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1. 发明申请

US20050124051A1 Hydroxylation of compactin to pravatatin by micromonospora 审中-公开
标题翻译：通过微单孢菌素将致密蛋白羟基化为普伐他汀
公开(公告)号：US20050124051A1
公开(公告)日：2005-06-09
申请号：US11014658
申请日：2004-12-16
申请人： Antonia Jekkel , Gabor Ambrus , Eva Ilkoy , Ildiko Horvath , Attila Konya , Istvan Szabo , Zsuzsanna Nagy , Gyula Horvath , Julia Mozes , Istvan Barta , Gyorgy Somogyi , Janos Salat , Sandor Boros
发明人： Antonia Jekkel , Gabor Ambrus , Eva Ilkoy , Ildiko Horvath , Attila Konya , Istvan Szabo , Zsuzsanna Nagy , Gyula Horvath , Julia Mozes , Istvan Barta , Gyorgy Somogyi , Janos Salat , Sandor Boros
IPC分类号： C12P7/62 , C07C69/30 , C12P1/04 , C12P7/42 , C12P17/06 , C12R1/29 , C12R1/31 , C12N1/21 , C12N9/18
CPC分类号： C12R1/29 , C12P7/42 , C12P17/06
摘要： The present invention relates to a new microbial process for the preparation of compound of formula (I) from a compound of general formula (II) wherein R stands for an alkali metal or ammonium ion, by the submerged culture of a strain which is able to 6β-hydroxylate the compound of formula (II) in aerobic fermentation and by the separation and purification of the product of formula (I) formed in the course of the biocoversion. The latter comprises the cultivation of a Micromonospora strain which is able to 6β-hydroxylate a compound of general formula (II)—wherein R is as defined above—at 25-32° C. on a nutrient medium containing available carbon—and nitrogen sources and mineral salts, thereafter feeding the substrate to be transformed into the developing culture, then hydroxilating the substrate until finishing of the bioconversion, then separating the compound of formula (I) from the culture broth and, if desired, purifying the same.
摘要翻译：本发明涉及一种由通式（II）化合物制备式（I）化合物的新型微生物方法，其中R代表碱金属或铵离子，通过浸没培养的能够在好氧发酵中通过分解和纯化在生物转化过程中形成的式（I）的产物，使式（II）化合物6β-羟化。后者包括培养微孢子虫菌株，其能够在含有可用碳源和氮源的营养培养基上在25-32℃下将通式（II）化合物（其中R如上定义）6β-羟基化然后将待转化的底物喂入显影培养物，然后将底物氢化，直到生物转化完成，然后从培养液中分离式（I）化合物，如果需要，将其纯化。

2. 发明申请

US20060281155A1 Microbial process for preparing pravastatin 审中-公开
公开(公告)号：US20060281155A1
公开(公告)日：2006-12-14
申请号：US11509662
申请日：2006-08-25
申请人： Antonia Jekkel , Attila Konya , Istvan Barta , Eva Ilkoy , Gyorgy Somogyi , Gabor Ambrus , Gyula Horvath , Karoly Albrecht , Istvan Szabo , Julianna Suto , Janos Salat , Attila Andor , Laszlo Birincsik , Sandor Boros , Ildiko Lang , Margit Nee Igloy
发明人： Antonia Jekkel , Attila Konya , Istvan Barta , Eva Ilkoy , Gyorgy Somogyi , Gabor Ambrus , Gyula Horvath , Karoly Albrecht , Istvan Szabo , Julianna Suto , Janos Salat , Attila Andor , Laszlo Birincsik , Sandor Boros , Ildiko Lang , Margit Nee Igloy
IPC分类号： C12P7/62
CPC分类号： C12R1/645 , C12P7/62
摘要： The present invention relates to a new microbial process for the preparation of the compound formula (I) from a compound of general formula (II) wherein R stands for an alkali metal or ammonium ion, by the submerged cultivation of a mold strain able to 6β-hydroxylate a compound of the Formula (II) in aerobic fermentation and by the separation and purification of the product of Formula (I) formed in the course of the bioconversion. The process comprises cultivating a strain of Mortierella maculata filamentous mold species that is able to 6β-hydroxylate a compound of the general Formula (II), on a nutrient medium containing assimilable carbon and nitrogen sources and mineral salts and separating the product formed from the fermentation broth, then isolating the compound of formula (I) and purifying the same. Novel strains of Mortierella maculata are also disclosed.

