公开(公告)号：US4840949A

公开(公告)日：1989-06-20

申请号：US107693

申请日：1987-10-09

申请人： Dezso Korbonits ,  Emil Minker ,  Zoltan Vargai ,  Gergely Heja ,  Gabor Kovacs ,  Agnes Gottsegen ,  Sandor Antus ,  Sandor Virag ,  Andrea Bolehovszky ,  Jeno Marton ,  Katalin Marmarosi nee Kellner ,  Lorand Debreczeni ,  Laszlo Tardos ,  Peter Kormoczy ,  Vera Gergely ,  Gabor Horvath

发明人： Dezso Korbonits ,  Emil Minker ,  Zoltan Vargai ,  Gergely Heja ,  Gabor Kovacs ,  Agnes Gottsegen ,  Sandor Antus ,  Sandor Virag ,  Andrea Bolehovszky ,  Jeno Marton ,  Katalin Marmarosi nee Kellner ,  Lorand Debreczeni ,  Laszlo Tardos ,  Peter Kormoczy ,  Vera Gergely ,  Gabor Horvath

IPC分类号： C07D473/04 ,  A61K31/52 ,  A61K31/522 ,  A61P11/04 ,  A61P11/14 ,  C07D271/06 ,  C07D273/02 ,  C07D473/06

CPC分类号： C07D473/06

摘要： The invention relates to new oxidiazole-alkyl-purine-derivatives of the Formula I ##STR1## and pharmaceutically acceptable salts thereof wherein A stands for C.sub.1-4 alkylene andR.sup.1 represents C.sub.1-6 alkyl, hydroxyalkyl, halogenoalkyl, carboxyalkyl, C.sub.5-6 cycloalkyl or aminoalkyl of the Formula --(CH.sub.2).sub.n --NR.sup.2 R.sup.3 in which group n is an integer 1-3; R.sup.2 and R.sup.3 each stand for hydrogen or C.sub.1-4 alkyl or together with the adjacent nitrogen atom they are attached to form a 5- or 6-membered nitrogen containing heterocyclic ring which may optionally comprise a further nitrogen atom or an oxygen atom as heteroatom; orR.sup.1 stands for phenyl, hydroxyphenyl, carboxyphenyl, benzyl or dimethoxybenzylThe compounds of the Formula I can be prepared by methods known per se and can be used in therapy as antitussive agents.

摘要翻译： 本发明涉及式I的新型氧化噻唑烷基嘌呤衍生物及其药学上可接受的盐，其中A代表C1-4亚烷基，R1代表C1-6烷基，羟基烷基，卤代烷基，羧基烷基，C5-6环烷基 或其中基团n为整数1-3的式 - （CH 2）n -NR 2 R 3的氨基烷基; R 2和R 3各自代表氢或C 1-4烷基或与它们相连的相邻氮原子一起形成5-或6-元含氮杂环，其可以任选地包含另外的氮原子或氧原子作为杂原子; 或R 1代表苯基，羟基苯基，羧基苯基，苄基或二甲氧基苄基。式I化合物可以通过本身已知的方法制备，并且可用于作为止咳剂的治疗。

公开(公告)号：US4565817A

公开(公告)日：1986-01-21

申请号：US474227

申请日：1983-03-11

申请人： Dezso Korbonits ,  Maria Szomor nee Wundele ,  Gergely Heja ,  Ida Szvoboda nee Kanzel ,  Pal Kiss ,  Csaba Gonczi ,  Endre Palosi ,  Gabor Kovacs ,  Judit Kun ,  Emil Minker ,  Sandor Virag ,  Gyula Sebestyen ,  Tamas Szuts

发明人： Dezso Korbonits ,  Maria Szomor nee Wundele ,  Gergely Heja ,  Ida Szvoboda nee Kanzel ,  Pal Kiss ,  Csaba Gonczi ,  Endre Palosi ,  Gabor Kovacs ,  Judit Kun ,  Emil Minker ,  Sandor Virag ,  Gyula Sebestyen ,  Tamas Szuts

IPC分类号： C07D413/06 ,  A61K31/52 ,  A61K31/522 ,  A61P11/00 ,  A61P11/08 ,  A61P11/14 ,  A61P29/00 ,  A61P31/14 ,  C07D20060101 ,  C07D271/06 ,  C07D401/14 ,  C07D473/08 ,  C07D473/14 ,  C07D473/10

CPC分类号： C07D473/08

摘要： Antitussive compounds of the formula I ##STR1## or physiologically acceptable acid addition salts thereof are disclosed, where A stands for straight or branched chain C.sub.1-5 alkylene or ##STR2## R.sub.1 stands for straight or branched chain C.sub.1-10 alkyl, halogenoalkyl, hydroxyalkyl, C.sub.5-6 cycloalkyl, vinyl, 2-ethoxyethyl, carbonylalkyl or aminoalkyl of the formula ##STR3## wherein R stands for hydrogen or methyl, n is 0 to 3,R.sub.2 stands for hydrogen or straight or branched chain alkyl,R.sub.3 stands for hydrogen or straight or branched chain alkyl or,R.sub.2 and R.sub.3 together with the nitrogen atom may form a 5-6 membered ring, which ring can optionally contain an oxygen or a second nitrogen atom, the latter, optionally substituted by methyl or,R.sub.1 can stand for a phenyl group of the formulaR.sub.4 R.sub.5 C.sub.6 H.sub.3 whereinR.sub.4 and R.sub.5 represent independently hydrogen, chlorine, hydroxy, methoxy, ethoxy, methyl or amino or,R.sub.1 may further stand for hydroxy, in this case the compound of the formula I may exist according to the conditions in the form of tautomers of the formula Ia ##STR4## and R.sub.1 may further stand for benzyl, 2,2-diphenylethyl or theophyllin-7-yl-methyl.

摘要翻译： 公开了式I的镇咳药（I）或其生理上可接受的酸加成盐，其中A代表直链或支链C 1-5亚烷基，或者R 1代表直链或支链C 1-10烷基， 卤代烷基，羟基烷基，C 5-6环烷基，乙烯基，2-乙氧基乙基，羰基烷基或下式的氨基烷基其中R代表氢或甲基，n为0-3，R2代表氢或直链或支链烷基，R3 代表氢或直链或支链烷基，或者R2和R3与氮原子一起可以形成5-6元环，该环可以任选地含有氧或第二氮原子，后者任选地被甲基或 R1可以代表式为R4R5C6H3的苯基，其中R4和R5独立地表示氢，氯，羟基，甲氧基，乙氧基，甲基或氨基，或者R1可以进一步代表羟基，在这种情况下可以存在式I化合物 根据 式Ia（Ia）或（Ib）和R1的互变异构体形式的条件可以进一步代表苄基，2,2-二苯基乙基或甲茶素-7-基 - 甲基。

公开(公告)号：US4960773A

公开(公告)日：1990-10-02

申请号：US266438

申请日：1988-11-02

申请人： Dezso Korbonits ,  Gergely Heja ,  Maria Szomor ,  Emil Minker

发明人： Dezso Korbonits ,  Gergely Heja ,  Maria Szomor ,  Emil Minker

IPC分类号： C07D473/18 ,  A61K31/52 ,  A61K31/522 ,  A61P11/14 ,  C07D473/06

CPC分类号： C07D473/06

摘要： The present invention relates to new compounds of Formula I ##STR1## and physiologically acceptable salts thereof wherein A and B stand for oxygen or --CH.sub.2 group with the proviso that if A stands for oxygen, then B stands for --CH.sub.2 group and R stands for hydrogen and, if A represents a --CH.sub.2 group, then B stands for oxygen, R stands for a --CH.sub.2 Q group wherein Q stands for hydrogen, and pyrrolidino, piperidino or morpholino and a process for the preparation thereof and pharmaceutical compositions containing as active ingredient a compound of the Formula (I) or a physiologically acceptable salt thereof.

公开(公告)号：US4511559A

公开(公告)日：1985-04-16

申请号：US472060

申请日：1983-03-04

申请人： Kalman Szendrei ,  Emil Minker ,  Zsuzsanna Rozsa ,  Lehel Koch ,  Lajos Wolf

发明人： Kalman Szendrei ,  Emil Minker ,  Zsuzsanna Rozsa ,  Lehel Koch ,  Lajos Wolf

IPC分类号： A61K36/18 ,  A61K20060101 ,  A61K31/715 ,  A61K36/00 ,  A61K36/25 ,  A61K36/28 ,  A61K36/42 ,  A61K36/48 ,  A61K36/53 ,  A61K36/71 ,  A61K36/73 ,  A61P29/00 ,  C08B20060101 ,  C08B37/00 ,  C12P19/04

CPC分类号： A61Q19/00 ,  A61K31/715 ,  A61K8/0216 ,  A61K8/73 ,  C08B37/006

摘要： A polysaccharide-concentrate obtained from plant of the genera Cucurbitaceae, Papilionaceae, Tiliaceae, Labiate, Malvaceae, Asteraceae, Umbelliferae, Rutaceae, Chenopodiaceae, Linaceae, Rosaceae and Plantaginaceae by extraction with water and precipitation of the polysaccharide with alcohol or acetone, if desired after further purification. The polysaccharides having a molecular weight between 75,000-2,000,000, containing maximum 5% of nitrogen, maximum 5% of phosphorus (expressed in P.sub.2 O.sub.5), maximum 25% of ash, minimum 30% of reducing sugar, minimum 60% of total sugar (after acidic hydrolysis, expressed as glucose) has been shown to have especially anti-inflammatory activity.

摘要翻译： 如果需要，通过用水萃取，用醇或丙酮沉淀，从葫芦科，蝴蝶科，茯苓科，菊科，菊科，菊科，伞形科，芸香科，藜科，藜科，藜科，Ros科等植物中获得的多糖浓缩物 进一步净化。 分子量为75,000-2,000,000，含最多5％氮，最多5％磷（以P2O5表示），最大25％灰分，最少30％还原糖，最低60％总糖（之后）的多糖 表现为葡萄糖的酸性水解已被证明具有特别的抗炎活性。