公开(公告)号：US4737505A

公开(公告)日：1988-04-12

申请号：US757515

申请日：1985-07-19

申请人： Jacques Guillaume ,  Francois Clemence ,  Lucien Nedelec ,  Francoise DeLevallee

发明人： Jacques Guillaume ,  Francois Clemence ,  Lucien Nedelec ,  Francoise DeLevallee

IPC分类号： A61K31/44 ,  A61K31/4427 ,  A61K31/445 ,  A61P25/04 ,  C07D401/04

CPC分类号： C07D401/04

摘要： Novel indole of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 12 carbon atoms, Z is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms, cyanoalkyl of 3 to 8 carbon atoms, hydroxyalkyl of 2 to 8 carbon atoms, --(CH.sub.2).sub.n --O--B, ##STR2## aralkyl of 7 to 12 carbon atoms optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --OH, CF.sub.3 --, CF.sub.3 O--, --NH.sub.2 and --NO.sub.2 and cycloalkyl alkyl of 4 to 12 carbon atoms, n is one integer from 2 to 8, B is selected from the group consisting of aryl and heteroaryl, both optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --OH, hydroxyalkyl of 1 to 5 carbon atoms, nitro, amino, CF.sub.3 --, alkenyl and alkenyloxy of 2 to 5 carbon atoms and alkynyl and alkynyloxy of 2 to 5 carbon atoms, a and b are both hydrogen or a is hydrogen and b is --OH or alkoxy of 1 to 8 carbon atoms or a and b together form a carbon-carbon bond and the 2-oxo with dotted lines indicates its possible presence with the double bond in the indole ring missing and its non-toxic, pharmaceutically acceptable acid addition salts having analgesic activity of the morphine type.

摘要翻译： 其中R选自氢，1至8个碳原子的烷基和7至12个碳原子的芳烷基的式VI的新型吲哚，Z选自氢，1至 具有2至8个碳原子的烯基，3至8个碳原子的氰基烷基，2至8个碳原子的羟烷基， - （CH 2）n OB，7-12个碳原子的芳基，其任选被至少一个 由1至5个碳原子的烷基和烷氧基组成的组，卤素，-OH，CF 3 - ，CF 3 O-，-NH 2和-NO 2以及4至12个碳原子的环烷基烷基，n是2至8的一个整数 B选自芳基和杂芳基，两者任选被至少一个由1至5个碳原子的烷基和烷氧基组成的组中的一个取代，卤素，-OH，1-5个碳原子的羟基烷基，硝基 ，2至5个碳原子的氨基，CF 3 - ，链烯基和烯氧基以及2至5个碳原子的炔基和炔氧基，a和ba 氢或a是氢并且b是-OH或1-8个碳原子的烷氧基或a和b一起形成碳 - 碳键，并且具有虚线的2-氧代表示其在吲哚中可能存在双键 戒指及其无毒，药学上可接受的具有吗啡类止痛活性的酸加成盐。