JP2013542958A5 - - Google Patents
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- JP2013542958A5 JP2013542958A5 JP2013537819A JP2013537819A JP2013542958A5 JP 2013542958 A5 JP2013542958 A5 JP 2013542958A5 JP 2013537819 A JP2013537819 A JP 2013537819A JP 2013537819 A JP2013537819 A JP 2013537819A JP 2013542958 A5 JP2013542958 A5 JP 2013542958A5
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- 125000000217 alkyl group Chemical group 0.000 claims 32
- 210000004027 cell Anatomy 0.000 claims 28
- 125000003342 alkenyl group Chemical group 0.000 claims 14
- 125000000304 alkynyl group Chemical group 0.000 claims 14
- 239000011230 binding agent Substances 0.000 claims 14
- -1 4-piperidinocarbonyl piperidinylmethyl Chemical group 0.000 claims 13
- 125000005647 linker group Chemical group 0.000 claims 13
- QWPXBEHQFHACTK-KZVYIGENSA-N (10e,12e)-86-chloro-12,14,4-trihydroxy-85,14-dimethoxy-33,2,7,10-tetramethyl-15,16-dihydro-14h-7-aza-1(6,4)-oxazina-3(2,3)-oxirana-8(1,3)-benzenacyclotetradecaphane-10,12-dien-6-one Chemical compound CN1C(=O)CC(O)C2(C)OC2C(C)C(OC(=O)N2)CC2(O)C(OC)\C=C\C=C(C)\CC2=CC(OC)=C(Cl)C1=C2 QWPXBEHQFHACTK-KZVYIGENSA-N 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 125000000623 heterocyclic group Chemical group 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- QWPXBEHQFHACTK-UHFFFAOYSA-N Maytansinol Natural products CN1C(=O)CC(O)C2(C)OC2C(C)C(OC(=O)N2)CC2(O)C(OC)C=CC=C(C)CC2=CC(OC)=C(Cl)C1=C2 QWPXBEHQFHACTK-UHFFFAOYSA-N 0.000 claims 7
- 150000001413 amino acids Chemical class 0.000 claims 7
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 108090000765 processed proteins & peptides Proteins 0.000 claims 7
- 150000001768 cations Chemical class 0.000 claims 6
- 125000001475 halogen functional group Chemical group 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 150000002148 esters Chemical class 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 150000007970 thio esters Chemical class 0.000 claims 5
- DVOOXRTYGGLORL-VKHMYHEASA-N (2r)-2-(methylamino)-3-sulfanylpropanoic acid Chemical group CN[C@@H](CS)C(O)=O DVOOXRTYGGLORL-VKHMYHEASA-N 0.000 claims 4
- BWGNESOTFCXPMA-UHFFFAOYSA-N Dihydrogen disulfide Chemical compound SS BWGNESOTFCXPMA-UHFFFAOYSA-N 0.000 claims 4
- 102000008394 Immunoglobulin Fragments Human genes 0.000 claims 4
- 108010021625 Immunoglobulin Fragments Proteins 0.000 claims 4
- GDFAOVXKHJXLEI-VKHMYHEASA-N N-methyl-L-alanine Chemical compound C[NH2+][C@@H](C)C([O-])=O GDFAOVXKHJXLEI-VKHMYHEASA-N 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 239000002202 Polyethylene glycol Substances 0.000 claims 4
- 150000001408 amides Chemical class 0.000 claims 4
- 230000001588 bifunctional effect Effects 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 125000003827 glycol group Chemical group 0.000 claims 4
- 125000005597 hydrazone group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 150000002466 imines Chemical class 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 229920001223 polyethylene glycol Polymers 0.000 claims 4
