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1. 发明授权

US4535090A 3,5-Diphenyl-1H-1,2,4-triazoles pharmaceutical compositions and uses 失效
标题翻译： 3,5-二苯基-1H-1,2,4-三唑类药物组合物及用途
公开(公告)号：US4535090A
公开(公告)日：1985-08-13
申请号：US434451
申请日：1982-10-15
申请人： Giulio Galliani , Amedeo Omodei-Sale , Pietro Consonni , Alessandro Assandri
发明人： Giulio Galliani , Amedeo Omodei-Sale , Pietro Consonni , Alessandro Assandri
IPC分类号： A61K9/08 , A61K9/107 , A61K31/41 , A61P11/00 , C07C243/38 , C07D249/08 , C07D249/10 , C07D405/04 , C07D405/10
CPC分类号： C07D249/08 , C07C243/38 , C07D405/04 , Y10S514/843
摘要： 3,5-diphenyl-1H-1,2,4-triazoles with contragestational activity of the following formula ##STR1## wherein R may be located on one or the other of the two adjacent nitrogen atoms and may represent hydrogen or a group R.sub.5 CO-- wherein R.sub.5 is an aliphatic saturated or unsaturated hydrocarbyl containing from 1 to 20 carbon atoms, R.sub.1, R.sub.2 and R.sub.3, each independently are selected from hydrogen, lower alkyl and lower alkoxy or R.sub.2 and R.sub.3 together may represent a methylenedioxy group, and R.sub.4 is an aliphatic saturated or unsaturated hydrocarbyl group of from 1 to 20 carbons, with the proviso that when R is hydrogen or an R.sub.5 CO-- group wherein R.sub.5 contains 4 or less carbon atoms, R.sub.4 must contain 5 or more carbons.These compounds have proven to be highly effective in terminating pregnancy in several animal species after a single parenteral injection.
摘要翻译：具有下式的映射活性的3,5-二苯基-1H-1,2,4-三唑：其中R可以位于两个相邻氮原子的一个或另一个上，并且可以表示氢或基团R 5 CO- 其中R 5是含有1至20个碳原子的脂族饱和或不饱和烃基，R 1，R 2和R 3各自独立地选自氢，低级烷基和低级烷氧基，或者R 2和R 3一起可表示亚甲二氧基，并且R 4是具有1至20个碳原子的脂肪族饱和或不饱和烃基，条件是当R是氢或R5含有4个或更少碳原子的R5CO-基时，R4必须含有5个或更多个碳。已经证明这些化合物在单次肠胃外注射后在几种动物物种中终止妊娠是非常有效的。

2. 发明授权

US4379155A 3,5-Disubstituted-1H-1,2,4-triazole derivatives 失效
标题翻译： 3,5-二取代-1H-1,2,4-三唑衍生物
公开(公告)号：US4379155A
公开(公告)日：1983-04-05
申请号：US284033
申请日：1981-07-17
申请人： Amedeo Omodei-Sale , Pietro Consonni , Giulio Galliani , Leonard J. Lerner
发明人： Amedeo Omodei-Sale , Pietro Consonni , Giulio Galliani , Leonard J. 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 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。

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。

4. 发明授权

US4313950A Antireproductive tricyclic ortho-fused nitrogen containing compounds 失效
标题翻译：抗生素三环邻位稠合含氮化合物
公开(公告)号：US4313950A
公开(公告)日：1982-02-02
申请号：US230138
申请日：1981-01-30
申请人： Umberto Guzzi , Amedeo Omodei-Sale , Giulio Galliani
发明人： Umberto Guzzi , Amedeo Omodei-Sale , Giulio Galliani
IPC分类号： C07D217/24 , C07D223/16 , C07D471/04 , C07D487/04 , A61K31/47
CPC分类号： C07D223/16 , C07D217/24 , C07D471/04 , C07D487/04 , Y10S514/96
摘要： New tricyclic ortho-fused nitrogen containing compounds of the following formula: ##STR1## wherein R and R.sub.1 are independently selected from hydrogen, fluoro, chloro, bromo and (C.sub.1 -C.sub.4)alkoxy; A may be --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --(CH.sub.2).sub.3 --; X represents a nitrogen atom or the group CH; and salts therewith of pharmaceutically acceptable acids.The compounds possess an outstanding antireproductive utility.
摘要翻译：新的具有下式的三环邻 - 稠合氮化合物：其中R和R 1独立地选自氢，氟，氯，溴和（C 1 -C 4）烷氧基; A可以是-CH 2 - ， - CH 2 -CH 2 - ， - CH = CH - 或 - （CH 2）3 - ; X表示氮原子或基团CH; 以及其与药学上可接受的酸的盐。该化合物具有突出的抗生素效用。

5. 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.

