JPWO2020028532A5 - - Google Patents
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- JPWO2020028532A5 JPWO2020028532A5 JP2021505847A JP2021505847A JPWO2020028532A5 JP WO2020028532 A5 JPWO2020028532 A5 JP WO2020028532A5 JP 2021505847 A JP2021505847 A JP 2021505847A JP 2021505847 A JP2021505847 A JP 2021505847A JP WO2020028532 A5 JPWO2020028532 A5 JP WO2020028532A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- trans
- cells
- fluorophenyl
- pharmaceutical composition
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 210000004027 cell Anatomy 0.000 claims description 39
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 20
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 20
- 239000000203 mixture Substances 0.000 claims description 20
- 150000001875 compounds Chemical class 0.000 claims description 15
- -1 2-(4-fluorophenyl)ethyl Chemical group 0.000 claims description 14
- 239000003550 marker Substances 0.000 claims description 13
- 241000124008 Mammalia Species 0.000 claims description 12
- 125000000260 trans-2-phenylcyclopropyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])[C@]1([H])C([H])([H])[C@@]1([H])* 0.000 claims description 11
- 150000004678 hydrides Chemical class 0.000 claims description 10
- 230000003053 immunization Effects 0.000 claims description 7
- 201000010099 disease Diseases 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 125000001424 substituent group Chemical group 0.000 claims description 6
- 125000001847 2-phenylcyclopropyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C1([H])C([H])([H])C1([H])* 0.000 claims description 5
- 210000001744 T-lymphocyte Anatomy 0.000 claims description 5
- 239000002671 adjuvant Substances 0.000 claims description 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 5
- 229910052736 halogen Inorganic materials 0.000 claims description 5
- 150000002367 halogens Chemical class 0.000 claims description 5
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 claims description 5
- 229910052757 nitrogen Inorganic materials 0.000 claims description 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 5
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 5
- LCDCPQHFCOBUEF-UHFFFAOYSA-N pyrrolidine-1-carboxamide Chemical group NC(=O)N1CCCC1 LCDCPQHFCOBUEF-UHFFFAOYSA-N 0.000 claims description 5
- 230000004936 stimulating effect Effects 0.000 claims description 5
- 230000000735 allogeneic effect Effects 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 230000035755 proliferation Effects 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 22
- 229940076838 Immune checkpoint inhibitor Drugs 0.000 claims 6
- 102000037984 Inhibitory immune checkpoint proteins Human genes 0.000 claims 6
- 108091008026 Inhibitory immune checkpoint proteins Proteins 0.000 claims 6
- 239000012274 immune-checkpoint protein inhibitor Substances 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 244000052769 pathogen Species 0.000 claims 2
- 230000001717 pathogenic effect Effects 0.000 claims 2
- 210000004881 tumor cell Anatomy 0.000 claims 2
- 102100022749 Aminopeptidase N Human genes 0.000 claims 1
- 108010032595 Antibody Binding Sites Proteins 0.000 claims 1
- 102100022005 B-lymphocyte antigen CD20 Human genes 0.000 claims 1
- 241000894006 Bacteria Species 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 102100036166 C-X-C chemokine receptor type 1 Human genes 0.000 claims 1
- 102100031650 C-X-C chemokine receptor type 4 Human genes 0.000 claims 1
- 102100032912 CD44 antigen Human genes 0.000 claims 1
