106 results about "Phosphodiesterase" patented technology

The present application relates to a crystal form of 4-[3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenethyl]pyridine-2(1H)-one, a preparation method therefor, a composition containing the crystal form and the use thereof in the treatment of phosphodiesterase-related diseases.

The invention belongs to the technical field of biological medicine, and particularly relates to a 2-hydroxy-6-alkoxy quinoline compound and application thereof, and the structure of the compound is shown as a formula (I) or a formula (II). The 2-hydroxy-6-alkoxy quinoline compound provided by the invention has a remarkable inhibition effect on phosphodiesterase type 3 (PDE3); moreover, the 2-hydroxy-6-alkoxy quinoline compound provided by the invention has good drug-like properties such as water solubility, liver stability, bioavailability and the like, can be applied to preparation of drugs for treating PDE3 related diseases, and provides a selectable range for the drugs for treating the PDE3 related diseases.

Sublingual compositions for the treatment of erectile dysfunction (ED) comprise unique combinations of phosphodiesterase-type 5 (PDE5) inhibitors and D1 / D2 dopamine receptor agonists. In preferred embodiments, a combination of four drug actives exhibits a full range of effectiveness for ED in which there is a short and long acting PDE5 inhibitor in combination with both a dopamine agonist and a CNS hormone to provide both a physiological response and a psychological / CNS action. A treatment for ED comprises administration of sublingual compositions in the physical form of sublingual tablets.

A construction and use of an environmentally adaptive co-regulated mRNA nanodelivery system. By incorporating EACR molecules into mRNA nanoparticles, the microenvironment is remodeled to be suitable for robust and sustained mRNA expression, while tissue damage associated with the self-immunogenicity of mRNA drugs is avoided. The nanodelivery system is compatible with ionizable lipid nanoparticles, cationic liposomes, cationic nanoemulsions, and polymeric nanoparticles. The EACR molecules include: anti-inflammatory drugs, tyrosine kinases / adaptors, JAK / STAT and MAPK pathway inhibitors, nutrients and metabolites, membrane transporters / ion channels, phosphodiesterase and cellular stress inhibitors, and natural viral proteins. The therapeutic mRNAs may encode tumor, viral, or bacterial antigens, immunomodulatory factors, therapeutic antibodies, or functional proteins / enzymes, and can play a role in the fields of regenerative medicine, protein supplementation / replacement therapy, targeted gene editing, and immunotherapy.

The present application provides compositions and methods for treating a disease or disorder using a therapeutically effective amount of a serotonenergy-causing drug and a therapeutically effective amount of a phosphodiesterase type 9 inhibitor.

Provided herein are oral dosage forms comprising a) a core tablet comprising (i) a drug layer comprising apremilast and hypromellose acetate succinate (HPMCAS) in an amorphous solid dispersion; and (ii) a swellable layer comprising one or more swellable polymers; and b) a coating layer disposed on the core tablet, wherein the oral dosage form surface comprises at least one drug release orifice. The disclosed oral dosage forms provide once-a-day dosing of apremilast and are suitable for treating diseases or disorders ameliorated by inhibiting phosphodiesterase subtype IV (PDE4).

To provide a recombinant polynucleotide for treating a particular disease of ectopic tissue calcification, and to provide a viral vector containing the recombinant polynucleotide.SOLUTION: Provided is a recombinant polynucleotide encoding a precursor polypeptide comprising an Azurocidin signal peptide fused to ectonucleotide pyrophosphatase / phosphodiesterase- 1 (ENPP1) or to ectonucleotide pyrophosphatase / phosphodiesterase-3 (ENPP3), the precursor polypeptide being proteolytically cleaved to produce soluble ENPP1 or soluble ENPP3 which is active to reduce ectopic calcification of soft tissue, upon expression of the polynucleotide in mammalian cells.SELECTED DRAWING: Figure 4

The invention relates in general to the field of CAR-T cells. The invention in particular relates to improved methods for obtaining CAR-T cells, and improved CAR-T cells, as well as uses thereof. The method in further relates to activating or expressing a phosphodiesterase (PDE) in T-cells during CAR-T cell generation.

The invention belongs to the technical field of microbial pharmacy, and discloses a polyketone macrolide compound generated by genetically engineered streptomyces as well as a preparation method and application thereof. The polyketone macrolide compound disclosed by the invention is a cinnamyl streptomycin derivative, has cell proliferation inhibition activity better than that of a natural product Cinnamomycin A-D, can exert anti-tumor activity by inhibiting activity of human exonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1) and activating an inherent immune pathway, can be prepared into a medicine or a medicinal composition, and can be used for preparing medicines or medicinal compositions. The compound is used for treating tumors and related diseases.

