29121-25-3

Upstream product

• 64-17-5 ethanol 
• 38692-80-7 2-(3-bromo-4-hydroxyphenyl)acetic acid 
• 156-38-7 4-hydroxyphenylacetate 
• 17138-28-2 (4-hydroxy-phenyl)-acetic acid ethyl ester 

Downstream Products

• 104744-00-5 [3-(4-{2-[2-(4-benzyloxy-phenyl)-acetylamino]-ethyl}-2-methoxy-phenoxy)-4-hydroxy-phenyl]-acetic acid ethyl ester 
• 17138-28-2 (4-hydroxy-phenyl)-acetic acid ethyl ester 
• 1168133-69-4 ethyl 2-(3-bromo-5-chloro-4-(cyclopropylmethoxy)phenyl)acetate 
• 1168111-82-7 2-(3-(benzo[c][1,2,5]thiadiazol-5-yl)-5-chloro-4-(cyclopropylmethoxy)phenyl)-4-methylpentanoic acid 
• 1168134-93-7 ethyl 2-(3-(benzo[c][1,2,5]thiadiazol-5-yl)-5-chloro-4-(cyclopropylmethoxy)phenyl)-4-methylpentanoate 
• 1168111-72-5 2-(3-(benzo[c][1,2,5]oxadiazol-5-yl)-5-chloro-4-(cyclopropylmethoxy)phenyl)-4-methylpentanoic acid 
• 1168134-92-6 ethyl 2-(3-(benzo[c][1,2,5]oxadiazol-5-yl)-5-chloro-4-(cyclopropylmethoxy)phenyl)-4-methylpentanoate 
• 1168135-11-2 2-(3-(benzo[d]thiazol-6-yl)-5-chloro-4-(cyclopropylmethoxy)phenyl)-4-methylpentanoic acid 
• 1168134-91-5 ethyl 2-(3-(benzo[d]thiazol-6-yl)-5-chloro-4-(cyclopropylmethoxy)phenyl)-4-methylpentanoate 
• 1168134-90-4 ethyl 2-(3-bromo-5-chloro-4-(cyclopropylmethoxy)phenyl)-4-methylpentanoate 
• 1168134-88-0 ethyl 2-(3-bromo-5-chloro-4-(cyclopropylmethoxy)phenyl)-4-methoxybutanoate 
• 1168120-61-3 1-(5-chloro-4'-isopropyl-6-(2,2,2-trifluoroethoxy)biphenyl-3-yl)cyclobutanecarboxylic acid 
• 1168134-75-5 ethyl 1-(5-chloro-4'-isopropyl-6-(2,2,2-trifluoroethoxy)biphenyl-3-yl)cyclobutanecarboxylate 
• 1168120-73-7 1-(5-chloro-4'-(methylthio)-6-(2,2,2-trifluoroethoxy)biphenyl-3-yl)cyclobutanecarboxylic acid 

Relevant academic research and scientific papers

L-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPAR?

Thyroid hormones (THs) operate numerous physiological processes through modulation of the nuclear thyroid hormone receptors and several other proteins. We report direct activation of the nuclear peroxisome proliferator-activated receptor gamma (PPAR?) and retinoid X receptor (RXR) by classical and nonclassical THs as another molecular activity of THs. The T4 metabolite TETRAC was the most active TH on PPARγwith nanomolar potency and binding affinity. We demonstrate that TETRAC promotes PPAR?/RXR signaling in cell-free, cellular, and in vivo settings. Simultaneous activation of the heterodimer partners PPARγand RXR resulted in high dimer activation efficacy. Compared to fatty acids as known natural ligands of PPARγand RXR, TETRAC differs markedly in its molecular structure and the PPAR?-TETRAC complex revealed a distinctive binding mode of the TH. Our observations suggest a potential connection of TH and PPAR signaling through overlapping ligand recognition and may hold implications for TH and PPAR pharmacology.

PYRROLE AMIDE INHIBITORS

The present invention provides for compounds of formula (I) wherein R1, R2, R3, and R10 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).

BROMODOMAIN INHIBITORS

The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, X1, X2, Y1, L1, G1, Rx, and Ry have any of the values defined thereof in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).

BROMODOMAIN INHIBITORS

Provided are compounds of formula (I), wherein A1, A2, A3, A4, X1, X2, Y1, L1, G1, Rx, and Ry have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).

TETRASUBSTITUTED BENZENES FOR TREATMENT OF EARLY ONSET ALZHEIMER'S DISEASE

Provided are compositions and methods for treating early onset familial Alzheimer's Disease. The compositions and methods can be used for improving one or more aspects of cognitive function in a patient suffering from early onset familial Alzheimer's Dise

Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin

As an extension of our analysis of the effect of halogenation on thiourea TRPV1 agonists, we have now modified selected 4-hydroxy(or 4-amino)-3- methoxyphenyl acetamide TRPV1 agonists by 5- or 6-halogenation on the aromatic A-region and evaluated them for potency for TRPV1 binding and regulation and for their pattern of agonism/antagonism (efficacy). Halogenation shifted the functional activity at TRPV1 toward antagonism with a greater extent of antagonism as the size of the halogen increased (I > Br > Cl), as previously observed for the thiourea series. The extent of antagonism was greater for halogenation at the 5-position than at the 6-position, in contrast to SAR for the thiourea series. In this series, compounds 55 and 75 showed the most potent antagonism, with Ki (ant) = 2.77 and 2.19 nM, respectively, on rTRPV1 expressed in Chinese hamster ovary cells. The compounds were thus ca. 40-60-fold more potent than 6′-iodononivamide.

N,N-DISUBSTITUTED AMINOALKYLBIPHENYL ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS

Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

TETRASUBSTITUTED BENZENES

Tetrasubstituted benzenes that act as modulators of gamma secretase and their use in the treatment of one or more symptoms of treating neurodegenerative disorders, e.g., Alzheimer's disease, are described.