- 102100023126 Cell surface glycoprotein MUC18 Human genes 0.000 claims 1
- 101710117490 Circumsporozoite protein Proteins 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 102100025680 Complement decay-accelerating factor Human genes 0.000 claims 1
- 102100033553 Delta-like protein 4 Human genes 0.000 claims 1
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 1
- 102100037241 Endoglin Human genes 0.000 claims 1
- 102000018651 Epithelial Cell Adhesion Molecule Human genes 0.000 claims 1
- 108010066687 Epithelial Cell Adhesion Molecule Proteins 0.000 claims 1
- 241000233866 Fungi Species 0.000 claims 1
- 102100039622 Granulocyte colony-stimulating factor receptor Human genes 0.000 claims 1
- 101710154606 Hemagglutinin Proteins 0.000 claims 1
- 102100031573 Hematopoietic progenitor cell antigen CD34 Human genes 0.000 claims 1
- 102100034458 Hepatitis A virus cellular receptor 2 Human genes 0.000 claims 1
- 101710083479 Hepatitis A virus cellular receptor 2 homolog Proteins 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 101000757160 Homo sapiens Aminopeptidase N Proteins 0.000 claims 1
- 101000897405 Homo sapiens B-lymphocyte antigen CD20 Proteins 0.000 claims 1
- 101000947174 Homo sapiens C-X-C chemokine receptor type 1 Proteins 0.000 claims 1
- 101000922348 Homo sapiens C-X-C chemokine receptor type 4 Proteins 0.000 claims 1
- 101000868273 Homo sapiens CD44 antigen Proteins 0.000 claims 1
- 101000623903 Homo sapiens Cell surface glycoprotein MUC18 Proteins 0.000 claims 1
- 101000856022 Homo sapiens Complement decay-accelerating factor Proteins 0.000 claims 1
- 101000872077 Homo sapiens Delta-like protein 4 Proteins 0.000 claims 1
- 101000908391 Homo sapiens Dipeptidyl peptidase 4 Proteins 0.000 claims 1
- 101000881679 Homo sapiens Endoglin Proteins 0.000 claims 1
- 101000746364 Homo sapiens Granulocyte colony-stimulating factor receptor Proteins 0.000 claims 1
- 101000777663 Homo sapiens Hematopoietic progenitor cell antigen CD34 Proteins 0.000 claims 1
- 101000994365 Homo sapiens Integrin alpha-6 Proteins 0.000 claims 1
- 101000599852 Homo sapiens Intercellular adhesion molecule 1 Proteins 0.000 claims 1
- 101001063456 Homo sapiens Leucine-rich repeat-containing G-protein coupled receptor 5 Proteins 0.000 claims 1
- 101001008874 Homo sapiens Mast/stem cell growth factor receptor Kit Proteins 0.000 claims 1
- 101000581981 Homo sapiens Neural cell adhesion molecule 1 Proteins 0.000 claims 1
- 101000610551 Homo sapiens Prominin-1 Proteins 0.000 claims 1
- 101000884271 Homo sapiens Signal transducer CD24 Proteins 0.000 claims 1
- 101000596234 Homo sapiens T-cell surface protein tactile Proteins 0.000 claims 1
- 101000835745 Homo sapiens Teratocarcinoma-derived growth factor 1 Proteins 0.000 claims 1
- 101000800116 Homo sapiens Thy-1 membrane glycoprotein Proteins 0.000 claims 1
- 101000801254 Homo sapiens Tumor necrosis factor receptor superfamily member 16 Proteins 0.000 claims 1
- 102100032816 Integrin alpha-6 Human genes 0.000 claims 1
- 102100037877 Intercellular adhesion molecule 1 Human genes 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 102100031036 Leucine-rich repeat-containing G-protein coupled receptor 5 Human genes 0.000 claims 1
- 102100027754 Mast/stem cell growth factor receptor Kit Human genes 0.000 claims 1
- 102000013013 Member 2 Subfamily G ATP Binding Cassette Transporter Human genes 0.000 claims 1
- 108010090306 Member 2 Subfamily G ATP Binding Cassette Transporter Proteins 0.000 claims 1
