C07D311/24

Cromolyn derivatives and related methods of imaging and treatment
10576171 · 2020-03-03 · ·

Novel cromolyn analogs useful as imaging agents for detecting atherosclerotic plaques and for treating atherosclerosis and Alzheimer's Disease, and methods of making the cromolyn analogs, are disclosed. The cromolyn analogs have the general formula: ##STR00001##
wherein: X is OH, C.sub.1-C.sub.6 alkoxyl; Y and Z are independently selected form a C.sub.1-C.sub.6 alkyl, C.sub.1-C.sub.6 alkoxyl, halogen, un-substiuted or C.sub.1-C.sub.6 substituted amine, .sup.18F, .sup.19F, or H; and n is 1, 2, or 3; and wherein for structure (I), if n are both 1 and Y and Z are both H and X is OH.

CROMOLYN DERIVATIVES AND RELATED METHODS OF IMAGING AND TREATMENT
20190388568 · 2019-12-26 ·

Novel cromolyn analogs useful as imaging agents for detecting atherosclerotic plaques and for treating atherosclerosis and Alzheimer's Disease, and methods of making the cromolyn analogs, are disclosed. The cromolyn analogs have the general formula:

##STR00001##

wherein X is OH, C.sub.1-C.sub.6 alkoxyl; Y and Z are independently selected from a C.sub.1-C.sub.6 alkyl, C.sub.1-C.sub.6 alkoxyl, halogen, un-substituted or C1-C6 substituted amine, .sup.18F, .sup.19F, or H; and n is 1, 2, or 3; and wherein for structure (I), if n are both 1 and Y and Z are both H and X is OH.

CROMOLYN DERIVATIVES AND RELATED METHODS OF IMAGING AND TREATMENT
20190388568 · 2019-12-26 ·

Novel cromolyn analogs useful as imaging agents for detecting atherosclerotic plaques and for treating atherosclerosis and Alzheimer's Disease, and methods of making the cromolyn analogs, are disclosed. The cromolyn analogs have the general formula:

##STR00001##

wherein X is OH, C.sub.1-C.sub.6 alkoxyl; Y and Z are independently selected from a C.sub.1-C.sub.6 alkyl, C.sub.1-C.sub.6 alkoxyl, halogen, un-substituted or C1-C6 substituted amine, .sup.18F, .sup.19F, or H; and n is 1, 2, or 3; and wherein for structure (I), if n are both 1 and Y and Z are both H and X is OH.

APP specific bace inhibitors (ASBIs) and uses thereof

In certain embodiments APP-specific BACE inhibitors (ASBIs) are provided as well as uses thereof. In certain embodiments methods of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction, and/or ameliorating one or more symptoms of a pre-Alzheimer's condition and/or cognitive dysfunction, or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease are provided where the method involves administering to a subject in need thereof an APP specific BACE inhibitor (ASBI) in an amount sufficient to prevent or delay the onset of a pre-Alzheimer's cognitive dysfunction, and/or to ameliorate one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or to prevent or delay the progression of a pre-Alzheimer's cognitive dysfunction to Alzheimer's disease. In certain embodiments the ASBI is a flavonoid (e.g. galangin) or flavonoid prodrug (e.g., galangin prodrug).

APP specific bace inhibitors (ASBIs) and uses thereof

In certain embodiments APP-specific BACE inhibitors (ASBIs) are provided as well as uses thereof. In certain embodiments methods of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction, and/or ameliorating one or more symptoms of a pre-Alzheimer's condition and/or cognitive dysfunction, or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease are provided where the method involves administering to a subject in need thereof an APP specific BACE inhibitor (ASBI) in an amount sufficient to prevent or delay the onset of a pre-Alzheimer's cognitive dysfunction, and/or to ameliorate one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or to prevent or delay the progression of a pre-Alzheimer's cognitive dysfunction to Alzheimer's disease. In certain embodiments the ASBI is a flavonoid (e.g. galangin) or flavonoid prodrug (e.g., galangin prodrug).

MACROPHAGES/MICROGLIA IN NEURO-INFLAMMATION ASSOCIATED WITH NEURODEGENERATIVE DISEASES

Described herein are methods of treating neuron inflammation conditions, for example, Alzheimer's disease, Parkinson's disease, Huntington's disease, ischemic stroke, and prion disease, comprising administering a therapeutically effective amount of cromolyn or a cromolyn derivative compound.

MACROPHAGES/MICROGLIA IN NEURO-INFLAMMATION ASSOCIATED WITH NEURODEGENERATIVE DISEASES

Described herein are methods of treating neuron inflammation conditions, for example, Alzheimer's disease, Parkinson's disease, Huntington's disease, ischemic stroke, and prion disease, comprising administering a therapeutically effective amount of cromolyn or a cromolyn derivative compound.

CROMOLYN DERIVATIVES AND RELATED METHODS OF IMAGING AND TREATMENT
20240058480 · 2024-02-22 ·

Novel cromolyn analogs useful as imaging agents for detecting atherosclerotic plaques and for treating atherosclerosis and Alzheimer's Disease, and methods of making the cromolyn analogs, are disclosed. The cromolyn analogs have the general formula:

##STR00001##

wherein X is OH, C.sub.1-C.sub.6 alkoxyl; Y and Z are independently selected from a C.sub.1-C.sub.6 alkyl, C.sub.1-C.sub.6 alkoxyl, halogen, un-substituted or C1-C6 substituted amine, .sup.18F, .sup.19F, or H; and n is 1, 2 , or 3; and wherein for structure (I), if n are both 1 and Y and Z are both H and X is OH.

CROMOLYN DERIVATIVES AND RELATED METHODS OF IMAGING AND TREATMENT
20240058480 · 2024-02-22 ·

Novel cromolyn analogs useful as imaging agents for detecting atherosclerotic plaques and for treating atherosclerosis and Alzheimer's Disease, and methods of making the cromolyn analogs, are disclosed. The cromolyn analogs have the general formula:

##STR00001##

wherein X is OH, C.sub.1-C.sub.6 alkoxyl; Y and Z are independently selected from a C.sub.1-C.sub.6 alkyl, C.sub.1-C.sub.6 alkoxyl, halogen, un-substituted or C1-C6 substituted amine, .sup.18F, .sup.19F, or H; and n is 1, 2 , or 3; and wherein for structure (I), if n are both 1 and Y and Z are both H and X is OH.

HDAC INHIBITORS

The present disclosure is directed to chromane compounds, chromane compounds demonstrating HDAC inhibition, and pharmaceutical compositions thereof. Additional embodiments include methods of using the chromane compounds. For example, the disclosure includes methods of inhibiting histone acetylation in a cell, comprising contacting the cell with a chromane compound of the disclosure. Additional embodiments include methods of treating a disease capable of treatment by inhibition of histone acetylation in a patient in need thereof, comprising administering a chromane compound of the disclosure.