Gpx4 inhibitors, pharmaceutical compositions thereof, and their use for treating gpx4-mediated diseases
US-2024246901-A1 · Jul 25, 2024 · US
Pyrazole derivatives as TNIK, IKKϵ and TBK1 inhibitor and pharmaceutical composition comprising same
US10294207B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10294207-B2 |
| Application number | US-201615083503-A |
| Country | US |
| Kind code | B2 |
| Filing date | Mar 29, 2016 |
| Priority date | Mar 30, 2015 |
| Publication date | May 21, 2019 |
| Grant date | May 21, 2019 |
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Abstract
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Provided is pyrazole derivatives as a TNIK (Traf2- and NCK-interacting kinase), IKKε (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor; the pyrazole derivative according to the present invention effectively inhibits TNIK, IKKε and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.
First claim
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What is claimed is: 1. A compound selected from the group consisting of: (1) N-benzyl-3-(4-fluorobenzamido)-1H-indazole-5-carboxamide; (2) N-(furan-2-yl-methyl)-3-(4-methoxybenzamido)-1H-indazole-5-carboxamide; (3) 3-(4-methoxybenzamido)-N-(thiophen-2-ylmethyl)-1H-indazole-5-carboxamide; (4) 3-(4-methoxybenzamido)-N-methyl-N-(thiophen-2-ylmethyl)-1H-indazole-5-carboxamide; (5) 4-methoxy-N-(5-(4,5,6,7-tetrahydrothieno[2,3-c]pyridine-6-carbonyl)-1H-indazol-3-yl)benzamide (6) 3-(4-(methylthio)benzamido)-N-(thiophen-2-ylmethyl)-1H-indazole-5-carboxamide; (7) 3-(1-methyl-1H-pyrazole-4-carboxamido)-N-(thiophen-2-ylmethyl)-1H-indazole-5-carboxamide; (8) 3-(5-methoxypicolinamido)-N-(thiophen-2-ylmethyl)-1H-indazole-5-carboxamide hydrochloride; (9) 3-(2-methoxynicotinamido)-N-(thiophen-2-ylmethyl)-1H-indazole-5-carboxamide; (10) 3-(4-tert-butylbenzamido)-N-(thiophen-2-ylmethyl)-1H-indazole-5-carboxamide; (11) 4-methoxy-N-(5-((thiophen-2-ylmethyl)amino)-1H-indazol-3-yl)benzamide; (13) 3-benzamido-N-(thiophen-2-ylmethyl)-1H-indazole-5-carboxamide; (14) 3-(4-fluorobenzamido)-N-(1-(thiophen-2-yl)ethyl)-1H-indazole-5-carboxamide; (15) 3-(4-fluorobenzamido)-N-(1-(thiophen-2-yl)cyclopropyl)-1H-indazole-5-carboxamide; (16) N-(1-cyanocyclopropyl)-3-(4-fluorobenzamido)-1H-indazole-5-carboxamide; (17) 3-(4-fluorobenzamido)-N-(1-(thiophen-2-yl)propyl)-1H-indazole-5-carboxamide; (18) 3-(4-fluorobenzamido)-N-(1-(thiophen-2-yl)butyl)-1H-indazole-5-carboxamide; (19) 3-(4-fluorobenzamido)-N-((5-methylthiophen-2-yl)methyl)-1H-indazole-5-carboxamide; (20) 3-(4-fluorobenzamido)-N-(2-phenylpropan-2-yl)-1H-indazole-5-carboxamide; (21) 3-(4-fluorobenzamido)-N-(4-(trifluoromethyl)benzyl)-1H-indazole-5-carboxamide; (22) N-(cyclohexylmethyl)-3-(4-fluorobenzamido)-1H-indazole-5-carboxamide; (23) N-(cyclopropylmethyl)-3-(4-fluorobenzamido)-1H-indazole-5-carboxamide; (24) N-butyl-3-(4-fluorobenzamido)-1H-indazole-5-carboxamide; (25) 3-(4-fluorobenzamido)-N-isopentyl-1H-indazole-5-carboxamide; (26) N-((1,2,4-oxadiazol-3-yl)methyl)-3-(4-fluorobenzamido)-1H-indazole-5-carboxamide; (27) 3-(4-fluorobenzamido)-N-(thiazol-5-ylmethyl)-1H-indazole-5-carboxamide 2,2,2-trifluoroacetate; (28) 3-(4-fluorobenzamido)-N-(pyridin-2-ylmethyl)-1H-indazole-5-carboxamide2,2,2-trifluoroacetate; (29) 