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Conjugated aromatic compounds for diagnosis and therapy

A compound, aryl technology, applied in the field of diagnostic and therapeutic conjugated aromatic compounds, which can solve problems such as difficulty in utilization

Inactive Publication Date: 2008-09-10
德克－泰克公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, exploiting this interrelationship has been difficult and there remains a need to more effectively couple the immune system to external regulatory sources of electromagnetic radiation

Method used

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  • Conjugated aromatic compounds for diagnosis and therapy
  • Conjugated aromatic compounds for diagnosis and therapy
  • Conjugated aromatic compounds for diagnosis and therapy

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0149] Phenylhydrazone resonance modulation

[0150] This example reveals particularly suitable conjugated aromatic compounds with modulatory and sensory agent functions. Some of these compounds include polyaryl mononitro or dinitrophenylhydrazones such as

[0151]

[0152] where R 1 hydrogen, hydroxy, 2- or 4-hydroxyphenyl, acetate, phosphate, azido, nitrile, amino, dimethylamino, sulfate, methanesulfonate, phosphoric acid, nitroso, succinic acid group or other water-soluble electrophilic groups capable of hydrogen bonding; R 2 for C 6 h 5 、C 6 h 4 OH, C 6 h 4 N 3 、C 6 h 4 CN, 4-HO-C 6 h 4 -C 6 h 4 、C 6 h 4 OPO 2 OH, C 6 h 4 OSO 2 H, C 6 h 4 NH 2 、C 6 h 4 NHMe 2 、C 6 h 4 OSO 2 Me, C 6 h 4 OCO(CH 2 ) x CO 2 H or C 6 h 5 Cl; and Ar is C 6 h 3 -2, 4 (NO 2 ) 2 、C 6 h 4 -4(NO 2 ), C 6 h 4 -3(NO 2 ) or C 6 h 3 -2, 4 (NO 2 ) 2 .

[0153] like image 3 As shown, these chemical structures are able to resonate between multi-dipole...

example 2

[0160] Antitumor and immunomodulatory properties of 4,4′-dihydroxybenzophenone-2,4-dinitrophenylhydrazone (A-007)

[0161] This example demonstrates that said compounds, including 4,4'-dihydroxybenzophenone-2,4-dinitrophenylhydrazone, have significant anticancer activity in an anticancer assay (IND 47,470). Specifically, among 53 people treated with topical A-007 (in the form of a 0.25% gel), a 37% objective response rate was observed, with 10 complete responses.

[0162] Table 1. Response of Skin Metastases to A-007 0.25% Gel Topically Applied Twice Daily to Cancerous Lesions

[0163] cancer

#

Application amount (g)

M / F#

reaction

duration

(week)

toxicity

[0164] breast cancer

27

0.01-2.43

30F

5 cases of CR, 7 cases of PR, 6 cases

case stable

6 weeks - 14.5

moon

7 cases of skin toxicity (mild

Spend)

melanoma

5

0.0...

example 3

[0171] Effects on the immune system

[0172] The lymphatic system includes lymphatic vessels that communicate with other structures and organs containing lymphoid tissue in the characteristic reticular form of connective tissue. Lymphatic vessels include lymphatic capillaries, which converge into larger lymphatic vessels that are similar in structure to veins, but have thinner walls and more valves. Lymph nodes are distributed throughout the body, with the highest concentration in the face and neck, armpits, chest, intestines, groin, elbows and knees. Superficial lymphatic vessels in the skin generally accompany veins, while deep lymphatic vessels generally accompany arteries. These lymphatic vessels network the lymph fluid throughout the body and are also an important distributional aspect of the immune system that acts to monitor and defend against foreign cells such as microbes and cancer cells.

[0173] The lymphatic system contains several types of lymphocytes. Some of...

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Abstract

Disclosed herein are compounds, compositions and methods for using such compounds and compositions in the treatment of hyperproliferative conditions, including precancerous and cancerous conditions. In one embodiment, the compounds include resonance modulating compounds that can be used in the method as a coupling agent that is capable of interacting with the immune system to monitor or stimulate immune function. Such resonance modulators have inherent electromagnetic properties that attract immune cells to a target area to which the resonance modulating agent has been applied. Electromagnetic properties (such as a voltage amplitude) of the target region are altered in the presence of the resonance modulator, and serve as an indicator of immune function. An external stimulus (such as an applied electromagnetic field) can also be applied to the resonance modulator to enhance its immune stimulating and attractant properties. Particular examples of resonance modulators are disclosed, and these substances generally possess resonating intramolecular dipole moments that are capable of electrostatic interaction with biological environments. In certain examples the compounds aggregate at sites of therapeutic action to enhance their therapeutic activity. In other examples the compounds stimulate platelet production.

Description

[0001] Statement of Government Support [0002] The United States Government may have certain rights in this invention. Portions of the work related to the development of the present invention were performed under Grant No. R43CA89772-01 from the National Cancer Institute. [0003] Cross References to Related Applications [0004] This application claims the benefit of previously filed US Provisional Application Serial No. 60 / 678,089, filed May 4, 2005, which is hereby incorporated by reference in its entirety. technical field [0005] The present invention relates to methods of monitoring and altering immune function, eg, during the diagnosis and / or treatment of infectious and neoplastic diseases. The present invention also discloses methods of treating lesions such as hyperproliferative lesions associated with infectious pathogens and / or inflammation. Background technique [0006] Immunotherapy involves modulating an individual's immune response to improve the innate...

Claims

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Application Information

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IPC IPC(8): A61K31/15A61K41/00C07C251/80C07C251/82
CPCA61P7/04A61P17/06A61P31/12A61P31/18A61P35/00A61P35/04A61P37/04C07C251/80C07C251/82A61K31/15
Inventor 李·罗伊·摩根
Owner 德克－泰克公司
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