JP2016530254A5 - - Google Patents
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- JP2016530254A5 JP2016530254A5 JP2016533294A JP2016533294A JP2016530254A5 JP 2016530254 A5 JP2016530254 A5 JP 2016530254A5 JP 2016533294 A JP2016533294 A JP 2016533294A JP 2016533294 A JP2016533294 A JP 2016533294A JP 2016530254 A5 JP2016530254 A5 JP 2016530254A5
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- Prior art keywords
- antibody
- hvr
- alkylene
- seq
- amino acid
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 150000001875 compounds Chemical class 0.000 claims 55
- 108090001123 antibodies Proteins 0.000 claims 46
- 102000004965 antibodies Human genes 0.000 claims 46
- 108091008116 antibody drug conjugates Proteins 0.000 claims 45
- 239000000611 antibody drug conjugate Substances 0.000 claims 44
- 125000003275 alpha amino acid group Chemical group 0.000 claims 38
- 125000000217 alkyl group Chemical group 0.000 claims 36
- 239000003814 drug Substances 0.000 claims 36
- 229910052739 hydrogen Inorganic materials 0.000 claims 26
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 22
- 229940079593 drugs Drugs 0.000 claims 22
- 125000002947 alkylene group Chemical group 0.000 claims 21
- 125000004450 alkenylene group Chemical group 0.000 claims 18
- 239000000562 conjugate Substances 0.000 claims 18
- 229910052799 carbon Inorganic materials 0.000 claims 15
- 125000005418 aryl aryl group Chemical group 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 102100019843 GFRA1 Human genes 0.000 claims 9
- 101700018531 GFRA1 Proteins 0.000 claims 9
- 102100006051 RET Human genes 0.000 claims 8
- 101700001630 RET Proteins 0.000 claims 8
- 125000004419 alkynylene group Chemical group 0.000 claims 8
- 229910052698 phosphorus Inorganic materials 0.000 claims 8
- 102100005647 KISS1R Human genes 0.000 claims 6
- 102100006820 PMEL Human genes 0.000 claims 6
- 101700035121 PMEL Proteins 0.000 claims 6
- 101710023820 SEMA5B Proteins 0.000 claims 6
- 102100006461 STEAP2 Human genes 0.000 claims 6
- 101710009478 STEAP2 Proteins 0.000 claims 6
- 239000000539 dimer Substances 0.000 claims 6
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 5
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 5
- 102100011003 LY6K Human genes 0.000 claims 5
- 101700026174 LY6K Proteins 0.000 claims 5
- 102100004376 SEMA5B Human genes 0.000 claims 5
- 102100010801 SLC52A2 Human genes 0.000 claims 5
- 101710004324 SLC52A2 Proteins 0.000 claims 5
- 101700073629 TDGF1 Proteins 0.000 claims 5
- 235000018417 cysteine Nutrition 0.000 claims 5
- -1 cysteine amino acid Chemical class 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 125000006832 (C1-C10) alkylene group Chemical group 0.000 claims 4
- 101710033964 KISS1R Proteins 0.000 claims 4
- 102100004927 LGR5 Human genes 0.000 claims 4
- 101700016076 LGR5 Proteins 0.000 claims 4
- 102100011000 LY6E Human genes 0.000 claims 4
- 101700048317 LY6E Proteins 0.000 claims 4
- 102100005491 TDGF1 Human genes 0.000 claims 4
- 101710023902 TMEFF1 Proteins 0.000 claims 4
- 102100018592 TMEFF1 Human genes 0.000 claims 4
- 125000000539 amino acid group Chemical group 0.000 claims 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 4
- 125000005647 linker group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 235000018102 proteins Nutrition 0.000 claims 4
- 102000004169 proteins and genes Human genes 0.000 claims 4
- 108090000623 proteins and genes Proteins 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 102100005868 CD180 Human genes 0.000 claims 3
- 101700060549 CD180 Proteins 0.000 claims 3
- 101700002874 CD72 Proteins 0.000 claims 3
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- 102000018358 Immunoglobulins Human genes 0.000 claims 3
- 108060003951 Immunoglobulins Proteins 0.000 claims 3
- XUJNEKJLAYXESH-REOHCLBHSA-N L-cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 3
- 102100009457 LY6G6D Human genes 0.000 claims 3
- 101710029022 LY6G6D Proteins 0.000 claims 3
- 210000002307 Prostate Anatomy 0.000 claims 3
- 102100009652 RNFT2 Human genes 0.000 claims 3
- 101700033014 RNFT2 Proteins 0.000 claims 3
- 101710026258 SHISA2 Proteins 0.000 claims 3
- 102100009048 SHISA2 Human genes 0.000 claims 3
- 102100005556 SLC34A2 Human genes 0.000 claims 3
- 102100009743 TNFRSF13C Human genes 0.000 claims 3
- 108060008548 TRPM4 Proteins 0.000 claims 3
- 125000004452 carbocyclyl group Chemical group 0.000 claims 3
- 235000019876 cocoa butter improver Nutrition 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 102000005962 receptors Human genes 0.000 claims 3
- 108020003175 receptors Proteins 0.000 claims 3
- HAXFWIACAGNFHA-UHFFFAOYSA-N 2,2'-Dipyridyldisulfide Chemical compound C=1C=CC=NC=1SSC1=CC=CC=N1 HAXFWIACAGNFHA-UHFFFAOYSA-N 0.000 claims 2
- JUIKUQOUMZUFQT-UHFFFAOYSA-N 2-bromoacetamide Chemical compound NC(=O)CBr JUIKUQOUMZUFQT-UHFFFAOYSA-N 0.000 claims 2
- 102100003236 ASPHD1 Human genes 0.000 claims 2
- 101710009226 ASPHD1 Proteins 0.000 claims 2
- FNXLCIKXHOPCKH-UHFFFAOYSA-N Bromamine Chemical compound BrN FNXLCIKXHOPCKH-UHFFFAOYSA-N 0.000 claims 2
- 102100019449 CD79B Human genes 0.000 claims 2
- 101700045471 CD79B Proteins 0.000 claims 2
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- 102000011412 Complement 3d Receptors Human genes 0.000 claims 2
- 108010023729 Complement 3d Receptors Proteins 0.000 claims 2
- 229920002676 Complementary DNA Polymers 0.000 claims 2
- 102000003425 EC 1.14.18.1 Human genes 0.000 claims 2
- 108060008724 EC 1.14.18.1 Proteins 0.000 claims 2
- 102100016662 ERBB2 Human genes 0.000 claims 2
- 101700025368 ERBB2 Proteins 0.000 claims 2
- 101700021818 FCRL1 Proteins 0.000 claims 2
- 102100017784 FCRL1 Human genes 0.000 claims 2
- 102100014301 GPR19 Human genes 0.000 claims 2
- 101700079199 GPR19 Proteins 0.000 claims 2
- PGLTVOMIXTUURA-UHFFFAOYSA-N Iodoacetamide Chemical compound NC(=O)CI PGLTVOMIXTUURA-UHFFFAOYSA-N 0.000 claims 2
- 101700055519 KISS1R Proteins 0.000 claims 2
- 108010076800 Kisspeptin-1 Receptors Proteins 0.000 claims 2
- 102100006044 MUC16 Human genes 0.000 claims 2
- 101700008449 MUC16 Proteins 0.000 claims 2
- NQTADLQHYWFPDB-UHFFFAOYSA-N N-hydroxy-Succinimide Chemical compound ON1C(=O)CCC1=O NQTADLQHYWFPDB-UHFFFAOYSA-N 0.000 claims 2
- 102100017963 PSCA Human genes 0.000 claims 2
- 101700038464 PSCA Proteins 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 101710037934 QRSL1 Proteins 0.000 claims 2
- 101710035379 SLC34A2 Proteins 0.000 claims 2
- 102000037167 SLC7A5 Human genes 0.000 claims 2
- 108091006212 SLC7A5 Proteins 0.000 claims 2
- 108050000099 Sema domain Proteins 0.000 claims 2
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- 101710030862 TNFRSF13C Proteins 0.000 claims 2
- 102100020392 TRPM4 Human genes 0.000 claims 2
- 101710013725 TYR Proteins 0.000 claims 2
- 102100008629 TYR Human genes 0.000 claims 2
- 239000000427 antigen Substances 0.000 claims 2
- 102000038129 antigens Human genes 0.000 claims 2
- 108091007172 antigens Proteins 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 239000002299 complementary DNA Substances 0.000 claims 2
- 125000000524 functional group Chemical group 0.000 claims 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- XMBWDFGMSWQBCA-UHFFFAOYSA-M iodide Chemical compound [I-] XMBWDFGMSWQBCA-UHFFFAOYSA-M 0.000 claims 2
- 210000004901 leucine-rich repeat Anatomy 0.000 claims 2
- PEEHTFAAVSWFBL-UHFFFAOYSA-N maleimide Chemical compound O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 claims 2
- 102000003735 mesothelin Human genes 0.000 claims 2
- 108090000015 mesothelin Proteins 0.000 claims 2
- 150000003573 thiols Chemical class 0.000 claims 2
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 claims 2
- FGYADSCZTQOAFK-UHFFFAOYSA-N 1-methylbenzimidazole Chemical group C1=CC=C2N(C)C=NC2=C1 FGYADSCZTQOAFK-UHFFFAOYSA-N 0.000 claims 1
- URSPTJYSBTXILH-UHFFFAOYSA-N 1-methylidenepiperazin-1-ium-4-ide Chemical group C=[N+]1CC[N-]CC1 URSPTJYSBTXILH-UHFFFAOYSA-N 0.000 claims 1
- 239000004475 Arginine Substances 0.000 claims 1
- 108091008154 B cell receptors Proteins 0.000 claims 1
- 108010003455 BLyS receptor Proteins 0.000 claims 1
- 206010061590 Blood disease Diseases 0.000 claims 1
- 102000001893 Bone Morphogenetic Protein Receptors Human genes 0.000 claims 1
- 108010040422 Bone Morphogenetic Protein Receptors Proteins 0.000 claims 1
- 101700079139 CASP7 Proteins 0.000 claims 1
- 101700020617 CD22 Proteins 0.000 claims 1
- 102100000189 CD22 Human genes 0.000 claims 1
- 102100016493 CD33 Human genes 0.000 claims 1
- 101700017647 CD33 Proteins 0.000 claims 1
- 101700037975 CD79A Proteins 0.000 claims 1
- 102100019443 CD79A Human genes 0.000 claims 1
- 102100005552 CR1 Human genes 0.000 claims 1
- 101700042195 CR1 Proteins 0.000 claims 1
- 101700020447 CR2 Proteins 0.000 claims 1
- 102100009368 CR2 Human genes 0.000 claims 1
