cas 156496-89-8, tert-Butyl 5-oxo-5,6-dihydropyridine-1(2H)-carboxylate

Articles about 156496-89-8Total 13 be found

CHOLINE METABOLISM INHIBITORS
The present disclosure relates to compounds, compositions and methods for inhibiting choline metabolism, e.g., conversion of choline to trimethylamine. Disclosed herein are compounds, compositions, and methods for inhibiting choline metabolism, e.g., conversion of choline to TMA. Also disclosed herein are compounds, methods and compositions for inhibiting choline metabolism by gut microbiota resulting in reduction in the formation of trimethylamine (TMA) and trimethylamine N-oxide (TMAO).
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(2020/07/05)

Discovery of a Cyclic Choline Analog That Inhibits Anaerobic Choline Metabolism by Human Gut Bacteria
The anaerobic conversion of choline to trimethylamine (TMA) by the human gut microbiota has been linked to multiple human diseases. The potential impact of this microbial metabolic activity on host health has inspired multiple efforts to identify small molecule inhibitors. Here, we use information about the structure and mechanism of the bacterial enzyme choline TMA-lyase (CutC) to develop a cyclic choline analog that inhibits the conversion of choline to TMA in bacterial whole cells and in a complex gut microbial community. In vitro biochemical assays and a crystal structure suggest that this analog is a competitive, mechanism-based inhibitor. This work demonstrates the utility of structure-based design to access inhibitors of radical enzymes from the human gut microbiota.
Bollenbach, Maud,Ortega, Manuel,Orman, Marina,Drennan, Catherine L.,Balskus, Emily P.
supporting information
p. 1980 - 1985
(2020/11/09)

DIPEPTIDE PIPERIDINE DERIVATIVES
The disclosure relates to pharmaceutical compositions, to methods of preparing such compositions, and to methods for using such compositions for treating or preventing a disease or condition associated with arginase activity.
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Paragraph 0294-0297; 0512-0514

(2019/10/17)

INHIBITORS OF ACTIVIN RECEPTOR-LIKE KINASE
Described herein are compounds that inhibit ALK2 and its mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
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Page/Page column 240

(2017/11/10)

PYRROLO[2,3-B]PYRIDINE CDK9 KINASE INHIBITORS
Disclosed are compounds of Formula (IIa), wherein R1, R2, R3A, R3B, R3C, R3D, R3E, and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (IIa)
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Page/Page column 815; 816

(2014/09/29)

Preparation of Z-α,β-unsaturated diazoketones from aldehydes. Application in the construction of substituted dihydropyridin-3-ones
The stereoselective preparation of α,β-unsaturated diazoketones with Z geometry is described from aldehydes and a new olefination reagent. When prepared from amino aldehydes, these diazoketones could be converted to substituted dihydropyridin-3-ones in just one step, after an intramolecular N-H insertion reaction. The straightforward synthesis of a natural trihydroxylated piperidine demonstrates the utility of these unsaturated diazoketones for the rapid construction of piperidines.
Rosset, Isac G.,Burtoloso, Antonio C. B.
p. 9464 - 9470
(2013/10/08)

SUBSTITUTED CYCLIC COMPOUNDS AND METHODS OF USE
The present invention provides novel substituted cyclic compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
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Paragraph 0248

(2013/09/26)

HYDROXAMATE-BASED INHIBITORS OF DEACETYLASES
The present teachings relate to compounds of Formula I and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, ring A, and ( formula II) are as defined herein. The present teachin
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Page/Page column 41

(2012/03/26)

COMPOUNDS, COMPOSITIONS AND METHODS USEFUL FOR CHOLESTEROL MOBILISATION
The invention relates to classes of pharmaceutically-active heterocyclic compounds and pharmaceutically acceptable salts, and hydrates thereof, and compositions comprising the same. The invention also relates to methods for treating or preventing a disease or disorder, which comprises administering a therapeutically or prophylactically effective amount a compound described herein.
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Page/Page column 178; 179

(2012/05/05)

Hydroxamate-Based Inhibitors of Deacetylases
The present teachings relate to compounds of Formula I: and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, ring A, and are as defined herein. The present teachings also provi
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Page/Page column 23

(2011/04/14)

Synthesis of 2-aza-1-cyano-4-hydroxyanthraquinones
Phthalide annulation of 2-alkylpyridin-3-ones results in the formation of the unexpected 2-aza-1-cyano-4-hydroxy-anthraquinones, the cyano moiety originating from the 3-cyanophthalide. These compounds hold great potential against Epstein-Barr Virus Early
Claessens, Sven,Jacobs, Jan,De Kimpe, Norbert
p. 741 - 744
(2008/01/06)

Synthesis of 3-oxooxa- and 3-oxoazacycloalk-4-enes by ring-closing metathesis. Application to the synthesis of an inhibitor of cathepsin K
3-Oxooxa- and 3-oxoazacycloalk-4-enes were obtained with good yield from 1-(ω-alkenyloxy)- and 1-(ω-alkenylamino)-but-3-en-2-ones by using a ring-closing metathesis. This methodology has been used to synthesize an inhibitor of cathepsin K.
Taillier, Catherine,Hameury, Thomas,Bellosta, Véronique,Cossy, Janine
p. 4472 - 4490
(2008/02/01)

Reversal of regiochemistry in the synthesis of isoxazoles by nitrile oxide cycloadditions
The isoxazolines 2a, 2b and 8 obtained from nitrile oxide cycloadditions to cyclohex-2-enone 1a and its analogues 1b and 7 reacted with nickel peroxide to give the isoxazoles 3a, 3b, and 9. In contrast, the correponding 2-bromocyclohex-2-enones 4a, 4b and
Easton,Easton, Christopher J.,Hughes,Merricc Hughes,Tiekink,Tiekink, Edward R. T.,Lubin,Lubin, Carolyn E.,Savage,Paul Savage,Simpson,Simpson, Gregory W.
p. 3589 - 3592
(2007/10/02)