219692-16-7

Upstream product

• 5597-50-2 3-(4-hydroxyphenyl)propionic acid methyl ester 

Downstream Products

• 340697-25-8 3-[3,5-dibromo-4-(3-nitrobenzyloxy)phenyl]propionic acid 
• 340698-00-2 3-[3,5-dibromo-4-(3-aminobenzyloxy)phenyl]propionic acid 
• 918945-74-1 methyl 3-[3,5-dibromo-4-(4-nitrophenoxy)phenyl] propanoate 

Relevant academic research and scientific papers

Discovery of an Isothiazole-Based Phenylpropanoic Acid GPR120 Agonist as a Development Candidate for Type 2 Diabetes

We have discovered a novel series of isothiazole-based phenylpropanoic acids as GPR120 agonists. Extensive structure-activity relationship studies led to the discovery of a potent GPR120 agonist 4x, which displayed good EC50 values in both calcium and β-arrestin assays. It also presented good pharmaceutical properties and a favorable PK profile. Moreover, it demonstrated in vivo antidiabetic activity in C57BL/6 DIO mice. Studies in WT and knockout DIO mice showed that it improved glucose handling during an OGTT via GPR120. Overall, 4x possessed promising antidiabetic effect and good safety profile to be a development candidate.

Synthesis and use of phenylpropionic acid derivatives

The invention discloses a series of phenylpropionic acid derivatives, a preparation method thereof, and a use of the derivatives in pharmacy. The derivatives are compounds represented by formula I. Pharmacodynamic experiments show that the compounds of formula I have good agonist activity to GPR120; an in-vivo metabolism research result shows that the compounds of the formula I have good metabolism stability; and unexpectedly, the compounds have substantially higher agonist activity to the GPR120 after a difluoro substitute group is introduced to a phenyl ring at the carboxyl terminal of the compounds of the formula I. The compounds of the formula I can be used for drugs for preventing diabetes, obesity and other metabolic diseases.

Isothiazole derivatives as GPR120 agonists for the treatment of type II diabetes

Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, G, and Q are defined herein.

ISOTHIAZOLE DERIVATIVES AS GPR120 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES

Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, G, and Q are defined herein.

GPR120 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES

Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, G, and Q are defined herein; and wherein R11, R21, R41, RB1 and G1, are defined herein.

Epigenetic profiling of the antitumor natural product psammaplin A and its analogues

A collection of analogues of the dimeric natural product psammaplin A that differ in the substitution on the (halo)tyrosine aryl ring, the oxime and the diamine connection has been synthesized. The effects on cell cycle, induction of differentiation and apoptosis of the natural-product inspired series were measured on the human leukaemia U937 cell line. Epigenetic profiling included induction of p21WAF1, effects on global H3 histone and tubulin acetylation levels as well as in vitro enzymatic assays using HDAC1, DNMT1, DNMT3A, SIRT1 and a peptide domain with p300/CBP HAT activity. Whereas the derivatives of psammaplin A with modifications in the length of the connecting chain, the oxime bond and the disulfide unit showed lower potency, the analogues with changes on the bromotyrosine ring exhibited activities comparable to those of the parent compound in the inhibition of HDAC1 and in the induction of apoptosis. The lack of HDAC1 activity of analogues modified on the disulfide bond suggests that its cleavage must occur in cells to produce the monomeric Zn2+-chelating thiol. This assumption is consistent with the molecular modelling of the complex of psammaplin A thiol with h-HDAC8. Only a weak inhibition of DNMT1, DNMT3A and residual activities with SIRT1 and a p300/CBP HAT peptide were measured for these compounds.

NOVEL PHARMACEUTICAL COMPOSITIONS COMPRISING AGONISTS OF THE THYROID RECEPTOR

The invention provides compounds of formula I or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition mediated by a thyroid receptor. Formula (I) wherein R1, R2, n, Y, Y', R3, R4, W and R5 are as defined in the specification.

THYROID RECEPTOR AGONISTS

The invention provides compounds of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition mediated by a thyroid receptor. Formula (I), wherein R1, R2, n, Y, Y', R3, R4, W and R5 are as defined in the specification.