Imidazo[4,5-B]Pyridine-7-Carboxamides 704

The present invention relates to new compounds of formula (I) as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.

Nobel compounds having selective inhibiting effect at gsk3

The present invention relates to new compounds of formula (I) wherein: Z is N and X is CH or N; Y is CONR5; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected from N, O or S; Q is phenyl or a 5 or 6 membered aromatic heterocyclicc ring containing one or more nitrogen atoms; R is C1-6alkylNR10R11 or C1-6alkylazetidine; R10 is hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C0-6alkylC3-6cycloalkyl, C0-6alkylaryl, C0-61alkylheteroaryl or C1-6alkylNR8R9; R11 is C1-6alkylNR8R9, C0-6alkylC3-6cycloalkyl or C0-6alkylheterocycloalkyl; as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.

COMPOUNDS AND THEIR USE AS BACE INHIBITORS

The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. 125-. (canceled)27. The method according to claim 26 , wherein Ris Calkyl.28. The method according to claim 27 , wherein Ris methyl or ethyl.29. The method according to claim 26 , wherein Ris aryl claim 26 , heteroaryl claim 26 , Calkynyl claim 26 , halogen claim 26 , NHC(O)Ror OR claim 26 , wherein:{'sub': '2-6', 'sup': '7', 'said aryl, heteroaryl, or Calkynyl is optionally substituted with one to three R.'}30. The method according to claim 26 , wherein Rand Rare independently hydrogen or heterocyclyl claim 26 , wherein:{'sub': '1-6', 'sup': '8', 'said heterocyclyl is optionally substituted with one or two substituents independently selected from Calkyl or OR.'}31. The method according to claim 26 , wherein Rand R claim 26 , together with the carbon to which they are attached claim 26 , form a ring B claim 26 , wherein ring B is:{'sub': '1-6', 'sup': '8', 'a 3-14 membered cycloalkyl or heterocyclyl monocyclic ring, or a 9-14 membered bicyclic cycloalkyl or heterocyclyl ring; optionally substituted by one or two substituents independently selected from oxo, halogen, Calkyl or OR; and optionally fused with an aryl or ...

Nobel compounds having selective inhibiting effect at gsk3

The present invention relates to new compounds, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy, such as provide compounds having a selective inhibiting effect at GSK3.

Compounds 620

This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.

Cyclohexane-1,2-naphthalene-1,2-imidazol compounds and their use as BACE inhibitors

Cyclohexane-1,2-naphthalene-1,2-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A-related pathologies such as Down's syndrome, -amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.

Derivatives of 5-Aryl-1H-Pyrrolo [2, 3B] Pyridine-3-Carboxamide or 5-Aryl-1H-Pyrrolo [2, 3B] Pyridine-3-Carboxylic Acid

The present invention relates to new compounds of formula I as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.

Compounds and their use as BACE inhibitors

The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A-related pathologies such as Down's syndrome, -amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (mild cognitive impairment), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

Compounds having selective inhibiting effect at GSK3

The present invention relates to new compounds of formula (I) wherein: Z is N and X is CH or N; Y is CONR5; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected from N, O or S; Q is phenyl or a 5 or 6 membered aromatic heterocyclic ring containing one or more nitrogen atoms; R is C1-6alkylNR10R11 or C1-6alkylazetidine; R10 is hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C0-6alkylC3-6cycloalkyl, C0-6alkylaryl, C0-61alkylheteroaryl or C1-6alkylNR8R9; R11 is C1-6alkylNR8R9, C0-6alkylC3-6cycloalkyl or C0-6alkylheterocycloalkyl; as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.

Novel 2-Phenyl-Imidazo[4,5-B]Pyridine Derivatives as Inhibitors of Glycogen Synthase Kinase for the Treatment of Dementia and Neurodegenerative Disorders

Compounds of formula I wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, as a base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, processes for their preparation and new intermediates used therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.

COMPOUNDS AND THEIR USE AS BACE INHIBITORS

The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. 125-. (canceled) The present invention relates to compounds and therapeutically acceptable salts thereof, their pharmaceutical compositions, processes for making them and their use as medicaments for treatment and/or prevention of various diseases. In particular the invention relates to compounds, which are inhibitors of β-secretase and hence inhibit the formation of amyloid β (Aβ) peptides and will be used for treatment and/or prevention of Aβ-related pathologies such as Alzheimer's disease, Down's syndrome and β-amyloid angiopathy, such as but not limited to cerebral amyloid angiopathy, hereditary cerebral hemorrhage, disorders associated with cognitive impairment, such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.The ...

