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65 results about "Metabotropic receptor" patented technology
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A metabotropic receptor is a type of membrane receptor of eukaryotic cells that acts through a second messenger. It may be located at the surface of the cell or in vesicles. Based on their structural and functional characteristics, the neurotransmitter receptor can be classified into two broad categories: metabotropic and ionotropic receptors. Ionotropic receptors form an ion channel pore. In contrast, metabotropic receptors are indirectly linked with ion channels on the plasma membrane of the cell through signal transduction mechanisms, often G proteins. Hence, G protein-coupled receptors are inherently metabotropic. Other examples of metabotropic receptors include tyrosine kinases and guanylyl cyclase receptors.
Novel Thieno-Pyridine and Thieno-Pyrimidine Derivatives and Their Use as Positive Allosteric Modulators of Mglur2-Receptors
The present invention relates to novel compounds, in particular novel thieno-pyridine and thieno-pyrimidine derivatives according to Formula (I), wherein all radicals are defined in the application. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 ("mGluR2") which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
Owner:ORTHO MCNEIL JANSSEN PHARMA
Novel pyridinone derivatives and their use as positive allosteric modulators of mglur2-receptors
The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) X R1 N Y (I) R2 R3 wherein all radicals are defined in the application. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
Owner:ORTHO MCNEIL JANSSEN PHARMA
Novel small molecule potentiators of metabotropic glutamate receptors
ActiveUS20110245247A1Increase mGlu receptor responseFunction increaseBiocideNervous disorderDiseaseAryl
The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula I
wherein X1 is N or C—R1, X2 is N or C—R2, X3 is N or C—R3, X4 is N or C—R4 provided that none or one of X1, X2, X3 or X4 is N; Y1 is N, C or C—R5, Y2 is N, C or C—R6, Y3 is Y1, Y2, N, C or C—R7, Y4 is N, C or C—R8 provided that only the moiety Y1, Y2, Y3 or Y4 to which Z is bound is C and further provided at most one of Y1, Y2, Y3 or Y4 is N; Z is O, S, S(O), S(O)2 or NRZ; Q is CH2 or CH2CH2, where one or two of the hydrogen atoms in CH2 or CH2CH2 may be replaced by halogen, C1-C4-alkyl or C1-C4-haloalkyl; R1 is inter alia hydrogen, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C4-haloalkoxy, C3-C8-cycloalkyl, a radical NR1aR1b, C-bound 3- to 7-membered, saturated heterocyclyl having 1 or 2 nitrogen atoms and 0 or 1 heteroatoms, selected from O and S, as ring members, aryl, aryl-CH2, aryloxy, hetaryl, hetaryloxy or hetaryl-CH2, wherein the heterocyclyl, aryl and hetaryl rings ring in the last six radicals themselves are unsubstituted or carry 1, 2, 3, 4 or 5 identical or different radicals R1c; R2 has one of the meanings given for R1; R3 and R4 are, inter alia, selected from hydrogen, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkyl, phenyl, C1-C4-haloalkoxy, a radical (CH2)nNR′R″; R5, R6, R7, R8 are, independently of each other, selected from hydrogen, halogen, etc.; Ra is C3-C6-cycloalkyl, C1-C6-haloalkyl or C1-C6-alkyl, which is unsubstituted or carries one radical selected from C1-C4-alkoxy, C1-C4-haloalkoxy and a radical NRa1Ra2; and the N-oxides and the pharmaceutically acceptable salts thereof.
