CN115515588A - 大环ulk1/2抑制剂 - Google Patents
大环ulk1/2抑制剂 Download PDFInfo
- Publication number
- CN115515588A CN115515588A CN202180027809.1A CN202180027809A CN115515588A CN 115515588 A CN115515588 A CN 115515588A CN 202180027809 A CN202180027809 A CN 202180027809A CN 115515588 A CN115515588 A CN 115515588A
- Authority
- CN
- China
- Prior art keywords
- alkyl
- cycloalkyl
- independently
- heterocycloalkyl
- aryl
- 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
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/28—Compounds containing heavy metals
- A61K31/282—Platinum compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/529—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202062977039P | 2020-02-14 | 2020-02-14 | |
| US62/977,039 | 2020-02-14 | ||
| PCT/US2021/018038 WO2021163627A1 (en) | 2020-02-14 | 2021-02-12 | Macrocyclic ulk1/2 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN115515588A true CN115515588A (zh) | 2022-12-23 |
Family
ID=77292762
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202180027809.1A Pending CN115515588A (zh) | 2020-02-14 | 2021-02-12 | 大环ulk1/2抑制剂 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US12594277B2 (https=) |
| EP (1) | EP4103183A4 (https=) |
| JP (1) | JP2023513793A (https=) |
| KR (1) | KR20220153582A (https=) |
| CN (1) | CN115515588A (https=) |
| AU (1) | AU2021221162A1 (https=) |
| CA (1) | CA3171185A1 (https=) |
| WO (1) | WO2021163627A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20230159556A1 (en) * | 2020-04-20 | 2023-05-25 | Tenova Pharmaceuticals Inc. | Novel protein kinase inhibitors |
| WO2022072668A1 (en) * | 2020-09-30 | 2022-04-07 | Salk Institute For Biological Studies | Patient selection biomarkers for treatment with ulk inhibitors |
| TW202404979A (zh) * | 2022-07-18 | 2024-02-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 抑制並誘導egfr降解的大環類化合物、其製備方法及其在醫藥上的應用 |
| WO2024017258A1 (zh) * | 2022-07-19 | 2024-01-25 | 百极弘烨(南通)医药科技有限公司 | Egfr小分子抑制剂、含其的药物组合物及其用途 |
| WO2024233766A1 (en) * | 2023-05-10 | 2024-11-14 | Erasca, Inc. | Macrocyclic ulk1/2 inhibitors and their use thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016196393A2 (en) * | 2015-05-29 | 2016-12-08 | Presage Biosciences, Inc. | Autophagy-inhibiting compounds and uses thereof |
| US20190284207A1 (en) * | 2014-08-25 | 2019-09-19 | Salk Institute For Biological Studies | Novel ulk1 inhibitors and methods using same |
Family Cites Families (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4675189A (en) | 1980-11-18 | 1987-06-23 | Syntex (U.S.A.) Inc. | Microencapsulation of water soluble active polypeptides |
| JPS60100516A (ja) | 1983-11-04 | 1985-06-04 | Takeda Chem Ind Ltd | 徐放型マイクロカプセルの製造法 |
| CA1256638A (en) | 1984-07-06 | 1989-06-27 | Motoaki Tanaka | Polymer and its production |
| JP2551756B2 (ja) | 1985-05-07 | 1996-11-06 | 武田薬品工業株式会社 | ポリオキシカルボン酸エステルおよびその製造法 |
| GB0206215D0 (en) | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
| US20050004186A1 (en) | 2002-12-20 | 2005-01-06 | Pfizer Inc | MEK inhibiting compounds |
| ES2325440T3 (es) | 2003-02-20 | 2009-09-04 | Smithkline Beecham Corporation | Compuestos de pirimidina. |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| US7504396B2 (en) | 2003-06-24 | 2009-03-17 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| WO2005049021A1 (en) | 2003-11-03 | 2005-06-02 | Oy Helsinki Transplantation R & D Ltd | Materials and methods for inhibiting neointimal hyperplasia |
| JP2007537238A (ja) | 2004-05-14 | 2007-12-20 | ファイザー・プロダクツ・インク | 異常細胞増殖の治療のためのピリミジン誘導体 |
| EP1794135A1 (en) | 2004-09-27 | 2007-06-13 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| MY169441A (en) * | 2004-12-08 | 2019-04-11 | Janssen Pharmaceutica Nv | 2,4, (4,6) pyrimidine derivatives |
| WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
| WO2006129100A1 (en) | 2005-06-03 | 2006-12-07 | Glaxo Group Limited | Novel compounds |
