18835-02-4Relevant academic research and scientific papers
AZETIDINE CYCLIC UREAS
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Page/Page column 222, (2021/11/26)
Provided are azetidine cyclic urea compounds that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF
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Paragraph 00561, (2020/09/27)
Provided herein are compounds, compositions, and methods useful for inhibiting protein tyrosine phosphatase, e.g., protein tyrosine phosphatase non-receptor type 2 (PTPN2) and/or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and for treating related diseases, disorders and conditions favorably responsive to PTPN 1 or PTPN2 inhibitor treatment, e.g., a cancer or a metabolic disease.
COMPOUNDS AND THEIR USE AS INHIBITORS OF N-MYRISTOYL TRANSFERASE
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Page/Page column 98, (2017/01/23)
This invention provides compounds of formula (I) and salts thereof, which have activity as inhibitors of N-myristoyl transferase (NMT). The invention also relates to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of N-myristoyl transferase provides a therapeutic or prophylactic effect, including protozoan infections (such as malaria and leishmaniasis), viral infections (such as human rhinovirus and HIV), and hyperproliferative disorders (such as B-cell lymphoma).
Synthesis of diverse acyclic precursors to pyrroles for studies of prebiotic routes to tetrapyrrole macrocycles
Chandrashaker, Vanampally,Ptaszek, Marcin,Taniguchi, Masahiko,Lindsey, Jonathan S.
, p. 8786 - 8808 (2016/10/13)
A chemical model for the origin of tetrapyrrole macrocycles under prebiotic conditions entails the condensation of acyclic dicarbonyl compounds and α-aminoketones to form pyrroles that are equipped for subsequent self-condensation. Development and exploration of the scope of the chemical model (including combinatorial reactions, studies of the effects of structurally defective substrates, and reactions in aqueous or organic media) have relied on the availability of diverse starting materials prepared by traditional chemical synthesis methods. Here the synthesis of all acyclic dicarbonyl compounds and α-aminoketones used in the prior prebiotic model studies is described. There are five sets of acyclic dicarbonyl compounds including (i) β-ketoesters bearing diverse 4-substituents, (ii) levulinic acid derivatives bearing selected 5-substituents (i.e., analogues of δ-aminolevulinic acid, ALA), (iii) meso-substituted β-ketoesters, (iv) meso-substituted β-diketones that contain one 4-substituent, and (v) hybrid molecules that contain both the β-ketoacyl unit and the levulinic acid skeleton (or homologue thereof). A variety of α-aminoketones (homologues of ALA) also have been prepared. Altogether, the synthesis of 53 compounds is described, encompassing 28 new compounds as well as 25 known compounds that have been more fully characterized or prepared via alternative routes. The ability to convert selected acyclic compounds directly via pyrroles to porphyrinogens in a single-flask process may also prove useful in mainstream syntheses of diverse tetrapyrroles regardless of possible prebiotic relevance.
Regioswitchable Palladium-Catalyzed Decarboxylative Coupling of 1,3-Dicarbonyl Compounds
Kenny, Miles,Christensen, Jeppe,Coles, Simon J.,Franckeviius, Vilius
supporting information, p. 3926 - 3929 (2015/08/19)
A palladium-catalyzed chemo- and regioselective coupling of 1,3-dicarbonyl compounds via an allylic linker has been developed. This reaction, which displays broad substrate scope, forms two C-C bonds and installs two all-carbon quaternary centers. The regioselectivity of the reaction can be predictably controlled by utilizing an enol carbonate of one of the coupling partners.
Design and synthesis of high affinity inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferases directed by ligand efficiency dependent lipophilicity (LELP)
Rackham, Mark D.,Brannigan, James A.,Rangachari, Kaveri,Meister, Stephan,Wilkinson, Anthony J.,Holder, Anthony A.,Leatherbarrow, Robin J.,Tate, Edward W.
supporting information, p. 2773 - 2788 (2014/04/17)
N-Myristoyltransferase (NMT) is an essential eukaryotic enzyme and an attractive drug target in parasitic infections such as malaria. We have previously reported that 2-(3-(piperidin-4-yloxy)benzo[b]thiophen-2-yl)-5-((1,3, 5-trimethyl-1H-pyrazol-4-yl)meth
An expedient approach for the synthesis of 1-Alkyl-4-propionylpyrrolidin-2- ones
Saadi, Fatma,Jebali, Khaoula,Arfaoui, Aicha,Amri, Hassen
, p. 42 - 48 (2013/11/06)
A simple and useful tandem addition-cyclization reaction of primary amines on a prepared α-functionalized propylvinyl ketone 3 in methanol at reflux is a promising route for the synthesis of a new family of 1-alkyl-4- propionylpyrrolidin-2-ones 4. Taylor and Francis Group, LLC.
NOVEL COMPOUNDS AND THEIR USE IN THERAPY
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Page/Page column 115, (2013/06/27)
The invention provides compounds which inhibit N-myristoyltransferase and are selective for protozoal N-myristoyltransferase and, consequently suitable to treat microbial infections, including viral and fungal infections, and protozoan infections such as malaria, leishmaniasis and sleeping sickness.
Catalytic decarboxylative alkenylation of enolates
Schroeder, Sybrin P.,Taylor, Nicholas J.,Jackson, Paula,Franckevicius, Vilius
supporting information, p. 3778 - 3781 (2013/08/23)
A palladium-catalyzed decarboxylative alkenylation of stabilized enolates has been developed, which gives rise to alkenylated dicarbonyl products from enol carbonates regioselectively with concomitant installation of a quaternary all-carbon center. The broad scope of the reaction has been demonstrated by successfully utilizing a range of enolates and external phenol nucleophiles.
Synthesis and photochemical characteristics of novel tribenzoporphyrazines possessing peripherally annulated tetrahydrodiazepine and diazepine rings
Goslinski, Tomasz,Piskorz, Jaroslaw,Brudnicki, Dawid,White, Andrew J.P.,Gdaniec, Maria,Szczolko, Wojciech,Tykarska, Ewa
scheme or table, p. 1004 - 1011 (2011/05/14)
Novel tribenzoporphyrazines possessing peripherally annulated tetrahydrodiazepine and diazepine rings were synthesized and characterized, and the substituent effects on their absorption spectra in various solvents and on singlet oxygen generation were stu
