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1. 发明申请

WO03000910A3 METABOLIC CONTROLLED FERMENTATION PROCESS FOR PSEUDOMONIC ACID PRODUCTION 审中-公开
标题翻译：拟除虫酸生产的代谢控制发酵工艺
公开(公告)号：WO03000910A3
公开(公告)日：2003-04-24
申请号：PCT/US0220044
申请日：2002-06-21
申请人： BIOGAL GYOGYSZERGYAR , TEVA PHARMA , GULYAS EVA , BALOGH GABOR , ERDEI JANOS , SERESS PETER
发明人： GULYAS EVA , BALOGH GABOR , ERDEI JANOS , SERESS PETER
IPC分类号： C12N1/20 , C12P17/16 , C12R1/38 , C12P17/18
CPC分类号： C12N1/20 , C12P17/162
摘要： An improved fermentation process for preparing pseudomonic acid A (mupirocin) is disclosed. The metabolically controlled fermentation process provides culturing a Pseudomonas sp. strain in a submerged medium at a temperature within about 20- 5 30°C. The pH of the fermentation medium is regulated to be at about 5.5-6.0 by feeding the fermentation medium with an assimilable carbon source, a mineral salt, or an acidic/alkali solution. Accordingly, the resulting fermentation broth contains an increased yield of highly purified pseudomonic acid A as the main component. The pseudomonic acid B as an impurity in the fermentation broth is significantly decreased.
摘要翻译：公开了用于制备假单胞菌酸A（莫匹罗星）的改进的发酵方法。代谢控制的发酵过程提供了培养假单胞菌属物种。在大约20-530℃的温度下在浸没的介质中应变。通过向发酵培养基中加入可吸收的碳源，矿物盐或酸性/碱性溶液，将发酵培养基的pH调节至约5.5-6.0。因此，所得发酵液包含高纯度假单胞菌酸A作为主要组分的产量增加。假发酵酸B作为发酵液中的杂质显着降低。

2. 发明申请

WO0046389A9 PROCESS FOR THE PREPARATION OF PSEUDOMONIC ACID A ANTIBIOTIC BY MICROBIOLOGICAL METHOD 审中-公开
标题翻译：通过微生物学方法制备抗坏血酸的方法
公开(公告)号：WO0046389A9
公开(公告)日：2001-09-07
申请号：PCT/US0002880
申请日：2000-02-03
申请人： BIOGAL GYOGYSZERGYAR , TEVA PHARMA , SZELL VALERIA , LANG ILDIKO , BARTA ISTVAN , TEGDES ANIKO , ALBRECHT KAROLY , MOZES JULIANNA , SZABO ISTVAN M , PETROCZKI MAGDOLNA , ERDEI JANOS , GULYAS EVA , BALOGH GABOR
发明人： SZELL VALERIA , LANG ILDIKO , BARTA ISTVAN , TEGDES ANIKO , ALBRECHT KAROLY , MOZES JULIANNA , SZABO ISTVAN M , PETROCZKI MAGDOLNA , ERDEI JANOS , GULYAS EVA , BALOGH GABOR
IPC分类号： C12P17/06 , A61K31/351 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/10 , A61P31/04 , A61P31/16 , A61P43/00 , C07D407/06 , C12N1/20 , C12P20060101 , C12P17/02 , C12P17/16 , C12P21/04 , C12R1/38
CPC分类号： C12R1/38 , C12P17/162
摘要： A procedure for the preparation of pseudomonic acid A comprising submerged cultivation of a Pseudomonas bacterium strain capable of biosynthesis of the substantially pure pseudomonic acid A in aerated conditions via fermentation; and isolation of the desired compound is disclosed. In particular, the procedure of the present invention comprises cultivation of the Pseudomonas sp. bacterium strain No. 19/26 deposited under accession No. NCAIM(P)B 001235 in the National Collection of the Agricultural and Industrial Microorganisms, Budapest, Hungary, or its pseudomonic acid A-producing mutant or variant, on a medium at a temperature of between about 20 DEG C and 30 DEG C containing organic nitrogen and carbon sources and, optionally, mineral salts.
摘要翻译：制备假单胞菌酸A的方法，其包括通过发酵在充气条件下能够生物合成基本上纯的假单胞菌酸A的假单胞菌属细菌菌株的浸没培养; 并公开了所需化合物的分离。特别地，本发明的方法包括培养假单胞菌属在保藏号NCAIM（P）B 001235，在匈牙利布达佩斯，布达佩斯的农业和工业微生物国家收藏品或其假肌酸A产生的突变体或变体中，在温度下的培养基上保藏的细菌菌株19/26 约20℃至30℃，含有机氮和碳源以及任选的无机盐。

