JPWO2020069027A5 - - Google Patents
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- JPWO2020069027A5 JPWO2020069027A5 JP2021516496A JP2021516496A JPWO2020069027A5 JP WO2020069027 A5 JPWO2020069027 A5 JP WO2020069027A5 JP 2021516496 A JP2021516496 A JP 2021516496A JP 2021516496 A JP2021516496 A JP 2021516496A JP WO2020069027 A5 JPWO2020069027 A5 JP WO2020069027A5
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- Japan
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- independently
- gene
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- occurrence
- alkyl
- 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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- 125000000623 heterocyclic group Chemical group 0.000 claims 132
- 125000000217 alkyl group Chemical group 0.000 claims 84
- 229910052736 halogen Inorganic materials 0.000 claims 78
- 150000002367 halogens Chemical class 0.000 claims 78
- 230000035772 mutation Effects 0.000 claims 54
- 125000001424 substituent group Chemical group 0.000 claims 50
- 125000000304 alkynyl group Chemical group 0.000 claims 42
- 229910052739 hydrogen Inorganic materials 0.000 claims 42
- 239000001257 hydrogen Substances 0.000 claims 42
- 125000002837 carbocyclic group Chemical group 0.000 claims 38
- 108090000623 proteins and genes Proteins 0.000 claims 36
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 34
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 34
- 230000004927 fusion Effects 0.000 claims 28
- 125000002947 alkylene group Chemical group 0.000 claims 26
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 24
- 125000004429 atom Chemical group 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 20
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 18
- 125000006649 (C2-C20) alkynyl group Chemical group 0.000 claims 16
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 16
- 125000004404 heteroalkyl group Chemical group 0.000 claims 16
- 239000008194 pharmaceutical composition Substances 0.000 claims 15
- 125000003358 C2-C20 alkenyl group Chemical group 0.000 claims 14
- 239000003112 inhibitor Substances 0.000 claims 14
- 125000004450 alkenylene group Chemical group 0.000 claims 12
- 125000004419 alkynylene group Chemical group 0.000 claims 12
- 229910052757 nitrogen Inorganic materials 0.000 claims 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 12
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 10
- 108010043471 Core Binding Factor Alpha 2 Subunit Proteins 0.000 claims 10
- 108010003374 fms-Like Tyrosine Kinase 3 Proteins 0.000 claims 10
- 102000004632 fms-Like Tyrosine Kinase 3 Human genes 0.000 claims 10
- 125000004474 heteroalkylene group Chemical group 0.000 claims 10
- 239000000651 prodrug Substances 0.000 claims 10
- 229940002612 prodrug Drugs 0.000 claims 10
- 108700026220 vif Genes Proteins 0.000 claims 10
- 101150101097 ASXL1 gene Proteins 0.000 claims 8
- 101100110209 Homo sapiens ASXL1 gene Proteins 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 8
- 208000030454 monosomy Diseases 0.000 claims 8
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 6
- 102100030550 Menin Human genes 0.000 claims 6
- 101710169972 Menin Proteins 0.000 claims 6
- 108091008121 PML-RARA Proteins 0.000 claims 6
- 102100025373 Runt-related transcription factor 1 Human genes 0.000 claims 6
- 201000005787 hematologic cancer Diseases 0.000 claims 6
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- -1 hydroxy, cyano, amino Chemical group 0.000 claims 6
- 108700028369 Alleles Proteins 0.000 claims 4
