A61K47/593

Stereoisomer peptides, their polymer conjugates, their encapsulation into nanoparticles, and uses thereof for the treatment of diseases caused by abnormal angiogenesis
09790286 · 2017-10-17 ·

This invention discloses the creation of a novel single ligand-targeted multi-stereoisomer peptide-polymer conjugate compounds comprising a group of different synthetic and chemically modified stereoisomer peptides that have been conjugated to a biocompatible polymer carrying a peptide ligand for targeted delivery and/or encapsulated in ligand targeted polymer nanoparticles. The unique physicochemical properties of the stereoisomer peptides provide therapeutic compounds with ideal biopharmaceutical properties. The stereoisomer peptides carried by the polymer are delivered to cells or tissues to inhibit, suppress, block, antagonize or disrupt, simultaneously and independently, the functional domain of different disease causing proteins. Therefore the compounds are novel therapeutics for the treatment of abnormal angiogenesis and inflammation which are the hall mark of most human diseases including but not limited to all cancers, metastasis, eye retinopathies, cardiovascular, brain, and neurodegenerative disorders, diabetes, and diseases caused by infectious microorganisms including virus, bacteria, fungi, and parasites.

MetAP-2 inhibitor polymersomes for therapeutic administration

The present invention provides methods to treating inflammation related disease and disorders such as an autoimmune disease and autoimmune related uveitis by administering compositions and formulations comprising MetAP-2 inhibitors as disclosed herein. The composition comprises a formulation of a fumagillol derivative that retains anti-inflammation activity and is associated with a block copolymer comprising a hydrophilic polymer moiety and a hydrophobic polymer moiety.

Multifunctional degradable nanoparticles with control over size and functionalities

In one aspect, the invention relates to polymers, crosslinked polymers, functionalized polymers, nanoparticles, and functionalized nanoparticles and methods of making and using same. In one aspect, the invention relates to degradable polymers and degradable nanoparticles. In one aspect, the invention relates to methods of preparing degradable nanoparticles and, more specifically, methods of controlling particle size during the preparation of degradable nanoparticles. In one aspect, the degradable nanoparticles are useful for complexing, delivering, and releasing payloads, including pharmaceutically active payloads. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

CONJUGATES INCLUDING AN ANTIBODY MOIETY, A POLYPEPTIDE THAT TRAVERSES THE BLOOD-BRAIN BARRIER, AND A CYTOTOXIN

The present invention relates to antibody-polypeptide-cytotoxin conjugates and methods of making, packaging, and using the conjugates. The polypeptide can be a Kunitz-type protease inhibitor or a derivative thereof that facilitates transport of the conjugate across the blood-brain barrier and/or into cancer cells outside the CNS, and the antibody moiety selectively binds a target within the CNS or in peripheral tumors to direct the cytotoxic agent to that target (e.g., a tumor or cancer cell). The conjugates can be further defined by the inclusion of a linker between the antibody moiety and the polypeptide; by the number of polypeptides and cytotoxic agents conjugated thereto; by the positions at which the entities within the conjugates are bound to one another; and by the larger configuration of the conjugate. Modified polypeptides (e.g., polypeptides conjugated to cytotoxic agents but not to an antibody moiety), pharmaceutical compositions, kits (e.g., including a modified polypeptide and an as-yet unconjugated antibody), and methods of making and using the conjugates are also features of the invention.

COMPOSITE CONTAINING POLY(GLYCEROL SEBACATE) FILLER

A filler material of a thermoset resin of a diacid/polyol, such as PGS is provided. The filler useful in forming composites, such as those in which the filler and a resin matrix are of the same material to provide a homogenous polymeric composition. Composites in which at least one of the matrix, the filler or both are PGS are also provided. Methods of forming such filler materials and composites are also disclosed. The composites allow extrusion process to form articles from materials that would not otherwise be capable of being extruded.

Affinity medicant conjugate
11241398 · 2022-02-08 · ·

In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The medicant moiety can be a toxin including an acylfulvene or a drug moiety. The affinity moiety can be an antibody, a binding protein, a steroid, a lipid, a growth factor, a protein, a peptide or non peptidic. The affinity moiety can be covalently bound to the medicant via a linker. Novel linkers that can be directed to cysteine, arginine or lysine residues based on solution pH allow greater flexibility in preserving and/or generating specific epitopes in the AMC.

POLYMER COMPOSED OF REPEAT UNITS HAVING A BIOLOGICALLY ACTIVE MOLECULE ATTACHED THERETO VIA A PH-SENSITIVE BOND
20170224828 · 2017-08-10 · ·

There is provided a polymer comprising: (i) a repeat unit derived from a compound of formula (I) (Formula (I)) wherein, R.sup.1 and R.sup.2 are each independently selected from OH, OR′, SH, SR′, NH.sub.2, NHR′ and NR′.sub.2; R′ is C.sub.1-20 hydrocarbyl; each n is independently 0 or an integer between 1 and 6; each m is independently 0 or an integer between 1 and 4, and preferably at least one m is 1; and q is an integer between 1 and 8; and; (ii) a biologically active molecule, wherein said biologically active molecule is covalently bonded to said repeat unit; as well as methods for preparing such polymers, particles comprising said polymers and uses of said polymers and particles including use in the treatment of disease.

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THERAPEUTIC NANOPARTICLES HAVING EGFR LIGANDS AND METHODS OF MAKING AND USING SAME
20170224620 · 2017-08-10 ·

Provided herein in part is a therapeutic nanoparticle that includes a biocompatible polymer; a polymer—EGFR ligand conjugate, wherein the EGFR ligand is covalently bound directly or through a chemical linker to the polymer, and a therapeutic agent.

Drug delivery scaffold or stent with a novolimus and lactide based coating such that novolimus has a minimum amount of bonding to the coating

Disclosed herein are drug delivery medical devices. A polymer coating for a medical device is provided which comprises a minimum amount of a drug bonded to the polymer in the coating.

Methods for providing polymeric synthetic nanocarriers for generating antigen-specific tolerance immune responses

Disclosed are synthetic nanocarrier compositions that provide controlled release of immunosuppressants as well as related methods. The synthetic nanocarrier compositions may also include antigen in some embodiments.