18522-95-7Relevant articles and documents
GRK2 INHIBITORS AND USES THEREOF
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Page/Page column 66; 68, (2021/12/08)
The present disclosure features useful methods to treat cancer, e.g., in a subject in need thereof. The methods described herein are useful in the treatment of disorders associated with GRK2 expression, e.g., cancer or cardiovascular disease. The present disclosure also features compounds (e.g., GRK2 inhibitors), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof.
NOVEL OXABOROLE ANALOGS AND USES THEREOF
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Paragraph 0219, (2018/09/21)
This application describes compounds, compositions, and methods which are useful in treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite.
Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure
Okawa, Tomohiro,Aramaki, Yoshio,Yamamoto, Mitsuo,Kobayashi, Toshitake,Fukumoto, Shoji,Toyoda, Yukio,Henta, Tsutomu,Hata, Akito,Ikeda, Shota,Kaneko, Manami,Hoffman, Isaac D.,Sang, Bi-Ching,Zou, Hua,Kawamoto, Tetsuji
, p. 6942 - 6990 (2017/09/07)
A novel class of therapeutic drug candidates for heart failure, highly potent and selective GRK2 inhibitors, exhibit potentiation of β-adrenergic signaling in vitro studies. Hydrazone derivative 5 and 1,2,4-triazole derivative 24a were identified as hit compounds by HTS. New scaffold generation and SAR studies of all parts resulted in a 4-methyl-1,2,4-triazole derivative with an N-benzylcarboxamide moiety with highly potent activity toward GRK2 and selectivity over other kinases. In terms of subtype selectivity, these compounds showed enough selectivity against GRK1, 5, 6, and 7 with almost equipotent inhibition to GRK3. Our medicinal chemistry efforts led to the discovery of 115h (GRK2 IC50 = 18 nM), which was obtained the cocrystal structure with human GRK2 and an inhibitor of GRK2 that potentiates β-adrenergic receptor (βAR)-mediated cAMP accumulation and prevents internalization of βARs in β2AR-expressing HEK293 cells treated with isoproterenol. Therefore, 115h appears to be a novel class of therapeutic for heart failure treatment.
METABOLICALLY ROBUST ANALOGS OF CYP-EICOSANOIDS FOR THE TREATMENT OF CARDIAC DISEASE
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Page/Page column 63-65, (2017/02/09)
The present invention relates to compounds according to general formula (I) which are metabolically robust analogues of bioactive lipid mediators derived from omega-3 polyunsaturated fatty acids (n-3 PUFAs).The present invention further relates to composi
ANALOGS OF CYP-EICOSANOIDS FOR USE IN TREATING OR PREVENTING A DISORDER ASSOCIATED WITH NEOVASCULARIZATION AND/OR INFLAMMATION
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Page/Page column 43; 44; 45, (2017/10/31)
The present invention relates to compounds according to general formula (I) which are metabolically robust analogues of bioactive lipid mediators derived from omega-3 polyunsaturated fatty acids (n-3 PUFAs) for use in treating or reducing the risk of deve
Dibutyltin oxide catalyzed aminolysis of oxalate to carbamate, oxamate and derivatives of imidazolidine trione
Kunde, Lalita B.,Kalyani, Vishwanath S.,Gupte, Sunil P.
experimental part, p. 402 - 407 (2010/08/06)
Catalytic aminolysis of oxalates by simple and substituted ureas has been shown to give carbamates, oxamates and derivatives of imidazolidine trione. Various substituted ureas and oxalates were screened to verify the applicability of the protocol. The rol
Novel eicosanoid derivatives
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Page/Page column 31, (2010/08/07)
The present invention provides compounds (n-3 PUFA derivatives) of formula (I): that modulate conditions associated with cardiac damage, especially cardiac arrhythmias.
Hydrogen bond patterns in solid state carboxylic acids. Vibrational behaviour of the catamer pattern as exhibited by the N-alkyloxamic acids
Wolfs, Ilse,Desseyn, Herman O.
, p. 1521 - 1528 (2007/10/03)
The vibrational study presented in this publication shows that the N-alkyloxamic acids are hydrogen bonded through a catamer hydrogen bond pattern in the solid state. Two different hydrogen bond patterns are possible for these products, and these patterns can be very clearly distinguished by their vibrational behaviour. Deuteration and low temperature spectra make the assignment and characterisation more obvious.