Cellular accumulation of phosphonate analogs of hiv protease inhibitor compounds
First Claim
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1. An HIV protease inhibitor compound comprising a phosphonate group.
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Abstract
Phosphonate substituted compounds with HIV protease inhibitory properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit 5 HIV protease activity and/or are useful therapeutically for the treatment of AIDS and other antiviral infections, as well as in assays for the detection of HIV protease.
15 Citations
200 Claims
- 1. An HIV protease inhibitor compound comprising a phosphonate group.
- 92. A compound of the formula MBF.
- 123. A compound selected from the Formulas:
- 138. In an HIV protease inhibitor, the improvement comprising a substituent having a phosphonate or phosphonate prodrug.
- 152. In an HIV protease inhibitor not containing a phosphonate or phosphonate prodrug, the improvement comprising a substituent having a phosphonate or phosphonate prodrug.
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166. An MBF compound of Table 100.
- 167. A compound described herein.
- 169. A method of making a compound described herein.
- 171. The use of a compound described here for treatment of HIV in humans.
- 173. The use of a compound described here in the manufacture of a medicament.
- 175. An HIV protease inhibitor compound capable of accumulating in human PBMCs.
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185. Use of a compound of the invention for the treatment of HIV infection.
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186. Use of a compound of the invention in the manufacture of a medicament.
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187. Use of a compound of the invention in the manufacture of a medicament for the treatment of disorders affecting white blood cells.
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188. Method of treating a disorder affecting white blood cells, comprising:
administering a compound of the invention to a patient in need of white-blood-cell targeting.
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189. Method of targeting a compound to white blood cells, comprising:
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selecting a compound having a desired pharmaceutical activity and having a first structure;
modifying said first structure by replacing one or more atom of said first structure with an organic substituent comprising a phosphonate group or incipient phosphonate group to provide a compound having a second structure.
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190. A method of manufacturing a non-nucleoside compound having both selectivity for white blood cells and a desired pharmaceutical activity, comprising:
- chemically synthesizing a first molecule having a first structure containing a phosphonate or incipient phosphonate group, wherein said first structure differs from a second structure of a compound known to have said desired pharmaceutical activity by having at least one hydrogen atom of said second structure replaced by an organic substituent comprising a phosphonate group or incipient phosphonate group.
- View Dependent Claims (191, 192)
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193. Method of accumulating an HIV protease inhibitor inside a white blood cell, comprising:
administering to a sample a composition comprising a compound of the invention. - View Dependent Claims (194, 195)
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196. Method of increasing half-life of a non-nucleoside compound having anti-retroviral activity, comprising:
replacing at least one hydrogen atom or organic radical of said compound by an organic substituent comprising a phosphonate group or incipient phosphonate.
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197. Method of designing a drug having specificity for white blood cells for synthesis, comprising,
obtaining a first list of first compounds having a desired activity; -
creating a second list of second compounds, each of said second compounds having a structure in which at least one hydrogen atom or organic radical of a compound of said first list has been replaced by an organic substituent comprising a phosphonate group or incipient phosphonate group; and
selecting a synthetic pathway capable of producing some or all of said second compounds from available starting materials, thereby providing a third list of compounds and associated synthetic techniques. - View Dependent Claims (198, 199)
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200. Method for producing a pharmaceutical composition having specificity for white blood cells, comprising:
admixing a therapeutically effective amount of a compound of the invention with a pharmaceutically acceptable carrier.
Specification