Patent classifications
C07J31/006
PROCESS FOR THE PREPARATION OF FULVESTRANT
The present invention relates to a process for the preparation of Fulvestrant which includes recovering the by-products deriving from the oxidation of the corresponding sulfide and then subjecting the by-products to a reduction reaction in the presence of specific reducing agents.
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.
19-NOR C3, 3-DISUBSTITUTED C21-N-PYRAZOLYL STEROIDS AND METHODS OF USE THEREOF
Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I):
##STR00001##
and pharmaceutically acceptable salts thereof; wherein , R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6, and R.sup.7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
C7 SUBSTITUTED OXYSTEROLS AND METHODS OF USE THEREOF
Compounds are provided according to Formula (A):
##STR00001##
and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1A, R.sup.1B, n, R.sup.2A, R.sup.2B, R.sup.3, and R.sup.4 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
POSITIVE RESIST COMPOSITION AND PATTERNING PROCESS
A positive resist composition is provided comprising (A) an acid generator in the form of a sulfonium salt consisting of a fluorine-containing sulfonate anion and a fluorine-containing sulfonium cation, (B) a quencher in the form of a sulfonium salt containing at least two fluorine atoms in its cation or containing at least 5 fluorine atoms in its anion and cation, and (C) a base polymer comprising repeat units (a1) having a carboxy group whose hydrogen is substituted by an acid labile group and/or repeat units (a2) having a phenolic hydroxy group whose hydrogen is substituted by an acid labile group. The resist composition exhibits a high sensitivity, high resolution and improved LWR or CDU.
FLUORINATED BILE ACIDS
Compounds of general formula (1):
##STR00001##
wherein R.sup.1, R.sup.2 and R.sup.3 are as defined herein;
are of use in the treatment and prevention of neurodegenerative disorders including Alzheimer's disease and Parkinson's disease.
SQUALAMINE SOLID FORMS AND METHODS OF MAKING THE SAME
Provided herein are crystalline solid forms of squalamine phosphate designated as Form 1 and Form 2, compositions containing one or both forms, and methods of their preparation and of their use.
C7 substituted oxysterols and methods of use thereof
Compounds are provided according to Formula (A): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1A, R.sup.1b, n, R.sup.2A, R.sup.2b, R.sup.3, and R.sup.4 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions. ##STR00001##
PREPARATIONS OF HYDROPHOBIC THERAPEUTIC AGENTS, METHODS OF MANUFACTURE AND USE THEREOF
The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic gent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, Meibomian gland dysfuntion or skin inflammatiom or a respiratory disease (e.g., asthma).
FARNESOID X RECEPTOR MODULATORS
The present application provides a compound of formula I:
##STR00001##
or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R.sup.1-R.sup.10, m, n, p, and are as described herein. The present invention relates generally to FXR modulators and to methods of making and using said compounds.