JP2019537585A5 - - Google Patents
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- JP2019537585A5 JP2019537585A5 JP2019522841A JP2019522841A JP2019537585A5 JP 2019537585 A5 JP2019537585 A5 JP 2019537585A5 JP 2019522841 A JP2019522841 A JP 2019522841A JP 2019522841 A JP2019522841 A JP 2019522841A JP 2019537585 A5 JP2019537585 A5 JP 2019537585A5
- Authority
- JP
- Japan
- Prior art keywords
- ezh2
- divalent
- cancer
- alkyl
- group
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 71
- 102100038970 Histone-lysine N-methyltransferase EZH2 Human genes 0.000 claims description 65
- 101000882127 Homo sapiens Histone-lysine N-methyltransferase EZH2 Proteins 0.000 claims description 65
- 238000000034 method Methods 0.000 claims description 40
- 206010028980 Neoplasm Diseases 0.000 claims description 35
- 201000011510 cancer Diseases 0.000 claims description 27
- 230000001404 mediated effect Effects 0.000 claims description 25
- 230000015556 catabolic process Effects 0.000 claims description 18
- 238000006731 degradation reaction Methods 0.000 claims description 18
- 125000000217 alkyl group Chemical group 0.000 claims description 16
- 239000003446 ligand Substances 0.000 claims description 16
- 239000003623 enhancer Substances 0.000 claims description 12
- 229910052760 oxygen Inorganic materials 0.000 claims description 12
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 claims description 11
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 claims description 11
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 9
- 229910052739 hydrogen Inorganic materials 0.000 claims description 7
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 6
- 206010006187 Breast cancer Diseases 0.000 claims description 6
- 208000026310 Breast neoplasm Diseases 0.000 claims description 6
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 208000022679 triple-negative breast carcinoma Diseases 0.000 claims description 6
- 238000011282 treatment Methods 0.000 claims description 5
- 238000011269 treatment regimen Methods 0.000 claims description 5
- FKSFKBQGSFSOSM-QFIPXVFZSA-N 1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-methyl-6-[6-(1-piperazinyl)-3-pyridinyl]-4-indolecarboxamide Chemical compound C1=C2N([C@@H](C)CC)C=C(C)C2=C(C(=O)NCC=2C(NC(C)=CC=2C)=O)C=C1C(C=N1)=CC=C1N1CCNCC1 FKSFKBQGSFSOSM-QFIPXVFZSA-N 0.000 claims description 4
- ZOIBZSZLMJDVDQ-UHFFFAOYSA-N 1-cyclopentyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[4-(4-morpholinylmethyl)phenyl]-4-indazolecarboxamide Chemical compound O=C1NC(C)=CC(C)=C1CNC(=O)C1=CC(C=2C=CC(CN3CCOCC3)=CC=2)=CC2=C1C=NN2C1CCCC1 ZOIBZSZLMJDVDQ-UHFFFAOYSA-N 0.000 claims description 4
- SZAYCVHJDOWSNY-UHFFFAOYSA-N 3-[ethyl(oxan-4-yl)amino]-2-methyl-N-[(1-methyl-3-oxo-5,6,7,8-tetrahydro-2H-isoquinolin-4-yl)methyl]-5-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]benzamide Chemical compound CCN(C1CCOCC1)c1cc(cc(C(=O)NCc2c3CCCCc3c(C)[nH]c2=O)c1C)-c1ccc(nc1)N1CCN(C)CC1 SZAYCVHJDOWSNY-UHFFFAOYSA-N 0.000 claims description 4
