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1. 发明申请

WO1997046523A1 ANTICOAGULANT PEPTIDE ALDEHYDE DERIVATIVES 审中-公开
标题翻译：抗坏血酸肽代谢物衍生物
公开(公告)号：WO1997046523A1
公开(公告)日：1997-12-11
申请号：PCT/HU1997000027
申请日：1997-06-05
申请人： GYOGYSZERKUTATO INTÉZET KFT. , BAJUSZ, Sándor , JUHASZ, Attila , BARABAS, Éva , FEHÉR, András , SZABO, Gabriella , SZÉLL, Erzsébet , VÉGHELYI, Irén , LAVICH, Emilia , KASZAS, Éva , LANGO, József , MORAVCSIK, Imre , SZEKER, Agnes , TASCHLER, Zsuzsanna , TOTH, Gábor , MOHAI, Zsuzsanna , SZALKAY, Anna, Mária , MAKK, Klára
发明人： GYOGYSZERKUTATO INTÉZET KFT.
IPC分类号： C07D207/09
CPC分类号： C07D207/16 , Y10S514/822
摘要： This invention relates to new peptide aldehyde derivatives of general formula (I): D-Xaa-Pro-Arg-H, wherein Xaa represents a 2-cycloheptyl-2-hydroxyacetyl or 2-cyclopentyl-2-hydroxyacetyl group, Pro represents an L-prolyl residue and Arg represents an L-arginyl residue, their acid-addition salts formed with an organic or inorganic acid and pharmaceutical compositions containing the same. The compounds of general formula (I) of the invention have valuable therapeutic, particularly anticoagulant, antiplatelet and antithrombotic, properties.
摘要翻译：本发明涉及通式（I）的新型肽醛衍生物：D-Xaa-Pro-Arg-H，其中Xaa表示2-环庚基-2-羟基乙酰基或2-环戊基-2-羟基乙酰基，Pro表示L - 脯氨酰残基，Arg表示L-精氨酰残基，它们与有机或无机酸形成的酸加成盐和含有它们的药物组合物。本发明通式（I）的化合物具有有价值的治疗，特别是抗凝血剂，抗血小板和抗血栓形成的特性。

2. 发明申请

WO1995001357A1 OPTICALLY ACTIVE 1-(4-NITROPHENYL)-4-METHYL-7,8-METHYLENEDIOXY-3,4-DIHYDRO-5H-2,3-BENZODIAZEPINE AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：光活性1-（4-硝基苯基）-4-甲基-7,8-甲基二氧代-3,4-二氢-5H- 2,3-苯并二氮杂及其制备方法
公开(公告)号：WO1995001357A1
公开(公告)日：1995-01-12
申请号：PCT/HU1994000024
申请日：1994-06-30
申请人： GYOGYSZERKUTATO INTÉZET KFT. , LING, István , HAMORI, Tamás , BOTKA, Péter , SOLYOM, Sándor , SIMAY, Antal , MORAVCSIK, Imre
发明人： GYOGYSZERKUTATO INTÉZET KFT.
IPC分类号： C07D491/056
CPC分类号： C07D491/04
摘要： The invention relates to the (+)- and (-)-enantiomers of the compounds of formula (I) as well as a process for the preparation of these enantiomers. This process comprises reducing 1-(4-nitrophenyl)-4-methyl-7,8-methylenedioxy-5H &cir& _-2,3-benzodiazepine of formula (II) by using an adduct formed from an (R)- or (S)-, respectively, 2-amino-1,1-diphenyl-alkan-1-ol derivative of general formula (III), wherein R1 and R2, which are different, stand for a straight or branched chain C1-4 alkyl group or an unsubstituted phenyl or benzyl group, with one molar equivalent of borane or a borane complex. The enantiomers of the compound of formula (I) are valuable intermediates in the synthesis of therapeutically active compounds.
摘要翻译：本发明涉及式（I）化合物的（+） - 和（ - ） - 对映异构体以及制备这些对映异构体的方法。该方法包括通过使用由（R） - 或（S（R））形成的加合物来还原式（II）的1-（4-硝基苯基）-4-甲基-7,8-亚甲基二氧基-5H和） - 分别为通式（III）的2-氨基-1,1-二苯基 - 烷-1-醇衍生物，其中不同的R 1和R 2表示直链或支链C 1-4烷基或未取代的苯基或苄基，与一摩尔当量的硼烷或硼烷络合物。式（I）化合物的对映异构体是合成治疗活性化合物的有价值的中间体。

