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180 results about "Β secretase" patented technology
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Amino-5-[4-(difluoromehtoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of beta-secretase
![Amino-5-[4-(difluoromehtoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of beta-secretase](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/9b458263-f0d6-4bd1-8869-72f2e272686a/US20070072925A1-20070329-C00001.png "Amino-5-[4-(difluoromehtoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of beta-secretase")
![Amino-5-[4-(difluoromehtoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of beta-secretase](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/9b458263-f0d6-4bd1-8869-72f2e272686a/US20070072925A1-20070329-C00002.png "Amino-5-[4-(difluoromehtoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of beta-secretase")
![Amino-5-[4-(difluoromehtoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of beta-secretase](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/9b458263-f0d6-4bd1-8869-72f2e272686a/US20070072925A1-20070329-C00003.png "Amino-5-[4-(difluoromehtoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of beta-secretase")
Owner:WYETH LLC
Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation
Owner:WYETH LLC
Dihydrospiro[dibenzo[a,d][7]annulene-5,4'-imidazol] compounds for the inhibition of beta-secretase
![Dihydrospiro[dibenzo[a,d][7]annulene-5,4'-imidazol] compounds for the inhibition of beta-secretase](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/ff3938b9-266f-464f-a99f-be2342573144/US20070203116A1-20070830-C00001.png "Dihydrospiro[dibenzo[a,d][7]annulene-5,4'-imidazol] compounds for the inhibition of beta-secretase")
![Dihydrospiro[dibenzo[a,d][7]annulene-5,4'-imidazol] compounds for the inhibition of beta-secretase](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/ff3938b9-266f-464f-a99f-be2342573144/US20070203116A1-20070830-C00002.png "Dihydrospiro[dibenzo[a,d][7]annulene-5,4'-imidazol] compounds for the inhibition of beta-secretase")
![Dihydrospiro[dibenzo[a,d][7]annulene-5,4'-imidazol] compounds for the inhibition of beta-secretase](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/ff3938b9-266f-464f-a99f-be2342573144/US20070203116A1-20070830-C00003.png "Dihydrospiro[dibenzo[a,d][7]annulene-5,4'-imidazol] compounds for the inhibition of beta-secretase")
Owner:WYETH
Cyclic amine bace-1 inhibitors having a benzamide substituent
ActiveUS20050119227A1Inhibition formationBiocideNervous disorderHMG-CoA reductaseNeuro-degenerative disease
Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein [0001]R1 is [0002]R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
Owner:PHARMACOPEIA DRUG DISCOVERY +1
4,5-dihydro-oxazol-2-yl amine derivatives
The present invention relates to a compounds of formula Iwherein R1, R1′, R2, R3, R4, X, Ar, and m are as defined in the specification and claims and pharmaceutically active acid addition salts thereof. Compounds of the invention have Asp2 (β-secretase, BACE 1 or Memapsin-2) inhibitory activity and are useful for the treatment of diseases characterized by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
Owner:F HOFFMANN LA ROCHE INC +1
Inhibition of Abeta production by beta-secretase BACE2
InactiveUS7183070B2Suppressed Aβ productionPromoting alternative non-amyloidogenic APP processing pathwayCompound screeningNervous disorderΒ amyloidAmyloid deposition
The present invention is based on the findings that BACE2, a homolog of β-secretase BACE, is able to stimulate processing of APP in a non-amyloidogenic pathway, thereby suppressing the level of Aβ. Accordingly, the present invention provides methods and means for the identification and use of modulators of this unique activity of BACE2 to suppress Aβ production. The compounds identified using the methods and means provided herein may be used as potential candidates for the treatment of Alzheimer's disease and other neurological diseases by reducing β-amyloid deposit formation.
Owner:SCIOS
Novel curcumin derivative
InactiveUS20100048901A1Prevention or treatment of Alzheimer's diseaseReduce usageOrganic active ingredientsNervous disorderNeuronMedicinal chemistry
The present invention provides a novel compound that is structurally similar to curcumin and has a suppressive effect on Aβ aggregation, a degradative effect on Aβ aggregates, an inhibitory effect on β-secretase, and a protective effect on neurons. The novel compound is a compound represented by the following general formula (Ia) or a salt thereof:wherein R1 represents a 4-hydroxy-3-methoxyphenyl group or the like, and R2 represents a 1H-indol-6-yl group or the like.
