128019-59-0Relevant academic research and scientific papers
TRICYCLIC PYRIDONES AND PYRIMIDONES
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Paragraph 0723; 0727-0729, (2021/06/26)
A compound of Formula (I) is provided: (I) where the variables are defined herein.
SPIRO-LACTAM COMPOUNDS AND METHODS OF TREATING VIRAL INFECTIONS USING THE SAME
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Page/Page column 86, (2021/12/28)
Disclosed are compounds, and pharmaceutically acceptable salts thereof, that can ameliorate or treat a viral infection in a subject in need thereof. The disclosure also includes conjugates of such compounds with a protease.
SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
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Page/Page column 51-52, (2018/03/01)
Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
COMPOUNDS FOR THE INHIBITION OF CELLULAR PROLIFERATION
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Page/Page column 113-114, (2012/02/01)
Compositions and methods for inhibiting translation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, (4) disorders associated with viral infections, and/or (5) non-proliferative metabolic disorders such as type II diabetes where inhibition of translation initiation is beneficial using the compounds disclosed herein.
Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives
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Page/Page column 30, (2010/11/24)
A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
HETEROARYL UREA DERIVATIVES USEFUL FOR INHIBITING CHKl
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Page/Page column 82; 83, (2008/06/13)
Substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division, also are disclosed.
ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
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Page/Page column 92, (2008/06/13)
The present invention relates to new compounds of formula (I) wherein A, B, P, Q, W, Rl and R2 are defined in the description; invention compounds are useful in the prevention or treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
The relationship between physicochemical properties, in vitro activity and pharmacokinetic profiles of analogues of diamine-containing efflux pump inhibitors
Watkins, William J.,Landaverry, Yakira,Leger, Roger,Litman, Renee,Renau, Thomas E.,Williams, Nicole,Yen, Rose,Zhang, Jason Z.,Chamberland, Suzanne,Madsen, Deidre,Griffith, David,Tembe, Vrushali,Huie, Keith,Dudley, Michael N.
, p. 4241 - 4244 (2007/10/03)
Following the optimization of diamine-containing efflux pump inhibitors with respect to in vitro potentiation activity, in vivo stability and acute toxicity, we addressed the question of how to control the pharmacokinetic properties of the series. Upon in
Chiral Synthesis and Enzymatic Resolution of (S)-(-)Piperazine-2-Carboxylic Acid Using Enzyme Alcalase
Wu, Guosheng,Zhao, Hua,Luo, Robert G.,Wei, Dean,Malhotra, Sanjay V.
, p. 343 - 345 (2007/10/03)
Enantiomerically pure (S)-piperazine-2-carboxylic acid was synthesized by kinetic resolution of methyl-4-(tert-butyroxycarbonyl)-piperazine-2-carboxylate using a low cost enzyme alcalase.
Design and synthesis of piperazine-based matrix metalloproteinase inhibitors
Cheng, Menyan,De, Biswanath,Pikul, Stanislaw,Almstead, Neil G.,Natchus, Michael G.,Anastasio, Melanie V.,McPhail, Sara J.,Snider, Catherine E.,Taiwo, Yetunde O.,Chen, Longyin,Dunaway, C. Michelle,Gu, Fei,Dowty, Martin E.,Mieling, Glen E.,Janusz, Michael J.,Wang-Weigand, Sherry
, p. 369 - 380 (2007/10/03)
A new generation of cyclic matrix metalloproteinase (MMP) inhibitors derived from dl-piperazinecarboxylic acid has been described. The design involves: incorporation of hydroxamic acid as the bidentate chelating agent for catalytic Zn2+, placement of a sulfonamide group at the 1N-position of the piperazine ring to fill the S1' pocket of the enzyme, and finally attachment of diverse functional groups at the 4N-position to optimize potency and peroral absorption. A unique combination of all three elements produced inhibitor 20 with high affinity for MMPs 1, 3, 9, and 13 (24, 18, 1.9, and 1.3 nM, respectively). X-ray crystallography data obtained for MMP-3 cocrystallized with 20 gave detailed information on key binding interactions defining an overall scaffold geometry for piperazine-based MMP inhibitors.
