- POLYMERIZABLE COMPOUND, POLYMERIZABLE COMPOSITION, AND LIQUID CRYSTAL DISPLAY ELEMENT
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To provide a polymerizable compound having a high polymerizability, a high conversion ratio and a high solubility in a liquid crystal composition, a polymerizable composition containing the compound, a liquid crystal composite prepared from the compositio
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- Total synthesis of the pyranoisoflavone kraussianone 1 and related isoflavones
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The first total synthesis of the pyranoisoflavone kraussianone 1 (1) is described. The key steps involved the Suzuki-Miyaura reaction for the construction of the isoflavone core and the regioselective formation of the dimethylpyran scaffolds to the phloroglucinol (ring A) and resorcinol (ring B) moieties of kraussianone 1 (1). This route also provided access to the related isoflavones eriosemaone D (2) and genistein (3) via simple structural modifications.
- Selepe, Mamoalosi A.,Drewes, Siegfried E.,Van Heerden, Fanie R.
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experimental part
p. 1680 - 1685
(2011/02/21)
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- Trace amine-associated receptor agonists: Synthesis and evaluation of thyronamines and related analogues
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We have previously shown that several thyronamines, decarboxylated and deiodinated metabolites of the thyroid hormone, potently activate an orphan G protein-coupled receptor in vitro (TAAR1) and induced hypothermia in vivo on a rapid time scale [Scanlan, T. S.; Suchland, K. L.; Hart, M. E.; Chiellini, G.; Huang, Y.; Kruzich, P. J.; Frascarelli, S.; Crossley, D. A.; Bunzow, J. R.; Ronca-Testoni, S.; Lin, E. T.; Hatton, D.; Zucchi, R.; Grandy, D. K. 3-Iodothyronamine is an endogenous and rapid-acting derivative of thyroid hormone. Nat. Med. 2004, 10 (6), 638-642]. Herein, we report the synthesis of these thyronamines. Additionally, a large number of thyroamine derivatives were synthesized in an effort to understand the molecular basis of TAAR1 activation and hypothermia induction. Several derivatives were found to potently activate both rTAAR1 and mTAAR1 in vitro (compounds 77, 85, 91, and 92). When administered to mice at a 50 mg/kg dose, these derivatives all induced significant hypothermia within 60 min and exhibited a hypothermic induction profile analogous to 3-iodothyronamine (1, T1AM) except 91, which proved to be more efficacious. On the basis of this result, a dose-dependent profile for 91 was generated and an ED50 of 30 μmol/kg was calculated. Compound 91 proved to be more potent than T1AM for TAAR1 activation and exhibits increased potency and efficacy for hypothermia induction. These data further strengthen the pharmacological correlation linking TAAR1 activation by thyronamines and hypothermia induction in mice.
- Hart, Matthew E.,Suchland, Katherine L.,Miyakawa, Motonori,Bunzow, James R.,Grandy, David K.,Scanlan, Thomas S.
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p. 1101 - 1112
(2007/10/03)
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- Synthesis of [125I]-, [2H]-, and [ 3H]-labeled 3-iodothyronamine (T1AM)
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3-Iodothyronamine (T1AM) is a novel metabolite of thyroid hormone. In HEK-293 cells expressing an orphan G-protein coupled receptor, the trace amine receptor, T1AM, potently increased cAMP accumulation. In mice, T1AM rapid
- Miyakawa, Motonori,Scanlan, Thomas
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p. 891 - 902
(2007/10/03)
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- Vitamin D analogues
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The present invention relates to novel triaromatic compounds having the general formula (I): as well as to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology, in car
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Page column 28
(2010/02/09)
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- Biphenyl derivatives substituted by an aromatic or heteroaromatic radical and pharamaceutical and cosmetic compositions containing same
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“Biphenyl derivatives substituted with an aromatic or heteroaromatic radical, and pharmaceutical and cosmetic compositions containing them” in which: Ar represents an aromatic or a heteroaromatic radical optionally substituted, in particular, with an alkyl or a carboxyl group, R2and R3represent, in particular, H or alkyl, or R2and R3, taken together, form a 5- or 6-membered ring, R4and R5represent, in particular, H or halogen, R6represents, in particular, H or lower alkyl, and the salts of the compounds of formula (I). These compounds can be used in particular in the treatment of dermatological complaints associated with a keratinization disorder, and for combating ageing of the skin.
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- Triaromatic compounds and pharmaceutical/cosmetic compositions comprised thereof
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Novel pharmaceutically/cosmetically-active triaromatic compounds have the structural formula (I): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
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