- 101710025651 CXCR5 Proteins 0.000 claims 1
- 108010061298 CXCR5 Receptors Proteins 0.000 claims 1
- 102000002045 Endothelin Human genes 0.000 claims 1
- 108050009340 Endothelin Proteins 0.000 claims 1
- ZUBDGKVDJUIMQQ-UBFCDGJISA-N Endothelin-1 Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(O)=O)NC(=O)[C@H]1NC(=O)[C@H](CC=2C=CC=CC=2)NC(=O)[C@@H](CC=2C=CC(O)=CC=2)NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CSSC[C@@H](C(N[C@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N2)=O)NC(=O)[C@@H](CO)NC(=O)[C@H](N)CSSC1)C1=CNC=N1 ZUBDGKVDJUIMQQ-UBFCDGJISA-N 0.000 claims 1
- 239000004471 Glycine Substances 0.000 claims 1
- 102100005785 HLA-DOB Human genes 0.000 claims 1
- 101710007991 HLA-DOB Proteins 0.000 claims 1
- 102000018713 Histocompatibility Antigens Class II Human genes 0.000 claims 1
- 108010027412 Histocompatibility Antigens Class II Proteins 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
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims 1
- RHGKLRLOHDJJDR-BYPYZUCNSA-N L-citrulline zwitterion Chemical compound NC(=O)NCCC[C@H]([NH3+])C([O-])=O RHGKLRLOHDJJDR-BYPYZUCNSA-N 0.000 claims 1
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 1
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-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
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims 1
- 206010024324 Leukaemias Diseases 0.000 claims 1
- 102000004086 Ligand-Gated Ion Channels Human genes 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- 210000004470 MDP Anatomy 0.000 claims 1
- 102100013822 MSLN Human genes 0.000 claims 1
- 101700047896 MSLN Proteins 0.000 claims 1
- 101700086625 MUC13 Proteins 0.000 claims 1
- 102000018697 Membrane Proteins Human genes 0.000 claims 1
- 108010052285 Membrane Proteins Proteins 0.000 claims 1
- 208000006876 Multiple Endocrine Neoplasia Type 2b Diseases 0.000 claims 1
- 206010073148 Multiple endocrine neoplasia Type 2A Diseases 0.000 claims 1
- 101700078964 NAG3 Proteins 0.000 claims 1
- 101700001465 NBR1 Proteins 0.000 claims 1
- 101710003528 NDUFS8 Proteins 0.000 claims 1
- 206010025310 Other lymphomas Diseases 0.000 claims 1
- 102100010174 P2RX5 Human genes 0.000 claims 1
- 101700059271 P2RX5 Proteins 0.000 claims 1
- 229960005190 Phenylalanine Drugs 0.000 claims 1
- 102000016462 Phosphate Transport Proteins Human genes 0.000 claims 1
- 108010092528 Phosphate Transport Proteins Proteins 0.000 claims 1
- 102000000033 Purinergic Receptors Human genes 0.000 claims 1
- 108010080192 Purinergic Receptors Proteins 0.000 claims 1
- 102100016246 RNF43 Human genes 0.000 claims 1
- 101700068825 SCAL2 Proteins 0.000 claims 1
- 102000014400 SH2 domains Human genes 0.000 claims 1
- 108050003452 SH2 domains Proteins 0.000 claims 1
- 108091006491 SLC34A2 Proteins 0.000 claims 1
- 101710034091 SPCC1322.09 Proteins 0.000 claims 1
- 108050003978 Semaphorin Proteins 0.000 claims 1
- 102000014105 Semaphorin Human genes 0.000 claims 1
- 101710023903 TMEFF2 Proteins 0.000 claims 1
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- 102100009502 TRAPPC10 Human genes 0.000 claims 1
- 101710029420 TRAPPC10 Proteins 0.000 claims 1
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- 108010010691 Trastuzumab Proteins 0.000 claims 1
- 102000018265 Virus Receptors Human genes 0.000 claims 1
- 108010066342 Virus Receptors Proteins 0.000 claims 1
- DACWQSNZECJJGG-UHFFFAOYSA-N [1,2,4]triazolo[1,5-a]pyridine Chemical group C1=CC=CN2N=CN=C21 DACWQSNZECJJGG-UHFFFAOYSA-N 0.000 claims 1
- 239000012190 activator Substances 0.000 claims 1
- 235000004279 alanine Nutrition 0.000 claims 1
- 235000001014 amino acid Nutrition 0.000 claims 1
- 125000000732 arylene group Chemical group 0.000 claims 1
- 201000002393 blood protein disease Diseases 0.000 claims 1
- 210000004027 cells Anatomy 0.000 claims 1
- 235000013477 citrulline Nutrition 0.000 claims 1
- 229960002173 citrulline Drugs 0.000 claims 1
- 230000001268 conjugating Effects 0.000 claims 1
- 230000001086 cytosolic Effects 0.000 claims 1
- 230000001419 dependent Effects 0.000 claims 1
- 101700027069 gliC Proteins 0.000 claims 1
- 201000002138 hematopoietic system disease Diseases 0.000 claims 1
- 125000005439 maleimidyl group Chemical group C1(C=CC(N1*)=O)=O 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 201000000414 oculocutaneous albinism type IA Diseases 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- 125000005936 piperidyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 101700034546 qacC Proteins 0.000 claims 1
- BQCADISMDOOEFD-UHFFFAOYSA-N silver Chemical compound [Ag] BQCADISMDOOEFD-UHFFFAOYSA-N 0.000 claims 1
- 229910052709 silver Inorganic materials 0.000 claims 1
- 239000004332 silver Substances 0.000 claims 1
- KEAYESYHFKHZAL-UHFFFAOYSA-N sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 229910000162 sodium phosphate Inorganic materials 0.000 claims 1
- 239000001488 sodium phosphate Substances 0.000 claims 1
- 102000002938 thrombospondin family Human genes 0.000 claims 1
- 108060008245 thrombospondin family Proteins 0.000 claims 1
- 108010037277 thymic shared antigen-1 Proteins 0.000 claims 1
- 229960000575 trastuzumab Drugs 0.000 claims 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 claims 1
- 239000004474 valine Substances 0.000 claims 1
- 0 CC(C)[C@@](C(N[C@@](CCCNC(N)=O)C(Nc1ccc(COC(*)=O)cc1)=O)=O)NC(CCCCCN(C(CC1*)=O)C1=O)=O Chemical compound CC(C)[C@@](C(N[C@@](CCCNC(N)=O)C(Nc1ccc(COC(*)=O)cc1)=O)=O)NC(CCCCCN(C(CC1*)=O)C1=O)=O 0.000 description 2
Claims (76)
- 式:
を有する抗体−薬物コンジュゲート化合物であって、
ここで、
Abは抗体であり;
Lは、式:
を有するリンカーであり;
ここでStrは抗体に共有結合したストレッチャー単位であり;Pepは2から12個のアミノ酸残基の任意のペプチド単位であり、Spは二量体の薬物部分に共有結合した任意のスペーサー単位であり、m及びnは0及び1から独立に選択され;
pは1から8の整数であり;
Dは式:
を有する二量体薬物部分であり、
ここで
R1は、H、P(O)3H2、C(O)NRaRb、又はLへの結合から選択され;
R2は、H、P(O)3H2、C(O)NRaRb、又はLへの結合から選択され;
Ra及びRbは、H及び一以上のFで任意置換されたC1−C6アルキルから独立に選択され、
又はRa及びRbは、5又は6員複素環基を形成し;
Tは、C3−C12アルキレン、Y、(C1−C6アルキレン)−Y−(C1−C6アルキレン)、(C1−C6アルキレン)−Y−(C1−C6アルキレン)−Y−(C1−C6アルキレン)、(C2−C6アルケニレン)−Y−(C2−C6アルケニレン)及び(C2−C6アルキニレン)−Y−(C2−C6アルキニレン)から選択されるテザー基であり;
ここで、YはO、S、NR1、アリール、及びヘテロアリールから独立に選択され;
ここで、アルキレン、アルケニレン、アリール、及びヘテロアリールは、F、OH、O(C1−C6アルキル)、NH2、NHCH3、N(CH3)2、OP(O)3H2、及びC1−C6アルキルで独立に任意置換され、ここでアルキルは、一以上のFで任意置換され;
又はアルキレン、アルケニレン、アリール及びヘテロアリールは、Lへの結合で独立に任意置換され;
D’は
から選択される薬物部分であり、
ここで波線はTへの結合部位を示し;
X1及びX2は、O及びNR3から独立して選択され、ここでR3は、H及び任意で一以上のFで置換されたC1−C6アルキルから選択され;
R4は、H、CO2R、又はLへの結合であり、ここでRはC1−C6アルキル又はベンジルであり;及び
R5は、H又はC1−C6アルキルである、抗体−薬物コンジュゲート化合物。 - Strが式:
を有し、
ここで、R6は、C1−C10アルキレン、C3−C8カルボシクリル、O−(C1−C8アルキル)、アリーレン、C1−C10アルキレン−アリーレン、アリーレン−C1−C10アルキレン、C1−C10アルキレン−(C3−C8カルボシクリル)、(C3−C8カルボシクリル)−C1−C10アルキレン、C3−C8ヘテロシクリル、C1−C10アルキレン−(C3−C8ヘテロシクリル)、(C3−C8ヘテロシクリル)−C1−C10アルキレン、C1−C10アルキレン−C(O)N(R8)−C2−C6アルキレン−N(R8)、N(R8)−(C2−C6アルキレン)及び(CH2CH2O)r−CH2からなる群から選択され;ここでR8は、H又はC1−C6アルキル、rは1から10の範囲の整数である、請求項1に記載の抗体−薬物コンジュゲート化合物。 - R6が(CH2)5である、請求項2に記載の抗体−薬物コンジュゲート化合物。
- mが0及びnが0である、請求項1に記載の抗体−薬物コンジュゲート化合物。
- mが0及びnが1である、請求項1に記載の抗体−薬物コンジュゲート化合物。
- Lは、抗体のシステインアミノ酸とジスルフィド結合を形成し、R9は、C2−C6アルキレン−Oであり、ここでアルキレンは、F、OH、O(C1−C6アルキル)、NH2、NHCH3、N(CH3)2、OP(O)3H2、及びC1−C6アルキルと任意置換され、ここでアルキルは一以上のFと任意置換される、請求項7に記載の抗体−薬物コンジュゲート化合物。
- mが1及びnが1である、請求項1に記載の抗体−薬物コンジュゲート化合物。
- mが1であり、Pepは、グリシン、アラニン、フェニルアラニン、リジン、アルギニン、バリン、及びシトルリンから独立に選択される2から12個のアミノ酸残基を含む、請求項1に記載の抗体−薬物コンジュゲート化合物。
- Pepがバリン−シトルリンである、請求項10に記載の抗体−薬物コンジュゲート化合物。
- nが1であり、Spがパラ−アミノベンジル又はパラ−アミノベンジルオキシカルボニルを含む、請求項1に記載の抗体−薬物コンジュゲート化合物。
- アミノ酸側鎖は、H、−CH3、−CH2(C6H5)、−CH2CH2CH2CH2NH2、−CH2CH2CH2NHC(NH)NH2、−CHCH(CH3)CH3、及び−CH2CH2CH2NHC(O)NH2から独立に選択される、請求項13に記載の抗体−薬物コンジュゲート化合物。
- Ra及びRbは、N−メチルピペラジニル、モルホリニル、ピペリジル、及びピロリジニルから選択される5又は6員複素環基を形成する、請求項1に記載の抗体−薬物コンジュゲート化合物。
- Tが、C3−C5アルキレンである、請求項1に記載の抗体−薬物コンジュゲート化合物。
- Tが、(CH2)3、(CH2)4及び(CH2)5から選択される、請求項24に記載の抗体−薬物コンジュゲート化合物。
- Tが、(C1−C6アルキレン)−Y−(C1−C6アルキレン)であり、Yが、Lへの結合で置換されるフェニルである、請求項1に記載の抗体−薬物コンジュゲート化合物。
- Tが、(C2−C6アルケニレン)−Y−(C2−C6アルケニレン)であり、Yが、Lへの結合で置換されるフェニルである、請求項1に記載の抗体−薬物コンジュゲート化合物。
- Yが、フェニル、ピリジル、1−メチル−1H−ベンゾ[d]イミダゾール、及び[1,2,4]トリアゾロ[1,5−a]ピリジンから選択される、請求項1に記載の抗体−薬物コンジュゲート化合物。
- 抗体が、(1)〜(51):
(1)BMPR1B(骨形成タンパク質レセプタータイプIB);
(2)E16(LAT1、SLC7A5);
(3)STEAP1(前立腺の6回膜貫通型上皮抗原);
(4)0772P(CA125、MUC16);
(5)MPF(MPF、MSLN、SMR、巨核球増強因子、メソテリン);
(6)Napi3b(NAPI−3B、NPTIIb、SLC34A2、溶質輸送体ファミリー34(リン酸ナトリウム)、メンバー2、II型ナトリウム依存性リン酸トランスポーター3b);
(7)Sema5b(FLJ10372、KIAA1445、Mm.42015、SEMA5B、SEMAG、セマフォリン 5b Hlog、セマドメイン(sema domain)、7回トロンボスポンジン反復(1型及び1型様)、膜貫通ドメイン(TM)及び短い細胞質ドメイン(セマフォリン)5B);
(8)PSCA hlg(2700050C12Rik、C530008O16Rik、RIKEN cDNA 2700050C12、RIKEN cDNA 2700050C12 遺伝子);
(9)ETBR(エンドセリンタイプBレセプター);
(10)MSG783(RNF124、仮想タンパク質 FLJ20315);
(11)STEAP2(HGNC_8639、IPCA−1、PCANAP1、STAMP1、STEAP2、STMP、前立腺癌関連遺伝子1、前立腺癌関連タンパク質1、前立腺の6回膜貫通型上皮抗原2、6回膜貫通型前立腺タンパク質);
(12)TrpM4(BR22450、FLJ20041、TRPM4、TRPM4B、一過性レセプター電位カチオンチャネル、サブファミリーM、メンバー4);
(13)CRIPTO(CR、CR1、CRGF、CRIPTO、TDGF1、奇形癌腫由来増殖因子);
(14)CD21(CR2(補体レセプター2)又はC3DR(C3d/エブスタインバーウイルスレセプター)又はHs.73792);