| WO2007028445A1 (en) | 2005-07-15 | 2007-03-15 | Glaxo Group Limited | 6-indolyl-4-yl-amino-5-halogeno-2-pyrimidinyl-amino derivatives |
| JP5161233B2 (ja) | 2006-10-19 | 2013-03-13 | ライジェル ファーマシューティカルズ, インコーポレイテッド | 自己免疫疾患の処置のためのjakキナーゼの阻害剤としての2,4−ピリミジンアミン誘導体 |
| DE102007010801A1 (de) | 2007-03-02 | 2008-09-04 | Bayer Cropscience Ag | Diaminopyrimidine als Fungizide |
| JP2010523639A (ja) | 2007-04-12 | 2010-07-15 | エフ.ホフマン−ラ ロシュ アーゲー | 医薬化合物 |
| WO2008140421A2 (en) * | 2007-05-15 | 2008-11-20 | S*Bio Pte Ltd | Heterocycloalkyl substituted pyrimidine derivatives |
| US8461147B2 (en) | 2007-12-03 | 2013-06-11 | Boehringer Ingelheim International Gmbh | Diaminopyridines for the treatment of diseases which are characterised by excessive or anomal cell proliferation |
| WO2009083185A2 (en) | 2007-12-28 | 2009-07-09 | Fovea Pharmaceuticals Sa | Compositions and methods for prophylaxis and treatment of cellular degenerative ophthalmic disorders |
| HRP20161310T1 (hr) | 2008-04-16 | 2016-12-02 | Portola Pharmaceuticals, Inc. | 2,6-diamino-pirimidin-5-il-karboksamidi kao inhibitori syk ili jak kinaza |
| EP2274288A2 (en) * | 2008-04-24 | 2011-01-19 | Incyte Corporation | Macrocyclic compounds and their use as kinase inhibitors |
| AU2009262198B2 (en) | 2008-06-25 | 2012-09-27 | Irm Llc | Pyrimidine derivatives as kinase inhibitors |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| EP2942392B1 (en) * | 2008-06-30 | 2018-10-03 | Janssen Biotech, Inc. | Differentiation of pluripotent stem cells |
| US20120114637A1 (en) | 2009-05-04 | 2012-05-10 | Santen Pharmaceutical Co., Ltd. | Mtor pathway inhibitors for treating ocular disorders |
| CA2763720A1 (en) | 2009-06-18 | 2010-12-23 | Cellzome Limited | Sulfonamides and sulfamides as zap-70 inhibitors |
| US20130040310A1 (en) * | 2009-12-15 | 2013-02-14 | Salk Institute For Biological Studies | Ulk1 compositions, inhibitors, screening and methods of use |
| CN102792160B (zh) | 2010-01-08 | 2015-08-19 | 新加坡科技研究局 | 用于治疗癌症的方法和组合物 |
| WO2011133668A2 (en) | 2010-04-20 | 2011-10-27 | President And Fellows Of Harvard College | Methods and compositions for the treatment of cancer |
| TW201217527A (en) | 2010-07-09 | 2012-05-01 | Biogen Idec Hemophilia Inc | Processable single chain molecules and polypeptides made using same |
| WO2012040602A2 (en) | 2010-09-23 | 2012-03-29 | President And Fellows Of Harvard College | Targeting mtor substrates in treating proliferative diseases |
| WO2012045195A1 (en) | 2010-10-09 | 2012-04-12 | Abbott Laboratories | Pyrrolopyrimidines as fak and alk inhibiters for treatment of cancers and other diseases |
| US8691777B2 (en) | 2011-01-27 | 2014-04-08 | Emory University | Combination therapy |
| CA2864394C (en) | 2011-03-02 | 2021-10-19 | Jack Roth | A method of predicting a response to a tusc2 therapy |
| CN103458970A (zh) | 2011-03-07 | 2013-12-18 | 泰莱托恩基金会 | Tfeb磷酸化抑制剂及其应用 |
| US20140343128A1 (en) | 2011-11-15 | 2014-11-20 | Novartis Ag | Combination of a phosphoinositide 3-kinase inhibitor and a modulator of the Janus Kinase 2 - Signal Transducer and Activator of Transcription 5 pathway |
| US9073944B2 (en) | 2012-02-21 | 2015-07-07 | Merck Patent Gmbh | Cyclic diaminopyrimidine derivatives |
| WO2013173506A2 (en) | 2012-05-16 | 2013-11-21 | Rigel Pharmaceuticals, Inc. | Method of treating muscular degradation |
| US20150250808A1 (en) | 2012-10-15 | 2015-09-10 | Vojo P. Deretic | Treatment of autophagy-based disorders and related pharmaceutical compositions, diagnostic and screening assays and kits |
| AU2013337717B2 (en) | 2012-11-01 | 2018-10-25 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using PI3 kinase isoform modulators |
| WO2014098932A1 (en) | 2012-12-17 | 2014-06-26 | The Brigham And Women's Hosptial, Inc. | Treatment of mtor hyperactive related diseases and disorders |
| CN103059030B (zh) | 2012-12-28 | 2015-04-29 | 北京师范大学 | 一种具有粘着斑激酶抑制作用的嘧啶类化合物及其制备方法和应用 |
