140658-44-2

Upstream product

• 3943-74-6 4-hydroxy-3-methoxybenzoic acid methyl ester 
• 67-56-1 methanol 
• 140658-45-3 1',3'-bis(4-carboxy-2-methoxy-5-nitrophenoxy)propane 
• 3018-48-2 1',3'-bis(4-carboxy-2-methoxyphenoxy)propane 
• 121-34-6 3-methoxy-4-hydroxybenzoic acid 
• 130107-96-9 1',3'-bis<2-methoxy-(4-methoxycarbonyl)phenoxy>propane 

Downstream Products

• 909797-72-4 C₂₁H₂₆N₂O₈ 

Relevant academic research and scientific papers

PYRROLOBENZODIAZEPINE CONJUGATES

A compound of formula (I) : (I) and its conjugates.

ISOQUINOLIDINOBENZODIAZEPINES

This disclosure provides novel isoquinolidinobenzodiazepines. These compounds can also be incorporated into antibody-drug conjugates.

PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF

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.

PYRROLOBENZODIAZEPINE CONJUGATES

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)

PYRROLOBENZODIAZEPINE CONJUGATES

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.

Macrocyclic pyrrolobenzodiazepine dimers as antibody-drug conjugate payloads

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.

PYRROLOBENZODIAZEPINE ANTI-HER2 ANTIBODY CONJUGATES

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.

MACROCYCLIC BENZODIAZEPINE DIMERS, CONJUGATES THEREOF, PREPARATION AND USES

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).

PYRROLOBENZODIAZEPINE-ANTIBODY CONJUGATES

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.

PYRROLOBENZODIAZEPINE-ANTIBODY CONJUGATES

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.