Yoshitomi Pharmaceutical Industries, Ltd.

Taito Company, Ltd.

Mitsubishi Pharma Corporation

Welfide Corporation

Other

Novartis Ag

Novartis Pharma Gmbh

Tadashi Mishina

Tetsuro Fujita

Kenji Chiba

Kunitomo Adachi

Koji Teshima

Shigeo Sasaki

Toshiyuki Kohara

Masatoshi Kiuchi

Tsuneo Fujii

Masahiko Yoneta

Guido Jordine

Stephan Abel

Tomonori Imayoshi

Ryoji Hirose

Kazuhiko Araki

Minoru Obata

Jun Inui

Atsushi Sakai

Yoshinao Tsuda

Tadao Nakamura

Noriyoshi Izumi

Kanou Harada

Hidenobu Kushuhara

Joji Yasuoka

Rumiko Masuda

Stefan Abel

Disclosed is a process for the production of 2-amino-2-[2-(4-C-alkyl-phenyl)ethyl]propane-1,3-diols.

Production of 2-amino-2-[2- (4-alkylphenyl) ethyl] propane-1, 3-diols

Disclosed is a process for the production of 2-amino-2-&lsqb;2-(4-C -alkyl-phenyl)ethyl&rsqb;propane-1,3-diols.

Production of 2-amin-2-&lsqb;2-(2-(40-C2-20-alkyl-phenyl)ethyl&rsqb;propane-1,3-diols

Medicinal compositions which can be processed into solutions and are useful in inhibiting rejection reactions against the transplantation of organs or bone marrow, in the maintenance immunotherapy therefor or in treating autoimmune diseases, characterized by containing 2-amino-2-&lsqb;2-(4-octylphenyl)ethyl&rsqb;propane-1,3-diol or pharmaceutically acceptable acid-addition salts thereof and cyclodextrins as a stabilizer optionally together with saccharides, if required.

Pharmaceutical composition

Benzene compound and pharmaceutical use thereof

An external preparation for topical administration which aims at inhibiting rejection reactions at organ or bone marrow transplantation or treating autoimmune diseases or allergic diseases and contains as the active ingredient 2-amino-2-(2-(4-octylphenyl)ethyl)propane-1,3-diol or a pharmaceutically acceptable acid addition salt thereof.

External preparation of 2-amino-2-(2-(4-octylphenyl)ethyl) propane-1,3-diol or pharmaceutically acceptable salts thereof for topical administration

Topical administration of

2-Amino-1,3-propanediol compounds of the formula (I) ##STR1## wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted cycloalkyl or the like, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, pharmaceutically acceptable salts thereof and immunosuppressants comprising these compounds as active ingredients. The 2-amino-1,3-propanediol compounds of the present invention show immunosuppressive action and are useful for suppressing rejection in organ or bone marrow tranplantation, prevention and treatment of autoimmune diseases or as reagents for use in medicinal and pharmaceutical fields.

2-amino-1,3-propanediol compound and immunosuppressant

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.

A 2-amino-1,3-propanediol compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, and an immunosuppressant containing the same as the active ingredient. In said formula R represents optionally substituted linear or branched carbon chain, optionally substituted aryl or optionally substituted cycloalkyl; and R.sup.2, R.sup.3, R.sup.4 and R.sup.5, which may be the same or different from one another, represent each hydrogen, alkyl, aralkyl, acyl or alkoxycarbonyl. The compound is immunodepressant and useful as an inhibitor against rejection in organ or bone marrow transplantation, as a preventive or remedy for autoimmune diseases and so forth, or a reagent in the medical and pharmaceutical fields. ##STR1##

A cycloalkylurea compound of the formula (I): ##STR1## wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, which compound inhibits ACAT and is useful as hypolipidemic and antiatherosclerotic medicine.

Cycloalkylurea compounds

A polyazaheterocycle compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein each symbol is as defined in the specification. Said compounds exhibit calcium antagonistic and/or calcium agonistic activities.

Polyazaheterocycle compounds

Growing community of inventors

Iruma, Japan

Tadashi Mishina