Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T84133 Target Info
Target Name Phosphodiesterase 10A (PDE10)
Synonyms cAMP and cAMPinhibited cGMP 3',5'cyclic phosphodiesterase 10A; cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Target Type Clinical trial Target
Gene Name PDE10A
Biochemical Class Phosphoric diester hydrolase
UniProt ID
PDE10_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2014139983
Title [1,2,4]Triazolo[4,3-A]Quinoxalines As Dual Pde2/Pde10 Inhibitors.
Abstract The present invention relates to novel compounds as dual PDE2/PDE10 inhibitors. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses thereof.
Applicant(s) H. Lundbeck A/S
Representative Drug(s) D02PFP Drug Info IC50 = 19 nM Click to Show More [1]
2 D09RWM Drug Info IC50 = 67 nM [1]
Patent ID WO2014019979
Title 4-Methyl-2,3,5,9,9B-Pentaaza-Cyclopenta[A]Naphthalenes.
Abstract The invention relates to 4-methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalene derivatives of general formula (I) which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D01LSP Drug Info IC50 = 1488 nM Click to Show More [1]
2 D0T8WU Drug Info IC50 = 2403 nM [1]
Patent ID WO2013000924
Title 1-Aryl-4-Methyl-[1,2,4]Triazolo[4,3-A]Quinoxaline Derivatives.
Abstract The present invention relates to novel l-aryl-4-methyl-[l,2,4]triazolo[4,3-a]- quinoxaline derivatives as inhibitors of phosphodiesterase 2 (PDE2) and to a lesser extent of phosphodiesterase 10 (PDE10) or as inhibitors of both, phosphodiesterases 2 and 10. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which PDE2 is involved, or disorders in which both PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases. The present invention also relates to radiolabeled compounds which may be useful for imaging and quantifying the PDE2 enzyme in tissues, using positron- emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D0X2UO Drug Info pIC50 = 5.32 Click to Show More [1]
2 D0QE7X Drug Info pIC50 = 5.79 [1]
3 D0LI6Z Drug Info pIC50 = 7.47 [1]
4 D0FV3G Drug Info pIC50 = 7.67 [1]
Patent ID WO2012104293
Title (1,2,4)Triazolo[4,3-A]Quinoxaline Derivatives As Inhibitors of Phosphodiesterases.
Abstract The invention relates to (1,2,4)triazolo[4,3-a]quinoxaline derivatives of Formula (I) which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D0J6KS Drug Info IC50 = 1 nM Click to Show More [1]
2 D09BDD Drug Info IC50 = 45 nM [1]
3 D0RI3W Drug Info IC50 > 1000 nM [1]
Patent ID WO2010054260
Title Imidazo[5,1-C][1,2,4]Benzotriazine Derivatives As Inhibitors of Phosphodiesterases.
Abstract The invention relates to imidazo[5,1-c][1,2,4]benzotriazine derivatives of formula (I): which are inhibitors of phosphodiesterase 2 or 10 useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type 2 diabetes, metabolic syndrome, glucose intolerance, and pain.
Applicant(s) Biotie Therapies Gmbh
Representative Drug(s) D0QI8G Drug Info IC50 = 0.7 nM Click to Show More [1]
2 D0L6AM Drug Info IC50 = 21.6 nM [1]
3 D0I5UY Drug Info IC50 = 258 nM [1]
4 D0MK7X Drug Info IC50 = 1540 nM [1]
Patent ID WO2010054253
Title Triazine Derivatives As Inhibitors of Phosphodiesterases.
Abstract The invention relates to triazine derivatives of formula (I): which are inhibitors of phosphodiesterase 2 or 10, useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type 2 diabetes, metabolic syndrome, glucose intolerance, and pain.
Applicant(s) Biotie Therapies Gmbh
Representative Drug(s) D0JJ8K Drug Info IC50 = 3.01 nM Click to Show More [1]
2 D07NRP Drug Info IC50 = 9.83 nM [1]
3 D0J8YF Drug Info IC50 = 10.1 nM [1]
4 D07ZTT Drug Info IC50 = 20.9 nM [1]
5 D0PP8O Drug Info IC50 = 70.94 nM [1]
6 D07EUB Drug Info IC50 = 114 nM [1]
7 D00YOY Drug Info IC50 = 282 nM [1]
8 D0D4YR Drug Info IC50 > 500 nM [1]
Patent ID WO2014001314
Title Combinations Comprising Pde 2 Inhibitors Such As 1-Aryl-4-Methyl- [1,2,4] Triazolo [4,3-A] Quinoxaline Compounds and Pde 10 Inhibitors for Use In The Treatment of Neurological or Metabolic Disorders.
Abstract 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.
Applicant(s) Janssen Pharmaceutica Nv
Patent ID WO2011110545
Title Imidazo [1, 2 -A] Pyrazine Derivatives and Their Use for The Prevention or Treatment of Neurological, Psychiatric and Metabolic Disorders and Diseases.
Abstract The present invention relates to novel imidazo[1,2-a]pyrazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
Applicant(s) Janssen Pharmaceutica Nv
Patent ID WO2011051342
Title Imidazo[1,2-B]Pyridazine Derivatives and Their Use As Pde10 Inhibitors.
Abstract The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
Applicant(s) Janssen Pharmaceutica Nv
References  Top
REF 1 Towards selective phosphodiesterase 2A (PDE2A) inhibitors: a patent review (2010 - present).Expert Opin Ther Pat. 2016 Aug;26(8):933-46.

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