Sankyo Company, Limited

Renascience Co., Ltd.

Yoshiya Amemiya

Hiroaki Yanagisawa

Hiroyuki Koike

Yasuo Shimoji

Toshio Sada

Takuro Kanazaki

Takeshi Oshima

Keiichi Matsuda

Koichi Fujimoto

Atsusuke Terada

Toshio Miyata

Kiyoshi Kurokawa

Atsusuke Trada

The present invention provides a compound represented by the following formula (I) wherein A is a cyclic group etc., B is a 1H-tetrazol-5-yl group or a 2,4-dioxothiazolidin-5-yl group, and Y is a single bond or a C6-10 arylene group, or a pharmacologically acceptable salt thereof or an ester thereof.

Phenylene derivative having tetrazole ring or thiazolidinedione ring

An angiotensin II antagonist of the formula: ##STR1## in which: R.sub.p.sup.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or C.sub.1 -C.sub.6 alkanoyl; R.sub.p.sup.2 represents a single bond, C.sub.1 -C.sub.4 alkylene or C.sub.1 -C.sub.4 alkylidene; R.sub.p.sup.3 and R.sub.p.sup.4 are independently selected from the group consisting of hydrogen and C.sub.1 -C.sub.6 alkyl; R.sub.p.sup.5 represents hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl, naphthyl, benzyl, diphenylmethyl, naphthylmethyl, alkanoyloxyalkyl, cycloalkanecarbonyloxyalkyl, alkoxycarbonyloxyalkyl, cycloalkyloxycarbonyloxyalkyl, (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methyl, (5-alkyl-2-oxo-1,3-dioxolen-4-yl)methyl or phthalaidyl; R.sub.p.sup.6 represents a carboxy or a tetrazol-5-yl; and X.sub.p represents an oxygen or sulfur, and pharmaceutically acceptable salts thereof. The compounds have hypotensive activity and can thus be used for the treatment and prophylaxis of hypertension.

Angiotensin II antagonist 1-biphenylmethylimidazole compounds and their

Compounds of the following formula (I) or the formula (I).sub.p : ##STR1## wherein R.sup.1 is alkyl or alkenyl; R.sup.2 and R.sup.3 are hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl, or aryl fused to cycloalkyl; R.sup.4 is hydrogen, alkyl, alkanoyl, alkenoyl, arylcarbonyl, alkoxycarbonyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydrothienyl, tetrahydrofuryl, a group of formula --SiR.sup.a R.sup.b R.sup.c, in which R.sup.a, R.sup.b and R.sup.c are alkyl or aryl, alkoxymethyl, (alkoxyalkoxy)methyl, haloalkoxymethyl, aralkyl, aryl or alkanoyloxymethoxycarbonyl; R.sup.5 is carboxy or --CONR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 hydrogens or alkyl, or R.sup.8 and R.sup.9 together form alkylene; R.sup.6 is hydrogen, alkyl, alkoxy or halogen; R.sup.7 is carboxy or tetrazol-5-yl; R.sub.p.sup.1 is hydrogen, alkyl, cycloalkyl or alkanoyl; R.sub.p.sup.2 is a single bond, alkylene or alkylidene; R.sub.p.sup.3 and R.sub.p.sup.4 are each hydrogen or alkyl; R.sub.p.sup.6 is carboxy or tetrazol-5-yl; and X.sub.p is oxygen or sulfur; and pharmaceutically acceptable salts and esters thereof. The compounds are AII receptor antagonists and thus have hypotensive activity and can be used for the treatment and prophylaxis of hypertension. The compounds may be prepared by reacting a biphenylmethyl compound with an imidazole compound.

Angiotensin II antagosist 1-biphenylmethylimidazole compounds and their

Compounds of formula (I): ##STR1## [wherein: A represents a group (IIa), (IIb) or (IIc): ##STR2## R.sup.1 is alkyl, alkenyl, cycloalkyl or a group of formula R.sup.4 --Y--R.sup.5 --, where: R.sup.4 is hydrogen, alkyl, or cycloalkyl, R.sup.5 is a single bond or alkylene, and Y is oxygen, sulfur or imino group; R.sup.2 is hydrogen, halogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted cycloalkyl, hydroxy, amino, alkylamino, dialkylamino, formyl, alkylcarbonyl, alkoxy, alkylthio, cyano or nitro; R.sup.3 is hydrogen, alkyl, carboxy, protected carboxy, carbamoyl or tetrazol-5-yl; X is of formula --CH.dbd., --N.dbd. or --C(COOR.sup.6).dbd., where R.sup.6 is hydrogen or a carboxy-protecting group; Z is a single bond, alkylene or vinylene; and B is carboxy, protected carboxy or tetrazol-5-yl]; and pharmaceutically acceptable salts and esters thereof have the ability to inhibit the action of angiotensin II and thus can be used for the treatment and prophylaxis of hypertension and cardiac diseases.

Biphenyl derivatives and their use for the treatment of hypertension and

Compounds of formula (I): ##STR1## (wherein n is 0 or 1, R.sup.1 and R.sup.2 are hydrogen or alkyl, one of A.sup.1 and A.sup.2 is --Z--Y and the other is --W--COOH, where W and Z are alkenylene or alkylene and Y is imidazolyl or pyridyl, and the broken lines represent two single bonds or one single bond and one double bond) and their salts, esters and amides have the ability to inhibit the synthesis of thromboxane A.sub.2 and hence are useful in the treatment of prophylaxis of thrombotic conditions. They may be prepared by introducing an imidazolyl or pyridyl group into the corresponding compound in which Y is replaced by an active group or atom.

Thianaphthene derivatives

Compounds of formula (I): ##STR1## (wherein n is 0 or 1, R.sup.1 and R.sup.2 are hydrogen or alkyl, one of A.sup.1 and A.sup.2 is --Z--Y and the other is --W--COOH, where W and Z are alkenylene or alkylene and Y is imidazolyl or pyridyl, and the broken lines represent two single bonds or one single bond and one double bond) and their salts, esters and amides have the ability to inhibit the synthesis of thromboxane A.sub.2 and hence are useful in the treatment or prophylaxis of thrombotic conditions. They may be prepared by introducing an imidazolyl or pyridyl group into the corresponding compound in which Y is replaced by an active group or atom.

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Tokyo, Japan

Yoshiya Amemiya