- NON-LYSOSOMAL GLUCOSYLCERAMIDASE INHIBITORS AND USES THEREOF
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The invention provides compounds for inhibiting glucosylceramidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.
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- HORMONE RECEPTOR MODULATORS FOR TREATING METABOLIC CONDITIONS AND DISORDERS
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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.
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- ISOXAZOLYL-CARBONYLOXY AZABICYCLO[3.2.1]OCTANYL COMPOUNDS AS FXR ACTIVATORS
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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.
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- COMPOSITIONS AND METHODS FOR MODULATING FXR
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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).
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Page/Page column 92; 93
(2012/07/13)
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- Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-Cyanopyrimidines. Part 2
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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
- 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
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scheme or table
p. 5280 - 5284
(2009/05/07)
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- 4-Amino-2-cyanopyrimidines: Novel scaffold for nonpeptidic cathepsin S inhibitors
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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
- 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
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scheme or table
p. 4642 - 4646
(2009/04/06)
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- INHIBITORS OF CATHEPSIN S
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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.
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Page/Page column 81
(2008/06/13)
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