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1. 发明授权

US4419359A Nitro-substituted polycyclic derivatives useful in the treatment of psoriasis 失效
标题翻译：用于治疗牛皮癣的硝基取代多环衍生物
公开(公告)号：US4419359A
公开(公告)日：1983-12-06
申请号：US345631
申请日：1982-02-04
申请人： Tibor Keve , Gyorgy Fekete , Csaba Lorincz , Janos Galambos , Bela Zsadon , Maria Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
发明人： Tibor Keve , Gyorgy Fekete , Csaba Lorincz , Janos Galambos , Bela Zsadon , Maria Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
IPC分类号： C07D461/00 , A61K31/435
CPC分类号： C07D461/00 , Y10S514/863
摘要： The present invention relates to the compounds of the Formulae 1a and 1b and pharmaceutically acceptable acid addition salts thereof.The new 9-nitro-apovincaminol-3',4',5'-trimethoxybenzoate of the Formula 1a ##STR1## and the 11-nitro-apovincaminol-3',4',5'-trimethoxy-benzoate of the Formula 1b ##STR2## and pharmaceutically acceptable acid addition salts thereof can be prepared by nitrating the apovincaminol-3',4',5'-trimethoxy-benzoate of the Formula 11, ##STR3## if desired separating the mixture of the compounds of the Formulae 1a and 1b thus obtained into its components, if desired converting a compound of the Formula 1a or 1b thus obtained into pharmaceutically acceptable acid addition salts thereof.The new compounds of the present invention can be used in therapy in the treatment of psoriasis.
摘要翻译：本发明涉及式1a和1b的化合物及其药学上可接受的酸加成盐。式1b的新的9-硝基 - 亚氨基胺醇-3'，4'，5'-三甲氧基苯甲酸酯和式1b的11-硝基 - 亚氨基胺醇-3'，4'，5'-三甲氧基 - 苯甲酸酯< IMAGE>及其药学上可接受的酸加成盐可以通过将式11的亚氨基胺醇-3'，4'，5'-三甲氧基 - 苯甲酸酯硝化，如果需要，将式1a的化合物和 1b，如果需要，将由此获得的式1a或1b的化合物转化为其药学上可接受的酸加成盐。本发明的新化合物可用于治疗牛皮癣的治疗。

2. 发明授权

US4424223A Polycyclic compounds containing a double bond in the D-ring pharmaceutical compositions containing them, and methods of treating psoriasis with them 失效
标题翻译：在含有它们的D环药物组合物中含有双键的多环化合物，以及用它们治疗牛皮癣的方法
公开(公告)号：US4424223A
公开(公告)日：1984-01-03
申请号：US345630
申请日：1982-02-04
申请人： Tibor Keve , Bela Zsadon , Gyorgy Fekete , Csaba Lorincz , Janos Galambos , Maria Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
发明人： Tibor Keve , Bela Zsadon , Gyorgy Fekete , Csaba Lorincz , Janos Galambos , Maria Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
IPC分类号： A61K31/435 , A61K31/475 , A61P17/00 , A61P17/16 , A61P43/00 , C07D461/00
CPC分类号： C07D461/00 , Y10S514/863
摘要： The invention relates to the new 17,18-dehydro-apovincaminol-3',4',5'-trimethoxy-benzoate of formula (I) ##STR1## and acid addition salts thereof. According to another aspect of the invention there is provided a process for the preparation of these new compounds. Still another aspect of the invention is a pharmaceutical composition for treating psoriasis.
摘要翻译：本发明涉及式（I）的新的17,18-脱氢阿朴氨酚-3'，4'，5'-三甲氧基 - 苯甲酸酯及其酸加成盐。根据本发明的另一方面，提供了制备这些新化合物的方法。本发明的另一方面是用于治疗牛皮癣的药物组合物。

