90 results about "Neurofibrillary tangle" patented technology

The present invention provides a 2-amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone 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.

The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone 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

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.

The present invention provides a 10,11-dihydrospiro[dibenzo[a,d][7]annulene-5,4′-imidazol]-5′(1′H)-one compound of formula IAlso provided are methods and compositions for the inhibition of β-secretase (BACE) and the treatment of β-amyloid deposits and neurofibrillary tangles.

The present invention provides an azolylacylquanidine 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.

The described invention provides methods for treating or preventing progression of a progressive cognitive disease, disorder or condition, and methods for improving resilience of cognitive function in a subject in need thereof.

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.

The present invention provides compounds having high affinity for amyloid β-protein which are for the diagnosis of diseases in which amyloid β-protein accumulates, for agents for specifically staining amyloid β-protein, and for the treatment and / or prophylaxis of diseases in which amyloid β-protein accumulates. The present invention also provides probes and staining agents for neurofibrillary tangles.

The present invention provides compounds, or salts or solvates thereof, which can be used as probes for the imaging diagnosis of diseases in which tau protein accumulates, and compositions and kits comprising such compounds, or salts or solvates thereof. The present invention also provides a method for staining neurofibrillary tangles in brain samples, and a pharmaceutical composition for the treatment and / or prophylaxis of a disease in which β-sheet structure is the cause or possible cause.

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.

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.

The present invention provides a 2-amino-5-piperidinylimidazolone 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.

The invention relates to a compound in a general formula (1), applications of pharmaceutically acceptable salt, esters, amides or predrug of the compound as a developing agent and an aggregation inhibitor of amyloid protein deposit and neurofibrillary tangle, a preparation method of a labeled compound used for development, and a method for conveying the compound to the amyloid protein deposit and the neurofibrillary tangle. When the compound is taken as the developing agent used for detecting in vivo or tissue amyloid protein deposit and neurofibrillary tangle, appropriate radioactive isotope or a contrast agent applicable to magnetic resonance detection needs to be used for labeling the compound. The compound is especially used for the diagnosis and treatment of patients with amyloid protein deposit and neurofibrillary tangle diseases including Alzheimer disease.

The present disclosure provides compositions containing a leptin product and methods of clinical therapy and diagnostic methods for progressive cognitive disorders. According to one aspect, the described invention provides a method for treating a progressive cognitive disorder. According to another aspect, the described invention provides a method for improving resilience of cognitive function in a subject in need thereof. According to another aspect, the described invention provides a method for identifying an effective therapeutic agent for treating a progressive cognitive dysfunction disease or disorder that results from at least one of accumulation of Aβ, hyperphosphorylation of tau, or accumulation of neurofibrillary tangles.

The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound 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.

A method for labeling structures, such as β-amyloid plaques and neurofibrillary tangles, in vivo or in vitro, is provided and comprises contacting brain tissue with one or more compounds, preferably radiolabeled for detection by positron emission tomography (PET).

The present invention provides a 2-amino-5-[substituted-4-(difluoromethoxy)phenyl]-5-phenylimidazolone compound 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.

Compounds, compositions and methods are contemplated in which senile plaques and / or neurofibrillary tangles are labeled using compounds with improved permeability across the blood brain barrier and improved selective binding to senile plaques and / or neurofibrillary tangles. Contemplated compounds are derivatives of FDDNP or curcumin, which most preferably have improved solubility in aqueous solvents. Labeling is typically performed using a PET detectable label, and especially 11C and 18F.

The present invention provides methods inhibiting formation of neurofibrillary tangles; and methods for treating disorders relating to apolipoprotein E (apoE) in a subject. The methods generally involve reducing the level of a carboxyl-terminal truncated form of apoE in a neuronal cell of a subject. The invention further provides isolated cells comprising a nucleic acid molecule encoding a carboxyl-terminal truncated form of apoE; and methods of screening compounds using the cells. The invention further provides compounds that inhibit an apoE cleavage enzyme, and that reduce the formation of neurofibrillary tangles in a neuronal cell. The invention further provides transgenic non-human animals that include as a transgene a nucleic acid that encodes a carboxyl-terminal truncated form of apoE; as well as methods of screening compounds using transgenic animals.

The present invention provides an indolylalkylpyridin-2-amine 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.

The present invention provides method of constructing Alzhemer's disease (AD) rat animal model through injecting wortmanin as phosphatidylinositol 3 kinase inhibitor and GF-109203X as protein kinase C inhibitor into rat lateral ventricle simultaneously. The method can induce AD-like abnormal excessive phosphorylation of hippocampal skelemin and neurofibrillary tangle-like pathologic changes and constitute rat animal model with co-existed learning and memory disorder. The model may be used in screening medicine for treating Alzhemer's disease and in the research of the internal relation between protein kinase and AD pathogenesis.

Compositions useful for labeling β-amyloid plaques and neurofibrillary tangles are provided. The compositions comprises compounds of formula (I):wherein R1 is selected from the group consisting of —C(O)-alkyl, —C(O)-alkylenyl-R4, —C(O)O-alkyl, —C(O)O-alkylenyl-R4, —C═C(CN)2-alkyl, —C═C(CN)2-alkylenyl-R4,wherein R4 is a radical selected from the group consisting of alkyl, substituted alkyl, aryl and substituted aryl; R5 is a radical selected from the group consisting of —NH2, —OH, —SH, —NH-alkyl, —NHR4, —NH-alkylenyl-R4, —O-alkyl, —O-alkylenyl-R4, —S-alkyl, and —S-alkylenyl-R4; R6 is a radical selected from the group consisting of —CN, —COOH, —C(O)O-alkyl, —C(O)O-alkylenyl-R4, —C(O)-alkyl, —C(O)-alkylenyl-R4, —C(O)-halogen, —C(O)NH-alkyl, —C(O)NH-alkylenyl-R4 and —C(O)NH2; R7 is a radical selected from the group consisting of O, NH, and S; and R8 is N, O or S; and R2 is selected from the group consisting of alkyl and alkylenyl-R10 and R3 is alkylenyl-R10, wherein R10 is selected from the group consisting of —OH, —OTs, halogen, spiperone, spiperone ketal, and spiperone-3-yl, or R2 and R3 together form a heterocyclic ring, optionally substituted with at least one radical selected from the group consisting of alkyl, alkoxy, OH, OTs, halogen, alkyl-R10, carbonyl, spiperone, spiperone ketal and spiperone-3-yl, and further wherein one or more of the hydrogen, halogen or carbon atoms are optionally replaced with a radiolabel.

The invention relates to applications of compounds of formulas (1)-(58), or pharmaceutically-acceptable salts, esters, amides or prodrugs thereof as developers and aggregation inhibitors of amyloid protein sediments and neurofibrillary tangles, a preparation method labeled compounds for imaging, and a method for transporting the compounds to amyloid protein sediments and neurofibrillary tangles. When serving as the developers used to detect the amyloid protein sediments and neurofibrillary tangles in body and tissue, the compounds need to use appropriate radioisotopes or contrast agents suitable for magnetic resonance detection to be labeled. The compounds of the invention are applied to diagnose and treat patients suffering from amyloid protein sediments and neurofibrillary tangles and Alzheimer disease.