3. 发明申请

WO02055490A3 METABOLIC CONTROLLED FERMENTATION PROCESS FOR CARBAMOYL TOBRAMYCIN PRODUCTION 审中-公开
标题翻译：碳水化合物生产的代谢控制发酵过程
公开(公告)号：WO02055490A3
公开(公告)日：2003-05-30
申请号：PCT/US0201843
申请日：2002-01-09
申请人： BIOGAL GYOGYSZERGYAR , TEVA PHARMA , BAKONDI-KOVACS ISTVAN , NOVOTNY LLONA CSUTOROS , ERDEI JANOS , BALOGH GABOR , SERESS PETER
发明人： BAKONDI-KOVACS ISTVAN , NOVOTNY LLONA CSUTOROS , ERDEI JANOS , BALOGH GABOR , SERESS PETER
IPC分类号： C12P19/48 , A61K31/70 , A61K31/7028 , A61P31/04 , C07H15/04 , C12P19/26 , C12R1/465
CPC分类号： C12P19/26
摘要： A metabolic controlled fermentation process has been developed for the production of carbamoyl tobramycin by the application of different Streptocmyces tenebrarius strains in submerged cultures at a temperature within about 37-41 DEG C on a medium containing assimilable carbon and nitrogen sources, mineral salts and controlling the assimilable carbon and nitrogen sources by feeding in an optimal range. As a result of this invention a high yield production of carbamoyl tobramycin with high purity could be achieved.
摘要翻译：已经开发了用于生产氨基甲酰妥布霉素的代谢控制发酵方法，其通过在含有可吸收的碳和氮源，矿物盐的培养基中在约37-41℃的温度下在浸没培养物中施用不同的链球菌属Tenebrarius菌株，并控制通过在最佳范围内饲养可吸收的碳氮源。作为本发明的结果，可以实现高产率的高纯度氨基甲酰妥布霉素。

4. 发明申请

WO2008127663A8 METHOD FOR REDUCING IMPURITY LEVEL IN MYCOPHENOLIC ACID FERMENTATION 审中-公开
标题翻译：降低MYCOPHENOLIC酸发酵过程中的污染程度的方法
公开(公告)号：WO2008127663A8
公开(公告)日：2008-12-18
申请号：PCT/US2008004724
申请日：2008-04-11
申请人： TEVA GYOGYSZERGYAR ZARTKOERUEN , TEVA PHARMA , TOTH LASZLO , ERDEI JANOS , SZIKSZAI BOGLARKA , BALOGH GABOR , GULYAS EVA
发明人： TOTH LASZLO , ERDEI JANOS , SZIKSZAI BOGLARKA , BALOGH GABOR , GULYAS EVA
IPC分类号： C12P17/04 , C07D307/88
CPC分类号： C12P17/04 , C07D307/88 , Y10T436/142222
摘要： The present invention relates to methods for reducing impurities of mycophenolic acid during fermentation by controlling the level of carbon source during fermentation of mycophenolic acid and for the isolation and use as a standard marker of the impurity homo-mycophenolic acid.
摘要翻译：本发明涉及在发酵过程中通过控制霉酚酸发酵过程中碳源水平以及分离和用作杂质均霉酚酸的标准标记来减少发酵过程中霉酚酸的杂质的方法。

