JP2024178191A5 - - Google Patents
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- JP2024178191A5 JP2024178191A5 JP2024146579A JP2024146579A JP2024178191A5 JP 2024178191 A5 JP2024178191 A5 JP 2024178191A5 JP 2024146579 A JP2024146579 A JP 2024146579A JP 2024146579 A JP2024146579 A JP 2024146579A JP 2024178191 A5 JP2024178191 A5 JP 2024178191A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- methyl
- ptm
- halogen
- ilm
- 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.)
- Pending
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 70
- 229910052736 halogen Inorganic materials 0.000 claims 60
- 150000002367 halogens Chemical class 0.000 claims 60
- 125000000217 alkyl group Chemical group 0.000 claims 48
- 229910052799 carbon Chemical group 0.000 claims 44
- 239000000126 substance Substances 0.000 claims 42
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 37
- 150000001875 compounds Chemical class 0.000 claims 36
- 125000005647 linker group Chemical group 0.000 claims 35
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 32
- 229910052757 nitrogen Inorganic materials 0.000 claims 31
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 29
- 229910052731 fluorine Inorganic materials 0.000 claims 28
- 229910052794 bromium Inorganic materials 0.000 claims 27
- 229910052801 chlorine Inorganic materials 0.000 claims 27
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 25
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 23
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 21
- 125000001424 substituent group Chemical group 0.000 claims 20
- 150000001721 carbon Chemical group 0.000 claims 19
- -1 polymorph Substances 0.000 claims 18
- 125000003342 alkenyl group Chemical group 0.000 claims 17
- 125000003118 aryl group Chemical group 0.000 claims 15
- 229910052760 oxygen Inorganic materials 0.000 claims 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 13
- 125000004429 atom Chemical group 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000000203 mixture Substances 0.000 claims 12
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 11
- 125000000753 cycloalkyl group Chemical group 0.000 claims 11
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 11
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 11
- 125000001188 haloalkyl group Chemical group 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 102000013498 tau Proteins Human genes 0.000 claims 10
- 108010026424 tau Proteins Proteins 0.000 claims 10
- 125000000304 alkynyl group Chemical group 0.000 claims 9
- 125000005842 heteroatom Chemical group 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 125000004432 carbon atom Chemical group C* 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 7
- 125000000524 functional group Chemical group 0.000 claims 7
- 208000035475 disorder Diseases 0.000 claims 6
- 125000002619 bicyclic group Chemical group 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 claims 4
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 claims 4
- 230000001588 bifunctional effect Effects 0.000 claims 4
- 125000004663 dialkyl amino group Chemical group 0.000 claims 4
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 230000017854 proteolysis Effects 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 230000000707 stereoselective effect Effects 0.000 claims 4
- 125000000547 substituted alkyl group Chemical group 0.000 claims 4
