Kyowa Hakko Kogyo Co., Ltd.

Kyowa Hakko Kirin Co., Limited

Kyowa Hakko Kogyo Kabushiki Kaisha

Kyowa Hakko Rogyo Kabushiki Kaisha

Hiroshi Kase

Isao Kawamoto

Hiroshi Sano

Akira Karasawa

Koji Yamada

Shizuo Shiozaki

Toru Yasuzawa

Katsuhiko Ando

Hiromi Nonaka

Kunikatsu Shirahata

Haruki Takai

Satoshi Nakanishi

Daisuke Machii

Katsuichi Shuto

Mitsuru Takahashi

Shigeto Kitamura

Shigeki Fujiwara

Hideaki Kusaka

Fumio Suzuki

Masaji Kasai

Chikara Murakata

Junichi Shimada

Yuzuru Matsuda

Takao Iida

Yutaka Saito

Tetsuji Ohno

Yoshihisa Kuwana

Ryo Okachi

Michio Ichimura

Joji Nakamura

Masayuki Teranishi

Kiyoshi Nakayama

Nobuaki Koike

Kozo Asano

Akira Sato

Makoto Morimoto

Shiro Akinaga

Hiromitsu Saito

Kazuhiro Kubo

Tadashi Hirata

Yutaka Ohsawa

Naoki Seno

Akihisa Mori

Minoru Kobayashi

Joji Goto

Kozo Yao

Noriaki Hirayama

Michiyo Kawakage

Etsuyo Shimizu

Tohru Yasuzawa

Kenji Omori

Junya Kase

Yutaka Waki

Kazutoshi Kuroda

Eiji Kobayashi

Shunji Ichikawa

Yuji Nomoto

Kenichi Mochida

Kenji Matsuno

Shiro Shirakura

Yasuo Onoda

Koji Suzuki

Iwao Kinoshita

Tomoko Ishikawa

Yoshikazu Morishita

Ken Nagashima

Shin-ichi Sasaki

Hisayo Nomoto

Hideaki Mizumoto

Kazuyuki Iwahashi

Megumi Takeuchi

Toshiro Koguchi

Kazuko Hashizume

Takashi Deguchi

Makoto Takayama

Masayuki Yamato

Dayao Zhao

Yuzuru Matauda

Kazuyuki Iwashashi

Tomoyuki Sano

Keiko Ohsawa

Katsuichi Shutoh

Minoru c/oPharm Research Center Kobayashi

Naoki c/o Pharm Research Center Seno

Shizuo c/o Pharm Research Center Shiozaki

Akihisa c/o Head Office Mori

Junya PharmaResCenter Kase

Shizuo PharmaResCenter Shiozaki

The present invention provides pharmaceutical compositions, which are useful for treatment of depression and the like, and which comprises a compound having an adenosine Areceptor antagonistic activity such as (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione or a pharmaceutically acceptable salt thereof and an antidepressant drug (for example, a tricyclic antidepressant, a tetracyclic antidepressant, a selective serotonin reuptake inhibitor, a selective noradrenalin reuptake inhibitor, a dopamine reuptake inhibitor, a serotonin-noradrenalin reuptake inhibitor, monoamine oxidase inhibitor, a 5-HTantagonist or the like), and the like.

Pharmaceutical composition containing KW-6002 and fluoxetine or paroxentine

Anxiety disorders, such as panic disorder, agoraphobia, obsessive-compulsive disorder, social phobia, post-traumatic stress disorder, generalized anxiety disorder, specific phobia, or the like, are treated by administering an effective amount of at least one adenosine Areceptor antagonist to a patient in need thereof, optionally in combination with an anxiolytic(s) other than the adenosine Areceptor antagonist.

Method of treating an anxiety disorder

Pharmaceutical composition

The present invention provides pharmaceutical compositions, which are useful for treatment of depression and the like, and which comprises a compound having an adenosine Areceptor antagonistic activity such as (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione or a pharmaceutically acceptable salt thereof and an antidepressant drug (for example, a tricyclic antidepressant, a tetracyclic antidepressant, a selective serotonin reuptake inhibitor, a selective noradrenalin reuptake inhibitor, a dopamine reuptake inhibitor, a serotonin-noradrenalin reuptake inhibitor, a monoamine oxidase inhibitor, a 5-HTantagonist or the like), and the like.

A method for treating migraine comprising administering, as an active ingredient, a xanthine derivative represented by the following formula or a pharmaceutically acceptable salt thereof. 

Agents for treating migraine

The present invention provides methods of treating restless legs syndrome or related disorders, comprising administering an effective amount of at least one adenosine Areceptor antagonist to a patient in need thereof. More preferably the adenosine Areceptor antagonist is a xanthine derivative or a pharmaceutically acceptable salt thereof.

Adenosine A2A receptor antagonists for treating restless legs syndrome or nocturnal myoclonus

The present invention is directed to methods of treating movement disorders by administering an effective amount of one or more adenosine Areceptor antagonists to a patient in need thereof. The present invention also provides methods of decreasing the adverse effects of L-DOPA in patients receiving L-DOPA therapy in the treatment of Parkinson's disease. The present invention further provides methods and compositions for treating Parkinson's disease patients with sub-clinically effective doses of L-DOPA by combining L-DOPA treatment with an effective amount of one or more adenosine Areceptor antagonists (i.e., L-DOPA sparing effect). The present invention further provides methods of effective treatment of Parkinson's disease by co-administering at least one adenosine Areceptor antagonist, L-DOPA and a dopamine agonist and/or a COMT inhibitor and/or a MAO inhibitor. The present invention further provides methods of prolonging effective treatment of Parkinson's disease by administering an adenosine Areceptor antagonist singly or together with a dopamine agonist, and/or a COMT inhibitor, and/or a MAO inhibitor without prior or subsequent administration of L-DOPA, delaying or removing on-set of L-DOPA motor complication.

Methods of treating patients suffering from movement disorders

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Xanthine derivatives

Imidazoquinazoline derivatives

Disclosed are xanthine derivatives represented by the following Formula (I): ##STR1## in which R.sup.1, R.sup.2, and R.sup.3 independently represent hydrogen or lower alkyl;

8-substituted styryl xanthine 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

Growing community of inventors

Koganei, Japan

Hiroshi Kase