公开(公告)号：US4254128A

公开(公告)日：1981-03-03

申请号：US963113

申请日：1978-11-22

申请人： Ben-Zion Weiner ,  Raul Suchi ,  Jeffrey Sterling ,  Haim Yellin

发明人： Ben-Zion Weiner ,  Raul Suchi ,  Jeffrey Sterling ,  Haim Yellin

IPC分类号： A61K31/15 ,  A01N45/00 ,  A61K31/185 ,  A61K31/195 ,  A61K31/215 ,  A61K31/445 ,  A61P31/04 ,  A61P31/10 ,  A61P31/12 ,  C07C67/00 ,  C07C241/00 ,  C07C243/20 ,  C07C243/22 ,  C07D213/77 ,  C07D215/28 ,  C07D215/42 ,  C07D233/80 ,  C07D295/22 ,  C07D295/30 ,  C07D327/06 ,  A61K31/40

CPC分类号： C07D213/77 ,  C07C243/00 ,  C07D215/42 ,  C07D233/80 ,  C07D295/30

摘要： The invention provides novel 2-adamantyl hydrazine derivatives of the general formula A ##STR1## In this formula R.sub.1 is hydrogen or a lower alkyl group of 1-4 carbon atoms; R.sub.2 and R.sub.3 are the same or different and are each hydrogen, an unsubstituted or substituted radical being a lower alkyl of 1-4 carbon atoms, a lower alkanoic acid radical of 2-4 carbon atoms or a lower alkyl ester thereof, adamantyl, aryl, aralkyl, in which the alkyl moiety has from 1-4 carbon atoms or an unsubstituted or substituted heterocyclic radical of aromatic character; or R.sub.2 and R.sub.3 together with the nitrogen atom to which they are attached form an unsubstituted or substituted non-aromatic cyclic radical.The invention further provides pharmaceutically acceptable acid addition salts of the above compounds.Several methods of preparation of the new compounds are described.The novel compounds according to the invention possess valuable antifungal (human and plant), antiviral, antiprotozoal and antimicrobial properties.

摘要翻译： 本发明提供了通式为A的新型2-金刚烷基肼衍生物。在该式中，R 1是氢或1-4个碳原子的低级烷基; R2和R3相同或不同，各自为氢，未取代或取代的基团为1-4个碳原子的低级烷基，2-4个碳原子的低级链烷酸基团或其低级烷基酯，金刚烷基，芳基 ，其中烷基部分具有1-4个碳原子的芳烷基或芳族特征的未取代或取代的杂环基; 或R 2和R 3与它们所连接的氮原子一起形成未取代或取代的非芳族环状基团。 本发明进一步提供上述化合物的药学上可接受的酸加成盐。 描述了几种制备新化合物的方法。 根据本发明的新化合物具有有价值的抗真菌（人和植物），抗病毒，抗原虫和抗微生物特性。

公开(公告)号：US4202892A

公开(公告)日：1980-05-13

申请号：US963114

申请日：1978-11-22

申请人： Ben-Zion Weiner ,  Jeffrey Sterling ,  Raul Suchi ,  Haim Yellin

发明人： Ben-Zion Weiner ,  Jeffrey Sterling ,  Raul Suchi ,  Haim Yellin

IPC分类号： A61K31/15 ,  A01N33/26 ,  A61K31/185 ,  A61K31/195 ,  A61K31/215 ,  A61P31/04 ,  A61P31/10 ,  A61P31/12 ,  C07C67/00 ,  C07C241/00 ,  C07C243/14 ,  C07C243/18 ,  C07C243/22 ,  C07D213/77 ,  C07D215/28 ,  C07D215/42 ,  C07D233/80 ,  C07D295/22 ,  C07D295/30 ,  C07D327/06 ,  A61K31/33 ,  A61K27/00 ,  C07C109/02

CPC分类号： C07D213/77 ,  C07C243/00 ,  C07D215/42 ,  C07D233/80 ,  C07D295/30

摘要： The invention provides novel 1- or 2-adamantylmethyl hydrazines of the general formula A ##STR1## In this formula Ad is 1- or 2-adamantyl, R.sub.1 and R.sub.2 are the same or different and are each hydrogen or a lower unsubstituted or substituted alkyl group of 1-4 carbon atoms; R.sub.3 and R.sub.4 are the same or different and are each hydrogen, an unsubstituted or substituted radical being a lower alkyl group of 1-4 carbon atoms a lower alkanoic acid radical of 2-4 carbon atoms or a lower alkyl ester thereof, adamantyl, aryl, aralkyl in which the alkyl moiety has 1-4 carbon atoms or an unsubstituted or substituted heterocyclic radical of aromatic character; or R.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached form a cyclic radical or non-aromatic character.The invention further provides pharmaceutically acceptable acid addition salts of the above compounds.Several methods of preparation of the new compounds are described.The novel compounds according to the invention possess valuable antifungal (human and plant), antiviral, antiprotozoal and antimicrobial properties.

摘要翻译： 本发明提供了通式A的新颖的1-或2-金刚烷基甲基肼。在该式中，Ad是1-或2-金刚烷基，R1和R2相同或不同，各自为氢或未被取代或取代的低级 1-4个碳原子的烷基; R3和R4相同或不同，各自为氢，未取代或取代的基团是1-4个碳原子的低级烷基，2-4个碳原子的低级链烷酸基团或其低级烷基酯，金刚烷基，芳基 ，其中烷基部分具有1-4个碳原子的芳烷基或芳族特征的未取代或取代的杂环基; 或R 3和R 4与它们所连接的氮原子一起形成环状基团或非芳族性质。 本发明进一步提供上述化合物的药学上可接受的酸加成盐。 描述了几种制备新化合物的方法。 根据本发明的新化合物具有有价值的抗真菌（人和植物），抗病毒，抗原虫和抗微生物特性。