Patent classifications
C07D239/72
HETEROCYCLIC DERIVATIVES AND USE THEREOF
The present invention relates to novel heterocyclic compounds useful in preparing drugs for the prevention or treatment of diseases associated with STAT3 protein. Specifically, these drugs are useful in the prevention or treatment of solid tumors, blood cancers, radiation or drug-resistant cancers, metastatic cancers, inflammatory diseases, immune system diseases, diabetes, macular degeneration, papillomavirus infections and tuberculosis.
HETEROCYCLIC DERIVATIVES AND USE THEREOF
The present invention relates to novel heterocyclic compounds useful in preparing drugs for the prevention or treatment of diseases associated with STAT3 protein. Specifically, these drugs are useful in the prevention or treatment of solid tumors, blood cancers, radiation or drug-resistant cancers, metastatic cancers, inflammatory diseases, immune system diseases, diabetes, macular degeneration, papillomavirus infections and tuberculosis.
DERIVATIVES OF PAPAVERINE THAT ARE EFFECTIVE HYPOXIC TUMOR RADIOSENSITIZERS
Disclosed herein are compounds, compositions, and methods for inhibiting mitochondrial oxygen consumption in a cancerous tissue. The compounds, compositions, and methods can be used to treat a subject with hypoxic cancerous tissue.
DERIVATIVES OF PAPAVERINE THAT ARE EFFECTIVE HYPOXIC TUMOR RADIOSENSITIZERS
Disclosed herein are compounds, compositions, and methods for inhibiting mitochondrial oxygen consumption in a cancerous tissue. The compounds, compositions, and methods can be used to treat a subject with hypoxic cancerous tissue.
Substituted pyrazole compounds containing pyrimidine and preparation method and use thereof
Disclosed are substituted pyrazole compounds containing pyrimidinyl as shown in Formula I: ##STR00001##
The definitions of each of the substituents can be seen in the description. The compounds of present invention have a good spectrum of bactericidal, insecticidal and acaricidal activity, and have good control effect on downy mildew of cucumber, powdery mildew of wheat, corn rust, rice blast, cucumber anthracnosis and the like. The compounds of present invention also show good insecticidal activity.
Substituted pyrazole compounds containing pyrimidine and preparation method and use thereof
Disclosed are substituted pyrazole compounds containing pyrimidinyl as shown in Formula I: ##STR00001##
The definitions of each of the substituents can be seen in the description. The compounds of present invention have a good spectrum of bactericidal, insecticidal and acaricidal activity, and have good control effect on downy mildew of cucumber, powdery mildew of wheat, corn rust, rice blast, cucumber anthracnosis and the like. The compounds of present invention also show good insecticidal activity.
KRas G12C inhibitors
The present invention provides compounds of the Formula I below ##STR00001##
where R1, R2 and m are as described herein, pharmaceutically acceptable salts of the compounds of Formula 1, and methods of using these compounds and salts for treating patients for cancer.
CURED PRODUCT, OPTICAL MEMBER, LENS, AND COMPOUND
The present invention provides a cured product obtained by curing a curable composition including a compound represented by General Formula 1, in which a birefringence n (587 nm) is 0.00n (587 nm)0.01.
Pol.sub.1-Sp.sub.1-L.sub.1-Ar-L.sub.2-Sp.sub.2-Pol.sub.2(General Formula 1)
In the formula, Ar represents a divalent group containing a ring structure selected from the group consisting of a quinoxaline ring and a quinazoline ring; L.sub.1 and L.sub.2 each represent a single bond, O, OC(O), OC(O)O, OC(O)NH, and the like; Sp.sub.1 and Sp.sub.2 each represent a single bond or a divalent linking group; Pol.sub.1 and Pol.sub.2 each represent a hydrogen atom or a polymerizable group; and the compound represented by General Formula 1 has at least one polymerizable group. The cured product of the present invention has a small Abbe number (d) and a large partial dispersion ratio (g, F), and is therefore useful for production of optical members.
4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections
This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R.sub.2 is hydrogen, NRR, C.sub.1-7 alkyl, arylC.sub.1-7 alkyl or C.sub.3-10 cycloalkyl; R.sub.4 is amino, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C.sub.1-7 alkyl or C.sub.3-10 cycloalkyl-C.sub.1-7 alkyl; R.sub.5 is hydrogen or C.sub.1-7 alkyl, or R.sub.5 and R.sub.4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene; R.sub.6 is halogen, heteroaryl or aryl; R and R are each independently hydrogen, C.sub.1-7 alkyl-carbonyl or C.sub.1-7 alkyl; provided that R.sub.4 is not phenyl substituted with morpholino when R.sub.2 is H and R.sub.5 is H, and provided that when NR.sub.4R.sub.5 is piperazinyl, said NR.sub.4R.sub.5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.
4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections
This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R.sub.2 is hydrogen, NRR, C.sub.1-7 alkyl, arylC.sub.1-7 alkyl or C.sub.3-10 cycloalkyl; R.sub.4 is amino, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C.sub.1-7 alkyl or C.sub.3-10 cycloalkyl-C.sub.1-7 alkyl; R.sub.5 is hydrogen or C.sub.1-7 alkyl, or R.sub.5 and R.sub.4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene; R.sub.6 is halogen, heteroaryl or aryl; R and R are each independently hydrogen, C.sub.1-7 alkyl-carbonyl or C.sub.1-7 alkyl; provided that R.sub.4 is not phenyl substituted with morpholino when R.sub.2 is H and R.sub.5 is H, and provided that when NR.sub.4R.sub.5 is piperazinyl, said NR.sub.4R.sub.5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.