： Eva Toth-Sarudy , Gabor Ambrus , Gyorgy Cseh , Janos Borvendeg , Imre Moravcsik , Gabriella Mezei
发明人： Eva Toth-Sarudy , Gabor Ambrus , Gyorgy Cseh , Janos Borvendeg , Imre Moravcsik , Gabriella Mezei
IPC分类号： A61K31/557 , A61K31/5575 , A61P15/00 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/0041 , Y02P20/55
摘要： The invention relates to new 16-amino-18,19,20-trinor-prostaglandin derivatives of general formula I, having at C-17 a substituted or unsubstituted phenyl group, wherein C-15 and C-16 may have either S or R configuration, Y stands for a hydrogen atom or a lower alkyl group, W stands for a hydrogen atom, halogen atom, hydroxy group, lower alkyl or alkoxy group, and their acid addition salts. These compounds can be prepared by removing the ester group and the p-nitrobenzyloxycarbonyl protective group of a 9.alpha.,11.alpha.,15-trihydroxy-16-p-nitrobenzyloxycarbonylamido-17-phenyl-5-cis,13-trans-18,19,20-trinor-prostadienoic acid derivative of general formula XII--wherein C-15 and C-16 may have either S or R configuration, W is as defined above, and Y stands for a lower alkyl group--in an optional sequence with the limitation that in those compounds of general formula I where W is as defined above and Y stands for a lower alkyl group, solely the p-nitrobenzyloxycarbonyl group is removed, and the resulting product of general formula I is optionally converted with an organic or inorganic acid into a salt.The new prostaglandin derivatives of the invention have valuable therapeutical properties, and can be applied in cattle raising for estrus and birth synchronization, furthermore in the veterinary praxis for the treatment of sterility, chronic endometritis and pyometry.
摘要翻译：本发明涉及具有C-17取代或未取代的苯基的通式I的新的16-氨基-18,19,20-三核 - 前列腺素衍生物，其中C-15和C-16可具有S或R 构型中，Y表示氢原子或低级烷基，W表示氢原子，卤素原子，羟基，低级烷基或烷氧基，以及它们的酸加成盐。这些化合物可以通过除去9α，11α，15-三羟基-16-对硝基苄氧羰基酰胺基-17-苯基-5-顺式，13-trn-18的酯基和对硝基苄氧羰基保护基来制备，其中C-15和C-16可以具有S或R构型，W如上所定义，Y代表低级烷基 - 在任选的序列中，具有通式XII-的19,20-三过 - 前列腺素酸衍生物 - 在通式I的那些化合物中的限制，其中W如上所定义，Y代表低级烷基，仅除去对硝基苄氧基羰基，所得到的通式I的产物任选地用有机或无机酸变成盐。本发明的新型前列腺素衍生物具有有价值的治疗特性，可用于发情期和出生同步的养牛，此外还适用于无菌治疗，慢性子宫内膜炎和高血压的兽医学应用。

3. 发明授权

US5156960A Microbial process for the production of immunosuppressive antibiotics 失效
标题翻译：用于生产免疫抑制抗体的微生物过程
公开(公告)号：US5156960A
公开(公告)日：1992-10-20
申请号：US454005
申请日：1989-12-20
申请人： Antonia Jekkel nee Bokany , Gabor Ambrus , Eva Toth-Sarudy , Istvan Mihaly , Agota Hulber nee Dobos , Attila Andor , Karoly Albrecht , Kalman Konczol , Valeria Szell , Eva Tomori nee Joszt , Imre Moravcsik , Kalman Polya , Janos Erdei , Lajos Kiss , Bela Makadi , Karoly Nagy , Bela Palotas , Etelka Deli nee Konszky , Karoly Buzasi , Aniko Molnar nee Antal , Gyorgy Santha , Vilma Szaszhegyesi
发明人： Antonia Jekkel nee Bokany , Gabor Ambrus , Eva Toth-Sarudy , Istvan Mihaly , Agota Hulber nee Dobos , Attila Andor , Karoly Albrecht , Kalman Konczol , Valeria Szell , Eva Tomori nee Joszt , Imre Moravcsik , Kalman Polya , Janos Erdei , Lajos Kiss , Bela Makadi , Karoly Nagy , Bela Palotas , Etelka Deli nee Konszky , Karoly Buzasi , Aniko Molnar nee Antal , Gyorgy Santha , Vilma Szaszhegyesi
IPC分类号： C12N1/14 , A61K31/545 , A61K38/00 , A61P37/06 , C07D501/00 , C07K7/64 , C12P1/00 , C12P21/04 , C12P35/00 , C12R1/645
CPC分类号： C12R1/645 , C07K7/645 , Y10S435/911
摘要： The invention relates to a microbial process for the production of immunosuppressive cyclosporine antibiotic complex or of its components, cyclosporine A, cyclosporine B and cyclosporine C, by the aerobic fermentation of a filamentous fungus strain biosynthesizing the above antibiotic(s) in a nutrient medium containing utilizable carbon and nitrogen sources as well as mineral salts, and by isolating the products formed, which comprises culturing a strain of the novel Tolypocladium varium fungus species producing the cyclosporine antibiotic complex, preferably tolypocladium varium sp. nov. CY/93, deposited at the National Collection of Agricultural and Industrial Microorganisms, Budapest, Hungary under the number NCAIM(P)F 001005, on a nutrient medium containing carbon sources, organic and inorganic nitrogen sources as well as mineral salts, under aerobic conditions, at 25.degree. to 30.degree. C., and, if desired, isolating and purifying the cyclosporine antibiotic complex or its components produced.
摘要翻译：本发明涉及通过在含营养培养基中生物合成上述抗生素的丝状真菌菌株的需氧发酵来生产免疫抑制环孢菌素抗生素复合物或其组分的环孢菌素A，环孢菌素B和环孢霉素C的微生物方法，可利用的碳源和氮源以及矿物盐，并且通过分离形成的产物，其包括培养产生环孢菌素抗生素复合物的新型Tolypocladium varium真菌物种的菌株，优选地变种球菌sp。 nov。 CY / 93，保藏在匈牙利布达佩斯国家农业和工业微生物收集库，编号为NCAIM（P）F 001005），在有氧条件下，含有碳源，有机和无机氮源以及矿物盐的营养培养基，25℃至30℃，如果需要，分离和纯化产生的环孢菌素抗生素复合物或其组分。

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