57 results about "PDE4B" patented technology

The compound shown in formula I, its stereoisomers or pharmaceutically acceptable salts, or a pharmaceutical composition containing them, and their use in the manufacture of a therapeutic agent for treating related diseases as a PDE4B inhibitor, wherein each group shown in formula (I) is as defined in the specification. [Chemical formula 1] TIFF2025518257000169.tif37156

The present disclosure provides a compound of formula H having excellent PDE4B inhibitory activity, and a pharmaceutical composition thereof and a use thereof. The compound provided by the present disclosure can be used for effectively treating PDE4-related diseases and disorders, including but not limited to inflammatory respiratory diseases, inflammatory bowel diseases, inflammatory joint diseases, inflammatory skin diseases, inflammatory eye diseases, and diseases or cancers of the peripheral or central nervous system.

The present disclosure provides a compound of formula H having excellent PDE4B inhibitory activity, and a pharmaceutical composition and use thereof. The compounds provided by the present disclosure are useful for the effective treatment of PDE4-related diseases and disorders, including but not limited to respiratory tract inflammatory diseases, inflammatory bowel diseases, arthritis diseases, skin inflammatory diseases, eye inflammatory diseases, and diseases or cancers of the peripheral or central nervous system. # imgabs0 #

The invention discloses a PDE4B-targeted siRNA liposome nano-drug as well as a preparation method and application thereof, and belongs to the technical field of biological medicines and nano-drugs. The preparation method comprises the following steps: dissolving cholesterol, DLin-MC3-DMA, DOPE and DSPE-PEG2000 in absolute ethyl alcohol to serve as an ethyl alcohol phase; dissolving siPDE4B into a sodium citrate buffer solution to serve as a water phase; then, rapidly mixing the ethanol phase and the water phase through a microfluidic device; and carrying out PBS dialysis on the obtained mixture to promote liposome assembly and remove ethanol so as to obtain the PDE4B-targeted siRNA liposome nano-drug. Compared with the prior art, the preparation process is simple, large-scale preparation can be achieved, and the prepared nano-drug has an excellent anti-pulmonary fibrosis effect, is low in toxicity, can be administrated in an inhalable mode and can effectively restrain IPF.

Provided are an oral pharmaceutical composition containing a PDE4B inhibitor compound as shown in formula (I) and a preparation method therefor. The composition contains the compound of formula (I), a filler, an adhesive, a disintegrant, a solubilizer, and a lubricant. The composition can be prepared into oral preparation forms such as a tablet, a capsule, a granule, and a dispersible tablet, and has the advantages of a high bioavailability, good content uniformity, good stability, easy industrialization, etc.

Disclosed are a compound as represented by formula I; a stereoisomer or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing same; and the use thereof as a PDE4B inhibitor in the preparation of a drug for the treatment of related diseases. Each group as shown in formula (I) is as defined in the description.

The present invention belongs to the field of medicine. Specifically, the present invention relates to a deuterated heterocyclic compound acting as a PDE4B inhibitor and the use thereof. Specifically, the present invention relates to a compound as shown in formula I, or a tautomer, a stereoisomer, a hydrate, a solvate, a pharmaceutically acceptable salt or a prodrug thereof.

The invention concerns an oral pharmaceutical composition consisting essentially of • the PDE4B-inhibitor of formula III in the dose of 18 mg or 9 mg and • optionally of one or more pharmaceutically acceptable carriers or excipients for use in the treatment of a patient suffering from one or more progressive fibrosing interstitial lung diseases (PF-ILD), wherein this oral pharmaceutical composition is to be administered to the patient twice daily. The invention further concerns oral pharmaceutical compositions comprising the PDE4B-inhibitor of formula III in the dose of 18 mg or 9 mg and a therapeutically effective dose of a second active ingredient selected from nintedanib or pirfenidone, wherein these oral pharmaceutical compositions are administered to the patient twice daily.

The present application relates to a compound of formula X having PDE4B inhibitory activity, a pharmaceutical composition thereof, and a use. The compound of formula X may be used for PDE4-related diseases and conditions, such as respiratory inflammatory diseases, inflammatory bowel diseases, arthritis, skin inflammatory diseases, eye inflammatory diseases, and peripheral or central nervous system diseases or cancers.

