Manzanita Pharmaceuticals, Inc.

Asilomar Pharmaceuticals, Inc.

Micrologix Biotech Inc.

Robert R Webb

Constance A McKee

Stephen B Kahl

David J Loury

Reyna J Simon

Conway C Chang

Binh T Dang

Christopher J Baldwin

G Craig Hill

Gordon Craig Hill

The invention features compounds of the general formula:B-L-Mwhere B is a binding agent capable of selectively binding to a nerve cell surface receptor and mediating absorption of the compound by the nerve cell; M is a moiety which performs a useful non-cytotoxic function when absorbed by a nerve cell, and can be a therapeutic moiety or an imaging moiety; and L is a linker coupling B to M. The invention also features methods of use of the compounds in, for example, treating conditions such as viral infections and pain, as well as in labeling nerve cells.

Compounds for delivery of therapeutic and imaging moieties to nerve cells

A compound for delivering a non-cytotoxic therapeutic moiety into nerve cells, the compound having the general formula:B-L-TMwhere:

Compounds for intracellular delivery of therapeutic moieties to nerve cells

A method for improving intracellular administration of a therapeutic agent is provided comprising: contacting cells with a compound comprising a charged derivative of a therapeutic agent having a therapeutic activity, the charged derivative being conjugated to a protein having a biological activity of being transported across a cell membrane into a cell; and having the cell transport the compound into the cell where the cell metabolizes at least a portion of the compound to form a charged metabolite product that possesses the therapeutic activity of the therapeutic agent, the charged metabolite product being less prone to being transported across the cell membrane out of the cell relative to the compound and less prone to being transported across the cell membrane out of the cell relative to the therapeutic agent.

The present invention provides two new classes of polyene macrolide amide derivatives useful for treating or preventing fungal infections. The new polyene macrolide amide derivatives exhibit antifungal activity and are more water-soluble than conventional polyene antibiotics, such as amphotericin B and amphotericin B methyl ester.

Water-soluble amide derivatives of polyene macrolides and preparation and uses thereof

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Rancho Penasquitos, CA, United States of America

Robert R Webb