Kyowa Hakko Kogyo Co., Ltd.

Roussel Uclaf

Akio Ishii

Akira Karasawa

Fumio Suzuki

Kazuhiro Kubo

Ichiro Miki

Junichi Shimada

Hiroyuki Obase

Etsuo Oshima

Shunji Ichikawa

Hiromi Nonaka

Tetsuji Ohno

Katsushige Gomi

Kenji Ohmori

Haruki Takai

Katsuichi Shuto

Shizuo Shiozaki

Joji Nakamura

Nobuo Kosaka

Iwao Kinoshita

Nobuaki Koike

Hiroaki Hayashi

Hidee Ishii

Yasuo Onoda

Yoshikazu Miwa

Hiroyuki Ishida

Makoto Morimoto

Daisuke Machii

Shigeto Kitamura

Takeshi Kuroda

Haruhiko Manabe

Toshiaki Kumazawa

Shiro Shirakura

Koji Suzuki

Hiromasa Kato

Nobuo Kasaka

Obase Hiroyuki

Hitoshi Takami

Kubo Shizuoka

Nobuyuki Kishibayashi

Katsura Sugawara

Shizuo Shioazaki

Kazuihiro Kubo

The present invention relates to novel xanthine derivatives of the formula (I) which are selectively antagonistic to an adenosine A.sub.2 receptor, and pharmaceutically acceptable salts thereof. Formula (I): ##STR1## In the formula, R.sup.1 and R.sup.2 are the same or different and each represents a hydrogen atom, a propyl group, a butyl group or an allyl group; R.sup.3 represents a hydrogen atom or a lower alkyl group; Y.sup.1 and Y.sup.2 are the same or different and each represents a hydrogen atom or a methyl group; and Z represents a substituted or unsubstituted phenyl group, a pyridyl group, an imidazolyl group, a furyl group or a thienyl group.

Xanthine derivatives

Methods for the treatment of Parkinson's disease comprising administering to a patient an agent which contains, as an active ingredient, a xanthine derivative or a pharmaceutically acceptable salt thereof. The xanthine derivative is represented by the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; and R.sup.4 is cycloalkyl, --(CH.sub.2).sub.n --R.sup.5, wherein R.sup.5 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; and n is an integer of 0 to 4, or ##STR2## wherein Y.sup.1 and Y.sup.2 represent independently hydrogen, halogen, or lower alkyl; and Z is substituted or unsubstituted aryl, ##STR3## wherein R.sup.6 is hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, nitro, or amino; and m is an integer of 1 to 4, or a substituted or unsubstituted heterocyclic group; and X.sup.1 and X.sup.2 are independently O or S.

Therapeutic agent for Parkinson's disease

Antidepressants

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

Benzenesulfonamide derivatives

Agents for the treatment of Parkinson's disease contain, as an active ingredient, a xanthine derivative or a pharmaceutically acceptable salt thereof. The xanthine derivative is represented by the formula: ##STR1## in which R.sup.1, R.sup.2 are R.sup.3 are independently hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; and R.sup.4 represents cycloalkyl, --(CH.sub.2).sub.n --R.sup.5 (in which R.sup.5 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; and n is an integer of 0 to 4), or ##STR2## in which Y.sup.1 and Y.sup.2 represent independently hydrogen, halogen, or lower alkyl; and Z represents substituted or unsubstituted aryl, ##STR3## in which R.sup.6 represents hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, nitro, or amino; and m represents an integer of 1 to 4, or a substituted or unsubstituted heterocyclic group; and X.sup.1 and X.sup.2 represent independently O or S.

A novel xanthine derivative of the formula (I): ##STR1## wherein one of R.sup.1 and R.sup.2 represents substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, substituted or unsubstituted alicyclic alkyl, substituted or unsubstituted phenyl, or substituted or unsubstituted benzyl; and the other represents

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 xanthine derivative of the formula (I): ##STR1## wherein R.sup.1 represents substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, substituted or unsubstituted alicyclic alkyl, substituted or unsubstituted phenyl, or substituted or unsubstituted benzyl;

Quinoline derivative having serotonin-3 receptor antagonizing activity

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.

There is disclosed a heterocyclic compound represented by general formula: ##STR1## wherein R.sup.1 represents hydrogen, lower alkyl or aryl; R.sup.2 represents hydrogen, hydroxyl or lower alkyl; A represents CH or N; X represents --O-- or --NH--; R.sup.3 represents hydrogen, hydroxyl or lower alkyl; R.sup.4 represents lower alkyl; represents 0 or 1, or a pharmaceutically acceptable salt thereof.

Certain 2-oxo-quinoline carboxylates or corresponding carboxamides

Growing community of inventors

Shizuoka, Japan

Akio Ishii