- 102000003729 Neprilysin Human genes 0.000 claims 1
- 108090000028 Neprilysin Proteins 0.000 claims 1
- 102100027347 Neural cell adhesion molecule 1 Human genes 0.000 claims 1
- 102000005348 Neuraminidase Human genes 0.000 claims 1
- 108010006232 Neuraminidase Proteins 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 102000001756 Notch2 Receptor Human genes 0.000 claims 1
- 108010029751 Notch2 Receptor Proteins 0.000 claims 1
- 101710093908 Outer capsid protein VP4 Proteins 0.000 claims 1
- 101710135467 Outer capsid protein sigma-1 Proteins 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 240000009188 Phyllostachys vivax Species 0.000 claims 1
- 241000223960 Plasmodium falciparum Species 0.000 claims 1
- 102100040120 Prominin-1 Human genes 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 101710176177 Protein A56 Proteins 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 102100038081 Signal transducer CD24 Human genes 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 229940126547 T-cell immunoglobulin mucin-3 Drugs 0.000 claims 1
- 102100035268 T-cell surface protein tactile Human genes 0.000 claims 1
- 102100026404 Teratocarcinoma-derived growth factor 1 Human genes 0.000 claims 1
- 102100033523 Thy-1 membrane glycoprotein Human genes 0.000 claims 1
- 102100033725 Tumor necrosis factor receptor superfamily member 16 Human genes 0.000 claims 1
- 241000700605 Viruses Species 0.000 claims 1
- 239000012736 aqueous medium Substances 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 210000002165 glioblast Anatomy 0.000 claims 1
- 239000012678 infectious agent Substances 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 244000045947 parasite Species 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 241000712461 unidentified influenza virus Species 0.000 claims 1
- 238000000034 method Methods 0.000 description 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- 230000005746 immune checkpoint blockade Effects 0.000 description 2
- 230000028993 immune response Effects 0.000 description 2
- 238000002649 immunization Methods 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862713823P | 2018-08-02 | 2018-08-02 | |
| US62/713,823 | 2018-08-02 | ||
| PCT/US2019/044421 WO2020028532A1 (en) | 2018-08-02 | 2019-07-31 | Adjuvant effect of the tlr1/2 agonist diprovocim synergizes with checkpoint-inhibiting antibodies to eliminate disease |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021533134A JP2021533134A (ja) | 2021-12-02 |
| JP2021533134A5 JP2021533134A5 (https=) | 2022-09-22 |
| JPWO2020028532A5 true JPWO2020028532A5 (https=) | 2022-09-22 |
Family
ID=69232110
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021505847A Pending JP2021533134A (ja) | 2018-08-02 | 2019-07-31 | チェックポイント阻害抗体と相乗効果を示し、疾患を排除するｔｌｒ１／２アゴニストジプロボッシムのアジュバント効果 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20210315992A1 (https=) |
| EP (1) | EP3829571B1 (https=) |
| JP (1) | JP2021533134A (https=) |
| KR (1) | KR20210029280A (https=) |
| CN (1) | CN113164445A (https=) |
| AU (2) | AU2019315952A1 (https=) |
| BR (1) | BR112021001992A2 (https=) |
| CA (1) | CA3108515A1 (https=) |
| IL (1) | IL280584B2 (https=) |
| WO (1) | WO2020028532A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11938182B2 (en) | 2020-03-26 | 2024-03-26 | Provectus Pharmatech, Inc. | Halogenated xanthenes as vaccine adjuvants |
| MX2022011765A (es) | 2020-03-26 | 2022-11-09 | Provectus Pharmatech Inc | Usos novedosos de xantenos halogenados en oncologia y virologia. |
