JP7013453B2 - 内皮安定化及び抗炎症活性を有する非触媒基質選択的ｐ３８α特異的ＭＡＰＫ阻害剤、及びその使用方法 - Google Patents

内皮安定化及び抗炎症活性を有する非触媒基質選択的ｐ３８α特異的ＭＡＰＫ阻害剤、及びその使用方法 Download PDF

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JP7013453B2
JP7013453B2 JP2019519608A JP2019519608A JP7013453B2 JP 7013453 B2 JP7013453 B2 JP 7013453B2 JP 2019519608 A JP2019519608 A JP 2019519608A JP 2019519608 A JP2019519608 A JP 2019519608A JP 7013453 B2 JP7013453 B2 JP 7013453B2
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cancer
mapk
pharmaceutical composition
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JP2019527239A5 (OSRAM
JP2019527239A (ja
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シャピロ，ポール
ハスデイ，ジェフリー
マッケレル，アレキサンダー
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ザ ユナイテッド ステイツ オブ アメリカ アズ リプレゼンティッド バイ ザ デパートメント オブ ベテランズ アフェアーズ アズ リプレゼンティッド バイ ザ デパートメント オブ ベテランズ アフェアーズ オフィス オブ ジェネラル カウンセル - ピーエスジー アイブイ (024)
University of Maryland Baltimore
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ザ ユナイテッド ステイツ オブ アメリカ アズ リプレゼンティッド バイ ザ デパートメント オブ ベテランズ アフェアーズ アズ リプレゼンティッド バイ ザ デパートメント オブ ベテランズ アフェアーズ オフィス オブ ジェネラル カウンセル - ピーエスジー アイブイ (024)
University of Maryland Baltimore
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • A61K31/16—Amides, e.g. hydroxamic acids
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    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
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    • A—HUMAN NECESSITIES
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    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/06—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals
    • C07D295/073—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • General Health & Medical Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
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  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2019519608A 2016-06-23 2017-06-22 内皮安定化及び抗炎症活性を有する非触媒基質選択的ｐ３８α特異的ＭＡＰＫ阻害剤、及びその使用方法 Active JP7013453B2 (ja)

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US201662353856P 2016-06-23 2016-06-23
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US201762469913P 2017-03-10 2017-03-10
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PCT/US2017/038697 WO2017223284A1 (en) 2016-06-23 2017-06-22 NON-CATALYTIC SUBSTRATE-SELECTIVE P38α-SPECIFIC MAPK INHIBITORS WITH ENDOTHELIAL-STABILIZING AND ANTI-INFLAMMATORY ACTIVITY, AND METHODS OF USE THEREOF

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JP2022046803A (ja) * 2016-06-23 2022-03-23 ユニバーシティ・オブ・メリーランド・ボルティモア 内皮安定化及び抗炎症活性を有する非触媒基質選択的ｐ３８α特異的ＭＡＰＫ阻害剤、及びその使用方法
US11926635B2 (en) 2020-05-18 2024-03-12 Gen1E Lifesciences Inc. P38α mitogen-activated protein kinase inhibitors
US11976049B2 (en) 2021-03-23 2024-05-07 Gen1E Lifesciences Inc. Substituted naphthyl p38alpha mitogen-activated protein kinase inhibitors
US12202810B2 (en) 2018-12-07 2025-01-21 University Of Maryland, Baltimore Non-ATP/catalytic site p38 mitogen activated protein kinase inhibitors
US12269792B2 (en) 2020-10-29 2025-04-08 Genie Lifesciences Inc. Crystalline 5-(dimethylamino)-N-(4-(morpholinomethyl) phenyl)naphthalene-1-sulfonamide di-hydrochloride di-hydrate

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Cited By (8)

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JP2022046803A (ja) * 2016-06-23 2022-03-23 ユニバーシティ・オブ・メリーランド・ボルティモア 内皮安定化及び抗炎症活性を有する非触媒基質選択的ｐ３８α特異的ＭＡＰＫ阻害剤、及びその使用方法
US11911393B2 (en) 2016-06-23 2024-02-27 University Of Maryland, Baltimore Non-catalytic substrate-selective p38alpha-specific MAPK inhibitors with endothelial-stabilizing and anti-inflammatory activity, and methods of use thereof
US11911392B2 (en) 2016-06-23 2024-02-27 University Of Maryland, Baltimore Non-catalytic substrate-selective p38α-specific MAPK inhibitors with endothelial-stabilizing and anti-inflammatory activity, and methods of use thereof
US12202810B2 (en) 2018-12-07 2025-01-21 University Of Maryland, Baltimore Non-ATP/catalytic site p38 mitogen activated protein kinase inhibitors
US11926635B2 (en) 2020-05-18 2024-03-12 Gen1E Lifesciences Inc. P38α mitogen-activated protein kinase inhibitors
US12269792B2 (en) 2020-10-29 2025-04-08 Genie Lifesciences Inc. Crystalline 5-(dimethylamino)-N-(4-(morpholinomethyl) phenyl)naphthalene-1-sulfonamide di-hydrochloride di-hydrate
US11976049B2 (en) 2021-03-23 2024-05-07 Gen1E Lifesciences Inc. Substituted naphthyl p38alpha mitogen-activated protein kinase inhibitors
US12331024B2 (en) 2021-03-23 2025-06-17 Gen1E Lifesciences Inc. Substituted naphthyl P38alpha mitogen-activated protein kinase inhibitors

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US20190151324A1 (en) 2019-05-23
EP3474835B1 (en) 2023-07-05
US20240366619A1 (en) 2024-11-07
EP3474835C0 (en) 2023-07-05
US11357781B2 (en) 2022-06-14
AU2017281222A1 (en) 2019-01-24
US20210267987A1 (en) 2021-09-02
US11911393B2 (en) 2024-02-27
AU2024202879B2 (en) 2025-08-14
EP3474835A1 (en) 2019-05-01
US20220331329A1 (en) 2022-10-20
JP2019527239A (ja) 2019-09-26
EP3474835A4 (en) 2020-04-29
WO2017223284A1 (en) 2017-12-28
JP7372993B2 (ja) 2023-11-01
AU2025259977A1 (en) 2025-11-20
CN116570594A (zh) 2023-08-11
US11911392B2 (en) 2024-02-27
CN109640970A (zh) 2019-04-16
AU2017281222B2 (en) 2022-06-16
AU2022218616B2 (en) 2024-02-29
AU2022218616A1 (en) 2022-09-15
CN109640970B (zh) 2023-05-23
AU2024202879A1 (en) 2024-05-23
JP2022046803A (ja) 2022-03-23

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