JPWO2020141460A5 - - Google Patents
Download PDFInfo
- Publication number
- JPWO2020141460A5 JPWO2020141460A5 JP2021538388A JP2021538388A JPWO2020141460A5 JP WO2020141460 A5 JPWO2020141460 A5 JP WO2020141460A5 JP 2021538388 A JP2021538388 A JP 2021538388A JP 2021538388 A JP2021538388 A JP 2021538388A JP WO2020141460 A5 JPWO2020141460 A5 JP WO2020141460A5
- Authority
- JP
- Japan
- Prior art keywords
- independently
- integer
- value
- conjugate
- alkyl
- 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
- 108090001123 antibodies Proteins 0.000 claims description 48
- 102000004965 antibodies Human genes 0.000 claims description 48
- 229910052739 hydrogen Inorganic materials 0.000 claims description 48
- 239000001257 hydrogen Substances 0.000 claims description 48
- 125000000217 alkyl group Chemical group 0.000 claims description 47
- 150000001875 compounds Chemical class 0.000 claims description 42
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 29
- 125000005647 linker group Chemical group 0.000 claims description 27
- 201000011510 cancer Diseases 0.000 claims description 26
- 239000003795 chemical substances by application Substances 0.000 claims description 26
- 210000004027 cells Anatomy 0.000 claims description 24
- 229920001184 polypeptide Polymers 0.000 claims description 24
- 229910052760 oxygen Inorganic materials 0.000 claims description 22
- 125000001072 heteroaryl group Chemical group 0.000 claims description 20
- 125000005418 aryl aryl group Chemical group 0.000 claims description 18
- -1 cetolizumab pegol Proteins 0.000 claims description 18
- 201000010099 disease Diseases 0.000 claims description 18
- 229910052757 nitrogen Inorganic materials 0.000 claims description 18
- 150000003839 salts Chemical class 0.000 claims description 17
- 239000011780 sodium chloride Substances 0.000 claims description 17
- 102000018358 Immunoglobulins Human genes 0.000 claims description 16
- 108060003951 Immunoglobulins Proteins 0.000 claims description 16
- 230000000890 antigenic Effects 0.000 claims description 16
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims description 16
- 125000004430 oxygen atoms Chemical group O* 0.000 claims description 16
- 125000004434 sulfur atoms Chemical group 0.000 claims description 16
- 150000002431 hydrogen Chemical class 0.000 claims description 15
- 239000000203 mixture Substances 0.000 claims description 15
- 125000004429 atoms Chemical group 0.000 claims description 14
- 125000005842 heteroatoms Chemical group 0.000 claims description 14
- 108010038807 Oligopeptides Proteins 0.000 claims description 12
- 102000015636 Oligopeptides Human genes 0.000 claims description 12
- 125000002877 alkyl aryl group Chemical group 0.000 claims description 12
- 238000003776 cleavage reaction Methods 0.000 claims description 12
- 230000001809 detectable Effects 0.000 claims description 12
- 108020004707 nucleic acids Proteins 0.000 claims description 12
- 150000007523 nucleic acids Chemical class 0.000 claims description 12
- 102000004169 proteins and genes Human genes 0.000 claims description 12
- 108090000623 proteins and genes Proteins 0.000 claims description 12
- 239000003814 drug Substances 0.000 claims description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims description 10
- 230000002062 proliferating Effects 0.000 claims description 9
- 229940072221 IMMUNOGLOBULINS Drugs 0.000 claims description 8
- 125000004350 aryl cycloalkyl group Chemical group 0.000 claims description 8
- 229920001222 biopolymer Polymers 0.000 claims description 8
- 239000002738 chelating agent Substances 0.000 claims description 8
- 125000006448 cycloalkyl cycloalkyl group Chemical group 0.000 claims description 8
