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180 results about "Β secretase" patented technology

Cycloalkyl amino-hydantoin compounds and use thereof for beta-secretase modulation

The present invention provides a 2-amino-5-cycloalkyl-hydantoin compound of formula I The present invention also provides methods and compositions for the inhibition of β-secretase (BACE) and the treatment of β-amyloid deposits and neurofibrillary tangles.
Owner:WYETH LLC

Peptide derivatives having β-secretase inhibitory activity

Provided are excellent β-secretase inhibitors, that is, compounds represented by the general formula (1) or prodrugs thereof:wherein A is amino or protected amino; B1 and B2 are each a single bond, alkylene of 1 to 3 carbon atoms, or the like; D is a single bond, —NHCO, or the like; E is —COOH, tetrazole ring, or the like; n is an integer of 1 to 3; m is an integer of 1 to 3; G is hydroxyl, a group represented by the general formula (2), or the like:in which Z is —NH, -Asp-Ala-NH—, -Asp-Ala-, -Asp-NH—, or the like; L is a 5-to 10-membered ring optionally containing a heteroatom and / or unsaturated bond; X is —COOH, tetrazole ring, or the like; Y is hydrogen, —COOH, or the like; and k is an integer of 1 to 4; and R1, R2, and R3 are each alkyl of 1 to 6 carbon atoms, or the like.
Owner:KISO

Terphenyl guanidines as beta-secretase inhibitors

The present invention provides terphenyl guanidine compounds of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.
Owner:WYETH LLC

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

Terphenyl guanidines as beta-secretase inhibitors

The present invention provides terphenyl guanidine compounds of formula IThe present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.
Owner:WYETH 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

Amino-pyridines as inhibitors of beta-secretase

The present invention provides an amino-pyridine compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.
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

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

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

Modification of amyloid-beta load in non-brain tissue

The present invention relates to methods and compositions for modulating levels of amyloidpeptide (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

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
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