107202-38-0Relevant academic research and scientific papers
IMIDAZOPYRIDAZINES AS MODULATORS OF IL-17
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Page/Page column 211, (2021/11/06)
The present application discloses compounds having the following formula: (I), or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined in the specification, as well as methods of making and using the compounds disclosed herein for treating or ameliorating an IL-17 mediated syndrome, disorder and/or disease.
A chiral organic base catalyst with halogen-bonding-donor functionality: Asymmetric Mannich reactions of malononitrile with: N -Boc aldimines and ketimines
Kuwano, Satoru,Suzuki, Takumi,Hosaka, Yusei,Arai, Takayoshi
supporting information, p. 3847 - 3850 (2018/04/19)
A chiral organic base catalyst with halogen-bonding-donor functionality has been developed. This quinidine-derived acid/base catalyst smoothly promoted the asymmetric Mannich reaction of malononitrile and various N-Boc imines with up to 98% ee. The cooperative interaction with both substrates was responsible for the high activity that allowed a reduction of the catalyst amount to 0.5 mol%.
PYRROLO [2, 3 - B] PYRAZINE - 7 - CARBOXAMIDE DERIVATIVES AND THEIR USE AS JAK AND SYK INHIBITORS
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Page/Page column 137, (2011/12/04)
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula (I), wherein the variables Q and R, R2, and R3 are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
Synthesis of novel potent hepatitis C virus NS3 protease inhibitors: Discovery of 4-hydroxy-cyclopent-2-ene-1,2-dicarboxylic acid as a N-acyl-l-hydroxyproline bioisostere
Thorstensson, Fredrik,Wangsell, Fredrik,Kvarnstroem, Ingemar,Vrang, Lotta,Hamelink, Elizabeth,Jansson, Katarina,Hallberg, Anders,Rosenquist, Asa,Samuelsson, Bertil
, p. 827 - 838 (2007/10/03)
Potent tetrapeptidic inhibitors of the HCV NS3 protease have been developed incorporating 4-hydroxy-cyclopent-2-ene-1,2-dicarboxylic acid as a new N-acyl-l-hydroxyproline mimic. The hydroxycyclopentene template was synthesized in eight steps from commercially available (syn)-tetrahydrophthalic anhydride. Three different amino acids were explored in the P1-position and in the P2-position the hydroxyl group of the cyclopentene template was substituted with 7-methoxy-2-phenyl-quinolin-4-ol. The P3/P4-positions were then optimized from a set of six amino acid derivatives. All inhibitors were evaluated in an in vitro assay using the full-length NS3 protease. Several potent inhibitors were identified, the most promising exhibiting a Ki value of 1.1 nM.
HCV NS-3 SERINE PROTEASE INHIBITORS
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Page/Page column 110, (2008/06/13)
Peptidomimetic compounds are described which inhibit the NS3 protease of the hepatitis C virus (HCV). The compounds have the formula where the variable definitions are as provided in the specification. The compounds comprise a carbocyclic P2 unit in conjunction with a novel linkage to those portions of the inhibitor more distal to the nominal cleavage site of the native substrate, which linkage reverses the orientation of peptidic bonds on the distal side relative to those proximal to the cleavage site.
