Gina Chiayi Chu

US Patent:

20210046048, Feb 18, 2021

Filed:

Jul 10, 2020

Appl. No.:

16/926033

Inventors:

- San Jose CA, US
Gina C.Y. Chu - San Diego CA, US
Yi Zhang - Los Angeles CA, US

Assignee:

Da Zen Theranostics, Inc. - San Jose CA

International Classification:

A61K 31/4045
A61K 31/337
A61K 31/58
A61K 31/4166
A61K 47/54
A61P 35/00

Abstract:

The present invention generally relates to artemisinin/dihydroartemisinin (DHA) derivatives, and their use for therapy, in particular cancer therapy. These tumor-homing artemisinin derivatives (THAD) comprise three moieties: an artemisinin/DHA or a derivative thereof, a heptamethine carbocyanine dye (HMCD) residue, and a linker that conjugates the HMCD dye residue to the artemisinin residue. The THAD include compounds wherein the linker is linked to one or two DHA residue(s) via one or more ether bonds, and wherein the linker is linked to two DHA residues via two bonds independently selected from ester, carbamate and thiocarbamate. The THAD of the invention provide improved growth inhibition of cancer cells. The present invention also relates to improved methods of cancer therapy wherein a THAD is administered to a cancer patient. In embodiments, one or more THAD may be co-administered in a coordinated administration schedule. Advantages of the THAD and their use include, among others, improved dose-response and/or efficacy. The invention also relates to new dyes, their drug conjugates, and processes of making them.

US Patent:

20210008217, Jan 14, 2021

Filed:

Jul 10, 2020

Appl. No.:

16/925582

Inventors:

- San Jose CA, US
Gina C.Y. Chu - San Diego CA, US
Yi Zhang - Los Angeles CA, US

Assignee:

Da Zen Theranostics, Inc. - San Jose CA

International Classification:

A61K 47/54
A61K 31/351
A61P 35/04

Abstract:

The present invention generally relates to tumor homing statin derivatives (THSD) and their use for therapy, in particular cancer therapy. These THSD comprise three moieties: a statin moiety which comprises a dihydroxyheptanoic acid unit (DHHA) fixated by linkage into its open chain form, a heptamethine carbocyanine dye (HMCD) moiety, and a linker that conjugates the DHHA of the statin to the dye moiety. The linker is linked to the DHHA via an ester bond (ester-linked statin derivative or ELSD), or via an amide bond (amide-linked statin derivative or ALSD). Thus linked to the DHHA, the linker provides a relatively stable link either for essentially no hydrolysis/statin release after administration, or preferably for very slow hydrolysis and statin release, as is the case for the ELSD. Embodiments include methods to provide the desired THSD, in particular the ELSD, with the DHHA in its open chain form. The invention also relates to methods wherein one or more ELSD is administered to a patient in a therapeutically effective amount, and methods wherein an ELSD and an ALSD are co-administered in a coordinated administration schedule. Advantages of the THSD and their use include, among others, improved efficacy and dose-response, and decreased statin-associated side effects.

US Patent:

20190269783, Sep 5, 2019

Filed:

Oct 21, 2017

Appl. No.:

16/343645

Inventors:

- Los Angeles CA, US
- Beverly Hills CA, US
Stefan Mrdenovic - Osijek, HR
Gina Chi-Yi Chu - Los Angeles CA, US
Ruoxiang Wang - Los Angeles CA, US
Qinghua Zhou - Chengdu (Sichuan province), CN
Jian Zhang - Ann Arbor MI, US
Leland W. K. Chung - Beverly Hills CA, US

International Classification:

A61K 47/54
A61K 31/366
A61K 33/243
A61K 31/5377
A61K 31/519
A61K 31/357
A61K 31/65
A61P 35/00
A61P 35/04

Abstract:

