167993-22-8Relevant academic research and scientific papers
1-PHENYL-2-PYRIDINYL ALKYL ALCOHOL DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
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Paragraph 0543; 0645, (2014/06/23)
Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and are useful for the prevention and/or treatment of an allergic disease state or a disease of the respiratory tract characterized by airway obstruction.
DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
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Paragraph 0754, (2013/04/10)
The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
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Page/Page column 150; 151, (2013/04/13)
The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
Thiourea and benzamide compounds, compositions and methods of treating or preventing inflammatory diseases and atherosclerosis
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, (2008/06/13)
The present invention provides compounds of formula (I). The present invention also provides methods of treating or preventing inflammation or atherosclerosis, and a pharmaceutical composition that contains a compound of formula (I).
Fine tuning of the cation affinity of artificial receptors based on cyclic peptides by intramolecular conformational control
Kubik, Stefan,Goddard, Richard
, p. 311 - 322 (2007/10/03)
A series of cyclic hexapeptides consisting of alternating 4-substituted 3-aminobenzoic acid units (R = CH3, Cl, CH2OCH3, OCH3, COOCH3) and residues of the natural amino acid proline has been prepared and their ion affinities have been investigated. Whereas the unsubstituted parent compound (R = H) is able to bind cations through cation-π interactions with the aromatic subunits, as well as anions through hydrogen bonding with the peptide NH groups, the introduction of substituents at the 4-positions of the aromatic rings results in complete loss of the anion affinity. The cation complex stabilities depend on the substituents and cover a wide range from Ka = 140 M-1 for R = CH3 to Ka = 10800 M-1 for R = COOCH3 (Ka = 1260 M-1 for R = H) with n-butyltrimethylammonium picrate. The conformations of the peptides in solution have been determined by one-and two-dimensional NMR techniques and FT-IR spectroscopy. It was found that all the substituents prevent the peptides from adopting the necessary conformation for anion binding. For one receptor (R = OCH3), the results have been corroborated by a crystal structure determination. AM1 calculations have been used to estimate the electrostatic potential surfaces of the substituted aromatic subunits. The variation in the cation complex stabilities can be mainly attributed to the effects of the substituents on the solution conformations of the peptides. The influence of the substituents on the electrostatic potentials of the aromatic peptide subunits appears to be less important.
