cas 157327-43-0, TERT-BUTYL 3-ACETYL-4-OXOPIPERIDINE-1-CARBOXYLATE

Articles about 157327-43-0Total 12 be found

Pyrazolyl-pyrimidones inhibit the function of human solute carrier protein SLC11A2 (hDMT1) by metal chelation
Solute carrier proteins (SLCs) control fluxes of ions and molecules across biological membranes and represent an emerging class of drug targets. SLC11A2 (hDMT1) mediates intestinal iron uptake and its inhibition might be used to treat iron overload diseases such as hereditary hemochromatosis. Here we report a micromolar (IC50 = 1.1 μM) pyrazolyl-pyrimidone inhibitor of radiolabeled iron uptake in hDMT1 overexpressing HEK293 cells acting by a non-competitive mechanism, which however does not affect the electrophysiological properties of the transporter. Isothermal titration calorimetry, competition with calcein, induced precipitation of radioactive iron and cross inhibition of the unrelated iron transporter SLC39A8 (hZIP8) indicate that inhibition is mediated by metal chelation. Mapping the chemical space of thousands of pyrazolo-pyrimidones and similar 2,2′-diazabiaryls in ChEMBL suggests that their reported activities might partly reflect metal chelation. Such metal chelating groups are not listed in pan-assay interference compounds (PAINS) but should be checked when addressing SLCs.
Embaby, Ahmed,Hediger, Matthias A.,Javor, Sacha,Manatschal, Cristina,Poirier, Marion,Reymond, Jean-Louis,Bühlmann, Sven,Pujol-Giménez, Jonai
p. 1023 - 1031
(2020/10/06)

BICYCLIC BIS-HETEROARYL DERIVATIVES AS MODULATORS OF PROTEIN AGGREGATION
The present invention relates to certain bicyclic bis-heteroaryl compounds of Formula (I), pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and
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Page/Page column 35; 36

(2018/09/08)

NEW ANTIBACTERIAL COMPOUNDS
The present invention relates to novel antibacterial compounds, pharmaceutical compositions containing them and their use as antimicrobials.
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Page/Page column 67-69

(2016/07/05)

Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses
FTY720 is the first oral small molecule approved for the treatment of people suffering from relapsing-remitting multiple sclerosis. It is a potent agonist of the S1P1 receptor, but its lack of selectivity against the S1P3 receptor ha
Demont, Emmanuel H.,Bailey, James M.,Bit, Rino A.,Brown, Jack A.,Campbell, Colin A.,Deeks, Nigel,Dowell, Simon J.,Eldred, Colin,Gaskin, Pam,Gray, James R. J.,Haynes, Andrea,Hirst, David J.,Holmes, Duncan S.,Kumar, Umesh,Morse, Mary A.,Osborne, Greg J.,Renaux, Jessica F.,Seal, Gail A. L.,Smethurst, Chris A.,Taylor, Simon,Watson, Robert,Willis, Robert,Witherington, Jason
p. 1003 - 1020
(2016/02/23)

EZH2 INHIBITORS AND USES THEREOF
The present invention provides compound of formula 1, or an isotopic form, a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, a polymorph, a prodrug, S-oxide or N-oxide thereof. The invention also relates toprocesses for their preparation, to pharmaceutical compositions containing them and use of the compound of formula 1, in the treatment of diseases or disorders mediated by EZH2 (enhancer of zeste homolog 2), particularly cancer.
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(2015/08/06)

AMINOQUINAZOLINE DERIVATIVES AND THEIR SALTS AND METHODS OF USE
The present invention relates to the field of medicine. Provided herein are aminoquinazoline derivatives, their salts and pharmaceutical formulations useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. Also provided herein are pharmaceutically acceptable compositions comprising the aminoquinazoline compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
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(2014/08/19)

An organocatalytic asymmetric allylic alkylation allows enantioselective total synthesis of hydroxymetasequirin-a and metasequirin-b tetramethyl ether diacetates
The first highly stereoselective organocatalytic intermolecular allylic alkylation of allylic alcohols with 1,3-dicarbonyls has been developed to allow the first enantioselective total synthesis of hydroxymetasequirin-A and metasequirin-B tetramethyl ethe
Wang, Pu-Sheng,Zhou, Xiao-Le,Gong, Liu-Zhu
supporting information
p. 976 - 979
(2014/03/21)

AMINOQUINAZOLINE DERIVATIVES AND THEIR SALTS AND METHODS OF USE
The present invention relates to the field of medicine. Provided herein are aminoquinazoline derivatives, their salts and pharmaceutical formulations useful in modulating the protein tyrosine kinase activity, and in modulating inter-and/or intra-cellular signaling. Also provided herein are pharmaceutically acceptable compositions comprising the aminoquinazoline compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
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(2013/06/05)

Discovery of novel tetrahydro-pyrazolo [4,3-c] pyridines for the treatment of neuropathic pain: Synthesis and neuropharmacology
We disclose the discovery of a novel series of tetrahydropyrido-pyrazoles that are potent inhibitors of tumour necrosis factor-alpha (TNF-α), nitric oxide and cannabinoid receptor subtype 1 (CB1). We report herein the synthesis and neuropharmacological screening results of the titled compounds in two acute pain and two neuropathic pain models in rodents. Particularly the analogue N-(4-bromophenyl)-3-tert-butyl-5-ethyl-4,5,6,7-tetrahydro-1H- pyrazolo[4,3-c]pyridine-1-carboxamide (8a) exhibited pronounced acute antinociceptive efficacy, also being effective in chronic constriction injury (ED50 = 23.8 mg/kg) and partial sciatic nerve injury (ED50 = 29.0 mg/kg) models with CB1 receptor activity (IC50 = 49.6 nM) and inhibitory effect on TNF-α (86.4% inhibition at 100 mg/kg). These results suggest the importance of the development of this lead as multi-targeted treatment strategy for neuropathic pain.
Yogeeswari, Perumal,Sharma, Monika,Samala, Ganesh,Gangadhar, Matharasala,Karthick, Srirama,Mallipeddi, Saketh,Semwal, Arvind,Sriram, Dharmarajan
p. 211 - 220
(2013/10/01)

THIADIAZOLE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF DISORDERS MEDIATED BY SLPL RECEPTORS
The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
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Page/Page column 28-29

(2010/12/31)

Guanidine derivatives
The invention relates to the guanine derivatives of general formula (I), and to hydrates or solvents thereof, for use as neuropeptide FF receptor antagonists in the treatment of pains and hyperalgesia, of withdrawal symptoms of addiction to alcohol, psych
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(2008/06/13)

GUANIDINE DERIVATIVES
The invention relates to the guanine derivatives of general formula (I), and to hydrates or solvents thereof, for use as neuropeptide FF receptor antagonists in the treatment of pains and hyperalgesia, of withdrawal symptoms of addiction to alcohol, psychotropic drugs or nicotine and in the prevention of or recovery from these addictions, for the regulation of insulin release, food intake, memory functions, blood pressure, electrolyte and energy metabolism, and in the treatment of urinary incontinence.
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Page/Page column 37

(2008/06/13)