- TREATMENT OF DRY EYE
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The present disclosure provides a method of treating dry eye by inhibition of Bruton's tyrosine kinase (hereinafter "BTK") inhibitors, pharmaceutical formulations comprising the same, and processes for preparing such compounds.
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Page/Page column 106; 107
(2014/02/16)
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- Tyrosine kinase inhibitors
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The present disclosure provides compounds such as pyrazolpyrimidine compounds, and pharmaceutically acceptable salts thereof, that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
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Page/Page column 251
(2014/03/26)
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- TYROSINE KINASE INHIBITORS
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The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
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Page/Page column 226-227
(2012/12/13)
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- Mild one-step synthesis of dibromo compounds from cyclic ethers
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A novel one-step method for mildly converting cyclic ethers into dibromo compounds is reported. Alcohols, oximes, aldehydes, and ketones are known to react under Appel or Corey-Fuchs reaction conditions, but apparently these have never been applied to oxetanes or larger cyclic ethers. Treatment of 3,3-dimethyloxetane (1) with tetrabromomethane and triphenylphosphine gave the corresponding dibromo compound 1,3-dibromo-2,2-dimethylpropane (2). The less-strained homologue oxolane (6) was also reacted giving 1,4-dibromobutane (7) in a 93% yield. Mechanistic interpretations are offered to explain the observed reaction rates of the conversions described.
- Billing, Peter,Brinker, Udo H.
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p. 11227 - 11231
(2013/02/23)
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- Cyclic Trimerization of Oxetanes
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Conditions for obtaining the optimum yield of the cyclic trimer in the cationic oligomerization of oxetanes have been determined.At moderate dilution (0.05 M) with catalytic quantities of BF3 in CH2Cl2, the yield of the cyclic trimer (1,5,9-trioxacyclododecane) from oxetane could be increased to 50percent at the expense of the cyclic tetramer (1,5,9,13-tetraoxacyclohexadecane), 12percent, and polymer.In contrast, 3,3-dimethyloxetane consumed the BF3 catalyst, which had to be renewed, producing, in a slow reaction, a homologous series of fluorohydrins, together with cyclic oligoethers.The fluorohydrins cyclized if treated with gaseous BF3 before work-up, boosting the isolated yields to 20percent cyclic trimer and 8percent cyclic tetramer.With PF5 in CH2Cl2 the catalyst was stable and the reaction fast, and no fluorohydrins were formed; no cyclic trimer but 73percent cyclic tetramer could be isolated.Other solvents (benzene, CHCl=CCl2, CH2ClCH2Cl), other catalysts (SbF5, AlEt3) and other oxetanes (3-methoxymethyl-3-methyloxetane, 3-halomethyl-3-methyloxetane) were also examined.
- Dale, Johannes,Fredriksen, Siw B.
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- Asymmetric Synthesis of (+)-Hirsutene
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The asymmetric total synthesis of (+)-hirsutene from the regio- and enantioselective 1,4-γ-addition reaction of (-)-(S)-allyl p-tolyl sulfoxide and 2-methyl-2-cyclopentenone is presented.In this total synthesis, a facile ring closure reaction involving enol thioether and enol acetate moieties and the deoxygenation reaction of a highly hindered secondary alcohol via its 2-propanesulfonate were found.An unexpected displacement reaction at the sulfur atom of alkenyl sulfoxides and the addition reactions of the cis sulfinylallyl anions with cyclic enones were also observed during the studies.
- Hua, Duy H.,Venkataraman, S.,Ostrander, Robert A.,Sinai, Gurudas-Z.,McCann, Peggy J.,et al.
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p. 507 - 515
(2007/10/02)
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