- Bulk Inclusions of Double Pyridazine Molecular Rotors in Hexagonal Tris(o-phenylene)cyclotriphosphazene
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A new generation of double pyridazine molecular rotors differing in intramolecular dipole-dipole spacing was synthesized. All rotor molecules formed bulk inclusions in a tris(o-phenylenedioxy)cyclotriphosphazene (TPP) host. Results of dielectric spectroscopy were fitted to a pair of nine-state models that accounted for interactions of neighboring dipoles at either an aligned or opposed possible orientation of the local threefold dipole rotation potentials within a channel of the TPP host. The results indicate dipole-dipole interaction strengths at the 100 to 200 K scale that lead dipoles to preferentially populate a subset of low-energy configurations. They also reveal that pyridazines with ethynyl substituents in 3- and 6-positions have slightly higher rotational barriers (3.2-3.5 kcal/mol) than those carrying one ethynyl and one tert-butyl group (1.9-3.0 kcal/mol). Upon cooling, these barriers reduce the rate of thermal transitions between the potential wells so much that the inclusions cannot achieve ordered dipolar ground states.
- Kaleta, Ji?í,Bastien, Guillaume,Wen, Jin,Dra?ínsky, Martin,Tortorici, Edward,Císa?ová, Ivana,Beale, Paul D.,Rogers, Charles T.,Michl, Josef
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- COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY
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The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.
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Page/Page column 96; 97
(2008/12/08)
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- Endothelin receptor antagonists
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This invention relates to pyridizinone derivatives of formula I STR1 wherein the various substituents are defined in the specification, and salts thereof, which have useful pharmacological properties, in particular endothelin receptor-antagonistic properties. The compounds are thus useful for the treatment of illnesses associated with endothelin activities, such as hypertension, cardiac insufficiency, coronary heart disease, renal, cerebral and myocardial ischaemia, renal insufficiency, cerebral infarct, subarachnoid haemorrhage, arteriosclerosis pulmonary high blood pressure, inflammations, asthma, prostate hyperplasia, endotoxic shock and in complications after the administration of immunosuppressants which produce renal vasoconstriction.
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- One-pot preparation of 6-substituted 3(2H)-pyridazinones from ketones
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A one-pot process for the preparation of 6-phenyl-3(2H)-pyridazinone from acetophenone and glyoxylic acid has been investigated and shown to have wide utility in the preparation of 6- and 5,6-substituted 3(2H)-pyridazinones. Limitations to the process encountered with 2'-hydroxyacetophenone and with basic hetero-aromatic ketones have been overcome, and the processes described offer the rapid and efficient synthesis of many 6-substituted pyridazinones from readily available ketones.
- Coates,McKillop
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p. 334 - 342
(2007/10/02)
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