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Anti-angiogenic agents and methods of use

An anti-angiogenesis and angiogenesis technology, applied in anti-inflammatory agents, cardiovascular system diseases, medical preparations containing active ingredients, etc., can solve the problem of limited number of anti-angiogenesis agents

Inactive Publication Date: 2010-08-11
SOUTHERN RES INST & IP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the number of safe and / or effective anti-angiogenic agents successfully discovered and / or identified to date is limited

Method used

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  • Anti-angiogenic agents and methods of use
  • Anti-angiogenic agents and methods of use
  • Anti-angiogenic agents and methods of use

Examples

Experimental program
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preparation example Construction

[0224] The preparation of such prodrug derivatives is discussed in various literature sources (examples are: Alexander et al., J. Med. Chem., 1988, 31, 318; Aligues-Martin ( Aligas-Martin et al., PCX WO pp / 41531, p. 30). The nitrogen functionality converted in the preparation of these derivatives is one (or more) of the nitrogen atoms in the compounds of the invention.

[0225] Prodrug forms of carboxyl compounds of the present invention include esters (-CO 2 R), wherein the R group corresponds to any alcohol having a pharmaceutically acceptable level of release in vivo by enzymatic or hydrolytic processes. Another prodrug derived from the carboxylic acid form of the present invention may be a quaternary salt structure as described by Bodor et al., Journal of Medicinal Chemistry, 1980, 23, 469

[0226]

[0227] It will of course be understood that the compounds of the present invention relate to all optical isomers and stereoisomers at every possible atom in the molecule....

example 1

[0232] Cell Proliferation Assay

[0233] Human primary cell lines (arterial endothelial, such as HAEC and HPAEC; venous endothelial HUVEC (from Cambrex BioScience Rockland) and lung fibroblasts LL47 (from American Type Cultures) were cultured according to instructions. American Type Culture Collection) and used it to assess the differential activity of target compounds against human endothelial versus fibroblasts by the CellTiter-Glo luminescent cell viability assay. This assay generates a luminescent signal, It is based on the quantification of ATP content in cell culture. The amount of ATP produced in cell culture reflects the number of viable cells. Therefore, this analysis is often used to assess cell proliferation and the cytotoxic effect of test compounds. Take approximately 5 × 10 3 Cells / well Cells were seeded in growth medium in 96-well plates. After 24 hours, various doses of the compound of interest were added to the cultures, each dose replicated four times. Afte...

example 2

[0235] Endothelial cell migration assay

[0236]Endothelial cell migration is a critical step in the angiogenic process that is decisive for the in situ recruitment response to vessel formation. Endothelial cell migration assays were performed using the permeable membrane chamber filter / insert chamber of the Biocoat Endothelial Cell Migration Angiogenesis System (BD Biosciences), which contains human fibronectin-coated 24-permeable membrane chamber plate with 3-μm pore size inserts. Inserts were incubated with endothelial cell basal medium containing 0.1% bovine serum albumin for 1 hr at 37 °C. Endothelial cells (HUVEC) were starved for 4 to 5 hours with 0.1% bovine serum albumin in endothelial cell basal medium, after which the cells were harvested and subsequently seeded (1×10 5 per well) in the upper chamber of a permeable membrane well plate, where each treatment was performed in 100 μl of 0.1% bovine serum albumin in endothelial cell basal medium. Add complete growth m...

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Abstract

The present disclosure relates generally to treating or preventing diseases associated with angiogenesis by administering to a patient certain compounds found to inhibit or substantially reduce angiogenesis. Compounds employed according to the present disclosure exhibit good anti-angiogenic activity as well as demonstrate a prophylactic effect for preventing and substantially reducing angiogenesis. Examples of such compounds include Ritanserin, Amiodarone, Terfenadinc, Perphenazine, Bithionol, and Clomipramine.

Description

technical field [0001] The present disclosure generally relates to treating or preventing diseases associated with angiogenesis by administering to a patient certain compounds that have been found to inhibit or substantially reduce angiogenesis. Compounds employed according to the present disclosure exhibit good anti-angiogenic activity and exhibit a prophylactic effect of preventing and substantially reducing angiogenesis. Examples of such compounds include Ritanserin, Amiodarone, Terfenadine, Perphenazine, Bithionol, and Clomipramine ). Background technique [0002] Angiogenesis refers to the formation of new blood vessels from pre-existing capillaries and is a series of events that play a key role in many physiological and pathological processes. Normal tissue growth (eg, in embryonic development, wound healing, and the menstrual cycle) is characterized by a reliance on neovascularization to supply oxygen and nutrients and to remove waste products. A number of differen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/542
CPCA61K31/5415A61K31/519A61K31/445A61K31/095A61K31/343A61K31/55A61P1/00A61P1/04A61P3/00A61P3/04A61P3/06A61P3/10A61P9/00A61P9/10A61P9/14A61P15/00A61P15/08A61P17/00A61P17/06A61P19/02A61P19/04A61P27/02A61P27/06A61P29/00A61P35/00A61P35/04A61P43/00A61K31/4465A61K31/542
Inventor 屈志参安舒·米塔尔·罗伊苏布拉马尼亚姆·阿南坦
Owner SOUTHERN RES INST & IP
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