JPWO2022040596A5 - - Google Patents
Download PDFInfo
- Publication number
- JPWO2022040596A5 JPWO2022040596A5 JP2023511915A JP2023511915A JPWO2022040596A5 JP WO2022040596 A5 JPWO2022040596 A5 JP WO2022040596A5 JP 2023511915 A JP2023511915 A JP 2023511915A JP 2023511915 A JP2023511915 A JP 2023511915A JP WO2022040596 A5 JPWO2022040596 A5 JP WO2022040596A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- substituted
- cancer
- antibody
- integer
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 135
- 125000005842 heteroatom Chemical group 0.000 claims 19
- 102000008394 Immunoglobulin Fragments Human genes 0.000 claims 18
- 108010021625 Immunoglobulin Fragments Proteins 0.000 claims 18
- 125000000732 arylene group Chemical group 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 17
- 239000012453 solvate Substances 0.000 claims 17
- 125000005647 linker group Chemical group 0.000 claims 15
- 229940127121 immunoconjugate Drugs 0.000 claims 11
- 206010028980 Neoplasm Diseases 0.000 claims 10
- 125000005549 heteroarylene group Chemical group 0.000 claims 10
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 10
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 125000002947 alkylene group Chemical group 0.000 claims 9
- 229940024606 amino acid Drugs 0.000 claims 9
- 235000001014 amino acid Nutrition 0.000 claims 9
- 150000001413 amino acids Chemical class 0.000 claims 9
- 239000012634 fragment Substances 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 6
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 5
- 125000004406 C3-C8 cycloalkylene group Chemical group 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 5
- 229960005190 phenylalanine Drugs 0.000 claims 5
- 206010009944 Colon cancer Diseases 0.000 claims 4
- PEEHTFAAVSWFBL-UHFFFAOYSA-N Maleimide Chemical compound O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 claims 4
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 4
- 102000002689 Toll-like receptor Human genes 0.000 claims 4
- 108020000411 Toll-like receptor Proteins 0.000 claims 4
- 239000000556 agonist Substances 0.000 claims 4
- 239000002246 antineoplastic agent Substances 0.000 claims 4
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 4
- 201000002528 pancreatic cancer Diseases 0.000 claims 4
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 4
- 229920001481 poly(stearyl methacrylate) Polymers 0.000 claims 4
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- -1 Compound compound Chemical class 0.000 claims 3
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 150000004820 halides Chemical class 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001301 oxygen Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims 3
- 125000005717 substituted cycloalkylene group Chemical group 0.000 claims 3
- 229960004441 tyrosine Drugs 0.000 claims 3
- NEMHIKRLROONTL-QMMMGPOBSA-N (2s)-2-azaniumyl-3-(4-azidophenyl)propanoate Chemical compound OC(=O)[C@@H](N)CC1=CC=C(N=[N+]=[N-])C=C1 NEMHIKRLROONTL-QMMMGPOBSA-N 0.000 claims 2
- CMUHFUGDYMFHEI-QMMMGPOBSA-N 4-amino-L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(N)C=C1 CMUHFUGDYMFHEI-QMMMGPOBSA-N 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 102100038078 CD276 antigen Human genes 0.000 claims 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 206010014733 Endometrial cancer Diseases 0.000 claims 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 2
- 102100035139 Folate receptor alpha Human genes 0.000 claims 2
- 101001023230 Homo sapiens Folate receptor alpha Proteins 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 2
- 102100023144 Zinc transporter ZIP6 Human genes 0.000 claims 2
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 2
- OTKPPUXRIADSGD-PPRNARJGSA-N avoparcina Chemical compound O([C@@H]1C2=CC=C(C(=C2)Cl)OC=2C=C3C=C(C=2O[C@H]2C([C@@H](O)[C@H](O)[C@@H](CO)O2)O[C@@H]2O[C@@H](C)[C@H](O)[C@H](N)C2)OC2=CC=C(C=C2)[C@@H](O)[C@H](C(N[C@H](C(=O)N[C@H]3C(=O)N[C@H]2C(=O)N[C@@H]1C(N[C@@H](C1=CC(O)=CC(O)=C1C=1C(O)=CC=C2C=1)C(O)=O)=O)C=1C=CC(O)=CC=1)=O)NC(=O)[C@H](NC)C=1C=CC(O[C@H]2[C@@H]([C@H](O)[C@@H](O)[C@H](C)O2)O)=CC=1)[C@H]1C[C@@H](N)[C@@H](O)[C@H](C)O1 OTKPPUXRIADSGD-PPRNARJGSA-N 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 201000010881 cervical cancer Diseases 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 208000037976 chronic inflammation Diseases 0.000 claims 2
- 208000037893 chronic inflammatory disorder Diseases 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 229940127089 cytotoxic agent Drugs 0.000 claims 2
- 201000004101 esophageal cancer Diseases 0.000 claims 2
- 125000005677 ethinylene group Chemical group [*:2]C#C[*:1] 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 208000005017 glioblastoma Diseases 0.000 claims 2
- 229930182480 glucuronide Natural products 0.000 claims 2
- 150000008134 glucuronides Chemical class 0.000 claims 2
- 201000010536 head and neck cancer Diseases 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 229940125697 hormonal agent Drugs 0.000 claims 2
- 230000002519 immonomodulatory effect Effects 0.000 claims 2
- 239000002955 immunomodulating agent Substances 0.000 claims 2
- 229960001438 immunostimulant agent Drugs 0.000 claims 2
- 239000003022 immunostimulating agent Substances 0.000 claims 2
- 230000003308 immunostimulating effect Effects 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 208000025113 myeloid leukemia Diseases 0.000 claims 2
- BZQFBWGGLXLEPQ-REOHCLBHSA-N phosphoserine Chemical compound OC(=O)[C@@H](N)COP(O)(O)=O BZQFBWGGLXLEPQ-REOHCLBHSA-N 0.000 claims 2
- 108090000765 processed proteins & peptides Proteins 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 201000002510 thyroid cancer Diseases 0.000 claims 2
