JPWO2020037079A5 - - Google Patents
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- Publication number
- JPWO2020037079A5 JPWO2020037079A5 JP2021507444A JP2021507444A JPWO2020037079A5 JP WO2020037079 A5 JPWO2020037079 A5 JP WO2020037079A5 JP 2021507444 A JP2021507444 A JP 2021507444A JP 2021507444 A JP2021507444 A JP 2021507444A JP WO2020037079 A5 JPWO2020037079 A5 JP WO2020037079A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- hydroxy
- amino
- cycloalkyl
- 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
- 125000000217 alkyl group Chemical group 0.000 claims description 575
- 229910052739 hydrogen Inorganic materials 0.000 claims description 187
- 239000001257 hydrogen Substances 0.000 claims description 187
- 125000001424 substituent group Chemical group 0.000 claims description 177
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 168
- 150000003839 salts Chemical class 0.000 claims description 162
- 239000012453 solvate Substances 0.000 claims description 157
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 134
- 150000001875 compounds Chemical class 0.000 claims description 120
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 119
- 125000005843 halogen group Chemical group 0.000 claims description 105
- 150000002431 hydrogen Chemical class 0.000 claims description 102
- 125000001072 heteroaryl group Chemical group 0.000 claims description 90
- -1 —OR 10c Chemical group 0.000 claims description 85
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 83
- 125000003118 aryl group Chemical group 0.000 claims description 77
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 70
- 125000003545 alkoxy group Chemical group 0.000 claims description 65
- 125000001188 haloalkyl group Chemical group 0.000 claims description 62
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 55
- 206010028980 Neoplasm Diseases 0.000 claims description 55
- 201000011510 cancer Diseases 0.000 claims description 35
- 229910052736 halogen Inorganic materials 0.000 claims description 32
- 150000002367 halogens Chemical class 0.000 claims description 32
- 229910052757 nitrogen Inorganic materials 0.000 claims description 32
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 32
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 28
- 201000005787 hematologic cancer Diseases 0.000 claims description 27
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 24
- 229910052799 carbon Inorganic materials 0.000 claims description 24
- 208000034951 Genetic Translocation Diseases 0.000 claims description 22
- 238000000034 method Methods 0.000 claims description 22
- 208000034578 Multiple myelomas Diseases 0.000 claims description 20
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 20
- 239000012472 biological sample Substances 0.000 claims description 16
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims description 16
- 125000003107 substituted aryl group Chemical group 0.000 claims description 14
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 14
- 125000005518 carboxamido group Chemical group 0.000 claims description 13
- 125000001153 fluoro group Chemical group F* 0.000 claims description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims description 12
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 12
- 125000004432 carbon atom Chemical group C* 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 6
- 150000003857 carboxamides Chemical class 0.000 claims description 5
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 claims description 4
- 125000003342 alkenyl group Chemical group 0.000 claims description 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 4
- 125000000623 heterocyclic group Chemical group 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- 230000004797 therapeutic response Effects 0.000 claims description 3
