Compound for androgen receptor degradation, and pharmaceutical use thereof
US-2024383877-A1 · Nov 21, 2024 · US
Kinase inhibitors
US9359354B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9359354-B2 |
| Application number | US-201414296730-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jun 5, 2014 |
| Priority date | Jun 6, 2013 |
| Publication date | Jun 7, 2016 |
| Grant date | Jun 7, 2016 |
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Abstract
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Compounds of formula (I) described herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
First claim
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The invention claimed is: 1. A compound or pharmaceutically acceptable salt, which is a compound selected from the group consisting of 1-[1′-(2-dimethylamino-ethyl)-3-isopropyl-1′H-[1,4′]bipyrazolyl-5-yl]-3-{(1S,4R)-4-[3-((2S,6R)-2,6-dimethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea formate salt; 1-{(1S,4R)-4-[3-((2S,6R)-2,6-dimethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-3-{3-isopropyl-1′-[2-(4-methyl-piperazin-1-yl) -ethyl]-1′H-[1,4′]bipyrazolyl-5-yl}-urea formate salt; 1-{(1S,4R)-4-[3-((2S,6R)-2,6-dimethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-3-[3-isopropyl-1′-(2-pyrrolidin-1-yl-ethyl)-1′H-[1,4′]bipyrazolyl-5-yl]-urea formate salt; 1-{(1S,4R)-4-[3-((2S,6R)-2,6-dimethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-3-[3-isopropyl-1′-(2-[1,4]oxazepan-4-yl-ethyl)-1′H-[1,4′]bipyrazolyl-5-yl]-urea formate salt; 1-[1′-(2-dimethylamino-ethyl)-3-isopropyl-1′H-[1,3′]bipyrazolyl-5-yl]-3-{(1S,4R)-4-[3-((2S,6R)-2,6-dimethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea formate salt; 1-[1′-(2-dimethylamino-ethyl)-3-isopropyl-1′H-[1,4′]bipyrazolyl-5-yl]-3-{(1S,4R)-4-[3-((S)-2-methyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea formate salt; 1-[1′-(2-dimethylamino-ethyl)-3-ethyl-1′H-[1,4′]bipyrazolyl-5-yl]-3-{(1S,4R)-4-[3-((S)-2-methyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea formate salt; 1-[1′-(2-dimethylamino-ethyl)-3-ethyl-1′H-[1,4′]bipyrazolyl-5-yl]-3-{(1S,4R)-4-[3-((2S,6R)-2,6-dimethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea formate salt; 1-{2-[3-(2-dimethylamino-ethoxy)-phenyl]-5-methyl-2H-pyrazol-3-yl}-3-{(1S,4R)-4-[3-((S)-2-methyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea formate salt; 1-[1′-(2-azetidin-1-yl-ethyl)-3-tert-butyl-1′H-[1,4′]bipyrazolyl-5-yl]-3-{(1S,4R)-4-[3-((S)-2-methyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea formate salt; 1-{3-tert-butyl-1′-[2-(3-dimethylamino-azetidin-1-yl)-ethyl]-1′H-[1,4′]bipyrazolyl-5-yl}-3-{(1S,4R)-4-[3-((S)-2-methyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea formate salt; 1-{5-tert-butyl-2-[3-(3-dimethylamino-azetidin-1-ylmethyl)-phenyl]-2H-pyrazol-3-yl}-3-{(1S,4R)-4-[3-((S)-2-methyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea formate salt; 1-(5-tert-butyl-2-methyl-2H-pyrazol-3-yl)-3-((1S,4R)-4-{3-[2,6-dichloro-4-(4-methyl-piperazin-1-ylmethyl)-phenyl]-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy}-1,2,3,4-tetrahydro-naphthalen-1-yl)-urea formate salt; 1-(5-tert-butyl-2-methyl-2H-pyrazol-3-yl)-3-{(1S,4R)-4-[3-(4-dimethylaminomethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea formate salt; 1-(5-tert-butyl-isoxazol-3-yl)-3-{(1S,4R)-4-[3-(4-dimethylaminomethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea; 1-(3-tert-butyl-1′-methyl-1′H-[1,4′]bipyrazolyl-5-yl)-3-{(1S,4R)-4-[3-(4-dimethylaminomethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea formate salt; 1-[3-tert-butyl-1′-(2-dimethylamino-ethyl)-1′H-[1,4′]bipyrazolyl-5-yl]-3-{4-[3-((2S,6R)-2,6-dimethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-cyclohexyl}-urea; 1-(5-tert-butyl)-2-p-tolyl-2H-pyrazol-3-yl)-3-{4-[3-((S)-2-methyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-cyclohexyl}-urea; 1-{5-tert-butyl-2-[3-(2-dimethylamino-ethoxy)-phenyl]-2H-pyrazol-3-yl}-3-{4-[3-((S)-2-methyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-cyclohexyl}-urea; 