公开(公告)号：US20060223150A1

公开(公告)日：2006-10-05

申请号：US10842221

申请日：2004-05-10

申请人： Vilmos Keri ,  Eva Ilkoy ,  Irma Hogye ,  Antonia Jekkel ,  Ilonu Bagdi ,  Gabor Ambrus ,  Attila Jakab ,  Attilla Andor ,  Lajos Deak ,  Istvan Szabo ,  Janos Balint ,  Zsuzsanna Scheidl ,  Etelka Deli ,  Gyula Horvath ,  Csaba Szabo ,  Ildiko Lang ,  Imre Szekely ,  Imre Moravcsik ,  Vera Kovacs ,  Szabolcs Matyas ,  Zsuasanna Sztaray ,  Laszlo Eszenyi

发明人： Vilmos Keri ,  Eva Ilkoy ,  Irma Hogye ,  Antonia Jekkel ,  Ilonu Bagdi ,  Gabor Ambrus ,  Attila Jakab ,  Attilla Andor ,  Lajos Deak ,  Istvan Szabo ,  Janos Balint ,  Zsuzsanna Scheidl ,  Etelka Deli ,  Gyula Horvath ,  Csaba Szabo ,  Ildiko Lang ,  Imre Szekely ,  Imre Moravcsik ,  Vera Kovacs ,  Szabolcs Matyas ,  Zsuasanna Sztaray ,  Laszlo Eszenyi

IPC分类号： C12P17/00 ,  C12N1/16

CPC分类号： C12P17/06

摘要： In a process for preparing mevinolin by fermentation of a biomass in a fermentation liquor, which includes dissolving mevinolin from the biomass into the fermentation liquor, and separating the biomass from the fermentation liquor to obtain a separated fermentation liquor, separating the mevinolin from the separated fermentation liquor, and recovering the end product, the improvement which comprises carrying out the dissolving at a pH between about 7.5 and about 10, and the separating of the mevinolin is carried out at a pH between about 4.5 and about 1.

摘要翻译： 在发酵液中通过发酵生物质来制备美维林的方法，其包括将生物质中的美维林溶解于发酵液中，并将生物质与发酵液分离以获得分离的发酵液，从分离的发酵液中分离出美维林 液体并回收最终产物，其改进包括在pH约7.5至约10之间进行溶解，并且在约4.5至约1之间的pH下进行甲维林的分离。

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。

公开(公告)号：US5053144A

公开(公告)日：1991-10-01

申请号：US503259

申请日：1990-04-02

申请人： Endre Szirmai ,  Sandor Babusek ,  Gezz Balogh ,  Atilla Nedves ,  Gyula Horvath ,  Zoltan Lebenyi ,  James Pinter

发明人： Endre Szirmai ,  Sandor Babusek ,  Gezz Balogh ,  Atilla Nedves ,  Gyula Horvath ,  Zoltan Lebenyi ,  James Pinter

IPC分类号： C01B33/32 ,  C01D7/00 ,  C01F5/24 ,  C01F7/06 ,  C01F11/18 ,  C01G49/06 ,  C02F1/52 ,  C05D3/02 ,  C05D9/02

CPC分类号： C05D9/02 ,  C01B33/32 ,  C01D7/00 ,  C01F11/18 ,  C01F5/24 ,  C01F7/066 ,  C01G49/06 ,  C02F1/5236 ,  C05D3/02

摘要： The method of the invention is advantageously applicable to realize a multistage chemical process during which liquid clarifiers suitable for the purification of water and sewage, furthermore, fine-disperse pulverulent solid products utilizable as pait pigments and fillers may be recovered. Each final product of the multistage chemical processes is a useful material, so the whole technology is waste free.

摘要翻译： 本发明的方法有利地适用于实现多级化学方法，其中可以回收适用于净化水和污水的液体澄清剂，此外，可以回收可用作pait颜料和填料的细分散粉状固体产品。 多级化学工艺的最终产品是一种有用的材料，因此整个技术无废弃物。

公开(公告)号：US4052407A

公开(公告)日：1977-10-04

申请号：US577348

申请日：1975-05-14

申请人： Gabor Ambrus ,  Istvan Barta ,  Zsuzsanna Mehesfalvi, nee Vajna ,  Gyula Horvath

发明人： Gabor Ambrus ,  Istvan Barta ,  Zsuzsanna Mehesfalvi, nee Vajna ,  Gyula Horvath

IPC分类号： C07D277/30 ,  C07D277/56 ,  C07D277/20

CPC分类号： C07D277/56 ,  C07D277/30

摘要： Novel thiazole derivatives of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or methyl, R.sub.3 is oxo, hydroxyl or acetoxy, have prostaglandin side chains and have an action that is more selective than that of natural prostaglandins. They inhibit the activity of enzymes inducing the decomposition of prostaglandins in the organism and thus they increase the endogenous level of prostaglandins. Various novel methods are provided for their production.

