84440-19-7Relevant articles and documents
SUBSTITUTED BICYCLE HETEROCYCLIC DERIVATIVES USEFUL AS ROMK CHANNEL INHIBITORS
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Page/Page column 107, (2018/06/06)
Disclosed are compounds of Formula (I) or a salt thereof, wherein R1 is (II) or (III); each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3, L1, L2, R1a, R1b, R1c, and n are define herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.
Investigation of copper-free alkyne/azide 1,3-dipolar cycloadditions using microwave irradiation
Chatkewitz, Lindsay E.,Halonski, John F.,Padilla, Marshall S.,Young, Douglas D.
supporting information, p. 81 - 84 (2017/12/28)
The prevalence of 1,3-dipolar cycloadditions of azides and alkynes within both biology and chemistry highlights the utility of these reactions. However, the use of a copper catalyst can be prohibitive to some applications. Consequently, we have optimized
SUBSTITUTED NITROGEN CONTAINING COMPOUNDS
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Page/Page column 85; 86, (2019/01/05)
Disclosed are compounds of Formula (I): or a salt thereof, Formula (II) wherein R1 is: or; each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3a, R3b, L1, B, V, Y, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.
Synthesis of N-unsubstituted 1,2,3-triazoles via a cascade including propargyl azides, allenyl azides, and triazafulvenes
Banert, Klaus,Hagedorn, Manfred,Hemeltjen, Claudia,Ihle, Andreas,Weigand, Kevin,Priebe, Hanno
, p. 338 - 361 (2016/11/21)
About thirty NH-1,2,3-triazoles with at least one additional functional group in a side chain at C-4 were prepared from propargyl substrates. These reactions included propargyl azides and their [3,3]-sigmatropic rearrangement to generate short-lived allenyl azides, which cyclized to form triazafulvenes that could be trapped by addition of N- or O-nucleophiles. In most cases, simple substrates and cheap sodium azide were utilized as starting compounds, and the syntheses were performed by using a one-pot procedure without isolation of any dangerous azides. This method to prepare NH-1,2,3-triazoles turned out to be compatible with quite different substitution patterns of the propargyl substrate.
MONOBACTAM ORGANIC COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
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Paragraph 0456, (2015/11/10)
This invention pertains generally to antibacterial compounds of Formula I, as further described herein, and pharmaceutically acceptable salts and formulations thereof. In certain aspects, the invention pertains to methods of using such compounds to treat infections such as those caused by Gram-negative bacteria.
Water-soluble NHC-Cu catalysts: Applications in click chemistry, bioconjugation and mechanistic analysis
Daz Velzquez, Heriberto,Ruiz Garca, Yara,Vandichel, Matthias,Madder, Annemieke,Verpoort, Francis
supporting information, p. 9350 - 9356 (2014/12/11)
Copper(i)-catalyzed 1,3-dipolar cycloaddition of azides and terminal alkynes (CuAAC), better known as "click" reaction, has triggered the use of 1,2,3-triazoles in bioconjugation, drug discovery, materials science and combinatorial chemistry. Here we report a new series of water-soluble catalysts based on N-heterocyclic carbene (NHC)-Cu complexes which are additionally functionalized with a sulfonate group. The complexes show superior activity towards CuAAC reactions and display a high versatility, enabling the production of triazoles with different substitution patterns. Additionally, successful application of these complexes in bioconjugation using unprotected peptides acting as DNA binding domains was achieved for the first time. Mechanistic insight into the reaction mechanism is obtained by means of state-of-the-art first principles calculations.
Optimizing the control of apoptosis by amide/triazole isosteric substitution in a constrained peptoid
Corredor, Miriam,Bujons, Jordi,Orzáez, Mar,Sancho, Mónica,Pérez-Payá, Enrique,Alfonso, Ignacio,Messeguer, Angel
, p. 892 - 896 (2013/07/27)
Apoptosis is a biological process relevant to several human diseases that is strongly regulated through protein-protein complex formation. We have previously reported a peptidomimetic compound as potent apoptotic modulator. Structural studies of this comp
15N NMR spectroscopic and theoretical GIAO-DFT studies for the unambiguous characterization of disubstituted 1,2,3-triazoles
Corredor, Miriam,Bujons, Jordi,Messeguer, Angel,Alfonso, Ignacio
, p. 7318 - 7325 (2013/10/22)
The 1,2,3-triazole ring has recently attracted a renewed interest as a structural scaffold with many applications in different fields. However, very often, the unambiguous assignment of the correct structure is not an easy task, and the development of rob
SYNTHESIS AND USE OF THERAPEUTIC METAL ION CONTAINING POLYMERIC PARTICLES
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, (2012/04/05)
Therapeutic particles contain metal ions and are characterized by the use of unique ligand sets capable of making the metal ion complex soluble in biological media to induce selective toxicity in diseased cells. The particles may comprise a polymeric base particle, at least one pharmaceutically active metal ion, including metal ions from more than one metal element, a ligand that is covalently attached to the polymeric base particle and attached to the metal ion via a stimuli-responsive bond, and a cell targeting component. When the metal ion-containing particle enters a pre-defined environment, the ligands binding the metal to the particle are broken, triggering release of the free metal ion while the original ligands remain covalently bound to the particle.
METHODS OF USING DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY (ADP-RIBOSE)POLYMERASE (PARP)
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Page/Page column 151-152, (2011/11/01)
Provided herein are methods of treating cancer comprising administering a topoisomerase inhibitor, temozolomide, or a platin in combination with a Compound of Formula (I) or Formula (II), where the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein.