Heterocyclic modulators of lipid synthesis
US-2024400552-A1 · Dec 5, 2024 · US
US10273229B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10273229-B2 |
| Application number | US-201515504120-A |
| Country | US |
| Kind code | B2 |
| Filing date | Aug 27, 2015 |
| Priority date | Aug 28, 2014 |
| Publication date | Apr 30, 2019 |
| Grant date | Apr 30, 2019 |
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The present invention provides kinase inhibitor analogs with improved properties, such as improved efficacy, pharmacokinetics, safety, and specificity. In some embodiments, the present invention provides lapatinib analogs that provide therapeutic benefits.
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We claim: 1. A method for producing an improved kinase inhibitor analog comprising exposing a starting kinase inhibitor to a cytochrome P450 monooxygenase to produce an analog, purifying said analog, and determining the kinase inhibition activity of said analog, wherein the kinase inhibition activity of said analog is determined against a kinase comprising EGFR, ErbB2, ErbB4, or Syk. 2. The method of claim 1 , wherein said kinase inhibitor analog comprises an introduced hydroxyl moiety. 3. The method of claim 1 , wherein said kinase inhibitor analog is further modified to provide additional kinase inhibitors. 4. The method of claim 2 , wherein the site of hydroxylation is further modified chemically to provide new kinase inhibitors. 5. The method of claim 1 , wherein the starting kinase inhibitor is lapatinib.
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