552331-30-3Relevant academic research and scientific papers
HETEROAROMATIC COMPOUNDS USEFUL IN THERAPY
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Page/Page column 51, (2021/02/26)
A compound of formula (I) useful in the treatment of a Pneumoviridae viral infection.
HETEROAROMATIC COMPOUNDS USEFUL IN THERAPY
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Paragraph 0279; 0280, (2020/02/15)
A compound of formula (I) or a pharmaceutically acceptable salt thereof, useful in therapy, in particular in the treatment of a viral infection or a disease linked to impaired or abnormal autophagy.
CONDENSED PYRIMIDINE OR PYRIDAZINE DERIVATIVES AS ANTIVIRAL AGENTS
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Page/Page column 34; 38, (2020/05/19)
A compound of formula (I) or a pharmaceutically acceptable salt thereof. The compound is a prodrug of a PI4KIIIβinhibitor and as such is useful as an antiviral agent. A pharmaceutical composition comprising the compound.
2,6-DIMETHYL-N-((PYRIDIN-4-YL)METHYL)IMIDAZO[1,2-B]PYRIDAZIN-8-AMINE AND 2,5-DIMETHYL-N-[(PYRIDIN-4-YL)METHYL]PYRAZOLO[1,5-A]PYRIMIDIN-7-AMINE DERIVATIVES FOR TREATING VIRAL INFECTIONS
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Page/Page column 23, (2020/05/19)
The compound is useful in therapy, in particular as an antiviral agent, e.g. in the treatment of an RNA viral infection. A pharmaceutical composition comprising the compound.
THIADIAZINE DERIVATIVES
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Page/Page column 35; 41, (2020/02/06)
The invention relates to thiadiazine derivatives, or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof, as well as to pharmaceutical compositions containing
FUSED PYRAZOLE DERIVATIVES AS KINASE INHIBITORS
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Page/Page column 53, (2017/05/07)
A series of substituted pyrazolo[1,5-a]pyrimidine and pyrazolo[1,5-a][1,3,5]- triazine derivatives of formula (I), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase ΙΙΙβ (ΡI4ΚΙΙΙβ) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.
Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel non-basic 1-(2H-indazole-5-yl)pyridin-2(1H)-one derivatives and mitigation of mutagenicity in Ames test
Igawa, Hideyuki,Takahashi, Masashi,Ikoma, Minoru,Kaku, Hiromi,Kakegawa, Keiko,Kina, Asato,Aida, Jumpei,Okuda, Shoki,Kawata, Yayoi,Noguchi, Toshihiro,Hotta, Natsu,Yamamoto, Syunsuke,Nakayama, Masaharu,Nagisa, Yasutaka,Kasai, Shizuo,Maekawa, Tsuyoshi
, p. 2504 - 2518 (2016/05/09)
To develop non-basic melanin-concentrating hormone receptor 1 (MCHR1) antagonists with a high probability of target selectivity and therapeutic window, we explored neutral bicyclic motifs that could replace the previously reported imidazo[1,2-a]pyridine or 1H-benzimidazole motif. The results indicated that the binding affinity of a chemically neutral 2H-indazole derivative 8a with MCHR1 (hMCHR1: IC50 = 35 nM) was comparable to that of the imidazopyridine and benzimidazole derivatives (1 and 2, respectively) reported so far. However, 8a was positive in the Ames test using TA1537 in S9- condition. Based on a putative intercalation of 8a with DNA, we introduced a sterically-hindering cyclopropyl group on the indazole ring to decrease planarity, which led to the discovery of 1-(2-cyclopropyl-3-methyl-2H-indazol-5-yl)-4-{[5-(trifluoromethyl)thiophen-3-yl]methoxy}pyridin-2(1H)-one 8l without mutagenicity in TA1537. Compound 8l exerted significant antiobesity effects in diet-induced obese F344 rats and exhibited promising safety profile.
GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
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Paragraph 0001131, (2015/04/15)
Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
Selective methylation of NH-containing heterocycles and sulfonamides using n, N -dimethylformamide dimethylacetal based on calculated pKa Measurements
Fairley, Gary,Hall, Catherine,Greenwood, Ryan
, p. 570 - 574 (2013/04/10)
The use of N,N-dimethylformamide dimethylacetal (DMF-DMA) as a suitable methylating agent for the methylation of NH-containing groups and heterocycles has been investigated. Use of ReactArray and calculated pKa measurements have allowed additional helpful information to be collated to determine optimum reaction conditions for a variety of substrates.
Synthesis and SAR of indazole-pyridine based protein kinase B/Akt inhibitors
Woods, Keith W.,Fischer, John P.,Claiborne, Akiyo,Li, Tongmei,Thomas, Sheela A.,Zhu, Gui-Dong,Diebold, Robert B.,Liu, Xuesong,Shi, Yan,Klinghofer, Vered,Han, Edward K.,Guan, Ran,Magnone, Shayna R.,Johnson, Eric F.,Bouska, Jennifer J.,Olson, Amanda M.,Jong, Ron de,Oltersdorf, Tilman,Luo, Yan,Rosenberg, Saul H.,Giranda, Vincent L.,Li, Qun
, p. 6832 - 6846 (2007/10/03)
A series of heteroaryl-pyridine containing inhibitors of Akt are reported. The synthesis and structure-activity relationships are discussed, leading to the discovery of a indazole-pyridine analogue (Ki = 0.16 nM). These compounds bind in the ATP binding site, are potent, ATP competitive, and reversible inhibitors of Akt activity. No selectivity amongst the Akt isoforms is observed for this analogue, but there is good selectivity against an panel of other kinases. It is least selective for other members of the AGC family of kinases but is nonetheless 40-fold selective for Akt over PKA. The compound shows cellular activity and significantly slows tumor growth in vivo.
