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1. 发明授权

US4151169A Process for preparing substituted 1,2,4-triazole derivatives 失效
标题翻译：制备取代的1,2,4-三唑衍生物的方法
公开(公告)号：US4151169A
公开(公告)日：1979-04-24
申请号：US921911
申请日：1978-07-03
申请人： Amedeo O. Sale , Giorgio Pifferi , Pietro Consonni , Alberto Diena , Bonaccorso R. Del Turco
发明人： Amedeo O. Sale , Giorgio Pifferi , Pietro Consonni , Alberto Diena , Bonaccorso R. Del Turco
IPC分类号： C07D249/08
CPC分类号： C07D249/08
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 compound 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，如上所定义的（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; 条件是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。

2. 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。

3. 发明授权

US3960858A 3-Hetero acyl-2,3-benzoxazepines 失效
标题翻译： 3-杂酰基-2,3-苯并氧氮杂
公开(公告)号：US3960858A
公开(公告)日：1976-06-01
申请号：US523789
申请日：1974-11-14
申请人： Giorgio Pifferi , Amedeo Omodei-Sale' , Pietro Consonni
发明人： Giorgio Pifferi , Amedeo Omodei-Sale' , Pietro Consonni
IPC分类号： C07D267/04 , C07D413/06
CPC分类号： C07D267/04
摘要： A new class of 2,3-benzoxazepine compounds of the formula ##SPC1##In the formula, R is heterocyclic acyl or heterocyclic acetyl. The compounds have central nervous system and anti-inflammatory activity.
摘要翻译：一类新的2,3-苯并氧氮杂鏻化合物，式中R是杂环酰基或杂环乙酰基。该化合物具有中枢神经系统和抗炎活性。

4. 发明授权

US4041048A 3,2-Benzoxazepine derivatives 失效
标题翻译： 3,2 - 苯并氧氮杂衍生物
公开(公告)号：US4041048A
公开(公告)日：1977-08-09
申请号：US523790
申请日：1974-11-14
申请人： Giorgio Pifferi , Amedeo Omodei-Sale' , Pietro Consonni
发明人： Giorgio Pifferi , Amedeo Omodei-Sale' , Pietro Consonni
IPC分类号： C07D267/04 , C07D267/14 , C07D267/02
CPC分类号： C07D267/14 , C07D267/04
摘要： 3,2-Benzoxazepines of the formula ##STR1## and their preparation. In formula (I), R respesents hydrogen or lower alkyl; R.sup.1 represents hydrogen, lower alkyl, lower alkenyl, hydroxy-lower alkyl, carbamyloxy-lower alkyl, acyl, amidino, carbamyl, mono- or di-substituted carbamyl; R.sup.2 may be in position 7 or 8 of the benzoxazepine ring and represents hydrogen, nitro, amino, acetamino or halo. The compounds are prepared by reacting 1,2,4,5-tetrahydro-3,2-benzoxazepine with a reactant which reacts with a secondary amino group to give substitution in the 2-position. The compounds have anti-inflammatory and central nervous system activity.
摘要翻译：式（I）的“3-苯并氧氮杂”＆lt; IMAGE＆gt;及其制备。在式（I）中，R表示氢或低级烷基; R 1表示氢，低级烷基，低级烯基，羟基 - 低级烷基，氨基甲酰氧基 - 低级烷基，酰基，脒基，氨基甲酰基，单或二取代的氨基甲酰基; R2可以位于苯并氧氮杂环的7或8位，代表氢，硝基，氨基，乙酰氨基或卤素。该化合物通过使1,2,4,5-四氢-3,3-苯并氧氮杂与与仲氨基反应以在2-位取代的反应物进行制备。该化合物具有抗炎和中枢神经系统活性。

