Patent classifications
A61K51/065
CYCLIC PEPTIDES AND THEIR CONJUGATES FOR ADDRESSING ALPHA-V-BETA-6 INTEGRIN IN VIVO
The invention provides conjugates of cyclic peptides as ligands for cellular surface receptors, in particular, as ligands for αvβ6-integrin. The conjugates further contain effector moieties and are suitable for use as therapeutic agent, diagnostic agent, agent for imaging, targeting moiety and as biomolecular research tool. The invention specifically relates to the use of conjugates with signalling moieties or radionuclides for in-vivo addressing of αvβ6-integrin.
TLR9 TARGETED CYTOTOXIC AGENTS
Disclosed are compositions and methods for targeted treatment of TLR9-expressing cancers. In particular, molecules containing a TLR9 targeting ligand, such as a CpG oligodeoxynucleotide, that target cytotoxic agents to TLR9-expressing malignant cells are disclosed. Compositions and methods are disclosed for targeted treatment of cancer or cancer-stem cells with extracellular TLR9 expression, such as primary human MDS progenitors and hematopoietic stem cell (HSC). In particular, molecules containing TLR9 targeting ligands that target cytotoxic agents to TLR9-expressing malignant cells are disclosed.
PSMA-TARGETED PAMAM DENDRIMERS FOR SPECIFIC DELIVERY OF IMAGING, CONTRAST AND THERAPEUTIC AGENTS
Prostate-specific membrane antigen (PSMA)-targeted PAMAM dendrimers (G4-PSMA) and their use for imaging or treating PSMA-expressing tumors or cells are disclosed.
Biodegradable compositions suitable for controlled release
Simple mixing/blending of a special class of drug-depot forming tri-block copolymers polymers, with the opportunity to cost-effectively tailor drug delivery performances of such biodegradable, injectable depots in a clinical and an industrial setting. How to visualize these depots for various imaging related purposes is described. A composition comprising (a) an active ingredient, preferably a pharmaceutically active ingredient (b) a solvent and (c) a mixture of at least two types of tri-block copolymers of formula (1)
B-A-B (1)
wherein B stands for a hydrophobic block and wherein A stands for a hydrophilic block, wherein the mixture is prepared by mixing at least two types of tri-block copolymers having a degree of modification of 100% and wherein the at least two types of B-A-B types of tri-block copolymers differ only on the type of end-group or wherein the mixture is prepared by mixing at least two types of tri-block copolymers, wherein one of the at least two tri-block copolymers has a degree of modification of 100% and one of the at least two tri-block copolymers has a degree of modification of 0% and wherein the at least two types of B-A-B types of tri-block copolymers differ only on the degree of modification of the end-groups.
RADIOPHARMACEUTICAL CONJUGATE
This invention relates new radiopharmaceutical conjugates for use in improved methods of diagnosis and treatment of cancer. The radiopharmaceutical conjugate comprises, in sequence: a metabolite that targets tumour cells, bound to a chelating agent capable of containing a radionuclide, bound to a linker capable of binding with an EPR agent in vitro or in vivo; or a chelating agent capable of containing a radionuclide, bound to a metabolite that targets tumour cells, bound to a linker capable of binding with an EPR agent in vitro or in vivo. The radiopharmaceutical conjugates of the present invention provide active and passive targeted radio nuclide delivery systems that can help to improve the biodistribution and pharmacological toxicity of the radiopharmaceuticals used for the diagnosis and therapy of cancer.
Pharmaceutical compositions and preparations for administration to the eye
Compounds comprising R-G-Cysteic Acid (i.e., R-G-NH—CH(CH.sub.2—SO.sub.3H)COOH or Arg-Gly-NH—CH(CH.sub.2—SO.sub.3H)COOH) and derivatives thereof, including pharmaceutically acceptable salts, hydrates, stereoisomers, multimers, cyclic forms, linear forms, drug-conjugates, pro-drugs and their derivatives. Also disclosed are methods for making and using such compounds including methods for inhibiting cellular adhesion to RGD binding sites or delivering other diagnostic or therapeutic agents to RGD binding sites in human or animal subjects.
Oligosaccharide conjugates for targeting bacteria and uses related thereto
This disclosure relates to conjugates for targeting bacteria and related uses. In certain embodiments, the disclosure relates to methods of transferring a molecule of interest into bacteria comprising mixing bacteria with a non-naturally occurring conjugate under conditions such that the conjugate is transported across the bacterial cell wall. Typically, the conjugate comprises an oligosaccharide and a molecule of interest. In certain embodiments, the molecule of interest may be a tracer or an antibiotic.
Fucoidan nanogels and methods of their use and manufacture
Described herein are polymeric drug-carrying nanogels that are capable of targeting to P-selectin for the treatment of cancer and other diseases and conditions associated with P-selectin. Furthermore, in certain embodiments, the nanogels presented here offer a drug release mechanism based on acidic pH in the microenvironment of a tumor, thereby providing improved treatment targeting capability and allowing use of lower drug doses, thereby reducing toxicity.
ANTIBODIES FOR CHELATED RADIONUCLIDES AND CLEARING AGENTS
The present application relates to antibodies which bind specifically to chelated radionuclides, including bispecific antibodies, It further relates to the use of such bispecific antibodies in applications such as radioimmunoimaging and radioimmunotherapy. It additionally relates to clearing agents and useful in such methods.
Core constructs and their uses in configuring pharmaceutical molecules
The present disclosure provides various core constructs. According to embodiments of the present disclosure, the core construct can be used to configure pharmaceutical molecules. In particular, the core construct may be conjugated with a functional element via the click chemistry.