- Quinazoline Derivatives Useful as CB-1 Inverse Agonists
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The present invention is directed to quinazoline derivatives, pharmaceutical compositions containing said derivatives and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. For example, the compounds of the present invention are useful in the treatment of metabolic disorders.
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Paragraph 0549-0550
(2016/04/20)
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- Orthogonal synthesis of a heterodimeric ligand for the development of the GdIII-GaIII ditopic complex as a potential pH-sensitive MRI/PET probe
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A heterodimeric polyaminocarboxylate ligand based on a DO3A-sulfonamide linked to AAZTA (6-amino-6-methylperhydro-1,4-diazepinetetracarboxylic acid) was synthesised via an orthogonal pathway in order to differentiate the two chelating cages and allow the formation of a GdIII-GaIII heteroditopic complex. The goal is to create a smart MRI/PET probe with pH dependent relaxivity and with the bimodal imaging approach that enables direct quantification of the stimulus, in this case pH. A 1H NMR relaxometric study of the Gd-Ga heteroditopic complex addressed the pH modulation of the relaxivity and thus its possible use as an MRI pH sensitive probe.
- Vologdin, Nikolay,Rolla, Gabriele A.,Botta, Mauro,Tei, Lorenzo
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p. 1683 - 1690
(2013/03/28)
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- PYRIDYL INHIBITORS OF HEDGEHOG SIGNALLING
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The invention provides novel inhibitors of hedgehog signaling that are useful as s therapeutic agent for treating malignancies where the compounds have the general formula (I): where A, X, Y R1, R2, R3, R4, m and n are as described herein.
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Page/Page column 101
(2009/11/29)
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- Pyridyl inhibitors of hedgehog signalling
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The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
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Page/Page column 79
(2010/10/20)
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- CCR5 ANTAGONISTS AS THERAPEUTIC AGENTS
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The present invention relates to compounds of formula (I) or pharmaceutically acceptable derivatives thereof, useful in the treatment or prophylaxis of CCR5-related diseases and disorders, for example, in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).
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