Mitsubishi Tanabe Pharma Corporation

Mitsubishi Pharma Corporation

Welfide Corporation

Yoshitomi Pharmaceutical Industries, Ltd.

Masatoshi Kiuchi

Kunitomo Adachi

Kunio Sugahara

Kenji Chiba

Tetsuro Fujita

Tadashi Mishina

Maiko Hamada

Toshiyuki Kohara

Koji Teshima

Kaoru Tashiro

Takanobu Kuroita

Hiroshi Sakashita

Yoshihito Tanaka

Shuzo Takeda

Mitsuharu Nakamura

Hiroyuki Sueoka

Hidemitsu Higashi

Kaoru Marukawa

Syuji Ehara

Akira Nishiyama

Jouji Yasuoka

Kei Sakata

Katsuya Yamamoto

Shigeki Kuwahara

Shuuzou Takeda

Hideo Tomozane

Nobutaka Kobayashi

The present invention provides a compound represented by the following formula (I): wherein each symbol is as described in the DESCRIPTION, which has a superior peripheral blood lymphocyte decreasing action, and is useful for the treatment or prophylaxis of autoimmune diseases; prophylaxis or suppression of resistance or acute rejection or chronic rejection of transplantation of organ or tissue; treatment or prophylaxis of graft-versus-host (GvH) disease due to bone marrow transplantation; or treatment or prophylaxis of allergic diseases.

Amine compound and use thereof for medical purposes

A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(&#x2550;O)(OH), X is an oxygen atom or a sulfur atom, Y is CHCHor CH&#x2550;CH, Ris cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), Ris alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), Rand Rmay be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5-8.

Provided is a novel amine compound represented by the following formula (I) having a superior peripheral blood lymphocyte decreasing action and superior in the immunosuppressive action, rejection suppressive action and the like, which shows decreased side effects of, for example, bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof. wherein each symbol is as defined in the specification.

Amine compound and pharmaceutical use thereof

Disclosed is a 2-aminobutanol compound represented by the following formula (I) or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof, as well as a production method of the 2-aminobutanol compound of formula (I). The 2-aminobutanol compounds of formula (I) have few side effects including bradycardia and have superior peripheral blood lymphocyte-decreasing effects.

2-aminobutanol compound and use thereof for medical purposes

The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration. The present inventors have found that the following benzylpiperidine derivative (the formula (1)) has a chemokine inhibitory activity. Further intensive studies have resulted in successful enhancement of the chemokine inhibitory activity and stability in blood of the present compound, as well as the completion of the present invention. wherein each symbol is as defined in the specification.

Benzylpiperidine compound

Benzene compound and pharmaceutical use thereof

The present invention relates to the imidazole derivative of the following formula (I)

Imidazole derivatives

A benzene compound of the formula ##STR1## wherein each symbol is as defined in the specification; an optically active isomer or salt thereof, a medicinal composition containing the same, and an immunosuppressant containing the same as the active ingredient. The compound, optically active isomer or salt has an excellent immunosuppressive effect and is useful as an inhibitor for the rejection reaction occurring in organ or bone marrow transplantation, and as a preventive or remedy for articular rheumatism, atopic eczema (dermatitis), Beh.cedilla.et's disease, uveal disease, systemic lupus erythematosus, Sjogren's syndrome, multiple sclerosis, myasthenia gravis, type I diabetes, endocrine ophthalmopathy, primary biliary, cirrhosis, Crohn's disease, glomerulonephritis, sarcoidosis, psoriasis, pemphigus, aplastic anemia, idiopathic thrombocytopenic purpura, allergy, polyarteritis nodosa, progressive systemic sclerosis, mixed connective-tissue disease, aortitis syndrome, polymyositis, dermatomyositis, Wegener's granuloma, ulcerative colitis, active chronic hepatitis, autoimmune hemolytic anemia, Evans' syndrome, bronchial asthma and pollinosis. It is useful also as an antifungal agent and hair growth stimulant.

Growing community of inventors

Osaka, Japan

Masatoshi Kiuchi