Mitsubishi Tanabe Pharma Corporation

Welfide Corporation

Kunio Sugahara

Masatoshi Kiuchi

Maiko Hamada

Hidemasa Hikawa

Shinji Miyoshi

Shinsuke Ooike

Kazunori Iwata

Minoru Tanaka

Kunitomo Adachi

Seigo Ishibuchi

Kaoru Tashiro

Naoto Fujie

Mitsuharu Nakamura

Hiroyuki Sueoka

Jun-ichi Endoh

Kaoru Marukawa

Syuji Ehara

Akira Nishiyama

Jouji Yasuoka

Kei Sakata

Katsuya Yamamoto

Meguru Murata

Kouichi Oshita

Nobutaka Kobayashi

Jun-Ichi Endoh

The invention provides a method of inhibiting binding between acetylated histone and a bromodomain-containing protein in a mammal, as well as a method of shrinking or killing of cancer cells expressing a bromodomain-containing protein or inhibiting the growth of cancer cells expressing a bromodomain-containing protein in a mammal. The methods involve administering an effective amount of (S)-2-[4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]-N-(4-hydroxyphenyl)acetamide or a dihydrate thereof to the mammal.

Antitumor agent

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.

Amine compound and use thereof for medical purposes

The present invention relates to a novel antitumor agent containing a compound that inhibits binding between acetylated histone and a bromodomain-containing protein, preferably a thienotriazolodiazepine compound represented by the following formula (I) wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof or a hydrate or solvate as an active ingredient.

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

A thienotriazolodiazepine compound of the following formula (I) a pharmaceutical agent containing the compound as an active ingredient, and a production intermediate and a production method of the thienotriazolodiazepine compound. Since this compound has an inhibitory action on costimulatory signal from CD28 on T cell, it is useful for the prophylaxis or suppression of rejection reaction in transplantation of organ or bone marrow and the like, and the prophylaxis or treatment of autoimmune diseases or allergic diseases.

Thienotriazolodiazepine compound and medicinal use thereof

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

Imidazole derivatives

Growing community of inventors

Osaka, Japan

Kunio Sugahara