JP2019512482A5 - - Google Patents
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- Publication number
- JP2019512482A5 JP2019512482A5 JP2018546618A JP2018546618A JP2019512482A5 JP 2019512482 A5 JP2019512482 A5 JP 2019512482A5 JP 2018546618 A JP2018546618 A JP 2018546618A JP 2018546618 A JP2018546618 A JP 2018546618A JP 2019512482 A5 JP2019512482 A5 JP 2019512482A5
- Authority
- JP
- Japan
- Prior art keywords
- fluoro
- phenyl
- carboxamide
- trifluoromethyl
- pyridine
- 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
- 0 *C(Nc1c(*)*(I)c(*)c(*)*1)=O Chemical compound *C(Nc1c(*)*(I)c(*)c(*)*1)=O 0.000 description 13
- RUJJFWKIAJWUKV-UHFFFAOYSA-N CC(C)c(c(C(F)(F)F)cc(F)c1)c1F Chemical compound CC(C)c(c(C(F)(F)F)cc(F)c1)c1F RUJJFWKIAJWUKV-UHFFFAOYSA-N 0.000 description 2
- WQEZEEIQQHGWFQ-UHFFFAOYSA-N CC(C)c(cc1F)c(C(F)(F)F)cc1F Chemical compound CC(C)c(cc1F)c(C(F)(F)F)cc1F WQEZEEIQQHGWFQ-UHFFFAOYSA-N 0.000 description 2
- XXLNKGOPDHIOCS-UHFFFAOYSA-N Cc(cc1)c(C(F)(F)F)cc1F Chemical compound Cc(cc1)c(C(F)(F)F)cc1F XXLNKGOPDHIOCS-UHFFFAOYSA-N 0.000 description 2
- UFKGPESBDLSXLB-AYHJJNSGSA-N CC(C1)N(C)CCN1c(c(NC(C(C(C(F)(F)F)=C1)=CNC1=O)=O)c1)cc(F)c1-c1cnc(N2C[C@H](C)O[C@H](C)C2)nc1 Chemical compound CC(C1)N(C)CCN1c(c(NC(C(C(C(F)(F)F)=C1)=CNC1=O)=O)c1)cc(F)c1-c1cnc(N2C[C@H](C)O[C@H](C)C2)nc1 UFKGPESBDLSXLB-AYHJJNSGSA-N 0.000 description 1
- UAIVFDJJMVMUGY-UHFFFAOYSA-N CC1N(C)CCN(C)C1 Chemical compound CC1N(C)CCN(C)C1 UAIVFDJJMVMUGY-UHFFFAOYSA-N 0.000 description 1
- RSEOCCGIORLDFD-UHFFFAOYSA-N CCCN(C)C1(CNC)COC1 Chemical compound CCCN(C)C1(CNC)COC1 RSEOCCGIORLDFD-UHFFFAOYSA-N 0.000 description 1
- RYAFIZYASRHWBM-UHFFFAOYSA-N CN(CC1)CC11N(C)CCC1 Chemical compound CN(CC1)CC11N(C)CCC1 RYAFIZYASRHWBM-UHFFFAOYSA-N 0.000 description 1
- HWTLFOPXWFNIAJ-UHFFFAOYSA-N CN1C2CN(C)CC1CC2 Chemical compound CN1C2CN(C)CC1CC2 HWTLFOPXWFNIAJ-UHFFFAOYSA-N 0.000 description 1
- ZFWWWWCAJVNZPE-UHFFFAOYSA-N CN1CC(CC2)N2CC1 Chemical compound CN1CC(CC2)N2CC1 ZFWWWWCAJVNZPE-UHFFFAOYSA-N 0.000 description 1
- XNLRUDFBVYFTKV-UHFFFAOYSA-N CN1CC2(CC2)N(C)CC1 Chemical compound CN1CC2(CC2)N(C)CC1 XNLRUDFBVYFTKV-UHFFFAOYSA-N 0.000 description 1
- YVNJJXGLGIACPR-UHFFFAOYSA-N CN1CC2=CCCN2CC1 Chemical compound CN1CC2=CCCN2CC1 YVNJJXGLGIACPR-UHFFFAOYSA-N 0.000 description 1
- OJYYBQNZIMFPOR-UHFFFAOYSA-N CN1CC2N(C)C=CC2C1 Chemical compound CN1CC2N(C)C=CC2C1 OJYYBQNZIMFPOR-UHFFFAOYSA-N 0.000 description 1
- RXYPXQSKLGGKOL-UHFFFAOYSA-N CN1CCN(C)CC1 Chemical compound CN1CCN(C)CC1 RXYPXQSKLGGKOL-UHFFFAOYSA-N 0.000 description 1
- YQWYNMOCRRYVCE-UHFFFAOYSA-N CN1CCN(C)CCC1 Chemical compound CN1CCN(C)CCC1 YQWYNMOCRRYVCE-UHFFFAOYSA-N 0.000 description 1
- XRYGCVVVDCEPRL-UHFFFAOYSA-N CNC1CCN(C)CC1 Chemical compound CNC1CCN(C)CC1 XRYGCVVVDCEPRL-UHFFFAOYSA-N 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022028700A JP2022071046A (ja) | 2016-03-01 | 2022-02-25 | Ｗｄｒ５タンパク質－タンパク質結合の阻害剤 |
