Pyrimidoindole derivatives and processes for preparation thereof
AssigneeFujisawa Pharmaceutical Co., Ltd.
InventorsMasayuki Kato, Shigetaka Nishino, Kiyotaka Ito, Hisashi Takasugi
Life of this patent
Estimating the term…
Abstract
A compound of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are each hydrogen, lower alkyl, lower alkenyl, aryl or ar(lower)alkyl, R.sup.4 is imidazolyl, which may have alkyl or imino-protective group as substituents, or pyridyl, A is lower alkylene, and is single bond or double bond, and pharmaceutically acceptable salts thereof, having 5-HT antagonism.
Claims9
A compound of the formula:
- ##STR5## wherein R.sup.1, R.sup.2, and R.sup.3 are each hydrogen, lower alkyl, lower alkenyl, C.sub.6-10 aryl or C.sub.6-10 ar(lower)alkyl,
- R.sup.4 is imidazolyl which is a 1H-imidazolyl or 1H-imidazolyl having an imino protective group as a substituent in the 1 position, each of which may have lower alkyl as substituent(s), the number of substituents including the imino protective group being 1 to 3, or is pyridyl,
- A is lower alkylene, and
- is single bond or double bond, and pharmaceutically acceptable salts thereof.
A compound of the formula ##STR6## wherein R.sup.1, R.sup.2 and R.sup.3 are each hydrogen, lower alkyl, lower alkenyl, C.sub.6-10 aryl or C.sub.6-10 ar(lower)alkyl,
- R.sup.4 is imidazolyl which is 1H-imidazolyl or 1-C.sub.6-10 ar(lower)alkyl substituted 1H-imidazolyl, each of which may have lower alkyl as substituent(s), the number of substituents including the 1-C.sub.6-10 ar(lower)alkyl group being 1 to 3 or is pyridyl,
- A is lower alkylene, and
- is single bond or double bond, and pharmaceutically acceptable salts thereof.
A pharmaceutical composition comprising a compound of the following formula ##STR7## wherein R.sup.1, R.sup.2 and R.sup.3 are each hydrogen, lower alkyl, lower alkenyl, C.sub.6-10 aryl or C.sub.6-10 ar(lower)alkyl, R.sup.4 is 1H-imidazolyl which may have 1 to 3 lower alkyl as substituent(s) or is pyridyl,
- A is lower alkylene, and
- is a single bond or double bond
- or pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable, substantially non-toxic carrier or excipient, said compound being present in an amount effective to perform as a 5-HT antagonist.
A method for treating or preventing 5-hydroxytryptamine mediated diseases which comprises administering a compound of the following formula ##STR8## wherein R.sup.1, R.sup.2 and R.sup.3 are each hydrogen, lower alkyl, lower alkenyl, C.sub.6-10 aryl or C.sub.6-10 ar(lower)alkyl, R.sup.4 is 1H-imidazolyl which may have 1 to 3 lower alkyl as substituent(s) or is pyridyl,
- A is lower alkylene, and
- is a single bond or double bond or pharmaceutically acceptable salt thereof in an amount effective to perform as a 5-hydroxytryptamine antagonist to human being or animals in need of such treatment or preventive administration.
A method for treating or preventing nausea or vomiting mediated by 5-hydroxytryptamine which comprises administering a compound of the following formula ##STR9## wherein R.sup.1, R.sup.2 and R.sup.3 are each hydrogen, lower alkyl, lower alkenyl, C.sub.6-10 aryl or C.sub.6-10 ar(lower)alkyl, R.sup.4 is 1H-imidazolyl which may have 1 to 3 lower alkyl as substituent(s) or is pyridyl,
- A is lower alkylene, and
- is a single bond or double bond
- or pharmaceutically acceptable salt thereof in an amount effective to perform as a 5-hydroxytryptamine antagonist to human being or animals in need of such treatment or preventive administration.
Dependencies are inferred from the claim text.