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1. 发明授权

US4429129A 1.alpha.-Ethyl-1.beta.-(2'-alkoxy carbonyl-2'-hydroxyiminoethyl)-10-methoxy 1,2,3,4,6,7,12,12.beta.-octahydroindolo(2,3A)quinolizines 失效
标题翻译： 1α-乙基-1β-（2'-烷氧基羰基-2'-羟基亚氨基乙基）-10-甲氧基1,2,3,4,6,7,12,12β-八氢吲哚（2,3A）喹嗪
公开(公告)号：US4429129A
公开(公告)日：1984-01-31
申请号：US410052
申请日：1982-08-20
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Tibor Keve , Lajos Dancsi , Janos Galambos , Ferenc Vezekenyi , Tibor Acs
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Tibor Keve , Lajos Dancsi , Janos Galambos , Ferenc Vezekenyi , Tibor Acs
IPC分类号： C07D461/00 , C07D471/14 , C07D471/22 , C07D459/00
CPC分类号： C07D471/14 , C07D461/00
摘要： The invention relates to a new process for the preparation of alkoxyvincaminic acid esters of the formula (I) ##STR1## and/or alkoxyapovincaminic acid esters of the formula (II) ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 independently stand for alkyl groups having from one to 6 carbon atoms.The compounds of the formulae (I) and (II) are pharmaceutically active, thus some of them show psychostimulant activity.
摘要翻译：本发明涉及一种制备式（I）的烷氧基氨基酸酯和式（II）的烷氧基氨基酸酯的新方法，其中R1，R2和R3 独立地代表具有1至6个碳原子的烷基。式（I）和（II）的化合物是药学活性的，因此它们中的一些显示出精神兴奋作用。

2. 发明授权

US4697017A Process for the preparation of 2-bromo-.alpha.-ergocryptine 失效
标题翻译：制备2-溴-α-麦角蛋白的方法
公开(公告)号：US4697017A
公开(公告)日：1987-09-29
申请号：US869203
申请日：1986-05-30
申请人： Gabor Megyeri , Tibor Keve , Janos Galambos , Lajos Kovacs, Jr. , Bela Stefko , Erik Bogsch , Ferenc Trischler
发明人： Gabor Megyeri , Tibor Keve , Janos Galambos , Lajos Kovacs, Jr. , Bela Stefko , Erik Bogsch , Ferenc Trischler
IPC分类号： A61K31/48 , A61P25/00 , C07D519/02
CPC分类号： C07D519/02
摘要： The invention relates to a novel process for the preparation of 2-bromo-.alpha.-ergocryptine and its acid addition salt by brominating .alpha.-ergocryptine in such a way that the bromination is carried out at room temperature by using a dimethylsulphoxide-hydrogen bromide mixture containing no more 0.02% of water and, if desired, converting the thus-obtained 2-bromo-.alpha.-ergocryptine to an acid addition salt in a known manner.
摘要翻译：本发明涉及通过溴化α-麦角灵素的方法制备2-溴-α-麦角灵及其酸加成盐的新方法，使得溴化在室温下通过使用二甲基亚砜 - 溴化氢混合物进行，该混合物含有不再需要0.02％的水，如果需要，以已知的方式将由此得到的2-溴-α-麦角灵转化为酸加成盐。

3. 发明授权

US4681887A Pharmaceutical compositions with a neuroleptic action and process for preparing same 失效
标题翻译：具有精神抑制作用的药物组合物及其制备方法
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。

4. 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。

5. 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。

6. 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。

7. 发明授权

US4753949A 2-chloronicergoline having antihypoxic activity 失效
标题翻译：具有抗低氧活性的2-氯麦角林
公开(公告)号：US4753949A
公开(公告)日：1988-06-28
申请号：US877294
申请日：1986-06-23
申请人： Gabor Megyeri , Tibor Keve , Bala Stefko , Erik Bogsch , Janos Galambos , Anna Kassi nee 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 , Bala Stefko , Erik Bogsch , Janos Galambos , Anna Kassi nee 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 , A61P3/00 , A61P3/14 , A61P9/00 , A61P25/02 , A61P25/28 , C07D457/02
CPC分类号： C07D457/02
摘要： The invention relates to a novel process for the preparation of partially new 2-halonicergoline derivatives of the formula (I), ##STR1## wherein X stands for chlorine, bromine or iodine atom, as well as their acid addition salts.The process of the invention comprises esterifying a novel 2-halo-1-methyllumilysergol of the formula (II), ##STR2## wherein X is the same as defined above, or an acid addition salt thereof and, if desired, converting the thus-obtained 2-halonicergoline derivative of the formula (I) to an acid addition salt.The compounds of the invention improve the cognitive function of the brain and show an antihypoxic as well as a strong .alpha.-adrenerg blocking and calcium-antagonistic action.
摘要翻译：本发明涉及制备式（I）的部分新的2-卤代麦角灵衍生物的新方法，其中X代表氯，溴或碘原子，以及它们的酸加成盐。本发明的方法包括酯化式（II）的新的2-卤代-1-甲基烯丙基谷维素，其中X与上述定义相同，或其酸加成盐，如果需要，转化将由此获得的式（I）的2-卤代麦角灵衍生物与酸加成盐反应。本发明的化合物改善了脑的认知功能，并且显示出抗低氧以及强的α-肾上腺素能阻断和钙拮抗作用。

