Sequoia Pharmaceuticals, Inc.

Dehui Duan

Michael Eissenstat

Ji-Hye Kang

John W Erickson

Sergi Gulnik

Jihye Kang

Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.

Compositions and methods for inhibiting cytochrome P450

Methods of inhibiting cytochrome P450 2D6 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450 2D6. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 2D6 enzymes.

Compositions and methods for inhibiting cytochrome P450 2D6

Diamide inhibitors of cytochrome P450

Benzofuran-containing amino acid compounds are provided that are potent inhibitors of cytochrome P450 (CYP) enzymes. The compounds have the general structure where at least one of R, R, R, R, R, and Ris &#x2014;S(O)&#x2014;(CH)-(benzofuranyl), &#x2014;(CH)&#x2014;N(R)(&#x2014;SO-benzofuranyl), &#x2014;C(O)&#x2014;(CH)-(benzofuranyl), &#x2014;(CH)&#x2014;N(R)(C(&#x2550;O)-(benzofuranyl), or C-Calkylene-(benzofuranyl). Pharmaceutical compositions containing the inhibitors are provided and these compositions can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.

Benzofuran-containing amino acid inhibitors of cytochrome P450

Methods for inhibiting drug degradation

Methods of inhibiting cytochrome P450 2D6 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450 2D6. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 2D6 enzymes. The compositions comprise 5-substituted benzofuran compounds having the formula I: 

5-substituted benzofurans as inhibitors of cytochrome P450 2D6

Compositions and methods of treating viral infections are provided. More particularly, compositions including a combination of protease inhibitors and cytochrome p450 enzyme inhibitors are provided. Methods of using the compositions for treatment of diseases or disorders caused by a virus such as HIV infections are also provided.

Growing community of inventors

Frederick, MD, United States of America

Dehui Duan