A61P11/02

Ultra-potent neutralization of GM-CSF by multispecific antibodies and uses thereof

The present invention provides multispecific antibodies, and antigen binding fragments thereof, that potently neutralize a cytokine and that may thus be useful in the prevention and/or treatment of inflammatory and/or autoimmune diseases. In particular, the present invention provides a multispecific antibody, or an antigen binding fragment thereof, comprising at least two different domains specifically binding to at least two different, non-overlapping sites in a cytokine and an Fc moiety. The invention also relates to nucleic acids that encode such antibodies and antibody fragments and immortalized B cells and cultured plasma cells that produce such antibodies and antibody fragments. In addition, the invention relates to the use of the antibodies and antibody fragments of the invention in screening methods as well as in the diagnosis, prophylaxis and treatment of inflammatory and/or autoimmune diseases.

Urea derivative or pharmacologically acceptable salt thereof

Provided is a compound having a formyl peptide receptor like 1 (FPRL1) agonist effect. The present invention relates to a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. The present invention also relates to a pharmaceutical composition containing the compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. ##STR00001##

CRYSTALS, PREPARATION METHOD AND APPLICATION OF A MUSCARINIC RECEPTOR ANTAGONIST

The present invention provides crystals of a quaternary ammonium salt structure compound, i.e., (2R,3R)-3-[(2-cyclopentyl-2-hydroxy-2-phenyl)ethoxy]-1-(3-phenoxypropyl) azabicyclo[2,2,2]octylonium bromide (Compound I). A Type-A crystal of Compound I displays diffraction peaks at the following diffraction angles 2θ in a X-ray powder diffraction pattern thereof: 5.7±0.2 degrees, 12.9±0.2 degrees, 16.7±0.2 degrees, 18.0±0.2 degrees, 19.5±0.2 degrees, 21.1±0.2 degrees, 22.3±0.2 degrees and 23.3±0.2 degrees. A Type-B crystal of Compound I displays diffraction peaks at the following diffraction angles 2θ in a X-ray powder diffraction pattern thereof: 5.2±0.2 degrees, 15.8±0.2 degrees, 16.9±0.2 degrees, 17.7±0.2 degrees, 19.5±0.2 degrees, 20.2±0.2 degrees and 22.1±0.2 degrees. The present application also relates to a new method for preparing Compound I and applications of the two novel crystals in the field of medicine.

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.

TRPV4 antagonists

The present invention relates to pyrrolidine sulfonamide analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.

Compositions and kits useful for treatment of respiratory illness

A stable liquid composition contained in a bottle wherein the composition comprises from about 0.001% to about 0.5% of phenylephrine hydrochloride, by weight of the stable liquid composition. The composition comprises less than about 0.1% of total aldehydes, by weight of the stable liquid composition, and has a pH from about 2 to about 6.5. The bottle comprises a material selected from polyethylene terephthalate (PET), glycol-modified polyethylene terephthalate (PETG), oriented polypropylene (OPP), polyvinylchloride (PVC), polyvinylidene chloride (PVDC), nylon, polyethylene terephthalate polyester (PETP), or combinations thereof.

α4β7 peptide monomer and dimer antagonists

The invention relates to peptide dimer compounds and peptide monomer compounds that potently inhibit binding of α4β7 to the mucosal addressin cell adhesion molecule (MAdCAM) in vivo, possess high selectivity against α4β1 binding, and have high stability under gastrointestinal conditions.

LPA-ASSOCIATED PROTEIN AND RNA EXPRESSION

Provided herein are, inter alia, methods and biomarkers to determine if a patient has or is at risk for developing an LPA-associated disease, to indicate the progressiveness of the disease, and/or to facilitate evaluation of responsiveness to therapy. Compositions and kits including the biomarker proteins and biomarker RNAs provided herein are further provided.

CD3-Binding Molecules Capable of Binding to Human and Non-Human CD3
20220056131 · 2022-02-24 · ·

The present invention relates to CD3-binding molecules capable of binding to human and non-human CD3, and in particular to such molecules that are cross-reactive with CD3 of a non-human mammal (e.g., a cynomolgus monkey). The invention also pertains to uses of such antibodies and antigen-binding fragments in the treatment of cancer, autoimmune and/or inflammatory diseases and other conditions.

BICYCLIC HETEROCYCLYL DERIVATIVES AS IRAK4 INHIBITORS
20220056046 · 2022-02-24 ·

The present invention provides bicyclic heterocyclyl kinase enzyme inhibitor compounds of formula (I), which are therapeutically useful as kinase inhibitors, particularly IRAK4 inhibitors.

##STR00001##

wherein A, Y, Z, X.sub.1, X.sub.2, X.sub.3, R.sub.1, R.sub.3, ‘m’, ‘n’ and ‘p’ have the meanings given in the specification and pharmaceutically acceptable salt or stereoisomer thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical composition comprising at least one of the compounds of compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.