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• 129825-11-2 1-(4-chloro-3-(trifluoromethyl)phenyl)ethanone 
• 17356-08-0 thiourea 

Relevant academic research and scientific papers

Discovery and structure-activity relationships study of positive allosteric modulators of the M3 muscarinic acetylcholine receptor

The M3 muscarinic acetylcholine receptor (mAChR) is a member of the family of mAChRs, which are associated with a variety of physiological functions including the contraction of various smooth muscle tissues, stimulation of glandular secretion, and regulation of a range of cholinergic processes in the central nerve system. We report here the discovery and a comprehensive structure--activity relationships (SARs) study of novel positive allosteric modulators (PAMs) of the M3 mAChR through a high throughput screening (HTS) campaign. Compound 9 exhibited potent in vitro PAM activity towards the M3 mAChR and significant enhancement of muscle contraction in a concentration-dependent manner when applied to isolated smooth muscle strips of rat bladder. Compound 9 also showed excellent subtype selectivity over other subtypes of mAChRs including M1, M2, and M4 mAChRs, and moderate selectivity over the M5 mAChR, indicating that compound 9 is an M3-preferring M3/M5 dual PAM. Moreover, compound 9 displayed acceptable pharmacokinetics profiles after oral dosing to rats. These results suggest that compound 9 may be a promising chemical probe for the M3 mAChR for further investigation of its pharmacological function both in vitro and in vivo.

2-AMINOTHIAZOLE DERIVATIVE OR SALT THEREOF

[Problem] To provide a compound useful as an active ingredient in a pharmaceutical composition for treating bladder storage disorders, dysuria, lower urinary tract diseases, and the like. [Solution] The inventors of the present invention have discovered that a 2-aminothiazole derivative exhibits an excellent muscarinic M3 receptor positive allosteric modulator activity, and has potential as a preventative or therapeutic agent against bladder and urinary tract diseases to which bladder contraction mediated by muscarinic M3 receptors contributes. The 2-aminothiazole derivative or salt thereof has potential as a preventative or therapeutic agent against bladder and urinary tract diseases such as, for example, dysuria including underactive bladder, and to which bladder contraction mediated by muscarinic M3 receptors contributes.

PYRIDO[3,4-D]PYRIMIDINYL ACETAMIDE DERIVATIVES AS TRPA1 MODULATORS

Provided are pyrido[3,4-d]pyrimidinyl acetamide derivatives as Transient Receptor Potential Ankyrin (TRPA) modulators. In particular, the compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by Transient Receptor Potential Ankyrin 1 (TRPAl). Also provided herein are processes for preparing the compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. Formula (I).

PYRIMIDINEDIONE-FUSED HETEROCYCLIC COMPOUNDS AS TRPA1 MODULATORS

The present invention is related to novel pyrimidinedione-fused heterocyclic compounds as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.

QUINAZOLINEDIONE DERIVATIVES AS TRPA1 MODULATORS

The present invention provides Quinazolinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by T