Conjuchem, Inc.

Conjuchem Biotechnologies Inc.

Prometic Biotherapeutics, Inc.

Advanced Diagnostics and Discovery

Karen Thibaudeau

Dominique Bridon

Peter G Milner

Dominique P Bridon

Martin Robitaille

Alan M Ezrin

Xicai Huang

Darren L Holmes

Roger Leger

Nissab Boudjellab

Richard Beliveau

Julie Carette

Michele Rasamoelisolo

Pierre Laurin

Jean-Paul Castaigne

Stacy Plum

Dominique Blanchard

Roger Léger

Jean-Philippe Estradier

Margaret Hardy

Thomas R Ulich

Subjects of the invention are a method of plasminogen supplementation in a plasminogen-deficient subject, and method for the treatment of plasminogen-deficiency in a plasminogen-deficient subject. These methods comprise administering to the plasminogen-deficient subject a dose of plasminogen, and more particularly Glu-plasminogen, for increasing the subject plasminogen activity level by at least about 1%, and more particularly by at least 10%, of the normal plasminogen activity and for maintaining the plasminogen activity level over a supplementation period or a treatment period. The plasminogen-deficient subject of the present invention may suffer from Type-I, Type-II plasminogen-deficiency or an acquired deficiency.

Plasminogen replacement therapy for plasminogen-deficiency

The present invention provides methods of administering an insulinotropic peptide in an amount effective to treat a disorder or condition while reducing nausea side effect by administering to a subject in need thereof an insulinotropic peptide conjugated to albumin. The present invention also provides methods of selecting a subject for administration of a conjugated insulinotropic peptide. Exemplary disorders or conditions treatable with an insulinotropic peptide include obesity and type II diabetes.

Method of treatment of diabetes and/or obesity with reduced nausea side effect

The present invention relates to compounds comprising modified corticotrophin releasing factor peptide and specifically urocortin and urocortin-related peptides, modified derivatives thereof, and conjugates of such modified peptides and derivatives to serum components, preferably serum proteins or peptides. The compounds and conjugates of the invention comprise a reactive group, which is covalently attached to a modified peptide or derivative, optionally through a linking group. The present invention also provides methods for the covalent attachment of a modified peptide or derivative to a serum protein or peptide to form a conjugate of the invention. The conjugates of the invention preferably exhibit a longer in vivo circulating half-life compared to the corresponding unconjugated peptides. The conjugates of the invention also retain at least some of the biological activity of the unconjugated peptides, and preferably exhibit increased biological activity compared to the unconjugated peptides. The present invention also provides methods for the treatment and prevention of a disease or disorder comprising the administration of one or more of the compounds or conjugates of the invention to a subject in need of such treatment or prevention.

Modified corticotropin releasing factor peptides and uses thereof

The present invention relates to a compound comprising a PYY peptide or a functional derivative thereof, which is coupled to a reactive group. Such a reactive group is capable of reacting on a blood component so as to form a stable covalent bond therewith. The present invention also relates to a conjugate comprising such a compound which is covalently bonded to a blood component. Moreover, the invention also relates to a method of enhancing, in a patient, the anti-obesity activity of a PYY peptide or functional derivative thereof.

Anti-obesity agents

Modified anti-angiogenic peptides are disclosed. The modified peptides are capable of forming a peptidase stabilized anti-angiogenic peptide. The modified anti-angiogenic peptides, particularly modified kringle 5 peptides are capable of forming a conjugate with a blood protein. Conjugates are prepared from anti-angiogenic peptides, particularly kringle 5 peptides, by combining the peptide with a reactive functional group with a blood protein. The conjugates may be formed in vivo or ex vivo. The conjugates are administered to patients to provide an anti-angiogenic effect.

Long lasting anti-angiogenic peptides

This invention relates to glucagon-like peptide 2 (GLP-2) derivatives. In particular, this invention relates to GLP-2 peptide derivatives having an extended in vivo half-life, for the treatment or prevention of gastrointestinal disorders or diseases such as inflammatory bowel disease and other gastrointestinal functions, from any segment of the gastrointestinal tract, from the oesophagus to the anus.

Long lasting glucagon-like peptide 2 (GLP-2) for the treatment of gastrointestinal diseases and disorders

A secretin or secretin derivative protected against peptidase activity. The secretin or derivative comprises a peptidic sequence and a reactive group selected from the group consisting of succinimidyl and maleimido groups capable of reacting with an amino group, hydroxyl group or thiol group on a blood component to form a stable covalent bond. The reactive group is attached at a position along the peptidic sequence that provides, when conjugated to a blood component, a higher stability against peptidase degradation than the unconjugated secretin or derivative, and therefore an increased maintenance of the therapeutic activity compared to the unconjugated secretin or derivative. Such a compound is thus effective to provide a source of secretin having a high stability against peptidases. A method for synthesizing such a compound is also described.

Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components

This invention relates to glucagon-like peptide 2 (GLP-2) derivatives. In particular this invention relates to GLP-2 peptide derivatives having an extended in vivo half-life, for the treatment or prevention of gastrointestinal disorders or diseases such as inflammatory bowel disease and other gastrointestinal functions, from any segment of the gastrointestinal tract, from the oesophagus to the anus.

Long lasting glucagon-like peptide 2 (glp-2) for the treatment of gastrointestinal diseases and disorders

A method for protecting a peptide from peptidase activity in vivo, the peptide being composed of between 2 and 50 amino acids and having a C-terminus and an N-terminus and a C-terminus amino acid and an N-terminus amino acid is described. In the first step of the method, the peptide is modified by attaching a reactive group to the C-terminus amino acid, to the N-terminus amino acid, or to an amino acid located between the N-terminus and the C-terminus, such that the modified peptide is capable of forming a covalent bond in vivo with a reactive functionality on a blood component. In the next step, a covalent bond is formed between the reactive group and a reactive functionality on a blood component to form a peptide-blood component conjugate, thereby protecting said peptide from peptidase activity. The final step of the method involves the analyzing of the stability of the peptide-blood component conjugate to assess the protection of the peptide from peptidase activity.

A method of synthesizing a modified therapeutic peptide capable of forming a peptidase-stabilized therapeutic peptide conjugate, the peptide having between 3 and 50 amino acids, is k. In a first step of the method, a therapeutic peptide having a carboxy terminal amino acid and amino terminal amino acid is synthesized. In a second step, pairs of cysteine residues present in the therapeutic peptide are sequentially and selectively oxidized to form disulfide bridges in the therapeutic peptide. In a third step, a protecting group is attached to remaining cysteine residues that do not form disulfide bridges in the therapeutic peptide. Finally, the peptide is coupled to a reactive group capable of reacting with amino groups, hydroxyl groups or thiol groups on a blood component to form a covalent bond therewith.

Antibodies to a therapeutic agent and its derivatives and conjugates are disclosed, including antibodies to argatroban and its derivatives and conjugates. The antibodies are useful as reagents in assays and diagnostic kits for determining the concentration of a therapeutic agent or its derivatives and conjugates in biological samples, and further have therapeutic uses in treatment for potential toxicity associated with stable therapeutic conjugates and derivatives, both in vivo and ex vivo.

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Montreal, Canada

Karen Thibaudeau