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

US4888350A New acyl-1H-1,2,4-triazole derivatives 失效
标题翻译：新的酰基-1H-1,2,4-三唑衍生物
公开(公告)号：US4888350A
公开(公告)日：1989-12-19
申请号：US915119
申请日：1986-10-03
申请人： Amedeo Omodei-Sale' , Pietro Consonni , Giulio Galliani
发明人： Amedeo Omodei-Sale' , Pietro Consonni , Giulio Galliani
IPC分类号： C07D233/54 , C07D249/08
CPC分类号： C07D233/64 , C07D233/54 , C07D249/08
摘要： New acyl -1H-1,2,4-triazole derivatives of the formula ##STR1## wherein R may be located on one of the two adjacent nitrogen atoms and may represent hydrogen; a group R.sub.5 -CO wherein R.sub.5 is selected from (C.sub.1-4)alkyl, (C.sub.2-4)alkenyl, (C.sub.2-4)alkynyl, phenyl, phenyl substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylenedioxy, benzyl, cinnamyl, amino, (C.sub.1-4)alkylamino, di-(C.sub.1 -C.sub.4)alkylamino, phenylamino, phenylamino wherein the phenyl ring may be substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylendioxy, halo(C.sub.1-4)alkyl, (C.sub.1-4)alkoxy and benzyloxy; a group R.sub.6 -SO.sub.2 wherein R.sub.6 may represent (C.sub.1-4)alkyl, phenyl, phenyl substituted by a radical selected from (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy, or phenactyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, allyloxy, propargyloxy, trifluormethyl, phenyl, halo and dimethylamino;R.sub.2 may represent the group ##STR2## wherein R.sub.7 is hydrogen or methyl and R.sub.8 is a (C.sub.1-4)alkyl radical, the group R.sub.5.sup.--CO or the group R.sub.6.sup.-- SO.sub.2 in which R.sub.5 and R.sub.6 are defined as above, or R.sub.7 and R.sub.8 taken together may represent a further bond between the carbon and oxygen atom;R.sub.3 and R.sub.4 are independently selected from hydrogen, halo, (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy;R.sub.1 and R.sub.4 taken together may also repesent a methylenedioxy group; with the provison that, when R represents hydrogen, R.sub.2 must be the group ##STR3## in which R.sub.8 must be the group R.sub.6.sup.--SO.sub.2 wherein R.sub.6 is as above defined; and salts therewith of pharmaceutically acceptable acids. The compounds possess antireproductive utility.
摘要翻译：式Ⅰ的新的酰基-1H-1,2,4-三唑衍生物，其中R可以位于两个相邻的氮原子之一上并且可以代表氢; 其中R 5选自（C 1-4）烷基，（C 2-4）烯基，（C 2-4）炔基，苯基，被一至三个独立地选自卤素，（C 1-4）烷基，（C 1-4）烷氧基，三氟甲基，氰基，硝基，氨基，二 - （C 1-4）烷基氨基，（C 2-4）酰氨基和亚甲二氧基，苄基，肉桂基，氨基，（C 1-4）烷基氨基，（C 1 -C 4）烷基氨基，苯基氨基，苯基氨基，其中苯环可以被一至三个独立地选自卤素，（C 1-4）烷基，（C 1-4）烷氧基，三氟甲基，氰基，硝基，氨基，二 - （C 1-4）烷基氨基，（C 2-4）酰氨基和甲基二氧基，卤代（C 1-4）烷基，（C 1-4）烷氧基和苄氧基; 基团R6-SO2，其中R6可以表示（C1-4）烷基，苯基，被选自（C1-4）烷基和（C1-4）烷氧基的基团取代的苯基或苯甲酰基; R 1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，卤素和二甲基氨基; R 2可以表示基团，其中R 7是氢或甲基，R 8是（C 1-4）烷基，R 5 -CO或其中R 5和R 6如上所定义的基团R 6 -SO 2，或R 7和一起可以代表碳和氧原子之间的另一个键; R 3和R 4独立地选自氢，卤素，（C 1-4）烷基和（C 1-4）烷氧基; R 1和R 4一起也可以代替亚甲二氧基; 当R表示氢时，R2必须是其中R8必须是R6-SO2的基团，其中R6如上所定义; 以及其与药学上可接受的酸的盐。该化合物具有抗生素效用。