- RXCVUHMIWHRLDF-HXUWFJFHSA-N 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1-one Chemical compound ClC1=C2CCN(C(C2=C(C(=C1)[C@@H](C1COC1)OC)Cl)=O)CC=1C(NC(=CC=1OC)C)=O RXCVUHMIWHRLDF-HXUWFJFHSA-N 0.000 claims description 4
- PFHDWRIVDDIFRP-UHFFFAOYSA-N 6-cyano-n-[(4,6-dimethyl-2-oxo-1h-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide Chemical compound C1=C(C#N)C=C2N(C(CC)CC)C=CC2=C1C(=O)NCC1=C(C)C=C(C)NC1=O PFHDWRIVDDIFRP-UHFFFAOYSA-N 0.000 claims description 4
- ULNXAWLQFZMIHX-UHFFFAOYSA-N GSK343 Chemical compound C1=C(C)NC(=O)C(CNC(=O)C=2C=3C=NN(C=3C=C(C=2)C=2C=C(N=CC=2)N2CCN(C)CC2)C(C)C)=C1CCC ULNXAWLQFZMIHX-UHFFFAOYSA-N 0.000 claims description 4
- LQTWDAYNGMMHLV-UHFFFAOYSA-N N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1-propan-2-ylpyrazolo[3,4-b]pyridine-4-carboxamide Chemical compound CCCc1cc(C)[nH]c(=O)c1CNC(=O)c1cc(nc2n(ncc12)C(C)C)-c1ccc(nc1)N1CCN(C)CC1 LQTWDAYNGMMHLV-UHFFFAOYSA-N 0.000 claims description 4
- ORILYTVJVMAKLC-UHFFFAOYSA-N adamantane Chemical compound C1C(C2)CC3CC1CC2C3 ORILYTVJVMAKLC-UHFFFAOYSA-N 0.000 claims description 4
- XRWSZZJLZRKHHD-WVWIJVSJSA-N asunaprevir Chemical compound O=C([C@@H]1C[C@H](CN1C(=O)[C@@H](NC(=O)OC(C)(C)C)C(C)(C)C)OC1=NC=C(C2=CC=C(Cl)C=C21)OC)N[C@]1(C(=O)NS(=O)(=O)C2CC2)C[C@H]1C=C XRWSZZJLZRKHHD-WVWIJVSJSA-N 0.000 claims description 4
- 229940125961 compound 24 Drugs 0.000 claims description 4
- NSQSAUGJQHDYNO-UHFFFAOYSA-N n-[(4,6-dimethyl-2-oxo-1h-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide Chemical compound C=1C(C=2C=CC(CN3CCOCC3)=CC=2)=CC(C(=O)NCC=2C(NC(C)=CC=2C)=O)=C(C)C=1N(CC)C1CCOCC1 NSQSAUGJQHDYNO-UHFFFAOYSA-N 0.000 claims description 4
- XQFINGFCBFHOPE-UHFFFAOYSA-N n-[(4,6-dimethyl-2-oxo-1h-pyridin-3-yl)methyl]-3-[ethyl-[4-[2-methoxyethyl(methyl)amino]cyclohexyl]amino]-2-methyl-5-(3-morpholin-4-ylprop-1-ynyl)benzamide Chemical compound C=1C(C#CCN2CCOCC2)=CC(C(=O)NCC=2C(NC(C)=CC=2C)=O)=C(C)C=1N(CC)C1CCC(N(C)CCOC)CC1 XQFINGFCBFHOPE-UHFFFAOYSA-N 0.000 claims description 4
- PFPSFENQCNMITC-MRXNPFEDSA-N n-[(4-methoxy-6-methyl-2-oxo-1h-pyridin-3-yl)methyl]-2-methyl-1-[(1r)-1-(oxan-4-yl)ethyl]indole-3-carboxamide Chemical compound C1=C(C)NC(=O)C(CNC(=O)C=2C3=CC=CC=C3N([C@H](C)C3CCOCC3)C=2C)=C1OC PFPSFENQCNMITC-MRXNPFEDSA-N 0.000 claims description 4
- HPODOLXTMDHLLC-QGZVFWFLSA-N n-[(4-methoxy-6-methyl-2-oxo-1h-pyridin-3-yl)methyl]-2-methyl-1-[(1r)-1-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]ethyl]indole-3-carboxamide Chemical compound C1=C(C)NC(=O)C(CNC(=O)C=2C3=CC=CC=C3N([C@H](C)C3CCN(CC(F)(F)F)CC3)C=2C)=C1OC HPODOLXTMDHLLC-QGZVFWFLSA-N 0.000 claims description 4
- DPJNKUOXBZSZAI-UHFFFAOYSA-N n-[(6-methyl-2-oxo-4-propyl-1h-pyridin-3-yl)methyl]-1-propan-2-yl-6-[6-(4-propan-2-ylpiperazin-1-yl)pyridin-3-yl]indazole-4-carboxamide Chemical compound C1=C(C)NC(=O)C(CNC(=O)C=2C=3C=NN(C=3C=C(C=2)C=2C=NC(=CC=2)N2CCN(CC2)C(C)C)C(C)C)=C1CCC DPJNKUOXBZSZAI-UHFFFAOYSA-N 0.000 claims description 4
