849671-56-3Relevant articles and documents
NON-LYSOSOMAL GLUCOSYLCERAMIDASE INHIBITORS AND USES THEREOF
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Paragraph 00179, (2020/12/01)
The invention provides compounds for inhibiting glucosylceramidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.
HORMONE RECEPTOR MODULATORS FOR TREATING METABOLIC CONDITIONS AND DISORDERS
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Page/Page column 264; 265, (2018/03/25)
The invention relates to activators of FXR useful in the treatment of autoimmune disorders, liver disease, intestinal disease, kidney disease, cancer, and other diseases in which FXR plays a role, having the Formula (I): (I), wherein L1, A, X1, X2, R1, R2, and R3 are described herein.
ISOXAZOLYL-CARBONYLOXY AZABICYCLO[3.2.1]OCTANYL COMPOUNDS AS FXR ACTIVATORS
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Paragraph 00412, (2018/09/25)
The disclosure relates to activators of FXR useful in the treatment of autoimmune disorders, liver disease, intestinal disease, kidney disease, cancer, and other diseases in which FXR plays a role, having the Formula (I): wherein L1, L2, A, B, R1, R2, R3, and R4 are described herein.
COMPOSITIONS AND METHODS FOR MODULATING FXR
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Page/Page column 92; 93, (2012/07/13)
The present invention relates to compounds of Formula (I), a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesiod X receptors (FXR).
Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-Cyanopyrimidines. Part 2
Irie, Osamu,Kosaka, Takatoshi,Kishida, Masashi,Sakaki, Junichi,Masuya, Keiichi,Konishi, Kazuhide,Yokokawa, Fumiaki,Ehara, Takeru,Iwasaki, Atsuko,Iwaki, Yuki,Hitomi, Yuko,Toyao, Atsushi,Gunji, Hiroki,Teno, Naoki,Iwasaki, Genji,Hirao, Hajime,Kanazawa, Takanori,Tanabe, Keiko,Hiestand, Peter C.,Malcangio, Marzia,Fox, Alyson J.,Bevan, Stuart J.,Yaqoob, Mohammed,Culshaw, Andrew J.,Hart, Terance W.,Hallett, Allan
scheme or table, p. 5280 - 5284 (2009/05/07)
We describe here orally active and brain-penetrant cathepsin S selective inhibitors, which are virtually devoid of hERG K+ channel affinity, yet exhibit nanomolar potency against cathepsin S and over 100-fold selectivity to cathepsin L. The new
4-Amino-2-cyanopyrimidines: Novel scaffold for nonpeptidic cathepsin S inhibitors
Irie, Osamu,Yokokawa, Fumiaki,Ehara, Takeru,Iwasaki, Atsuko,Iwaki, Yuki,Hitomi, Yuko,Konishi, Kazuhide,Kishida, Masashi,Toyao, Atsushi,Masuya, Keiichi,Gunji, Hiroki,Sakaki, Junichi,Iwasaki, Genji,Hirao, Hajime,Kanazawa, Takanori,Tanabe, Keiko,Kosaka, Takatoshi,Hart, Terance W.,Hallett, Allan
scheme or table, p. 4642 - 4646 (2009/04/06)
We describe here a novel 4-amino-2-cyanopyrimidine scaffold for nonpeptidomimetic cathepsin S selective inhibitors. Some of the synthesized compounds have sub-nanomolar potency and high selectivity toward cathepsin S along with promising pharmacokinetic a
INHIBITORS OF CATHEPSIN S
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Page/Page column 81, (2008/06/13)
The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.