Rapamycin analogs and uses thereof

Novel rapamycin analogs with C-7 modifications selectively inhibit mTORC1, addressing the limitations of existing therapies by enhancing mTORC1 inhibition with minimal impact on mTORC2, thereby improving therapeutic outcomes and reducing side effects.

JP7727700B2Active Publication Date: 2025-08-21JANSSEN PHARMA NV
View PDF 10 Cites 0 Cited by

Patent Information

Application Number
JP2023189414
Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Priority Date
2018-06-15
Filing Date
2023-11-06
Publication Date
2025-08-21
Estimated Expiration
2039-06-17

AI Technical Summary

Technical Problem

Existing rapamycin-based therapies fail to selectively inhibit mTORC1 without affecting mTORC2, leading to undesirable side effects and metabolic dysregulation.

Method used

Development of novel rapamycin analogs with specific modifications at the C-7 position that selectively inhibit mTORC1 over extended periods without affecting mTORC2, improving solubility and pharmacokinetics.

Benefits of technology

These analogs effectively inhibit mTORC1 while sparing mTORC2, offering potential therapeutic benefits with reduced side effects and improved metabolic regulation.

✦ Generated by Eureka AI based on patent content.

Smart Images

  • Figure 0007727700000356
    Figure 0007727700000356
  • Figure 0007727700000357
    Figure 0007727700000357
  • Figure 0007727700000358
    Figure 0007727700000358
Patent Text Reader

Abstract

To provide a compound useful for modulating mTORC1 activity.SOLUTION: A novel rapamycin analog is provided which is represented by, for example, the following formula (II). Unlike rapamycin and everolimus, a compound of the invention does not inhibit pAKT for a relatively long period of time (for example, 24 hours and 48 hours). The compound of the invention also shows improved solubility and improved pharmacokinetics than rapamycin.SELECTED DRAWING: None
Need to check novelty before this filing date? Find Prior Art

Citation Information

Patent Citations

  • Rapamycin derivative

    JP1995509246A

  • Semisynthetic Analog Immunomodulators of Rapamycin (Macrolides)

    JP1997505299A

  • Rapamycin Derivatives Useful as Immunosuppressants

    JP1997506604A

  • Rapamycin derivative

    JP1998500661A

  • Materials and methods for treating or preventing pathogenic fungal infections

    JP2002514165A