Patent classifications
C07D255/02
Spiroacridine-Triazine Hybrids and Applications for Electroluminescent Devices
The present invention relates to compounds of the formula (1), to the use thereof in electroluminescent devices, and particularly organic electroluminescence devices, comprising said compounds according to the invention.
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Spiroacridine-Triazine Hybrids and Applications for Electroluminescent Devices
The present invention relates to compounds of the formula (1), to the use thereof in electroluminescent devices, and particularly organic electroluminescence devices, comprising said compounds according to the invention.
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Substituted imidazo ring systems and methods
Imidazo ring systems substituted at the 1-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
Substituted imidazo ring systems and methods
Imidazo ring systems substituted at the 1-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
Compounds for use as iron (III) MRI contrast agents containing anionic pendents and ancillary groups
Macrocyclic complexes and macrocyclic compounds. The macrocyclic complexes or macrocyclic compounds have a TACN moiety with one or more amine group(s) or a O- or S-substituted TACN moiety. The macrocyclic complexes have a high-spin Fe(III) atom coordinated to the TACN moiety. The macrocyclic complexes can be used in imaging methods.
MALONITRILE DERIVATIVES
The invention relates to a compound of formula (I) wherein R.sup.1-R.sup.2 are as defined in the description and in the claims The compound of formula (I) can be used as a medicament.
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DENDRIMER FOR THERAPY AND IMAGING
Provided herein is a dendrimer comprising: i) a core unit (C); and ii) building units (BU), wherein the core unit is covalently attached to at least two building units; the dendrimer having from two to six generations of building units; wherein building units of different generations are covalently attached to one another; and the dendrimer further comprising: iii) one or more first terminal groups attached to an outermost building unit, wherein each first terminal group comprises a radionuclide-containing moiety; and iv) one or more second terminal groups attached to an outermost building unit, wherein each second terminal group comprises a pharmacokinetic-modifying moiety; or a salt thereof. Also provided are compositions comprising the dendrimers, and methods of using the dendrimers and compositions in diagnostic and therapeutic applications.
COMPOUNDS FOR USE IN DIAGNOSIS AND/OR MONITORING OF FIBROSIS
There is provided a composition comprising: (i) a compound of Formula I: (I), or a pharmaceutically acceptable salt thereof, and (ii) a nuclide M, or a pharmaceutically acceptable salt of the compound of Formula I and/or the nuclide M, wherein C is a chelator selected from the group consisting of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA), 1,4,8,11-tetraazacycl otetradecane-1,4,8,11-tetraacetic acid (TETA), diethylenetriaminepentaacetic acid (DTPA), desferrioxamine B (DFO), 1,4,7-Triazacyclononane-1-glutaric acid-4,7-acetic acid (NOTAGA), 2-[4,7,10-Tris(carboxymethyl)-1,4,7,10-tetraza-1-cyclododecyl]glutaric acid (DOTAGA and a derivative of any one of the foregoing chelators, L (Formula L) is a linker: (L), wherein m is an integer within the range of from 1 to 20, and X is NH or C(O) and forms an amide bond, i.e. C(O)NH, with a C(O) or NH moiety of the chelator, p is 0 or 1, Q is a peptide of SEQ ID NO: 1, a peptide analogue of SEQ ID NO: 1 having at least 88.8% identity to SEQ ID NO. 1, and/or a peptide of SEQ ID NO: 1, a peptide analogue of SEQ ID NO: 1 having at least 88.8% identity to SEQ ID NO: 1 and in which the C-terminal COOH can be replaced by CONH.sub.2, and M is selected from the group consisting of .sup.68Ga, .sup.18F, .sup.64Cu, .sup.44Sc, .sup.89Zr, .sup.111In, .sup.67Ga, .sup.99mTc, Mn, Gd, .sup.177Lu.and .sup.86/90Y. The composition may be used in in diagnosing and/or monitoring of fibrosis.
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COMPOUNDS FOR USE IN DIAGNOSIS AND/OR MONITORING OF FIBROSIS
There is provided a composition comprising: (i) a compound of Formula I: (I), or a pharmaceutically acceptable salt thereof, and (ii) a nuclide M, or a pharmaceutically acceptable salt of the compound of Formula I and/or the nuclide M, wherein C is a chelator selected from the group consisting of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA), 1,4,8,11-tetraazacycl otetradecane-1,4,8,11-tetraacetic acid (TETA), diethylenetriaminepentaacetic acid (DTPA), desferrioxamine B (DFO), 1,4,7-Triazacyclononane-1-glutaric acid-4,7-acetic acid (NOTAGA), 2-[4,7,10-Tris(carboxymethyl)-1,4,7,10-tetraza-1-cyclododecyl]glutaric acid (DOTAGA and a derivative of any one of the foregoing chelators, L (Formula L) is a linker: (L), wherein m is an integer within the range of from 1 to 20, and X is NH or C(O) and forms an amide bond, i.e. C(O)NH, with a C(O) or NH moiety of the chelator, p is 0 or 1, Q is a peptide of SEQ ID NO: 1, a peptide analogue of SEQ ID NO: 1 having at least 88.8% identity to SEQ ID NO. 1, and/or a peptide of SEQ ID NO: 1, a peptide analogue of SEQ ID NO: 1 having at least 88.8% identity to SEQ ID NO: 1 and in which the C-terminal COOH can be replaced by CONH.sub.2, and M is selected from the group consisting of .sup.68Ga, .sup.18F, .sup.64Cu, .sup.44Sc, .sup.89Zr, .sup.111In, .sup.67Ga, .sup.99mTc, Mn, Gd, .sup.177Lu.and .sup.86/90Y. The composition may be used in in diagnosing and/or monitoring of fibrosis.
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2-Pyrazole Anilines and Related Analogs for Inhibiting YAP/TAZ-TEAD
The present disclosure relates to novel compounds, to said compounds for use as a medicine, more in particular for the prevention or treatment of diseases mediated by activity of YAP/TAZ-TEAD transcription, yet more in particular for the prevention or treatment of cancer or fibrosis. The present disclosure also relates to a method for the prevention or treatment of said diseases comprising the use of the novel compounds.