2H-imidazol-4-amine compounds and their use as BACE inhibitors

... 2H-imidazol-4-amine compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A-related pathologies such as Down's syndrome, -amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. methods of therapy, and pharmaceutical compositions containing such compounds.

COMPOUNDS AND THEIR USE AS BACE INHIBITORS

The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. 125-. (canceled)27. The method according to claim 26 , wherein Ris Calkyl.28. The method according to claim 27 , wherein Ris methyl or ethyl.29. The method according to claim 26 , wherein Ris aryl claim 26 , heteroaryl claim 26 , Calkynyl claim 26 , halogen claim 26 , NHC(O)Ror OR claim 26 , wherein:{'sub': '2-6', 'sup': '7', 'said aryl, heteroaryl, or Calkynyl is optionally substituted with one to three R.'}30. The method according to claim 26 , wherein Rand Rare independently hydrogen or heterocyclyl claim 26 , wherein:{'sub': '1-6', 'sup': '8', 'said heterocyclyl is optionally substituted with one or two substituents independently selected from Calkyl or OR.'}31. The method according to claim 26 , wherein Rand R claim 26 , together with the carbon to which they are attached claim 26 , form a ring B claim 26 , wherein ring B is:{'sub': '1-6', 'sup': '8', 'a 3-14 membered cycloalkyl or heterocyclyl monocyclic ring, or a 9-14 membered bicyclic cycloalkyl or heterocyclyl ring; optionally substituted by one or two substituents independently selected from oxo, halogen, Calkyl or OR; and optionally fused with an aryl or ...

Novel Compounds Having Selective Inhibiting Effect at GSK3

Compounds of formula I wherein Z, X, Y, ring P, ring Q, R, R3, R4, n and m are as defined in the specification, as a free base or a pharmaceutically acceptable salt, solvate or solvate of a salt; processes for their preparation and new intermediates used therein, pharmaceutical formulations containing said compounds, and the use of said compounds in therapy.

Novel Compounds Having Selective Inhibiting Effect at GSK3

The present invention relates to new compounds of formula I wherein Z is N; Y is CONR5, NR5CO, SO2NR5, NR5SO2, CH2NR5, NR5, NR5CONR5, CH2CO, CO, O or CH2O; X is CH or N; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected from N, O or S and said phenyl ring or 5 or 6 membered heteroaromatic ring may optionally be fused with a 5 or 6 membered saturated, partially saturated or unsaturated ring containing one or more atoms selected from C, N, O or S; Q is C1-6alkyl, C2-6alkenyl or C2-6alkynyl, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy, such as provide compounds having a selective inhibiting effect at GSK3.

Cycloalkyl ether compounds and their use as BACE inhibitors

Cycloalkyl ether compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A-related pathologies such as Down's syndrome, -amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration and pharmaceutical compositions containing such compounds.

COMPOUNDS AND THEIR USE AS BACE INHIBITORS

The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. 125-. (canceled)27. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00026', 'claim 26'}, 'a therapeutically effective amount of a compound or a pharmaceutically acceptable salt thereof according to ; and'}at least one pharmaceutically acceptable excipient, carrier r diluent.28. A method of treating Alzheimer's Disease in a patient in need thereof claim 26 , wherein the method comprises administering to said patient a therapeutically effective amount of a compound or a pharmaceutically acceptable salt thereof according to .29. A method of treating Alzheimer's Disease in a patient in need thereof claim 27 , wherein the method comprises administering to said patient a therapeutically effective amount of a pharmaceutical composition according to . The present invention relates to compounds and therapeutically acceptable salts thereof, their pharmaceutical compositions, processes for making them and their use as medicaments for treatment and/or prevention of various diseases. In particular the invention relates to compounds, which are inhibitors of β-secretase and hence inhibit the formation of amyloid ...

Compounds having selective inhibiting effect at GSK3

Selective phenyl substituted aminopyrazine inhibitors of GSK3 useful for the prevention and/or treatment of cognitive disorders.

