1229453-99-9

Usage

Uses

Used in Pharmaceutical Industry:
N-(1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6-((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide is used as a potential enzyme or receptor inhibitor for the development of new therapeutic agents. Its design suggests that it may be effective in modulating biological pathways implicated in various diseases, offering a novel approach to treatment.
Used in Drug Discovery Research:
In the field of drug discovery, N-(1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6-((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide serves as a lead molecule for further optimization and development. Its unique structural features provide a foundation for medicinal chemists to explore modifications that could enhance its potency, selectivity, and pharmacokinetic properties, ultimately aiming to improve its therapeutic index.
Used in Targeted Therapies:
N-(1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6-((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide may be utilized in targeted therapies, where its specific interactions with biological targets could lead to more precise treatments with fewer side effects. This is particularly relevant in the treatment of cancer and other complex diseases where traditional broad-spectrum approaches may have limitations.

Upstream product

• 1188909-55-8 phenyl (1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)carbamate 
• 1229456-45-4 tert-butyl ((6-((1H-indol-5-yl)oxy)-pyrimidin-4-yl)methyl)(methyl)carbamate 
• 1229454-86-7 5-((6-((benzyloxy)methyl)pyrimidin-4-yl)oxy)-1H-indole 
• 149978-42-7 1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-amine 
• 1229456-44-3 1-(5-(6-(hydroxymethyl)pyrimidin-4-yloxy)-1H-indol-1-yl)ethanone 
• 914802-11-2 4-(benzyloxymethyl)-6-chloropyrimidine 
• 1953-54-4 indol-5-ol 

Relevant academic research and scientific papers

The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration

A noninvasive topical ocular therapy for the treatment of neovascular or wet age-related macular degeneration would provide a patient administered alternative to the current standard of care, which requires physician administered intravitreal injections. This manuscript describes a novel strategy for the use of in vivo models of choroidal neovascularization (CNV) as the primary means of developing SAR related to efficacy from topical administration. Ultimately, this effort led to the discovery of acrizanib (LHA510), a small-molecule VEGFR-2 inhibitor with potency and efficacy in rodent CNV models, limited systemic exposure after topical ocular administration, multiple formulation options, and an acceptable rabbit ocular PK profile.

PYRIMIDIN-4-YL)OXY)-1H-INDOLE-1-CARBOXAMIDE DERIVATIVES AND USE THEREOF

This invention relates to certain metabolites of N-(1-methyl-5-(trifluoromethyl)-1H- pyrazol-3-yl)-5-((6-((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide In particular, the present invention relates to pharmaceutical compositions comprising these metabolites, as well as processes for their preparation and their use in the treatment of diseases.

Pyridyloxyindoles Inhibitors of VEGF-R2 and Use Thereof for Treatment of Disease

The invention relates to novel organic compounds of formula (I), and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumour diseases and ocular neovascular diseases.