C07J31/00

Pharmaceutical composition for prevention, treatment or delay of Alzheimer's disease or dementia containing G protein-coupled receptor 19 agent as active ingredient

The present invention relates to a pharmaceutical composition for preventing, treating or delaying an Alzheimer's disease (AD) or dementia including a G protein-coupled receptor19 (GPCR19) agonist or its pharmaceutically acceptable salt as an active ingredient and a food composition for preventing, treating or delaying an Alzheimer's disease or dementia. The GPCR19 agonist according to the present invention has an effect of improving cognitive and behavioral disorders without harming the health of objects when administrated to the objects and has an effect of preventing the Alzheimer's disease or dementia or delaying or treating the progression of the disease in the objects with the disease by suppressing apoptosis of the brain tissue, enhancing immunity, and reducing formation of an amyloid (A) plague.

Method for fully automated synthesis of 16β-18F-fluoro-5α-dihydrotestosterone (18F-FDHT)

The automated synthesis of clinically relevant amounts of 16-.sup.18F-fluoro-5-dihydrotestosterone (.sup.18F-FDHT) using a commercially available radiosynthesizer. Synthesis was performed in 90 minutes with a decay-corrected radiochemical yield of 295%. The specific activity was 4.6 Ci/mol (170 GBq/mol) at end of formulation with a starting activity of 1.0 Ci (37 GBq). The formulated .sup.18F-FDHT yielded sufficient activity for multiple patient doses and passed all quality control tests required for routine clinical use.

Cytotoxic agents that preferentially target leukemia inhibitory factor (LIF) for the treatment of malignancies and as new contraceptive agents
10053485 · 2018-08-21 · ·

Described herein are new anti-cancer compounds and methods of using such compounds, acting through a new mechanism of action by simultaneous inhibition of leukemia inhibitory factor (LIF) and MDM2.

METHODS FOR PREPARATION OF BILE ACIDS AND DERIVATIVES THEREOF
20180222937 · 2018-08-09 ·

The present application relates to a method of preparing compounds of Formula (A) or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof.

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OXYSTEROLS AND METHODS OF USE THEREOF

Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.8 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

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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##

Sulfated oligosaccharide derivatives

The invention relates to novel compounds that have utility as inhibitors of heparan sulfate-binding proteins; compositions comprising the compounds, and use of the compounds and compositions thereof for the antiangiogenic, antimetastatic, anti-inflammatory, antimicrobial, anticoagulant and/or antithrombotic treatment of a mammalian subject.

SELECTIVE PROGESTERONE RECEPTOR MODULATOR (SPRM) REGIMEN
20180155388 · 2018-06-07 ·

The invention is directed to a pharmaceutical composition comprising a progesterone receptor antagonist namely (11,17)-17-Hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethy)estra-4,9-dien-3-one for the treatment and/or prophylaxis of Uterine Fibroids (myomas, uterine leiomyoma) that is administered to a patient diagnosed with Uterine Fibroids following a specific regimen. Additionally, the invention is directed to a method for treating Uterine Fibroids (myomas, uterine leiomyoma) and/or for reducing Uterine Fibroids (myomas, uterine leiomyoma) size and symptoms related to Uterine Fibroids following a specific regimen as well as treatment of Heavy Menstrual Bleeding (HMB).

CHOLIC ACID DERIVATIVE, AND PREPARATION METHOD AND MEDICAL USE THEREOF
20180148470 · 2018-05-31 ·

The present invention relates to a cholic acid derivative, and a preparation method and a medical use thereof. In particular, the present invention relates to a cholic acid derivative of formula (I), a stereoisomer, or a pharmaceutically acceptable salt thereof. The series of compounds can be used to treat FXR mediated diseases, including cardiovascular disease, atherosclerosis, arteriosclerosis, hypercholesterolemia, hyperlipidemia and chronic hepatitis diseases, chronic liver diseases, gastrointestinal diseases, nephrosis, heart vascular diseases, metabolic diseases, cancer (for example colorectal cancer) or neurological diseases, such as strokes and other diseases, with a wide range of medical applications, and are expected to develop into a new generation of FXR agonists.

NOVEL CHOLESTEROL METABOLITE, 5-CHOLESTEN, 3BETA-25-DIOL, DISULFATE (25HCDS) FOR THERAPY OF METABOLIC DISORDERS, HYPERLIPIDEMIA, DIABETES, FATTY LIVERS DISEASES AND ATHEROSCLEROSIS
20180127457 · 2018-05-10 ·

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.