A61P5/00

PROCESS FOR THE PRODUCTION OF CONDENSED IMIDAZOLO DERIVATIVES
20180002292 · 2018-01-04 ·

The present invention relates to a process for providing the compound of formula I, comprising the step of reacting a compound of formula VII with a base in the presence of an alkaline- or alkaline earth metal salt (MX), wherein LG is a leaving group. The presence of an alkaline- or alkaline earth metal salt was surprisingly found to render said reaction highly reliable in terms of the yield and purity of the compound of formula I obtained. In a further aspect, the present invention relates to the compound of formula I, having less than an amount of 1.50% or less than an amount of 1.25% or less than an amount of 1.00% or less than an amount of 0.75% or less than an amount of 0.50% or less than an amount of 0.25% or less than an amount of 0.10% of the compound of formula VIII.

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POLYMERIC DRUG CONJUGATES WITH TETHER GROUPS FOR CONTROLLED DRUG DELIVERY

Described herein is a cyclodextrin containing polymer conjugate.

GHRELIN ANALOGUES
20180009849 · 2018-01-11 ·

The present invention relates, inter alia, to ghrelin analogues and their medical use, for example in the treatment of cachexia, chronic obstructive pulmonary disease, gastrointestinal disorders (e.g., gastroparesis and/or inflammatory disorders such as colitis, gut barrier dysfunction, and ischemia reperfusion injury), loss of body weight, and decreased appetite.

COMPOSITIONS COMPRISING 15-HEPE AND METHODS OF USING THE SAME
20180008567 · 2018-01-11 ·

The present disclosure relates to the compositions, formulations and methods of treating or preventing diseases mediated by peroxisome proliferator-activated receptors (PPARs) by administration of 15-HEPE.

GLUCAGON-RECEPTOR SELECTIVE POLYPEPTIDES AND METHODS OF USE THEREOF

This invention relates to isolated polypeptides that are glucagon-receptor selective analogs and peptide derivatives thereof. These analogs are selective for human glucagon receptor with improved solubility, thermal stability, and physicochemical properties as compared to native endogenous glucagon. This invention also relates to methods of using such polypeptides in a variety of therapeutic and diagnostic indications, as well as methods of producing such polypeptides. These analogs are useful, alone or in combination with other therapeutic peptides, in methods of treating obesity, diabetes, metabolic disorders, and other disorders or disease.

Benzothia(di)azepine compounds and their use as bile acid modulators

The invention relates to 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives of formula (1). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.

LASOFOXIFENE TREATMENT OF BREAST CANCER

The disclosure provides methods for treating estrogen receptor positive (ER.sup.+) cancer in women with an effective amount of lasofoxifene, a pharmaceutically acceptable salt thereof, or a prodrug thereof. The disclosure also includes the detection of the Estrogen Receptor 1 (ESR1) gene mutations that lead to endocrine resistance and treatment of endocrine resistant ER.sup.+ cancers.

LASOFOXIFENE TREATMENT OF BREAST CANCER

The disclosure provides methods for treating estrogen receptor positive (ER.sup.+) cancer in women with an effective amount of lasofoxifene, a pharmaceutically acceptable salt thereof, or a prodrug thereof. The disclosure also includes the detection of the Estrogen Receptor 1 (ESR1) gene mutations that lead to endocrine resistance and treatment of endocrine resistant ER.sup.+ cancers.

SYNTHETIC METHODS FOR PREPARATION OF 4-(2-CHLORO-4-METHOXY-5-METHYLPHENYL)-N-[(1S)-2-CYCLOPROPYL-1-(3-FLUORO-4-METHYLPHENYL)ETHYL]-5-METHYL-N-PROP-2-YNYL-1,3-THIAZOL-2-AMINE

The present disclosure relates to the fields of chemistry and medicine, more particularly to processes for making 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-prop-2-ynyl-1,3-thi-azol-2-amine (Compound 1), pharmaceutically acceptable salts, and crystalline forms thereof, for the treatment of congenital adrenal hyperplasia (CAH).

Use of 2-pentanone and specific receptor thereof in manufacture of products regulating cell functions

Use of 2-pentanone and specific receptor thereof in a manufacture of a product regulating a cell function, a regulation of cell function, a manufacture of a product promoting an increase in an intracellular calcium ion concentration, or a manufacture of a product promoting an increase in a neuronal firing rate is provided. In the present disclosure, the specific receptor of 2-pentanone is expressed in cultured cells or animals, and its specific binding to 2-pentanone opens ligand-gated cation channels, resulting in an increase of intracellular calcium ion concentration, depolarization of cell membranes, and generation of electrical activity or endocrine activity, thereby finally achieving precise regulation of tissue cells and organ functions. After being treated, cells can be activated rapidly, producing effects with a rapid onset; once the treatment is stopped, the experimental effect can be quickly terminated to allow the cells to return to their original state quickly.