Abstract: The invention relates to a bradykinin (BK) B2-receptor antagonist having structural fomula (I) for use in prophylactic treatment of angioedema (AE) or in a method of treating AE, wherein said compound is at least once orally administered in a therapeutically effective dose to prevent, alleviate or treat AE symptoms. This invention also provides a method of prophylactic treatment of a human patient suffering from AE or a method for on-demand treatment of a human patient who has experienced an acute AE attack, comprising orally administering to the human patient a therapeutically effective dose of the compound of formula (I) at least once to thereby alleviate or treat AE symptoms of the patient.

Abstract: The present invention relates to a dinitroxide biradical compound of general formula (I): In formula (I), A is a carbon, an ammonium, or a phosphonium; each of A1 to A6 is a single bond, O, N, N(O), S, S(O), SO2, C(O), or a (C1-C4) alkyl chain; and Z1 and Z2 are selected from R1 and R2 in combination, so that there is always at least one R2 group that is substituted with R3 group. In Z1 and Z2, R1 is an H, an aryl, or a heteroaryl; R2 is an alkyl chain, an alkenyl chain, an alkynyl chain, a cycloalkyl, a heterocycloalkyl, an aryl, or a heteroaryl; and R3 is an alkyl chain, an alkenyl chain, an alkynyl chain, a cycloalkyl, a heterocycloalkyl, an aryl, a heteroaryl, an ether, an ester, or an azide. When Z1 and Z2 are combined together with the same carbon atom of the nitroxide ring to which they are bonded, they form a spirocycloalkyl or a spiroheterocycloalkyl, the spirocycloalkyl or the spiroheterocycloalkyl being substituted with R3.

Abstract: Non aqueous solvents or mixtures for DNP NMR spectroscopy, method to prepare said solvents or mixtures and use of said solvents or mixtures The present invention concerns a method to determine the efficiency of a solvent to impregnate a sample material for use in a dynamic nuclear polarization (DNP) nuclear magnetic resonance (NMR) experiments, characterized in that the method comprising: —selecting a non-aqueous solvent, —providing a polarizing agent that is soluble in the non-aqueous solvent, —dissolving the polarizing agent in the non-aqueous solvent, —impregnating or dissolving the sample material with the non-aqueous solvent containing the polarizing agent, —performing a solid state DNP NMR experiment on the impregnated sample material, —determining a DNP enhancement factor of the DNP NMR experiment.

Abstract: The invention concerns a dinitroxide biradical compound, in which the two nitroxide units are held by a rigid linkage, of general formula (I) in which—A is a carbon, an ammonium or a phosphonium, each of A1 to A6 is selected separately from the group comprising a single bond, O, N, N(O), S, S(O), SO2, C(O), a (C1-C4) alkyl chain, Z1 and Z2 are chosen from RI and R2 in combination, such that there is always, in the combination, at least one R2 group that needs to be substituted by an R3 group, RI is an H, a (C6-C18) aryl or a (C3-C18) heteroaryl, R2 a (C1-C17) alkyl chain, a (C1-C17) alkenyl chain, a (C1-C17) alkynyl chain, a (C4-C17) cycloalkyl, a (C4-C17) heterocycloalkyl, a (C6-C18) aryl, a (C3-C18) heteroaryl, R3 is a (C1-C17) alkyl chain, a (C1-C17) alkenyl chain, a (C1-C17) alkynyl chain, a (C4-C17) cycloalkyl, a (C4-C17) heterocycloalkyl, a (C6-C18) aryl, a (C3-C18) heteroaryl, an ether —OR, an ester —C(O)O—R (in which R is any hydrocarbon radical), an azide, and in which, when Z1 and Z2 are combined to

Abstract: The present invention concerns materials consisting in a porous and structured network, this network being at least in part formed by Si atoms, or Si atoms and metal atoms, linked to each other's via siloxy bonds, the amount of radical ranging from 0.50 to 0.03 mmol of radical per gram of material, and in that the network is formed with a sol-gel step using an organosilane for the introduction of the organic molecules allowing their regular distribution within the porous structured material. The invention also concern a process for the preparation of such material and a method of analysis by Nuclear Magnetic Resonance (NMR) of an analyte wherein it uses dynamic nuclear polarization generated with a material according to the invention.

Abstract: The present invention is concerned with radiolabelled quinoline and quinolinone derivatives according Formula (I-A)* or (I-B)* showing metabotropic glutamate receptor antagonistic activity, in particular mGlu1 receptor activity, and their preparation; it further relates to compositions comprising them, as well as their use for marking and identifying metabotropic glutamate receptor sites and for imaging an organ.

Abstract: The present invention concerns compounds of formula. In a preferable embodiment, X represents O; R1 represents C1-4alkyl; cycloC3-12alkyl or (cycloC3-12alkyl)C1-6alkyl, wherein one or more hydrogen atoms in a C1-6alkyl-moiety or in a cycloC3-12alkyl-moiety optionally may be replaced by C1-6alkyloxy, aryl, halo or thienyl; R2 represents hydrogen; halo; C1-6alkyl or amino; R3 and R4 each independently represent hydrogen or C1-6alkyl; or R2 and R3 may be taken together to form —R2—R3—, which represents a bivalent radical of formula -Z4-CH2—CH2—CH2— or -Z4-CH2—CH2— with Z4 being O or NR11 wherein R11 is C1-6alkyl; and wherein each bivalent radical is optionally substituted with C1-6alkyl; or R3 and R4 may be taken together to form a bivalent radical of formula —CH2—CH2—CH2—CH2—; R5 represents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo.

Abstract: A new two-dimensional NMR carbon-proton chemical shift correlation experiment, the MAS-J-HMQC experiment, is proposed for rotating solids. The magnetization transfer used to obtain the correlations is based on scalar heteronuclear J couplings. The 2D map provides through-bond chemical shift correlations between directly bonded proton carbon pairs in a similar way to corresponding high-resolution liquid state experiments. The transfer through J coupling is shown to be efficient and more selective that those based on heteronuclear dipolar couplings. The experiment, which works at high MAS spinning rates, yields the unambiguous assignment of the proton resonances. The experiment is demonstrated on several organic compounds.