The invention is directed to an improved method of manufacturing the PDE4B-inhibitor of formula XX

The invention relates to a preparation method and application of a dihydrothienopyrimidine derivative. The invention provides a compound which is used as a PDE4B inhibitor and has a brand-new structure, a preparation method of the compound and application of the compound in the aspect of treating PDE4B-mediated diseases. Experiments prove that the compounds have a relatively strong inhibition effect on PDE4B enzyme, and can be used as promising compounds for treating PDE4B-mediated diseases.

The invention belongs to the technical field of bioinformatics, and discloses a PTC risk hierarchical evaluation model and application. According to the model disclosed by the invention, the expression level of a biomarker is taken as an input variable, and the biomarker comprises BDKRB1, CXCL9, GP1BA, GPR132, ITGA5, KCNMB2, LPAR1, MEFV, MEP1A, MXD1, OPRK1, PDE4B, PROK2, RTP4, SERPINE1 and TNFSF15. According to the model disclosed by the invention, gene expression is combined with tumor immune microenvironment and drug sensitivity by integrating gene expression data, a statistical model and clinical verification, so that multi-dimensional risk assessment is realized, accurate assessment of prognosis risk of papillary thyroid carcinoma patients is realized, and a basis is provided for clinical individualized treatment.

The invention concerns an oral pharmaceutical composition comprisingeither 18 mg or 9 mg of the PDE4B-inhibitor of formula IIIa therapeutically effective dose of a second active agent selected from the group consisting of nintedanib or pirfenidone andoptionally, one or more pharmaceutically acceptable carriers or excipients for the treatment of a patient suffering from a progressive fibrosing interstitial lung disease (PF-ILD), wherein this oral pharmaceutical composition is to be administered to said patient twice daily.The invention further concerns the use of the PDE4B-inhibitor of formula III for preparing an oral pharmaceutical composition comprising either 18 mg or 9 mg of the PDE4B-inhibitor of formula III for use in a method of treating a patient suffering from one or more Progressive Fibrosing Interstitial Lung Diseases (PF-ILDs), wherein said oral pharmaceutical composition is to be orally administered twice daily to said patient in combination with a therapeutically effective amount of a therapeutically effective dose of a second active agent selected from the group consisting of nintdanib and pirfenidone.

The invention belongs to the field of medicines, and particularly relates to a deuterated heterocyclic compound serving as a PDE4B inhibitor and application of the deuterated heterocyclic compound. The invention specifically relates to a compound as shown in a formula I, or a tautomer, a stereoisomer, a hydrate, a solvate, a pharmaceutically acceptable salt or a prodrug thereof. The compound has a relatively good PDE4B inhibition effect. # imgabs0 #

The present invention belongs to the field of medicine. Specifically, the present invention relates to a deuterated heterocyclic compound acting as a PDE4B inhibitor and the use thereof. Specifically, the present invention relates to a compound as shown in formula I, or a tautomer, a stereoisomer, a hydrate, a solvate, a pharmaceutically acceptable salt or a prodrug thereof.

The invention discloses a marker and a probe composition for early diagnosis of high-grade cervical lesions and cervical cancer and application of the marker and the probe composition. The marker is a PDE4B gene. According to the present invention, with the application of the marker, the methylation state of the gene can be sensitively and specifically detected so as to be used for the detection of the cervical exfoliated cell DNA, and the composition is used for the screening of the asymptomatic population in the non-invasive manner so as to reduce the harm caused by the invasive detection; the composition has higher sensitivity and accuracy, and can realize real-time monitoring.

The invention concerns an oral pharmaceutical composition consisting essentially ofthe PDE4B-inhibitor of formula IIIin the dose of 18 mg or 9 mg andoptionally of one or more pharmaceutically acceptable carriers or excipientsfor use in the treatment of a patient suffering from one or more progressive fibrosing interstitial lung diseases (PF-ILD), wherein this oral pharmaceutical composition is to be administered to the patient twice daily.The invention further concerns oral pharmaceutical compositions comprising the PDE4B-inhibitor of formula III in the dose of 18 mg or 9 mg and a therapeutically effective dose of a second active ingredient selected from nintedanib or pirfenidone, wherein these oral pharmaceutical compositions are administered to the patient twice daily.

