Conjuchem, Inc.

Conjuchem Biotechnologies Inc.

Abbott Laboratories Corporation

Dominique P Bridon

Alan M Ezrin

Darren L Holmes

Peter G Milner

Martin Robitaille

Karen Thibaudeau

Serge St Pierre

Benoit L'Archeveque

Anouk Leblanc

Nissab Boudjellab

Keeve D Jaffe

Grant A Krafft

Roger Léger

John C Russell

Alexander Krantz

George J Dawson

Wolin Huang

Tami J Pilot-Matias

Tracey L Colpitts

John W Erickson

Isa K Mushahwar

Barry Lee Dowell

Xiaoxing Qiu

Richard Beliveau

Catherine A Brennan

Elaine Marie Brate

Dong Xie

Xicai Huang

Wlodzimierz Mandecki

Steven C March

Arthur M Hanel

David J Daghfal

Mark F Knigge

Lucie Jetté

Michele Rasamoelisolo

Dominique Blanchard

Kim Sverker Pettersson

Julie Carette

Vincent T Yue

Corinne Benquet

Angelica Fleser

Margaret Hardy

Elena Afonina

Jun Liang

Robert R Dufresne

Sandra DeMeyer

Mauno Antero Vihinen

Timo Petteri Piironen

Hans Lilja

Robert S Dufresne

Isaac S-y Sze, Deceased

Nisssab Boudjellab

Pamella A Schroeder-Poliak

Robert P Dufresne

The present invention relates to C34 peptide derivatives that are inhibitors of viral infection and/or exhibit antifusogenic properties. In particular, this invention relates to C34 derivatives having inhibiting activity against human immunodeficiency virus (HIV), respiratory syncytial virus (RSV), human parainfluenza virus (HPV), measles virus (MeV), and simian immunodeficiency virus (SIV) with long duration of action for the treatment of the respective viral infections.

Long lasting fusion peptide inhibitors for HIV infection

Peptides exhibiting anti-viral and anti-fusogenic activity are modified to provide greater stability and improved half-life in vivo. The selected peptides include fusion inhibitors DP178 and DP107 and related peptides and analogs thereof. The modified peptides are capable of forming covalent bonds with one or more blood components, preferably a mobile blood component.

Modified human immunodeficiency virus anti-fusogenic GP41 peptides comprising a maleimide-containing group

Long-lasting antiviral fusion inhibitor peptide conjugates comprising albumin and human immunodeficiency virus (HIV) peptides

This invention relates to growth hormone releasing factor (GRF) derivatives. In particular, this invention relates to GRF peptide derivatives having an extended in vivo half-life, for promoting the endogenous production or release of growth hormone in humans and animals.

Long lasting growth hormone releasing factor derivatives

Methods and compositions are provided for identifying compounds having affinity or complementarity to a target molecule. Compounds according to the invention may be described by the formula E-C&#x2014;R&#x2014;C-A, wherein E is a therapeutic or diagnostic agent, R is a reactive group, Cand Care connector groups between E and R and between R and A, respectively, and A is an affinity group comprising the sequence F--Y-E-E. Compounds according to the invention may be used for labeling the target molecule, particularly where the target molecule is naturally found in a complex mixture, such as a physiological fluid, like blood. By affinity labeling in vivo, the lifetime of physiologically active entities can be greatly enhanced by becoming bound to long-lived blood components. The covalently bound entity may also serve as an antagonist or agonist of a particular binding protein or as an enzyme inhibitor.

Affinity markers for human serum albumin

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

Long lasting fusion peptide inhibitors of viral infection

Modified insulinotropic peptides are disclosed. The modified insulinotropic peptides are capable of forming a peptidase stabilized insulinotropic peptide. The modified insulinotropic peptides are capable of forming covalent bonds with one or more blood components to form a conjugate. The conjugates may be formed in vivo or ex vivo. The modified peptides are administered to treat humans with diabetes and other related diseases.

Long lasting synthetic glucagon-like peptide {GLP-1}

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.

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

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.

Long lasting synthetic glucagon-like peptide (GLP-1)

Methods of and compositions for pulmonary delivery of therapeutic agents which are capable of forming covalent bonds with a site of interest or which have formed a covalent bond with a pulmonary solution protein are disclosed. Therapeutic agents useful in the invention include wound healing agents, antibiotics, anti-inflammatories, anti-oxidants, anti-proliferatives, immunosupressants, anti-infective and anti-cancer agents.

Pulmonary delivery for bioconjugation

Conjugates are prepared from antinociceptive agents, particularly opioids or opioid analogs, more particularly dynorphins, endorphins, deltorphins, enkephalins or analogs thereof, by combining said antinociceptive agent with a material providing a functionally reactive group capable of reacting with a blood component (preferably a blood cell or protein). Said conjugates permit extension of the therapeutic life of the antinociceptive agent. They may be administered to patients to alleviate pain, produce analgesic effects, or assist in cases of narcotics withdrawal, and may also be used as probes for receptor activity. The administration to the patient may be made either in vivo or ex vivo and may be performed by either introducing the derivative including the reactive functional group into the patient's vascular system or preparing such a conjugate externally (or in vitro) and introducing that conjugate to the patient's vascular system.

Method for alleviating pain or providing an analgesic effect in a patient

Conjugates are prepared from antinociceptive agents, particularly opioids or opioid analogs, more particularly dynorphins, endorphins, deltorphins, enkephalins or analogs thereof, by combining said antinociceptive agent with a material providing a functionally reactive group capable of reacting with a blood component (preferably a blood cell or protein). Said conjugates permit extension of the therapeutic life of the antinociceptive agent. They may be administered to patients to alleviate pain, produce analgesic effects, or assist in cases of narcotics withdrawal, and may also be used as probes for receptor activity. The administration to the patient may be made either in vivo or ex vivo and may be performed by either introducing the derivative including the reactive functional group into the patient's vascular system or preparing such a conjugate externally (or in vitro) and introducing that conjugate to the patient's vascular system

Antinociceptive agent derivative

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Outremont, Canada

Dominique P Bridon