Patent classifications
C07J1/00
Use of compounds in preparation of a medicament for treatment of hemorrhagic stroke
Disclosed is a use of 5α-androstane-3β,5,6β-triol, an analogue, a deuterated derivative, and a pharmaceutically acceptable salt thereof in manufacture of a medicament for the treatment of hemorrhagic stroke in a patient. The hemorrhagic stroke is intracerebral hemorrhage or subarachnoid hemorrhage.
Polysubstituted benzene, preparation method thereof, and method of using the same
A polysubstituted benzene compound, preparation method thereof, and method of using the same. The compound has a formula I or I′, where X represents carbon, sulfur, or oxygen; R.sup.1 represents a C.sub.1-16 alkyl, C.sub.2-16 alkenyl, or C.sub.2-10 alkynyl; R.sup.2 represents hydrogen, halogen, C.sub.1-16 alkyl, C.sub.2-16 alkenyl, or C.sub.2-10 alkynyl; or an aryl group or a substituted aryl group by 1-5 groups selected from halogen, C.sub.1-26 alkyl, C.sub.1-3 halogenated alkyl, O—C.sub.1-3 alkyl, hydroxyl, amino, nitro, cyano group, aldehyde group and ester group; or a heteroaryl group or a substituted heteroaryl group by 1-5 groups selected from halogen, C.sub.1-26 alkyl, C.sub.1-3 halogenated alkyl, O—C.sub.1-3 alkyl, hydroxyl, amino, nitro, cyano group, aldehyde group and ester group; the heteroaryl group is a 3-10-membered heteroaryl group including N, S, O, or a combination thereof.
SHIP INHIBITORS AND USES THEREOF
The present invention relates to SHIP inhibitor compounds and methods for using these compounds. In particular, the present invention discloses the following methods: (i) a method of treating graft versus host disease in a subject; (ii) a method of inhibiting a SHIP1 protein in a cell; (iii) a method of selectively inhibiting a SHIP1 protein in a cell; (iv) a method for treating or preventing graft-versus-host disease (GVHD) in a recipient of an organ or tissue transplant; (v) a method of modulating SHIP activity in a cell expressing SHIP1 or SHIP2; (vi) a method of ex vivo or in vitro treatment of transplants; (vii) a method of inhibiting tumor growth and metastasis in a subject; (viii) a method of treating a hematologic malignancy in a subject; (ix) a method of inducing apoptosis of multiple myeloma cells; (x) a method of treating multiple myeloma in a subject; (xi) a method of inhibiting the proliferation of a human breast cancer cell; and (xii) a method of treating breast cancer in a subject.
SMALL MOLECULES ACTIVE AGAINST GRAM-NEGATIVE BACTERIA
Disclosed are novel compounds that accumulate in Gram-negative bacteria. Also disclosed are method of antimicrobial treatment using the compounds.
Quantitative profiling of progesterone metabolites for the prediction of spontaneous preterm delivery
Disclosed are methods for identifying a pregnant female who is susceptible to spontaneous preterm delivery. In particular, disclosed are methods for identifying a pregnant female who is susceptible to spontaneous preterm delivery based on ratios of steroids in samples obtained from the pregnant female.
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-carboxylcytosine 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.
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-carboxylcytosine 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.
C19 SCAFFOLDS AND STEROIDS AND METHODS OF USE AND MANUFACTURE THEREOF
The present disclosure relates to stereodefined polycyclic (e.g., tetracyclic) compounds that contain quaternary centers at one or multiple ring fusions, synthetic methods for preparing such compounds, and methods of using such compounds to treat a disease, such as a brain tumor and, particularly, a glioma.
NEUROACTIVE 19-ALKOXY-17-SUBSTITUTED STEROIDS, PRODRUGS THEREOF, AND METHODS OF TREATMENT USING SAME
The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
INTERMEDIATES FOR THE PREPARATION OF 11-METHYLENE STEROIDS
Compounds having the formula
##STR00001##
or solvates of the compounds can be used as intermediates in the preparation of the synthetic steroids, Etonogestrel and Desogestrel, as well as other pharmaceutically active agents.