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Phosphonate compounds having immuno-modulatory activity

A phosphonate, compound technology, applied in the field of compounds that inhibit at least one kinase, can solve the problem of short-lived drugs, undesired systemic distribution, etc.

Inactive Publication Date: 2007-03-21
GILEAD SCI INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, oral administration may result in (a) uptake of the drug across cellular and tissue barriers, such as the blood-brain barrier, epithelial cells, or cell membranes, resulting in undesired systemic distribution, and / or (b) drug uptake in the gastrointestinal tract. short stay

Method used

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  • Phosphonate compounds having immuno-modulatory activity
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  • Phosphonate compounds having immuno-modulatory activity

Examples

Experimental program
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Embodiment approach

[0244] Specific values ​​describing radicals, substituents, and ranges, as with specific embodiments of the invention described herein, are illustrative only; they do not exclude other defined values ​​or values ​​within other defined ranges.

[0245] In a particular embodiment of the invention, A 1 has the following formula:

[0246]

[0247] In another particular embodiment of the invention, A 1 has the following formula:

[0248]

[0249] In another particular embodiment of the invention, A 1 has the following formula:

[0250]

[0251] In another particular embodiment of the invention, A 1 has the following formula:

[0252]

[0253] In another particular embodiment of the invention, A 1 has the following formula:

[0254]

[0255] and W 5a is a carbocyclic or heterocyclic ring, where W 5a independently by 0 or 1 R 2 group substitution. The specific value of M12a is 1.

[0256] In another particular embodiment of the invention, A 1 has the follo...

Embodiment

[0708] Summary of Examples

[0709] A number of exemplary preparations of the compounds of the invention are provided herein, eg, in the Examples below. These methods are intended to illustrate the nature of these preparations and are not intended to limit the scope of applicable methods. Certain compounds of the invention are useful as intermediates in the preparation of other compounds of the invention. For example, the interconversion of various phosphonate compounds of the invention is illustrated below.

[0710] Phosphonate R-link-P(O)(OR 1 ) 2 , R-link-P(O)(OR 1 )(OH)

[0711] and R-link-P(O)(OH) 2 mutual change.

[0712] Schemes 32-38 below describe the general structure R-link-P(O)(OR 1 ) 2 The preparation of the phosphonate, wherein R 1 The groups can be the same or different. R appended to the phosphonate, or its precursor 1 Groups can be changed using defined chemical transformations. Interconversion reactions of ph...

approach 36 Embodiment 2

[0830]

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Abstract

The invention is related to phosphorus substituted kinase inhibitory compounds and conjugates, compositions containing such compounds and conjugates, and therapeutic methods that include the administration of such compounds and conjugates, as well as to processes and intermediates useful for preparing such compounds and conjugates.

Description

[0001] Priority Right of the Invention [0002] Pursuant to 35 U.S.C. §119(e), this application claims the benefit of priority to U.S. Provisional Patent Application Serial No. 60 / 622,962, filed October 26, 2004; and pursuant to 35 U.S.C. §119(e), this application claims Having the benefit of priority of U.S. Provisional Patent Application Serial No. 60 / 531932, filed December 22, 2003; and this application also claims the benefit of U.S. Patent Application Serial No. 10 / 832811 and PCT Application, both filed April 26, 2004 Priority benefit of No. PCT / US2004 / 013062. Each of the above-referenced applications is hereby incorporated by reference in its entirety. field of invention [0003] The present invention generally relates to phosphonate-containing compounds having kinase inhibitory activity, ie, compounds that inhibit at least one kinase. Background of the invention [0004] Improving the delivery of drugs ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/662
Inventor W·J·沃特金斯
Owner GILEAD SCI INC