Abstract: A process to isolate a compound of Formula (2a) or a salt or solvate thereof, comprising a) reacting a mixture of diastereoisomers of Formulae (2a, 2b) with a basic heterocyclic-aldehyde compound and an optically active amine in the presence of a base; and b) separating the compound of Formula (2a) from the product of step a) by acid extraction. The compound of Formula (2a) may be produced with an enantiomeric excess of 98%. Compounds of Formula (2a) are useful intermediates in a process to prepare a bicyclic ?-amino tetrazole derivative of Formula (I) which finds utility in treating neuropathic pain and disorders of the central nervous system.

Abstract: The present invention relates to novel cycloundecadepsipeptide compounds and their analogues which bind and inhibit cyclophilins, have reduced immunosuppressive activity and improved physicochemical properties including water solubility. The present invention further relates to pharmaceutical compositions containing said depsipeptide compounds and their analogues for use in the treatment or prevention of diseases and pathologies which may be ameliorated by the inhibition of cyclophilin activity.

Abstract: A process to isolate a compound of Formula (2a) or a salt or solvate thereof, comprising a) reacting a mixture of diastereoisomers of Formulae (2a, 2b) with a basic heterocyclic-aldehyde compound and an optically active amine in the presence of a base; and b) separating the compound of Formula (2a) from the product of step a) by acid extraction. The compound of Formula (2a) may be produced with an enantiomeric excess of 98%. Compounds of Formula (2a) are useful intermediates in a process to prepare a bicyclic ?-amino tetrazole derivative of Formula (I) which finds utility in treating neuropathic pain and disorders of the central nervous system.

Abstract: The present invention relates to novel cycloundecadepsipeptide compounds and their analogues which bind and inhibit cyclophilins, have reduced immunosuppressive activity and improved physicochemical properties including water solubility. The present invention further relates to pharmaceutical compositions containing said depsipeptide compounds and their analogues for use in the treatment or prevention of diseases and pathologies which may be ameliorated by the inhibition of cyclophilin activity.

Abstract: Disclosed herein are mono or di-succinate compounds where one or both of the acid groups in the succinate core are protected in the form of biologically labile moieties, and the use of said compounds to enhance mitochondrial function. The compounds may be of formula (I) wherein R1 is H or an optionally substituted alkyl group or a group of formula (II) and R2 is independently a group according to formula (II) where formula (II) is as defined 10 herein.

Abstract: The present invention relates to novel cycloundecadepsipeptide compounds and their analogues which bind and inhibit cyclophilins, have reduced immunosuppressive activity and improved physicochemical properties including water solubility. The present invention further relates to pharmaceutical compositions containing said depsipeptide compounds and their analogues for use in the treatment or prevention of diseases and pathologies which may be ameliorated by the inhibition of cyclophilin activity.

Abstract: The present invention relates to novel cycloundecadepsipeptide compounds and their analoges which bind and inhibit cyclophilins, have reduced immunosuppressive activity and improved physicochemical properties including water solubility. The present invention further relates to pharmaceutical compositions containing said depsipeptide compounds and their analoges for use in the treatment or prevention of diseases and pathologies which may be ameliorated by the inhibition of cyclophilin activity.

Abstract: Disclosed herein are mono or di-succinate compounds where one or both of the acid groups in the succinate core are protected in the form of biologically labile moieties, and the use of said compounds to enhance mitochondrial function. The compounds may be of formula (I) wherein R1 is H or an optionally substituted alkyl group or a group of formula (II) and R2 is independently a group according to formula (II) where formula (II) is as defined 10 herein.

Abstract: The present invention relates to novel cycloundecadepsipeptide compounds and their analogues which bind and inhibit cyclophilins, have reduced immunosuppressive activity and improved physicochemical properties including water solubility. The present invention further relates to pharmaceutical compositions containing said depsipeptide compounds and their analogues for use in the treatment or prevention of diseases and pathologies which may be ameliorated by the inhibition of cyclophilin activity.

Abstract: The invention provides named compounds of formula (I), pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions and their use in therapy.

Abstract: The invention provides named compounds of formula (I), wherein R4 is a N-substituted quinuclidine (I) pharmaceutical compositions containing them and a process for preparing the pharmaceutical compositions. Their use in therapy for the treatment of conditions mediated by M3 muscarinic receptors, such as chronic obstructive pulmonary disease is also disclosed.

Abstract: The invention provides named compounds of formula (I), wherein R4 is a N-substituted quinuclidine (I) pharmaceutical compositions containing them and a process for preparing the pharmaceutical compositions. Their use in therapy for’ the treatment of conditions mediated by M3 muscarinic receptors, such as chronic obstructive pulmonary disease is also disclosed.