The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Jun. 18, 2019

Filed:

Nov. 05, 2018
Applicant:

Astellas Pharma Inc., Chuo-ku, JP;

Inventors:

Yutaka Nakajima, Tokyo, JP;

Sunao Imada, Tokyo, JP;

Eriko Yamamoto, Tokyo, JP;

Kazuyuki Tsuchiya, Tokyo, JP;

Yu Harayama, Tokyo, JP;

Shunichiro Matsumoto, Tokyo, JP;

Assignee:

ASTELLAS PHARMA INC., Chuo-ku, JP;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 401/10 (2006.01); C07D 207/16 (2006.01); C07D 403/10 (2006.01); A61K 31/4439 (2006.01); A61K 31/496 (2006.01); A61P 37/06 (2006.01); A61P 37/08 (2006.01); A61P 13/12 (2006.01);
U.S. Cl.
CPC ...
C07D 207/16 (2013.01); A61K 31/4439 (2013.01); A61K 31/496 (2013.01); A61P 13/12 (2018.01); A61P 37/06 (2018.01); A61P 37/08 (2018.01); C07D 401/10 (2013.01); C07D 403/10 (2013.01);
Abstract

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)—N-(1-cyanocyclopropyl)-4-(difluoro{4-[(4-methylpiperazin-1-yl)methyl]-2-(trifluoromethyl)phenyl}methyl)-1-[(1-methylcyclopropyl)carbonyl]-L-prolinamide, (4R)—N-(1-cyanocyclopropyl)-4-(difluoro{4-[(4-methylpiperazin-1-yl)methyl]-2-(trifluoromethyl)phenyl}methyl)-1-{[1-(trifluoromethyl)cyclopropyl]carbonyl}-L-prolinamide, (4R)—N-(1-cyanocyclopropyl)-4-[{4-[(4-ethylpiperazin-1-yl)methyl]-2-(trifluoromethyl)phenyl}(difluoro)methyl]-1-{[1-(trifluoromethyl)cyclopropyl]carbonyl}-L-prolinamide, (4R)—N-(1-cyanocyclopropyl)-4-[{4-[(4-ethylpiperazin-1-yl)methyl]-2-(trifluoromethyl)phenyl}(difluoro)methyl]-1-[(1-methylcyclopropyl)carbonyl]-L-prolinamide, and salts thereof.


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