A61K2121/00

Polymorphs of N-[(6-cyano-2-fluoro)-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide as kallikrein inhibitors

The invention provides new polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide, pharmaceutical compositions containing them and their use in therapy. ##STR00001##

Lysin polypeptides active against Gram-negative bacteria

The present disclosure provides methods and compositions useful for the prophylactic and therapeutic amelioration and treatment of infections caused by Gram-negative bacteria, including Pseudomonas aeruginosa. The disclosure further provides compositions and methods of incorporating and utilizing lysin polypeptides of the present disclosure for augmenting the efficacy of antibiotics generally suitable for the treatment of Gram-negative bacterial infection.

Methods of using c-Met modulators

Methods of treating cancer by administering a compound of Formula I, ##STR00001##
or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments are described, wherein R.sup.1 is halo; R.sup.2 is halo; and Q is CH or N.

Methods for inhibiting fibrosis in a subject in need thereof

In one aspect, the invention provides methods for treating, inhibiting, alleviating or preventing fibrosis in a mammalian subject suffering, or at risk of developing a disease or disorder caused or exacerbated by fibrosis and/or inflammation. In one embodiment, the invention provides methods of treating a subject suffering from renal fibrosis. In one embodiment, the invention provides methods of reducing proteinuria in a subject suffering from a renal disease or condition associated with proteinuria. The methods comprise the step of administering, to a subject in need thereof, an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation.

STERILIZATION METHOD AND STERILIZATION APPARATUS
20200246632 · 2020-08-06 · ·

Provided a method of sterilization by ultraviolet irradiation whereby effects on the human body can be mitigated and an odor that arises after ultraviolet irradiation can be controlled. The sterilization method includes: a step (a) of irradiating a skin of a hand or arm with ultraviolet having a wavelength of 200 nm or more and 230 nm or less; and a step (b) of applying a topical skin preparation, cosmetic, or aqueous solution containing at least one amino acid or amino acid derivative selected from an amino acid group A to a region of the skin irradiated with the ultraviolet. The amino acid group A includes valine, leucine, isoleucine, glutamic acid, arginine, serine, aspartic acid, proline, and glycine.

pHLIP® peptide-mediated epitope tethering at cell surfaces

The invention features methods and compositions for eliciting an anti-tumor response in a subject comprising administering to the subject a pHLIP construct comprising an antibody recruiting molecule linked to one or more pHLIP peptides by a non-cleavable linker compound. The construct increases the amount of the antibody recruiting molecule on the surface of a diseased cell.

Compositions and methods for inhibiting the activity of LAR family phosphatases

A method of inhibiting and/or reducing the activity, signaling, and/or function of leukocyte-common antigen related (LAR) family of phosphatases in a cell of a subject induced by proteoglycans includes administering to the cell a therapeutic agent that inhibits one or more of catalytic activity, signaling, and function of the LAR family phosphatases without inhibiting binding to or activation the LAR family phosphatases by the proteoglycans.

Methods for alleviating symptoms of sporadic amyotrophic lateral sclerosis by neutralizing a HERV-K envelope protein using an anti-HERV-K envelope protein antibody

The present invention relates to a novel antibody against HERV-K envelope that targets a conserved region not affected by glycosylation or by native conformation, and its use in diagnostics and/or in therapy.

THE OPTIMAL 225ACTINIUM--213BISMUTH GENERATOR FOR ALPHA-PARTICLE RADIOIMMUNOTHERAPY
20200230266 · 2020-07-23 · ·

The present invention is directed to a method for the preparation of a radiolabled conjugate composition comprising Bismuth-213 loaded targeting moieties that have been diluted with cold targeting moieties in a predetermined ratio of amount of cold targeting moieties to amount of Bismuth-213 loaded targeting moieties. Said ratio is determined by determining the amount T of target moieties per diseased cell to be treated, and determining the amount Z of Bismuth-213 atoms needed to kill a diseased cell, and contacting targeting moieties with Bismuth-213 atoms in a ratio of T over Z, to form a conjugate composition with a predetermined ratio of cold targeting moieties and Bismuth-213 loaded targeting moieties. The invention is further directed to a conjugate that can be prepared with the method according to the invention, a pharmaceutical formulation comprising the conjugate according to the invention.

Pharmaceutical composition for preventing or treating immune diseases or inflammatory diseases, containing biguanide derivative compound as active ingredient

The present invention relates to a biguanide derivative compound capable of effectively preventing and treating immune diseases. The biguanide-based derivative compound according to the present invention inhibits the generation of IL-17 and TNF-, which are inflammatory cytokines, increases the activity of regulatory T cells having an immunomodulatory function, and exhibits excellent therapeutic effects in animal models of immune diseases. Accordingly, the biguanide-based derivative compound can be usefully used as an immunosuppressant or a pharmaceutical composition capable of preventing or treating various immune diseases, such as autoimmune diseases, inflammatory diseases, and transplant rejection, caused by the dysregulation of immune responses.