3. 发明授权

US4680397A Apovincaminol derivative 失效
标题翻译：亚氨基酚衍生物
公开(公告)号：US4680397A
公开(公告)日：1987-07-14
申请号：US727130
申请日：1985-04-25
申请人： Tibor Keve , Bela Zsadon , Gyorgy Fekete , Janos Galambos , Margit Barta nee Bukovecz , Laszlo Szporny , Lilla Forgacs , Arpad Kiraly , Gyongyver Soos , Bela Kiss , Maria Zajer nee Balazs
发明人： Tibor Keve , Bela Zsadon , Gyorgy Fekete , Janos Galambos , Margit Barta nee Bukovecz , Laszlo Szporny , Lilla Forgacs , Arpad Kiraly , Gyongyver Soos , Bela Kiss , Maria Zajer nee Balazs
IPC分类号： A61K31/475 , A61P17/00 , A61P43/00 , C07D461/00
CPC分类号： C07D461/00
摘要： The invention relates to new apovincaminol derivatives of the formula /I/ ##STR1## wherein R.sub.1 is hydrogen, nitro or halogen,R.sub.2 is a substituted or unsubstituted alkyl or phenyl group,R.sub.3 and R.sub.4 together form a valency bond or each independently represents hydrogen, hydroxyl or an --OR.sub.5 group, in whichR.sub.5 is substituted or unsubstituted alkanoyl or benzoyl group,with the proviso that if R.sub.2 stands for a 3,4,5-trimethoxyphenyl group and R.sub.1 is hydrogen, R.sub.3 and R.sub.4 together do not form a valency bond, or if R.sub.2 is a 3,4,5-trimethoxyphenyl group and R.sub.3 and R.sub.4 both are hydrogen, R.sub.1 is other than hydrogen, nitro or bromine, and acid addition salts thereof.The compounds may be used in the therapy of various skin diseases accompanied by a pathological cell proliferation, preferably psoriasis.
摘要翻译：本发明涉及式I /（I）的新的氨基嘌呤醇衍生物，其中R1是氢，硝基或卤素，R2是取代或未取代的烷基或苯基，R3和R4一起形成价键或各自独立地表示氢，羟基或-OR 5基团，其中R 5为取代或未取代的烷酰基或苯甲酰基，条件是如果R 2表示3,4,5-三甲氧基苯基且R 1为氢，则R 3和R 4一起不为形成价键，或者如果R2是3,4,5-三甲氧基苯基，且R3和R4都是氢，R1不是氢，硝基或溴，以及其酸加成盐。该化合物可用于治疗伴随病理细胞增殖的各种皮肤疾病，优选牛皮癣。

4. 发明授权

US5204355A 15-nitro-2.beta., 3.beta.-dihydro- and 15-nitro-2.beta.,3.beta.,6,7-tetrahydrotabersonine derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译： 15-NITRO-2 + 62,3（BETA）-DIHYDRO-和15-NITRO-2（BETA），3（BETA），6,7-四氢异喹啉衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US5204355A
公开(公告)日：1993-04-20
申请号：US806975
申请日：1991-12-12
申请人： Bela Zsadon , Margit Barta n/e/ e Bukovecz , Maria Szilasi , Tibor Keve , Janos Galambos , Viktoria Bolya nee Kassay , Sandor Szabo , Emilia Repasi, nee Balogh , Laszlo Szporny , Bela Kiss , Egon Karpati , Eva Palosi , Zsolt Szombathelyi , Adam Sarkadi , Erzsebet Lapis , Aniko Gere , Mih,acu/a/ ly Bodo , Katalin Csomor , Judit Laszy , Zsolt Szentirmay
发明人： Bela Zsadon , Margit Barta n/e/ e Bukovecz , Maria Szilasi , Tibor Keve , Janos Galambos , Viktoria Bolya nee Kassay , Sandor Szabo , Emilia Repasi, nee Balogh , Laszlo Szporny , Bela Kiss , Egon Karpati , Eva Palosi , Zsolt Szombathelyi , Adam Sarkadi , Erzsebet Lapis , Aniko Gere , Mih,acu/a/ ly Bodo , Katalin Csomor , Judit Laszy , Zsolt Szentirmay
IPC分类号： A61K31/435 , A61P25/28 , A61P43/00 , C07D471/16 , C07D471/20
CPC分类号： C07D471/20
摘要： The invention relates to novel 15-nitro-2.beta.,3.beta.-dihydro- and 15-nitro-2.beta.,3.beta.,6,7-tetrahydrotabersonine derivatives of the formula (I), ##STR1## wherein R.sup.1 stands for hydrogen;R.sup.2 stands for hydrogen or a C.sub.1-6 alkyl group; and the symbol represents a single or double bond as well as their salts.The invention further relates to pharmaceutical compositions containing the above compounds as well as a process for the preparation of the above compounds of formula (I) and of the pharmaceutical compositions.The compounds of formula (I) exert a reducing or inhibitory effect on cerebral edema and show antihypoxic properties. Thus, they are useful for the prevention or treatment of brain injuries of various origin induced by hypoxia of the brain.

