Patent classifications
C07D227/02
HETEROARYL COMPOUNDS COMPRISING NITROGEN AND USE THEREOF
The present invention relates to heteroaryl compounds comprising nitrogen and use thereof, and more specifically to compounds which exhibit a remarkable effect on inhibiting proliferation of cancer cells and metastasis and recurrence of cancer, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient.
The compounds according to the present invention exhibit a remarkable effect on inhibiting proliferation of cancer cells and metastasis and recurrence of cancer with a reduced dose compared to that of existing drugs. Accordingly, the compounds can be effectively used for treating various types of cancer, such as uterine cancer, breast cancer, gastric cancer, brain cancer, rectal cancer, colorectal cancer, lung cancer, skin cancer, blood cancer, pancreatic cancer, renal cancer, prostate cancer, bladder cancer, and liver cancer, and for inhibiting proliferation of cancer cells and metastasis of cancer.
HETEROARYL COMPOUNDS COMPRISING NITROGEN AND USE THEREOF
The present invention relates to heteroaryl compounds comprising nitrogen and use thereof, and more specifically to compounds which exhibit a remarkable effect on inhibiting proliferation of cancer cells and metastasis and recurrence of cancer, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient.
The compounds according to the present invention exhibit a remarkable effect on inhibiting proliferation of cancer cells and metastasis and recurrence of cancer with a reduced dose compared to that of existing drugs. Accordingly, the compounds can be effectively used for treating various types of cancer, such as uterine cancer, breast cancer, gastric cancer, brain cancer, rectal cancer, colorectal cancer, lung cancer, skin cancer, blood cancer, pancreatic cancer, renal cancer, prostate cancer, bladder cancer, and liver cancer, and for inhibiting proliferation of cancer cells and metastasis of cancer.
3-(benzylamino)-4-(cyclohexylamino)-n-(2-(piperazin-1-yl)ethyl)benzenesulfonamide derivatives and related ferrostatin-1 analogues as cell death inhibitors for treating e.g. stroke
The present invention relates to 3-(benzylamino)-4-(cyclohexylamino)-N-(2-(piperazin-1-yl)ethyl)benzenesulfonamide derivatives and related ferrostatin-1 (Fer-1) analogues as cell death inhibitors by inhibition of ferroptosis and/or oxytosis for the treatment of stroke, myocardial infarction, diabetes, sepsis, the prevention of transplant rejection, neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, dementia with Lewy bodies and Friedreich's ataxia. The present invention further relates to pharmaceutical compositions of these compounds and discloses methods for making the compounds and the corresponding intermediate.
3-(benzylamino)-4-(cyclohexylamino)-n-(2-(piperazin-1-yl)ethyl)benzenesulfonamide derivatives and related ferrostatin-1 analogues as cell death inhibitors for treating e.g. stroke
The present invention relates to 3-(benzylamino)-4-(cyclohexylamino)-N-(2-(piperazin-1-yl)ethyl)benzenesulfonamide derivatives and related ferrostatin-1 (Fer-1) analogues as cell death inhibitors by inhibition of ferroptosis and/or oxytosis for the treatment of stroke, myocardial infarction, diabetes, sepsis, the prevention of transplant rejection, neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, dementia with Lewy bodies and Friedreich's ataxia. The present invention further relates to pharmaceutical compositions of these compounds and discloses methods for making the compounds and the corresponding intermediate.
NEMO COILED COIL MIMICS AND METHODS OF USING SAME
This invention relates to macrostructures (and pharmaceutical formulations containing them) that include a parallel coiled-coil structure, wherein the parallel coiled-coil comprises a first coil of Formula I and a second coil of Formula II:
T.sub.1-f.sub.0-g.sub.0-a.sub.1-b.sub.1-c.sub.1-d.sub.1-e.sub.1-f.sub.1-g.sub.1-a.sub.2-b.sub.2-c.sub.2-d.sub.2-e.sub.2-f.sub.2-g.sub.2-a.sub.3-b.sub.3-c.sub.3-d.sub.3-e.sub.3-T.sub.2 (I)
T.sub.3-g′.sub.0-a′.sub.1-b′.sub.1-c′.sub.1-d′.sub.1-e′.sub.1-f′.sub.1-g′.sub.1-a′.sub.2-b′.sub.2-c′.sub.2-d′.sub.2-e′.sub.2-f′.sub.2-g′.sub.2-a′.sub.3-b′.sub.3-c′.sub.3-d′.sub.3-e′.sub.3-f′.sub.3-T.sub.4 (II),
as described in the present application. Methods of using these macrostructures are also disclosed.