7. 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。

8. 发明授权

US4576746A Novel .beta.-lactam acetic acid derivatives 失效
标题翻译：新型β-内酰胺乙酸衍生物
公开(公告)号：US4576746A
公开(公告)日：1986-03-18
申请号：US354572
申请日：1982-03-04
申请人： Duccio Favara , Amedeo Omodei-Sale' , Pietro Consonni
发明人： Duccio Favara , Amedeo Omodei-Sale' , Pietro Consonni
IPC分类号： C07D205/08 , C07D477/00 , C07D477/04 , C07D487/04
CPC分类号： C07D477/04 , C07C67/343 , C07D205/08
摘要： New .beta.-lactam acetic acid derivatives I ##STR1## wherein R represents alkyl, alkyl substituted with amino, protected amino, mono- or di-alkylamino, hydroxy, protected hydroxy or alkoxy, and alkenyl, and their salts are useful as intermediates for preparing 1-azabicyclo [3.2.0]hept-2-ene antibiotics II ##STR2## The process for preparing the .beta.-lactam acetic acid derivatives I as well as the overall process which starting from the acids I leads to the antibiotics II are also claimed.
摘要翻译：新的β-内酰胺乙酸衍生物I其中R代表烷基，被氨基，被保护的氨基，一或二 - 烷基氨基，羟基，被保护的羟基或烷氧基和烯基取代的烷基及其盐可用作制备1-氮杂双环[3.2.0]庚-2-烯抗生素II制备β-内酰胺乙酸衍生物I的方法以及从酸I引入抗生素II开始的总体方法是也声称。

9. 发明授权

US4459302A Acyl-1H-1,2,4-triazole derivatives 失效
公开(公告)号：US4459302A
公开(公告)日：1984-07-10
申请号：US87375
申请日：1979-10-23
申请人： Amedeo Omodei-Sale , Pietro Consonni , Giulio Galliani
发明人： Amedeo Omodei-Sale , Pietro Consonni , Giulio Galliani
IPC分类号： A61K31/41 , C07D233/54 , C07D249/08 , C07D249/12 , C07D405/04
CPC分类号： C07D233/64 , C07D233/54 , C07D249/08 , Y10S514/841
摘要： New acyl-1H-1,2,4-triazole derivatives of the formula ##STR1## wherein R may be located on one of the two adjacent nitrogen atoms and may represent hydrogen; a group R.sub.5 -CO wherein R.sub.5 is selected from (C.sub.1-4)alkyl, (C.sub.2-4)alkenyl, (C.sub.2-4)alkynyl, phenyl, phenyl substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylenedioxy, benzyl, cinnamyl, amino, (C.sub.1-4)alkylamino, di-(C.sub.1 -C.sub.4)alkylamino, phenylamino, phenylamino wherein the phenyl ring may be substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylenedioxy, halo(C.sub.1-4)alkyl, (C.sub.1-4)alkoxy and benzyloxy;a group R.sub.6 -SO.sub.2 wherein R.sub.6 may represent (C.sub.1-4)alkyl, phenyl, phenyl substituted by a radical selected from (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy, or phenacyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, halo and dimethylamino;R.sub.2 may represent a (C.sub.1-4)alkyl radical or the group ##STR2## wherein R.sub.7 is hydrogen or methyl and R.sub.8 is a (C.sub.1-4)alkyl radical, the group R.sub.5 -CO or the group R.sub.6 -SO.sub.2 in which R.sub.5 and R.sub.6 are defined as above, or R.sub.7 and R.sub.8 taken together may represent a further bond between the carbon and oxygen atom;R.sub.3 and R.sub.4 are independently selected from hydrogen, halo, (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy;R.sub.1 and R.sub.4 taken together may also represent a methylenedioxy group; with the proviso that, when R represents hydrogen, R.sub.2 must be the group ##STR3## in which R.sub.8 must be the group R.sub.5 -CO or the group R.sub.6 -SO.sub.2 wherein R.sub.5 and R.sub.6 are as above defined;and salts therewith of pharmaceutically acceptable acids. The compounds possess antireproductive utility.

10. 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。

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