Japan Tobacco Inc.

Toyo Boseki Kabushiki Kaisha

Takeo Katsushima

Hiroaki Taguchi

Masakazu Ban

Akihiko Watanabe

Mitsuru Takahashi

Kiyotaka Shinoda

Takashi Nakagawa

Yuko Shinagawa

Hajime Kinoshita

Shuhei Deguchi

Shoichi Aoki

Motohide Sato

A compound of the formula [I] wherein Ris optionally substituted aryl group or optionally substituted heteroaryl group; Ris optionally substituted Calkyl group, Ccycloalkyl group and the like; Ris hydrogen atom, Calkyl group, hydroxyl group and the like; Ris hydrogen atom, Calkyl group and the like; Rand Rare each Calkyl group and the like; Ris optionally substituted aryl group or optionally substituted heteroaryl group; X, Xand Xare each Calkylene group and the like; and Xand Xare each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided. The compound of the present invention is useful as a therapeutic drug of diseases accompanied by abnormal calcium homeostasis, or osteoporosis, hypoparathyreosis, osteosarcoma, periodontal disease, bone fracture, steoarthrosis, chronic rheumatoid arthritis, Paget's disease, humoral hypercalcemia, autosomal dominant hypocalcemia and the like. In addition, an intermediate for the compound is provided.

Calcium receptor antagonists

A compound of the formula [I]wherein Ris optionally substituted aryl group or optionally substituted heteroaryl group; Ris optionally substituted Calkyl group, Ccycloalkyl group and the like; Ris hydrogen atom, Calkyl group, hydroxyl group and the like; Ris hydrogen atom, Calkyl group and the like; Rand Rare each Calkyl group and the like; Ris optionally substituted aryl group or optionally substituted heteroaryl group; X, Xand Xare each Calkylene group and the like; and Xand Xare each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided. The compound of the present invention is useful as a therapeutic drug of diseases accompanied by abnormal calcium homeostasis, or osteoporosis, hypoparathyreosis, osteosarcoma, periodontal disease, bone fracture, steoarthrosis, chronic rheumatoid arthritis, Paget's disease, humoral hypercalcemia, autosomal dominant hypocalcemia and the like. In addition, an intermediate for the compound is provided.

Calcium receptor antagonist

3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I):

3-piperidyl-4-oxoquinazoline derivatives and pharmaceutical compositions comprising the same

Benzylaminoethoxybenzene derivatives, production thereof and use thereof

Novel substituted acetamide compounds of the formula ##STR1## wherein R.sup.1 is hydrogen atom, a lower alkyl group, a lower acyl group, or an aryl group; R.sup.2 is cyano group or aminocarbonyl group; R.sup.3 is a halogen atom, nitro group, a lower alkoxy group, a group of the formula: --NR.sup.4 R.sup.5 (wherein R.sup.4 is hydrogen atom, a lower alkyl group or a group of the formula: --COCH.sub.2 OR.sup.1 ; R.sup.5 is hydrogen atom or a lower alkyl group), or a cyclic amino group of the formula: ##STR2## (wherein R.sup.6 and R.sup.7 are each an alkylene group having 1 to 3 carbon atoms, and X is oxygen atom or methylene), or a pharmaceutically acceptable acid addition salt thereof, which have excellent anti-allergic activity and are useful for the prophylaxis and treatment of various allergic diseases, and a pharmaceutical composition containing the amide compound as set forth above as an active ingredient.

Novel substituted acetamide compounds and use as anti-allergic agents

Novel benzothiazole derivatives of the formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, a lower alkyl group or a lower acyl group; X and Y are the same or different and are each hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, nitro group, amino group, cyano group, trifluoromethyl group, a group of the formula: --COOR.sup.2 (wherein R.sup.2 is hydrogen atom, a lower alkyl group, an alkali metal, an alkaline earth metal, or a cation of amine), or a group of the formula: --CONR.sup.3 R.sup.4 (wherein R.sup.3 and R.sup.4 are the same or different and are each hydrogen atom or a lower alkyl group) or a pharmaceutically acceptable acid addition salt thereof, which have excellent anti-allergic activity and are useful for the prophylaxis and treatment of various allergic diseases, and a pharmaceutical composition containing the compound as set forth above as an active ingredient.

Novel benzothiazole derivatives

Novel amide compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, acetyl, or propionyl; R.sup.2 is hydrogen or chlorine; R.sup.3 is hydrogen or a group of the formula: --CO.sub.2 R.sup.6 (wherein R.sup.6 is hydrogen, lower alkyl or alkali metal); R.sup.4 is hydrogen, trifluoromethyl, cyano, aminocarbonyl, or a group of the formula: --CO.sub.2 R.sup.7 (wherein R.sup.7 is hydrogen, lower alkyl, or alkali metal); R.sup.5 is hydrogen, or a group of the formula: --CO.sub.2 R.sup.8 (wherein R.sup.8 is hydrogen, lower alkyl, or alkali metal), which have excellent anti-allergic activity and are useful for the prophylaxis and treatment of various allergic diseases, and a pharmaceutical composition containing the amide compound as set forth above as an active ingredient.

Amide compounds

Novel pyrimidine compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.1 ' are each hydrogen atom, a lower alkyl, benzyl, an alkali metal, or ammonium; R.sub.2 is hydrogen atom, a halogen atom, a lower alkyl, a lower alkoxy, an aryl, a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each hydrogen atom, a lower alkyl, or an aryl), or a group of the formula: ##STR3## [wherein R.sub.5 and R.sub.6 are each an alkylene having 1 to 3 carbon atoms, and X is oxygen atom, methylene, or a group of the formula: &gt;N-Y (wherein Y is hydrogen atom, a lower alkyl, benzyl, or an aryl)], which have excellent antiallergic activities and are useful for the prophylaxis and treatment of various allergic diseases, and a pharmaceutical composition containing said pyrimidine compound as an active ingredient.

Growing community of inventors

Takatsuki, Japan

Takeo Katsushima