The invention concerns an oral pharmaceutical composition consisting essentially of • the PDE4B-inhibitor of formula III in the dose of 18 mg or 9 mg and • optionally of one or more pharmaceutically acceptable carriers or excipients for use in the treatment of a patient suffering from one or more progressive fibrosing interstitial lung diseases (PF-ILD), wherein this oral pharmaceutical composition is to be administered to the patient twice daily. The invention further concerns oral pharmaceutical compositions comprising the PDE4B-inhibitor of formula III in the dose of 18 mg or 9 mg and a therapeutically effective dose of a second active ingredient selected from nintedanib or pirfenidone, wherein these oral pharmaceutical compositions are administered to the patient twice daily.

Disclosed in the present invention are a polycyclic PDE4B selective inhibitor and the use thereof. Specifically, disclosed in the present invention are a compound as shown in formula (I), or a stereoisomer, a tautomer, a hydrate, a solvate, a pharmaceutically acceptable salt or a prodrug thereof. The compound of the present invention is a PDE4B selective inhibitor, and can be used in the preparation of a drug for treating and / or preventing PDE4B-related diseases.

A compound represented by formula I, stereoisomers or pharmaceutically acceptable salts thereof, or a pharmaceutical composition containing same, and the use thereof as a PDE4B inhibitor in the preparation of a drug for treatment of related diseases. Each group in formula (I) is as defined in the description.

The present invention relates to use of a compound of formula (I), or a stereoisomer thereof, a tautomer thereof, a pharmaceutically acceptable salt thereof, or a composition thereof in the preparation of a medicament for treating psoriasis and atopic dermatitis. The present invention also relates to a method for treating psoriasis and atopic dermatitis. The method comprises administering an effective dose of the compound of formula (I), or the stereoisomer thereof, the tautomer thereof, the pharmaceutically acceptable salt thereof, or the composition thereof.

This invention provides a novel target PDE4B for the prevention and treatment of Cryptococcus neoformans brain infection. Specifically, it relates to the application of drugs targeting phosphodiesterase PDE4B in the preparation of drugs for the prevention and / or treatment of Cryptococcus neoformans meningoencephalitis. The drug targeting PDE4B is the PDE4B agonist MR-L2 (CAS: 2374703-19-0). The PDE4B agonist MR-L2 described in this invention can significantly reduce Cryptococcus neoformans brain infection, providing an effective prevention and treatment method for Cryptococcus neoformans meningoencephalitis.

Provided in the present invention are a compound targeting phosphodiesterase subtype PDE4B or a pharmaceutically acceptable salt thereof, and a preparation method therefor. The structure of the compound is shown as formula I. Also provided are a pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt thereof, and the use thereof in the treatment of phosphodiesterase subtype PDE4B mediated diseases.

The invention provides a new application of psoralen isoflavone, the psoralen isoflavone can significantly inhibit protein expression of PDE4B in dinitrochlorobenzene induced AD mouse skin and TNF-alpha / I FN-gamma stimulated keratinocytes, and after treatment with the psoralen isoflavone, dermatitis characteristics such as skin redness and swelling, scales and ulceration of AD mice can be effectively improved; the psoralen isoflavone can be used for remarkably reducing the scratching frequency of AD mice and effectively relieving pruritus; the psoralen isoflavone can reduce the skin percutaneous moisture loss of AD mice; hamp, Hamp; e dyeing shows that the psoralen obviously reduces the skin epidermis thickness of AD mice; toluidine blue staining shows that the psoralen isoflavone remarkably reduces the number of mast cells in AD mouse skin tissue and improves the infiltration state of the mast cells, and the psoralen isoflavone has important application value in preparation of a PDE4B inhibitor.

The invention discloses a polycyclic PDE4B selective inhibitor and an application thereof. Specifically, the invention discloses a compound as shown in a formula (I), and a stereoisomer, a tautomer, a hydrate, a solvate, a pharmaceutically acceptable salt or a prodrug thereof. The compound provided by the invention is a PDE4B selective inhibitor, and can be used for preparing drugs for treating and / or preventing diseases related to PDE4B. # imgabs0 #

The present invention belongs to the field of medicine, and specifically, the present invention relates to deuterated heterocyclic compounds as PDE4B inhibitors and applications thereof. Specifically, it relates to a compound represented by Formula I, or its tautomers, stereoisomers, hydrates, solvates, pharmaceutically acceptable salts, or prodrugs.