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 claims 3
- 208000034799 Tauopathies Diseases 0.000 claims 3
- 239000012867 bioactive agent Substances 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 2
- 125000004777 2-fluoroethyl group Chemical group [H]C([H])(F)C([H])([H])* 0.000 claims 2
- 102100033350 ATP-dependent translocase ABCB1 Human genes 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 108091007065 BIRCs Proteins 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 2
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 2
- 101001017818 Homo sapiens ATP-dependent translocase ABCB1 Proteins 0.000 claims 2
- 102000055031 Inhibitor of Apoptosis Proteins Human genes 0.000 claims 2
- 101150051118 PTM1 gene Proteins 0.000 claims 2
- REFJWTPEDVJJIY-UHFFFAOYSA-N Quercetin Chemical compound C=1C(O)=CC(O)=C(C(C=2O)=O)C=1OC=2C1=CC=C(O)C(O)=C1 REFJWTPEDVJJIY-UHFFFAOYSA-N 0.000 claims 2
- LOUPRKONTZGTKE-WZBLMQSHSA-N Quinine Chemical compound C([C@H]([C@H](C1)C=C)C2)C[N@@]1[C@@H]2[C@H](O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-WZBLMQSHSA-N 0.000 claims 2
- 238000009825 accumulation Methods 0.000 claims 2
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 claims 2
- 125000004442 acylamino group Chemical group 0.000 claims 2
- 238000004220 aggregation Methods 0.000 claims 2
- 230000002776 aggregation Effects 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- LOUPRKONTZGTKE-UHFFFAOYSA-N cinchonine Natural products C1C(C(C2)C=C)CCN2C1C(O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-UHFFFAOYSA-N 0.000 claims 2
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 206010015037 epilepsy Diseases 0.000 claims 2
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 2
- 230000004927 fusion Effects 0.000 claims 2
- 238000001727 in vivo Methods 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 2
- LOUPRKONTZGTKE-LHHVKLHASA-N quinidine Chemical compound C([C@H]([C@H](C1)C=C)C2)C[N@@]1[C@H]2[C@@H](O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-LHHVKLHASA-N 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 125000003003 spiro group Chemical group 0.000 claims 2
- DNXIKVLOVZVMQF-UHFFFAOYSA-N (3beta,16beta,17alpha,18beta,20alpha)-17-hydroxy-11-methoxy-18-[(3,4,5-trimethoxybenzoyl)oxy]-yohimban-16-carboxylic acid, methyl ester Natural products C1C2CN3CCC(C4=CC=C(OC)C=C4N4)=C4C3CC2C(C(=O)OC)C(O)C1OC(=O)C1=CC(OC)=C(OC)C(OC)=C1 DNXIKVLOVZVMQF-UHFFFAOYSA-N 0.000 claims 1
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 1
- 125000006677 (C1-C3) haloalkoxy group Chemical group 0.000 claims 1
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 1
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 1
- SGTNSNPWRIOYBX-UHFFFAOYSA-N 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile Chemical compound C1=C(OC)C(OC)=CC=C1CCN(C)CCCC(C#N)(C(C)C)C1=CC=C(OC)C(OC)=C1 SGTNSNPWRIOYBX-UHFFFAOYSA-N 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- 208000031277 Amaurotic familial idiocy Diseases 0.000 claims 1
- ITPDYQOUSLNIHG-UHFFFAOYSA-N Amiodarone hydrochloride Chemical group [Cl-].CCCCC=1OC2=CC=CC=C2C=1C(=O)C1=CC(I)=C(OCC[NH+](CC)CC)C(I)=C1 ITPDYQOUSLNIHG-UHFFFAOYSA-N 0.000 claims 1
- 208000022211 Arteriovenous Malformations Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 125000004650 C1-C8 alkynyl group Chemical group 0.000 claims 1
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 1
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 1
