公开(公告)号：US3988322A

公开(公告)日：1976-10-26

申请号：US481466

申请日：1974-06-20

申请人： Tibor Kekesy ,  Szabolcs Szeberenyi ,  Gyorgy Beer ,  Antal Dudas ,  Gyorgy Hajos ,  Laszlo Szporny ,  Eva Czajlik nee Csizer

发明人： Tibor Kekesy ,  Szabolcs Szeberenyi ,  Gyorgy Beer ,  Antal Dudas ,  Gyorgy Hajos ,  Laszlo Szporny ,  Eva Czajlik nee Csizer

IPC分类号： C07J31/00 ,  A61K31/585 ,  A61P39/02 ,  C07J21/00

CPC分类号： C07J21/00

摘要： Pharmaceutically active steroids of the formula (I) ##SPC1##whereinX.sub.1 and X.sub.2 each is hydrogen, mercapto or acetylthio andX.sub.3 and X.sub.4 each is hydrogen or acetylthio orX.sub.3 and X.sub.4 form together a valence bond, with the proviso that at least one of X.sub.1 to X.sub.4 is selected from the group consisting of mercapto and acetylthio. The compounds are prepared as follows: a compound of the formula (III) ##SPC2##wherein Z.sub.1 is hydrogen and Z.sub.2 is hydrogen or acetylthio or Z.sub.1 and Z.sub.2 form together a valence bond, is brominated, the thus-obtained compound of the formula ##SPC3##Wherein Y.sub.1 and Y.sub.2 each is hydrogen or bromine, Y.sub.3 is bromine, Y.sub.4 is hydrogen or acetylthio or Y.sub.3 and Y.sub.4 form together a valence bond, is reacted with an alkali methal thioacetate or with an alkali metal hydrosulphide. Thioacetic acid can be coupled onto the obtained product, and/or optionally the obtained thioacetyl compound can be subjected to alcoholysis.The compounds of the formula (I) can be used in the prevention or treatment of poisoning caused by mercury or by other heavy metals.

摘要翻译： 式（I）的药学活性类固醇，其中X 1和X 2各自为氢，巯基或乙酰硫基，X 3和X 4各自为氢或乙酰硫基，或者X 3和X 4一起形成价键，条件是X 1至X 4中的至少一个 选自巯基和乙酰硫基。 化合物如下制备：其中Z 1为氢且Z 2为氢或乙酰硫基或Z 1和Z 2一起形成价键的式（III）化合物被溴化，由此获得的式WHEREIN Y1和Y2的化合物 各自为氢或溴，Y 3为溴，Y 4为氢或乙酰硫基或Y 3和Y 4一起形成价键，与硫代乙酸碱金属或与碱金属硫化氢反应。 硫代乙酸可以偶联到所得产物上，和/或任选得到的硫代乙酰基化合物可以进行醇解。

公开(公告)号：US5157038A

公开(公告)日：1992-10-20

申请号：US566274

申请日：1990-08-10

申请人： Edit Toth ,  Jozsef Torley ,  Bela Hegedus ,  Laszlo Szporny ,  Bela Kiss ,  Eva Palosi ,  Dora Groo ,  Istvan Laszlovszky ,  Erzsebet Lapis ,  Ferenc Auth ,  Laszlo Gaal

发明人： Edit Toth ,  Jozsef Torley ,  Bela Hegedus ,  Laszlo Szporny ,  Bela Kiss ,  Eva Palosi ,  Dora Groo ,  Istvan Laszlovszky ,  Erzsebet Lapis ,  Ferenc Auth ,  Laszlo Gaal

IPC分类号： A61K31/42 ,  A61K31/445 ,  A61K31/4465 ,  A61P3/00 ,  A61P25/00 ,  A61P43/00 ,  C07D211/48 ,  C07D491/10 ,  C07D491/107 ,  C07D491/113 ,  C07D493/10 ,  C07D498/10

