147106-99-8

Upstream product

• 22446-37-3 methyl (2-hydroxyphenyl)acetate 
• 109-64-8 1,3-dibromo-propane 

Downstream Products

• 185802-89-5 [2-(3-Bromo-propoxy)-phenyl]-acetic acid 
• 787619-54-9 [2-(3-Morpholin-4-yl-propoxy)-phenyl]-acetic acid methyl ester 

Relevant academic research and scientific papers

PDE9 inhibitors for treating type 2 diabetes,metabolic syndrome, and cardiovascular disease

The invention provides compounds of Formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs, wherein A, P, J, x, and R10 are as defined herein; pharmaceutical compositions thereof; and methods of using the pharmaceutical compositions for the treatment of diseases, including, diabetes, including type 1 and type 2 diabetes, hyperglycemia, dyslipidemia, impaired glucose tolerance, metabolic syndrome, and/or cardiovascular disease.

Synthesis and biological evaluation of phenylacetyl derivatives having low central nervous system permeability as potent and selective M2 muscarinic receptor antagonists

A series of phenylacetyl derivatives containing the 5,10-dihydro-11H- dibenzo[b,e][1,4]diazepin-11-one or 5,11-dihydro-6H-pyrido[2,3- b][1,4]benzodiazepin-6-one skeleton was prepared and evaluated for their binding affinities to muscarinic receptors in vitro and for antagonism of bradycardia, salivation and tremor in vivo. Among them, compounds 56 and 66 had high affinity for M2 muscarinic receptors in the heart (pK(i) = 8.7 and 8.9, respectively) with low affinity for M3 muscarinic receptors in the submandibular gland. A structure-activity relationship (SAR) study suggested that the high M2 selectivity over the M3 muscarinic receptors of 56 may be attributed to the direction of the carboxamide carbonyl group. In in vivo studies, 56 and 66 antagonized oxotremorine-induced bradycardia in rats on both intravenous and oral administration, and their heart rate increasing effect in dogs with nocturnal bradycardia was about 3-fold greater than that of AF-DX 116. Furthermore, they had almost no influence on oxotremorine- induced tremor in mice, presenting no evidence of central transfer.

Perhydroisoindole derivatives and pharmaceutical compositions containing them

This invention relates to derivatives of perhydroisoindol of formula: STR1 in which the radicals R are hydrogen atoms or together form a bond, the symbols R' are phenyl radicals which can be substituted by a halogen atom or a methyl radical in position 2 or 3, X is an oxygen atom or an NH radical, R1 is optionally substituted phenyl, or cyclohexadienyl, naphthyl, or heterocyclyl, R2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino, R3 is halogen or OH and R4 is H or halogen if R3 is halogen, in their isomer forms, or mixture thereof, and possibly also their salts when they exist, and preparation thereof. The derivatives of the invention are particularly interesting as P substance antagonist.