(15)CD79b(CD79B、CD79β、IGb(免疫グロブリン関連β(immunoglobulin−associated beta))、B29);
(16)FcRH2(IFGP4、IRTA4、SPAP1A(SH2ドメイン含有ホスファターゼアンカータンパク質1a)、SPAP1B、SPAP1C);
(17)HER2;
(18)NCA;
(19)MDP;
(20)IL20Rα;
(21)ブレビカン;
(22)EphB2R;
(23)ASLG659;
(24)PSCA;
(25)GEDA;
(26)BAFF−R(B細胞活性化因子レセプター、BLySレセプター3、BR3);
(27)CD22(B細胞レセプターCD22−Bアイソフォーム);
(28)CD79a(CD79A、CD79α、免疫グロブリン関連アルファ;
(29)CXCR5(バーキットリンパ腫レセプター1;
(30)HLA−DOB(MHCクラスII分子のベータサブユニット);
(31)P2X5(プリンレセプターP2Xリガンド開口型イオンチャネル5;
(32)CD72(B細胞分化抗原CD72、Lyb−2);
(33)LY64(リンパ球抗原64(RP105)、ロイシンリッチリピート(LRR)ファミリーのI型膜タンパク質);
(34)FcRH1(Fcレセプター様タンパク質1);
(35)IRTA2(免疫グロブリンスーパーファミリーレセプタートランスロケーション関連2);
(36)TENB2(推定上の膜貫通型プロテオグリカン);
(37)PMEL17(シルバーホモログ;SILV;D12S53E;PMEL17;(SI);(SIL);ME20;gp100);
(38)TMEFF1(EGF様及び2つのフォリスタチン様ドメインを有する膜貫通型タンパク質1;Tomoregulin−1;H7365;C9orf2;C9ORF2;U19878;X83961;
(39)GDNF−Ra1(GDNFファミリーレセプターアルファ1;GFRA1;GDNFR;GDNFRA;RETL1;TRNR1;RET1L;GDNFR−アルファ1;GFR−ALPHA−1;U95847;BC014962);
(40)Ly6E(リンパ球抗原6複合体、遺伝子座E;Ly67、RIG−E、SCA−2、TSA−1);
(41)TMEM46(シサホモログ(shisa homolog)2(アフリカツメガエル);SHISA2);
(42)Ly6G6D(リンパ球抗原6複合体、遺伝子座G6D;Ly6−D、MEGT1);
(43)LGR5(ロイシンリッチリピート含有Gタンパク質共役型レセプター5;GPR49、GPR67);
(44)RET(retプロトオンコジーン;MEN2A;HSCR1;MEN2B;MTC1;(PTC);CDHF12;Hs.168114;RET51;RET−ELE1);
(45)LY6K(リンパ球抗原6複合体、遺伝子座K;LY6K;HSJ001348;FLJ35226);
(46)GPR19(Gタンパク質共役型レセプター19;Mm.4787);
(47)GPR54(KISS1レセプター;KISS1R;GPR54;HOT7T175;AXOR12);
(48)ASPHD1(アスパラギン酸β−ヒドロキシラーゼドメイン含有1;LOC253982);
(49)チロシナーゼ(TYR;OCAIA;OCA1A;チロシナーゼ;SHEP3);
(50)TMEM118(リングフィンガータンパク質、膜貫通型2;RNFT2;FLJ14627);及び
(51)GPR172A(Gタンパク質共役型レセプター172A;GPCR41;FLJ11856;D15Ertd747e)
の一以上のレセプターに結合する、請求項1に記載の抗体−薬物コンジュゲート化合物。 - 抗体が、抗CD22抗体である、請求項1に記載の抗体−薬物コンジュゲート化合物。
- 抗CD22抗体が、3つの軽鎖超可変領域(HVR−L1、HVR−L2及びHVR−L3)及び3つの重鎖超可変領域(HVR−H1、HVR−H2及びHVR−H3)を含み、
HVR−L1が配列番号1のアミノ酸配列を含み;
HVR−L2が配列番号2のアミノ酸配列を含み;
HVR−L3が配列番号3のアミノ酸配列を含み;
HVR−H1が配列番号4のアミノ酸配列を含み;
HVR−H2が配列番号5のアミノ酸配列を含み;及び
HVR−H3が配列番号6のアミノ酸配列を含む、請求項33に記載の抗体−薬物コンジュゲート化合物。 - 抗体が、抗MUC16抗体である、請求項1に記載の抗体−薬物コンジュゲート化合物。
- 抗MUC16抗体が、3つの軽鎖超可変領域(HVR−L1、HVR−L2及びHVR−L3)及び3つの重鎖超可変領域(HVR−H1、HVR−H2及びHVR−H3)を含み、
HVR−L1が配列番号7のアミノ酸配列を含み;
HVR−L2が配列番号8のアミノ酸配列を含み;
HVR−L3が配列番号9のアミノ酸配列を含み;
HVR−H1が配列番号10のアミノ酸配列を含み;
HVR−H2が配列番号11のアミノ酸配列を含み;及び
HVR−H3が配列番号12のアミノ酸配列を含む、請求項35に記載の抗体−薬物コンジュゲート化合物。 - 抗MUC16抗体が、配列番号15−32から選択される軽鎖配列又は配列番号33−46から選択される重鎖配列に位置する一以上の遊離システインアミノ酸残基を含むシステイン操作抗体である、請求項35に記載の抗体−薬物コンジュゲート化合物。
- 抗体が、抗HER2抗体である、請求項1に記載の抗体−薬物コンジュゲート化合物。
- 抗HER2抗体がトラスツズマブである、請求項1に記載の抗体−薬物コンジュゲート化合物。
- 抗体が、抗CD33抗体である、請求項1に記載の抗体−薬物コンジュゲート化合物。
- 抗CD33抗体が、3つの軽鎖超可変領域(HVR−L1、HVR−L2及びHVR−L3)及び3つの重鎖超可変領域(HVR−H1、HVR−H2及びHVR−H3)を含み、
HVR−L1が配列番号51のアミノ酸配列を含み;
HVR−L2が配列番号52のアミノ酸配列を含み;
HVR−L3が配列番号53のアミノ酸配列を含み;
HVR−H1が配列番号54のアミノ酸配列を含み;
HVR−H2が配列番号55のアミノ酸配列を含み;及び
HVR−H3が配列番号56のアミノ酸配列を含む、請求項40に記載の抗体−薬物コンジュゲート化合物。 - 抗CD33抗体が、配列番号57の軽鎖可変領域又は配列番号58の重鎖可変領域を含む、請求項40に記載の抗体−薬物コンジュゲート化合物。
- 抗CD33抗体が、3つの軽鎖超可変領域(HVR−L1、HVR−L2及びHVR−L3)及び3つの重鎖超可変領域(HVR−H1、HVR−H2及びHVR−H3)を含み、
HVR−L1が配列番号59のアミノ酸配列を含み;
HVR−L2が配列番号60のアミノ酸配列を含み;
HVR−L3が配列番号61のアミノ酸配列を含み;
HVR−H1が配列番号62のアミノ酸配列を含み;
HVR−H2が配列番号63のアミノ酸配列を含み;及び
HVR−H3が配列番号64のアミノ酸配列を含む、請求項40に記載の抗体−薬物コンジュゲート化合物。 - 抗CD33抗体が、配列番号65、配列番号67、配列番号69、及び配列番号71から選択される軽鎖可変領域又は配列番号66、配列番号68、配列番号70、及び配列番号72から選択される重鎖可変領域を含む、請求項40に記載の抗体−薬物コンジュゲート化合物。
- 請求項1から44の何れか一項に記載の抗体−薬物コンジュゲート化合物、及び薬学的に許容される賦形剤を含む薬学的組成物。
- 癌を治療するための医薬であって、請求項45に記載の薬学的組成物の治療的有効量を含む、医薬。
- a)請求項45に記載の薬学的組成物;及び
b)使用説明書
を含む、癌を治療するためのキット。 - 式:
を有するリンカー−薬物中間体であって、
ここで、Xは、マレイミド、チオール、アミノ、ブロミド、ブロモアセトアミド、ヨードアセトアミド、p−トルエンスルホン酸塩、ヨウ化物、ヒドロキシル、カルボキシル、ピリジルジスルフィド、及びN−ヒドロキシスクシンイミドから選択される反応性官能基であり;
Lは、式:
を有するリンカーであり;
ここで、StrはXに共有結合したストレッチャー単位であり;Pepは2から12個のアミノ酸残基の任意のペプチド単位であり、Spは二量体の薬物部分に共有結合した任意のスペーサー単位であり、m及びnは0及び1から独立に選択され;
Dは式:
を有する二量体薬物部分であり、
ここで
R1は、H、P(O)3H2、C(O)NRaRb、又はLへの結合から選択され;
R2は、H、P(O)3H2、C(O)NRaRb、又はLへの結合から選択され;
Ra及びRbは、H及び一以上のFで任意置換されたC1−C6アルキルから独立に選択され、又はRa及びRbは5又は6員複素環基を形成し;
Tは、C3−C12アルキレン、Y、(C1−C6アルキレン)−Y−(C1−C6アルキレン)、(C1−C6アルキレン)−Y−(C1−C6アルキレン)−Y−(C1−C6アルキレン)、(C2−C6アルケニレン)−Y−(C2−C6アルケニレン)及び(C2−C6アルキニレン)−Y−(C2−C6アルキニレン)から選択されるテザー基であり;
ここで、YはO、S、NR1、アリール、及びヘテロアリールから独立に選択され;
ここで、アルキレン、アルケニレン、アリール、及びヘテロアリールは、F、OH、O(C1−C6アルキル)、NH2、NHCH3、N(CH3)2、OP(O)3H2、及びC1−C6アルキルで独立に任意置換され、ここでアルキルは、一以上のFで任意置換され;
又はアルキレン、アルケニレン、アリール及びヘテロアリールは、Lへの結合で独立に任意置換され;
D’は
から選択される薬物部分であり、
ここで波線はTへの結合部位を示し;
X1及びX2は、O及びNR3から独立に選択され、ここでR3は、H及び一以上のFで任意置換されたC1−C6アルキルから選択され;
R4は、H、CO2R、又はLへの結合であり、ここでRはC1−C6アルキル又はベンジルであり;及び
R5は、H又はC1−C6アルキルである、リンカー−薬物中間体。 - 式:
を有するリンカー−薬物中間体に抗体をコンジュゲートすることを含み、
ここで、
Xは、マレイミド、チオール、アミノ、ブロミド、ブロモアセトアミド、ヨードアセトアミド、p−トルエンスルホン酸塩、ヨウ化物、ヒドロキシル、カルボキシル、ピリジルジスルフィド、及びN−ヒドロキシスクシンイミドから選択される反応性官能基であり;
Lは、式:
を有するリンカーであり;
ここで、StrはXに共有結合したストレッチャー単位であり;Pepは2から12個のアミノ酸残基の任意のペプチド単位であり、Spは二量体の薬物部分に共有結合した任意のスペーサー単位であり、m及びnは0及び1から独立に選択され;
Dは式:
を有する二量体薬物部分であり、
ここで
R1は、H、P(O)3H2、C(O)NRaRb、又はLへの結合から選択され;
R2は、H、P(O)3H2、C(O)NRaRb、又はLへの結合から選択され;
Ra及びRbは、H及び一以上のFで任意置換されたC1−C6アルキルから独立に選択され又はRa及びRbは5又は6員複素環基を形成し;
Tは、C3−C12アルキレン、Y、(C1−C6アルキレン)−Y−(C1−C6アルキレン)、(C1−C6アルキレン)−Y−(C1−C6アルキレン)−Y−(C1−C6アルキレン)、(C2−C6アルケニレン)−Y−(C2−C6アルケニレン)及び(C2−C6アルキニレン)−Y−(C2−C6アルキニレン)から選択されるテザー基であり;
ここで、YはO、S、NR1、アリール、及びヘテロアリールから独立に選択され;
ここで、アルキレン、アルケニレン、アリール、及びヘテロアリールは、F、OH、O(C1−C6アルキル)、NH2、NHCH3、N(CH3)2、OP(O)3H2、及びC1−C6アルキルで独立に任意置換され、ここでアルキルは、一以上のFで任意置換され;
又はアルキレン、アルケニレン、アリール及びヘテロアリールは、Lへの結合で独立に任意置換され;
D’は
から選択される薬物部分であり、
ここで波線はTへの結合部位を示し;
X1及びX2は、O及びNR3から独立に選択され、ここでR3は、H及び一以上のFで任意置換されたC1−C6アルキルから選択され;
R4は、H、CO2R、又はLへの結合であり、ここでRはC1−C6アルキル又はベンジルであり;及び
R5は、H又はC1−C6アルキルであり、
これにより抗体−薬物コンジュゲート化合物が形成される、請求項1に記載の抗体−薬物コンジュゲート化合物を製造するための方法。 - 抗体がシステイン操作抗体であり、リンカー−薬物中間体のXがマレイミドである、請求項39に記載の抗体−薬物コンジュゲート化合物を製造するための方法。
- 式:
を有するCBI二量体薬物部分化合物であって、
ここで
R1は、H、P(O)3H2、C(O)NRaRbから選択され;
R2は、H、P(O)3H2、C(O)NRaRbから選択され;
Ra及びRbは、H及び一以上のFで任意置換されたC1−C6アルキルから独立に選択され、
又はRa及びRbは、5又は6員複素環基を形成し;
Tは、C3−C12アルキレン、Y、(C1−C6アルキレン)−Y−(C1−C6アルキレン)、(C1−C6アルキレン)−Y−(C1−C6アルキレン)−Y−(C1−C6アルキレン)、(C2−C6アルケニレン)−Y−(C2−C6アルケニレン)及び(C2−C6アルキニレン)−Y−(C2−C6アルキニレン)から選択されるテザー基であり;
ここで、YはO、S、NR1、アリール、及びヘテロアリールから独立に選択され;
ここで、アルキレン、アルケニレン、アリール、及びヘテロアリールは、F、OH、O(C1−C6アルキル)、NH2、NHCH3、N(CH3)2、OP(O)3H2、及びC1−C6アルキルで独立に任意置換され、ここでアルキルは、一以上のFで任意置換され;
又はアルキレン、アルケニレン、アリール及びヘテロアリールは、Lへの結合で独立に任意置換され;
D’は
から選択される薬物部分であり、
ここで波線はTへの結合部位を示し;
X1及びX2は、O及びNR3から独立に選択され、ここでR3は、H及び一以上のFで任意置換されたC1−C6アルキルから選択され;
R4は、H、CO2Rであり、ここでRはC1−C6アルキル又はベンジルであり;及び
R5は、H又はC1−C6アルキルであり、ただしX 1 −R 1 又はX 2 −R 1 の一つがOHであり、TがC 3 −C 12 アルキレン、且つR 2 がHである場合、もう一方のX 1 −R 1 又はX 2 −R 1 がOHではない、CBI二量体薬物部分化合物。 - pが、1、2、3又は4である、請求項1から22の何れか一項に記載のコンジュゲート。
- pが、1又は2である、請求項1から22の何れか一項に記載のコンジュゲート。
- Abが抗HER2抗体である、請求項57から59の何れか一項に記載のコンジュゲート。
- Abが抗CLL−1抗体である、請求項57から59の何れか一項に記載のコンジュゲート。
- Abが抗CD22抗体である、請求項57から59の何れか一項に記載のコンジュゲート。
- Abが抗CD79b抗体である、請求項57から59の何れか一項に記載のコンジュゲート。
- 請求項65から67の何れか一項に記載の抗体−薬物コンジュゲート、及び薬学的に許容される賦形剤を含む、薬学的組成物。
- 血液疾患を治療するための医薬であって、請求項65から67のいずれか一項に記載の抗体−薬物コンジュゲートの治療的有効量を含む、医薬。
- 白血病を治療するための医薬であって、請求項65から67のいずれか一項に記載の抗体−薬物コンジュゲートの治療的有効量を含む、医薬。
- リンパ腫を治療するための医薬であって、請求項65から67のいずれか一項に記載の抗体−薬物コンジュゲートの治療的有効量を含む、医薬。
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PCT/US2014/042560 WO2015023355A1 (en) | 2013-08-12 | 2014-06-16 | 1-(chloromethyl)-2,3-dihydro-1h-benzo[e]indole dimer antibody-drug conjugate compounds, and methods of use and treatment |
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Families Citing this family (44)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN114246952A (zh) | 2010-06-08 | 2022-03-29 | 基因泰克公司 | 半胱氨酸改造的抗体和偶联物 |
US11147852B2 (en) | 2011-12-23 | 2021-10-19 | Pfizer Inc. | Engineered antibody constant regions for site-specific conjugation and methods and uses therefor |
CA2931340A1 (en) * | 2013-12-13 | 2015-06-18 | Genentech, Inc. | Anti-cd33 antibodies and immunoconjugates |
JP6980384B2 (ja) * | 2013-12-16 | 2021-12-15 | ジェネンテック, インコーポレイテッド | 1−(クロロメチル)−2,3−ジヒドロ−1h−ベンゾ[e]インドール二量体抗体−薬物コンジュゲート化合物、並びに使用及び処置の方法 |
KR102405762B1 (ko) | 2013-12-16 | 2022-06-07 | 제넨테크, 인크. | 펩타이드 모방체 화합물 및 이의 항체-약물 컨쥬게이트 |
PE20161394A1 (es) | 2013-12-16 | 2017-01-06 | Genentech Inc | Compuestos peptidomimeticos y sus conjugados de anticuerpo-farmaco |
MY180257A (en) * | 2014-01-27 | 2020-11-26 | Pfizer | Bifunctional cytotoxic agents |
EP3160513B1 (en) | 2014-06-30 | 2020-02-12 | Glykos Finland Oy | Saccharide derivative of a toxic payload and antibody conjugates thereof |
EA201790545A1 (ru) | 2014-09-12 | 2017-07-31 | Дженентек, Инк. | Антитела и иммуноконъюгаты против her2 |
BR112017003236A2 (pt) | 2014-09-12 | 2017-11-28 | Genentech Inc | anticorpos elaborados com cisteína, conjugados de droga e anticorpos, método de preparação de conjugado de droga e anticorpo e composição farmacêutica |
AR101846A1 (es) | 2014-09-12 | 2017-01-18 | Genentech Inc | Anticuerpos anti-cll-1 e inmunoconjugados |
EP3226909A1 (en) | 2014-12-03 | 2017-10-11 | Genentech, Inc. | Quaternary amine compounds and antibody-drug conjugates thereof |
CN114395050A (zh) | 2015-03-09 | 2022-04-26 | 海德堡医药有限责任公司 | 鹅膏毒素-抗体轭合物 |
AU2016238551B2 (en) | 2015-03-20 | 2020-01-02 | Pfizer Inc. | Bifunctional cytotoxic agents containing the CTI pharmacophore |