- 150000003568 thioethers Chemical class 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 239000003431 cross linking reagent Substances 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 150000002825 nitriles Chemical class 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 125000000636 p-nitrophenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)[N+]([O-])=O 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- AGGWFDNPHKLBBV-YUMQZZPRSA-N (2s)-2-[[(2s)-2-amino-3-methylbutanoyl]amino]-5-(carbamoylamino)pentanoic acid Chemical compound CC(C)[C@H](N)C(=O)N[C@H](C(O)=O)CCCNC(N)=O AGGWFDNPHKLBBV-YUMQZZPRSA-N 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- FADYJNXDPBKVCA-UHFFFAOYSA-N L-Phenylalanyl-L-lysin Natural products NCCCCC(C(O)=O)NC(=O)C(N)CC1=CC=CC=C1 FADYJNXDPBKVCA-UHFFFAOYSA-N 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- FADYJNXDPBKVCA-STQMWFEESA-N Phe-Lys Chemical compound NCCCC[C@@H](C(O)=O)NC(=O)[C@@H](N)CC1=CC=CC=C1 FADYJNXDPBKVCA-STQMWFEESA-N 0.000 claims 2
- JKHXYJKMNSSFFL-IUCAKERBSA-N Val-Lys Chemical compound CC(C)[C@H](N)C(=O)N[C@H](C(O)=O)CCCCN JKHXYJKMNSSFFL-IUCAKERBSA-N 0.000 claims 2
- 239000000427 antigen Substances 0.000 claims 2
- 102000036639 antigens Human genes 0.000 claims 2
- 108091007433 antigens Proteins 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 125000004069 aziridinyl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000003700 epoxy group Chemical group 0.000 claims 2
- 208000024908 graft versus host disease Diseases 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 2
- 208000015181 infectious disease Diseases 0.000 claims 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000006501 nitrophenyl group Chemical group 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 108010073969 valyllysine Proteins 0.000 claims 2
- 125000001917 2,4-dinitrophenyl group Chemical group [H]C1=C([H])C(=C([H])C(=C1*)[N+]([O-])=O)[N+]([O-])=O 0.000 claims 1
- 102100031585 ADP-ribosyl cyclase/cyclic ADP-ribose hydrolase 1 Human genes 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 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
- 208000020084 Bone disease Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 101150013553 CD40 gene Proteins 0.000 claims 1
- 102100032912 CD44 antigen Human genes 0.000 claims 1
- 101100314454 Caenorhabditis elegans tra-1 gene Proteins 0.000 claims 1
- 241000189662 Calla Species 0.000 claims 1
- 108010071942 Colony-Stimulating Factors Proteins 0.000 claims 1
- 102000007644 Colony-Stimulating Factors Human genes 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 102000001301 EGF receptor Human genes 0.000 claims 1
- 108060006698 EGF receptor Proteins 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
- 102100031517 Fc receptor-like protein 1 Human genes 0.000 claims 1
- 102100031511 Fc receptor-like protein 2 Human genes 0.000 claims 1
- 102100031512 Fc receptor-like protein 3 Human genes 0.000 claims 1
- 102100031513 Fc receptor-like protein 4 Human genes 0.000 claims 1
- 102100031507 Fc receptor-like protein 5 Human genes 0.000 claims 1
- 102000009465 Growth Factor Receptors Human genes 0.000 claims 1
- 108010009202 Growth Factor Receptors Proteins 0.000 claims 1
- 101000777636 Homo sapiens ADP-ribosyl cyclase/cyclic ADP-ribose hydrolase 1 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
- 101000846913 Homo sapiens Fc receptor-like protein 1 Proteins 0.000 claims 1
- 101000846911 Homo sapiens Fc receptor-like protein 2 Proteins 0.000 claims 1
- 101000846910 Homo sapiens Fc receptor-like protein 3 Proteins 0.000 claims 1
- 101000846909 Homo sapiens Fc receptor-like protein 4 Proteins 0.000 claims 1
- 101000846908 Homo sapiens Fc receptor-like protein 5 Proteins 0.000 claims 1