- OUGDEOOFDGWUAC-QMMMGPOBSA-N (2S)-2-amino-3-(3-sulfooxyphenyl)propanoic acid Chemical compound S(=O)(=O)(O)OC=1C=C(C[C@H](N)C(=O)O)C=CC1 OUGDEOOFDGWUAC-QMMMGPOBSA-N 0.000 claims 1
- YYTDJPUFAVPHQA-VKHMYHEASA-N (2s)-2-amino-3-(2,3,4,5,6-pentafluorophenyl)propanoic acid Chemical compound OC(=O)[C@@H](N)CC1=C(F)C(F)=C(F)C(F)=C1F YYTDJPUFAVPHQA-VKHMYHEASA-N 0.000 claims 1
- DJZAVKNBQZFEAL-QMMMGPOBSA-N (2s)-2-amino-3-(2-aminophenyl)propanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1N DJZAVKNBQZFEAL-QMMMGPOBSA-N 0.000 claims 1
- QTCRLZGTYUJQIE-ZETCQYMHSA-N (2s)-2-amino-3-(2-sulfooxyphenyl)propanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1OS(O)(=O)=O QTCRLZGTYUJQIE-ZETCQYMHSA-N 0.000 claims 1
- YDYSBABSIVBERF-ZETCQYMHSA-N (2s)-2-amino-3-(2-sulfophenyl)propanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1S(O)(=O)=O YDYSBABSIVBERF-ZETCQYMHSA-N 0.000 claims 1
- DDLYNVBJVVOUGB-QMMMGPOBSA-N (2s)-2-amino-3-(3-aminophenyl)propanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=CC(N)=C1 DDLYNVBJVVOUGB-QMMMGPOBSA-N 0.000 claims 1
- SUPCVWGCSKIXFE-QMMMGPOBSA-N (2s)-2-amino-3-(3-sulfophenyl)propanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=CC(S(O)(=O)=O)=C1 SUPCVWGCSKIXFE-QMMMGPOBSA-N 0.000 claims 1
- PEMUHKUIQHFMTH-QMMMGPOBSA-N (2s)-2-amino-3-(4-bromophenyl)propanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=C(Br)C=C1 PEMUHKUIQHFMTH-QMMMGPOBSA-N 0.000 claims 1
- OHQAEAFCFJFHEV-JAVCKPHESA-N (2s)-2-amino-3-(4-hydroxy-4-sulfocyclohexa-1,5-dien-1-yl)propanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CCC(O)(S(O)(=O)=O)C=C1 OHQAEAFCFJFHEV-JAVCKPHESA-N 0.000 claims 1
- BJOQKIKXKGJLIJ-NSHDSACASA-N (2s)-2-amino-3-(4-prop-2-ynylphenyl)propanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=C(CC#C)C=C1 BJOQKIKXKGJLIJ-NSHDSACASA-N 0.000 claims 1
- ALQIUGWFHKQQHV-QMMMGPOBSA-N (2s)-2-amino-3-(4-sulfophenyl)propanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=C(S(O)(=O)=O)C=C1 ALQIUGWFHKQQHV-QMMMGPOBSA-N 0.000 claims 1
- SDZGVFSSLGTJAJ-ZETCQYMHSA-N (2s)-2-azaniumyl-3-(2-nitrophenyl)propanoate Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1[N+]([O-])=O SDZGVFSSLGTJAJ-ZETCQYMHSA-N 0.000 claims 1
- YTHDRUZHNYKZGF-QMMMGPOBSA-N (2s)-2-azaniumyl-3-(3-nitrophenyl)propanoate Chemical compound OC(=O)[C@@H](N)CC1=CC=CC([N+]([O-])=O)=C1 YTHDRUZHNYKZGF-QMMMGPOBSA-N 0.000 claims 1
- PQUSMXUQSMSWNN-QMMMGPOBSA-N (2s)-3-(2-amino-4-hydroxyphenyl)-2-azaniumylpropanoate Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1N PQUSMXUQSMSWNN-QMMMGPOBSA-N 0.000 claims 1
- ZXSBHXZKWRIEIA-JTQLQIEISA-N (2s)-3-(4-acetylphenyl)-2-azaniumylpropanoate Chemical compound CC(=O)C1=CC=C(C[C@H](N)C(O)=O)C=C1 ZXSBHXZKWRIEIA-JTQLQIEISA-N 0.000 claims 1
- SXIFEQOVCDBNET-QMMMGPOBSA-N 2-[(2s)-2-amino-2-carboxyethyl]benzoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1C(O)=O SXIFEQOVCDBNET-QMMMGPOBSA-N 0.000 claims 1
- BGFTWECWAICPDG-UHFFFAOYSA-N 2-[bis(4-chlorophenyl)methyl]-4-n-[3-[bis(4-chlorophenyl)methyl]-4-(dimethylamino)phenyl]-1-n,1-n-dimethylbenzene-1,4-diamine Chemical compound C1=C(C(C=2C=CC(Cl)=CC=2)C=2C=CC(Cl)=CC=2)C(N(C)C)=CC=C1NC(C=1)=CC=C(N(C)C)C=1C(C=1C=CC(Cl)=CC=1)C1=CC=C(Cl)C=C1 BGFTWECWAICPDG-UHFFFAOYSA-N 0.000 claims 1
- SKMKJBYBPYBDMN-RYUDHWBXSA-N 3-(difluoromethoxy)-5-[2-(3,3-difluoropyrrolidin-1-yl)-6-[(1s,4s)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]pyridin-2-amine Chemical compound C1=C(OC(F)F)C(N)=NC=C1C1=CC(N2[C@H]3C[C@H](OC3)C2)=NC(N2CC(F)(F)CC2)=N1 SKMKJBYBPYBDMN-RYUDHWBXSA-N 0.000 claims 1
- JANONUPBHGWOBP-QMMMGPOBSA-N 3-[(2s)-2-amino-2-carboxyethyl]benzoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=CC(C(O)=O)=C1 JANONUPBHGWOBP-QMMMGPOBSA-N 0.000 claims 1
- JZRBSTONIYRNRI-VIFPVBQESA-N 3-methylphenylalanine Chemical compound CC1=CC=CC(C[C@H](N)C(O)=O)=C1 JZRBSTONIYRNRI-VIFPVBQESA-N 0.000 claims 1
- IRZQDMYEJPNDEN-UHFFFAOYSA-N 3-phenyl-2-aminobutanoic acid Natural products OC(=O)C(N)C(C)C1=CC=CC=C1 IRZQDMYEJPNDEN-UHFFFAOYSA-N 0.000 claims 1
- YXDGRBPZVQPESQ-QMMMGPOBSA-N 4-[(2s)-2-amino-2-carboxyethyl]benzoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=C(C(O)=O)C=C1 YXDGRBPZVQPESQ-QMMMGPOBSA-N 0.000 claims 1
- XWQVQSXLXAXOPJ-QNGMFEMESA-N 4-[[[6-[5-chloro-2-[[4-[[(2r)-1-methoxypropan-2-yl]amino]cyclohexyl]amino]pyridin-4-yl]pyridin-2-yl]amino]methyl]oxane-4-carbonitrile Chemical compound C1CC(N[C@H](C)COC)CCC1NC1=CC(C=2N=C(NCC3(CCOCC3)C#N)C=CC=2)=C(Cl)C=N1 XWQVQSXLXAXOPJ-QNGMFEMESA-N 0.000 claims 1
- PZNQZSRPDOEBMS-QMMMGPOBSA-N 4-iodo-L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(I)C=C1 PZNQZSRPDOEBMS-QMMMGPOBSA-N 0.000 claims 1
- GTVVZTAFGPQSPC-UHFFFAOYSA-N 4-nitrophenylalanine Chemical compound OC(=O)C(N)CC1=CC=C([N+]([O-])=O)C=C1 GTVVZTAFGPQSPC-UHFFFAOYSA-N 0.000 claims 1
- 102100023990 60S ribosomal protein L17 Human genes 0.000 claims 1
- 102100031585 ADP-ribosyl cyclase/cyclic ADP-ribose hydrolase 1 Human genes 0.000 claims 1
- 102100026423 Adhesion G protein-coupled receptor E5 Human genes 0.000 claims 1
- 108010008014 B-Cell Maturation Antigen Proteins 0.000 claims 1
- 102000006942 B-Cell Maturation Antigen Human genes 0.000 claims 1
- 102100038080 B-cell receptor CD22 Human genes 0.000 claims 1
- 102100024222 B-lymphocyte antigen CD19 Human genes 0.000 claims 1
- 102100022005 B-lymphocyte antigen CD20 Human genes 0.000 claims 1
- 102100024217 CAMPATH-1 antigen Human genes 0.000 claims 1
- 101710185679 CD276 antigen Proteins 0.000 claims 1
- 102000017420 CD3 protein, epsilon/gamma/delta subunit Human genes 0.000 claims 1
- 108050005493 CD3 protein, epsilon/gamma/delta subunit Proteins 0.000 claims 1
- 102100032912 CD44 antigen Human genes 0.000 claims 1
- 108010065524 CD52 Antigen Proteins 0.000 claims 1
- 102100025221 CD70 antigen Human genes 0.000 claims 1