WO2016205176A1 (en) * | 2015-06-15 | 2016-12-22 | Genentech, Inc. | Antibodies and immunoconjugates |
TW201718647A (zh) | 2015-06-16 | 2017-06-01 | 建南德克公司 | 抗-cll-1抗體及使用方法 |
CN111533778B (zh) * | 2015-07-28 | 2023-04-25 | 上海皓元生物医药科技有限公司 | 一种抗体偶联药物连接子的工业化生产方法 |
MA43345A (fr) | 2015-10-02 | 2018-08-08 | Hoffmann La Roche | Conjugués anticorps-médicaments de pyrrolobenzodiazépine et méthodes d'utilisation |
MA43354A (fr) | 2015-10-16 | 2018-08-22 | Genentech Inc | Conjugués médicamenteux à pont disulfure encombré |
DE102016105449A1 (de) * | 2015-10-29 | 2017-05-04 | Georg-August-Universität Göttingen Stiftung Öffentlichen Rechts | Bifunktionale Prodrugs |
JP6412906B2 (ja) | 2015-11-03 | 2018-10-24 | 財團法人工業技術研究院Industrial Technology Research Institute | 化合物、リンカー−薬物およびリガンド−薬物複合体 |
CA3005454A1 (en) | 2015-11-18 | 2017-05-26 | Sorrento Therapeutics, Inc. | Chemically-locked bispecific antibodies |
TWI778491B (zh) | 2015-11-30 | 2022-09-21 | 美商輝瑞股份有限公司 | 位點專一性her2抗體藥物共軛體 |
JP2019522633A (ja) | 2016-05-20 | 2019-08-15 | ジェネンテック, インコーポレイテッド | Protac抗体コンジュゲート及び使用方法 |
CN109313200B (zh) | 2016-05-27 | 2022-10-04 | 豪夫迈·罗氏有限公司 | 用于表征位点特异性抗体-药物缀合物的生物分析性方法 |
WO2017214024A1 (en) * | 2016-06-06 | 2017-12-14 | Genentech, Inc. | Silvestrol antibody-drug conjugates and methods of use |
EP3475284B1 (en) | 2016-06-24 | 2022-11-02 | Mersana Therapeutics, Inc. | Pyrrolobenzodiazepines and conjugates thereof |
WO2018031662A1 (en) | 2016-08-11 | 2018-02-15 | Genentech, Inc. | Pyrrolobenzodiazepine prodrugs and antibody conjugates thereof |
WO2018065501A1 (en) * | 2016-10-05 | 2018-04-12 | F. Hoffmann-La Roche Ag | Methods for preparing antibody drug conjugates |
AU2017343565A1 (en) * | 2016-10-10 | 2019-05-30 | Cellerant Therapeutics, Inc. | Isoquinolidinobenzodiazepine (IQB)-1(chloromethyl)-2,3-dihydro-1H-benzo[e]indole (CBI) dimers |
CA3084459A1 (en) | 2016-10-16 | 2018-04-19 | Cellerant Therapeutics, Inc. | Anti-il1-rap antibodies |
US10864279B2 (en) | 2016-12-16 | 2020-12-15 | Industrial Technology Research Institute | Linker-drug and antibody-drug conjugate (ADC) employing the same |
EP3441386B1 (en) * | 2017-08-11 | 2024-04-17 | Georg-August-Universität Göttingen | Method for the synthesis of monoprotected bifunctional prodrugs and antibody drug conjugates based thereon as well as a method for preparing antibody drug conjugates |
US11364303B2 (en) | 2017-09-29 | 2022-06-21 | Pfizer Inc. | Cysteine engineered antibody drug conjugates |
WO2020089811A1 (en) | 2018-10-31 | 2020-05-07 | Novartis Ag | Dc-sign antibody drug conjugates |
WO2020123275A1 (en) | 2018-12-10 | 2020-06-18 | Genentech, Inc. | Photocrosslinking peptides for site specific conjugation to fc-containing proteins |
GB201901197D0 (en) | 2019-01-29 | 2019-03-20 | Femtogenix Ltd | G-A Crosslinking cytotoxic agents |
EP3936151A4 (en) * | 2019-03-07 | 2023-01-11 | ABL Bio, Inc. | ANTIBODY-DRUG CONJUGATE AND USE OF THE DRUG |
AU2021312225A1 (en) | 2020-07-21 | 2023-02-16 | Genentech, Inc. | Antibody-conjugated chemical inducers of degradation of BRM and methods thereof |
JP2021006531A (ja) * | 2020-09-01 | 2021-01-21 | ハンジョウ ディーエーシー バイオテック シーオー.,エルティディ.Hangzhou Dac Biotech Co.,Ltd. | 細胞結合分子の共役のための架橋連結体 |
CN115192732A (zh) * | 2021-04-01 | 2022-10-18 | 成都百利多特生物药业有限责任公司 | 一种dna毒性二聚体化合物及其偶联物 |
AR128330A1 (es) | 2022-01-26 | 2024-04-17 | Genentech Inc | Inductores químicos de degradación conjugados con anticuerpo y métodos de estos |
AR128331A1 (es) | 2022-01-26 | 2024-04-17 | Genentech Inc | Inductores químicos de degradación conjugados con anticuerpos y métodos de estos |
AU2022447933A1 (en) | 2022-03-25 | 2023-11-09 | Baili-Bio (Chengdu) Pharmaceutical Co, Ltd. | Dna toxic dimer compound and conjugate thereof |
Family Cites Families (282)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4816567A (en) | 1983-04-08 | 1989-03-28 | Genentech, Inc. | Recombinant immunoglobin preparations |
JPS6098584A (ja) | 1983-11-02 | 1985-06-01 | Canon Inc | カメラ―体形vtr |
US5807715A (en) | 1984-08-27 | 1998-09-15 | The Board Of Trustees Of The Leland Stanford Junior University | Methods and transformed mammalian lymphocyte cells for producing functional antigen-binding protein including chimeric immunoglobulin |
US5583024A (en) | 1985-12-02 | 1996-12-10 | The Regents Of The University Of California | Recombinant expression of Coleoptera luciferase |
WO1991002536A1 (en) | 1989-08-23 | 1991-03-07 | Scripps Clinic And Research Foundation | Compositions and methods for detection and treatment of epstein-barr virus infection and immune disorders |
US5959177A (en) | 1989-10-27 | 1999-09-28 | The Scripps Research Institute | Transgenic plants expressing assembled secretory antibodies |
US5256643A (en) | 1990-05-29 | 1993-10-26 | The Government Of The United States | Human cripto protein |
AU9016591A (en) | 1990-10-25 | 1992-05-26 | Tanox Biosystems, Inc. | Glycoproteins associated with membrane-bound immunoglobulins as antibody targets on B cells |
US5440021A (en) | 1991-03-29 | 1995-08-08 | Chuntharapai; Anan | Antibodies to human IL-8 type B receptor |
US5543503A (en) | 1991-03-29 | 1996-08-06 | Genentech Inc. | Antibodies to human IL-8 type A receptor |
JP4156662B2 (ja) | 1991-03-29 | 2008-09-24 | ジェネンテック・インコーポレーテッド | ヒトpf4a受容体とその使用 |
CA2103059C (en) | 1991-06-14 | 2005-03-22 | Paul J. Carter | Method for making humanized antibodies |
JP3050424B2 (ja) | 1991-07-12 | 2000-06-12 | 塩野義製薬株式会社 | ヒトエンドセリンリセプター |
US5264557A (en) | 1991-08-23 | 1993-11-23 | The United States Of America As Represented By The Department Of Health And Human Services | Polypeptide of a human cripto-related gene, CR-3 |
WO1993006217A1 (en) | 1991-09-19 | 1993-04-01 | Genentech, Inc. | EXPRESSION IN E. COLI OF ANTIBODY FRAGMENTS HAVING AT LEAST A CYSTEINE PRESENT AS A FREE THIOL, USE FOR THE PRODUCTION OF BIFUNCTIONAL F(ab')2 ANTIBODIES |
US6011146A (en) | 1991-11-15 | 2000-01-04 | Institut Pasteur | Altered major histocompatibility complex (MHC) determinant and methods of using the determinant |
US6153408A (en) | 1991-11-15 | 2000-11-28 | Institut Pasteur And Institut National De La Sante Et De La Recherche Medicale | Altered major histocompatibility complex (MHC) determinant and methods of using the determinant |
IL107366A (en) | 1992-10-23 | 2003-03-12 | Chugai Pharmaceutical Co Ltd | Genes coding for megakaryocyte potentiator |
US5644033A (en) | 1992-12-22 | 1997-07-01 | Health Research, Inc. | Monoclonal antibodies that define a unique antigen of human B cell antigen receptor complex and methods of using same for diagnosis and treatment |
US5801005A (en) | 1993-03-17 | 1998-09-01 | University Of Washington | Immune reactivity to HER-2/neu protein for diagnosis of malignancies in which the HER-2/neu oncogene is associated |
US5869445A (en) | 1993-03-17 | 1999-02-09 | University Of Washington | Methods for eliciting or enhancing reactivity to HER-2/neu protein |
US6214345B1 (en) | 1993-05-14 | 2001-04-10 | Bristol-Myers Squibb Co. | Lysosomal enzyme-cleavable antitumor drug conjugates |
US5773223A (en) | 1993-09-02 | 1998-06-30 | Chiron Corporation | Endothelin B1, (ETB1) receptor polypeptide and its encoding nucleic acid methods, and uses thereof |
US5750370A (en) | 1995-06-06 | 1998-05-12 | Human Genome Sciences, Inc. | Nucleic acid encoding human endothlein-bombesin receptor and method of producing the receptor |
US5789199A (en) | 1994-11-03 | 1998-08-04 | Genentech, Inc. | Process for bacterial production of polypeptides |
US5840523A (en) | 1995-03-01 | 1998-11-24 | Genetech, Inc. | Methods and compositions for secretion of heterologous polypeptides |
JPH08336393A (ja) | 1995-04-13 | 1996-12-24 | Mitsubishi Chem Corp | 光学活性なγ−置換−β−ヒドロキシ酪酸エステルの製造法 |
US5707829A (en) | 1995-08-11 | 1998-01-13 | Genetics Institute, Inc. | DNA sequences and secreted proteins encoded thereby |
US20020193567A1 (en) | 1995-08-11 | 2002-12-19 | Genetics Institute, Inc. | Secreted proteins and polynucleotides encoding them |
JP3646191B2 (ja) | 1996-03-19 | 2005-05-11 | 大塚製薬株式会社 | ヒト遺伝子 |
CA2254843A1 (en) | 1996-05-17 | 1997-11-27 | Schering Corporation | Human b-cell antigens, related reagents |
US5945511A (en) | 1997-02-20 | 1999-08-31 | Zymogenetics, Inc. | Class II cytokine receptor |
US20030185830A1 (en) | 1997-02-25 | 2003-10-02 | Corixa Corporation | Compositions and methods for the therapy and diagnosis of prostate cancer |
US7033827B2 (en) | 1997-02-25 | 2006-04-25 | Corixa Corporation | Prostate-specific polynucleotide compositions |
US6261791B1 (en) | 1997-03-10 | 2001-07-17 | The Regents Of The University Of California | Method for diagnosing cancer using specific PSCA antibodies |
US6541212B2 (en) | 1997-03-10 | 2003-04-01 | The Regents Of The University Of California | Methods for detecting prostate stem cell antigen protein |