Compounds and Their Use as BACE Inhibitors

The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. 125-. (canceled)27. A compound according to or a pharmaceutically acceptable salt thereof claim 26 , wherein Ris Calkyl.28. A compound according to or a pharmaceutically acceptable salt thereof claim 27 , wherein Ris methyl or ethyl.29. A compound according to or a pharmaceutically acceptable salt thereof claim 26 , wherein Ris aryl claim 26 , heteroaryl claim 26 , Calkynyl claim 26 , halogen claim 26 , NHC(O)Ror ORwherein:{'sub': '2-6', 'sup': '7', 'said aryl, heteroaryl, or Calkynyl is optionally substituted with one to three R.'}30. A compound according to or a pharmaceutically acceptable salt thereof claim 26 , wherein Rand Rare independently hydrogen or heterocyclyl wherein:{'sub': '1-6', 'sup': '8', 'said heterocyclyl is optionally substituted with one or two substituents independently selected from Calkyl or OR.'}31. A compound according to or a pharmaceutically acceptable salt thereof claim 26 , wherein Rand R claim 26 , together with the carbon to which they are attached claim 26 , form a ring B claim 26 , wherein ring B is:{'sub': '1-6', 'sup': '8', 'a 3-14 membered cycloalkyl or heterocyclyl monocyclic ring, ...

Compounds and their use as BACE inhibitors

The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A-related pathologies such as Down's syndrome, -amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (mild cognitive impairment), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

Cyclohexane-1,2-indene-1,2-imidazol compounds and their use as BACE inhibitors

Cyclohexane-1,2-indene-1,2-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A-related pathologies such as Down's syndrome, -amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.

Compounds and their use as BACE inhibitors

The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

Novel Imidazo [4,5-b] Pyridine Derivatives as Inhibitors of Glycogen Synthase Kinase 3 for Use in the Treatment of Dementia and Neurodegenerative Disorders

Compounds of formula I wherein X is or Y; and wherein A, Y, R1, R2, R3, R4 and R5 are as defined in the specification as a base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, processes for their preparation, new intermediates used therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.

Compounds and their use as BACE Inhibitors

The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

2H-Imidazol-4-Amine Compounds and Their Use as Bace Inhibitors

2H-imidazol-4-amine compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. methods of therapy, and pharmaceutical compositions containing such compounds. 2. A compound according to selected from the group consisting of:(1r,4r)-4″-Amino-5″-methyl-6′-(2-methylpropoxy)-3′H-dispiro[cyclohexane-1,2′-indene-1′,2″-imidazol]-4-ol;(1r, 1′R,4R)-4″-Amino-5″-methyl-6′-(2-methylpropoxy)-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4-ol;(1r,1′S,4S)-4″-Amino-5″-methyl-6′-(2-methylpropoxy)-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4-ol;(1r,4r)-6′-(2,2-Difluoropropoxy)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r,4r)-4″-Amino-6′-bromo-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4-ol;(1r,1′R,4R)-4″-Amino-6′-bromo-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4-ol;(1r,1′S,4S)-4″-Amino-6′-bromo-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4-ol;(1r,4r)-6′-(Cyclobutylethynyl)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1′,2″-imidazol]-4″-amine;(1r,1′R,4R)-6′-(Cyclobutylethynyl)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r,1′S,4S)-6′-(Cyclobutylethynyl)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r,4r)-4-Methoxy-5″-methyl-6′-(3-methylbut-1-yn-1-yl)-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r,1′R,4R)-4-Methoxy-5″-methyl-6′-(3-methylbut-1-yn-1-yl)-3′ ...

Cyclohexane-1,2'-Indene-1',2"-Imidazol Compounds and Their Use as Bace Inhibitors

Cyclohexane-1,2′-indene-1′,2″-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.

