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Activating Cl- secretion

a technology of cl-secretion and activation, which is applied in the field of activation of cl-secretion, can solve the problems of limited bioavailability, short-lived activities of compounds such as utp, and disappearance, and achieve the effect of stable activation of cl-secretion

Inactive Publication Date: 2002-03-21
SOUTHERN RES INST & IP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Benefits of technology

[0009] Compounds employed according to the present invention provide relatively stable activation of Cl.sup.- secretion in CF cells and tissues and appear to work by a mechanism independent of either intracellular Ca.sup.2+ or cAMP. Compounds employed according to the present invention elicit Cl.sup.- secretion that is active in CF and normal epithelia. and do not appear to require .DELTA.F508 CFTR at the cell surface.

Problems solved by technology

However, drugs such as UTP are rapidly cleared at the airway cell surface by endogenous ectonucleotidases, and therefore may have limited bioavailablility in vivo.
Moreover, the activities of compounds such as UTP are often short lived, and disappear within minutes unless fresh compound is continuously provided on to airway epithelium in vivo.

Method used

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Embodiment Construction

[0032] The compounds employed pursuant to the present invention are represented by the following formula: 7

[0033] wherein A is a 5 or 6 membered unsaturated heterocyclic ring containing at least one N atom; 8

[0034] X.sup.2 is O, NH, NR,

[0035] each R individually is alkyl, cycloalkyl, aryl, alkaryl and aralkyl,

[0036] each R.sup.2 individually is H, alkyl, cycloalkyl, aryl, alkaryl and aralkyl;

[0037] Y is a halogen; alkythio group or nitrogenous moiety.

[0038] Examples of some suitable 5 and 6 membered single ring groups suitable as the A moiety are 9

[0039] R and R.sup.2 are the same as defined above.

[0040] Examples of some suitable nitrogenous moieties for Y are N.sub.2, N.sub.3, NO.sub.2, NH.sub.2, CN, NCS, NHR, N(R).sub.2, and N.dbd.N--N(R).sub.2. R is the same as defined above.

[0041] The alkyl moieties of the R, R.sup.2 and Y groups typically contain 1-22 carbon atoms and more typically 1-12 carbon atoms. The cycloalkyl moieties include saturated and unsaturated ring groups such as...

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Abstract

Compounds represented by formula (I), wherein A is a 5 or 6-membered unsaturated heterocyclic ring containing at least one N atom; B is X2 is O, NH, NR, CH2, CHR or CR2, each R individually is alkyl, cycloalkyl, aryl, alkaryl and aralkyl, each R2 individually is H, alkyl, cycloalkyl, aryl, alkaryl, and aralkyl; Y is a halogen; alkythio group or nitrogenous moiety, are useful for activating Cl- secretion, and can be used for treating cystic fibrosis.

Description

[0001] The present invention is concerned with activating Cl.sup.-secretion in a patient. More particularly the present invention is especially concerned with treating patients suffering from cystic fibrosis by administering certain heterocyclic nitrogen containing compounds.BACKGROUND OF INVENTION[0002] Insufficient Cl.sup.- transport in epithelial cells has been associated with disease in individuals and especially with cystic fibrosis. In particular, the cystic fibrosis transmembrane conductance regulator (CFTR) functions as a Cl.sup.- channel. At the surface of epithelial cells. it also regulates the activity of other ion channels, including amiloride-sensitive Na.sup.+ channels, and other Cl.sup.-transport pathways. Cystic fibrosis mice lack Cl.sup.- transport capabilities in their nasal airways. lung cells, and intestines. In humans with cystic fibrosis, sweat ducts cannot properly reabsorb Cl.sup.-. It has also been suggested that the Pseudomonas predisposition in cystic fibr...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/4164A61K31/655
CPCA61K31/655A61K31/4164Y10S514/851
Inventor MADDRY, JOSEPH A.SORSCHER, ERIC J.
Owner SOUTHERN RES INST & IP
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