- 108060001253 CD99 Proteins 0.000 claims 1
- 102000024905 CD99 Human genes 0.000 claims 1
- 108010021064 CTLA-4 Antigen Proteins 0.000 claims 1
- 229940045513 CTLA4 antagonist Drugs 0.000 claims 1
- 102100029756 Cadherin-6 Human genes 0.000 claims 1
- 101100463133 Caenorhabditis elegans pdl-1 gene Proteins 0.000 claims 1
- 102100024423 Carbonic anhydrase 9 Human genes 0.000 claims 1
- RAPBNVDSDCTNRC-UHFFFAOYSA-N Chlorobenzilate Chemical compound C=1C=C(Cl)C=CC=1C(O)(C(=O)OCC)C1=CC=C(Cl)C=C1 RAPBNVDSDCTNRC-UHFFFAOYSA-N 0.000 claims 1
- 102100039496 Choline transporter-like protein 4 Human genes 0.000 claims 1
- 102000002029 Claudin Human genes 0.000 claims 1
- 108050009302 Claudin Proteins 0.000 claims 1
- 102100039498 Cytotoxic T-lymphocyte protein 4 Human genes 0.000 claims 1
- 102100036466 Delta-like protein 3 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
- 108091006020 Fc-tagged proteins Proteins 0.000 claims 1
- 102100023600 Fibroblast growth factor receptor 2 Human genes 0.000 claims 1
- 101710182389 Fibroblast growth factor receptor 2 Proteins 0.000 claims 1
- 102100041003 Glutamate carboxypeptidase 2 Human genes 0.000 claims 1
- 102100032530 Glypican-3 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
- 101000777636 Homo sapiens ADP-ribosyl cyclase/cyclic ADP-ribose hydrolase 1 Proteins 0.000 claims 1
- 101000718243 Homo sapiens Adhesion G protein-coupled receptor E5 Proteins 0.000 claims 1
- 101000884305 Homo sapiens B-cell receptor CD22 Proteins 0.000 claims 1
- 101000980825 Homo sapiens B-lymphocyte antigen CD19 Proteins 0.000 claims 1
- 101000897405 Homo sapiens B-lymphocyte antigen CD20 Proteins 0.000 claims 1
- 101000868273 Homo sapiens CD44 antigen Proteins 0.000 claims 1
- 101000934356 Homo sapiens CD70 antigen Proteins 0.000 claims 1
- 101000910338 Homo sapiens Carbonic anhydrase 9 Proteins 0.000 claims 1
- 101000914324 Homo sapiens Carcinoembryonic antigen-related cell adhesion molecule 5 Proteins 0.000 claims 1
- 101000914321 Homo sapiens Carcinoembryonic antigen-related cell adhesion molecule 7 Proteins 0.000 claims 1
- 101000928513 Homo sapiens Delta-like protein 3 Proteins 0.000 claims 1
- 101000892862 Homo sapiens Glutamate carboxypeptidase 2 Proteins 0.000 claims 1
- 101001014668 Homo sapiens Glypican-3 Proteins 0.000 claims 1
- 101001103039 Homo sapiens Inactive tyrosine-protein kinase transmembrane receptor ROR1 Proteins 0.000 claims 1
- 101001057504 Homo sapiens Interferon-stimulated gene 20 kDa protein Proteins 0.000 claims 1
- 101001055144 Homo sapiens Interleukin-2 receptor subunit alpha Proteins 0.000 claims 1
- 101000998120 Homo sapiens Interleukin-3 receptor subunit alpha Proteins 0.000 claims 1
- 101000777628 Homo sapiens Leukocyte antigen CD37 Proteins 0.000 claims 1
- 101000868279 Homo sapiens Leukocyte surface antigen CD47 Proteins 0.000 claims 1
- 101001065568 Homo sapiens Lymphocyte antigen 6E Proteins 0.000 claims 1
- 101001008874 Homo sapiens Mast/stem cell growth factor receptor Kit Proteins 0.000 claims 1
- 101000628547 Homo sapiens Metalloreductase STEAP1 Proteins 0.000 claims 1
- 101001133056 Homo sapiens Mucin-1 Proteins 0.000 claims 1
- 101000623901 Homo sapiens Mucin-16 Proteins 0.000 claims 1
- 101000934338 Homo sapiens Myeloid cell surface antigen CD33 Proteins 0.000 claims 1
- 101000581981 Homo sapiens Neural cell adhesion molecule 1 Proteins 0.000 claims 1
- 101001103036 Homo sapiens Nuclear receptor ROR-alpha Proteins 0.000 claims 1
- 101000897042 Homo sapiens Nucleotide pyrophosphatase Proteins 0.000 claims 1
- 101000617725 Homo sapiens Pregnancy-specific beta-1-glycoprotein 2 Proteins 0.000 claims 1
- 101001123448 Homo sapiens Prolactin receptor Proteins 0.000 claims 1
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims 1
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims 1
- 101000835984 Homo sapiens SLIT and NTRK-like protein 6 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
- 101000669402 Homo sapiens Toll-like receptor 7 Proteins 0.000 claims 1
- 101000800483 Homo sapiens Toll-like receptor 8 Proteins 0.000 claims 1
- 101000904724 Homo sapiens Transmembrane glycoprotein NMB Proteins 0.000 claims 1
- 101000801433 Homo sapiens Trophoblast glycoprotein Proteins 0.000 claims 1
- 101000851376 Homo sapiens Tumor necrosis factor receptor superfamily member 8 Proteins 0.000 claims 1
- 101000666896 Homo sapiens V-type immunoglobulin domain-containing suppressor of T-cell activation Proteins 0.000 claims 1
- 101000685848 Homo sapiens Zinc transporter ZIP6 Proteins 0.000 claims 1
- 102100039615 Inactive tyrosine-protein kinase transmembrane receptor ROR1 Human genes 0.000 claims 1
- 102100026878 Interleukin-2 receptor subunit alpha Human genes 0.000 claims 1
- 102100033493 Interleukin-3 receptor subunit alpha Human genes 0.000 claims 1
- 108010056045 K cadherin Proteins 0.000 claims 1
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims 1
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims 1
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims 1
- 102100031586 Leukocyte antigen CD37 Human genes 0.000 claims 1
- 102100032913 Leukocyte surface antigen CD47 Human genes 0.000 claims 1
- 102100032131 Lymphocyte antigen 6E Human genes 0.000 claims 1
- 102100027754 Mast/stem cell growth factor receptor Kit Human genes 0.000 claims 1
- 102000003735 Mesothelin Human genes 0.000 claims 1
- 108090000015 Mesothelin Proteins 0.000 claims 1
- 102100026712 Metalloreductase STEAP1 Human genes 0.000 claims 1
- 102100034256 Mucin-1 Human genes 0.000 claims 1
- 102100023123 Mucin-16 Human genes 0.000 claims 1
- 102100025243 Myeloid cell surface antigen CD33 Human genes 0.000 claims 1
- 102100035486 Nectin-4 Human genes 0.000 claims 1
