243469-65-0

Usage

Physical Form

Yellow crystalline solid

Molecular Weight

192.63 g/mol

Applications

Used in the pharmaceutical industry as an intermediate in drug synthesis
Exhibits diverse biological activities:
Anti-inflammatory properties
Anti-cancer properties
Functions as a versatile building block in organic synthesis
Employed in the production of various fine chemicals

Stability

Stable under normal temperatures and pressures

Handling

Should be handled with caution due to potential health hazards

Upstream product

• 186581-53-3 diazomethane 
• 262606-83-7 methyl (2,6-dichloro-3-{[methyl(pent-4-enyl)amino]carbonyl}pyridin-4-yl)acetate 
• 124-41-4 sodium methylate 
• 875-35-4 2,6-dichloro-4-methylnicotinonitrile 
• 5444-02-0 2,6-dihydroxy-3-cyano-4-methylpyrimidine 
• 67-56-1 methanol 

Relevant academic research and scientific papers

Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time

Histone methyltransferase EZH2, which is the catalytic subunit of the PRC2 complex, catalyzes the methylation of histone H3K27 - a transcriptionally repressive post-translational modification (PTM). EZH2 is commonly mutated in hematologic malignancies and frequently overexpressed in solid tumors, where its expression level often correlates with poor prognosis. First generation EZH2 inhibitors are beginning to show clinical benefit, and we believe that a second generation EZH2 inhibitor could further build upon this foundation to fully realize the therapeutic potential of EZH2 inhibition. During our medicinal chemistry campaign, we identified 4-thiomethyl pyridone as a key modification that led to significantly increased potency and prolonged residence time. Leveraging this finding, we optimized a series of EZH2 inhibitors, with enhanced antitumor activity and improved physiochemical properties, which have the potential to expand the clinical use of EZH2 inhibition.

SUBSTITUTED NITROGEN CONTAINING COMPOUNDS

Disclosed are compounds of Formula (I): or a salt thereof, Formula (II) wherein R1 is: or; each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3a, R3b, L1, B, V, Y, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.

SUBSTITUTED BICYCLE HETEROCYCLIC DERIVATIVES USEFUL AS ROMK CHANNEL INHIBITORS

Disclosed are compounds of Formula (I) or a salt thereof, wherein R1 is (II) or (III); each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3, L1, L2, R1a, R1b, R1c, and n are define herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.

5,7-DIHYDRO-PYRROLO-PYRIDINE DERIVATIVES FOR TREATING NEUROLOGICAL AND NEURODEGENERATIVE DISEASES

The present invention provides, in part, compounds of Formula (I): or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N- oxide, wherein: R1, R2, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4- associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

NEW TRPA1 ANTAGONISTS

The present invention relates to bicyclic heterocyclic derivatives of Forrmula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by TRPA1 channel inhibition or antagonism.

NEW TRPA1 ANTAGONISTS

The present invention relates to compounds of Formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by TRPA1 channel inhibition or antagonism.

A novel approach to conformationally restricted analogues of nicotine and anabasine by an intramolecular Hamaguchi-Ibata reaction

A short synthesis of methyl (SR)-8,10-dichloro- 1,2,3,4,5,6-hexahydro-6- hydroxy-1-methyl-1,9-phenanthroline-6-carboxylate (14) has been achieved en route to conformationally restricted analogues of nicotine and anabasine. The key feature of this process involves an efficient intramolecular Hamaguchi- Ibata reaction of 11. (C) 2000 Elsevier Science Ltd.

Studies on the preparation of 3,4-disubstituted 2-methoxypyridines

The synthesis of 2-methoxy-4-methylpyridine-3-carbonitrile (3) and its conversion, by way of alkylation of the C(4) methyl group, into the pyridyl acetic acid ester 6 is described.