JPWO2020038415A5 - - Google Patents
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- Publication number
- JPWO2020038415A5 JPWO2020038415A5 JP2021509151A JP2021509151A JPWO2020038415A5 JP WO2020038415 A5 JPWO2020038415 A5 JP WO2020038415A5 JP 2021509151 A JP2021509151 A JP 2021509151A JP 2021509151 A JP2021509151 A JP 2021509151A JP WO2020038415 A5 JPWO2020038415 A5 JP WO2020038415A5
- Authority
- JP
- Japan
- Prior art keywords
- piperazin
- pyrrolidin
- pyridazin
- imidazo
- pyridin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 15
- 125000000623 heterocyclic group Chemical group 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000005647 linker group Chemical group 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 230000001404 mediated effect Effects 0.000 claims 5
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 5
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- XKJCHHZQLQNZHY-UHFFFAOYSA-N phthalimide Chemical compound C1=CC=C2C(=O)NC(=O)C2=C1 XKJCHHZQLQNZHY-UHFFFAOYSA-N 0.000 claims 4
- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 claims 4
- 125000004452 carbocyclyl group Chemical group 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- GSAFGEITCNSCAJ-YTKQHNFLSA-N 2-(2,6-dioxopiperidin-3-yl)-5-[3-[[4-[6-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]methyl]pyrrolidin-1-yl]isoindole-1,3-dione Chemical compound C1C[C@@H](N(C1)C2=NN3C(=NC=C3C4=NC(=CC=C4)N5CCN(CC5)CC6CCN(C6)C7=CC8=C(C=C7)C(=O)N(C8=O)C9CCC(=O)NC9=O)C=C2)C1=CC(=CC=C1)F GSAFGEITCNSCAJ-YTKQHNFLSA-N 0.000 claims 2
- GUXGUSYUJZREHG-KWRHIPAJSA-N 3-[5-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]-3-oxoprop-1-ynyl]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione Chemical compound FC=1C=C(C=CC=1)[C@@H]1N(CCC1)C=1C=CC=2N(N=1)C(=CN=2)C1=CC=CC(=N1)N1CCN(CC1)C(C#CC1=CC=C2CN(C(C2=C1)=O)C1C(NC(CC1)=O)=O)=O GUXGUSYUJZREHG-KWRHIPAJSA-N 0.000 claims 2
- KORPLFDBDVBAFK-KWRHIPAJSA-N 3-[6-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]-3-oxoprop-1-ynyl]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione Chemical compound FC=1C=C(C=CC=1)[C@@H]1N(CCC1)C=1C=CC=2N(N=1)C(=CN=2)C1=CC=CC(=N1)N1CCN(CC1)C(C#CC=1C=C2CN(C(C2=CC=1)=O)C1C(NC(CC1)=O)=O)=O KORPLFDBDVBAFK-KWRHIPAJSA-N 0.000 claims 2
- RIYXRIJSDXMVNL-PBBFAOSKSA-N N-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]-2-[4-[6-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]acetamide Chemical compound C1N(C2=NC(=CC=C2)C=2N3C(=NC=2)C=CC(N2[C@H](CCC2)C2=CC(F)=CC=C2)=N3)CCN(C1)CC(=O)NC1=CC=2C(=O)N(C(=O)C=2C=C1)C1C(=O)NC(=O)CC1 RIYXRIJSDXMVNL-PBBFAOSKSA-N 0.000 claims 2
- JIGZJNQMIOEJSM-UHFFFAOYSA-N N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-[4-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]amino]ethyl]piperazin-1-yl]-2-(oxan-4-ylamino)benzamide Chemical compound C1C(NC2=C(C(=O)NC=3C4=CC(CC5=CC(F)=CC(F)=C5)=CC=C4NN=3)C=CC(N3CCN(CC3)CCNC3=CC=C4C(=C3)C(=O)N(C4=O)C3C(=O)NC(=O)CC3)=C2)CCOC1 JIGZJNQMIOEJSM-UHFFFAOYSA-N 0.000 claims 2
- HMQGMDOSEOPTJW-UHFFFAOYSA-N N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-[4-[[1-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]azetidin-3-yl]methyl]piperazin-1-yl]-2-(oxan-4-ylamino)benzamide Chemical compound O=C1C(N2C(=O)C3=CC(N4CC(CN5CCN(CC5)C5=CC=C(C(=O)NC=6C7=CC(=CC=C7NN=6)CC6=CC(=CC(=C6)F)F)C(NC6CCOCC6)=C5)C4)=CC=C3C2=O)CCC(=O)N1 HMQGMDOSEOPTJW-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 108091005682 Receptor kinases Proteins 0.000 claims 2
- 102000005937 Tropomyosin Human genes 0.000 claims 2
- 108010030743 Tropomyosin Proteins 0.000 claims 2
- 125000004450 alkenylene group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 230000015556 catabolic process Effects 0.000 claims 2
