13 results about "Phosphodiesterase-4" patented technology

This invention belongs to the field of medicinal chemistry, specifically relating to benzofuran compounds or their pharmaceutically acceptable salts, their preparation methods, and applications. The benzofuran compounds of this invention can significantly inhibit the activity of phosphodiesterase 4 and can be used to prepare drugs for treating inflammatory diseases, autoimmune diseases, or neuropsychiatric disorders, especially for stroke and ischemic dementia-related diseases.

The invention discloses an application of a novel phosphodiesterase 4 (PDE4) inhibitor ZL-n-91 in preparation of drugs for treating growth and metastasis of small cell lung cancer. In-vitro cytology experiments and in-vivo zoology experiments show that the phosphodiesterase 4 inhibitor ZL-n-91 can significantly inhibit proliferation and metastasis of small cell lung cancer, and the phosphodiesterase 4 inhibitor ZL-n-91 is expected to treat small cell lung cancer and has good development and application prospects.

The invention discloses an application of a novel phosphodiesterase 4 (PDE4) inhibitor ZL-n-91 in preparation of medicines for treating growth and metastasis of oral cancer. In-vitro cytology experiments and in-vivo zoology experiments show that the phosphodiesterase 4 inhibitor ZL-n-91 can significantly inhibit proliferation and migration of the oral cancer, reveals that the phosphodiesterase 4 inhibitor ZL-n-91 is expected to treat the oral cancer, and has good development and application prospects.

The invention belongs to the technical field of biological medicines, and particularly relates to a xanthone-based compound as well as a preparation method and application thereof. The invention provides a xanthone-based compound with a novel structure, experiments prove that the xanthone-based compound has an excellent inhibition effect on phosphodiesterase 4, the compound reaches the activity level of a nanomole level, the activity of part of the compound is even remarkably superior to that of a positive control Rolipram, and the xanthone-based compound can be used as a phosphodiesterase 4 inhibitor and can be used for preparing a phosphodiesterase 4 inhibitor. The compound is applied to treatment of phosphodiesterase 4 type related diseases, and has important medicinal value and wide application prospect in preparation of drugs for treating phosphodiesterase 4 type related diseases including pulmonary fibrosis.

The present invention provides a oxazole compound represented by Formula (1), or a salt thereof:wherein R1 is an aryl group which may have one or more substituents; R2 is an aryl group or a nitrogen atom-containing heterocyclic group each of which may have one or more substituents; and W is a divalent group represented by —Y1-A1- or —Y2—C(═O)— wherein Y1 is a group such as —C(═O)—, A1 is a group such as a lower alkylene group, and Y2 is a group such as a piperazinediyl group. The oxazole compound has a specific inhibitory action against phosphodiesterase 4.

This invention relates to a phosphodiesterase 4 (PDE4) inhibitor composition, belonging to the field of pharmaceutical formulations. The composition comprises a PDE4 inhibitor, a suspending agent, and other pharmaceutically acceptable excipients. The PDE4 inhibitor composition prepared by this invention has advantages such as good taste, convenient administration, high patient acceptance, and greater flexibility in clinical application.

The invention relates to a medicament and a method for treating or preventing vascular diseases. Specifically, the invention relates to a method for treating or preventing vascular endothelial dysfunction related diseases by down-regulating phosphodiesterase 4, and application of a phosphodiesterase 4 inhibitor in preparation of drugs for treating or preventing vascular endothelial dysfunction related diseases.

The low aqueous solubility of roflumilast in parenteral preparations and topical emulsions, suspensions, gels or solutions can be improved by including a blend of water-miscible solvents in the pharmaceutical composition. The blend of water-miscible solvents can include diethylene glycol monoethyl ether (Tradename Transcutol®); abbreviated DEGEE) and water. The ratio of diethylene glycol monoethyl ether to water is from 1:10 to 20:1. The resulting composition has improved bioavailability and efficacy and can be used to inhibit phosphodiesterase 4 in a patient in need of such treatment.

Roflumilast crystals have been shown to increase in size during storage. The size of the roflumilast crystals can affect the bioavailability and efficacy of a pharmaceutical composition. The growth of roflumilast crystals can be inhibited during storage by including hexylene glycol in the composition. The resulting composition has improved bioavailability and efficacy and can be used to inhibit phosphodiesterase 4 in patient in need of such treatment.

Disclosed are indolone compounds having phosphodiesterase 4 inhibitory activity, the compounds being represented by Formula I, which can be used as phosphodiesterase 4 inhibitors in therapeutic or prophylactic drugs for Behcet's disease, atopic dermatitis, psoriasis, inflammatory bowel disease, chronic obstructive pulmonary disease, pulmonary fibrosis, and other inflammatory diseases.

Disclosed are methods for treating Jordan's syndrome in a subject in need thereof and methods of reducing at least one sign or symptom of Jordan's syndrome in a subject in need thereof. The methods comprise administering a therapeutically effective amount of a phosphodiesterase 4 (PDE4) inhibitor to the subject. The PDE4 inhibitor may be BPN14770 and may be administered daily.

Provided herein are phosphodiesterase 4 (PDE4) inhibitors, e.g., a compound of Formula (I) or (II), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a disease, disorder, or condition associated with PDE4 malfunction.