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1. 发明公开

US20240307560A1 HEPTAMETHINE CARBOCYANINE DYE-DOTA CONJUGATES COMPLEXED WITH LUTETIUM-177, YTTRIUM-90, OR GALLIUM-68, AND THEIR USES FOR IMAGE-GUIDED RADIOTHERAPY 审中-公开
公开(公告)号：US20240307560A1
公开(公告)日：2024-09-19
申请号：US18270463
申请日：2021-12-30
申请人： Da Zen Theranostics, Inc.
发明人： Leland W.K. Chung , Ruoxiang Wang , Yi Zhang
IPC分类号： A61K51/04
CPC分类号： A61K51/0446 , A61K51/0406 , A61K51/0497
摘要： Embodiments of the present invention generally relate to conjugates of heptamethine carbocyanine dye (HMCD)-chelator radiometal complexes, radiopharmaceutical formulations comprising such complexes and their use, in particular for internal radiotherapy and/or imaging of cancer. In particular, in embodiments, provided are DZ-1-Lys-DOTA conjugates complexed with Lutetium-177, Yttrium-90 or Gallium-68, or combinations thereof. Some embodiments provide improved radiotherapy with complexes of Lutetium-177 or Yttrium-90. Further embodiments provide improved radioimaging with Gallium-68 complexes, and their use. Yet further embodiments provide improved image-guided therapy by using matched theranostic pairs of such conjugates, wherein for therapy purposes the radiometal is selected from one or more of Lutetium-177, Yttrium-90, each of which for imaging purposes may be paired with Gallium-68, for improved image-guided radiotherapy.

2. 发明申请

US20190262312A1 COMPOUNDS AND METHODS TO SENSITIZE CANCER CELLS TO CISPLATIN 审中-公开
公开(公告)号：US20190262312A1
公开(公告)日：2019-08-29
申请号：US16343697
申请日：2017-10-21
申请人： CEDARS-SINAI MEDICAL CENTER , DA ZEN THERANOSTICS, INC.
发明人： Liyuan Yin , Yi Zhang , Stefan Mrdenovic , Gina Chi-Yi Chu , Ruoxiang Wang , Qinghua Zhou , Jian Zhang , Leland W. K. Chung
IPC分类号： A61K31/404 , A61K31/282 , A61P35/00 , A61K31/366 , A61K31/513 , A61K31/351 , A61K31/337 , A61K31/47 , A61K31/22
摘要： 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.

3. 发明授权

US12121510B2 Compounds and methods to sensitize cancer cells to cisplatin 有权
公开(公告)号：US12121510B2
公开(公告)日：2024-10-22
申请号：US16343697
申请日：2017-10-21
申请人： Cedars-Sinai Medical Center , Da Zen Theranostics, Inc.
发明人： Liyuan Yin , Yi Zhang , Stefan Mrdenovic , Gina Chia Yi Chu , Ruoxiang Wang , Qinghua Zhou , Jian Zhang , Leland W. K. Chung
IPC分类号： A61P35/00 , A61K31/22 , A61K31/282 , A61K31/337 , A61K31/351 , A61K31/357 , A61K31/366 , A61K31/40 , A61K31/404 , A61K31/4045 , A61K31/47 , A61K31/505 , A61K31/513 , A61K31/519 , A61K31/5377 , A61K31/555 , A61K31/65 , A61K31/704 , A61K31/7068 , A61K33/243 , A61K47/52 , A61K47/54 , A61K47/55 , A61K49/00 , A61P35/04 , C07D209/10 , C07D405/14 , C07D493/18 , C09B23/01 , A61K45/06
CPC分类号： A61K31/404 , A61K31/22 , A61K31/282 , A61K31/337 , A61K31/351 , A61K31/357 , A61K31/366 , A61K31/40 , A61K31/4045 , A61K31/47 , A61K31/505 , A61K31/513 , A61K31/519 , A61K31/5377 , A61K31/555 , A61K31/65 , A61K31/704 , A61K31/7068 , A61K33/243 , A61K47/52 , A61K47/545 , A61K47/55 , A61K49/0004 , A61K49/0032 , A61P35/00 , A61P35/04 , C07D209/10 , C07D405/14 , C07D493/18 , C09B23/0016 , C09B23/0066 , A61K45/06 , A61K31/4045 , A61K2300/00 , A61K33/243 , A61K2300/00 , A61K31/366 , A61K2300/00 , A61K31/7068 , A61K2300/00 , A61K31/704 , A61K2300/00 , A61K31/337 , A61K2300/00 , A61K31/40 , A61K2300/00 , A61K31/404 , A61K2300/00 , A61K31/47 , A61K2300/00 , A61K31/22 , A61K2300/00 , A61K31/505 , A61K2300/00 , A61K31/555 , A61K2300/00 , A61K31/282 , A61K2300/00
摘要： 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.