Owner:ABBVIE DEUTSHLAND GMBH & CO KG
1, 4-disubstituted 3-cyano-pyridone derivatives and their use as positive allosteric modulators of mglur2-receptors
The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I)
wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
Owner:JANSSEN-CILAG SA +1
3-cyano-4-(4-phenyl-piperidin-1-yl)-pyridin-2-one derivatives
The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
Owner:ADDEX PHARM SA
3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
Owner:ADDEX PHARM SA +1
1,4-disubstituted 3-cyano-pyridone derivatives and their use as positive mglur2-receptor modulators
The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
Owner:ADDEX PHARM SA +1
1,3-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h,1 h-1,4 bipyridinyl-2-ones
The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
Owner:JANSSEN PHARMA INC +1
Novel small molecule potentiators of metabotropic glutamate receptors i
The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula Iwherein X2 is N or C—R2, X3 is N or C—R3, X4 is N or C—R4 provided that none or one of X2, X3 or X4 is N; Y1 is N, C or C—R5, Y2 is N, C or C—R6, Y3 is N, C or C—R7, Y4 is N, C or C—R8 provided that only the moiety Y1, Y2, Y3 or Y4 to which Z is bound is C and further provided at most one of Y1, Y2, Y3 or Y4 is N; Z is O, S, S(O), S(O)2 or NRZ; Q is CH2 or CH2CH2, where one or two of the hydrogen atoms in CH2 or CH2CH2 may be replaced by halogen, C1-C4-alkyl or C1-C4-haloalkyl; R1 is inter alia hydrogen, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C4-haloalkoxy, C3-C8-cycloalkyl, a radical NR1aR1b, C-bound 3- to 7-membered, saturated heterocyclyl having 1 or 2 nitrogen atoms and 0 or 1 heteroatoms, selected from O and S, as ring members, aryl, aryl-CH2, aryloxy, hetaryl, hetaryloxy or hetaryl-CH2, wherein the heterocyclyl, aryl and hetaryl rings ring in the last six radicals themselves are unsubstituted or carry 1, 2, 3, 4 or 5 identical or different radicals R1c; R2, R3 and R4 are, inter alia, selected from hydrogen, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkyl, phenyl, C1-C4-haloalkoxy, a radical (CH2)nNR′R″; R5, R6, R7, R8 are, independently of each other, selected from hydrogen, halogen, etc.; Ra is C3-C6-cycloalkyl, C1-C6-haloalkyl or C1-C6-alkyl, which is unsubstituted or carries one radical selected from C1-C4-alkoxy, C1-C4-haloalkoxy and a radical NRa1Ra2, Rb is hydrogen, halogen or C1-C4-alkyl; and the N-oxides and the pharmaceutically acceptable salts thereof.
Owner:ABBVIE DEUTSHLAND GMBH & CO KG
Imidazo[1,2-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
The present invention relates to novel compounds, in particular novel imidazo[1,2-a]piridine derivatives according to Formula (I). The compounds according to the invention are positive allosteric modulators of metabotropic receptors-sub-type 2 (‘mGluR2’) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
![Imidazo[1,2-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors](https://images-eureka.patsnap.com/patent_img/7a615225-622a-4e3f-abde-7173854efe1c/US20110009441A1-20110113-C00001.png "Imidazo[1,2-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors")
![Imidazo[1,2-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors](https://images-eureka.patsnap.com/patent_img/7a615225-622a-4e3f-abde-7173854efe1c/US20110009441A1-20110113-C00002.png "Imidazo[1,2-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors")
![Imidazo[1,2-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors](https://images-eureka.patsnap.com/patent_img/7a615225-622a-4e3f-abde-7173854efe1c/US20110009441A1-20110113-C00003.png "Imidazo[1,2-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors")
Owner:ADDEX PHARM SA
1,3-disubstituted-4-phenyl-1h-pyridin-2-ones
The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
Owner:ADDEX PHARM SA +1
3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors
The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
![3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors](https://images-eureka.patsnap.com/patent_img/8b04a2d6-588d-4ccd-b5d6-e968e664d154/US20110306642A1-20111215-C00001.png "3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors")
![3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors](https://images-eureka.patsnap.com/patent_img/8b04a2d6-588d-4ccd-b5d6-e968e664d154/US20110306642A1-20111215-C00002.png "3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors")
![3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors](https://images-eureka.patsnap.com/patent_img/8b04a2d6-588d-4ccd-b5d6-e968e664d154/US20110306642A1-20111215-C00003.png "3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors")
Owner:ADDEX PHARM SA +1
Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors
The present invention relates to novel compounds, in particular novel indole and benzomorpholine derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
Owner:ADDEX PHARM SA +1
1,3-disubstituted 4-(aryl-x-phenyl)-1h-pyridin-2-ones
The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
Owner:ADDEX PHARM SA +1
Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
The present invention relates to novel indole and benzoxazine derivatives which are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”) and which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