CPC分类号： C07D491/10

摘要： The invention relates to novel 2-oxo-1-oxa-8-azaspiro[4,5]decane derivatives of the formula (I), ##STR1## wherein X means oxygen or an >NR group, whereinR stands for hydrogen; a C.sub.1-12 alkyl; C.sub.3-6 cycloalkyl; carbocyclic C.sub.6-10 aryl or carbocyclic C.sub.6-10 aryl-C.sub.1-4 alkyl group, the two latter two substituents optionally substituted on their aromatic moiety by one or more, same or different halogen, one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trihalomethyl group; or a tosyl group;R.sup.1 and R.sup.2 together represent a methylene group or, when X stands for an >NR group wherein R is as defined above, one of R.sup.1 and R.sup.2 m may represent a hydroxyl group and the other one is a methyl group; andR.sup.3 means hydrogen, benzyl, (C.sub.1-4 alkoxy)carbonyl, phenoxycarbonyl, benzyloxycarbonyl, formyl, piperidin-1-ylcarbonyl, morpholin-4-ylcarbonyl, 4-methylpiperazin-1-ylcarbonyl, 4-(2-hydroxethyl)piperazin-1-ylcarbonyl, 2-chloro-3-nicotinoylcarbamoyl or C.sub.1-6 alkylcarbamoyl group,as well as their acid addition and quaternary ammonium salts.

公开(公告)号：US5547949A

公开(公告)日：1996-08-20

申请号：US351448

申请日：1994-12-08

申请人： Sandor Maho ,  Zoltan Tuba ,  Aniko Gere ,  Pal Vittay ,  Bela Kiss ,  Eva Palosi ,  Laszlo Szporny ,  Erzsebet C. Francsicsne ,  Anna M. Boorne ,  Gabor Balogh ,  Sandor Gorog

发明人： Sandor Maho ,  Zoltan Tuba ,  Aniko Gere ,  Pal Vittay ,  Bela Kiss ,  Eva Palosi ,  Laszlo Szporny ,  Erzsebet C. Francsicsne ,  Anna M. Boorne ,  Gabor Balogh ,  Sandor Gorog

IPC分类号： A61K31/57 ,  A61K31/58 ,  A61P3/06 ,  C07D239/42 ,  C07D239/48 ,  C07D239/50 ,  C07D491/10 ,  C07J20060101 ,  C07J9/00 ,  C07J43/00 ,  A61K31/56

CPC分类号： C07D239/42 ,  C07D239/48 ,  C07D239/50 ,  C07D491/10 ,  C07J43/003

摘要： Novel, therapeutically active 21-aminosteroids of formula (I) ##STR1## with pregnane skeleton, are disclosed wherein two of X, Y and Z are a nitrogen atom each and the third one is a methine group; R.sup.1 and R.sup.2 are independently from each other, a primary amino group bearing as substituent a branched-chain C.sub.4-8 alkyl -alkenyl or -alkynyl group, or a C.sub.4-10 cycloalkyl group comprising 1 to 3 ring(s) and being optionally substituted by at least one C.sub.1-3 alkyl group; or R.sup.1 and R.sup.2 are each a spiro-heterocyclic secondary amino group containing at most 10 carbon atoms and optionally at least one oxygen atom as additional heteroatom; or one of R.sup.1 and R.sup.2 is an unsubstituted heterocyclic secondary amino group containing 4 to 7 carbon atoms and the other one is an above-identified primary amino group, an above-identified spiro-heterocyclic secondary amino group, or a heterocyclic secondary amino group containing 4 to 7 carbon atoms and substituted by at least one C.sub.1-4 alkyl group; and n is 1 or 2, as well as their acid addition salts and pharmaceutical compositions containing these compounds.

