HIV replication inhibitors of formula ##STR00001##
wherein -a.sup.1=a.sup.2-a.sup.3=a.sup.4- is CHCHCHCH, NCHCHCH, NCHNCH, NCHCHN, NNCHCH; -b.sup.1=b.sup.2-b.sup.3=b.sup.4- is CHCHCHCH, NCHCHCH, NCHNCH, NCHCHN, NNCHCH; n and m is 0-4, R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; C.sub.1-6alkyl; C.sub.1-6alkyloxycarbonyl; R.sup.2 is OH; halo; C.sub.1-6alkyl, C.sub.2-6alkenyl or C.sub.2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; S(O).sub.pR.sup.6; C(NH)R.sup.6; R.sup.2a is CN; amino; substituted amino; C.sub.1-6alkyl; halo; C.sub.1-6alkyloxy; carbonyl; CHNNHC(O)R.sup.16; C.sub.1-6alkyloxyC.sub.1-6alkyl; C.sub.2-6alkenyl or C.sub.2-6alkynyl; C(NOR.sup.8)C.sub.1-4alkyl; R.sup.7 or XR.sup.7; R.sup.3 is CN; amino; C.sub.1-6alkyl; halo; C.sub.1-6alkyloxy; substituted carbonyl; CHNNHC(O)R.sup.16; substituted C.sub.1-6alkyl; C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl or C.sub.2-6alkynyl; C(NOR.sup.8)C.sub.1-4alkyl; R.sup.7; XR.sup.7; R.sup.4 is halo; OH; C.sub.1-6alkyl, C.sub.2-6alkenyl or C.sub.2-6alkynyl; C.sub.3-7cycloalkyl; C.sub.1-6alkyloxy; CN; nitro; polyhaloC.sub.1-6alkyl; polyhaloC.sub.1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C.sub.1-4alkyl)amino or R.sup.7; -A-B is CR.sup.5N, NN, CH.sub.2CH.sub.2, CSNH, CONH, CHCH; and the use of these compounds for the prevention or the treatment of HIV infection.

HIV replication inhibitors of formula ##STR00001##
wherein a.sup.1=a.sup.2-a.sup.3=a.sup.4- is CHCHCHCH, NCHCHCH, NCHNCH, NCHCHN, NNCHCH; -b.sup.1=b.sup.2-b.sup.3=b.sup.4- is CHCHCHCH, NCHCHCH, NCHNCH, NCHCHN, NNCHCH; n and m is 0-4, R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; C.sub.1-6alkyl; C.sub.1-6alkyloxycarbonyl; R.sup.2 is OH; halo; C.sub.1-6alkyl, C.sub.2-6alkenyl or C.sub.2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; S(O).sub.pR.sup.6; C(NH)R.sup.6; R.sup.2a is CN; amino; substituted amino; C.sub.1-6alkyl; halo; C.sub.1-6alkyloxy; carbonyl; CHNNHC(O)R.sup.16; C.sub.1-6alkyloxyC.sub.1-6alkyl; C.sub.2-6alkenyl or C.sub.2-6alkynyl; C(NOR.sup.8)C.sub.1-4alkyl; R.sup.7 or XR.sup.7; R.sup.3 is CN; amino; C.sub.1-6alkyl; halo; C.sub.1-6alkyloxy; substituted carbonyl; CHNNHC(O)R.sup.16; substituted C.sub.1-6alkyl; C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl or C.sub.2-6alkynyl; C(NOR.sup.8)C.sub.1-4alkyl; R.sup.7; XR.sup.7; R.sup.4 is halo; OH; C.sub.1-6alkyl, C.sub.2-6alkenyl or C.sub.2-6alkynyl; C.sub.3-7cycloalkyl; C.sub.1-6alkyloxy; CN; nitro; polyhaloC.sub.1-6alkyl; polyhaloC.sub.1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C.sub.1-4alkyl)amino or R.sup.7; A-B- is CR.sup.5N, NN, CH.sub.2CH.sub.2, CSNH, CONH, CHCH; and the use of these compounds for the prevention or the treatment of HIV infection.

The present invention relates to novel biguanide derivatives including their pharmaceutically acceptable salts. The invention also relates processes for the preparation of, intermediates used in the preparation of, pharmaceutical compositions containing and the uses of such compounds in treating disorders such as diabetes.

Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K activity, including compounds that selectively inhibit PI3K activity. Methods of using PI3K inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K inhibitory compounds to inhibit PI3K-mediated processes in vitro and in vivo.

Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K activity, including compounds that selectively inhibit PI3K activity. Methods of using PI3K inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K inhibitory compounds to inhibit PI3K-mediated processes in vitro and in vivo.

The present invention relates to a method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK) and the use of the compounds in the prevention or treatment of disease, including pre-diabetes, type 2 diabetes, syndrome X, metabolic syndrome and obesity. ##STR00001##

The present invention relates to a method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK) and the use of the compounds in the prevention or treatment of disease, including pre-diabetes, type 2 diabetes, syndrome X, metabolic syndrome and obesity. ##STR00001##

The present invention provides purine nucleoside analog compounds and methods of use thereof for treatment of certain injuries, disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries. The present invention further provides methods of synthesizing such compounds, and intermediates useful in the synthesis of such compounds.

The present invention provides purine nucleoside analog compounds and methods of use thereof for treatment of certain injuries, disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries. The present invention further provides methods of synthesizing such compounds, and intermediates useful in the synthesis of such compounds.

The present invention relates to compounds of formula (I),

##STR00001## wherein R.sup.1, R.sup.2 and R.sup.3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.