1025762-98-4

Usage

Uses

Used in Pharmaceutical Research and Development:
1-(4-fluorophenyl)-5-iodo-1H-indazole is used as a research compound for studying the properties and potential applications of indazole-based drugs. Its unique structure, with fluorine and iodine atoms attached to the indazole ring, makes it a valuable tool in the development of new therapeutic agents.
Used in Drug Design and Synthesis:
In the pharmaceutical industry, 1-(4-fluorophenyl)-5-iodo-1H-indazole is used as a key intermediate in the synthesis of various indazole-based drugs. Its specific functional groups and structural features allow for the creation of novel drug candidates with potentially improved pharmacological properties.
Used in Biological Activity Studies:
1-(4-fluorophenyl)-5-iodo-1H-indazole is employed as a test compound in biological assays to evaluate its potential biological activities. These studies aim to determine the compound's interactions with various biological targets and its effects on cellular processes, which can provide insights into its therapeutic potential for treating specific conditions.
Used in Chemical Property Analysis:
1-(4-fluorophenyl)-5-iodo-1H-indazole is also used in the analysis of chemical properties, such as reactivity, stability, and solubility. Understanding these properties is crucial for optimizing the compound's synthesis and formulation, as well as for predicting its behavior in biological systems.

Upstream product

• 934601-20-4 1-(4-fluorophenyl)-1H-indazole-5-amine 
• 823-85-8 4-fluorophenyhydrazine hydrochloride 
• 534-17-8 caesium carbonate 
• 146137-76-0 2-Fluoro-5-iodo-benzaldehyde 

Downstream Products

• 1025762-99-5 1-(1-(4-fluorophenyl)-1H-indazol-5-yl)cyclohexanol 
• 1028459-50-8 S-1-(4-fluorophenyl)-1H-indazol-5-yl benzothioate 
• 1028459-20-2 (1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-phenyl-propan-2-amine 
• 1028459-26-8 1-(1-(4-fluorophenyl)-1H-indazol-5-yloxy)-2-methyl-1-phenylpropan-2-amine 
• 1034153-23-5 (1R,2S)-1-((1-(4-fluorophenyl)-1H-indazol-5-yl)oxy)-1-(3-methoxyphenyl)propan-2-amine 
• 1034148-00-9 2,2,2-trifluoro-N-((1R,2S)-1-((1-(4-fluorophenyl)-1H-indazol-5-yl)oxy)-1-phenylpropan-2-yl)acetamide 
• 1028458-64-1 N-[(1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-phenyl-propan-2-yl]cyclopropanesulfonamide 
• 1034148-16-7 N-((1R,2S)-1-(1-(4-fluorophenyl)-1H-indazol-5-yloxy)-1-(6-methoxypyridin-3-yl)propan-2-yl)cyclopropanecarboxamide 
• 1028527-85-6 (1R,2S)-1-((1-(4-fluorophenyl)-1H-indazol-5-yl)oxy)-1-(4-(methylthio)phenyl)propan-2-amine 

Relevant academic research and scientific papers

Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases

A class of potent, nonsteroidal, selective indazole ether-based glucocorticoid receptor modulators (SGRMs) was developed for the inhaled treatment of respiratory diseases. Starting from an orally available compound with demonstrated anti-inflammatory activity in rat, a soft-drug strategy was implemented to ensure rapid elimination of drug candidates to minimize systemic GR activation. The first clinical candidate 1b (AZD5423) displayed a potent inhibition of lung edema in a rat model of allergic airway inflammation following dry powder inhalation combined with a moderate systemic GR-effect, assessed as thymic involution. Further optimization of inhaled drug properties provided a second, equally potent, candidate, 15m (AZD7594), that demonstrated an improved therapeutic ratio over the benchmark inhaled corticosteroid 3 (fluticasone propionate) and prolonged the inhibition of lung edema, indicating potential for once-daily treatment.

Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators

A structure-based design approach led to the identification of a novel class of indazole ether based, non-steroidal glucocorticoid receptor (GR) modulators. Several examples were identified that displayed cell potency in the picomolar range, inhibiting LPS-induced TNF-α release by primary peripheral blood mononuclear cells (PBMCs). Additionally, an improved steroid hormone receptor binding selectivity profile, compared to classical steroidal GR agonists, was demonstrated. The indazole ether core tolerated a broad range of substituents allowing for modulation of the physiochemical parameters. A small sub-set of indazole ethers, with pharmacokinetic properties suitable for oral administration, was investigated in a rat antigen-induced joint inflammation model and demonstrated excellent anti-inflammatory efficacy.

CRYSTALLINE FORM OF INDAZOLYL AMIDE DERIVATIVES FOR THE TREATMENT GLUCOCORTICOID RECEPTOR MEDIATED DISORDERS

Crystalline forms of 2,2,2-trifluoro-N-[(lR,2S)-l-[l-(4-fluorophenyl)in- dazol-5-yl]oxy-l-(3-methoxyphenyl)propan-2-yl]acetamide, processes for obtaining them, pharmaceutical intermediates used in their manu? facture, pharmaceutical compositions containing them, and their use in medical treatment.

MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-κB ACTIVITY AND USE THEREOF

Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically acceptable salt, or hydrate, thereof, wherein X is (Ia); or X is (Ib); or X is (Ic); (Id) is heterocycle or heteroaryl; E is -N-, -NR1-, -O-, -S-, -SO2- or -CR2-; F is -N-, -NR1a-, -O-, -S-, SO2- or -CR2a-; G is N, -NR1b-, -O-, -S-, SO2- or -CR2b-, provided that the E-F-G containing heterocyclic ring formed does not contain a S-S or S-O bond, and at least one of E, F and G is a heteroatom; J, Ja, M, Ma, Q, Rx, Ry, R1, R1a, R1b, R2, R2a, R2b, and R3 to R21, Z, Za, Zb, and Zc are as defined above.

MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-κB ACTIVITY AND USE THEREOF

Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein (Ia) is heterocycle or heteroaryl; J, Ja, E, F, G, Ma, M, Q, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.