- 230000005945 translocation Effects 0.000 claims description 3
- 101100347605 Arabidopsis thaliana VIII-A gene Proteins 0.000 claims description 2
- 101100347612 Arabidopsis thaliana VIII-B gene Proteins 0.000 claims description 2
- ZSGQKGDJOQYHAW-LSLKUGRBSA-N N-[1-[1-[(2S)-2-aminopropanoyl]piperidin-4-yl]ethyl]-7-methyl-1H-indole-2-carboxamide Chemical compound N[C@@H](C)C(=O)N1CCC(CC1)C(C)NC(=O)C=1NC2=C(C=CC=C2C=1)C ZSGQKGDJOQYHAW-LSLKUGRBSA-N 0.000 claims description 2
- AEUGFQSECICIPH-UHFFFAOYSA-N N-[4-(3-aminopropanoylamino)cyclohexyl]-7-methyl-1H-indole-2-carboxamide Chemical compound Cc1cccc2cc([nH]c12)C(=O)NC1CCC(CC1)NC(=O)CCN AEUGFQSECICIPH-UHFFFAOYSA-N 0.000 claims description 2
- 125000004429 atom Chemical group 0.000 claims description 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000002349 favourable effect Effects 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 67
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 31
- 239000000203 mixture Substances 0.000 claims 18
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 12
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 12
- 230000002489 hematologic effect Effects 0.000 claims 3
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 1
- MJPPGVVIDGQOQT-UHFFFAOYSA-N 2-bromo-5-(2-bromo-2-nitroethenyl)furan Chemical compound [O-][N+](=O)C(Br)=CC1=CC=C(Br)O1 MJPPGVVIDGQOQT-UHFFFAOYSA-N 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- LCIYFINKFGDAHD-UHFFFAOYSA-N azepane;3-nitrobenzoic acid Chemical compound C1CCCNCC1.OC(=O)C1=CC=CC([N+]([O-])=O)=C1 LCIYFINKFGDAHD-UHFFFAOYSA-N 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2025010749A JP2025063306A (ja) | 2018-08-14 | 2025-01-24 | 置換インドール及びその使用方法 |
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862718746P | 2018-08-14 | 2018-08-14 | |
| US62/718,746 | 2018-08-14 | ||
| US201862773770P | 2018-11-30 | 2018-11-30 | |
| US62/773,770 | 2018-11-30 | ||
| US201962857120P | 2019-06-04 | 2019-06-04 | |
| US62/857,120 | 2019-06-04 | ||
| PCT/US2019/046569 WO2020037079A1 (en) | 2018-08-14 | 2019-08-14 | Substituted indoles and methods of use thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2025010749A Division JP2025063306A (ja) | 2018-08-14 | 2025-01-24 | 置換インドール及びその使用方法 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021536428A JP2021536428A (ja) | 2021-12-27 |
| JPWO2020037079A5 true JPWO2020037079A5 (https=) | 2022-08-23 |
| JP2021536428A5 JP2021536428A5 (https=) | 2022-08-23 |
| JP7627209B2 JP7627209B2 (ja) | 2025-02-05 |
Family
ID=69525931
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021507444A Active JP7627209B2 (ja) | 2018-08-14 | 2019-08-14 | 置換インドール及びその使用方法 |
| JP2025010749A Pending JP2025063306A (ja) | 2018-08-14 | 2025-01-24 | 置換インドール及びその使用方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2025010749A Pending JP2025063306A (ja) | 2018-08-14 | 2025-01-24 | 置換インドール及びその使用方法 |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US12116358B2 (https=) |
| EP (1) | EP3837240A4 (https=) |
| JP (2) | JP7627209B2 (https=) |
| KR (1) | KR20210065097A (https=) |
| CN (1) | CN112585119A (https=) |
| AU (2) | AU2019321464B2 (https=) |
| BR (1) | BR112021002633A2 (https=) |
| CA (1) | CA3109214A1 (https=) |
| CO (1) | CO2021003300A2 (https=) |
| IL (2) | IL310632A (https=) |
| MA (1) | MA53235A (https=) |
| MX (2) | MX2021001690A (https=) |
| MY (1) | MY207663A (https=) |
| PH (1) | PH12021550296A1 (https=) |
| SG (1) | SG11202101367YA (https=) |
| WO (1) | WO2020037079A1 (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2020530844A (ja) | 2017-08-14 | 2020-10-29 | エピザイム，インコーポレイティド | Ｓｅｔｄ２を阻害することにより癌を処置する方法 |
| SG11202105325QA (en) * | 2018-11-30 | 2021-06-29 | Epizyme Inc | Methods of treating whsc1-overexpressing cancers by inhibiting setd2 |
| WO2021032935A1 (en) * | 2019-08-21 | 2021-02-25 | Kalvista Pharmaceuticals Limited | Enzyme inhibitors |
