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1. 发明专利

JPS588058A 16-AMINO-PROSTAGLANDIN DERIVATIVES, MANUFACTURE AND MEDICINAL COMPOSITION 失效
公开(公告)号：JPS588058A
公开(公告)日：1983-01-18
申请号：JP9977781
申请日：1981-06-29
申请人： GYOGYSZERKUTATO INTEZET
发明人： JIYAPORU ARUBURUSU , EBA TOOTOOSARUDEI , JIYORUJIYU CHIEE , ISUTOBAAN BARUTA , GIYURA HORUBAATO
IPC分类号： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C12P31/00

3. 发明专利

JPS5522661A 1*66DIMETHYLL3*44DIMETHYLLDDMANNITOL 失效
公开(公告)号：JPS5522661A
公开(公告)日：1980-02-18
申请号：JP5520079
申请日：1979-05-04
申请人： GYOGYSZERKUTATO INTEZET
发明人： JIYANOSU KUSUZUMAN , PARU SOHARU , ENDORE SUSANIII , EMIRIA KIRARII NII BUIDA
IPC分类号： A61K31/255 , A61K31/047 , A61P35/00 , A61P35/02 , C07C67/00 , C07C301/00 , C07C303/26 , C07C303/28 , C07C309/63 , C07C309/66

4. 发明专利

JPS5163171A Chiazoorushinkyudotainoseiho 失效
公开(公告)号：JPS5163171A
公开(公告)日：1976-06-01
申请号：JP5715675
申请日：1975-05-14
申请人： Gyogyszerkutato Intezet
发明人： GABORU AMUBURUSU , ISUTOBAN BARUTA , ZUSUZUSANNA MEESUFUARUI , GYURA HORUASU
IPC分类号： C07D277/20 , C07D277/30 , E21D23/00 , E21D23/04
CPC分类号： E21D23/0021 , C07C67/00 , C07C67/307 , C07C67/343 , C07D277/30 , E21D23/0409 , C07C69/716

5. 发明专利

JPH0680078B2 失效
公开(公告)号：JPH0680078B2
公开(公告)日：1994-10-12
申请号：JP28585185
申请日：1985-12-20
申请人： GYOGYSZERKUTATO INTEZET
发明人： SAANDORU BAIYUSU , ERUJEEBETO SUEERU , DAANIERU BAGUDEI , EEBA BARABAASU , MARIAN DEIOOSEGI , JUJA FUITORERU , FUERENTSU IOOJA , JURA HORUBAATSU , EEBA TOMORI
IPC分类号： C07K5/08 , A61K38/06 , C07K1/113 , C07K5/06 , C07K5/065 , C07K5/087

7. 发明申请

WO0121607A3 PROCESS FOR THE PREPARATION OF MYCOPHENOLIC ACID AND DERIVATIVES THEREOF 审中-公开
标题翻译：制备麦芽酚酸及其衍生物的方法
公开(公告)号：WO0121607A3
公开(公告)日：2001-09-07
申请号：PCT/HU0000099
申请日：2000-09-22
申请人： GYOGYSZERKUTATO INTEZET , BARTA ISTVAN , BOROS SANDOR , AMBRUS GABOR , HORVATH GYULA , SZABO ANTAL , SZABO ISTVAN MIHALY , JEKKEL ANTONIA , KONYA ATTILA , MOZES JULIANNA , SALAT JANOS , SOMOGYI GYOERGY
发明人： BARTA ISTVAN , BOROS SANDOR , AMBRUS GABOR , HORVATH GYULA , SZABO ANTAL , SZABO ISTVAN MIHALY , JEKKEL ANTONIA , KONYA ATTILA , MOZES JULIANNA , SALAT JANOS , SOMOGYI GYOERGY
IPC分类号： C07D307/88 , C12P17/04
CPC分类号： C12P17/04 , C07D307/88
摘要： The invention relates to a microbiological process for the preparation of compounds of general formula (I), wherein R1 means methyl or hydroxymethyl group and R2 stands for hydroxyl or amino group, which comprises growing a Penicillium waksmani fungal strain able to biosynthesising mycophenolic acid on a culture medium containing assimilable carbon and nitrogen sources as well as mineral salts at 22 DEG C to 30 DEG C, separating the compound of general formula (I), wherein R1 means methyl group and R2 stands for hydroxyl group, from the fermentation broth and, if desired, purifying it and, if desired, bioconverting it a) by using the cultures of Streptomyces griseoruber No. 1/6 actinomycete strain deposited at the National Collection of Agricultural and Industrial Microorganisms as Streptomyces sp. No. 1/6 under No. NCAIM (P)B 001275 to prepare a compound of general formula (I), wherein R1 means methyl group and R2 stands for amino group; or b) by using the cultures of Streptomyces resistomycificus No. 1/28 actinomycete strain deposited at the National Collection of Agricultural and Industrial Microorganisms under No. NCAIM (P)B 001276 to prepare a compound of general formula (I), wherein R1 means hydroxymethyl group and R2 stands for amino group on a culture medium containing assimilable carbon and nitrogen sources as well as mineral salts under submerged, aerated conditions up to completion of the bioconversion, then separating the compound of general formula (I) formed from the culture and, if desired, purifying it.
摘要翻译：本发明涉及制备通式（I）化合物的微生物方法，其中R1表示甲基或羟甲基，R2代表羟基或氨基，其包括生长青霉菌真菌菌株能够在含有可同化碳源和氮源的培养基以及22℃至30℃的无机盐中生物合成霉酚酸，分离通式（I）的化合物，其中R1表示甲基，R2表示羟基，如果需要，对其进行纯化，如果需要，将其生物转化为a）通过使用保藏在国家农业部收集的灰霉链霉菌（Streptomyces griseoruber）1/6放线菌菌株的培养物工业微生物作为在NCAIM（P）B 001275号下的链霉菌（Streptomyces sp。）1/6，制备通式（I）的化合物，其中R1表示甲基，R2表示氨基; 或b）通过使用在NCAIM（P）B 001276号国家农业和工业微生物收集库保藏的依赖于链霉菌链霉菌（Streptomyces）的1/28放线菌菌株的培养物来制备通式（I）化合物，其中R1表示羟甲基，R2代表含有可同化碳源和氮源的培养基上的氨基，以及在浸没的充气条件下直至生物转化完成的矿物盐，然后将通式 I）由培养物形成，如果需要，可以纯化。

