N-substituted 4-aminoquinazoline derivatives and methods of use

US10273229B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-10273229-B2
Application numberUS-201515504120-A
CountryUS
Kind codeB2
Filing dateAug 27, 2015
Priority dateAug 28, 2014
Publication dateApr 30, 2019
Grant dateApr 30, 2019

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  1. Title

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  2. Abstract

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  3. Assignees and inventors

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  4. Key dates

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  5. First independent claim

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  6. CPC / IPC classifications

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  7. Citations and related patents

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Abstract

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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.

First claim

Opening claim text (preview).

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.

Assignees

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Classifications

  • Heterorings having nitrogen atoms as the only ring heteroatoms · CPC title

  • cell-free systems · CPC title

  • Phosphotransferases in general · CPC title

  • Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A) · CPC title

  • Oxidoreductases acting on paired donors, with incorporation or reduction of molecular oxygen (1.14) · CPC title

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Frequently asked questions

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What does patent US10273229B2 cover?
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.
Who is the assignee on this patent?
Codexis Inc
What technology area does this patent fall under?
Primary CPC classification C07D405/04. Mapped technology areas include Chemistry & Metallurgy.
When was this patent published?
Publication date Tue Apr 30 2019 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).