C07D473/24

7-substituted sulfonimidoylpurinone compounds and derivatives for the treatment and prophylaxis of virus infection

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.

7-substituted sulfonimidoylpurinone compounds and derivatives for the treatment and prophylaxis of virus infection

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.

COMPOUNDS AND METHODS FOR TARGETING HSP90

Described herein are compounds that may selectively bind to Hsp90, methods of using the compounds, and kits including the compounds. The compounds may include detection moieties such as fluorophores that may allow for selective detection of Hsp90 in a sample.

COMPOUNDS AND METHODS FOR TARGETING HSP90

Described herein are compounds that may selectively bind to Hsp90, methods of using the compounds, and kits including the compounds. The compounds may include detection moieties such as fluorophores that may allow for selective detection of Hsp90 in a sample.

INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA

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.

INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA

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.

Substituted 6-aminopurines for targeting HSP90
10112947 · 2018-10-30 · ·

Described herein are 6-aminopurine compounds comprising formula (III) that may selectively bind to Hsp90, methods of using the compounds, and kits including the compounds. Formula (III) may link to detection moieties such as fluorophores that may allow for selective detection of Hsp90 in a sample. ##STR00001##

Substituted 6-aminopurines for targeting HSP90
10112947 · 2018-10-30 · ·

Described herein are 6-aminopurine compounds comprising formula (III) that may selectively bind to Hsp90, methods of using the compounds, and kits including the compounds. Formula (III) may link to detection moieties such as fluorophores that may allow for selective detection of Hsp90 in a sample. ##STR00001##

Adenylyl cyclase inhibitors, pharmaceutical compositions and method of use thereof
10081633 · 2018-09-25 ·

The present invention relates to novel adenine based inhibitors of adenylyl cyclase of the formula: ##STR00001##
wherein X, L, R1, R2, R5 are those defined herein. Compounds of the present invention are useful to treat cardiovascular diseases. The present invention also relates to a method of preventing heart failure by administering an effective amount of compound according to the invention following vascular injury and reperfusion therapy.

HIV inhibiting bicyclic pyrimidine derivatives

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.