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 238000006731 degradation reaction Methods 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 239000003446 ligand Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- KNCYXPMJDCCGSJ-UHFFFAOYSA-N piperidine-2,6-dione Chemical compound O=C1CCCC(=O)N1 KNCYXPMJDCCGSJ-UHFFFAOYSA-N 0.000 claims 2
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 2
- 125000006832 (C1-C10) alkylene group Chemical group 0.000 claims 1
- APRUIDKBAJQJRN-XGDNGBMYSA-N 2-(2,6-dioxopiperidin-3-yl)-5-[2-[4-[6-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]ethylamino]isoindole-1,3-dione Chemical compound O=C1NC(CCC1N1C(C2=CC=C(C=C2C1=O)NCCN1CCN(CC1)C1=NC(=CC=C1)C1=CN=C2N1N=C(C=C2)N1[C@H](CCC1)C1=CC(=CC=C1)F)=O)=O APRUIDKBAJQJRN-XGDNGBMYSA-N 0.000 claims 1
- GATVUHGZGNWIHZ-PBBFAOSKSA-N 2-(2,6-dioxopiperidin-3-yl)-5-[[2-[4-[6-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]-2-oxoethyl]amino]isoindole-1,3-dione Chemical compound O=C1NC(CCC1N1C(C2=CC=C(C=C2C1=O)NCC(=O)N1CCN(CC1)C1=NC(=CC=C1)C1=CN=C2N1N=C(C=C2)N1[C@H](CCC1)C1=CC(=CC=C1)F)=O)=O GATVUHGZGNWIHZ-PBBFAOSKSA-N 0.000 claims 1
- HAOMASYZSUGNTB-BONSOQDYSA-N 3-[5-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]propyl]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione Chemical compound FC=1C=C(C=CC=1)[C@@H]1N(CCC1)C=1C=CC=2N(N=1)C(=CN=2)C1=CC=CC(=N1)N1CCN(CC1)CCCC1=CC=C2CN(C(C2=C1)=O)C1C(NC(CC1)=O)=O HAOMASYZSUGNTB-BONSOQDYSA-N 0.000 claims 1
- MDRMKDKRQWVBFF-BONSOQDYSA-N 3-[6-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]propyl]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione Chemical compound FC=1C=C(C=CC=1)[C@@H]1N(CCC1)C=1C=CC=2N(N=1)C(=CN=2)C1=CC=CC(=N1)N1CCN(CC1)CCCC=1C=C2CN(C(C2=CC=1)=O)C1C(NC(CC1)=O)=O MDRMKDKRQWVBFF-BONSOQDYSA-N 0.000 claims 1
- 206010006895 Cachexia Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 208000035473 Communicable disease Diseases 0.000 claims 1
- 208000016192 Demyelinating disease Diseases 0.000 claims 1
- 206010012305 Demyelination Diseases 0.000 claims 1
- 206010067601 Dysmyelination Diseases 0.000 claims 1
- FKUUPOKOGMWVTB-BONSOQDYSA-N O=C1NC(CCC1N1C(C2=CC=C(C=C2C1=O)N1CC(C1)CN1CCN(CC1)C1=NC(=CC=C1)C1=CN=C2N1N=C(C=C2)N1[C@H](CCC1)C1=CC(=CC=C1)F)=O)=O Chemical compound O=C1NC(CCC1N1C(C2=CC=C(C=C2C1=O)N1CC(C1)CN1CCN(CC1)C1=NC(=CC=C1)C1=CN=C2N1N=C(C=C2)N1[C@H](CCC1)C1=CC(=CC=C1)F)=O)=O FKUUPOKOGMWVTB-BONSOQDYSA-N 0.000 claims 1
- 208000003251 Pruritus Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000004419 alkynylene group Chemical group 0.000 claims 1
- 208000022531 anorexia Diseases 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000004566 azetidin-1-yl group Chemical group N1(CCC1)* 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 230000005494 condensation Effects 0.000 claims 1
- 238000009833 condensation Methods 0.000 claims 1
- 206010061428 decreased appetite Diseases 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 230000014509 gene expression Effects 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 230000002018 overexpression Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2018/101715 | 2018-08-22 | ||
| CN2018101715 | 2018-08-22 | ||
| CNPCT/CN2019/086894 | 2019-05-14 | ||
| CN2019086894 | 2019-05-14 | ||
| PCT/CN2019/101850 WO2020038415A1 (fr) | 2018-08-22 | 2019-08-21 | Composés de dégradation de récepteurs à activité kinase liés à la tropomyosine (trk) et méthodes d'utilisation |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021535104A JP2021535104A (ja) | 2021-12-16 |
| JPWO2020038415A5 true JPWO2020038415A5 (fr) | 2022-08-29 |
| JP7472103B2 JP7472103B2 (ja) | 2024-04-22 |
Family
ID=69592803
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021509151A Active JP7472103B2 (ja) | 2018-08-22 | 2019-08-21 | トロポミオシン受容体キナーゼ（ｔｒｋ）分解化合物とその使用方法 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US12065442B2 (fr) |