| IL293340A (en) | 2019-12-02 | 2022-07-01 | Storm Therapeutics Ltd | Polyheterocyclic compounds as mettl3 inhibitors |
| WO2021168313A1 (en) * | 2020-02-19 | 2021-08-26 | Epizyme, Inc. | Setd2 inhibitors and related methods and uses, including combination therapies |
| KR102682775B1 (ko) * | 2020-06-26 | 2024-07-08 | 홀로스메딕 주식회사 | 신규한 화합물의 제조방법 |
| CN115536648B (zh) * | 2021-06-29 | 2024-09-17 | 深圳开悦生命科技有限公司 | 一类抑制rna解旋酶dhx33的多环化合物及其应用 |
| KR20230152076A (ko) * | 2021-02-26 | 2023-11-02 | 셀진 코포레이션 | 다발성 골수종을 치료하는 방법 |
| WO2022231377A1 (ko) * | 2021-04-29 | 2022-11-03 | 홀로스메딕 주식회사 | 신규한 화합물 및 이를 포함하는 암 예방 또는 치료용 약학 조성물 및 그의 용도 |
| US20240299352A1 (en) * | 2021-06-09 | 2024-09-12 | Epizyme, Inc. | Combination therapies with setd2 inhibitors |
| JP2024539726A (ja) * | 2021-11-01 | 2024-10-29 | エピザイム，インコーポレイティド | Ｎ－（（１ｒ，３ｓ）－３－（４－アセチルピペラジン－１－イル）シクロヘキシル）－４－フルオロ－７－メチル－１ｈ－インドール－２－カルボキサミドの結晶形態 |
| CN116794170B (zh) * | 2022-03-18 | 2025-11-14 | 上海润石医药科技有限公司 | 一种化合物的生物样品检测方法 |
| WO2024067709A1 (zh) * | 2022-09-30 | 2024-04-04 | 苏州阿尔脉生物科技有限公司 | 吡啶酰胺类衍生物、包含其的药物组合物及其医药用途 |
| WO2024091450A1 (en) * | 2022-10-24 | 2024-05-02 | The Regents Of The University Of California | Compounds and methods for treating cancer |
| WO2024097606A1 (en) * | 2022-10-31 | 2024-05-10 | Eli Lilly And Company | Ahr agonists |
| CN120548313A (zh) * | 2023-01-19 | 2025-08-26 | 百济神州(苏州)生物科技有限公司 | 作为PRMT5的MTA协同抑制剂的5-氨基-1H-吡咯并[3,2-b]吡啶-2-甲酰胺衍生物 |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL63907A0 (en) | 1980-09-24 | 1981-12-31 | Cetus Corp | Diagnostic method and antibody probe for use therein |
| ATE53862T1 (de) | 1982-01-22 | 1990-06-15 | Cetus Corp | Verfahren zur charakterisierung von hla und die darin benutzten cdns-testmittel. |
| US4582788A (en) | 1982-01-22 | 1986-04-15 | Cetus Corporation | HLA typing method and cDNA probes used therein |
| US4683194A (en) | 1984-05-29 | 1987-07-28 | Cetus Corporation | Method for detection of polymorphic restriction sites and nucleic acid sequences |
| US4595766A (en) | 1984-10-26 | 1986-06-17 | Ciba-Geigy Corporation | Process for the preparation of an indoline carboxylic acid |
| US4683202A (en) | 1985-03-28 | 1987-07-28 | Cetus Corporation | Process for amplifying nucleic acid sequences |
| CA1284931C (en) | 1986-03-13 | 1991-06-18 | Henry A. Erlich | Process for detecting specific nucleotide variations and genetic polymorphisms present in nucleic acids |
| CA1338457C (en) | 1986-08-22 | 1996-07-16 | Henry A. Erlich | Purified thermostable enzyme |
| US6921763B2 (en) | 1999-09-17 | 2005-07-26 | Abbott Laboratories | Pyrazolopyrimidines as therapeutic agents |
| AU2003265382A1 (en) * | 2002-08-23 | 2004-03-11 | Pharmacia & Upjohn Company Llc | Antibacterial benzoic acid derivatives |
| US20040110802A1 (en) | 2002-08-23 | 2004-06-10 | Atli Thorarensen | Antibacterial benzoic acid derivatives |
| KR20080007649A (ko) | 2005-05-11 | 2008-01-22 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 피페리딘환을 가지는 인돌 유도체의 결정 및 그의 제조방법 |
| RU2416603C9 (ru) * | 2005-10-25 | 2012-06-20 | Сионоги Энд Ко., Лтд. | Производные аминодигидротиазина |
| US7838542B2 (en) | 2006-06-29 | 2010-11-23 | Kinex Pharmaceuticals, Llc | Bicyclic compositions and methods for modulating a kinase cascade |
| US20100035862A1 (en) * | 2008-06-25 | 2010-02-11 | Abbott Laboratories | Novel aza-cyclic indole-2-carboxamides and methods of use thereof |
| EP2330894B8 (en) | 2008-09-03 | 2017-04-19 | BioMarin Pharmaceutical Inc. | Compositions including 6-aminohexanoic acid derivatives as hdac inhibitors |
| US20110021362A1 (en) | 2009-07-20 | 2011-01-27 | Constellation Pharmaceuticals | Agents for stimulating activity of methyl modifying enzymes and methods of use thereof |
| CA2784894A1 (en) | 2009-12-23 | 2011-06-30 | Sanofi | Indolyl-piperidinyl benzylamines as beta-tryptase inhibitors |