公开(公告)号：US4028348A

公开(公告)日：1977-06-07

申请号：US658863

申请日：1976-02-17

申请人： Pal Bite ,  Imre Moravcsik ,  Inge Schafer ,  Gyula Horvath ,  Zsuzsanna Mehesfalvi nee Vajna ,  Janos Borvendeg ,  Ilona Hermann nee Szente

发明人： Pal Bite ,  Imre Moravcsik ,  Inge Schafer ,  Gyula Horvath ,  Zsuzsanna Mehesfalvi nee Vajna ,  Janos Borvendeg ,  Ilona Hermann nee Szente

IPC分类号： C07J53/00 ,  C07J41/00 ,  C07J43/00

CPC分类号： C07J53/00

摘要： Novel 6-amino-5.alpha.,19-cycloandrostane derivatives of formula I and their pharmaceutically acceptable addition salts ##STR1## wherein X denotes any of the groups of the formula =CH(OR), =CO or =C=N-OR.sub.1,Y denotes any of the groups of the formula =CO, =CH(OR.sub.1), =C=N-OR.sub.1, =C(OR.sub.1)-C.tbd.CH or ##STR2## wherein R denotes a hydrogen atom, a C.sub.1-4 alkyl group or a C.sub.2-5 acyl group, andR.sub.1 denotes a hydrogen atom, a straight-chained or branched C.sub.1-5 alkyl group, a straight-chained or branched C.sub.1-5 hydroxyalkyl group, a C.sub.3-8 cycloalkyl group, an allyl group, or a benzyl group, andR.sub.3 has the same meaning as R.sub.2 but if R.sub.2 is a sec. or tert. alkyl group or an alicyclic group, then R.sub.3 can only be a hydrogen atom; and if R.sub.2 is a benzyl group then R.sub.3 can only be a hydrogen atom or a primary alkyl group, furtherR.sub.2 and R.sub.3 may denote together with the adjcacent nitrogen atom a piperidine, a morpholine, or an N-methylpiperazine group. These compounds have exhibited an aldosterone-antagonistic effect on rats.

摘要翻译： 式I的新型6-氨基-5α，19-环戊二烯衍生物及其药学上可接受的加成盐（I）其中X表示式= CH（OR），= CO或= C = N -OR1，Y表示式= CO，= CH（OR1），= C = N-OR1，= C（OR1）-C3ONDCH或者其中R表示氢原子，C1 -4-烷基或C 2-5酰基，R 1表示氢原子，直链或支链C 1-5烷基，直链或支链C 1-5羟基烷基，C 3-8环烷基， 烯丙基或苄基，R3与R2具有相同的含义，但如果R2为秒。 或叔。 烷基或脂环基，那么R 3只能是氢原子; 并且如果R 2是苄基，那么R 3只能是氢原子或伯烷基，R 2和R 3可以与相邻的氮原子一起表示哌啶，吗啉或N-甲基哌嗪基。 这些化合物对大鼠表现出醛固酮拮抗作用。

公开(公告)号：US4829076A

公开(公告)日：1989-05-09

申请号：US97111

申请日：1987-09-16

申请人： Geza Szilagyi ,  Eva Bozo ,  Laszlo Czollner ,  Laszlo Jaszlits ,  Gyorgy Rabloczky ,  Jozsef Borsi ,  Istvan Elekes ,  Gyongyi Nagy nee Csokas ,  Andras Varro ,  ZSuzanne Lang nee Rihmer ,  Gyorgy Cseh ,  Gyula Horvath ,  Ilona Bodi

发明人： Geza Szilagyi ,  Eva Bozo ,  Laszlo Czollner ,  Laszlo Jaszlits ,  Gyorgy Rabloczky ,  Jozsef Borsi ,  Istvan Elekes ,  Gyongyi Nagy nee Csokas ,  Andras Varro ,  ZSuzanne Lang nee Rihmer ,  Gyorgy Cseh ,  Gyula Horvath ,  Ilona Bodi

IPC分类号： A61K31/445 ,  A61K31/451 ,  A61K31/455 ,  A61P3/00 ,  A61P9/10 ,  A61P9/12 ,  C07D211/90 ,  C07D401/12 ,  C07D405/12

CPC分类号： C07D401/12 ,  C07D211/90 ,  C07D405/12

摘要： The invention relates to new substituted dihydropyridine derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.6 are as defined herein after, the racemic and optically active variants as well as mixtures thereof, furthermore the acid addition salts of these compounds, pharmaceutical compositions containing the same and a process for the preparation thereof.The compounds of the general formula (I) can be advantageously applied for the treatment of pathologically severe hypertensions, their toxicity is low and they possess an advantageous therapeutic index.