5. 发明授权

US4758666A Process for the preparation of an apovincaminol derivative 失效
标题翻译：阿朴菌素衍生物的制备方法
公开(公告)号：US4758666A
公开(公告)日：1988-07-19
申请号：US861550
申请日：1986-05-09
申请人： Janos Galambos , Tibor Keve , Bela Stefko , Gyorgy Fekete , Bela Zsadon , Anna Kassai nee Zieger , Klara Horvath nee Otta
发明人： Janos Galambos , Tibor Keve , Bela Stefko , Gyorgy Fekete , Bela Zsadon , Anna Kassai nee Zieger , Klara Horvath nee Otta
IPC分类号： C07D461/00
CPC分类号： C07D461/00
摘要： The invention relates to a new process for the preparation of 17,18-dehydro-apovincaminol-trimethoxy-benzoate of the formula (I) ##STR1## and acid addition salts thereof. According to the invention compound of the formula (I) is prepared starting from 17,18-dehydrovincamine of the formula (IIa) ##STR2## and/or 17,18-dehydro-epivincamine of formula (IIb) ##STR3## by reducing with a complex metal hydride, acylating the new hydroxy-vincaminol derivative obtained selectively with 3,4,5-trimethoxy-benzoic acid or a derivative thereof capable of acylation, optionally in the presence of a catalyst and/or an acid binding agent, and treating the corresponding acylated hydroxylderivative obtained with formic acid, in the presence of an acid chloride, and, if desired, converting the compound of formula (I) obtained into an acid addition salt thereof.
摘要翻译：本发明涉及一种制备式（I）所示的17,18-脱氢 - 氨基亚氨基三醇 - 苯甲酸酯（I）的新方法及其酸加成盐。根据本发明，式（I）化合物是从式（IIa）（IIa）的17,18-脱氢丁胺和/或式（IIb）的17,18-脱氢 - 亚氨基胺开始制备的。（IIb），通过用复合金属氢化物还原，任选地在催化剂和/或催化剂存在下酰化用3,4,5-三甲氧基 - 苯甲酸或其能够酰化的衍生物选择性地得到的新的羟基 - 长春花母醇衍生物并且在酰氯存在下处理由甲酸获得的相应的酰化羟基衍生物，如果需要，将得到的式（I）化合物转化为其酸加成盐。

6. 发明授权

US4357468A Sorbents of cellulose basis capable of forming inclusion complexes and a process for the preparation thereof 失效
标题翻译：能够形成包合物的纤维素基质的吸附剂及其制备方法
公开(公告)号：US4357468A
公开(公告)日：1982-11-02
申请号：US288764
申请日：1981-07-31
申请人： Jozsef Szejtli , Bela Zsadon , Eva Fenyvesi , nee Otta; Klara Horvath , Ferenc Tudos
发明人： Jozsef Szejtli , Bela Zsadon , Eva Fenyvesi , nee Otta; Klara Horvath , Ferenc Tudos
IPC分类号： C08L1/00 , C08B11/08 , C08B15/00 , C08B37/16
CPC分类号： C08B37/0012 , C08B11/08
摘要： The invention relates to new sorbents of cellulose basis capable of forming inclusion complexes, as well as to a process for the preparation thereof. The new sorbents according to the invention are cellulose derivatives containing structural units of the general formula (I), ##STR1## wherein Cell is a group derived by removing m hydroxy groups from the glucose unit of the cellulose chain,m is an integer of 1 to 3,CD is a group derived by removing one hydroxy group from the .alpha., .beta. or .gamma.-cyclodextrin molecule,n is an integer of 1 to 5, andp stands for 0 or 1, which may optionally vary even within a single chain.The cellulose derivatives according to the invention are substances of loose structure, with large specific surface area and good swelling properties, which can be applied for solving the most diverse adsorption tasks. Thus e.g. the substances can be applied for the preparation of smoke filters in cigarettes, waste water purification (de-poisoning) filters, inserts for removing solvent vapors, etc., furthermore for solving specific tasks of fractionation according to molecular dimensions.
摘要翻译：本发明涉及能够形成包合络合物的新型纤维素基质吸附剂，以及其制备方法。根据本发明的新吸附剂是含有通式（I），Cell {[OCH 2（CHOH）pCH 2] nOCD} m（I）的结构单元的纤维素衍生物，其中Cell是从葡萄糖中除去m个羟基衍生的基团纤维素链的单位，m为1〜3的整数，CD为从α，β或γ-环糊精分子除去一个羟基衍生的基团，n为1〜5的整数，p为0 或1，其可以任选地在单链内变化。根据本发明的纤维素衍生物是松散结构的物质，具有大的比表面积和良好的溶胀性能，可用于解决最多样化的吸附任务。因此，例如该物质可用于制备香烟中的烟雾过滤器，废水净化（去中毒）过滤器，用于除去溶剂蒸气的插入物等，此外用于根据分子尺寸解决特定的分馏任务。

