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C17-heteroaryl derivatives of oleanolic acid and methods of use thereof

A technology of heteroaryldiyl and alkyl groups, which can be used in medical preparations, drug combinations, and pharmaceutical formulations containing active ingredients, and can solve problems such as differences

Active Publication Date: 2015-07-08
REATA PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although betulinic acid derivatives have shown comparable anti-inflammatory properties, their pharmacology also appears to be significantly different compared to OA-derived compounds (Liby et al., 2007b)

Method used

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  • C17-heteroaryl derivatives of oleanolic acid and methods of use thereof
  • C17-heteroaryl derivatives of oleanolic acid and methods of use thereof
  • C17-heteroaryl derivatives of oleanolic acid and methods of use thereof

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Embodiment Construction

[0025] Disclosed herein are novel compounds and compositions having antioxidant and / or anti-inflammatory properties, methods of their manufacture, and methods of their use, including methods for treating and / or preventing disease.

[0026] I. Definition

[0027] When used in the context of chemical groups: "hydrogen" means -H; "hydroxyl" means -OH; "oxo" means =O; "carbonyl" means -C( =O)-; "Carboxyl" means -C(=O)OH (also written as -COOH or -CO 2 H); "halo" means independently -F, -Cl, -Br or -I; "amino" means -NH 2 ; "Hydroxyamino" means -NHOH; "nitro" means -NO 2 ; imino means =NH; "cyano" means -CN; "isocyanate" means -N=C=O; "azido" means -N 3 ; in a monovalent context, "phosphate group" means -OP(O)(OH) 2 or its deprotonated form; in a divalent context, "phosphate" means -OP(O)(OH)O- or its deprotonated form; "mercapto" means -SH; and "thio / Thio" means =S; "sulfonyl" means -S(O) 2 -; and "sulfinyl" means -S(O)-.

[0028] In the context of a chemical formula, the ...

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Abstract

Disclosed herein are novel C17-heteroaryl derivatives of oleanolic acid, including those of the formula (I): wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example, as antioxidant inflammation modulators, and compositions thereof are also provided.

Description

[0001] This application claims the benefit of U.S. Provisional Patent Application No. 61 / 699,199, filed September 10, 2012, which is hereby incorporated by reference in its entirety. [0002] Pursuant to 37 C.F.R.1.821(c), the Sequence Listing is hereby filed in an ASCII text file named "REATP0076US_SequenceListing_ST25.txt (REATP0076US_Sequence Listing_ST25.txt)" dated September 9, 2013 created and has a size of about 1KB. The entire contents of the aforementioned documents are hereby incorporated by reference. Background technique [0003] I.Technical field [0004] The present invention relates generally to the fields of biology and medicine. More specifically, the present invention relates to compounds, compositions and methods for the treatment and prevention of diseases, such as those associated with oxidative stress and inflammation. [0005] II. Description of related technologies [0006] The anti-inflammatory and anti-proliferative activities of the naturally occ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00A61K31/56A61P29/00
CPCC07D271/10C07J63/008C07D271/06A61P29/00A61P39/06
Inventor 江昕克里斯多福·F·班德麦琳·维斯尼克
Owner REATA PHARMA INC
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