3. 发明申请

WO1994010328A1 PROCESS FOR THE ISOLATION AND PURIFICATION OF MEVINOLIN 审中-公开
标题翻译：梅毒素的分离和纯化方法
公开(公告)号：WO1994010328A1
公开(公告)日：1994-05-11
申请号：PCT/HU1993000051
申请日：1993-09-08
申请人： BIOGAL GYOGYSZERGYAR RT , KÉRI, Vilmos , ILKOY, Éva , HOGYE, Irma , JEKKEL, Antónia , BAGDI, Ilona , AMBRUS, Gábor , JAKAB, Attila , ANDOR, Attila , DEAK, Lajos , SZABO, István , BALINI, János , SHEIDL, Zsuzsanna , DELI, Etelka , HORVATH, Gyula , SZABO, Csaba , LANG, Ildikó , SZÉKELY, Imre , MORAVCSIK, Imre , KOVACS, Vera , MATYAS, Szabolcs , SZTARAY, Zsuzanna , ESZENYI, László
发明人： BIOGAL GYOGYSZERGYAR RT
IPC分类号： C12P17/06
CPC分类号： C12P7/62 , C12P17/06
摘要： The present invention relates to a process for the isolation of mevinolin by dissolving the active ingredient from the biomass into the fermentation liquor and subsequently separating it from the filtered fermentation liquor, which comprises carrying out the dissolution at a pH value between 7.5 and 10.0, preferably between 8.0 and 9.0, separating the active ingredient from the filtered liquor at a pH value between 4.5 and 1.0, preferably between 2.2 and 2.0, filtering and purifying it by methods known per se, preferably by recrystallization.
摘要翻译：本发明涉及一种通过将活性成分从生物质中溶解到发酵液中并随后将其从过滤的发酵液中分离出来来分离mevinolin的方法，其中包括在7.5至10.0之间的pH值下进行溶解，优选在8.0和9.0之间，在4.5至1.0之间，优选在2.2和2.0之间的pH值下将过滤液体中的活性成分分离，通过本身已知的方法，优选通过重结晶进行过滤和纯化。

4. 发明申请

WO1998024792A1 ANTICOAGULANT GLYCOSIDES AND PHARMACEUTICAL COMPOSITIONS THEREOF 审中-公开
标题翻译：抗血清糖苷及其药物组合物
公开(公告)号：WO1998024792A1
公开(公告)日：1998-06-11
申请号：PCT/HU1997000078
申请日：1997-12-01
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , KOVACSNÉ BOZO, Éva , KUSZMANN, János , SZABO, Gabriella , BOROS, Sándor , RETTEGI, Tivadar , KASZAS, Éva , KENYERES, Lászlóné , MATUCZ, Éva , MORAVCSIK, Imre , ORBAN, Ottóné , TURUCZNÉ FERWAGNER, Mónika
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07D497/08
CPC分类号： C07H15/14
摘要： This invention relates to novel 2,6-anhydro-1,2-dithio-D-manno- and D-altropyranosides of formula (I) wherein R1 represents a hydroxy or an azido group, R2 representa a nitro, cyano, amidino, aminothiocarbonyl, -C(=NH)-OCH3, -C(=NH)-NH-NH2, -C(=NH)-SCH3 or an acetamido group, and the acid addition salts thereof formed with organic or inorganic acids, if possible as well as pharmaceutical compositions containing them. The compounds of the invention possess valuable therapeutic, particularly anticoagulant properties.
摘要翻译：本发明涉及式（I）的新颖的2,6-脱水-1,2-二硫代-D-甘露糖和D-吡喃吡咯烷，其中R1代表羟基或叠氮基，R2代表硝基，氰基，脒基，氨基硫代羰基，-C（= NH）-OCH 3，-C（= NH）-NH-NH 2，-C（= NH）-SCH 3或乙酰氨基，其酸加成盐与有机或无机酸形成，如果可能，以及含有它们的药物组合物。本发明的化合物具有有价值的治疗，特别是抗凝血性质。

