30 results about "Phosphodiesterase I" patented technology

The present invention relates to a phosphodiesterase 4 inhibitor capable of avoiding vomiting. The phosphodiesterase 4 inhibitor is a compound, a prodrug or a solvate represented by DTPM; and the DTPM is named as 1-(4-difluoro methoxy-3-(tetrahydrofuran-3-oxyl) phenyl)-3-dimethyl-1-ketone, and has a chemical formula shown as below. A plurality of experiments have proved that the DTPM has better effect on improvement of learning and memory compared with an existing antidepressant PDE4 inhibitor; in a Beagle dog vomiting effect observation experiment, no obvious vomiting inducing reaction is observed; and the DTPM has an inhibitor intensity 5000 times of that of other PDE4D families. The inhibitor provided by the invention can become a drug for treating depression and Alzheimer's disease and improving the cognitive ability, and capable of effectively reducing and even avoiding adverse reactions like vomiting.

The invention relates to the combined use of a PDE4 inhibitor with a HMG-CoA reductase inhibitor for the preventive and curative treatment of an inflammatory pulmonary disease.

The invention discloses an oxazole ring containing 2,4-disubstituted pyrazole compound. The structural formula of the compound is represented by a formula I shown in the description, wherein the quantity of R is 1, R is H, halogen, nitro, hydroxyl or C1-4 alkyl or alkoxy, and R1 and R2 are the same or different and are independently selected from H and C1-4 alkyl or alkoxy separately. The invention simultaneously provides a preparation method for the compound and an application of the compound. The oxazole ring containing 2,4-disubstituted pyrazole compound provided by the invention has good bioactivity and can serve as a phosphodiesterase (PDE4) and TNF[alpha] inhibitor; and the preparation method is simple and is high in yield, and the application of oxazole and pyrazole structures in the aspect of serving as phosphodiesterase (PDE4) and TNF[alpha] inhibitors is extended.

The invention relates to panels of biomarkers including proteins phosphatase 1 regulatory subunit 14A and/or 2′,3′-cyclic-nucleotide 3′-phosphodiesterase and/or phosphorylated tau or fragments thereof and methods using thereof for diagnosing, staging, treating and assessing the response of a treatment for a neurocognitive disorder characterised by tau toxicity, in particular for Alzheimer's disease. The present invention shows that the biomarkers disclosed herein are elevated in the brain of subjects with an advanced stage of a neurocognitive disorder (Braak stage V/VI) and/or are regulated in the CSF of AD subjects in comparison to cognitively affected non-AD controls; and/or regulated in response to two casein kinase 1 delta inhibitors.

The invention discloses a differential nuclease digestion method and application thereof to detecting mRNA internal modification through LC-MS. The differential nuclease enzyme-digestion method comprises, according to the characteristic of difference of S1 nuclease and phosphodiesterase I in digestion of the 5'-end cap structure of mRNA, digesting the mRNA into nucleosides through the S1 nuclease and the phosphodiesterase I, then performing LC-MS detecting analysis, and combining the detecting results of digestion through the two nucleases to differentiate N7-methyguanosine (m7G) in the cap and the inside of the mRNA and according to the achieve qualitative and quantitative analysis on the m7G inside the mRNA. The differential nuclease enzyme-digestion method is high in sensitivity and selectivity, can quantitatively detect the content of m7G inside encaryotic mRNA and further can be applied to study of related functions of the m7G inside the mRNA.

The present invention relates to novel solid forms of phosphodiesterase type 5 (PDE5) inhibitors, especially to complex co-crystals, and to the solvates and/or the polymorphs of same. Said substances can be used to produce a pharmaceutical composition containing same as the useful active ingredient. Said compounds can exhibit a constant storage stability.

The present invention relates to a therapeutic or prophylactic method for treating Parkinson's disease by administering an effective amount of a compound having a phosphodiesterase 10 inhibitory activity; and also relates to a pharmaceutical composition for treatment or prophylaxis of Parkinson's disease comprising as an active ingredient a compound having a phosphodiesterase 10 inhibitory activity. Moreover, the present invention relates to a method for enhancing dopamine signal in the brain, which comprises administering an effective amount of a compound having a phosphodiesterase 10 inhibitory activity; and also relates to pharmaceutical composition for enhancing dopamine signal in brain comprising as an active ingredient a compound having a phosphodiesterase 10 inhibitory activity.