Owner:JANSSEN PHARMA INC +1
1',3'-disubstituted-4-pheny-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones
The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I)wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.![1',3'-disubstituted-4-pheny-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones](https://images-eureka.patsnap.com/patent_img/7ae53444-6c65-4251-85cf-9f1714b8b24d/US20130196992A1-20130801-C00001.png "1',3'-disubstituted-4-pheny-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones")
![1',3'-disubstituted-4-pheny-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones](https://images-eureka.patsnap.com/patent_img/7ae53444-6c65-4251-85cf-9f1714b8b24d/US20130196992A1-20130801-C00002.png "1',3'-disubstituted-4-pheny-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones")
![1',3'-disubstituted-4-pheny-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones](https://images-eureka.patsnap.com/patent_img/7ae53444-6c65-4251-85cf-9f1714b8b24d/US20130196992A1-20130801-C00003.png "1',3'-disubstituted-4-pheny-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones")
Owner:ADDEX PHARM SA +1
7-ARYL-1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
![7-ARYL-1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS](https://images-eureka.patsnap.com/patent_img/31c8fb25-3239-4ae4-bb7d-b77e84d3fc27/US20120184528A1-20120719-C00001.png "7-ARYL-1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS")
![7-ARYL-1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS](https://images-eureka.patsnap.com/patent_img/31c8fb25-3239-4ae4-bb7d-b77e84d3fc27/US20120184528A1-20120719-C00002.png "7-ARYL-1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS")
![7-ARYL-1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS](https://images-eureka.patsnap.com/patent_img/31c8fb25-3239-4ae4-bb7d-b77e84d3fc27/US20120184528A1-20120719-C00003.png "7-ARYL-1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS")
Owner:JANSSEN PHARMA INC +1
1,2,4-triazolo [4,3-A] pyridine derivatives and their use for the treatment of prevention of neurological and psychiatric disorders
The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.![1,2,4-triazolo [4,3-A] pyridine derivatives and their use for the treatment of prevention of neurological and psychiatric disorders](https://images-eureka.patsnap.com/patent_img/d7c7b245-5bc3-42e7-80c0-7e46aa191791/US08937060-20150120-C00001.PNG "1,2,4-triazolo [4,3-A] pyridine derivatives and their use for the treatment of prevention of neurological and psychiatric disorders")
![1,2,4-triazolo [4,3-A] pyridine derivatives and their use for the treatment of prevention of neurological and psychiatric disorders](https://images-eureka.patsnap.com/patent_img/d7c7b245-5bc3-42e7-80c0-7e46aa191791/US08937060-20150120-C00002.PNG "1,2,4-triazolo [4,3-A] pyridine derivatives and their use for the treatment of prevention of neurological and psychiatric disorders")
![1,2,4-triazolo [4,3-A] pyridine derivatives and their use for the treatment of prevention of neurological and psychiatric disorders](https://images-eureka.patsnap.com/patent_img/d7c7b245-5bc3-42e7-80c0-7e46aa191791/US08937060-20150120-C00003.PNG "1,2,4-triazolo [4,3-A] pyridine derivatives and their use for the treatment of prevention of neurological and psychiatric disorders")
Owner:JANSSEN PHARMA INC +1
1,3-disubstituted 4-(aryl-X-phenyl)-1H-pyridin-2-ones
The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I)wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
Owner:ADDEX PHARM SA +1
1,4-disubstituted 3-cyano-pyridone derivatives and their use as positive mGluR2-receptor modulators
The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
Owner:ADDEX PHARM SA +1
1,2,3-triazolo [4,3-a] pyridine derivatives and thier use for the treatment of prevention of neurological and psychiatric disorders
The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
![1,2,3-triazolo [4,3-a] pyridine derivatives and thier use for the treatment of prevention of neurological and psychiatric disorders](https://images-eureka.patsnap.com/patent_img/f2c27e6e-35c3-4b59-9b84-ec0714366fad/US20120184525A1-20120719-C00001.png "1,2,3-triazolo [4,3-a] pyridine derivatives and thier use for the treatment of prevention of neurological and psychiatric disorders")
![1,2,3-triazolo [4,3-a] pyridine derivatives and thier use for the treatment of prevention of neurological and psychiatric disorders](https://images-eureka.patsnap.com/patent_img/f2c27e6e-35c3-4b59-9b84-ec0714366fad/US20120184525A1-20120719-C00002.png "1,2,3-triazolo [4,3-a] pyridine derivatives and thier use for the treatment of prevention of neurological and psychiatric disorders")
![1,2,3-triazolo [4,3-a] pyridine derivatives and thier use for the treatment of prevention of neurological and psychiatric disorders](https://images-eureka.patsnap.com/patent_img/f2c27e6e-35c3-4b59-9b84-ec0714366fad/US20120184525A1-20120719-C00003.png "1,2,3-triazolo [4,3-a] pyridine derivatives and thier use for the treatment of prevention of neurological and psychiatric disorders")
Owner:JANSSEN PHARMA INC +1
mGluR1 antagonists as therapeutic agents
In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1—R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.
