Patent classifications
C07D271/107
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.
TERBENZOCYCLOPENTADIENE COMPOUND, HIGH POLYMER, MIXTURE, COMPOSITION AND ORGANIC ELECTRONIC DEVICE
Disclosed are a terbenzocyclopentadiene compound of better solubility and film-forming property, and a high polymer, mixture, composition and organic electronic device comprising same. This terbenzocyclopentadiene compound contains a benzocyclopentadiene structure. The matching of energy level and the symmetry of the structure provide a possibility for increasing the chemical/environmental stability of terbenzocyclopentadiene compounds and photoelectric devices. This terbenzocyclopentadiene compound has a better solubility in an organic solvent, and also facilitates forming a high-quality film by a printing method due to a high molecular weight. After this terbenzocyclopentadiene compound is used in OLED, particularly as a luminescent layer material, a higher quantum efficiency, luminescence stability and device life time can be provided.
MITOTIC KINESIN INHIBITORS AND METHODS OF USE THEREOF
This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors.
##STR00001##
MITOTIC KINESIN INHIBITORS AND METHODS OF USE THEREOF
This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors.
##STR00001##
COMPOSITIONS AND METHODS FOR TREATING CANCERS
The invention describes compounds that inhibit both HDAC and GSK3? (i.e., HDAC/GSK3? dual inhibitors). The invention further describes compositions containing these HDAC/GSK3? dual inhibitors, as well as methods and kits using these HDAC/GSK3? dual inhibitors to treat various medical conditions. The invention also provides methods and kits using a HDAC inhibitor and a GSK3? to treat various medical conditions, and compositions containing a HDAC inhibitor and a GSK3?. Medical conditions treatable with various embodiments of the invention include but are not limited to cancers and tumors.
COMPOSITIONS AND METHODS FOR TREATING CANCERS
The invention describes compounds that inhibit both HDAC and GSK3? (i.e., HDAC/GSK3? dual inhibitors). The invention further describes compositions containing these HDAC/GSK3? dual inhibitors, as well as methods and kits using these HDAC/GSK3? dual inhibitors to treat various medical conditions. The invention also provides methods and kits using a HDAC inhibitor and a GSK3? to treat various medical conditions, and compositions containing a HDAC inhibitor and a GSK3?. Medical conditions treatable with various embodiments of the invention include but are not limited to cancers and tumors.
BROAD SPECTRUM ANTIVIRAL COMPOUNDS AND USES THEREOF
Disclosed herein, inter alia, are agents having antiviral activity and methods of use thereof.
BROAD SPECTRUM ANTIVIRAL COMPOUNDS AND USES THEREOF
Disclosed herein, inter alia, are agents having antiviral activity and methods of use thereof.
GLP-1 receptor modulators
Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where represents either or both the R and S form of the compound): ##STR00001##
where A, B, C, Y.sub.1, Y.sub.2, Z, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, W.sub.1, n, p and q are as defined herein.