Owner:TOKYO INST OF TECH +1
Macrocyclic beta-secretase inhibitors
Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, n and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
Owner:MERCK SHARP & DOHME LLC
Substituted amide beta secretase inhibitors
Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
Owner:MERCK SHARP & DOHME LLC
Aminoacetamide acyl guanidines as beta-secretase inhibitors
There is provided a series of substituted acyl guanidines of Formula (Ik) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R2, R3, R4, R5, R25, R26 and R27 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
Owner:BRISTOL MYERS SQUIBB CO
Dihydrospiro[dibenzo[a,d][7]annulene-5,4'-imidazol] compounds for the inhibition of beta-secretase
![Dihydrospiro[dibenzo[a,d][7]annulene-5,4'-imidazol] compounds for the inhibition of beta-secretase](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/b3b16ac0-78ff-4919-8c2f-d4e4f94a8c23/US07582667-20090901-C00001.png "Dihydrospiro[dibenzo[a,d][7]annulene-5,4'-imidazol] compounds for the inhibition of beta-secretase")
![Dihydrospiro[dibenzo[a,d][7]annulene-5,4'-imidazol] compounds for the inhibition of beta-secretase](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/b3b16ac0-78ff-4919-8c2f-d4e4f94a8c23/US07582667-20090901-C00002.png "Dihydrospiro[dibenzo[a,d][7]annulene-5,4'-imidazol] compounds for the inhibition of beta-secretase")
![Dihydrospiro[dibenzo[a,d][7]annulene-5,4'-imidazol] compounds for the inhibition of beta-secretase](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/b3b16ac0-78ff-4919-8c2f-d4e4f94a8c23/US07582667-20090901-C00003.png "Dihydrospiro[dibenzo[a,d][7]annulene-5,4'-imidazol] compounds for the inhibition of beta-secretase")
Owner:WYETH LLC
2-amino-3,4-dihydro-quinoline derivatives useful as inhibitors of beta-secretase (BACE)
The present invention is directed to 2-amino-3,4-dihydro-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of β-secretase, also known as β-site cleaving enzyme and BACE, BACE1, Asp2 and memapsin2.
Owner:JANSSEN PHARMA NV
Amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of beta-secretase
![Amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of beta-secretase](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/2d08bfba-45d2-4379-9f8f-c77c18ae1003/US07423158-20080909-C00001.png "Amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of beta-secretase")
![Amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of beta-secretase](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/2d08bfba-45d2-4379-9f8f-c77c18ae1003/US07423158-20080909-C00002.png "Amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of beta-secretase")
![Amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of beta-secretase](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/2d08bfba-45d2-4379-9f8f-c77c18ae1003/US07423158-20080909-C00003.png "Amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of beta-secretase")
Owner:WYETH LLC
Novel phenylcarboxyamides as beta-secretase inhibitors
There is provided a series of novel phenylcarboxyamides of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and Y as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
Owner:BRISTOL MYERS SQUIBB CO
Methods and compositions for detecting and quantifying sappb
InactiveUS20090162878A1Treating and preventing and ameliorating effectEfficient modulationImmunoglobulins against animals/humansBiological material analysisBiochemistryΒ amyloid
The present invention provides methods (assays) for detecting and / or quantifying sAPPβ, a secreted β-secretase (BACE1) cleavage fragment of the β-amyloid precursor protein (APP), in a biological sample. One such method includes contacting a biological sample with a first antibody that selectively binds to a BACE1 cleavage site on sAPPβ and detecting the presence of the antibody. Also provided are compositions, including antibodies that selectively bind to the BACE1 cleavage site of sAPPβ. Kits containing such compositions are also provided. Methods of diagnosing a neurodegenerative disease, such as AD, using the methods and compositions of the present invention are further provided. Methods for identifying BACE1 modulators, candidate compounds that are BACE1 modulators, and methods for treating, preventing or ameliorating neurodegenerative disease, such as AD, using such compounds or pharmaceutical compositions containing such compounds are also provided.