- 229940079593 drugs Drugs 0.000 claims description 8
- 125000005349 heteroarylcycloalkyl group Chemical group 0.000 claims description 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 8
- 239000002245 particle Substances 0.000 claims description 8
- OZAIFHULBGXAKX-UHFFFAOYSA-N precursor Substances N#CC(C)(C)N=NC(C)(C)C#N OZAIFHULBGXAKX-UHFFFAOYSA-N 0.000 claims description 8
- 239000007787 solid Substances 0.000 claims description 8
- 230000003381 solubilizing Effects 0.000 claims description 8
- 230000000087 stabilizing Effects 0.000 claims description 8
- 125000003118 aryl group Chemical group 0.000 claims description 7
- 230000001939 inductive effect Effects 0.000 claims description 7
- 206010003816 Autoimmune disease Diseases 0.000 claims description 6
- 125000003275 alpha amino acid group Chemical group 0.000 claims description 6
- 125000004432 carbon atoms Chemical group C* 0.000 claims description 6
- 201000009030 carcinoma Diseases 0.000 claims description 6
- 239000000126 substance Substances 0.000 claims description 6
- 229910052717 sulfur Inorganic materials 0.000 claims description 6
- 206010024324 Leukaemias Diseases 0.000 claims description 5
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 5
- 206010025323 Lymphomas Diseases 0.000 claims description 5
- 206010025310 Other lymphomas Diseases 0.000 claims description 5
- 206010039491 Sarcoma Diseases 0.000 claims description 5
- 201000000053 blastoma Diseases 0.000 claims description 5
- 201000008184 embryoma Diseases 0.000 claims description 5
- 230000036210 malignancy Effects 0.000 claims description 5
- 125000001624 naphthyl group Chemical group 0.000 claims description 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 5
- 125000001424 substituent group Chemical group 0.000 claims description 5
- 150000003461 sulfonyl halides Chemical class 0.000 claims description 5
- PMOOKBAYUNEHOF-IKHMJLPLSA-N (2S,3S,4S,5R,6R)-6-[[(4aR,6aR,6bS,8aS,14aR,14bR)-8a-carboxy-4,4,6a,6b,11,11,14b-heptamethyl-1,2,3,4a,5,6,7,8,9,10,12,13,14,14a-tetradecahydropicen-3-yl]oxy]-3,5-dihydroxy-4-[(1R,2R,3S,4R)-2,3,4-trihydroxycyclohexyl]oxyoxane-2-carboxylic acid Chemical compound O([C@H]1[C@H](O)[C@H](O[C@H]([C@@H]1O)OC1CC[C@]2(C)[C@H]3CCC=4[C@@]([C@@]3(CC[C@H]2C1(C)C)C)(C)CC[C@]1(CCC(CC1=4)(C)C)C(O)=O)C(O)=O)[C@@H]1CC[C@@H](O)[C@H](O)[C@H]1O PMOOKBAYUNEHOF-IKHMJLPLSA-N 0.000 claims description 4
- WUWDLXZGHZSWQZ-WQLSENKSSA-N (3Z)-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-1H-indol-2-one Chemical compound N1C(C)=CC(C)=C1\C=C/1C2=CC=CC=C2NC\1=O WUWDLXZGHZSWQZ-WQLSENKSSA-N 0.000 claims description 4
- RTQWWZBSTRGEAV-PKHIMPSTSA-N 2-[[(2S)-2-[bis(carboxymethyl)amino]-3-[4-(methylcarbamoylamino)phenyl]propyl]-[2-[bis(carboxymethyl)amino]propyl]amino]acetic acid Chemical compound CNC(=O)NC1=CC=C(C[C@@H](CN(CC(C)N(CC(O)=O)CC(O)=O)CC(O)=O)N(CC(O)=O)CC(O)=O)C=C1 RTQWWZBSTRGEAV-PKHIMPSTSA-N 0.000 claims description 4
- 108010004463 Abciximab Proteins 0.000 claims description 4
- 108010007562 Adalimumab Proteins 0.000 claims description 4
- 108010090726 Alefacept Proteins 0.000 claims description 4
- 108010090838 Alemtuzumab Proteins 0.000 claims description 4
- 108010067213 Basiliximab Proteins 0.000 claims description 4
- 108010005144 Bevacizumab Proteins 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 108010022830 Cetuximab Proteins 0.000 claims description 4
- 108010084740 Daclizumab Proteins 0.000 claims description 4
- 108010008165 Etanercept Proteins 0.000 claims description 4
- 229960003297 Gemtuzumab ozogamicin Drugs 0.000 claims description 4
- 229940022353 Herceptin Drugs 0.000 claims description 4
- 229940088597 Hormone Drugs 0.000 claims description 4
