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 T77400 Target Info
Target Name Phosphodiesterase 2A (PDE2A)
Synonyms cGMP-dependent 3',5'-cyclic phosphodiesterase; PDE-II; Cyclic-GMP phosphodiesterase; Cyclic GMP-stimulated phosphodiesterase; Cyclic GMP stimulated phosphodiesterase; CGSPDE; CGS-PDE
Target Type Clinical trial Target
Gene Name PDE2A
Biochemical Class Phosphoric diester hydrolase
UniProt ID
PDE2A_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2015164508
Title Substituted [1,2,4] Triazolo [1,5-A] Pyrimidin-7-Yl Compounds As Pde2 Inhibitors.
Abstract The invention provides a chemical entity of Formula (I) wherein R1, R2, X, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods as disclosed herein, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by PDE2 activity; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training protocols; and treating peripheral disorders, including hematological, cardiovascular, gastroenterological, and dermatological disorders.
Applicant(s) Dart Neuroscience (Cayman) Ltd
Representative Drug(s) D0H4LG Drug Info pIC50 > 7 Click to Show More [1]
2 D0HC5P Drug Info pIC50 > 7 [1]
3 D0T8MJ Drug Info pIC50 > 7 [1]
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 = 1 nM Click to Show More [1]
2 D09RWM Drug Info IC50 = 34 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 = 5 nM Click to Show More [1]
2 D0T8WU Drug Info IC50 = 12 nM [1]
Patent ID WO2013034761
Title Pyridine Compounds and Uses Thereof.
Abstract The present invention is directed to pyridine compounds of Formula (I). Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds as therapeutic agents treating neurological and psychiatric disorders.
Applicant(s) Runmussen Lars Kyhn
Representative Drug(s) D0SV1I Drug Info IC50 = 69 nM Click to Show More [1]
2 D0D0QT Drug Info IC50 = 471 nM [1]
Patent ID WO2013034758
Title Substituted Triazolopyrazines and Uses Thereof.
Abstract The present invention is directed to substituted triazolopyrazine compounds of Formula (I). Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds as therapeutic agents treating neurological and psychiatric disorders.
Applicant(s) Anne Techau Bruun et al
Representative Drug(s) D01ITP Drug Info IC50 = 6.3 nM Click to Show More [1]
2 D0A8EV Drug Info IC50 = 7.2 nM [1]
Patent ID WO2013034755
Title Triazolopyrazine Derivatives and Their Use for Treating Neurological and Psychiatric Disorders.
Abstract The present invention is directed to triazolopyrazine compounds of Formula (I). Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds as therapeutic agents treating neurological and psychiatric disorders.
Applicant(s) Anne Techau Bruun et al
Representative Drug(s) D05VBJ Drug Info IC50 = 21 nM [1]
Patent ID WO2012168817
Title Pyrazolo[3,4-D]Pyrimidine Compounds and Their Use As Pde2 Inhibitors and/or Cyp3A4 Inhibitors.
Abstract The present invention provides, inter alia, compounds of Formula (I) and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal. The present invention further provides compounds of Formula (Id) and pharmaceutically acceptable salts thereof as CYP3A4 selective inhibitors.
Applicant(s) Pfizer Inc
Representative Drug(s) D01IRA Drug Info IC50 = 1.43 nM Click to Show More [1]
2 D07OOA Drug Info IC50 = 2.3 nM [1]
3 D07YWQ Drug Info IC50 = 9.54 nM [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 = 2 nM Click to Show More [1]
2 D09BDD Drug Info IC50 = 3 nM [1]
3 D0RI3W Drug Info IC50 = 3 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) D0L6AM Drug Info IC50 = 0.77 nM Click to Show More [1]
2 D0I5UY Drug Info IC50 = 17.8 nM [1]
3 D0MK7X Drug Info IC50 = 59.1 nM [1]
4 D0QI8G Drug Info IC50 = 210 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) D0PP8O Drug Info IC50 = 2.325 nM Click to Show More [1]
2 D07NRP Drug Info IC50 = 2.99 nM [1]
3 D07ZTT Drug Info IC50 = 3.83 nM [1]
4 D0D4YR Drug Info IC50 = 4.12 nM [1]
5 D00YOY Drug Info IC50 = 7.12 nM [1]
6 D07EUB Drug Info IC50 = 28.6 nM [1]
7 D0JJ8K Drug Info IC50 = 171 nM [1]
8 D0J8YF Drug Info IC50 = 2055 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) D0QE7X Drug Info pIC50 = 8.11 Click to Show More [1]
2 D0LI6Z Drug Info pIC50 = 8.64 [1]
3 D0FV3G Drug Info pIC50 = 9.54 [1]
Patent ID WO2014010732
Title Heterocyclic Compound.