8. 发明申请

WO0109113A3 HETEROCYCLIC COMPOUNDS INHIBITING ANGIOGENESIS 审中-公开
标题翻译：杂环化合物抑制血管生成
公开(公告)号：WO0109113A3
公开(公告)日：2001-06-14
申请号：PCT/HU0000088
申请日：2000-08-02
申请人： GYOGYSZERKUTATO INTEZET , MAKK NANDOR , AMBRUS GABOR , TEGDES ANIKO , JENEY ANDRAS , TIMAR FERENC
发明人： MAKK NANDOR , AMBRUS GABOR , TEGDES ANIKO , JENEY ANDRAS , TIMAR FERENC
IPC分类号： A61K31/335 , A61K31/34 , A61K31/4427 , A61K31/5377 , A61P17/06 , A61P19/02 , A61P27/02 , A61P35/00 , A61P35/04 , A61P43/00 , C07D313/00 , C07D405/12 , C07D407/12
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 -COOR , -CONR R , -CONR CONR R or -CH2OR , wherein R stands for a C2-6 alkyl group; a C1-6 alkyl group substituted; or a C3-6 cycloalkyl group; R and R 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 neovascularisation in living tissues and as such can be used for preventing and inhibiting angiogenesis appearing in connection with tumour growth and for preventing the formation of tumour metastases.
摘要翻译：本发明涉及通式（I）的化合物，其中R代表通式-COOR 1，-CONR 2 R 3，-CONR 4 CONR 4 R 5或-CONR 4 CONR 4 R 5或 -CH 2 OR 6，其中R 1代表C 2-6烷基; C 1-6烷基取代; 或C 3-6环烷基; R 2和R 3相同或不同，并且氢原子或任选可被取代的C 1-6烷基彼此独立地独立地表示。 5-或6-元环烷基或杂芳基; 及其互变异构体，溶剂合物及其混合物，以及这些化合物的酸加成盐。本发明还涉及包含通式（I）化合物作为活性剂的药物组合物。根据本发明的血管生成抑制剂抑制活组织中的新生血管形成，因此可以用于预防和抑制与肿瘤生长有关的血管生成并防止肿瘤转移的形成。