- 208000000483 Central Nervous System Vascular Malformations Diseases 0.000 claims 1
- 235000001258 Cinchona calisaya Nutrition 0.000 claims 1
- PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 claims 1
- 108010036949 Cyclosporine Proteins 0.000 claims 1
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical compound F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 claims 1
- 108010081348 HRT1 protein Hairy Proteins 0.000 claims 1
- 102100021881 Hairy/enhancer-of-split related with YRPW motif protein 1 Human genes 0.000 claims 1
- 206010019233 Headaches Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 201000008450 Intracranial aneurysm Diseases 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 201000009906 Meningitis Diseases 0.000 claims 1
- 102100040243 Microtubule-associated protein tau Human genes 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 208000009905 Neurofibromatoses Diseases 0.000 claims 1
- 208000002537 Neuronal Ceroid-Lipofuscinoses Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims 1
- 102100032783 Protein cereblon Human genes 0.000 claims 1
- ZVOLCUVKHLEPEV-UHFFFAOYSA-N Quercetagetin Natural products C1=C(O)C(O)=CC=C1C1=C(O)C(=O)C2=C(O)C(O)=C(O)C=C2O1 ZVOLCUVKHLEPEV-UHFFFAOYSA-N 0.000 claims 1
- LCQMZZCPPSWADO-UHFFFAOYSA-N Reserpilin Natural products COC(=O)C1COCC2CN3CCc4c([nH]c5cc(OC)c(OC)cc45)C3CC12 LCQMZZCPPSWADO-UHFFFAOYSA-N 0.000 claims 1
- QEVHRUUCFGRFIF-SFWBKIHZSA-N Reserpine Natural products O=C(OC)[C@@H]1[C@H](OC)[C@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)C[C@H]2[C@@H]1C[C@H]1N(C2)CCc2c3c([nH]c12)cc(OC)cc3 QEVHRUUCFGRFIF-SFWBKIHZSA-N 0.000 claims 1
- HWTZYBCRDDUBJY-UHFFFAOYSA-N Rhynchosin Natural products C1=C(O)C(O)=CC=C1C1=C(O)C(=O)C2=CC(O)=C(O)C=C2O1 HWTZYBCRDDUBJY-UHFFFAOYSA-N 0.000 claims 1
- NCDNCNXCDXHOMX-UHFFFAOYSA-N Ritonavir Natural products C=1C=CC=CC=1CC(NC(=O)OCC=1SC=NC=1)C(O)CC(CC=1C=CC=CC=1)NC(=O)C(C(C)C)NC(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-UHFFFAOYSA-N 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- LGGHDPFKSSRQNS-UHFFFAOYSA-N Tariquidar Chemical compound C1=CC=CC2=CC(C(=O)NC3=CC(OC)=C(OC)C=C3C(=O)NC3=CC=C(C=C3)CCN3CCC=4C=C(C(=CC=4C3)OC)OC)=CN=C21 LGGHDPFKSSRQNS-UHFFFAOYSA-N 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- 229960005260 amiodarone Drugs 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 230000002555 anti-neurodegenerative effect Effects 0.000 claims 1
- 230000005744 arteriovenous malformation Effects 0.000 claims 1
- 229960004099 azithromycin Drugs 0.000 claims 1
- MQTOSJVFKKJCRP-BICOPXKESA-N azithromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)N(C)C[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 MQTOSJVFKKJCRP-BICOPXKESA-N 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 229960000830 captopril Drugs 0.000 claims 1
- FAKRSMQSSFJEIM-RQJHMYQMSA-N captopril Chemical compound SC[C@@H](C)C(=O)N1CCC[C@H]1C(O)=O FAKRSMQSSFJEIM-RQJHMYQMSA-N 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229960001265 ciclosporin Drugs 0.000 claims 1
- 229960002626 clarithromycin Drugs 0.000 claims 1
- AGOYDEPGAOXOCK-KCBOHYOISA-N clarithromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@](C)([C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)OC)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 AGOYDEPGAOXOCK-KCBOHYOISA-N 0.000 claims 1
- 229930182912 cyclosporin Natural products 0.000 claims 1
- 230000006378 damage Effects 0.000 claims 1
