摘要:
Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 7, 8, 9 or 10, and each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, --COOR.sup.5 where R.sup.5 is an ester group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl;R.sup.3 is nitrile, carboxy, --COOR.sup.8 where R.sup.8 is an ester group, or --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl; andR.sup.4 is --NR.sup.11 R.sup.12, --NR.sup.11 COR.sup.12, --N(COR.sup.11).sub.2 or --N.dbd.CHOCH.sub.2 R.sup.11 where R.sup.11 and R.sup.12 are each hydrogen or C.sub.1-4 alkyl optionally substituted with carboxy, --N.dbd.CH--NR.sup.13 R.sup.14 where R.sup.13 is hydrogen or C.sub.1-4 alkyl and R.sup.14 is C.sub.1-4 alkyl, optionally substituted phenyl or optionally substituted heteroaryl, ##STR2## where X is C.sub.2-4 alkylene, or --NHSO.sub.2 R.sup.15 where R.sup.15 is C.sub.1-4 alkyl, trifluoromethyl or optionally substituted phenyl; and salts thereof.
摘要翻译:其中n为0,1或2并且R 1连接在7,8,9或10位的任何位置的式“IMAGE”的药物化合物,并且每个R 1为卤素,羧基,三氟甲基,羟基,C 1-4烷基 C 1-4烷氧基,C 1-4烷硫基,羟基-C 1-4烷基,羟基-C 1-4烷氧基,含氮杂环基,硝基,三氟甲氧基,-COOR 5,其中R5是酯基,-COR6,-CONR6R7或 - NR 6 R 7,其中R 6和R 7各自为氢或C 1-4烷基; R 2是选自噻吩基,吡啶基,苯并噻吩基,喹啉基,苯并呋喃基或苯并咪唑基的苯基,萘基或杂芳基,所述苯基,萘基和杂芳基任选被取代,或R 2是任选被C 1-4烷基取代的呋喃基; R3是腈,羧基,-COOR8,其中R8是酯基,或-CONR9R10,其中R9和R10各自是氢或C1-4烷基; 并且R 4为-NR 11 R 12,-NR 11 COR 12,-N(COR 11)2或-N = CHOCH 2 R 11,其中R 11和R 12各自为氢或任选被羧基取代的C 1-4烷基,-N = CH-NR 13 R 14,其中R 13为氢或C1- 4烷基和R 14是C 1-4烷基,任选取代的苯基或任选取代的杂芳基,其中X是C 2-4亚烷基或-NHSO 2 R 15,其中R 15是C 1-4烷基,三氟甲基或任选取代的苯基; 及其盐。
摘要:
The present invention relates to compounds that modulate neurotransmission by promoting the release of neurotransmitters such as acetylcholine, dopamine and norepinephrine. More particularly, the present invention relates to thio-bridged aryl compounds that are capable of modulating acetylcholine receptors and pharmaceutical compositions comprising such compounds. The compounds disclosed are useful for the treatment of dysfunctions of the central and autonomic nervous systems.
摘要:
The present invention relates to compounds of the Formula (I) which are useful for treating conditions associated with mGluR3 receptors, such as depression, schizophrenia and migraine, pharmaceutical compositions thereof, and methods of using the same.
摘要:
The present invention relates to compounds of the Formula (I) which are useful for treating conditions associated with mGluR3 receptors, such as depression, schizophrenia and migraine, pharmaceutical compositions thereof, and methods of using the same.