477259-57-7

Upstream product

• 2038-57-5 3-Phenylpropan-1-amine 
• 77970-72-0 2,2,2-trifluoro-N-(3-phenyl-propyl)acetamide 

Downstream Products

• 10079-78-4 p-β-(amino-n-propyl)-benzenesulfonamide 

Relevant academic research and scientific papers

Discovery of enantioselectivity of urea inhibitors of soluble epoxide hydrolase

Soluble epoxide hydrolase (sEH) hydrolyzes epoxyeicosatrienoic acids (EETs) in the metabolic pathway of arachidonic acid and has been considered as an important therapeutic target for chronic diseases such as hypertension, diabetes and inflammation. Although many urea derivatives are known as sEH inhibitors, the enantioselectivity of the inhibitors is not highlighted in spite of the stereoselective hydrolysis of EETs by sEH. In an effort to explore the importance of enantioselectivity in the urea scaffold, a series of enantiomers with the stereocenter adjacent to the urea nitrogen atom were prepared. The selectivity of enantiomers of 1-(α-alkyl-α-phenylmethyl)-3-(3-phenylpropyl)ureas showed wide range differences up to 125 fold with the low IC50 value up to 13 nM. The S-configuration with planar phenyl and small alkyl groups at α-position is crucial for the activity and selectivity. However, restriction of the free rotation of two α-groups with indan-1-yl or 1,2,3,4-tetrahydronaphthalen-1-yl moiety abolishes the selectivity between the enantiomers, despite the increase in activity up to 13 nM. The hydrophilic group like sulfonamido group at para position of 3-phenylpropyl motif of 1-(α-alkyl-α-phenylmethyl-3-(3-phenylpropyl)urea improves the activity as well as enantiomeric selectivity. All these ureas are proved to be specific inhibitor of sEH without inhibition against mEH.

1,3-disubstituted urea derivatives, optical isomer thereof, or pharmaceutically acceptable salts thereof, and a pharmaceutical composition for preventing or treating cardiovascular disease comprising the same as an active ingredient

The present invention relates to a 1,3-disubstituted urea derivative compound, an optical isomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for preventing or treating cardiovascular disorders containing the same as an active ingredient. The 1,3-disubstituted urea derivative compound excellently suppresses soluble epoxide hydrolase (sEH), and thus effectively blocks a metabolic pathway for epoxyeicosatrienoic acid (EET) to become dihydroxyeicosatrienoic acid (DHET), thereby being useful as pharmaceutical compositions for preventing or treating cardiovascular disorders.(AA) Positive control group(BB) Example 2-1(CC) Example 2-2(DD) Example 2-1(EE) Example 2-4(FF) Example 2-5(GG) Example 2-6(HH) Example 2-7(II) Example 2-8(JJ) Example 2-9(KK) Example 2-10(LL) Example 2-11(MM) Example 2-12(NN) Example 2-13(OO) Example 2-14(PP) Example 2-15(QQ) Example 2-16(RR) Example 2-17(SS) Example 2-18(TT) Example 2-19(UU) Example 2-20(VV) Example 2-21(WW) Example 2-22(XX) Example 2-23(YY) Example 2-24(Z1) Example 2-25(Z2) Example 2-26COPYRIGHT KIPO 2017

12-EPI-PLEUROMUTILINS

A compound selected from 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-sulfanyl)-acetyl]-12-epi-mutilins, or 14-0-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-oxy)-acetyl]-12-epi-mutilins, wherein 12-epi-mutilin is characterized in that the mutilin ring at position 12 is substituted by two substituents, the first substituent at position 12 of the mutilin ring is a methyl group which methyl group has the inverse stereochemistry compared with the stereochemistry of the methyl group at position 12 of the naturally occurring pleuromutilin ring, the second substituent at position 12 of the mutilin ring is a hydrocarbon group comprising at least one nitrogen atom and all other substituents of the mutilin ring having the same stereochemistry compared with the stereochemistry of the substituents at the corresponding positions in the naturally occurring pleuromutilin ring; optionally in the form of a salt and/or solvate, wherein the naturally occurring pleuromutilin is of formula PLEU, processes for the preparation of such compounds and their use as pharmaceuticals.

AMINOALCOHOL DERIVATIVES AND THEIR USE AS BETA-3 ADRENERGIC RECEPTOR AGONISTS

The present invention relates to a compound formula [I] or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.

Aminoalcohol derivatives

The present invention relates to a compound formula [I]: wherein R1 is hydrogen or halogen, R2 is hydrogen or an amino protective group, R3 is hydrogen or lower alkyl, X is bond, —CH2— or —O—, and Y is ?in which R4 is lower alkoxycarbonyl, ?in which R5 is carboxy(lower)alkyl, etc., ?in which R6 is hydroxy, etc., and so on, or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.