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1. 发明申请

WO1994014788A1 NOVEL DERIVATIVES OF A FIVE-MEMBERED RING FUSED BENZENE, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：五元醇环氧树脂的新型衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：WO1994014788A1
公开(公告)日：1994-07-07
申请号：PCT/HU1993000078
申请日：1993-12-17
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , HOFFMAN, György , DOBAY, László , FISCHER, János , PERÉNYI, Éva , EZER, Elemér , MATUZ, Judit , SAGHY, Katalin , SZPORNY, László , HAJOS, György
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07D307/83
CPC分类号： C07D295/205 , C07C69/738 , C07C235/78 , C07C2602/08 , C07D307/83
摘要： The invention relates to novel, therapeutically active acid, salt, ester and amide derivatives of a 5-membered ring fused benzene of formula (I), wherein R is selected from hydroxy, (C1-4)alkoxycarbonylmethoxy, (C1-4)alkylamino, cyclohexylamino; phenylamino optionally substituted by halogen; (C1-4)alkoxycarbonylmethylamino, 1-(C1-4)alkoxycarbonyl-2-phenylethylamino, pyrrolidino and N-(C1-4)alkoxycarbonylpiperazino; and X stands for oxygen or methylene, with the proviso that X means oxygen when R stands for hydroxy; and their salts formed with H2 receptor antagonists, when X means oxygen and R stands for hydroxy, as well as pharmaceutical compositions containing the above compounds. The invention relates also to a process for the preparation of the above compounds and compositions. The compounds of formula (I) show significant gastrocytoprotective and gastric acid secretion inhibitory activities. In addition, they possess an antibacterial activity against the pathogenic bacterial strain Helicobacter pylori. Thus, they are useful for the prevention and/or healing of various ulcerative diseases of the digestive system (oesophagus, stomach and duodenum).
摘要翻译：本发明涉及式（I）的5-元环稠合苯的新的治疗活性的酸，盐，酯和酰胺衍生物，其中R选自羟基，（C 1-4）烷氧基羰基甲氧基，（C 1-4）烷基氨基，环己基氨基; 任选被卤素取代的苯基氨基; （C 1-4）烷氧基羰基甲基氨基，1-（C 1-4）烷氧基羰基-2-苯基乙基氨基，吡咯烷子基和N-（C 1-4）烷氧基羰基哌嗪基; X代表氧或亚甲基，条件是当R代表羟基时，X表示氧; 并且它们的盐与H 2受体拮抗剂形成，当X表示氧，R代表羟基时，以及含有上述化合物的药物组合物。本发明还涉及制备上述化合物和组合物的方法。式（I）化合物显示出显着的胃细胞保护和胃酸分泌抑制活性。此外，它们对致病性细菌菌株幽门螺杆菌具有抗菌活性。因此，它们可用于预防和/或愈合消化系统（食道，胃和十二指肠）的各种溃疡性疾病。

2. 发明申请

WO1994014749A1 DOUBLE ESTERS OF BENZOYLACRYLIC ACIDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：苯甲酰丙烯酸双酯，含有它们的药物组合物及其制备方法
公开(公告)号：WO1994014749A1
公开(公告)日：1994-07-07
申请号：PCT/HU1993000068
申请日：1993-12-10
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , BALLO, Ildikó , FISCHER, János , PETÉNYI, Éva , EZER, Elemér , MATUZ, Judit , SAGHY, Katalin , SZPORNY, László , HAJOS, György
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07C69/738
CPC分类号： C07C69/738
摘要： The invention relates to novel double esters of benzoylacrylic acid of general formula (I), pharmaceutical compositions containing them and a process for their preparation. In general formula (I), R stands for a C1-4 alkyl group; or a phenyl group optionally substituted by one or more C1-4 alkoxy group(s); or 3-phenyl-3-oxo-1(E)-propenyl group; and n is 2, 3 or 4. The compounds of general formula (I) possess excellent antiulcer properties and a significant effect against Helicobacter pylori bacteria. Thus, they are useful for the therapeutic and/or prophylactic treatment of various ulcers of the oesophagus, stomach and duodenum.
摘要翻译：本发明涉及通式（I）的苯甲酰基丙烯酸的新型双酯，含有它们的药物组合物及其制备方法。在通式（I）中，R代表C 1-4烷基; 或任选被一个或多个C 1-4烷氧基取代的苯基; 或3-苯基-3-氧代-1（E） - 丙烯基; 并且n为2,3或4.通式（I）的化合物具有优良的抗溃疡性质和对幽门螺杆菌的显着效果。因此，它们可用于治疗和/或预防性治疗食管，胃和十二指肠的各种溃疡。

