An object of the invention is to provide a .sup.11C-labeled O.sup.6-benzylguanine capable of obtaining a PET image and a process for producing the same. The .sup.11C-labeled O.sup.6-benzylguanine of the invention is represented by the following chemical formula (a). ##STR00001##
The .sup.11C-labeled O.sup.6-benzylguanine is produced by: a coupling step of cross-coupling a methyl iodide labeled with .sup.11C and the following organotin compound (b) (R.sup.1 represents an alkyl group, and R.sup.2 and R.sup.3 represent a leaving group which can be eliminated with a base) in the presence of a palladium complex, a phosphine ligand, and cuprous halide in an aprotic lactam; and a desorption step of desorbing the leaving groups R.sup.2 and R.sup.3 of the coupling product obtained by the coupling step with a base. ##STR00002##

An object of the invention is to provide a .sup.11C-labeled O.sup.6-benzylguanine capable of obtaining a PET image and a process for producing the same. The .sup.11C-labeled O.sup.6-benzylguanine of the invention is represented by the following chemical formula (a). ##STR00001##
The .sup.11C-labeled O.sup.6-benzylguanine is produced by: a coupling step of cross-coupling a methyl iodide labeled with .sup.11C and the following organotin compound (b) (R.sup.1 represents an alkyl group, and R.sup.2 and R.sup.3 represent a leaving group which can be eliminated with a base) in the presence of a palladium complex, a phosphine ligand, and cuprous halide in an aprotic lactam; and a desorption step of desorbing the leaving groups R.sup.2 and R.sup.3 of the coupling product obtained by the coupling step with a base. ##STR00002##

Pyrimidine derivatives of formula (I):

##STR00001##

optionally with a detectable isotope, pharmaceutical composition and method of preparation thereof. Pyrimidine derivatives for use in treatment or prevention of bacterial infection in a host mammal in need of such treatment or prevention and use as inhibitors of biofilm formation on a surface of biomaterial or medical device, particularly of cardiovascular device such as prosthetic heart valve or pacemakers. Pyrimidine derivatives for use as radiotracer in diagnosing or prognosing bacterial infection in a host mammal.

Provided is a series of homologous small molecule immune agonists and novel bifunctional immune targeting compounds having targeting and immune activation functions, which are obtained by coupling the small molecule immune agonists to targeting drugs. The resulting immune targeting compounds are beneficial for enhancing immune activation effects, and anti-tumor and other disease fighting effects of the targeting drug. The enhanced effect is produced from a synergy of immunological anti-tumor factors (such as IFN-) and inhibition at pathogenic targeting sites.

Provided is a series of homologous small molecule immune agonists and novel bifunctional immune targeting compounds having targeting and immune activation functions, which are obtained by coupling the small molecule immune agonists to targeting drugs. The resulting immune targeting compounds are beneficial for enhancing immune activation effects, and anti-tumor and other disease fighting effects of the targeting drug. The enhanced effect is produced from a synergy of immunological anti-tumor factors (such as IFN-) and inhibition at pathogenic targeting sites.

It is found that a nucleoside derivative represented by the following general formula (1) has an anti-viral activity and is less toxic to host cells. ##STR00001##
[in the formula, R.sup.1 represents a hydrogen or halogen atom, R.sup.2 represents a hydrogen or halogen atom, R.sup.3 represents a cyano group, an alkyl group which may have a substituent, an alkenyl group which may have a substituent, an alkynyl group which may have a substituent, a halogen atom, or an azido group, R.sup.4 represents an amino group, a hydrogen atom, a halogen atom, or a hydroxy group, R.sup.5 represents a nitrogen atom or a methine group, R.sup.6 represents a hydrogen atom or a hydroxy group, and R.sup.7 represents a hydrogen atom or a hydroxy group].

Disclosed is a liver specific delivery (LSD)-based entecavir antiviral prodrug, i.e., a nucleoside cyclic phosphate compound, and the application thereof. Specifically, disclosed are a compound as represented by formula (I) and isomers, pharmaceutically acceptable salts, hydrates, and solvates of the compound, and a corresponding pharmaceutical composition. Also disclosed is the application of the compound of the present invention, used separately or used in combination with other antiviral drugs, against viruses, especially the application against hepatitis B virus (HBV). ##STR00001##

Disclosed is a liver specific delivery (LSD)-based entecavir antiviral prodrug, i.e., a nucleoside cyclic phosphate compound, and the application thereof. Specifically, disclosed are a compound as represented by formula (I) and isomers, pharmaceutically acceptable salts, hydrates, and solvates of the compound, and a corresponding pharmaceutical composition. Also disclosed is the application of the compound of the present invention, used separately or used in combination with other antiviral drugs, against viruses, especially the application against hepatitis B virus (HBV). ##STR00001##

The present disclosure relates to a method of loading a toll like receptor (TLR)7/8 agonist into a liposome using remote loading and a kit of parts suitable for the loading of a TLR7/8 agonist into a liposome by said method. The present disclosure further relates to a liposome comprising a salt of a TLR7/8 agonist in the liposome interior and to the use of said liposome for stimulation of an immune response and/or treatment of a clinical condition. Finally, the present disclosure relates to a TLR7/8 agonist which is suitable for being remotely loaded into a liposome.

The present disclosure relates to a method of loading a toll like receptor (TLR)7/8 agonist into a liposome using remote loading and a kit of parts suitable for the loading of a TLR7/8 agonist into a liposome by said method. The present disclosure further relates to a liposome comprising a salt of a TLR7/8 agonist in the liposome interior and to the use of said liposome for stimulation of an immune response and/or treatment of a clinical condition. Finally, the present disclosure relates to a TLR7/8 agonist which is suitable for being remotely loaded into a liposome.