Disclosed is a method for preparing oxetan-2-ylmethanamine, which belongs to the field of organic synthesis. [2-(1-ethoxyethoxy)methyl]propylene oxide is used as an initial raw material, and reacted in the presence of potassium tert-butoxide and trimethylsulfoxonium iodide; the resulting product is reacted with a sulfonyl compound and triethylamine; the resulting product is reacted with a compound of phthalimide; the resulting product is reacted with an amino group-containing compound, to obtain oxetan-2-ylmethanamine. The method according to the disclosure allows for an overall yield of not less than 30% in scale-up production (kilogram level), which is higher. Moreover, compared with the traditional method for preparing oxetan-2-ylmethanamine, a palladium-carbon catalytic hydrogenation step is not required, and dangerous chemical-sodium azide is not required in the method according to the disclosure. Thus, the method has high safety, low production cost, simple operations, and thereby is suitable for industrial production.

Provided herein is the design and synthesis of novel molecular rotor fluorophores of formula I useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are the compounds for use in methods for diagnosis and treatment of diseases associated with an amyloid or amyloid like proteins, such as e.g. Alzheimer's disease or traumatic brain injury (TBI), Parkinson's disease, vascular dementia, amyotrophic lateral sclerosis, Down syndrome, traumatic brain injury, chronic traumatic encephalopathy, schizophrenia or depression. Exemplary compounds are e.g. N-heterocyclyl substituted 2-cyano-3-(naphthalen-2-yl)acrylamide derivatives, such as e.g. (E)-2-cyano-N-(2-(2-hydroxy)ethoxy)ethyl)-3-(6-(pyrrolidin-1-yl)naphthalen-2-yl) acrylamide (example 1): Experimental data on in-vitro binding studies with amyloid beta is provided.

##STR00001##

Provided herein is the design and synthesis of novel molecular rotor fluorophores of formula I useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are the compounds for use in methods for diagnosis and treatment of diseases associated with an amyloid or amyloid like proteins, such as e.g. Alzheimer's disease or traumatic brain injury (TBI), Parkinson's disease, vascular dementia, amyotrophic lateral sclerosis, Down syndrome, traumatic brain injury, chronic traumatic encephalopathy, schizophrenia or depression. Exemplary compounds are e.g. N-heterocyclyl substituted 2-cyano-3-(naphthalen-2-yl)acrylamide derivatives, such as e.g. (E)-2-cyano-N-(2-(2-hydroxy)ethoxy)ethyl)-3-(6-(pyrrolidin-1-yl)naphthalen-2-yl) acrylamide (example 1): Experimental data on in-vitro binding studies with amyloid beta is provided.

##STR00001##

The present application is directed to biaryl piperidine amide compounds, or pharmaceutically acceptable salts, solvates, and prodrugs thereof, and methods of use thereof.

Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.

Disclosed are compounds of Formula 1, N-oxides of the compounds and salts of the compounds and N-oxides:

##STR00001##

wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, Q.sup.1, Q.sup.2, J, Y.sup.1, and Y.sup.2 are as defined in the disclosure.

Also disclosed are compositions containing the compounds, N-oxides and salts, and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of such a compound, N-oxide, salt or composition.

Disclosed are compounds of Formula 1, N-oxides of the compounds and salts of the compounds and N-oxides:

##STR00001##

wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, Q.sup.1, Q.sup.2, J, Y.sup.1, and Y.sup.2 are as defined in the disclosure.

Also disclosed are compositions containing the compounds, N-oxides and salts, and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of such a compound, N-oxide, salt or composition.

The present application relates to maleates of a compound of Formula I, methods for preparing the same, pharmaceutical compositions thereof and uses thereof in the treatment of tumors, such as non-small cell lung cancer, breast cancer, and other malignant tumors.

##STR00001##

The present application relates to maleates of a compound of Formula I, methods for preparing the same, pharmaceutical compositions thereof and uses thereof in the treatment of tumors, such as non-small cell lung cancer, breast cancer, and other malignant tumors.

##STR00001##

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.