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公开(公告)号：EP0178176A3
公开(公告)日：1988-03-23
申请号：EP85307264
申请日：1985-10-10
发明人： Vezert, Csilla , Tegyey, Zsuzsanna , Cholnoky, Eszter , Urogdi, Laszlo , Tudos, Helga , Szporny, Laszlo , Kisfaludy, Lajos , Palosi, Eva , Otvos, Laszlo , Ronai, Sara
IPC分类号： C07D273/04 , A61K31/535 , C07C153/057
CPC分类号： C07D273/04
摘要： 57 The present invention relates to optically active or racemic tetrahydro-1,2,4-oxadiazine-5-thione derivatives, to methods for their preparation, and pharmaceutical compositions containing the said compounds. Methods for the anticonvulsive treatment of mammals, especially human beings are described. The compounds of the formula I have similar activity to diphenyl hydantoin but their toxicity is much lower.
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2.发明公开
公开(公告)号：EP0387091A3
公开(公告)日：1992-05-06
申请号：EP90302544.3
申请日：1990-03-09
发明人： Molnar, Csaba , Hajos, Gyorgy , Szporny, Laszlo , Toth, Jozsef , Kiraly, Arpad , Boor, nee Mezei, Anna , Csorgei, Janos , Szekely, Krisztina , Forgacs, Lilla , Fekete, Gyorgy , Herenyi, Bulcsu , Holly, Sandor , Szunyog, Jozsef
CPC分类号： C07J5/0092 , C07J13/005
摘要： The invention relates to Δ¹⁴-16α,17-dihydroxypregnane derivatives of general formula (I),
wherein
A represents a hydrogen atom, or hydroxyl or trifluoroacetoxy group;
X represents a hydrogen or halogen atom with the proviso that
if A is a hydrogen atom, X is also a hydrogen atom;
R represents a hydrogen atom, a benzoyl or C₁₋₈ alkanoyl group;
and --- represents a single or double bond between the two adjacent carbon atoms,
as well as pharmaceutical compositions containing these compounds and a process for their preparation. The compounds of general formula (I) possess valuable antiinflammatory effects and thus may be used as active ingredients in antiinflammatory pharmaceutical compositions. They may also be useful in the preparation of other therapeutically useful steroid derivatives.-
公开(公告)号：EP0178176B1
公开(公告)日：1992-01-02
申请号：EP85307264.3
申请日：1985-10-10
申请人： RICHTER GEDEON VEGYESZETI GYAR R.T. , Magyar Tudomanyos Akadémia Központi Kémiai Kutato Intézete
发明人： Vezert, Csilla , Tegyey, Zsuzsanna , Cholnoky, Eszter , Urogdi, Laszlo , Tudos, Helga , Szporny, Laszlo , Kisfaludy, Lajos , Palosi, Eva , Otvos, Laszlo , Ronai, Sara
IPC分类号： C07D273/04 , A61K31/535 , C07C327/42
CPC分类号： C07D273/04
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4.发明公开Novel acrylic amide derivatives, a process for their preparation, pharmaceutical compositions containing the same and their use in medicine 失效新型丙烯酰胺衍生物，其制备方法，含有该组合物的药物组合物及其在医药中的应用
公开(公告)号：EP0408106A3
公开(公告)日：1991-04-24
申请号：EP90201742.5
申请日：1990-06-29
发明人： Fodor, Tamas , Fischer, Janos , Dobay, Laszlo , Ezer, Elemér , Matuz, Judit , Saghy, Katalin , Szporny, Laszlo , Hajos, György
IPC分类号： C07C323/60 , C07C317/24 , A61K31/10 , C07C315/04 , C07C319/20 , C07D295/18 , C07D277/06
CPC分类号： C07D295/185 , C07C317/44 , C07C323/54 , C07D207/16
摘要： Novel acrylic amide derivative of the formula
wherein
R¹ represents a hydrogen or a halogen atom or a C₁₋₄alkyl, a C₁₋₄alkoxy or a nitro group.
