A61P5/44

Therapeutic Uses of Relacorilant, a Heteroaryl-ketone Fused Azadecalin Glucocorticoid Receptor Modulator
20200268723 · 2020-08-27 ·

Methods and compositions are disclosed for diagnosing a patient suspected of suffering from, and for treating a patient suffering from, a disorder such as hypercortisolemia, metabolic syndrome, pre-diabetes, diabetes, Cushing's syndrome, Cushing's Disease, hyperglycemia secondary to hypercortisolemia, a liver disease, a cardiac disorder, high blood pressure, a blood clotting disorder, a cancer, a psychological disorder, weight gain, a disorder of glucose control, a bone disorder (e.g., osteoporosis), hypogonadism, pseudoacromegaly, pituitary tumors, functional hypercortisolism, ACTH secreting tumors, peripheral neuropathy, dyslipidemia and other disorders.

The methods and compositions include administration of a heteroaryl-ketone fused azadecalin glucocorticoid receptor modulator (GRM). The preferred heteroaryl-ketone fused azadecalin GRM is relacorilant ((R)-(1-(4-fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone). In some cases, the GRM (e.g., relacorilant) is orally administered. In some cases, the GRM (e.g., relacorilant) is orally administered without food.

Therapeutic Uses of Relacorilant, a Heteroaryl-ketone Fused Azadecalin Glucocorticoid Receptor Modulator
20200268723 · 2020-08-27 ·

Methods and compositions are disclosed for diagnosing a patient suspected of suffering from, and for treating a patient suffering from, a disorder such as hypercortisolemia, metabolic syndrome, pre-diabetes, diabetes, Cushing's syndrome, Cushing's Disease, hyperglycemia secondary to hypercortisolemia, a liver disease, a cardiac disorder, high blood pressure, a blood clotting disorder, a cancer, a psychological disorder, weight gain, a disorder of glucose control, a bone disorder (e.g., osteoporosis), hypogonadism, pseudoacromegaly, pituitary tumors, functional hypercortisolism, ACTH secreting tumors, peripheral neuropathy, dyslipidemia and other disorders.

The methods and compositions include administration of a heteroaryl-ketone fused azadecalin glucocorticoid receptor modulator (GRM). The preferred heteroaryl-ketone fused azadecalin GRM is relacorilant ((R)-(1-(4-fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone). In some cases, the GRM (e.g., relacorilant) is orally administered. In some cases, the GRM (e.g., relacorilant) is orally administered without food.

BIOLOGICAL MATERIALS AND THERAPEUTIC USES THEREOF
20200255825 · 2020-08-13 ·

There is provided agents for modulation of a chronic inflammatory response wherein the agent modulates the biological activity of citrullinated tenascin-C. There is also provided methods of identifying agents modulating citrullinated tenascin-C and chronic inflammation. There are also provided therapeutic uses of such agents.

COMPOUNDS HAVING ANTI-INFLAMMATORY AND ANTI-OXIDANT ACTIVITY
20200199170 · 2020-06-25 ·

The present invention relates to new compounds of formula (1) wherein R is C(O)CH.sub.2OH or CH(OH)CH.sub.2OH; R.sub.1, is O or OH; R.sub.2 is H or OH; R.sub.3 is H or C.sub.1-C.sub.4alkyl; R.sub.4 is H or C.sub.1C.sub.4alkyl. These compounds are obtained by a process using at least one bacterium belonging to the Actinobacteria class, preferably belonging to the Rhodococcus genus. Thanks to their antiinflammatory and anti-oxidant properties, the compounds of the invention can be advantageously used in the treatment of inflammatory diseases, autoimmune diseases and of diseases in need of a joined anti-inflammatory and anti-oxidant activity.

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Diamide Compounds Having Muscarinic Receptor Antagonist and Beta2 Adrenergic Receptor Agonist Activity

The invention relates to a pharmaceutical composition comprising an isotonic aqueous solution comprising a compound of formula I:

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or a pharmaceutically acceptable salt thereof.

Inhalable formulation

This invention provides a process for preparing an inhalable active pharmaceutical ingredient comprising the steps of heating a suspension of an active pharmaceutical ingredient in a liquefied propellant in a vessel, evaporating the propellant and collecting the resultant powder.

Treatment of allergic rhinitis using a combination of mometasone and olopatadine

The present patent application relates to a method of treating allergic rhinitis in a subject (preferably a human) by administering a combination of mometasone or its salt and olopatadine or its salt.

Corticosteroids for the treatment of joint pain

Corticosteroid microparticle formulations are provided for use for treating pain, including pain caused by inflammatory diseases such as osteoarthritis or rheumatoid arthritis, and for slowing, arresting or reversing structural damage to tissues caused by an inflammatory disease, for example damage to articular and/or peri-articular tissues caused by osteoarthritis or rheumatoid arthritis. Corticosteroid microparticle formulations are administered locally as a sustained release dosage form (with or without an immediate release component) that results in efficacy accompanied by clinically insignificant or no measurable effect on endogenous cortisol production.

METHODS FOR OVERCOMING GLUCOCORTICOID RESISTANCE AND FOR DETERMINING GLUCOCORTICOID RESISTANCE POTENTIAL IN CANCER

The invention provides methods for overcoming glucocorticoid resistance of cancers by inhibition of CASP1. Also disclosed are diagnostic methods for determining glucocorticoid resistance potential by measuring expression level or promoter methylation status of CASP1 gene and/or NLRP3 gene.

Diamide compounds having muscarinic receptor antagonist and Beta2 adrenergic receptor agonist activity

The invention relates to a pharmaceutical composition comprising an isotonic aqueous solution comprising a compound of formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof.