429677-00-9Relevant academic research and scientific papers
Structure-activity relationships for a series of (Bis(4-fluorophenyl)methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability
Giancola, JoLynn B.,Bonifazi, Alessandro,Cao, Jianjing,Ku, Therese,Haraczy, Alexandra J.,Lam, Jenny,Rais, Rana,Coggiano, Mark A.,Tanda, Gianluigi,Newman, Amy Hauck
, (2020/09/17)
Despite considerable efforts to develop medications to treat psychostimulant use disorders, none have proven effective, leaving an underserved patient population and unanswered questions as to what mechanism(s) of action should be targeted for developing
ATYPICAL INHIBITORS OF MONOAMINE TRANSPORTERS; METHOD OF MAKING; AND USE THEREOF
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Paragraph 0094; 0095; 0102, (2019/05/30)
Disclosed herein are a series of modafinil analogue compounds that bind with moderate to high affinity to the dopamine (DA) transporter (DAT) and several analogues also having affinity for the serotonin (5-HT) transporter (SERT) and/or sigma-1 receptor. E
INHIBITORS OF BACTERIAL GLYCOSYL TRANSFERASES
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Paragraph 00546; 00547-00548, (2016/12/22)
Described herein are compounds of Formula (I'), Formula (IA), Formulae (I)-(VII), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrug sthereof. The invention also provides pharmaceutical compositions of the compounds for human and veterinary use. Compounds of the present invention are useful for inhibiting bacterial growth and therefore are useful in treating and/or preventing bacterial infections. Methods of using the compounds for treating and/or preventing a bacterial infection in a subject are also described.
QUINOLINE DERIVATIVES USEFUL AS CB-1 INVERSE AGONISTS
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Paragraph 0582, (2015/09/23)
The present invention is directed to quinoline derivatives, pharmaceutical compositions containing said derivatives and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, in the treatment of disorders
QUINOLINE DERIVATIVES USEFUL AS CB-1 INVERSE AGONISTS
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Paragraph 0578, (2015/09/28)
The present invention is directed to quinoline derivatives, pharmaceutical compositions containing said derivatives and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, in the treatment of disorders
PYRAZINE COMPOUNDS FOR TREATING GPR119 RELATED DISORDERS
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Page/Page column 65, (2009/10/21)
The application relates to compounds of Formula (Ia), and pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers and N-oxides thereof. The application also relates to pharmaceutical compositions comprising t
Nonpeptide inhibitors of cathepsin G: Optimization of a novel β-ketophosphonic acid lead by structure-based drug design
Greco, Michael N.,Hawkins, Michael J.,Powell, Eugene T.,Almond Jr., Harold R.,Corcoran, Thomas W.,De Garavilla, Lawrence,Kauffman, Jack A.,Recacha, Rosario,Chattopadhyay, Debashish,Andrade-Gordon, Patricia,Maryanoff, Bruce E.
, p. 3810 - 3811 (2007/10/03)
The serine protease cathepsin G (EC 3.4.21.20; Cat G), which is stored in the azurophilic granules of neutrophils (polymorphonuclear leukocytes) and released on degranulation, has been implicated in various pathological conditions associated with inflammation. By employing high-throughput screening, we identified β-ketophosphonic acid 1 as a moderate inhibitor of Cat G (IC50 = 4.1 μM). We were fortunate to obtain a cocrystal of 1 with Cat G and solve its structure by X-ray crystallography (3.5 A). Structural details from the X-ray analysis of 1·Cat G served as a platform for optimization of this lead compound by structure-based drug design. With the aid of molecular modeling, substituents were attached to the 3-position of the 2-naphthyl ring of 1, which occupies the S1 pocket of Cat G, to provide an extension into the hydrophobic S3 region. Thus, we arrived at analogue 7 with an 80-fold potency improvement over 1 (IC50 = 53 nM). From these results, it is evident that the β-ketophosphonic acid unit can form the basis for a novel class of serine protease inhibitors. Copyright
