- PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF
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Conjugates and compounds for making conjugates which are PBD molecules linked via the N10 position are disclosed, along with the use of the conjugates for treating proliferative diseases, including cancer.
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Paragraph 1225-1227
(2018/05/26)
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- PYRROLOBENZODIAZEPINE CONJUGATES
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A compound of formula (I) : (I) and its conjugates.
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Page/Page column 139; 140
(2018/04/27)
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- ISOQUINOLIDINOBENZODIAZEPINES
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This disclosure provides novel isoquinolidinobenzodiazepines. These compounds can also be incorporated into antibody-drug conjugates.
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Paragraph 000551-000553
(2018/04/13)
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- PYRROLOBENZODIAZEPINE CONJUGATES
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A conjugate of formula (I), wherein L is a Ligand unit, D is a Drug Linker unit of formula (II), wherein either: (a) R10 and R11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (b)
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Page/Page column 100
(2017/09/05)
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- PYRROLOBENZODIAZEPINE CONJUGATES
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A conjugate of formula (I): L - (DL)p (I) wherein L is a Ligand unit, D is a Drug Linker unit of formula (II) wherein p is an integer of from 1 to 20.
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Page/Page column 97-98
(2017/09/05)
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- Macrocyclic pyrrolobenzodiazepine dimers as antibody-drug conjugate payloads
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Macrocyclic pyrrolobenzodiazepine dimers were designed and evaluated for use as antibody-drug conjugate payloads. Initial structure–activity exploration established that macrocyclization could increase the potency of PBD dimers compared with non-macrocyclic analogs. Further optimization overcame activity-limiting solubility issues, leading to compounds with highly potent (picomolar) activity against several cancer cell lines. High levels of in vitro potency and specificity were demonstrated with an anti-mesothelin conjugate.
- Donnell, Andrew F.,Zhang, Yong,Stang, Erik M.,Wei, Donna D.,Tebben, Andrew J.,Perez, Heidi L.,Schroeder, Gretchen M.,Pan, Chin,Rao, Chetana,Borzilleri, Robert M.,Vite, Gregory D.,Gangwar, Sanjeev
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supporting information
p. 5267 - 5271
(2017/11/16)
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- PYRROLOBENZODIAZEPINE ANTI-HER2 ANTIBODY CONJUGATES
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A conjugate of formula (I) L - (DL)p (I) wherein L is an antibody (Ab) which binds HER2, D is a Drug Linker unit of formula (A) wherein p is an integer of from 1 to 20.
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Page/Page column 37; 38
(2017/09/07)
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- MACROCYCLIC BENZODIAZEPINE DIMERS, CONJUGATES THEREOF, PREPARATION AND USES
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Macrocyclic benzodiazepine dimers having a structure represented by formula (I) where A and B are independently according to formulae (Ia) or (Ib) ]; and the other variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used as the drug component in an antibody-drug conjugate (ADC).
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Paragraph 00167; 00169
(2017/01/09)
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- ANTIBODIES AND ANTIBODY-DRUG CONJUGATES
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This application provides antibodies and antigen binding fragments thereof which are capable of specifically binding the 5T4 cell surface antigen, antibody-drug conjugates, and antibody-imaging agent conjugates, as well as means and methods for producing and using them.
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Paragraph 0464
(2015/11/03)
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- PYRROLOBENZODIAZEPINE-ANTIBODY CONJUGATES
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Conjugates of specific PBD dimers with an antibody that that binds to HER2, the antibody comprising a VH domain having the sequence according to SEQ ID NO. 1.
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Page/Page column 41; 42
(2015/04/28)
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- PYRROLOBENZODIAZEPINE-ANTIBODY CONJUGATES
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Conjugates of specific PBD dimers with an antibody that that binds to CD19, the antibody comprising a VH domain having the sequence according to any one of SEQ ID NOs. 1, 2, 3, 4, 5 or 6, optionally further comprising a VL domain having the sequence according to any one of SEQ ID NOs. 7, 8, 9, 10, 11 or 12.