- UEJJHQNACJXSKW-UHFFFAOYSA-N 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione Chemical compound O=C1C2=CC=CC=C2C(=O)N1C1CCC(=O)NC1=O UEJJHQNACJXSKW-UHFFFAOYSA-N 0.000 claims description 3
- 206010005003 Bladder cancer Diseases 0.000 claims description 3
- 206010009944 Colon cancer Diseases 0.000 claims description 3
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 3
- 206010057444 Oropharyngeal neoplasm Diseases 0.000 claims description 3
- 206010033128 Ovarian cancer Diseases 0.000 claims description 3
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 3
- 206010060862 Prostate cancer Diseases 0.000 claims description 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 3
- 206010038111 Recurrent cancer Diseases 0.000 claims description 3
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 3
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 3
- 208000002495 Uterine Neoplasms Diseases 0.000 claims description 3
- 125000002015 acyclic group Chemical group 0.000 claims description 3
- 150000001408 amides Chemical class 0.000 claims description 3
- 150000001721 carbon Chemical class 0.000 claims description 3
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 3
- 208000022136 colorectal lymphoma Diseases 0.000 claims description 3
- 125000004122 cyclic group Chemical group 0.000 claims description 3
- 238000000354 decomposition reaction Methods 0.000 claims description 3
- 208000005017 glioblastoma Diseases 0.000 claims description 3
- 125000005842 heteroatom Chemical group 0.000 claims description 3
- GOTYRUGSSMKFNF-UHFFFAOYSA-N lenalidomide Chemical compound C1C=2C(N)=CC=CC=2C(=O)N1C1CCC(=O)NC1=O GOTYRUGSSMKFNF-UHFFFAOYSA-N 0.000 claims description 3
- 229960004942 lenalidomide Drugs 0.000 claims description 3
- 208000032839 leukemia Diseases 0.000 claims description 3
- 230000003211 malignant effect Effects 0.000 claims description 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 3
- 201000001441 melanoma Diseases 0.000 claims description 3
- SBOJXQVPLKSXOG-UHFFFAOYSA-N o-amino-hydroxylamine Chemical compound NON SBOJXQVPLKSXOG-UHFFFAOYSA-N 0.000 claims description 3
- 201000002528 pancreatic cancer Diseases 0.000 claims description 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 3
- UVSMNLNDYGZFPF-UHFFFAOYSA-N pomalidomide Chemical compound O=C1C=2C(N)=CC=CC=2C(=O)N1C1CCC(=O)NC1=O UVSMNLNDYGZFPF-UHFFFAOYSA-N 0.000 claims description 3
- 229960000688 pomalidomide Drugs 0.000 claims description 3
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims description 3
- 229920006395 saturated elastomer Polymers 0.000 claims description 3
- 125000003003 spiro group Chemical group 0.000 claims description 3
- 229910052717 sulfur Inorganic materials 0.000 claims description 3
- 229960003433 thalidomide Drugs 0.000 claims description 3
- 210000001519 tissue Anatomy 0.000 claims description 3