- RAXXELZNTBOGNW-UHFFFAOYSA-N Imidazole Chemical compound C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims description 4
- 108010053490 Infliximab Proteins 0.000 claims description 4
- DEFJQIDDEAULHB-IMJSIDKUSA-N L-alanyl-L-alanine Chemical compound C[C@H](N)C(=O)N[C@@H](C)C(O)=O DEFJQIDDEAULHB-IMJSIDKUSA-N 0.000 claims description 4
- 101710010909 MS4A1 Proteins 0.000 claims description 4
- 102100000165 MS4A1 Human genes 0.000 claims description 4
- 229960001521 Motavizumab Drugs 0.000 claims description 4
- 108090000393 Muromonab-CD3 Proteins 0.000 claims description 4
- 229960003816 Muromonab-CD3 Drugs 0.000 claims description 4
- 108010035649 Natalizumab Proteins 0.000 claims description 4
- 229920000272 Oligonucleotide Polymers 0.000 claims description 4
- 108010029597 Omalizumab Proteins 0.000 claims description 4
- 229960000470 Omalizumab Drugs 0.000 claims description 4
- 108010019613 Palivizumab Proteins 0.000 claims description 4
- 108010061219 Panitumumab Proteins 0.000 claims description 4
- 108010062724 Ranibizumab Proteins 0.000 claims description 4
- 229960003876 Ranibizumab Drugs 0.000 claims description 4
- 108010001645 Rituximab Proteins 0.000 claims description 4
- 108010070144 Single-Chain Antibodies Proteins 0.000 claims description 4
- 102000005632 Single-Chain Antibodies Human genes 0.000 claims description 4
- 108010032100 TACI receptor-IgG Fc fragment fusion protein Proteins 0.000 claims description 4
- 101710037530 TRX4 Proteins 0.000 claims description 4
- 231100000765 Toxin Toxicity 0.000 claims description 4
- 108010010691 Trastuzumab Proteins 0.000 claims description 4
- 229950007217 Tremelimumab Drugs 0.000 claims description 4
- 229950000815 Veltuzumab Drugs 0.000 claims description 4
- 229960000446 abciximab Drugs 0.000 claims description 4
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims description 4
- 229960002964 adalimumab Drugs 0.000 claims description 4
- 108010056243 alanylalanine Proteins 0.000 claims description 4
- 229960002459 alefacept Drugs 0.000 claims description 4
- 229960000548 alemtuzumab Drugs 0.000 claims description 4
- 125000002947 alkylene group Chemical group 0.000 claims description 4
- 239000003242 anti bacterial agent Substances 0.000 claims description 4
- 239000003429 antifungal agent Substances 0.000 claims description 4
- 239000000427 antigen Substances 0.000 claims description 4
- 102000038129 antigens Human genes 0.000 claims description 4
- 108091007172 antigens Proteins 0.000 claims description 4
- 239000002246 antineoplastic agent Substances 0.000 claims description 4
- 239000003096 antiparasitic agent Substances 0.000 claims description 4
- 239000003443 antiviral agent Substances 0.000 claims description 4
- 229960004669 basiliximab Drugs 0.000 claims description 4
- 108010051561 belimumab Proteins 0.000 claims description 4
- 229960003270 belimumab Drugs 0.000 claims description 4
- 229960000397 bevacizumab Drugs 0.000 claims description 4
- 230000027455 binding Effects 0.000 claims description 4
- 239000003124 biologic agent Substances 0.000 claims description 4
- 229960000419 catumaxomab Drugs 0.000 claims description 4
- 108090000758 catumaxomab Proteins 0.000 claims description 4
- 229960005395 cetuximab Drugs 0.000 claims description 4
- 108091006028 chimera Proteins 0.000 claims description 4
- 229960002806 daclizumab Drugs 0.000 claims description 4
- 108010063231 eculizumab Proteins 0.000 claims description 4
- 229960002224 eculizumab Drugs 0.000 claims description 4
- 108010010371 efalizumab Proteins 0.000 claims description 4
- 229960000284 efalizumab Drugs 0.000 claims description 4
- 108040009258 epidermal growth factor-activated receptor activity proteins Proteins 0.000 claims description 4
