Kyowa Hakko Kogyo Co., Ltd.

Kyowa Hakko Kogyo Kabushiki Kaisha

Roussel Uclaf

Ihara Chemical Kogyo Kabushiki Kaisha

Kyowa Hakko Kogyo K.k.

Kyowa Hakko Kabushiki Kaisha

Kazuhiro Kubo

Akira Karasawa

Hiroyuki Obase

Akio Ishii

Etsuo Oshima

Ichiro Miki

Fumio Suzuki

Tetsuji Ohno

Junichi Shimada

Kenji Ohmori

Haruki Takai

Masayuki Teranishi

Hiromi Nonaka

Yutaka Kasuya

Yoshimasa Oiji

Hidee Ishii

Junichi Ikeda

Koji Yamada

Shunji Ichikawa

Yuji Nomoto

Hiroshi Takizawa

Shoji Oda

Takeshi Kuroda

Nobuhiro Nakamizo

Toshiaki Kumazawa

Joji Nakamura

Shiro Shirakura

Hiroaki Hayashi

Keisuke Isozumi

Masashi Yanase

Hiroyuki Harakawa

Toyofumi Yamada

Hajime Takahashi

Hiroshi Sano

Mitsuru Takahashi

Hiroshi Kase

Katsuhiko Ando

Isao Kawamoto

Tadashi Hirata

Yoshisuke Nakasato

Katsuichi Shuto

Yuzuru Matsuda

Mayumi Yoshida

Tadafumi Tamura

Hisashi Hosoe

Hisayo Nomoto

Kei Okazaki

Mika Nozawa

Shinichiro Toki

Ikufumi Yoshitake

Masaaki Nito

Novel xanthine compounds represented by the following formula: ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.3 independently represents hydrogen or lower alkyl;

Xanthine compounds

Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.14 represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.

Tricyclic compounds and intermediates thereof

Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6 alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 --O, CH.sub.2 --(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.14 represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.

Novel tricyclic compound represented by formula ##STR1## possess a TXA.sub.2 biosynthesis inhibiting activity and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.

Tricyclic compounds as TXA.sub.2 antagonists

Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.

Tricyclic thromboxane A.sub.2 antagonists

Novel xanthine compounds represented by the following formula: ##STR1## wherein each of X.sup.1 and X.sup.2 independently represents oxygen or sulfur; and Q represents; ##STR2## where ----- represents a single bond or a double bond; Y represents a single bond or alkylene, n represents 0 or 1, each of W.sup.1 and W.sup.2 independently represents hydrogen, lower alkyl or amino, Z represents --CH.sub.2 -, --O--, --S-- or --NH--; represents ##STR3## each of R.sup.1 and R.sup.2 independently represents hydrogen, lower alkyl, allyl or propargyl; and R.sup.3 represents hydrogen or lower alkyl, and when Q represents the groups other than ##STR4## each of R.sup.1, R.sup.2 and R.sup.3 independently represents hydrogen or lower alkyl; provided that when Q is ##STR5## then R.sup.1 R.sup.2 and R.sup.3 are not simultaneously methyl; and pharmaceutically acceptable salts thereof have a diuretic effect, a renal-protecting effect and a bronchodilatory effect.

Xanthine derivatives

There are disclosed condensed purine derivatives represented by formula; ##STR1## in which R.sup.3 represents hydrogen, lower alkyl or benzyl; each of X.sup.1 and X.sup.2 independently represents hydrogen, lower alkyl, aralkyl or phenyl; and n is an integer of 0 or 1; R.sup.1 represents hydrogen, lower alkyl, alicyclic alkyl, noradamantan-3-yl, dicyclopropylmethyl or styryl; and R.sup.2 represents hydrogen, lower alkyl or alicyclic alkyl; or a pharmaceutically acceptable salt thereof. The derivatives and pharmaceutically acceptable salts are useful as diuretics, renal protecting agents, antiallergic agents and hypotensives.

Condensed purine derivatives

Novel Tricyclic compound represented by formula ##STR1## possess a TXA.sub.2 biosynthesis inhibiting act and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.

A pyrazoloquinoline derivative having the formula (I): ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 independently represent a hydrogen atom or a lower alkyl group; R.sup.4 represents a hydrogen atom, a lower alkyl group, a halogen-substituted lower alkyl group, or a lower alkoxycarbonyl group; the dotted line means that the pyrazole ring has two conjugated double bonds; and R.sup.4 is bonded to the nitrogen atom at the 1-position or 2-position, or pharmacologically acceptable salts thereof. These compounds exhibit excellent anti-inflammatory activity and hepatic insufficiency treating activity.

Pyrazoloquinoline derivatives

Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic acitvity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.

A hexitol derivative represented by formula (I) ##STR1## wherein R represents hydrogen, unsubstituted or lower alkyl-substituted cycloalkyl, lower alkenyl, lower alkoxy, lower alkanoyl, piperidyl or ##STR2## wherein each of m and n independently represents an integer of 0 to 3; each of X, Y and Z independently represents hydrogen, lower alkyl, lower alkoxy, lower alkanoyl, lower alkanoyloxy, hydroxyl, halogen or nitro or a pharmaceutically acceptable salt thereof.

Hexitol derivatives

Novel tricyclic compound represented by formula (I): ##STR1## possess a TXA.sub.2 biosynthesis inhibiting activity and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.

A compound of formula (I): ##STR1## wherein R.sub.1 represents hydrogen, hydroxy or acetoxy and R.sub.2 represents hydroxy or acetoxy.

Bioxanthracene derivatives

Novel xanthine compounds represented by the following formula: ##STR1## and pharmaceutically acceptable salts thereof have a diuretic action, a renal-protecting action and a vasodilative action. The compounds are useful as a diuretic, a renal-protecting agent and an antihypertensive agent.

Compounds of the formula ##STR1## wherein R.sub.3 is H or alkyl, Q.sub.1 and Q.sub.2 are independently hydrogen, alkyl, hydroxyl, alkoxyl, amino, mono or di alkylamino, nitro or halo or pharmaceutically acceptable salts are useful as cardiotonics.

Quinazoline-substituted pyridazinone derivatives having cardiotonic

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Kazuhiro Kubo