56872-39-0

Upstream product

• 108-30-5 succinic acid anhydride 
• 108-95-2 phenol 
• 3153-44-4 4-(4-methoxy-phenyl)-4-oxo-butyric acid 
• 6311-68-8 monophenyl succinate 
• 100-66-3 methoxybenzene 
• 33527-94-5 4-acetoxyiodobenzene 
• 113425-33-5 4-hydroxy-1-(4-hydroxyphenyl)-butan-1-one 
• 540-38-5 p-Iodophenol 
• 24849-48-7 4-hydroxybenzoylacrylic acid 
• 15118-67-9 ethyl 3-(4-methoxybenzoyl)-propionate 
• 7446-70-0 aluminium trichloride 
• 108-88-3 toluene 
• 860426-16-0 succinic acid ethyl ester-phenyl ester 
• 7182-43-6 4-(4-hydroxy-phenyl)-4-oxo-butyronitrile 

Downstream Products

• 39560-32-2 4-hydroxy-gamma-oxobenzenebutanoic acid,methyl ester 
• 66123-43-1 4-(4-hydroxyphenyl)-4-oxobutanoic acid ethyl ester 
• 959251-49-1 Acetic acid 4-(4-cyclohexylidene-5-oxo-4,5-dihydro-furan-2-yl)-phenyl ester 
• 91540-69-1 4-dimethylthiocarbamoyloxygamma-oxobenzenebutanoic acid,methyl ester 
• 134858-58-5 1-<4-(2-carboxyethyl)phenoxy>-3-1-(N⁴-phenyl-piperazinyl)>propane 
• 134858-68-7 (1-(4-Chloro-benzoyl)-5-methoxy-2-{4-[3-(4-phenyl-piperazin-1-yl)-propoxy]-phenyl}-1H-indol-3-yl)-acetic acid; hydrochloride 
• 119348-34-4 4-<4-<(4-acetyl-3-hydroxy-2-propylphenyl)methoxy>phenyl>-4-oxobutanoic acid 
• 119348-33-3 4-<4-<(4-acetyl-3-hydroxy-2-propylphenyl)methoxy>phenyl>-4-oxobutanoic acid ethyl ether 
• 91121-67-4 4-(4-Isopropoxy-phenyl)-4-oxo-butyric acid 
• 7021-11-6 4-(4-hydroxyphenyl)butanoic acid 
• 855233-95-3 5-(4-acetoxy-phenyl)-3H-furan-2-one 
• 14328-06-4 5-(4-hydroxyphenyl)-γ-butyrolactone 
• 91584-73-5 (4S,5R)-5-{4-[3-(4-Acetyl-3-hydroxy-2-propyl-phenoxy)-propylsulfanyl]-phenyl}-4-methyl-dihydro-furan-2-one 
• 91584-73-5 (4R,5R)-5-{4-[3-(4-Acetyl-3-hydroxy-2-propyl-phenoxy)-propylsulfanyl]-phenyl}-4-methyl-dihydro-furan-2-one 

Relevant academic research and scientific papers

Preparation of aromatic γ-hydroxyketones by means of Heck coupling of aryl halides and 2,3-dihydrofuran, catalyzed by a palladium(ii) glycine complex under microwave irradiation

A series of aromatic γ-hydroxyketones were prepared by means of Heck coupling reaction of aryl halides and 2,3-dihydrofuran, catalyzed by PdCl2·Gly2 and under microwave irradiation. This synthetic transformation involves the formation of an aryl-dihydrofuranoic intermediate, followed by an unusual opening of the heterocycle promoted by a water molecule and the formation of the ketone carbonyl function through keto-enol tautomerism. This journal is

Composition and kit comprising piperazine derivatives and metformin, and use thereof in the treatment of diabetes

The present invention relates to a composition comprising, in combination, metformin or a salt thereof, a pharmaceutically acceptable carrier or excipient and at least one compound of formula (I), the enantiomers, diastereoisomers or pharmaceutically acceptable salts thereof. Formula (I). The present invention also relates to the use of said composition for the treatment of diseases associated with insulin resistance syndrome.

PIPERAZINE DERIVATIVES, METHODS FOR PREPARING SAME, AND USES THEREOF IN THE TREATMENT OF INSULIN RESISTANCE

The invention relates to a compound of formula (I), where R1, R2, R7, m, n, and L1 are as defined in claim 1, and to the methods for preparing same, to the pharmaceutical compositions containing same, and to the

ARYL GPR120 RECEPTOR AGONISTS AND USES THEREOF

Aryl GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.

Antileukotrienic phenethylamido derivatives of arylalkanoic acids in the treatment of ulcerative colitis

A series of arylalkanoic acid derivatives bearing methyl(phenethyl)amino groups were prepared and their inhibition of LTB4 biosynthesis was evaluated. Regression analysis showed the slightly different parabolic dependences of this activity on lipophilicity of α-methyl and α-unsubstituted alkanoic acid derivatives. The relationship derived for α-unsubstituted alkanoic acids was extended by previously prepared group of similar derivatives of arylacetic acids without any change of regression coefficients and statistical criteria. It was concluded that the most active compounds belong to 2-arylpropanoic acid derivatives with lipophilicity close to log Popt (=6.97). But generally, the structural changes in the acidic part of compounds under study did not yield the substantial improvement of LTB4 biosynthesis inhibition in comparison with the previously prepared series of derivatives IV. The anti-inflammatory effect of the compounds under study was evaluated in three animal models of inflammation and their possible utilization in the treatment of ulcerative colitis (UC) was followed. From 12 evaluated compounds, 4 compounds are more active in UC inhibition than the standard sulfasalazine but it can be stated that the change of connecting chain between aromatic ring and carboxyl did not bring about the important improvement of this activity in comparison with previous derivatives of arylacetic acids. Possible relation between LTB4 biosynthesis inhibition and ulcerative colitis is seriously broken by the compound 8a with carbonyl as the additional functional group on the connecting chain between carboxyl and aromatic ring.