- 229950005476 elacridar Drugs 0.000 claims 1
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 231100000869 headache Toxicity 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 208000017476 juvenile neuronal ceroid lipofuscinosis Diseases 0.000 claims 1
- MWDZOUNAPSSOEL-UHFFFAOYSA-N kaempferol Natural products OC1=C(C(=O)c2cc(O)cc(O)c2O1)c3ccc(O)cc3 MWDZOUNAPSSOEL-UHFFFAOYSA-N 0.000 claims 1
- 238000010172 mouse model Methods 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000006938 muscular dystrophy Diseases 0.000 claims 1
- OSFCMRGOZNQUSW-UHFFFAOYSA-N n-[4-[2-(6,7-dimethoxy-3,4-dihydro-1h-isoquinolin-2-yl)ethyl]phenyl]-5-methoxy-9-oxo-10h-acridine-4-carboxamide Chemical compound N1C2=C(OC)C=CC=C2C(=O)C2=C1C(C(=O)NC1=CC=C(C=C1)CCN1CCC=3C=C(C(=CC=3C1)OC)OC)=CC=C2 OSFCMRGOZNQUSW-UHFFFAOYSA-N 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 201000004931 neurofibromatosis Diseases 0.000 claims 1
- 201000007607 neuronal ceroid lipofuscinosis 3 Diseases 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- MXXWOMGUGJBKIW-YPCIICBESA-N piperine Chemical compound C=1C=C2OCOC2=CC=1/C=C/C=C/C(=O)N1CCCCC1 MXXWOMGUGJBKIW-YPCIICBESA-N 0.000 claims 1
- 229940075559 piperine Drugs 0.000 claims 1
- WVWHRXVVAYXKDE-UHFFFAOYSA-N piperine Natural products O=C(C=CC=Cc1ccc2OCOc2c1)C3CCCCN3 WVWHRXVVAYXKDE-UHFFFAOYSA-N 0.000 claims 1
- 235000019100 piperine Nutrition 0.000 claims 1
- 229960001285 quercetin Drugs 0.000 claims 1
- 235000005875 quercetin Nutrition 0.000 claims 1
- 229960001404 quinidine Drugs 0.000 claims 1
- 229960000948 quinine Drugs 0.000 claims 1
- BJOIZNZVOZKDIG-MDEJGZGSSA-N reserpine Chemical compound O([C@H]1[C@@H]([C@H]([C@H]2C[C@@H]3C4=C([C]5C=CC(OC)=CC5=N4)CCN3C[C@H]2C1)C(=O)OC)OC)C(=O)C1=CC(OC)=C(OC)C(OC)=C1 BJOIZNZVOZKDIG-MDEJGZGSSA-N 0.000 claims 1
- 229960003147 reserpine Drugs 0.000 claims 1
- NCDNCNXCDXHOMX-XGKFQTDJSA-N ritonavir Chemical compound N([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1SC=NC=1)CC=1C=CC=CC=1)C(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-XGKFQTDJSA-N 0.000 claims 1
- 229960000311 ritonavir Drugs 0.000 claims 1
- MDMGHDFNKNZPAU-UHFFFAOYSA-N roserpine Natural products C1C2CN3CCC(C4=CC=C(OC)C=C4N4)=C4C3CC2C(OC(C)=O)C(OC)C1OC(=O)C1=CC(OC)=C(OC)C(OC)=C1 MDMGHDFNKNZPAU-UHFFFAOYSA-N 0.000 claims 1
- 150000003384 small molecules Chemical class 0.000 claims 1
- 210000000278 spinal cord Anatomy 0.000 claims 1
- 208000037959 spinal tumor Diseases 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 229950005890 tariquidar Drugs 0.000 claims 1
- 229960001722 verapamil Drugs 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962875500P | 2019-07-17 | 2019-07-17 | |
| US62/875,500 | 2019-07-17 | ||
| PCT/US2020/042645 WO2021011913A1 (en) | 2019-07-17 | 2020-07-17 | Tau-protein targeting compounds and associated methods of use |
| JP2022502929A JP7548992B2 (ja) | 2019-07-17 | 2020-07-17 | タウタンパク質標的化化合物および関連する使用方法 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022502929A Division JP7548992B2 (ja) | 2019-07-17 | 2020-07-17 | タウタンパク質標的化化合物および関連する使用方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2024178191A JP2024178191A (ja) | 2024-12-24 |
| JP2024178191A5 true JP2024178191A5 (https=) | 2025-03-24 |
Family
ID=71996063
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022502929A Active JP7548992B2 (ja) | 2019-07-17 | 2020-07-17 | タウタンパク質標的化化合物および関連する使用方法 |