Cyclohexane-1,2'-Naphthalene-1',2"-Imidazol Compounds and Their Use as Bace

Cyclohexane-1,2′-naphthalene-1′,2″-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds. 2. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Calkyl.3. A compound according to claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris methyl or ethyl.4. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris aryl claim 1 , heteroaryl claim 1 , Calkynyl claim 1 , halogen claim 1 , NHC(O)Ror OR claim 1 , wherein said aryl claim 1 , heteroaryl claim 1 , or Calkynyl is optionally substituted with one to three R.5. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare independently hydrogen claim 1 , Ccycloalkyl or heterocyclyl wherein said Ccycloalkyl or heterocyclyl is optionally substituted with one or two substituents independently selected from Calkyl or OR.6. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rtogether with the carbon to which they are attached claim 1 , form a ring B claim 1 , which is a 3-14 membered cycloalkyl or heterocyclyl monocyclic ring; and wherein ring B is optionally substituted by one or two substituents independently selected from oxo claim 1 , halogen claim 1 , Calkyl or OR ...

Cycloalkyl Ether Compounds and Their Use as Bace Inhibitors

Cycloalkyl ether compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration and pharmaceutical compositions containing such compounds. 2. A compound according to selected from the group consisting of:(1r,4r)-4-Methoxy-5″-methyl-6′-[(1-methylcyclopropyl)methoxy]-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r,4r)-6′-[(3,3-Difluorocyclobutyl)methoxy]-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1′,2″-imidazol]-4″-amine;(1r,4r)-6′-(Cyclopropylmethoxy)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r, 1′R,4R)-6′-(Cyclopropylmethoxy)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r, 1′S,4S)-6′-(Cyclopropylmethoxy)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r,4r)-6′-[(2,2-Difluorocyclopropyl)methoxy]-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1′,2″-imidazol]-4″-amine;(1r,4r)-6′-(Cyclobutylmethoxy)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1 r, 1′R,4R)-6′-(Cyclobutylmethoxy)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r, 1′S,4S)-6′-(Cyclobutylmethoxy)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine, and(1r,4r)-6′-(2-Cyclopropylethoxy)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine,or a pharmaceutically acceptable salt of any foregoing compound.3. A ...

BIS(SULFONAMIDE) DERIVATIVES AND THEIR USE AS MPGES INHIBITORS

The present invention relates to bis(sulfonamide) compounds and pharmaceutically acceptable salts thereof. The present invention also relates to pharmaceutical compositions comprising these compounds and to their use as a medicament for the treatment and/or prevention of a disease, disorder or condition in which modulation of microsomal prostaglandin E synthase-1 activity is beneficial, such as pain, inflammation and cancer. 2. The compound of formula (I) according to claim 1 , whereinA is phenyl, indolyl or dihydroindolyl;{'sup': '1', 'sub': '2', 'Ris H or —CHOH;'}{'sup': 2', '4, 'sub': 1-4', '1-4, 'Ris H, bromine, chlorine, fluorine, C-alkyl, fluoro-C-alkyl or —C≡C—R;'}{'sup': '3', 'sub': 1-4', '1-4, 'Ris H, bromine, chlorine, fluorine, C-alkyl, C-alkoxy, cyano or oxo; and'}{'sup': '4', 'sub': 1-4', '3-7', '1-4, 'Ris C-alkyl, C-cycloalkyl or phenyl, wherein phenyl is optionally substituted with C-alkyl.'}3. The compound of formula (I) according to claim 1 , whereinA is phenyl, indolyl or dihydroindolyl;{'sup': '1', 'Ris H;'}{'sup': '2', 'Ris chlorine; and'}{'sup': '3', 'sub': 1-2', '1-2, 'Ris H, C-alkyl, C-alkoxy, cyano or oxo.'}4. The compound of formula (I) according to claim 1 , whereinA is phenyl;{'sup': '1', 'sub': '2', 'Ris H or —CHOH;'}{'sup': '2', 'sub': 1-4', '1-4, 'Ris H, chlorine, C-alkyl or fluoro-C-alkyl; and'}{'sup': '3', 'sub': 1-2', '1-2, 'Ris H, C-alkyl, C-alkoxy, cyano or oxo.'}5. The compound of formula (I) according to claim 1 , wherein A is phenyl and Ris H.6. The compound of formula (I) according to claim 1 , wherein A is indolyl or dihydroindolyl and Ris H.7. The compound of formula (I) according to claim 1 , wherein Ris chlorine.8. A compound claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , selected from the group consisting of2-(2-(4-chloro-2-phenethoxyphenyl)ethylsulfonamido)benzenesulfonamide,2-(2-(4-chloro-2-(2-methoxyphenethoxy)phenyl)ethylsulfonamido)benzenesulfonamide,2-(2-(4-chloro-2-(3-methoxyphenethoxy)phenyl) ...