5. 发明公开

EP1409703A4 METABOLIC CONTROLLED FERMENTATION PROCESS FOR PSEUDOMONIC ACID PRODUCTION 审中-公开
标题翻译：代谢产物的代谢控制发酵法
公开(公告)号：EP1409703A4
公开(公告)日：2004-08-18
申请号：EP02744598
申请日：2002-06-21
申请人： BIOGAL GYOGYSZERGYAR
发明人： GULYAS EVA , BALOGH GABOR , ERDEI JANOS , SERESS PETER
IPC分类号： C12N1/20 , C12P17/16 , C12R1/38 , A61K31/35
CPC分类号： C12N1/20 , C12P17/162

6. 发明公开

EP1151131A4 PROCESS FOR THE PREPARATION OF PSEUDOMONIC ACID A ANTIBIOTIC BY MICROBIOLOGICAL METHOD 审中-公开
标题翻译：微生物法对于抗生素的假单胞菌一个以生产
公开(公告)号：EP1151131A4
公开(公告)日：2004-05-12
申请号：EP00908473
申请日：2000-02-03
申请人： BIOGAL GYOGYSZERGYAR
发明人： SZELL VALERIA , LANG ILDIKO , BARTA ISTVAN , TEGDES ANIKO , ALBRECHT KAROLY , MOZES NEE SUTO JULIANNA , SZABO ISTVAN M , PETROCZKI MAGDOLNA , ERDEI JANOS , GULYAS EVA , BALOGH GABOR
IPC分类号： C12P17/06 , A61K31/351 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/10 , A61P31/04 , A61P31/16 , A61P43/00 , C07D407/06 , C12N1/20 , C12P20060101 , C12P17/02 , C12P17/16 , C12P21/04 , C12R1/38
CPC分类号： C12R1/38 , C12P17/162

7. 发明申请

WO2009004394A8 PROCESS FOR THE SYNTHESIS OF 9a-HYDROXY-STEROIDS 审中-公开
标题翻译：合成9-羟基甾体的方法
公开(公告)号：WO2009004394A8
公开(公告)日：2010-01-14
申请号：PCT/HU2008000078
申请日：2008-06-30
申请人： RICHTER GEDEON NYRT , OLASZ KATALIN , TEGDES ANIK , GANCSOS VALERIA , HANTOS GABOR , KOENCZOEL KALMAN , BALOGH GABOR , ERDELYI SANDOR
发明人： OLASZ KATALIN , TEGDES ANIK , GANCSOS VALERIA , HANTOS GABOR , KOENCZOEL KALMAN , BALOGH GABOR , ERDELYI SANDOR
IPC分类号： C07J21/00
CPC分类号： C07J21/003
摘要： The present invention relates to a novel selective synthesis of 9a-hydroxy-steroid derivatives of the general formula (I) (I) - wherein the meaning of -A-A'- is -CH2-CH2- or -CH=CH- group - by the bioconversion of compounds of the general formula (II) (II) wherein the meaning of -A-A'- is -CH2-CH2- or -CH=CH- group - by using Nocardia farcinica bacterium strain, deposition number of which is NCAIM (P) - B 001342, as hydroxylating microorganism in the bioconversion.
摘要翻译：本发明涉及通式（I）（I）的9-羟基类固醇衍生物的新型选择性合成，其中-A-A'-的含义是-CH 2 -CH 2 - 或-CH = CH-基 - 通过使用诺卡氏菌（Nocardia farcinica）细菌菌株对其中-A-A'-的含义为-CH 2 -CH 2 - 或-CH = CH-基团的通式（II）（II）的化合物的生物转化，其为NCAIM（P）-B 001342，作为生物转化中的羟化微生物。

