JPWO2019204537A5 - - Google Patents
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- JPWO2019204537A5 JPWO2019204537A5 JP2020558018A JP2020558018A JPWO2019204537A5 JP WO2019204537 A5 JPWO2019204537 A5 JP WO2019204537A5 JP 2020558018 A JP2020558018 A JP 2020558018A JP 2020558018 A JP2020558018 A JP 2020558018A JP WO2019204537 A5 JPWO2019204537 A5 JP WO2019204537A5
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- Prior art keywords
- disease
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- pharmaceutically acceptable
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- 150000001875 compounds Chemical class 0.000 claims description 26
- 238000000034 method Methods 0.000 claims description 13
- 101001109145 Homo sapiens Receptor-interacting serine/threonine-protein kinase 1 Proteins 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 34
- -1 dehydrogen Chemical class 0.000 claims 25
- 150000003839 salts Chemical class 0.000 claims 22
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 18
- 201000010099 disease Diseases 0.000 claims 17
- 208000035475 disorder Diseases 0.000 claims 17
- 208000011580 syndromic disease Diseases 0.000 claims 12
- 125000004093 cyano group Chemical group *C#N 0.000 claims 11
- 206010033799 Paralysis Diseases 0.000 claims 10
- 208000021090 palsy Diseases 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- 208000002320 spinal muscular atrophy Diseases 0.000 claims 9
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 8
- 206010012289 Dementia Diseases 0.000 claims 8
- 201000007737 Retinal degeneration Diseases 0.000 claims 8
- 208000006011 Stroke Diseases 0.000 claims 8
- 206010051379 Systemic Inflammatory Response Syndrome Diseases 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 201000000585 muscular atrophy Diseases 0.000 claims 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 7
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 7
- 230000000750 progressive effect Effects 0.000 claims 7
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 5
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 5
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 5
- LDSKYBVNIGKJHA-UHFFFAOYSA-N 2h-1,4-oxazine-2-carboxamide Chemical compound NC(=O)C1OC=CN=C1 LDSKYBVNIGKJHA-UHFFFAOYSA-N 0.000 claims 5
- 208000024827 Alzheimer disease Diseases 0.000 claims 5
- 208000023105 Huntington disease Diseases 0.000 claims 5
- 206010020751 Hypersensitivity Diseases 0.000 claims 5
- 208000018737 Parkinson disease Diseases 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000001153 fluoro group Chemical group F* 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 4
- 206010003694 Atrophy Diseases 0.000 claims 4
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 4
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 4
- 206010009900 Colitis ulcerative Diseases 0.000 claims 4
- 208000011231 Crohn disease Diseases 0.000 claims 4
- 208000032843 Hemorrhage Diseases 0.000 claims 4
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 4
- 206010028289 Muscle atrophy Diseases 0.000 claims 4
- 206010033645 Pancreatitis Diseases 0.000 claims 4
- 201000004681 Psoriasis Diseases 0.000 claims 4
- 206010061481 Renal injury Diseases 0.000 claims 4
- 206010063837 Reperfusion injury Diseases 0.000 claims 4
- 206010040047 Sepsis Diseases 0.000 claims 4
- 208000034799 Tauopathies Diseases 0.000 claims 4
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 4
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 4
- 230000001154 acute effect Effects 0.000 claims 4
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 4
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 4
- 230000037444 atrophy Effects 0.000 claims 4
- 208000034158 bleeding Diseases 0.000 claims 4
- 230000000740 bleeding effect Effects 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 208000020832 chronic kidney disease Diseases 0.000 claims 4
- 238000007917 intracranial administration Methods 0.000 claims 4
- 208000028867 ischemia Diseases 0.000 claims 4