摘要翻译： PCT No.PCT / HU93 / 00035 Sec。 371日期1994年12月8日第 102（e）日期1994年12月8日PCT提交1993年6月8日PCT公布。 公开号WO93 / 25570 日期：1993年12月23日公开了具有孕烷骨架的式（I）＆lt; IMAGE＆gt;（I）＆lt; IMAGE＆gt;中的新型治疗活性的21-氨基甾体，其中X，Y和Z中的两个各自为氮原子， 次甲基; R1和R2彼此独立地是带有支链C4-8烷基 - 烯基或 - 炔基的取代基的伯氨基或包含1〜3个环的C4-10环烷基，并且任选地被 至少一个C 1-3烷基; 或R 1和R 2各自为含有至多10个碳原子的螺杂环仲氨基和任选的至少一个氧原子作为其它杂原子; R 1和R 2中的一个是含有4至7个碳原子的未取代的杂环仲氨基，另一个是上述的伯氨基，上述的螺杂环仲氨基或含有 4至7个碳原子并被至少一个C 1-4烷基取代; 和n为1或2，以及它们的酸加成盐和含有这些化合物的药物组合物。

公开(公告)号：US5198446A

公开(公告)日：1993-03-30

申请号：US736962

申请日：1991-07-29

申请人： Sandor Farkas ,  Sandor Foldeak ,  Egon Karpati ,  Peter Hegyes ,  Janos Kreidl ,  Laszlo Szporny ,  Laszlo Czibula ,  Szilvia Petofi-Vass

发明人： Sandor Farkas ,  Sandor Foldeak ,  Egon Karpati ,  Peter Hegyes ,  Janos Kreidl ,  Laszlo Szporny ,  Laszlo Czibula ,  Szilvia Petofi-Vass

IPC分类号： A61K31/695 ,  C07F7/08 ,  C07F7/10

CPC分类号： C07F7/0812 ,  C07F7/0818

摘要： A method of treating a mammalian subject for Parkinson's disease or to provide a central muscle relaxant effect, which comprises the step of administering to the mammalian subject in need of the treatment, a therapeutically effective amount of a compound of the Formula (I) ##STR1## wherein m is 1,2 or 3;R.sub.1 and R.sub.2 each independently stand for hydrogen, C.sub.1 to C.sub.4 straight or branched chain alkyl, C.sub.1 to C.sub.4 alkoxy, C.sub.5 to C.sub.7 cycloalkyl, or halogen; andB is a 5- or 6-membered saturated or unsaturated heterocyclic group containing a nitrogen heteroatom, the heterocyclic group being bound through its heterocyclic nitrogen atom to the remainder of the compound, and which can contain one or two additional heteroatoms selected form the group consisting of an oxygen heteroatom, a sulfur heteroatom, and one or two additional nitrogen heteroatoms, which may be as an .dbd.N--, --NH-- or --NR-- group, where R is a C.sub.1 to C.sub.5 alkyl or C.sub.1 to C.sub.5 alkycarbonyl group, the nitrogen-containing heterocyclic group is unsubstituted or substituted on one of its carbon atoms by C.sub.1 to C.sub.4 alkyl or C.sub.1 to C.sub.4 alkoxycarbonyl; or a pharmaceutically acceptable salt thereof.

公开(公告)号：US4859682A

公开(公告)日：1989-08-22

申请号：US40938

申请日：1987-04-21

申请人： Tibor Keve ,  Gabor Megyeri ,  Bela Stefko ,  Lajos Kovacs, Jr. ,  Anna Kassai nee Zieger ,  Bela Kiss ,  Istvan Laszlovszky ,  Erzsebet Lapis ,  Eva Palosi ,  Dora Groo ,  Laszlo Szporny

发明人： Tibor Keve ,  Gabor Megyeri ,  Bela Stefko ,  Lajos Kovacs, Jr. ,  Anna Kassai nee Zieger ,  Bela Kiss ,  Istvan Laszlovszky ,  Erzsebet Lapis ,  Eva Palosi ,  Dora Groo ,  Laszlo Szporny

IPC分类号： A61K31/48 ,  A61P9/00 ,  A61P25/18 ,  C07D457/02

CPC分类号： C07D457/02

摘要： The invention relates to novel 2-halogenated 8- and 1,8-substituted ergolene derivatives of the formula (I) and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the formula (I) ##STR1## wherein X stands for a halogen;R stands for a C.sub.1-4 alkyl group andR" means a hydroxyl group; orR stands for an acyl or substituted acyl group andR" represents a halogen or an --OR' group, whereinR' stands for an acyl or substituted acyl group; orR stands for hydrogen andR" means a halogen or an --OR' group, wherein R' stands for an acyl or substituted acyl group; and the dotted line means a double bond between the 8-9 or 9-10 positions.The compounds of the formula (I) possess an antipsychotic and antihypoxic action and a negligable extrapyramidal side-effect.

