949159-97-1

Usage

Uses

Used in Pharmaceutical Research and Development:
Ethanone,1-(2-amino-4-fluoro-5-methoxyphenyl)is employed as a research compound for the development of new drugs and treatments. Its unique chemical structure and properties allow it to interact with biological targets, potentially leading to the discovery of novel therapeutic agents.
Used in Medicinal Chemistry:
In the field of medicinal chemistry, Ethanone,1-(2-amino-4-fluoro-5-methoxyphenyl)- serves as a valuable starting point for the design and synthesis of new chemical entities. Its structural features can be modified to optimize its pharmacological properties, such as potency, selectivity, and bioavailability, making it a versatile building block for drug discovery.
Used in Drug Discovery:
Ethanone,1-(2-amino-4-fluoro-5-methoxyphenyl)is used as a lead compound in drug discovery, where it can be further optimized to improve its therapeutic potential. Its unique chemical and biological properties make it a promising candidate for the development of new drugs to treat various diseases and conditions.
Used in Chemical Synthesis:
Ethanone,1-(2-amino-4-fluoro-5-methoxyphenyl)can also be used as an intermediate in the synthesis of other organic compounds, particularly those with pharmaceutical or biological relevance. Its reactivity and functional groups make it a useful building block for the preparation of more complex molecules with potential applications in various industries.

Upstream product

• 1262882-70-1 4-fluoro-N,3-dimethoxy-N-methylbenzamide 
• 82846-18-2 4?fluoro-3-methoxybenzoic acid 
• 64287-19-0 1-(4-fluoro-3-methoxy-phenyl)ethanone 
• 949159-96-0 1-(4-fluoro-5-methoxy-2-nitrophenyl)ethanone 

Downstream Products

• 1378294-19-9 7-(benzyloxy)-4-bromo-6-methoxycinnoline 
• 1378294-21-3 7-(benzyloxy)-4-(6-fluoro-5-methylpyridin-3-yl)-6-methoxycinnoline 

Relevant academic research and scientific papers

COMPOUND OF CAMPTOTHECIN AND PREPARATION AND USE THEREOF

The present disclosure relates to a compound of formula I, a pharmaceutical composition thereof and the use thereof as an anti-tumor drug.

COMPOUND OF CAMPTOTHECIN AND PREPARATION AND USE THEREOF

The present disclosure relates to a compound of formula I, a pharmaceutical composition thereof and the use thereof as an anti-tumor drug.

Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer

A radiolabeled tracer for imaging therapeutic targets in the brain is a valuable tool for lead optimization in CNS drug discovery and for dose selection in clinical development. We report the rapid identification of a novel phosphodiesterase 10A (PDE10A) tracer candidate using a LC-MS/MS technology. This structurally distinct PDE10A tracer, AMG-7980 (5), has been shown to have good uptake in the striatum (1.2% ID/g tissue), high specificity (striatum/thalamus ratio of 10), and saturable binding in vivo. The PDE10A affinity (KD) and PDE10A target density (Bmax) were determined to be 0.94 nM and 2.3 pmol/mg protein, respectively, using [ 3H]5 on rat striatum homogenate. Autoradiography on rat brain sections indicated that the tracer signal was consistent with known PDE10A expression pattern. The specific binding of [3H]5 to rat brain was blocked by another structurally distinct, published PDE10A inhibitor, MP-10. Lastly, our tracer was used to measure in vivo PDE10A target occupancy of a PDE10A inhibitor in rats using LC-MS/MS technology.

PHOSPHODIESTERASE 10 INHIBITORS

The present invention if directed to certain cinnoline compounds that are PDE10 inhibitors, pharmaceutical compositions containing such compounds and processes for preparing such compounds. The invention is also directed to methods of treating diseases mediated by PDE10 enzyme, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.