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公开(公告)号:US4526892A
公开(公告)日:1985-07-02
申请号:US448364
申请日:1982-12-09
申请人: Patricia Salvati , Anna M. Caravaggi , Aldemio Temperilli , Germano Bosisio , Osvaldo Sapini , Enrico di Salle
发明人: Patricia Salvati , Anna M. Caravaggi , Aldemio Temperilli , Germano Bosisio , Osvaldo Sapini , Enrico di Salle
IPC分类号: C07D457/06 , A61K31/48
CPC分类号: C07D457/06
摘要: Novel ergoline derivatives formed by reaction of an 8-carboxy ergoline with a carbodiimide and having hypotensive and antiprolatinic activity.
摘要翻译: 通过8-羧基麦角灵与碳二亚胺的反应形成的具有降血压和抗抑素活性的新型麦角灵衍生物。
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公开(公告)号:US4317912A
公开(公告)日:1982-03-02
申请号:US129333
申请日:1980-03-11
IPC分类号: C07D457/02 , A61K31/40 , A61K31/48 , A61P9/12 , C07D487/06 , A61K31/445 , A61K31/535 , C07D487/00
CPC分类号: C07D487/06
摘要: A compound is disclosed of the formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom, or a carboxy, alkoxycarbonyl, piperidinocarbonyl, 1-pyrrolidinylcarbonyl, morpholinocarbonyl, carbamoyl or benzylcarbamoyl group, or an alkylcarbamoyl or dialkylcarbamoyl group in which the, or each, alkyl group has from 1 to 4 carbon atoms;R.sub.2 represents a hydrogen or fluorine atom, or a cyano, acetyl or carbamoyl group; andR.sub.3 represents a hydrogen atom or a methyl group; and represents a single or a double bond, with the proviso that R.sub.1 and R.sub.2 do not simultaneously represent hydrogen atoms;or a pharmaceutically acceptable salt thereof.
摘要翻译: 公开了式(I)的化合物:其中R 1表示氢原子,或羧基,烷氧基羰基,哌啶子基羰基,1-吡咯烷基羰基,吗啉代羰基,氨基甲酰基或苄基氨基甲酰基,或烷基氨基甲酰基或二烷基氨基甲酰基 其中或每个烷基具有1至4个碳原子; R2表示氢或氟原子,或氰基,乙酰基或氨基甲酰基; 并且R 3表示氢原子或甲基; 并且表示单键或双键,条件是R1和R2不同时表示氢原子; 或其药学上可接受的盐。
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公开(公告)号:US4321381A
公开(公告)日:1982-03-23
申请号:US188620
申请日:1980-09-19
IPC分类号: C07D457/04 , A61K31/48 , A61P9/12 , C07D457/02 , A61K31/495
CPC分类号: C07D457/02
摘要: Compounds and process for making same are disclosed, the compounds having the formula (I): ##STR1## wherein R.sub.1 represents methyl, phenyl, piperidino, 1-pyrrolidinyl, morpholino or 4-methyl-1-piperazinyl, alkyl or alkoxy having from 1 to 4 carbon atoms, amino, substituted amino of the formula NHR' (wherein R' is alkyl having from 1 to 4 carbon atoms, cycloalkyl, a benzyl, or phenyl) or substituted amino of the formula NR" R"' (wherein R" and R"' both represent alkyl having from 1 to 4 carbon atoms);R.sub.2 represents a hydrogen atom, alkyl having from 1 to 4 carbon atoms, or phenyl;R.sub.3 represents a fluorine atom, cyano, difluoromethyl, difluorobromomethyl, trifluoromethyl, methylthio, methylsulphonyl, sulphonamido, an alkoxy having from 1 to 4 carbon atoms, an alkanoyl having from 2 to 5 carbon atoms, or benzoyl;R.sub.4 represents a hydrocarbon having from 1 to 4 carbon atoms;R.sub.5 represents a hydrogen atom or methoxy;R.sub.6 represents a hydrogen or halogen atom or methyl; andR.sub.7 represents a hydrogen atom or methyl. The 2-cyano derivatives are especially preferred.The compounds are useful as antihypertensive agents.
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公开(公告)号:US4252941A
公开(公告)日:1981-02-24
申请号:US72289
申请日:1979-09-04
IPC分类号: C07D457/04 , A61K31/48 , A61P9/12 , C07D457/02
CPC分类号: C07D457/02
摘要: Compounds and process for making same are disclosed, the compounds having the formula (I): ##STR1## wherein R.sub.1 represents a methyl, phenyl, piperidino, 1-pyrrolidinyl, morpholino or 4-methyl-1-piperazinyl group, an alkyl or alkoxy group having from 1 to 4 carbon atoms, an amino group, a substituted amino group of the formula NHR' (wherein R' represents an alkyl group having from 1 to 4 carbon atoms, a cycloalkyl group, a benzyl group, or a phenyl group) or a substituted amino group of the formula NR" R"' (wherein R" and R"' both represent alkyl groups having from 1 to 4 carbon atoms);R.sub.2 represents a hydrogen atom, an alkyl group having from 1 to 4 carbon atoms, or a phenyl group;R.sub.3 represents a fluorine atom, a cyano, difluoromethyl, difluorobromomethyl, trifluoromethyl, methylthio, methylsulphonyl, or sulphonamido group, an alkoxy group having from 1 to 4 carbon atoms, an acyl group having from 2 to 4 carbon atoms, or a benzoyl group;R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms;R.sub.5 represents a hydrogen atom or a methoxy group;R.sub.6 represents a hydrogen or halogen atom or a methyl group; andR.sub.7 represents a hydrogen atom or a methyl group.The 2-cyano derivatives are especially preferred.
摘要翻译: 公开了化合物及其制备方法,具有式(I)的化合物:其中R 1表示甲基,苯基,哌啶子基,1-吡咯烷基,吗啉代或4-甲基-1-哌嗪基, 具有1至4个碳原子的烷基或烷氧基,氨基,式NHR'的取代氨基(其中R'表示具有1至4个碳原子的烷基,环烷基,苄基或 苯基)或式NR“R”'的取代氨基(其中R“和R”“均表示具有1至4个碳原子的烷基); R2表示氢原子,具有1至4个碳原子的烷基或苯基; R 3表示氟原子,氰基,二氟甲基,二氟溴甲基,三氟甲基,甲硫基,甲磺酰基或磺酰胺基,具有1至4个碳原子的烷氧基,具有2至4个碳原子的酰基或苯甲酰基; R4表示具有1至4个碳原子的烃基; R5表示氢原子或甲氧基; R6表示氢或卤素原子或甲基; 并且R 7表示氢原子或甲基。 2-氰基衍生物是特别优选的。
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