158688-63-2Relevant articles and documents
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
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Page/Page column 100; 102, (2020/01/31)
This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
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Page/Page column 174-175; 176, (2020/07/31)
This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
CYANO-SUBSTITUTED HETEROCYCLES WITH ACTIVITY AS INHIBITORS OF USP30
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Page/Page column 90, (2018/04/21)
The present invention relates to cyano-substituted-heterocycles of Formula (I) with activity as inhibitors of deubiquitilating enzymes, in particular, ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30), having utility in a variety of therapeutic areas including cancer and conditions involving mitochondrial dysfunction. (Formula (I))
CYANOPYRROLIDINE DERVIVATIVES AS INHIBITORS FOR DUBS
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Page/Page column 42, (2017/07/14)
The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of Cezanne 1 and ubiquitin C-terminal hydrolase 30 or Ubiquitin Specific Peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of cancer. Compounds of the invention include compounds having the formula (I): pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c, R1d, R1e, R1f and A are as defined herein.
Facile synthesis of fluorinated 1-desazapurines
Iaroshenko, Viktor O.,Sevenard, Dmitri V.,Volochnyuk, Dmitriy M.,Wang, Yan,Martiloga, Alexander,Tolmachev, Andrei O.
experimental part, p. 1865 - 1875 (2009/12/30)
A preparative approach towards 1-desazapurines, starting from 4(5)-aminoimidazoles and polyfluoroalkyl-containing 1,3-CCC-biselectrophiles was developed. As a result, a set of fluorinated 1-desazapurines was synthesized. Additionally, a synthetic route to 1-desazapurines bearing a sugar-mimicking group is proposed. Georg Thieme Verlag Stuttgart.
Reduction of 1-Aryl-4-Nitroimidazoles to 4-Amino-1-Arylimidazoles
Suwinski, J.,Walczak, K.
, p. 675 - 682 (2007/10/02)
1-aryl-4-nitroimidazoles on reduction with hydrogen in methanol at 25 degC, in the presence of Raney nickel, yield the unstable 4-amino-1-aryl-imidazoles which can be acylated e.g. with pentafluorophenyl formate, formic acid in the presence of dicyclohexy