| EP (1) | EP3841098A4 (fr) |
| JP (1) | JP7472103B2 (fr) |
| KR (1) | KR20210069634A (fr) |
| CN (3) | CN112888681A (fr) |
| AU (1) | AU2019323446A1 (fr) |
| BR (1) | BR112021003098A2 (fr) |
| CA (1) | CA3110267A1 (fr) |
| IL (1) | IL280984B1 (fr) |
| MX (1) | MX2021001957A (fr) |
| WO (1) | WO2020038415A1 (fr) |
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| WO2020038415A1 (fr) | 2018-08-22 | 2020-02-27 | Cullgen (Shanghai), Inc. | Composés de dégradation de récepteurs à activité kinase liés à la tropomyosine (trk) et méthodes d'utilisation |
| US11969472B2 (en) | 2018-08-22 | 2024-04-30 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| GB201820165D0 (en) * | 2018-12-11 | 2019-01-23 | Ucb Biopharma Sprl | Therapeutic agents |
| EP4076536A4 (fr) * | 2019-12-17 | 2024-05-01 | Kymera Therapeutics, Inc. | Agents de dégradation d'irak et leurs utilisations |
| JP2023514872A (ja) * | 2020-02-26 | 2023-04-11 | クルゲン（シャンハイ），インク． | トロポミオシン受容体キナーゼ（ｔｒｋ）分解化合物とその使用方法 |
| JP2023518423A (ja) * | 2020-03-19 | 2023-05-01 | カイメラ セラピューティクス， インコーポレイテッド | Ｍｄｍ２分解剤およびそれらの使用 |
| WO2021222542A1 (fr) * | 2020-04-30 | 2021-11-04 | President And Fellows Of Harvard College | Dérivés de 5-amino-2-pipéridinon-3-yl-1-oxoisoindoline pour la dégradation des agents de dégradation ikzf2 |
| US11739101B2 (en) | 2020-05-06 | 2023-08-29 | Nurix Therapeutics, Inc. | Bifunctional degraders of hematopoietic progenitor kinase and therapeutic uses thereof |
| CN113801062B (zh) * | 2020-06-15 | 2023-05-26 | 沈阳药科大学 | 3-氨基-5-(3,5-二氟苄基)-1h-吲唑的制备方法 |
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| JP2024539269A (ja) * | 2021-10-22 | 2024-10-28 | グルータクス セラピューティクス （シャンハイ） カンパニー、リミテッド | Ｃｒｂｎ ｅ３リガーゼリガンド化合物、当該リガンド化合物に基づいて開発したタンパク質分解剤及びそれらの応用 |
| AU2022388571A1 (en) | 2021-11-10 | 2024-05-09 | Gilead Sciences, Inc. | Bifunctional degraders of hematopoietic progenitor kinase and therapeutic uses thereof |
| EP4180428A1 (fr) | 2021-11-12 | 2023-05-17 | Genzyme Corporation | Composé cristallin d'imidazo[4,5-b]pyridine, compositions pharmaceutiques et leur utilisation dans le traitement d'états médicaux |
| CN114230518A (zh) * | 2021-12-13 | 2022-03-25 | 海南梵圣生物科技有限公司 | 一种5-苄基-1h-吲唑-3-胺类化合物的制备方法 |
| EP4455133A1 (fr) * | 2021-12-24 | 2024-10-30 | Suzhou Kintor Pharmaceuticals, Inc. | Agent de dégradation de multiples protéines pourvu d'un squelette imide |
| WO2023239629A1 (fr) | 2022-06-06 | 2023-12-14 | Plexium, Inc. | Composés et compositions pharmaceutiques qui dégradent cdk2 |
| WO2023249994A1 (fr) * | 2022-06-22 | 2023-12-28 | Mayo Foundation For Medical Education And Research | Méthodes et matériels pour le traitement du cancer |
| TW202412851A (zh) * | 2022-08-05 | 2024-04-01 | 大陸商深圳市新樾生物科技有限公司 | 蛋白激酶降解劑、藥物及應用 |
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2019
- 2019-08-21 WO PCT/CN2019/101850 patent/WO2020038415A1/fr unknown
- 2019-08-21 US US17/269,670 patent/US12065442B2/en active Active
- 2019-08-21 KR KR1020217008232A patent/KR20210069634A/ko unknown
- 2019-08-21 CA CA3110267A patent/CA3110267A1/fr active Pending
- 2019-08-21 EP EP19852808.5A patent/EP3841098A4/fr active Pending
- 2019-08-21 AU AU2019323446A patent/AU2019323446A1/en active Pending
- 2019-08-21 MX MX2021001957A patent/MX2021001957A/es unknown
- 2019-08-21 CN CN201980067402.4A patent/CN112888681A/zh active Pending
- 2019-08-21 JP JP2021509151A patent/JP7472103B2/ja active Active
- 2019-08-21 CN CN202210693243.2A patent/CN115626927B/zh active Active
- 2019-08-21 CN CN202311721460.9A patent/CN118530239A/zh active Pending
- 2019-08-21 BR BR112021003098-0A patent/BR112021003098A2/pt unknown
- 2019-08-21 IL IL280984A patent/IL280984B1/en unknown
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