Methods and compositions of targeted drug development

A space-oriented, drug-active technology, applied in the field of targeted drug development and composition, can solve problems such as intensive technical resources

Inactive Publication Date: 2009-04-22
约瑟夫・P・埃里科
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] By the same token, the drawbacks of the combination of high-throughput screening and combinatorial chemistry methods are undoubtedly firstly the resource-intensive nature of the technology, and secondly the fact that legal entities drive most of the development away from the development of novel drugs to iteratively improve the treatment of the same condition

Method used

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  • Methods and compositions of targeted drug development
  • Methods and compositions of targeted drug development
  • Methods and compositions of targeted drug development

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0267] Example 1: Vascular Endothelial Growth Factor

[0268] The following examples involve the production of one or more pharmacophores based at least in part on the antibodies provided against the target molecule (in this example, human vascular endothelial cell growth factor (VEGF-A) (SEQ ID NO: 2)). In short, human vascular endothelial cell growth factor (VEGF-A) is presented to many animals (for example, a group of mice with no genetic similarity). Vaccination and repeated presentation of VEGF-A lead to the appearance of various IgG antibodies (polyclonal high affinity antibodies) against this molecule in animals. These antibodies vary from animal to animal, because each has a different genetic potential for antibody production (different combinations of possible CDRs). The variability in antibodies causes them to bind to VEGF-A molecules on different surface areas of the molecule. It is expected that at least one of the antibodies binds to the active region of the VEGF-A mo...

Embodiment 2

[0293] Example 2: Influenza glycoprotein

[0294] Another desirable target is a protein associated with viral infection, such as hemagglutinin. Hemagglutinin is an antigen glycoprotein found on the surface of influenza virus, which is responsible for the binding of the virus to infected cells.

[0295] Despite active advocacy campaigns initiated by vaccine manufacturers, medical associations, and government agencies dedicated to public health, millions of people in the United States (some estimates range as high as 10% to 20% of U.S. residents) are infected with influenza each year . Most people with flu will recover within 1-2 weeks, but others will develop life-threatening complications (such as pneumonia). Although many people generally think that influenza is nothing more than a severe cold, influenza can be fatal, especially for weak, elderly or chronically ill individuals. In the United States, an average of about 36,000 people die from influenza each year, and 114,000 peopl...

Embodiment 3

[0312] Example 3: Angiopoietin

[0313] Angiogenesis (the budding of new capillaries from pre-existing vascular structures) is a key aspect of fetal and child development, as their circulatory system grows up during growth. In adults, angiogenesis is required for normal tissue repair and for remodeling of female reproductive organs (ovulation and placental development). However, certain pathological conditions such as tumor growth and diabetic retinopathy also require angiogenesis. A known factor involved in angiogenesis is angiopoietin, which is a single polypeptide chain containing 123 amino acids.

[0314] Angiopoietin is one of the common cytokines, which is used by cancer to help the rapid growth of cancer. In this case, tumor cells secrete angiogenin to recruit greater blood flow to the tumor. Therefore, the discovery of drugs that can inhibit the production or activity of angiogenin will be of great significance.

[0315] Chavali et al. have disclosed the results of their c...

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Abstract

The present invention is directed to methods for developing one or more drugs for one or more targeted therapies and compositions derived therefrom. In accordance with one aspect of the present invention, combinatorial chemistry techniques for use with high throughput screening techniques for identifying small molecule affinity and / or activity interactions are avoided by instead utilizing the natural mechanisms of antigen response to effect a massively parallel screening of naturally occurring molecules against an antigen. Other aspects of the invention provide compositions derived thereform as well as therapeutic methods of use for the compounds.

Description

[0001] Cross-references to related applications [0002] This application claims priority to U.S. Provisional Application No. 60 / 761,123 filed on January 23, 2006, which is incorporated herein by reference in its entirety. [0003] Introduce the materials submitted on the compact disc for reference [0004] The sequence listing, which is part of the disclosure of the present invention, includes a computer-readable format and a written sequence listing, which contains the nucleotide and / or amino acid sequence of the present invention. The sequence listing information recorded in computer-readable form is the same as that recorded in the written sequence listing. The full text of the subject of the sequence listing is incorporated herein by reference. Technical field [0005] The present invention relates generally to the development of new chemical entities for disease treatment, and more specifically to methods of identifying lead molecules for use in quasi-reasonable drug design. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/33G16B15/30G16B20/30
CPCC07K2318/20A61K31/00G06F19/16C07K2317/565G06F19/706C07K16/00G06F19/18C07K2316/96C07K2317/76G16B15/00G16B20/00G16C20/50A61P43/00Y02A50/30G16B20/30G16B15/30A61K39/395
Inventor 约瑟夫·P·埃里科B·B·穆加格I·J·特奇
Owner 约瑟夫・P・埃里科
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