- PYRROLOTRIAZINE INHIBITORS OF IRAK4 ACTIVITY
-
The present invention relates to pyrrolotriazine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
- -
-
Page/Page column 46; 47
(2016/09/26)
-
- PYRAZOLOPYRIMIDINE INHIBITORS OF IRAK4 ACTIVITY
-
The present invention relates to pyrazolopyrimidine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
- -
-
Page/Page column 71; 72
(2016/09/26)
-
- Enhanced rate and selectivity by carboxylate salt as a basic cocatalyst in chiral N-heterocyclic carbene-catalyzed asymmetric acylation of secondary alcohols
-
The rate and enantioselectivity of chiral NHC-catalyzed asymmetric acylation of alcohols with an adjacent H-bond donor functionality are remarkably enhanced in the presence of a carboxylate cocatalyst. The degree of the enhancement is correlated with the basicity of the carboxylate. With a cocatalyst and a newly developed electron-deficient chiral NHC, kinetic resolution and desymmetrization of cyclic diols and amino alcohols were achieved with extremely high selectivity (up to s = 218 and 99% ee, respectively) at a low catalyst loading (0.5 mol %). This asymmetric acylation is characterized by a unique preference for alcohols over amines, which are not converted into amides under the reaction conditions.
- Kuwano, Satoru,Harada, Shingo,Kang, Bubwoong,Oriez, Raphael,Yamaoka, Yousuke,Takasu, Kiyosei,Yamada, Ken-Ichi
-
p. 11485 - 11488
(2013/09/02)
-
- Scope of the directed dihydroxylation: Application to cyclic homoallylic alcohols and trihaloacetamides
-
The synthesis and directed dihydroxylation of a range of cyclic alkenes was investigated. Both homoallylic alcohols and homoallylic trihaloacetamides were found to be efficient directing groups, giving rise to good to excellent levels of remote asymmetric induction with OsO4-TMEDA. Interestingly, in all cases examined, trifluoroacetamides were found to be superior to trichloroacetamides as directing groups and an argument is presented which rationalises this observation.
- Donohoe, Timothy J.,Mitchell, Lee,Waring, Michael J.,Helliwell, Madeleine,Bell, Andrew,Newcombe, Nicholas J.
-
p. 2173 - 2186
(2007/10/03)
-
- Synthesis of [3H2]-(R,R)-1,2-diaminocyclohexaneoxalatoplatinum(II), [3H2]-oxaliplatin
-
A synthesis of [3H2]-(R,R)-1,2-diaminocyclohexaneoxalatoplatinum(II), [3H2]-Oxaliplatin, 2, is described, rac-trans-4-Cyclohexene-1,2- dicarboxylic acid diethyl ester, 6, was converted to rac-trans-1,2- diaminoc
- Burgos, Alain,Ellames, George J.
-
p. 443 - 449
(2007/10/03)
-
- 2-Methyl-4,5-dihydroimidazole as a Doubly Nucleophilic Unit: Preparation of Dihydroimidazole Azaprostanoids
-
2-Methyl-4,5-dihydroimidazole is incorporated as a doubly nucleophilic synthon, by successive alkylations at N-1 and C-2(Me), into monocyclic 9,12- and 8,11-diazaprostanoids containing the dihydroimidazole moiety. 2-Methyl-3a,4,7,7a-tetrahydrobenzimidazole is prepared (from 1,2,3,6-tetrahydrophthalic anhydride) and elaborated in the same way into a diazaprostacyclin precursor.
- Jones, Raymond C. F.,Schofield, Julie
-
p. 375 - 383
(2007/10/02)
-
- Detectable molecules, method of preparation and use
-
A detectable molecule of the formula where A3 is A2 or a polymer, where A3 has at least one modifiable reactive group selected from the group consisting of amino, hydroxy, cis .OH, halides, aryl, imidazoyl, carbonyl, carboxy, thiol or a residue comprising an activated carbon; --X-- is selected from the group consisting of STR1 a C1 -C10 branched or unbranched alkyl or aralkyl, which may be substituted by --OH; --Y-- is a direct bond to --E--, or --Y-- is --E--R2 -- where R2 is a C1 -C10 branched or unbranched alkyl; Za is chlorine, bromine or iodine; E is O, NH or an acylic divalent sulfur atom; Detb is a chemical moiety capable of being detected, preferably comprising biotin or a metal chelator of the formula: STR2 or the 4-hydroxy or acyloxy derivative thereof, where R3 is C1 -C4 alkyl or CH2 COOM, M is the same or different and selected from the group consisting of hydrogen, a metal or non-metal cation or is C1 -C10 alkyl, aryl or aralkyl; and m is an integer from 1 to the total number of modified reactive groups on A3. The detectable molecules are useful in in vitro or in vivo assays or therapy.
- -
-
-