Title:
リシンジンジパインのケトン阻害剤
Document Type and Number:
Japanese Patent JP7113815
Kind Code:
B2
Abstract:
The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
Inventors:
Conrad, Andrew W.
Galemo, Robert A. Junior
Dominey, Stephen S.
Lynch, Kathy.
Holsinger, Leslie Jay.
Galemo, Robert A. Junior
Dominey, Stephen S.
Lynch, Kathy.
Holsinger, Leslie Jay.
Application Number:
JP2019514780A
Publication Date:
August 05, 2022
Filing Date:
September 15, 2017
Export Citation:
Assignee:
Cortex Sea Me, Incorporated
International Classes:
C07C233/62; A61K31/16; A61K31/41; A61K31/42; A61K31/44; A61K31/4439; A61K31/513; A61K45/00; A61P1/02; A61P1/16; A61P3/06; A61P3/10; A61P9/00; A61P11/00; A61P13/12; A61P17/06; A61P19/02; A61P21/02; A61P25/00; A61P25/08; A61P25/14; A61P25/16; A61P25/18; A61P25/28; A61P27/02; A61P27/06; A61P29/00; A61P31/04; A61P35/00; A61P43/00; C07C317/28; C07C321/14; C07C381/00; C07D239/36; C07D257/04; C07D261/12; C07D401/12; C07D413/12
Domestic Patent References:
| JP61183253A | ||||
| JP2016518341A | ||||
| JP63253061A |
Foreign References:
| WO2016057413A2 |
Other References:
Bialas, A. et al.,Exploring the Sn Binding Pockets in Gingipains by Newly Developed Inhibitors: Structure-Based Design, Chemistry, and Activity,Journal of Medicinal Chemistry,2006年,49(5),pp. 1744-1753
Kolb, M. et al.,Synthesis of Fluorinated α-Amino Ketones, III. Preparation of Fluorinated Ketone Analogues of Phenylalanine, Lysine, and p-(Guanidino)phenylalanine,Liebigs Annalen der Chemie,1990年,(1),pp. 1-6
Wood, W. J. L. et al.,Synthesis of a Diverse Library of Mechanism-Based Cysteine Protease Inhibitors,Journal of Combinatorial Chemistry,2003年,5(6),869-880, Supporting Information pp. 1-4
REGISTRY(STN)[online],Entered STN: 2008年6月10日,検索日:2021年7月13日,CAS登録番号1026912-38-8
REGISTRY(STN)[online],Entered STN: 2008年6月6日,検索日:2021年7月13日,CAS登録番号1025940-84-4
Kato, D. et al.,Activity-based probes that target diverse cysteine protease families,Nature Chemical Biology,2005年,1(1),pp. 33-38
Kolb, M. et al.,Synthesis of Fluorinated α-Amino Ketones, III. Preparation of Fluorinated Ketone Analogues of Phenylalanine, Lysine, and p-(Guanidino)phenylalanine,Liebigs Annalen der Chemie,1990年,(1),pp. 1-6
Wood, W. J. L. et al.,Synthesis of a Diverse Library of Mechanism-Based Cysteine Protease Inhibitors,Journal of Combinatorial Chemistry,2003年,5(6),869-880, Supporting Information pp. 1-4
REGISTRY(STN)[online],Entered STN: 2008年6月10日,検索日:2021年7月13日,CAS登録番号1026912-38-8
REGISTRY(STN)[online],Entered STN: 2008年6月6日,検索日:2021年7月13日,CAS登録番号1025940-84-4
Kato, D. et al.,Activity-based probes that target diverse cysteine protease families,Nature Chemical Biology,2005年,1(1),pp. 33-38
Attorney, Agent or Firm:
Shimizu Hatsushi
Masao Haruna
Hirotaka Yamaguchi
Shun Jinbe
Ryuichi Inoue
Toshimitsu Sato
Koichi Niimi
Tomohiko Kobayashi
Hideki Kodera
Masato Ozeki
Kazuya Kawamoto
Masao Haruna
Hirotaka Yamaguchi
Shun Jinbe
Ryuichi Inoue
Toshimitsu Sato
Koichi Niimi
Tomohiko Kobayashi
Hideki Kodera
Masato Ozeki
Kazuya Kawamoto