Patent classifications
C07D215/42
MANGANESE (III) CATALYZED C--H AMINATIONS
Reactions that directly install nitrogen into CH bonds of complex molecules are significant because of their potential to change the chemical and biological properties of a given compound. Selective intramolecular CH amination reactions that achieve high levels of reactivity, while maintaining excellent site-selectivity and functional-group tolerance is a challenging problem. Herein is reported a manganese perchlorophthalocyanine catalyst [Mn.sup.III(ClPc)] for intermolecular benzylic CH amination of bioactive molecules and natural products that proceeds with unprecedented levels of reactivity and site-selectivity. In the presence of Brnsted or Lewis acid, the [Mn.sup.III(ClPc)]-catalyzed CH amination demonstrates unique tolerance for tertiary amine, pyridine and benzimidazole functionalities. Mechanistic studies indicate that CH amination proceeds through an electrophilic metallonitrene intermediate via a stepwise pathway where CH cleavage is the rate-determining step of the reaction. Collectively these mechanistic features contrast previous base-metal catalyzed CH aminations.
Compounds for preventing, inhibiting, or treating cancer, AIDS and/or premature aging
The manufacture and use of compounds of formula (Ia) or a pharmaceutically acceptable salt thereof for preventing, inhibiting or treating cancer, AIDS and/or premature aging. The compounds of formula (Ia) being: ##STR00001##
where: R independently represents a hydrogen atom, a halogen atom, a (C.sub.1-C.sub.3)alkyl group, a CN group, a hydroxyl group, a COOR.sub.1 group, a (C.sub.1-C.sub.3)fluoroalkyl group, a NO.sub.2 group, a NR.sub.1R.sub.2 group, or a (C.sub.1-C.sub.3)alkoxy group; R is a hydrogen atom, a halogen atom, a (C.sub.1-C.sub.3)alkyl group, a NO.sub.2 group, a (C.sub.1-C.sub.3)alkoxy group, or a NR.sub.1R.sub.2 group; and R.sub.1 and R.sub.2 are a hydrogen atom or a (C.sub.1-C.sub.3) alkyl group.
Methods and Compositions for Inhibition of Bromodomain and Extratermial Proteins
The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.
Methods and Compositions for Inhibition of Bromodomain and Extratermial Proteins
The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.
AMINONAPHTHOQUINONE COMPOUNDS AND PHARMACEUTICAL COMPOSITION FOR BLOCKING UBIQUITINATION-PROTEASOME SYSTEM IN DISEASES
The invention relates to new compounds of formula (I)
##STR00001##
with low cytotoxicity for blocking the ubiquitination-proteasome system in diseases. Accordingly, these compounds can be used in treatment of disorders including, but not limited to, cancers.
AMINONAPHTHOQUINONE COMPOUNDS AND PHARMACEUTICAL COMPOSITION FOR BLOCKING UBIQUITINATION-PROTEASOME SYSTEM IN DISEASES
The invention relates to new compounds of formula (I)
##STR00001##
with low cytotoxicity for blocking the ubiquitination-proteasome system in diseases. Accordingly, these compounds can be used in treatment of disorders including, but not limited to, cancers.
NITROGEN-CONTAINING HETEROCYCLIC COMPOUND
A compound represented by the general formula, or a salt thereof, has exceptional CXCL10 inhibitory activity and is useful as a treatment agent for the prevention and/or treatment, etc., of diseases involving overproduction of CXCL10. In the formula: R.sup.1 is a C.sub.1-6 alkyl group, etc.; R.sup.2 is a hydrogen atom, etc.; R.sup.3 is a halogen atom, etc.; Z.sup.1, Z.sup.2, and Z.sup.3 are CH, etc.; X.sup.1 is CONH, etc.; ring A is a phenyl group, etc.; R.sup.4 is a halogen atom, etc.; and m is an integer of 0-5.
##STR00001##
HETEROCYCLIC COMPOUND
The present invention relates to a compound which can be useful for the treatment or prevention of SPT-related diseases including cancer and congenital diseases associated with sphingolipid accumulation (including Niemann-Pick disease).
HETEROCYCLIC COMPOUND
The present invention relates to a compound which can be useful for the treatment or prevention of SPT-related diseases including cancer and congenital diseases associated with sphingolipid accumulation (including Niemann-Pick disease).
Activators and therapeutic applications thereof
The invention presents methods of identifying small molecule compounds that are activators of tumor suppressor protein p53 pathway, and its associated family members p63 and p73, function. The invention is further drawn to methods of killing tumor cells and treating cancers or other conditions requiring activation of the p53 family member pathways and DNA damage response pathways with the small molecules.