- 101000777628 Homo sapiens Leukocyte antigen CD37 Proteins 0.000 claims 1
- 101000628547 Homo sapiens Metalloreductase STEAP1 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
- 101000934376 Homo sapiens T-cell differentiation antigen CD6 Proteins 0.000 claims 1
- 101000716102 Homo sapiens T-cell surface glycoprotein CD4 Proteins 0.000 claims 1
- 101000834948 Homo sapiens Tomoregulin-2 Proteins 0.000 claims 1
- 101000851376 Homo sapiens Tumor necrosis factor receptor superfamily member 8 Proteins 0.000 claims 1
- 206010061598 Immunodeficiency Diseases 0.000 claims 1
- 208000029462 Immunodeficiency disease Diseases 0.000 claims 1
- 102000004877 Insulin Human genes 0.000 claims 1
- 108090001061 Insulin Proteins 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 102100031586 Leukocyte antigen CD37 Human genes 0.000 claims 1
- 102000008072 Lymphokines Human genes 0.000 claims 1
- 108010074338 Lymphokines Proteins 0.000 claims 1
- PEEHTFAAVSWFBL-UHFFFAOYSA-N Maleimide Chemical compound O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 claims 1
- 208000002030 Merkel cell carcinoma Diseases 0.000 claims 1
- 102100026712 Metalloreductase STEAP1 Human genes 0.000 claims 1
- 102100023123 Mucin-16 Human genes 0.000 claims 1
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- 201000002481 Myositis Diseases 0.000 claims 1
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- 108090000028 Neprilysin Proteins 0.000 claims 1
- 102100027347 Neural cell adhesion molecule 1 Human genes 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
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- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
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- 102100025131 T-cell differentiation antigen CD6 Human genes 0.000 claims 1
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- 235000015097 nutrients Nutrition 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 230000007170 pathology Effects 0.000 claims 1
- NMHMNPHRMNGLLB-UHFFFAOYSA-N phloretic acid Chemical group OC(=O)CCC1=CC=C(O)C=C1 NMHMNPHRMNGLLB-UHFFFAOYSA-N 0.000 claims 1
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- 229940088594 vitamin Drugs 0.000 claims 1
- 229930003231 vitamin Natural products 0.000 claims 1
- 0 Cc1ccc(CI***)cc1 Chemical compound Cc1ccc(CI***)cc1 0.000 description 2
- KQUZQAWZXGZTLS-UHFFFAOYSA-N CC(C)C(CC(N1CC(CC2)CCC2S)=O)C1=O Chemical compound CC(C)C(CC(N1CC(CC2)CCC2S)=O)C1=O KQUZQAWZXGZTLS-UHFFFAOYSA-N 0.000 description 1
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- UVBMZKBIZUWTLV-UHFFFAOYSA-N CCCN(C)CCC Chemical compound CCCN(C)CCC UVBMZKBIZUWTLV-UHFFFAOYSA-N 0.000 description 1
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40983110P | 2010-11-03 | 2010-11-03 | |
| US61/409,831 | 2010-11-03 | ||
| PCT/US2011/059131 WO2012061590A1 (en) | 2010-11-03 | 2011-11-03 | Cytotoxic agents comprising new ansamitocin derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013542958A JP2013542958A (ja) | 2013-11-28 |
| JP2013542958A5 true JP2013542958A5 (enExample) | 2014-12-18 |
Family
ID=46024826
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013537819A Pending JP2013542958A (ja) | 2010-11-03 | 2011-11-03 | アンサマイトシン誘導体を含む細胞傷害性剤 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US9090629B2 (enExample) |
| EP (1) | EP2635301A4 (enExample) |
