Mitsubishi Tanabe Pharma Corporation

Mitsuharu Nakamura

Seigo Ishibuchi

Yoichi Naka

Katsuhiko Itoh

Hiroshi Sumichika

Takao Kamahori

Hisao Takayanagi

Maiko Hamada

Masatoshi Kiuchi

Kunio Sugahara

Makoto Kawano

Takashi Naka

The present invention relates to a production method of 4-alkoxy-3-trifluoromethylbenzyl alcohol at a high conversion ratio, which can strictly suppress production of a byproduct by using DIBAL as a reducing agent. 

4-alkoxy-3-(trifluoromethyl)benzyl alcohol production method

The present invention relates to an amide derivative of the formula (1), having a C5a receptor antagonistic action wherein each symbol is as defined in the specification. The above-mentioned amide derivative, an optically active form thereof and a pharmaceutically acceptable salt thereof are promising as an agent for the treatment or prophylaxis of diseases or syndromes caused by inflammation caused by C5a [e.g., autoimmune diseases such as rheumatism, systemic lupus erythematosus and the like, sepsis, adult respiratory distress syndrome, chronic obstructive pulmonary disease, allergic diseases such as asthma and the like, atherosclerosis, cardiac infarction, brain infarction, psoriasis, Alzheimer's disease and serious organ injury (e.g., pneumonia, nephritis, hepatitis and pancreatitis and the like) due to activation of leukocytes caused by ischemia reperfusion, trauma, burn, surgical invasion and the like]. Moreover, they are useful as a therapeutic or prophylactic agent for the infectious diseases caused by bacteria and virus that invade via a C5a receptor.

Amide derivatives and medicinal 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

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Tokyo, Japan

Mitsuharu Nakamura