DE69824287T2 (de) | 1997-03-10 | 2005-06-16 | The Regents Of The University Of California, Oakland | Prostata stammzell-antigen (psca) |
US6555339B1 (en) | 1997-04-14 | 2003-04-29 | Arena Pharmaceuticals, Inc. | Non-endogenous, constitutively activated human protein-coupled receptors |
US6319688B1 (en) | 1997-04-28 | 2001-11-20 | Smithkline Beecham Corporation | Polynucleotide encoding human sodium dependent phosphate transporter (IPT-1) |
WO1998051824A1 (en) | 1997-05-15 | 1998-11-19 | Abbott Laboratories | Reagents and methods useful for detecting disease of the urinary tract |
US6890749B2 (en) | 1997-05-15 | 2005-05-10 | Abbott Laboratories | Reagents and methods useful for detecting diseases of the prostate |
US6040498A (en) | 1998-08-11 | 2000-03-21 | North Caroline State University | Genetically engineered duckweed |
US6602677B1 (en) | 1997-09-19 | 2003-08-05 | Promega Corporation | Thermostable luciferases and methods of production |
US20030060612A1 (en) | 1997-10-28 | 2003-03-27 | Genentech, Inc. | Compositions and methods for the diagnosis and treatment of tumor |
US20020034749A1 (en) | 1997-11-18 | 2002-03-21 | Billing-Medel Patricia A. | Reagents and methods useful for detecting diseases of the breast |
US6110695A (en) | 1997-12-02 | 2000-08-29 | The Regents Of The University Of California | Modulating the interaction of the chemokine, B Lymphocyte Hemoattractant, and its Receptor, BLR1 |
AU762991B2 (en) | 1998-03-13 | 2003-07-10 | Burnham Institute, The | Molecules that home to various selected organs or tissues |
JP2002520000A (ja) | 1998-05-13 | 2002-07-09 | エピミューン, インコーポレイテッド | 免疫応答を刺激するための発現ベクターおよびそのベクターの使用方法 |
US20030064397A1 (en) | 1998-05-22 | 2003-04-03 | Incyte Genomics, Inc. | Transmembrane protein differentially expressed in prostate and lung tumors |
US20020187472A1 (en) | 2001-03-09 | 2002-12-12 | Preeti Lal | Steap-related protein |
EP1413582B1 (en) | 1998-08-27 | 2006-03-15 | Spirogen Limited | Dimeric pyrrolobenzodiazepines |
WO2000012130A1 (en) | 1998-08-27 | 2000-03-09 | Smithkline Beecham Corporation | Rp105 agonists and antagonists |
JP4689781B2 (ja) | 1998-09-03 | 2011-05-25 | 独立行政法人科学技術振興機構 | アミノ酸輸送蛋白及びその遺伝子 |
WO2000020579A1 (en) | 1998-10-02 | 2000-04-13 | Mcmaster University | Spliced form of erbb-2/neu oncogene |
WO2001057188A2 (en) | 2000-02-03 | 2001-08-09 | Hyseq, Inc. | Novel nucleic acids and polypeptides |
US20020119158A1 (en) | 1998-12-17 | 2002-08-29 | Corixa Corporation | Compositions and methods for the therapy and diagnosis of ovarian cancer |
US6962980B2 (en) | 1999-09-24 | 2005-11-08 | Corixa Corporation | Compositions and methods for the therapy and diagnosis of ovarian cancer |
US20030091580A1 (en) | 2001-06-18 | 2003-05-15 | Mitcham Jennifer L. | Compositions and methods for the therapy and diagnosis of ovarian cancer |
US6858710B2 (en) | 1998-12-17 | 2005-02-22 | Corixa Corporation | Compositions and methods for the therapy and diagnosis of ovarian cancer |
US6468546B1 (en) | 1998-12-17 | 2002-10-22 | Corixa Corporation | Compositions and methods for therapy and diagnosis of ovarian cancer |
EP1141017B1 (en) | 1998-12-30 | 2008-09-10 | Beth Israel Deaconess Medical Center, Inc. | Characterization of the soc/crac calcium channel protein family |
US20030190669A1 (en) | 1998-12-30 | 2003-10-09 | Genentech, Inc. | Secreted and transmembrane polypeptides and nucleic acids encoding the same |
CN1201004C (zh) | 1999-01-29 | 2005-05-11 | 考丽克萨有限公司 | HER-2/neu融合蛋白 |
GB9905124D0 (en) | 1999-03-05 | 1999-04-28 | Smithkline Beecham Biolog | Novel compounds |
AU3395900A (en) | 1999-03-12 | 2000-10-04 | Human Genome Sciences, Inc. | Human lung cancer associated gene sequences and polypeptides |
US7312303B2 (en) | 1999-05-11 | 2007-12-25 | Genentech, Inc. | Anti-PRO4980 antibodies |
AU4952600A (en) | 1999-06-03 | 2000-12-28 | Takeda Chemical Industries Ltd. | Screening method with the use of cd100 |
US6949245B1 (en) | 1999-06-25 | 2005-09-27 | Genentech, Inc. | Humanized anti-ErbB2 antibodies and treatment with anti-ErbB2 antibodies |
EP2283867B1 (en) | 1999-06-25 | 2014-05-21 | ImmunoGen, Inc. | Methods of treatment using anti-ERBB antibody-maytansinoid conjugates |
US20030119113A1 (en) | 1999-07-20 | 2003-06-26 | Genentech, Inc. | Secreted and transmembrane polypeptides and nucleic acids encoding the same |
US7297770B2 (en) | 1999-08-10 | 2007-11-20 | Genentech, Inc. | PRO6496 polypeptides |
US7294696B2 (en) | 1999-08-17 | 2007-11-13 | Genentech Inc. | PRO7168 polypeptides |
AU7573000A (en) | 1999-09-01 | 2001-03-26 | Genentech Inc. | Secreted and transmembrane polypeptides and nucleic acids encoding the same |
US20030129192A1 (en) | 1999-09-10 | 2003-07-10 | Corixa Corporation | Compositions and methods for the therapy and diagnosis of ovarian cancer |
US20030232056A1 (en) | 1999-09-10 | 2003-12-18 | Corixa Corporation | Compositions and methods for the therapy and diagnosis of ovarian cancer |
US20030206918A1 (en) | 1999-09-10 | 2003-11-06 | Corixa Corporation | Compositions and methods for the therapy and diagnosis of ovarian cancer |
BR0014480A (pt) | 1999-10-04 | 2002-06-11 | Medicago Inc | Método para regular a transcrição de genes estranhos |
US7125978B1 (en) | 1999-10-04 | 2006-10-24 | Medicago Inc. | Promoter for regulating expression of foreign genes |
US6750054B2 (en) | 2000-05-18 | 2004-06-15 | Lexicon Genetics Incorporated | Human semaphorin homologs and polynucleotides encoding the same |
EP1226177B1 (en) | 1999-10-29 | 2008-07-09 | Genentech, Inc. | Anti-prostate stem cell antigen (psca) antibody compositions and methods of use |
EP2404927B1 (en) | 1999-11-29 | 2016-05-11 | The Trustees of Columbia University in the City of New York | Isolation of five novel genes coding for new fc receptors-type melanoma involved in the pathogenesis of lymphoma/melanoma |
EP1248800A2 (en) | 1999-11-30 | 2002-10-16 | Corixa Corporation | Compositions and methods for therapy and diagnosis of breast cancer |
CA2393738A1 (en) | 1999-12-10 | 2001-06-14 | Epimmune Inc. | Inducing cellular immune responses to her2/neu using peptide and nucleic acid compositions |
EP2295078A3 (en) | 1999-12-23 | 2011-03-23 | ZymoGenetics, L.L.C. | Method for treating inflammation |
US6610286B2 (en) | 1999-12-23 | 2003-08-26 | Zymogenetics, Inc. | Method for treating inflammation using soluble receptors to interleukin-20 |
DK1246846T3 (da) | 1999-12-23 | 2008-12-08 | Zymogenetics Inc | Oplöselig interleukin-20-receptor |
NZ502058A (en) | 1999-12-23 | 2003-11-28 | Ovita Ltd | Isolated mutated nucleic acid molecule for regulation of ovulation rate |
WO2001045746A2 (en) | 1999-12-24 | 2001-06-28 | Genentech, Inc. | Methods and compositions for prolonging elimination half-times of bioactive compounds |
US20040001827A1 (en) | 2002-06-28 | 2004-01-01 | Dennis Mark S. | Serum albumin binding peptides for tumor targeting |
US7294695B2 (en) | 2000-01-20 | 2007-11-13 | Genentech, Inc. | PRO10268 polypeptides |
WO2001053463A2 (en) | 2000-01-21 | 2001-07-26 | Corixa Corporation | COMPOUNDS AND METHODS FOR PREVENTION AND TREATMENT OF HER-2/neu ASSOCIATED MALIGNANCIES |
US20030224379A1 (en) | 2000-01-21 | 2003-12-04 | Tang Y. Tom | Novel nucleic acids and polypeptides |
AU2001238596A1 (en) | 2000-02-22 | 2001-09-03 | Millennium Pharmaceuticals, Inc. | 18607, a novel human calcium channel |
US20030219806A1 (en) | 2000-02-22 | 2003-11-27 | Millennium Pharmaceuticals, Inc. | Novel 18607, 15603, 69318, 12303, 48000, 52920, 5433, 38554, 57301, 58324, 55063, 52991, 59914, 59921 and 33751 molecules and uses therefor |
US20040005561A1 (en) | 2000-03-01 | 2004-01-08 | Corixa Corporation | Compositions and methods for the detection, diagnosis and therapy of hematological malignancies |
US20040002068A1 (en) | 2000-03-01 | 2004-01-01 | Corixa Corporation | Compositions and methods for the detection, diagnosis and therapy of hematological malignancies |
AU2001245280A1 (en) | 2000-03-07 | 2001-09-17 | Hyseq, Inc. | Novel nucleic acids and polypeptides |
AU2001249411B2 (en) | 2000-03-24 | 2007-02-15 | Fahri Saatcioglu | Novel prostate-specific or testis-specific nucleic acid molecules, polypeptides,and diagnostic and therapeutic methods |
AU2001250412A1 (en) | 2000-03-31 | 2001-10-08 | Ipf Pharmaceuticals Gmbh | Diagnostic and medicament for analysing the cell surface proteome of tumour and inflammatory cells and for treating tumorous and inflammatory diseases, preferably using specific chemokine receptor analysis and the chemokine receptor-ligand interaction |
US7279294B2 (en) | 2000-04-03 | 2007-10-09 | The United States Of America As Represented By The Secretary, Dept. Of Health And Human Services, Nih | Tumor markers in ovarian cancer |
CA2402392A1 (en) | 2000-04-07 | 2001-10-18 | Arena Pharmaceuticals, Inc. | Non-endogenous, constitutively activated known g protein-coupled receptors |
