Title:
PHENYLDIFLUOROMETHYL-SUBSTITUTED PROLINEAMIDE COMPOUND
Document Type and Number:
WIPO Patent Application WO/2018/139438
Kind Code:
A1
Abstract:
[Problem] To provide a compound useful as a cathepsin S inhibitor.
[Solution] The present inventors have studied on a compound which has a cathepsin S-inhibiting activity and can be used as an active ingredient for a pharmaceutical composition for preventing and/or treating an autoimmune disease such as systemic lupus erythematosus (SLE) and lupus nephritis, an allergy, or organ, bone marrow or tissue graft rejection. As a result, it has been confirmed that a phenyldifluoromethyl-substituted prolineamide compound according to the present invention has a cathepsin S-inhibiting activity. This confirmation leads to the accomplishment of the present invention. The phenyldifluoromethyl-substituted prolineamide compound according to the present invention has a cathepsin S-inhibiting activity, and can be used as a prophylactic and/or therapeutic agent for an autoimmune disease such as SLE and nephritis, an allergy, or organ, bone marrow or tissue graft rejection.
Inventors:
NAKAJIMA YUTAKA (JP)
IMADA SUNAO (JP)
YAMAMOTO ERIKO (JP)
TSUCHIYA KAZUYUKI (JP)
HARAYAMA YU (JP)
MATSUMOTO SHUNICHIRO (JP)
IMADA SUNAO (JP)
YAMAMOTO ERIKO (JP)
TSUCHIYA KAZUYUKI (JP)
HARAYAMA YU (JP)
MATSUMOTO SHUNICHIRO (JP)
Application Number:
PCT/JP2018/001927
Publication Date:
August 02, 2018
Filing Date:
January 23, 2018
Export Citation:
Assignee:
ASTELLAS PHARMA INC (JP)
International Classes:
C07D207/16; A61K31/4439; A61K31/496; A61P13/12; A61P37/06; A61P37/08; C07D401/10; C07D403/10
Domestic Patent References:
| WO2010121918A1 | 2010-10-28 | |||
| WO2012059507A1 | 2012-05-10 | |||
| WO2010142650A1 | 2010-12-16 | |||
| WO2017144483A1 | 2017-08-31 |
Foreign References:
| JP2012524116A | 2012-10-11 | |||
| JP2016532646A | 2016-10-20 | |||
| US20160244417A1 | 2016-08-25 | |||
| JP2005526753A | 2005-09-08 |
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ANNALS OF THE RHEUMATIC DISEASES, vol. 74, 2015, pages 452 - 463
WUTS: "Greene's Protective Groups in Organic Synthesis", 2006
PROG. MED., vol. 5, 1985, pages 2157 - 2161
"Pharmaceutical Research and Development, Drug Design, Hirokawa Publishing Company", vol. 7, 1990, HIROKAWA-SHOTEN LTD.
A. D. MEIJEREF. DIEDERICH: "Metal-Catalyzed Cross-Coupling Reactions", 1997, VCH PUBLISHERS INC., pages: 163 - 198
"Courses in Experimental Chemistry", vol. 14, 2005
S.R. SANDLERW. KARO: "Organic Functional Group Preparations", vol. 1, 1991, ACADEMIC PRESS, INC.
WITTIG, G. ET AL., U. BER., vol. 87, 1954, pages 1318
J. AM. CHEM., SOC., vol. 78, 1956, pages 5694 - 5695
J. ORG. CHEM., vol. 51, 1986, pages 439 - 445
"J. Chem. Soc., Chem. Commun.", 1987, CHEMICAL SOCIETY OF JAPAN, pages: 1625 - 1627
"J. Am. Chem. Soc.", vol. 132, 2010, pages: 18199 - 18205
ORGANIC LETTERS, vol. 14, no. 20, 2012, pages 5370 - 5373
M. HUDLICKY: "Reductions in Organic Chemistry", 1996, ACS
R.C. LAROCK: "Comprehensive Organic Transformations", 1999, VCH PUBLISHERS, INC.
T.J. DONOHOE: "Oxidation and Reduction in Organic Synthesis (Oxford Chemistry Primers 6", 2000, OXFORD SCIENCE PUBLICATIONS
JAMA, vol. 195, 1966, pages 145
ADVANCES IN IMMUNOLOGY, vol. 37, 1985, pages 269 - 390
JOURNAL OF BIOMEDICINE AND BIOTECHNOLOGY, vol. 2011, 2011, pages 271694
Attorney, Agent or Firm:
MORIHIRA, Koichiro et al. (JP)
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