Hitachi Chemical Company, Ltd.

Other

Showa Denko K.k.

Hiroshi Azuma

Masayuki Ishikawa

Shigeru Ito

Akiko Sugimoto

Shuichiro Sato

Takahisa Saito

Katsuyuki Keino

Yoshimi Takashima

Hidehisa Hamasaki

Shuji Ota

Tomohiro Yamaguchi

Haruo Yamashita

Noriko Takahashi

Katsura Suzuki

4,5-Dihydro-&lsqb;1H&rsqb;-benz&lsqb;g&rsqb;indazole-3-carboxylic acid derivatives represented by the following formula, or their salts, have excellent antagonism to endothelin receptors and are useful as preventives or remedies for diseases such as hypertension, angina pectoris, myocardial infarction, brain infarction, cerebrovascular contraction, renal insufficiency, hepatic dysfunction, arteriosclerosis and post-PTCA restenosis.

4,5-dihydro-&lsqb;1H&rsqb;-benz&lsqb;g&rsqb;indazole-3-carboxylic acid derivatives

6-[[3-[4-(2-Methoxyphenyl)-1-piperazinyl)propyl]-amino]-1,3-dimethyluracil can be used as a therapeutic agent for urinary obstruction.

Method for treating urinary obstruction

A method for treating urinary obstruction by administering a 2-(4-phenyl-1-piperazinylalkyl)aminopyrimidine derivative represented by the formula ##STR1## wherein R.sub.1 and R.sub.3 may be the same or different and independently represent hydrogen, halogen, an amino group, a hydroxyl group, a straight or branched chain lower alkyl group, a straight or branched chain lower alkoxy group, or a straight or branched chain hydroxy-lower alkyl group, R.sub.2 represents hydrogen, halogen, a carboxyl group, a straight or branched chain lower alkyl group, a straight or branched chain lower alkylcarbonyl group, or a straight or branched chain lower alkyloxycarbonyl group, R.sub.4 and R.sub.5 may be the same or different and independently represent hydrogen, halogen, a straight or branched chain lower alkyl group, or a straight or branched chain lower alkoxy group, and n represents an integer of 2 to 6 or a pharmaceutically acceptable acid addition salt thereof to a mammal including a human afflicted with urinary obstruction. The aminopyrimidine derivatives have a selective activity on the .alpha..sub.1 -adrenoceptors in the urinary tracts.

A 2,6,7,8-substituted quinazoline represented by the following formula ##STR1## wherein R.sub.1 and R.sub.3 each represent a lower alkyl group, R.sub.2 represents a lower alkoxy-carbonyl group, and A represents a lower alkyl group, or a phenyl or benzyl group which is unsubstituted or substituted by a substituent selected from the class consisting of halogen atoms, a trifluoromethyl group and lower alkyl groups, or its acid addition salt. The said compound can be prepared by reacting a compound represented by the following formula ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and A are as defined, with ammonia. A pharmaceutical composition comprising the said compound as an active ingredient is useful for the treatment of disorders of the circulatory system.

2,6,7,8-Substituted quinazolines, process for production thereof, and

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Asaka, Japan

Hiroshi Azuma