9. 发明授权

US5380724A Piperazine and homopiperazine derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：哌嗪和高哌嗪衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US5380724A
公开(公告)日：1995-01-10
申请号：US78601
申请日：1993-06-16
申请人： Zoltan Zubovics , Katalin Goldschmidt , Katalin Szilagyi , Ferenc Andrasi , Eszter Hodula , Lajos Toldy , Klara Sutka , Zsuzsanna Fittler , Laszlo Sebestyen , Katalin Gorgenyi , Istvan Sziraki , Jozsef Gyimesi , Valeria Vitkoczi
发明人： Zoltan Zubovics , Katalin Goldschmidt , Katalin Szilagyi , Ferenc Andrasi , Eszter Hodula , Lajos Toldy , Klara Sutka , Zsuzsanna Fittler , Laszlo Sebestyen , Katalin Gorgenyi , Istvan Sziraki , Jozsef Gyimesi , Valeria Vitkoczi
IPC分类号： A61K31/50 , A61K31/496 , A61K31/505 , A61K31/517 , A61K31/519 , A61P1/04 , A61P1/16 , A61P3/00 , A61P3/10 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/08 , A61P13/12 , A61P29/00 , A61P37/06 , C07D237/20 , C07D239/48 , C07D239/50 , C07D239/94 , C07D239/95 , C07D403/06 , C07D475/00 , C07D475/06 , C07D475/08 , A61K31/495 , C07D239/02 , C07D403/04 , C07D487/00
CPC分类号： C07D239/95 , C07D237/20 , C07D239/50 , C07D475/06 , C07D475/08 , Y02P20/55
摘要： This invention relates to novel compounds of the general formula (I) and the pharmaceutically acceptable acid addition salts thereof. In the general formula (I) ##STR1## wherein Lip, A.sup.1, A.sup.2, Het and n are defined as in the specification. The compounds of the general formula (I) inhibit the lipid peroxidation and therefore, they are useful for the treatment or prevention of diseases and conditions wherein the inhibition of lipid peroxidation is desirable.
摘要翻译：本发明涉及通式（I）的新化合物及其药学上可接受的酸加成盐。在通式（I）中，其中Lip，A1，A2，Het和n如说明书中所定义。通式（I）的化合物抑制脂质过氧化，因此它们可用于治疗或预防需要脂质过氧化抑制的疾病和病症。

10. 发明授权

US4308278A Anorexigenic 4-[(3,4-dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives 失效
标题翻译：厌氧性4 - [（3,4-二烷氧基苯基）烷基] -2-咪唑烷酮衍生物
公开(公告)号：US4308278A
公开(公告)日：1981-12-29
申请号：US90450
申请日：1979-11-01
申请人： Geza Schneider , Ferenc Andrasi , Pal Berzsenyi , Arpad Lazar , Sandor Elek , Istvan Elekes , Istvan Polgari
发明人： Geza Schneider , Ferenc Andrasi , Pal Berzsenyi , Arpad Lazar , Sandor Elek , Istvan Elekes , Istvan Polgari
IPC分类号： A61K31/415 , A61K31/4166 , A61P1/00 , A61P3/04 , C07C45/71 , C07D233/32 , C07D233/34 , C07D233/38 , C07D233/78
CPC分类号： C07C255/00 , C07C45/71 , C07D233/32 , C07D233/38 , C07D233/78 , Y10S514/91
摘要： 4-[(3,4-Dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives having the formula I ##STR1## wherein R.sup.1 stands for a cycloalkyl group containing from 3 to 6 carbon atoms or benzyl group;R.sup.2 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.3 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.4 stands for hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms or an alkoxycarbonyl group containing from 1 to 4 carbon atoms; andR.sup.5 stands for hydrogen atom or an alkoxycarbonyl group containing from 1 to 4 carbon atoms,are prepared by(a) reducing a hydantoin derivative having the general formula II, wherein R.sup.1 and R.sup.2 are as defined above, with lithium aluminum hydride in a neutral organic solvent, or(b) hydrogenating catalytically an 1,3-dihydro-2H-imidazol-2-one derivative having the general formula III, wherein R.sup.1 and R.sup.3 are as defined above, while the meaning of R.sup.4 is hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, or(c) reacting a carbamate derivative having the general formula IV, wherein R.sup.1 is as defined above, while R.sup.6 stands for an alkyl group containing from 1 to 4 carbon atoms, with an organic or inorganic base.The compounds having the formula I possess valuable therapeutical properties, mainly anorexigenic activity.
摘要翻译： 4 - [（3,4-二烷氧基苯基）烷基] -2-咪唑啉酮衍生物，其具有式I其中R1代表含有3至6个碳原子的环烷基或苄基; R2代表氢原子或含有1至4个碳原子的烷基; R3代表氢原子或含有1至4个碳原子的烷基; R4表示氢原子或含有1至4个碳原子的烷基或含有1至4个碳原子的烷氧基羰基; 并且R5代表氢原子或含有1至4个碳原子的烷氧基羰基，是通过以下步骤制备的：（a）将具有通式II的乙内酰脲衍生物（其中R 1和R 2如上定义）与中性的氢化铝锂有机溶剂，或（b）催化氢化具有通式III的1,3-二氢-2H-咪唑-2-酮衍生物，其中R 1和R 3如上所定义，而R 4的含义是氢原子或烷基含有1至4个碳原子的基团，或（c）使具有通式IV的氨基甲酸酯衍生物与其中R 1如上定义，而R6代表含有1至4个碳原子的烷基，与有机或无机基础。具有式I的化合物具有有价值的治疗性质，主要是厌食症活性。

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