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Triaryl methane compounds for sickle cell disease

A technology of compounds and compound systems, applied in the direction of silicon organic compounds, compounds of group 4/14 elements of the periodic table, active ingredients of heterocyclic compounds, etc., can solve problems such as inability to inhibit Gardos channels and prevent potassium loss

Inactive Publication Date: 2000-04-19
PRESIDENT & FELLOWS OF HARVARD COLLEGE +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Other imidazole-containing compounds have been found not to inhibit Gardos channels and prevent potassium loss

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0298] Example: In vitro activity

[0299] This example demonstrates the in vitro activity of several enumerated compounds of formula (I) in inhibiting the Gardos channel of erythrocytes and / or mitogen-induced cell proliferation. This assay is generally applicable to demonstrate the activity of other compounds of formula (I) in vitro.

[0300] 7.1 Experimental procedure

[0301] Inhibition percentage and IC of Gardos channel (10 μM compound) 50 The assay is as described in Brugnara et al., 1993, J. Biol. Chem. 268(12):8760-8768. Inhibition percentage and IC of mitotic factor-induced cell proliferation (10μM compound) with 3T3 mouse fibroblasts (ATCCNo.CRL 1658) 50 The assay was as described in Benzaquen et al. (1995, Nature Medicine 1:534-540). Tribendazole is reported for comparison purposes. Other cell lines, eg, cancer cells, endothelial cells and fibroblasts, and likewise many other cells, can be used in cell proliferation assays. The choice of a particular cell line...

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Abstract

The present invention provides compounds useful as medicaments for the treatment of sickle cell disease and diseases characterized by undesirable or abnormal cell proliferation. These compounds are substituted triarylmethane compounds or analogs thereof, wherein one or more aryl groups are partially substituted by heteroaryl, cycloalkyl or heterocycloalkyl groups and / or wherein the quaternary carbon is replaced by a different atom such as silicon, germanium , nitrogen or phosphorus substitution. They inhibit mammalian cell proliferation, inhibit the Gardos channel in cytoplasm, reduce sickle cell dehydration and / or delay red blood cell sickling and deformation.

Description

[0001] 1. Comparison of related applications [0002] This application is a continuation-in-part of co-pending application No. 08 / 618,592, filed March 20, 1996, and co-pending application No. 08 / 618,760, filed March 20, 1996, Each of these applications is a continuation-in-part of Application No. 08 / 307,874, filed September 16, 1994 and now abandoned. This application is also a continuation-in-part of co-pending application serial no. , each of which is a continuation-in-part of Application No. 08 / 307,887 filed September 16, 1994 and now abandoned. These applications are fully incorporated herein by reference. 2. Field of invention [0003] The present invention relates to aromatic organic compounds, Ca for erythrocyte and / or mammalian cell proliferation 2+ Potent and safe specific inhibitor of activated potassium channels (Gardos channels). The compound can be used as an in situ treatment method for the treatment or prevention of sickle cell disease to reduce dehydration ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/14A61K31/40C07C217/18C07C217/20C07D207/08C07F7/08C07F7/10C07F7/18
Inventor 卡洛·布鲁格纳拉乔斯·哈伯林爱米尔·贝洛特马克·弗洛伊摩维兹理查德·隆巴尔迪约翰·克利福德高莹铎里姆·M·海达尔尤金·W·凯莱赫法尔吉尼·M·凯尔阿德尔·M·穆萨耶西·P·萨奇德瓦孙明华赫德·N·塔夫脱
Owner PRESIDENT & FELLOWS OF HARVARD COLLEGE
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