- SUBSTITUTED TRIAZINONES AS THYROID HORMONE RECEPTOR AGONISTS
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The application relates to a compound of Formula (I') or (I), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of thyroid hormone receptors, a pharmaceutical composition comprising a compound of Formula (I') or (I), and a method of treating or preventing a disease or disorder regulated by thyroid hormone.
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Paragraph 00421-00422
(2021/07/24)
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- ANTIVIRAL PYRIDOPYRAZINEDIONE COMPOUNDS
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The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by herpesviruses.
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Paragraph 0731-0732
(2020/04/09)
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- SUBSTITUTED 1,2-DIHYDRO-3H-PYRROLO[1,2-C]IMIDAZOL-3-ONE ANTIBACTERIAL COMPOUNDS
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The invention relates to antibacterial compounds of formula (I) wherein M is one of the groups MA, MB and MC represented below wherein R1, MA, MB and MC are as defined in the specification; and to salts thereof.
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Page/Page column 89-90
(2017/03/21)
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- Phosphothreonine as a Catalytic Residue in Peptide-Mediated Asymmetric Transfer Hydrogenations of 8-Aminoquinolines
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Phosphothreonine (pThr) was found to constitute a new class of chiral phosphoric acid (CPA) catalyst upon insertion into peptides. To demonstrate the potential of these phosphopeptides as asymmetric catalysts, enantioselective transfer hydrogenations of a previously underexplored substrate class for CPA-catalyzed reductions were carried out. pThr-containing peptides lead to the observation of enantioselectivities of up to 94:6 e.r. with 2-substituted quinolines containing C8-amino functionality. NMR studies indicate that hydrogen-bonding interactions promote strong complexation between substrates and a rigid β-turn catalyst.
- Shugrue, Christopher R.,Miller, Scott J.
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supporting information
p. 11173 - 11176
(2016/07/06)
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- Polysubstituted Pyridinylaminoalkylene- and Pyridinyloxyalkylene-Cyclopropanamine Compounds, a Process for Their Preparation and Pharmaceutical Compositions Containing Them
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Compounds of formula (I): wherein: n represents an integer of from 1 to 6 inclusive, X represents an oxygen atom or an NR6 group, Y represents a carbon atom or a nitrogen atom,Z represents a carbon atom or a nitrogen atom,R1 and R2 represent a hydrogen atom or an alkyl or arylalkyl group,R3 and R4 represent a hydrogen atom or an alkyl group, R5 represents a hydrogen atom or an alkyl, halogen, hydroxy, alkoxy, cyano, nitro, acyl, alkoxycarbonyl, trihaloalkyl, trihaloalkoxy or optionally substituted amino group, R6 represents a hydrogen atom or an alkyl or arylalkyl group,Ra, Rb, Rc, Rd and Re are as defined in the description. Medicinal products containing the same which are useful as specific nicotinic ligands of α4β2 receptors.
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Page/Page column 7
(2010/12/29)
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- Preparation and affinity profile of novel nicotinic ligands
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Novel nicotinic ligands, characterized by the presence of an amino substituted cyclopropane ring connected to a pyridine nucleus, are described. Pharmacological investigation revealed that these compounds exhibit highest affinity for the rat α4β2 subtype of the nicotinic receptor with no affinity for the muscarinic receptor. No appreciable affinity for the muscular or for the ganglionic nicotinic receptor was observed at concentrations up to 10 μM. The increase in cortical ACh release as well as a positive effect on memory in a social recognition test in rat are exemplified.
- Charton, Yves,Guillonneau, Claude,Lockhart, Brian,Lestage, Pierre,Goldstein, Solo
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p. 2188 - 2193
(2008/12/22)
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- Polysubstituted 1,1-pyridylamioncyclopropanamine compounds
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A compound selected from those of formula (I): wherein: n represents an integer from 1 to 6 inclusive, R1 and R2 represent a hydrogen atom, a (C1-C6)alkyl group or an aryl-(C1-C6)alkyl grou
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Page/Page column 6
(2010/11/25)
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- Cyclopropyl building blocks for organic synthesis, 58(+): A new short access to amino acids incorporating an aminocyclopropyl moiety from N,N-dibenzylcarboxamides
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Our recently reported titanium-mediated transformation of N,N-dialkylcarboxamides to cyclopropylamines has been applied to N,N-dibenzyl-2-benzyloxyacetamide using a variety of alkylmagnesium bromides to yield 1-(benzyloxymethyl)-1-(dibenzylamino)cyclopropane (15a, 48percent) and 2-substituted analogs 15b-f (33-48percent). These have been transformed in just a few steps into N-Boc-protected methyl esters of 1-aminocyclopropanecarboxylic acid (1, 29percent overall), coronamic acid (2, 35percent) and norcoronamic acid (21percent), 2,3-methanoglutamic acid (21g, 19percent) and 2,3-methanoornithine (211, 12percent). Similarly, the corresponding derivatives of 3,4-methano-γ-aminobutyric acid (26, 23percent) and 4-spirocyclopropane-γ-butyrolactam (32, 44percent) have been synthesized.
- Kordes, Markus,Winsel, Harald,De Meijere, Armin
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p. 3235 - 3245
(2007/10/03)
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- N-Adamantane-substituted tetrapeptide amides
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N-Adamantane-substituted tetrapeptide amides and the pharmacologically acceptable salts thereof are disclosed herein. These compounds are analogs of enkephalin wherein the methionine or leucine of position 5 has been substituted by an adamantyl amide and the glycine of position 2 has been substituted by various amino acid residues. Optionally the tyrosine of position 1 and the phenylalanine of position 4 may be substituted by various amino acid residues. These compounds exhibit agonist activity at opiate receptor sites and are useful as analgesics.
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