Yoshitomi Pharmaceutical Industries, Ltd.

Taito Company, Ltd.

Other

Mitsubishi Pharma Corporation

Welfide Corporation

Novartis Ag

Novartis Pharma Gmbh

Tetsuro Fujita

Kunitomo Adachi

Tadashi Mishina

Kenji Chiba

Shigeo Sasaki

Koji Teshima

Masahiko Yoneta

Toshiyuki Kohara

Masatoshi Kiuchi

Ryoji Hirose

Yukio Hoshino

Guido Jordine

Stephan Abel

Tokushi Hanano

Takeshi Ikumoto

Yoshiyuki Aoki

Takeki Okumoto

Chiba Kenji

Susumu Hirase

Stefan Abel

The present invention relates to a compound of the general formulawherein R, R, Rand Rare each a hydrogen or an acyl, a pharmaceutically acceptable acid addition salt thereof or a hydrate thereof; a pharmaceutical comprising this compound; a pharmaceutical composition comprising this compound and a pharmaceutically acceptable carrier; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)propane-1,3-diol, the derivatives of the two compounds whose amino group and/or hydroxy group are(is) protected or a salt thereof. The compound of the present invention shows superior immunosuppressive action with less toxicity and higher safety, and is useful as a drug for prevention or suppression of rejection of organs or bone marrow transplantation, or as a drug for prevention or treatment of various autoimmune diseases or allergic diseases.

2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same

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

Benzene compound and pharmaceutical use thereof

A process for preparing 2-amino malonic acid derivatives of formula (1):

Process for preparing 2-amino malonic acid derivatives and 2-amino-1,3-propanediol derivatives, and intermediates for preparing the same

The present invention relates to a compound of the general formula

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##

Immunosuppressant

There are disclosed 2-aminopentanoic acid compounds represented by the formula ##STR1## wherein R is as defined in the specification, their optical isomers, their pharmacologically acceptable salts and their use as an immunosuppressant.

Growing community of inventors

Muko, Japan

Tetsuro Fujita