15936-71-7

Upstream product

• 15936-68-2 2-[(4-chloro-2-methyl-phenyl)-hydrazono]-propionic acid ethyl ester 
• 609-14-3 2-acetylpropanoic acid ethyl ester 
• 95-69-2 4-chloro-2-methylbenzeneamine 
• 617-35-6 2-oxo-propionic acid ethyl ester 
• 58791-94-9 (4-chloro-2-methylphenyl)hydrazine 

Downstream Products

• 15936-74-0 5-chloro-7-methyl-1H-indole-2-carboxylic acid 
• 442910-45-4 tert-butyl 7-(bromomethyl)-1H-indole-1-carboxylate 

Relevant academic research and scientific papers

Substituted Indoles

The invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, th

Detailed structure-activity relationship of indolecarboxamides as H 4 receptor ligands

A series of 76 derivatives of the indolecarboxamide 1 were synthesized, which allows a detailed SAR investigation of this well known scaffold. The data enable the definition of a predictive QSAR model which identifies several compounds with an activity comparable to 1. A selection of these new H 4R antagonists was synthesized and a comparison of predicted and measured values demonstrates the robustness of the model (47-55). In addition to the H4-receptor activity general CMC and DMPK properties were investigated. Some of the new analogs are not only excellently soluble, but display a significantly increased half-life in mouse liver microsomes as well. These properties qualify these compounds as a possible new standard for future in vivo studies (e.g 51, 52 and 55). Moreover, the current studies also provide valuable information on the potential receptor ligand interactions between the indolcarboxamides and the H4R protein.

SPIRO-PIPERIDINE DERIVATIVES

The present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety, depressive disorders and other diseases. The compounds of present invention are represented by the general formula (I) wherein R1 to R1, X and Y are as defined in the specification.