Yoshitomi Pharmaceutical Industries, Ltd.

Japan Tobacco Inc.

Minoru Moriwaki

Tetsuya Tahara

Michio Terasawa

Kenji Chiba

Masao Abe

Takashi Nakagawa

Shunichi Manabe

Hirotsugu Komatsu

Masanori Shindo

Hiroshi Mikashima

Syuji Ehara

Takeshi Nakamura

Hiroyuki Kitani

Yukio Hoshino

Takanori Oe

Hiroshi Tanaka

Kazuhiro Goto

Masao Hisadome

Hideaki Sato

Takeki Okumoto

Syuji Yuasa

Mariko Nagasawa

Hidekazu Aratani

Hiroshi Kitajima

Kenichi Onishi

Mariko Amano

Yoichi Akiyama

Shuji Yuasa

Kenichi Demizu

Thienylazole compound and thienotriazolodiazepine compound

A therapeutic agent for osteoporosis, comprising an azepine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof as an active ingredient, a method for treating osteoporosis comprising administering said compound and a use of said compound for the production of a therapeutic agent for osteoporosis. The compounds of the formula (I) have superior bone resorption-inhibitory activity and act to reduce the increased amount of calcium in blood serum, which is caused by bone resorption. Accordingly, these compounds are usable as pharmaceutical agents to effectively inhibit bone resorption, to prevent decrease of bone mass and to prevent or suppress the increase of calcium amount in blood serum which is caused by the progress of bone resorption, with regard to Paget's disease, hypercalcemia, osteoporosis and so on in which the progress of bone resorption is considered to be deeply associated with the symptom, and to the symptoms of progressing bone resorption (development into osteoporosis) along with inflammatory joint diseases such as rheumatoid arthritis.

Therapeutic agent for osteoporosis and diazepine compound

N-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno �3,2-f!�1,2,4!triazolo�4,3-a!�1,4!diazepin-6-yl )-N'- (2-methoxyphenyl)urea, optical isomers thereof and pharmaceutically acceptable salts thereof. The compounds of the present invention strongly and selectively inhibit the expression of VCAM-1 and have an inhibitory effect on leukocyte adhesion to vascular endothelial cells. Accordingly, the compounds of the present invention can be used as cell adhesion inhibitors for prophylaxis or treatment of various diseases in which cell adhesion is involved in the onset and progress thereof.

Thienotriazolodiazepine compound and pharmaceutical use thereof

Immunosuppressive drug

Stable crystals of an acid addition salt of an optically active thienotriazolodiazepine compound or its hydrate of the formula ##STR1## wherein R.sup.1 is hydrogen, R.sup.2 is 2-phenylethyl substituted by alkyl having 1 to 5 carbon atoms, 2-morpholinocarbonylethyl or alkyl having 6 to 12 carbon atoms, or R.sup.1 and R.sup.2 may combinedly form a saturated 5-membered ring having one substituent selected from the group consisting of morpholinomethyl, morpholinocarbonyl and N,N-dipropylcarbamoyl, R.sup.3 is halogen, alkyl having 1 to 5 carbon atoms or alkoxy having 1 to 5 carbon atoms, R.sup.4 is trifluoromethyl or alkyl having 1 to 5 carbon atoms, R.sup.5 is hydrogen or methyl, m is 1-2, and n is 0-2. The present invention provides optically active thienotriazolodiazepine compounds having strong PAF-antagonistic activity as markedly stable crystals which are excellent in crystalline property, permit purification by recrystallization, and have high chemical purity and optical purity, thereby rendering industrial large-scale synthesis attainable. In addition, crystallization thereof facilitates medicinal standardization and pharmaceutical formulation.

Optically active thienotriazolodiazepine compounds

Ester-substituted thienotriazolodiazepine compounds and pharmaceutical

2-alkyl thieno(triazolo)diazepine compounds and pharmaceutical uses

A thienotriazolodiazepine compound of the formula: ##STR1## wherein each symbol is as defined in the specification or a pharmaceutically acceptable salt thereof, and pharmaceutical uses thereof. Said compounds exhibit PAF-antagonistic activity and are useful for the prevention or treatment of various PAF-induced diseases.

Thienotriazolodiazepine compounds and pharmaceutical uses thereof

A thienotriazolodiazepine compound of the formula: ##STR1## wherein each symbol is as defined in the spedification, or a pharmaceutically acceptable acid addition salt thereof, and pharmaceutically uses thereof. Said compounds exhibit PAF-antagonistic acitivty and are useful for the prevention or treatment of various PAF-induced diseases.

A thienotriazolodiazepine compound of the formula: ##STR1## wherein A is alkylene or substituted alkylene and each other symbol is as defined in the specification and a pharmaceutically acceptable acid addition salt thereof, and pharmaceutical uses thereof. Said compounds exhibit PAF-antagonistic activity and are useful for the prevention or treatment of various PAF-induced diseases.

PAF-antagonistic thienotriazolodiazepine compounds and pharmaceutical

Heterocyclic-substituted oxoalkanoic acid derivatives

Growing community of inventors

Oita, Japan

Minoru Moriwaki