Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-02-28
1997-07-22
Springer, David B.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514351, 514398, 514460, 514538, 514562, 5483201, 548495, 546293, 549419, 560 16, 562426, G07D20920, G07D30912, A61K 3135, A61K 31405
Patent
active
056504284
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a novel arylsulfonamide derivative having antagonism specific to a thromboxane A.sub.2 receptor and a pharmaceutical composition, particularly, a thromboxane A.sub.2 antagonist, containing said arylsulfonamide derivative as an effective ingredient.
BACKGROUND ART
It is known that thromboxane A.sub.2 (TxA.sub.2) is an autacoid synthesized in cells such as platelets and exhibits a strong platelet agglutination of platelets, constriction of smooth muscle or the like. Accordingly, it is suggested that a TxA.sub.2 receptor antagonist would be effective in the treatment and prevention of diseases relating to TxA.sub.2 action [Japanese Unexamined Patent Publication (Kokai) No. 4-257556, Japanese Examined Patent Publication (Kokoku) No. 57-35910 and so on]. As examples of such diseases, there may be mentioned cardiac infarction, cerebral infarction, pneumobstruction, thrombosis, renal insufficiency, gestational toxemia and asthma due to bronchoconstriction. Efficacy is expected in the treatment and prevention of various diseases as mentioned above, and thus, development of more excellent novel TxA.sub.2 receptor antagonists was desired.
DISCLOSURE OF INVENTION
Under the circumstances, the inventors of the present invention first analyzed and considered the three-dimensional structural elements of TxA.sub.2 and TxA.sub.2 receptor antagonists by means of the techniques of computer graphics and molecular force field calculation. Then, various compounds, which were designed using the techniques of computer graphics and molecular force field calculation, in view of the above results, were synthesized. Further, the physiological activities of various synthesized compounds were evaluated to find novel arylsulfonamide derivatives having TxA.sub.2 receptor antagonism, and the present invention was completed.
Accordingly, the present invention relates to an arylsulfonamide derivative of the general formula (I): ##STR2## wherein R.sup.1 is an unsubstituted phenyl or naphthyl group, or a phenyl group substituted by 1 to 3 (preferably 1 or 2) same or different substituents selected from the group consisting of a halogen atom, alkyl group (preferably straight or branched alkyl group with 1 to 10, more preferably 1 to 3 carbon atoms), nitro group and alkoxy group (preferably straight or branched alkoxy group with 1 to 10, more preferably 1 to 3 carbon atoms), R.sup.2 is a straight, branched, or branched cyclic alkyl group with 1 to 15 (preferably 1 to 8) carbon atoms, phenyl, phenyloxyl group, phenyloxy group substituted by one or more halogen atoms, cycloalkyl group with 5 to 7 carbon atoms (preferably, cyclohexyl group), indolyl group (preferably, 3-indolyl group), alkylthiol group with 1 to 4 (preferably 1 to 2) carbon atoms, hydroxyl group, protected hydroxyl group (for example, tetrahydropyranyloxy, preferably 2-tetrahydropyranyloxy group), imidazolyl group (preferably, 1-imidazolyl group), pyridyloxyl group (preferably, 3-pyridyloxy group), or --OSO.sub.2 R.sup.4 group, R.sup.4 is a straight or branched alkyl group with 1 to 15 (preferably, 1 to 8, more preferably 1 to 3) carbon atoms, or unsubstituted phenyl or thienyl group, or a phenyl or thienyl group substituted by 1 to 3 same or different substituents selected from the group consisting of a halogen atom, alkyl group (preferably straight or branched alkyl group with 1 to 10, more preferably 1 to 3 carbon atoms), nitro group and alkoxy group (preferably straight or branched alkoxy group with 1 to 10, more preferably 1 to 3 carbon atoms), R.sup.3 is a hydrogen atom or straight or branched alkyl group with 1 to 20 (preferably 1 to 5, more preferably 1 to 3) carbon atoms, n is an integer of 0 to 10 (preferably 0 to 2), p is an integer of 0 to 10 (preferably 0 or 1), X is a group of the general formul a is a direct bond or phenylene group (that is, 1,2-, 1,3- or 1,4-phenylene group), or a salt thereof.
Further, the present invention relates to a pharmaceutical composition, particularly an antagonist to thromboxane A.s
REFERENCES:
Chemical Abstracts, vol. 97, abstract 6774e (1982).
Chemical Abstracts, vol. 120, abstract 299279r (1994).
Kawada Yoshiko
Maeda Shihoko
Miyoshi Yasuo
Mizuguchi Masatsugu
Nakajima Akihiro
NKK Corporation
Springer David B.
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