Patent classifications
C07D311/58
TWO-PHOTON FLUORESCENT PROBE COMPOUND SELECTIVE FOR AMYLOID BETA PLAQUES AND METHOD FOR IMAGING AMYLOID BETA PLAQUES USING SAME
The present invention relates to a two-photon fluorescent probe compound represented by Chemical Formula 1 below, and a method for imaging amyloid beta plaques using same, wherein the two-photon fluorescent probe compound according to the present invention maintains an excellent two-photon fluorescence cross-section while at the same time maintaining efficient BBB permeability by minimizing background fluorescence such that a high signal-to-noise ratio is exhibited, and can effectively image Aβ plaques since high selectivity and sensitivity to Aβ plaques are exhibited, and can thus be usefully used in the field of neurodegenerative disease research, including early diagnosis and treatment of Alzheimer's disease. [Chemical Formula 1]
Process for preparation of optically pure and optionally substituted 2-(1-hydroxy-alkyl)-chromen-4-one derivatives and their use in preparing pharmaceuticals
The present invention relates to compounds useful as pharmaceutical intermediates, to processes for preparing the intermediates, to intermediates used in the processes, and to the use of the intermediates in the preparation of pharmaceuticals. In particular, the present invention concerns enantiomerically pure optionally substituted 2-(1-hydroxy-alkyl)-chromen-4-one derivatives represented by formula (IA) and (IB), processes for preparing the alcohol derivatives and their use in preparing pharmaceuticals.
Process for preparation of optically pure and optionally substituted 2-(1-hydroxy-alkyl)-chromen-4-one derivatives and their use in preparing pharmaceuticals
The present invention relates to compounds useful as pharmaceutical intermediates, to processes for preparing the intermediates, to intermediates used in the processes, and to the use of the intermediates in the preparation of pharmaceuticals. In particular, the present invention concerns enantiomerically pure optionally substituted 2-(1-hydroxy-alkyl)-chromen-4-one derivatives represented by formula (IA) and (IB), processes for preparing the alcohol derivatives and their use in preparing pharmaceuticals.
TOCOPHEROL DERIVATIVES AND METHODS OF USE
Tocol derivative compounds, compositions comprising these tocol derivatives and methods of using the tocol derivatives are provided herein. Specifically the tocol derivatives have a partially unsaturated hydrocarbon tail and are thus distinct from the tocopherols. The hydrocarbon tails do not have a trans carbon-carbon double bond in the second isoprene unit of the hydrocarbon tail and are distinct from the tocotrienols. The compounds are expected to allow improved interaction with the a-tocopherol transfer protein receptor than the tocotrienols and better bioactivity than the tocopherols.
TOCOPHEROL DERIVATIVES AND METHODS OF USE
Tocol derivative compounds, compositions comprising these tocol derivatives and methods of using the tocol derivatives are provided herein. Specifically the tocol derivatives have a partially unsaturated hydrocarbon tail and are thus distinct from the tocopherols. The hydrocarbon tails do not have a trans carbon-carbon double bond in the second isoprene unit of the hydrocarbon tail and are distinct from the tocotrienols. The compounds are expected to allow improved interaction with the a-tocopherol transfer protein receptor than the tocotrienols and better bioactivity than the tocopherols.
SUBSTITUTED BICYCLIC COMPOUNDS
Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V):
##STR00001##
and/or a salt thereof, wherein R.sub.1 is —OH or —OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
SUBSTITUTED BICYCLIC COMPOUNDS
Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V):
##STR00001##
and/or a salt thereof, wherein R.sub.1 is —OH or —OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
A CONTROLLED DRUG RELEASE SYSTEM OF PHOTORESPONSIVE NANOCARRIERS, METHODS OF MAKING AND USING THEREOF
Disclosed herein is a controlled drug release system of photoresponsive nanocarriers. Also provided are methods of making the nanocarriers. Also provided are method of using the nanocarriers for the treatment of diseases.
A CONTROLLED DRUG RELEASE SYSTEM OF PHOTORESPONSIVE NANOCARRIERS, METHODS OF MAKING AND USING THEREOF
Disclosed herein is a controlled drug release system of photoresponsive nanocarriers. Also provided are methods of making the nanocarriers. Also provided are method of using the nanocarriers for the treatment of diseases.
PREPARATION OF CANNABICHROMENE AND RELATED CANNABINOIDS
Methods for the production of cannabichromene and related cannabinoid compounds are disclosed. The methods include: forming a reaction mixture comprising 3,7-dimethylocta-2,6-dienal, a diamine, and olivetol or a related starting material; and maintaining the reaction mixture under conditions sufficient to form the desired product. Methods of the present disclosure may also include one-pot conversion of cannabichromene-type products to cannabinol-type products.