Abstract: The present invention provides a macrocyclic compound of formula (I) compositions and kits comprising this compound and their use for preventing or treating pain, or inducing hypothermia or hypotension.

Abstract: The present disclosure provides a macrocyclic compound of formula (I) (I), compositions and kits comprising this compound and their use for preventing or treating pain without inducing hypothermia, hypotension or ileum relaxation.

Abstract: Antibodies and antigen-binding fragments thereof that specifically recognize Neurotensin receptor type 1 (NTSR1) are described. These anti-NTSR1 antibodies and antigen-binding fragments thereof, such as single-chain Fv (scFv), are able to inhibit neurotensin-mediated activation of NTSR1 in normal and tumor cells. Methods and uses of antibodies and antigen-binding fragments thereof for treatment of diseases or conditions associated with NTSR1 activity, such as NTSR1-positive cancers or certain metabolic diseases, are also described. Cyclic peptides mimicking the conformation of the second extracellular loop of NTSR1 and capable of inducing the production of anti-NTSR1 antibodies in animals such as chickens are also described.

Abstract: The present application relates to a compound of formulae (I), (II) or (III) or a pharmaceutically acceptable salt thereof, methods and uses thereof for treating disorders associated with matriptase activity.

Abstract: The present invention provides bacterial ATP synthase inhibitors such as a compound of formula (I): There are provided compositions and kits using such compounds and inhibitors.

Abstract: The present description relates to a conjugated anti-interleukin-5 receptor ?-subunit (IL-5R?) compound comprising cholic acid (ChAc) or a variant thereof, the ChAc conjugated to a non-cell penetrating peptide comprising a nuclear localization sequence (NLS) conjugated to an anti-interleukin-5 receptor ?-subunit (IL-5R?) compound and further conjugated to chemotherapeutic agent and/or a radionuclide.

Abstract: The present application relates to a compound of formulae (I), (II) or (III) or a pharmaceutically acceptable salt thereof, methods and uses thereof for treating disorders associated with matriptase activity.

Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

Abstract: The present invention provides matriptase inhibitors and compositions for treating and preventing orthomyxovirus infections such as flue infections. The present invention also provides novel compounds, compositions, methods of use, uses and kits thereof for inhibiting matriptase. Such compounds are useful for treating and prevention orthomyxovirus infections, such as flu infections, and for inhibiting tumor growth, progression and/or metastasis.

Abstract: The present invention provides bacterial ATP synthase inhibitors such as a compound of formula (I): There are provided compositions and kits using such compounds and inhibitors.

Abstract: The present invention provides a macrocyclic compound of formula (I) compositions and kits comprising this compound and their use for preventing or treating pain, or inducing hypothermia or hypotension.

Abstract: The present invention provides bacterial ATP synthase inhibitors such as a compound of formula (I): (Formula (I)) (A) in combination with an aminoglycoside antibiotic for preventing or treating a bacterial infection in a subject; or (B) (a) for preventing or treating an infection caused by an electron transport-deficient bacteria in a subject; or (b) for the disinfection, sterilization and/or antisepsis of an object contaminated with an electron transport-deficient bacteria. There are provided compositions and kits using such compounds and inhibitors.

Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

Abstract: The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R1, R2, R3, R4, R5, R6, n1, m, p Z1, Z2, and Z3 are as described in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.

Abstract: The present invention includes novel compounds and pharmaceutically acceptable formulations of said compounds which exhibit antibiotic activity against microorganisms bearing a guanine riboswitch that controls the expression of the guaA gene, including organisms which are resistant to certain antibiotic families, and which are useful as antibacterial agents for treatment or prophylaxis of bacterial infections in animals or in humans, in particular but not limited to infections of the mammary gland, or their use as antiseptics, agents for sterilization or disinfection.

Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone sceretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

Abstract: The present invention relates to cyclic amino acid molecules and methods of preparing the same, and in particular the macrocyclization of amino acids or linear peptides bound to a solid support.

Abstract: The present invention provides matriptase inhibitors and compositions for treating and preventing orthomyxovirus infections such as flue infections. The present invention also provides novel compounds, compositions, methods of use, uses and kits thereof for inhibiting matriptase. Such compounds are useful for treating and prevention orthomyxovirus infections, such as flu infections, and for inhibiting tumor growth, progression and/or metastasis.

Abstract: The present invention provides matriptase inhibitors and compositions for treating and preventing orthomyxovirus infections such as flu infections. The present invention also provides novel compounds, compositions, methods of use, uses and kits thereof for inhibiting matriptase. Such compounds are useful for treating and preventing orthomyxovirus infections, such as flu infections, and for inhibiting tumor growth, progression and/or metastasis.

Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone sceretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.