6. 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。

7. 发明授权

US4119635A Substituted 1,2,4-triazole derivatives 失效
标题翻译：取代的1,2,4-三唑衍生物
公开(公告)号：US4119635A
公开(公告)日：1978-10-10
申请号：US720479
申请日：1976-09-03
申请人： Amedeo Omodei-Sale , Giorgio Pifferi , Pietro Consonni , Alberto Diena , Bonaccorso Rosselli del Turco
发明人： Amedeo Omodei-Sale , Giorgio Pifferi , Pietro Consonni , Alberto Diena , Bonaccorso Rosselli del Turco
IPC分类号： C07C243/38 , C07D249/08
CPC分类号： C07D249/08 , C07C243/38
摘要： New 1-alkyl-3,5-disubstituted-1,2,4-triazole derivatives of following formula I ##STR1## wherein R may represent phenyl; phenyl substituted by a radical selected from (C.sub.1-4)alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec.-butyl, isobutyl or tert.-butyl, (C.sub.1-4)alkoxy, e.g. methoxy, ethoxy, propoxy, butoxy, isobutyloxy or tert.-butoxy, fluoro, chloro, bromo, nitro, amino, cyano, carbamoyl, carboxy, hydroxymethyl, methylenedioxy and trifluoromethyl; dichlorophenyl; dimethoxyphenyl; 3,4,5-trimethoxyphenyl;R.sub.1 may represent phenyl, phenyl substituted by a radical selected from (C.sub.1-4)alkyl as above defined, (C.sub.1-4)alkoxy as above defined; fluoro, chloro, bromo, hydroxymethyl, (C.sub.2-4)aliphatic acyloxymethyl, e.g. acetoxymethyl, propionyloxymethyl or butyryloxymethyl, carbamoyloxymethyl, bromomethyl and dimethylaminomethyl; dimethylphenyl; dimethoxyphenyl; phenyl contemporaneously substituted by o-hydroxymethyl and chloro;R.sub.2 represents a (C.sub.1-4)alkyl group as above defined;With the proviso that R and R.sub.1 cannot simultaneously represent phenyl;With the further proviso that, when R is phenyl, R.sub.1 cannot be p-chlorophenyl;And processes for their preparation.The compounds of the invention have CNS depressant utility. They are especially useful as sedatives and hypnotics. Some of the compounds of the invention are also useful as anxiety relieving means.
摘要翻译：新的下式I的1-烷基-3,5-二取代-1,2,4-三唑衍生物其中R可以表示苯基; 被选自（C 1-4）烷基的基团取代的苯基，例如甲基，乙基，丙基，异丙基，丁基，仲丁基，异丁基或叔丁基，（C 1-4）烷氧基。甲氧基，乙氧基，丙氧基，丁氧基，异丁氧基或叔丁氧基，氟，氯，溴，硝基，氨基，氰基，氨基甲酰基，羧基，羟甲基，亚甲二氧基和三氟甲基; 二氯苯; 二甲氧基苯基; 3,4,5-三甲氧基苯基; R 1可以表示苯基，被选自上述定义的（C 1-4）烷基的基团取代的苯基，如上定义的（C 1-4）烷氧基; 氟，氯，溴，羟甲基，（C 2-4）脂族酰氧基甲基，乙酰氧基甲基，丙酰氧基甲基或丁酰氧基甲基，氨基甲酰氧基甲基，溴甲基和二甲基氨基甲基; 二甲基苯基; 二甲氧基苯基; 同时由邻羟甲基和氯取代的苯基; R2表示如上定义的（C 1-4）烷基; R和R1不能同时表示苯基; 另外，当R是苯基时，R 1不能是对氯苯基; 及其制备方法。

8. 发明授权

US4774325A New 8-substituted nucleoside and purine derivatives, the process for the preparation thereof and the pharmaceutical compositions containing them 失效
标题翻译：新的8-取代的核苷和嘌呤衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4774325A
公开(公告)日：1988-09-27
申请号：US776472
申请日：1985-09-16
申请人： Silvano Casadio , Duccio Favara , Amedeo Omodei-Sale , Ezio Panto
发明人： Silvano Casadio , Duccio Favara , Amedeo Omodei-Sale , Ezio Panto
IPC分类号： C07D473/34 , A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61K31/708 , A61P3/06 , C07D303/22 , C07D309/12 , C07D473/16 , C07D473/18 , C07F9/6561 , C07H19/16 , C07H19/167 , C07H19/20
CPC分类号： C07D303/22 , C07D309/12 , C07D473/18 , C07H19/16 , C07H19/20
摘要： New 8-substituted nucleoside and purine derivatives of the general formula: ##STR1## wherein R represents an amino group or an hydroxy group possibly in the corresponding keto tautomeric form, R.sub.1 is hydrogen or an amino group, R.sub.2 is hydrogen or a .beta.-D-ribofuranosyl radical wherein the primary hydroxy group and/or the two secondary hydroxy groups may be derivatized, R.sub.3 is an optionally substituted aryl or monocyclic heteroaryl radical and, X is --O-- or --S--. The new compounds have antihyperlipaemic activity.
摘要翻译：新的8-取代的核苷和嘌呤衍生物，其通式如下：其中R表示氨基或可能具有相应的酮互变异构形式的羟基，R 1是氢或氨基，R 2是氢或β-D - 呋喃核糖基，其中伯羟基和/或两个仲羟基可以被衍生化，R 3是任选取代的芳基或单环杂芳基，并且X是-O-或-S-。新化合物具有抗高血脂活性。

