Unlock instant, AI-driven research and patent intelligence for your innovation.
For use in the treatment of neurological disorders or metabolic combinations used in obstacles
What is Al technical title?
Al technical title is built by PatSnap Al team. It summarizes the technical point description of the patent document.
A technology of PDE10 and inhibitors, applied in the field of phosphodiesterase 2 inhibitors
Active Publication Date: 2018-03-06
JANSSEN PHARMA NV
View PDF8 Cites 0 Cited by
Summary
Abstract
Description
Claims
Application Information
AI Technical Summary
This helps you quickly interpret patents by identifying the three key elements:
Problems solved by technology
Method used
Benefits of technology
Problems solved by technology
[0018] Thus, PDE10 inhibitors may have a pharmacological profile similar to current antipsychotic drugs that primarily treat the positive symptoms of schizophrenia, but PDE10 inhibitors also have the potential to improve the negative and cognitive symptoms of schizophrenia, Concomitant lack of non-target related side effects such as EPS or prolactin release commonly observed with currently effective antipsychotics
Method used
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more
Image
Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
Click on the blue label to locate the original text in one second.
Reading with bidirectional positioning of images and text.
Smart Image
Examples
Experimental program
Comparison scheme
Effect test
example 1
[0471] Examples 1a and 1b
[0472] 1-(5-Butoxypyridin-3-yl)-4-methyl-8-(morpholin-4-ylmethyl)[1,2,4]triazol[4,3-a]quinoxa Phenoline hydrochloride (B-1a) and oxalate (B-1b)
[0473]
[0474] .2HCl(B-1a) or .x C 2 h 2 o 4 (B-1b)
[0475] Formation of B-1a
[0476] To intermediate compound I-5 (7.5g, 18.19mmol) in THF / H 2 Add Pd(AcO) to a solution in O (10:1, 180 mL) 2 (0.12g, 0.54mmol), XantPhos (0.52g, 1.09mmol), Cs 2 CO 3 (23.88 g, 72.76 mmol) and intermediate compound 1-20 (4.51 g, 21.82 mmol). The reaction mixture was closed in a sealed tube and stirred at room temperature for 10 min and then at 114 °C for 45 min. Then, the crude mixture was washed with EtOAc and H 2 Diluted with O, the organic layer was separated and dried (MgSO 4 ), filtered and the solvent was concentrated in vacuo. The crude mixture was purified by chromatography (silica, MeOH in DCM, 0 / 100 to 2 / 98), the desired fractions were collected and the solvent was concentrated in vacuo to give ...
[0487] To a stirred solution of Intermediate 1-8 (2.3 g, 7.12 mmol) dissolved in DCE (50 mL) was added morpholine (1.37 mL, 15.67 mmol) and the mixture was heated at 80 °C for 15 min under microwaveirradiation (with The reaction was divided into three batches). Sodium triacetoxyborohydride (1.81 g, 8.55 mmol) was then added in portions and the mixture was heated again under the same conditions as previously described for 20 min. The mixture was then treated with H 2 O quenched and extracted with DCM. The organic layer was separated and dried (Na 2 SO 4 ), filtered and evaporated the solvent in vacuo. The crude compound was purified by chromatography (silica, MeOH in EtOAC, 2 / 98 to 10 / 90), the desired fractions were collected and the solvent was evaporated to give the final compound as a light yellow solid B-3 (1.6 g, 57%), this compound was further washed w...
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More
PUM
Login to View More
Abstract
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.
Description
field of invention [0001] 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 / 051324 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]triazoles [ Use of 4,3-a]-quinoxaline derivatives for the enhancement of said PDE10 inhibitors and to said PDE10 inhibitors for said PDE2 inhibitors, in particular 1-aryl-4-methyl - the use of [1,2,4]triazol[4,3-a]-...
Claims
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More
Application Information
Patent Timeline
Application Date:The date an application was filed.
Publication Date:The date a patent or application was officially published.
First Publication Date:The earliest publication date of a patent with the same application number.
Issue Date:Publication date of the patent grant document.
PCT Entry Date:The Entry date of PCT National Phase.
Estimated Expiry Date:The statutory expiry date of a patent right according to the Patent Law, and it is the longest term of protection that the patent right can achieve without the termination of the patent right due to other reasons(Term extension factor has been taken into account ).
Invalid Date:Actual expiry date is based on effective date or publication date of legal transaction data of invalid patent.
Login to View More 
Login to View More 