- 102100034808 CCAAT/enhancer-binding protein alpha Human genes 0.000 claims 4
- 101710168309 CCAAT/enhancer-binding protein alpha Proteins 0.000 claims 4
- 102000012302 DNA (cytosine-5)-methyltransferase 3A Human genes 0.000 claims 4
- 108050002829 DNA (cytosine-5)-methyltransferase 3A Proteins 0.000 claims 4
- 102100032742 Histone-lysine N-methyltransferase SETD2 Human genes 0.000 claims 4
- 101000654725 Homo sapiens Histone-lysine N-methyltransferase SETD2 Proteins 0.000 claims 4
- 101000653374 Homo sapiens Methylcytosine dioxygenase TET2 Proteins 0.000 claims 4
- 102000012011 Isocitrate Dehydrogenase Human genes 0.000 claims 4
- 108010075869 Isocitrate Dehydrogenase Proteins 0.000 claims 4
- 108010019437 Janus Kinase 2 Proteins 0.000 claims 4
- 101150105104 Kras gene Proteins 0.000 claims 4
- 102100030803 Methylcytosine dioxygenase TET2 Human genes 0.000 claims 4
- 101150073096 NRAS gene Proteins 0.000 claims 4
- 102100025372 Nuclear pore complex protein Nup98-Nup96 Human genes 0.000 claims 4
- 102100022678 Nucleophosmin Human genes 0.000 claims 4
- 108010025568 Nucleophosmin Proteins 0.000 claims 4
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims 4
- 102100022748 Wilms tumor protein Human genes 0.000 claims 4
- 101710127857 Wilms tumor protein Proteins 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 230000002559 cytogenic effect Effects 0.000 claims 4
- 125000004663 dialkyl amino group Chemical group 0.000 claims 4
- 230000001747 exhibiting effect Effects 0.000 claims 4
- 125000004438 haloalkoxy group Chemical group 0.000 claims 4
- 125000001188 haloalkyl group Chemical group 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 230000002018 overexpression Effects 0.000 claims 4
- 125000003107 substituted aryl group Chemical group 0.000 claims 4
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 4
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- ZBNZXTGUTAYRHI-UHFFFAOYSA-N Dasatinib Chemical compound C=1C(N2CCN(CCO)CC2)=NC(C)=NC=1NC(S1)=NC=C1C(=O)NC1=C(C)C=CC=C1Cl ZBNZXTGUTAYRHI-UHFFFAOYSA-N 0.000 claims 2
- 102100029095 Exportin-1 Human genes 0.000 claims 2
- 101150090105 Ezh2 gene Proteins 0.000 claims 2
- 206010064571 Gene mutation Diseases 0.000 claims 2
- 101150008172 HOXA9 gene Proteins 0.000 claims 2
- 108010020382 Hepatocyte Nuclear Factor 1-alpha Proteins 0.000 claims 2
- 102100022057 Hepatocyte nuclear factor 1-alpha Human genes 0.000 claims 2
- 102100039489 Histone-lysine N-methyltransferase, H3 lysine-79 specific Human genes 0.000 claims 2
- 108010048671 Homeodomain Proteins Proteins 0.000 claims 2
- 102000009331 Homeodomain Proteins Human genes 0.000 claims 2
- 101000963360 Homo sapiens Histone-lysine N-methyltransferase, H3 lysine-79 specific Proteins 0.000 claims 2
- 101100149326 Homo sapiens SETD2 gene Proteins 0.000 claims 2
- 101150009057 JAK2 gene Proteins 0.000 claims 2
- 239000002067 L01XE06 - Dasatinib Substances 0.000 claims 2
- 229940123628 Lysine (K)-specific demethylase 1A inhibitor Drugs 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 108050000252 Nuclear pore complex protein NUP98-NUP96 Proteins 0.000 claims 2
- 101100485284 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) CRM1 gene Proteins 0.000 claims 2
- 101150080074 TP53 gene Proteins 0.000 claims 2
- 206010053871 Trisomy 8 Diseases 0.000 claims 2
- 101150094313 XPO1 gene Proteins 0.000 claims 2
- 229960002448 dasatinib Drugs 0.000 claims 2
- 239000012649 demethylating agent Substances 0.000 claims 2
- 108700002148 exportin 1 Proteins 0.000 claims 2