n is an integer of 0 to 2,
A represents an amino acid residue derived from a naturally occuring amino acid or an antipode thereof which is connected to the acrylic acyl residue through its amino group; or a residue derived from thiazolidinecarboxylic acid connected to the acrylic acyl group through its nitrogen, or a derivative of the above residues wherein any free carboxy group is esterified with a C₁₋₄alkyl group or is amidated; or A represents a group of formula
wherein
R₂ is a hydrogen atom or a phenyl, a C₁₋₄alkyl or a C₁₋₄alkoxycarbonyl group,
and their salts which have interesting cytoprotective and antiulcer activities are provided. A process is also described for the preparation of said compounds.-
5.发明公开Octahydroindolo-[2,3-a]quinolizin-l-yl-alkanecarboxylic acid amides and salts thereof 失效八氢吲哚-2-磺酸盐-1-基 - 烷烃 - 羧基酰胺和硫酸盐
公开(公告)号：EP0177361A2
公开(公告)日：1986-04-09
申请号：EP85307113.2
申请日：1985-10-04
发明人： Soti, Ferenc , Szantay, Csaba , Incze, Maria , Balogh, Zsuzsanna , Ezer, Elemer , Matuz, Judit , Szporny, Laszlo , Hajos, Gyorgy , Kuthi, Csaba
IPC分类号： C07D471/14 , A61K31/395
CPC分类号： C07D471/14
摘要： The invention relates to new 1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]quinolizin-1-yl-alkanecarboxylic acid amides of the general formula (I),
wherein
R, and R 2 represent a hydrogen or halogen atom, or a hydroxyl, nitro or C 1-4 alkoxy group;
R 3 and R 4 represent a hydrogen atom or a C 1-4 alkyl group;
R 5 and R 6 represent a hydrogen atom, C 1-8 alkyl group, C 3-8 alkenyl or cycloalkyl group, aryl or aralkyl group, heteroaryl or heteroaralkyl goup containing oxygen, nitrogen or sulphur atom, all these goups being optionally substituted; or
R 5 and R 6 together represent a,w-alkyl group, wherein one carbon atom may optionally be replaced by an oxygen or nitrogen atom; and
G means a C 1-4 straight chained alkylidene group, as well as to their therapeutically useful acid addition salts and pharmaceutical compositions containing these compounds.
Furthermore, the invention relates to a process for preparing these compounds and compositions.
The compounds of the general formula (I) have valuable therapeutic properties, namely vasodilatory, spasmolytic, antiarrhythmic and gastrocytoprotective effects. The gastrocytoprotective effect is particularly important.-
6.发明授权Butenoic acid amides, their salts, pharmaceutical compositions containing them and process for preparing same 失效丁烯酸酰胺，其盐，含有它们的它们的制备方法的药物组合物。
公开(公告)号：EP0309261B1
公开(公告)日：1994-02-02
申请号：EP88308831.2
申请日：1988-09-23
发明人： Fodor, Tamas , Dobay, Laszlo , Fischer, Janos , Stefko, Bela , Ezer, Elemer , Saghy, Katalin , Szporny, Laszlo , Matuz, Judit
IPC分类号： C07C233/01 , A61K31/195
CPC分类号： A61K31/195 , C07C233/12 , Y02P20/55
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7.发明公开
公开(公告)号：EP0387090A3
公开(公告)日：1992-05-06
申请号：EP90302543.5
申请日：1990-03-09
发明人： Molnar, Csaba , Hajos, Gyorgy , Szporny, Laszlo , Toth, Jozsef , Kiraly, Arpad , Boor nee Mezei, Arma , Csorgei, Janos , Szekely, Krisztina , Forgacs, Lilla , Fekete, Gyorgy , Herenyi, of Bulcsu , Holly, Sandor , Szunyog, Jozef
CPC分类号： C07J71/0031 , C07J7/008
摘要： The invention relates to novel Δ¹⁴-16α,17-dihydroxy-pregnane-16,17-cyclic aldehyde acetal and -cyclic ketone ketal derivatives of general formula (I),
wherein
A stands for hydrogen or hydroxyl group;