This invention discloses a genetically engineered bacterium capable of synthesizing large quantities of natural cyclic diguanylate (c-di-GMP) and its applications. It involves knocking out the major phosphodiesterase gene chr1_233 as described in claim 1 within the sphingobium xenophagum C2 strain. This invention rationally designs and modifies the c-di-GMP synthesis and degradation pathways and the inhibitory site of major diguanylate cyclase activity in heterologous sphingobium-consuming bacteria, constructing a series of genetically engineered bacteria capable of synthesizing large quantities of natural c-di-GMP. This provides the industry with a green, simple, economical, and efficient method for producing natural c-di-GMP, and offers a series of high-quality and inexpensive raw materials for the preparation of STING agonists or immune adjuvants, or for the preparation of drugs for treating diseases related to STING protein function.

The invention relates to the technical field of enzyme preparation preparation and fragrance-retaining beads, in particular to an enzyme preparation, a preparation method thereof and a deodorizing and odor-removing fragrance-retaining bead. Wherein the enzyme preparation comprises a compound enzyme microcapsule and a protease microcapsule in a mass ratio of (3-6): 1; a core material of the compound enzyme microcapsule is prepared from the following components in parts by mass: 12 to 15 parts of lipase, 2 to 4 parts of amylase, 5 to 8 parts of fig lysozyme, 2 to 4 parts of cellulase, 1 to 3 parts of pectinase and 1 to 3 parts of phosphodiesterase (PDE). The enzyme preparation disclosed by the invention is added into the aroma-retaining beads for use, so that the antibacterial, deodorizing and peculiar smell removing effects of the aroma-retaining beads can be effectively improved.

The present disclosure relates generally to processes for providing compounds that can be used as inhibitors of ectonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1), which inhibitors can be useful in treating or preventing soft bone diseases, such as hypophosphatasia (HPP).

The invention discloses an application of an overexpression level transfer gene GlpQ in improving the fertility of male silkworms, and the nucleotide sequence of the GlpQ is shown as SEQ ID NO.3. After the GlpQ1 gene is overexpressed, the reproductive activity of the male silkworms is obviously enhanced, the number of female silkworms capable of mating with each male silkworm on average is obviously increased, and the reproductive activity of the male silkworms is obviously improved. Correspondingly, the number of female silkworms capable of being fertilized by the male silkworms is also obviously increased, the testis development process can be promoted, the gene may act on the testis outer membrane to promote the increase of the testis volume and act on the seminal vesicle to promote sperm formation, and therefore the gene can be used for the fertility of the male silkworms.

This application relates to a series of novel compounds that are selective inhibitors of phosphodiesterase type 9 ("PDE9") for the treatment of chronic heart failure. More specifically, this application relates to pyrazolo[3,4-d]pyrimidinone compounds for use in the treatment and prevention of chronic heart failure.

To provide small-molecule modulators of ectonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1).SOLUTION: Provided is a compound having the structure of Formula (I), or a pharmaceutically acceptable salt or solvate thereof: SELECTED DRAWING: None

The present invention discloses a method for detecting the boson content in cosmetics, which relates to the technical field of cosmetics detection. The method comprises the following steps: gray-scaling a fluorescent image, marking potential edge pixels according to gradient amplitude; reducing the potential edge pixels, eliminating invalid edge pixels, dilating non-potential edge pixels, and generating a final actual contour based on the intersection of the potential contour and the effective contour; accurately extracting the intersection of the potential contour and the effective contour by combining microfluidic chip technology with fluorescent markers, adopting gradient analysis and morphological optimization, further screening out effective edge pixels by establishing a coordinate system and structural element window analysis, and finally determining a precise final contour based on the overlap of the potential contour and the effective contour. This method not only improves detection efficiency, but also significantly enhances the accuracy and reliability of the detection results.

The present invention relates to a product for treating, preventing or ameliorating prostate cancer in a subject in need thereof, wherein the product induces the expression of PDE4D7 or promotes the activity of phosphodiesterase 4D7. The product may be a direct or indirect activator of PDE4D7 activity, or a product for expressing or promoting PDE4D7 expression in a subject. The invention also defines kits of the product and in vitro or ex vivo uses of the product.

The application discloses a steroid-indole alkaloid hybrid dimer compound, a preparation method thereof and application of the compound in preparation of an antitumor chemotherapy drug sensitizer, and first prepares the steroid-indole diketopiperazine alkaloid hybrid compound from a fungus Aspergillus sp. EGF15-0-3 rice culture medium. The compound is a new skeleton compound first discovered in nature. It is first discovered that the hybrid compound has Tdp1 inhibitory activity and can be applied as a tyrosine-DNA phosphodiesterase 1 (Tdp1) inhibitor. It is first discovered that the hybrid compound has chemotherapy sensitization activity on a tumor chemotherapy drug topotecan TPT, which provides a drug source molecule and data support for development of a new natural antitumor combination inhibitor, and has important significance for development and utilization of marine Aspergillus sp. fungus resources.

