Patent classifications
C07J1/00
METHODS FOR THE EPIGENETIC ANALYSIS OF DNA, PARTICULARLY CELL-FREE DNA
Methods are provided for the epigenetic analysis of cell-free DNA using organic boranes to convert oxidized 5-methylcytosine residues in the cell-free DNA to dihydrouracil (DHU) residues. Cell-free DNA is contacted with an organic borane selected to successively bring about reduction, deamination, and decarboxylation of oxidized 5-methylcytosine residues such as 5-carboxymethylcytosine and 5-formylcytosine, resulting in DHU residues in place thereof. Following amplification, the treated cell-free DNA is sequenced, with the DHU residues read as thymine residues. Reaction mixtures, kits and additional methods are also provided, as are related methods for the epigenetic analysis of DNA, including cell-free DNA.
(17-ß)-3-Oxoandrost-4-En-17-Yl Undecanoate Compositions and Methods of Their Preparation and Use
Disclosed herein are compositions having a lipophilic active agent and methods of their use.
Non-surgical prevention of boar taint and aggressive behavior
Embodiments of the present invention provide a pharmaceutical intervention in the neonatal pig that inhibits and delays development and activation of the HPG axis, growth of the boar testis and inhibits testicular production of testosterone and androstenone, which prevents the development of aggressive behavior in the maturing boars and the presence of boar taint in the meat. The invention comprises treatment with a combination of an androgen and an estrogen in the newborn male piglet using extended drug delivery methods, with a defined duration of no more than 12 weeks, for the purpose of inhibiting the production of testosterone and androstenone and the accumulation of the boar taint-inducing molecules androstenone and skatole in the fat.
LYMPH DIRECTING PRODRUGS
The present invention relates to compounds and their uses, in particular, compounds in the form of prodrugs that promote transport of a pharmaceutical agent to the lymphatic system and subsequently enhance release of the parent drug.
(17-ß)-3-OXOANDROST-4-EN-17YL TRIDECANOATE COMPOSITIONS AND METHODS OF THEIR PREPARATION AND USE
Described here are substantially pure (17-)-3-Oxoandrost-4-en-17-yl tridecanoate compositions, methods of their preparation and uses thereof.
ORALLY ACTIVE LEUKEMIA INHIBITORY FACTOR (LIF) ANTAGONISTS FOR THE TREATMENT OF CANCER
Described herein are novel LIF/LIFR inhibitors that exhibit improved cytotoxicity and bioavailability. These LIF/LIFR inhibitors are particularly useful for the treatment of tumors associated with overexpression of LIF.
METHOD OF PREPARING ESTRADIOL DERIVATIVES BY SOLID-PHASE SYNTHESIS
The present invention relates to a method of preparing estradiol derivatives and/or estrone derivatives, which are suitable for radiolabeling. The present invention further relates to the estradiol derivatives and/or estrone derivatives, preferably obtained by the method of the present invention, as well as to the use of the estradiol derivatives and/or estrone derivatives for radiolabeling with diagnostic and/or therapeutic radionuclides. The present invention further relates to a method of imaging and/or diagnosis of breast cancer as well as to a method of treatment of breast cancer.
15beta-substituted estrone derivatives as selective inhibitors of 17beta-hydroxysteoid-dehydrogenases, method of preparation and use thereof
15-substituted derivatives of estrone of general formula I wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 are independently selected from the group consisting of: C.sub.1-C.sub.4 alkyl, C.sub.1-C.sub.4 alkoxy, C.sub.1-C.sub.4 halogenalkyl, halogen, COOR.sup.6 wherein R.sup.6 is C.sub.1-C.sub.4 alkyl; H, OH; optionally, R.sup.3, R.sup.4 and R.sup.5 are each formed by a hydrogen atom, while R.sup.1 and R.sup.2 together form an aryl group, preferably naphthyl, in which the aromatic ring in position C-15 can be mono-, di-, tri-, tetra- and penta-substituted with substituents R.sup.1-R.sup.5. Compounds of the invention may be used for diagnosis and possibly also for the treatment of estrogen-dependent diseases.
Methods for preparation of bile acids and derivatives thereof
The present application relates to a method of preparing compounds of Formula (I) or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, R.sub.1 is H, -OH, -OH, or an oxo group. ##STR00001##
Estrogen receptor modulators
Described herein, inter alia, are compositions and methods for treating or preventing hyperproliferative disorders, including cancer.