8. 发明申请

WO2009004394A3 PROCESS FOR THE SYNTHESIS OF 9a-HYDROXY-STEROIDS 审中-公开
标题翻译：合成9-羟基甾体的方法
公开(公告)号：WO2009004394A3
公开(公告)日：2009-05-07
申请号：PCT/HU2008000078
申请日：2008-06-30
申请人： RICHTER GEDEON NYRT , OLASZ KATALIN , TEGDES ANIKO , GANCSOS VALERIA , HANTOS GABOR , KOENCOEL KALMAN , BALOGH GABOR , ERDELYI SANDOR
发明人： OLASZ KATALIN , TEGDES ANIKO , GANCSOS VALERIA , HANTOS GABOR , KOENCOEL KALMAN , BALOGH GABOR , ERDELYI SANDOR
IPC分类号： C07J21/00
CPC分类号： C07J21/003
摘要： The present invention relates to a novel selective synthesis of 9a-hydroxy-steroid derivatives of the general formula (I) (I) - wherein the meaning of -A-A'- is -CH2-CH2- or -CH=CH- group - by the bioconversion of compounds of the general formula (II) (II) wherein the meaning of -A-A'- is -CH2-CH2- or -CH=CH- group - by using Nocardia farcinica bacterium strain, deposition number of which is NCAIM (P) - B 001342, as hydroxylating microorganism in the bioconversion.
摘要翻译：本发明涉及通式（I）（I）的9-羟基类固醇衍生物的新型选择性合成，其中-A-A'-的含义是-CH 2 -CH 2 - 或-CH = CH-基 - 通过使用诺卡氏菌（Nocardia farcinica）细菌菌株对其中-A-A'-的含义为-CH 2 -CH 2 - 或-CH = CH-基团的通式（II）（II）的化合物的生物转化，其为NCAIM（P）-B 001342，作为生物转化中的羟化微生物。