3. 发明授权

US06696599B2 Microbial process for preparing pravastatin 失效
标题翻译：制备普伐他汀的微生物过程
公开(公告)号：US06696599B2
公开(公告)日：2004-02-24
申请号：US10437058
申请日：2003-05-14
申请人： Antonia Jekkel , Attila Konya , Istvan Barta , Eva Ilkoy , Gyorgy Somogyi , Gabor Ambrus , Gyula Horvath , Karoly Albrecht , Istvan Szabo , Julianna Mozes Nee Suto , Janso Salat , Attila Andor , Laszlo Birincsik , Sandor Boros , Ildiko Lang , Margit Bidlo Nee Igloy
发明人： Antonia Jekkel , Attila Konya , Istvan Barta , Eva Ilkoy , Gyorgy Somogyi , Gabor Ambrus , Gyula Horvath , Karoly Albrecht , Istvan Szabo , Julianna Mozes Nee Suto , Janso Salat , Attila Andor , Laszlo Birincsik , Sandor Boros , Ildiko Lang , Margit Bidlo Nee Igloy
IPC分类号： C07C6702
CPC分类号： C12R1/645 , C12P7/62
摘要： The present invention relates to a new microbial process for the preparation of the compound formula (I) from a compound of general formula (II) wherein R stands for an alkali metal or ammonium ion, by the submerged cultivation of a mold strain able to 6&bgr;-hydroxylate a compound of the Formula (II) in aerobic fermentation and by the separation and purification of the product of Formula (I) formed in the course of the bioconversion. The process comprises cultivating a strain of Mortierella maculata filamentous mold species that is able to 6&bgr;-hydroxylate a compound of the general Formula (II), on a nutrient medium containing assimilable carbon and nitrogen sources and mineral salts and separating the product formed from the fermentation broth, then isolating the compound of formula (I) and purifying the same. Novel strains of Mortierella maculata are also disclosed.
摘要翻译：本发明涉及一种由通式（II）的化合物制备式（I）化合物的新的微生物方法，其中R代表碱金属或铵离子，通过浸没式培养能够提供6β 在需氧发酵中通过分解和纯化在生物转化过程中形成的式（I）的产物来氢化式（II）化合物。该方法包括在含有可吸收的碳和氮源和矿物盐的营养培养基上培养能够将通式（II）的化合物6β-羟基化的高山被孢霉丝状菌种的菌株，并分离由发酵形成的产物肉汤，然后分离式（I）化合物并纯化。还公开了高山被孢霉的新型菌株。

4. 发明授权

US06750366B2 Microbial process for preparing pravastatin 失效
标题翻译：制备普伐他汀的微生物过程
公开(公告)号：US06750366B2
公开(公告)日：2004-06-15
申请号：US10011176
申请日：2001-12-05
申请人： Antonia Jekkel , Attila Konya , Istvan Barta , Eva Ilkoy , Gyorgy Somogyi , Gabor Ambrus , Gyula Horvath , Karoly Albrecht , Istvan Szabo , Julianna Mozes Nee Suto , Janso Salat , Attila Andor , Laszlo Birinesik , Sandor Boros , Ildiko Lang , Margit Bidlo Nee Igloy
发明人： Antonia Jekkel , Attila Konya , Istvan Barta , Eva Ilkoy , Gyorgy Somogyi , Gabor Ambrus , Gyula Horvath , Karoly Albrecht , Istvan Szabo , Julianna Mozes Nee Suto , Janso Salat , Attila Andor , Laszlo Birinesik , Sandor Boros , Ildiko Lang , Margit Bidlo Nee Igloy
IPC分类号： C07C6902
CPC分类号： C12R1/645 , C12P7/62
摘要： The present invention relates to a new microbial process for the preparation of the compound formula (I): from a compound of general formula (II): wherein R stands for an alkali metal or ammonium ion, by the submerged cultivation of a mold strain able to 6&bgr;-hydroxylate a compound of the Formula (II) in aerobic fermentation and by the separation and purification of the product of Formula (I) formed in the course of the bioconversion. The process comprises cultivating a strain of Mortierella maculata filamentous mold species that is able to 6&bgr;-hydroxylate a compound of the general Formula (II), on a nutrient medium containing assimilable carbon and nitrogen sources and mineral salts and separating the product formed from the fermentation broth, then isolating the compound of formula (I) and purifying the same. Novel strains of Mortierella maculata are also disclosed.
摘要翻译：本发明涉及一种制备式（I）化合物的新的微生物方法：由通式（II）的化合物：其中R代表碱金属或铵离子，通过浸没式培养可变形的模具在有氧发酵中通过分解和纯化在生物转化过程中形成的式（I）的产物来将式（II）的化合物改性为6β-羟基化。该方法包括在含有可吸收的碳和氮源和矿物盐的营养培养基上培养能够将通式（II）的化合物6β-羟基化的高山被孢霉丝状菌种的菌株，并分离由发酵形成的产物肉汤，然后分离式（I）化合物并纯化。还公开了高山被孢霉的新型菌株。

