220436-03-3

Upstream product

• 220435-92-7 2-chloro-4-(3-dimethylamino-2-propen-1-on-1-yl)-benzoic acid, methyl ester 
• 2644-70-4 hydrazine hydrochloride 
• 220436-02-2 2-chloro-4-(3-dimethylaminopropyn-1-yl)-benzoic acid methyl ester 
• 185312-82-7 4-bromo-2-chlorobenzoic acid methyl ester 

Downstream Products

• 220436-04-4 2-chloro-4-(1-methyl-1H-pyrazol-3-yl)-benzoic acid methyl ester 
• 220436-05-5 2-Chloro-4-(1-methyl-1H-pyrazol-3-yl)-benzoic Acid 
• 220436-07-7 [2-Chloro-4-(1-methyl-1H-pyrazol-3-yl)-phenyl]-(6,11-dihydro-5H-pyrido[2,3-b][1,5]benzodiazepin-6-yl)-methanone 
• 332109-91-8 2-chloro-4-(1-methyl-1H-pyrazol-3-yl)-benzoyl chloride 

Relevant academic research and scientific papers

Pyridobenzodiazepines: A novel class of orally active, vasopressin V 2 receptor selective agonists

Our efforts in seeking low molecular weight agonists of the antidiuretic peptide hormone arginine vasopressin (AVP) have led to the identification of the clinical candidate WAY-151932 (VNA-932). Further exploration of the structural requirements for agonist activity has provided another class of potent, orally active, non-peptidic vasopressin V2 receptor selective agonists exemplified by the 5,11-dihydro-pyrido[2,3-b][1,5]benzodiazepine as a candidate for further development.

Vasopressin agonist formulation and process

This invention provides novel formulations for vasopressin agonist compounds, or a pharmaceutically acceptable salt thereof, having the general structure: and processes for making them, the formulations comprising from about 1% to about 20% of active ingredient, from about 1% to about 18% of a surfactant component, from about 50% to about 80% of a component of one or more polyethylene glycols, from about 1% to about 20% of a component of one or more sucrose fatty acid esters and/or polyvinylpyrrolidone and, optionally, one or more preservatives or antioxidants.

Tricyclic pyrido vasopressin agonists

The present invention provides compounds of the general formula: wherein W is O or NH, optionally substituted, as well as methods and pharmaceutical compositions utilizing these compounds for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, or temporary delay of urination.

Tricyclic pyridine N-oxides vasopressin agonists

The present invention provides compounds of the general formula: as well as methods and pharmaceutical compositions utilizing these compounds for the inducement of temporary delay of urination or the treatment of disorders which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders.

Tricyclic vasopressin agonists

The present invention provides compounds of the general formula: wherein W is O or NH, optionally substituted, as well as methods and pharmaceutical compositions utilizing these compounds for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, or temporary delay of urination.

Process for converting propargylic amine-N-oxides to enaminones

This invention concerns the use of a hydroxylic solvent in the preparation of enaminones from the corresponding amine N-oxides or propargylic amines via the general process outlined below: STR1