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Page/Page column 41; 42
(2015/04/28)
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- PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF
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A compound which is selected from A: and salts and solvates thereof.
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Page/Page column 109; 110
(2015/04/28)
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- PYRROLOBENZODIAZEPINE-ANTIBODY CONJUGATES
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Conjugates of specific PBD dimers with an antibody that binds to CD22, the antibody comprising a VH domain having the sequence according to SEQ ID NO. 1.
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Page/Page column 41
(2015/04/28)
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- PYRROLOBENZODIAZEPINE-ANTIBODY CONJUGATES
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Conjugates of specific PBD dimers with an antibody that binds to PSMA, the antibody comprising a VH domain having the sequence according to any one of SEQ ID NOs. 1, 3, 5, 7, 8, 9, or 10, optionally further comprising a VL domain having the sequence 5 according to any one of SEQ ID NOs. 2, 4, 6, 11, 12, 13, 14, 15, 16, 17, or 18.
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Page/Page column 43
(2015/04/28)
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- HUMANIZED ANTI-TN-MUC1 ANTIBODIES AND THEIR CONJUGATES
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Humanized anti-Tn-MUC1 antibodies and conjugates thereof. Conjugates comprising pyrrolobenzodiazepines (PBDs) having a labile protecting group in the form of a linker to the antibody are described.
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Page/Page column 150; 151
(2015/11/09)
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- PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF
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A compound which is selected from A, B and C, and salts and solvates thereof, as well as conjugates thereof with cell binding agents.
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Page/Page column 111-113
(2014/05/07)
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- NOVEL ANTIBODY CONJUGATES AND USES THEREOF
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Provided are novel antibody drug conjugates (ADCs), and methods of using such ADCs to treat proliferative disorders.
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Page/Page column 111; 112
(2014/09/03)
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- INTERMEDIATES USEFUL FOR THE SYNTHESIS OF PYRROLOBENZODIAZEPINES
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A compound of formula (I): which is substantially free of any of the corresponding compound of formula (IB): methods of making such compounds, and the further transformation of such compounds.
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Page/Page column 64-65
(2011/11/01)
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- PYRROLOBENZODIAZEPINES USED TO TREAT PROLIFERATIVE DISEASES
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Pyrrolobenzodiazepine dimers I having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit, and conjugates of these compounds.
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Page/Page column 70
(2011/11/01)
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- Linker Length Modulates DNA Cross-Linking Reactivity and Cytotoxic Potency of C8/C8′ Ether-Linked C2-exo-Unsaturated Pyrrolo[2,1-c][1,4]benzodiazepine (PBD) Dimers
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A C2/C2′-exo-unsaturated pyrrolo[2,1-c][1,4]benzodiazepine (PBD) dimer 4b (DRG-16) with a C8-O(CH2)nO-C8′ diether linkage (n = 5) has been synthesized that shows markedly superior in vitro cytotoxic potency (e.g., > 3400-fold in IGRO
- Gregson, Stephen J.,Howard, Philip W.,Gullick, Darren R.,Hamaguchi, Anzu,Corcoran, Kathryn E.,Brooks, Natalie A.,Hartley, John A.,Jenkins, Terence C.,Patel, Sejal,Guille, Matthew J.,Thurston, David E.
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p. 1161 - 1174
(2007/10/03)
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- Synthesis of sequence-selective C8-linked pyrrolo[2,1-c][1,4]benzodiazepine DNA interstrand cross-linking agents
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An efficient convergent synthesis of a homologous series of C8-linked pyrrolobenzodiazepine dimers with remarkable DNA interstrand cross-linking activity and potent in vitro cytotoxicity is reported. The 'amino thioacetal' cyclization procedure was used t
- Thurston, David E.,Bose, D. Subhas,Thompson, Andrew S.,Howard, Philip W.,Leoni, Alberto,Croker, Stephen J.,Jenkins, Terrence C.,Neidle, Stephen,Hartley, John A.,Hurley, Laurence H.
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p. 8141 - 8147
(2007/10/03)
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