Patent classifications
C07D213/80
Compositions and methods for enhancing bioenergetic status in female germ cells
Compositions and methods comprising bioenergetic agents for restoring the quality of aged oocytes, enhancing oogonial stem cells or improving derivatives thereof (e.g., cytoplasm or isolated mitochondria) for use in fertility-enhancing procedures, are described.
Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity
This invention relates to substituted 4-pyridones of formula 1 ##STR00001##
and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity
This invention relates to substituted 4-pyridones of formula 1 ##STR00001##
and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
COMPOUNDS AND METHODS OF USE
The present invention provides compounds useful in treating or preventing inflammation, acne, bacterial conditions and promoting the appearance of healthy skin and compositions including these compounds.
COMPOUNDS AND METHODS OF USE
The present invention provides compounds useful in treating or preventing inflammation, acne, bacterial conditions and promoting the appearance of healthy skin and compositions including these compounds.
PROCESS FOR THE PREPARATION OF INTERMEDIATE OF DOLUTEGRAVIR
The present invention provides a novel processes for preparation of methyl 3-(benzyloxy)-5-(2,4-difluorobenzylcarbamoyl)-4-oxo-1-(2-oxoethyl)-1,4-dihydropyiridine-2-carboxylate using novel intermediates.
Neprilysin inhibitors
In one aspect, the invention relates to compounds having the formula: ##STR00001##
where R.sup.1-R.sup.6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
Neprilysin inhibitors
In one aspect, the invention relates to compounds having the formula: ##STR00001##
where R.sup.1-R.sup.6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
COMPOSITIONS AND METHODS FOR DELIVERING PHARMACEUTICALLY ACTIVE AGENTS
The invention relates to modified lysines of the formula (I). The invention further relates to polypeptides comprising one or more modified lysine residues, pharmaceutical delivery systems comprising these polypeptides, pharmaceutical compositions containing them, and to their use in therapy.
##STR00001##
Inhibitors of collagen prolyl 4-hydroxylase
Biheteroaryl dicarboxylates and esters, and salts thereof which are useful as modulators of CP4H activity and more particularly as inhibitors of CP4H. Compounds of formula: ##STR00001## and salts thereof where: X is S, O, NH, or NR, where R is an alkyl group having 1-3 carbon atoms; R.sub.1 and R.sub.2 independently are —OR.sub.7, or —NHSO.sub.2R.sub.8, where R.sub.7 is selected from: hydrogen, alkyl, alkenyl, alkoxyalkyl, —R′—CO—R″, —R′—CO—O—R″, —CO—R″, —R′—O—CO—R″, —R′—CO—NR″, —CO—NR″, or —R′—O—CO—NR″, and R.sub.8 is selected from hydrogen, alkyl, aryl, arylalkyl; R.sub.3, R.sub.4 and R.sub.6 independently are hydrogen, alkyl, alkoxy, alkenyl, alkenoxy, haloalkyl, haloalkenyl, halogen, hydroxyl, hydroxyalkyl, hydroxyalkenyl, aryl, aryloxy, arylalkyl or arylalkyloxy; R.sub.5 is hydrogen, halogen, alkyl having 1-3 carbon atoms, or alkoxy having 1-3 carbon atoms; —R′— is a divalent straight chain or branched alkylene, and —R″ is an alkyl, alkenyl, arylalkyl, or aryl group. Methods for inhibition of CP4H in vivo and in vitro.