5. 发明申请

WO1995013268A1 ULCER-INHIBITING TRIAZOLE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：抑制三唑衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：WO1995013268A1
公开(公告)日：1995-05-18
申请号：PCT/HU1993000063
申请日：1993-11-12
申请人： GYOGYSZERKUTATO INTÉZET KFT. , MARTONNÉ, Merész, Magdolna , KUSZMANN, János , ANDRASI, Ferenc , BERZSENYI, Pál , SEBESTYÉN, László , MORAVCSIK, Imre , SZIRAKI, István
发明人： GYOGYSZERKUTATO INTÉZET KFT.
IPC分类号： C07D249/12
CPC分类号： C07D249/12
摘要： The invention relates to novel 1,2,4-triazole derivatives of formulae (Ia) and (Ib), wherein R1 and R2, which are the same or different, stand for hydrogen; C1-4 alkyl or C1-4 alkenyl group; or a phenyl group optionally substituted by C1-4 alkyl or alkoxy group; and n is 0, 1 or 2, and acid-addition salts of these compounds. The invention further relates to pharmaceutical compositions containing these compounds as well as a process for the preparation of the compounds of formulae (Ia) and (Ib). The compounds of formulae (Ia) and (Ib) inhibit gastric-acid secretion and exert a significant protective effect on the gastric mucosa (cytoprotective action). Thus, they can be used for inhibiting and treating ulcers of the digestive system.
摘要翻译：本发明涉及式（Ia）和（Ib）的新的1,2,4-三唑衍生物，其中相同或不同的R 1和R 2代表氢; C 1-4烷基或C 1-4烯基; 或任选被C 1-4烷基或烷氧基取代的苯基; 和n为0,1或2，以及这些化合物的酸加成盐。本发明还涉及含有这些化合物的药物组合物以及制备式（Ia）和（Ib）化合物的方法。式（Ia）和（Ib）的化合物抑制胃酸分泌并对胃粘膜发挥显着的保护作用（细胞保护作用）。因此，它们可用于抑制和治疗消化系统的溃疡。

6. 发明申请

WO1997046576A1 ANTICOAGULANT PEPTIDYL-ARGININE ALDEHYDE DERIVATIVES 审中-公开
标题翻译：抗坏血酸蛋白酶阿德福德衍生物
公开(公告)号：WO1997046576A1
公开(公告)日：1997-12-11
申请号：PCT/HU1997000028
申请日：1997-06-05
申请人： GYOGYSZERKUTATO INTÉZET KFT. , BAJUSZ, Sándor , JUHASZ, Attila , BARABAS, Éva , FEHÉR, András , SZABO, Gabriella , SZÉLL, Erzsébet , VÉGHELYI, Irén , LAVICH, Emilia , KASZAS, Éva , LANGO, József , MORAVCSIK, Imre , SZEKER, Agnes , TASCHLER, Zsuzsanna , TOTH, Gábor , MOHAI, Zsuzsanna , SZALKAY, Anna Mária , MAKK, Klára
发明人： GYOGYSZERKUTATO INTÉZET KFT.
IPC分类号： C07K05/06
CPC分类号： C07K5/06078 , A61K38/00
摘要： The invention relates to new peptidyl-arginine aldehyde derivatives of general formula (I): Q-D-Xaa-Pro-Arg-H, wherein Q represents an acyl group of formula Q'-O-CO-, where Q' represents an alkyl group with 1-3 carbon atoms, D-Xaa represents 3-cyclobutyl-D-alanyl- or 3-cyclo-pentyl-D-alanyl- group, Pro stands for L-prolyl- group, and Arg stands for L-arginyl- group, and acid-addition salts thereof formed with an organic or inorganic acid and pharmaceutical compositions containing the same. The compounds of formula (I) have valuable therapeutic, particularly anticoagulant, properties together with inhibiting platelet functions and thrombosis development.
摘要翻译：本发明涉及通式（I）的新型肽基 - 精氨酸醛衍生物：QD-Xaa-Pro-Arg-H，其中Q表示式Q'-O-CO-的酰基，其中Q'表示烷基具有1-3个碳原子，D-Xaa表示3-环丁基-D-丙氨酰或3-环戊基-D-丙氨酰基，Pro代表L-脯氨酰基，Arg代表L-精氨酰基及其与有机酸或无机酸形成的酸加成盐和含有它们的药物组合物。式（I）化合物具有有价值的治疗性，特别是抗凝血性，以及抑制血小板功能和血栓形成。

