Other

Wisconsin Alumni Research Foundation

Chugai Seiyaku Kabushiki Kaisha

Kuraray Co., Ltd.

Kureha Kagaku Kogyo Kabushiki Kaisha

Nihon University

Nibon University

Rikkyo Gakuin

Sachiko Yamada

Masato Shimizu

Hector Floyd Deluca

Hiroaki Takayama

Tatsuo Suda

Makoto Makishima

Masayuki Ishikawa

Satoshi Sasaki

Koichi Niimura

Yuji Maeda

Antonio Mourino

Chikara Kaneko

Masayuki Ohmori

Akiko Sugimoto

Hiroaki Tokiwa

Yukiko Miyamoto

Kazuki Maekawa

Yusuke Watarai

Takeru Kudo

Manabu Matsunawa

Kenji Fukushima

Michiyasu Ishizawa

Keiko Nakayama

The present invention provides a VDR ligand which does not induce hypercalcemia that is an adverse reaction of a vitamin D3 preparation; and a composition which comprises lithocholic acid propionate, a salt thereof, a solvate thereof, or a prodrug thereof.

Function-selective vitamin D receptor agonist

The present invention provides a compound which functions as a selective vitamin D receptor modulator and has action-selectivity or tissue-selectivity such that it does not induce hypercalcemia but causes other effects. There is provided a compound represented by formula (I), a solvate thereof or a prodrug thereof. 

Vitamin D receptor modulators with partial agonist activity

A novel 2,2-di-substituted 19-norvitamin D derivative. It is a compound represented by the general formula (I) wherein R1 and R2 are the same or different and each represents hydroxy and A represents hydrogen, or an unsubstituted linear or branched alkyl. 

2,2-Di-substituted 1alpha,25-dihydroxy-19-norvitamin D derivative

The present invention provides a method for the synthesis of an A-ring synthon phosphine oxide used in the preparation of 19-nor vitamin D compounds, and to novel synthetic intermediates formed during the synthesis. The new method prepares the phosphine oxide from (D)-glucose.

Synthesis of A-ring synthon of 19-NOR-1&#x3b1;,25-dihydroxyvitamin D3 from (D)-glucose

Synthesis of A-ring synthon of 19-nor-1&agr;,25-dihydroxyvitamin D3 from (D)-glucose

A composition for improving calcium metabolism comprising, as an active ingredient, (20S,22R)-22-methyl-1.alpha.,25-dihydroxyvitamin D.sub.3 ; and a method of treating a calcium metabolism disorder in a mammal comprising administering a therapeutically effective amount of (20S,22R)-22-methyl-1.alpha.,25-dihydroxyvitamin D.sub.3.

Composition for improving calcium metabolism

The present invention discloses a novel, labelled vitamin D.sub.3 derivative in which hydrogen atoms on the skeleton portion, i.e. 6- and 19-positions, are substituted with a deuterium atom or a tritium atom, as well as a novel production process of the labelled vitamin D.sub.3 derivative carried out by way of sulfur dioxide addition reaction of a vitamin D.sub.3 derivative. The labelled portion of the novel vitamin D.sub.3 is resistant against in vivo metabolism and make a long period tracing of its pharmacodynamics in a living body possible.

Labelled vitamin D.sub.3 derivative and production process thereof

There are disclosed 6,19-epidioxyvitamin D.sub.3 derivatives which are represented by the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each a hydrogen atom or a hydroxyl group; when R.sub.1 is a hydrogen atom, R.sub.2 represents a hydroxyl group and R.sub.3 is a hydrogen atom or a hydroxyl group; when both R.sub.1 and R.sub.2 represent a hydroxyl group, R.sub.3 is a hydrogen atom or a hydroxyl group; and when R.sub.1 is a hydroxyl group and R.sub.2 is a hydrogen atom, R.sub.3 represents a hydroxyl group. The compounds are highly capable of inducing differentiation of human myeloid leukemia cells with minimum effects on calcium metabolism and are useful as an agent to treat leukemia.

Novel vitamin D.sub.3 derivatives and process for producing the same

A 24,25-dihydroxycholestane derivatives of the formula ##STR1## wherein A is a steroid residue and R is an aryl group and a process for preparation of the same are disclosed. The derivatives are an intermediate for synthesis of 24,25-dihydroxycholecalciferol having useful physicological activity like that of vitamin D.sub.3. 24,25-Dihydroxycholecalciferol can be produced in an industrially advantageous method via the intermediate which is easily prepared from commercially available starting compounds.

24,25-Dihydroxycholestans and process for preparing the same

A novel vitamin D.sub.3 derivative of the formula ##STR1## (wherein R.sub.1 is hydrogen or a hydroxyl group) which exhibits strong biological activity like that of vitamin D and is useful as a medicine; and a process for producing the same are disclosed.

Novel vitamin D.sub.3 derivative and process for preparing the same

1.alpha.,2.alpha.-Dihydroxycholecaliciferol having improved vitamin D activities and a process for preparing the same are disclosed.

1.alpha., 2.alpha.-Dihydroxycholecalciferol and process for preparing

Growing community of inventors

Hachioji, Japan

Sachiko Yamada