Conjugates of active pharmaceutical ingredients

Patent metadata

Field	Value
Publication number	US-11559585-B2
Application number	US-201816622722-A
Country	US
Kind code	B2
Filing date	Jun 15, 2018
Priority date	Jun 16, 2017
Publication date	Jan 24, 2023
Grant date	Jan 24, 2023

Abstract

The present inventions provides drug-drug conjugates, drug-porphyrin conjugates, nanoparticles of the conjugates, as well as modified nanoparticles having PEGylated exteriors or encapsulated by red blood cell vesicles. The conjugates, nanoparticles and nanocarriers are useful for treating cancers and other diseases, as well as for imaging diseased tissue or organs.

First claim

What is claimed is:

1. A compound having the structure of:

2. A compound having the structure of:

3. A compound having the structure of:

4. A nanoparticle comprising a plurality of conjugates of claim 3 , wherein the nanoparticle comprises an interior and an exterior.

5. A method of preparing a nanoparticle of claim 4 , comprising forming a reaction mixture comprising a plurality of conjugates of claim 3 under conditions suitable for the plurality of conjugates to self-assemble and form nanoparticles.

6. A method of treating a disease or condition, comprising administering to a subject in need thereof, a therapeutically effective amount of a conjugate of claim 3 , thereby treating the disease or condition.

7. A method of treating a disease or condition via sonodynamic therapy, comprising
administering to a subject in need thereof, a therapeutically effective amount of a conjugate of claim 3 ; and
exposing the subject to a sonic wave, thereby treating the disease via sonodynamic therapy.

8. A method of imaging a tissue or organ, comprising administering to a subject to be imaged, an effective amount of a conjugate of claim 3 ,
such that the conjugate or nanoparticle concentrates in the tissue or organ; and imaging the tissue or organ using a suitable device.

9. A method of detecting a tumor in a subject, comprising
administering to the subject an effective amount of a conjugate of claim 3 ;
exposing the subject to radiation at a first wavelength; and
detecting any emitted radiation from the conjugate or nanoparticle, thereby detecting the tumor.

10. A system comprising a conjugate of claim 3 , and a laser.

11. A nanoparticle comprising a plurality of conjugates of claim 2 , wherein the nanoparticle comprises an interior and an exterior.

12. A method of preparing a nanoparticle of claim 11 , comprising forming a reaction mixture comprising a plurality of conjugates of claim 2 under conditions suitable for the plurality of conjugates to self-assemble and form nanoparticles.

13. A method of treating a disease or condition, comprising administering to a subject in need thereof, a therapeutically effective amount of a conjugate of claim 2 , thereby treating the disease or condition.

14. A method of treating a disease or condition via sonodynamic therapy, comprising
administering to a subject in need thereof, a therapeutically effective amount of a conjugate of claim 2 ; and
exposing the subject to a sonic wave, thereby treating the disease via sonodynamic therapy.

15. A method of imaging a tissue or organ, comprising administering to a subject to be imaged, an effective amount of a conjugate of claim 2 ,
such that the conjugate or nanoparticle concentrates in the tissue or organ; and imaging the tissue or organ using a suitable device.

16. A method of detecting a tumor in a subject, comprising
administering to the subject an effective amount of a conjugate of claim 2 ;
exposing the subject to radiation at a first wavelength; and
detecting any emitted radiation from the conjugate or nanoparticle, thereby detecting the tumor.

17. A system comprising a conjugate of claim 2 , and a laser.

18. A nanoparticle comprising a plurality of conjugates of claim 1 , wherein the nanoparticle comprises an interior and an exterior.

19. A method of preparing a nanoparticle of claim 18 , comprising forming a reaction mixture comprising a plurality of conjugates of claim 1 under conditions suitable for the plurality of conjugates to self-assemble and form nanoparticles.

20. A method of treating a disease or condition, comprising administering to a subject in need thereof, a therapeutically effective amount of a conjugate of claim 1 , thereby treating the disease or condition.

21. A method of treating a disease or condition via sonodynamic therapy, comprising
administering to a subject in need thereof, a therapeutically effective amount of a conjugate of claim 1 ; and
exposing the subject to a sonic wave, thereby treating the disease via sonodynamic therapy.

22. A method of imaging a tissue or organ, comprising administering to a subject to be imaged, an effective amount of a conjugate of claim 1 ,
such that the conjugate or nanoparticle concentrates in the tissue or organ; and imaging the tissue or organ using a suitable device.

23. A method of detecting a tumor in a subject, comprising
administering to the subject an effective amount of a conjugate of claim 1 ;
exposing the subject to radiation at a first wavelength; and
detecting any emitted radiation from the conjugate or nanoparticle, thereby detecting the tumor.

24. A system comprising a conjugate of claim 1 , and a laser.

Assignees

• Univ California

Inventors

• Li Yuanpei
• Xue Xiangdong
• Huang Yee
• Ma Zhao

Classifications

• A61K31/704

  attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin {(digitoxin A61K31/7048)} · CPC title

• G01N23/02

  by transmitting the radiation through the material · CPC title

• A61K31/4965

  Non-condensed pyrazines · CPC title

• A61K41/0033

  Sonodynamic cancer therapy with sonochemically active agents or sonosensitizers, having their cytotoxic effects enhanced through application of ultrasounds (ultrasound therapy per se A61N7/00) · CPC title

• A61K31/475

  having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine (vincamine A61K31/4375) · CPC title