- 101710043865 Nectin-4 Proteins 0.000 claims 1
- 102100027347 Neural cell adhesion molecule 1 Human genes 0.000 claims 1
- 102100021969 Nucleotide pyrophosphatase Human genes 0.000 claims 1
- CIQHWLTYGMYQQR-QMMMGPOBSA-N O(4')-sulfo-L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(OS(O)(=O)=O)C=C1 CIQHWLTYGMYQQR-QMMMGPOBSA-N 0.000 claims 1
- GEYBMYRBIABFTA-VIFPVBQESA-N O-methyl-L-tyrosine Chemical compound COC1=CC=C(C[C@H](N)C(O)=O)C=C1 GEYBMYRBIABFTA-VIFPVBQESA-N 0.000 claims 1
- 239000004952 Polyamide Substances 0.000 claims 1
- 239000004721 Polyphenylene oxide Substances 0.000 claims 1
- 102100022019 Pregnancy-specific beta-1-glycoprotein 2 Human genes 0.000 claims 1
- 101710089372 Programmed cell death protein 1 Proteins 0.000 claims 1
- 102100029000 Prolactin receptor Human genes 0.000 claims 1
- 101710202113 Prolow-density lipoprotein receptor-related protein 1 Proteins 0.000 claims 1
- 102100021923 Prolow-density lipoprotein receptor-related protein 1 Human genes 0.000 claims 1
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims 1
- 102100029986 Receptor tyrosine-protein kinase erbB-3 Human genes 0.000 claims 1
- 101710100969 Receptor tyrosine-protein kinase erbB-3 Proteins 0.000 claims 1
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims 1
- 101150036449 SIRPA gene Proteins 0.000 claims 1
- 108091006576 SLC34A2 Proteins 0.000 claims 1
- 108091006938 SLC39A6 Proteins 0.000 claims 1
- 108091007561 SLC44A4 Proteins 0.000 claims 1
- 102100025504 SLIT and NTRK-like protein 6 Human genes 0.000 claims 1
- 102100038081 Signal transducer CD24 Human genes 0.000 claims 1
- 102100038437 Sodium-dependent phosphate transport protein 2B Human genes 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
- 229940124614 TLR 8 agonist Drugs 0.000 claims 1
- 101150117918 Tacstd2 gene Proteins 0.000 claims 1
- 102100039390 Toll-like receptor 7 Human genes 0.000 claims 1
- 102100033110 Toll-like receptor 8 Human genes 0.000 claims 1
- 102100023935 Transmembrane glycoprotein NMB Human genes 0.000 claims 1
- 102100033579 Trophoblast glycoprotein Human genes 0.000 claims 1
- 102100036857 Tumor necrosis factor receptor superfamily member 8 Human genes 0.000 claims 1
- 102100027212 Tumor-associated calcium signal transducer 2 Human genes 0.000 claims 1
- 102100038282 V-type immunoglobulin domain-containing suppressor of T-cell activation Human genes 0.000 claims 1
- 108091008605 VEGF receptors Proteins 0.000 claims 1
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 claims 1
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 claims 1
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 claims 1
- NLWGJLDXMMCNKN-UHFFFAOYSA-N [amino(phenyl)methyl] carbamate Chemical compound NC(=O)OC(N)C1=CC=CC=C1 NLWGJLDXMMCNKN-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 235000004279 alanine Nutrition 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- 125000004419 alkynylene group Chemical group 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 239000000427 antigen Substances 0.000 claims 1
- 102000036639 antigens Human genes 0.000 claims 1
- 108091007433 antigens Proteins 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 230000001588 bifunctional effect Effects 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 229940127276 delta-like ligand 3 Drugs 0.000 claims 1
- 229950006137 dexfosfoserine Drugs 0.000 claims 1
- BFXLJWUGRPGMFU-UHFFFAOYSA-N dipropoxyphosphinothioyl n,n-diethylcarbamodithioate;sulfane Chemical compound S.CCCOP(=S)(OCCC)SC(=S)N(CC)CC BFXLJWUGRPGMFU-UHFFFAOYSA-N 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229940125542 dual agonist Drugs 0.000 claims 1
- DFBKLUNHFCTMDC-GKRDHZSOSA-N endrin Chemical compound C([C@@H]1[C@H]2[C@@]3(Cl)C(Cl)=C([C@]([C@H]22)(Cl)C3(Cl)Cl)Cl)[C@@H]2[C@H]2[C@@H]1O2 DFBKLUNHFCTMDC-GKRDHZSOSA-N 0.000 claims 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 1
- IJJVMEJXYNJXOJ-UHFFFAOYSA-N fluquinconazole Chemical compound C=1C=C(Cl)C=C(Cl)C=1N1C(=O)C2=CC(F)=CC=C2N=C1N1C=NC=N1 IJJVMEJXYNJXOJ-UHFFFAOYSA-N 0.000 claims 1
- 125000005179 haloacetyl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 1
- TVIDEEHSOPHZBR-AWEZNQCLSA-N para-(benzoyl)-phenylalanine Chemical compound C1=CC(C[C@H](N)C(O)=O)=CC=C1C(=O)C1=CC=CC=C1 TVIDEEHSOPHZBR-AWEZNQCLSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- DCWXELXMIBXGTH-QMMMGPOBSA-N phosphonotyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(OP(O)(O)=O)C=C1 DCWXELXMIBXGTH-QMMMGPOBSA-N 0.000 claims 1
- 229920002647 polyamide Polymers 0.000 claims 1
- 229920000728 polyester Polymers 0.000 claims 1
- 229920000570 polyether Polymers 0.000 claims 1
- 229920001184 polypeptide Polymers 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 102000004196 processed proteins & peptides Human genes 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 229940044616 toll-like receptor 7 agonist Drugs 0.000 claims 1
- 210000004881 tumor cell Anatomy 0.000 claims 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims 1
- JPZXHKDZASGCLU-LBPRGKRZSA-N β-(2-naphthyl)-alanine Chemical compound C1=CC=CC2=CC(C[C@H](N)C(O)=O)=CC=C21 JPZXHKDZASGCLU-LBPRGKRZSA-N 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063068342P | 2020-08-20 | 2020-08-20 | |
| US63/068,342 | 2020-08-20 | ||
| US202063118365P | 2020-11-25 | 2020-11-25 | |
| US63/118,365 | 2020-11-25 | ||
| PCT/US2021/047009 WO2022040596A1 (en) | 2020-08-20 | 2021-08-20 | Antibody-tlr agonist conjugates, methods and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023538071A JP2023538071A (ja) | 2023-09-06 |
| JPWO2022040596A5 true JPWO2022040596A5 (https=) | 2024-08-28 |
| JP2023538071A5 JP2023538071A5 (https=) | 2024-08-28 |
Family
ID=77802239