Owner:THE TRUSTEES OF COLUMBIA UNIV IN THE CITY OF NEW YORK
Methods for Alzheimer's Disease Treatment and Cognitive Enhancement
InactiveUS20110245307A1Improving/enhancing cognitive stateReduces myalgiaBiocideNervous disorderBryostatin IBiological activation
The present invention relates to compositions comprising a combination of PKC activators and PKC inhibitors and methods to modulate α-secretase activity; improve or enhance cognitive ability; and / or reduce neurodegeneration in individuals suffering from diseases that impair cognitive ability, particularly Alzheimer's Disease. The invention also relates to methods for improving or enhancing cognitive ability. The present invention also provides methods for increasing the generation of non-amyloidogenic soluble APP (sAPP) comprising the activation of protein kinase C (PKC) in the brain and inhibiting PKC in peripheral tissues. Macrocyclic lactones (i.e. bryostatin class and neristatin class) are preferred PKC activators and Vitamin E is a preferred PKC inhibitor for use in the inventive composition.
Owner:BLANCHETTE ROCKEFELLER NEUROSCI INST
Succinoyl aminopyrazoles and related compounds
This invention is directed to a class of compounds (Formula I) including succinoyl amino pyrazoles, succinoyl amino thiadiazoles, succinoyl amino acid esters, succinoyl amino acid amides, succinoyl amino alcohols, succinoyl amino ketones, succinoyl amino hydantoins, succinoyl anilines, and succinoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting β-amyloid peptide release and / or synthesis, a method for inhibiting γ-secretase activity and a method for treating neurological disorders associated with β-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.
Owner:ELAN PHARM INC
2-Amino-5-piperidinylimidazolone compounds and use thereof for beta-secretase modulation
Owner:WYETH LLC
Modification of amyloid-beta load in non-brain tissue
The present invention relates to methods and compositions for modulating levels of amyloid-β peptide (Aβ) exhibited by non-neuronal (i.e., peripheral) cells, fluids, or tissues. The invention also relates to modulation of Aβ levels via selective modulation (e.g., inhibition) of γ-secretase activity. The invention also relates to methods of preventing, treating or ameliorating the symptoms of a disorder, including but not limited to an Aβ-related disorder, by administering a compound that result in the modulation of γ-secretase in a non-neuronal tissue, either directly or indirectly to prevent, treat or ameliorate the symptoms of a brain Aβ disorder, such as Alzheimer's disease.
Owner:MODGENE
Assays using amyloid precursor proteins with modified beta-secretase cleavage sites to monitor beta-secretase activity
InactiveUS7196163B2More productiveOrganic active ingredientsPeptide/protein ingredientsWild typeAmyloid
Provided are methods of identifying inhibitors of β-secretase that employ modified β-secretase substrates. The modified β-secretase substrates have β-secretase cleavage sites that are altered from wild type. The amino acid sequences of the altered β-secretase cleavage sites contain different amino acids in at least one of the positions P2-P1-P1′-P2′ of the β-secretase cleavage site. Many of the modified β-secretase substrates are more efficient substrates for β-secretase than are corresponding substrates having wild-type sequences, that is, these modified substrates are more susceptible to enzymatic breakdown by β-secretase. Recombinant polynucleotide molecules encoding the modified β-secretase substrates are provided. Antibodies that recognize cleavage products of the modified β-secretase substrates are provided. Stable cell lines expressing the modified β-secretase substrates are provided. Transgenic animals expressing the modified β-secretase substrates are provided.
Owner:MERCK SHARP & DOHME CORP
Methods for Alzheimer's disease treatment and cognitive enhance
InactiveUS20050065205A1Reduces myalgiaIncreased Tolerated DoseBiocideNervous disorderDepressantBryostatin I
The present invention relates to compositions comprising a combination of PKC activators and PKC inhibitors and methods to modulate α-secretase activity; improve or enhance cognitive ability; and / or reduce neurodegeneration in individuals suffering from diseases that impair cognitive ability, particularly Alzheimer's Disease. The invention also relates to methods for improving or enhancing cognitive ability. The present invention also provides methods for increasing the generation of non-amyloidogenic soluble APP (sAPP) comprising the activation of protein kinase C (PKC) in the brain and inhibiting PKC in peripheral tissues. Macrocyclic lactones (i.e. bryostatin class and neristatin class) are preferred PKC activators and Vitamin E is a preferred PKC inhibitor for use in the inventive composition.
Owner:COGNITIVE RES ENTERPRISES INC
Azolylacylguanidines as beta-secretase inhibitors
Owner:WYETH LLC
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