| JP2024071190A JP2024102151A (ja) | 2016-03-01 | 2024-04-25 | Ｗｄｒ５タンパク質－タンパク質結合の阻害剤 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662301673P | 2016-03-01 | 2016-03-01 | |
| US62/301,673 | 2016-03-01 | ||
| PCT/CA2017/050269 WO2017147700A1 (en) | 2016-03-01 | 2017-03-01 | Inhibitors of wdr5 protein-protein binding |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022028700A Division JP2022071046A (ja) | 2016-03-01 | 2022-02-25 | Ｗｄｒ５タンパク質－タンパク質結合の阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019512482A JP2019512482A (ja) | 2019-05-16 |
| JP2019512482A5 true JP2019512482A5 (enExample) | 2020-04-09 |
| JP7624690B2 JP7624690B2 (ja) | 2025-01-31 |
Family
ID=59743306
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018546618A Active JP7624690B2 (ja) | 2016-03-01 | 2017-03-01 | Ｗｄｒ５タンパク質－タンパク質結合の阻害剤 |
| JP2022028700A Pending JP2022071046A (ja) | 2016-03-01 | 2022-02-25 | Ｗｄｒ５タンパク質－タンパク質結合の阻害剤 |
| JP2024071190A Pending JP2024102151A (ja) | 2016-03-01 | 2024-04-25 | Ｗｄｒ５タンパク質－タンパク質結合の阻害剤 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022028700A Pending JP2022071046A (ja) | 2016-03-01 | 2022-02-25 | Ｗｄｒ５タンパク質－タンパク質結合の阻害剤 |
| JP2024071190A Pending JP2024102151A (ja) | 2016-03-01 | 2024-04-25 | Ｗｄｒ５タンパク質－タンパク質結合の阻害剤 |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US11319299B2 (enExample) |
| EP (1) | EP3423451B1 (enExample) |
| JP (3) | JP7624690B2 (enExample) |
| KR (1) | KR20180120720A (enExample) |
| CN (1) | CN109195965B (enExample) |
| AU (1) | AU2017226004B2 (enExample) |
| BR (1) | BR112018067392A2 (enExample) |
| CA (1) | CA3015406A1 (enExample) |
| CL (1) | CL2018002505A1 (enExample) |
| CO (1) | CO2018010504A2 (enExample) |
| DK (1) | DK3423451T3 (enExample) |
| EA (1) | EA038109B1 (enExample) |
| EC (1) | ECSP18073726A (enExample) |
| IL (1) | IL261472B (enExample) |
| MX (1) | MX2018010374A (enExample) |
| WO (1) | WO2017147700A1 (enExample) |
| ZA (1) | ZA201805879B (enExample) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2019507179A (ja) | 2016-03-01 | 2019-03-14 | プロペロン セラピューティックス インコーポレイテッド | Ｗｄｒ５タンパク質−タンパク質結合の阻害剤 |
| US11319299B2 (en) * | 2016-03-01 | 2022-05-03 | Propellon Therapeutics Inc. | Substituted carboxamides as inhibitors of WDR5 protein-protein binding |
| 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 |
| KR102816969B1 (ko) | 2017-03-27 | 2025-06-10 | 하이드로-퀘벡 | 전해질 조성물에서 또는 전극 첨가제로서 사용하기 위한 염 |
| WO2019046944A1 (en) * | 2017-09-06 | 2019-03-14 | Propellon Therapeutics Inc. | INHIBITORS OF PROTEIN BINDING WDR5-PROTEIN |
| US10501466B2 (en) | 2017-09-19 | 2019-12-10 | Vanderbilt University | WDR5 inhibitors and modulators |
| JP2021510152A (ja) * | 2018-01-04 | 2021-04-15 | 北京大学深▲ヂェン▼研究生院Ｐｅｋｉｎｇ Ｕｎｉｖｅｒｓｉｔｙ Ｓｈｅｎｚｈｅｎ Ｇｒａｄｕａｔｅ Ｓｃｈｏｏｌ | Ｌｓｄ１とｈｄａｃとを標的として同時に阻害する化合物及びその用途 |
| 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 |
| CN108715585A (zh) * | 2018-04-23 | 2018-10-30 | 中国药科大学 | 苯基联三氮唑类mll1-wdr5蛋白-蛋白相互作用抑制剂 |