3-(4-fluorobenzamido)-N-(pyridin-4-ylmethyl)-1H-indazole-5-carboxamide; (30) N-(cyclopropyl(thiophen-2-yl)methyl)-3-(4-fluorobenzamido)-1H-indazole-5-carboxamide; (33) 3-(4-fluorobenzamido)-N-(3-methyl-1-(thiophen-2-yl)butyl)-1H-indazole-5-carboxamide; (34) 3-(4-fluorobenzamido)-N-(2-(thiophen-2-yl)butan-2-yl)-1H-indazole-5-carboxamide; (35) 3-(2,4-difluorobenzamido)-N-(thiophen-2-ylmethyl)-1H-indazole-5-carboxamide; (36) 3-(4-fluorobenzamido)-N-(thiophen-2-ylmethyl)-1H-indazole-5-carboxamide; (37) 3-(4-fluorobenzamido)-N-(1-phenylethyl)-1H-indazole-5-carboxamide; (38) 3-(4-fluorobenzamido)-N-(1-phenylpropyl)-1H-indazole-5-carboxamide; (39) 3-(phenylsulfonamido)-N-(thiophen-2-ylmethyl)-1H-indazole-5-carboxamide; (40) N-benzyl-3-(4-(4-methylpiperazin-1-yl)benzamido)-1H-indazole-5-carboxamide; (41) N-(1-phenylpropyl)-3-(4-(piperazin-1-yl)benzamido)-1H-indazole-5-carboxamide; (42) N-methyl-3-(4-morpholinobenzamido)-N-(thiophen-2-ylmethyl)-1H-indazole-5-carboxamide; (43) 3-(4-morpholinobenzamido)-N-(1-(thiophen-2-yl)ethyl)-1H-indazole-5-carboxamide; (44) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-(1-(thiophen-2-yl)ethyl)-1H-indazole-5-carboxamide; (45) N-(2-hydroxy-1-(thiophen-2-yl)ethyl)-3-(4-(4-methylpiperazin-1-yl)benzamido)-1H-indazole-5-carboxamide; (46) 3-(4-morpholinobenzamido)-N-(thiophen-3-ylmethyl)-1H-indazole-5-carboxamide; (47) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-(thiophen-3-ylmethyl)-1H-indazole-5-carboxamide; (48) 3-(4-morpholinobenzamido)-N-(1-(thiophen-2-yl)cyclopropyl)-1H-indazole-5-carboxamide; (49) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-(1-(thiophen-2-yl)cyclopropyl)-1H-indazole-5-carboxamide; (50) N-(furan-2-ylmethyl)-3-(4-morpholinobenzamido)-1H-indazole-5-carboxamide; (51) N-(furan-2-ylmethyl)-3-(4-(4-methylpiperazin-1-yl)benzamido)-1H-indazole-5-carboxamide; (52) 3-(4-morpholinobenzamido)-N-(1-(pyridin-3-yl)ethyl)-1H-indazole-5-carboxamide; (53) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-(1-(pyridin-3-yl)ethyl)-1H-indazole-5-carboxamide; (54) 3-(4-morpholinobenzamido)-N-(1-(thiophen-2-yl)propyl)-1H-indazole-5-carboxamide; (55) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-(1-(thiophen-2-yl)propyl)-1H-indazole-5-carboxamide; (56) 3-(4-morpholinobenzamido)-N-(pyridin-3-ylmethyl)-1H-indazole-5-carboxamide 2,2,2-trifluoroacetate; (57) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-(pyridin-3-ylmethyl)-1H-indazole-5-carboxamide bis(2,2,2-trifluoroacetate); (58) 3-(4-morpholinobenzamido)-N-(1-(thiophen-2-yl)butyl)-1H-indazole-5-carboxamide; (59) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-(1-(thiophen-2-yl)butyl)-1H-indazole-5-carboxamide; (60) N-((5-methylthiophen-2-yl)methyl)-3-(4-morpholinobenzamido)-1H-indazole-5-carboxamide; (61) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-((5-methylthiophen-2-yl)methyl)-1H-indazole-5-carboxamide; (62) 3-(4-morpholinobenzamido)-N-(2-phenylpropan-2-yl)-1H-indazole-5-carboxamide; (63) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-(2-phenylpropan-2-yl)-1H-indazole-5-carboxamide; (64) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-(2-phenylpropan-2-yl)-1H-indazole-5-carboxamide hydrochloride; (65) 3-(4-morpholinobenzamido)-N-(4-(trifluoromethyl)benzyl)-1H-indazole-5-carboxamide; (66) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-(4-(trifluoromethyl)benzyl)-1H-indazole-5-carboxamide; (67) 