- BICYCLIC FUSED PYRIDINE COMPOUNDS AS INHIBITORS OF TAM KINASES
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Provided herein are compounds of the Formula (I): and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein Ring A, X1, X2, X3, R1, R2 and R3 are as defined herein
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Paragraph 00433
(2019/06/23)
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- PYRAZOLOPYRIMIDINE DERIVATIVES AS BTK INHIBITORS FOR THE TREATMENT OF CANCER
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This invention relates to novel compounds. The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK). The invention also contemplates the use of t
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Paragraph 00349; 00350
(2017/05/02)
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- NOVEL 5 OR 8-SUBSTITUTED IMIDAZO [1, 5-a] PYRIDINES AS INDOLEAMINE AND/OR TRYPTOPHANE 2, 3-DIOXYGENASES
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Disclosed herein are 5 or 8-substituted imidazo[l,5-a]pyridines and pharmaceutical compositions comprising at least one such 5 or 8-substituted imidazo[l,5-a]pyridines, processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain 5 or 8- substituted imidazo[l,5-a]pyridines that can be useful for inhibiting indoleamine 2,3- dioxygenase and/or tryptophane 2,3-dioxygenase and for treating diseases or disorders mediated thereby.
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Paragraph 0482
(2016/10/31)
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- SPIRO[CYCLOBUTANE-1,3'-INDOLIN]-2'-ONE DERIVATIVES AS BROMODOMAIN INHIBITORS
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The present invention provides novel spiro[cyclobutane-1,3'-indolin]-2'- derivatives of formula (I) in which Cy R1, R2, R4, L and 'm' are have the meaning given in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful as bromodomain inhibitors in the treatment or prevention of diseases or disorders where bromodomain inhibition is desired.
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Page/Page column 62
(2017/01/02)
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- PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
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Compounds of the formula I or II: wherein X, m, Ar, R1 and R2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.
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Page/Page column 59
(2012/02/01)
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- The Grob/Eschenmoser fragmentation of cycloalkanones bearing β-electron withdrawing groups: A general strategy to acyclic synthetic intermediates
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Introduction of a β-electron withdrawing group to cycloalkanones allows facile C-C bond fragmentation. The reaction has been demonstrated with a large range of ring sizes, bearing various leaving and electron withdrawing groups, and using a variety of nitrogen and oxygen containing nucleophiles (>30 examples). The application of fragmentation products to the preparation of substituted γ-lactones has been demonstrated. Mechanistic studies are reported which are suggestive of a Grob/Eschenmoser type reaction.
- Hierold, Judith,Hsia, Tina,Lupton, David W.
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scheme or table
p. 783 - 792
(2011/03/21)
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- Novel electrochemical deoxygenation reaction using diphenylphosphinates
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The electrochemical reduction of diphenylphosphinate esters leads smoothly and in high yields to the corresponding deoxygenated products. In comparison with the previously developed methodologies, the electrolysis could be performed at lower temperature and with a higher current density, resulting in a shorter reaction time.
- Lam, Kevin,Marko, Istvan E.
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supporting information; experimental part
p. 406 - 409
(2011/04/18)
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- Chemoselective chemical and electrochemical deprotections of aromatic esters
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Alcohols can be easily and chemoselectively deprotected from the corresponding aromatic esters by using either SmI2/HMPA or by electrolysis In the presence of a proton source.
- Lam, Kevin,Marko, Istvan E.
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experimental part
p. 2752 - 2755
(2009/11/30)
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- Toluates: unexpectedly versatile reagents
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The mechanism of the monoelectronic reduction of aromatic esters has been investigated. The unexpected synthetic utility of the toluate moiety in the deoxygenation of alcohols and the allylation of ketones is also reported. Finally, the use of aromatic esters as robust, though easily removable, protecting groups is depicted.
- Lam, Kevin,Markó, István E.
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experimental part
p. 10930 - 10940
(2010/02/28)
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- Modulators of 11- beta hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same
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The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1 and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1.
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Page/Page column 50
(2010/11/28)
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- Facile cleavage of silyl protecting groups with catalytic amounts of FeCl3
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A very mild and environmentally benign method for removal of silyl protecting groups using catalytic amounts of iron ion in MeOH is presented. The method is particularly effective for cleaving triethylsilyl (TES) protecting groups. Georg Thieme Verlag Stuttgart.
- Yang, Yong-Qing,Cui, Jia-Rong,Zhu, Lin-Gui,Sun, Ya-Ping,Wu, Yikang
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p. 1260 - 1262
(2007/10/03)
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- A general efficient strategy for cis-3a-aryloctahydroindole alkaloids via stereocontrolled ZnBr2-catalyzed rearrangement of 2,3-aziridino alcohols
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(Matrix presented) A short and general approach to the cis-3a-aryloctahydroindole alkaloids has been developed on the basis of a key stereocontrolled ZnBr2-catalyzed rearrangement of 2,3-aziridino alcohols. Two representative members, (±)-crina
- Song, Zhen Lei,Wang, Bao Min,Tu, Yong Qiang,Fan, Chun An,Zhang, Shu Yu
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p. 2319 - 2321
(2007/10/03)
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- Fused pyrimidines, their production and use
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New fused pyrimidines of the general formula (I): STR1 wherein the ring A is a pyridine ring which may be hydrogenated or a benzene ring which may be hydrogenated, X is an amino group or a hydroxyl group, R1, R2, R3 and R
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