68679-84-5Relevant academic research and scientific papers
CYCLIC TETRAMER COMPOUNDS AS PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) INHIBITORS FOR THE TREATMENT OF METABOLIC DISORDERS
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Paragraph 0636-0637, (2020/06/16)
The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein R1, R1, R1, R1, R1, R1, R1, R1, R1, X1, X2, and X3 are described herein.
Enantioselective redox-relay oxidative heck arylations of acyclic alkenyl alcohols using boronic acids
Mei, Tian-Sheng,Werner, Erik W.,Burckle, Alexander J.,Sigman, Matthew S.
supporting information, p. 6830 - 6833 (2013/06/05)
A general, highly selective asymmetric redox-relay oxidative Heck reaction using achiral or racemic acyclic alkenols and boronic acid derivatives is reported. This reaction delivers remotely functionalized arylated carbonyl products from acyclic alkenol substrates, with excellent enantioselectivity under mild conditions, bearing a range of useful functionality. A preliminary mechanistic investigation suggests that the regioselectivity of the initial migratory insertion is highly dependent on the electronic nature of the boronic acid and more subtle electronic effects of the alkenyl alcohol.
Catalytic asymmetric reductive acyl cross-coupling: Synthesis of enantioenriched acyclic α,α-disubstituted ketones
Cherney, Alan H.,Kadunce, Nathaniel T.,Reisman, Sarah E.
supporting information, p. 7442 - 7445 (2013/06/27)
The first enantioselective Ni-catalyzed reductive acyl cross-coupling has been developed. Treatment of acid chlorides and racemic secondary benzyl chlorides with a NiII/bis(oxazoline) catalyst in the presence of Mn0 as a stoichiometric reductant generates acyclic α,α-disubstituted ketones in good yields and high enantioselectivity without requiring stoichiometric chiral auxiliaries or pregeneration of organometallic reagents. The mild, base-free reaction conditions are tolerant of a variety of functional groups on both coupling partners.
SUBSTITUTED PYRAZOLE COMPOUNDS AS LPAR ANTAGONISTS
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Page/Page column 38, (2014/01/09)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, pulmonary fibrosis
A combination of in vivo selection and cell sorting for the identification of enantioselective biocatalysts
Fernandez-Alvaro, Elena,Snajdrova, Radka,Jochens, Helge,Davids, Timo,Boettcher, Dominique,Bornscheuer, Uwe T.
supporting information; experimental part, p. 8584 - 8587 (2011/11/07)
The "carrot and stick" principle could be combined with cell sorting to enable the selection of enantioselective esterase variants from a mutant library. Hence, the enormous diversity generated in directed evolution experiments is now easily accessible by this high-throughput system. In line with the principle, the hydrolysis of 1 glycerin supports cell growth, whereas the hydrolysis of 2 leads to cell death. Copyright
Controlling chiral organization of molecular rods on Au(111) by molecular design
Knudsen, Martin M.,Kalashnyk, Nataliya,Masini, Federico,Cramer, Jacob R.,Laegsgaard, Erik,Besenbacher, Flemming,Linderoth, Trolle R.,Gothelf, Kurt V.
supporting information; experimental part, p. 4896 - 4905 (2011/05/16)
Chiral self-assembled structures formed from organic molecules adsorbed on surfaces have been the subject of intense investigation in the recent decade, owing both to relevance in applications such as enantiospecific heterogeneous catalysis or chiral sepa
Natural diversity to guide focused directed evolution
Jochens, Helge,Bornscheuer, Uwe T.
experimental part, p. 1861 - 1866 (2011/11/29)
Simultaneous multiple site-saturation mutagenesis was performed at four active-site positions of an esterase from Pseudomonas fluorescens to improve its ability to convert 3-phenylbutyric acid esters (3-PBA) in an enantioselective manner. Based on an appropriate codon choice derived from a structural alignment of 1751 sequences of α/β-hydrolase fold enzymes, only those amino acids were considered for library creation that appeared frequently in structurally equivalent positions. Thus, the number of mutants to be screened could be substantially reduced while the number of functionally intact variants was increased. Whereas the wild-type esterase showed only marginal activity and poor enantioselectivity (Etrue=3.2) towards 3-PBA-ethyl ester, a significant number of hits with improved rates (up to 240-fold) and enantioselectivities (up to Etrue=80) were identified in these "smart" libraries.
Pyrazolopyrimidines as therapeutic agents
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, (2008/06/13)
The present invention is directed to pyrazolopyrimidine derivatives of formula (I) wherein the substituents are defined herein, which are useful as kinase inhibitors and as such are useful for affecting angiogenesis and diseases and conditions associated with angiogenesis.
Pyrazolopyrimidines as therapeutic agents
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, (2008/06/13)
The present invention provides compounds of Formula I, including pharmaceutically acceptable salts and/or prodrugs thereof, where G, R2, and R3 are defined as described herein.
A,3-Allylic Strain as a Control Element in the Paterno-Buechi Reaction of Chiral Silyl Enol Ethers: Synthesis of Diastereomerically Pure Oxetanes Containing Four Contiguous Stereogenic Centers
Bach, Thorsten,Joedicke, Kai,Kather, Kristian,Froehlich, Roland
, p. 2437 - 2445 (2007/10/03)
The facial diastereoselectivity in the Paterno-Buechi reaction of chiral enol ethers and benzaldehyde was studied. The substituents (RS, RL) at the stereogenic carbon atom (-C*HRSRL) attached to the β-position o
