C07C49/252

Half-curcuminoids as amyloid-beta PET imaging agents

Provided herein are curcumin analogues that are able to interact with amyloid beta (Aβ) and to attenuate the copper-induced crosslinking of Aβ. Also provided herein are methods of using the compounds as imaging agents of amyloid beta and for the treatment of diseases associated with amyloid beta. Methods of preparing unlabeled and radiolabeled compounds useful for interacting with amyloid beta and pharmaceutical compositions are also provided.

Half-curcuminoids as amyloid-beta PET imaging agents

Provided herein are curcumin analogues that are able to interact with amyloid beta (Aβ) and to attenuate the copper-induced crosslinking of Aβ. Also provided herein are methods of using the compounds as imaging agents of amyloid beta and for the treatment of diseases associated with amyloid beta. Methods of preparing unlabeled and radiolabeled compounds useful for interacting with amyloid beta and pharmaceutical compositions are also provided.

COMPOUNDS HAVING S1P5 RECEPTOR AGONISTIC ACTIVITY

A compound represented by the general formula (V)

##STR00001##

wherein all the symbols are as defined in the specification, has an improved balance of the agonist activity against the S1P.sub.5 receptor relative to the S1P.sub.1 receptor, and can thus serve as a therapeutic agent for S1P.sub.5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.

COMPOUNDS HAVING S1P5 RECEPTOR AGONISTIC ACTIVITY

A compound represented by the general formula (V)

##STR00001##

wherein all the symbols are as defined in the specification, has an improved balance of the agonist activity against the S1P.sub.5 receptor relative to the S1P.sub.1 receptor, and can thus serve as a therapeutic agent for S1P.sub.5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.

Half-Curcuminoids as Amyloid-Beta PET Imaging Agents
20190255198 · 2019-08-22 ·

Provided herein are curcumin analogues that are able to interact with amyloid beta (A) and to attenuate the copper-induced crosslinking of A. Also provided herein are methods of using the compounds as imaging agents of amyloid beta and for the treatment of diseases associated with amyloid beta. Methods of preparing unlabeled and radiolabeled compounds useful for interacting with amyloid beta and pharmaceutical compositions are also provided.

Compounds having S1P5 receptor agonistic activity

A compound represented by the general formula (V) ##STR00001##
wherein all the symbols are as defined in the specification, has an improved balance of the agonist activity against the S1P.sub.5 receptor relative to the S1P.sub.1 receptor, and can thus serve as a therapeutic agent for S1P.sub.5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.

Compounds having S1P5 receptor agonistic activity

A compound represented by the general formula (V) ##STR00001##
wherein all the symbols are as defined in the specification, has an improved balance of the agonist activity against the S1P.sub.5 receptor relative to the S1P.sub.1 receptor, and can thus serve as a therapeutic agent for S1P.sub.5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.

Half-curcuminoids as amyloid-beta pet imaging agents

Provided herein are curcumin analogues that are able to interact with amyloid beta (A?) and to attenuate the copper-induced crosslinking of A?. Also provided herein are methods of using the compounds as imaging agents of amyloid beta and for the treatment of diseases associated with amyloid beta. Methods of preparing unlabeled and radiolabeled compounds useful for interacting with amyloid beta and pharmaceutical compositions are also provided.

Half-curcuminoids as amyloid-beta pet imaging agents

Provided herein are curcumin analogues that are able to interact with amyloid beta (A?) and to attenuate the copper-induced crosslinking of A?. Also provided herein are methods of using the compounds as imaging agents of amyloid beta and for the treatment of diseases associated with amyloid beta. Methods of preparing unlabeled and radiolabeled compounds useful for interacting with amyloid beta and pharmaceutical compositions are also provided.

COMPOUNDS HAVING S1P5 RECEPTOR AGONISTIC ACTIVITY

A compound represented by the general formula (V)

##STR00001##

wherein all the symbols are as defined in the specification, has an improved balance of the agonist activity against the S1P.sub.5 receptor relative to the S1P.sub.1 receptor, and can thus serve as a therapeutic agent for S1P.sub.5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.