9. 发明申请

WO2009001148A3 INDUSTRIAL METHOD FOR THE SYNTHESIS OF 17-ACETOXY-11ß-[4-(DIMETHYLAMINO)-PHENYL]-21-METHOXY-19-NORPREGNA-4,9-DIEN-3,20-DIONE AND THE KEY INTERMEDIATES OF THE PROCESS 审中-公开
标题翻译：合成17-乙酰基-11β-[4-（二甲基氨基）苯基] -2-甲氧基-19-壬基-4,9-二烯-3,20-二酮的工业方法及其工艺的主要中间体
公开(公告)号：WO2009001148A3
公开(公告)日：2009-03-19
申请号：PCT/HU2008000073
申请日：2008-06-19
申请人： RICHTER GEDEON NYRT , BODI JOZSEF , VISKY GYOERGY , SZELES JANOS , MAHO SANDOR , SANTA CSABA , CSOERGEI JANOS , TUBA ZOLTAN , TERDY LASZLO , MOLNAR CSABA , ARANYI ANTAL , HORVATH ZOLTAN , BALOGH GABOR
发明人： BODI JOZSEF , VISKY GYOERGY , SZELES JANOS , MAHO SANDOR , SANTA CSABA , CSOERGEI JANOS , TUBA ZOLTAN , TERDY LASZLO , MOLNAR CSABA , ARANYI ANTAL , HORVATH ZOLTAN , BALOGH GABOR
IPC分类号： C07J21/00 , C07J41/00 , C07J51/00
CPC分类号： C07J41/0083 , C07J21/006 , C07J41/0094 , C07J51/00 , Y02P20/55
摘要： The present invention relates to a process for the synthesis of the known 17-acetoxy-11-ß-[4-(dimethylamino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione (further on CDB-4124) of formula (I) from 3,3-[1,2-etandiyl-bis(oxy)]-oestr-5(10),9(l l)-dien-17-one of formula (II). Compound CDB-4124 belongs to the group of anti-hormones. The process according to the invention is the following: i) formation of an epoxide on the double bond in position 5(10) of 3,3-[l,2-ethandiyl- bis(oxy)]-oestr-5(10),9(l l)-dien-17-one of formula (II) with hydrogen peroxide; ii) addition of hydrogen cyanide formed in situ on position 17 of the obtained 5,10a- epoxy-3,3-[l,2-ethandiyl-bis(oxy)]-5a-oestr-9(l l)-en-17-one of formula (III); iii) silylation of the hydroxyl group in position 17 of the formed 5,10a-epoxy-3,3-[l,2- ethandiyl-bis(oxy)]-17a-hydroxy-5a-oestr-9(l l)-en-17ß-carbonitrile of formula (IV) with trimethyl chlorosilane; iv) reacting the obtained 5,10a-epoxy-3,3-[l,2-ethandiyl-bis(oxy)]-17-[trimethyl-silyl-oxy]-5a-oestr-9(l l)-en-17ß-carbonitrile of formula (V) with 4-(dimethylamino)-phenyl magnesium bromide Grignard reagent in the presence of CuCl (Teutsch reaction); v) silylation of the hydroxyl group in position 5 of the formed l lß-[4-(dimethyl-amino)-phenyl] -3,3 - [1,2-ethandiyl-bis(oxy)] -5 -hydroxy- 17a- [trimethylsilyl-(oxy)] -5 a-oestr-9-en-17ß-carbonitrile of formula (VI) with trimethyl chlorosilane; vi) reacting the obtained llß-[4-(dimethylamino)-phenyl]-3,3-[l,2-ethandiyl-bis(oxy)]-5,17a-bis-[trimethyl-silyl-(oxy)]-5a-oestr-9-en-17ß-carbonitrile of formula (VII) with diisobutyl aluminum hydride and after addition of acid to the reaction mixture; vii) methoxy-methylation of the obtained l lß-[4-(dimethylamino)-phenyl]-3,3-[1,2-ethandiyl-bis(oxy)]-5, 17a-bis-[trimethyl-silyl-(oxy)]-5a-oestr-9-en-17ß-carbaldehide of formula (VIII) with methoxy-methyl Grignard reagent formed in situ, while hydrolyzing the trimethylsilyl protective groups; viii) oxidation of the hydroxyl group in position 20 of the obtained 17,20?-dihydroxy-11ß-[4-(dimemylarnino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3-one of formula (IX) with dicyclohexyl carbodiimide in the presence of dimethyl sulfoxide and a strong organic acid (Swern oxidation), and in given case after purification by chromatography; ix) acetylation of the hydroxyl group in position 17 of the obtained 11ß-[4-(dimethylamino)-phenyl] -17-hydroxy-21-methoxy-19-norpregna-4,9-dien-3,20-dione of formula (X) with acetic anhydride in the presence of perchloric acid, and in given case the obtained 7-acetoxy-11ß-[4-(dimethylamino)-phenyl)]-21-methoxy-19-norpregna-4,9-dien-3,20-dione of formula (I) is purified by chromatography. The invention also relates to the new intermediates of formula (VII) and (VIII).
摘要翻译：本发明涉及合成已知的17-乙酰氧基-11-β-[4-（二甲基氨基） - 苯基] -2-甲氧基-19-去甲基-4,9-二烯-3,20-二酮（10），9（11） - 二酮-17-（式（I）的化合物（CDB-4124） II）。化合物CDB-4124属于抗激素类。根据本发明的方法如下：i）在3,3- [1,2-乙二基 - 双（氧基）] - 甲酯-5（10）的5（10）位的双键上形成环氧化物，，（II）的9（II） - 二烯-17-酮与过氧化氢反应; ii）在获得的5,10a-环氧-3,3- [1,2-乙二基 - 双（氧基）]-5α-异（9）-en-17的位置17上原位形成的氰化氢的加入 - 一个式（III）的化合物; iii）形成的5,10a-环氧-3,3- [1,2-乙二基 - 双（氧基）]-17α-羟基-5a-甲酯-9（11）-en的17位羟基的甲硅烷基化（IV）的-17β-腈与三甲基氯硅烷反应; iv）使得到的5,10a-环氧-3,3- [1,2-乙二基 - 双（氧基）] - 17- [三甲基 - 甲硅烷氧基] -5a-甲酯-9（II）-en-17β （V）与4-（二甲基氨基） - 苯基溴化镁Grignard试剂在CuCl存在下的反应（Teutsch反应）; v）形成的11β-[4-（二甲基 - 氨基） - 苯基] -3,3 - [1,2-乙二基 - 双（氧基）] -5-羟基-17α的位置5的羟基的甲硅烷基化 - （三甲基甲硅烷基 - （氧基）]-5α-甲基-9-烯-17β-甲腈与三氯甲硅烷; vi）使所得的11β-[4-（二甲基氨基） - 苯基] -3,3- [1,2-乙二基 - 双（氧基）] -5,17a-双 - [三甲基 - 甲硅烷基 - （氧基）（Ⅶ）的5-甲基-9-烯-17β-腈与二异丁基氢化铝反应，并向反应混合物中加入酸; vii）所得的11β-[4-（二甲基氨基） - 苯基] -3,3- [1,2-乙二基 - 双（氧基）] -5,17a-双 - [三甲基甲硅烷基 - （氧基）]-5α-甲基-9-烯-17β-al底物与甲氧基甲基格氏试剂原位形成，同时水解三甲基甲硅烷基保护基; viii）所获得的17,20β-二羟基-11β-[4-（二甲基氨基）苯基] -21-甲氧基-19-去甲基-4,9-二烯-3-酮的20位羟基氧化式（Ⅸ）与二环己基碳二亚胺在二甲基亚砜和强有机酸（Swern氧化）存在下反应，在给定的情况下通过色谱纯化; ix）得到的17β-[4-（二甲基氨基） - 苯基] -17-羟基-21-甲氧基-19-去甲基-4,9-二烯-3,20-二酮的17位羟基乙酰化为式（X）与高氯酸存在下的乙酸酐反应，在给定情况下得到的7-乙酰氧基-11β-[4-（二甲基氨基） - 苯基）] - 21-甲氧基-19-去甲基-4,9-二烯 - （I）的3,20-二酮通过色谱法纯化。本发明还涉及式（VII）和（VIII）的新中间体。

