A61P3/10

POLYMORPHIC AND AMORPHOUS FORMS OF (R)-2-HYDROXY-2-METHYL-4-(2,4,5-TRIMETHYL-3,6-DIOXOCYCLOHEXA-1,4-DIENYL)BUTANAMIDE

Disclosed herein are polymorphic and amorphous forms of anhydrate, hydrate, and solvates of (R)-2-hydroxy-2-methyl-4-(2,4,5-trimethyl-3,6-dioxocyclohexa-1,4-dienyl)butanamide and methods of using such compositions for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging. Further disclosed are methods of making such polymorphic and amorphous forms.

New Azabenzimidazole Derivatives
20180002349 · 2018-01-04 ·

The present invention relates to compounds of general formula (I), wherein R.sup.1, R.sup.2, R.sup.3, A.sup.1, A.sup.2, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the AMP-activated protein kinase (AMPK) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.

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Methyoxy-Substituted Pyrrolopyridine Modulators of RORC2 and Methods of Use Thereof

The present invention provides methoxy-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.

Tetrazolones as a Carboxylic Acid Bioisosteres
20180002297 · 2018-01-04 ·

The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.

BICYCLIC COMPOUND

Provided is a bicyclic compound having an acetyl-CoA carboxylase inhibitory action. A compound represented by the formula:

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wherein each symbol is as described in the DESCRIPTION, or a salt thereof has an acetyl-CoA carboxylase inhibitory action, is useful for the prophylaxis or treatment of cancer, inflammatory diseases and the like, and has superior efficacy.

TRICYCLIC SULFONES AS ROR GAMMA MODULATORS

There are described RORγ modulators of the formula (I),

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and formula (II)

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or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

SYNTHESIS OF HETEROCYCLIC COMPOUNDS
20180002332 · 2018-01-04 ·

Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I):

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or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P.sup.1 and P.sup.2 are as defined in this disclosure.

MIXTURE OF CARBOXYLIC ACIDS FOR TREATING PATIENTS WITH KIDNEY FAILURE

Our invention is a mixture of carboxylic acids: citric acid, succinic acid, fumaric acid and malic acid, and any possible combinations thereof. This product is used orally or also intravenously, in the treatment of patients with chronic renal failure, hyperammonemia or human conditions having negative nitrogen balance. This product is beneficial in decreasing the serum values of urea and serum ammonium, while promoting by transamination of the oxalacetate formed via succinate, fumarate and malate, the biosynthesis of non-essential amino acids; by transamination of the alpha ketoglutarate formed via citrate, it generates glutamic acid and related amino acids such as glutamine. This treatment prevents, preserves and even improves kidney function. In other patients it delays deterioration of renal function and the urgent need for renal replacement therapy. In others, it is used as a supplemental renal replacement treatment to improve the patient's quality of life and improve laboratory parameters.

METHODS AND AGENTS FOR TREATING DISEASE

The present invention provides compounds having the general structural formula (I) [formula should be inserted here] and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving elevated levels of aldosterone or abnormal or excessive fibrosis, such as kidney disease and hypertension.

HETEROCYCLIC INHIBITORS OF MONOCARBOXYLATE TRANSPORTERS

The invention provides compounds that inhibit monocarboxylate transporters, such as MCT1 and MCT4. Compounds of the invention can be used for treatment of a condition in a patient, wherein the condition is characterized by the heightened activity or by the high prevalence of MCT1 and/or MCT4, such as cancer or type II diabetes.