Kyowa Hakko Kogyo Co., Ltd.

Kyowa Hakko Kogyo K.k.

Haruki Takai

Daisuke Machii

Akira Karasawa

Hiroshi Kase

Shigeki Fujiwara

Kazuhiro Kubo

Katsushige Gomi

Hiromi Nonaka

Kozo Yao

Iwao Kinoshita

Akio Ishii

Tetsuji Ohno

Hideaki Kusaka

Nobuo Kosaka

Yasuo Onoda

Michiyo Kawakage

Hiroyuki Ishida

Yuji Nomoto

Masayuki Teranishi

Yutaka Kasuya

Koji Yamada

Makoto Morimoto

Hiroyuki Obase

Katsuichi Shuto

Michio Ichimura

Joji Nakamura

Koji Suzuki

Tsuyoshi Yamagata

Shigeru Aono

Ken Nagashima

Shin-ichi Sasaki

Makoto Yoshida

Tadashi Hirata

Nobuhiro Nakamizo

Kenji Matsuno

Toshiaki Kumazawa

Soichiro Sato

Tomoko Ishikawa

Kaoru Atsuki

Takahiro Moriyama

Yuko Okamura

Masako Uchii

Nobuo Kasaka

Katsura Sugawara

Takashi Seishi

Tomomi Sugiyama

Hisakatsu Seo

The present invention provides tricyclic compounds which are useful for the treatment of pollakiuria and urinary incontinence and which are represented by general formula (I):

Tricyclic compounds

Disclosed are quinazoline derivatives represented by formula (I): wherein R.sup.1 represents hydrogen, lower alkyl, alkenyl, or aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 represent hydrogen, lower alkyl, lower alkoxy, lower alkanoyl, or the like; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 represent hydrogen, lower alkyl, lower alkoxy, aralkyloxy, or the like, or any adjoining two of them are combined to form methylenedioxy or the like; R.sup.10 represents hydrogen, lower alkyl, or the like; R.sup.11 and R.sup.12 represent hydrogen, lower alkyl, cycloalkyl, phenyl, or aralkyl, or R.sup.11 and R.sup.12 are combined together with N to form a heterocyclic group; and n represents 0, 1 or 2, and pharmaceutically acceptable salts thereof. These compounds have adenosine uptake inhibitory activity and are useful for the protection of myocardium and for the prevention or treatment of renal diseases such as nephritis and diabetic nephropathy.

Quinazoline derivatives

The present invention relates to indole derivatives represented by formula (I): ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen, lower alkyl, hydroxy, lower alkoxy, halogen, --O--(CH.sub.2).sub.n --OR.sup.5, or ##STR2## R.sup.3 represents hydrogen, lower alkyl, or ##STR3## R.sup.4 represents hydroxy, lower alkoxy, substituted or unsubstituted aryloxy, or --NR.sup.10 R.sup.11, and X represents CO or SO.sub.2, with the proviso that when R.sup.3 is hydrogen or lower alkyl, and X is CO, R.sup.4 is --NR.sup.10 R.sup.11, or pharmaceutically acceptable salts thereof.

Indole derivatives

Imidazoquinazoline derivatives

The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C--R.sup.11 (wherein R.sup.11 represents hydrogen, substituted or unsubstituted lower alkyl, or halogen), or a pharmaceutically acceptable salt thereof as an active ingredient.

Isoquinolines having adenosine uptake inhibitor activity

The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C--R.sup.11 (wherein R.sup.11 represents hydrogen, substituted or unsubstituted lower alkyl, or halogen),

Quinazolines and phthalazines having adenosine uptake inhibitor activity

Piperidinyl-dioxoquinazolines as adenosine reuptake inhibitors

The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C-R.sup.11 (wherein R.sup.11 represents hydrogen, substituted or unsubstituted lower alkyl, or halogen), or a pharmaceutically acceptable salt thereof as an active ingredient.

Benzotriazines having adenosine uptake inhibitor activity

Benzenesulfonamide derivatives

A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.

Triphenylmethane derivatives

There is provided a pyridine derivative represented by the formula (I) ##STR1## wherein each of R.sup.1 and R.sup.2 independently represents hydrogen or lower alkyl and each of R.sup.3 and R.sup.4 independently represents hydrogen, lower alkyl, alicyclic alkyl, substituted or unsubstituted polycyclic alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic group, or R.sup.3 and R.sup.4 are combined with nitrogen atom adjacent thereto to form a substituted or unsubstituted alicyclic heterocyclic group, or pharmaceutically acceptable salt thereof. The pyridine derivative exhibits bone resorption inhibiting effect and is useful as a medicament for treating osteoporosis.

Pyridine derivatives

A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits born absorption inhibiting effects and is useful as a medicament for treating osteoporosis.

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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Shizuoka, Japan

Haruki Takai