766558-32-1

Upstream product

• 766558-31-0 N-(2-hydroxyethyl)-4-methoxy-2,6,N-trimethylbenzenesulphonamide 
• 5292-43-3 bromoacetic acid tert-butyl ester 
• 55661-08-0 4-methoxy-2,6-dimethylbenzenesulfonyl chloride 
• 874-63-5 3,5-dimethylmethoxybenzene 

Downstream Products

• 1190970-07-0 4-methoxy-N,2,6-trimethyl-N-(2-(2-oxo-2-(2-(piperidin-1-ylmethyl)-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)ethoxy)ethyl)benzenesulfonamide 
• 1190970-46-7 4-methoxy-N,2,6-trimethyl-N-[2-[2-oxo-2-(4-phenyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-5-yl)-ethoxy]-ethyl]-benzenesulfonic acid amide 
• 1190969-97-1 N-(2-(2-(4-ethyl-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)-2-oxoethoxy)ethyl)-4-methoxy-N,2,6-trimethylbenzenesulfonamide 
• 1186240-86-7 N-((1-(2-(2-(4-methoxy-N,2,6-trimethylphenylsulfonamido)ethoxy)acetyl)-4-(4-methylpiperazin-1-yl)piperidin-4-yl)methyl)isonicotinamide hydrochloride 
• 1186240-25-4 N-((1-(2-(2-(4-methoxy-N,2,6-trimethylphenylsulfonamido)ethoxy)acetyl)-4-(4-methylpiperazin-1-yl)piperidin-4-yl)methyl)isonicotinamide 
• 1361332-94-6 N-[2-[2-[4-[2-(dimethylamino)ethyl]-1-piperazinyl]-2-oxoethoxy]ethyl]-4-methoxy-N,2,6-trimethylbenzenesulfonamide fumarate 
• 766558-28-5 4-methoxy-N,2,6-trimethyl-N-[2-[2-[4-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-1-piperazinyl]-2-oxoethoxy]ethyl]benzenesulfonamide fumarate 

Relevant academic research and scientific papers

From bradykinin B2 receptor antagonists to orally active and selective bradykinin B1 receptor antagonists

The bradykinin (BK) B1 receptor is an attractive target for the treatment of chronic pain and inflammation. Starting from a dual B1 and B2 antagonist, novel antagonists were designed that display low-nanomolar affinity for human B1 receptor and selectivity over B2. Initially, potent imidazoline derivatives were studied, but these compounds suffered from low bioavailability. This issue could be overcome by the use of less basic amino derivatives leading to orally active compounds.

NEW COMPOUNDS

Novel compounds of which the following is exemplary:

NOVEL COMPOUNDS

Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumour pain and headache diseases. The following is exemplary:

NOVEL B1-ANTAGONISTS

Disclosed are compounds of the formula I wherein A, Y, R1, R2, R3, R4 and R5 are defined, suitable for treating diseases and symptoms of diseases caused at least to some extent by stimulation of bradykinin-B1 receptors, the preparation thereof and the use thereof.

SUBSTITUTED SULFONAMIDE DERIVATIVES

The invention relates to substituted sulfonamide derivatives, processes for the preparation thereof, medicaments containing these compounds and the use of substituted sulfonamide derivatives for the preparation of medicaments.

SUBSTITUTED SULFONAMIDE DERIVATIVES

The invention relates to substituted sulfonamide derivatives, processes for the preparation thereof, medicaments containing these compounds and the use of substituted sulfonamide derivatives for the preparation of medicaments.

Substituted Sulfonamide Compounds

Substituted sulfonamide compounds corresponding to the formula I wherein m, n, p, Q, R1, R2, R3, R4, X, Y and Z have the respective meanings defined herein, pharmaceutical compositions containing such compounds, a process for their preparation, and the use of such compounds for the treatment and/or inhibition of pain and other conditions mediated by bradykinin receptor 1 (B1R) and/or bradykinin receptor 2 (B2R).

Substituted Sulfonamide Compounds

Substituted sulfonamide compounds corresponding to formula I: a process for their preparation, pharmaceutical compositions comprising such compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment of pain or other disorders or diseases that are mediated at least in part by B1R receptors.

N-OXIDE ARYL SULFONES AND SULFOXIDES

N-oxide aryl sulfones and sulfoxides of Formula (I) are provided: in which the variables are as described herein. Such compounds may be used to modulate bradykinin receptor activity in vivoor in vitro, and are particularly useful in the treatment of condi