7. 发明申请

WO1997014685A1 PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：吡嗪衍生物
公开(公告)号：WO1997014685A1
公开(公告)日：1997-04-24
申请号：PCT/HU1996000058
申请日：1996-10-14
申请人： GYOGYSZERKUTATO INTÉZET KFT , TOLDY, Rózsa +hf , TOLDY, Márta +hm , TOLDY, András +hm , ZUBOVICS, Zoltán , SZILAGYI, Katalin , VIDA, Franciska , ANDRASI, Ferenc , SUTKA, Klára , HODULA, Eszter , SZEKERES, Tibor , FEHÉR, Gábor , MORAVCSIK, Imre , MATYUS, Péter , SEBESTYÉN, László , SZABO, Hilda , ZARA, Erzsébet , HORVATH, Edit
发明人： GYOGYSZERKUTATO INTÉZET KFT , TOLDY, Rózsa +hf , TOLDY, Márta +hm , TOLDY, András +hm , TOLDY, Lajos +di
IPC分类号： C07D239/50
CPC分类号： C07D295/13 , C07D239/50
摘要： The invention refers to novel pyrimidine derivatives of formula (I), wherein R stands for a group of formula (a), wherein Ar means an aromatic homocyclic group, R and R represent hydrogen, halogen, hydroxy, alkyl, optionally substituted alkoxy, alkylthio group and oxidized derivatives thereof, optionally substituted amino, carboxy and derivatives thereof, sulfo and/or sulfonamido; and p, q and r are 0 or 1; R and R stand for amino; or a moiety derived from a nitrogen-containing heterocycle; X means a single bond; an optionally oxidized sulfur atom; or an optionally substituted nitrogen atom; A stands for an optionally substituted alkylene group; and n is 1 or 2. The invention relates also to a process and the intermediates for the preparation of the compounds of formula (I). The compounds according to the invention possess a remarkable lipid peroxidation inhibiting effect which is detectable both under in vitro and in vivo conditions. Thus, these compounds are useful for the prevention and/or treatment e.g. of injuries of the head, brain and spinal cord; as well as tissue damages arising from ischemia (including e.g. reperfusion injuries), myocardial infarction or coronary heart disease.
摘要翻译：本发明涉及式（I）的新颖的嘧啶衍生物，其中R 1代表式（a）的基团，其中Ar表示芳族的双环基团，R 4和R 5表示氢，卤素，羟基，烷基，任选取代的烷氧基，烷硫基及其氧化衍生物，任选取代的氨基，羧基及其衍生物，磺基和/或亚磺酰氨基; 和p，q和r为0或1; R 2和R 3代表氨基; 或衍生自含氮杂环的部分; X表示单键; 任选氧化的硫原子; 或任选取代的氮原子; A代表任选取代的亚烷基; 并且n为1或2.本发明还涉及用于制备式（I）化合物的方法和中间体。根据本发明的化合物具有显着的脂质过氧化抑制作用，其在体外和体内条件下均可检测。因此，这些化合物可用于预防和/或治疗。头部，脑部和脊髓受伤; 以及由缺血（包括例如再灌注损伤），心肌梗死或冠心病引起的组织损伤。