US20030119115A1 (en) | 2000-05-17 | 2003-06-26 | Genentech, Inc. | Secreted and transmembrane polypeptides and nucleic acids encoding the same |
WO2001090304A2 (en) | 2000-05-19 | 2001-11-29 | Human Genome Sciences, Inc. | Nucleic acids, proteins, and antibodies |
US20020051990A1 (en) | 2000-06-09 | 2002-05-02 | Eric Ople | Novel gene targets and ligands that bind thereto for treatment and diagnosis of ovarian carcinomas |
WO2001098351A2 (en) | 2000-06-16 | 2001-12-27 | Incyte Genomics, Inc. | G-protein coupled receptors |
JP2004502414A (ja) | 2000-06-30 | 2004-01-29 | ヒューマン ジノーム サイエンシーズ, インコーポレイテッド | B7様ポリヌクレオチド、ポリペプチドおよび抗体 |
EP1294885A2 (en) | 2000-06-30 | 2003-03-26 | Amgen, Inc. | B7-like molecules and uses thereof |
WO2002002634A2 (en) | 2000-06-30 | 2002-01-10 | Incyte Genomics, Inc. | Human extracellular matrix and cell adhesion polypeptides |
WO2002006339A2 (en) | 2000-07-03 | 2002-01-24 | Curagen Corporation | Proteins and nucleic acids encoding same |
US20040044179A1 (en) | 2000-07-25 | 2004-03-04 | Genentech, Inc. | Secreted and transmembrane polypeptides and nucleic acids encoding the same |
US6891030B2 (en) | 2000-07-27 | 2005-05-10 | Mayo Foundation For Medical Education And Research | T-cell immunoregulatory molecule |
US7205108B2 (en) | 2000-07-28 | 2007-04-17 | Ulrich Wissenbach | Trp8, Trp9 and Trp10, novel markers for cancer |
US7229623B1 (en) | 2000-08-03 | 2007-06-12 | Corixa Corporation | Her-2/neu fusion proteins |
AU2001283360A1 (en) | 2000-08-14 | 2002-02-25 | Corixa Corporation | Methods for diagnosis and therapy of hematological and virus-associated malignancies |
PL365789A1 (en) | 2000-08-14 | 2005-01-10 | Corixa Corporation | Compositions and methods for the therapy and diagnosis of her-2/neu-associated malignancies |
GB0020953D0 (en) | 2000-08-24 | 2000-10-11 | Smithkline Beecham Biolog | Vaccine |
EP1445317A3 (en) | 2000-08-24 | 2004-12-15 | Genentech Inc. | Compositions and methods for the diagnosis and treatment of tumor |
WO2002022660A2 (en) | 2000-09-11 | 2002-03-21 | Hyseq, Inc. | Novel nucleic acids and polypeptides |
US20030119121A1 (en) | 2000-09-15 | 2003-06-26 | Genentech, Inc. | Secreted and transmembrane polypeptides and nucleic acids encoding the same |
ATE333888T1 (de) | 2000-09-15 | 2006-08-15 | Zymogenetics Inc | Verwendung eines polypeptids, welches die extrazelluläre domäne von il-20ra und il-20rb enthält, zur behandlung von entzündungen |
US6613567B1 (en) | 2000-09-15 | 2003-09-02 | Isis Pharmaceuticals, Inc. | Antisense inhibition of Her-2 expression |
UA83458C2 (uk) | 2000-09-18 | 2008-07-25 | Байоджен Айдек Ма Інк. | Виділений поліпептид baff-r (рецептор фактора активації в-клітин сімейства tnf) |
CA2422814A1 (en) | 2000-09-18 | 2002-03-21 | Biogen, Inc. | Cripto mutant and uses thereof |
EP1474528A4 (en) | 2000-10-13 | 2006-06-14 | Protein Design Labs Inc | METHODS FOR DIAGNOSING PROSTATE CANCER, COMPOSITIONS AND METHODS FOR SCREENING PROSTATE CANCER MODULATORS |
AU2002230659A1 (en) | 2000-11-07 | 2002-05-21 | Zymogenetics Inc. | Human tumor necrosis factor receptor |
US20020150573A1 (en) | 2000-11-10 | 2002-10-17 | The Rockefeller University | Anti-Igalpha-Igbeta antibody for lymphoma therapy |
WO2002061087A2 (en) | 2000-12-19 | 2002-08-08 | Lifespan Biosciences, Inc. | Antigenic peptides, such as for g protein-coupled receptors (gpcrs), antibodies thereto, and systems for identifying such antigenic peptides |
WO2002054940A2 (en) | 2001-01-12 | 2002-07-18 | University Of Medicine & Dentistry Of New Jersey | Bone morphogenetic protein-2 in the treatment and diagnosis of cancer |
US20030119119A1 (en) | 2001-01-16 | 2003-06-26 | Genentech, Inc. | Secreted and transmembrane polypeptides and nucleic acids encoding the same |
US20030119126A1 (en) | 2001-01-16 | 2003-06-26 | Genentech, Inc. | Secreted and transmembrane polypeptides and nucleic acids encoding the same |
US7754208B2 (en) | 2001-01-17 | 2010-07-13 | Trubion Pharmaceuticals, Inc. | Binding domain-immunoglobulin fusion proteins |
WO2002059377A2 (en) | 2001-01-24 | 2002-08-01 | Protein Design Labs | Methods of diagnosis of breast cancer, compositions and methods of screening for modulators of breast cancer |
AU2002251841A1 (en) | 2001-01-30 | 2002-08-12 | Corixa Corporation | Compositions and methods for the therapy and diagnosis of pancreatic cancer |
WO2002064775A1 (en) | 2001-02-12 | 2002-08-22 | Bionomics Limited | Identification of genes involved in the tumourigenic process |
AU2002258518A1 (en) | 2001-03-14 | 2002-09-24 | Millennium Pharmaceuticals, Inc. | Nucleic acid molecules and proteins for the identification, assessment, prevention, and therapy of ovarian cancer |
US20040236091A1 (en) | 2001-03-28 | 2004-11-25 | Chicz Roman M. | Translational profiling |
WO2003008537A2 (en) | 2001-04-06 | 2003-01-30 | Mannkind Corporation | Epitope sequences |
US6820011B2 (en) | 2001-04-11 | 2004-11-16 | The Regents Of The University Of Colorado | Three-dimensional structure of complement receptor type 2 and uses thereof |
JP5232350B2 (ja) | 2001-04-17 | 2013-07-10 | ザ ボード オブ トラスティーズ オブ ザ ユニバーシティ オブ アーカンソー | Ca125遺伝子のリピート配列並びに診断および治療的介入のためのその使用 |
CA2444691A1 (en) | 2001-04-18 | 2002-10-31 | Protein Design Labs, Inc. | Methods of diagnosis of lung cancer, compositions and methods of screening for modulators of lung cancer |
DE60230868D1 (de) | 2001-04-26 | 2009-03-05 | Biogen Inc | Criptoblockierende antikörper und deren verwendung |
JP2005504513A (ja) | 2001-05-09 | 2005-02-17 | コリクサ コーポレイション | 前立腺癌の治療及び診断のための組成物及び方法 |
WO2002092836A2 (en) | 2001-05-11 | 2002-11-21 | Sloan-Kettering Institute For Cancer Research | Nucleic acid sequence encoding ovarian antigen, ca125, and uses thereof |
EA007275B1 (ru) | 2001-05-24 | 2006-08-25 | Займодженетикс, Инк. | Слитые белки taci-иммуноглобулина |
WO2002098358A2 (en) | 2001-06-04 | 2002-12-12 | Eos Biotechnology, Inc. | Methods of diagnosis and treatment of androgen-dependent prostate cancer, prostate cancer undergoing androgen-withdrawal, and androgen-independent prostate cancer |
JP2005518185A (ja) | 2001-06-04 | 2005-06-23 | キュラジェン コーポレイション | 新規タンパク質およびそれをコード化する核酸 |
ATE483976T1 (de) | 2001-06-05 | 2010-10-15 | Exelixis Inc | Gfats als modifikatoren des p53-wegs und verwendungsverfahren |
WO2002099060A2 (en) | 2001-06-05 | 2002-12-12 | Exelixis, Inc. | Dgks as modifiers of the p53 pathway and methods of use |
US7235358B2 (en) | 2001-06-08 | 2007-06-26 | Expression Diagnostics, Inc. | Methods and compositions for diagnosing and monitoring transplant rejection |
WO2002101075A2 (en) | 2001-06-13 | 2002-12-19 | Millennium Pharmaceuticals, Inc. | Novel genes, compositions, kits, and methods for identification, assessment, prevention, and therapy of cervical cancer |
AU2002347428A1 (en) | 2001-06-18 | 2003-01-02 | Eos Biotechnology Inc. | Methods of diagnosis of ovarian cancer, compositions and methods of screening for modulators of ovarian cancer |
US7189507B2 (en) | 2001-06-18 | 2007-03-13 | Pdl Biopharma, Inc. | Methods of diagnosis of ovarian cancer, compositions and methods of screening for modulators of ovarian cancer |
US20030148408A1 (en) | 2001-09-18 | 2003-08-07 | Genentech, Inc. | Compositions and methods for the diagnosis and treatment of tumor |
US7705120B2 (en) | 2001-06-21 | 2010-04-27 | Millennium Pharmaceuticals, Inc. | Compositions, kits, and methods for identification, assessment, prevention, and therapy of breast cancer |
WO2003002717A2 (en) | 2001-06-28 | 2003-01-09 | Schering Corporation | Biological activity of ak155 |
US20030120040A1 (en) | 2001-06-29 | 2003-06-26 | Genentech, Inc. | Secreted and Transmembrane polypeptides and nucleic acids encoding the same |
AU2002314433A1 (en) | 2001-07-02 | 2003-01-21 | Licentia Ltd. | Ephrin-tie receptor materials and methods |
US20040076955A1 (en) | 2001-07-03 | 2004-04-22 | Eos Biotechnology, Inc. | Methods of diagnosis of bladder cancer, compositions and methods of screening for modulators of bladder cancer |
WO2003003984A2 (en) | 2001-07-05 | 2003-01-16 | Curagen Corporation | Novel proteins and nucleic acids encoding same |
US7446185B2 (en) | 2001-07-18 | 2008-11-04 | The Regents Of The University Of California | Her2/neu target antigen and use of same to stimulate an immune response |
WO2003009814A2 (en) | 2001-07-25 | 2003-02-06 | Millennium Pharmaceuticals, Inc. | Novel genes, compositions, kits, and methods for identification, assessment, prevention, and therapy of prostate cancer |
HUP0500992A3 (en) | 2001-08-03 | 2007-11-28 | Genentech Inc | Tacis and br3 polypeptides and uses thereof |
CA2457819A1 (en) | 2001-08-14 | 2003-02-27 | The General Hospital Corporation | Nucleic acid and amino acid sequences involved in pain |
US20030092013A1 (en) | 2001-08-16 | 2003-05-15 | Vitivity, Inc. | Diagnosis and treatment of vascular disease |
WO2003018621A2 (en) | 2001-08-23 | 2003-03-06 | Oxford Biomedica (Uk) Limited | Genes |
