63362-34-5

Upstream product

• 100-26-5 Pyridine-2,5-dicarboxylic acid 
• 49668-89-5 5-(methoxycarbonyl)-2-methylpyridine 1-oxide 
• 108-24-7 acetic anhydride 
• 56026-36-9 methyl 6-(hydroxymethyl)nicotinate 
• 5470-70-2 Methyl 6-methylnicotinate 
• 881-86-7 dimethyl 2,5-pyridine dicarboxylate 
• 144-55-8 sodium hydrogencarbonate 
• 7087-68-5 N-ethyl-N,N-diisopropylamine 

Downstream Products

• 775545-30-7 6-(hydroxymethyl)pyridine-3-carboxylic acid 
• 1620673-70-2 4-{8-amino-3-[(6R,8aS)-1,1-dimethyl-3-oxohexahydro[1,3]oxazolo[3,4-a]pyridin-6-yl]imidazo[1,5-a]pyrazin-1-yl}-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide 
• 1620673-62-2 4-{8-amino-3-[(1S,6R,8aS)-1-methyl-3-oxohexahydro[1,3]oxazolo[3,4-a]pyridin-6-yl]imidazo[1,5-a]pyrazin-1-yl}-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide 
• 1620673-64-4 4-{8-amino-3-[(1R,6R,8aS)-1-methyl-3-oxohexahydro[1,3]oxazolo[3,4-a]pyridin-6-yl]imidazo[1,5-a]pyrazin-1-yl}-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide 
• 1419222-52-8 (2S,5R)-benzyl 5-(((3-chloropyrazin-2-yl)methyl)carbamoyl)-2-(hydroxymethyl)piperidine-1-carboxylate 
• 1419222-51-7 (3S,6S)-1-((benzyloxy)carbonyl)-6-(hydroxymethyl)piperidine-3-carboxylic acid 
• 1419223-59-8 (3S,6S)-1-benzyl 3-methyl 6-(hydroxymethyl)piperidine-1,3-dicarboxylate 
• 1620675-52-6 (3S,6R)-1-((benzyloxy)carbonyl)-6-(hydroxymethyl)piperidine-3-carboxylic acid 
• 1620675-50-4 (3S,6R)-1-benzyl 3-methyl 6-(hydroxymethyl)piperidine-1,3-dicarboxylate 
• 1419222-53-9 (2S,5R)-benzyl 2-(acetoxymethyl)-5-(((3-chloropyrazin-2-yl)methyl)-carbamoyl)piperidine-1-carboxylate 
• 56026-36-9 methyl 6-(hydroxymethyl)nicotinate 

Relevant academic research and scientific papers

Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes

Bruton's tyrosine kinase (BTK) is a Tec family kinase with a well-defined role in the B cell receptor (BCR) pathway. It has become an attractive kinase target for selective B cell inhibition, and for the treatment of B cell related diseases. Many BTK inhibitors have been discovered for the treatment of cancer and rheumatoid arthritis, including a series of BTK inhibitors based on 8-amino-imidazo[1,5-a]pyrazine we recently reported. The X-ray crystal structures of BTK with inhibitors were also published, which provided great help for the SAR design. Here we report our SAR work introducing ring constraints for the 3-position piperidine amides on the BTK inhibitors based on 8-amino-imidazo[1,5-a]pyrazine. This modification improved the potency in BTK inhibitions, as well as the PK profile and the off-target selectivity. The dose-dependent efficacy of two BTK inhibitors was observed in the rat collagen induced arthritis (CIA) model.

BTK INHIBITORS

The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts or stereoisomers thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated disorders.

BTK INHIBITORS

Provided are Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.

OCULAR HYPOTENSIVE AGENT COMPRISING COMPOUND CAPABLE OF INHIBITING HISTONE DEACETYLASE AS ACTIVE INGREDIENT

An object of the present invention is to find a novel pharmacological effect of a compound having an HDAC inhibitory effect. The compound having an HDAC inhibitory effect of the invention has an excellent effect of cell morphological change on trabecular meshwork cells and/or effect of intraocular pressure reduction, and is therefore useful as a preventive and/or therapeutic agent for a disease considered to be associated with aqueous humor circulation and/or intraocular pressure, particularly as a preventive and/or therapeutic agent for glaucoma or ocular hypertension.

NOVEL (2-AMINOPHENYL)PYRIDINECARBOXAMIDE DERIVATIVE HAVING UREA STRUCTURE

Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represen

Fused bicyclic-N-bridged-heteroaromatic carboxamides for the treatment of disease

The invention provides compounds of Formula I: 1These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat conditions or diseases in which α7 is known to be involved.

2-Carbaldoximes of pyridine-4- and 5-carboxylic acids

A series of pyridine-2-carbaldoximes, all of which are substituted at the 4- or 5-position with derivatives of the corresponding carboxylic acids, have been prepared via the corresponding pyridine-2-carbaldehydes.