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US-2024383827-A1 · Nov 21, 2024 · US
NON-CATALYTIC SUBSTRATE-SELECTIVE P38alpha-SPECIFIC MAPK INHIBITORS WITH ENDOTHELIAL-STABILIZING AND ANTI-INFLAMMATORY ACTIVITY, AND METHODS OF USE THEREOF
US2019151324A1 · US · A1
| Field | Value |
|---|---|
| Publication number | US-2019151324-A1 |
| Application number | US-201716312499-A |
| Country | US |
| Kind code | A1 |
| Filing date | Jun 22, 2017 |
| Priority date | Jun 23, 2016 |
| Publication date | May 23, 2019 |
| Grant date | — |
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- Title
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- Abstract
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Abstract
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Compounds that inhibit p38α MAPK protein, and methods of using the same, are provided for treating or preventing diseases such as cancer or inflammatory diseases.
First claim
Opening claim text (preview).
1 . (canceled) 2 . A p38-α MAPK inhibitor compound of Formula 1 or Formula 2, or a pharmaceutically acceptable salt, solvate, hydrate, cocrystal, or prodrug thereof: wherein in Formula 1 and Formula 2, Q is —CH— or N; each of R 1 , R 2 , R 3 , and R 4 is independently hydrogen or optionally substituted alkyl, alkoxy, aryl, or heteroaryl; R 5 is —SO 2 —, —CH(OH)—, —O—, or —N(CH 3 )—; each of R 10 and R 10′ is independently —OH, —NH 2 , or —SH; L 1 is —CH 2 —, —C(CH 3 ) 2 — or —C(CH 2 CH 2 )—; each of L 2 and L 3 is independently —CH 2 —, —CH 2 CH 2 —, or —CH 2 CH 2 CH 2 —; each of L 4 , L 5 , and L 5′ is independently —NHCO—, —CONH—, —SO 2 NH—, —NHSO 2 —, or —CH═CH—; each of L 6 and L 6′ is independently an optionally substituted C 1 -C 6 alkyl chain; and Ar 1 is an optionally substituted aryl or heteroaryl ring. 3 . The p38α MAPK inhibitor compound of claim 2 , wherein the compound has any one of Formula 11, Formula 12, Formula 13, or Formula 14, or a pharmaceutically acceptable salt, solvate, hydrate, cocrystal, or prodrug thereof: wherein in Formula 11, Formula 12, Formula 13, and Formula 14, Q is —CH— or N; each of R 1 , R 2 , R 3 , R 4 , R 6 , R 7 , R 8 , and R 9 is independently hydrogen or optionally substituted alkyl, alkoxy, aryl, or heteroaryl; R 5 is —SO 2 —, —CH(OH)—, —O—, or —N(CH 3 )—; L 1 is —CH 2 —, —C(CH 3 ) 2 , or —C(CH 2 CH 2 )—; each of L 2 and L 3 is independently —CH 2 —, —CH 2 CH 2 —, or —CH 2 CH 2 CH 2 —; L 4 is —NHCO—, —CONH—, —SO 2 NH—, —NHSO 2 —, or —CH═CH—; Ar 1 is an optionally substituted aryl or heteroaryl ring; and X is a halogen. 4 . The p38α MAPK inhibitor compound of claim 2 , wherein the compound has any one of Formulas 1001 to 1256, or a pharmaceutically acceptable salt, solvate, hydrate, cocrystal, or prodrug thereof: wherein in Formulas 1001 to 1256, Formula R 3 R 4 R 5 R 9 L 1 L 4 Y 1001 H H —SO 2 — H —CH 2 — —NHCO— CH 1002 —OEt H —SO 2 — H —CH 2 — —NHCO— CH 1003 H Ph —SO 2 — H —CH 2 — —NHCO— CH 1004 —OEt Ph —SO 2 — H —CH 2 — —NHCO— CH 1005 H H —SO 2 — H —C(CH 2 CH 2 )— —NHCO— CH 1006 —OEt H —SO 2 — H —C(CH 2 CH 2 )— —NHCO— CH 1007 H Ph —SO 2 — H —C(CH 2 CH 2 )— —NHCO— CH 1008 —OEt Ph —SO 2 — H —C(CH 2 CH 2 )— —NHCO— CH 1009 H H —SO 2 — 4-oxazolyl —CH 2 — —NHCO— CH 1010 —OEt H —SO 2 — 4-oxazolyl —CH 2 — —NHCO— CH 1011 H Ph —SO 2 — 4-oxazolyl —CH 2 — —NHCO— CH 1012 —OEt Ph —SO 2 — 4-oxazolyl —CH 2 — —NHCO— CH 1013 H H —SO 2 — 4-oxazolyl —C(CH 2 CH 2 )— —NHCO— CH 1014 —OEt H —SO 2 — 4-oxazolyl —C(CH 2 CH 2 )— —NHCO— CH 1015 H Ph —SO 2 — 4-oxazolyl —C(CH 2 CH 2 )— —NHCO— CH 1016 —OEt Ph —SO 2 — 4-oxazolyl —C(CH 2 CH 2 )— —NHCO— CH 1017 H H —CH(OH)— H —CH 2 — —NHCO— CH 1018 —OEt H —CH(OH)— H —CH 2 — —NHCO— CH 1019 H Ph —CH(OH)— H —CH 2 — —NHCO— CH 1020 —OEt Ph —CH(OH)— H —CH 2 — —NHCO— CH 1021 H H —CH(OH)— H —C(CH 2 CH 2 )— —NHCO— CH 1022 —OEt H —CH(OH)— H —C(CH 2 CH 2 )— —NHCO— CH 1023 H Ph —CH(OH)— H —C(CH 2 CH 2 )—
Assignees
Inventors
Classifications
Amides; Imides · CPC title
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms · CPC title
linked by a chain containing hetero atoms as chain links · CPC title
with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings · CPC title
Sulfonamides (compounds containing a para-N-benzene-sulfonyl-N- group A61K31/63) · CPC title
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Frequently asked questions
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- What does patent US2019151324A1 cover?
- Compounds that inhibit p38α MAPK protein, and methods of using the same, are provided for treating or preventing diseases such as cancer or inflammatory diseases.
- Who is the assignee on this patent?
- Univ Maryland, Us Veterans Affairs
- What technology area does this patent fall under?
- Primary CPC classification A61K31/5375. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Thu May 23 2019 00:00:00 GMT+0000 (Coordinated Universal Time) (A1). 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).