BIS(SULFONAMIDE) DERIVATIVES AND THEIR USE AS MPGES INHIBITORS

The present invention relates to bis(sulfonamide) compounds and pharmaceutically acceptable salts thereof. The present invention also relates to pharmaceutical compositions comprising these compounds and to their use as a medicament for the treatment and/or prevention of a disease, disorder or condition in which modulation of microsomal prostaglandin E synthase-1 activity is beneficial, such as pain, inflammation and cancer. 2. The compound of formula (I) according to claim 1 , wherein{'sup': '1', 'sub': '2', 'Ris H or —CHOH;'}{'sup': 2', '3, 'sub': 1-4', '1-4, 'Ris H, halogen, C-alkyl, fluoro-C-alkyl or —C≡C—R;'}{'sup': '3', 'sub': 1-4', '3-7', '1-4, 'Ris C-alkyl, C-cycloalkyl or phenyl, wherein phenyl is optionally substituted with one or more C-alkyl;'}{'sub': 2', '2', '2, 'sup': '4', 'X is CH, CHF, CF, O, S, SO, SO, NH or NR; and'}{'sup': '4', 'sub': '1-4', 'Ris Calkyl.'}3. The compound of formula (I) according to claim 1 , wherein{'sup': '1', 'sub': '2', 'Ris H or —CHOH;'}{'sup': 2', '3, 'sub': 3', '3, 'Ris bromine, chlorine, fluorine, CH, CFor —C≡C—R;'}{'sup': '3', 'sub': 1-4', '3-7', '1-4, 'Ris C-alkyl, C-cycloalkyl or phenyl, wherein phenyl is optionally substituted with one or more C-alkyl; and'}{'sub': 2', '2, 'X is CH, CFor O.'}4. The compound of formula (I) according to claim 1 , wherein{'sup': '1', 'sub': '2', 'Ris H or —CHOH;'}{'sup': 2', '3, 'sub': 3', '3, 'Ris bromine, chlorine, fluorine, CH, CFor —C≡C—R;'}{'sup': '3', 'sub': '3', 'Ris tert-butyl, iso-propyl, cyclobutyl, cyclopropyl, cyclopentyl, phenyl, wherein phenyl is optionally substituted with a CHgroup; and'}{'sub': '2', 'X is CFor O.'}5. The compound of formula (I) according to claim 1 , wherein Ris —CHOH.6. The compound of formula (I) according to claim 1 , wherein Ris chlorine.7. The compound of formula (I) according to claim 1 , wherein X is O.8. A compound claim 1 , or a pharmaceutically acceptable salt thereof selected from the group consisting of2-[(2-[4-Bromo-2-(tetrahydro-2H-pyran-4- ...

Novel compounds having selective inhibiting effect at GSK3

Disclosed are compounds of formula (I) wherein: Z is N; P is phenyl; Y is CONR5, NR5CO, SO2NR5, NR5SO2, CH2NR5, NR5CONR5, CH2CO, CO or CH2O; X is N; P is phenyl; Q is alkyl, alkenyl or alkynyl; R is C0-6alkyl(SO2)NR1R2; and the remainder of the substituents are as described in the specification. Compounds of the type disclosed have a selective inhibiting effect on glycogen synthase kinase 3 (GSK3) and are useful for the treatment or prevention of diseases such as Alzheimer's disease, Parkinson's disease, frontotemporal dementia Parkinson's type, Parkinson dementia complex of Guam, HIV dementia, diseases with associated neurofibrillar tangle pathologies and dementia pugilistica.

New compounds ii

The present invention relates to new compounds of formula (I) as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.