- 102000017256 epidermal growth factor-activated receptor activity proteins Human genes 0.000 claims description 4
- 229960000403 etanercept Drugs 0.000 claims description 4
- 125000000524 functional group Chemical group 0.000 claims description 4
- 108020001507 fusion proteins Proteins 0.000 claims description 4
- 102000037240 fusion proteins Human genes 0.000 claims description 4
- 229910052736 halogen Inorganic materials 0.000 claims description 4
- 150000002367 halogens Chemical class 0.000 claims description 4
- 239000005556 hormone Substances 0.000 claims description 4
- 229960001001 ibritumomab tiuxetan Drugs 0.000 claims description 4
- 108010061572 ibritumomab tiuxetan Proteins 0.000 claims description 4
- 238000003384 imaging method Methods 0.000 claims description 4
- 230000002519 immonomodulatory Effects 0.000 claims description 4
- 229960000598 infliximab Drugs 0.000 claims description 4
- 239000003446 ligand Substances 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 108010062313 mepolizumab Proteins 0.000 claims description 4
- 229960005108 mepolizumab Drugs 0.000 claims description 4
- 108010045030 monoclonal antibodies Proteins 0.000 claims description 4
- 102000005614 monoclonal antibodies Human genes 0.000 claims description 4
- 108010008564 motavizumab Proteins 0.000 claims description 4
- 239000002105 nanoparticle Substances 0.000 claims description 4
- 229960005027 natalizumab Drugs 0.000 claims description 4
- 229960000402 palivizumab Drugs 0.000 claims description 4
- 229960001972 panitumumab Drugs 0.000 claims description 4
- 108010042024 pertuzumab Proteins 0.000 claims description 4
- 229960002087 pertuzumab Drugs 0.000 claims description 4
- 108091008117 polyclonal antibodies Proteins 0.000 claims description 4
- 108010046141 rilonacept Proteins 0.000 claims description 4
- 229960001886 rilonacept Drugs 0.000 claims description 4
- 229960004641 rituximab Drugs 0.000 claims description 4
- 108010017584 romiplostim Proteins 0.000 claims description 4
- 229960004262 romiplostim Drugs 0.000 claims description 4
- 239000000523 sample Substances 0.000 claims description 4
- 108010078548 tocilizumab Proteins 0.000 claims description 4
- 229960003989 tocilizumab Drugs 0.000 claims description 4
- 239000003053 toxin Substances 0.000 claims description 4
- 229960000575 trastuzumab Drugs 0.000 claims description 4
- 108010072993 tremelimumab Proteins 0.000 claims description 4
- 125000005559 triazolylene group Chemical group 0.000 claims description 4
- 108010063727 veltuzumab Proteins 0.000 claims description 4
- 206010003210 Arteriosclerosis Diseases 0.000 claims description 3
- 208000006673 Asthma Diseases 0.000 claims description 3
- 206010011401 Crohn's disease Diseases 0.000 claims description 3
- 206010018651 Graft versus host disease Diseases 0.000 claims description 3
- 208000009329 Graft vs Host Disease Diseases 0.000 claims description 3
- 206010028417 Myasthenia gravis Diseases 0.000 claims description 3
- 206010028980 Neoplasm Diseases 0.000 claims description 3
- 208000003154 Papilloma Diseases 0.000 claims description 3
- 206010039073 Rheumatoid arthritis Diseases 0.000 claims description 3
- 241000580858 Simian-Human immunodeficiency virus Species 0.000 claims description 3
- 206010047461 Viral infection Diseases 0.000 claims description 3
- 208000001756 Virus Disease Diseases 0.000 claims description 3
- 229960002833 aflibercept Drugs 0.000 claims description 3
- 108010081667 aflibercept Proteins 0.000 claims description 3
- 201000001320 atherosclerosis Diseases 0.000 claims description 3
- 201000009596 autoimmune hypersensitivity disease Diseases 0.000 claims description 3