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023511915A Pending JP2023538071A (ja) | 2020-08-20 | 2021-08-20 | 抗体－ｔｌｒアゴニストコンジュゲート、その方法及び使用 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20230302150A1 (https=) |
| EP (1) | EP4199968A1 (https=) |
| JP (1) | JP2023538071A (https=) |
| KR (1) | KR20230073200A (https=) |
| AU (1) | AU2021327396A1 (https=) |
| CA (1) | CA3190606A1 (https=) |
| TW (1) | TW202227449A (https=) |
| WO (1) | WO2022040596A1 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN121555430A (zh) | 2018-05-11 | 2026-02-24 | 比姆医疗股份有限公司 | 使用可编程碱基编辑器系统取代病原性氨基酸的方法 |
| AU2022297426A1 (en) * | 2021-06-22 | 2024-02-01 | Taxis Pharmaceuticals, Inc. | Therapeutic compounds |
| KR20250038769A (ko) * | 2022-07-26 | 2025-03-19 | 자임워크스 비씨 인코포레이티드 | 면역조절제 퓨린 유래 화합물, 이의 접합체 및 이의 사용 방법 |
| JP2025535713A (ja) | 2022-10-07 | 2025-10-28 | アンブレツクス・インコーポレイテツド | 薬物リンカー及びその抗体コンジュゲート |
| AU2024209360A1 (en) | 2023-01-16 | 2025-09-04 | Ambrx, Inc. | Anti-cd70 antibody-drug conjugates |
| WO2024178310A1 (en) | 2023-02-23 | 2024-08-29 | Ambrx, Inc. | Trop2-directed antibody-drug conjugates and uses thereof |
| TW202521564A (zh) * | 2023-08-14 | 2025-06-01 | 美商英特利亞醫療公司 | 用於基於細胞之療法的ｃｄ７０ ｃａｒ－ｔ組合物及方法 |
| KR20250161096A (ko) * | 2024-05-07 | 2025-11-17 | 바이티디 주식회사 | Vista 및 msln에 특이적으로 결합하는 이중특이적 항체 및 이의 용도 |
| WO2025250885A1 (en) * | 2024-05-31 | 2025-12-04 | Oncotelic, Inc. | In situ tumor-infiltrating lymphocyte therapeutics for cancer |
Family Cites Families (143)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| US4263428A (en) | 1978-03-24 | 1981-04-21 | The Regents Of The University Of California | Bis-anthracycline nucleic acid function inhibitors and improved method for administering the same |
| US4289872A (en) | 1979-04-06 | 1981-09-15 | Allied Corporation | Macromolecular highly branched homogeneous compound based on lysine units |
| EP0052322B1 (de) | 1980-11-10 | 1985-03-27 | Gersonde, Klaus, Prof. Dr. | Verfahren zur Herstellung von Lipid-Vesikeln durch Ultraschallbehandlung, Anwendung des Verfahrens und Vorrichtung zur Durchführung des Verfahrens |
| IE52535B1 (en) | 1981-02-16 | 1987-12-09 | Ici Plc | Continuous release pharmaceutical compositions |
| FR2504010B1 (fr) | 1981-04-15 | 1985-10-25 | Sanofi Sa | Medicaments anticancereux contenant la chaine a de la ricine associee a un anticorps antimelanome et procede pour leur preparation |
| US4485045A (en) | 1981-07-06 | 1984-11-27 | Research Corporation | Synthetic phosphatidyl cholines useful in forming liposomes |
| DE3374837D1 (en) | 1982-02-17 | 1988-01-21 | Ciba Geigy Ag | Lipids in the aqueous phase |
| US4671958A (en) | 1982-03-09 | 1987-06-09 | Cytogen Corporation | Antibody conjugates for the delivery of compounds to target sites |
| DE3218121A1 (de) | 1982-05-14 | 1983-11-17 | Leskovar, Peter, Dr.-Ing., 8000 München | Arzneimittel zur tumorbehandlung |
| EP0102324A3 (de) | 1982-07-29 | 1984-11-07 | Ciba-Geigy Ag | Lipide und Tenside in wässriger Phase |
| US4511502A (en) | 1982-12-22 | 1985-04-16 | Genentech, Inc. | Purification and activity assurance of precipitated heterologous proteins |
| US4511503A (en) | 1982-12-22 | 1985-04-16 | Genentech, Inc. | Purification and activity assurance of precipitated heterologous proteins |
| US4512922A (en) | 1982-12-22 | 1985-04-23 | Genentech, Inc. | Purification and activity assurance of precipitated heterologous proteins |
| US4820352A (en) | 1983-01-10 | 1989-04-11 | Bausch & Lomb Incorporated | Cleaning and conditioning solutions for contact lenses and methods of use |
| US4544545A (en) | 1983-06-20 | 1985-10-01 | Trustees University Of Massachusetts | Liposomes containing modified cholesterol for organ targeting |
| HUT35524A (en) | 1983-08-02 | 1985-07-29 | Hoechst Ag | Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance |
| US4870008A (en) | 1983-08-12 | 1989-09-26 | Chiron Corporation | Secretory expression in eukaryotes |
| DE3483949D1 (de) | 1983-09-26 | 1991-02-21 | Udo Dr Med Ehrenfeld | Mittel und erzeugnis fuer die diagnose und therapie von tumoren sowie zur behandlung von schwaechen der zelligen und humoralen immunabwehr. |
| EP0143949B1 (en) | 1983-11-01 | 1988-10-12 | TERUMO KABUSHIKI KAISHA trading as TERUMO CORPORATION | Pharmaceutical composition containing urokinase |
| EP0154316B1 (en) | 1984-03-06 | 1989-09-13 | Takeda Chemical Industries, Ltd. | Chemically modified lymphokine and production thereof |
| US4625014A (en) | 1984-07-10 | 1986-11-25 | Dana-Farber Cancer Institute, Inc. | Cell-delivery agent |
| US4542225A (en) | 1984-08-29 | 1985-09-17 | Dana-Farber Cancer Institute, Inc. | Acid-cleavable compound |
| US4659839A (en) | 1984-10-10 | 1987-04-21 | Mallinckrodt, Inc. | Coupling agents for radiolabeled antibody fragments |
| GB8430252D0 (en) | 1984-11-30 | 1985-01-09 | Beecham Group Plc | Compounds |
| EP0188256B1 (en) | 1985-01-14 | 1991-08-21 | NeoRx | Metal radionuclide labeled proteins for diagnosis and therapy |
| DE3675588D1 (de) | 1985-06-19 | 1990-12-20 | Ajinomoto Kk | Haemoglobin, das an ein poly(alkenylenoxid) gebunden ist. |
| DE3676670D1 (de) | 1985-06-26 | 1991-02-07 | Cetus Corp | Solubilisierung von proteinen fuer pharmazeutische zusammensetzungen mittels polymerkonjugierung. |
| US4680338A (en) | 1985-10-17 | 1987-07-14 | Immunomedics, Inc. | Bifunctional linker |
| AU6543286A (en) | 1985-10-25 | 1987-05-19 | Zymogenetics Inc. | Method of using bar1 for secreting foreign proteins |
| US4699784A (en) | 1986-02-25 | 1987-10-13 | Center For Molecular Medicine & Immunology | Tumoricidal methotrexate-antibody conjugate |
| AU597574B2 (en) | 1986-03-07 | 1990-06-07 | Massachusetts Institute Of Technology | Method for enhancing glycoprotein stability |
