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1. 再颁专利

USRE30456E 2-Substituted phenyl-s-triazolo[5,1-a] isoquinoline compounds 失效
标题翻译： 2-取代的苯基 - 三唑并[5,1-a]异喹啉化合物
公开(公告)号：USRE30456E
公开(公告)日：1980-12-23
申请号：US32205
申请日：1979-04-23
申请人： Amedeo Omodei-Sale , Pietro Consonni , Leonard Lerner
发明人： Amedeo Omodei-Sale , Pietro Consonni , Leonard Lerner
IPC分类号： A61K31/41 , A61K31/435 , A61K31/47 , A61P25/04 , A61P25/20 , A61P29/00 , C07D209/00 , C07D209/46 , C07D217/24 , C07D221/00 , C07D249/00 , C07D249/16 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D209/46 , C07D217/24
摘要： A new process for preparing s-triazolo[5,1-a]-isoquinoline derivatives of the formula ##STR1## wherein A represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--; R is selected from hydrogen, amino, lower alkylamino, di-lower alkylamino, acylamino, diacylamino, ureido, thioureido, carbethoxythioureido, benzoylthioureido, sulfhydryl, lower alkyl, trifluoromethyl, phenyl, substituted phenyl, pyridyl, methylpyridyl and dimethylpyridyl; and R.sub.1 and R.sub.2 each independently represents hydrogen or lower alkoxy, by condensation of a 2-amino-3,4-dihydro-1(2H)-isoquinolinone with an imidolyl, cyanamide, cyanic or thiocyanic derivative.New compounds of the formula I wherein A represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, R has the same meaning as above with the exclusion of hydrogen, methyl, phenyl, and trifluoromethyl, R.sub.1 and R.sub.2 have the same meaning as above, with the proviso that when A represents the group --CH.dbd.CH--, R cannot be tolyl or pyridyl.The new compounds and some of the intermediates of the process are active as antiinflammatories, CNS depressants and anti-fertility agents.

2. 发明授权

US4075341A 2-Substituted phenyl-5-triazols [5,1-a] isoquinoline compounds 失效
标题翻译： 2-取代的苯基-5-三唑类{8 5,1-a {9 {0异喹啉化合物
公开(公告)号：US4075341A
公开(公告)日：1978-02-21
申请号：US636330
申请日：1975-11-28
申请人： Amedeo Omodei-Sale , Pietro Consonni , Leonard Lerner
发明人： Amedeo Omodei-Sale , Pietro Consonni , Leonard Lerner
IPC分类号： C07D217/24 , C07D471/04 , A61K31/53
CPC分类号： C07D471/04 , C07D217/24
摘要： A new process for preparing s-triazolo[5,1-a]-isoquinoline derivatives of the formula ##STR1## wherein A represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--; R is selected from hydrogen, amino, lower alkylamino, di-lower alkylamino, acylamino, diacylamino, ureido, thioureido, carbethoxythioureido, benzoylthioureido, sulfhydryl, lower alkyl, trifluoromethyl, phenyl, substituted phenyl, pyridyl, methylpyridyl and dimethylpyridyl; and R.sub.1 and R.sub.2 each independently represents hydrogen or lower alkoxy; by condensation of a 2-amino-3,4-dihydro-1(2H)-isoquinolinone with an imidolyl, cyanamide, cyanic or thiocyanic derivative.New compounds of the formula I wherein A represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, R has the same meaning as above with the exclusion of hydrogen, methyl, phenyl, and trifluoromethyl, R.sub.1 and R.sub.2 have the same meaning as above, with the proviso that when A represents the group --CH.dbd.CH--, R cannot be tolyl or pyridyl.The new compounds and some of the intermediates of the process are active as antiinflammatories, CNS depressants and anti-fertility agents.
摘要翻译：一种制备式（I）的三唑并[5,1-a] - 异喹啉衍生物的新方法，其中A代表基团-CH 2 -CH 2 - 或-CH = CH-; R选自氢，氨基，低级烷基氨基，二低级烷基氨基，酰氨基，二酰基氨基，脲基，硫脲基，乙氧基硫代脲基，苯甲酰硫基脲基，巯基，低级烷基，三氟甲基，苯基，取代的苯基，吡啶基，甲基吡啶基和二甲基吡啶基。并且R 1和R 2各自独立地表示氢或低级烷氧基; 通过2-氨基-3,4-二氢-1（2H） - 异喹啉酮与亚氨基，氨基氰，氰基或硫氰酸衍生物的缩合。

3. 发明授权

US4370336A 3,5-Disubstituted-1H-1,2,4-triazole derivatives as antifertility agents 失效
标题翻译： 3,5-二取代-1H-1,2,4-三唑衍生物作为抗菌剂
公开(公告)号：US4370336A
公开(公告)日：1983-01-25
申请号：US254729
申请日：1981-04-16
申请人： Amedeo Omodei-Sale , Pietro Consonni , Giulio Galliani , Leonard Lerner
发明人： Amedeo Omodei-Sale , Pietro Consonni , Giulio Galliani , Leonard Lerner
IPC分类号： C07D249/08 , A61K31/41
CPC分类号： C07D249/08
摘要： New 3,5-disubstituted-1H-1,2,4-triazoles of formula ##STR1## wherein: R is selected from hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, fluoro, chloro and dimethylamino;R.sub.1 represents a (C.sub.1-4)alkyl group;R.sub.2 is selected from hydrogen, fluoro, chloro, (C.sub.1-4)alkyl, methoxy and ethoxy;R.sub.3 is selected from hydrogen, fluoro, chloro, (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy;R and R.sub.3 taken together represent a methylenedioxy group; with the proviso that, when simultaneously R, R.sub.2 and R.sub.3 represent hydrogen,cannot be methyl;with the further proviso that, when simultaneously R.sub.2 and one of R and R.sub.3 represent hydrogen, R.sub.1 and the other of R and R.sub.3 cannot simultaneously represent methyl;and salts therewith of pharmaceutically acceptable acids.The compounds possess anti-reproductive utility.
摘要翻译：新的式（I）的3,5-二取代-1H-1,2,4-三唑其中：R选自氢，（C 1-4）烷基，（C 1-4）烷氧基，烯丙氧基，炔丙氧基，三氟甲基，苯基，氟，氯和二甲基氨基; R1表示（C1-4）烷基; R 2选自氢，氟，氯，（C 1-4）烷基，甲氧基和乙氧基; R3选自氢，氟，氯，（C1-4）烷基和（C1-4）烷氧基; R和R3一起代表亚甲二氧基; 条件是当同时R，R 2和R 3表示氢时，不能是甲基; 进一步的条件是当R 2和R 3中的一个表示氢时，R 1和R 3和R 3中的另一个不能同时表示甲基; 以及其与药学上可接受的酸的盐。这些化合物具有抗生殖效用。

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