169040-40-8

Upstream product

• 17630-76-1 5-chloroindole 2,3-dione 
• 578-57-4 2-bromoanisole 
• 16750-63-3 2-methoxyphenylmagnesium bromide 

Downstream Products

• 1243153-58-3 C₁₅H₁₃ClN₂O₂ 
• 352278-37-6 C₂₂H₂₄ClN₃O₄ 
• 352278-36-5 C₂₂H₂₄ClN₃O₄ 
• 905077-87-4 5-chloro-3-hydroxy-3-(2-methoxyphenyl)-1-{[4-methoxy-2-(trifluoromethoxy)phenyl]sulfonyl}-1,3-dihydro-2H-indol-2-one 
• 492429-87-5 5-chloro-3-(2-methoxyphenyl)-1,3-dihydro-2H-indol-2-one 
• 169040-43-1 3,5-dichloro-3-(2-methoxyphenyl)-1,3-dihydro-2H-indol-2-one 

Relevant academic research and scientific papers

Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties

Herein we report the discovery of a novel series of vasopressin 1b (V1b) receptor antagonists, starting from potent but metabolically labile oxindole SSR149415. Masking the proline N,N-dimethyl amide moiety as an oxazole and attaching a benzylic amine moiety to the northern phenyl ring resulted in potent and selective V1b receptor antagonists with improved metabolic stability and improved pharmacokinetic properties in rat. Compound 18c was found to be efficacious in a rat model of anti-depressant activity.

Synthesis of [11C]SSR149415 and preliminary imaging studies using positron emission tomography

SSR149415 was the first non-peptide vasopressin-(V1b) receptor antagonist reported. It has been used to probe the role of V1b receptors in animal models of depression, aggression, and stress-anxiety, and was progressed to clinical tr

A concise silylamine approach to 2-amino-3-hydroxy-indoles with potent in vivo antimalaria activity

The development of a concise strategy to access 2-amino-3-hydroxy-indoles, which are disclosed as novel antimalarials with potent in vivo activity, is reported. Starting from isatins the target compounds are synthesized in 2 steps and in good yields via oxoindole intermediates by employing tert- butyldimethylsilyl amine (TBDMSNH2) as previously unexplored ammonia equivalent.

SUBSTITUTED OXINDOL DERIVATIVES AND MEDICAMENTS CONTAINING THE SAME

The invention relates to novel oxindol derivatives of general formula (1) wherein the substituents A, B, R1, R2 and R3 have the designations cited in patent claim 1, and to medicaments containing said derivatives for the prophylaxis and/or treatment of vasopressin-dependent or oxytocin-dependent diseases.

Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing them

The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6 and R7 are defined according to claim 1, and to medicaments containin

Phenylsulfonyl-1,3-dihydro-2h-indole-2-one derivatives, their preparation and their therapeutic use

The invention relates to compounds of formula: and also to the salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, with affinity for and selectivity towards the arginine-vasopressin V1b receptors and/or for the ocytocin receptors and, furthermore, for certain compounds, affinity for the V1a receptors. The invention also relates to the process for preparing them, to the intermediate compounds of formula (IV) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for preparing medicinal products.