Abstract Provided is a compound having a PDE2A selective inhibitory effect which is useful as a prophylactic/therapeutic drug for integration disorder syndrome, Alzheimer's disease and the like. Provided is a compound represented by formula (1): [symbols in the formula are explained in the specification] or a salt thereof.
Applicant(s) Takeda Pharmaceutical Co., Ltd
Representative Drug(s) D09PMC Drug Info N.A. Click to Show More [1]
2 D0A5YE Drug Info N.A. [1]
3 D0KN9S Drug Info N.A. [1]
Patent ID WO2006072615
Title Triazolophthalazines As Pde2-Inhibitors.
Abstract The compounds of formula (I) in which R1 and R2 have the meanings as given in the description are novel effective PDE2 inhibitors.
Applicant(s) Altana Pharma Ag
Representative Drug(s) D0MA2R Drug Info IC50 < 32 nM [1]
Patent ID WO2006072612
Title Triazolophthalazines As Pde2- Inhibitors.
Abstract The compounds of formula I in which R1, R2 and R3 have the meanings as given in the description are novel effective PDE2 inhibitors. (l).
Applicant(s) Altana Pharma Ag
Representative Drug(s) D0MA2R Drug Info IC50 < 32 nM [1]
Patent ID WO2006024640
Title Triazolophthalazines.
Abstract The compounds of formula (I) in which R1 and R2 have the meanings as given in the description are novel effective PDE2 inhibitors.
Applicant(s) Altana Pharma Ag
Representative Drug(s) D0MA2R Drug Info IC50 < 32 nM [1]
Patent ID WO2005061497
Title Pyrido[2,3-D]Pyrimidine-2,4-Diamines As Pde 2 Inhibitors.
Abstract The invention provides compounds of formula (I) prodrugs thereof, and the pharmaceutically acceptable salts of the compounds or prodrugs, wherein n, X, and Y are as defined herein; pharmaceutical compositions thereof; combinations thereof; and uses thereof.
Applicant(s) Pfizer Products Inc
Representative Drug(s) D0OC1S Drug Info IC50 < 50 nM [1]
Patent ID WO2005041957
Title Oxindole Derivatives and Their Use As Phosphodiesterase Type 2 Inhibitors.
Abstract The present invention provides compounds, methods and kits for treatment of disease states or disorders mediated by PDE2. Oxindole derivatives are provided which have therapeutic use and as PDE2 inhibitors.
Applicant(s) Pfizer Products Inc
Representative Drug(s) D0AK5Y Drug Info IC50 = 40 nM [1]
Patent ID WO2004089953
Title Purin-6-One-Derivatives.