3. 发明申请

WO1990013559A1 NOVEL 9'alpha'-HYDROXY-3-OXO-4,24(25)-STIGMASTADIEN-26-OIC ACID DERIVATIVES, A PROCESS FOR PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：新的9α-羟基-3-OXO-4,24（25）-STIGMASTADIEN-26-酸式衍生物，其制备方法和含有其的药物组合物
公开(公告)号：WO1990013559A1
公开(公告)日：1990-11-15
申请号：PCT/HU1990000033
申请日：1990-05-10
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , AMBRUS, Gábor , MADERSPACH, Andrea , JEKKEL, Antalné , JAVOR, András , ILKOY, Éva , HAJOS, György , SZPORNY, László , NAGY, József , HORVATH, Gyula , MORAVCSIK, Imre
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07J09/00
CPC分类号： C07J9/005
摘要： The invention relates to novel 9 alpha -hydroxy-3-oxo-4,24(25)-stigmastadien-26-oic acid derivatives of general formula (I), wherein M stands for hydrogen, C1-4 alkyl or a pharmaceutically acceptable cation. Further the invention relates to a process for preparing these compounds. The new compounds of general formula (I) exert anti-hypercholesteremic effect.
摘要翻译：本发明涉及通式（I）的新型9α-羟基-3-氧代-4,24（25） - 蓖麻醇二酯-26-酸酸衍生物，其中M代表氢，C 1-4烷基或药学上可接受的阳离子。此外，本发明涉及一种制备这些化合物的方法。通式（I）的新化合物发挥抗胆固醇的作用。

4. 发明申请

WO1994014768A1 NOVEL PYRROLINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：新型吡咯衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：WO1994014768A1
公开(公告)日：1994-07-07
申请号：PCT/HU1993000076
申请日：1993-12-17
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , HOFFMAN, György , FISCHER, János , EZER, Elemér , MATUZ, Judit , SAGHY, Katalin , SZPORNY, László , HAJOS, György
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07D207/38
CPC分类号： C07D207/38
摘要： The invention relates to novel pyrroline derivatives of formula (I), wherein R represents hydrogen, halogen, a C1-4alkyl or nitro group; R represents hydrogen or a C1-4alkyl group; R represents a C1-4alkyl group; m is 1 or 2; and n is 0 or 1, with the proviso that R means hydrogen when n is 1, as well as pharmaceutical compositions containing these compounds. The invention relates also to a process for the preparation of the above compounds and compositions. The compounds of formula (I) exert cytoprotective activity as well as antibacterial activity against Helicobacter pylori strains. Thus, they are useful for the prevention and/or healing of various inflammatory and ulcerative diseases of the duodenum, stomach and oesophagus.
摘要翻译：本发明涉及式（I）的新型吡咯啉衍生物，其中R表示氢，卤素，C1-4烷基或硝基; R 1表示氢或C 1-4烷基; R 2表示C 1-4烷基; m为1或2; 且n为0或1，条件是当n为1时，R 1表示氢，以及含有这些化合物的药物组合物。本发明还涉及制备上述化合物和组合物的方法。式（I）化合物对幽门螺杆菌菌株具有细胞保护活性以及抗菌活性。因此，它们可用于预防和/或愈合十二指肠，胃和食道的各种炎性和溃疡性疾病。