- 230000001684 chronic Effects 0.000 claims description 3
- 238000001514 detection method Methods 0.000 claims description 3
- 201000009910 diseases by infectious agent Diseases 0.000 claims description 3
- 230000003463 hyperproliferative Effects 0.000 claims description 3
- 230000004968 inflammatory condition Effects 0.000 claims description 3
- 239000000463 material Substances 0.000 claims description 3
- 201000008482 osteoarthritis Diseases 0.000 claims description 3
- 201000004681 psoriasis Diseases 0.000 claims description 3
- 201000010874 syndrome Diseases 0.000 claims description 3
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims description 3
- 210000004881 tumor cells Anatomy 0.000 claims description 3
- 230000017613 viral reproduction Effects 0.000 claims description 3
- MCTWTZJPVLRJOU-UHFFFAOYSA-O 1-Methylimidazole Chemical compound CN1C=C[NH+]=C1 MCTWTZJPVLRJOU-UHFFFAOYSA-O 0.000 claims description 2
- 230000002378 acidificating Effects 0.000 claims description 2
- 230000003213 activating Effects 0.000 claims description 2
- 125000000539 amino acid group Chemical group 0.000 claims description 2
- 238000006243 chemical reaction Methods 0.000 claims description 2
- 239000003153 chemical reaction reagent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000002255 enzymatic Effects 0.000 claims description 2
- 125000005549 heteroarylene group Chemical group 0.000 claims description 2
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims description 2
- 230000001590 oxidative Effects 0.000 claims description 2
- 239000000546 pharmaceutic aid Substances 0.000 claims description 2
- 239000003638 reducing agent Substances 0.000 claims description 2
- 150000003852 triazoles Chemical class 0.000 claims description 2
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000006737 (C6-C20) arylalkyl group Chemical group 0.000 claims 1
- 239000012190 activator Substances 0.000 claims 1
- 239000012434 nucleophilic reagent Substances 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- HAXFWIACAGNFHA-UHFFFAOYSA-N 2,2'-Dipyridyldisulfide Chemical compound C=1C=CC=NC=1SSC1=CC=CC=N1 HAXFWIACAGNFHA-UHFFFAOYSA-N 0.000 description 3
- 150000003923 2,5-pyrrolediones Chemical class 0.000 description 3
- 108090000695 Cytokines Proteins 0.000 description 3
- 102000004127 Cytokines Human genes 0.000 description 3
- 108010027059 Inotuzumab Ozogamicin Proteins 0.000 description 3
- 229950004101 Inotuzumab ozogamicin Drugs 0.000 description 3
- 229950007283 Oregovomab Drugs 0.000 description 3
- 206010041823 Squamous cell carcinoma Diseases 0.000 description 3
- 150000001299 aldehydes Chemical class 0.000 description 3
- 150000001336 alkenes Chemical class 0.000 description 3
- 125000003545 alkoxy group Chemical group 0.000 description 3
- IVRMZWNICZWHMI-UHFFFAOYSA-N azide Chemical compound [N-]=[N+]=[N-] IVRMZWNICZWHMI-UHFFFAOYSA-N 0.000 description 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 3
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 3
- XFXPMWWXUTWYJX-UHFFFAOYSA-N cyanide Chemical compound N#[C-] XFXPMWWXUTWYJX-UHFFFAOYSA-N 0.000 description 3
- 150000001993 dienes Chemical class 0.000 description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-M dihydrogenphosphate Chemical compound OP(O)([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-M 0.000 description 3
- 125000005677 ethinylene group Chemical group [*:2]C#C[*:1] 0.000 description 3
- 150000004820 halides Chemical class 0.000 description 3
- 125000001475 halogen functional group Chemical group 0.000 description 3
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 3
- 150000002576 ketones Chemical class 0.000 description 3
