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Novel compounds for treatment of cancer and disorders associated with angiogenesis function

A compound, alkyl technology, applied in the direction of active ingredients, applications, biocides, etc. of heterocyclic compounds, which can solve problems such as troublesome and time-consuming

Inactive Publication Date: 2007-12-19
UNIV OF SOUTHERN CALIFORNIA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Traditional pharmacokinetic studies, although necessary, are cumbersome and time-consuming, requiring large numbers 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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preparation example Construction

[0142] The double derivative SC147 was prepared by the direct reaction of hydrazine monohydrate with two molar equivalents of ethyl pyrrolo[1,2-a]quinoline-4-carboxylate 15 as described in Nagarajan et al. ((1972) Indian J.Chem.10:344-350) (Scheme 2) and then obtained sequentially.

[0143] Scenario 2

[0144]

[0145] In EDC / DMAP followed by TFA and anisole in the presence of Base) propionic acid, Boc-3-amino-3-(4-fluorophenyl)propionic acid, Boc-3-amino-3-(4-cyanophenyl)propionic acid, Boc-3-amino-3-( Reaction of 4-methoxyphenyl)propanoic acid with Boc-3-amino-3-(4-trifluoromethylphenyl)propanoic acid can give SC160, SC161, SC162, SC163, SC164 and SC165 (Scheme 3).

[0146]

[0147] In the presence of EDC / DMAP followed by TFA and anisole, SC166, SC167, SC168, SC169, SC170, SC171 and SC172 can be obtained by reacting 14a with the corresponding acids (15a-g) shown in Scheme 4, respectively (Scheme 4 ).

[0148]

[0149] SC173 can be obtained by reacting 14a with 2...

Embodiment I

[0209] Chemical

[0210] All reactions were performed under nitrogen atmosphere. Through silica gel plate TLC (Merck 60, F 254 , 0.2mm) to monitor the progress of the reaction. with MgSO 4 The organic solution was dried; evaporation meant removal of solvent on a rotary evaporator under reduced pressure. Melting points were determined using a Gallenkamp apparatus and were not corrected. IR spectra were recorded from thin films on a Perkin-Elmer 398 and FT 1600 spectrophotometer. Recorded on a Brüker 300-MHz spectrometer using TMS as internal standard 1 H NMR spectra; chemical shifts are expressed in [delta] values ​​(ppm) and coupling constants in (J) Hz. Mass spectrometric data were determined by forward insertion at 70 eV using a VG70 spectrometer. Merck silica gel (Kieselgel 60 / 230-400 mesh) was used as a flash chromatography column. Elemental analysis was performed on a Perkin-Elmer 240C elemental analyzer, and the results were within ±0.4% of theoretical values. Y...

Embodiment II

[0275] We created a database of 10,000 reported and patented integrase inhibitor compounds, which in some cases may target additional DNA processing enzymes even more potent than integrase. Using this database, we developed various pharmacophore models, followed by toxicity prediction using the ADMET Predictor software package (Simulations Plus, Inc., Lancaster, CA) and cluster analysis to group most antiviral compounds with cytotoxic compounds. separate. Based on these pharmacophore models, the salicylhydrazides we identified as possible lead compounds were included in our anticancer drug discovery program. To continue developing this class of compounds, we searched our internal multiconformation database of ~4500,000 compounds and identified >2,200 compounds that share common structural features and pharmacophore fragments. We then obtained 950 analogs from commercial sources and preliminarily screened them by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide-cyt...

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Abstract

Novel compounds for the treatment of cancer and diseases associated with angiogenic function. Also disclosed are methods of preparing compounds, pharmaceutical compositions containing these compounds, and packaged products, using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, kidney cancer and prostate cancer), as well as methods for diseases linked to angiogenic function (such as age-related macular degeneration, macular dystrophy, and diabetes), methods for monitoring therapy, methods for constructing gene expression profiles, and methods for modulating cell growth, cell Methods of cycle, apoptosis or gene expression.

Description

[0001] related application [0002] This application is a continuation-in-part of prior US Patent Application Serial No. 11 / 027,465, filed December 29,2004. This application also claims priority to US Provisional Application Serial No. 60 / 624,253, filed November 1, 2004. The contents of US Patent Application Serial No. 11 / 027,465 and US Provisional Application Serial No. 60 / 624,253 are incorporated herein by reference. field of invention [0003] The present invention relates to therapeutic compounds useful in the treatment of cancer and diseases associated with angiogenic function. More particularly, the present invention relates to novel compounds and their use in the treatment of cancers such as leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer and prostate cancer, and their function in relation to angiogenesis. associated diseases such as age-related macular degeneration, macular dystrophy and diabetes. ...

Claims

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Application Information

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IPC IPC(8): A01N43/58A01N43/60A01N43/54A01N43/42A01N43/30A01N43/56A01N43/38A01N43/16A01N37/18A61K31/50A61K31/495A61K31/517A61K31/505A61K31/47A61K31/425A61K31/415A61K31/40A61K31/35A61K31/16C07D239/00C07D239/70C07D471/00C07D487/00C07D491/00C07D241/36C07D403/00C07D413/00C07D311/04C07D311/74C07D241/00C07D249/00
Inventor N·尼马蒂A·加鲁法洛
Owner UNIV OF SOUTHERN CALIFORNIA
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