Patent classifications
A61K47/548
DRUG CONTAINING LIVER TARGETING SPECIFIC LIGAND AND THYROID HORMONE RECEPTOR AGONIST
Provided is a drug containing a liver targeting specific ligand and a thyroid hormone receptor agonist in its structure, which is a new drug structure formed by linking the liver targeting specific ligand with the thyroid hormone receptor agonist through a branched chain, a linker and a linking chain. Thyroid hormone receptors (TRs) are divided into two subtypes, TR-α and TR-β, wherein, TR-β is mainly expressed in liver, and TR-α is mainly expressed in heart, nervous system, etc. In certain embodiments, it is envisaged that the provided drug has the action of liver targeting, can specifically bring the thyroid hormone receptor agonist into liver, without entering heart and other issues, and may thereby avoid side effects caused by the action of the thyroid hormone receptor agonist on other issues, and maintain its therapeutic efficacy in the treatment of lipid metabolism disorders and related complications.
Systemic and local ex vivo gene therapy of the skeleton
Methods are disclosed herein for increasing bone mass and strength or bone fracture healing in a subject. The methods include administering to the subject a therapeutically effective amount of multipotent stem cells, wherein each multipotent stem cell is transformed with a recombinant nucleic acid molecule comprising a heterologous promoter operably linked to a nucleic acid encoding platelet derived growth factor (PDGF) B, and wherein the multipotent stem cells express a sufficient amount of PDGFB to increase bone mass and strength or bone fracture healing. A lentiviral vector also is disclosed that includes a phosphoglycerate kinase-1 (PGK) promoter operably linked to a nucleic acid encoding PDGFB.
BISPHOSPHONATE-CONTAINING VACCINE PHARMACEUTICAL COMPOSITION FOR HUMORAL IMMUNITY
The present invention aims to provide a vaccine pharmaceutical composition universally usable for induction of humoral immunity against various antigens and exerting a high antibody production inducing effect. The present invention relates to a vaccine pharmaceutical composition for inducing humoral immunity, including: an antigen; and an immunity induction promoter that is a bisphosphonate.
FORMULATION COMPRISING A GEMCITABINE-PRODRUG
This invention relates to pharmaceutical formulations of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate, a monophosphate derivative of the well-known oncology drug gemcitabine. In particular, the invention relates to formulations which comprise a polar aprotic solvent, preferably dimethyl acetamide (DMA). Formulations comprising these solvent provide therapeutically effective treatments of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate. The invention also relates to methods of using said formulations and kits comprising said formulations.
CONJUGATES OF HYALURONIC ACID AND AMINOBISPHOSPHONATES AND THE THERAPEUTIC USE THEREOF
The present invention describes conjugates of hyaluronic acid (HA) and an amino-bisphosphonate (N-BP) of general formula (I):
##STR00001##
wherein L, m, n and x are as defined in claim 1, and the salts thereof
Said conjugates and the pharmaceutical compositions thereof are useful in the intra-articular and/or locoregional treatment of osteoarthrosis and its repercussions at cartilage and subchondral level; in the treatment of post-menopausal or drug-induced osteoporosis; in the treatment of bone fragility due to trauma or disease; and in the intraosseous and/or locoregional treatment of disorders characterised by altered metabolic bone turnover, in particular Paget's disease. They are also useful to improve the osseointegration of prostheses.
IMMUNITY-INDUCING AGENT COMPRISING ANTIGEN PEPTIDE-ADJUVANT NUCLEOTIDE CONJUGATE AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
The present invention provides an immunity-inducing agent comprising, as an active component, a polynucleotide/peptide conjugate in which a single-chain polynucleotide or polynucleotide derivative comprising a CpG motif, and an antigenic peptide are bound via a spacer, wherein the spacer is covalently bound at one end thereof to the polynucleotide or polynucleotide derivative and covalently bound at the other end thereof to the antigenic peptide, as well as a pharmaceutical composition comprising said immunity-inducing agent.
Parathyroid hormone, insulin, and related peptides conjugated to bone targeting moieties and methods and making and using thereof
Described herein is insulin, an insulin-like growth factor, parathyroid hormone, a fragment of parathyroid hormone, or a parathyroid hormone related protein that includes at least one bone targeting moiety, wherein the bone targeting moiety is covalently bonded to the peptide. Also described herein are the methods of making these compositions that prevent or treat conditions associated with bone loss and preventing bone fractures, and/or the inability to initiate de novo bone turnover and stimulate bone fracture repair.
Trityl-mono-GalNAc compounds and their use
This invention generally relates to the field of phosphoramidite derivatives. In particular, the invention relates to N-Acetylgalactosamine (GalNAc) compounds, in particular phosphoramidite or phosphonoamidite molecules of formula (I) with only one GalNAc moiety (formula II) and to conjugates of nucleic acid molecules with such N-Acetylgalactosamine containing molecules. Also provided are methods for preparation of these molecules and possible uses thereof, in particular in medicine. Wherein R.sup.1 is H or C.sub.1-6alkyl; R.sup.2 is a triphenylmethyl-based hydroxyl protecting group R.sup.3 is a phosphorus-containing group, particularly a phosphoramidite or a phosphonoamidite group, and K is represented by the general formula (II). ##STR00001##
HYDROSOLUBLE HYDROXYBISPHOSPHONIC DERIVATIVES OF DOXORUBICIN
The invention relates to hydrosoluble hydroxybisphosphonic derivatives of doxorubicin of formula (I) and the pharmaceutically acceptable salts thereof. The invention also relates to the use of said compounds as a drug, especially in the treatment of a bone tumour. The invention further relates to the pharmaceutical compositions comprising such compounds, the methods for the synthesis thereof and synthesis intermediates.
##STR00001##
PSMA BINDING LIGAND-LINKER CONJUGATES AND METHODS FOR USING
Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.