Patent classifications
C07D207/08
Lipids and Lipid Compositions for the Delivery of Active Agents
This invention provides for a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R.sup.A, R.sup.B, R.sub.2 and R.sub.4 are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
##STR00001##
SMALL LIPOPEPTIDOMIMETIC INHIBITORS OF GHRELIN O-ACYL TRANSFERASE
Compositions and methods are disclosed that relate to small molecule lipopeptidomimetic inhibitors of mammalian ghrelin O-acyl transferase (GOAT). Compounds of general Formula (I) and substructures thereof, i.e., Formulae (II), (IIa), (IIa1), (IIa2), (IIb), (IIb1), (IIb2), (IIc) and (III), are shown to exhibit potent inhibition of the octanoylation of ghrelin peptide, where the resulting non-octanoylated (des-acyl) form of ghrelin lacks GHSr ligand activity that is associated with weight gain and insulin resistance. These and related embodiments will find uses for treating subjects known to have, or suspected of being at risk for having, a condition that would benefit from a decreased level of acylated ghrelin peptide, such as type II diabetes, impaired glucose tolerance, insulin resistance, Prader-Willi syndrome (PWS) and obesity.
HETEROCYCLIC SULFONAMIDES, USES AND PHARMACEUTICAL COMPOSITIONS THEREOF
The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I:
##STR00001##
as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.
CYTOTOXIC AND ANTI-MITOTIC COMPOUNDS, AND METHODS OF USING THE SAME
Compounds having cytotoxic and/or anti-mitotic activity are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having cytotoxic and/or anti-mitotic activity.
EBNA1 inhibitors and their method of use
Pharmaceutical compositions of the invention comprise EBNA1 inhibitors useful for the treatment of diseases caused by EBNA1 activity such as cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by lytic Epstein-Barr Virus (EBV) infection.
EBNA1 inhibitors and their method of use
Pharmaceutical compositions of the invention comprise EBNA1 inhibitors useful for the treatment of diseases caused by EBNA1 activity such as cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by lytic Epstein-Barr Virus (EBV) infection.
Beta-hydroxy heterocyclic amines and their use in the treatment of hyperglycaemia
There is herein provided a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R.sup.1, ring A, m and n have meanings as provided in the description. ##STR00001##
Beta-hydroxy heterocyclic amines and their use in the treatment of hyperglycaemia
There is herein provided a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R.sup.1, ring A, m and n have meanings as provided in the description. ##STR00001##
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.
HETEROCYCLIC COMPOUND
Provided is a heterocyclic compound having a superior RBP4-lowering action and useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4. A compound represented by the formula (I):
##STR00001##
wherein each symbol is as defined in the Description, or a salt thereof has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4.