416852-69-2Relevant academic research and scientific papers
MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE
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Page/Page column 22, (2019/01/16)
Provided are IDO inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases. Formula I
Organocatalytic Stereoconvergent Synthesis of α-CF3 Amides: Triketopiperazines and Their Heterocyclic Metamorphosis
Foster, Robert W.,Lenz, Eva N.,Simpkins, Nigel S.,Stead, Darren
supporting information, p. 8810 - 8813 (2017/07/11)
The highly enantioselective alkylation of α-CF3 enolates, generated from triketopiperazines, has been accomplished through use of a bifunctional thiourea organocatalyst to facilitate 1,4-addition to varied enone acceptors. On treatment with appropriate nitrogen nucleophiles, the chiral triketopiperazine products undergo a metamorphosis, to provide novel fused heterocyclic lactams such as extended pyrazolopyrimidines.
PIPERIDINE DERIVATIVES AND METHODS OF USE THEREOF
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Page/Page column 72, (2008/12/08)
The present invention relates to Compounds of Formula (I), compositions comprising the compounds, and methods of using the compounds to treat or prevent pain, diabetes, a diabetic complication, impaired glucose tolerance (IGT) or impaired fasting glucose (IFG) in a patient.
Novel substituted (pyridin-3-yl)phenyloxazolidinones: Antibacterial agents with reduced activity against monoamine oxidase A and increased solubility
Reck, Folkert,Zhou, Fei,Eyermann, Charles J.,Kern, Gunther,Carcanague, Dan,Ioannidis, Georgine,Illingworth, Ruth,Poon, Grace,Gravestock, Michael B.
, p. 4868 - 4881 (2008/03/12)
Oxazolidinones represent a new and promising class of antibacterial agents. Current research in this area is mainly concentrated on improving the safety profile and the antibacterial spectrum. Oxazolidinones bearing a (pyridin-3-yl)phenyl moiety (e.g., 3) generally show improved antibacterial activity compared to linezolid but suffer from potent monoamine oxidase A (MAO-A) inhibition and low solubility. We now disclose the finding that new analogues of 3 with acyclic substituents on the pyridyl moiety exhibit excellent activity against Gram-positive pathogens, including linezolid-resistant Streptococcus pneumoniae. Generally, more bulky substituents yielded significantly reduced MAO-A inhibition relative to the unsubstituted compound 3. The MAO-A SAR can be rationalized on the basis of docking studies using a MAO-A/MAO-B homology model. Solubility was enhanced with incorporation of polar groups. One optimized analogue, compound 13, showed low clearance in the rat and efficacy against S. pneumoniae in a mouse pneumonia model.
3- `4- {6-SUBSTITUTED ALKANOYL) PYRIDIN-3-YL} -3-PHENYL! -5- (1H-1, 2, 3-TRIAZOL-1-YLMETHYL) -1, 3-OXAZOLIDIN-2-ONES AS ANTIBACTERIAL AGENTS
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Page/Page column 54-55, (2010/02/15)
Compounds of formula (I) as well as pharmaceutically-acceptable salts and pro-drugs thereof are disclosed wherein R1, R2, R3, and R4 are defined herein. Also disclosed are processes for making compounds of formula (I) as well as methods of using compounds of formula (I) for treating bacterial infections.
BENZIMIDAZOLONE DERIVATIVES
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Page 50, (2010/11/30)
This invention relates to benzimidazolone derivatives, represented by compounds of a general formula [I] ???[in which R1 and R2 stand for, e.g., hydrogen atoms; R3a, R3b, R4, R5 stand for, e.g., hydrogen atoms and alkyl groups; R6 stands for e.g., aryl or heteroaryl groups; A ring stands for 5- to 8-membered aliphatic heterocyclic ring containing one nitrogen atom; and Z stands for carbonyl group or sulfonyl group]. The benzimidazolone derivatives of the invention exhibit antagonism to muscarinic acetylcholine receptors, and are useful as treating agent and/or prophylactic of Parkinson's disease; drug-induced parkinsonism, dystonia, akinesia, pancreatitis, bilestone/cholecystitis, biliary dyskinesia, achalasia, pain, itch, cholinergic urticaria, irritable bowel syndrome, vomiting, nausea, dizziness, Meniere's disease, motion sickness and urinary disturbance.
Piperidine-containing β-arylpropionic acids as potent antagonists of αvβ3/αvβ5 integrins
De Corte, Bart L.,Kinney, William A.,Liu, Li,Ghosh, Shyamali,Brunner, Livia,Hoekstra, William J.,Santulli, Rosemary J.,Tuman, Robert W.,Baker, Judith,Burns, Candace,Proost, Jef C.,Tounge, Brett A.,Damiano, Bruce P.,Maryanoff, Bruce E.,Johnson, Dana L.,Galemmo Jr., Robert A.
, p. 5227 - 5232 (2007/10/03)
The synthesis and SAR of a new class of piperidine-based αvβ3/αvβ5 integrin antagonists is described.
1,2,3,4-Tetrahydroquinoline-containing αVβ 3 integrin antagonists with enhanced oral bioavailability
Ghosh, Shyamali,Santulli, Rosemary J.,Kinney, William A.,DeCorte, Bart L.,Liu, Li,Lewis, Joan M.,Proost, Jef C.,Leo, Gregory C.,Masucci, John,Hageman, William E.,Thompson, Andrew S.,Chen, Ian,Kawahama, Reiko,Tuman, Robert W.,Galemmo Jr., Robert A.,Johnson, Dana L.,Damiano, Bruce P.,Maryanoff, Bruce E.
, p. 5937 - 5941 (2007/10/03)
Selective reduction of the quinoline yielded potent α vβ53 antagonists with improved oral bioavailability relative to the corresponding quinoline derivatives. Reduction of the quinoline ring in an αvβ3 antagonist yielded a 1,2,3,4-tetrahydro derivative as two diastereomers, the four isomers of which were separated by sequential chiral HPLC. Two isomers had significant αVβ3 antagonist activity with improved oral bioavailability, relative to the corresponding quinoline derivative.
PIPERIDINYL COMPOUNDS THAT SELECTIVELY BIND INTEGRINS
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Page 104, (2010/11/30)
The invention is directed to piperidinyl compounds of formula (I) and (II) that selectively bind integrin receptors and methods for treating an integrin mediated disorder, wherein W, R2, Z and q are described in the application.