| US20130137748A1 (en) | 2010-02-03 | 2013-05-30 | Oncotherapy Science, Inc. | Whsc1 and whsc1l1 for target genes of cancer therapy and diagnosis |
| JP2012107001A (ja) | 2010-10-22 | 2012-06-07 | Shionogi & Co Ltd | インドールアミド化合物を含有する医薬 |
| WO2013063417A1 (en) | 2011-10-27 | 2013-05-02 | Memorial Sloan-Kettering Cancer Center | Methyltransferase inhibitors for treating cancer |
| US9446064B2 (en) | 2013-03-14 | 2016-09-20 | Epizyme, Inc. | Combination therapy for treating cancer |
| EP3119390A4 (en) | 2014-03-21 | 2017-09-20 | Glaxosmithkline Intellectual Property (No. 2) Limited | Methods of treating cancer |
| NZ725860A (en) | 2014-04-04 | 2019-08-30 | Iomet Pharma Ltd | Indole derivatives for use in medicine |
| WO2015164482A1 (en) | 2014-04-22 | 2015-10-29 | The Johns Hopkins University | Inhibitors of drug-resistant mycobacterium tuberculosis |
| US9902702B2 (en) | 2014-07-15 | 2018-02-27 | Bristol-Myers Squibb Company | Spirocycloheptanes as inhibitors of rock |
| WO2016025635A2 (en) | 2014-08-13 | 2016-02-18 | Epizyme, Inc. | Combination therapy for treating cancer |
| WO2016040505A1 (en) | 2014-09-10 | 2016-03-17 | Epizyme, Inc. | Smyd inhibitors |
| WO2016079321A1 (en) | 2014-11-20 | 2016-05-26 | Cemm Forschungszentrum Für Molekulare Medizin Gmbh | Antagonists of setdb2 for use in the therapy of infectious diseases |
| US9717745B2 (en) | 2015-03-19 | 2017-08-01 | Zhejiang DTRM Biopharma Co. Ltd. | Pharmaceutical compositions and their use for treatment of cancer and autoimmune diseases |
| WO2017106259A1 (en) | 2015-12-17 | 2017-06-22 | Albert Einstein College Of Medicine, Inc. | Nuclear receptor set domain containing protein 2 transition state and uses thereof |
| CN106317043B (zh) | 2016-08-19 | 2018-11-02 | 成都理工大学 | 一种大麻素受体2激动剂 |
| JP2020530844A (ja) | 2017-08-14 | 2020-10-29 | エピザイム，インコーポレイティド | Ｓｅｔｄ２を阻害することにより癌を処置する方法 |
| SG11202105325QA (en) | 2018-11-30 | 2021-06-29 | Epizyme Inc | Methods of treating whsc1-overexpressing cancers by inhibiting setd2 |
| WO2021168313A1 (en) | 2020-02-19 | 2021-08-26 | Epizyme, Inc. | Setd2 inhibitors and related methods and uses, including combination therapies |
| US20240299352A1 (en) | 2021-06-09 | 2024-09-12 | Epizyme, Inc. | Combination therapies with setd2 inhibitors |
| JP2024539726A (ja) | 2021-11-01 | 2024-10-29 | エピザイム，インコーポレイティド | Ｎ－（（１ｒ，３ｓ）－３－（４－アセチルピペラジン－１－イル）シクロヘキシル）－４－フルオロ－７－メチル－１ｈ－インドール－２－カルボキサミドの結晶形態 |
-
2019
- 2019-08-14 CN CN201980054976.8A patent/CN112585119A/zh active Pending
- 2019-08-14 MA MA053235A patent/MA53235A/fr unknown
- 2019-08-14 IL IL310632A patent/IL310632A/en unknown
- 2019-08-14 MX MX2021001690A patent/MX2021001690A/es unknown
- 2019-08-14 BR BR112021002633-9A patent/BR112021002633A2/pt unknown
- 2019-08-14 EP EP19849109.4A patent/EP3837240A4/en active Pending
- 2019-08-14 AU AU2019321464A patent/AU2019321464B2/en active Active
- 2019-08-14 CA CA3109214A patent/CA3109214A1/en active Pending
- 2019-08-14 US US17/268,151 patent/US12116358B2/en active Active
- 2019-08-14 MY MYPI2021000755A patent/MY207663A/en unknown
- 2019-08-14 WO PCT/US2019/046569 patent/WO2020037079A1/en not_active Ceased
- 2019-08-14 IL IL280709A patent/IL280709B2/en unknown
- 2019-08-14 SG SG11202101367YA patent/SG11202101367YA/en unknown
- 2019-08-14 JP JP2021507444A patent/JP7627209B2/ja active Active
- 2019-08-14 KR KR1020217006988A patent/KR20210065097A/ko active Pending
-
2021
- 2021-02-10 PH PH12021550296A patent/PH12021550296A1/en unknown
- 2021-02-11 MX MX2025006292A patent/MX2025006292A/es unknown
- 2021-03-12 CO CONC2021/0003300A patent/CO2021003300A2/es unknown
-
2025
- 2025-01-24 JP JP2025010749A patent/JP2025063306A/ja active Pending
- 2025-06-19 AU AU2025204601A patent/AU2025204601A1/en active Pending
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