38 results about "PDE4 Inhibitors" patented technology

The present invention relates to a pharmaceutical composition containing a PDE4 inhibitor, in particular compound A. Further provided in the present invention are a method for preparing the pharmaceutical composition, and the use of the pharmaceutical composition in the treatment of a disease.

Provided herein are methods and compositions involving chromene derivatives acting as TCR or TCR-Nck inhibitors, and PDE4 inhibitors. The provided methods include the use of a chromene derivative in combination with a PDE4 inhibitor for treating a disease or disorder.

Disclosed are a difluoromethoxyphenyl PDE4 inhibitor represented by formula I and a use thereof. The compound has the effects of resisting inflammation, treating psoriasis, treating lung injury, treating chronic obstructive pulmonary disease, etc.

The present invention relates to the crystal Form 2 of the compound of formula (I), to the process for its isolation and to the pharmaceutical compositions thereof. The present invention also relates to the crystal Form 2 of the compound of formula (I) for use as a medicament and for the manufacture of a medicament for the prevention and / or treatment of an inflammatory respiratory or obstructive respiratory disease.

This invention discloses a ginsenoside Rg5 derivative with the molecular formula: C 42 H 74 O 12 The molecular weight is 770.5180. Furthermore, this invention also discloses the synthesis method and application of this derivative. The synthesis method of this invention is simple and safe, and the synthesized ginsenoside Rg5 derivative exhibits strong stability and superior therapeutic effect on non-alcoholic steatohepatitis (NAH). This invention is the first to combine the prepared ginsenoside Rg5 derivative with the PDE4 inhibitor (R)-(-)-Rolipram, showing significantly better efficacy than either drug alone. When the molar ratio of the two drugs is 1:1, the drug exhibits even better therapeutic effect on NHA, showing promising application prospects.

The present disclosure relates to PDE4 inhibitor compounds, pharmaceutical compositions containing the compounds, and methods of using such compounds to treat disease.

Provided is the use of a PDE4 inhibitor for treating and / or preventing chronic obstructive pulmonary diseases or related diseases thereof.

A class of PDE4 inhibitor compounds, isomers, solvates, deuterated derivatives or pharmaceutically acceptable salts thereof. Medicaments comprising the compounds, isomers, solvates, deuterated derivatives and pharmaceutically acceptable salts thereof, and their use in the preparation of a medicament for the treatment of diseases associated with PDE4 inhibition, such as autoimmune diseases, cancer.

The present invention relates to a pyrimido[6,1-a]isoquinolin-4-one derivative and its use. The structural formula of the pyrimido[6,1-a]isoquinolin-4-one derivative of the present invention is shown in Formula (I): #imgabs0# wherein R1, R2, R3, X, and Y are as described in the specification. The compound of the present invention can simultaneously inhibit PDE3 and PDE4 and exhibits superior efficacy compared to existing dual-target PDE3 and PDE4 inhibitors.

The invention relates to a PDE4 inhibitor, a preparation method of the PDE4 inhibitor and application of the PDE4 inhibitor in medicine. Specifically, the invention relates to a compound shown in a general formula (I), a preparation method of the compound, a pharmaceutical composition containing the compound and application of the compound as a PDE4 inhibitor, especially application of the compound in preparation of drugs for treating PDE4-related diseases. # imgabs0 #

The invention discloses a PDE4 inhibitor as well as a preparation method and application thereof, and belongs to the technical field of medicines. Aiming at a PDE4 target spot, 36 novel PDE4 inhibitors are designed and synthesized in the invention. The synthesized PDE4 inhibitor has an obvious inhibition effect on PDE4, most of the compounds have anti-inflammatory activity, and the compound 11b has been proved to have an effect of treating pulmonary fibrosis.

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.

Provided herein are methods and compositions related to treating motor neuron diseases, such as ALS, in a subject by administering to the subject (e.g., orally administering to the subject) a composition comprising nicotinamide riboside, pterostilbene and a phosphodiesterase (PDE) inhibitor, including a PDE4 inhibitor such as ibudilast, and also including a thiol / cysteine donor, such as acetylcysteine.

The present disclosure relates to a method of reducing adverse events due to systemic administration of a PDE4 inhibitor to a patient. The method comprises transdermally administering to the patient a PDE4 inhibitor, for example, over at least about 12 hours.

Provided is the use of a PDE4 inhibitor for treating and / or preventing chronic obstructive pulmonary diseases or related diseases thereof.