- 208000012947 ischemia reperfusion injury Diseases 0.000 claims 4
- 210000003734 kidney Anatomy 0.000 claims 4
- 210000004185 liver Anatomy 0.000 claims 4
- 210000004072 lung Anatomy 0.000 claims 4
- 230000020763 muscle atrophy Effects 0.000 claims 4
- 201000006938 muscular dystrophy Diseases 0.000 claims 4
- 208000010125 myocardial infarction Diseases 0.000 claims 4
- 208000033808 peripheral neuropathy Diseases 0.000 claims 4
- 201000008752 progressive muscular atrophy Diseases 0.000 claims 4
- 230000000241 respiratory effect Effects 0.000 claims 4
- 230000004258 retinal degeneration Effects 0.000 claims 4
- 230000002123 temporal effect Effects 0.000 claims 4
- 230000009529 traumatic brain injury Effects 0.000 claims 4
- LNMJNLPDCAHOPL-UHFFFAOYSA-N 1H-pyrazolo[3,4-d]pyrimidine-6-carboxamide Chemical compound N=1N=CC=2C=1NC(=NC=2)C(=O)N LNMJNLPDCAHOPL-UHFFFAOYSA-N 0.000 claims 3
- 201000001320 Atherosclerosis Diseases 0.000 claims 3
- 208000016192 Demyelinating disease Diseases 0.000 claims 3
- 208000032319 Primary lateral sclerosis Diseases 0.000 claims 3
- 208000034189 Sclerosis Diseases 0.000 claims 3
- 206010046298 Upper motor neurone lesion Diseases 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 230000002490 cerebral effect Effects 0.000 claims 3
- 230000001054 cortical effect Effects 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 230000007850 degeneration Effects 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 201000010901 lateral sclerosis Diseases 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 208000005264 motor neuron disease Diseases 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 239000011593 sulfur Substances 0.000 claims 2
- FLIVEWVRMQLLJL-HHXXYDBFSA-N (4R,6R)-4-fluoro-N-[(3S)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-6-phenyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole-2-carboxamide Chemical compound CN1C2=C(OC[C@H](NC(=O)C3=NN4[C@H](C[C@@H](F)C4=C3)C3=CC=CC=C3)C1=O)C=CC=C2 FLIVEWVRMQLLJL-HHXXYDBFSA-N 0.000 claims 1
- FLIVEWVRMQLLJL-IEZWGBDMSA-N (4S,6S)-4-fluoro-N-[(3S)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-6-phenyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole-2-carboxamide Chemical compound F[C@H]1C[C@H](N2N=C(C=C21)C(=O)N[C@H]1COC2=C(N(C1=O)C)C=CC=C2)C1=CC=CC=C1 FLIVEWVRMQLLJL-IEZWGBDMSA-N 0.000 claims 1
- 125000006661 (C4-C6) heterocyclic group Chemical group 0.000 claims 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 125000001960 7 membered carbocyclic group Chemical group 0.000 claims 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- SLZYJBMRHYNCKC-UHFFFAOYSA-N 7H-pyrazolo[4,3-c]pyridine-6-carboxamide Chemical compound N=1N=CC2=CN=C(CC2=1)C(=O)N SLZYJBMRHYNCKC-UHFFFAOYSA-N 0.000 claims 1
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 210000001367 artery Anatomy 0.000 claims 1
- 230000003143 atherosclerotic effect Effects 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 1
- 229960004316 cisplatin Drugs 0.000 claims 1
- 125000004980 cyclopropylene group Chemical group 0.000 claims 1
- 229910052805 deuterium Inorganic materials 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 210000003205 muscle Anatomy 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- 125000004001 thioalkyl group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862660397P | 2018-04-20 | 2018-04-20 | |
| US62/660,397 | 2018-04-20 | ||
| PCT/US2019/028011 WO2019204537A1 (en) | 2018-04-20 | 2019-04-18 | N-[4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazol e-2-carboxamide derivatives and related compounds as rip1 kinase inhibitors for treating e.g. irritable bowel syndrome (ibs) |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021522206A JP2021522206A (ja) | 2021-08-30 |
| JPWO2019204537A5 true JPWO2019204537A5 (https=) | 2022-04-22 |
| JP2021522206A5 JP2021522206A5 (https=) | 2022-04-22 |
| JP7398391B2 JP7398391B2 (ja) | 2023-12-14 |
Family
ID=66397474