摘要翻译： 本发明涉及式（I）的新型2-卤代8-和1,8-取代的麦角烯衍生物及其酸加成盐，含有它们的药物组合物及其制备方法。 在式（I）中，其中X代表卤素; R代表C 1-4烷基，R“表示羟基; 或R表示酰基或取代的酰基，R“表示卤素或-OR'基团，其中R'表示酰基或取代的酰基; 或R表示氢，R“表示卤素或-OR'基团，其中R'表示酰基或取代的酰基; 虚线表示8-9或9-10位之间的双键。 式（I）的化合物具有抗精神病和抗低氧作用和可忽略的锥体束外副作用。

公开(公告)号：US4839362A

公开(公告)日：1989-06-13

申请号：US853844

申请日：1986-04-18

申请人： Janos Kreidl ,  Gyorgy Visky ,  Laszlo Czibula ,  Bela Stefko ,  Maria Farkas nee Kirjak ,  Zsolt Szombathelyi ,  Egon Karpati ,  Bela Kiss ,  Katalin Csomor ,  Laszlo Szporny ,  Lilla Forgacs ,  Csaba Kuthi ,  Aniko Gere

发明人： Janos Kreidl ,  Gyorgy Visky ,  Laszlo Czibula ,  Bela Stefko ,  Maria Farkas nee Kirjak ,  Zsolt Szombathelyi ,  Egon Karpati ,  Bela Kiss ,  Katalin Csomor ,  Laszlo Szporny ,  Lilla Forgacs ,  Csaba Kuthi ,  Aniko Gere

IPC分类号： A61K31/47 ,  A61P9/08 ,  C07D461/00

CPC分类号： C07D461/00

摘要： The invention relates to the preparation of cis and trans stereoisomers of racemic and optically active eburnamenine derivatives of the general formula (Ia) ##STR1## or (Ib), ##STR2## wherein R.sub.1 stands for a C.sub.1-4 alkyl group; andR stands for hydrogen, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, an acyl or substituted acyl group,as well as their acid addition salts, of which the trans compounds are novel.The invention also relates to the compounds of the general formula (IIIa) ##STR3## and (IIIb), ##STR4## wherein R.sub.1 and R' represent a C.sub.1-4 alkyl group. The compounds of the general formulae (Ia) and (Ib) possess a vasodilatory effect which is substantially higher than that of pentoxifyllin, a known peripheral vasodilator.

摘要翻译： 本发明涉及制备通式（Ia），（Ia）或（Ib），（Ⅰb）的外消旋和光学活性依勃他宁衍生物的顺式和反式立体异构体，其中R1代表C1-4 烷基; R代表氢，C1-6烷基，C2-6链烯基，酰基或取代的酰基，以及它们的酸加成盐，其反式化合物是新的。 本发明还涉及通式（IIIa）的化合物（IIIa）和（IIIb），其中R1和R'代表C1-4烷基。 通式（Ia）和（Ib）的化合物具有明显高于已知外周血管扩张剂己酮可可林的血管扩张作用。

公开(公告)号：US4725617A

公开(公告)日：1988-02-16

申请号：US828011

申请日：1986-02-10

申请人： Tamas Fodor ,  Laszlo Dobay ,  Janos Fischer ,  Bela Stefko ,  Bela Kiss ,  Zsolt Szombathelyi ,  Egon Karpati ,  Istvan Laszlovszky ,  Laszlo Szporny

发明人： Tamas Fodor ,  Laszlo Dobay ,  Janos Fischer ,  Bela Stefko ,  Bela Kiss ,  Zsolt Szombathelyi ,  Egon Karpati ,  Istvan Laszlovszky ,  Laszlo Szporny