NEMO COILED COIL MIMICS AND METHODS OF USING SAME
This invention relates to macrostructures (and pharmaceutical formulations containing them) that include a parallel coiled-coil structure, wherein the parallel coiled-coil comprises a first coil of Formula I and a second coil of Formula II:
T.sub.1-f.sub.0-g.sub.0-a.sub.1-b.sub.1-c.sub.1-d.sub.1-e.sub.1-f.sub.1-g.sub.1-a.sub.2-b.sub.2-c.sub.2-d.sub.2-e.sub.2-f.sub.2-g.sub.2-a.sub.3-b.sub.3-c.sub.3-d.sub.3-e.sub.3-T.sub.2 (I)
T.sub.3-g′.sub.0-a′.sub.1-b′.sub.1-c′.sub.1-d′.sub.1-e′.sub.1-f′.sub.1-g′.sub.1-a′.sub.2-b′.sub.2-c′.sub.2-d′.sub.2-e′.sub.2-f′.sub.2-g′.sub.2-a′.sub.3-b′.sub.3-c′.sub.3-d′.sub.3-e′.sub.3-f′.sub.3-T.sub.4 (II),
as described in the present application. Methods of using these macrostructures are also disclosed.
3-(BENZYLAMINO)-4-(CYCLOHEXYLAMINO)-N-(2-(PIPERAZIN-1-YL)ETHYL)BENZENESULFONAMIDE DERIVATIVES AND RELATED FERROSTATIN-1 ANALOGUES AS CELL DEATH INHIBITORS FOR TREATING E.G. STROKE
The present invention relates to 3-(benzylamino)-4-(cyclohexylamino)-N-(2-(piperazin-1-yl)ethyl)benzenesulfonamide derivatives and related ferrostatin-1 (Fer-1) analogues as cell death inhibitors by inhibition of ferroptosis and/or oxytosis for the treatment of stroke, myocardial infarction, diabetes, sepsis, the prevention of transplant rejection, neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, dementia with Lewy bodies and Friedreich's ataxia. The present invention further relates to pharmaceutical compositions of these compounds and discloses methods for making the compounds and the corresponding intermediate.
Kit for detecting ctDNA and expression of drug-resistant genes related to applicability of tumor chemotherapeutic drugs
A kit for determining ctDNA concentration and a method for determining ctDNA concentration is disclosed, wherein the method comprising dissolving extracted ctDNA in Tris-HCl buffer with pH>7.0 and adding into the buffer 2,7-bis(1-methyl-4-vinylpyridine)-9-ethylcarbazole iodised salt as a molecular probe, calculating the concentration of ctDNA in the solution by measuring the Fluorescence intensity of the solution. It has extremely high sensitivity in the determination of 0 g/ml50 g/ml ctDNA solution.
Kit for detecting ctDNA and expression of drug-resistant genes related to applicability of tumor chemotherapeutic drugs
A kit for determining ctDNA concentration and a method for determining ctDNA concentration is disclosed, wherein the method comprising dissolving extracted ctDNA in Tris-HCl buffer with pH>7.0 and adding into the buffer 2,7-bis(1-methyl-4-vinylpyridine)-9-ethylcarbazole iodised salt as a molecular probe, calculating the concentration of ctDNA in the solution by measuring the Fluorescence intensity of the solution. It has extremely high sensitivity in the determination of 0 g/ml50 g/ml ctDNA solution.
NEMO COILED COIL MIMICS AND METHODS OF USING SAME
This invention relates to macrostructures (and pharmaceutical formulations containing them) that include a parallel coiled-coil structure, wherein the parallel coiled-coil comprises a first coil of Formula I and a second coil of Formula II:
T.sub.1-f.sub.0-g.sub.0-a.sub.1-b.sub.1-c.sub.1-d.sub.1-e.sub.1-f.sub.1-g.sub.1-a.sub.2-b.sub.2-c.sub.2-d.sub.2-e.sub.2-f.sub.2-g.sub.2-a.sub.3-b.sub.3-c.sub.3-d.sub.3-e.sub.3-T.sub.2 (I)
T.sub.3-g.sub.0-a.sub.1-b.sub.1-c.sub.1-d.sub.1-e.sub.1-f.sub.1-g.sub.1-a.sub.2-b.sub.2-c.sub.2-d.sub.2-e.sub.2-f.sub.2-g.sub.2-a.sub.3-b.sub.3-c.sub.3-d.sub.3-e.sub.3-f.sub.3-T.sub.4 (II), as described in the present application. Methods of using these macrostructures are also disclosed.