- 108010054452 nuclear pore complex protein 98 Proteins 0.000 claims 2
- 108700025694 p53 Genes Proteins 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 230000008707 rearrangement Effects 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 2
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 230000005945 translocation Effects 0.000 claims 2
- 208000034298 trisomy chromosome 8 Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862736974P | 2018-09-26 | 2018-09-26 | |
| US62/736,974 | 2018-09-26 | ||
| PCT/US2019/053015 WO2020069027A1 (en) | 2018-09-26 | 2019-09-25 | Treatment of hematological malignancies with inhibitors of menin |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022503792A JP2022503792A (ja) | 2022-01-12 |
| JP2022503792A5 JP2022503792A5 (https=) | 2022-10-04 |
| JPWO2020069027A5 true JPWO2020069027A5 (https=) | 2022-10-04 |
Family
ID=69949505
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021516496A Pending JP2022503792A (ja) | 2018-09-26 | 2019-09-25 | メニン阻害剤を用いた血液悪性腫瘍の処置 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20230095934A1 (https=) |
| EP (1) | EP3856173A4 (https=) |
| JP (1) | JP2022503792A (https=) |
| CN (1) | CN113164443A (https=) |
| WO (1) | WO2020069027A1 (https=) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017192543A1 (en) | 2016-05-02 | 2017-11-09 | Regents Of The University Of Michigan | Piperidines as menin inhibitors |
| EP3805215A1 (en) | 2016-06-10 | 2021-04-14 | Vitae Pharmaceuticals, LLC | Inhibitors of the menin-mll interaction |
| CN110691779B (zh) | 2017-03-24 | 2023-10-10 | 库拉肿瘤学公司 | 治疗血液系统恶性肿瘤和尤因肉瘤的方法 |
| CA3058448A1 (en) | 2017-03-31 | 2018-10-04 | The Regents Of The University Of Michigan | Piperidines as covalent menin inhibitors |
| BR122023024273A2 (pt) | 2018-02-27 | 2024-02-20 | Incyte Corporation | Compostos imidazopirimidinas e triazolopirimidinas, seus usos, método para inibir uma atividade de um receptor de adenosina e composição farmacêutica dos mesmos |
| WO2019222677A1 (en) | 2018-05-18 | 2019-11-21 | Incyte Corporation | Fused pyrimidine derivatives as a2a / a2b inhibitors |
| GEP20237548B (en) | 2018-07-05 | 2023-10-10 | Incyte Corp | Fused pyrazine derivatives as a2a /a2b inhibitors |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
| JP7554829B2 (ja) | 2019-12-19 | 2024-09-20 | ヤンセン ファーマシューティカ エヌ．ベー． | 置換直鎖スピロ誘導体 |
| MX2022012471A (es) | 2020-04-07 | 2022-11-30 | Syndax Pharmaceuticals Inc | Combinaciones de inhibidores de menina e inhibidores de cyp3a4 y métodos de uso de las mismas. |
| CN114478568A (zh) * | 2020-10-27 | 2022-05-13 | 苏州优理生物医药科技有限公司 | 一种噻吩并嘧啶类化合物、包含其药物组合物及其应用 |
| CN117177744A (zh) | 2021-01-29 | 2023-12-05 | 塞迪拉治疗股份有限公司 | Cdk2抑制剂及其使用方法 |
| EP4334320A1 (en) * | 2021-05-08 | 2024-03-13 | JANSSEN Pharmaceutica NV | Substituted spiro derivatives |
| MX2023013174A (es) | 2021-05-08 | 2023-11-30 | Janssen Pharmaceutica Nv | Derivados espiro sustituidos. |
| MX2023013436A (es) * | 2021-05-11 | 2023-12-12 | Janssen Pharmaceutica Nv | Terapias de combinacion. |
| TW202311262A (zh) | 2021-05-14 | 2023-03-16 | 美商錫達斯醫藥股份有限公司 | Menin-mll交互作用之抑制劑 |
| WO2022253167A1 (en) | 2021-06-01 | 2022-12-08 | Janssen Pharmaceutica Nv | SUBSTITUTED PHENYL-1H-PYRROLO [2, 3-c] PYRIDINE DERIVATIVES |
| CN117425659A (zh) | 2021-06-03 | 2024-01-19 | 詹森药业有限公司 | 哒嗪或被螺环胺取代的1,2,4-三嗪 |
| WO2022257047A1 (en) * | 2021-06-09 | 2022-12-15 | Acerand Therapeutics (Hong Kong) Limited | Diazaspirobicylic compounds as protein-protein interaction inhibitors and applications thereof |
