公开(公告)号：US06815465B1

公开(公告)日：2004-11-09

申请号：US10048659

申请日：2002-06-03

申请人： Nándor Makk ,  Gábor Ambrus ,  Anikó Tegdes ,  András Jeney ,  Ferenc Timár

发明人： Nándor Makk ,  Gábor Ambrus ,  Anikó Tegdes ,  András Jeney ,  Ferenc Timár

IPC分类号： A61K31445

CPC分类号： C07D405/12 ,  C07D313/00

摘要： The invention relates to compounds of general formula (I) wherein R stands for a group of general formula —COOR1, —CONR2R3, —CONR4CONR4R5 or —CH2OR6, wherein R1 stands for a C2-6 alkyl group; a C1-6 alkyl group substituted; or a C3-6 cycloalkyl group; R2 and R3 are identical or different and stand independently from each other for hydrogen atom or a C1-6 alkyl group which optionally may be substituted; a 5- or 6-membered cycloalkyl or a heteroaryl group; and their tautomers, solvates and the mixtures thereof and acid addition salts of these compounds. The invention also relates to pharmaceutical compositions comprising compounds of general formula (I) as active agent. The angiogenesis-inhibitors according to the invention inhibit the neovascularization in living tissues and as such can be used for preventing and inhibiting angiogenesis appearing in connection with tumor growth and for preventing the formation of tumor metastases.

公开(公告)号：US06812007B1

公开(公告)日：2004-11-02

申请号：US09578587

申请日：2000-04-19

申请人： Vilmos Kéri ,  Irma Högye ,  Antónia Jekkel ,  Ilona Bagdi ,  Gábor Ambrus ,  Attila Jakab ,  Attila Andor ,  Lajos Deák ,  István Szabó ,  János Bálint ,  Zsuzsanna Scheidl ,  Etelka Deli ,  Gyula Horváth ,  Csaba Szabó ,  Ildikó Láng ,  Imre Székely ,  Imre Moravcsik ,  Vera Kovács ,  Szabolcs Mátyás ,  Zsuzsanna Sztáray ,  László Eszenyi ,  Éva Ilköy

发明人： Vilmos Kéri ,  Irma Högye ,  Antónia Jekkel ,  Ilona Bagdi ,  Gábor Ambrus ,  Attila Jakab ,  Attila Andor ,  Lajos Deák ,  István Szabó ,  János Bálint ,  Zsuzsanna Scheidl ,  Etelka Deli ,  Gyula Horváth ,  Csaba Szabó ,  Ildikó Láng ,  Imre Székely ,  Imre Moravcsik ,  Vera Kovács ,  Szabolcs Mátyás ,  Zsuzsanna Sztáray ,  László Eszenyi ,  Éva Ilköy

IPC分类号： C12P1706

CPC分类号： C12P17/06 ,  C12P7/62

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 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，并回收最终产物，其改进包括在7.5至约10之间的pH下进行溶解，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：US06905851B1

公开(公告)日：2005-06-14

申请号：US10030726

申请日：2000-06-29

申请人： Antónia Jekkel ,  Gábor Ambrus ,  Éva Ilkóy ,  Ildikó Horváth ,  Attila Kónya ,  István Mihály Szabó ,  Zsuzsanna Nagy ,  Gyula Horváth ,  Júlia Mózes ,  István Barta ,  György Somogyi ,  János Salát ,  Sándor Boros

发明人： Antónia Jekkel ,  Gábor Ambrus ,  Éva Ilkóy ,  Ildikó Horváth ,  Attila Kónya ,  István Mihály Szabó ,  Zsuzsanna Nagy ,  Gyula Horváth ,  Júlia Mózes ,  István Barta ,  György Somogyi ,  János Salát ,  Sándor Boros

IPC分类号： C12P7/62 ,  C07C69/30 ,  C12P1/04 ,  C12P7/42 ,  C12P17/06 ,  C12R1/29 ,  C12R1/31 ,  C12P17/42

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 bioconversion. 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-羟基化。 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。