摘要:
The present invention discloses new processes in the preparation of midazolam (VII), ##STR1## a commercially important pharmaceutical, as well a new intermediates in those processes from a known benzophenone (I) starting material.
摘要:
##STR1## Compounds of formula (I), and salts and prodrugs thereof, wherein X is O,S,NR 4 or CH 2 ; R 1 represents H, certain optionally substituted C 1-6 alkyl, or C 3-7 cycloalkyl; R 2 represents phenyl having certain optional substituents; R 3 represents C 1-6 alkyl, halo or NR 6 R 7 ; m is 2,3 or 4; n is 1,2,3,4,5,6 7 or 8 when X is CH 2 or 2,3,4,5,6,7 or 8 when X is O, S or NR 4 ; and x is 0,1,2, or 3; are CCK and/or gastrin antagonists. They and compositions thereof are therefore useful in therapy.
摘要翻译:式(I)化合物及其盐和前体药物,其中X为O,S,NR4或CH2; R1表示H,某些任选取代的C 1-6烷基或C 3-7环烷基; R2表示具有某些任选取代基的苯基; R 3表示C 1-6烷基,卤代或NR 6 R 7; m是2,3或4; 当X为CH 2时,n为1,2,3,4,5,6,7或8,X为O,S或NR4时为2,3,4,5,6,7或8; x为0,1,2或3; 是CCK和/或胃泌素拮抗剂。 因此,它们及其组合物可用于治疗。
摘要:
Novel 2-substituted-aminomethyl-1,4-benzodiazepines which have been found to be antagonists of the function of cholecystokinins (CCK), to the preparation of these compounds, and to the use of these compounds to antagonize the function of CCK, which antagonism is useful, e.g., for the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems of mammals, especially of humans.
摘要:
Novel imidazobenzodiazepines and their analogs are useful as anticonvulsants, muscle relaxant, anxiolytic and sedative agents. Preferred compounds of this class belong to the imidazo[1,5-a][1,4]diazepine series which may have a very wide variety of organic substituents. As especially preferred genus included within the purview of the invention encompasses a compound of the formula ##STR1## wherein R.sub.1 is hydrogen and lower alkyl, preferably methyl; R.sub.3 and R.sub.5 are hydrogen; R.sub.4 is hydrogen, nitro and halogen, most preferably chlorine, and in a most preferred embodiment when positioned on the fused benzo portion of the imidazobenzodiazepine is in the 8-position thereof. R.sub.6 is phenyl or halo, nitro, or lower alkyl-substituted phenyl, preferably halo, with fluorine being the preferred halogen, the substituted fluoro being positioned in the 2-position of the phenyl moiety and R.sub.2 is hydrogen and lower alkyl.
摘要:
Novel Imidazobenzodiazepines and their analogs are useful as anticonvulsants, muscle relaxant, anxiolytic and sedative agents. Preferred compounds of this class belong to the imidazo[1,5-a][1,4]diazepine series which may have a very wide variety of organic substituents. An especially preferred genus included within the purview of the invention encompasses a compound of the formula ##STR1## wherein R.sub.1 is hydrogen and lower alkyl preferably methyl; R.sub.3 and R.sub.5 are hydrogen; R.sub.4 is hydrogen, nitro and halogen, most preferably, chlorine, and in a most preferred embodiment when positioned on the fused benzo portion of the imidazobenzodiazepine is in the 8-position thereof, R.sub.6 is phenyl or halo, nitro, or lower alkyl-substituted phenyl, preferably, halo, with fluorine being the preferred halogen, the substituted fluoro being positioned in the 2-position of the phenyl moiety and R.sub.2 is hydrogen and lower alkyl.
摘要:
Novel aldehyde adducts of 1,4-benzodiazepine-4-oxides, novel azeto-�1,4!-benzodiazepine derivatives derived therefrom, acid addition salts thereof and methods for their preparation. The aldehyde adducts have the general formula I; the azeto-�1,4!-benzodiazepine derivatives have the general formula III. ##STR1##
摘要:
Compounds of the formula ##STR1## wherein R.sub.2 is lower alkyl and each of rings A and B is unsubstituted or substituted by a member selected from the group consisting of nitro, trifluoromethyl, halogen, alkyl and alkoxy, and processes for their preparation.
摘要:
1,5-Benzodiazocines of the general formula ##STR1## their 5N-oxides, and acid addition salts thereof. In the above formula R.sub.1 =H, Halogen, CF.sub.3, --CN, --NO, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 alkylthio; R.sub.2 =H, C.sub.1-6 alkyl or furyl; R.sub.3 =H, C.sub.1-6 alkyl, hydroxy-(C.sub.1-6 alkyl), C.sub.2-6 alkenyl or benzyl; and R.sub.4 =phenyl, (C.sub.1-6 alkyl)-phenyl, nitrophenyl, halophenyl or pyridyl. Also the production of such compounds from compounds of the benzodiazepine series.