US6902930B2 (en) | 2001-08-29 | 2005-06-07 | Vanderbilt University | Human Mob-5 (IL-24) receptors and uses thereof |
US20030124579A1 (en) | 2001-09-05 | 2003-07-03 | Eos Biotechnology, Inc. | Methods of diagnosis of ovarian cancer, compositions and methods of screening for modulators of ovarian cancer |
JP2005505271A (ja) | 2001-09-06 | 2005-02-24 | アジェンシス, インコーポレイテッド | 癌の処置および検出において有用なsteap−1と名称が与えられる核酸および対応するタンパク質 |
WO2003025138A2 (en) | 2001-09-17 | 2003-03-27 | Protein Design Labs, Inc. | Methods of diagnosis of cancer compositions and methods of screening for modulators of cancer |
US20050004017A1 (en) | 2001-09-18 | 2005-01-06 | Yuval Reiss | Methods and compositions for treating hcap associated diseases |
CA2460621A1 (en) | 2001-09-19 | 2003-03-27 | Nuvelo, Inc. | Novel nucleic acids and polypeptides |
US7091186B2 (en) * | 2001-09-24 | 2006-08-15 | Seattle Genetics, Inc. | p-Amidobenzylethers in drug delivery agents |
US20030077644A1 (en) | 2001-09-28 | 2003-04-24 | Bing Yang | Diagnosis and treatment of diseases caused by mutations in CD72 |
US20040249144A1 (en) | 2001-10-03 | 2004-12-09 | Zairen Sun | Regulated breast cancer genes |
WO2003029277A2 (en) | 2001-10-03 | 2003-04-10 | Rigel Pharmaceuticals, Inc. | Modulators of lymphocyte activation and migration |
US20050123925A1 (en) | 2002-11-15 | 2005-06-09 | Genentech, Inc. | Compositions and methods for the diagnosis and treatment of tumor |
EP1578385A4 (en) | 2001-10-19 | 2011-11-09 | Genentech Inc | COMPOSITIONS AND METHODS FOR THE DIAGNOSIS AND TREATMENT OF INFLAMMATORY INTESTINAL DISEASES |
WO2003035846A2 (en) | 2001-10-24 | 2003-05-01 | National Jewish Medical And Research Center | Structure of tall-1 and its cognate receptor |
JP4255382B2 (ja) | 2001-10-31 | 2009-04-15 | アルコン,インコーポレイテッド | 骨形成タンパク質(bmp)、bmpレセプターおよびbmp結合タンパク質ならびに緑内障の診断および処置におけるそれらの使用 |
US20030232350A1 (en) | 2001-11-13 | 2003-12-18 | Eos Biotechnology, Inc. | Methods of diagnosis of cancer, compositions and methods of screening for modulators of cancer |
WO2003042661A2 (en) | 2001-11-13 | 2003-05-22 | Protein Design Labs, Inc. | Methods of diagnosis of cancer, compositions and methods of screening for modulators of cancer |
US7344843B2 (en) | 2001-11-29 | 2008-03-18 | Serono Genetics Institute S.A. | Agonists and antagonists of prolixin for the treatment of metabolic disorders |
WO2003048202A2 (en) | 2001-12-03 | 2003-06-12 | Asahi Kasei Pharma Corporation | Nf-kappab activating genes |
AU2002366951A1 (en) | 2001-12-10 | 2003-07-09 | Nuvelo,Inc. | Novel nucleic acids and polypeptides |
US20030134790A1 (en) | 2002-01-11 | 2003-07-17 | University Of Medicine And Dentistry Of New Jersey | Bone Morphogenetic Protein-2 And Bone Morphogenetic Protein-4 In The Treatment And Diagnosis Of Cancer |
US7452675B2 (en) | 2002-01-25 | 2008-11-18 | The Queen's Medical Center | Methods of screening for TRPM4b modulators |
AU2003215365A1 (en) | 2002-02-21 | 2003-09-09 | Duke University | Treatment methods using anti-cd22 antibodies |
EP2388265A1 (en) | 2002-02-22 | 2011-11-23 | Genentech, Inc. | Compositions and methods for the treatment of immune related diseases |
WO2003083047A2 (en) | 2002-03-01 | 2003-10-09 | Exelixis, Inc. | MP53s AS MODIFIERS OF THE p53 PATHWAY AND METHODS OF USE |
US20050220798A1 (en) | 2002-06-04 | 2005-10-06 | Reinhard Ebner | Cancer-linked gene as target for chemotherapy |
WO2003104399A2 (en) | 2002-06-07 | 2003-12-18 | Avalon Pharmaceuticals, Inc | Cancer-linked gene as target for chemotherapy |
EP2258712A3 (en) | 2002-03-15 | 2011-05-04 | Multicell Immunotherapeutics, Inc. | Compositions and Methods to Initiate or Enhance Antibody and Major-histocompatibility Class I or Class II-restricted T Cell Responses by Using Immunomodulatory, Non-coding RNA Motifs |
CA2486490A1 (en) | 2002-03-19 | 2003-12-31 | Curagen Corporation | Therapeutic polypeptides, nucleic acids encoding same, and methods of use |
CA2478981A1 (en) | 2002-03-21 | 2003-10-02 | Sunesis Pharmaceuticals, Inc. | Identification of kinase inhibitors |
JP2005520566A (ja) | 2002-03-22 | 2005-07-14 | バイオジェン・アイデック・エムエイ・インコーポレイテッド | Cripto特異的抗体 |
US7193069B2 (en) | 2002-03-22 | 2007-03-20 | Research Association For Biotechnology | Full-length cDNA |
US7317087B2 (en) | 2002-03-25 | 2008-01-08 | The Uab Research Foundation | Members of the FC receptor homolog gene family (FCRH1-3, 6), related reagents, and uses thereof |
WO2003083074A2 (en) | 2002-03-28 | 2003-10-09 | Idec Pharmaceuticals Corporation | Novel gene targets and ligands that bind thereto for treatment and diagnosis of colon carcinomas |
US20030194704A1 (en) | 2002-04-03 | 2003-10-16 | Penn Sharron Gaynor | Human genome-derived single exon nucleic acid probes useful for gene expression analysis two |
BR0308953A (pt) | 2002-04-05 | 2006-03-14 | Agensys Inc | composições, proteìna, polinucleotìdeo, método de geração de uma resposta imune, método de detecção, composição farmacêutica, anticorpo ou seu fragmento, animal transgênico, hibridoma, método de fornecimento de um agente citotóxico ou agente de diagnóstico e método de inibição do crescimento de células cancerosas |
US20040101874A1 (en) | 2002-04-12 | 2004-05-27 | Mitokor Inc. | Targets for therapeutic intervention identified in the mitochondrial proteome |
MXPA04010092A (es) | 2002-04-16 | 2004-12-13 | Genentech Inc | Composiciones y metodos para el diagnostico y tratamiento de tumores. |
AU2003239158A1 (en) | 2002-04-17 | 2003-11-03 | Baylor College Of Medicine | Aib1 as a prognostic marker and predictor of resistance to encocrine therapy |
WO2003093444A2 (en) | 2002-05-03 | 2003-11-13 | Incyte Corporation | Transporters and ion channels |
US20090068178A1 (en) | 2002-05-08 | 2009-03-12 | Genentech, Inc. | Compositions and Methods for the Treatment of Tumor of Hematopoietic Origin |
CA2485983A1 (en) | 2002-05-15 | 2003-11-27 | Avalon Pharmaceuticals | Cancer-linked gene as target for chemotherapy |
AU2003232453A1 (en) | 2002-05-30 | 2003-12-19 | David K. Bol | Human solute carrier family 7 member 11 (hslc7a11) |
AU2003240495A1 (en) | 2002-06-04 | 2003-12-19 | Incyte Corporation | Diagnostics markers for lung cancer |
DK1513934T3 (da) | 2002-06-06 | 2011-05-02 | Oncotherapy Science Inc | Gener og polypeptider relateret til humane coloncancersygdomme |
WO2003104270A2 (en) | 2002-06-06 | 2003-12-18 | Ingenium Pharmaceuticals Ag | Dudulin 2 genes, expression products, non-human animal model: uses in human hematological disease |
WO2003105758A2 (en) | 2002-06-12 | 2003-12-24 | Avalon Pharmaceuticals, Inc. | Cancer-linked gene as target for chemotherapy |
US20040249130A1 (en) | 2002-06-18 | 2004-12-09 | Martin Stanton | Aptamer-toxin molecules and methods for using same |
EP1552002A4 (en) | 2002-06-18 | 2006-02-08 | Archemix Corp | APTAMER TOXIN MOLECULES AND METHOD FOR THEIR USE |
WO2004000221A2 (en) | 2002-06-20 | 2003-12-31 | The Regents Of The University Of California | Compositions and methods for modulating lymphocyte activity |
EP1534331B1 (en) | 2002-06-21 | 2014-10-29 | Johns Hopkins University School of Medicine | Membrane associated tumor endothelium markers |
WO2004009622A2 (en) | 2002-07-19 | 2004-01-29 | Cellzome Ag | Protein complexes of cellular networks underlying the development of cancer and other diseases |
CN1692127A (zh) | 2002-07-25 | 2005-11-02 | 健泰科生物技术公司 | Taci抗体及其用途 |
ES2556641T3 (es) | 2002-07-31 | 2016-01-19 | Seattle Genetics, Inc. | Conjugados de fármacos y su uso para tratar cáncer, una enfermedad autoinmune o una enfermedad infecciosa |
AU2003251471A1 (en) | 2002-08-06 | 2004-02-25 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with human cxc chemokine receptor 5(cxcr5) |
JP2004121218A (ja) | 2002-08-06 | 2004-04-22 | Jenokkusu Soyaku Kenkyusho:Kk | 気管支喘息または慢性閉塞性肺疾患の検査方法 |
MXPA05001933A (es) | 2002-08-19 | 2005-04-28 | Genentech Inc | Composiciones y metodos para el diagnostico y tratamiento de tumores. |
AU2003278725A1 (en) | 2002-08-27 | 2004-03-19 | Bristol-Myers Squibb Company | Polynucleotide predictor set for identifying protein tyrosine kinase modulators |
WO2004020595A2 (en) | 2002-08-29 | 2004-03-11 | Five Prime Therapeutics, Inc. | Novel human polypeptides encoded by polynucleotides |
AU2002951346A0 (en) | 2002-09-05 | 2002-09-26 | Garvan Institute Of Medical Research | Diagnosis of ovarian cancer |
MXPA05002455A (es) | 2002-09-06 | 2005-06-03 | Mannkind Corp | Secuencias de epitopes. |
EP1581648A2 (en) | 2002-09-09 | 2005-10-05 | Nura, Inc. | G protein coupled receptors and uses thereof |
JP2004113151A (ja) | 2002-09-27 | 2004-04-15 | Sankyo Co Ltd | 癌遺伝子及びその用途 |
EP1554309A2 (en) | 2002-10-03 | 2005-07-20 | McGILL UNIVERSITY | Antibodies and cyclic peptides which bind cea (carcinoembryonic antigen) and their use as cancer therapeutics |