10. 发明申请

WO2006038047A8 ENVIRONMENT-FRIEND PROCESS FOR THE SYNTHESIS OF QUATERNARY AMMONIO-STERO?DS 审中-公开
标题翻译：环境友好过程的合成季铵盐
公开(公告)号：WO2006038047A8
公开(公告)日：2007-03-29
申请号：PCT/HU2005000104
申请日：2005-09-15
申请人： RICHTER GEDEON VEGYESZET , TUBA ZOLTAN , MAHO SANDOR , SZABO GYOERGYI , GALIK GYOERGY , BALOGH GABOR
发明人： TUBA ZOLTAN , MAHO SANDOR , SZABO GYOERGYI , GALIK GYOERGY , BALOGH GABOR
IPC分类号： C07J43/00
CPC分类号： C07J43/003
摘要： The invention relates to a new, environment-friend process for the synthesis of the known 4,4'-[3a,17ß-bis(acetoxy)-5a-androstane-2ß,l6ß-diyl]-bis(l,l-dimethyl-?i?erazinium) dibromide of formula (I) (from now on pipecuronium bromide) and l-[3a,17ß-bis(acetoxy)-2ß-(l-piperidinyl)-5a-androstane-16ß-yl]-l-methyl-piperidinium bromide of formula (II) (from now on vecuronium bromide). Furthermore the invention relates to the new intermediates of formula (III) and formula (IV) of the process, wherein the meaning of X is benzenesulfonate - in given case para-substituted with a methyl or a nitro group or a bromine atom - methanesulfonate, ethanesulfonate or trifluoromethanesulfonate ion.
摘要翻译：本发明涉及一种合成已知的4,4' - [3a，17β-双（乙酰氧基）-5a-雄甾烷-2β，6β-二基] - 双（1,1-二甲基）（I）的二溴化物（从现在起溴化铵）和1- [3a，17β-双（乙酰氧基）-2β-（1-哌啶基）-5a-雄甾烷-16β-基] -1 （II）的甲基 - 哌啶鎓溴化物（从现在起在维库溴铵）。此外，本发明涉及该方法的式（III）和式（IV）的新中间体，其中X的含义是苯磺酸盐 - 在给定情况下用甲基或硝基或溴原子甲烷磺酸酯取代，乙磺酸盐或三氟甲磺酸根离子。

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