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Compositions and methods for the treatment of pathological condition(s) related to GPR35 and/or GPR35-HERG complex

The technology of a compound, 2NR101R102, is applied in the field of compositions and methods for treating pathological conditions related to GPR35 and/or GPR35-HERG complexes

Inactive Publication Date: 2013-08-07
CORNING INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are no reports in the literature suggesting that GPR35-containing hERG and GPCRs can physically interact to form a signaling complex

Method used

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  • Compositions and methods for the treatment of pathological condition(s) related to GPR35 and/or GPR35-HERG complex
  • Compositions and methods for the treatment of pathological condition(s) related to GPR35 and/or GPR35-HERG complex
  • Compositions and methods for the treatment of pathological condition(s) related to GPR35 and/or GPR35-HERG complex

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0686] 1. Preparation of compounds of formula (I), (II), (III), (IV), (V) and (VI)

[0687] The following are examples of the preparation of compounds of formula (I), (II), (III), (IV), (V) and (VI). This embodiment is exemplary only, and is not intended to limit the present disclosure.

[0688]

[0689] i.2-Dicyanomethylene-3-cyano-4,5-dimethyl-5-[4’-n-butylphenyl]-2,5-dihydrofuran

[0690] 3-Hydroxy-3-[4'-n-butylphenyl]-2-butanone 10.0g (0.0455 mol), malononitrile 6.0g (0.091 mol), lithium ethoxide 2.3ml (2.3mmol) and THF50ml Mix and boil at reflux overnight. The pure product (2-dicyanomethylene-3-cyano-4,5-dimethyl-5-[4'-n-butylphenyl]-2,5-dihydrofuran) was obtained from ethanol Recrystallization of to generate 9.95g: 69.1% yield.mp: 129.3-130.5°C. 1H NMR: δ7.259(d,2H),7.112(d,2H),2.638(t,2H,CH 2 ),2.225(s,3H,Me),1.997(s,3H,Me),1.60-1.28(m,4H,CH 2 ),0.931(t,3H,CH 3 ). 13 C NMR: 182.476, 175.753, 145.841, 131.069, 129.692(2C), 125.075(2C), 110.914, 110.406, 109.08...

Embodiment 2

[0786] 1. Materials and Methods

[0787] i.Material

[0788] Toprinast was obtained from BioMol International Inc (Plymouth Meeting, PA). cell culture compatibility 384 Biosensor Microplates were obtained from Corning Incorporated (Corning, NY).

[0789] Both HEK293 and HT-29 cells were obtained from American Type Cell Culture (Manassas, VA). Cell culture media were as follows: (1) Eagle's medium (MEM) supplemented with 10% fetal bovine serum (FBS), 4.5 g / L glucose, 2 mM glutamine, and antibiotics for HEK293; and (2) McCoy' s5a modified medium supplemented with 10% FBS, 4.5 g / L glucose, 2 mM glutamine, and antibiotics for human colorectal adenocarcinoma HT29.

[0790] The HEK hERG stable cell line (HEK-hERG) and the CHO hERG stable cell line (CHO-hERG) were maintained according to Sun et al. (J. Biol. Chem. 2006, 281:5877). Cells were subcloned 1-2 times per week, and cells with less than 15 passages were used for all experiments.

[0791] ii. Calcium flux test

[0792...

Embodiment 3

[0835] 1. Materials and Methods

[0836] i.Material

[0837] Toprinast was obtained from BioMol International Inc (Plymouth Meeting, PA). cell culture compatibility 384 Biosensor Microplates were obtained from Corning Incorporated (Corning, NY). All tyrphostin compounds were obtained from Sigma Chemical Co. (St. Louis, MO).

[0838] Both HEK293 and HT-29 were obtained from the American Type Cell Culture (Manassas, VA). Cell culture media were as follows: (1) Eagle's medium (MEM) supplemented with 10% fetal bovine serum (FBS), 4.5 g / L glucose, 2 mM glutamine, and antibiotics for HEK293; and (2) McCoy' s5a modified medium supplemented with 10% FBS, 4.5 g / L glucose, 2 mM glutamine, and antibiotics for human colorectal adenocarcinoma HT29.

[0839] ii. Calcium flux test

[0840] Fluo-4Direct TM Calcium assay kit was purchased from Invitrogen (Starter pack, catalog number F10471). HEK293 cells (15,000 cells / well) and HT29 cells (30,000 cells / well) were seeded into poly-D-l...

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Abstract

Disclosed are compositions and methods for the prevention and / or treatment of diseases which are pathophysiologically related to GPR35, and / or GPR35-HERG signaling complex. For example, disclosed are compounds for preventing and / or treating diseases which are pathophysiologically related to GPR35 in a subject.

Description

[0001] Cross References to Related Applications [0002] This application claims priority under 35 U.S.C. §119 to U.S. Provisional Application No. 61 / 365,861, filed July 20, 2010, the contents of which are based upon and incorporated by reference in its entirety. [0003] sequence listing [0004] This application contains a Sequence Listing filed electronically with the USPTO via the EFS website as "20110712_SP10_204_ST25.txt," 37,594 bytes in size and created on July 13, 2011. Due to the electronic filing of sequence listings, electronically filed sequence listings serve as paper copies required by 37 CFR §1.821(c) and CRFs required by §1.821(e). The information contained in the Sequence Listing is hereby incorporated by reference and does not exceed the disclosure in the filed International Application. Background technique [0005] G protein-coupled receptors (GPCRs) have been and continue to be one of the most abundant drug target families. There are at least two key d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/34C07D213/74C07D307/52C07D307/66C07D333/16C07D333/20C07D333/22C07D333/36C07D333/38C07C229/56C07C255/42
CPCC07C255/34C07D333/20C07C255/42C07C229/58C07D213/74C07D333/36C07D333/38C07D307/66C07D207/34C07D307/52C07D333/22C07D333/16C07C229/56A61P29/00A61P3/00A61P3/04A61P35/00A61P35/02A61P3/06A61P43/00A61P9/00A61P9/06A61P9/10A61P9/12A61P3/10
Inventor 邓华云方晔贺明谦H·胡钮渭钧孙海燕
Owner CORNING INC
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