摘要:
The present invention relates to a benzobis(thiadiazole) derivative represented by the following general formula (1):
wherein R 1 represents a linear or branched alkyl group, or any one of the groups of the following formula (2):
wherein R represents a linear or branched alkyl group; R 2 represents a hydrogen atom; and R 3 represents a hydrogen atom, a linear or branched alkyl group, or any one of the groups of the formula (2); with the proviso that at least one of R 1 and R 3 represents any one of the groups of the formula (2); and two R 1 groups, two R 2 groups, and two R 3 groups may be the same as, or different from each other.
摘要:
The subject invention features compounds having the structure:, wherein X is O, S, CH2 or NR5; Y is O or S; R1 is H, substituted or unsubstituted C1C15 alkyl, C1-C8 alkylaryl, -C(O)OR4, -C(O)NR4R5, -CR6R6'OR4,-CR6R6'OC(O)R4, - CR6R6'OC(O)NHR7, -C(O)NR1oR11, -C(O)NR8R9 NR8R9, -N(R5)C(O)NHR5, or CH2R4; R2 is a substituted or unsubstituted, straight chain C1-C30 alkyl or branched C3 C30 alkyl, aryl, alkylaryl, arylalkyl, heteroarylalkyl or cycloalkyl; R3 is H or substituted or unsubstituted C1-C6 alkyl or C3-C10 cycloalkyl; R4 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl, -CH2-aryl, aryl -C1-C15 alkyl, heteroaryl-C1-C15alkyl or C3-C10 cycloalkyl; R5 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl C1-C30alkyl, heteroarylalkyl or cycloalkyl; R6 and R6' are each independently H, substituted or unsubstituted C1-C6 alkyl, dialkyl or C3-C10 cycloalkyl or together form a 3-7 membered ring system; R7 is H or substituted or unsubstituted C1-C12 alkyl or C3-C10 cycloalkyl; R8 and R9 are each independently H, substituted or unsubstituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylaryl, or NR8R9 together form a substituted piperazine or piperidine ring or a dihydro-1H-isoquinoline ring system, or a specific enantiomer thereof, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating diabetes or obesity by administering a therapeutically effective amount of the compounds of the invention.
摘要:
The present invention relates to a benzobis(thiadiazole) derivative represented by the following general formula (1): wherein R 1 represents a linear or branched alkyl group, or any one of the groups of the following formula (2): wherein R represents a linear or branched alkyl group; R 2 represents a hydrogen atom; and R 3 represents a hydrogen atom, a linear or branched alkyl group, or any one of the groups of the formula (2); with the proviso that at least one of R 1 and R 3 represents any one of the groups of the formula (2); and two R 1 groups, two R 2 groups, and two R 3 groups may be the same as, or different from each other.
摘要:
In some aspects, the disclosure provides compounds comprising nucleic acid modifying moieties, such as nucleic acid binding dyes comprising activatable groups. In some aspects, the disclosure provides nucleic acid probes comprising compounds of the disclosure, and methods of making the same. In some aspects, the disclosure provides methods of using compounds of the disclosure, such as methods of labeling and/or detecting non-viable organisms or non-viable cells, and methods of detecting contamination or infection.
摘要:
The present invention relates to compounds of formula I: in which R 1 , R 2 , R 3 and R 4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.
摘要:
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.