Novel Compounds for Treatment of Cancer and Disorders Associated with Angiogenesis Function

a technology of angiogenesis and therapeutic compounds, which is applied in the direction of heterocyclic compound active ingredients, biocide, drug compositions, etc., can solve the problems of inability to achieve easy and straightforward ways with current technologies, and inability to achieve oral anticancer drugs. , to achieve the effect of modulating (increasing or decreasing) expression and low density lipoprotein

Inactive Publication Date: 2010-05-13
UNIV OF SOUTHERN CALIFORNIA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although various strategies have been used to identify drug targets, it is becoming appreciated that there are no easy and straightforward ways to do so with current technologies.
Second, there is an overwhelming redundancy built into the biological systems serving as targets, due to the abundance of sequence and structural homology.
Although antiviral drugs are almost always administered orally, only very few anticancer drugs are orally active.
However, one major hurdle to overcome in a drug discovery program is the identification of a suitable lead compound having desired biological activity.
Traditional pharmacokinetic studies, although essential, are cumbersome and timeconsuming and require a large number of animals.

Method used

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  • Novel Compounds for Treatment of Cancer and Disorders Associated with Angiogenesis Function
  • Novel Compounds for Treatment of Cancer and Disorders Associated with Angiogenesis Function
  • Novel Compounds for Treatment of Cancer and Disorders Associated with Angiogenesis Function

Examples

Experimental program
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example i

Chemistry

[0127]All reactions were carried out under a nitrogen atmosphere. Progress of the reaction was monitored by TLC on silica gel plates (Merck 60, F254, 0.2 mm). Organic solutions were dried over MgSO4; evaporation refers to removal of solvent on a rotary evaporator under reduced pressure. Melting points were measured using a Gallenkamp apparatus and are uncorrected. IR spectra were recorded as thin films on Perkin-Elmer 398 and FT 1600 spectrophotometers. 1H NMR spectra were recorded on a Brüker 300-MHz spectrometer with TMS as an internal standard: chemical shifts are expressed in δ values (ppm) and coupling constants (J) in Hz. Mass spectral data were determined by direct insertion at 70 eV with a VG70 spectrometer. Merck silica gel (Kieselgel 60 / 230-400 mesh) was used for flash chromatography columns. Elemental analyses were performed on a Perkin-Elmer 240 C elemental analyzer, and the results are within ±0.4% of the theoretical values. Yields refer to purified products an...

example ii

[0170]We built a 10,000 compound database of reported and patented integrase inhibitors, which are in some instances likely to target additional DNA processing enzymes, possibly even more potently than integrase. Using this database, we developed various pharmacophore models followed by toxicity prediction using ADMET Predictor software package (Simulations Plus, Inc., Lancaster, Calif.) and cluster analysis to separate a majority of antiviral compounds from cytotoxics. On the basis of these pharmacophores, we identified the salicylhydrazide class of compounds as potential leads for inclusion in our anticancer drug discovery program. Pursuing development of this class of compounds, we searched our in-house multiconformational database of ˜4.5 million compounds and identified >2,200 compounds that possess common structural features and pharmacophore fragments. We then acquired 950 analogues from commercial sources and subjected them to 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazo...

example iii

[0196]

TABLE 750% Cytotoxic concentration (IC50) values of a series of SCs in HEYovarian cancer cellscompdStructureIC50SC2012SC2021SC2036SC2041SC2056SC2061SC2076SC2084SC2098SC2101SC21110SC2121SC21312SC2141SC21512SC2165SC2174SC2184SC2192SC2204SC2214SC2228SC2234SC2244SC2252SC2265SC2276SC2286SC2298SC2303SC2313SC2326SC2335SC2348SC2357SC2362SC2377SC2383SC2393SC2405SC2415SC2425SC2436SC24415SC2451SC2461SC24714SC2482SC2492SC2502SC25115SC25216SC25312SC25417SC25514SC2563SC2572SC2582SC25918SC26010SC26111SC26211SC2635SC2645SC2655SC2667SC26810SC2705SC2716SC2727SC27311SC27411SC27512SC27613SC27714SC27813SC2796SC2806

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Abstract

Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating cell growth, cell cycle, apoptosis, or gene expression.

Description

RELATED APPLICATIONS[0001]The present application is a continuation-in-part of pending prior U.S. patent application Ser. No. 11 / 027,465 filed on Dec. 29, 2004. The present application also claims priority to U.S. Provisional Application Ser. No. 60 / 624,253 filed on Nov. 1, 2004. The contents of U.S. patent application Ser. No. 11 / 027,465 and U.S. Provisional Application Ser. No. 60 / 624,253 are incorporated herein by reference.FIELD OF THE INVENTION[0002]The present invention relates to therapeutic compounds for treatment of cancer and disorders associated with angiogenesis function. More specifically, the invention relates to novel compounds and their uses in treating cancer such as leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer, as well as disorders associated with angiogenesis function such as age-related macular degeneration, macular dystrophy, and diabetes.BACKGROUND OF THE INVENTION[000...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/4985C07D487/04C07D471/14C07D401/14C07D403/14A61K31/4439A61K31/497A61P35/00A61P35/02C12N5/00
CPCC07D487/04C07D471/14A61P35/00A61P35/02A61P35/04
Inventor NEAMATI, NOURI
Owner UNIV OF SOUTHERN CALIFORNIA
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