X stands for hydrogen or halogen with the proviso that if A is hydrogen, then X also means hydrogen;
R stands for hydrogen,benzoyl or C₁ ⁻ ₈alkanoyl group;
R¹ and R², which are the same or different, stand for hydrogen or a C₁ ⁻ ₄alkyl group; or one of R¹ and R² is hydrogen and the other is phenyl group; or R¹ and R² together form a C₄ ⁻ ₅alkylene group; --- means a single or double bond between two adjacent carbon atoms,
as well as pharmaceutical compositions containing these compounds and a process for their preparation. The compounds of general formula (I) possess a very strong antiinflammatory effect and only week harmful side effect. Thus, they can be used as active ingredients of antiinflammatory pharmaceutical compositions being useful in the therapy.-
公开(公告)号：EP0240338B1
公开(公告)日：1990-07-04
申请号：EP87302841.9
申请日：1987-04-01
发明人： Fischer, Janos , Ezer, Elemer , Szporny, Laszlo , Dobay, Laszlo , Matuz, Judit , Wagner, Tibor
IPC分类号： C07C69/738 , C07C67/00 , A61K31/215
CPC分类号： A61K31/215 , C07C69/00 , C07C69/738
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9.发明公开Novel salicylates, their salts, pharmaceutical compositions containing them and process for preparing same 失效水杨酸酯，它们的盐，含有它们和它们的制备方法的药物组合物。
公开(公告)号：EP0309262A2
公开(公告)日：1989-03-29
申请号：EP88308832.0
申请日：1988-09-23
发明人： Fischer Janos , Dobay, Laszlo , Major, Mihaly , Ezer, Elemer , Matuz, Judit , Saghy, Katalin , Hajos, Gyorgy , Szporny, Laszlo
CPC分类号： C07C69/738 , Y02P20/55
摘要： Compounds of the general formula (I),
wherein
R is hydrogen, halogen, C₁₋₄alkyl, C₁₋₄alkoxy or a C₁₋₄acylamino group; and
R₁ is hydrogen or a carboxyl-protective group, in the E and/or Z configuration, as well as their salts, show both a cytoprotective effect and anti-inflammatory action. Their toxicity is low.摘要翻译： 通式（I）
的化合物worin R是氢，卤素，C 1-4烷基，C 1-4烷氧基或一个C1-4acylamino基; 且R 1为氢或羧基保护基，在E和/或Z构型，以及它们的盐，同时显示一个细胞保护作用和抗炎症作用。 其毒性低。 -
公开(公告)号：EP0179662A3
公开(公告)日：1987-01-14
申请号：EP85307686
申请日：1985-10-24
发明人： Perjes, Istvan , Selmeczi, Andras , Klebovich, Imre , Hajos, Gyorgy , Simon, Ferenc , Misley, Atilla , Szporny, Laszlo , Vereczkey, Laszlo , Toth, Edit , Torley, Jozsef , Sarkozy, Peter
IPC分类号： A23K01/16
CPC分类号： A23K50/30 , A23K20/111
摘要： The invention relates to fodder additives comprising a compound inducing the microsomal enzyme system of the liver, such as a compound of the formula (I) wherein
R i , R 2 and R 3 which may be the same or different represent hydrogen, halogen, trihalomethyl, or alkyl or alkoxy group each containing from 1 to 6 carbon atoms; R 4 is phenyl, dialkylaminocarbonyl or alkoxycarbonyl having from 1 to 6 carbon atoms in the alkyl and alkoxy moieties, respectively; R 5 is hydrogen or methyl, or together with R 4 and the nitrogen atom to which they are attached forms a heterocyclic ring having up to 8 members; n is an integer 1, 2, 3, 4 or 5; m is 0 or 1; a is 0 or 1,
with the proviso that if a = 0, R 1 is trihalomethyl and R 2 and R 3 both are hydrogen. The compounds are preferably used in amount of 0.5 to 99% by weight, in admixture with a conventional carrier and/or additive and optionally at least one further active ingredient conventionally used in the animal husbandry. The enzyme-inducing compounds used according to the invention accelerate the elimination of various xenobiotics metabolizing in the iiver.
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