5. 发明授权

US06682913B1 Microbial process for preparing pravastatin 失效
公开(公告)号：US06682913B1
公开(公告)日：2004-01-27
申请号：US09497805
申请日：2000-02-03
申请人： Antonia Jekkel , Attila Konya , Istvan Barta , Eva Ilkoy , Gyorgy Somogyi , Gabor Ambrus , Gyula Horvath , Karoly Albrecht , Istvan Szabo , Julianna Mozes nee Suto , Janso Salat , Attila Andor , Laszlo Birincsik , Sandor Boros , Ildiko Lang , Margit Bidlo nee Igloy
发明人： Antonia Jekkel , Attila Konya , Istvan Barta , Eva Ilkoy , Gyorgy Somogyi , Gabor Ambrus , Gyula Horvath , Karoly Albrecht , Istvan Szabo , Julianna Mozes nee Suto , Janso Salat , Attila Andor , Laszlo Birincsik , Sandor Boros , Ildiko Lang , Margit Bidlo nee Igloy
IPC分类号： C12P762
CPC分类号： C12R1/645 , C12P7/62
摘要： The present invention relates to a new microbial process for the preparation of the compound formula (I) from a compound of general formula (II) wherein R stands for an alkali metal or ammonium ion, by the submerged cultivation of a mold strain able to 6&bgr;-hydroxylate a compound of the Formula (II) in aerobic fermentation and by the separation and purification of the product of Formula (I) formed in the course of the bioconversion. The process comprises cultivating a strain of Mortierella maculata filamentous mold species that is able to 6&bgr;-hydroxylate a compound of the general Formula (II), on a nutrient medium containing assimilable carbon and nitrogen sources and mineral salts and separating the product formed from the fermentation broth, then isolating the compound of formula (I) and purifying the same. Novel strains of Mortierella maculata are also disclosed.

6. 发明授权

US5288863A Process for the preparation of high-purity 1-(3-chloro-phenyl)-4-methyl-7,8-dimethoxy-5H-2,3-benzodiazepine 失效
标题翻译：制备高纯度1-（3-氯 - 苯基）-4-甲基-7,8-二甲氧基-5H-2,3-苯并二氮杂的方法
公开(公告)号：US5288863A
公开(公告)日：1994-02-22
申请号：US878379
申请日：1992-05-04
申请人： Gyorgy Somogyi , Peter Botka , Gyula Horvath , Antal Simay , Roozsa Gyenge , Imre Moravcsik , Erno Orban , Tamas Hamori , Jeno Korosi , Csilla Kiss , Tibor Balogh , Maria Bidlo nee Igloi , nee Dievald; Emilia Uskert
发明人： Gyorgy Somogyi , Peter Botka , Gyula Horvath , Antal Simay , Roozsa Gyenge , Imre Moravcsik , Erno Orban , Tamas Hamori , Jeno Korosi , Csilla Kiss , Tibor Balogh , Maria Bidlo nee Igloi , nee Dievald; Emilia Uskert
IPC分类号： A61K31/55 , A61P25/00 , C07D243/02 , C07D243/04 , C07D243/12
CPC分类号： C07D243/02
摘要： The invention relates to a process for the preparation of 1-(3-chlorophenyl)-4-methyl-7,8-dimethoxy-5 H-2,3-benzodiazepine of formula (I) ##STR1## in high purity and in a quality suitable for pharmaceutical purposes. According to the invention the reaction of 1 mole of 2-acetonyl-3'-chloro-4,5-dimethoxybenzophenone of formula (II) ##STR2## with 3-7 moles of hydrazine hydrate in an organic solvent or in a mixture of organic solvents at a temperature between 15.degree. C. and 85.degree. C. is carried out in the absence of air oxygen, optionally in the presence of water. The crude product is then recrystallized from an aliphatic alcohol containing 1 to 5 carbon atom(s).
摘要翻译：本发明涉及制备式（I）的1-（3-氯苯基）-4-甲基-7,8-二甲氧基-5H（OVS）-2,3-苯并二氮杂的方法（*化学结构*）（I）在高纯度和适合制药目的的质量。根据本发明，将1摩尔式（II）的2-丙酰基-3'-氯-4,5-二甲氧基二苯甲酮（*化学结构*）（II）与3-7摩尔水合肼在有机溶剂中的反应或在有机溶剂的混合物中，在15摄氏度至85摄氏度之间的温度下，在无空气氧气的情况下，任选地在水的存在下进行。然后将粗产物从含有1至5个碳原子的脂族醇中重结晶。

