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Compositions and methods for suppression of carbonic anhydrase activity

A composition and compound technology, applied in the direction of drug combination, organic active ingredients, diseases, etc., can solve the problems of low bioavailability, small size, abnormal sensation of face and limbs, etc.

Inactive Publication Date: 2015-02-18
CELLIXBIO PTE LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The reduced compound (thiol) is not bulky and shows excellent CA inhibitory activity (in the low nanomolar range) compared to the corresponding sterically hindered disulfide, which is difficult to access The limited space of the active site of the enzyme, and its low bioavailability, poor pharmacokinetics, and common side effects such as toe numbness, loss of taste, movement disorders, facial and extremity paresthesias and blurred vision

Method used

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  • Compositions and methods for suppression of carbonic anhydrase activity
  • Compositions and methods for suppression of carbonic anhydrase activity
  • Compositions and methods for suppression of carbonic anhydrase activity

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Embodiment Construction

[0031] definition

[0032] As used herein, the following terms and phrases shall have the meanings set forth below. Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art.

[0033] The compounds of the present invention may exist in the form of pharmaceutically acceptable salts. The compounds of the invention may also exist in the form of pharmaceutically acceptable esters (ie, the methyl and ethyl esters of the acids of formula I to be used as prodrugs). The compounds of the invention may also be solvated, ie hydrated. Solvation may act or occur during the manufacturing process, ie due to the hygroscopic nature of the initially anhydrous compound of formula I (hydration).

[0034] Compounds that have the same molecular formula but differ in the nature or in the sequence in which their atoms are joined or in the arrangement of their atoms in space are termed "isomers". Isomer...

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Abstract

Provided are the compounds of formula (I) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula (I), and methods for treating or preventing or modulating carbonic anhydrase activity in a disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral admimstration, syrup, or injection. Such compositions may be used to treatment of glaucoma, epileptic seizures, Idiopathic intracranial hypertension (pseudotumor cerebri), altitude sickness, cystinuria, periodic paralysis and dural ectasia, congestive heart failure, drug induced edema, diuretic, intermittent claudication resulting from obstructed arteries in the limbs, and vascular dementia.

Description

[0001] priority [0002] This application claims the benefit of Indian Provisional Patent Application No. 1810 / CHE / 2012, filed May 8, 2012, the entire disclosure of which is relied upon for all purposes and is incorporated by reference in its entirety In this application. technical field [0003] The present disclosure relates generally to compounds and compositions useful for inhibiting carbonic anhydrase activity. More specifically, the invention relates to the treatment of a subject with a pharmaceutically acceptable dose of a compound, stereoisomer, enantiomer, crystal, ester, salt, hydrate, prodrug, or mixture thereof. Background technique [0004] Carbonic anhydrases (CAs; also known as carbonic dehydratases EC 4.2.1.1) are ubiquitous metalloenzymes in prokaryotes and eukaryotes encoded by four evolutionarily unrelated gene families. CAs catalyze CO 2 A simple physiological reaction into bicarbonate ions and protons. The active sites of most CAs contain zinc ions (...

Claims

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Application Information

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IPC IPC(8): C07D285/135A61K31/433
CPCC07D285/135C07D417/12A61P1/08A61P1/16A61P3/10A61P7/00A61P7/10A61P9/00A61P9/04A61P9/10A61P11/06A61P11/08A61P13/02A61P13/12A61P15/08A61P19/10A61P25/00A61P25/04A61P25/08A61P25/28A61P27/06A61P35/00A61P43/00
Inventor M·坎杜拉
Owner CELLIXBIO PTE LTD
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