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公开(公告)号：US4024149A
公开(公告)日：1977-05-17
申请号：US624614
申请日：1975-10-22
IPC分类号： C07D249/08 , C07D471/04 , C07D487/04
CPC分类号： C07D249/08 , C07D471/04
摘要： New heterocyclic compounds represented by the following formula: ##STR1## wherein: R and R.sub.1 are independently selected from hydrogen, hydroxy, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, (C.sub.3-5)alkenyloxy, (C.sub.3-5)alkynyloxy, (C.sub.3-6)cycloalkyloxy, or halo or taken together represent a methylenedioxy group; the symbols W and A are defined as follows:1. W is the nitrogen atom and A is the group ##STR2## in which the carbon atom bearing the radical R.sub.2 is linked to the benzene ring and R.sub.2 is hydrogen, hydroxy, (C.sub.1-4)alkoxy or (C.sub.2-4)aliphatic acyloxy;2. W is the group =CH-- and A is --CH.sub.2 --, --CH.sub.2 --CH.sub.2 -- or --CH=CH--.The compounds have antireproductive utility.
摘要翻译： 由下式表示的新的杂环化合物：其中：
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公开(公告)号：US4379155A
公开(公告)日：1983-04-05
申请号：US284033
申请日：1981-07-17
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 I ##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 R, R.sub.2 and R.sub.3 simultaneously represent hydrogen, R.sub.1 cannot be methyl;with the further proviso that, when R.sub.2 and one of R and R.sub.3 simultaneously represent hydrogen, R.sub.1 and the other of R and R.sub.3 cannot simultaneously represent methyl; and with the still further proviso that compounds of formula I are excluded wherein R.sub.2 is hydrogen and one of R and R.sub.3 is simultaneously a 2-positioned alkyl group and the other of R and R.sub.3 is hydrogen; and salts thereof with pharmaceutically acceptable acids. The compounds possess anti-reproductive utility.
摘要翻译： 新的式I的3,5-二取代的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R，R 2和R 3同时表示氢时，R 1不能是甲基; 进一步的条件是当R 2和R 3中的一个同时表示氢时，R 1和R 3和R 3中的另一个不能同时代表甲基; 并且另外的条件是排除式I化合物，其中R 2是氢，R 3和R 3之一同时是2-位烷基，R和R 3中的另一个是氢; 和其盐与药学上可接受的酸。 这些化合物具有抗生殖效用。
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公开(公告)号：US4075342A
公开(公告)日：1978-02-21
申请号：US629339
申请日：1975-11-06
IPC分类号： A61K31/47 , A61K31/4745 , C07D209/44 , C07D235/02 , C07D471/04
CPC分类号： C07D235/02 , C07D209/44 , C07D471/04 , Y10S514/843
摘要： Novel tricyclic compounds containing two ring notrogen atoms and represented by the following formula I ##STR1## wherein: A is one of the groups --CH.sub.2 --; --CH.dbd.CH--; and --CH.sub.2 --CH.sub.2 --;R is hydrogen, lower alkyl, lower alkoxy, lower alkenyloxy, lower alkynyloxy, cyclo(C.sub.3-6 alkyl)oxy, hydroxy, benzyloxy, halo, sulfamoyl, cyano, trifluoromethyl or nitro; R.sub.1 is hydrogen, lower alkoxy or halo; or R and R.sub.1 taken together are methylenedioxy; the sequence ##STR2## is one of the following moieties: ##STR3## WHEREIN R.sub.2 is hydrogen or lower alkyl; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is hydrogen, methyl, carboxy, carbo(lower alkoxy), carbamyl, mono- or di-(lower alkyl) carbamyl or hydroxymethyl; provided that when the sequence ##STR4## is one of the moieties a) and b) wherein R.sub.2 is hydrogen or lower alkyl, A is not --CH.dbd.CH--; when the sequence ##STR5## is one of the moieties (a) and (b) wherein R.sub.2 is hydrogen, A is not --CH.sub.2 --; and when the sequence ##STR6## is one of the moieties (c) and (d) wherein R.sub.3 is hydrogen and when both R and R.sub.1 are hydrogen, A is not --CH.dbd.CH--; and the salts thereof with a non-toxic pharmaceutically-acceptable acid. The compounds of the invention have antireproductive activity.
摘要翻译： 含有两个环的雌激素原子的新型三环化合物，由以下代表
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公开(公告)号：US4007276A
公开(公告)日：1977-02-08
申请号：US684592
申请日：1976-05-10
IPC分类号： C07D487/04 , A61K31/407 , A61K31/41 , A61K31/4196 , A61P25/00 , A61P25/04 , A61P29/00 , C07D20060101 , C07D209/46 , C07D209/52 , C07D209/80 , C07D209/94 , C07D217/00 , C07D217/24 , C07D249/08 , C07D249/16
CPC分类号： C07D217/24 , C07D209/46
摘要： New s-triazolo[5,1-a]isoindole derivatives of following formula I ##STR1## wherein R is selected from hydrogen, amino, lower alkyl amino, di-lower alkyl amino, acylamino, diacylamino, benzoylamino, 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, chloro or lower alkoxy.A process for their manufacture which comprises the reaction of 2-aminophthalimidine with a reagent R-Z wherein R has the same meaning as above, and Z represents one of the following groups: ##STR2## wherein R.sub.3 is C.sub.1 -C.sub.4 alkyl. The compounds and some of the intermediates of the process are useful as antiinflammatories, analgesics, CNS depressants, antimicrobials and anti-fertility agents.
摘要翻译： 下式I的新的三唑并[5,1-a]异吲哚衍生物其中R选自氢，氨基，低级烷基氨基，二低级烷基氨基，酰氨基，二酰氨基，苯甲酰氨基，脲基，硫脲基， 苯甲酰基硫脲基，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，氯或低级烷氧基。
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公开(公告)号：US3616227A
公开(公告)日：1971-10-26
申请号：US3616227D
申请日：1968-09-16
申请人： SAMUEL C PAN , LEONARD J LERNER
发明人： PAN SAMUEL C , LERNER LEONARD J
IPC分类号： C07J17/00 , C07J75/00 , C07C167/00
摘要： This invention relates to Alpha -glucosides of steroids containing hydroxy groups in both the 16 Alpha - and 17-positions and the method for preparing them by reacting with a polysaccharide or an oligosaccharide, such as maltose, in the presence of a source of the enzyme: amylase or transglucosylase. The Alpha -glucosides are new compounds that possess estrogenic activity. They may be used, therefore, as antifertility agents.
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