C07D241/36

Coferons and methods of making and using them

The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes one or more pharmacophores which potentially binds to a target molecule with a dissociation constant of less than 300 μM and a linker element connected to the pharmacophore. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to the pharmacophore.

Coferons and methods of making and using them

The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes one or more pharmacophores which potentially binds to a target molecule with a dissociation constant of less than 300 μM and a linker element connected to the pharmacophore. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to the pharmacophore.

Piperazine heteroaryl derivative, preparation method therefor and use of same in medicine

The present invention relates to a piperazine heteroaryl derivative, a preparation method therefor and the use of same in medicine. In particular, the present invention relates to the piperazine heteroaryl derivative as shown in the general formula (I), a preparation method therefor, a pharmaceutical composition comprising the derivative, and the use of same as a capsid protein inhibitor, in particular in the prevention and/or treatment of diseases such as hepatitis B, influenza, herpes, AIDS, etc. The definitions of each group in the general formula (I) are the same as those defined in the description. ##STR00001##

Substituted quinoxalines as positive allosteric modulators of mGluR4
09763938 · 2017-09-19 · ·

The present invention relates to the use of novel quinoxaline derivatives of formula (I) ##STR00001##
as positive allosteric modulators for modulating metabotropic glutamate receptor subtype 4 (mGluR4) and/or altering glutamate level or glutamatergic signalling.

METHOD FOR PRODUCING FULLERENE DERIVATIVE

This method for producing a fullerene derivative is a method for producing a fullerene derivative having a partial structure shown by formula (1) by reacting a predetermined halogenated compound and two carbon atoms adjacent to each other for forming a fullerene skeleton in a mixed solvent of an aromatic solvent and an aprotic polar solvent having a C═O or S═O bond in the presence of at least one metal selected from the group comprising manganese, iron, and zinc;

##STR00001##

(in formula (1), C* are each carbon atoms adjacent to each other for forming a fullerene skeleton, A is a linking group having 1-4 carbon atoms for forming a ring structure with two C*, in which a portion thereof may be a substituted or condensed group).

Pyruvate kinase activators for use in treating blood disorders

Described herein are compounds that activate pyruvate kinase R, pharmaceutical compositions and methods of use thereof. These compounds are represented by Formula (I): wherein R.sup.1, R.sup.2, L.sup.1, and L.sup.2 are as defined herein. ##STR00001##

Pyruvate kinase activators for use in treating blood disorders

Described herein are compounds that activate pyruvate kinase R, pharmaceutical compositions and methods of use thereof. These compounds are represented by Formula (I): wherein R.sup.1, R.sup.2, L.sup.1, and L.sup.2 are as defined herein. ##STR00001##

Compositions and methods for treating CNS disorders

Provided herein is a compound of Formula (I-I), or a pharmaceutically acceptable salt thereof, wherein the variables are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I-I), and methods of using the compounds, e.g. in the treatment of CNS-related disorders. ##STR00001##

PYRUVATE KINASE ACTIVATORS FOR USE IN TREATING BLOOD DISORDERS

Described herein are compounds that activate pyruvate kinase R, pharmaceutical compositions and methods of use thereof. These compounds are represented by Formula (I): wherein R.sup.1, R.sup.2, L.sup.1, and L.sup.2 are as defined herein.

##STR00001##

PYRUVATE KINASE ACTIVATORS FOR USE IN TREATING BLOOD DISORDERS

Described herein are compounds that activate pyruvate kinase R, pharmaceutical compositions and methods of use thereof. These compounds are represented by Formula (I): wherein R.sup.1, R.sup.2, L.sup.1, and L.sup.2 are as defined herein.

##STR00001##