Adenine derivatives substituted at the C2, N6, and N9 purine positions having antisenescent and combined photoprotective UVA/UVB effects. These substances are particularly suitable as anti-senescent and UV-photoprotective component in cosmetic preparations, plant protection preparations and in preparations for the treatment/application of tissue cultures. ##STR00001##

Provided is a heterocyclic amide compound that may have a PRS inhibitory action and is expected to be useful as a prophylactic or therapeutic agent for PRS associated diseases and the like including cancer. A compound represented by the following formula (I): ##STR00001##
wherein a group represented by ##STR00002##
is a group represented by the following formula (II) or the following formula (III): ##STR00003##
and other symbols are as described in the DESCRIPTION, or a salt thereof.

Provided is a heterocyclic amide compound that may have a PRS inhibitory action and is expected to be useful as a prophylactic or therapeutic agent for PRS associated diseases and the like including cancer. A compound represented by the following formula (I): ##STR00001##
wherein a group represented by ##STR00002##
is a group represented by the following formula (II) or the following formula (III): ##STR00003##
and other symbols are as described in the DESCRIPTION, or a salt thereof.

The present invention provides a process of producing a trifluoromcthoxylated aryl or trifluoromothoxylated heteroaryl having the structure:

##STR00001## wherein A is an aryl or heteroaryl, each with or without substitution; and R.sub.1 is H, -(alkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(alkylaryl), -(alkylheteroaryl), NH-(alkyl), N(alkyl).sub.2, NH-(alkenyl), NH-(alkynyl) NH-(aryl), NH-(heteroaryl), O-(alkyl), O-(alkenyl), O-(alkynyl), O-(aryl), O-(heteroaryl), S-(alkyl), S-(alkenyl), S-(alkynyl), S-(aryl), or S-(heteroaryl), comprising: (a) reacting a compound having the structure:

##STR00002## with a trifluoromethylating agent in the presence of a base in a first suitable solvent under conditions to produce a compound having the structure:

##STR00003##

and (b) maintaining the compound produced in step (a) in a second suitable solvent under conditions sufficient to produce the trifluoromethoxylated aryl or trifluormethoxylated heteroaryl having the structure:

##STR00004##

The present invention provides a process of producing a trifluoromcthoxylated aryl or trifluoromothoxylated heteroaryl having the structure:

##STR00001## wherein A is an aryl or heteroaryl, each with or without substitution; and R.sub.1 is H, -(alkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(alkylaryl), -(alkylheteroaryl), NH-(alkyl), N(alkyl).sub.2, NH-(alkenyl), NH-(alkynyl) NH-(aryl), NH-(heteroaryl), O-(alkyl), O-(alkenyl), O-(alkynyl), O-(aryl), O-(heteroaryl), S-(alkyl), S-(alkenyl), S-(alkynyl), S-(aryl), or S-(heteroaryl), comprising: (a) reacting a compound having the structure:

##STR00002## with a trifluoromethylating agent in the presence of a base in a first suitable solvent under conditions to produce a compound having the structure:

##STR00003##

and (b) maintaining the compound produced in step (a) in a second suitable solvent under conditions sufficient to produce the trifluoromethoxylated aryl or trifluormethoxylated heteroaryl having the structure:

##STR00004##

The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

The present invention relates to a substituted purine derivative of formula (1) wherein R.sup.1 is alkoxy or the like, R.sup.2 is alkyl or the like, Ring Q.sup.1 is aryl or the like, W.sup.1 is alkylene or the like, Ring Q.sup.2 is aromatic carbocyclyl or the like, n is 1-4, R.sup.3 is hydrogen atom or the like, X.sup.1 is single bond or the like, W.sup.2 is alkylene or the like, and R.sup.4 is hydrogen atom or the like, or a pharmaceutically acceptable salt thereof, which has a potent inhibitory effect against TLR7, and thereby is useful for treating autoimmune disease. ##STR00001##

The present invention relates to a substituted purine derivative of formula (1) wherein R.sup.1 is alkoxy or the like, R.sup.2 is alkyl or the like, Ring Q.sup.1 is aryl or the like, W.sup.1 is alkylene or the like, Ring Q.sup.2 is aromatic carbocyclyl or the like, n is 1-4, R.sup.3 is hydrogen atom or the like, X.sup.1 is single bond or the like, W.sup.2 is alkylene or the like, and R.sup.4 is hydrogen atom or the like, or a pharmaceutically acceptable salt thereof, which has a potent inhibitory effect against TLR7, and thereby is useful for treating autoimmune disease. ##STR00001##

The invention provides a new convergent approach for the synthesis of 2-fluoro-6-methylene-carbocyclic adenosine (FMCA) and 2-fluoro-6-methylene-carbocyclic guanosine (FMCG) from a readily available starting material in eight steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, (1S,3R, 4R)-3-tert-butoxy -4-(tert-butoxymethyl)-2-fluoro-5-methylenecyclopentanol (compound 8 of scheme 1A or a) in only six (6) steps is also provided. Prodrugs of these compounds are also prepared.