7. 发明授权

US4851416A Berban derivatives as .alpha..sub.2 -adrenergic antagonists 失效
标题翻译： Berban衍生物作为α2-肾上腺素能拮抗剂
公开(公告)号：US4851416A
公开(公告)日：1989-07-25
申请号：US867323
申请日：1986-05-23
申请人： Szilveszter Vizi , Csaba Szantai , Lajos Szabo , Istvan Toth , Gabor Kovacs , Jeno Marton , Laszlo Harsing , Gyorgy Somogyi , Jozsef Gaal
发明人： Szilveszter Vizi , Csaba Szantai , Lajos Szabo , Istvan Toth , Gabor Kovacs , Jeno Marton , Laszlo Harsing , Gyorgy Somogyi , Jozsef Gaal
IPC分类号： C07D453/00 , A61K31/47 , A61P25/02 , A61P25/24 , A61P25/26 , C07D455/03 , C07D471/04
CPC分类号： C07D455/00
摘要： The invention relates to novel racemic or optically active berban derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent independently from the other a hydroxyl, straight or branched chain alkoxy group 1 to 6 carbon atoms or R.sup.1 and R.sup.2 together represent a C.sub.1-3 alkylenedioxy group;R.sup.3 and R.sup.4 represent independently from the other hydrogen, straight or branched chain alkyl group, having 1 to 6 carbon atoms and optionally substituted by hydroxyl group, or a C.sub.2-6 alkoxycarbonyl or cyano group; andR.sup.5 represents hydrogen, straight or branched chain alkyl group having 1 to 6 carbon atoms, C.sub.1-7 aliphatic or aromatic acyl group or C.sub.1-7 alkylsulphonyl or arylsulphonyl group, anda salt thereof, to pharmaceutical compositions containing them, to the use as well as to process for preparing the novel compounds. The compounds of the formula (I) are selective .alpha..sub.2 -adrenergic receptor-blocking substances and thus, they may be used for the treament of depressive illnesses.
摘要翻译：本发明涉及式（I）的新型外消旋或光学活性伯类衍生物，其中R 1和R 2彼此独立地表示1至6个碳原子的羟基，直链或支链烷氧基或R1和R2 一起代表C1-3亚烷基二氧基; R3和R4独立地表示独立于具有1-6个碳原子并且任选被羟基取代的另一个氢，直链或支链烷基或C 2-6烷氧羰基或氰基; 并且R 5表示氢，具有1〜6个碳原子的直链或支链烷基，C 1-7脂族或芳族酰基或C 1-7烷基磺酰基或芳基磺酰基及其盐与含有它们的药物组合物以及用于制备新化合物的方法。式（I）化合物是选择性α2-肾上腺素能受体阻断物质，因此可用于抑郁症的治疗。