| US10844044B2 (en) | 2018-06-14 | 2020-11-24 | Vanderbilt University | WDR5 inhibitors and modulators |
| 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 |
| US10807959B2 (en) | 2018-08-16 | 2020-10-20 | Vanderbilt University | WDR5-MLL1 inhibitors and modulators |
| CN109734674B (zh) | 2019-02-26 | 2022-08-26 | 中国药科大学 | 苯胺类wdr5蛋白-蛋白相互作用抑制剂及其制法和用途 |
| WO2020179859A1 (ja) | 2019-03-06 | 2020-09-10 | 第一三共株式会社 | ピロロピラゾール誘導体 |
| 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 |
| CN111039860B (zh) * | 2019-12-02 | 2022-09-13 | 河北科技大学 | 2-羟基-n-(4’-氯联苯-2-基)烟酰胺的合成方法及应用 |
| CN113024538B (zh) * | 2019-12-24 | 2022-09-09 | 南开大学 | 吡唑酰胺类化合物及其制备和在防治植物病菌病和杀虫中的应用 |
| 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 |
| CN114539073A (zh) * | 2022-02-18 | 2022-05-27 | 郑州萃智医药科技有限公司 | 3-溴-2-氯-4,6-二氟苯胺的合成方法 |
| CA3245866A1 (en) * | 2022-03-14 | 2023-09-21 | Huyabio International, Llc | BLOOD-BRAIN BARRIER CROSSING PROTEIN-PROTEIN INTERACTION INHIBITORS (MLL1-WDR5) AND THEIR USES |
| US20230286948A1 (en) * | 2022-03-14 | 2023-09-14 | Huyabio International, Llc | Haloalkylpyridyl triazole mll1-wdr5 protein-protein interaction inhibitor |
| AR129265A1 (es) | 2022-05-12 | 2024-08-07 | Syngenta Crop Protection Ag | Compuestos de alcoxi-heteroaril-carboxamida o tioamida |
| CN119365449A (zh) * | 2022-07-01 | 2025-01-24 | 甘李药业股份有限公司 | 一种用作wdr5抑制剂的化合物或其可药用盐及其应用 |
| WO2024015478A2 (en) * | 2022-07-14 | 2024-01-18 | Huyabio International, Llc | Combination therapies of wdr5 inhibitors and pd-1 inhibitors |
| CN115974965B (zh) * | 2022-08-31 | 2025-09-12 | 中国科学技术大学 | 一种靶向wdr5的多肽抑制剂及其用途 |
| WO2026058961A1 (en) | 2024-09-13 | 2026-03-19 | Alivexis, Inc. | Wdr5 inhibitors, compounds, pharmaceutical compositions, and methods of use thereof |
| CN119143715B (zh) * | 2024-11-12 | 2025-03-14 | 天津匠新致成科技有限公司 | 二芳基团甲基哌嗪类化合物及其制备方法、药物组合物和应用 |
| CN119661474A (zh) * | 2024-12-16 | 2025-03-21 | 中国药科大学 | 一类羟肟酸类的双靶点化合物衍生物及其应用 |
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|---|---|---|---|---|
| KR100354309B1 (ko) | 1993-11-12 | 2003-01-06 | 파마시아 앤드 업존 캄파니 | 피리미딘-티오알킬및알킬에테르화합물 |
| JPH0959236A (ja) | 1995-08-23 | 1997-03-04 | Dai Ichi Seiyaku Co Ltd | ベンズアミド化合物 |
| US20010051719A1 (en) | 1996-12-19 | 2001-12-13 | Smithkline Beecham P.L.C. | Novel compounds |
| US6541669B1 (en) | 1998-06-08 | 2003-04-01 | Theravance, Inc. | β2-adrenergic receptor agonists |
| DE19952146A1 (de) | 1999-10-29 | 2001-06-07 | Boehringer Ingelheim Pharma | Arylalkane, Arylalkene und Aryl-azaalkane, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung |
| CN100355751C (zh) | 2000-03-29 | 2007-12-19 | 西克拉塞尔有限公司 | 2－取代的4－杂芳基－嘧啶、其组合物及其用途 |
| JP2002193938A (ja) | 2000-12-01 | 2002-07-10 | Bayer Ag | ４−アリールピリジン誘導体 |
| EP1389194A2 (en) | 2001-04-27 | 2004-02-18 | Vertex Pharmaceuticals Incorporated | Inhibitors of bace |
| GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| CN1681487A (zh) | 2002-07-15 | 2005-10-12 | 美瑞德生物工程公司 | 化合物、组合物及其使用方法 |
