Patent classifications
C07D217/08
Substituted tetrahydroisoquinoline ethylbenzamide anti-cancer agents
The compounds herein disclosed are N-substituted tetrahydroisoquinoline ethylbenzamide compounds that have modifications on the phenyl rings by introducing groups with various electronic properties. These derivatives of N-substituted tetrahydroisoquinoline ethylbenzamide compounds have been shown to have anti-proliferative activity against cells. In particular, the compounds have been found to be effective in inhibiting the proliferation of cancer cells, such as cancer cells that originated in breast tissue. Additionally, it has been shown that the novel compounds have IC.sub.50 values against the breast cancer cells that are 6- to 10-fold less than the IC.sub.50 of Tamoxifen.
Substituted tetrahydroisoquinoline ethylbenzamide anti-cancer agents
The compounds herein disclosed are N-substituted tetrahydroisoquinoline ethylbenzamide compounds that have modifications on the phenyl rings by introducing groups with various electronic properties. These derivatives of N-substituted tetrahydroisoquinoline ethylbenzamide compounds have been shown to have anti-proliferative activity against cells. In particular, the compounds have been found to be effective in inhibiting the proliferation of cancer cells, such as cancer cells that originated in breast tissue. Additionally, it has been shown that the novel compounds have IC.sub.50 values against the breast cancer cells that are 6- to 10-fold less than the IC.sub.50 of Tamoxifen.
ACLY INHIBITORS AND USES THEREOF
The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.
ACLY INHIBITORS AND USES THEREOF
The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.
Chilled Compressed Air Electric Vehicle (EV) Fast-Charge System and Method
An air cooling system for an electric vehicle charge cable includes a compressed air supply, at least one filter, at least one dryer and a super cooler subsystem for chilling compressed air from the compressed air supply. A coupling on the charging cable supplies the chilled compressed air to the charging cable. The system is configured to maintain an exterior surface of the charging cable below a predetermined temperature during vehicle charging. The system further includes a routing structure directing the chilled compressed air to flow back to a charging station to maintain the charging cable at a temperature of no more than a predetermined temperature. The system may operate in closed loop mode that is based on geographic climate zone. A method for air cooling an electric vehicle charging cable is also disclosed.
Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation
In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by NO bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.
NRF2 ACTIVATOR
Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use and production.
NRF2 ACTIVATOR
Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use and production.
IRE-1ALPHA INHIBITORS
Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
IRE-1ALPHA INHIBITORS
Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.