| US5229490A (en) | 1987-05-06 | 1993-07-20 | The Rockefeller University | Multiple antigen peptide system |
| US5080891A (en) | 1987-08-03 | 1992-01-14 | Ddi Pharmaceuticals, Inc. | Conjugates of superoxide dismutase coupled to high molecular weight polyalkylene glycols |
| US4847325A (en) | 1988-01-20 | 1989-07-11 | Cetus Corporation | Conjugation of polymer to colony stimulating factor-1 |
| GB8824591D0 (en) | 1988-10-20 | 1988-11-23 | Royal Free Hosp School Med | Fractionation process |
| US5047335A (en) | 1988-12-21 | 1991-09-10 | The Regents Of The University Of Calif. | Process for controlling intracellular glycosylation of proteins |
| EP0401384B1 (en) | 1988-12-22 | 1996-03-13 | Kirin-Amgen, Inc. | Chemically modified granulocyte colony stimulating factor |
| US4902502A (en) | 1989-01-23 | 1990-02-20 | Cetus Corporation | Preparation of a polymer/interleukin-2 conjugate |
| US5324844A (en) | 1989-04-19 | 1994-06-28 | Enzon, Inc. | Active carbonates of polyalkylene oxides for modification of polypeptides |
| US5122614A (en) | 1989-04-19 | 1992-06-16 | Enzon, Inc. | Active carbonates of polyalkylene oxides for modification of polypeptides |
| DE69026306T2 (de) | 1989-05-27 | 1996-10-17 | Seikagaku Kogyo Co Ltd | Verfahren für die Herstellung von Polyethylenglykolderivate und modifizierte Proteine. |
| US5219564A (en) | 1990-07-06 | 1993-06-15 | Enzon, Inc. | Poly(alkylene oxide) amino acid copolymers and drug carriers and charged copolymers based thereon |
| US5492821A (en) | 1990-11-14 | 1996-02-20 | Cargill, Inc. | Stabilized polyacrylic saccharide protein conjugates |
| US5252714A (en) | 1990-11-28 | 1993-10-12 | The University Of Alabama In Huntsville | Preparation and use of polyethylene glycol propionaldehyde |
| WO1992016555A1 (en) | 1991-03-18 | 1992-10-01 | Enzon, Inc. | Hydrazine containing conjugates of polypeptides and glycopolypeptides with polymers |
| US5595732A (en) | 1991-03-25 | 1997-01-21 | Hoffmann-La Roche Inc. | Polyethylene-protein conjugates |
| US5281698A (en) | 1991-07-23 | 1994-01-25 | Cetus Oncology Corporation | Preparation of an activated polymer ester for protein conjugation |
| CA2118130A1 (en) | 1992-04-14 | 1993-10-28 | Jean M. J. Frechet | Dendritic based macromolecules and method of production |
| ZA933926B (en) | 1992-06-17 | 1994-01-03 | Amgen Inc | Polyoxymethylene-oxyethylene copolymers in conjuction with blomolecules |
| AU5006993A (en) | 1992-08-21 | 1994-03-15 | Enzon, Inc. | Novel attachment of polyalkylene oxides to bio-effecting substances |
| US5382657A (en) | 1992-08-26 | 1995-01-17 | Hoffmann-La Roche Inc. | Peg-interferon conjugates |
| NZ250375A (en) | 1992-12-09 | 1995-07-26 | Ortho Pharma Corp | Peg hydrazone and peg oxime linkage forming reagents and protein derivatives |
| US5298643A (en) | 1992-12-22 | 1994-03-29 | Enzon, Inc. | Aryl imidate activated polyalkylene oxides |
| US5349001A (en) | 1993-01-19 | 1994-09-20 | Enzon, Inc. | Cyclic imide thione activated polyalkylene oxides |
| US5321095A (en) | 1993-02-02 | 1994-06-14 | Enzon, Inc. | Azlactone activated polyalkylene oxides |
| IL104734A0 (en) | 1993-02-15 | 1993-06-10 | Univ Bar Ilan | Bioactive conjugates of cellulose with amino compounds |
| WO1994028024A1 (en) | 1993-06-01 | 1994-12-08 | Enzon, Inc. | Carbohydrate-modified polymer conjugates with erythropoietic activity |
| WO1995000162A1 (en) | 1993-06-21 | 1995-01-05 | Enzon, Inc. | Site specific synthesis of conjugated peptides |
| GB9317618D0 (en) | 1993-08-24 | 1993-10-06 | Royal Free Hosp School Med | Polymer modifications |
| US5643575A (en) | 1993-10-27 | 1997-07-01 | Enzon, Inc. | Non-antigenic branched polymer conjugates |
| US5919455A (en) | 1993-10-27 | 1999-07-06 | Enzon, Inc. | Non-antigenic branched polymer conjugates |
| US5951974A (en) | 1993-11-10 | 1999-09-14 | Enzon, Inc. | Interferon polymer conjugates |
| KR960705579A (ko) | 1993-11-10 | 1996-11-08 | 에릭에스. 딕커 | 개선된 인터페론 중합체 결합체(Improved interferon polymer conjugates) |
| US5446090A (en) | 1993-11-12 | 1995-08-29 | Shearwater Polymers, Inc. | Isolatable, water soluble, and hydrolytically stable active sulfones of poly(ethylene glycol) and related polymers for modification of surfaces and molecules |
| US5473034A (en) | 1994-03-18 | 1995-12-05 | Hyogo Prefectural Government | Method for producing protein-synthetic polymer conjugate and said conjugate produced thereby |
| US5629384A (en) | 1994-05-17 | 1997-05-13 | Consiglio Nazionale Delle Ricerche | Polymers of N-acryloylmorpholine activated at one end and conjugates with bioactive materials and surfaces |
| WO1995033490A1 (en) | 1994-06-02 | 1995-12-14 | Enzon, Inc. | Method of solubilizing substantially water insoluble materials |
| US5730990A (en) | 1994-06-24 | 1998-03-24 | Enzon, Inc. | Non-antigenic amine derived polymers and polymer conjugates |
| US5650234A (en) | 1994-09-09 | 1997-07-22 | Surface Engineering Technologies, Division Of Innerdyne, Inc. | Electrophilic polyethylene oxides for the modification of polysaccharides, polypeptides (proteins) and surfaces |
| US5824784A (en) | 1994-10-12 | 1998-10-20 | Amgen Inc. | N-terminally chemically modified protein compositions and methods |
| WO1996041813A2 (en) | 1994-11-09 | 1996-12-27 | Offord Robin E | Functionalized polymers for site-specific attachment |
| US5738846A (en) | 1994-11-10 | 1998-04-14 | Enzon, Inc. | Interferon polymer conjugates and process for preparing the same |
| IL116085A (en) | 1994-12-16 | 1999-12-31 | Ortho Pharma Corp | Spray dried erythropoietin |
| US5932462A (en) | 1995-01-10 | 1999-08-03 | Shearwater Polymers, Inc. | Multiarmed, monofunctional, polymer for coupling to molecules and surfaces |
| AU5893696A (en) | 1995-06-07 | 1996-12-30 | Novo Nordisk A/S | Modification of polypeptides |