5. 发明申请

WO1993012787A1 NEW PHARMACEUTICAL COMPOSITIONS INHIBITING GASTRIC ACID SECRETION AND EXERTING GASTROCYTOPROTECTIVE EFFECT 审中-公开
标题翻译：新型药物组合物抑制胃酸分泌和促进胃肠道保护作用
公开(公告)号：WO1993012787A1
公开(公告)日：1993-07-08
申请号：PCT/HU1992000059
申请日：1992-12-18
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , DOBAY, László , FISCHER, János , MARVANYOS, Ede , FODOR, Tamás , TRISCHLER, Ferenc , PERÉNYI, Éva , GASPAR, Katalin , EZER, Elemér , MATUZ, Judith , SAGHY, Katalin , SZPORNY, László , HAJOS, György
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： A61K31/415
CPC分类号： C07D233/64 , A61K31/35 , A61K31/38 , A61K31/415 , C07C317/44 , C07D311/24 , A61K2300/00
摘要： The invention relates to new pharmaceutical compositions inhibiting gastric acid secretion and exerting gastrocytoprotective effect which contain as active ingredient a 10:1-1:10 (w/w) mixture of a compound of general formula (II), wherein X represents an oxygen or sulfur atom, and R represents a hydrogen atom, a hydroxy, C1-4 alkyl or C1-4 alkoxy group, or a compound of general formula (III), wherein R represents a hydrogen or halogen atom, and a compound of general formula (IV), or a compound of general formula (I), wherein A represents a group of general formulas (V) or (VI), wherein X, R and R have the same meaning as above, and B is the protonated form of the compound of general formula (IV), in admixture with carriers and additives known in the art, furthermore to processes preparing the same and to a treatment method for the therapy and/or prophylaxis of mammals - including men - suffering from inflammatory and ulcerous diseases of the esophagus, stomach and duodenum.
摘要翻译：本发明涉及抑制胃酸分泌和施用胃保护作用的新药物组合物，其含有作为通式（II）化合物的10:1-1:10（w / w）混合物的活性成分，其中X表示氧或硫原子，R表示氢原子，羟基，C 1-4烷基或C 1-4烷氧基，或通式（III）的化合物，其中R 1表示氢或卤素原子，通式（Ⅳ）或通式（I）的化合物，其中A表示通式（Ⅴ）或（Ⅵ）的基团，其中X，R和R 1具有与上述相同的含义，B 是通式（IV）化合物的质子化形式，与本领域已知的载体和添加剂的混合物，以及其制备方法以及用于治疗和/或预防哺乳动物（包括男性）的治疗方法来自食道，胃和十二指肠的炎性和溃疡性疾病。

6. 发明申请

WO1989005799A1 NOVEL TETRAHYDROPYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：新型四氢吡啶衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：WO1989005799A1
公开(公告)日：1989-06-29
申请号：PCT/HU1988000078
申请日：1988-12-13
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , SOLYOM, Sándor , HARSANYI, Kálmán , EZER, Elemér , MATUZ, Judit , SZPORNY, László , SAGHY, Katalin , HAJOS, György , SZÉKELY, Krisztina , HEGEDÜS, Béla
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07D211/70
CPC分类号： C07D211/70
摘要： The invention relates to novel tetrahydropyridine derivatives of formula (I) and pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In formula (I), R1 means hydrogen or a C1-6 alkyl group; R2 and R3 stand, independently from each other, for hydrogen or a C1-6 alkyl group; or alternatively R2 and R3 together represent a chemical bond; R4 means halogen, a trifluoromethyl or a C1-6 alkyl group; R1 and R3 are in Z (cis) or E (trans) position in their mutual relation when R2 and R3 do not form together a chemical bond or the meaning of R1 is different from that of R2, with the proviso that R1 and R2 are different from hydrogen when R4 means a 4-methyl group. The compounds of formula (I) show a strong cytoprotective action on the gastric mucosa by inhibiting the gastric acid secretion and are useful antiulcer agents.
摘要翻译：本发明涉及式（I）的新型四氢吡啶衍生物及其药学上可接受的酸加成盐，含有它们的药物组合物及其制备方法。在式（I）中，R 1表示氢或C 1-6烷基; R2和R3彼此独立地表示氢或C1-6烷基; 或者R2和R3一起表示化学键; R4表示卤素，三氟甲基或C1-6烷基; 当R 2和R 3不一起形成化学键时，R 1和R 3在它们的相互关系中为Z（顺式）或E（反）位，或者R1的含义不同于R 2，条件是R 1和R 2为当R4表示4-甲基时，与氢不同。式（I）化合物通过抑制胃酸分泌显示对胃粘膜的强的细胞保护作用，并且是有用的抗溃疡剂。