| JP2024146579A Pending JP2024178191A (ja) | 2019-07-17 | 2024-08-28 | タウタンパク質標的化化合物および関連する使用方法 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022502929A Active JP7548992B2 (ja) | 2019-07-17 | 2020-07-17 | タウタンパク質標的化化合物および関連する使用方法 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US11912699B2 (https=) |
| EP (1) | EP3999182A1 (https=) |
| JP (2) | JP7548992B2 (https=) |
| CN (2) | CN119954801A (https=) |
| WO (1) | WO2021011913A1 (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2767532T3 (en) | 2012-12-21 | 2016-09-12 | Nat Inst For Quantum And Radiological Science And Tech | New connection for reproduction of tau protein heavy in the brain. |
| WO2019195609A2 (en) | 2018-04-04 | 2019-10-10 | Arvinas Operations, Inc. | Modulators of proteolysis and associated methods of use |
| TW201946624A (zh) | 2018-05-09 | 2019-12-16 | 新旭生技股份有限公司 | 雜芳基化合物及其用途 |
| EP3999182A1 (en) * | 2019-07-17 | 2022-05-25 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated methods of use |
| CN114728071B (zh) | 2019-11-13 | 2024-12-06 | 新旭生技股份有限公司 | 用于降解tau蛋白聚集体的化合物及其用途 |
| EP4121046A4 (en) * | 2020-03-18 | 2024-04-24 | Dana-Farber Cancer Institute, Inc. | Targeted degraders of aberrant tau based on the pet tracer pbb3 |
| AU2021337466A1 (en) | 2020-09-01 | 2023-03-30 | Enveric Biosciences Canada Inc. | Halogenated psilocybin derivatives and methods of using |
| AU2022207648A1 (en) | 2021-01-13 | 2023-07-27 | Monte Rosa Therapeutics Ag | Isoindolinone compounds |
| WO2022251614A1 (en) * | 2021-05-28 | 2022-12-01 | Beth Israel Deaconess Medical Center, Inc. | Protacs with transcription factor targeting moieties |
| CA3226162A1 (en) | 2021-07-09 | 2023-01-12 | Plexium, Inc. | Aryl compounds and pharmaceutical compositions that modulate ikzf2 |
| CA3235512A1 (en) * | 2021-10-22 | 2023-04-27 | Xiaobao Yang | Crbn e3 ligase ligand compound, protein degrader developed based thereon and their applications |
| CN115385908B (zh) * | 2022-07-26 | 2024-04-12 | 阿茨可利(杭州)医学科技有限公司 | 靶向促进tau蛋白去磷酸化的小分子嵌合体及其应用 |
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| CN111372585A (zh) | 2017-11-16 | 2020-07-03 | C4医药公司 | 用于靶蛋白降解的降解剂和降解决定子 |
| EP3710443A1 (en) | 2017-11-17 | 2020-09-23 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides |
| US20190300521A1 (en) | 2018-04-01 | 2019-10-03 | Arvinas Operations, Inc. | Brm targeting compounds and associated methods of use |
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| US11389438B2 (en) * | 2019-02-25 | 2022-07-19 | Chdi Foundation, Inc. | Compounds for targeting mutant huntingtin protein and uses thereof |
| EP3999182A1 (en) * | 2019-07-17 | 2022-05-25 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated methods of use |
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2020
- 2020-07-17 EP EP20753840.6A patent/EP3999182A1/en active Pending
- 2020-07-17 CN CN202510130079.8A patent/CN119954801A/zh active Pending
- 2020-07-17 JP JP2022502929A patent/JP7548992B2/ja active Active
- 2020-07-17 WO PCT/US2020/042645 patent/WO2021011913A1/en not_active Ceased
- 2020-07-17 CN CN202080063078.1A patent/CN114867727B/zh active Active
- 2020-07-17 US US16/932,590 patent/US11912699B2/en active Active
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2023
- 2023-10-13 US US18/486,668 patent/US12559486B2/en active Active
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2024
- 2024-08-28 JP JP2024146579A patent/JP2024178191A/ja active Pending
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