Benzimidazole is a heterocyclic aromaticorganic compound. IUPAC nomenclature is a systematic way of naming organic chemical compounds. ... A chemical formula (also called molecular formula) is a concise way of expressing information about the atoms that constitute a particular chemical compound. ... The molecular mass of a substance (less accurately called molecular weight and abbreviated as MW) is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... The melting point of a solid is the temperature at which it changes state from solid to liquid. ... Alternate use: Boiling point Boiling Point, known in Japan as 3-4X Jūgatsu (3-4X10月 lit. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences and alloys. ... The simplified molecular input line entry specification or SMILES is a specification for unambiguously describing the structure of chemical molecules using short ASCII alpha-numeric strings. ... Heterocyclic compounds are substances which contain a ring structure as found in benzene and the aromatic compounds, or aromatic hydrocarbons, but in which other atoms than carbon, such as sulfur, oxygen or nitrogen are found as part of the ring. ... In chemistry, an aromatic molecule is one in which electrons are free to cycle around circular arrangements of atoms, which are alternately singly and doubly bonded to one another. ... An organic compound is any of a large class of chemical compounds whose molecules contain carbon, with exception of carbides, carbonates and carbon oxides. ...
Novel benzimidazole derivatives represented by the formula (I): ##STR1## wherein R.sub.3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable salts.
The benzimidazole derivative or its pharmaceutically acceptable salt of claim 1, wherein said derivative is selected from the group consisting of 6-benzenesulfonylcarbamoyl-1-(2-chlorobenzyl)-2-methylbenzimidazole, 1-(biphenyl-4-ylmethyl)-6-(1-butanesulfonylcarbamoyl)-2-methylbenzimidazol e, 1-(biphenyl-4-ylmethyl)-6-(1-butanesulfonylcarbamoyl)-2-ethylbenzimidazole, 6-benzenesulfonylcarbamoyl-2-cyclopropyl-1-(2-fluorobenzyl)benzimidazole, 6-benzenesulfonylcarbamoyl-1-(2,4-dichlorobenzyl)-2-methylbenzimidazole, 6-benzenesulfonylcarbamoyl-1-(2,4-difluorobenzyl-2-methylbenzimidazole, 6-(1-butanesulfonylcarbamoyl)-1-[(3-fluorobiphenyl-4-yl)methyl]-2-methylbe nzimidazole, 1-(2,4-dichlorobenzyl)-2-methyl-6-(1-pentanesulfonylcarbamoyl)benzimidazol e, and 1-(4-biphenylmethyl)-2-ethyl-6-(1-pentanesulfonylcarbamoyl)benzimidazole.
The compound of formula (24) may be converted into a benzimidazole compound of formula (25) in the same manner as in the step (e) of converting the compound of formula (20) into the compound of formula (21).
It is therefore an object of the present invention to provide a percutaneous preparation superior in percutaneous absorption of benzimidazole compound and duration of efficacy, that exhibits an improved stability of the benzimidazole compound (which is as an active ingredient) in the preparation.
When a pharmacologically acceptable acid addition salt of the benzimidazole compound is used, an organic base (e.g., ethanolamine and the like) or an inorganic base (e.g., sodium hydroxide and sodium carbonate and the like) may be concurrently added to the adhesive layer, whereby said acid addition salt becomes a free base in the adhesive layer.
The 2-mercaptobenzimidazole inhibits reactions between the benzimidazole compound and the components contained in the adhesive in trace amounts, thereby affording an improved stability of the benzimidazole compound in the preparation.