cas 7364-25-2, 3-Indazolinone | Articles data

Articles about 7364-25-2Total 10 be found

FERROPORTIN INHIBITORS AND METHODS OF USE
The subject matter described herein is directed to Ferroportin inhibitor compounds of Formula I and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds and methods of administering the compounds for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis.
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Paragraph 0447; 0448

(2020/07/07)

Discovery of isatin and 1H-indazol-3-ol derivatives as D-amino acid oxidase (DAAO) inhibitors
D-Amino acid oxidase (DAAO) is a potential target in the treatment of schizophrenia as its inhibition increases brain D-serine level and thus contributes to NMDA receptor activation. Inhibitors of DAAO were sought testing [6+5] type heterocycles and identified isatin derivatives as micromolar DAAO inhibitors. A pharmacophore and structure-activity relationship analysis of isatins and reported DAAO inhibitors led us to investigate 1H-indazol-3-ol derivatives and nanomolar inhibitors were identified. The series was further characterized by pKa and isothermal titration calorimetry measurements. Representative compounds exhibited beneficial properties in in vitro metabolic stability and PAMPA assays. 6-fluoro-1H-indazol-3-ol (37) significantly increased plasma D-serine level in an in vivo study on mice. These results show that the 1H-indazol-3-ol series represents a novel class of DAAO inhibitors with the potential to develop drug candidates.
Szilágyi, Bence,Kovács, Péter,Ferenczy, Gy?rgy G.,Rácz, Anita,Németh, Krisztina,Visy, Júlia,Szabó, Pál,Ilas, Janez,Balogh, Gy?rgy T.,Monostory, Katalin,Vincze, István,Tábi, Tamás,Sz?k?, éva,Keser?, Gy?rgy M.
p. 1579 - 1587
(2018/02/23)

Method for preparing 1-benzyl-3-hydroxy-1H-3-indazole sodium salt
The invention relates to a method for preparing 1-benzyl-3-hydroxy-1H-3-indazole sodium salt. The method is characterized in that o-aminobenzoic acid, concentrated hydrochloric acid, a NaNO2 solution and solid Na2SO3 are taken as starting raw materials, a proper amount of a NaOH solution and a proper amount of benzyl chloride are added, and 1-benzyl-3-hydroxy-1H-3-indazole sodium salt is obtained through multi-step reaction filtering dehydration. The method is easily accessible in raw material, mild in reaction condition, low in cost and suitable for factory large-scale production.
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Paragraph 0007; 0023; 0024

(2017/08/31)

PYRIMIDINE OR PYRIDINE COMPOUNDS, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USES THEREOF
The present invention disclosed a class of pyrimidine or pyridine compounds, pharmaceutically acceptable salts, stereoisomers, prodrugs and solvates thereof, preparation method therefor and pharmaceutical compositions and pharmaceutical uses thereof. The compounds can inhibit the variants of EGFR (Epidermis Growth Factor Receptor) proteinases, and therefore can inhibit the growth of a variety of tumor cells effectively. The compounds can be used to prepare antitumor drugs, used for the treatment, combined therapy or prevention of various different cancers. The compounds can overcome the drug resistance induced by the existing first-generation EGFR inhibitors such as gefitinib, erlotinib and so on. Particularly, the compounds can be used to prepare drugs for treating or preventing diseases, disturbances, disorders or conditions mediated by epidermis growth factor receptor variants (such as L858R activated mutants, Exon19 deletion activated mutants and T790M resistant mutants).
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Paragraph 0350-0352

(2017/09/19)

Synthesis and biological evaluations of novel bendazac lysine analogues as potent anticataract agents
Novel bendazac analogues and their salts have been designed and prepared. The resulting compounds (13c-d, 15c, 17c) showed very good aqueous solubility (>100 mg/mL). An in vitro assay showed that most of the resulting compounds had potent protective activ
Shen, Hong,Gou, Shaohua,Shen, Jianping,Zhu, Yanqin,Zhang, Yindi,Chen, Xuetai
scheme or table
p. 2115 - 2118
(2010/06/19)

Sydnones as Masked Hydrazines for Heterocycle Formation: Reactions of 3-(2-Substituted Phenyl)sydnones with HCl
In general, reaction of 3-(2-substituted phenyl)sydnones with HCl gives products derived from cleavage of the sydnone ring to the corresponding hydrazine and subsequent cyclization to the side chain.In one case, 3-(2-aminophenyl)sydnone (43), the product obtained, 1-amino-1H-benzimidazole (47), apparently results from nucleophilic interception by the side chain prior to complete cleavage of the sydnone ring.
Gelvin, Christopher R.,Turnbull, Kenneth
p. 1931 - 1943
(2007/10/02)

NEW CONVENIENT METHODS FOR THE SYNTHESIS OF 1,2-DIHYDRO-3H-INDAZOL-3-ONE AND ITS 1-ACYL DERIVATIVES
The acid hydrolysis of the readily obtainable 3-(o-carboxyphenyl)sydnones (6a-d) afforded 3-indazolones (3a-d) in yields over 90 percent. By transacylation between 1-acyl-3-acyloxyindazoles (11a-d) and 3-indazolones (3a, c), the corresponding 1-acyl-3-indazolones 10a-d resulted in pure state and yields also over 90 percent.
Dumitrascu, Florea,Plaveti, Marieta,Raileanu, Dan
p. 917 - 924
(2007/10/03)

Acyl Derivatives of Indazolin-3-one
1- and 2-Ethanoyl-, propanoyl-, butanoyl- and benzoylindazolin-3-ones have been prepared and the 2-isomers have been shown to exist in two tautomeric forms.Sulphonylation and further acylation of these compounds are described and some rearrangements in the series are discussed.
Anderson, Robert M.
p. 3933 - 3959
(2007/10/02)

The Reactioon of Benzylidenetriphenylphosphoranes with Benzenediazonium-2-carboxylate
The title reaction affords to the adducts 3 which upon alkaline treatment give compounds 5, while by thermolysis give 6 and 7.Hydrochloride salts of 3 in refluxing xylene afford to chlorohydrazones 10 as the major products.A mechanism is proposed for thermal decomposition of 3.
Compagini, Anna,Lo Vullo, Adriana,Chiacchio, Ugo,Corsaro, Antonio,Purrello, Giovanni
p. 641 - 643
(2007/10/02)

Reactions of Hydrazides and Hydrazones with n-Butyl-lithium
Aromatic hydrazides give indazol-3(2H)-ones in good yield when treated with 3 equivalents of n-butyl-lithium; aliphatic and heterocyclic hydrazides afford the corresponding aldehydes under the same conditions.
Barton, Derek H. R.,Lukacs, Gabor,Wagle, Dilip
p. 450 - 452
(2007/10/02)