130107-96-9Relevant academic research and scientific papers
Macrocyclic pyrrolobenzodiazepine dimers as antibody-drug conjugate payloads
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
, p. 5267 - 5271 (2017)
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.
Partially bio-based poly(amide imide)s by polycondensation of aromatic diacylhydrazides based on lignin-derived phenolic acids and aromatic dianhydrides: Synthesis, characterization, and computational studies
Kuhire, Sachin S.,Sharma, Pragati,Chakrabarty, Suman,Wadgaonkar, Prakash P.
, p. 3636 - 3645 (2017)
Two new bio-based diacylhydrazide monomers, namely, 4,4′-(propane-1,3-diylbis(oxy))bis(3-methoxybenzohydrazide) and 4,4′-(propane-1,3-diylbis(oxy))bis(3,5-dimethoxybenzohydrazide) were synthesized starting from lignin-derived phenolic acids, namely, vanillic acid and syringic acid. A series of poly(amide imide)s was synthesized by polycondensation of these diacylhydrazide monomers with commercially available aromatic dianhydrides. Poly(amide imide)s showed inherent viscosity in the range 0.44–0.56 dL?g?1 and exhibited good solubility in organic solvents. Poly(amide imide)s could be cast into transparent, flexible, and tough films from their N,N-dimethylacetamide solutions. Poly(amide imide)s showed 10% weight loss in the temperature range 340–364?°C indicating their good thermal stability. Glass transition temperature (Tg) of poly(amide imides)s were measured by DSC and DMA which were in the range 201–223?°C and 214–248?°C, respectively. The Tg values of poly(amide imide)s were dependent on the number methoxy substituents on aromatic rings of diacylhydrazide monomers. Molecular dynamics simulation studies revealed that chain rigidity is the dominant factor for observed trends in Tg.
PYRROLOBENZODIAZEPINE CONJUGATES
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Page/Page column 139; 140, (2018/04/27)
A compound of formula (I) : (I) and its conjugates.
ISOQUINOLIDINOBENZODIAZEPINES
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Paragraph 000547-000550, (2018/04/13)
This disclosure provides novel isoquinolidinobenzodiazepines. These compounds can also be incorporated into antibody-drug conjugates.
PYRROLOBENZODIAZEPINE CONJUGATES
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Page/Page column 99, (2017/09/05)
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
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Page/Page column 97-98, (2017/09/05)
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.
PYRROLOBENZODIAZEPINE ANTI-HER2 ANTIBODY CONJUGATES
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Page/Page column 37, (2017/09/07)
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.
BIO-BASED AROMATIC DIISOCYANATES FOR PREPARATION OF POLYURETHANES
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Page/Page column 8; 9, (2016/07/27)
The present invention provides bio-based aromatic diisocyanate of formula (I). [Formula should be inserted here] wherein X is –OCH3, Y is selected from -H or –OCH3, and m = 0-12. The present invention further provides a method for pr
MACROCYCLIC BENZODIAZEPINE DIMERS, CONJUGATES THEREOF, PREPARATION AND USES
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Paragraph 00167-00168, (2017/01/09)
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).
PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF
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Page/Page column 109, (2015/04/28)
A compound which is selected from A: and salts and solvates thereof.
