- SUBSTITUTED OXOPYRIDINE DERIVATIVES
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The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular vascular disorders, preferably thrombotic
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Page/Page column 66
(2020/07/14)
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- 3-ARYL-2H-PYRAZOLO[4,3-b]PYRIDINE COMPOUNDS AND THEIR USE AS AMPA RECEPTOR MODULATORS
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Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, N-oxides, or solvates thereof, Also provided herein are pharmaceutical compositions comprising compounds of Formula (I) and methods of using compounds of Formula (I).
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Paragraph 0198; 0199
(2018/05/03)
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- Compounds Having CRTH2 Antagonist Activity
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Compounds of general formula (I) wherein W is chloro or fluoro; Z is a group SO2R1; wherein R1 is —C3-C8 cycloalkyl or heterocyclyl optionally substituted with one or more substituents chosen from hal
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Page/Page column 15
(2009/08/14)
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- COMPOUNDS HAVING CRTH2 ANTAGONIST ACTIVITY
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Compounds of general formula (I): wherein W is chloro or fluoro; Z is a group SO2R1; wherein R1 is -C3-C8 cycloalkyl or heterocyclyl optionally substituted with one or more substituents chosen from halo, -CN, -C1-C6 alkyl, -SOR3, -SO2R3, -SO2N(R2)2, -N(R2)2, -NR2C(O)R3, -CO2R2, -CONR2R3, -NO2, -OR2, -SR2, -O(CH2)POR2, and - O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, -Ci-C6 alkyl, -C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, -C1-C6 alkyl, -C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
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Page/Page column 44
(2009/09/05)
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- Dynamic models for the thermal deazetization of 2,3-diazabicyclo[2.2.1]hept-2-ene
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Kinetic studies on the thermal nitrogen extrusion from 2,3-diazabicyclo[2.2.1]hept-2-ene-exo,exo-5,6-d2 are reported. The ratio of rate constants for formation of the label-isomeric products (bicyclo[2.1.0]pentane-exo,exo-2,3-d2 and -endo,endo-2,3-d2) is found to exhibit no statistically significant temperature dependence. A comparison of gas-phase and solution-phase results is presented. The results are interpreted in terms of two complementary dynamic models. In the first, classical trajectory calculations are run on a three-dimensional projection (two geometric coordinates) of the potential energy hypersurface. These calculations correctly identify the major product, and reproduce the near temperature-independence of the rate-constant ratio, but do not match the ratio quantitatively. Modification of the trajectory calculations to simulate the effect of collisions with solvent molecules also qualitatively matches the observed difference between gas-phase and solution-phase behavior. In the second model, the vector of atomic displacements corresponding to the reaction coordinate at the transition state for nitrogen loss is identified by both semiempirical and ab initio calculations. The components of this vector pointing along the paths to the post-transition-state minima are computed and are shown to lead to a prediction of the product ratio that is in good (if partly fortuitous) agreement with the experimental result. The vector model is used to predict isotope effects on the product ratio, which are then investigated experimantally with 2,3-diazabicyclo[2.2.1]hept-2-ene-endo,endo-1,4,5,6,7,7-d6 and -endo-7-d.
- Lyons, Barbara A.,Pfeifer, J?rg,Peterson, Thomas H.,Carpenter, Barry K.
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p. 2427 - 2437
(2007/10/02)
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- SMALL RING COMPOUNDS-XLI. CYCLOBUTENE CYCLOADDITIONS; SYNTHESIS AND REACTIVITY IN THE BICYCLOHEXAN-2-ONE SERIES
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Cyclobutene, prepared by base-induced elimination from tosyloxycyclobutane 19 undergoes cycloaddition with ethyl propiolate in the presence of AlCl3 to provide ethyl bicyclohex-2-ene-2-carboxylate 20.This cycloadduct at room temperature and in the presence of AlCl3 undergoes forbidden ring opening into ethyl cyclohexa-1,3-diene-2-carboxylate 21.The cycloaddition of cyclobutene with dichloroketene provides 3,3-dichlorobicyclohexan-2-one 24 and after reductive halogen removal the endo 3-chloro bicyclohexan-2-one 28 (the first study of this strained system).However, further dechlorination of 28 results in rearrangement and fragmentation reactions.
- Fadel, A.,Salauen, J.,Conia, J. M.
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p. 1567 - 1574
(2007/10/02)
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