30 results about "Phosphodiesterase I" patented technology

A compound having PDE inhibitory represented by formula (1), W1-W2 (1), wherein (i) W1 isand W2 is(ii) W1 isand W2 isor (iii) W1 isand W2 isor a pharmaceutically acceptable salt thereof; and a method of treating or preventing schizophrenia.

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 present invention is directed to pyrazolopyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

The present invention relates to co-crystals of tadalafil with hydroxyl-substituted benzoic acid coformers having the following structure.Said co-crystals can be used to produce a pharmaceutical composition containing the same as the useful active ingredient. Said co-crystals can exhibit a constant storage stability.

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 present invention is directed to substituted cyclobutyl benzimidazole compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

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 invention discloses pyrazolo[3,4-d]pyrimidone compounds and application thereof in preparation of a phosphodiesterase IX inhibitor. The structure of the compounds is shown as a formula (1); in the formula, when R' is 2-chlorophenyl, R refers to phenyl, substituted phenyl, benzyl, substituted benzyl, 3-methylpyridine, 1-phenylethyl, diphenylmethyl or CHCH3CONHR1, wherein R1 refers to phenyl ormethyl, methoxyl, ethoxyl, isopropoxy, methylthio, NHCOCH3 or NCH3CH3 substituted phenyl; when R' is phenyl, R refers to CHCH3CONHR2, wherein R2 refers to methoxyl or ethoxyl substituted phenyl; and when R' is methyl, R refers to 4-methoxy-benzyl, diphenylmethyl or N-(2-amino-cyclohexyl)-4-methoxy-benzenesulfonamide. The pyrazolo[3,4-d]pyrimidone compounds have activity of inhibiting phosphodiesterase IX, can serve as the phosphodiesterase IX inhibitor, can be used for preparing the phosphodiesterase IX inhibitor, and have wide application prospect. The compounds are shown as the formula (1).

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

Compounds of the general formula (I), wherein one of X1 and X2 represents N, and the other one of X1 and X2 represents —C(CH3), A represents unsubstituted or substituted 5-, 6- or 10-membered aryl or heteroaryl, n is 0 or 1 and B is a bicyclic heteromoiety defined in the specification. Compounds are phosphodiesterase 10A inhibitors and can find use in medicine in the treatment psychotic, neurological and cognitive functions diseases and disorders. (I)

The present invention relates to combinations of inhibitors of phosphodiesterase 2 (PDE2) and inhibitors of phosphodiesterase 10 (PDE10). In particular, the present invention relates to 1-aryl-4-methyl-[1,2,4]triazol[4,3-a]-quinoxaline derivatives and inhibitors of phosphodiesterase 10 (PDE10) Combination of this derivative has been found to inhibit phosphodiesterase 2 (PDE2). Particular PDE10 inhibitors are selected from the group consisting of MP-10, PQ-10, TP-10, papaverine, and compounds disclosed in WO 2011 / 051342 and WO 2011 / 110545. The invention also relates to pharmaceutical compositions comprising these combinations, to processes for the preparation of these compositions, to PDE2 inhibitors, in particular 1-aryl-4-methyl-[1,2,4]triazole[ 4,3-a]-quinoxaline derivatives for the enhanced use of said PDE10 inhibitors and to said PDE10 inhibitors for said PDE2 inhibitors, in particular 1-aryl-4-methyl Use of ‑[1,2,4]triazol[4,3‑a]‑quinoxaline derivatives for enhancing the effect and to the use of these combinations and compositions for the prevention and treatment of disorders involving PDE2 and PDE10 , such disorders as neurological and psychiatric disorders, and endocrine or metabolic diseases.