IPC分类号： C07K14/81 ,  A61K38/00 ,  A61P9/12 ,  A61P27/02 ,  A61P27/06 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  A61K31/395 ,  C07D207/09

CPC分类号： C07K5/0222 ,  A61K38/00 ,  Y02P20/55

摘要： The present invention relates to a compound of the formula (I) ##STR1## wherein R.sup.1 stands for methyl or a group of the formula R.sup.3 --NH--(CH.sub.2).sub.4 --wherein R.sup.3 is hydrogen or a protective group being compatible with the peptide bond,R.sup.2 represents hydrogen, a protective group being compatible with the peptide bond or a cation derived from an organic or inorganic basethe pharmaceutically acceptable salts and diastereomers thereof.The compounds of the invention are useful for inhibiting the effect of the angiotensin converting ensime and they can be used in the therapy as blood pressure reducing agents and for the treatment of cardiac failure and glaucoma.

摘要翻译： 本发明涉及式（I）化合物（I）其中R1代表甲基或式R3-NH-（CH2）4-基团，其中R3是氢或保护基与 肽键，R2表示氢，与肽键相容的保护基或衍生自有机或无机碱的阳离子，其药学上可接受的盐和非对映异构体。 本发明的化合物可用于抑制血管紧张素转化酶的作用，可用于作为降血压剂的治疗和用于治疗心脏衰竭和青光眼。

公开(公告)号：US4681887A

公开(公告)日：1987-07-21

申请号：US877298

申请日：1986-06-23

申请人： Gabor Megyeri ,  Tibor Keve ,  Bela Stefko ,  Erik Bogsch ,  Janos Galambos ,  Anna Kassainee Zieger ,  Ferenc Trischler ,  Eva Palosi ,  Dora Groo ,  Egon Karpati ,  Zsolt Szombathelyi ,  Laszlo Szporny ,  Bela Kiss ,  Istvan Laszlovszky ,  Erzsebet Lapis

发明人： Gabor Megyeri ,  Tibor Keve ,  Bela Stefko ,  Erik Bogsch ,  Janos Galambos ,  Anna Kassainee Zieger ,  Ferenc Trischler ,  Eva Palosi ,  Dora Groo ,  Egon Karpati ,  Zsolt Szombathelyi ,  Laszlo Szporny ,  Bela Kiss ,  Istvan Laszlovszky ,  Erzsebet Lapis

IPC分类号： A61K31/48 ,  A61P25/18 ,  A61P25/20 ,  A61P43/00 ,  C07D457/02 ,  A61K31/44

CPC分类号： A61K31/48 ,  C07D457/02

摘要： The invention relates to pharmaceutical compositions with a neuroleptic action as well as to a process for preparing these compositions.The active ingredients of the compositions of the invention are 2-halo-6-methyl-9-ergolene derivatives of the formula (I), ##STR1## wherein X represents a chlorine, bromine or iodine atom as well as their acid addition salts.The compositions of the invention contain an effective dose of compound of the general formula (I) or an acid addition salt thereof.

摘要翻译： 本发明涉及具有精神抑制作用的药物组合物以及制备这些组合物的方法。 本发明组合物的活性成分是式（I）的2-卤代-6-甲基-9-麦角烯衍生物，其中X代表氯，溴或碘原子，以及它们的酸 加成盐。 本发明的组合物含有有效剂量的通式（I）化合物或其酸加成盐。

公开(公告)号：US4645774A

公开(公告)日：1987-02-24

申请号：US803792

申请日：1985-12-02

申请人： Edit Toth ,  Jozsef Torley ,  Eva Palosi ,  Szabolcs Szeberenyi ,  Laszlo Szporny ,  Sandor Gorog ,  Istvan Hajdu

发明人： Edit Toth ,  Jozsef Torley ,  Eva Palosi ,  Szabolcs Szeberenyi ,  Laszlo Szporny ,  Sandor Gorog ,  Istvan Hajdu

