52424-57-4

Upstream product

• 7732-18-5 water 
• 40878-21-5 [3-(3,4-dimethoxy-phenyl)-5-oxo-pyrrolidin-3-yl]-acetic acid ethyl ester 
• 40878-20-4 3-cyano-3-(3,4-dimethoxy-phenyl)-pentanedioic acid diethyl ester 
• 93-17-4 3,4-dimethoxyphenylacetonitrile 

Downstream Products

• 167262-84-2 1-(3,4,5-triethoxy-benzoyl)-3-(3,4-dimethoxy-phenyl)-3-(2-hydroxy-ethyl)-pyrrolidine 
• 167262-72-8 1-(3,4,5-trimethoxy-benzoyl)-3-(3,4-dimethoxy-phenyl)-3-(2-hydroxy-ethyl)-pyrrolidine 
• 178371-32-9 1-(3,4,5-trimethoxy-benzoyl)-3-[2-[4-[1-(4-carboxy-phenylmethyl)-1 H-benzoimidazole-2-carbonyl]-piperidin-1-yl]-ethyl]-3-(3,4-dimethoxy-phenyl)-pyrrolidine hydrochloride salt 
• 379233-85-9 1-(3,4,5-trimethoxy-benzoyl)-3-(3,4-dimethoxy-phenyl)-3-(2-methanesulfonyl-ethyl)-pyrrolidine 

Relevant academic research and scientific papers

Novel substituted 4-(1H-benzimidazol-2-yl) [1,4]diazepanes useful for the treatment of allergic diseases

The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.

SUBSTITUTED PYRROLIDIN-3-YL-ALKYL-PIPERIDINES

The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.

Synthesis and structure-activity relationships for a series of substituted pyrrolidine NK1/NK2 receptor antagonists

We recently described the synthesis and characterization of MDL 105,212, a non peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors. Here we report the synthesis and structure-activity relationships for a series of analogs of MDL 105,212 with regards to: NK1 and NK2 receptor binding affinity, physical-chemical characterization; in vitro absorption potential; in vitro metabolic stability; and efficacy in a capsaicin-challenge conscious guinea pig model after oral administration.