Fujisawa Pharmaceutical Company, Ltd.

Astellas Pharma Gmbh

Takehiko Ohkawa

Teruo Kyoto Oku

Hiroyuki Setoi

Tatsuya Zenkoh

Yuki Sawada

Masashi Hashimoto

Hirokazu Tanaka

Kentaro Sato

Hitoshi Sawada

Ichiro Shima

Keiji Hemmi

Chiyoshi Kasahara

Naoki Ishibashi

Kenichiro Imamura

Takeshi Murakami

Seiji Yoshimura

Ryota Shiraki

Akio Kuroda

Kazuhiko Ohne

Toshio Kurosaki

Hiroki Fukudome

Tomoaki Kawano

Hirofumi Ishii

Mitsuru Hosaka

Kazuhiko Osoda

Yutaka Inoki

Ciyoshi Kasahara

Aiko Wada

There is provided a compound which can be used for therapy of diseases in which 11&#x3b2;-hydroxysteroid dehydrogenase type 1 (11&#x3b2;-HSD1) participates, in particular diabetes, insulin resistance. It has been found that a triazole derivative wherein the triazole ring is substituted with a trisubstituted methyl group in the 2-position or a pharmaceutically acceptable salt thereof has a strong 11&#x3b2;-HSD1 inhibitory activity. Moreover, the triazole derivative of the invention exhibits an excellent blood-glucose level-lowering action and hence can be used for therapy of diabetes, insulin resistance.

Triazole derivative or salt thereof

A compound of the formula (I) or a pharmaceutically acceptable salt thereof: [wherein

2-cyanopyrrolidinecarboxamide compound

The present invention relates to a compound of the formula (I) wherein R1 is benzofuranyl substituted by halogen, or styryl substituted by halogen; R2 is substituted hydroxy, substituted mercapto or substituted sulfonyl; and X is or pharmaceutically acceptable salts thereof. The compound (1) of the present invention and pharmaceutically acceptable salts thereof possess a strong inhibitory activity on the production of nitric oxide (NO), and are useful for prevention and/or treatment of NO-mediated diseases in human being and animals 

Peptide compounds

Substituted dipeptides having nos inhibiting activity

Benzamide derivatives as vasopressin antagonists

This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc. and represented by general formula (I):

Benzamide derivatives having a vasopressin antagonistic activity

This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc. and represented by the general formula (I):

Benzamide derivatives and their use as vasopressin antagonists

An oxaspiro �2,5!octane derivative of the formula: ##STR1## useful in inhibiting angiogenesis in solid tumors.

Oxaspiro(2,5)octane derivative

Oxaspiro�2,5! octanes of the formula ##STR1## inhibit angiogenesis and are particularly suitable for the treatment of solid tumors. In preferred embodiments, R.sup.1 is a carbamoyl derivative, R.sup.2 is an alkoxy substituent and R.sup.3 is ##STR2## Pharmaceutical salts of these compounds, such as methyl, amonium and organic amine salts also exhibit desirable properties.

Oxaspiro�2,5! octane derivative

Compounds having the structure below ##STR1## and pharmaceutically acceptable salts thereof exhibit vasopressin antagonistic activity, vasodilating activity, hypotensive activity, activity for inhibiting saccharide release in the liver, activity for inhibiting growth of mesagium cells, water diuretic activity, platelet agglutination inhibitory activity, oxytocin antagonistic activity and the like, and are useful in treating or preventing hypertension, heart failure, renal insufficiency, edema, ascites, vasopressin parasecretion syndrome, hepatocirrhosis, hyponatremia, hypokalemia, diabetic or circulation disorder, oxytocin related diseases and the like.

Benzamide derivatives and pharmaceutical composition comprising the same

The invention relates to a cyclohexane derivative, useful as an angiogenesis inhibitor, of the formula: ##STR1## wherein R.sup.1 is halomethyl; or arylthiomethyl which may have amino, lower alkoxy or acylamino,

Cyclohexane derivatives and pharmaceutical compositions

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Osaka, Japan

Takehiko Ohkawa