Sulfonamide derivatives of the general formula (I): ##STR1## wherein preferably R.sup.1 represents a lower alkoxy group, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined in the specification, A and B may be the same or different from each other and each represents .dbd.N-- or .dbd.CH--, E represents an aromatic 6-membered cyclic group, which may have 1 or 2 nitrogen atoms in the ring, and may be substituted with 1 to 3 substituents which may be the same or different from one another with the proviso that a combination of R.sup.1 which is a hydrogen atom, lower alkyl group, nitro group or amino group which may be protected, R.sup.2 and R.sup.3 which are each a hydrogen atom, A and B which are each .dbd.CH-- and E which is a phenyl group which may be substituted with 1 to 3 substituents G which may be the same or different from one another is excluded, or pharmacologically acceptance salts of them.
The present invention provides a method for inhibiting tubulin polymerization and for treating rheumatism by administering to individuals in need thereof an effective amount of sulfonamide derivatives represented by the general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and each independently represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, a hydroxy group; each R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represents a hydrogen atom; A represents any group of (1) 5-membered heterocyclic group which is optionally substituted by a lower alkyl group or phenyl group, whose ring members include at least 1 nitrogen atom and may include any atom(s) selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom, (2) an alicyclic group which is optionally substituted by a lower alkyl group or phenyl group, and (3) an alicyclic group whose ring members include at least 1 nitrogen atom and may include any atom(s) selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom, or pharmaceutically acceptable salts thereof together with a pharmaceutically acceptable excipient or carrier. The sulfonamide derivatives have low toxicity and a potent effect of inhibiting tubulin polymerization.
The present invention relates to a compound of the following Formula (1) or the pharmaceutically acceptable salts thereof, having low toxicity and a potent effect of inhibiting tubulin polymerization, and the use thereof as a pharmaceutical composition: ##STR1## (wherein R.sup.1 and R.sup.2 may be the same or different and each independently represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, a hydroxy group; each R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represents a hydrogen atom; A represents any group of (1) 5-membered heterocyclic group (except triazoyl group) optionally substituted by a lower alkyl group or phenyl group whose ring members include at least 1 nitrogen atom and may include any atom(s) selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom, and (2) a 3 to 10-membered alicyclic group whose ring members include at least 1 nitrogen atom and may include any atom(s) selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom).
N-aryl arylsulfonamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
This invention is directed to compounds of formula (III): ##STR1## wherein B, C, D, E, R.sup.1, R.sup.2 and R.sup.3 are disclosed herein. These compounds are disclosed as being useful as anti coagulants.
N-(2-((4-Hydroxyphenyl)amino)pyridin-3-yl)-4-methoxybenzenesulfonamide Crystalline Form 1, ways to make it, compositions containing it and methods of treatment of diseases using it are disclosed.
