52505-46-1Relevant articles and documents
GLUCOSE UPTAKE INHIBITORS AND USES THEREOF
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Paragraph 00491, (2021/05/21)
The present invention relates to novel compounds that modulate cellular glucose uptake by affecting various targets, including, but not limited to those related to glycolysis and known transporters/co-transporters of the GLUT family. The compounds according to the invention are useful for treating cancer such as: neuroendrocrine neoplasms, gastrointestinal stromal tumors (GIST), renal cell carcinoma, paraganglioma, pheochromocytoma, pituitary adenoma, colorectal cancer, lung cancer, gastric cancer, pancreatic cancer sarcoma, head and neck cancer, melanoma, ovarian cancer and other cancers that rely on high levels of glycolysis for survival and proliferation; as well as in treating of autoimmune diseases, inflammation, infectious diseases, and metabolic diseases.
cGAS ANTAGONIST COMPOUNDS
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Paragraph 0507, (2017/11/06)
Disclosed are novel compounds of Formula (I) that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.
New annelated thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidines, with potent anticancer activity, designed through VLAK protocol
Lauria, Antonino,Abbate, Ilenia,Patella, Chiara,Martorana, Annamaria,Dattolo, Gaetano,Almerico, Anna Maria
, p. 416 - 424 (2013/06/26)
Drug design was performed through the Virtual Lock-and-Key (VLAK) protocol. This in silico approach allowed to select new annelated thienotriazolopyrimidine derivatives, potentially antitumor drugs. Starting from benzothieno[2,3-e][1,2,3]triazolo[1,5-a]py
Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b] thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents
Romagnoli, Romeo,Baraldi, Pier Giovanni,Kimatrai Salvador, Maria,Preti, Delia,Aghazadeh Tabrizi, Mojgan,Bassetto, Marcella,Brancale, Andrea,Hamel, Ernest,Castagliuolo, Ignazio,Bortolozzi, Roberta,Basso, Giuseppe,Viola, Giampietro
supporting information, p. 2606 - 2618 (2013/05/09)
Two new series of inhibitors of tubulin polymerization based on the 2-(alkoxycarbonyl)-3-(3′,4′,5′-trimethoxyanilino)benzo[b] thiophene and thieno[2,3-b]pyridine molecular skeletons were synthesized and evaluated for antiproliferative activity on a panel
Design, synthesis, and structure-activity relationships of novel spiro-piperidines as acetyl-CoA carboxylase inhibitors
Kamata, Makoto,Yamashita, Tohru,Kina, Asato,Funata, Masaaki,Mizukami, Atsushi,Sasaki, Masako,Tani, Akiyoshi,Funami, Miyuki,Amano, Nobuyuki,Fukatsu, Kohji
scheme or table, p. 3643 - 3647 (2012/07/17)
Spiro-lactone (S)-1 is a potent acetyl-CoA carboxylase (ACC) inhibitor and was found to be metabolically liable in human hepatic microsomes. To remove one of the risk factors in human study by improving the metabolic stability, we focused on modifying the
TRICYCLIC HETEROCYCLIC COMPOUNDS AS PHOSPHOINOSITIDE 3-KINASE INHIBITORS
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Page/Page column 16; 21, (2011/04/13)
Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N-H, N-(C1-C10 alkyl) or S; each X is independently CH or N; R1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R2 is (LQ)mY; and each R3 is independently H, C1-C10 alkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110δ, and therefore have utility in therapy.
SPIRO-RING COMPOUND
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Page/Page column 59, (2009/12/23)
The present invention aims to provide a compound having an acetyl-CoA carboxylase (ACC) inhibitory action, which is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention provides a compound represented by the formula (I): wherein R1 is a hydrogen atom or a substituent; ring P is an optionally substituted 6-membered nitrogen-containing aromatic heterocycle; ring Q is an optionally further substituted 5- to 7-membered nitrogen-containing non-aromatic heterocycle; and ring R is an optionally fused 5- to 7-membered non-aromatic ring, which is further optionally substituted, or a salt thereof.
HETEROCYCLIC COMPOUND
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Page/Page column 43, (2009/12/07)
The present invention provides a compound having an ACC inhibitory action, which is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention provides a compound represented by the formula (I): wherein each symbol is as in the specification, or a salt thereof.
THIENO-PYRIDINONE DERIVATIVES AS KINASE INHIBITORS
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Page/Page column 40-41, (2010/02/11)
A series of thieno[2,3-b]pyridin-6(7H)-one derivatives, substituted in the 3-position by an arylcarbonyl or heteroarylcarbonyl moiety, being inhibitors of p38 MAP kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.
BICYCLIC HETEROAROMATIC COMPOUNDS AS KINASE INHIBITORS
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Page 45-46, (2008/06/13)
A series of 5-6 fused ring bicyclic heteroaromatic derivatives, based in particular on the 6-oxo-6,7-dihydrothieno[2,3-b]pyridine ring system, being inhibitors of p38 kinase, are accordingly of use in medicine, for example in the treatment and/or preventi