Patent classifications
A61P1/12
AZABICYCLOOCTANE DERIVATIVES AS FXR AGONISTS FOR USE IN THE TREATMENT OF LIVER AND GASTROINTESTINAL DISEASES
The invention provides methods for modulating the activity of farnesoid X receptors (FXRs) using compounds of Formula (I) or (II). In particular, the invention provides for the use of compounds of Formula (I) or (II), or a stereoisomer, enantionmer or pharmaceutically acceptable salt thereof, for treating or preventing liver and gastrointestinal diseases.
USE OF TAURINE IN PREVENTION AND/OR TREATMENT OF DISEASES INDUCED BY VIRUSES OF GENUS CORONAVIRUS AND/OR GENUS ROTAVIRUS
The present invention provides use of taurine in prevention and/or treatment of diseases induced by viruses of genus coronavirus and/or genus rotavirus, for example, porcine epidemic diarrhea, porcine transmissible gastroenteritis, rotavirus diarrhea and the like.
Diaminopyrimidine derivatives and processes for the preparation thereof
The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT.sub.4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.
Beta-hairpin peptidomimetics
Beta-hairpin peptidomimetics of the general formula (I), cyclo(P.sup.1-p.sup.2-p.sup.3-p.sup.4-p.sup.5-p.sup.6-p.sup.7p.sup.8p.sup.9-p.sup.10-p.sup.11-p.sup.12-T.sup.1-T.sup.2], and pharmaceutically acceptable salts thereof, with P.sup.1 to P.sup.12, T.sup.1 and T.sup.2 being elements as defined in the description and the claims, have broad spectrum Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as Klebsiella pneumoniae and/or Acinetobacter baumannii and/or Escherichia coli. They can be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
QUINOLONE COMPOUND
The present invention provides a compound represented by the formula (I)
##STR00001##
wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R.sup.1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R.sup.2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R.sup.3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
LINEAR POLYSACCHARIDE BASED FILM PRODUCTS
Film products, especially suitable for oral delivery, which can be formed during manufacture in the form of large and/or heavy film strips or sheets and subsequently cut into uniform dosage units, each dosage unit being uniform in content and having distributed therein a linear polysaccharide, such as pullulan, a plasticizer, and an active component.
BICYCLIC COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF
The present disclosure relates to a class of substituted bicyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts and pharmaceutical compositions containing them. The disclosure also relates to the process of preparation of compounds of Formula (I).
##STR00001##
These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of retinoic acid-related orphan receptor gamma (RORγ) such as inflammatory and/or autoimmune disorder, rheumatoid arthritis, psoriasis, psoriatic arthritis, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, COPD, cancer, cell proliferation, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, systemic lupus, erythematosus or other disorders.
COMPOSITION CONTAINING EXTRACT OR FRACTION OF GENUS JUSTICIA PLANT
The present invention relates to a pharmaceutical composition, food composition and cosmetic composition for preventing, treating, or improving allergic diseases comprising extract or fraction of a plant of the Justicia genus as an active ingredient. The extract or a fraction of a plant of the Justicia genus according to the present invention can inhibit IgE antibody secretion and the degranulation of mast cells and basophils, and exhibits an excellent anti-allergic effect, and thus can effectively prevent, treat, or improve allergic diseases.
FUSION POLYPEPTIDE CONTAINING GLP AND IMMUNOGLOBULIN HYBRID FC AND USE THEREOF
The present invention relates to a fusion polypeptide containing a glucagon-like peptide (GLP) and an immunoglobulin hybrid Fc, and more specifically, to a fusion polypeptide with an increased half-life and improved efficacy compared to the conventional fusion polypeptide based on the discovery of an immunoglobulin hybrid Fc suitable for GLP or analogs thereof, and a pharmaceutical composition for treating diabetes, inflammatory bowel disease, endoenteritis or diarrhea caused by anticancer chemotherapy, or short bowel syndrome, containing the fusion polypeptide. The fusion polypeptide of the present invention has an increased half-life and improved resistance to DPP-4 enzyme compared to those of GLP-1 and GLP-2, and it thus has improved drug efficacy in treating diabetes, inflammatory bowel disease, endoenteritis or diarrhea caused by anticancer chemotherapy, or short bowel syndrome, compared to those of the conventional drugs. Accordingly, the fusion polypeptide of the present invention can be effectively applied to pharmaceutical drugs.
ANTI-IGF-I RECEPTOR ANTIBODY
The present invention provides an anti-IGF-I receptor antibody that binds specifically to an IGF-I receptor of a vertebrate and has the proliferation-inducing activity of a vertebrate-derived cell, or a fragment thereof, or derivatives of these.