摘要:
This invention provides novel compounds and pharmaceutical methods comprising the administration of a compound of the Formula I: ##STR1## wherein n, m, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are variables.
摘要:
This invention provides novel, optionally substituted tetrahydropyridoindoles which are useful serotonergic agents for the treatment of central nervous system disorders.
摘要:
Propanoic acid derivatives of the formula: ##STR1## where R.sup.1 is a C.sub.1-8 alkyl group optionally substituted by hydroxyl or --COOH and R.sup.2 is hydrogen or a protecting group, are useful as anti-thrombotic agents.
摘要:
Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, hydroxyl, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, acyloxy, --O-glucoside, optionally substituted phenyl or optionally substituted phenyl-C.sub.1-4 alkoxy;R.sup.3 istetrazolyl, orand R.sup.4 and R.sup.5 are each hydrogen, hydroxy, acyloxy, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halo, optionally substituted phenyl, --SO.sub.3 H or --NR'R" where R' and R" are each hydrogen or C.sub.1-4 alkyl;provided that when R.sup.3 is --CR'R".CHR'"CO.sub.2 H or tetrazolyl, R.sup.1 and R.sup.2 are each hydroxyl, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, acyloxy, --O-glucoside, optionally substituted phenyl or optionally substituted phenyl C.sub.1-4 alkoxy; andor a pharmaceutically acceptable salt or ester thereof.
摘要:
Methods of treating an immune disease, cell proliferation, restenosis and vascular smooth muscle cells using the pharmaceutical compounds of the formula ##STR1## in which 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; and salts thereof.
摘要:
This invention provides a method of treating diabetic complications in mammals which comprises the administration of a compound of the Formula I: ##STR1## in which n, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are variables.
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 alkyl 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 alkyl 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:式“IMAGE”的药物化合物,其中n为0,1或2,R 1连接在7,8,9或10位的任何位置,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R 5为烷基,-COR 6,-CONR 6 R 7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; R 3是腈,羧基,-COOR 8,其中R 8是烷基,或-CONR 9 R 10,其中R 9和R 10各自是氢或C 1-4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:
This invention provides novel compounds and pharmaceutical methods comprising the administration of a compound of the Formula I: ##STR1## wherein n, m, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are variables.
摘要:
This invention provides a method of treating diabetic complications in mammals which comprises the administration of a compound of the Formula I: ##STR1## in which n, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are variables.
摘要:
A pharmaceutical compound of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 5, 6, 7, 8, 9 or 10, and each R.sup.1 is halo, trifluoromethyl, C.sub.1-4 alkoxy, hydroxy, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, trifluoromethoxy, carboxy, --COOR.sup.5 where R.sup.5 is an ester group, --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, --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl, or R.sup.11 SO.sub.2 -- where R.sup.11 is C.sub.1-4 alkyl or optionally substituted phenyl; and R.sup.4 is --NR.sup.12 R.sup.13, --NHCOR.sup.12, --N(COR.sup.12).sub.2 or --N.dbd.CHOCH.sub.2 R.sup.12 where R.sup.12 and R.sup.13 are each hydrogen or C.sub.1-4 alkyl optionally substituted with carboxy, ##STR2## where X is C.sub.2-4 alkylene, or --NHSO.sub.2 R.sup.14 where R.sup.14 is C.sub.1-4 alkyl or optionally substituted phenyl; provided that when n is 0, R.sup.3 is nitrile and R.sup.4 is --NH.sub.2, R.sup.2 is not phenyl or phenyl substituted in the para-position with a single chloro, hydroxy or methoxy substituent; and salts thereof.
摘要翻译:式(*化学结构*)(I)的药物化合物,其中n为0,1或2,R 1在任何位置5,6,7,8,9或10处连接,并且每个R 1为卤素 三氟甲基,C 1-4烷氧基,羟基,硝基,C 1-4烷基,C 1-4烷硫基,羟基-C 1-4烷基,羟基-C 1-4烷氧基,三氟甲氧基,羧基,-COOR 5,其中R 5为酯基, CONR 6 R 7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,-CONR9R10,其中R9和R10各自是氢或C1-4烷基,或R11SO2-,其中R11是C1-4烷基或任选取代的苯基; 并且R 4为-NR 12 R 13,-NHCOR 12,-N(COR 12)2或-N = CHOCH 2 R 12,其中R 12和R 13各自为氢或任选被羧基取代的C 1-4烷基,(*化学结构*)其中X为C 2-4亚烷基 或-NHSO 2 R 14,其中R 14是C 1-4烷基或任选取代的苯基; 条件是当n为0时,R3为腈,R4为-NH2,R2不为苯基或在对位被苯基取代的苯基与单个氯,羟基或甲氧基取代基取代; 及其盐。