8. 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。

9. 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.

10. 发明授权

US08569498B2 Process for the preparation of piperazine compounds and hydrochloride salts thereof 有权
标题翻译：制备哌嗪化合物及其盐酸盐的方法
公开(公告)号：US08569498B2
公开(公告)日：2013-10-29
申请号：US13140281
申请日：2009-12-18
申请人： Laszlo Czibula , Balint Juhasz , Eva Againe Csongor , Ferenc Sebok , Janos Galambos , Katalin Nogradi
发明人： Laszlo Czibula , Balint Juhasz , Eva Againe Csongor , Ferenc Sebok , Janos Galambos , Katalin Nogradi
IPC分类号： C07D295/135 , C07D295/14
CPC分类号： C07D295/135
摘要： The invention relates to a new process for the preparation of compounds of general formula (I) whereinR1 and R2 represent independently hydrogen or C1-6 alkyl with straight or branched chain optionally substituted with aryl group, or C2-7 alkenyl containing 1-3 double bonds, or monocyclic, bicyclic or tricyclic aryl optionally substituted with one or more C1-6 alkoxy, trifluoro-C1-6 alkoxy, C1-6-alkoxycarbonil, C1-6alkanoyl, aryl, C1-6 alkylthio, halogen or cyano, or optionally substituted monocyclic, bicyclic or tricyclic C3-14 cycloalkyl group, R1 and R2 together with the adjacent nitrogen form a saturated or unsaturated optionally substituted monocyclic or bicyclic heterocyclic ring which may contain further heteroatoms selected from oxygen, nitrogen, or sulphur atoms and hydrochloric acid alts and/or hydrates and/or solvates thereof, by dissolving or suspending trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine of formula (III) or a salt or a hydrate or a solvate thereof in an inert solvent in the presence a base then adding a carbonic acid derivative of general formula (VI) wherein R is alkyl with C1-6 straight or branched chain or C1-2 fully halogenated alkyl, Z is —O—R or —X, wherein R is as described above, X is halogen, and reacting the compound of general formula (IV) obtained wherein R is as described above, in situ or, optionally in isolated state with an amine of general formula (V) wherein R1 and R2 are as described above to obtain the compound of general formula (I) and then optionally forming the hydrochloride salts and/or hydrates and/or solvates thereof.
摘要翻译：本发明涉及一种制备通式（I）化合物的新方法，其中R 1和R 2独立地表示氢或任选被芳基取代的具有直链或支链的C 1-6烷基，或含有1-3个任选被一个或多个C 1-6烷氧基，三氟-C 1-6烷氧基，C 1-6 - 烷氧羰基，C 1-6烷酰基，芳基，C 1-6烷硫基，卤素或氰基取代的单环，双环或三环芳基，或任选取代的单环，双环或三环C 3-14环烷基，R 1和R 2与相邻的氮一起形成饱和或不饱和的任选取代的单环或双环杂环，其可以含有选自氧，氮或硫原子的其它杂原子和盐酸盐和/或水合物和/或溶剂化物，通过溶解或悬浮式（III）的反式4- {2- [4-（2,3-二氯苯基） - 哌嗪-1-基] - 乙基} - 环己胺或盐或水合物或在惰性溶剂中，在碱的存在下加入通式（VI）的碳酸衍生物，其中R为烷基，C 1-6直链或支链或C 1-2完全卤代烷基，Z为-OR或-X 其中R如上所述，X是卤素，并且其中R如上所述获得的通式（IV）化合物原位或任选地在分离状态下与通式（Ⅴ）的胺反应，其中R 1和 R2如上所述，得到通式（I）的化合物，然后任选地形成盐酸盐和/或其水合物和/或溶剂化物。

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