Patent classifications
A61K41/00
Conjugates of active pharmaceutical ingredients
The present inventions provides drug-drug conjugates, drug-porphyrin conjugates, nanoparticles of the conjugates, as well as modified nanoparticles having PEGylated exteriors or encapsulated by red blood cell vesicles. The conjugates, nanoparticles and nanocarriers are useful for treating cancers and other diseases, as well as for imaging diseased tissue or organs.
Nanoparticles for treatment of choroidal neovascularization and other indications
The present invention generally relates to particles such as nanoparticles and, in particular, to targeted nanoparticles. In some cases, the particles may have a targeting moiety that is inhibited from recognizing a target, for example, by being positioned within the particle at an internal location. The application of a stimulus, such as light, may allow the targeting moiety to interact externally of the particle. Accordingly, the particles may be targeted to specific locations using the application of a suitable stimulus. For instance, in one embodiment, particles containing cell-penetrating peptides attached via a first attachment and a second attachment containing a photocleavable entity may be administered to a subject, and light may be applied, e.g., to the eye, to cleave the photocleavable entity. However, despite the cleavage, the peptides remain associated with the particle via the first attachment, and thus, the particles may be able to penetrate cells within the eye due to peptides. Other aspects are generally directed to methods of making or using such particles, kits involving such particles, or the like.
METHODS OF TREATING TUMORS WITH PRO DRUGS
Methods of treating tumors by administering compounds to a patient are provided. Compounds such as pro drugs, e.g., 5-aminolevulinic acid (5-ALA), may be administered to the patient orally, by injection, intravenously, or topically, which then accumulate preferentially as compounds such as protoporphyrin IX (PpIX) in tumor cells. After such accumulation, compounds such as PpIX are then activated in various aspects to treat tumors cells, thereby treating cancer. Cancers such as glioblastoma may be treated.
COMBINATION CANCER THERAPY WITH DYRK1 INHIBITORS AND INHIBITORS OF THE RAS-RAF-MEK-ERK (MAPK) PATHWAY
The present invention provides compositions and methods for the treatment of neoplasms, in particular, by targeting of quiescent and proliferating cancers cells with DYRK1 inhibitor in combination with other treatments effective against certain neoplastic conditions, in particular, anti-cancer treatment with a MEK inhibitor or a b-RAF inhibitor, or a KRAS inhibitor.
EMBOLIZING AGENT PRECURSOR PHARMACEUTICAL COMPOSITION
Disclosed herein are compositions and methods for an embolizing agent precursor. The embolizing agent precursor may include a gaseous component and a first stabilizer to stabilize the gaseous component, the first stabilizer may include a a polymer, and wherein a gas portion of the gaseous component is selected from the group consisting of sulphur hexafluoride and C3-6 perfluorocarbons. The embolizing agent precursor may further include an oil component which comprises a C1-7 hydrocarbon, a second stabilizer to stabilize the oil component, and a vaporous component configured to enlarge the gaseous component.
BIODEGRADABLE COMPOSITIONS AND IMPLANTS
The present invention relates to an ocular composition comprising a) at least 0.1% w/w of a therapeutic agent; b) 5 to 95% w/w of a photopolymerizable composition comprising 3 to 70% w/w of one or more compounds of formula I: (I) wherein R.sub.1 is hydrogen or a linear or branched C.sub.1-C.sub.3 alkyl; R.sub.2 is an acrylate or methacrylate group; n is 2 or 3 and m is equal or greater than 1, the weight percentage of the one or more compounds of formula I being based on the total weight of the photopolymerizable composition; c) 0.1 to 40% w/w of a biodegradable polymer selected from the group consisting of lactide/glycolide copolymer (including poly(lactide-co-glycolide) (PLGA)), poly (L-lactide) (PLA), polyhydroxyalkanoates, including polyhydroxybutyrate, polyglycolic acid (PGA), polycaprolactone (PCL), poly (DL-lactide) (PDL), poly (D-lactide), lactide/caprolactone copolymer,
BIODEGRADABLE COMPOSITIONS AND IMPLANTS
The present invention relates to an ocular composition comprising a) at least 0.1% w/w of a therapeutic agent; b) 5 to 95% w/w of a photopolymerizable composition comprising 3 to 70% w/w of one or more compounds of formula I: (I) wherein R.sub.1 is hydrogen or a linear or branched C.sub.1-C.sub.3 alkyl; R.sub.2 is an acrylate or methacrylate group; n is 2 or 3 and m is equal or greater than 1, the weight percentage of the one or more compounds of formula I being based on the total weight of the photopolymerizable composition; c) 0.1 to 40% w/w of a biodegradable polymer selected from the group consisting of lactide/glycolide copolymer (including poly(lactide-co-glycolide) (PLGA)), poly (L-lactide) (PLA), polyhydroxyalkanoates, including polyhydroxybutyrate, polyglycolic acid (PGA), polycaprolactone (PCL), poly (DL-lactide) (PDL), poly (D-lactide), lactide/caprolactone copolymer,
NEW COMPOUND FOR PHOTODYNAMIC THERAPY OF CANCER, COMPOSITION INCLUDING SAME, AND METHOD FOR PHOTODYNAMIC THERAPY OF CANCER
The present disclosure relates to a novel compound for photodynamic therapy of cancer, a composition including the same, and a method for photodynamic therapy of cancer, and more specifically, a novel photosensitizer compound based on Nplmidazole having a C═S functional group introduced, a composition and sensor including the same and a method for photodynamic therapy using the same.
COMPOSITIONS AND METHODS FOR OPTOCHEMICAL CONTROL OF MTOR SIGNALING AND MTOR-DEPENDENT AUTOPHAGY
Compositions and methods for selective mTOR inhibition and/or increase of autophagy in a tissue of a subject have been developed for the treatment of cancer. Caged mTOR inhibitor prodrugs including photo-cleavable protecting groups are provided for selective chemotherapy through an optochemical treatment system. Pharmaceutical compositions of mTOR inhibitors that are deactivated (caged) with a photo-removable protecting group to controllably block the inhibitory activity of the inhibitor are provided. The photo-removable group is cleavable upon exposure to light irradiation, releasing the active inhibitor of mTOR signaling and autophagy at the site of irradiation. An exemplary caged mTOR inhibitor prodrug is a caged OSI-027 prodrug having a DEACM moiety bound thereto (cOSI-027). The cOSI-027 is activated in the region of a tumor by removal of the DEACM protecting group by exposure to light at 420 nm.
TREATMENT OF PSYCHIATRIC CONDITIONS SUCH AS RESISTANT DEPRESSION, BIPOLAR DISORDER AND/OR MAJOR DEPRESSIVE DISORDER VIA APPLICATION OF REPETITIVE TRANSCRANIAL MAGNETIC STIMULATION WITH THYROID HORMONE TREATMENT AND/OR QUETIAPINE
The present invention relates to treatment of a psychiatric condition, for example resistant depression (RD), bipolar disorder (either threshold or sub-threshold) and/or major depressive disorder via application of repetitive transcranial magnetic stimulation with a drug treatment, in particular application of repetitive transcranial magnetic stimulation with treatment to modulate the activity of the neurones and induce neuroplasticity and the use of Thyroid hormone treatment to increase quantity or activity of thyroid hormones, for example for treatment of thyroid dysfunction. Patients may be selected for treatment by testing for the presence of normal thyroid function.