Chugai Seiyaku Kabushiki Kaisha

Noboru Kubodera

Isao Matsunaga

Katsuhito Miyamoto

Kiyoshige Ochi

Shun-ichi Hata

Hiroyuki Nabata

Hiroyuki Nagano

Kazushige Sakai

Mitiro Takagi

Yasuhiro Ohba

Eigoro Murayama

Yasumi Uchida

Masahiro Kato

Hiroyoshi Watanabe

Yasushi Murakami

Akira Kawase

Tamotsu Yamazaki

Shun-Ichi Hata

Masuo Koizumi

Hiroshi Nakakimura

Tetsuhiro Mikami

Kazuo Sasahara

Sakae Wada

1.alpha.-hydroxy-vitamin D derivatives represented by formula ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group; and R.sub.2 represents a straight-chain or branched C.sub.2 -C.sub.7 alkyl, C.sub.2 -C.sub.7 alkenyl, or C.sub.2 -C.sub.7 alkynyl group. The compounds exhibit calcium metabolism regulating activity and differentiation stimulating activity on tumor cells, and are useful as treating agents for diseases caused by abnormal calcium metabolism, such as osteoporosis and osteomalacia, or as antitumor agents.

Vitamin D derivative with substituent at the 2.beta.-position

A 1.alpha.-hydroxy-vitamin D derivative represented by formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group; and R.sub.2 represents a straight-chain or branched lower alkyl, lower alkenyl or lower alkynyl group, which is substituted with a hydroxyl group, a halogen atom, a cyano group, a lower alkoxy group, an amino group or an acylamino group, is disclosed. The compound exhibits calcium metabolism regulating activity and differentiation stimulating activity on tumor cells, etc. and is useful as a treating agent for diseases caused by abnormal calcium metabolism, such as osteoporosis and osteomalacia, or as an antitumor agent.

Process for producing 1,2,3-trioxysteroid derivatives

22-Thiavitamin D.sub.3 derivatives

22-oxacholecalciferol derivative and process for preparing the same

Vitamin D derivatives of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 which may be the same or different each represents a hydrogen atom or a hydroxyl group; X is an oxygen atom, the group of the formula OR.sub.4 (where R.sub.4 is either a hydrogen atom or a lower alkyl having 4 to 6 carbon atoms that may or may not be substituted by a hydroxyl group), or the group of the formula=N-OR.sub.5 (where R.sub.5 is either a hydrogen atom or a lower alkyl group having 1 to 5 carbon atoms that may or may not be substituted by a hydroxyl group, an amino group or a lower alkylamino group having 1 to 3 carbon atoms), provided that the carbon atom at 20-position is linked to X by a single bond when X is the group of the formula OR.sub.4, and by a double bond in other cases, and a process for preparing the derivatives are disclosed. The derivatives have both the immunoregulating action and the ability to induce differentiation in tumor cells and hence are useful as medicines such as antiallergic agents, antirheumatic agents and antitumor agents.

Vitamin D derivatives, process for producing the same and their use in

A 1.alpha.-hydroxy vitamin D.sub.3 derivative of the formula: ##STR1## where R.sub.1 is a hydroxyl group, an amino group or the group: OR' (where R' is a lower alkyl group having 1 to 7 carbon atoms that may or may not be substituted by a hydroxyl group, a halogen atom, a cyano group, a lower alkoxy group having 1 to 3 carbon atoms, an amino group, or an acylamino group); R.sub.2 is a hydrogen atom or a hydroxyl group), and a process for preparing the same are disclosed. The compound represented by the formula above has the calcium control action and the ability to induce differentiation in tumor cells and, therefore, are useful as an antitumor agents and a medicine for treating calcium dysbolism-caused diseases.

vitamin D.sub.3 derivatives having a substituent at 2-position

Phenylpiperazine derivatives of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a straight- or branched-chain saturated or unsaturated alkyl group having 1 to 8 carbon atoms which may be substituted at any position by a hydroxyl group, a carboxyl group, a lower alkoxycarbonyl group or an oxo group; and R.sub.2 is a hydrogen atom, a halogen atom, a lower alkyl group or a sulfamoyl group, and a process for producing the same are disclosed. The derivatives of the formula have alpha blocking and serotonin antagonizing activities and are useful as a drug.

Phenyliperazine derivatives

Compounds of the formula ##STR1## (wherein R.sub.1 is a lower alkyl group, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, represent a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a trifluoromethyl group or a lower alkoxycarbonyl group; two adjacent groups of R.sub.2, R.sub.3 and R.sub.4 may combine to form a methylenedioxy group; n is an integer of 2 to 6) or salts thereof, are disclosed. These compounds are useful as agents for treating circulatory diseases because they have hypotensive action and are capable of increasing the cerebral blood flow, decreasing the heart rate and suppressing ventricular arrhythmia due to myocardial ischemia.

Method for treating circulatory diseases by using (2-lower

An agent for treating diseases in circulatory organs which comprises a piperazine compound of the formula ##STR1## wherein R.sub.1, R.sub.2 and A are as defined hereunder, or a salt thereof and a pharmaceutically acceptable carrier.

Compositions and methods for treating diseases in circulatory organs

Dibenz[b,f][1,4]oxazepine derivatives represented by the formula ##STR1## [wherein R.sub.1, n, R.sub.2 and R.sub.3 are as defined in the specification], and a process for preparing the same are disclosed. The object compounds have excellent serum cholesterol lowering activity, serum lipid lowering activity, blood lipid peroxide lowering activity and anti-aggregation of platelet activity, and therefore are useful as a drug.

Benzoxazepine derivatives and process for preparing the same

Growing community of inventors

Shizuoka-ken, Japan

Noboru Kubodera