9. 发明授权

US4340607A Antimicrobial 3H-naphtho[1,2-d]imidazoles 失效
标题翻译：抗微生物3H-萘并[1,2-d]咪唑
公开(公告)号：US4340607A
公开(公告)日：1982-07-20
申请号：US236468
申请日：1981-02-20
申请人： Emilio Toja , Amedeo Omodei-Sale , Domenica Selva
发明人： Emilio Toja , Amedeo Omodei-Sale , Domenica Selva
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P25/04 , A61P29/00 , A61P31/04 , C07D235/02 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D405/02
CPC分类号： C07D235/02
摘要： 3H-naphtho[1,2-d]imidazole derivatives of formula ##STR1## wherein R stands for (C.sub.1-6)alkyl, (C.sub.3-6)alkenyl, (C.sub.3-6)alkynyl or (C.sub.3-7)cycloalkyl, R.sub.1 and R.sub.2, each independently may represent hydrogen, halogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkylthio, (C.sub.1-4)alkoxy or halo(C.sub.1-4)alkoxy, R.sub.3 and R.sub.4, each independently, represent hydrogen or (C.sub.1-4)alkoxy, R.sub.5 stands for hydrogen, (C.sub.1-4)alkyl, (C.sub.3-4)alkoxy, mono- and di-(C.sub.2-4)alkylamino, (C.sub.2-4)alkanoylamino, carboxymethoxy and [carbo(C.sub.1-4)alkoxy]methoxy and R.sub.6 is hydrogen or R.sub.4 and R.sub.6 taken together may represent a methylenedioxy radical with the proviso that when R.sub.5 is hydrogen at least one of R.sub.3 and R.sub.4 must be different from hydrogen, useful as antimicrobial agents.
摘要翻译：其中R代表（C 1-6）烷基，（C 3-6）烯基，（C 3-6）炔基或（C 3-7）环烷基，R 1 并且R 2各自独立地表示氢，卤素，（C 1-4）烷基，（C 1-4）烷硫基，（C 1-4）烷氧基或卤代（C 1-4）烷氧基，R 3和R 4各自独立地表示氢或（C 1-4）烷氧基，R5代表氢，（C1-4）烷基，（C3-4）烷氧基，单 - 和二 - （C2-4）烷基氨基，（C2-4）烷酰基氨基，羧甲氧基和[ C 1-4）烷氧基]甲氧基并且R 6是氢或R 4和R 6一起可以代表亚甲二氧基，条件是当R 5是氢时，R 3和R 4中的至少一个必须不同于氢，可用作抗微生物剂。

10. 发明授权

US4461894A Naphth[1,2-d]imidazoles 失效
标题翻译：萘[1,2-d]咪唑
公开(公告)号：US4461894A
公开(公告)日：1984-07-24
申请号：US371768
申请日：1982-04-26
申请人： Amedeo Omodei-Sale , Emilio Toia
发明人： Amedeo Omodei-Sale , Emilio Toia
IPC分类号： C07D221/04 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/4427 , A61K31/445 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5355 , A61K31/5377 , A61P25/00 , C07D235/02 , C07D261/20 , C07D263/60 , C07D401/06 , C07D401/12 , C07D403/08 , C07D487/00
CPC分类号： C07D235/02 , C07D263/60
摘要： Naphth[1,2-d]imidazoles and naphth[2,1-d]oxazoles of formula ##STR1## wherein R and R.sub.1 are hydrogen, halogen, alkyl or alkoxy, R.sub.2 is hydrogen or halogen and A is one of the following moieties ##STR2## wherein R.sub.3 is alkyl, cycloalkyl, or a --(CH.sub.2).sub.n NR.sub.5 R.sub.6 group in which n is 1, 2 or 3, R.sub.5 is hydrogen or alkyl, R.sub.6 is alkyl or R.sub.5 and R.sub.6 taken together with the adjacent nitrogen atom are a 4- to 7-membered saturated hetero ring which may contain a further hetero atom and optionally may be substituted, e.g., with phenyl or substituted phenyl, R.sub.4 is hydrogen, alkyl, cycloalkyl or a --(CH.sub.2).sub.n NR.sub.5 R.sub.6 group, provided that one of R.sub.3 and R.sub.4 is a --(CH.sub.2).sub.n --NR.sub.5 R.sub.6 group, and R.sub.7 is --(CH.sub.2).sub.n --NR.sub.5 R.sub.6, or a pharmaceutically-acceptable acid addition salt thereof. They are made by contacting a corresponding naphth[1,2-d]imidazole or a naphth[2,1-d]oxazole wherein one of R.sub.3 and R.sub.4 or R.sub.7 is a --(CH.sub.2).sub.n X group wherein X is the residue of a reactive ester with an appropriate amine of the formula HNR.sub.5 R.sub.6 in the presence of an acid acceptor. The new compounds are useful as CNS-depressant agents.

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