US20060183120A1 (en) | 2002-10-04 | 2006-08-17 | Teh Bin T | Molecular sub-classification of kidney tumors and the discovery of new diagnostic markers |
MXPA05004677A (es) | 2002-10-31 | 2005-11-17 | Genentech Inc | Metodos y composiciones para aumentar la produccion de anticuerpos. |
EP1581169A4 (en) | 2002-11-08 | 2008-09-17 | Genentech Inc | COMPOSITIONS AND METHODS FOR TREATING DISEASES RELATED TO NATURAL K CELLS |
EP1578940A4 (en) | 2002-11-13 | 2007-12-12 | Genentech Inc | METHOD AND COMPOSITIONS FOR DYSPLASED DIAGNOSIS |
JP2006516189A (ja) | 2002-11-15 | 2006-06-29 | ザ ボード オブ トラスティーズ オブ ザ ユニバーシティ オブ アーカンソー | Ca125遺伝子、および診断および治療のためのその使用 |
JP4915980B2 (ja) | 2002-11-15 | 2012-04-11 | エムユーエスシー ファウンデーション フォー リサーチ デベロップメント | 補体レセプター2標的化補体調節因子 |
WO2004046342A2 (en) | 2002-11-20 | 2004-06-03 | Biogen Idec Inc. | Novel gene targets and ligands that bind thereto for treatment and diagnosis of carcinomas |
US7557092B2 (en) | 2002-11-21 | 2009-07-07 | University Of Utah Research Foundation | Purinergic modulation of smell |
AU2003298786A1 (en) | 2002-11-26 | 2004-06-18 | Protein Design Labs, Inc. | Methods of detecting soft tissue sarcoma, compositions and methods of screening for soft tissue sarcoma modulators |
US20070154886A1 (en) | 2002-12-06 | 2007-07-05 | Macina Roberto A | Composition, splice variants and methods relating to ovarian specific genes and proteins |
JP2004198419A (ja) | 2002-12-13 | 2004-07-15 | Bayer Healthcare Llc | Timp1を用いた検出方法 |
WO2004058171A2 (en) | 2002-12-20 | 2004-07-15 | Protein Design Labs, Inc. | Antibodies against gpr64 and uses thereof |
AU2003299819A1 (en) | 2002-12-23 | 2004-07-22 | Human Genome Sciences, Inc. | Neutrokine-alpha conjugate, neutrokine-alpha complex, and uses thereof |
WO2004063709A2 (en) | 2003-01-08 | 2004-07-29 | Bristol-Myers Squibb Company | Biomarkers and methods for determining sensitivity to epidermal growth factor receptor modulators |
US20050227301A1 (en) | 2003-01-10 | 2005-10-13 | Polgen | Cell cycle progression proteins |
WO2004063355A2 (en) | 2003-01-10 | 2004-07-29 | Protein Design Labs, Inc. | Novel methods of diagnosis of metastatic cancer, compositions and methods of screening for modulators of matastatic cancer |
WO2004065577A2 (en) | 2003-01-14 | 2004-08-05 | Bristol-Myers Squibb Company | Polynucleotides and polypeptides associated with the nf-kb pathway |
EP1583821A4 (en) | 2003-01-15 | 2007-07-18 | Millennium Pharm Inc | METHODS AND COMPOSITIONS FOR TREATING UROLOGICAL DISORDERS USING GENES 44390, 54181, 211, 5687, 884, 1405, 636, 4421, 5410, 30905, 2045, 16405, 18560, 2047, 33751, 52872, 14063, 20739, 32544, 43239, 44373, 51164, 53010, 16852, 1587, 2207, 22245, 2387, 52908, 69112, 14990, 18547, 115, 579 |
AU2004205684A1 (en) | 2003-01-23 | 2004-08-05 | Genentech, Inc. | Methods for producing humanized antibodies and improving yield of antibodies or antigen binding fragments in cell culture |
WO2004065491A1 (en) | 2003-01-24 | 2004-08-05 | Schering Ag | Hydrophilic, thiol-reactive cyanine dyes and conjugates thereof with biomolecules for fluorescence diagnosis |
CA2516128A1 (en) | 2003-02-14 | 2004-09-02 | Sagres Discovery, Inc. | Therapeutic targets in cancer |
US20030224411A1 (en) | 2003-03-13 | 2003-12-04 | Stanton Lawrence W. | Genes that are up- or down-regulated during differentiation of human embryonic stem cells |
AU2004284075A1 (en) | 2003-10-22 | 2005-05-06 | Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services | Pyrrolobenzodiazepine derivatives, compositions comprising the same and methods related thereto |
SG195524A1 (en) | 2003-11-06 | 2013-12-30 | Seattle Genetics Inc | Monomethylvaline compounds capable of conjugation to ligands |
PT2161283E (pt) | 2003-11-17 | 2014-08-29 | Genentech Inc | Composições que compreendem anticorpos contra cd79b conjugados a um agente de inibição do crescimento ou agente citotóxico e métodos para o tratamento de tumor de origem hematopoiética |
GB0404577D0 (en) | 2004-03-01 | 2004-04-07 | Spirogen Ltd | Pyrrolobenzodiazepines |
EP1723152B1 (en) | 2004-03-09 | 2015-02-11 | Spirogen Sàrl | Pyrrolobenzodiazepines |
AU2005286607B2 (en) | 2004-09-23 | 2011-01-27 | Genentech, Inc. | Cysteine engineered antibodies and conjugates |
KR101103108B1 (ko) | 2005-06-20 | 2012-01-04 | 제넨테크, 인크. | 종양의 진단 및 치료를 위한 조성물 및 방법 |
ES2708763T3 (es) | 2005-07-07 | 2019-04-11 | Seattle Genetics Inc | Compuestos de monometilvalina que tienen modificaciones de la cadena lateral de fenilalanina en el extremo C |
US8871720B2 (en) | 2005-07-07 | 2014-10-28 | Seattle Genetics, Inc. | Monomethylvaline compounds having phenylalanine carboxy modifications at the C-terminus |
CN101296907B (zh) | 2005-09-01 | 2013-03-27 | 弗·哈夫曼-拉罗切有限公司 | 作为p2x3和p2x2/3调节剂的二氨基嘧啶类 |
ES2374964T3 (es) | 2006-01-25 | 2012-02-23 | Sanofi | Agentes citotóxicos que comprenden nuevos derivados de tomaimicina. |
EP2446904B1 (en) | 2006-05-30 | 2015-04-29 | Genentech, Inc. | Anti-CD22 antibodies, their immunoconjugates and uses thereof |
JP5622390B2 (ja) | 2006-07-18 | 2014-11-12 | サノフイ | 癌治療用対epha2アンタゴニスト抗体 |
EP1914242A1 (en) | 2006-10-19 | 2008-04-23 | Sanofi-Aventis | Novel anti-CD38 antibodies for the treatment of cancer |
TWI412367B (zh) | 2006-12-28 | 2013-10-21 | Medarex Llc | 化學鏈接劑與可裂解基質以及其之綴合物 |
CL2008001334A1 (es) | 2007-05-08 | 2008-09-22 | Genentech Inc | Anticuerpo anti-muc16 disenado con cisteina; conjugado que lo comprende; metodo de produccion; formulacion farmaceutica que lo comprende; y su uso para tratar el cancer. |
ES2435779T3 (es) | 2007-07-19 | 2013-12-23 | Sanofi | Agentes citotóxicos que comprenden nuevos derivados de tomaimicina y su uso terapéutico |
ES2450755T3 (es) | 2007-10-19 | 2014-03-25 | Genentech, Inc. | Anticuerpos anti-TENB2 modificados por ingeniería genética con cisteína, y conjugados de anticuerpo y fármaco |
SG10201706294VA (en) | 2009-02-05 | 2017-09-28 | Immunogen Inc | Novel benzodiazepine derivatives |
DE102009051799B4 (de) * | 2009-11-03 | 2021-07-01 | Georg-August-Universität Göttingen Stiftung Öffentlichen Rechts | Bifunktionale Prodrugs und Drugs |
JP5856065B2 (ja) | 2009-11-30 | 2016-02-09 | ジェネンテック, インコーポレイテッド | 腫瘍の診断と治療のための組成物と方法 |
CN102971329B (zh) | 2010-04-15 | 2016-06-29 | 麦迪穆有限责任公司 | 用于治疗增殖性疾病的吡咯并苯并二氮杂卓 |
CN103068405A (zh) * | 2010-04-15 | 2013-04-24 | 西雅图基因公司 | 靶向吡咯并苯并二氮杂卓结合物 |
DK2528625T3 (da) * | 2010-04-15 | 2013-10-14 | Spirogen Sarl | Pyrrolobenzodiazepiner og konjugater deraf |
DK3108886T3 (da) | 2010-04-21 | 2020-08-10 | Syntarga Bv | Konjugater af CC-1065-analoger og bifunktionelle linkere |
EP2678037B1 (en) | 2011-02-25 | 2014-12-03 | Lonza Ltd | Branched linker for protein drug conjugates |
US8852599B2 (en) | 2011-05-26 | 2014-10-07 | Bristol-Myers Squibb Company | Immunoconjugates, compositions for making them, and methods of making and use |
CN103987407B (zh) | 2011-10-14 | 2016-08-24 | 麦迪穆有限责任公司 | 吡咯并苯并二氮杂卓及其偶联物 |
CN104428007B (zh) | 2012-07-09 | 2018-03-16 | 基因泰克公司 | 包含抗cd22抗体的免疫缀合物 |
JP2015527318A (ja) | 2012-07-09 | 2015-09-17 | ジェネンテック, インコーポレイテッド | 抗cd22を含む免疫複合体 |
JP6980384B2 (ja) | 2013-12-16 | 2021-12-15 | ジェネンテック, インコーポレイテッド | 1−(クロロメチル)−2,3−ジヒドロ−1h−ベンゾ[e]インドール二量体抗体−薬物コンジュゲート化合物、並びに使用及び処置の方法 |
PE20161394A1 (es) | 2013-12-16 | 2017-01-06 | Genentech Inc | Compuestos peptidomimeticos y sus conjugados de anticuerpo-farmaco |
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2014
- 2014-06-16 EA EA201690195A patent/EA201690195A1/ru unknown
- 2014-06-16 SG SG11201601005XA patent/SG11201601005XA/en unknown
- 2014-06-16 EP EP14736243.8A patent/EP3033111B1/en active Active
- 2014-06-16 KR KR1020167006280A patent/KR20160042080A/ko not_active Application Discontinuation
- 2014-06-16 CN CN201480055557.3A patent/CN105636612B/zh active Active
- 2014-06-16 CA CA2918139A patent/CA2918139A1/en not_active Abandoned
- 2014-06-16 AU AU2014307080A patent/AU2014307080B2/en not_active Ceased
- 2014-06-16 BR BR112016002829A patent/BR112016002829A2/pt not_active IP Right Cessation
- 2014-06-16 MX MX2016001862A patent/MX2016001862A/es unknown
- 2014-06-16 TW TW103120758A patent/TWI636792B/zh not_active IP Right Cessation
- 2014-06-16 JP JP2016533294A patent/JP6993084B2/ja active Active
- 2014-06-16 WO PCT/US2014/042560 patent/WO2015023355A1/en active Application Filing
- 2014-06-16 US US14/305,643 patent/US10442836B2/en active Active
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2016
- 2016-01-12 IL IL243586A patent/IL243586A0/en unknown
- 2016-02-04 PH PH12016500246A patent/PH12016500246A1/en unknown
- 2016-02-09 CL CL2016000318A patent/CL2016000318A1/es unknown
- 2016-03-11 CR CR20160125A patent/CR20160125A/es unknown
- 2016-09-08 HK HK16110669.1A patent/HK1222544A1/zh unknown
- 2016-09-13 HK HK16110804.7A patent/HK1222566A1/zh unknown
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2019
- 2019-10-25 JP JP2019194288A patent/JP2020040954A/ja active Pending
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