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 3
- 206010046766 uterine cancer Diseases 0.000 claims description 3
- CAICZZJHNJHHDJ-UHFFFAOYSA-N 1-(4,4,5,5,5-pentafluoropentylsulfinyl)nonane Chemical compound CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F CAICZZJHNJHHDJ-UHFFFAOYSA-N 0.000 claims description 2
- KQZLRWGGWXJPOS-NLFPWZOASA-N 1-[(1R)-1-(2,4-dichlorophenyl)ethyl]-6-[(4S,5R)-4-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-5-methylcyclohexen-1-yl]pyrazolo[3,4-b]pyrazine-3-carbonitrile Chemical compound ClC1=C(C=CC(=C1)Cl)[C@@H](C)N1N=C(C=2C1=NC(=CN=2)C1=CC[C@@H]([C@@H](C1)C)N1[C@@H](CCC1)CO)C#N KQZLRWGGWXJPOS-NLFPWZOASA-N 0.000 claims description 2
- -1 Compound 3 Chemical compound 0.000 claims description 2
- 102000003960 Ligases Human genes 0.000 claims description 2
- 108090000364 Ligases Proteins 0.000 claims description 2
- 102100032783 Protein cereblon Human genes 0.000 claims description 2
- 101000776133 Viola hederacea Leaf cyclotide 1 Proteins 0.000 claims description 2
- 238000002512 chemotherapy Methods 0.000 claims description 2
- 229940126214 compound 3 Drugs 0.000 claims description 2
- 229940125877 compound 31 Drugs 0.000 claims description 2
- 238000001794 hormone therapy Methods 0.000 claims description 2
- 125000001165 hydrophobic group Chemical group 0.000 claims description 2
- 238000009169 immunotherapy Methods 0.000 claims description 2
- 239000003112 inhibitor Substances 0.000 claims description 2
- 238000001959 radiotherapy Methods 0.000 claims description 2
- 238000001356 surgical procedure Methods 0.000 claims description 2
- QFLWZFQWSBQYPS-AWRAUJHKSA-N (3S)-3-[[(2S)-2-[[(2S)-2-[5-[(3aS,6aR)-2-oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-4-yl]pentanoylamino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-[1-bis(4-chlorophenoxy)phosphorylbutylamino]-4-oxobutanoic acid Chemical compound CCCC(NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CCCCC1SC[C@@H]2NC(=O)N[C@H]12)C(C)C)P(=O)(Oc1ccc(Cl)cc1)Oc1ccc(Cl)cc1 QFLWZFQWSBQYPS-AWRAUJHKSA-N 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 1
- 0 *C(c1c(C2*)c(*)ccc1)N2C(CCC(N1)=O)C1=O Chemical compound *C(c1c(C2*)c(*)ccc1)N2C(CCC(N1)=O)C1=O 0.000 description 5
- 206010031096 Oropharyngeal cancer Diseases 0.000 description 1
- 201000006958 oropharynx cancer Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662414195P | 2016-10-28 | 2016-10-28 | |
| US62/414,195 | 2016-10-28 | ||
| PCT/US2017/058718 WO2018081530A1 (en) | 2016-10-28 | 2017-10-27 | Compositions and methods for treating ezh2-mediated cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019537585A JP2019537585A (ja) | 2019-12-26 |
| JP2019537585A5 true JP2019537585A5 (enExample) | 2021-09-16 |
Family
ID=62024052
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019522841A Pending JP2019537585A (ja) | 2016-10-28 | 2017-10-27 | Ｅｚｈ２媒介性がんを治療するための組成物および方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US20190255041A1 (enExample) |
