The embodiments use an innovative approach with the goal of permanent eradication of the virus. Instead of using drugs that block different stages of the virus life cycle (which have failed to induce a permanent cure), or approaches attempting to track infected cells, the embodiments use small virucidal molecules that are known to destroy the virus in vitro and that can easily penetrate all human cells, including memory cells or other reservoir cells. The problem with the use of small molecules is their toxicity to humans or animals when administered in doses sufficient to achieve intracellular concentrations high enough to destroy the virus in all forms. The embodiments overcome these toxicities (especially the comatose state) by using a 24-hour treatment with general anesthesia, endotracheal intubation with hemodynamic support, and controlled monitored ventilation; also, a combination of these molecules are used which decreases toxicity but has additive virucidal effects.

The embodiments use an innovative approach with the goal of permanent eradication of the virus. Instead of using drugs that block different stages of the virus life cycle (which have failed to induce a permanent cure), or approaches attempting to track infected cells, the embodiments use small virucidal molecules that are known to destroy the virus in vitro and that can easily penetrate all human cells, including memory cells or other reservoir cells. The problem with the use of small molecules is their toxicity to humans or animals when administered in doses sufficient to achieve intracellular concentrations high enough to destroy the virus in all forms. The embodiments overcome these toxicities (especially the comatose state) by using a 24-hour treatment with general anesthesia, endotracheal intubation with hemodynamic support, and controlled monitored ventilation; also, a combination of these molecules are used which decreases toxicity but has additive virucidal effects.

This disclosure features compositions (e.g., re-constitutable solids, such as lyophilized cakes; or liquid compositions, such as solutions or suspensions, e.g., reconstituted lyophilized cakes) that are suitable for subcutaneous administration. The compositions include a crystalline form (e.g., Form A) of 6-O-(4-dimethylaminoethoxy)cinnamoyl fumagillol, free base and one or more pharmaceutically acceptable excipients and/or one or more pharmaceutically acceptable carriers (e.g., one or more bulking agents; one or more dispersing agents; one or more buffers; one or more suspending agents; water, e.g., water for injection (“WFI”)).

This disclosure features compositions (e.g., re-constitutable solids, such as lyophilized cakes; or liquid compositions, such as solutions or suspensions, e.g., reconstituted lyophilized cakes) that are suitable for subcutaneous administration. The compositions include a crystalline form (e.g., Form A) of 6-O-(4-dimethylaminoethoxy)cinnamoyl fumagillol, free base and one or more pharmaceutically acceptable excipients and/or one or more pharmaceutically acceptable carriers (e.g., one or more bulking agents; one or more dispersing agents; one or more buffers; one or more suspending agents; water, e.g., water for injection (“WFI”)).

The present invention provides a novel dihydroorotic acid dehydrogenase inhibitor which is applicable to various diseases. When used as an active ingredient, a compound represented by formula (I): ##STR00001##
(wherein X represents a halogen atom, R.sup.1 represents a hydrogen atom, R.sup.2 represents an alkyl group containing 1 to 7 carbon atoms, R.sup.3 represents —CHO, and R.sup.4 represents —CH.sub.2—CH═C(CH.sub.3)—R.sup.0 (wherein R.sup.0 represents an alkyl group containing 1 to 12 carbon atoms which may have a substituent on the terminal carbon and/or on a non-terminal carbon, etc.)),
an optical isomer thereof or a pharmaceutically acceptable salt thereof has a high inhibitory effect on dihydroorotic acid dehydrogenase and can be used as an immunosuppressive agent, a therapeutic agent for rheumatism, an anticancer agent, a therapeutic agent for graft rejection, an antiviral agent, an anti-H. pylori agent, a therapeutic agent for diabetes or the like.

The present invention provides a novel dihydroorotic acid dehydrogenase inhibitor which is applicable to various diseases. When used as an active ingredient, a compound represented by formula (I): ##STR00001##
(wherein X represents a halogen atom, R.sup.1 represents a hydrogen atom, R.sup.2 represents an alkyl group containing 1 to 7 carbon atoms, R.sup.3 represents —CHO, and R.sup.4 represents —CH.sub.2—CH═C(CH.sub.3)—R.sup.0 (wherein R.sup.0 represents an alkyl group containing 1 to 12 carbon atoms which may have a substituent on the terminal carbon and/or on a non-terminal carbon, etc.)),
an optical isomer thereof or a pharmaceutically acceptable salt thereof has a high inhibitory effect on dihydroorotic acid dehydrogenase and can be used as an immunosuppressive agent, a therapeutic agent for rheumatism, an anticancer agent, a therapeutic agent for graft rejection, an antiviral agent, an anti-H. pylori agent, a therapeutic agent for diabetes or the like.

The use of dianhydrogalactitol provides a novel therapeutic modality for the treatment of glioblastoma multiforme and medulloblastoma. Dianhydrogalactitol acts as an alkylating agent on DNA that creates N7 methylation. Dianhydrogalactitol is effective in suppressing the growth of cancer stem cells and is active against tumors that are refractory to temozolomide; the drug acts independently of the MGMT repair mechanism.

The use of dianhydrogalactitol provides a novel therapeutic modality for the treatment of glioblastoma multiforme and medulloblastoma. Dianhydrogalactitol acts as an alkylating agent on DNA that creates N7 methylation. Dianhydrogalactitol is effective in suppressing the growth of cancer stem cells and is active against tumors that are refractory to temozolomide; the drug acts independently of the MGMT repair mechanism.

The use of dianhydrogalactitol provides a novel therapeutic modality for the treatment of glioblastoma multiforme and medulloblastoma. Dianhydrogalactitol acts as an alkylating agent on DNA that creates N7 methylation. Dianhydrogalactitol is effective in suppressing the growth of cancer stem cells and is active against tumors that are refractory to temozolomide; the drug acts independently of the MGMT repair mechanism.

The invention provides novel compositions and methods for the treatment of Radiation-Induced Bystander Effects (RIBE), resulting from radiation exposure. In one preferred embodiment the inventions includes novel therapeutic agents, including but not limited to quercetin and quercetin analogs, as well as E64, CA074, CA074Me, that interfere with the activity of Cathepsin B.