Provided herein are methods for treating hypophosphoesterase (HPP), the methods comprising administering a therapeutically effective amount of an inhibitor of exonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1).

The disclosure relates to the use of phosphodiesterase 1 (PDE1) inhibitors for preventing or treating chemobrain, e.g., inhibiting or mitigating one or more symptoms of chemobrain, e.g., feeling of mental fogginess, deficit in attention, disorganized behavior or thinking, confusion, impaired concentration, difficulty finding the right word, difficulty learning new skills, difficulty multitasking, memory impairment (e.g., short-term memory problems, long-term memory problems, impaired verbal memory, impaired visual memory), and / or fatigue.

This invention relates to pharmaceutical compositions, including compositions adapted for intranasal administration, comprising an active ingredient, including dexmedetomidine, pomalidomide, a selective phosphodiesterase type 4 inhibitor such as roflumilast, or combinations thereof, useful in the treatment of traumatic brain injury (TBI), including to prevent or reduce the neurological sequalae of TBI.

The invention relates to the technical field of medicines, in particular to a novel medical application of a phosphodiesterase 4B inhibitor namiklast, and particularly relates to an application of namiklast in preparation of a medicine for treating intervertebral disc fibrosis through targeted inhibition of macrophage-myofibroblast transformation.

The application discloses a preparation method of an amido pyrazole compound and a method for preparing sildenafil by using the same. The amido pyrazole compound is shown as formula I. The compound of formula I is prepared by using 2-pentanone as an industrial chemical, and can be used for synthesizing sildenafil which is a selective inhibitor of type 5 phosphodiesterase (PDE5). The method has the advantages of easy availability of raw materials, simple operation, avoidance of nitration reaction, avoidance of safety hidden dangers caused by the nitration reaction from a technical source, and avoidance of environmental protection pressure caused by a large amount of nitration waste liquid, and is suitable for development into a green and sustainable production process of sildenafil bulk drug.

The invention relates to kinase inhibitors, and specifically to inhibitors of the kinase c-RAF, comprising a cyclic peptide component capable of inhibiting complex formation between c-RAF and phosphodiesterase-8A (PDE8A). The inhibitors find use in various medical applications including the treatment of cancer, and in particular cancers which carry gain-of-function mutations in Ras (e.g. KRAS, NRAS or HRAS) and / or RAF mutations (e.g. mutations in A-RAF, B-RAF or c-RAF / RAF1).

The present invention relates to a pharmaceutical product comprising a single dose dry powder inhalation device and a pharmaceutical composition filled in a capsule, the pharmaceutical composition comprising micronized particles of a compound of formula (I) and a carrier. The invention also relates to a pharmaceutical or pharmaceutical composition for the treatment of respiratory diseases and to a method for the treatment of respiratory diseases. # imgabs0 #

Substituted benzoxazole and benzofuran chemical entities of Formula (I):wherein, V, W, X, Y, Z, and m have any of the values described herein and compositions comprising such chemical entities; processes for making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; and the treatment of one or more disorders, including neurological, cognitive, immunological, and inflammatory disorders, as well as other conditions and diseases involving PDE7 or cyclic nucleotide signaling.

A method of reducing fear memory in a mammal comprising the step of inhibiting or reducing cAMP signaling in the mammal. The cAMP signaling can be reduced using an adenylyl cyclase 1 (AC1) inhibitor or using a phosphodiesterase, such as a cAMP-specific phosphodiesterase, such as PDE4.

The present invention relates to a product for use in the treatment, prevention, or remission of prostate cancer in subjects requiring treatment, prevention, or remission, wherein the product induces the expression of PDE4D7 or promotes the activity of phosphodiesterase 4D7. The product may be a direct or indirect activator of PDE4D7 activity, or a product for causing or promoting the expression of PDE4D7 in a subject. The present invention further specifies kits of elements and the in vitro or ex vivo use of the product.

A method for altering the PK profile of a pharmaceutical formulation containing a PDE-4 inhibitor, such as roflumilast, to reduce the spike in Cmax. The spike in Cmax is reduced by topically administering the PDE-4 inhibitor in combination with one or more phosphate ester surfactants. Reducing the spike in Cmax will reduce gastrointestinal side effects and result in better patient compliance.

The invention relates to the technical field of medicines, in particular to a substituted pyrimidinone compound or pharmaceutically acceptable salt thereof as well as a preparation method and application of the substituted pyrimidinone compound. The structure of the substituted pyrimidinone compound is shown as a formula (I) or a formula (II). The substituted pyrimidone compound provided by the invention shows a good inhibition effect on phosphodiesterase, can be applied as a phosphodiesterase type 1 inhibitor, and has an important medicinal value and a wide application prospect. In addition, the preparation method of the substituted pyrimidinone compound is simple and suitable for large-scale industrial production and application.