439928-25-3

Usage

Structure

A derivative of pyridoindole with a pyridine ring fused to an indole ring, with a bromine atom at the 6th position and a tetrahydro group.

Properties

Unique chemical and physical properties due to the presence of the bromine atom and the tetrahydro group.

Applications

Potential applications in medicinal chemistry, including as an antitumor and antimicrobial agent.

Pharmacological activities

May have interesting pharmacological activities due to its ability to interact with biological targets.

Upstream product

• 41979-39-9 4-piperidone hydrochloride 
• 50709-33-6 2-bromophenylhydrazine hydrochloride 
• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 

Downstream Products

• 1095263-33-4 (1R,2R)-2-[(6-bromo-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indol-2-yl)carbonyl]-N-(1-cyanocyclopropyl)cyclohexanecarboxamide 
• 313368-91-1 4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido-[3’,4’:4,5]-pyrrolo[1,2,3-de]quinoxalin-8-(7H)-yl)-1-(4-fluorophenyl)-1-butanone 
• 1059630-13-5 (4aS,9bR)-6-bromo-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole (S)-(+)-mandelic acid salt 

Relevant academic research and scientific papers

(1 R,2 R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3- b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): A potent and highly selective cathepsin k inhibitor for the treatment of osteoarthritis

Directed screening of nitrile compounds revealed 3 as a highly potent cathepsin K inhibitor but with cathepsin S activity and very poor stability to microsomes. Synthesis of compounds with reduced molecular complexity, such as 7, revealed key SAR and demonstrated that baseline physical properties and in vitro stability were in fact excellent for this series. The tricycle carboline P3 unit was discovered by hypothesis-based design using existing structural information. Optimization using small substituents, knowledge from matched molecular pairs, and control of lipophilicity yielded compounds very close to the desired profile, of which 34 (AZD4996) was selected on the basis of pharmacokinetic profile.

AZA-RING FUSED INDOLE AND INDOLINE DERIVATIVES

The present application relates to indole and indoline derivatives of formula (I) wherein a, R1, m, L, and Q are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions of such compounds.

Novel Compound - 827

The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases, including cathepsins B, K, C, F, H, L, O, S, W and X. Of particular interest are diseases associated with Cathepsin K.