3-(4-morpholinobenzamido)-N-(1-phenylcyclopropyl)-1H-indazole-5-carboxamide; (68) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-(1-phenylcyclopropyl)-1H-indazole-5-carboxamide; (69) N-((2-methylpyridin-4-yl)methyl)-3-(4-morpholinobenzamido)-1H-indazole-5-carboxamide; (70) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-((2-methylpyridin-4-yl)methyl)-1H-indazole-5-carboxamide; (71) 3-(4-morpholinobenzamido)-N-((6-(trifluoromethyl)pyridin-3-yl)methyl)-1H-indazole-5-carboxamide; (72) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-((6-(trifluoromethyl)pyridin-3-yl)methyl)-1H-indazole-5-carboxamide; (73) 3-(2-methyl-4-morpholinobenzamido)-N-(thiophen-2-ylmethyl)-1H-indazole-5-carboxamide; (74) 3-(2-methyl-4-(4-methylpiperazin-1-yl)benzamido)-N-(thiophen-2-ylmethyl)-1H-indazole-5-carboxamide; (75) 3-(3-(4-(4-methylpiperazin-1-yl)benzamido)-1H-indazol-5-yl)-3-oxo-2-(thiophen-2-yl)propanoic acid; (76) (S)-3-(4-(3-methylpiperazin-1-yl)benzamido)-N-(1-phenylcyclopropyl)-1H-indazole-5-carboxamide; (77) (R)-3-(4-(3-methylpiperazin-1-yl)benzamido)-N-(1-phenylcyclopropyl)-1H-indazole-5-carboxamide; (78) 3-(3-methyl-4-morpholinobenzamido)-N-(thiophen-2-ylmethyl)-1H-indazole-5-carboxamide; (79) 3-(3-methyl-4-(4-methylpiperazin-1-yl)benzamido)-N-(thiophen-2-ylmethyl)-1H-indazole-5-carboxamide; (80) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-(1-(thiophen-3-yl)ethyl)-1H-indazole-5-carboxamide; (81) N-(1-(furan-2-yl)ethyl)-3-(4-(4-methylpiperazin-1-yl)benzamido)-1H-indazole-5-carboxamide; (82) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-(1-(thiazol-2-yl)ethyl)-1H-indazole-5-carboxamide; (83) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-(1-(thiazol-5-yl)ethyl)-1H-indazole-5-carboxamide; (84) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-(1-(thiazol-2-yl)propyl)-1H-indazole-5-carboxamide; (85) 3-(4-(4-methylpiperazin-1-yl)benzamido)-N-(pyridin-2-ylmethyl)-1H-indazole-5-carboxamide bis(2,2,2-trifluoroacetate); (86) 3-(4-morpholinobenzamido)-N-(pyridin-2-ylmethyl)-1H-indazole-5-carboxamide; (87) N-(cyclohexylmethyl)-3-(4-(4-methylpiperazin-1-yl)benzamido)-1H-indazole-5-carboxamide; (88) N-(cyclohexylmethyl)-3-(4-morpholinobenzamido)-1H-indazole-5-carboxamide; (89) 3-(4-(3,5-dimethylpiperazin-1-yl)benzamido)-N-(thiophen-2-ylmethyl)-1H-indazole-5-carboxamide 2,2,2-trif
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- C07D231/56Primary
Benzopyrazoles; Hydrogenated benzopyrazoles · CPC title
linked by a chain containing hetero atoms as chain links · CPC title
linked by a chain containing hetero atoms as chain links · CPC title
linked by a chain containing hetero atoms as chain links · CPC title
linked by a chain containing hetero atoms as chain links · CPC title
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- What does patent US10294207B2 cover?
- Provided is pyrazole derivatives as a TNIK (Traf2- and NCK-interacting kinase), IKKε (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor; the pyrazole derivative according to the present invention effectively inhibits TNIK, IKKε and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS canc…
- Who is the assignee on this patent?
- Green Cross Corp
- What technology area does this patent fall under?
- Primary CPC classification C07D231/56. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue May 21 2019 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).