A61K31/4422

Deuterated pharmaceutical compositions and methods of treating cardiovascular diseases

Provided herein is a pharmaceutical composition comprising (i) a phosphodiesterase inhibitor or an adenosine receptor antagonist, (ii) a calcium channel blocker, (iii) a histamine H.sub.1-receptor agonist, a histamine H.sub.2-receptor agonist, or a histamine H.sub.3-receptor antagonist, and (iv) a β.sub.2-adrenoreceptor agonist; wherein at least one of two or more active pharmaceutical compounds is deuterium enriched. Also provided herein is a pharmaceutical composition comprising at least one of two or more deuterated compounds which increase pharmacokinetic half-life (increasing the duration of action) and reduce side effects by allowing for reduction of the dose levels. A method of use thereof pharmaceutical composition for treating, preventing, or ameliorating a cardiovascular disease.

Deuterated pharmaceutical compositions and methods of treating cardiovascular diseases

Provided herein is a pharmaceutical composition comprising (i) a phosphodiesterase inhibitor or an adenosine receptor antagonist, (ii) a calcium channel blocker, (iii) a histamine H.sub.1-receptor agonist, a histamine H.sub.2-receptor agonist, or a histamine H.sub.3-receptor antagonist, and (iv) a β.sub.2-adrenoreceptor agonist; wherein at least one of two or more active pharmaceutical compounds is deuterium enriched. Also provided herein is a pharmaceutical composition comprising at least one of two or more deuterated compounds which increase pharmacokinetic half-life (increasing the duration of action) and reduce side effects by allowing for reduction of the dose levels. A method of use thereof pharmaceutical composition for treating, preventing, or ameliorating a cardiovascular disease.

NON-AQUEOUS SUSTAINED RELEASE DRUG DELIVERY SYSTEM
20230054250 · 2023-02-23 ·

A non-aqueous sustained release drug delivery system, which contains, based on the total weight of the sustained release drug delivery system, about 0.1-20% of an active agent, about 0.5-50% of a drug solvent, about 1-98% of a drug sustained release agent, about 0.1-85% of a drug solubilizer, about 0.1-10% of an efficacy enhancer, about 0-1% of an antioxidant, and about 0-8% of an acid-base regulator. The non-aqueous sustained release drug delivery system can yield an improved sustained release effect, improve bioavailability, and enhance the therapeutic effect.

NON-AQUEOUS SUSTAINED RELEASE DRUG DELIVERY SYSTEM
20230054250 · 2023-02-23 ·

A non-aqueous sustained release drug delivery system, which contains, based on the total weight of the sustained release drug delivery system, about 0.1-20% of an active agent, about 0.5-50% of a drug solvent, about 1-98% of a drug sustained release agent, about 0.1-85% of a drug solubilizer, about 0.1-10% of an efficacy enhancer, about 0-1% of an antioxidant, and about 0-8% of an acid-base regulator. The non-aqueous sustained release drug delivery system can yield an improved sustained release effect, improve bioavailability, and enhance the therapeutic effect.

Novel Ferroportin Inhibitors

The invention relates to novel compounds of the general formula (I),

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with Het-2 being an optionally substituted bicyclic heteroaryl of the formula

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pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for the use as ferroportin inhibitors, more particularly for the use in the prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, such as particularly iron overload states such as in particular thalassemia and hemochromatosis.

LIQUID NIMODIPINE COMPOSITIONS
20230053961 · 2023-02-23 ·

Liquid compositions comprising nimodipine having improved nimodipine concentrations are provided herein. Methods of improving neurological outcome by reducing the incidence and severity of ischemic deficits in patients with subarachnoid hemorrhage from ruptured intracranial berry aneurysms with the liquid compositions of the present invention are also detailed herein.

LIQUID NIMODIPINE COMPOSITIONS
20230053961 · 2023-02-23 ·

Liquid compositions comprising nimodipine having improved nimodipine concentrations are provided herein. Methods of improving neurological outcome by reducing the incidence and severity of ischemic deficits in patients with subarachnoid hemorrhage from ruptured intracranial berry aneurysms with the liquid compositions of the present invention are also detailed herein.

PHARMACOLOGICAL COMPOSITION FOR TREATING PROCTOLOGICAL DISEASES (VARIANTS)
20220362247 · 2022-11-17 ·

This invention relates to medicine and more particularly to pharmacological compositions for treating proctologic diseases. The pharmacological composition comprises 3.3-7.5 wt % methyluracil, 0.13-0.3 wt % nifedipine, 1.3-5 wt % lidocaine, a pharmacologically acceptable carrier—rest. The pharmacological composition could be in the form of gel, or ointment, or cream, or suppositories, or suspended gel, or lotion, or emulsion.

PHARMACOLOGICAL COMPOSITION FOR TREATING PROCTOLOGICAL DISEASES (VARIANTS)
20220362247 · 2022-11-17 ·

This invention relates to medicine and more particularly to pharmacological compositions for treating proctologic diseases. The pharmacological composition comprises 3.3-7.5 wt % methyluracil, 0.13-0.3 wt % nifedipine, 1.3-5 wt % lidocaine, a pharmacologically acceptable carrier—rest. The pharmacological composition could be in the form of gel, or ointment, or cream, or suppositories, or suspended gel, or lotion, or emulsion.

PHARMACOLOGICAL COMPOSITION FOR TREATING PROCTOLOGICAL DISEASES (VARIANTS)
20220362247 · 2022-11-17 ·

This invention relates to medicine and more particularly to pharmacological compositions for treating proctologic diseases. The pharmacological composition comprises 3.3-7.5 wt % methyluracil, 0.13-0.3 wt % nifedipine, 1.3-5 wt % lidocaine, a pharmacologically acceptable carrier—rest. The pharmacological composition could be in the form of gel, or ointment, or cream, or suppositories, or suspended gel, or lotion, or emulsion.