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：US5179089A

公开(公告)日：1993-01-12

申请号：US792255

申请日：1991-11-14

申请人： Kalman Takacs ,  Iloma Kiss neAjzert ,  Istvan Hermecz ,  Janos Ori ,  Maria H. Pap ,  Zsolt Bencze ,  Peter S. Kormoczy ,  Maria Szabo ,  Judit Szeredy nee Varga ,  Csaba Vertesi ,  Lorand Debreczeni ,  Jozsef Gaal ,  Zoltan Kapui

发明人： Kalman Takacs ,  Iloma Kiss neAjzert ,  Istvan Hermecz ,  Janos Ori ,  Maria H. Pap ,  Zsolt Bencze ,  Peter S. Kormoczy ,  Maria Szabo ,  Judit Szeredy nee Varga ,  Csaba Vertesi ,  Lorand Debreczeni ,  Jozsef Gaal ,  Zoltan Kapui

IPC分类号： A61K31/47 ,  A61K31/33 ,  A61K31/472 ,  A61K31/4725 ,  A61P11/08 ,  A61P29/00 ,  A61P37/08 ,  C07D217/12 ,  C07D217/16 ,  C07D217/26

CPC分类号： C07D217/16

摘要： The invention relates to novel compounds of the general formula (I), ##STR1## wherein R means hydrogen or a straight or branched chain C.sub.1-6 alkoxy group;R.sup.1 stands for hydrogen or a straight or branched chain C.sub.1-6 alkyl group;R.sup.2 represents hydrogen or a straight or branched chain C.sub.1-6 alkyl group;R.sup.3 means hydrogen, a straight or branched chain C.sub.1-6 alkyl group optionally substituted by one or two hydroxyl and/or one or two straight or branched chain C.sub.1-4 alkoxy group(s); or a C.sub.4-7 cycloalkyl group;R.sup.4 stands for hydrogen or a straight or branched chain C.sub.1-6 alkyl group optionally substituted by one or two hydroxyl and/or one or two straight or branched chain C.sub.1-4 alkoxy group(s); or a C.sub.4-7 cycloalkyl group; orR.sup.3 and R.sup.4 together with the nitrogen atom, to which they are attached form a 4 to 8-membered cyclic group of formula ##STR2## optionally substituted by one or two straight or branched chain C.sub.1-4 alkoxy and/or one or two straight or branched chain C.sub.1-4 alkyl group(s), where optionally an oxygen or sulfur atom or an N-R.sup.5 group may be substituted for a ring carbon atom, where R.sup.5 means hydrogen or a straight or branched chain C.sub.1-6 aliphatic alkyl group, the 4- to 8-membered cycle optionally being condensed with a benzene ring;R.sup.6 stands for hydrogen or a C.sub.1-10 acyl group and the salts and hydrates thereof as well as pharmaceutical compositions containing these compounds.The compounds of the invention antagonize the effects of constrictive mediators, e.g. histamine, acetylcholine or serotonin; they show an antiallergic action and possess an antiinflammatory effect. Thus, these compounds can therapeutically be used as bronchodilators as well as antiallergic or antiinflammatory drugs, particularly in the treatment of bronchial asthma.

公开(公告)号：US5218117A

公开(公告)日：1993-06-08

申请号：US951448

申请日：1992-09-25

申请人： Kalman Takacs ,  Iloma Kiss nee Ajzert ,  Istvan Hermecz ,  Janos Ori ,  Maria H. Pap ,  Zsolt Bencze ,  Peter Szekely Kormoczy ,  Maria Szabo ,  Judit Szeredy ,  Csaba Vertesi ,  Lorand Debreczeni ,  Jozsef Gaal ,  Zoltan Kapui

发明人： Kalman Takacs ,  Iloma Kiss nee Ajzert ,  Istvan Hermecz ,  Janos Ori ,  Maria H. Pap ,  Zsolt Bencze ,  Peter Szekely Kormoczy ,  Maria Szabo ,  Judit Szeredy ,  Csaba Vertesi ,  Lorand Debreczeni ,  Jozsef Gaal ,  Zoltan Kapui

IPC分类号： C07D217/16

CPC分类号： C07D217/16

摘要： The invention relates to novel compounds of the general formula (I), ##STR1## The compounds of the invention antagonize the effects of constrictive mediators, e.g. histamine, acetylcholine or serotonin; they show an antiallergic action and possess an antiinflammatory effect. Thus, these compounds can therapeutically be used as bronchodilators as well as antiallergic or antiinflammatory drugs, particularly in the treatment of bronchial asthma.

摘要翻译： 本发明涉及通式（I）的新化合物，（I）本发明的化合物拮抗收缩性介质的作用，例如， 组胺，乙酰胆碱或5-羟色胺; 它们显示抗过敏作用并具有抗炎作用。 因此，这些化合物可以治疗性地用作支气管扩张剂以及抗过敏药或抗炎药，特别是用于治疗支气管哮喘。