- NOVEL NON-SYSTEMIC TGR5 AGONISTS
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The present invention relates to tricyclic compounds of formula (I) and formula (II), or a pharmaceutically acceptable salt thereof. The present tricyclic compounds are useful non-sytemic TGR5 agonists that can be used to treat diabetic diseases in human. The present invention provides a pharmaceutical composition containing tricyclic compounds of formula (I) and formula (II) and a method of making as well as a method of using same in treating patients inflicted with metabolic disorders by administering same. The compounds of the present invention may be used in combination with additional anti-diabetic drugs.
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Page/Page column 82
(2018/02/28)
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- INHIBITING THE TRANSIENT RECEPTOR POTENTIAL A1 ION CHANNEL
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The present invention relates to pharmaceutical compounds of the Formula (I), or a pharmaceutically acceptable salt or composition thereof, and methods of their use for the treatment of pain, respiratory conditions, as well as inhibiting the Transient Receptor Potential Al ion channel (TRPA1).
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- Heteroaryl and benzyl amide compounds
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Compounds of formula I wherein R1, R2, R4, R5, A, B, D and n are as defined, and pharmaceutically acceptable salts thereof, processes for their preparation, their use as pharmaceuticals and pharmaceutical compositions comprising them.
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Page/Page column 17
(2010/11/28)
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- Three chloro(trifluoromethyl)pyridines as model substrates for regioexhaustive functionalization
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As a further test of the concept of regioexhaustive functionalization, 2-chloro-6-(trifluoromethyl)pyridine, 2-chloro-5-(trifluoromethyl)pyridine and 3-chloro-4-(trifluoromethyl)-pyridine were each converted into the three possible carboxylic acids 2, 4, 6, 8, 10, 12, 16, 17 and 20. This was achieved by employing several, but not all of the organometallic "tool-box methods": transformation of a more basic organometallic species into a less basic isomer by transmetalation-equilibration, site discriminating deprotonation with lithium N,N-diisopropylamide or lithium 2,2,6,6- tetramethylpiperidide, regio-divergent iodine migration and steric screening of acidic positions by a bulky trialkylsilyl group. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004.
- Cottet, Fabrice,Schlosser, Manfred
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p. 3793 - 3798
(2007/10/03)
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- Halogen shuffling in pyridines: Site selective electrophilic substitutions of 2-chloro-6-(trifluoromethyl)pyridine
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When treated with lithium diisopropylamide in tetrahydrofuran at -85 °C and subsequently with iodine, 2-chloro-6-(trifluoromethyl)pyridine is neatly converted into its 3-iodo derivative. The latter can be quantitatively isomerized to afford 2-chloro-4-iodo-6-(trifluoromethyl)pyridine. Either iodo compound can serve as the starting material for further manipulation in reaction sequences consisting of halogen/metal exchange and electrophilic trapping.
- Mongin, Florence,Tognini, Antonio,Cottet, Fabrice,Schlosser, Manfred
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p. 1749 - 1752
(2007/10/03)
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