Owner:SCHERING CORP
1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones
The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I)wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.![1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones](https://images-eureka.patsnap.com/patent_img/52ce5e06-4d47-4b17-88ae-c360f8e2b2f5/US20130197019A1-20130801-C00001.png "1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones")
![1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones](https://images-eureka.patsnap.com/patent_img/52ce5e06-4d47-4b17-88ae-c360f8e2b2f5/US20130197019A1-20130801-C00002.png "1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones")
![1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones](https://images-eureka.patsnap.com/patent_img/52ce5e06-4d47-4b17-88ae-c360f8e2b2f5/US20130197019A1-20130801-C00003.png "1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones")
Owner:JANSSEN PHARMA INC +1
mGluR1 Antagonists as therapeutic agents
In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.
Owner:SCHERING CORP
Oxazole derivatives as positive allosteric modulators of metabotropic glutamate receptors
The present invention provides new compounds of formula I, wherein P, A, W, B, Q, R1 and R2 are defined as in formula I; invention compounds are positive allosteric modulators of metabotropic receptors—subtype 5 (“mGluR5”) which are useful for the treatment or prevention of central nervous system disorders such as for example: cognitive decline, both positive and negative symptoms in schizophrenia as well as other disorders in which the mGluR5 subtype of glutamate metabotropic receptor is involved.
Owner:ADDEX PHARM SA
1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors
InactiveUS9012448B2Organic active ingredientsNervous disorderAllosteric modulatorMetabotropic glutamate receptor
The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I)wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.![1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors](https://images-eureka.patsnap.com/patent_img/5dfc5c4d-3f20-4882-a275-337c2bc6f9c8/US09012448-20150421-C00001.PNG "1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors")
![1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors](https://images-eureka.patsnap.com/patent_img/5dfc5c4d-3f20-4882-a275-337c2bc6f9c8/US09012448-20150421-C00002.PNG "1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors")
![1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors](https://images-eureka.patsnap.com/patent_img/5dfc5c4d-3f20-4882-a275-337c2bc6f9c8/US09012448-20150421-C00003.PNG "1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors")
Owner:JANSSEN PHARMA INC
1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
InactiveUS8946205B2Treatment and prevention and control and amelioration and reduction of risk of diseaseReduce disease riskBiocideNervous disorderAllosteric modulatorMetabotropic glutamate receptor
The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.![1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors](https://images-eureka.patsnap.com/patent_img/e6472739-307f-477a-aed8-8c71d5f447e1/US08946205-20150203-C00001.PNG "1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors")
![1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors](https://images-eureka.patsnap.com/patent_img/e6472739-307f-477a-aed8-8c71d5f447e1/US08946205-20150203-C00002.PNG "1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors")
![1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors](https://images-eureka.patsnap.com/patent_img/e6472739-307f-477a-aed8-8c71d5f447e1/US08946205-20150203-C00003.PNG "1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors")
Owner:JANSSEN PHARMA INC +1
Pyrrole Derivatives as Positive Allosteric Modulators of Metabotropic Receptors
The present invention relates to new compounds which are Pyrrole derivatives of formula (I) wherein A, B, P, Q5W, R1 and R2 are defined in the description. Invention compounds are useful in the prevention or treatment of central or peripheral nervous system disorders as well as other disorders modulated by mGluR5 receptors.
Owner:ADDEX PHARM SA
Novel thiazoles derivatives and their use as positive allosteric modulators of metabotropic glutamate receptors
The present invention relates to novel compounds of Formula (I), wherein M, P, A and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
Owner:ADDEX PHARM SA
Novel 2-amino-4-pyrazolyl-thiazole derivatives and their use as allosteric modulators of metabotropic glutamate receptors
The present invention relates to novel compounds of Formula (1), wherein M, A and B are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors-subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
Owner:BOLEA CHRISTELLE +5
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