Novel high-affinity and selective biaromatic 4-substituted γ-hydroxybutyric acid (GHB) analogues as GHB ligands: Design, synthesis, and binding studies

γ-Hydroxybutyrate (GHB) is a metabolite of γ-aminobutyric acid (GABA) and has been proposed to function as a neurotransmitter or neuromodulator. GHB is used in the treatment of narcolepsy and is a drug of abuse. GHB binds to both GABAB receptors and specific high-affinity GHB sites in brain, of which the latter have not been linked unequivocally to function, but are speculated to be GHB receptors. In this study, a series of biaromatic 4-substituted GHB analogues, including 4′-phenethylphenyl, 4′-styrylphenyl, and 4′-benzyloxyphenyl GHB analogues, were synthesized and characterized pharmacologically in a [3H](E,RS)-(6,7, 8,9-tetrahydro-5-hydroxy-5H-benzocyclohept-6-ylidene)acetic acid ([ 3H]NCS-382) binding assay and in GABAA and GABA B receptor binding assays. The compounds were selective for the high-affinity GHB binding sites and several displayed Ki values below 100 nM. The affinity of the 4-[4′-(2-iodobenzyloxy)phenyl] GHB analogue 17b was shown to reside predominantly with the R-enantiomer (Ki = 22 nM), which has higher affinity than previously reported GHB ligands.

Studies on non-thiazolidinedione antidiabetic agents. 3. Preparation and biological activity of the metabolites of TAK-559

Preparation and biological activity of the metabolites of the potent antihyperglycemic and antihyperlipidemic agent, (E)-4-{4-[(5-methyl-2-phenyl-1, 3-oxazol-4-yl)methoxy]benzyloxyimino}-4-phenylbutyric acid (TAK-559) (1), were investigated. Metabolites M

Ion triggered alkylation of biological targets by silyloxy aromatic agents

A silyloxy aromatic derivative capable of alkylating a target biological molecule when activated by ionic strength. A sequence directed reagent may be constructed by conjugating a methyl silyloxy aromatic derivative to a hexamethylamino linker attached to either the 5' or 3' terminus of an oligonucleotide. Annealing this modified fragment of DNA to its complementary sequence allows for target modification subsequent to ionic activation. The product of this reaction is a covalent crosslink between the reagent and target strands resulting from an alkylation of DNA by the activated silyloxy aromatic derivative. In a preferred embodiment, a nitrophenyl or bromo group is attached to a methyl group of the silyloxy aromatic derivative. This reagent may be similarly linked to an oligonucleotide probe. Activation of the alkylating agent by an ionic signal (X) which may naturally occur, or may be introduced into the media containing the target molecule, such as by the introduction of a salt (MX).

Ion triggered alkylation of biological targets by silyloxy aromatic agents

A silyloxy aromatic derivative capable of alkylating a target biological molecule when activated by ionic strength. A sequence directed reagent may be constructed by conjugating a methyl silyloxy aromatic derivative to a hexamethyiamino linker attached to either the 5' or 3' terminus of an oligonucleotide. Annealing this modified fragment of DNA to its complementary sequence allows for target modification subsequent to ionic activation. The product of this reaction is a covalent crosslink between the reagent and target strands resulting from an alkylation of DNA by the activated silyloxy aromatic derivative. In a preferred embodiment, a nitrophenyl or bromo group is attached to a methyl group of the silyloxy aromatic derivative. This reagent may be similarly linked to an oligonucleotide probe. Activation of the alkylating agent by an ionic signal (X) which may naturally occur, or may be introduced into the media containing the target molecule, such as by the introduction of a salt (MX).

Orally active β-lactam inhibitors of human leukocyte elastase. 2. Effect of C-4 substitution

The effect of changing the C-4 substituent of 3,3-diethyl-1- [(benzylamino)carbonyl]-2-azetidinone on inhibition of HLE and in a model of HLE-induced lung damage in hamsters was explored. Substituents at this position do not appear to interact strongly with HLE with the most potent compounds having k(obs)/[I] = 6900 M-1 s-1. However, substituents at this position had a marked effect on in vivo activity. The greatest oral activity in the lung hemorrhage assay was achieved with C-4 aryl carboxylic acid ethers (60-85% inhibition at 30 mg/kg po). Based upon the established mechanism of inhibition by these compounds, the C-4 substituent would be released, and therefore, the pharmacological potential of these C-4 substituents was of considerable concern. Fortunately, compounds containing 4-hydroxybenzoic acid and 4-hydroxyphenylacetic acid ethers at C-4 were among the most active analogs. These phenolic acids are also found as urinary metabolites in healthy humans. Other heteroaryls at C-4 were also orally active in this model despite relatively modest enzyme activity.