| EP (1) | EP3532464A4 (enExample) |
| JP (1) | JP2019537585A (enExample) |
| KR (1) | KR20190084063A (enExample) |
| CN (1) | CN110167924A (enExample) |
| AU (2) | AU2017348322B8 (enExample) |
| CA (1) | CA3041840A1 (enExample) |
| EA (1) | EA201991071A1 (enExample) |
| IL (1) | IL266053A (enExample) |
| MX (1) | MX2019004950A (enExample) |
| SG (2) | SG11201903483VA (enExample) |
| WO (1) | WO2018081530A1 (enExample) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102667413B1 (ko) * | 2016-10-27 | 2024-05-21 | 삼성전자주식회사 | 음성 명령에 기초하여 애플리케이션을 실행하는 방법 및 장치 |
| KR20190084063A (ko) | 2016-10-28 | 2019-07-15 | 이칸 스쿨 오브 메디슨 엣 마운트 시나이 | Ｅｚｈ２-매개성 암 치료용 조성물 및 방법 |
| WO2018106870A1 (en) | 2016-12-08 | 2018-06-14 | Icahn School Of Medicine At Mount Sinai | Compositions and methods for treating cdk4/6-mediated cancer |
| US11191741B2 (en) | 2016-12-24 | 2021-12-07 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide |
| JP2021515013A (ja) | 2018-03-06 | 2021-06-17 | アイカーン スクール オブ メディスン アット マウント シナイ | セリンスレオニンキナーゼ（ａｋｔ）分解／破壊化合物および使用方法 |
| FI3784663T3 (fi) | 2018-04-23 | 2023-10-06 | Celgene Corp | Substituoituja 4-aminoisoindoliini-1,3-dioniyhdisteitä ja niiden käyttö lymfooman hoitamiseksi |
| EP3810145A4 (en) | 2018-06-21 | 2022-06-01 | Icahn School of Medicine at Mount Sinai | Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use |
| CN112969696B (zh) * | 2018-11-02 | 2024-06-11 | 达纳-法伯癌症研究公司 | 乙酰化书写器抑制剂的开发及其用途 |
| JP7503851B2 (ja) | 2019-05-06 | 2024-06-21 | アイカーン スクール オブ メディスン アット マウント シナイ | Ｈｐｋ１の分解剤としてのヘテロ二官能性化合物 |
| CN112457365B (zh) | 2019-09-09 | 2023-06-09 | 中国医学科学院药物研究所 | 一类靶向蛋白质水解通路的功能分子及其制备和应用 |
| JP7763753B2 (ja) | 2019-09-26 | 2025-11-04 | ノバルティス アーゲー | アザキノリン化合物およびその使用 |
| CN110862434B (zh) * | 2019-10-28 | 2021-07-06 | 中山大学 | 一种可促进TGF-β1蛋白靶向降解的化合物及其制备方法与应用 |
| EP4053122B1 (en) | 2019-10-31 | 2024-10-09 | Daegu-Gyeongbuk Medical Innovation Foundation | Compound comprising ezh2 inhibitor and e3 ligase binder and pharmaceutical composition for preventing or treating ezh2-associated disease comprising same as active ingredient |
| WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| CN111303133A (zh) * | 2020-03-25 | 2020-06-19 | 清华大学 | 降解ezh2蛋白的小分子化合物 |
| CN112920176B (zh) * | 2020-05-25 | 2022-11-04 | 四川大学华西医院 | 可诱导prc2蛋白复合物核心亚基降解的双功能化合物和药物组合物及应用 |
| US12103924B2 (en) | 2020-06-01 | 2024-10-01 | Icahn School Of Medicine At Mount Sinai | Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use |
| MX2023001603A (es) * | 2020-08-13 | 2023-03-07 | Hanmi Pharmaceutical Co Ltd | Derivados de dioxoloisoquinolinona novedosos y uso de los mismos. |
| CN113214203A (zh) * | 2020-12-16 | 2021-08-06 | 中山大学肿瘤防治中心（中山大学附属肿瘤医院、中山大学肿瘤研究所） | 基于ezh2蛋白降解的小分子化合物及其应用 |
| WO2022159650A1 (en) * | 2021-01-22 | 2022-07-28 | Icahn School Of Medicine At Mount Sinai | HETEROBIFUNCTIONAL COMPOUNDS AS DEGRADERS OF eEF1A2 |