7. 发明授权

US4547572A Cyclodextrin polymers swelling quickly and to a great extent in water and process for the preparation thereof 失效
标题翻译：环糊精聚合物在水中迅速膨胀并在很大程度上膨胀并且用于其制备
公开(公告)号：US4547572A
公开(公告)日：1985-10-15
申请号：US577153
申请日：1984-02-06
申请人： Eva Fenyvesi , Jozsef Szejtli , Bela Zsadon , Balazs Antal , Ildiko Wagner nee Kohary
发明人： Eva Fenyvesi , Jozsef Szejtli , Bela Zsadon , Balazs Antal , Ildiko Wagner nee Kohary
IPC分类号： C08L5/00 , A61K9/20 , A61K47/40 , C08B37/16 , C08G59/00 , C08G59/02
CPC分类号： C08B37/0012 , A61K9/205
摘要： The invention relates to cyclodextrin polymers swelling quickly and to a great extent in water and a process for the preparation thereof.The cyclodextrin polymers according to the invention contain as additive n-octanol having or glycol derivative or glycerol.The cyclodextrin polymers according to the invention are prepared by reacting cyclodextrin and epichlorohydrin in aqueous alkaline medium. In the reaction the cyclodextrin is reacted with 10 to 20 moles of an alkali hydroxide, 10 to 20 moles of epichlorohydrin and 2 to 8 moles of an alcohol additive, n-octanol, glycol derivative or glycerol calculated on 1 mole of cyclodextrin optionally in the presence of 10 to 15 moles of an organic solvent vaporizing at the reaction temperature or 8 to 12 moles of a high boiling organic solvent assuring heterogeneous phase.
摘要翻译：本发明涉及在水中快速且很大程度地溶胀的环糊精聚合物及其制备方法。根据本发明的环糊精聚合物含有具有或二醇衍生物或甘油的添加剂正辛醇。根据本发明的环糊精聚合物通过环糊精和表氯醇在碱性水溶液中反应来制备。在反应中，环糊精与10至20摩尔碱金属氢氧化物，10至20摩尔表氯醇和2至8摩尔醇添加剂，正辛醇，乙二醇衍生物或甘油按1摩尔环糊精计算，任选地在存在10至15摩尔在反应温度下蒸发的有机溶剂或8至12摩尔的高沸点有机溶剂以确保异相。

8. 发明授权

US4274985A Cyclodextrin-polyvinyl alcohol polymers and a process for the preparation thereof in a pearl, foil, fiber or block form 失效
标题翻译：环糊精 - 聚乙烯醇聚合物及其以珍珠，箔，纤维或块形式制备的方法
公开(公告)号：US4274985A
公开(公告)日：1981-06-23
申请号：US55536
申请日：1979-07-09
申请人： Jozsef Szejtli , Eva Fenyvesi , Sandor Zoltan , Bela Zsadon , Ferenc Tudos
发明人： Jozsef Szejtli , Eva Fenyvesi , Sandor Zoltan , Bela Zsadon , Ferenc Tudos
IPC分类号： C08F8/00 , C08B37/16 , C08L5/16 , C08L29/00 , C08L29/04
CPC分类号： C08B37/0012 , C08L5/16
摘要： The present invention concerns new cyclodextrin-polyvinyl alcohol polymers capable of forming inclusion complexes. The preparation of said polymers by cross-linking a cyclodextrin, a mixture of cyclodextrins, or carbohydrate mixtures containing cyclodextrins in the presence of polyvinyl alcohol, polyvinyl acetate or a polyvinyl alcohol-polyvinyl acetate copolymer, with a polyfunctional coupling reactant capable of reacting with the cyclodextrins and with the polymers present is also within the scope of the invention.
摘要翻译：本发明涉及能形成包合物的新的环糊精 - 聚乙烯醇聚合物。在聚乙烯醇，聚乙酸乙烯酯或聚乙烯醇 - 聚乙酸乙烯酯共聚物存在下，通过交联环糊精，环糊精混合物或含有环糊精的碳水化合物混合物与能与其反应的多官能偶联反应物来制备所述聚合物环糊精和存在的聚合物也在本发明的范围内。

9. 发明授权

US4535152A Water soluble cyclodextrin polymers substituted by ionic groups and process for the preparation thereof 失效
标题翻译：由离子基团取代的水溶性环糊精聚合物及其制备方法
公开(公告)号：US4535152A
公开(公告)日：1985-08-13
申请号：US580098
申请日：1984-02-14
申请人： Jozsef Szejtli , Eva Fenyvesi , Bela Zsadon , Maria Szilasi , Lajos Decsei
发明人： Jozsef Szejtli , Eva Fenyvesi , Bela Zsadon , Maria Szilasi , Lajos Decsei
IPC分类号： C08G59/00 , C08B37/16 , C08G59/14 , C08G65/28 , C08G65/32
CPC分类号： C08B37/0012
摘要： The invention relates to water soluble cyclodextrin polymers substituted by ionic groups, containing structural units of formula (I) ##STR1##
摘要翻译：本发明涉及由离子基团取代的含有式（I）的结构单元的水溶性环糊精聚合物。

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