Patent classifications
C07D271/107
NOVEL TRYPTOPHAN HYDROXYLASE INHIBITOR AND PHARMACEUTICAL COMPOSITION INCLUDING SAME
The present invention relates to a novel tryptophan hydroxylase inhibitor and a pharmaceutical composition including same, wherein the novel tryptophan hydroxylase inhibitor has an excellent inhibitory effect on TPH1, and thus can be usefully used for the prevention or treatment of disorders, such as metabolic disorders, cancer, digestive or cardiovascular system disorders, related to TPH1 activity. In particular, the novel tryptophan hydroxylase inhibitor has an excellent treatment effect on inflammatory bowel disorders, and thus can be usefully used for the treatment of inflammatory bowel disorder.
(HETERO)ARYL SULFONAMIDE COMPOUND AND FORMULATION FOR CONTROLLING HARMFUL ORGANISMS
A compound represented by formula (I) or a salt thereof, as well as a formulation for controlling harmful organisms, an insecticidal formulation, an acaricidal formulation, a nematicidal formulation, or a formulation for controlling or exterminating endoparasites, containing at least one compound selected from the group consisting of the compounds described above and salts thereof, as an active ingredient.
##STR00001##
In formula (I), Ar.sup.1 is a benzene ring or a 5- to 6-membered heteroaryl ring, R.sup.1 is a C1 to C6 alkyl group, a halogeno group, or the like, n represents the number of R.sup.1 and is 0, 1, 2, or 3, and in the case of n being 2 or more, two or more R.sup.1 may be the same as or different from one another, R.sup.2 is a C1 to C6 alkyl group, a C1 to C6 haloalkyl group, or the like, R.sup.3 is a hydrogen atom, a C1 to C6 alkyl group, a C1 to C6 alkylcarbonyl group, or the like, and AR.sup.2 represents a substituted or unsubstituted heteroaryl group.
MONITORING AND DOSAGE CONTROL OF TAGGED TREATMENT POLYMERS IN INDUSTRIAL WATER SYSTEMS
The present invention relates to a fluorescently-tagged (co)polymer useful as a scale inhibitor in industrial water systems. Said (co)polymer comprises a (i) reactive fluorescent compound selected from a diazole compound (ii) at least one monoethylenically unsaturated acid monomer, and (iii) optionally, at least one monoethylenically unsaturated acid-free monomer.
MONITORING AND DOSAGE CONTROL OF TAGGED TREATMENT POLYMERS IN INDUSTRIAL WATER SYSTEMS
The present invention relates to a fluorescently-tagged (co)polymer useful as a scale inhibitor in industrial water systems. Said (co)polymer comprises a (i) reactive fluorescent compound selected from a diazole compound (ii) at least one monoethylenically unsaturated acid monomer, and (iii) optionally, at least one monoethylenically unsaturated acid-free monomer.
METABOLICALLY STABLE N-ACYLAMINOOXADIAZOLES USEFUL AS ANTIBACTERIAL AGENTS
The present invention is related to the development of therapeutics and prophylactics for the treatment and/or prevention of bacterial infections in humans and other mammals. A new class of small molecules is disclosed that inhibits the bacterial trans-translation/ribosome rescue mechanism and thus blocks infection of host cells by bacteria. Also disclosed are methods of using the small molecule inhibitors in the treatment/prevention of bacterial infections.
Oxadiazole inhibitors of HIPK2 for treating kidney fibrosis
Compounds that are selective inhibitors of Smad3 activation are disclosed. The compounds have the following structure: ##STR00001##
in which Z is an oxadiazole. The compounds disclosed are useful in treatment of fibrotic disease, particularly renal fibrosis, and similar diseases associated with the dysregulation of the HIPK2/Smad3 signaling pathway.
Oxadiazole inhibitors of HIPK2 for treating kidney fibrosis
Compounds that are selective inhibitors of Smad3 activation are disclosed. The compounds have the following structure: ##STR00001##
in which Z is an oxadiazole. The compounds disclosed are useful in treatment of fibrotic disease, particularly renal fibrosis, and similar diseases associated with the dysregulation of the HIPK2/Smad3 signaling pathway.
TAGGED TREATMENT POLYMERS FOR MONITORING ANTISCALANT CONCENTRATIONS IN INDUSTRIAL WATER SYSTEMS
The present invention relates to a fluorescently-tagged (co)polymer useful as a scale inhibitor in industrial water systems. Said (co)polymer comprises a (i) reactive fluorescent compound selected from a diazole compound (ii) at least one monoethylenically unsaturated acid monomer, and (iii) optionally, at least one monoethylenically unsaturated acid-free monomer.
Non-beta lactam antibiotics
The invention provides a newly discovered oxadiazole class of antibiotics. The oxadiazoles impair cell-wall biosynthesis and exhibit activities against the Gram-positive bacteria such as the bacterium Staphylococcus aureus, including methicillin-resistant S. aureus (MRSA) and vancomycin-resistant and linezolid-resistant S. aureus. For example, 5-(1H-indol-5-yl)-3-(4-(4-(trifluoromethyl)phenoxy)phenyl)-1,2,4-oxadiazole (antibiotic 75b) was efficacious in a mouse model of MRSA infection, exhibiting a long half-life, a high volume of distribution, and low clearance. Antibiotic 75b antibiotic is bactericidal and is orally bioavailable. This class of antibiotics can be used as a therapeutic agent against infections by Gram-positive bacteria such as MRSA.
Non-beta lactam antibiotics
The invention provides a newly discovered oxadiazole class of antibiotics. The oxadiazoles impair cell-wall biosynthesis and exhibit activities against the Gram-positive bacteria such as the bacterium Staphylococcus aureus, including methicillin-resistant S. aureus (MRSA) and vancomycin-resistant and linezolid-resistant S. aureus. For example, 5-(1H-indol-5-yl)-3-(4-(4-(trifluoromethyl)phenoxy)phenyl)-1,2,4-oxadiazole (antibiotic 75b) was efficacious in a mouse model of MRSA infection, exhibiting a long half-life, a high volume of distribution, and low clearance. Antibiotic 75b antibiotic is bactericidal and is orally bioavailable. This class of antibiotics can be used as a therapeutic agent against infections by Gram-positive bacteria such as MRSA.