| US12042543B2 (en) * | 2021-04-30 | 2024-07-23 | Northwestern University | Substituted 3-amino-5-phenylbenzamide compounds as covalent inhibitors of enhancer zeste homolog 2 (EZH2) and proteolysis-targeting chimeric derivatives thereof (PROTACs) that induce degradation of EZH2 |
| PE20252789A1 (es) | 2023-05-24 | 2025-12-22 | Kumquat Biosciences Inc | Compuestos heterociclicos y usos de estos |
| CN121263417A (zh) | 2023-06-30 | 2026-01-02 | 金橘生物科技公司 | 取代的稠合三环胺化合物及其作为ras抑制剂的用途 |
| AU2024374420A1 (en) | 2023-11-02 | 2026-04-16 | Kumquat Biosciences Inc. | Degraders and uses thereof |
| WO2025121807A1 (ko) * | 2023-12-08 | 2025-06-12 | 인제대학교 산학협력단 | Ezh2 저해제 및 mettl3 억제제를 포함하는 암의 예방 또는 치료용 약제학적 조성물 |
| KR20250088371A (ko) * | 2023-12-08 | 2025-06-17 | 인제대학교 산학협력단 | Ezh2 저해제 및 jak3 억제제를 포함하는 암의 예방 또는 치료용 약학적 조성물 |
| CN118420604A (zh) * | 2024-03-29 | 2024-08-02 | 中国药科大学 | 一种以降冰片烯为疏水基团修饰的ezh2蛋白降解剂及其制备方法和应用 |
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| US6486214B1 (en) | 1997-09-10 | 2002-11-26 | Rutgers, The State University Of New Jersey | Polyanhydride linkers for production of drug polymers and drug polymer compositions produced thereby |
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| NZ590160A (en) | 2003-11-21 | 2012-07-27 | Array Biopharma Inc | AKT protein kinase inhibitors |
| JP5274842B2 (ja) | 2004-12-28 | 2013-08-28 | エグゼリクシス， インコーポレイテッド | 免疫疾患、炎症疾患および増殖疾患の処置のためのセリン−スレオニンキナーゼモジュレーター（ｐ７０Ｓ６Ｋ、Ａｋｔ−１およびＡｋｔ−２）としての［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジンまたは［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジン化合物 |
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2017
- 2017-10-27 KR KR1020197015152A patent/KR20190084063A/ko not_active Withdrawn
- 2017-10-27 CA CA3041840A patent/CA3041840A1/en not_active Abandoned
- 2017-10-27 AU AU2017348322A patent/AU2017348322B8/en not_active Ceased
- 2017-10-27 US US16/345,591 patent/US20190255041A1/en not_active Abandoned
- 2017-10-27 WO PCT/US2017/058718 patent/WO2018081530A1/en not_active Ceased
- 2017-10-27 MX MX2019004950A patent/MX2019004950A/es unknown
- 2017-10-27 SG SG11201903483VA patent/SG11201903483VA/en unknown
- 2017-10-27 JP JP2019522841A patent/JP2019537585A/ja active Pending
- 2017-10-27 EA EA201991071A patent/EA201991071A1/ru unknown
- 2017-10-27 SG SG10202104386UA patent/SG10202104386UA/en unknown
- 2017-10-27 CN CN201780081246.8A patent/CN110167924A/zh active Pending
- 2017-10-27 EP EP17863645.2A patent/EP3532464A4/en not_active Withdrawn
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2019
- 2019-04-15 IL IL266053A patent/IL266053A/en unknown
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2020
- 2020-07-10 US US16/926,418 patent/US11510920B2/en active Active
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2022
- 2022-03-03 AU AU2022201488A patent/AU2022201488A1/en not_active Abandoned
- 2022-11-01 US US17/978,696 patent/US12274697B2/en active Active
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