8. 发明授权

US6075018A 1-[2-(substituted vinyl)]-3,4-dihydro-4-dihydro-5H-2,3-benzodiazepine derivatives 失效
标题翻译： 1- [2-（取代的乙烯基）] -3,4-二氢-4-二氢-5 + E，H + EE -2,3-苯并二氮杂衍生物
公开(公告)号：US6075018A
公开(公告)日：2000-06-13
申请号：US599235
申请日：1996-02-09
申请人： Pal Vago , Jozsef Reiter , Istvan Gyertyan , Gabor Gigler , Ferenc Andrasi , Anna Bakonyi , Pal Berzsenyi , Peter Botka, deceased , Erszebet Birkas , Tamas Hamori , Edit Horvath , Katalin Horvath , Jeno Korosi, deceased , Gyorgyne Mate , Imre Moravcsik , Gyorgy Somogyi , Eszter Szentkuti , Gabor Zolyomi
发明人： Pal Vago , Jozsef Reiter , Istvan Gyertyan , Gabor Gigler , Ferenc Andrasi , Anna Bakonyi , Pal Berzsenyi , Peter Botka, deceased , Erszebet Birkas , Tamas Hamori , Edit Horvath , Katalin Horvath , Jeno Korosi, deceased , Gyorgyne Mate , Imre Moravcsik , Gyorgy Somogyi , Eszter Szentkuti , Gabor Zolyomi
IPC分类号： A61K31/55 , A61K31/551 , A61P25/00 , C07D243/02 , C07D243/04 , C07D405/06 , C07D491/04 , C07D491/056 , C07D493/04 , A61K31/395
CPC分类号： C07D405/06 , C07D243/02 , C07D491/04 , C07D493/04
摘要： The invention relates to new 1-[2-(substituted vinyl)]-3,4-dihydro-5H-2,3-benzodiazepine derivatives, a process for the preparation thereof and pharmaceutical compositions comprising them. The new 1-[2-(substituted vinyl)]-3,4-dihidro-5H-2,3-benzodiazepine derivatives according to the invention correspond to the general formula (I), ##STR1## wherein the variables are hereinbelow defined: The new compounds according to the invention affect the central nervous system and can be used to advantage in the therapy.
摘要翻译：本发明涉及新的1- [2-（取代的乙烯基）] -3,4-二氢-5 + E，非H + EE-2,3-苯并二氮杂衍生物，其制备方法和包含它们的药物组合物。根据本发明的新的1- [2-（取代的乙烯基）] -3,4-二阴离子-5 + E，非H + EE -2,3-苯并二氮杂衍生物对应于通式（I），其中变量在下文中定义：根据本发明的新化合物影响中枢神经系统并且可以在治疗中有利地使用。

9. 发明授权

US4389838A Single-twist stranding 失效
标题翻译：单捻绞合
公开(公告)号：US4389838A
公开(公告)日：1983-06-28
申请号：US375724
申请日：1982-05-07
申请人： Georg Adelhard , Herbert Hasselberg , Manfred Obermeier , Karl Sierwald , Jozsef Szedlacsek , Gyorgy Somogyi
发明人： Georg Adelhard , Herbert Hasselberg , Manfred Obermeier , Karl Sierwald , Jozsef Szedlacsek , Gyorgy Somogyi
IPC分类号： D07B3/08 , D07B7/10
CPC分类号： D07B7/10 , D07B3/085
摘要： A single-twist stranding machine includes a stranding disc and nipple for stranding together a plurality of filaments, wires, conductors or the like, a rotatably mounted take-up spool onto which the stranded-together elements are wound, a flyer coaxial with the spool and including a frame and deflection pulleys to run the stranded-together elements from the stranding means to the spool, the flyer revolving about the spool, and a common drive motor. The specific improvement disclosed includes a differential gear transmission having two input gears and an output gear; a first transmission for drivingly connecting the drive motor to the flyer, one of the input gears of the differential gear transmission is a part of the first transmission; a second transmission drivingly connects the output gear to the spool for causing the spool to rotate; and a control drive operates the other input gear to vary the speed relation of flyer and spool in dependance upon the input speed of the stranding elements.
摘要翻译：单捻绞合机包括绞合盘和用于将多根细丝，线，导体等绞合在一起的接头，可旋转地安装的卷绕卷轴，绞合在一起的元件缠绕在其上，与卷轴同轴的飞轮并且包括框架和偏转滑轮以将绞合的元件从绞合装置运行到卷轴，围绕卷轴旋转的飞翼和公共驱动马达。所公开的具体改进包括具有两个输入齿轮和输出齿轮的差速齿轮传动装置; 用于将驱动马达驱动地连接到飞轮的第一变速器，差速齿轮变速器的输入齿轮之一是第一变速器的一部分; 第二传动装置驱动地将输出齿轮连接到卷轴以使卷轴转动; 并且控制驱动器操作另一个输入齿轮，以根据绞合元件的输入速度改变飞轮和滑阀的速度关系。

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