1180495-74-2

Upstream product

• 1180495-73-1 7-chloro-6-methoxy-1H-indole-2,3-dione 
• 33234-36-5 2-chloro-3-methoxybenzoic acid 
• 4294-95-5 4-methoxyanthranilic acid 
• 1180495-72-0 N-(2-chloro-3-methoxyphenyl)-2-hydroxyiminoacetamide 
• 85893-87-4 2-chloro-3-methoxyaniline hydrochloride 

Downstream Products

• 1180495-76-4 methyl 3-chloro-2-(4-isopropylthiazole-2-carboxamido)-4-methoxybenzoate 
• 1180495-75-3 2-amino-3-chloro-4-methoxy benzoic acid methyl ester 

Relevant academic research and scientific papers

Macrocyclic serine protease inhibitors, pharmaceutical compositions thereof, and their use for treating HCV infections

Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, and pharmaceutical compositions and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.

HALOGENATED QUINAZOLIN-THF-AMINES AS PDE1 INHIBITORS

The present invention provides halogenated quinazolin-THF-amines as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

Structure-activity relationship studies of SETD8 inhibitors

SETD8 (also known as SET8, PR-SET7, or KMT5A (lysine methyltransferase 5A)) is the only known lysine methyltransferase that catalyzes the monomethylation of histone H4 lysine 20 (H4K20). In addition to H4K20, SETD8 monomethylates non-histone substrates such as the tumor suppressor p53 and the proliferating cell nuclear antigen (PCNA). Because of its role in regulating diverse biological processes, SETD8 has been pursued as a potential therapeutic target. We recently reported the first substrate-competitive SETD8 inhibitor, UNC0379 (1), which is selective for SETD8 over 15 other methyltransferases. We characterized this inhibitor in a battery of biochemical and biophysical assays. Here we describe our comprehensive structure-activity relationship (SAR) studies of this chemical series. In addition to 2- and 4-substituents, we extensively explored 6- and 7-substituents of the quinazoline scaffold. These SAR studies led to the discovery of several new compounds, which displayed similar potencies as compound 1 and interesting SAR trends. This journal is

MACROCYCLIC SERINE PROTEASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR USE FOR TREATING HCV INFECTIONS

Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, and pharmaceutical compositions and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.

MACROCYCLIC SERINE PROTEASE INHIBITORS USEFUL AGAINST VIRAL INFECTIONS, PARTICULARLY HCV

Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula (Ia) or (Ib), pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.

MACROCYCLIC SERINE PROTEASE INHIBITORS

Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula Ia or Ib, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.

MACROCYCLIC SERINE PROTEASE INHIBITORS

Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof