Non nucleoside reverse transcriptase inhibitors
First Claim
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1. A non-nucleoside reverse transcriptase inhibitor compound comprising a phosphonate group.
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Abstract
Phosphorus-substituted imidazole compounds with anti-HIV properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit reverse transcriptase activity and are useful therapeutically for the inhibition of such enzymes, as well as in assays for the detection of such enzymes.
48 Citations
236 Claims
- 1. A non-nucleoside reverse transcriptase inhibitor compound comprising a phosphonate group.
- 140. A compound of the formula:
- 148. A compound of the formula:
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169. A compound of the formula MBF.
- 170. In a non-nucleotide reverse transcriptase inhibitor, the improvement comprising a substituent having a phosphonate or phosphonate prodrug.
- 186. In a non-nucleotide reverse transcriptase inhibitor not containing a phosphonate or phosphonate prodrug, the improvement comprising a substituent having a phosphonate or phosphonate prodrug.
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202. An MBF compound of Table 100.
- 203. A compound described herein.
- 205. A method of making a compound described herein.
- 207. The use of a compound described here for treatment of HIV in humans.
- 209. The use of a compound described here in the manufacture of a medicament.
- 211. An non-nucleotide reverse transcriptase inhibitor compound capable of accumulating in human PBMCs.
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221. Use of a compound of the invention for the treatment of HIV infection.
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222. Use of a compound of the invention in the manufacture of a medicament.
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223. 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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224. 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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225. 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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226. 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 precursor 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 (227, 228)
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229. Method of accumulating an non-nucleotide reverse transcriptase inhibitor inside a white blood cell, comprising:
administering to a sample a composition comprising a compound of the invention. - View Dependent Claims (230, 231)
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232. 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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233. Method of designing a drug having specificity for white blood cells for synthesis, comprising:
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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 (234, 235)
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236. 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