Patent(s) and the Corresponding Patented Drug(s) |
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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 |
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[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 |
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[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) |
D0QE7X |
Drug Info
|
pIC50 = 5.79 |
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[1] |
2
|
D0LI6Z
|
Drug Info
|
pIC50 = 7.47
|
[1] |
3
|
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 |
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[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 |
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[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 |
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[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 |