- HETEROCYCLIC CYTOKINE INHIBITORS
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The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. In particular, compounds of the invention are useful as anti-inflammatory, anti-pain or anti-cancer agents. There are further provided m
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Page/Page column 124
(2010/11/27)
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- COMPOUNDS USEFUL AS ANTAGONISTS OF CCR2
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The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful
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Page/Page column 52
(2008/06/13)
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- QUINAZOLINONE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS
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The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
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Page/Page column 84-85
(2008/06/13)
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- QUINOXALINES AS B RAF INHIBITORS
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The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
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Page/Page column 80-81
(2010/11/08)
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- An efficient Pd(II)-based catalyst system for carboxylation of aromatic C-H bond by addition of a phosphenium salt
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Addition of a phosphenium dramatically improved the reaction yields in the carboxylation of arenes by formic acid catalyzed by Pd(II). Control experiments revealed that the majority of the phosphenium triflate was converted to a mixed anhydride of phosphonic acid and formic acid (7), which however did not substitute for the phosphenium to improve the reaction yield.
- Sakakibara, Ken,Yamashita, Makoto,Nozaki, Kyoko
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p. 959 - 962
(2007/10/03)
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- SUBSTITUTED QUINAZOLONES AS ANTI-CANCER AGENTS
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The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
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Page/Page column 71
(2010/02/15)
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- Palladium(II)-catalyzed sequential hydroxylation-carboxylation of biphenyl using formic acid as a carbonyl source
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(Equation Presented) A simultaneous hydroxylation-carboxylation of biphenyl occurred to give 4′-hydroxy-4-biphenylcarboxylic acid, which has wide potential application as a polyester monomer.
- Shibahara, Fumitoshi,Kinoshita, Shinsuke,Nozaki, Kyoko
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p. 2437 - 2439
(2007/10/03)
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- OPIOID RECEPTOR ACTIVE COMPOUNDS
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The invention provides compounds of formula I: wherein R1 to R4 and n have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating pain and treating other conditions which involve, for example, binding opioid receptors using compounds of formula I.
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- FURTHER STUDIES ON THE EXTENDED HAMMETT EQUATION COMPRISING THE HYDROPHOBIC CONSTANT: REACTIVITY DATA FOR BENZOIC ACIDS, ARYLACETIC ACIDS, β-ARYLPROPIONIC ACIDS, trans- AND cis-CINNAMIC ACIDS, METHYL BENZOATES; DISSOCIATION CONSTANTS, DDM REACTION AND ALKALINE HYDROLYSIS IN VARIOUS W...
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The extended Hammett equation Δ = ρ? + h? comprising the hydrophobic constant ? is found to be effective in the title compounds and reactivities in various solvent mixtures.In 32 vol.percent tert-butanol-water hm decreases in the order ArCOOMe (-0.25), cis-ArCH=CHCOOH (-0.18), ArCOOH and ArCH2COOH (-0.16), ArCH2CH2COOH and trans-ArCH=CHCOOH (-0.07).For ArCOOH, mixtures like 40-60percent methanol, 50percent ethanol, 50percent acetone and 50percent dioxane give similar hm values of circa -0.05.For ArCH2COOH the effects of 3-iodo and 4-iodo substituents are acid-weakening in32percent tert-butanol.The consequences of the h? term for ρ, ?, and the averaging of ? values, are discussed.
- Hoefnagel, Anthonius J.,Wepster, Bartholomeus M.
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p. 119 - 135
(2007/10/02)
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- SELECTIVE MONO- OR DIMETALATION OF ARENES BY MEANS OF SUPERBASIC REAGENTS
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If employed in tetrahydrofuran, stoichiometric amounts of butyllithium and potassium tert-butoxide react with benzene under clean monometalation.In hexane suspension, however, considerable amounts of meta- and para-disubstituted by-products are obtained (approx. 10percent).They become preponderant if a three-fold excess of the metalating agent is used.Naphthalene leads under the same conditions to a mixture of two mono- and ten di-substituted derivatives. - Alkyl groups, as present in tert-butylbenzene, retard the metalation at both m- and p-positions, while trialkylsilyl groups deactivate only m-position.In either case exclusive monosubstitution occurs. - Perdeuterobenzene undergoes metalation and subsequent electrophilic mono- or disubstitution to afford isotope labeled compounds with moderate, though synthetically attractive yields.The kinetic isotope effects and product ratios can be taken as evidence for aggregate formation at the level of both the superbasic metalating reagent and the organometallic intermediates.
- Schlosser, Manfred,Choi, Jung Hoon,Takagishi, Sadahito
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p. 5633 - 5648
(2007/10/02)
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