IPC分类号： A61K31/135 ,  A61K31/40 ,  A61K31/445 ,  A61K31/535 ,  A61K31/5375 ,  A61P43/00 ,  C07C67/00 ,  C07C213/00 ,  C07C217/18 ,  C07D207/20 ,  C07D295/08 ,  C07D295/092 ,  C12N9/02

CPC分类号： C07D295/088

摘要： The invention relates to new aminoethoxybenzylalcohol derivatives of the formula (I) ##STR1## wherein R.sub.1 is hydrogen, halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms;R.sub.2 is halogen, trihalomethyl, or alkoxy having from one to 4 carbon atoms;R.sub.3 and R.sub.4 stand for methyl or together with the adjacent nitrogen form an up to 8-membered ring optionally containing oxygen,and acid addition or quaternary ammonium salts thereof.The compounds of formula (I) are pharmacologically active, thus show enzyme-inducing effect. The pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.

摘要翻译： 本发明涉及式（I）的新的氨基乙氧基苄醇衍生物：其中R 1是氢，卤素，三卤代甲基，具有1至4个碳原子的烷基或具有1至4个碳原子的烷氧基; R2是卤素，三卤甲基或具有1至4个碳原子的烷氧基; R3和R4代表甲基或与相邻的氮一起形成任选含有氧的至多8元环，及其酸加成或季铵盐。 式（I）化合物具有药理活性，因此显示出酶诱导作用。 含有它们作为活性成分的药物组合物也在本发明的范围内。

公开(公告)号：US4618611A

公开(公告)日：1986-10-21

申请号：US565901

申请日：1983-12-27

申请人： Edit Toth ,  Jozsef Torley ,  Gyorgy Fekete ,  Laszlo Szporny ,  Laszlo Vereczkey ,  Eva Palosi ,  Imre Klebovich ,  Pal Vittay ,  Sandor Gorog ,  Istvan Hajdu

发明人： Edit Toth ,  Jozsef Torley ,  Gyorgy Fekete ,  Laszlo Szporny ,  Laszlo Vereczkey ,  Eva Palosi ,  Imre Klebovich ,  Pal Vittay ,  Sandor Gorog ,  Istvan Hajdu

IPC分类号： A61K31/135 ,  A61K31/415 ,  A61K31/495 ,  A61K31/53 ,  A61P25/30 ,  C07C67/00 ,  C07C213/00 ,  C07C217/18 ,  C07D233/60 ,  C07D295/08 ,  C07D295/092 ,  C07C149/32 ,  C07D295/02

CPC分类号： C07D295/088

摘要： The invention relates to new aminopropanol derivatives of the formula (I) ##STR1## wherein R.sub.1 is halogen, trihalomethyl, alkoxy having from one to 3 carbon atoms or alkyl having from one to 3 carbon atoms,R.sub.2 is alkyl having from one to 3 carbon atoms, andR.sub.3 is cycloalkyl having from 3 to 6 carbon atoms, orR.sub.2 and R.sub.3 together with the nitrogen they are attached to form an up to 8 membered ring optionally containing oxygen or a further nitrogen as an additional hetero atom, and optionally substituted with alkyl having from one to 4 carbon atoms or benzyl,and acid addition and quaternary ammonium salts thereof.According to another aspect of the invention there are provided processes for the preparation of these compounds.The new compounds are suitable for the treatment of acute ethanolic intoxication. Pharmaceutical compositions containing them are also within the scope of the invention.

摘要翻译： 本发明涉及式（I）的新的氨基丙醇衍生物其中R 1为卤素，三卤代甲基，具有1至3个碳原子的烷氧基或具有1至3个碳原子的烷基，R 2为具有一个 3个碳原子，R3是具有3至6个碳原子的环烷基，或者R 2和R 3与它们连接的氮一起形成任选含有氧或另外的氮作为另外的杂原子的至多8元环，以及 任选被具有1至4个碳原子的烷基取代或苄基，及其酸加成盐和季铵盐。 根据本发明的另一方面，提供了这些化合物的制备方法。 新化合物适用于急性乙醇中毒治疗。 含有它们的药物组合物也在本发明的范围内。