- 201000007270 liver cancer Diseases 0.000 description 3
- 125000006502 nitrobenzyl group Chemical group 0.000 description 3
- 108010060422 oregovomab Proteins 0.000 description 3
- ABLZXFCXXLZCGV-UHFFFAOYSA-N phosphorous acid Chemical compound OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 description 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 3
- 150000003871 sulfonates Chemical class 0.000 description 3
- LSNNMFCWUKXFEE-UHFFFAOYSA-N sulfonic acid Chemical compound OS(O)=O LSNNMFCWUKXFEE-UHFFFAOYSA-N 0.000 description 3
- 125000005490 tosylate group Chemical group 0.000 description 3
- 206010008342 Cervix carcinoma Diseases 0.000 description 2
- 206010017758 Gastric cancer Diseases 0.000 description 2
- 206010073071 Hepatocellular carcinoma Diseases 0.000 description 2
- 206010038389 Renal cancer Diseases 0.000 description 2
- 201000010881 cervical cancer Diseases 0.000 description 2
- 201000010982 kidney cancer Diseases 0.000 description 2
- 201000011549 stomach cancer Diseases 0.000 description 2
- 206010000830 Acute leukaemia Diseases 0.000 description 1
- 208000009956 Adenocarcinoma Diseases 0.000 description 1
- 206010061424 Anal cancer Diseases 0.000 description 1
- 206010005003 Bladder cancer Diseases 0.000 description 1
- 210000004556 Brain Anatomy 0.000 description 1
- 206010009944 Colon cancer Diseases 0.000 description 1
- 206010014733 Endometrial cancer Diseases 0.000 description 1
- 208000005017 Glioblastoma Diseases 0.000 description 1
- 210000004072 Lung Anatomy 0.000 description 1
- 206010061269 Malignant peritoneal neoplasm Diseases 0.000 description 1
- 208000002154 Non-Small-Cell Lung Carcinoma Diseases 0.000 description 1
- 108009000071 Non-small cell lung cancer Proteins 0.000 description 1
- 206010033128 Ovarian cancer Diseases 0.000 description 1
- 208000008443 Pancreatic Carcinoma Diseases 0.000 description 1
- 206010034299 Penile cancer Diseases 0.000 description 1
- 206010060862 Prostate cancer Diseases 0.000 description 1
- 206010038038 Rectal cancer Diseases 0.000 description 1
- 206010061934 Salivary gland cancer Diseases 0.000 description 1
- 208000000587 Small Cell Lung Carcinoma Diseases 0.000 description 1
- 206010041067 Small cell lung cancer Diseases 0.000 description 1
- 210000002784 Stomach Anatomy 0.000 description 1
- 206010046766 Uterine cancer Diseases 0.000 description 1
- 206010047741 Vulval cancer Diseases 0.000 description 1
- 201000011165 anus cancer Diseases 0.000 description 1
- 201000011231 colorectal cancer Diseases 0.000 description 1
- 230000002496 gastric Effects 0.000 description 1
- 230000002440 hepatic Effects 0.000 description 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 201000005296 lung carcinoma Diseases 0.000 description 1
- 201000005244 lung non-small cell carcinoma Diseases 0.000 description 1
- 230000000269 nucleophilic Effects 0.000 description 1
- 201000002528 pancreatic cancer Diseases 0.000 description 1
- 201000002524 peritoneal carcinoma Diseases 0.000 description 1
- 201000001275 rectum cancer Diseases 0.000 description 1
- 201000002510 thyroid cancer Diseases 0.000 description 1
- 201000005112 urinary bladder cancer Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962788039P | 2019-01-03 | 2019-01-03 | |
| US62/788,039 | 2019-01-03 | ||
| PCT/IB2020/000019 WO2020141460A2 (en) | 2019-01-03 | 2020-01-02 | Compounds comprising cleavable linker and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2022515885A JP2022515885A (ja) | 2022-02-22 |
| JPWO2020141460A5 true JPWO2020141460A5 (ru) | 2023-01-19 |
Family
ID=71407384
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021538388A Pending JP2022515885A (ja) | 2019-01-03 | 2020-01-02 | 切断可能なリンカーを含む化合物及びその使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20210393795A1 (ru) |