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020558018A Active JP7398391B2 (ja) | 2018-04-20 | 2019-04-18 | Ｎ－［４－オキソ－２，３－ジヒドロ－１，５－ベンズオキサゼピン－３－イル］－５，６－ジヒドロ－４Ｈ－ピロロ［１，２－ｂ］ピラゾール－２－カルボキサミド誘導体及び例えば過敏性腸症候群（ＩＢＳ）を処置するためのＲＩＰ１キナーゼ阻害剤としての関連化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US11634436B2 (https=) |
| EP (1) | EP3781571B1 (https=) |
| JP (1) | JP7398391B2 (https=) |
| CN (1) | CN112074519B (https=) |
| WO (1) | WO2019204537A1 (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI763630B (zh) | 2015-07-02 | 2022-05-11 | 瑞士商赫孚孟拉羅股份公司 | 雙環內醯胺及其使用方法 |
| EP3526219B1 (en) | 2016-10-17 | 2021-12-15 | F. Hoffmann-La Roche AG | Bicyclic pyridone lactams and methods of use thereof |
| US11072607B2 (en) | 2016-12-16 | 2021-07-27 | Genentech, Inc. | Inhibitors of RIP1 kinase and methods of use thereof |
| CN112689636B (zh) | 2018-09-10 | 2024-08-20 | 科研制药株式会社 | 新型杂原子芳香族酰胺衍生物以及含有其的药剂 |
| WO2021046515A1 (en) | 2019-09-06 | 2021-03-11 | Board Of Regents, The University Of Texas System | Inhibitors of receptor interacting protein kinase i for the treatment of disease |
| IL291665B2 (en) | 2019-09-27 | 2025-07-01 | Univ Texas | Inhibitors of receptor interacting protein kinase i for the treatment of disease |
| JP2023502514A (ja) * | 2019-11-26 | 2023-01-24 | ボード オブ レジェンツ，ザ ユニバーシティ オブ テキサス システム | 疾患の処置のための受容体相互作用プロテインキナーゼｉの阻害剤 |
| JP7701162B2 (ja) * | 2020-02-28 | 2025-07-01 | 科研製薬株式会社 | 新規ヘテロ芳香族アミド誘導体又はその塩からなる医薬 |
| AU2021225921A1 (en) * | 2020-02-28 | 2022-09-22 | Board Of Regents, The University Of Texas System | Inhibitors of Receptor Interacting Protein Kinase I for the treatment of disease |
| AR121717A1 (es) * | 2020-04-02 | 2022-06-29 | Rigel Pharmaceuticals Inc | Inhibidores de rip1k |
| CN115038707B (zh) * | 2020-05-14 | 2024-11-22 | 中国医药研究开发中心有限公司 | 氮杂卓类稠环化合物及其医药用途 |
| TW202214617A (zh) | 2020-06-02 | 2022-04-16 | 法商賽諾菲公司 | 作為ｒｉｐｋ１抑制劑之異㗁唑啶及其用途 |
| GB202010409D0 (en) * | 2020-07-07 | 2020-08-19 | Reviral Ltd | Pharmaceutical compounds |
| AU2021329777A1 (en) * | 2020-08-18 | 2023-03-09 | Hutchison Medipharma Limited | Pyrimidinone compounds and uses thereof |
| WO2022171111A1 (en) * | 2021-02-10 | 2022-08-18 | Zai Lab (Us) Llc | Heteroaryl-fused bicyclic compound as rip1-kinase inhibitors and uses thereof |
| WO2023020486A1 (zh) * | 2021-08-17 | 2023-02-23 | 广州市恒诺康医药科技有限公司 | Rip1激酶抑制剂类化合物及其组合物和用途 |
| CN115806557B (zh) * | 2021-09-14 | 2025-02-14 | 中国科学院上海有机化学研究所 | 抑制细胞程序性死亡的化合物及其制备方法 |
| WO2023083847A1 (en) | 2021-11-11 | 2023-05-19 | Sanofi | Isoxazolidines as ripk1 inhibitors and use thereof |
| WO2023109918A1 (zh) * | 2021-12-17 | 2023-06-22 | 中国科学院上海药物研究所 | 含氮杂环化合物、其制备方法及其用途 |
| CN116640156B (zh) * | 2022-02-22 | 2025-10-24 | 上海齐鲁制药研究中心有限公司 | Ripk1抑制剂 |
| CN117645579A (zh) * | 2022-09-02 | 2024-03-05 | 科辉智药生物科技(深圳)有限公司 | 作为ripk1抑制剂的氮杂䓬类稠环化合物及其应用 |
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| TWI763630B (zh) | 2015-07-02 | 2022-05-11 | 瑞士商赫孚孟拉羅股份公司 | 雙環內醯胺及其使用方法 |
| CN108602809B (zh) | 2015-12-04 | 2022-09-30 | 戴纳立制药公司 | 异噁唑烷衍生的受体相互作用蛋白激酶1(ripk 1)的抑制剂 |
| CN108430992A (zh) * | 2015-12-17 | 2018-08-21 | 阿斯特克斯医疗公司 | 作为h-pgds抑制剂的喹啉-3-甲酰胺 |
| WO2017109724A1 (en) | 2015-12-21 | 2017-06-29 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides as kinase inhibitors |
| CA3009324A1 (en) | 2015-12-23 | 2017-06-29 | President And Fellows Of Harvard College | Cortistatin analogs and uses thereof |
| MA44007A (fr) | 2016-02-05 | 2018-12-19 | Denali Therapeutics Inc | Inhibiteurs du récepteur interagissant avec protéine kinase 1 |
| EP3526219B1 (en) | 2016-10-17 | 2021-12-15 | F. Hoffmann-La Roche AG | Bicyclic pyridone lactams and methods of use thereof |
| US11072607B2 (en) | 2016-12-16 | 2021-07-27 | Genentech, Inc. | Inhibitors of RIP1 kinase and methods of use thereof |
-
2019
- 2019-04-18 WO PCT/US2019/028011 patent/WO2019204537A1/en not_active Ceased
- 2019-04-18 CN CN201980026880.0A patent/CN112074519B/zh active Active
- 2019-04-18 EP EP19721945.4A patent/EP3781571B1/en active Active
- 2019-04-18 JP JP2020558018A patent/JP7398391B2/ja active Active
-
2020
- 2020-10-09 US US17/067,638 patent/US11634436B2/en active Active
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