8. 发明专利

CA2006144A1 MICROBIAL PROCESS FOR THE PRODUCTION OF IMMUNOSUPPRESSIVE ANTIBIOTICS 未知
公开(公告)号：CA2006144A1
公开(公告)日：1990-06-20
申请号：CA2006144
申请日：1989-12-20
申请人： JEKKEL, ANTONIA , AMBRUS, GABOR , SARUDY, EVA T. , SZABO, ISTVAN M. , HUELBER, AGOTA , ANDOR, ATTILA , ALBRECHT, KAROLY , KOENCZOEL, KALMAN , SZELL, VALERIA , TOMORI, EVA , MORAVCSIK, IMRE , POLYA, KALMAN , ERDEI, JANOS , KISS, LAJOS , NAGY, KAROLY , PALOTAS, BELA , DELI, ETELKA , BUZASI, KAROLY , MOLNAR, ANIKO , SANTHA, GYOERGY , SZASZHEGYESI, VILMA , MAKADI, BELA
发明人： JEKKEL, ANTONIA , AMBRUS, GABOR , SARUDY, EVA T. , SZABO, ISTVAN M. , HUELBER, AGOTA , ANDOR, ATTILA , ALBRECHT, KAROLY , KOENCZOEL, KALMAN , SZELL, VALERIA , TOMORI, EVA , MORAVCSIK, IMRE , POLYA, KALMAN , ERDEI, JANOS , KISS, LAJOS , NAGY, KAROLY , PALOTAS, BELA , DELI, ETELKA , BUZASI, KAROLY , MOLNAR, ANIKO , SANTHA, GYOERGY , SZASZHEGYESI, VILMA , MAKADI, BELA
IPC分类号： C12N1/14 , A61K31/545 , A61K38/00 , A61P37/06 , C07D501/00 , C07K7/64 , C12P1/00 , C12P21/04 , C12P35/00 , C12R1/645
摘要： The invention relates to a microbial process for the production of immunosuppressive cyclosporine antibiotic complex or of its components, cyclosporine A, cyclosporine B and cyclosporine C, by the aerobic fermentation of a filamentous fungus strain biosynthesizing the above antibiotic(s) in a nutrient medium containing utilizable carbon and nitrogen sources as well as mineral salts, and by isolating the products formed, which comprises culturing a strain of the novel Tolypocladium varium fungus species producing the cyclosporine antibiotic complex, preferably tolypocladium varium sp. nov. CY/93, deposited at the National Collection of Agricultural and Industrial Microorganisms, Budapest, Hungary under the number NCAIM(P)F 001005, on a nutrient medium containing carbon sources, organic and inorganic nitrogen sources as well as mineral salts, under aerobic conditions, at 25 DEG to 30 DEG C., and, if desired, isolating and purifying the cyclosporine antibiotic complex or its components produced.

