Patent classifications
C07C235/56
NOVEL INHIBITORS OF GUANOSINE MONOPHOSPHATE SYNTHETASE AS THERAPEUTIC AGENTS
The invention provides a series of GMPS enzyme inhibitors. The invention includes potent GMPS inhibitors that specifically and covalently bind to GMPS, exhibit broad anti-cancer activity, block the infection efficiency of viruses, and have the potentials to suppress undesired immune responses. These novel inhibitors of GMPS, and their derivatives, have tremendous potentials to be used as therapeutic agents for the treatment of cancers, viral infection and immune disorders.
NOVEL INHIBITORS OF GUANOSINE MONOPHOSPHATE SYNTHETASE AS THERAPEUTIC AGENTS
The invention provides a series of GMPS enzyme inhibitors. The invention includes potent GMPS inhibitors that specifically and covalently bind to GMPS, exhibit broad anti-cancer activity, block the infection efficiency of viruses, and have the potentials to suppress undesired immune responses. These novel inhibitors of GMPS, and their derivatives, have tremendous potentials to be used as therapeutic agents for the treatment of cancers, viral infection and immune disorders.
Small Molecule Inhibitors Selective For Polo-Like Kinase Proteins
Disclosed are small molecule PLK inhibitors that can target the polo box domain (PBD). Inhibitors can have an atomic mass of about 1000 Da or less and a general structure of
##STR00001##
For instance, the inhibitors can include an alkyl benzamido benzoic acid core structure.
IDO INHIBITORS
- James Aaron Balog ,
- Emily Charlotte Cherney ,
- Weiwei Guo ,
- Audris Huang ,
- Jay A. Markwalder ,
- Steven P. Seitz ,
- Weifang Shan ,
- David K. Williams ,
- Natesan Murugesan ,
- Susheel Jethanand Nara ,
- Saumya Roy ,
- Soodamani Thangavel ,
- Ramesh Kumar Sistla ,
- Srinivas Cheruku ,
- Srinivasan Thangathirupathy ,
- Yadagiri Kanyaboina ,
- Nagalakshmi Pulicharla
There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
DP ANTAGONIST
An object of the present invention is to provide a DP receptor antagonist. A compound represented by general formula (I):
##STR00001## (wherein all symbols are as shown in the specification) and a pharmaceutically acceptable salt thereof have DP receptor antagonistic activity and are also highly safe, and thus are useful as active ingredients of pharmaceuticals for DP receptor-mediated diseases. In addition, the compound represented by the general formula (I) and the pharmaceutically acceptable salt thereof also have good transferability to the central nervous system, and thus are particularly useful as a preventive and/or therapeutic agent for diseases associated with DP receptors present in the central nervous system among DP receptor-mediated diseases, that is, sleep-wake disorders.
NOVEL SULFONYLAMINOBENZAMIDE COMPOUNDS AS ANTHELMINTICS
The present invention relates to a new compound of formula (I) wherein the variables have the meaning as indicated in the claims; or an enantiomer or salt thereof. The compounds of formula (I) are useful in the control of parasites, in particular endoparasites, in and on vertebrates.
##STR00001##
Optical film, circularly polarizing plate and organic electroluminescent display device
Provided is an optical film containing a cellulose derivative, the optical film having an in-plane retardation Ro.sub.550 within the range of 120 to 160 nm measured at a wavelength of 550 nm under an atmosphere of a temperature of 23° C. and a relative humidity of 55%, and a ratio Ro.sub.450/Ro.sub.550 within the range of 0.65 to 0.99, Ro.sub.450/Ro.sub.550 being a ratio of an in-plane retardation Ro.sub.450 measured at a wavelength of 450 nm to the in-plane retardation Ro.sub.550 measured at a wavelength of 550 nm, wherein, a substituent of a glucose skeleton in the cellulose derivative satisfies the requirements (a) and (b) which are described in the specification, and the optical film contains a compound A satisfying the following condition defined by Expression (a1) which is described in the specification.
Optical film, circularly polarizing plate and organic electroluminescent display device
Provided is an optical film containing a cellulose derivative, the optical film having an in-plane retardation Ro.sub.550 within the range of 120 to 160 nm measured at a wavelength of 550 nm under an atmosphere of a temperature of 23° C. and a relative humidity of 55%, and a ratio Ro.sub.450/Ro.sub.550 within the range of 0.65 to 0.99, Ro.sub.450/Ro.sub.550 being a ratio of an in-plane retardation Ro.sub.450 measured at a wavelength of 450 nm to the in-plane retardation Ro.sub.550 measured at a wavelength of 550 nm, wherein, a substituent of a glucose skeleton in the cellulose derivative satisfies the requirements (a) and (b) which are described in the specification, and the optical film contains a compound A satisfying the following condition defined by Expression (a1) which is described in the specification.
Hepatitis B capsid assembly modulators
Described herein are hepatitis B capsid assembly modulators and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of hepatitis B.
Immunomodulator and anti-inflammatory compounds
The present invention provides dihydroorotate dehydrogenase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders wherein the inhibition of Dihydroorotate dehydrogenase is known to show beneficial effect.