The present invention generally relates to sensitizer compounds and their use in combination with Tyrosine Kinase Inhibitors (TKIs) for sensitizing tumor, cancer or pre-cancerous cells to TKI treatment. In particular, the present invention relates to administration regimes that combine TKIs such as Gefitinib or Icotinib with TKI-sensitizing DZ1 esters and amides conjugated to statin or platin-based drugs, or to Artemisinin, including, without limitation: DZ1-Simvastatin amide, DZ1-Simvastatin ester, DZ1-Cisplatin ester, and DZ1-Cisplatin amide, DZ1-Artemisinin ester, and DZ1-Artemisinin amide. Furthermore, the present invention relates to improved TKI treatment of cancers by sensitizing tumor, cancer or pre-cancerous cells, in particular cancers that develop TKI resistance, including e.g. lung cancer and pancreatic cancer.

US Patent:

20190269801, Sep 5, 2019

Filed:

Oct 21, 2017

Appl. No.:

16/343732

Inventors:

- Los Angeles CA, US
Stefan Mrdenovic - Osijek, HR
Yi Zhang - Los Angeles CA, US
Gina Chi-Yi Chu - Los Angeles CA, US
Ruoxiang Wang - Los Angeles CA, US
Frank N. Chang - Dresher PA, US
George Paul Tuszynski - Pittsgrove NJ, US

Assignee:

CEDARS-SINAI MEDICAL CENTER - Los Angeles CA

International Classification:

A61K 49/00
A61P 35/00
A61K 31/22
A61K 31/282
A61K 31/337
A61K 31/366
A61K 31/4045
A61K 31/47
A61K 31/505
A61K 31/555
A61K 31/704
A61K 33/243
A61K 31/7068
A61K 47/52
A61K 47/55

Abstract:

This application relates to dye-therapeutic moiety conjugates for imaging, targeting, and treating cancerous cells and/or tumors.

US Patent:

20190262312, Aug 29, 2019

Filed:

Oct 21, 2017

Appl. No.:

16/343697

Inventors:

- Los Angeles CA, US
- Beverly Hills CA, US
Stefan Mrdenovic - Osijek, HR
Gina Chi-Yi Chu - Los Angeles CA, US
Ruoxiang Wang - Los Angeles CA, US
Qinghua Zhou - Chengdu (Sichuan province), CN
Jian Zhang - Ann Arbor MI, US
Leland W. K. Chung - Beverly Hills CA, US

Assignee:

CEDARS-SINAI MEDICAL CENTER - Los Angeles CA
DA ZEN THERANOSTICS, INC. - Beverly Hills CA

International Classification:

A61K 31/404
A61K 31/282
A61P 35/00
A61K 31/366
A61K 31/513
A61K 31/351
A61K 31/337
A61K 31/47
A61K 31/22

Abstract:

The present invention generally relates to sensitizer compounds and their use to sensitize cancer and/or pre-cancerous cells of certain cancers to treatment with certain resistance-prone therapeutics used in cancer therapy. In embodiments, the conjugates of particular esters or amides of Near Infrared Dyes, are used as sensitizers to avoid or overcome therapeutic resistance once formed. In embodiments, the sensitizers include conjugates with Cisplatin, Simvastatin, Artemisinin, platin-based compounds or statins. In embodiments, the resistance prone cancer therapeutics include cisplatin, gemcitabine, doxorubicin, paclitaxel, docetaxel, and platin-based compounds. These may be administered in combination with the sensitizer, or the sensitizer itself may comprise an therapeutic-derived moiety conjugated to the sensitizer, for example as is the case for dye-CIS conjugated sensitizers. Alternatively, the sensitizer may be co-administered with one or more therapeutic. Embodiments of the invention may advantageously be used in cancers that have a tendency to develop resistance to such cancer therapeutics and/or to form metastases, including e.g. lung, pancreatic, prostate, testicular, ovarian, cervical, bladder, breast, head and neck, esophageal, and stomach, cancers, germ cell tumors, lymphomas and other cancers.