4. 发明申请

US20210046048A1 Artemisinin Derivatives 有权
公开(公告)号：US20210046048A1
公开(公告)日：2021-02-18
申请号：US16926033
申请日：2020-07-10
申请人： Da Zen Theranostics, Inc.
发明人： Leland W.K. Chung , Gina C.Y. Chu , Yi Zhang
IPC分类号： A61K31/4045 , A61K31/337 , A61K31/58 , A61K31/4166 , A61K47/54 , A61P35/00
摘要： 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.

5. 发明公开

US20240261263A1 COMPOUNDS AND METHODS TO SENSITIZE CANCER CELLS TO TYROSINE KINASE INHIBITORS 审中-公开
公开(公告)号：US20240261263A1
公开(公告)日：2024-08-08
申请号：US18530467
申请日：2023-12-06
申请人： Da Zen Theranostics, Inc. , Cedars-Sinai Medical Center
发明人： Liyuan Yin , Yi Zhang , Stefan Mrdenovic , Gina Chi-Yi Chu , Ruoxiang Wang , Qinghua Zhou , Jian Zhang , Leland W.K. Chung
IPC分类号： A61K31/404 , A61K31/22 , A61K31/282 , A61K31/337 , A61K31/351 , A61K31/357 , A61K31/366 , A61K31/40 , A61K31/4045 , A61K31/47 , A61K31/505 , A61K31/513 , A61K31/519 , A61K31/5377 , A61K31/555 , A61K31/65 , A61K31/704 , A61K31/7068 , A61K33/243 , A61K45/06 , A61K47/52 , A61K47/54 , A61K47/55 , A61K49/00 , A61P35/00 , A61P35/04 , C07D209/10 , C07D405/14 , C07D493/18 , C09B23/01
CPC分类号： A61K31/404 , A61K31/22 , A61K31/282 , A61K31/337 , A61K31/351 , A61K31/357 , A61K31/366 , A61K31/40 , A61K31/4045 , A61K31/47 , A61K31/505 , A61K31/513 , A61K31/519 , A61K31/5377 , A61K31/555 , A61K31/65 , A61K31/704 , A61K31/7068 , A61K33/243 , A61K47/52 , A61K47/545 , A61K47/55 , A61K49/0004 , A61K49/0032 , A61P35/00 , A61P35/04 , C07D209/10 , C07D405/14 , C07D493/18 , C09B23/0016 , C09B23/0066 , A61K45/06
摘要： 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.

6. 发明申请

US20220031855A1 Organic Anion Transporting Peptide-Based Cancer Imaging and Therapy 有权
公开(公告)号：US20220031855A1
公开(公告)日：2022-02-03
申请号：US17318802
申请日：2021-05-12
申请人： Da Zen Theranostics, Inc.
发明人： Leland W.K. Chung
IPC分类号： A61K47/54 , C09B23/01 , A61K51/04
摘要： A dye-drug conjugate for preventing, treating, or imaging cancer having the following structure: wherein R1 and R2 are independently selected from the group consisting of —H, alkyl, alkyl-sulphonate, alkylcarboxylic, alkylamino, aryl, —SO3H, —PO3H, —OH, —NH2, and -halogen; wherein Y1 and Y2 is independently selected from the group consisting of alkyl, aryl, aralkyl, alkylsulphonate, alkylcarboxylic, alkylamino, ω-alkylaminium, ω-alkynyl, PEGyl, PEGylcarboxylate, ω-PEGylaminium, ω-acyl-NH, ω-acyl-lysinyl-, ω-acyl-triazole, ω-PEGylcarboxyl-NH—, ω-PEGylcarboxyl-lysinyl, and ω-PEGylcarboxyl-triazole; wherein X is selected from the group consisting of a hydrogen, halogen, CN, Me, NH2, SH and OH; and R3 and R4 are independently a hydrogen, a therapeutic agent, or an imaging moiety, wherein the therapeutic agent is selected from the group consisting of a platinum-based therapeutic agent, a small molecule therapeutic agent, a peptide, a protein, a polymer, an siRNA, a microRNA, and a nanoparticle, wherein the imaging is a radio-isotope selected from the group consisting of F18, I-125, I-124 I-123, I-131, and small molecule labeled with any of these isotopes, or wherein the imaging moiety is a chelator-complexed radioactive isotope, wherein the radioactive isotope is selected from the group consisting of Cu-64, In-111, Tc-99m, Ga-68, Lu-177, Zo-89, Th-227 and Gd-157.

