Patent classifications
C07J31/003
SELECTIVE PROGESTERONE RECEPTOR MODULATORS (SPRM) AND STABILIZED ESTROGEN LEVEL IN PATIENT
The present invention is related to Selective Progesterone Receptor Modulators (SPRM) as described and defined herein, and covers the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of sexual hormone dependent diseases and gynaecological diseases in particular Endometriosis or Uterine Fibroids (UF), as a sole agent or in combination with other active ingredients wherein circulating endogenous estradiol concentration of treated women is maintained to a level in a range of 40 pg/mL to 85 pg/mL.
NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF
Compounds are provided according to Formula (I):
##STR00001##
and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v):
##STR00002##
and wherein L.sup.1, L.sup.2, L.sup.3, X.sup.1, X.sup.2, Y, R.sup.Z4, R.sup.Z5, R.sup.Z6, n, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.14, R.sup.17, R.sup.19, R.sup.20, R.sup.23a, R.sup.23b, and R.sup.24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.
NEUROACTIVE STEROIDS AND COMPOSITIONS THEREOF
Provided herein is a compound of Formula (I):
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sup.1a, R.sup.1b, R.sup.2a, R.sup.2b, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7a, R.sup.11a, R.sup.11b, R.sup.12a, R.sup.12b, R.sup.16a, R.sup.16b, R.sup.19, R.sup.11a, R.sup.22, R.sup.X, R.sup.Y and n are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.
Androstane and pregnane steroids with potent allosteric gaba receptor chloride ionophore modulating properties
This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage. ##STR00001##
Neuroactive steroids, compositions, and uses thereof
Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v), and wherein L.sup.1, L.sup.2, L.sup.3, X.sup.1, X.sup.2, Y, R.sup.z4, R.sup.z5, R.sup.z6, n, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.14, R.sup.17, R.sup.19, R.sup.20, R.sup.23a, R.sup.23b, and R.sup.24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals. ##STR00001##
NOVEL CHOLESTEROL METABOLITE, 5-CHOLESTEN, 3BETA-25-DIOL, DISULFATE (25HCDS) FOR THERAPY OF METABOLIC DISORDERS, HYPERLIPIDEMIA, DIABETES, FATTY LIVERS DISEASES AND ATHEROSCLEROSIS
5-cholesten, 3,25-diol, disulfate (25HCDS) has been found to be an authentic PPAR agonist and LXR antagonist, and is used for the therapy of lipid disorders and inflammatory diseases, including without limitation fatty liver, inflammatory bowel, and atherosclerotic diseases.
ANDROSTANE AND PREGNANE STEROIDS WITH POTENT ALLOSTERIC GABA RECEPTOR CHLORIDE IONOPHORE MODULATING PROPERTIES
This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage.
##STR00001##
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.
NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF
Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v), and wherein L.sup.1, L.sup.2, L.sup.3, X.sup.1, X.sup.2, Y, R.sup.z4, R.sup.z5, R.sup.z6, n, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.14, R.sup.17, R.sup.19, R.sup.20, R.sup.23a, R.sup.23b, and R.sup.24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.
##STR00001##
NEUROACTIVE STEROIDS AND COMPOSITIONS THEREOF
Provided herein is a compound of Formula (I):
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sup.1a, R.sup.1b, R.sup.2a, R.sup.2b, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6a, R.sup.16b, R.sup.7a, R.sup.7a, R.sup.11a, R.sup.11b, R.sup.12a, R.sup.12b, R.sup.16a, R.sup.16b, R.sup.19, R.sup.11a, R.sup.22, R.sup.X, R.sup.Y and n are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.