公开(公告)号：US4663330A

公开(公告)日：1987-05-05

申请号：US744213

申请日：1985-06-13

申请人： Maurice Prost ,  Michel de Claviere ,  Peter Polster

发明人： Maurice Prost ,  Michel de Claviere ,  Peter Polster

IPC分类号： C07D215/22 ,  A61K31/47 ,  A61P3/00 ,  A61P9/00 ,  C07D215/233 ,  C07D317/00 ,  C07D405/12

CPC分类号： C07D215/233

摘要： The invention relates to novel decahydroquinolinol derivatives represented by the general formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, in which X represents oxygen or sulphur, R represents an alkyl radical having from 1 to 3 carbon atoms, R.sub.1 represents fluorine, chlorine, bromine or methoxy, R.sub.2 represents hydrogen or methoxy or R.sub.1 and R.sub.2, when they are taken together, represent a 2,3-methylenedioxy or 3,4-methylenedioxy radical.The compounds of the invention are inhibitors of calcium translocation at the level of the cell membrane and are useful more particularly in the treatment of pathological syndromes of the cardiovascular system such as, for instance, angina pectoris.

摘要翻译： 本发明涉及由以下通式表示的新型十氢喹啉醇衍生物：其中X代表氧或硫，R代表具有1至3个碳原子的烷基，R1代表氟，氯 ，溴或甲氧基，R 2表示氢或甲氧基或R 1和R 2，当它们一起时，表示2,3-亚甲二氧基或3,4-亚甲二氧基。 本发明的化合物是细胞膜水平的钙易位的抑制剂，并且更具体地用于治疗心血管系统的病理综合征，例如心绞痛。

公开(公告)号：US4332805A

公开(公告)日：1982-06-01

申请号：US184129

申请日：1980-09-04

申请人： Maurice Prost ,  Michel de Claviere

发明人： Maurice Prost ,  Michel de Claviere

IPC分类号： C07D215/22 ,  A61K31/47 ,  A61P9/06 ,  A61P9/10 ,  A61P25/02 ,  C07D215/02 ,  C07D215/233

CPC分类号： C07D215/233 ,  Y10S514/818 ,  Y10S514/821

摘要： Decahydroquinolinol derivatives corresponding to the general formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, in which R.sup.1 represents hydrogen, a methyl, ethyl, n-propyl, n-butyl or phenyl radical or a phenyl radical having one substituent or two identical or different substituents selected from chlorine, bromine atoms and a methyl group.Ar represents a phenyl or naphthyl radical or a phenyl radical having one substituent or two identical or different substituents selected from fluorine, chlorine and bromine atoms and methyl, methoxy, acetyl and cyano groups,X represents oxygen or sulfur,n represents 2 or 3.They are useful as antiarrhthmic and local anaesthetic agents.

摘要翻译： 对应于以下通式的十氢喹啉醇衍生物：其中R 1表示氢，甲基，乙基，正丙基，正丁基或苯基或具有一个取代基或两个相同的苯基 或选自氯，溴原子和甲基的不同取代基。 Ar表示苯基或萘基或具有一个取代基或两个相同或不同的选自氟，氯和溴原子的取代基的苯基，甲基，甲氧基，乙酰基和氰基，X表示氧或硫，n表示2或3。 它们可用作抗惊厥和局部麻醉剂。

公开(公告)号：US4173636A

公开(公告)日：1979-11-06

申请号：US884705

申请日：1978-03-08

申请人： Maurice Prost

发明人： Maurice Prost

IPC分类号： C07D215/42 ,  C07D215/44 ,  A61K31/47

CPC分类号： C07D215/42 ,  C07D215/44 ,  Y10S514/929

摘要： The invention relates to decahydroquinoline derivatives represented by the general formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein R.sup.1 represents an alkyl or alkoxy group, a lower dialkylamino group, an optionally substituted phenyl group, a heterocyclic group; R.sup.2 represents an alkyl group, an optionally substituted phenyl group, a naphthyl group, an unsaturated heterocyclic group, an aralkyl group or an alicyclic group; and R.sup.3 represents a substituted furyl group, an aralkyl group or a group represented by the general formula: ##STR2## wherein A represents an alkylene group; Y represents an oxygen or sulphur atom, a carbonyl, carbonyl-hydroxyimino, carbonyl-hydrazono or sulphoxide group, or a group; ##STR3## n is O or an integer of from 1 to 4, with the proviso that when n is O, Y represents a carbonyl group; and R.sup.4 and R.sup.5, which are identical or different, each represent hydrogen, a halogen atom or a methyl, methoxy or acetyl group.Certain compounds of formula I have been found to possess useful analgesic properties while others have been found to be potentially useful in the treatment of high blood pressure.

摘要翻译： 本发明涉及由以下通式表示的十氢喹啉衍生物及其药学上可接受的酸加成盐，其中R1表示烷基或烷氧基，低级二烷基氨基，任意取代的苯基，杂环基; R2表示烷基，任选取代的苯基，萘基，不饱和杂环基，芳烷基或脂环族基; R 3表示取代的呋喃基，芳烷基或由以下通式表示的基团：其中A表示亚烷基; Y表示氧或硫原子，羰基，羰基 - 羟基亚氨基，羰基 - 亚氨基或亚砜基或基团; n为0或1〜4的整数，条件是当n为O时，Y表示羰基; 和相同或不同的R 4和R 5各自表示氢，卤素原子或甲基，甲氧基或乙酰基。 已经发现某些式I化合物具有有用的镇痛特性，而其他已被发现可能有用于治疗高血压。