7. 发明授权

US11878000B2 Compounds and methods to sensitize cancer cells to tyrosine kinase inhibitors 有权
公开(公告)号：US11878000B2
公开(公告)日：2024-01-23
申请号：US16343645
申请日：2017-10-21
申请人： Cedars-Sinai Medical Center , Da Zen Theranostics, Inc.
发明人： Liyuan Yin , Yi Zhang , Stefan Mrdenovic , Gina Chia Yi Chu , Ruoxiang Wang , Qinghua Zhou , Jian Zhang , Leland W. K. Chung
IPC分类号： A61K31/395 , A61K31/404 , A61P35/00 , A61K31/22 , A61K31/282 , A61K31/337 , A61K31/351 , A61K31/366 , A61K31/47 , A61K31/513 , A61K47/54 , A61P35/04 , A61K33/243 , A61K31/357 , A61K31/519 , A61K31/5377 , A61K31/65 , A61K47/55 , A61K47/52 , A61K31/4045 , A61K31/505 , A61K31/555 , A61K31/704 , A61K31/7068 , A61K49/00 , C07D493/18 , C07D209/10 , C07D405/14 , A61K31/40 , C09B23/01 , A61K45/06
CPC分类号： A61K31/404 , A61K31/22 , A61K31/282 , A61K31/337 , A61K31/351 , A61K31/357 , A61K31/366 , A61K31/40 , A61K31/4045 , A61K31/47 , A61K31/505 , A61K31/513 , A61K31/519 , A61K31/5377 , A61K31/555 , A61K31/65 , A61K31/704 , A61K31/7068 , A61K33/243 , A61K47/52 , A61K47/545 , A61K47/55 , A61K49/0004 , A61K49/0032 , A61P35/00 , A61P35/04 , C07D209/10 , C07D405/14 , C07D493/18 , C09B23/0016 , C09B23/0066 , A61K45/06 , A61K31/4045 , A61K2300/00 , A61K33/243 , A61K2300/00 , A61K31/366 , A61K2300/00 , A61K31/7068 , A61K2300/00 , A61K31/704 , A61K2300/00 , A61K31/337 , A61K2300/00 , A61K31/40 , A61K2300/00 , A61K31/404 , A61K2300/00 , A61K31/47 , A61K2300/00 , A61K31/22 , A61K2300/00 , A61K31/505 , A61K2300/00 , A61K31/555 , A61K2300/00 , A61K31/282 , A61K2300/00
摘要： 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.

8. 发明公开

US20230226198A1 Artemisinin Derivatives 审中-公开
公开(公告)号：US20230226198A1
公开(公告)日：2023-07-20
申请号：US18123240
申请日：2023-03-17
申请人： DA ZEN THERANOSTICS, INC.
发明人： Leland W.K. Chung , Gina C.Y. Chu , Yi Zhang
IPC分类号： A61K47/55 , A61K47/54 , A61P35/00
CPC分类号： A61K47/552 , A61K47/545 , A61P35/00
摘要： 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.

9. 发明申请

US20230116399A1 Tumor Homing Statin Derivatives 有权
公开(公告)号：US20230116399A1
公开(公告)日：2023-04-13
申请号：US18076213
申请日：2022-12-06
申请人： Da Zen Theranostics, Inc.
发明人： Leland W.K. Chung , Gina C.Y. Chu , Yi Zhang
IPC分类号： A61K47/54 , A61P35/04 , A61K31/351 , A61P35/00 , A61K31/337 , A61K31/4045 , A61K31/4166 , A61K31/58
摘要： 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.

10. 发明申请

US20210008217A1 Tumor Homing Statin Derivatives 有权
公开(公告)号：US20210008217A1
公开(公告)日：2021-01-14
申请号：US16925582
申请日：2020-07-10
申请人： Da Zen Theranostics, Inc.
发明人： Leland W.K. Chung , Gina C.Y. Chu , Yi Zhang
IPC分类号： A61K47/54 , A61K31/351 , A61P35/04
摘要： 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.

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