This disclosure features methods and compositions for treating diseases of the gastrointestinal tract with a PDE4 inhibitor.

The invention relates to the technical field of biological medicines, and discloses an application of phosphodiesterase PDE4D in preparation of a medicine for treating virus infectious diseases, and an application of a phosphodiesterase PDE4 inhibitor or a salt thereof in preparation of a medicine for treating virus infectious diseases for a long time. Experiments prove that the expression of PDE4D can significantly inhibit the replication of VSV, HSV, PR8 and other viruses; the cell death can be obviously inhibited; the inflammatory response caused by virus infection can be inhibited; the PDE4 inhibitor can induce the expression of PDE4D after long-term treatment; long-term treatment with the PDE4 inhibitor can significantly inhibit embryo loss of pregnant rats caused by virus infection; long-term treatment with the PDE4 inhibitor can reduce viral load of lung and placenta tissues of pregnant rats and pathological changes caused by viral infection.

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.

The invention relates to a pharmaceutical composition for treating degenerative diseases and application thereof. The pharmaceutical composition is particularly suitable for preventing and treating Alzheimer's disease (AD). The pharmaceutical composition disclosed by the invention comprises a combination of a PDE4 inhibitor and a PDE10A inhibitor, and can be used for remarkably activating a cAMP-PKA-CREB signal channel, enhancing the stress tolerance of neurons, reducing the pathological accumulation of A beta and p-tau and improving the plasticity of nerves. The invention provides an innovative medicine composition with potential clinical application value, and a new strategy is provided for intervention of neurodegenerative diseases.

This invention discloses a PDE4 inhibitor, its preparation method, and its applications, belonging to the field of pharmaceutical technology. Targeting PDE4, this invention designed and synthesized 36 novel PDE4 inhibitors. The synthesized PDE4 inhibitors exhibit significant inhibitory effects on PDE4, and most compounds possess anti-inflammatory activity. Compound 11b has been shown to have therapeutic effects on pulmonary fibrosis.

The present invention relates to compounds and methods useful as phosphodiesterase type 4 (PDE4) inhibitors for the treatment or prevention of diseases.

The invention discloses a synthesis method of a PDE4 inhibitor apremilast, and belongs to the technical field of organic synthesis. The preparation method comprises the following steps: taking 3-ethoxy-4-methoxystyrene as an initial raw material, and carrying out aziridine treatment on olefin to obtain an intermediate 1; carrying out nucleophilic ring opening on the intermediate 1 and methyl mercaptide to obtain an intermediate 2; then the intermediate 2 and a tartaric acid resolving agent are subjected to salification and alkali treatment reaction to obtain a chiral intermediate 3, and the intermediate 3 and 3-acetamino phthalic anhydride are subjected to condensation reaction to obtain an intermediate 4; and oxidizing the intermediate 4 to obtain apremilast. The invention develops a green and efficient synthesis process of apremilast, the target product is prepared through five-step reaction, the process breaks through the situation that a traditional route depends on high-pressure hydrogenation conditions and use of highly toxic reagents, normal-pressure operation and mild temperature are adopted in the whole process, and the requirement of low-temperature reaction is avoided. The safety in industrial production is improved to a great extent, and the method is more suitable for industrial continuous production.

This invention relates to natural extracts, specifically to the use of a *Selaginella uncinata* extract in the preparation of medicaments for the treatment and / or prevention of phosphodiesterase type 4 (PDE4)-related diseases. The extract of this invention and the biflavonoids therein possess significant PDE4 inhibitory activity and can be used to prepare PDE4 inhibitors for the treatment and / or prevention of PDE4-related diseases.

This document describes compounds of formula (I), or pharmaceutically acceptable salts thereof, methods for their preparation, and methods for their use in treating or preventing a variety of conditions, including ulcerative colitis, Crohn's disease, chronic obstructive pulmonary disease (COPD), adult respiratory distress syndrome, infant respiratory distress syndrome, cough, psoriatic arthritis, or psoriasis. #imgabs0#

The application discloses application of a compound for targeting and inhibiting PDE4B in preparation of a medicine for preventing and / or treating sepsis. The PDE4B selective inhibitor, especially the BR compound, has remarkable curative effect on improving survival rate of sepsis and protecting multiple organ functions, has no obvious side effect, is safer than a non-selective PDE4 inhibitor, provides a clear direction for development of a medicine for treating sepsis, and has a wide clinical application prospect.