公开(公告)号：US4675404A

公开(公告)日：1987-06-23

申请号：US885315

申请日：1986-07-14

申请人： Luigi Bernardi ,  Aldemio Temperilli ,  Germano Bosisio ,  Gabriella Traquandi ,  Rosanna Eccel ,  Alessandro Rossi ,  Patricia Salvati

发明人： Luigi Bernardi ,  Aldemio Temperilli ,  Germano Bosisio ,  Gabriella Traquandi ,  Rosanna Eccel ,  Alessandro Rossi ,  Patricia Salvati

IPC分类号： C07D457/02 ,  C07D457/06 ,  A61K31/48

CPC分类号： C07D457/06 ,  C07D457/02

摘要： Ergoline derivatives of formula: ##STR1## wherein n=0,1,2; R.sub.1 =H, CH.sub.3 ; R.sub.2 =H, CH.sub.3, halogen; R.sub.3 =H, OCH.sub.3 ; R.sub.4 =hydrocarbon group and R.sub.5 is a residue of general formula II, III, IV, V, VI, VII: ##STR2## wherein R.sub.6 =H, Cl, OCH.sub.3, NR.sub.11 R.sub.12, wherein R.sub.11 and R.sub.12 =H, lower alkyl; phenyl or are bonded together to form a heterocyclic ring, R.sub.7, R.sub.8 and R.sub.9 and R.sub.10 =H or C.sub.1 -C.sub.3 alkyl, with the proviso that if R.sub.5 is of formula II and R.sub.2 =R.sub.7 =R.sub.8 =H, then R.sub.4 is not methyl or n is not 0.Pharmaceutically acceptable acid addition salts are also provided. A method for their preparation is also provided.The compounds have anti-depressive, anti-hypertensive and antiprolactin activity.

摘要翻译： 式：其中n = 0,1,2; R1 = H，CH3; R2 = H，CH3，卤素; R3 = H，OCH3; R4 =烃基，R5是通式Ⅱ，Ⅲ，Ⅳ，Ⅴ，Ⅵ，Ⅶ的残基：其中R6 = H，Cl，OCH3，NR11R12，其中R11和R12 = H，低级烷基; 苯基或键合在一起形成杂环，R 7，R 8和R 9和R 10 = H或C 1 -C 3烷基，条件是如果R 5为式II且R 2 = R 7 = R 8 = H，则R 4不是甲基 或n不为0.还提供药学上可接受的酸加成盐。 还提供了它们的制备方法。 该化合物具有抗抑郁，抗高血压和抗催乳素活性。

公开(公告)号：US4801588A

公开(公告)日：1989-01-31

申请号：US73438

申请日：1987-07-15

申请人： Aldemio Temperilli ,  Rosanna Eccel ,  Enzo Brambilla ,  Patricia Salvati

发明人： Aldemio Temperilli ,  Rosanna Eccel ,  Enzo Brambilla ,  Patricia Salvati

IPC分类号： C07D487/04 ,  A61K31/40 ,  A61P9/12 ,  C07D457/02 ,  C07D487/06 ,  A61K31/415 ,  C07D487/02

CPC分类号： C07D487/06

摘要： Compounds of the formula I: ##STR1## wherein R.sub.1 =H, CH.sub.3 ; m=0,1; R.sub.2 =R.sub.3 =H or R.sub.2, R.sub.3 =bond, R.sub.4 =C.sub.1 -C.sub.4 hydrocarbon, n=1 or 2 and their pharmaceutically acceptable salts are antihypertensive agents. Their preparation and pharmaceutical compositions containing them are also described.

摘要翻译： 式I的化合物：其中R 1 = H，CH 3; m = 0,1; R2 = R3 = H或R2，R3 =键，R4 = C1-C4烃，n = 1或2，其药学上可接受的盐是抗高血压药。 还描述了它们的制备方法和含有它们的药物组合物。