7. 发明申请

WO1994014750A1 NOVEL SALICYLIC ACID DERIVATIVES, THEIR SALTS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：新型脂肪酸衍生物及其盐，含有它们的药物组合物及其制备方法
公开(公告)号：WO1994014750A1
公开(公告)日：1994-07-07
申请号：PCT/HU1993000077
申请日：1993-12-17
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , HOFFMAN, György , FISCHER, János , EZER, Elemér , MATUZ, Judit , SAGHY, Katalin , SZPORNY, László , HAJOS, György
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07C69/88
CPC分类号： C07D233/64 , C07C65/40 , C07C69/88 , C07D277/48 , C07D295/205
摘要： There is provided a novel salicylic acid derivative of formula (I), wherein R means hydrogen or a C1-4alkyl group; R stands for hydroxy; a C1-4alkoxy group; or a group of formula (A), wherein R means hydrogen or benzyl group; and R stands for a C1-4alkyl group; or a group of formula (B), wherein R means a C1-4alkyl group, as well as a salt thereof formed with a H2 receptor antagonist, preferably with Cimetidine or Famotidine; and a pharmaceutical composition containing said compound. A process for the preparation of the above compounds and compositions is also described. The compounds of formula (I) and their salts with Famotidine or Cimetidine possess significant gastric acid secretion inhibitory and gastrocytoprotective effects and exert also an antibacterial effect against Helicobacter pylori. Thus, they are useful for the prevention and/or healing of various ulcerous diseases of the oesophagus, stomach and duodenum in a mammal including man.
摘要翻译：提供了式（I）的新型水杨酸衍生物，其中R表示氢或C1-4烷基; R 1代表羟基; C 1-4烷氧基; 或式（A）的基团，其中R 2表示氢或苄基; 和R 3代表C 1-4烷基; 或式（B）的基团，其中R 4表示C 1-4烷基，以及与H 2受体拮抗剂，优选与西咪替丁或法莫替丁形成的盐; 和含有所述化合物的药物组合物。还描述了制备上述化合物和组合物的方法。式（I）化合物及其与法莫替丁或西咪替丁的盐具有显着的胃酸分泌抑制作用和胃细胞保护作用，并对幽门螺杆菌也具有抗菌作用。因此，它们可用于预防和/或愈合包括人在内的哺乳动物的食道，胃和十二指肠的各种溃疡性疾病。

8. 发明申请

WO1991008203A1 NOVEL THIAZOLIDINONE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：新型噻唑烷酮衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：WO1991008203A1
公开(公告)日：1991-06-13
申请号：PCT/HU1990000077
申请日：1990-11-23
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT , SZABADKAI, István , HARSANYI, Kálmán , SZABO, Zsoltné , HEGEDÜS, Béla , EZER, Elemér , MATUZ, Judit , SZPORNY, László , SAGHY, Katalin , HAJOS, György , CSEHI, Attila , BALOGH, Gábor
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT
IPC分类号： C07D277/14
CPC分类号： C07D277/14
摘要： The present invention relates to novel compounds of general formula (I), wherein R means hydrogen or C1-4alkyl group; and Y stands for cyano, trifluoromethyl, aryloxy or aryl(C1-4alkyl)oxy group. The compounds according to the invention show a gastric acid secretion-inhibiting effect and therefore, they are useful for the treatment of gastric and duodenal ulcers. In addition, they exert a cytoprotective action against gastric laesions induced, e.g. by indomethacin or acid-containing alcohol.
摘要翻译：本发明涉及通式（I）的新化合物，其中R表示氢或C 1-4烷基; Y代表氰基，三氟甲基，芳氧基或芳基（C 1-4烷基）氧基。根据本发明的化合物显示出胃酸分泌抑制作用，因此它们可用于治疗胃和十二指肠溃疡。此外，它们对诱导的胃液进行细胞保护作用，例如，通过吲哚美辛或含酸的酒精。