Abstract The compounds of a certain formula (I) in which e.g. R2, R3, R4 and R5 have the meanings as given below are novel effective PDE2 inhibitors. R2 is hydrogen, 1-4C-alkyl, 1-hydroxy-2-4C-alkyl, 1-4C-alkylcarbonyl or 1-(acetyloxy)-2-4C-alkyl and R3 is Arylbutyl, Heteroarylbutyl, Arylpropyl, Heteroarylpropyl, Arylethyl or Heteroarylethyl; wherein Aryl is phenyl, naphthalenyl or indanyl, each of which optionally substituted up to three times identically or differently by halogen, hydroxyl, nitro, trifluoromethyl, carboxyl, 1-4C-alkyl, 1-4C-alkoxy or 1-4C-alkoxycarbonyl, Heteroaryl is pyridinyl, pyrazinyl, pyridazinyl, pyrimidinyl, quinazolinyl, quinoxalinyl, cinnolinyl, quinolyl, isoquinolyl, naphthyridinyl, phthalazinyl, indolyl, isoindolyl, indazolyl, purinyl, pteridinyl, benzofuranyl, benzoxazolyl, benzothiazolyl, benzimidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrrolyl, pyrazolyl, furanyl or thiophenyl, each of which optionally substituted up to three times identically or differently by halogen, hydroxyl, nitro, trifluoromethyl, carboxyl, 1-4C-alkyl, 1-4C-alkoxy or 1-4C-alkoxycarbonyl, R4 is 1-4C-alkoxy which is completely or predominantly substituted by fluorine and R5 is halogen, hydroxyl, nitro, trifluoromethyl, carboxyl, 1-4C-alkyl, 1-4C-alkoxy, 1 -4C-alkoxy which is completely or predominantly substituted by fluorine, 1-4C-alkoxycarbonyl, amino, mono- or di-1-4C-alkylamino, aminocarbonyl, mono- or di-1-4C-alkylaminocarbonyl, 1-4C-alkylcarbonylamino, 1-4C-alkylcarbonyloxy, 1-4C-alkylsulfonylamino, phenylcarbonylamino, phenylcarbonylamino substituted in the phenyl moiety by R6 and/or R7, benzylcarbonylamino, benzylcarbonylamino substituted in the phenyl moiety by R8 and/or R9, phenylsulfonylamino, phenylsulfonylamino substituted in the phenyl moiety by R10 and/or R11, benzylsulfonylamino or benzylsulfonylamino substituted in the phenyl moiety by R12 and/or R13.
Applicant(s) Altana Pharma Ag
Representative Drug(s) D0K3QR Drug Info IC50 < 35 nM [1]
Patent ID WO2004041258
Title Cyclic Nucleotide Phosphodiesterase Inhibitors, Preparation and Uses.
Abstract The invention concerns the use of PDE2 inhibitors for treating disorders of the central and peripheral nervous system, a method for therapeutic treatment by administering to an animal said inhibitors. More specifically, the invention concerns novel benzodiazepinone derivatives and their uses in therapeutics more particularly for treating pathologies involving activity of type 2 cyclic nucleotide phosphodiesterase. The invention also concerns methods for preparing same and novel synthesis intermediates.
Applicant(s) Neuro3D
Representative Drug(s) D0TK5G Drug Info IC50 = 6 nM [1]
Patent ID WO2002050078
Title Novel Substituted Imidazotriazinones As Pde Ii-Inhibitors.
Abstract The invention relates to novel substituted imidazotriazinones (I), methods for the production thereof, and the use thereof for producing medicaments particularly for improving perception, concentration capacity, learning capacity and/or memory capacity.
Applicant(s) Bayer Ag
Representative Drug(s) D0L0MI Drug Info IC50 = 4.7 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
United States Patent and Trademark Office (USPTO)
Patent ID US20120214791
Title Imidazo[5,1-F][1,2,4]Triazines for The Treatment of Neurological Disorders.
Applicant(s) Pfizer Incorporated
Representative Drug(s) D05UNO Drug Info IC50 = 0.633 nM Click to Show More [1]
2 D00ONN Drug Info IC50 = 1.25 nM [1]
3 D0ET2A Drug Info IC50 = 1.61 nM [1]
4 D0KZ5Q Drug Info IC50 = 2.3 nM [1]
5 D08CEK Drug Info IC50 = 7.89 nM [1]
European Patent Office (EPO)
Patent ID EP1749824
Title Benzodiazepine Derivatives, Their Preparation and Therapeutic Use Thereof.
Applicant(s) Neuro3D
Representative Drug(s) D0TK5G Drug Info IC50 = 6 nM [1]
Patent ID EP1548011
Title Benzo[1,4]Diazepin-2-One Derivatives As Phosphodiesterase Pde2 Inhibitors, Preparation and Therapeutic Use Thereof.
Applicant(s) Neuro3D
Representative Drug(s) D0TK5G Drug Info IC50 = 6 nM [1]
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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