1-{5-(cyano-dimethyl-methyl)-2-[3-(2-dimethylamino-ethoxy)-phenyl]-2H-pyrazol-3-yl}-3-{(1S,4R)-4-[3-((S)-2-methyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydronaphthalen-1-yl}-urea; 1-{5-(cyano-dimethyl-methyl)-2-[3-(2-dimethylamino-ethoxy)-phenyl]-2H-pyrazol-3-yl}-3-{(1S,4R)-4-[3-((2S,6R)-2,6-dimethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea; 1-(5-tert-butyl-2-methyl-2H-pyrazol-3-yl)-3-((1S,4R)-4-{3-[4-(2-dimethylamino-ethoxy)-piperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy}-1,2,3,4-tetrahydro-naphthalen-1-yl)-urea hydrogen chloride salt; 1-[5-tert-butyl-2-(2-hydroxy-ethyl)-2H-pyrazol-3-yl]-3-((1S,4R)-4-{3-[4-(2-dimethylamino-ethoxy)-piperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy}-1,2,3,4-tetrahydro-naphthalen-1-yl)-urea hydrogen chloride salt; 1-(3-tert-butyl-1′-methyl-1′H-[1,4′]bipyrazolyl-5-yl)-3-((1S,4R)-4-{3-[4-(2-dimethylamino-ethoxy)-piperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy}-1,2,3,4-tetrahydro-naphthalen-1-yl)-urea hydrogen chloride salt; 1-(5-tert-butyl-isoxazol-3-yl)-3-((1S,4R)-4-{3-[4-(2-dimethylamino-ethoxy)-piperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy}-1,2,3,4-tetrahydro-naphthalen-1-yl)-urea hydrogen chloride salt; 1-(5-tert-butyl-2-propyl-2H-pyrazol-3-yl)-3-((1S,4R)-4-{3-[4-(2-dimethylamino-ethoxy)-piperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy}-1,2,3,4-tetrahydro-naphthalen-1-yl)-urea hydrogen chloride salt; 1-[5-tert-butyl-2-(2-methoxy-ethyl)-2H-pyrazol-3-yl]-3-((1S,4R)-4-{3-[4-(2-dimethylamino-ethoxy)-piperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy}-1,2,3,4-tetrahydro-naphthalen-1-yl)-urea hydrogen chloride salt; 1-(5-tert-butyl-2-methyl-2H-pyrazol-3-yl)-3-{(1S,4R)-4-[3-((S)-3-{[(2-hydroxy-ethyl)-methyl-amino]-methyl}-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea hydrogen chloride salt; 1-(5-tert-butyl-2-methyl-2H-pyrazol-3-yl)-3-{(1S,4R)-4-[3-((S)-3-dimethylaminomethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea hydrogen chloride salt; 1-(5-tert-butyl-2-methyl-2H-pyrazol-3-yl)-3-{(1S,4R)-4-[3-(4-{[(2-methoxy-ethyl) -methyl-amino]-methyl}-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea; 1-(5-tert-butyl-2-methyl-2H-pyrazol-3-yl)-3-{(1S,4R)-4-[3-(4-{[(2-hydroxy-ethyl)-methyl-amino]-methyl}-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea hydrogen chloride salt; 1-(5-tert-butyl-2-methyl-2H-pyrazol-3-yl)-3-{(1S,4R)-4-[3-(4-[1,4]oxazepan-4-ylmethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea hydrogen chloride salt; 1-(5-tert-butyl-2-methyl-2H-pyrazol-3-yl)-3-((1S,4R)-4-{3-[4-(4-methyl-piperazin-1-ylmethyl)-piperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy}-1,2,3,4-tetrahydro-naphthalen-1-yl)-urea hydrogen chloride salt; 1-(5-tert-butyl-2-methyl-2H-pyrazol-3-yl)-3-{(1S,4R)-4-[3-((R)-3-{[(2-hydroxy-ethyl)-methyl-amino]-methyl}-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea hydrogen chloride salt; 1-[5-tert-butyl-2-(2-methoxy-ethyl)-2H-pyrazol-3-yl]-3-{(1S,4R)-4-[3-(4-dimethylaminomethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea; 1-(5-tert-butyl-2-ethyl-2H-pyrazol-3-yl)-3-{(1S,4R)-4-[3-(4-dimethylaminomethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea formate salt; N-[5-tert-butyl-3-(3-{(1S,4R)-4-[3-(4-dimethylaminomethyl-piperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-ureido)-2-methoxyphenyl]methanesulfonamide hydrogen chloride salt; 1-(5-tert-butyl-2-methyl-2H-pyrazol-3-yl)-3-{(1S,4R)-4-[3-((2S,4S)-4-dimethylamino-1-methyl-pyrrolidin-2-yl)-[1,2,4]triazolo[4,3-a]pyri
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Antiasthmatics · CPC title
- C07D471/10Primary
Spiro-condensed systems · CPC title
Ortho-condensed systems · CPC title
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- What does patent US9359354B2 cover?
- Compounds of formula (I) described herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
- Who is the assignee on this patent?
- Chiesi Farma Spa
- What technology area does this patent fall under?
- Primary CPC classification C07D471/10. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Jun 07 2016 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).