| US5672662A (en) | 1995-07-07 | 1997-09-30 | Shearwater Polymers, Inc. | Poly(ethylene glycol) and related polymers monosubstituted with propionic or butanoic acids and functional derivatives thereof for biotechnical applications |
| US5747639A (en) | 1996-03-06 | 1998-05-05 | Amgen Boulder Inc. | Use of hydrophobic interaction chromatography to purify polyethylene glycols |
| TW517067B (en) | 1996-05-31 | 2003-01-11 | Hoffmann La Roche | Interferon conjugates |
| EP1731174A3 (en) | 1996-08-02 | 2007-01-17 | Ortho-McNeil Pharmaceutical, Inc. | Polypeptides having a covalently bound N-terminal polyethylene glycol via hydrazone or oxime bond |
| US5980948A (en) | 1996-08-16 | 1999-11-09 | Osteotech, Inc. | Polyetherester copolymers as drug delivery matrices |
| US6214966B1 (en) | 1996-09-26 | 2001-04-10 | Shearwater Corporation | Soluble, degradable poly(ethylene glycol) derivatives for controllable release of bound molecules into solution |
| DE69800640T2 (de) | 1997-01-29 | 2001-07-05 | Polymasc Pharmaceuticals Plc, London | Pegylationsverfahren |
| EP0981548A4 (en) | 1997-04-30 | 2005-11-23 | Enzon Inc | GLYCOSYLATABLE SINGLE CHAIN ANTIGEN-BINDING PROTEINS, MANUFACTURE AND USE THEREOF |
| US5990237A (en) | 1997-05-21 | 1999-11-23 | Shearwater Polymers, Inc. | Poly(ethylene glycol) aldehyde hydrates and related polymers and applications in modifying amines |
| WO1998055500A1 (en) | 1997-06-06 | 1998-12-10 | Kyowa Hakko Kogyo Co., Ltd. | Chemically modified polypeptides |
| ATE375363T1 (de) | 1997-07-14 | 2007-10-15 | Bolder Biotechnology Inc | Derivate des wachstumshormons und verwandte proteine |
| PT1538206E (pt) | 1997-09-16 | 2010-04-12 | Centocor Ortho Biotech Inc | Método para a síntese química e construção completa de genes e genomas |
| US6129912A (en) | 1997-09-26 | 2000-10-10 | Uab Research Foundation | Polyethylene glycol-protein compositions which reduce the antigenic display of red blood cells |
| US6201072B1 (en) | 1997-10-03 | 2001-03-13 | Macromed, Inc. | Biodegradable low molecular weight triblock poly(lactide-co- glycolide) polyethylene glycol copolymers having reverse thermal gelation properties |
| US6004573A (en) | 1997-10-03 | 1999-12-21 | Macromed, Inc. | Biodegradable low molecular weight triblock poly(lactide-co-glycolide) polyethylene glycol copolymers having reverse thermal gelation properties |
| DE19748489A1 (de) | 1997-11-03 | 1999-05-06 | Roche Diagnostics Gmbh | Polyethylenglykol-derivatisierte Biomoleküle und deren Verwendung in heterogenen Nachweisverfahren |
| US6448369B1 (en) | 1997-11-06 | 2002-09-10 | Shearwater Corporation | Heterobifunctional poly(ethylene glycol) derivatives and methods for their preparation |
| US5985263A (en) | 1997-12-19 | 1999-11-16 | Enzon, Inc. | Substantially pure histidine-linked protein polymer conjugates |
| US5981709A (en) | 1997-12-19 | 1999-11-09 | Enzon, Inc. | α-interferon-polymer-conjugates having enhanced biological activity and methods of preparing the same |
| JP2002505338A (ja) | 1998-03-05 | 2002-02-19 | カイロン コーポレイション | 生物学的に活性な分子の血清半減期を増加するための方法 |
| DK1411075T3 (da) | 1998-03-12 | 2008-10-27 | Nektar Therapeutics Al Corp | Fremgangsmåde til fremstilling af polymerkonjugater |
| US6552167B1 (en) | 1998-08-28 | 2003-04-22 | Gryphon Therapeutics, Inc. | Polyamide chains of precise length |
| US6420339B1 (en) | 1998-10-14 | 2002-07-16 | Amgen Inc. | Site-directed dual pegylation of proteins for improved bioactivity and biocompatibility |
| US6451346B1 (en) | 1998-12-23 | 2002-09-17 | Amgen Inc | Biodegradable pH/thermosensitive hydrogels for sustained delivery of biologically active agents |
| US6281211B1 (en) | 1999-02-04 | 2001-08-28 | Euro-Celtique S.A. | Substituted semicarbazides and the use thereof |
| JP2002542349A (ja) | 1999-04-16 | 2002-12-10 | ダブリューエム・マーシュ・ライス・ユニバーシティー | ポリ（プロピレンフマラート）−ジアクリレートマクロマーで交差結合された生体分解性のポリ（プロピレンフマラート）ネットワーク |
| US6331539B1 (en) | 1999-06-10 | 2001-12-18 | 3M Innovative Properties Company | Sulfonamide and sulfamide substituted imidazoquinolines |
| US6756382B2 (en) | 1999-06-10 | 2004-06-29 | 3M Innovative Properties Company | Amide substituted imidazoquinolines |
| US7144574B2 (en) | 1999-08-27 | 2006-12-05 | Maxygen Aps | Interferon β variants and conjugates |
| US6348558B1 (en) | 1999-12-10 | 2002-02-19 | Shearwater Corporation | Hydrolytically degradable polymers and hydrogels made therefrom |
| AU781839B2 (en) | 1999-12-22 | 2005-06-16 | Nektar Therapeutics | Sterically hindered derivatives of water soluble polymers |
| DK1259563T4 (en) | 1999-12-22 | 2016-11-21 | Nektar Therapeutics | PROCEDURE FOR PREPARING 1-BENZOTRIAZOLYL CARBONATE ESTERS OF WATER SOLUBLE POLYMERS |
| US6413507B1 (en) | 1999-12-23 | 2002-07-02 | Shearwater Corporation | Hydrolytically degradable carbamate derivatives of poly (ethylene glycol) |
| US6646110B2 (en) | 2000-01-10 | 2003-11-11 | Maxygen Holdings Ltd. | G-CSF polypeptides and conjugates |
| WO2001062827A2 (en) | 2000-02-22 | 2001-08-30 | Shearwater Corporation | N-maleimidyl polymer derivatives |
| AU2001257577A1 (en) | 2000-02-28 | 2001-09-03 | Shearwater Corporation | Water-soluble polymer conjugates of artelinic acid |
| US6436386B1 (en) | 2000-11-14 | 2002-08-20 | Shearwater Corporation | Hydroxyapatite-targeting poly (ethylene glycol) and related polymers |
| US6667312B2 (en) | 2000-12-08 | 2003-12-23 | 3M Innovative Properties Company | Thioether substituted imidazoquinolines |
| UA75622C2 (en) | 2000-12-08 | 2006-05-15 | 3M Innovative Properties Co | Aryl ether substituted imidazoquinolines, pharmaceutical composition based thereon |
| US6677347B2 (en) | 2000-12-08 | 2004-01-13 | 3M Innovative Properties Company | Sulfonamido ether substituted imidazoquinolines |