Novel compounds having selective inhibiting effect at GSK3

Disclosed is a compound having formula I wherein: Z is N; Y is CONR5, NR5CO, SO2NR5, NR5CH2, NR5CONR5, C1-6alkylene, CH2CO, COCH2, CH=CH, OCH2 or CH2O; X is CH or N; P is phenyl or a 6 membered heteroaromatic ring containing one or more heteroatoms independently selected from N, O or S and said phenyl ring or heteroaromatic ring may optionally be fused with a 5 or 6 membered saturated, partially saturated or unsaturated ring containing one or more atoms selected from C, N, O or S; Q is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more nitrogen atoms and said phenyl ring or heteroaromatic ring may optionally be fused with a 5 or 6 membered saturated, partially saturated or unsaturated ring containing one or more atoms selected from C, N, O or S; R is C1-6alkylNR1-R11 or C1-6alkylazetidine which azetidine ring may be optionally substituted by A; and the remainder of the substituents are as described in the specification. Also disclosed is the use of the above compound in the manufacture of a medicament for the prevention and/or treatment of diseases or disorders of the nervous system or for hyperglycaemia or for contraception or for baldness.

NEW COMPOUNDS 578.

La presente invención se refiere a nuevos compuestos de fórmula (I) y su composiciones farmacéuticas. Adicionalmente, la presente invención se refiere a métodos terapéuticos para el tratamiento y/o prevención de patologías relacionadas con Abeta tales como síndrome de Down, angiopatía 13-amiloide tal como, a modo no taxativo, angiopatía amiloide cerebral o hemorragia cerebral hereditaria, trastornos asociados con deficiencia cognitiva tales como, a modo no taxativo, deterioro cognitivo leve, enfermedad de Alzheimer, pérdida de memoria, síntomas de déficit atencional asociados con la enfermedad de Alzheimer, neurodegeneración asociada con enfermedades tales como enfermedad de Alzheimer o demencia, incluyendo demencia de origen mixto vascular y degenerativo, demencia presenil, demencia senil y demencia asociada con la enfermedad de Parkinson, parálisis supranuclear progresiva o degeneración córtico-basal.

New 2-phenylimidazo [4,5-b] pyridine derivatives as inhibitors of glycogen synthase kinase for the treatment of dementia and neurodegenerative disorders

Foreliggende oppfinnelse angår nye forbindelser med formel (I) som en fri base eller et farmasøytisk akseptabelt salt, solvat eller solvat av et salt derav, en fremgangsmåte for deres fremstilling og nye intermediater anvendt deri, farmasøytiske formuleringer som inneholder nevnte terapeutisk aktive forbindelser og anvendelse av nevnte aktive forbindelser ved behandling.

5h-pyrrolo [ 3, 4-b] pyridin derivatives and their use

The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

Cycloalkyl ether compounds and their use as bace inhibitors

Cycloalkyl ether compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Αβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration and pharmaceutical compositions containing such compounds. Formula (I) wherein A is -O-, or -CH2-, n is 0 or 1.

Novel imidazo [4,5 -b] pyridine derivatives as inhibitors of glycogen synthase kinase 3 for use in the treatment of dementia and neurodegenerative disorders

COMPOUNDS AND ITS USE AS BACE INHIBITORS

La presente invención se refiere a compuestos de fórmula (I) y sus composiciones farmacéuticas. Asimismo, la presente invención se refiere a métodos terapéuticos para el tratamiento y/o la prevención de patologías relacionadas con A?, como síndrome de Down, angiopatía ?-amiloide como, a modo no taxativo, angiopatía amiloide cerebral o hemorragia cerebral hereditaria, trastornos asociados con el deterioro cognitivo como, a modo no taxativo, MCI ("deterioro cognitivo leve"), mal de Alzheimer, pérdida de memoria, síntomas de déficit de atención asociados con mal de Alzheimer, neurodegeneración asociada con enfermedades como mal de Alzheimer o demencia, incluida demencia de origen vascular y degenerativo mixto, demencia presenil, demencia senil y demencia asociada con mal de Parkinson, parálisis supranuclear progresiva o degeneración corticobasal.

SUBSTITUTED DERIVATIVES OF 3H-IMIDAZOL- (4.5 B (BETA)) PIRIDINA-2-IL BENZOATES AND BENZAMIDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND APPLICATIONS

La presente invención se refiere a nuevos compuestos de fórmula I en donde X es como una base libre o una sal farmacéuticamente aceptable, solvato o solvato de sal del mismo, un proceso para su preparación y nuevos intermediarios usados en la misma, formulaciones farmacéuticas que contienen dichos compuestos terapéuticamente activos y el uso de dichos compuestos activos en terapia. The present invention relates to new compounds of formula I wherein X is as a free base or a pharmaceutically acceptable salt, solvate or solvate thereof, a process for its preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and the use of said active compounds in therapy.