摘要翻译： 本发明涉及通式（I）的新的取代二氢吡啶衍生物，其中R 1和R 6如本文所定义，外消旋和光学活性变体及其混合物，此外，这些化合物的酸加成盐， 含有该组合物的药物组合物及其制备方法。 通式（I）的化合物可以有利地用于治疗病态严重的高血压，其毒性低，并且具有有利的治疗指标。

公开(公告)号：US4703036A

公开(公告)日：1987-10-27

申请号：US811937

申请日：1985-12-20

申请人： Sandor Bajusz ,  Erzsbet Szell nee Hasenohrl ,  Daniel Bagdy ,  Eva Barabas ,  Mariann Dioszegi ,  Zsuzsa Fittler ,  Ferencz Jozsa ,  Gyula Horvath ,  Eva Tomori nee Jozst

发明人： Sandor Bajusz ,  Erzsbet Szell nee Hasenohrl ,  Daniel Bagdy ,  Eva Barabas ,  Mariann Dioszegi ,  Zsuzsa Fittler ,  Ferencz Jozsa ,  Gyula Horvath ,  Eva Tomori nee Jozst

IPC分类号： C07K5/08 ,  A61K38/06 ,  C07K1/113 ,  C07K5/065 ,  C07K5/087 ,  A61K37/43

CPC分类号： C07K5/06078

摘要： The invention relates to new peptide-aldehydes and a process for the preparation thereof, furthermore to pharmaceutical compositions containing the same.According to a feature of the present invention there are provided new peptide-aldehyde derivatives corresponding to the general formula (I) ##STR1## wherein R.sub.1 represents hydrogen or C.sub.1-6 alkyl group,R.sub.2 stands for C.sub.1-6 alkyl group, furthermore R.sub.1 and R.sub.2 are linked to the amino group of the Xxx alpha-amino acid,Xxx represents a D-phenylalanine residue or a D-alpha-amino acid group having in the side chain a C.sub.1-4 alkyl group,Pro stands for L-proline residue,Yyy stands for L-, D- or DL-arginine residue andA represents an acid residue.The new peptide-aldehyde derivatives of the invention possess valuable anticoagulant activity.

摘要翻译： 本发明涉及新的肽醛及其制备方法，此外还涉及含有该肽的药物组合物。 根据本发明的特征，提供了对应于通式（I）的新的肽 - 醛衍生物：其中R 1表示氢或C 1-6烷基，R 2表示C 1-6烷基， 此外R1和R2连接到Xxxα-氨基酸的氨基，Xxx表示D-苯丙氨酸残基或在侧链中具有C1-4烷基的D-α-氨基酸基，Pro代表L 脯氨酸残基，Yyy代表L-，D-或DL-精氨酸残基，A代表酸残基。 本发明的新型肽 - 醛衍生物具有有价值的抗凝血活性。

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。

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。

公开(公告)号：US5241063A

公开(公告)日：1993-08-31

申请号：US717823

申请日：1991-06-19

申请人： Andras Toro ,  Gabor Ambrus ,  Istvan Pallagi ,  Nandor Makk ,  Gyula Horvath ,  Ferenc Szederkenyi ,  Eva Ilkoy ,  Antonia Jekkel ,  Imre Moravcsik ,  Kalman Konczol

发明人： Andras Toro ,  Gabor Ambrus ,  Istvan Pallagi ,  Nandor Makk ,  Gyula Horvath ,  Ferenc Szederkenyi ,  Eva Ilkoy ,  Antonia Jekkel ,  Imre Moravcsik ,  Kalman Konczol

IPC分类号： C07J7/00 ,  C07J21/00

CPC分类号： C07J7/0045 ,  C07J21/00

摘要： The invention relates to a novel process for the preparation of 17 .alpha.-hydroxy-20-oxopregnane derivatives of the general formula (I), ##STR1## wherein R.sub.1 means a hydroxy or an oxo group; andthe dotted lines optionally represent one or more additional valence bond(s), with the proviso that the dotted line in the 4-position and the dotted line in the 5-position cannot each simultaneously be an additional valence bond from steroids having 23,24-dinor-17(20)-dehydrocholan-22-oic -22-oic acid structure.According to the process of the invention a steroid derivative having 23,24-dinorcholan-22-oic acid structure, containing a double bond in 17(20)-position, is transformed to 17.alpha., 20-epoxy-23,24-dinorcholanoic acid, the latter is converted to a reactive acid derivative, which is then reacted with a salt-containing azide ion to yield a 17.alpha., 20-epoxy-23,24-dinorcholanoic acyl azide derivative and the azide obtained is reacted with a mineral or organic acid in an aqueous medium.

摘要翻译： 本发明涉及制备通式（I）的17α-羟基-20-氧代孕烷衍生物的新方法，其中R1表示羟基或氧代基; 并且虚线可选地表示一个或多个另外的价键，条件是4-位中的虚线和5-位的虚线不能同时作为具有23的类固醇的另外的价键， 24-二酮-17（20） - 脱氢胆烷-22-酸-22-酸结构。 根据本发明的方法，在17（20） - 位中含有双键的具有23,24-二肌醇二十二酸结构的类固醇衍生物转化为17α，20-环氧-23,24-二肉桂酸 酸，后者转化为反应性酸衍生物，然后与含盐的叠氮化物离子反应，得到17α，20-环氧-23,24-二牛油酰基叠氮化物衍生物，所得叠氮化物与矿物质反应 或有机酸。