9. 发明申请

WO1994014784A1 NEW THIAZOLIDINONE DERIVATIVES AND A PROCESS FOR THE PREPARATION THEREOF 审中-公开
标题翻译：新的噻唑烷酮衍生物及其制备方法
公开(公告)号：WO1994014784A1
公开(公告)日：1994-07-07
申请号：PCT/HU1993000080
申请日：1993-12-22
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , SZABADKAI, István , HARSANYI, Kálmán , CSALA, Edina , SZANTAY, Csaba , BIHARI, Mária , HEGEDÜS, Béla , EZER, Elemér , MATUZ, Judit , SAGHY, Katalin , SZPORNY, László , HAJOS, György
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07D277/14
CPC分类号： C07D277/14
摘要： The invention relates to new 3-benzyl-2-thiazolidinone derivatives of general formula (I), wherein X represents halogen atom, C1-4-alkyl, nitro or trifluoromethyl group, Y represents halogen atom, C1-4-alkyl, C1-4-alkoxy or trifluoromethyl group, Z represents hydrogen or halogen atom, and to pharmaceutical compositions containing the same, furthermore to processes for the preparation of these derivatives or pharmaceutical compositions containing them. Compounds of general formula (I) are potent inhibitors of gastric acid secretion furthermore exert antiinflammatory activity which is comparable to that of the known indomethacin, thus can be active ingredients of pharmaceutical compositions with significant therapeutic effect serving for the treatment of mammals including humans.
摘要翻译：本发明涉及通式（I）的新的3-苄基-2-噻唑烷酮衍生物，其中X代表卤素原子，C1-4烷基，硝基或三氟甲基，Y代表卤素原子，C1-4烷基，C1- 4-烷氧基或三氟甲基，Z表示氢或卤素原子，以及含有它们的药物组合物，此外用于制备这些衍生物或含有它们的药物组合物的方法。通式（I）的化合物是胃酸分泌的有效抑制剂，进一步具有与已知的吲哚美辛相当的抗炎活性，因此可以是具有显着治疗作用的药物组合物的活性成分，用于治疗包括人的哺乳动物。

10. 发明申请

WO1994014431A1 GASTROCYTOPROTECTIVE PHARMACEUTICAL COMPOSITION AND PROCESS FOR THE PREPARATION THEREOF 审中-公开
标题翻译：胃肠道保护性药物组合物及其制备方法
公开(公告)号：WO1994014431A1
公开(公告)日：1994-07-07
申请号：PCT/HU1993000085
申请日：1993-12-29
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , FISCHER, János , HOFFMANN, György , EZER, Elemér , MATUZ, Judit , SAGHY, Katalin , SZPORNY, László , HAJOS, György
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： A61K31/34
CPC分类号： A61K31/495 , A61K31/60 , A61K31/34 , A61K2300/00
摘要： The present invention relates to a gastrocytoprotective pharmaceutical composition containing as active agents a compound of general formula (I), wherein R means hydrogen or a C1-4alkyl group; R stands for: hydroxyl group; C1-4alkoxy group; or a group of general formula (A), wherein R means hydrogen or benzyl group; and R means a C1-4alkyl group; or stands for a group of general formula (B), wherein R means a C1-4alkyl group, and ranitidine in a weight ratio of 10:1 to 1:10 together with carriers and auxiliaries known per se, and to a process for the preparation thereof. A favourable active agent of general formula (I) is e.g. methyl 4-(3-carboxy-4-hydroxyphenyl)-4-oxo-(2E)-butenoate. The combination of the above active agents according to the invention exerts also an antibacterial effect (against the Helicobacter pylori strain).
摘要翻译：本发明涉及含有通式（I）化合物作为活性剂的胃保护性药物组合物，其中R表示氢或C1-4烷基; R 1代表：羟基; C 1-4烷氧基; 或通式（A）的基团，其中R 2表示氢或苄基; 且R 3表示C 1-4烷基; 或代表一组通式（B），其中R 4表示C 1-4烷基，雷尼替丁与本身已知的载体和辅助剂的重量比为10:1至1:10，并且与其制备方法。通式（I）的有利的活性剂是例如。 4-（3-羧基-4-羟基苯基）-4-氧代 - （2E） - 丁烯酸甲酯。根据本发明的上述活性剂的组合也产生抗菌作用（针对幽门螺杆菌菌株）。

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