1226807-98-2

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 50608-35-0 (5-chloro-2-nitrobenzylamino)acetic acid ethyl ester 
• 73033-58-6 5-chloro-2-nitrobenzyl alcohol 
• 57750-81-9 4-chloro-2-(chloromethyl)-1-nitrobenzene 

Downstream Products

• 1226807-99-3 [(2-amino-5-chlorobenzyl)-tert-butoxycarbonylamino]acetic acid ethyl ester 
• 1226808-00-9 7-chloro-2-oxo-1,2,3,5-tetrahydrobenzo[1,4]diazepine-4-carboxylic acid tert-butyl ester 
• 1228088-30-9 trans-8-chloro-5-methyl-1-(4-pyridin-2-yloxycyclohexyl)-4,6-dihydro-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine 
• 1342802-99-6 trans-8-chloro-5-methyl-1-(4-pyridin-2-yl-cyclohexyl)-5,6-dihydro-4H-2,3,5,10b-tetraazabenzo[e]azulene 
• 1342802-95-2 trans-8-chloro-1-(4-pyridin-2-yl-cyclohexyl)-4H,6H-2,3,5,10b-tetraaza-benzo[e]azulene-5-carboxylic acid tert-butyl ester 
• 1339126-76-9 8-chloro-1-(4-hydroxy-4-phenylcyclohexyl)-4H,6H-2,3,5,10b-tetraazabenzo[e]azulene-5-carboxylic acid tert-butyl ester 
• 1337966-03-6 8-Chloro-1-(4-hydroxy-4-o-tolyl-cyclohexyl)-4H,6H-2,3,5,10b-tetraaza-benzo[e]azulene-5-carboxylic acid tert-butyl ester 
• 1337966-02-5 8-chloro-1-(4-oxo-cyclohexyl)-4H,6H-2,3,5,10b-tetraazabenzo[e]azulene-5-carboxylic acid tert-butyl ester 
• 1337966-01-4 cis/trans-8-chloro-1-(4-hydroxycyclohexyl)-4H,6H-2,3,5,10b-tetraazabenzo[e]azulene-5-carboxylic acid tert-butyl ester 
• 1337965-33-9 trans-8-chloro-5-methyl-1-(4-phenyl-cyclohexyl)-5,6-dihydro-4H-2,3,5,10b-tetraazabenzo[e]azulene 
• 1337965-31-7 trans-8-chloro-1-(4-phenyl-cyclohexyl)-4H,6H-2,3,5,10b-tetraaza-benzo[e]azulene-5-carboxylic acid tert-butyl ester 
• 1337965-64-6 trans-8-chloro-1-(4-phenyl-cyclohexyl)-5-pyridin-2-yl-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulene 
• 1337965-62-4 trans-8-chloro-1-(4-phenyl-cyclohexyl)-5-pyridin-2-ylmethyl-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulene 
• 1337965-60-2 trans-8-chloro-5-methanesulfonyl-1-(4-phenyl-cyclohexyl)-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulene 

Relevant academic research and scientific papers

Development of a triazolobenzodiazepine-based PET probe for subtype-selective vasopressin 1A receptor imaging

Objectives: To enable non-invasive real-time quantification of vasopressin 1A (V1A) receptors in peripheral organs, we sought to develop a suitable PET probe that would allow specific and selective V1A receptor imaging in vitro and in vivo. Methods: We sy

Discovery of Balovaptan, a Vasopressin 1a Receptor Antagonist for the Treatment of Autism Spectrum Disorder

We recently reported the discovery of a potent, selective, and brain-penetrant V1a receptor antagonist, which was not suitable for full development. Nevertheless, this compound was found to improve surrogates of social behavior in adults with autism spect

ARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES

The present invention is concerned with aryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The invention further provides methods for the manufacture of such compounds and

HETEROARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES

The present invention provides heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

ARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES

The present invention is concerned with aryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I, wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as Via receptor modulators, and in

ARYL-/HETEROARYL-CYCLOHEXENYL-TETRAAZABENZO[E]AZULENES

The present invention is concerned with aryl-/heteroaryl-cyclohexenyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The invention further provides methods for the manufacture of such compounds and pharmaceutical compositions containing them. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, in appropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

ARYL - /HETEROARYL - CYCLOHEXENYL - TETRAAZABENZO [E] AZULENES AS VASOPRESSIN ANTAGONISTS

The present invention is concerned with aryl-/heteroaryl-cyclohexenyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

HETEROBIARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES

The present invention relates to heterobiaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as V1a receptor modulators, and in

HETEROARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES

The present invention is concerned with heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

HETEROBIARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES

The present invention relates to heterobiaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula (I), wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor ant