New derivatives of 5-aryl-1h-pyrrolo [2, 3b] pyridine-3-carboxamide or 5-aryl-1h-pyrrolo [2, 3b] pyridine-3-carboxylic acid

The present invention relates to new compounds of formula I as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.

New compounds 575

The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

Bis (sulfonamide) derivatives and their use as mpges inhibitors

Compounds having selective inhibiting effect at GSK3

The present invention relates to new compounds of formula I wherein: Z is N and X is CH or N; Y is CONR 5 ; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected from N, O or S; Q is phenyl or a 5 or 6 membered aromatic heterocyclicc ring containing one or more nitrogen atoms; R is C 1-6 alkylNR 10 R 11 or C 1-6 alkylazetidine; R 10 is hydrogen, C 1 - 6 alkyl, C 2-6 alkenyl, C 2 - 6 alkynyl, C 0 - 6 alkylC 3 - 6 cycloalkyl, C 0 - 6 alkylaryl, C 0 - 6 alkylheteroaryl or C 1 - 6 alkylNR 8 R 9 ; R 11 is C 1 - 6 alkylNR 8 R 9 , C 1 - 6 alkylC 3 - 6 cycloalkyl or C 0 - 6 alkylheterocycloalkyl; as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.

Cyclohexane-1,2'-naphthalene-1',2"-imidazole compounds and their use as bace inhibitors

Cyclohexane-1,2'-naphthalene-1',2''-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aß-related pathologies such as Down's syndrome, ß-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.

Compounds and their use as bace inhibitors

Un compuesto que es (1r,1'R,4R)-4-metoxi-5''-metil-6'-[5-(prop-1-in-1-il)piridin-3-il]-3'H-diespiro[ciclohexano-1,2'- indeno-1',2''-imidazol]-4''-amina:**Fórmula** o una sal farmacéuticamente aceptable de esto. A compound that is (1r, 1'R, 4R) -4-methoxy-5 '' - methyl-6 '- [5- (prop-1-in-1-yl) pyridin-3-yl] -3' H-diespiro [cyclohexane-1,2'-indene-1 ', 2' '-imidazole] -4' '-amine: ** Formula ** or a pharmaceutically acceptable salt thereof.

New compounds 578

The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

Bis(sulfonamide) derivatives and their use as mpges inhibitors

Novel imidazo [4,5 -b] pyridine derivatives as inhibitors of glycogen synthase kinase 3 for use in the treatment of dementia and neurodegenerative disorders

The present invention relates to new compounds of formula (I) Wherein X is or Y; as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.

