JP2017535246A5 - - Google Patents

Info

Publication number

JP2017535246A5

JP2017535246A5 JP2017512808A JP2017512808A JP2017535246A5 JP 2017535246 A5 JP2017535246 A5 JP 2017535246A5 JP 2017512808 A JP2017512808 A JP 2017512808A JP 2017512808 A JP2017512808 A JP 2017512808A JP 2017535246 A5 JP2017535246 A5 JP 2017535246A5

Authority

JP

Japan

Prior art keywords

seq

amino acid

acid sequence

set forth

sequence set

Prior art date

2015-09-04

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

• Espacenet
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• 150000001413 amino acids Chemical group 0.000 claims 114
• 239000000611 antibody drug conjugate Substances 0.000 claims 17
• 229940049595 antibody-drug conjugate Drugs 0.000 claims 17
• 206010028980 Neoplasm Diseases 0.000 claims 13
• 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims 12
• 201000011510 cancer Diseases 0.000 claims 11
• 210000004027 cell Anatomy 0.000 claims 11
• 239000008194 pharmaceutical composition Substances 0.000 claims 11
• 108010047041 Complementarity Determining Regions Proteins 0.000 claims 8
• 229940127089 cytotoxic agent Drugs 0.000 claims 7
• 239000002254 cytotoxic agent Substances 0.000 claims 7
• 231100000599 cytotoxic agent Toxicity 0.000 claims 7
• 238000000034 method Methods 0.000 claims 7
• 101000798109 Homo sapiens Melanotransferrin Proteins 0.000 claims 6
• 102100032239 Melanotransferrin Human genes 0.000 claims 6
• 208000000453 Skin Neoplasms Diseases 0.000 claims 5
• 239000003814 drug Substances 0.000 claims 5
• 201000000849 skin cancer Diseases 0.000 claims 5
• 101000984753 Homo sapiens Serine/threonine-protein kinase B-raf Proteins 0.000 claims 4
• 102100027103 Serine/threonine-protein kinase B-raf Human genes 0.000 claims 4
• YUOCYTRGANSSRY-UHFFFAOYSA-N pyrrolo[2,3-i][1,2]benzodiazepine Chemical compound C1=CN=NC2=C3C=CN=C3C=CC2=C1 YUOCYTRGANSSRY-UHFFFAOYSA-N 0.000 claims 4
• 210000005102 tumor initiating cell Anatomy 0.000 claims 4
• 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims 3
• 229940079593 drug Drugs 0.000 claims 3
• 238000000338 in vitro Methods 0.000 claims 3
• 102000039446 nucleic acids Human genes 0.000 claims 3
• 108020004707 nucleic acids Proteins 0.000 claims 3
• 150000007523 nucleic acids Chemical class 0.000 claims 3
• 208000022679 triple-negative breast carcinoma Diseases 0.000 claims 3
• 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims 2
• 108010027164 Amanitins Proteins 0.000 claims 2
• 206010006187 Breast cancer Diseases 0.000 claims 2
• 208000026310 Breast neoplasm Diseases 0.000 claims 2
• 206010009944 Colon cancer Diseases 0.000 claims 2
• 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
• 101100261262 Homo sapiens MELTF gene Proteins 0.000 claims 2
• 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
• 206010027480 Metastatic malignant melanoma Diseases 0.000 claims 2
• CIORWBWIBBPXCG-JZTFPUPKSA-N amanitin Chemical compound O=C1N[C@@H](CC(N)=O)C(=O)N2CC(O)C[C@H]2C(=O)N[C@@H](C(C)[C@@H](O)CO)C(=O)N[C@@H](C2)C(=O)NCC(=O)N[C@@H](C(C)CC)C(=O)NCC(=O)N[C@H]1CS(=O)C1=C2C2=CC=C(O)C=C2N1 CIORWBWIBBPXCG-JZTFPUPKSA-N 0.000 claims 2
• 235000001014 amino acid Nutrition 0.000 claims 2
• 108010044540 auristatin Proteins 0.000 claims 2
• HXCHCVDVKSCDHU-LULTVBGHSA-N calicheamicin Chemical compound C1[C@H](OC)[C@@H](NCC)CO[C@H]1O[C@H]1[C@H](O[C@@H]2C\3=C(NC(=O)OC)C(=O)C[C@](C/3=C/CSSSC)(O)C#C\C=C/C#C2)O[C@H](C)[C@@H](NO[C@@H]2O[C@H](C)[C@@H](SC(=O)C=3C(=C(OC)C(O[C@H]4[C@@H]([C@H](OC)[C@@H](O)[C@H](C)O4)O)=C(I)C=3C)OC)[C@@H](O)C2)[C@@H]1O HXCHCVDVKSCDHU-LULTVBGHSA-N 0.000 claims 2
