Abstract: A dicarba analogue of insulin comprising an A-chain and a B-chain or fragments, salts, solvates, derivatives, isomers or tautomers of the A-chain, the B-chain or both, provided that the dicarba analogue is not [A7,B7-(2,7-diaminosuberoyl]-des-(B26-B30)-insulin B25-amide.

Abstract: According to the present invention, there is provided a range of new conotoxin derivatives and methods for synthesizing these analogues and other intramolecular dicarba bridge-containing peptides, including dicarba-disulfide bridge-containing peptides.

Abstract: The present invention relates to methods for forming dicarba bridges in organic compounds. This involves the use of a pair of complementary metathesisable groups on the organic compound, and subjecting the compound to cross-metathesis under microwave radiation conditions. In an alternative, the compounds contain a turn-inducing group between the pair of cross-metathesisable groups to facilitate the cross-metathesis.

Abstract: According to the present invention, there is provided a range of new conotoxin derivatives and methods for synthesizing these analogues and other intramolecular dicarba bridge-containing peptides, including dicarba-disulfide bridge-containing peptides.

Abstract: A service value calculation system includes: crisis problem inspection means which detects a crisis or a problem of a service object; and virtual damage amount calculation means which calculates a virtual damage amount generated if a detected crisis or problem is not solved when a service is not applied and calculates the service value.

Abstract: According to the present invention, there is provided a range of new conotoxin derivatives and methods for synthesizing these analogues and other intramolecular dicarba bridge-containing peptides, including dicarba-disulfide bridge-containing peptides.

Abstract: The present invention relates to methods for forming dicarba bridges in organic compounds. This involves the use of a pair of complementary metathesisable groups on the organic compound, and subjecting the compound to cross-metathesis under microwave radiation conditions. In an alternative, the compounds contain a turn-inducing group between the pair of cross-metathesisable groups to facilitate the cross-metathesis.

Abstract: According to the present invention, there is provided a range of new conotoxin derivatives and methods for synthesizing these analogues and other intramolecular dicarba bridge-containing peptides, including dicarba-disulfide bridge-containing peptides.

Abstract: Described herein are methods for forming two or more dicarba bridges, as well as new compounds containing dicarba bridges.

Abstract: A method for the preparation of a compound of formula (VI): in which R2 is an optionally substituted C1–C6 alkyl; R4 is H, OH, an optionally substituted C1–C6 alkyl or an optionally substituted C1–C6 alkoxy; R5 is an optionally substituted aryl, an optionally substituted aralkyl, or an optionally substituted alkyl; and R6 is H or an optionally substituted C1–C6 alkyl; the method including the step of subjecting a ketone of formula (V) in which R2, R4 and R5 are as defined above, to reductive amination with an amine of formula R3NH2 in which R3 is an optionally substituted alkyl, and a reductant to form the compound of formula (VI), wherein the reaction is conducted in the presence of a supercritical fluid or a liquefied gas.

Abstract: The invention provides a method of synthesis of a substituted or unsubstituted carbinol compound, comprising the steps of subjecting the corresponding substituted or unsubstituted aromatic aldehyde to acyloin condensation mediated by yeast in the presence of either (a) a supereritical fluid or (b) a liquefied gas, and recovering the carbinol compound. Preferably the yeast is Saccharomyces cerevisiae. In a particularly preferred embodiment the aromatic aldehyde is benzaldehyde and the carbinol is phenylacetylcarbinol, according to the reaction (I): in which the benzaldehyde, the pyruvic acid, or both may optionally be substituted.

Abstract: The invention provides compounds of the formula II: wherein R represents propyl, butyl, pentyl, neo-pentyl or cyclohexyl, and salts thereof. These compounds are selective GABAC receptor antagonists. The invention also provides a method of enhancing the cognitive activity of an animal and a method of stimulating memory capacity in an animal, comprising administering to the animal an effective amount of a compound of formula II or a pharmaceutically acceptable salt thereof.

Abstract: Organic compounds, such as precursors for aryl ethylamines such as ephedrine, aryl propylamines such as fluoxetine and propionic acid derivatives such as ibuprofen, naproxen and fenoprofen, are subjected to a yeast mediated reduction conducted in the absence of a solvent. The yeast is moistened with water and contacted with the organic compound. The yeast may then be contacted with an organic solvent to dissolve the product of the reaction into the solvent, and a solid/liquid separation used to separate the product from the yeast.

Abstract: The invention provides methods for enhancing cognitive activity and stimulating memory capacity, comprising the step of administering an effective amount of a compound with GABAC receptor antagonist activity to an animal in need of such treatment. Preferably the compound has selective GABAc receptor antagonist activity, and more preferably comprises a phosphinic acid group. The invention also provides novel compounds and compositions. The methods of the invention are useful in the treatment of dementias and conditions involving cognitive deficit, or memory impairment.

Abstract: This invention relates to yeast-mediated catalysis in organic solvents, and in particular the yeast-mediated condensation between pyruvate and a substituted aromatic aldehyde to yield the corresponding acyloin (hydroxy ketone) compound. The invention provides a method of synthesis of a substituted carbinol compound, comprising the step of subjecting the corresponding substituted aromatic aldehyde to acyloin condensation mediated by a yeast in an organic solvent under non-fermenting conditions. Preferably the yeast is Saccharomyces cerevisiae. In a preferred embodiment, the reaction is that between pyruvate and benzaldehyde to yield phenylacetylcarbinol, the precursor to ephedrine, to yield a product of high enantiomeric purity.

Abstract: The invention provides novel sulphonylurea, sulphonylthiourea and sulphonylguanidine compounds which have the ability to block potassium ion channels regulated by intracellular concentrations of ATP. Methods of synthesis, pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes, cardiac arrhythmias, ischaemic and hypoxic cardiovascular incidents, and cancers are also claimed.