摘要:
The invention concerns a novel substance class of nonpolar halogenated β-carbolines having the structural formula (I), wherein the C ring has one, two or three double bonds, X means -C(Hal)3, -CH(Hal)2, -CH2(Hal) or =C(Hal)2 where Hal = F, Cl, Br or I, and the substituents R?1, R2, R3 and R4¿ have the following meanings: R1: -H, a C¿1?-C18 alkyl group (e.g. methyl, ethyl, propyl, n-butyl, iso-butyl, tert.butyl, etc.), -CH2-CH=CH2, CH2-C6H5, an acyl or aroyl group provided that R?1¿ can also be a free electron pair if nitrogen participates in the formation of a double bond; R2: -H, -COOH, -COOCH¿3?, -COOC2H5, -COOCH2-CH=CH2, -COOCH2-C6H5, -COONH2, -CO2NR2, -CH2OAc, -CH2-OH, etc.; R?3¿: H-, HO-, CH¿3?O-, C2H5O-, C6-H5CH2O-, CH3COO-, C2H5COO-, etc.; R?4¿: H-, HO-, CH¿3?O-, C2H5O-, C6H5-CH2O-, CH3COO-, C2H5COO-, etc. Synthetically produced derivatives of this substance class and also derivatives with halogenated alkyl and alkylide groups in position 1 inhibit complex I and II of the mitochondrial respiratory chain even in very low concentrations.
摘要:
The invention concerns a novel substance class of nonpolar halogenated β-carbolines having the structural formula (I), wherein the C ring has one, two or three double bonds, X means -C(Hal)3, -CH(Hal)2, -CH2(Hal) or =C(Hal)2 where Hal = F, Cl, Br or I, and the substituents R?1, R2, R3 and R4¿ have the following meanings: R1: -H, a C¿1?-C18 alkyl group (e.g. methyl, ethyl, propyl, n-butyl, iso-butyl, tert.butyl, etc.), -CH2-CH=CH2, CH2-C6H5, an acyl or aroyl group provided that R?1¿ can also be a free electron pair if nitrogen participates in the formation of a double bond; R2: -H, -COOH, -COOCH¿3?, -COOC2H5, -COOCH2-CH=CH2, -COOCH2-C6H5, -COONH2, -CO2NR2, -CH2OAc, -CH2-OH, etc.; R?3¿: H-, HO-, CH¿3?O-, C2H5O-, C6-H5CH2O-, CH3COO-, C2H5COO-, etc.; R?4¿: H-, HO-, CH¿3?O-, C2H5O-, C6H5-CH2O-, CH3COO-, C2H5COO-, etc. Synthetically produced derivatives of this substance class and also derivatives with halogenated alkyl and alkylide groups in position 1 inhibit complex I and II of the mitochondrial respiratory chain even in very low concentrations.
摘要:
The present invention relates to novel protease-sensitive peptides, related compounds or salts thereof having the structure Den-R-NH-Pep (wherein Den is a denatonium residue and Pep designates a protease-sensitive peptide) as well as bioresponsive sensors comprising same, which may be used for diagnostic purposes, in particular for detection of inflammation, as well as to related methods and uses.
摘要:
The present invention relates to methods for predicting the probability of a treatment response of a human cancer patient to an immune checkpoint blocker treatment e.g. with anti PD-1, and to methods for predicting the probability of survival of a human cancer patient following an immune checkpoint blocker treatment, and to apparatuses and kits which can be used in these methods.
摘要:
The present invention relates to methods for predicting the probability of a treatment response of a human cancer patient to an immune checkpoint blocker treatment e.g. with anti PD-1, and to methods for predicting the probability of survival of a human cancer patient following an immune checkpoint blocker treatment, and to apparatuses and kits which can be used in these methods.
摘要:
The present invention relates to monoclonal anti-human-GDF-15 antibodies. The antibodies include chimeric antibodies and humanized antibodies. The invention also relates to monoclonal anti-human-GDF-15 antibodies including murine antibodies, chimeric antibodies and humanized antibodies for use in methods for the treatment of cancer cachexia and also for the treatment of cancer. The invention also provides pharmaceutical compositions, kits, methods and uses and cell lines capable of producing the monoclonal antibodies of the invention.
摘要:
The present invention relates to a new compound according to formula (I) as well as to the use of this compound in medicine, in the prevention of the aggregation of phosphorylated Tau proteins, the treatment or prevention of a tauopathy and in the treatment or prevention of a neurodegenerative disease, preferably selected from the group consisting of Primary age-related tauopathy (PART) dementia, Chronic traumatic encephalopathy, Progressive supranuclear palsy, Corticobasal degeneration and Alzheimer's disease, more preferably Alzheimer's disease.
摘要:
The present invention relates to a set of polypeptides and its uses. In particular, the present invention relates to a set of polypeptides whereby this set comprises two polypeptides each of which comprises a targeting moiety "T" binding to an antigen "A" and a fragment of "F" of a functional domain, wherein said two polypeptides are not associated with each other in absence of a substrate that has "A" at (on) its surface and wherein, upon dimerization of "F", the resulting dimer becomes functional. Furthermore, medical and diagnostic uses of said set are described. Moreover, the present invention relates to nucleic acid molecule(s) encoding said set of polypeptides. The present invention also relates to a vector comprising the nucleotide sequence of nucleic acid molecule(s) encoding said set of polypeptides. Furthermore, the present invention relates to pharmaceutical compositions comprising said set of polypeptides. Moreover, the present invention relates to a kit comprising said set of polypeptides.