• 229930195731 calicheamicin Natural products 0.000 claims 2
• 239000003638 chemical reducing agent Substances 0.000 claims 2
• 230000037430 deletion Effects 0.000 claims 2
• 238000012217 deletion Methods 0.000 claims 2
• AMRJKAQTDDKMCE-UHFFFAOYSA-N dolastatin Chemical group CC(C)C(N(C)C)C(=O)NC(C(C)C)C(=O)N(C)C(C(C)C)C(OC)CC(=O)N1CCCC1C(OC)C(C)C(=O)NC(C=1SC=CN=1)CC1=CC=CC=C1 AMRJKAQTDDKMCE-UHFFFAOYSA-N 0.000 claims 2
• 229930188854 dolastatin Natural products 0.000 claims 2
• 239000003937 drug carrier Substances 0.000 claims 2
• VQNATVDKACXKTF-XELLLNAOSA-N duocarmycin Chemical compound COC1=C(OC)C(OC)=C2NC(C(=O)N3C4=CC(=O)C5=C([C@@]64C[C@@H]6C3)C=C(N5)C(=O)OC)=CC2=C1 VQNATVDKACXKTF-XELLLNAOSA-N 0.000 claims 2
• 229960005501 duocarmycin Drugs 0.000 claims 2
• 229930184221 duocarmycin Natural products 0.000 claims 2
• RWSXRVCMGQZWBV-WDSKDSINSA-N glutathione Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@@H](CS)C(=O)NCC(O)=O RWSXRVCMGQZWBV-WDSKDSINSA-N 0.000 claims 2
• 201000005249 lung adenocarcinoma Diseases 0.000 claims 2
• 201000005202 lung cancer Diseases 0.000 claims 2
• 208000020816 lung neoplasm Diseases 0.000 claims 2
• -1 maytansinoid Natural products 0.000 claims 2
• 208000021039 metastatic melanoma Diseases 0.000 claims 2
• 229940125645 monoclonal antibody drug Drugs 0.000 claims 2
• 230000035772 mutation Effects 0.000 claims 2
• 230000002285 radioactive effect Effects 0.000 claims 2
• 238000006467 substitution reaction Methods 0.000 claims 2
• NFGXHKASABOEEW-UHFFFAOYSA-N 1-methylethyl 11-methoxy-3,7,11-trimethyl-2,4-dodecadienoate Chemical compound COC(C)(C)CCCC(C)CC=CC(C)=CC(=O)OC(C)C NFGXHKASABOEEW-UHFFFAOYSA-N 0.000 claims 1
• 239000004475 Arginine Substances 0.000 claims 1
• 108010024636 Glutathione Proteins 0.000 claims 1
• 101000766306 Homo sapiens Serotransferrin Proteins 0.000 claims 1
• XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 1
• PWKSKIMOESPYIA-BYPYZUCNSA-N L-N-acetyl-Cysteine Chemical compound CC(=O)N[C@@H](CS)C(O)=O PWKSKIMOESPYIA-BYPYZUCNSA-N 0.000 claims 1
• 239000004472 Lysine Substances 0.000 claims 1
• KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 1
• 229960004308 acetylcysteine Drugs 0.000 claims 1
• 150000001412 amines Chemical group 0.000 claims 1
• ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 1
• 230000004611 cancer cell death Effects 0.000 claims 1
• 150000001875 compounds Chemical class 0.000 claims 1
• 230000001268 conjugating effect Effects 0.000 claims 1
• UFULAYFCSOUIOV-UHFFFAOYSA-N cysteamine Chemical compound NCCS UFULAYFCSOUIOV-UHFFFAOYSA-N 0.000 claims 1
• XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 1
• 235000018417 cysteine Nutrition 0.000 claims 1
• 229960002433 cysteine Drugs 0.000 claims 1
• 230000003013 cytotoxicity Effects 0.000 claims 1
• 231100000135 cytotoxicity Toxicity 0.000 claims 1
• 229960003180 glutathione Drugs 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 238000012544 monitoring process Methods 0.000 claims 1
• 238000004237 preparative chromatography Methods 0.000 claims 1
• 241000894007 species Species 0.000 claims 1
• 239000003381 stabilizer Substances 0.000 claims 1
• 239000000126 substance Substances 0.000 claims 1
• 150000003573 thiols Chemical class 0.000 claims 1
• DGVVWUTYPXICAM-UHFFFAOYSA-N β‐Mercaptoethanol Chemical compound OCCS DGVVWUTYPXICAM-UHFFFAOYSA-N 0.000 claims 1