| EP (1) | EP3906063A4 (ru) |
| JP (1) | JP2022515885A (ru) |
| KR (1) | KR20210099658A (ru) |
| CN (2) | CN114306635A (ru) |
| EA (1) | EA202191855A1 (ru) |
| WO (1) | WO2020141460A2 (ru) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111278845A (zh) | 2017-07-04 | 2020-06-12 | 尹图赛利有限公司 | 包含可裂解接头的化合物及其用途 |
| KR20230031981A (ko) | 2019-05-14 | 2023-03-07 | 프로벤션 바이오, 인코포레이티드 | 제1형 당뇨병을 예방하기 위한 방법 및 조성물 |
| MX2022015872A (es) | 2020-06-11 | 2023-05-16 | Provention Bio Inc | Metodos y composiciones para prevenir diabetes tipo 1. |
| CN114874287B (zh) * | 2022-05-20 | 2024-04-02 | 联宁（苏州）生物制药有限公司 | 一种抗体偶联药物-连接子lnd1042的合成方法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3041736B2 (ja) * | 1991-11-01 | 2000-05-15 | コニカ株式会社 | ハロゲン化銀写真感光材料 |
| JP2005291974A (ja) * | 2004-03-31 | 2005-10-20 | Kyocera Chemical Corp | フェルダジル基を有する磁性有機粒子、粒子固定方法及びマイクロアレイ |
| CN105899539B (zh) * | 2014-01-10 | 2021-11-09 | 博笛生物科技有限公司 | 用于免疫疗法的化合物和组合物 |
| KR101628872B1 (ko) * | 2014-05-28 | 2016-06-09 | 주식회사 레고켐 바이오사이언스 | 자가-희생 기를 포함하는 화합물 |
| WO2018124758A2 (ko) * | 2016-12-28 | 2018-07-05 | 주식회사 인투셀 | 베타-갈락토사이드가 도입된 자가-희생 기를 포함하는 화합물 |
| CN111278845A (zh) * | 2017-07-04 | 2020-06-12 | 尹图赛利有限公司 | 包含可裂解接头的化合物及其用途 |
-
2020
- 2020-01-02 EP EP20735849.0A patent/EP3906063A4/en active Pending
- 2020-01-02 US US17/419,435 patent/US20210393795A1/en active Pending
- 2020-01-02 CN CN202111628316.1A patent/CN114306635A/zh active Pending
- 2020-01-02 WO PCT/IB2020/000019 patent/WO2020141460A2/en unknown
- 2020-01-02 CN CN202080007805.2A patent/CN113423431A/zh active Pending
- 2020-01-02 JP JP2021538388A patent/JP2022515885A/ja active Pending
- 2020-01-02 EA EA202191855A patent/EA202191855A1/ru unknown
- 2020-01-02 KR KR1020217024209A patent/KR20210099658A/ko unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2020527599A5 (ru) | ||
| TWI715611B (zh) | 抗體藥物偶聯物的共價鍵連接子及其製備方法與應用 | |
| CN114456186B (zh) | 一种喜树碱类衍生物及其配体-药物偶联物 | |
| FI105155B (fi) | Menetelmä terapeuttisesti käyttökelpoisten sappihappojohdannaisten valmistamiseksi | |
| KR20200041914A (ko) | 면역자극제 톨-유사 수용체 7 (tlr7) 효능제로서의 6-아미노-7,9-디히드로-8h-퓨린-8-온 유도체 | |
| KR20200041913A (ko) | 면역자극제로서 톨-유사 수용체 7 (tlr7) 효능제로서의 6-아미노-7,9-디히드로-8h-퓨린-8-온 유도체 | |
| JP7393810B2 (ja) | 部位特異的抗体コンジュゲーション及びその具体例としての抗体－薬物コンジュゲート | |
| JP2017531028A5 (ru) | ||
| KR102014383B1 (ko) | G 단백질 연결 수용체의 활성 조절 인간 항체 | |
| CN113456829A (zh) | 新型亲水连接体和其在配体-药物共轭偶联物上的应用 | |
| JP2023541969A (ja) | 可溶性タグを有する分子および関連方法 | |
| US20160220711A1 (en) | Methods and compositions for tumor vasculature imaging and targeted therapy | |
| JPWO2020141460A5 (ru) | ||
| KR20230154892A (ko) | 항-her2 항체-약물 접합체 및 이의 용도 | |
| JPWO2020141459A5 (ru) | ||
| Calce et al. | HER2-mediated anticancer drug delivery: strategies to prepare targeting ligands highly specific for the receptor | |
| CN111643676A (zh) | 一种双特异性二聚体、双特异性二聚体-药物偶联物及其应用 | |
| RU2020104697A (ru) | Соединения, содержащие расщепляемый линкер, и способы их применения | |
| CA2547435A1 (en) | Targeting of erb antigens | |
| Coyne et al. | Synthesis of gemcitabine-(C4-amide)-[anti-HER2/neu] utilizing a UV-photoactivated gemcitabine intermediate: cytotoxic anti-Neoplastic activity against chemotherapeutic-resistant mammary adenocarcinoma SKBr-3 | |
| US10114014B2 (en) | Macromolecular conjugates for isolation, immobilization and visualization of proteins | |
| KR20190097745A (ko) | G 단백질 연결 수용체의 일종인 리소포스파티딕산 수용체2 특이적 인간 항체 | |
| Martin | The development of disulphide-bridging chemistry for the generation of antibody-protein conjugates | |
| WO2023178641A1 (zh) | 一种dna毒性二聚体化合物及其偶联物 | |
| TW202304920A (zh) | 一種dna毒性二聚體化合物及其偶聯物 |