9. 发明授权

US5430017A Oral pharmaceutical composition containing cyclosporin and process for preparing same 失效
标题翻译：含有环孢菌素的口服药物组合物及其制备方法
公开(公告)号：US5430017A
公开(公告)日：1995-07-04
申请号：US915719
申请日：1993-05-20
申请人： Kovacs Antalne , Kiss Tamasne , Jancso Sandor , Jusztin Istvanne , Kovacs Istvan , Takacs Erzsebet , Orban Erno , Tomori Lazlone , Kurthy Maria , Balogh Tibor , Jaszlits Laszlo , Moravcsik Imre
发明人： Kovacs Antalne , Kiss Tamasne , Jancso Sandor , Jusztin Istvanne , Kovacs Istvan , Takacs Erzsebet , Orban Erno , Tomori Lazlone , Kurthy Maria , Balogh Tibor , Jaszlits Laszlo , Moravcsik Imre
IPC分类号： A61K9/08 , A61K38/00 , A61K38/13 , A61K47/10 , A61K47/34 , A61P37/06 , A61K31/74
CPC分类号： A61K47/10 , A61K38/13
摘要： The invention relates to a pharmaceutical composition for oral administration containing cyclosporin A and/or cyclosporin G as active ingredient, which possess advantageous absorption characteristics, and to a process for preparing this composition. The composition according to the invention comprises 1 part by mass of one or more cyclosporin(s) dissolved in 4 to 50 parts by volume of propylene glycol, 0 to 25 parts by volume of ethanol and 0.0 to 5 parts by mass of a polyoxyethylene/polyoxypropylene block polymer in homogenized state. Based on examinations carried out at 100.degree. C., the stability of solutions prepared according to the invention does not differ from that of the commercially available Sandimmun oral solution.
摘要翻译：本发明涉及含有环孢菌素A和/或环孢菌素G作为活性成分的具有有利吸收特征的口服给药组合物，以及制备该组合物的方法。根据本发明的组合物包含1质量份溶解在4至50体积份丙二醇中的一种或多种环孢菌素，0至25体积份乙醇和0.0至5质量份聚氧乙烯/ 聚丙烯嵌段聚合物处于均匀状态。基于在100℃下进行的检查，根据本发明制备的溶液的稳定性与市售的Sandimmun口服溶液的稳定性没有差异。

10. 发明申请

WO1997049716A1 NOVEL ANTICOAGULANT GLYCOSIDES AND PHARMACEUTICAL COMPOSITIONS THEREOF 审中-公开
标题翻译：新型抗血清糖蛋白及其药物组合物
公开(公告)号：WO1997049716A1
公开(公告)日：1997-12-31
申请号：PCT/HU1997000031
申请日：1997-06-23
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , KOVACSNÉ BOZO, Éva , KUSZMANN, János , SZABO, Gabriella , BOROS, Sándor , MORAVCSIK, Imre
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07H15/203
CPC分类号： C07H15/203
摘要： This invention relates to novel 1,5-dithio-pyranosides of formula (I) wherein R1 represents hydrogen, hydroxy or an azido group, R2 represents hydroxy, azido, amino or an acetamido group, R3 represents hydroxy or an azido group, R4 represents hydrogen, methyl or a hydroxymethyl group, R5 represents hydrogen, R4 and R5 together represent a methylene group, R6 represents a nitro, cyano, amidino, aminothiocarbonyl, -C(=NH)-OCH3, -C(=NH)-NH-NH2 or -C(=NH)-SCH3 group, with the proviso that R6 represents only a group other than a nitro or cyano group if R1-R3 each represents hydroxy groups, and R4 as well as R5 represent hydrogen, furthermore that R6 represents only a group other than a nitro group if R1-R3 each represents hydroxy groups, R4 represents a hydroxymethyl group and R5 represents hydrogen, and the acid addition salts thereof formed with organic or inorganic acids, if possible and pharmaceutical compositions containing the same. The compounds of the invention possess valuable therapeutic, particularly anticoagulant properties.
摘要翻译：本发明涉及式（I）的新的1,5-二硫代吡喃糖苷，其中R 1表示氢，羟基或叠氮基，R 2表示羟基，叠氮基，氨基或乙酰氨基，R 3表示羟基或叠氮基，R 4表示氰基，脒基，氨基硫代羰基，-C（= NH）-OCH 3，-C（= NH）-NH-（甲氧基羰基） NH 2或-C（= NH）-SCH 3基团，条件是如果R 1 -R 3各自表示羟基，则R 6表示除硝基或氰基以外的基团，R 4和R 5表示氢，此外，R 6表示如果R 1 -R 3各自表示羟基，则R 4表示羟甲基，R 5表示氢，并且其有机酸或无机酸形成的酸加成盐，以及含有它们的药物组合物。本发明的化合物具有有价值的治疗，特别是抗凝血性质。

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