Novartis Ag

Spinifex Pharmaceuticals Pty Ltd

Starpharma Pty Limited

Prana Biotechnology Limited

Thomas David McCarthy

Alan Naylor

Peter Michael Kelly

Alexander Redvers Eberlin

Craig James Stewart Boyle

John Paul Watts

Jane Brown

Kevin Jeffrey Barnham

Barry Ross Matthews

Robert Cherny

Owen Timothy Grogan

Susanne Pallich

Andrew Rainsford Bakeb

Andrew Rainsford Baker

The present invention relates to heterocyclic compounds useful for antagonizing angiotensin II Type 2 (AT) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with ATreceptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.

Heterocyclic compounds and methods of their use

The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT) receptor. More particularly the invention relates to compounds of formula (I), as described herein, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with ATreceptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.

Heterocyclic compounds and methods for their use

The invention relates to heterocyclic angiotensin II type 2 (AT) receptor antagonists of formula (I), and pharmaceutically acceptable salts thereof, ((I) in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of neuropathic or inflammatory pain. 

Pyrrolidine derivatives as angiotensin II type 2 antagonists

The present invention relates generally to compounds that are useful in antagonizing the angiotensin II type 2 (AT) receptor. More particularly, the invention relates to substituted isoquinoline compounds and their use as ATreceptor antagonists. Pharmaceutical compositions comprising the compounds and their use in modulating the ATreceptor and therapies that require modulation of the ATreceptor are described.

The present invention relates to heterocyclic compounds useful for antagonizing angiotensin II Type 2 (AT) receptor. More particularly the invention relates to piperazine and diazepine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with ATreceptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.

The present invention relates to heterocyclic compounds useful for antagonizing angiotensin II Type 2 (AT) receptor. More particularly the invention relates to piperidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with ATreceptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.

The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with ATreceptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.

(S)-2-(Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described.

Salts and solvates of a tetrahydroisoquinoline derivative

The present invention provides methods and compositions for the effective treatment of impaired nerve signal conduction. Compositions including selective ATreceptor antagonists as active agents and methods of use in relation to improving nerve signal conduction or reversing impaired nerve signal conduction are described.

Methods and compositions for improved nerve conduction velocity

Salt and solvates of a tetrahydroisoquinoline derivative

A microbicidal delivery system including: a microbicidal composition including a microbicidal compound including a dendrimer including one or more surface groups of formula (IV); a microbicidally active derivative thereof, or pharmaceutically acceptable salt or solvate thereof; and a carrier, excipient or diluent therefor; and a prophylactic device; the microbicidal composition being carried on a surface of the prophylactic device and being compatible therewith.

Delivery system

The present invention relates to a contraceptive composition including an effective amount of a dendrimer compound including one or more naphthyl disulphonic acid surface groups, or a pharmaceutically acceptable salt or solvate of the dendrimer compound; and a pharmaceutically acceptable carrier, excipient and/or diluent therefor. The contraceptive composition may also exhibit antimicrobial activity. The invention also relates to a method of selectively reducing or preventing conception in a female animal, including a human, which method includes administering to the animal an effective amount of a contraceptive composition which composition includes an effective amount of a dendrimer compound including one or more naphthyl disulphonic acid surface groups, or a pharmaceutically acceptable salt or solvate of the dendrimer compound; and a pharmaceutically acceptable carrier, excipient and/or diluent therefor.

Contraceptive composition

The present invention relates to compounds which inhibit the binding of metal ions to a region in the N-terminal loop of the &#x3b2;-amyloid peptide which includes a cluster of histidine residues. In addition, the invention relates to pharmaceutical compositions including these compounds as the active agent, and to methods of treatment involving the administration of these compounds. The compounds of the invention are useful in the treatment of Alzheimer's Disease and other amyloid-related conditions. In a first aspect the present invention provides a compound which interacts with the &#x3b2;-amyloid peptide in such a way that the N-terminal loop of the peptide (amino acid residues 1-15) is blocked or destabilised, thereby inhibiting the binding of one or more metal ions to at least one histidine residue within the N-terminal loop. Preferably the compound inhibits binding of Cu, Znand Feions, but not Mgor Caions.

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Old Greenwich, CT, United States of America

Thomas David McCarthy