| TW593427B (en) | 2000-12-18 | 2004-06-21 | Nektar Therapeutics Al Corp | Synthesis of high molecular weight non-peptidic polymer derivatives |
| TWI246524B (en) | 2001-01-19 | 2006-01-01 | Shearwater Corp | Multi-arm block copolymers as drug delivery vehicles |
| US7083970B2 (en) | 2001-04-19 | 2006-08-01 | The Scripps Research Institute | Methods and compositions for the production of orthogonal tRNA-aminoacyl tRNA synthetase pairs |
| US6656398B2 (en) | 2001-06-19 | 2003-12-02 | Corning Incorporated | Process of making a pattern in a film |
| US6656389B2 (en) | 2001-06-29 | 2003-12-02 | International Business Machines Corporation | Thermal paste for low temperature applications |
| US6908963B2 (en) | 2001-10-09 | 2005-06-21 | Nektar Therapeutics Al, Corporation | Thioester polymer derivatives and method of modifying the N-terminus of a polypeptide therewith |
| AU2002352524B2 (en) | 2001-11-07 | 2007-10-04 | Nektar Therapeutics | Branched polymers and their conjugates |
| US6716821B2 (en) | 2001-12-21 | 2004-04-06 | Immunogen Inc. | Cytotoxic agents bearing a reactive polyethylene glycol moiety, cytotoxic conjugates comprising polyethylene glycol linking groups, and methods of making and using the same |
| WO2003070740A1 (en) | 2002-02-15 | 2003-08-28 | The Research Foundation Of State University Of New York | RIBOZYMES WITH BROAD tRNA AMINOACYLATION ACTIVITY |
| AU2003240482B2 (en) | 2002-05-30 | 2009-03-12 | The Scripps Research Institute | Copper-catalysed ligation of azides and acetylenes |
| MXPA05006740A (es) | 2002-12-20 | 2005-10-05 | 3M Innovative Properties Co | Imidazoquinolinas arilo-sustituidas. |
| BRPI0413558A (pt) | 2003-08-12 | 2006-10-17 | 3M Innovative Properties Co | compostos contendo imidazo substituìdo por hidroxilamina |
| DK1812031T3 (en) | 2004-11-01 | 2015-09-14 | Univ California | Compositions and methods for the modification of biomolecules |
| EP1828224B1 (en) | 2004-12-22 | 2016-04-06 | Ambrx, Inc. | Compositions containing, methods involving, and uses of non-natural amino acids and polypeptides |
| TWI372629B (en) | 2005-03-18 | 2012-09-21 | Novo Nordisk As | Acylated glp-1 compounds |
| EP1939202A4 (en) * | 2005-09-22 | 2010-06-16 | Dainippon Sumitomo Pharma Co | NEW ADENINE CONNECTION |
| JP4616237B2 (ja) | 2006-11-07 | 2011-01-19 | 日本電信電話株式会社 | シリコン化合物薄膜の形成方法 |
| GB0624500D0 (en) * | 2006-12-07 | 2007-01-17 | Istituto Superiore Di Sanito | A novel passive vaccine for candida infections |
| AR065784A1 (es) * | 2007-03-20 | 2009-07-01 | Dainippon Sumitomo Pharma Co | Derivados de 8-oxo adenina,medicamentos que los contienen y usos como agentes terapeuticos para enfermedades alergicas, antivirales o antibacterianas. |
| WO2012168431A2 (en) | 2011-06-10 | 2012-12-13 | Novo Nordisk A/S | Polypeptides |
| EP2726502A1 (en) | 2011-07-01 | 2014-05-07 | Bayer Intellectual Property GmbH | Relaxin fusion polypeptides and uses thereof |
| CN112587671A (zh) * | 2012-07-18 | 2021-04-02 | 博笛生物科技有限公司 | 癌症的靶向免疫治疗 |
| EP3125943B1 (en) | 2014-04-04 | 2026-04-22 | Merck Sharp & Dohme LLC | Phosphate based linkers for intracellular delivery of drug conjugates |
| CA2874083C (en) * | 2014-12-05 | 2024-01-02 | Universite Laval | Tdp-43-binding polypeptides useful for the treatment of neurodegenerative diseases |
| TN2018000112A1 (en) * | 2015-10-29 | 2019-10-04 | Novartis Ag | Antibody conjugates comprising toll-like receptor agonist |
| JP2022500413A (ja) * | 2018-09-12 | 2022-01-04 | シルバーバック セラピューティックス インコーポレイテッド | Ｔｏｌｌ様受容体アゴニストの抗体コンジュゲート |
| JP7695885B2 (ja) * | 2019-02-12 | 2025-06-19 | アンブルックス，インコーポレイテッド | 抗体－ｔｌｒアゴニストコンジュゲートを含有する組成物、その方法、及び使用 |
-
2021
- 2021-08-20 EP EP21772883.1A patent/EP4199968A1/en active Pending
- 2021-08-20 KR KR1020237009263A patent/KR20230073200A/ko active Pending
- 2021-08-20 US US18/022,099 patent/US20230302150A1/en active Pending
- 2021-08-20 WO PCT/US2021/047009 patent/WO2022040596A1/en not_active Ceased
- 2021-08-20 TW TW110130967A patent/TW202227449A/zh unknown
- 2021-08-20 JP JP2023511915A patent/JP2023538071A/ja active Pending
- 2021-08-20 AU AU2021327396A patent/AU2021327396A1/en active Pending
- 2021-08-20 CA CA3190606A patent/CA3190606A1/en active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| IL323631A (en) | Compositions containing, methods and uses of antibody-TLR agonist conjugates | |
| CN113766954B (zh) | 喜树碱衍生物 | |
| TW202308700A (zh) | 抗體偶聯藥物的製備方法及應用 | |
| WO2023131219A1 (en) | Conjugates, compositions and methods of use | |
| JP2023099069A (ja) | Ｔｌｒ７／８アゴニスト化合物の切断可能なコンジュゲート、その調製方法および使用 | |
| KR20230008723A (ko) | 전하 변이체 링커 | |
| JP2021113191A (ja) | メイタンシノイド誘導体、そのコンジュゲート、及び使用方法 | |
| JP2024512986A (ja) | 改良された物理化学的特性および薬理学的特性を有する酵素トリガー自己反応性リンカー | |
| CN106267225B (zh) | 三马来酰亚胺型连接子及其应用 | |
| CN103566377A (zh) | 癌症的靶向免疫治疗 | |
| KR20240015670A (ko) | 안트라사이클린 항체 접합체 | |
| TW202227449A (zh) | 抗體－ｔｌｒ促效劑偶聯物、其方法及用途 | |
| JPWO2020168017A5 (https=) | ||
| JP7811217B2 (ja) | 抗ｈｅｒ２抗体－免疫アゴニストコンジュゲート及びその使用 | |
| TW201838657A (zh) | 具有自分解肽連接子之類美登素衍生物及其結合物 | |
| JP2022541517A (ja) | 抗体－ｓｔｉｎｇアゴニスト複合体および免疫療法におけるそれらの使用 | |
| US20200061079A1 (en) | Isoquinolidinobenzodiazepine (iqb)-1(chloromethyl)-2,3-dihydro-1h-benzo[e]indole (cbi) dimers | |
| JPWO2022040596A5 (https=) | ||
| KR20190039570A (ko) | 세코-시클로프로파피롤로인돌 화합물, 그의 항체-약물 접합체, 및 제조 및 사용 방법 | |
| CN116457023A (zh) | 抗体-tlr激动剂缀合物、方法及其用途 | |
| WO2024207177A1 (en) | Antibody, linkers, payload, conjugates and applications thereof | |
| WO2024075764A1 (ja) | 抗体薬物複合体の製造方法及びそれに用いる酵素 | |
| CN115003679A (zh) | 酞菁染料与抗体或肽的缀合物 | |
| NZ778565B2 (en) | Compositions containing, methods and uses of antibody-tlr agonist conjugates | |
| WO2026051926A1 (zh) | 一种基于依喜替康的抗体-药物偶联物及其制备方法和用途 |