| JP (1) | JP2013542958A (enExample) |
| CN (2) | CN103269712B (enExample) |
| AU (1) | AU2011323316B2 (enExample) |
| BR (1) | BR112013010853A2 (enExample) |
| CA (1) | CA2816681A1 (enExample) |
| EA (1) | EA201390642A1 (enExample) |
| MX (1) | MX2013005046A (enExample) |
| WO (1) | WO2012061590A1 (enExample) |
Families Citing this family (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014089177A2 (en) | 2012-12-04 | 2014-06-12 | Massachusetts Institute Of Technology | Compounds, conjugates and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines |
| CN103933575B (zh) | 2013-01-23 | 2017-09-29 | 上海新理念生物医药科技有限公司 | 一种三齿型连接子及其应用 |
| JP6423804B2 (ja) * | 2013-02-28 | 2018-11-14 | イミュノジェン・インコーポレーテッド | 細胞結合剤及び細胞毒性剤を含む複合体 |
| WO2014134457A2 (en) * | 2013-02-28 | 2014-09-04 | Immunogen, Inc. | Conjugates comprising cell-binding agents and cytotoxic agents |
| JP6847388B2 (ja) | 2013-03-15 | 2021-03-31 | レゲネロン ファーマシューティカルス，インコーポレーテッド | 生物活性分子、そのコンジュゲート、及び治療用途 |
| US10208125B2 (en) | 2013-07-15 | 2019-02-19 | University of Pittsburgh—of the Commonwealth System of Higher Education | Anti-mucin 1 binding agents and uses thereof |
| BR112016004023A2 (pt) | 2013-08-26 | 2022-11-16 | Regeneron Pharma | Composição, métodos para preparar uma composição e para tratar uma doença, e, composto |
| EP2881735A1 (en) * | 2013-12-05 | 2015-06-10 | Kittiwake Developments Ltd. | Method for Determining the Concentration of Iron Ions in Hydrocarbon Compositions |
| BR112017020149A8 (pt) | 2015-03-27 | 2023-05-02 | Regeneron Pharma | Derivados de maitansinoide, conjugados dos mesmos e métodos de uso |
| IL292798A (en) | 2015-05-04 | 2022-07-01 | Cytomx Therapeutics Inc | Anti-cd166 antibodies, activatable anti-cd166 antibodies, preparations containing them and their uses |
| CN106267225B (zh) | 2015-05-29 | 2020-03-06 | 上海新理念生物医药科技有限公司 | 三马来酰亚胺型连接子及其应用 |
| CN106279352B (zh) | 2015-05-29 | 2020-05-22 | 上海新理念生物医药科技有限公司 | 海兔毒素10的衍生物及其应用 |
| ES2821649T3 (es) | 2015-06-08 | 2021-04-27 | Shangdong Danhong Pharmaceutical Co Ltd | Método para preparar derivados de imidazol e intermedios de los mismos y formas cristalinas |
| CN106243127B (zh) * | 2015-06-09 | 2021-01-26 | 凯惠科技发展(上海)有限公司 | 抗体药物偶联物、中间体、制备方法、药物组合物及应用 |
| EP3373910B1 (en) | 2015-11-10 | 2023-07-12 | Children's Research Institute, Children's National Medical Center | Echinomycin formulation, method of making and method of use thereof |
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2011
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- 2011-11-03 EA EA201390642A patent/EA201390642A1/ru unknown
- 2011-11-03 BR BR112013010853A patent/BR112013010853A2/pt not_active IP Right Cessation
- 2011-11-03 CA CA2816681A patent/CA2816681A1/en not_active Abandoned
- 2011-11-03 CN CN201180062234.3A patent/CN103269712B/zh not_active Expired - Fee Related
- 2011-11-03 JP JP2013537819A patent/JP2013542958A/ja active Pending
- 2011-11-03 US US13/883,344 patent/US9090629B2/en not_active Expired - Fee Related
- 2011-11-03 MX MX2013005046A patent/MX2013005046A/es unknown
- 2011-11-03 WO PCT/US2011/059131 patent/WO2012061590A1/en not_active Ceased
- 2011-11-03 CN CN201610728548.7A patent/CN106349254A/zh active Pending
- 2011-11-03 EP EP11838805.7A patent/EP2635301A4/en not_active Withdrawn
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2015
- 2015-05-22 US US14/719,753 patent/US20160058882A1/en not_active Abandoned