A61K31/425

LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONIST AND PREPARATION METHOD THEREFOR

Certain compounds are lysophosphatidic acid receptor antagonists have high LPAR1 antagonist activity and selectivity, low toxicity, good metabolic stability, promising pharmaceutical development prospects, and may be used for preventing or treating LPAR1-related diseases or illnesses. The IC50 values of some of the compounds may be as low as 300 nM or below, even 50 nM or below. In addition, CC50 value range of the compounds may be as high as 200 μM or above. Furthermore, the compounds have good metabolic stability in humans, mice and rats.

Maslinic and oleanolic acids derivatives for treating SARS-CoV-2 infection

Provided are methods of using oleanolic acid and derivatives for treating coronavirus infection. The method includes using propargyl-moiety containing oleanolic acid derivatives for inhibiting coronavirus growth by impairing the viral replication of SARS-CoV-2 through inhibition of the viral function of SARS-CoV-2 main protease.

Method for increasing cell proliferation in pancreatic beta cells, treatment method, and composition

The present invention relates to a method of increasing cell proliferation in a population of pancreatic beta cells and a method of treating a subject for a condition associated with an insufficient level of insulin secretion. Also disclosed is a composition. The composition includes a dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1 A) inhibitor and a transforming growth factor beta (TGFP) superfamily signaling pathway inhibitor.

Inhibitors of SARM1 NADase activity and uses thereof

The present disclosure provides compounds useful as inhibitors of SARM1 NADase activity, compositions thereof, and methods of using the same. The present disclosure provides compounds useful for treating a neurodegenerative or neurological disease or disorder, compositions thereof, and methods of using the same.

CARBOSTYRIL DERIVATIVES AND MOOD STABILIZERS FOR TREATING MOOD DISORDERS

The pharmaceutical composition of the present invention comprises a carbostyril derivative which is a dopamine-serotonin system stabilizer and a mood stabilizer in a pharmaceutically acceptable carrier. The carbostyril derivative may be aripiprazole or a metabolite thereof. The mood stabilizer may include but is not limited to lithium, valproic acid, divalproex sodium, carbemazapine, oxcarbamazapine, zonisamide, lamotragine, topiramate, gabapentin, levetiracetam or clonazepam. These compositions are used to treat patients with mood disorders, particularly bipolar disorder with or without psychotic features, manta or mixed episodes. Methods are provided for separate administration of a carbostyril derivative and a mood stabilizer to a patient with a mood disorder.

CARBOSTYRIL DERIVATIVES AND MOOD STABILIZERS FOR TREATING MOOD DISORDERS

The pharmaceutical composition of the present invention comprises a carbostyril derivative which is a dopamine-serotonin system stabilizer and a mood stabilizer in a pharmaceutically acceptable carrier. The carbostyril derivative may be aripiprazole or a metabolite thereof. The mood stabilizer may include but is not limited to lithium, valproic acid, divalproex sodium, carbemazapine, oxcarbamazapine, zonisamide, lamotragine, topiramate, gabapentin, levetiracetam or clonazepam. These compositions are used to treat patients with mood disorders, particularly bipolar disorder with or without psychotic features, manta or mixed episodes. Methods are provided for separate administration of a carbostyril derivative and a mood stabilizer to a patient with a mood disorder.

CARBOSTYRIL DERIVATIVES AND MOOD STABILIZERS FOR TREATING MOOD DISORDERS

The pharmaceutical composition of the present invention comprises a carbostyril derivative which is a dopamine-serotonin system stabilizer and a mood stabilizer in a pharmaceutically acceptable carrier. The carbostyril derivative may be aripiprazole or a metabolite thereof. The mood stabilizer may include but is not limited to lithium, valproic acid, divalproex sodium, carbemazapine, oxcarbamazapine, zonisamide, lamotragine, topiramate, gabapentin, levetiracetam or clonazepam. These compositions are used to treat patients with mood disorders, particularly bipolar disorder with or without psychotic features, manta or mixed episodes. Methods are provided for separate administration of a carbostyril derivative and a mood stabilizer to a patient with a mood disorder.

GLUTAMATE AGENTS IN THE TREATMENT OF MENTAL DISORDERS
20210294011 · 2021-09-23 ·

Methods of treating mental disorders, including anxiety disorders such as obsessive-compulsive disorder, are provided. The methods comprise administering an effective amount of a glutamate modulator to an individual in need thereof. Also provided are methods of enhancing the activity of a serotonin reuptake inhibitor (SRI) comprising co-administering a glutamate modulator and a serotonin reuptake inhibitor. Pharmaceutical composition comprising a serotonin reuptake inhibitor and a glutamate modulator are also provided.

GLUTAMATE AGENTS IN THE TREATMENT OF MENTAL DISORDERS
20210294011 · 2021-09-23 ·

Methods of treating mental disorders, including anxiety disorders such as obsessive-compulsive disorder, are provided. The methods comprise administering an effective amount of a glutamate modulator to an individual in need thereof. Also provided are methods of enhancing the activity of a serotonin reuptake inhibitor (SRI) comprising co-administering a glutamate modulator and a serotonin reuptake inhibitor. Pharmaceutical composition comprising a serotonin reuptake inhibitor and a glutamate modulator are also provided.

OCULAR FORMULATIONS FOR DRUG-DELIVERY AND PROTECTION OF THE ANTERIOR SEGMENT OF THE EYE
20210275501 · 2021-09-09 ·

The present application relates to topical formulations comprising Compound-I

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or its free base, and a second active agent selected from nicotinic acid, nicotinamide, and vitamin K, and a combination thereof, for treating ocular neovascularization. The present application also relates to pharmaceutical compositions comprising particles of Compound-I or its free base, and suspension formulations comprising the particle compositions of Compound-I or its free base.