Astellas Pharma Gmbh

Yu Harayama

Kazuyuki Tsuchiya

Yutaka Nakajima

Sunao Imada

Shunichiro Matsumoto

Eriko Yamamoto

Hidenori Ohki

Toshio Yamanaka

Hiroaki Mizuno

Shigeki Kunikawa

Takuya Makino

Junya Ishida

Hiroaki Ohtake

Ayako Toda

Phenyldifluoromethyl-substituted prolinamide compounds that have a cathepsin S inhibitory effect, and are usable as active ingredients of pharmaceutical compositions for preventing and/or treating autoimmune diseases including systemic lupus erythematosus (SLE) and lupus nephritis, allergies, or graft rejection of an organ, bone marrow or tissue. Such compounds include (4R)&#x2014;N-(1-cyanocyclopropyl)-4-(difluoro{4-[(4-methylpiperazin-1-yl)methyl]-2-(trifluoromethyl)phenyl}methyl)-1-[(1-methylcyclopropyl)carbonyl]-L-prolinamide, (4R)&#x2014;N-(1-cyanocyclopropyl)-4-(difluoro{4-[(4-methylpiperazin-1-yl)methyl]-2-(trifluoromethyl)phenyl}methyl)-1-{[1-(trifluoromethyl)cyclopropyl]carbonyl}-L-prolinamide, (4R)&#x2014;N-(1-cyanocyclopropyl)-4-[{4-[(4-ethylpiperazin-1-yl)methyl]-2-(trifluoromethyl)phenyl}(difluoro)methyl]-1-{[1-(trifluoromethyl)cyclopropyl]carbonyl}-L-prolinamide, (4R)&#x2014;N-(1-cyanocyclopropyl)-4-[{4-[(4-ethylpiperazin-1-yl)methyl]-2-(trifluoromethyl)phenyl}(difluoro)methyl]-1-[(1-methylcyclopropyl)carbonyl]-L-prolinamide, and salts thereof.

Phenyldifluoromethyl-substituted prolinamide compound

The present invention relates to a new cyclic peptide compound or a salt thereof, which has anti-hepatitis C virus activities based on inhibitory activity against the RNA replication of hepatitis C virus replicon, a process for preparation thereof, a pharmaceutical composition comprising the same, and a method for prophylactic and/or therapeutic treatment of hepatitis C in a human being or an animal.

Cyclic peptide compounds

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Tokyo, Japan

Yu Harayama