| JP2023527792A (ja) | 2020-05-27 | 2023-06-30 | アキシャル セラピューティクス，インク． | Ｔｌｒ２調節剤化合物、医薬組成物、及びそれらの使用 |
| CN115697363A (zh) * | 2020-07-14 | 2023-02-03 | Dic株式会社 | 细胞杀伤性t细胞(ctl)活化用组合物 |
| US20250367166A1 (en) * | 2022-04-29 | 2025-12-04 | The Scripps Research Institute | Next generation diprovocims that activate the innate and adaptive immune response |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4599231A (en) | 1984-03-09 | 1986-07-08 | Scripps Clinic And Research Foundation | Synthetic hepatitis B virus vaccine including both T cell and B cell determinants |
| US5180806A (en) | 1988-05-16 | 1993-01-19 | The Scripps Research Institute | Polypeptides and compositions of human papillomavirus latent proteins, diagnostic systems and methods |
| US6489354B1 (en) | 1999-03-02 | 2002-12-03 | Merck & Co., Inc. | 3-alkyl substituted pyrrolidine modulators of chemokine receptor activity |
| US6942866B2 (en) | 2000-08-16 | 2005-09-13 | Apovia, Inc. | Malaria immunogen and vaccine |
| DK1418905T3 (da) * | 2001-08-08 | 2007-09-10 | Pentraxin Therapeutics Ltd | Terapeutisk middel til depletering af en uönsket proteinpopulation fra plasma |
| US7361352B2 (en) | 2001-08-15 | 2008-04-22 | Acambis, Inc. | Influenza immunogen and vaccine |
| CA2636424A1 (en) * | 2006-01-09 | 2007-10-25 | The Regents Of The University Of California | Immunostimulatory combinations of tnfrsf, tlr, nlr, rhr, purinergic receptor, and cytokine receptor agonists for vaccines and tumor immunotherapy |
| EP2981281B1 (en) * | 2013-04-03 | 2020-07-15 | IBC Pharmaceuticals, Inc. | Combination therapy for inducing immune response to disease |
| US9918959B2 (en) * | 2014-08-06 | 2018-03-20 | The Board Of Regents Of The University Of Texas System | TLR-independent small molecule adjuvants |
| CA2974956A1 (en) * | 2015-01-29 | 2016-08-04 | The Trustees Of The University Of Pennsylvania | Checkpoint inhibitor and vaccine combinations and use of same for immunotherapy |
| MX2017012939A (es) * | 2015-04-08 | 2018-05-22 | Novartis Ag | Terapias cd20, terapias cd22 y terapias de combinacion con una celula que expresa un receptor quimerico de antigeno (car) de cd19. |
| FI3436048T3 (fi) * | 2016-03-31 | 2025-09-15 | Biontech Us Inc | Neoantigeeneja ja niiden käyttömenetelmiä |
| KR102522730B1 (ko) | 2016-06-29 | 2023-04-19 | 더 보드 오브 리젠츠 오브 더 유니버시티 오브 텍사스 시스템 | 디프로보심: 새로운 강력한 부류의 tlr 작용제 |
| US20180088749A1 (en) | 2016-09-26 | 2018-03-29 | Uber Technologies, Inc. | Customized content generation for a user interface for a network service |
| US20180169224A1 (en) | 2016-12-12 | 2018-06-21 | Wisconsin Alumni Research Foundation | Tlr agonists for reducing activation-induced pd-1 expression on t cells and methods of use |
-
2019
- 2019-07-31 CN CN201980065609.8A patent/CN113164445A/zh active Pending
- 2019-07-31 AU AU2019315952A patent/AU2019315952A1/en not_active Abandoned
- 2019-07-31 EP EP19844778.1A patent/EP3829571B1/en active Active
- 2019-07-31 BR BR112021001992-8A patent/BR112021001992A2/pt unknown
- 2019-07-31 US US17/265,333 patent/US20210315992A1/en active Pending
- 2019-07-31 IL IL280584A patent/IL280584B2/en unknown
- 2019-07-31 KR KR1020217006180A patent/KR20210029280A/ko not_active Ceased
- 2019-07-31 JP JP2021505847A patent/JP2021533134A/ja active Pending
- 2019-07-31 WO PCT/US2019/044421 patent/WO2020028532A1/en not_active Ceased
- 2019-07-31 CA CA3108515A patent/CA3108515A1/en active Pending
-
2025
- 2025-06-03 AU AU2025204146A patent/AU2025204146A1/en active Pending
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