7160-44-3Relevant academic research and scientific papers
NOVEL BINDER-DRUG CONJUGATES (ADCs) AND USE OF SAME
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Paragraph 3728-3730, (2015/10/05)
The present patent application relates to novel binder-drug conjugates (ADCs) of N,N-dialkylauristatins directed against the target epidermal growth factor receptor (EGFR, gene ID 1956), effective metabolites of these ADCs, methods for producing these ADCs, use of these ADCs for treatment and or prevention of diseases as well as the use of these ADCs to produce pharmaceutical drugs for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic diseases such as cancer, for example. Such treatments may be administered as monotherapy or in combination with other pharmaceutical drugs or other therapeutic measures.
Novel Binder-Drug Conjugates (ADCs) and Use of Same
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Page/Page column, (2014/05/20)
The present patent application relates to novel binder-drug conjugates (ADCs) of N,N-dialkylauristatins directed against the target epidermal growth factor receptor (EGFR, gene ID 1956), effective metabolites of these ADCs, methods for producing these ADCs, use of these ADCs for treatment and or prevention of diseases as well as the use of these ADCs to produce pharmaceutical drugs for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic diseases such as cancer, for example. Such treatments may be administered as monotherapy or in combination with other pharmaceutical drugs or other therapeutic measures.
Auristatin derivatives and use thereof
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Page/Page column, (2014/05/20)
The present application relates to novel derivatives of monomethylauristatin F, to processes for preparing these derivatives, to the use of these derivatives for treating and/or preventing diseases, and also to the use of these derivatives for preparing medicaments for treating and/or preventing diseases, more particularly hyperproliferative and/or angiogenic disorders such as, for example, cancerous disorders. Such treatments may be practised as a monotherapy or else in combination with other medicaments or further therapeutic measures.
NEW BINDER-DRUG CONJUGATES (ADCS) AND USE THEREOF
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Page/Page column, (2013/03/28)
The present application relates to new binder-drug conjugates (ADCs) of N,N-dialkylauristatins that are directed against the target C4.4a, to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for treating and/or preventing illnesses, and also to the use of these ADCs for producing medicaments for treating and/or preventing illnesses, more particularly hyperproliferative and/or angiogenic diseases such as, for example, cancer diseases. Such treatments may be practised as a monotherapy or else in combination with other medicaments or further therapeutic measures.
Syntheses of conformationally constricted molecules as potential NAALADase/PSMA inhibitors
Ding, Pingyu,Miller, Marvin J.,Chen, Yi,Helquist, Paul,Oliver, A. Jayne,Wiest, Olaf
, p. 1805 - 1808 (2007/10/03)
Matrix presented. Two six-membered ring targeted analogues of PSMA inhibitors (4a and 4b) were designed on the basis of a computational analysis and synthesized. (E,Z)-Diene 10 was subjected to the nitroso Diels-Alder reaction to give the 1,4-trans six-me
Diastereoselectivity and Reactivity in the Diels-Alder Reactions of α-Chloronitroso Ethers
Felber, Helena,Kresze, Guenter,Prewo, Roland,Vasella, Andrea
, p. 1137 - 1146 (2007/10/02)
The structure of the α-chloronitroso ether 1, obtained from the hydroximolactone 2 and tert-butyl hypochlorite (89percent), was established by X-ray crystallographic analysis.The cycloadditions of 1 with dienes 3 and 8-11 led to the N-unsubstituted 3,6-dihydro-2H-1,2-oxazines 6 and 12-16 in high enantiomeric excess (Table 1).Due to the additional α-alkoxy group, the reactivity of 2 is much superior to the one of known α-chloronitrosoalkanes.The reactive conformation of 1 was deduced from the X-ray analysis as well as the high diastereoselectivity of the cycloadditions.The importance of the α-alkoxy group was evidenced from the similar reactivity of the racemic α-chloronitroso ethers 25-27 which were prepared from the hydroximo ethers 28-30 and tert-butyl hypochlorite.
