摘要:
Disclosed are sulfonamidoquinoline compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R1, R2, R3 and R4 are as described herein. In certain embodiments, a compound disclosed herein inhibits ubiquitination, and can be used to treat disease by blocking the degradation of tumor suppressors.
摘要:
wherein R1 through R8 are as defined in the claims, exhibit a positive allosteric GABAB modulator effect and are thus useful as positive allosteric modulators of the GABAB receptor.
摘要:
Novel compounds having a formula embodiments of a method of making the same, and of a composition comprising them are disclosed herein. Also disclosed are embodiments of a method of treating or preventing a metabolic disorder in a subject, comprising administering to a subject ( e.g. , via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and treating or preventing a metabolic disorder in the subject. Additionally disclosed are embodiments of a method of treating or preventing inflammation in an intestinal region of a subject, comprising administering to the subject ( e.g. , via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and thereby treating or preventing inflammation in the intestinal region of the subject.
摘要:
A process for preparing a compound of formula (ii),
comprising (a) treating a compound of formula (i) with H 2 and a platinum oxide catalyst under reducing conditions; and (b) subjecting the product of step (a) to resolution with di-toluoyl-L-tartaric acid to provide compound (ii) in about 97% enantiomeric excess.
摘要:
Disclosed herein are embodiments of a system for treating water. The system comprises a biochar inlet, and optionally a metal salt inlet, ozone inlet, organic carbon compound inlet or any combination thereof. The biochar may be produced by biomass pyrolysis and the pyrolysis may be coupled to energy generation. The system also comprises a filtration device, such as a reactive filtration device. The system produces a treated water stream and a reject stream, which may be further separated into a recycled water stream and a solid product. The solid product may be suitable as a soil amendment for application to agricultural land, or for recycling. A method for using the system to treat water also is disclosed.
摘要:
In this application is described the expression and purification of a recombinant Plasmodium falciparum (FVO) MSP-1 42 . The method of the present invention produces a highly purified protein that retains folding and disulfide bridging of the native molecule. The recombinant MSP-1 42 is useful as a diagnostic reagent, for use in antibody production, and as a vaccine.
摘要:
The present invention relates antidotes to anticoagulants targeting factor Xa. The antidotes are factor Xa protein derivatives that bind to the factor Xa inhibitors thereby substantially neutralizing them but do not assemble into the prothrombinase complex. The derivatives describe herein lack or have reduced intrinsic coagulant activity. Disclosed herein are methods of stopping or preventing bleeding in a patient that is currently undergoing anticoagulant therapy with a factor Xa inhibitor.