186129-25-9

Usage

Uses

Used in Pharmaceutical Industry:
1-Methyl-1H-indole-5-carboxylic acid is used as a key intermediate in the synthesis of diazaspiro ROCK inhibitors for the treatment of various diseases. These inhibitors play a crucial role in modulating the activity of ROCK (Rho-associated protein kinase) enzymes, which are involved in several cellular processes, including cell proliferation, migration, and apoptosis. By targeting ROCK enzymes, these inhibitors can potentially help in the treatment of diseases associated with abnormal cell growth and function.

InChI:InChI=1/C10H9NO2/c1-11-5-4-7-6-8(10(12)13)2-3-9(7)11/h2-6H,1H3,(H,12,13)

Upstream product

• 128742-76-7 methyl 1-methyl-1H-indole-5-carboxylate 
• 10075-52-2 5-bromo-1-methyl-H-indole 
• 1670-81-1 1H-Indole-5-carboxylic acid 
• 74-88-4 methyl iodide 
• 6482-39-9 sodium methyl carbonate 
• 124-38-9 carbon dioxide 
• 32996-16-0 ethyl indole-5-carboxylate 
• 1011-65-0 5-methoxycarbonylindole 
• 112398-75-1 5-chloro-1-methyl-1H-indole 

Downstream Products

• 380922-37-2 N-methylindoline-5-carboxylic acid 
• 916518-57-5 5-(5,5-dimethyl-1,3,2-dioxaborinan-2-yl)-1-methyl-1H-indole 
• 837392-62-8 1-methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole 
• 603-76-9 1-methylindole 
• 1608118-01-9 C₂₇H₃₀N₄O₂ 
• 1608117-95-8 C₂₆H₂₉N₅O₂ 
• 884507-16-8 5-isocyanato-1-methyl-1H-indole 

Relevant academic research and scientific papers

Identification of an indol-based multi-target kinase inhibitor through phenotype screening and target fishing using inverse virtual screening approach

A series of 1,3,5-substituted indole derivatives was prepared to explore the anti-proliferative activity against a panel of human tumour cell lines. A 5-carboxamide derivative (27) emerged as the most potent compound of this series, inhibiting the HeLa cell growth at sub-micromolar concentrations. Target fishing of 27 using a combination of inverse virtual screening (IVS) approach and ligand-based shape similarity study identified the top-ranked targets for 27 as belonging to kinome. These results were further confirmed by in vitro binding assays, leading to the identification of 27 as multi-target kinase inhibitor. The compound 27 was further characterized for its antiproliferative activity by in cell studies, showing a mechanism of action involving modification of the cell cycle, increase in ROS release and caspase 3-expression and decrease in ERK expression.

Milled Dry Ice as a C1 Source for the Carboxylation of Aryl Halides

The use of carbon dioxide as a C1 chemical feedstock remains an active field of research. Here we showcase the use of milled dry ice as a method to promote the availability of CO 2in a reaction solution, permitting practical synthesis of arylcarboxylic acids. Notably, the use of milled dry ice produces marked increases in yields relative to those obtained with gaseous CO 2, as previously reported in the literature.

Structure-Based Design of Dual Partial Peroxisome Proliferator-Activated Receptor γagonists/Soluble Epoxide Hydrolase Inhibitors

Polypharmaceutical regimens often impair treatment of patients with metabolic syndrome (MetS), a complex disease cluster, including obesity, hypertension, heart disease, and type II diabetes. Simultaneous targeting of soluble epoxide hydrolase (sEH) and p

Discovery and synthesis of 2-amino-1-methyl-1H-imidazol-4(5H)-ones as GPCR ligands; an approach to develop breast cancer drugs via GPCR associated PAR1 and PI3Kinase inhibition mechanism

Efforts were taken to synthesis and characterize 2-amino-1-methyl-1H-imidazole-4(5H)-one derivatives (4a-u) through a four-step reaction. The achieved compounds in remarkable yield have characterized through standard analytical techniques such as FTIR, LC

Sodium Methyl Carbonate as an Effective C1 Synthon. Synthesis of Carboxylic Acids, Benzophenones, and Unsymmetrical Ketones

Reported is the synthesis of carboxylic acids, symmetrical ketones, and unsymmetrical ketones with selectivity achieved by exploiting the differential reactivity of sodium methyl carbonate with Grignard and organolithium reagents.

FUNCTIONALISED AND SUBSTITUTED INDOLES AS ANTI-CANCER AGENTS

The present invention relates to anti-tropomyosin compounds, processes for their preparation, and methods for treating or preventing a proliferative disease, preferably cancer, using compounds of the invention.

SPHINGOSINE-1-PHOSPHATE RECEPTOR AGONISTS, METHODS OF PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE AGENT

The present invention relates to novel compounds of Formula 1 as sphingosine-1-phosphate receptor agonists which can be effectively used for the treatment of autoimmune diseases, a method for preparing the same, and a pharmaceutical composition comprising

JAK INHIBITOR

A JAK inhibitor comprising, as an active ingredient, a nitrogen-containing heterocyclic compound represented by formula (I) {wherein W represents a nitrogen atom or -CH-; X represents -C (=O) - or -CHR4- (wherein R4 represents a hydrogen atom, or the like); R1 represents the formula described below [wherein Q1 represents-CR8-(wherein R8 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like); Q2 represents -NR15- (wherein R15 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like); and R5 and R6 may be the same or different and each represents a hydrogen atom, halogen, carboxy, substituted or unsubstituted lower alkyl, or the like], or the like; and R2 and R3 may be the same or different and each represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like} or a pharmaceutically acceptable salt thereof.

BTK protein kinase inhibitors

This application discloses pyridine and pyrimidine compounds according to formula I wherein R1, R2, R3, R4, R5, X1 and A are as described herein which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of formula I and at least one carrier, diluent or excipient.

HCV PROTEASE INHIBITORS

This invention relates to the compounds of formula (I) shown below. Each variable in formula (I) is defined in the specification. These compounds can be used to treat hepatitis C virus infection.