| AU2003270489A1 (en) | 2002-09-09 | 2004-03-29 | Cellular Genomics, Inc. | 6-ARYL-IMIDAZO(1,2-a)PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF |
| GB0412072D0 (en) | 2004-05-28 | 2004-06-30 | Syngenta Participations Ag | Chemical compounds |
| RU2401265C2 (ru) | 2004-06-10 | 2010-10-10 | Айрм Ллк | Соединения и композиции в качестве ингибиторов протеинкиназы |
| WO2006081172A2 (en) | 2005-01-26 | 2006-08-03 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| WO2006124731A2 (en) | 2005-05-12 | 2006-11-23 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| DE102005022977A1 (de) | 2005-05-19 | 2006-12-07 | Merck Patent Gmbh | Phenylchinazolinderivate |
| US20070254894A1 (en) | 2006-01-10 | 2007-11-01 | Kane John L Jr | Novel small molecules with selective cytotoxicity against human microvascular endothelial cell proliferation |
| KR20080092412A (ko) | 2006-02-06 | 2008-10-15 | 아이알엠 엘엘씨 | 단백질 키나제 억제제로서의 화합물 및 조성물 |
| CA2644143C (en) | 2006-04-05 | 2013-10-01 | Novartis Ag | Combinations comprising bcr-abl/c-kit/pdgf-r tk inhibitors for treating cancer |
| CA2679659C (en) | 2007-03-01 | 2016-01-19 | Novartis Ag | Pim kinase inhibitors and methods of their use |
| BRPI0813356A2 (pt) | 2007-06-15 | 2014-12-30 | Irm Llc | Inibidores de proteína quinase e métodos para uso dos mesmos |
| CN101875617B (zh) | 2009-03-23 | 2015-05-20 | 中国医学科学院药物研究所 | 烷氧基取代芳环的氨甲酰基类芳酸化合物及其制法和用途 |
| MX2011011661A (es) | 2009-05-07 | 2011-11-18 | Astrazeneca Ab | Compuestos 1-cianoetilheterociclilcarboxamida sustituidos 750. |
| WO2011129936A2 (en) | 2010-04-16 | 2011-10-20 | Kinex Pharmaceuticals, Llc | Compositions and methods for the prevention and treatment of cancer |
| WO2011149874A2 (en) | 2010-05-26 | 2011-12-01 | Schering Corporation | N-phenyl imidazole carboxamide inhibitors of 3-phosphoinositide-dependent protein kinase-1 |
| WO2011156557A2 (en) | 2010-06-11 | 2011-12-15 | Thomas James B | Compounds active at the neurotensin receptor |
| WO2011159685A2 (en) | 2010-06-16 | 2011-12-22 | The Regents Of The University Of Michigan | Inhibition of wdr5 interaction with its binding partners and therapeutic methods |
| WO2012066065A1 (en) | 2010-11-17 | 2012-05-24 | Novartis Ag | Phenyl-heteroaryl amine compounds and their uses |
| TW201406736A (zh) | 2012-06-28 | 2014-02-16 | Fujifilm Corp | 新穎的醯胺衍生物或其鹽 |
| WO2014048878A1 (en) | 2012-09-26 | 2014-04-03 | Evotec (Uk) Ltd. | Phenyl- or pyridyl- pyrrolo[2,3b]pyrazine derivatives useful in the treatment or prevention of proliferative disorders or dysplasia |
| CA2887598A1 (en) | 2012-10-12 | 2014-04-17 | Takeda Pharmaceutical Company Limited | Cyclopropanamine compound and use thereof |
| US9079866B2 (en) | 2013-02-04 | 2015-07-14 | Janssen Pharmaceutica Nv | Flap modulators |
| CA2932353A1 (en) | 2013-12-13 | 2015-06-18 | Steven P. Treon | Methods to treat lymphoplasmacytic lymphoma |
| EP3079683A4 (en) | 2013-12-13 | 2017-12-20 | Dana-Farber Cancer Institute, Inc. | Methods to treat lymphoplasmacytic lymphoma |
