摘要:
A pharmaceutical composition is disclosed which comprises a physiologically active substance other than insulin possessing peptide bonds in its structure and being inactivable by digestive enzymes, and a synthetic chymotrypsin inhibitor. The composition is particularly suitable for intestinal absorption of the active substance.
摘要:
Benzoylpiperazine esters and acid addition salts thereof are disclosed, which esters have the following formula: wherein A represents a single bond or an alkylene group, vinylene group, -O-alkylene group or methine group, R 1 represents a bicyclic carbon ring residue which may be substituted with a lower alkyl group, lower alkoxy group, oxo group or nitro group or a halogen atom, or may be partially saturated; a fluorene residue which may contain an oxo group; a fluorenylidene group; an anthracene residue; a phenathrene residue which may be substituted with a lower alkyl group, or may be partially saturated; a benzofuran residue or thianaphthene residue which may be substituted with a lower alkyl group or lower alkoxy group; a benzopyran residue or benzoazine residue which may be substituted with an oxo group or phenyl group and partially saturated; a phthalimide residue; a benzodiazine residue; an isooxazole residue which may be substituted with a lower alkyl group or phenyl group; or an alkylene dioxybenzene residue or xanthene residue; and R 2 represents an alkyl group, cycloalkyl group, cycloalkylalkyl group or aralkyl group; except the case where A is a single bond, R l is and R 2 is a methyl group. The esters exhibit excellent chymotrypsin inhibitive activity.
摘要:
A pharmaceutical composition is disclosed which comprises a physiologically active substance other than insulin possessing peptide bonds in its structure and being inactivable by digestive enzymes, and a synthetic chymotrypsin inhibitor. The composition is particularly suitable for intestinal absorption of the active substance.
摘要:
Benzopyrans represented by the formula wherein A represents a direct bond or -CH 2 O-
R 1 represents a C 3 -C 5 alkyl group, a hydroxy-(C 3 -C 5 alkyl) group, a lower alkyl-amino-lower alkyl group, a ni- trato-(C 3 -C 5 alkyl) group or a phenyl-(C 1 -C 5 ) alkyl group where the phenyl may be substituted by a lower alkoxy group, R 2 represents hydrogen, halogen, OH, N0 2 , a carbamoyl group, a lower alkyl group, a lower alkoxy group, a lower alkyleneoxy group or an acetyl group, R 3 represents hydrogen or N0 2 , B represents a direct bond, a C 1 -C 7 alkylene group, a -O-lower alkylene group or a -CONH-lower alkylene group, and n represents 1 or 2; and their acid addition salts are useful, for example, in reducing heart beat rate, myocardial oxygen consumption and blood pressure.
摘要:
The invention provides compounds of the formula wherein A represents a direct bond or the group -O-CH 2 -,
B represents a C 1 -C 11 alkylene group bonded to a carbon atom of the aromatic ring D either directly or through -O-, -S-, -SO- or -NH-, W represents a carbon or nitrogen atom, R, represents a C 1 -C 7 alkyl group, a hydroxy-C 1 -C 6 alkyl group, or a phenyl- or diphenyl- alkyl group with the alkyl group having 1 to 4 carbon atoms, R 2 represents hydrogen, halogen, OH, C 1 -C 4 alkyl, N0 2 , C 1 -C 4 alkoxy, acetyl, allyloxy, carbamoyl or sulfamoyl, and when two or more R 2 groups exist, they may be idential or different, and n represents 1, 2 or 3 and m represents 1 or 2, provided that n + m > 4; and acid addition salts thereof; processes for producing them; and pharmaceutical compositions comprising them for use in the treatment of diseases of the cardiovascular system.
摘要:
An antiatherosclerotic agent comprises as active ingredient dilazep or its acid addition salt. The agent may also include acetylsalicylic acid as a further active agent.
摘要:
Benzoylpiperazine esters and acid addition salts thereof are disclosed, which esters have the following formula: wherein A represents a single bond or an alkylene group, vinylene group, -O-alkylene group or methine group, R 1 represents a bicyclic carbon ring residue which may be substituted with a lower alkyl group, lower alkoxy group, oxo group or nitro group or a halogen atom, or may be partially saturated; a fluorene residue which may contain an oxo group; a fluorenylidene group; an anthracene residue; a phenathrene residue which may be substituted with a lower alkyl group, or may be partially saturated; a benzofuran residue or thianaphthene residue which may be substituted with a lower alkyl group or lower alkoxy group; a benzopyran residue or benzoazine residue which may be substituted with an oxo group or phenyl group and partially saturated; a phthalimide residue; a benzodiazine residue; an isooxazole residue which may be substituted with a lower alkyl group or phenyl group; or an alkylene dioxybenzene residue or xanthene residue; and R 2 represents an alkyl group, cycloalkyl group, cycloalkylalkyl group or aralkyl group; except the case where A is a single bond, R l is and R 2 is a methyl group. The esters exhibit excellent chymotrypsin inhibitive activity.