DERIVATIVES OF ISOINDOL AS BACE INHIBITORS

SE REFIERE A COMPUESTOS DERIVADOS DE 4-FLUORO-1H-ISOINDOL-3-AMINA DE FORMULA (I) DONDE R1 ES HALOGENO, CN, ALQUILO(C1-C6), ALQUENILO(C2-C6), ENTRE OTROS; A ES ARILO O HETEROARILO OPCIONALMENTE SUSTITUIDO CON R5, EN DONDE R5 ES HALOGENO, CN, CICLOALQUILO(C3-C6), ENTRE OTROS; B ES ARILO O HETEROARILO OPCIONALMENTE SUSTITUIDO CON R6, EN DONDE R6 ES HALOGENO, HIDROXI O CN; C ES H, HALOGENO, CICLOALQUILO(C3-C6), HETEROCICLILO, ENTRE OTROS; m ES DE 0 A 2. SON COMPUESTOS PREFERIDOS: 5-(3-(3-AMINO-4-FLUORO-1-(2-METILPIRIDIN-4-IL)-1H-ISOINDOL-1-IL)-4-FLUOROFENIL)NICOTINONITRILO; 4-FLUORO-1-(2-FLUORO-5-(5-FLUOROPIRIDIN-3-IL)FENIL)-1-(2-METILPIRIDIN-4-IL)-1H-ISOINDOL-3-AMINA; 4-FLUORO-1-(2-FLUORO-5-(PIRIMIDIN-5-IL)FENIL)-1-(2-(TRIFLUOROMETIL)PIRIDIN-4-IL)-1H-ISOINDOL-3-AMINA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA B-SECRETASA (BACE) SIENDO UTILES EN EL TRATAMIENTO DEL SINDROME DE DOWN, ENFERMEDAD DE ALZHEIMER, ANGIOPATIA AMILOIDE CEREBRAL, DEMENCIA SENIL REFERS TO COMPOUNDS DERIVED FROM 4-FLUORO-1H-ISOINDOL-3-AMINE FROM FORMULA (I) WHERE R1 IS HALOGEN, CN, ALKYL (C1-C6), ALKENYL (C2-C6), AMONG OTHERS; A IS ARYL OR HETEROARILO OPTIONALLY SUBSTITUTED WITH R5, WHERE R5 IS HALOGEN, CN, CYCLOALKYL (C3-C6), AMONG OTHERS; B IS ARYL OR HETEROARILO OPTIONALLY SUBSTITUTED WITH R6, WHERE R6 IS HALOGEN, HYDROXY OR CN; C IS H, HALOGEN, CYCLOALKYL (C3-C6), HETEROCYCLYL, AMONG OTHERS; m IS FROM 0 TO 2. PREFERRED COMPOUNDS ARE: 5- (3- (3-AMINO-4-FLUORO-1- (2-METHYLPYRIDIN-4-IL) -1H-ISOINDOL-1-IL) -4-FLUOROPHENYL) NICOTINONITRILE; 4-FLUORO-1- (2-FLUORO-5- (5-FLUOROPYRIDIN-3-IL) PHENYL) -1- (2-METHYLPYRIDIN-4-IL) -1H-ISOINDOL-3-AMINE; 4-FLUORO-1- (2-FLUORO-5- (PYRIMIDIN-5-IL) PHENYL) -1- (2- (TRIFLUOROMETHYL) PYRIDIN-4-IL) -1H-ISOINDOL-3-AMINE; AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE INHIBITORS OF B-SECRETASE (BACE) BEING USEFUL IN THE TREATMENT OF DOWN'S SYNDROME, ALZHEIMER'S ...

COMPOUNDS DERIVED FROM SPIRO 1’,2’’-IMIDAZOLE AND THEIR USE AS INHIBITORS OF beta-SECRETASE (BACE)

La presente invención se refiere a compuestos de fórmula (I) derivados de espiro 1’,2’’-imidazol y sus composiciones farmacéuticas. Un ejemplo de estos compuestos es el compuesto de fórmula Asimismo, la presente invención se refiere al uso de estos compuestos como inhibidores de beta-secretasa (BACE) para el tratamiento y/o la prevención de patologías relacionadas con Aß, como síndrome de Down, angiopatía ß-amiloide como, a modo no taxativo, angiopatía amiloide cerebral o hemorragia cerebral hereditaria, trastornos asociados con el deterioro cognitivo como, a modo no taxativo, MCI ("deterioro cognitivo leve"), mal de Alzheimer, pérdida de memoria, síntomas de déficit de atención asociados con mal de Alzheimer, neurodegeneración asociada con enfermedades como mal de Alzheimer o demencia, incluida demencia de origen vascular y degenerativo mixto, demencia presenil, demencia senil y demencia asociada con mal de Parkinson, parálisis supranuclear progresiva o degeneración corticobasal.

New imidazo[ 4,5-b]pyridine-7-carboxamides 704

The present invention relates to new compounds of formula (I) as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.

Cyclohexane-1,2'-indene-1',2"-imidazol compounds and their use as bace inhibitors

Cyclohexane-1,2'-indene-1',2''-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.

Bis(sulfonamide) derivatives and their use as mpges inhibitors

The present invention relates to bis(sulfonamide) compounds and pharmaceutically acceptable salts thereof. The present invention also relates to pharmaceutical compositions comprising these compounds and to their use as a medicament for the treatment and/or prevention of a disease, disorder or condition in which modulation of microsomal prostaglandin E synthase-1 activity is beneficial, such as pain, inflammation and cancer.

Cyclohexane-1,2'-indene-1',2"-imidazol compounds and their use as bace inhibitors

Cyclohexane-1,2'-indene-1',2''-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.

Compounds and their use as bace inhibitors

The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A?~-related pathologies such as Down's syndrome, amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral haemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. FIG. 1A