The invention provides a composition containing a phosphodiesterase inhibitor nanoparticle and a protein kinase inhibitor. The composition is characterized in that the nanoparticles contain the phosphodiesterase inhibitor and polylactose glycolic acid, the phosphodiesterase inhibitor and the protein kinase inhibitor are both products available in the market in China and other countries, and the composition has a synergetic antibacterial function (the drug combination index is less than 1) on multiple bacteria.

Compounds and compositions, and methods of use thereof, are provided and have utility in inhibiting hedgehog signaling and/or phosphodiesterase-4 activity.

Applications of phosphodiesterase type 4 inhibitors in preparation of novel anti-inflammatory drugs are disclosed. Salviacoccin, isocolumbin, teupernin A and bidentatin are effective phosphodiesterasetype 4 inhibitors, and teupernin C does not have obvious inhibition effect. In the salviacoccin, the isocolumbin, the teupernin A and the bidentatin, the isocolumbin has highest inhibition effect close to that of a positive drug that is rolipram.

The present invention relates to the field of molecular biology, biochemistry and biotechnology, namely, to compound 2-acetyl-6-(2-(2-(4-bromobenzylidene)hydrazinyl) thiazole-4-yl)-3,7,9-trihydroxy-8,9b-dimethyldibenzo[b,d]furan-1(9bh)-one, which is a hydrazine-thiazole derivative of usnic acid of formula I and which is able to inhibit the action of human tyrosyl-DNA-phosphodiesterase 1 enzyme. Technical result: increase in inhibitory action towards human tyrosyl-DNA-phosphodiesterase 1 enzyme (Tdp1) and increase in the number of inhibitors of this enzyme.

The invention discloses phosphodiesterase 4 inhibitors and an application thereof, which finds that the labiacinol, isopredomyl lactone, scorpion prostaglandin A and bidentenol are effective phosphodiesterase 4 inhibitors, and the inhibitory effect of scorpion prostaglandin C is not obvious. Among the labiacinol, isopredomyl lactone, scorpion prostaglandin A and bidentenol, the isopredomyl lactonehas the strongest inhibitory effect, which is close to the positive drug rolipram.

The present invention relates to combinations of phosphodiesterase 2 (PDE2) inhibitors with inhibitors of phosphodiesterase 10 (PDE 10). In particular, the invention relates to combinations of 1-aryl-4- methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives which have been found to inhibit phosphodiesterase 2 (PDE2), with inhibitors of phosphodiesterase 10 (PDE10). Particular PDE10 inhibitors are selected from the group of MP-10, PQ-10, TP-10, papaverine, and the compounds disclosed in WO 2011/051342 and in WO 2011/110545. The invention is also directed to pharmaceutical compositions comprising such combinations, to processes for preparing such compositions, to the use of PDE2 inhibitors, in particular of 1- aryl-4-methyl- [1,2,4]triazolo[4,3-a]-quinoxaline derivatives for the potentiation of said PDE10 inhibitors, and to the use of said PDE10 inhibitors for the potentiation of the effect of said PDE2 inhibitors, in particular, 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives, and to the use of such combinations and compositions for the prevention and treatment of disorders in which PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases.

The invention discloses a method for detecting the karyon DNA (deoxyribonucleic acid) and mitochondrion DNA methylation levels of a corn through high-performance liquid chromatography. The preparation method of a hydrolysis mixed solution for treating 100 parts of DNA of 1 mu g comprises the following step: adding 250 U of Benzonase, 300 muU of phosphodiesterase I and 200 U of alkaline phosphatase into 5 mL of Tris-HCl hydrolysis buffer solution having a pH value of 7.9, wherein the pH values of mobile phases are as follows: the pH value of mitochondrion DNA is regulated to 3.42 with phosphoric acid, and the pH value of karyon DNA is regulated to 3.0 with phosphoric acid; the chromatographic conditions are as follows: a C18 filler chromatographic column is used, the flow rate is 0.8 mL/min, the detector wavelength is 287 nm, the column temperature is 35 DEG C, and the sample size is 20 muL; and methanol, 5mM sodium pentanesulfonate and triethylamine of which the ratio is 10:90:0.2 (V/V) are used as the mobile phases, and the pH values are respectively regulated to 3.42 and 3.0 with phosphoric acid. The method is simple and easy to implement, and all the components can be completely separated within 20 minutes.