| CA3220099A1 (en) | 2021-06-17 | 2022-12-22 | Wei Cai | (r)-n-ethyl-5-fluoro-n-isopropyl-2-((5-(2-(6-((2-methoxyethyl)(methyl)amino)-2-methylhexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-1,2,4-triazin-6-yl)oxy)benzamide besylate salt for the treatment of diseases such as cance |
| MX2023015436A (es) | 2021-06-26 | 2024-02-21 | Cedilla Therapeutics Inc | Inhibidores de cdk2 y metodos de uso de los mismos. |
| CN118234497A (zh) * | 2021-12-15 | 2024-06-21 | 丹娜-法伯癌症研究所 | 通过破坏menin-mll表观遗传复合体靶向治疗胃肠道间质瘤(gist) |
| WO2023150635A1 (en) * | 2022-02-04 | 2023-08-10 | Kura Oncology, Inc. | Treatment of hematological malignancies with menin inhibitors and p-glycoprotein inhibitors |
| KR20240161147A (ko) | 2022-03-14 | 2024-11-12 | 슬랩 파마슈티컬스 엘엘씨 | 다중 사이클릭 화합물 |
| TW202415660A (zh) * | 2022-09-02 | 2024-04-16 | 大陸商和記黃埔醫藥（上海）有限公司 | 三嗪類化合物及其用途 |
| CN120456907A (zh) * | 2022-11-02 | 2025-08-08 | 库拉肿瘤学公司 | 急性白血病的治疗方法 |
| WO2024112819A1 (en) * | 2022-11-22 | 2024-05-30 | Dana-Farber Cancer Institute, Inc. | Men1 mutations and uses thereof |
| CN120529900A (zh) * | 2022-11-24 | 2025-08-22 | 奥莱松基因组股份有限公司 | 用于治疗癌症的LSD1抑制剂和Menin抑制剂的组合 |
| CN118994033B (zh) * | 2023-05-17 | 2025-09-16 | 成都先导药物开发股份有限公司 | 一种sdnx-5613的合成方法及其中间体化合物 |
| KR20260039698A (ko) * | 2023-07-17 | 2026-03-20 | 쿠라 온콜로지, 인크. | 결정 형태의 메닌 억제제 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2017514505A (ja) * | 2014-05-07 | 2017-06-08 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 急性骨髄性白血病の新規バイオマーカー |
| WO2016040330A1 (en) * | 2014-09-09 | 2016-03-17 | The Regents Of The University Of Michigan | Thienopyrimidine and thienopyridine compounds and methods of use thereof |
| AR104020A1 (es) * | 2015-06-04 | 2017-06-21 | Kura Oncology Inc | Métodos y composiciones para inhibir la interacción de menina con proteínas mill |
| AU2016324920B2 (en) * | 2015-09-14 | 2022-03-03 | Brunangelo Falini | Dactinomycin compositions and methods for the treatment of acute myeloid leukemia |
| EP4643952A3 (en) * | 2016-01-26 | 2026-01-14 | Memorial Sloan Kettering Cancer Center | Targeting chromatin regulators for inhibiting leukemogenic gene expression in npm1 |
| CN109152784B (zh) * | 2016-03-16 | 2021-12-28 | 库拉肿瘤学公司 | 经取代的menin-mll抑制剂及使用方法 |
| CN109640987B (zh) * | 2016-03-16 | 2022-12-02 | 库拉肿瘤学公司 | Menin-mll的桥联双环抑制剂及使用方法 |
| WO2017192543A1 (en) * | 2016-05-02 | 2017-11-09 | Regents Of The University Of Michigan | Piperidines as menin inhibitors |
| CA2937896A1 (en) * | 2016-08-02 | 2018-02-02 | Universite De Montreal | Use of mubritinib for the treatment of poor prognosis acute myeloid leukemia |
| WO2018024602A1 (en) * | 2016-08-04 | 2018-02-08 | Bayer Aktiengesellschaft | 2,7-diazaspiro[4.4]nonanes |
| BR112019008762A2 (pt) * | 2016-11-02 | 2019-07-16 | Arog Pharmaceuticals, Inc. | método para o tratamento de um distúrbio proliferativo mutado em flt3 |
| WO2018106820A1 (en) * | 2016-12-07 | 2018-06-14 | Kura Oncology, Inc. | Methods of promoting beta cell proliferation |
| US10703757B2 (en) * | 2016-12-23 | 2020-07-07 | Plexxikon Inc. | Compounds and methods for CDK8 modulation and indications therefor |
| CN110691779B (zh) * | 2017-03-24 | 2023-10-10 | 库拉肿瘤学公司 | 治疗血液系统恶性肿瘤和尤因肉瘤的方法 |
-
2019
- 2019-09-25 EP EP19867072.1A patent/EP3856173A4/en active Pending
- 2019-09-25 CN CN201980078019.9A patent/CN113164443A/zh active Pending
- 2019-09-25 WO PCT/US2019/053015 patent/WO2020069027A1/en not_active Ceased
- 2019-09-25 JP JP2021516496A patent/JP2022503792A/ja active Pending
- 2019-09-26 US US17/278,527 patent/US20230095934A1/en not_active Abandoned
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