| CN104926801B (zh) * | 2014-03-22 | 2019-06-04 | 浙江大学 | 取代氮杂环类衍生物、含其的药物组合物及其在抗肿瘤中的应用 |
| CN105585565B (zh) | 2014-10-23 | 2019-10-01 | 中国医学科学院药物研究所 | 含2-苯胺基-4-噻唑基吡啶衍生物及其制法和药物组合物与用途 |
| CN105837575B (zh) | 2015-01-13 | 2019-01-15 | 四川大学 | 3-乙炔基吡唑并嘧啶衍生物及其制备方法和用途 |
| CN105175284B (zh) * | 2015-07-21 | 2017-06-16 | 中国药科大学 | 酰胺类化合物、制备方法及其医药用途 |
| JP2019507179A (ja) | 2016-03-01 | 2019-03-14 | プロペロン セラピューティックス インコーポレイテッド | Ｗｄｒ５タンパク質−タンパク質結合の阻害剤 |
| IL302705A (en) | 2016-03-01 | 2023-07-01 | Immatics Biotechnologies Gmbh | Peptides, combinations of peptides, cell-based drugs for use in immunotherapy against bladder cancer and other types of cancer |
| US11319299B2 (en) | 2016-03-01 | 2022-05-03 | Propellon Therapeutics Inc. | Substituted carboxamides as inhibitors of WDR5 protein-protein binding |
| WO2017221092A1 (en) | 2016-06-20 | 2017-12-28 | Novartis Ag | Triazolopyridine compounds and uses thereof |
| US10160763B2 (en) | 2016-09-13 | 2018-12-25 | Vanderbilt University | WDR5 inhibitors and modulators |
| WO2019046944A1 (en) | 2017-09-06 | 2019-03-14 | Propellon Therapeutics Inc. | INHIBITORS OF PROTEIN BINDING WDR5-PROTEIN |
| US10501466B2 (en) | 2017-09-19 | 2019-12-10 | Vanderbilt University | WDR5 inhibitors and modulators |
| WO2020086857A1 (en) | 2018-10-24 | 2020-04-30 | Vanderbilt University | Wdr5 inhibitors and modulators |
| WO2021026672A1 (en) | 2019-08-09 | 2021-02-18 | Novartis Ag | Heterocyclic wdr5 inhibitors as anti-cancer compounds |
-
2017
- 2017-03-01 US US16/080,866 patent/US11319299B2/en active Active
- 2017-03-01 EP EP17759039.5A patent/EP3423451B1/en active Active
- 2017-03-01 WO PCT/CA2017/050269 patent/WO2017147700A1/en not_active Ceased
- 2017-03-01 BR BR112018067392A patent/BR112018067392A2/pt not_active IP Right Cessation
- 2017-03-01 CN CN201780024229.0A patent/CN109195965B/zh active Active
- 2017-03-01 AU AU2017226004A patent/AU2017226004B2/en not_active Ceased
- 2017-03-01 JP JP2018546618A patent/JP7624690B2/ja active Active
- 2017-03-01 KR KR1020187028037A patent/KR20180120720A/ko not_active Ceased
- 2017-03-01 MX MX2018010374A patent/MX2018010374A/es unknown
- 2017-03-01 DK DK17759039.5T patent/DK3423451T3/da active
- 2017-03-01 CA CA3015406A patent/CA3015406A1/en active Pending
- 2017-03-01 EA EA201891974A patent/EA038109B1/ru unknown
-
2018
- 2018-08-29 IL IL261472A patent/IL261472B/en unknown
- 2018-08-31 CL CL2018002505A patent/CL2018002505A1/es unknown
- 2018-08-31 ZA ZA2018/05879A patent/ZA201805879B/en unknown
- 2018-09-28 CO CONC2018/0010504A patent/CO2018010504A2/es unknown
- 2018-10-01 EC ECSENADI201873726A patent/ECSP18073726A/es unknown
-
2022
- 2022-02-25 JP JP2022028700A patent/JP2022071046A/ja active Pending
- 2022-05-06 US US17/738,707 patent/US12264147B2/en active Active
-
2024
- 2024-04-25 JP JP2024071190A patent/JP2024102151A/ja active Pending
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