Kyowa Hakko Kogyo Co., Ltd.

Fujifilm Corporation

Kyowa Hakko Kirin Co., Limited

Hideaki Kusaka

Hiromi Nonaka

Hiroshi Kase

Akira Karasawa

Haruki Takai

Shigeki Fujiwara

Daisuke Machii

Kozo Yao

Michiyo Kawakage

Junichi Shimada

Fumio Suzuki

Satoshi Nakanishi

Yoshihisa Ohta

Hiroshi Yano

Tohru Yasuzawa

Kotaro Takasaki

Yoshinori Yamashita

Chikara Murakata

Yuji Nomoto

Yuzuru Matsuda

Kenichi Mochida

Kimihisa Ueno

Ryuichiro Nakai

Takashi Kuwabara

Tamotsu Eguchi

Chiharu Nakagawa

Miho Suda

Akira Horiguchi

Emi Shimoike

Akira Ogawa

Hiroshi Magara

A therapeutic and/or prophylactic agent for restenosis, which comprises a thiadiazoline derivative represented by the general formula (0), or a pharmaceutically acceptable salt thereof: [wherein, n represents an integer of 1 to 3, Rrepresents aryl, &#x2014;NRCONR(wherein Rrepresents a hydrogen atom or the like, and Rrepresents lower alkyl or the like) or the like, Rrepresents lower alkyl, Rrepresents a hydrogen atom or the like, and Rrepresents aryl or the like].

Therapeutic agent for restenosis

A condensed purine derivative represented by Formula (I):wherein X&#x2014;Y-Z represents RN&#x2014;C&#x2550;O or N&#x2550;C&#x2014;W, Rrepresents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aromatic heterocyclic group, a substituted or unsubstituted alicyclic heterocyclic group or the like, n represents an integer of from 0 to 3, Vrepresents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, Vrepresents a substituted lower alkyl group or a substituted or unsubstituted aromatic heterocyclic group, and when Vrepresents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group, and for example, X&#x2014;Y-Z represents RN&#x2014;C&#x2550;O and Rrepresents a substituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted alicyclic heterocyclic group, a halogen atom, a lower alkylthio group, &#x2014;NRR, &#x2014;COH, a lower alkoxycarbonyl group, &#x2014;COHal, &#x2014;CONRRor &#x2014;CHO, Vmay represent a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group; or a pharmacologically acceptable salt thereof.

Fused purine derivatives

Remedies for diabetes

Process for producing xanthine derivatives with bacteria and fungi

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

There is provided a novel xanthine Compound(I) ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represent hydroxy-substituted, oxo-substituted or unsubstituted lower alkyl, Y is a single bond or alkylene, and Q is ##STR2## wherein R.sup.3 and R.sup.4 are the same or different and each represent hydrogen or hydroxy, n is 0 or 1; provided that when both of R.sup.3 and R.sup.4 are hydrogen, at least one of R.sup.1 and R.sup.2 is hydroxy-substituted or oxo-substituted lower alkyl; or a pharmaceutically acceptable salt thereof. The xanthine compound has adenosine A.sub.1 receptor antagonizing activity, and thus shows diuretic effect, renal-protecting effect, bronchodilatory effect, cerebral function improving effect and anti-dementia effect.

8-tricycloalkyl xanthine derivatives

Growing community of inventors

Shizuoka, Japan

Hideaki Kusaka