| JP2016506930A (ja) | 2013-01-25 | 2016-03-07 | ライジェル ファーマシューティカルズ, インコーポレイテッド | 炎症性腸疾患を処置するための化合物および方法 |
| EP3473299A1 (en) | 2013-06-05 | 2019-04-24 | Salk Institute for Biological Studies | Vitamin d receptor agonists to treat diseases involving cxcl12 activity |
| US10300058B2 (en) | 2014-04-18 | 2019-05-28 | Xuanzhu Pharma Co., Ltd. | Tyrosine kinase inhibitor and uses thereof |
| EP3159338A4 (en) | 2014-06-17 | 2018-01-24 | Korea Research Institute of Chemical Technology | Pyrimidine-2,4-diamine derivative and anticancer pharmaceutical composition comprising same as effective ingredient |
| RS62017B1 (sr) | 2014-09-17 | 2021-07-30 | Celgene Car Llc | Mk2 inhibitori i njihova upotreba |
| KR102608590B1 (ko) | 2014-09-24 | 2023-12-01 | 솔크 인스티튜트 포 바이올로지칼 스터디즈 | 종양 살상 바이러스 및 이의 사용방법 |
| CN105524045B (zh) | 2014-10-22 | 2020-04-10 | 山东轩竹医药科技有限公司 | 四环类间变性淋巴瘤激酶抑制剂 |
| US20160159774A1 (en) | 2014-12-05 | 2016-06-09 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| CN106188029B (zh) | 2015-05-05 | 2018-09-18 | 山东轩竹医药科技有限公司 | 二并环类间变性淋巴瘤激酶抑制剂 |
| WO2017024019A1 (en) | 2015-08-04 | 2017-02-09 | Celgene Corporation | Methods for treating chronic lymphocytic leukemia and the use of biomarkers as a predictor of clinical sensitivity to immunomodulatory therapies |
| CN105801603B (zh) * | 2016-04-13 | 2018-10-02 | 成都倍特药业有限公司 | 一种具有大环结构的alk抑制剂及其制备方法 |
| AU2017346845B2 (en) | 2016-10-18 | 2021-12-02 | Dana-Farber Cancer Institute, Inc. | Pyrimido-diazepinone kinase scaffold compounds and methods of treating DCLK1/2-mediated disorders |
| WO2018102366A1 (en) | 2016-11-30 | 2018-06-07 | Ariad Pharmaceuticals, Inc. | Anilinopyrimidines as haematopoietic progenitor kinase 1 (hpk1) inhibitors |
| JP6684700B2 (ja) | 2016-12-26 | 2020-04-22 | アイシン精機株式会社 | 乗員検知装置 |
| CN110831937A (zh) | 2017-05-02 | 2020-02-21 | 韩国化学研究院 | 嘧啶衍生物化合物、其光学异构体或其药学上可接受的盐及包含其为有效成分的Tyro3相关疾病的预防或治疗用组合物 |
| PE20220597A1 (es) | 2019-05-10 | 2022-04-22 | Deciphera Pharmaceuticals Llc | Inhibidores de la autofagia de fenilaminopirimidina amida y metodos de uso de estos |
| US11518758B2 (en) | 2019-05-10 | 2022-12-06 | Deciphera Pharmaceuticals, Llc | Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof |
| PE20221083A1 (es) | 2019-06-17 | 2022-07-05 | Deciphera Pharmaceuticals Llc | Inhibidores de la autofagia de la amida aminopirimidina y sus metodos de uso |
| KR20220154094A (ko) | 2020-02-14 | 2022-11-21 | 솔크 인스티튜트 포 바이올로지칼 스터디즈 | Ulk1/2 억제제를 이용한 단일 및 병용 요법 |
| KR20220153581A (ko) | 2020-02-14 | 2022-11-18 | 솔크 인스티튜트 포 바이올로지칼 스터디즈 | Ulk1/2 의 억제제 및 이의 사용 방법 |
| US20230159556A1 (en) * | 2020-04-20 | 2023-05-25 | Tenova Pharmaceuticals Inc. | Novel protein kinase inhibitors |
| WO2022072668A1 (en) | 2020-09-30 | 2022-04-07 | Salk Institute For Biological Studies | Patient selection biomarkers for treatment with ulk inhibitors |
-
2021
- 2021-02-12 KR KR1020227028938A patent/KR20220153582A/ko active Pending
- 2021-02-12 AU AU2021221162A patent/AU2021221162A1/en active Pending
- 2021-02-12 US US17/799,634 patent/US12594277B2/en active Active
- 2021-02-12 CN CN202180027809.1A patent/CN115515588A/zh active Pending
- 2021-02-12 EP EP21753844.6A patent/EP4103183A4/en active Pending
- 2021-02-12 WO PCT/US2021/018038 patent/WO2021163627A1/en not_active Ceased
- 2021-02-12 CA CA3171185A patent/CA3171185A1/en active Pending
- 2021-02-12 JP JP2022549144A patent/JP2023513793A/ja active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20190284207A1 (en) * | 2014-08-25 | 2019-09-19 | Salk Institute For Biological Studies | Novel ulk1 inhibitors and methods using same |
| WO2016196393A2 (en) * | 2015-05-29 | 2016-12-08 | Presage Biosciences, Inc. | Autophagy-inhibiting compounds and uses thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2021163627A1 (en) | 2021-08-19 |
| CA3171185A1 (en) | 2021-08-19 |
| AU2021221162A1 (en) | 2022-09-22 |
| US12594277B2 (en) | 2026-04-07 |
| JP2023513793A (ja) | 2023-04-03 |
| US20230099804A1 (en) | 2023-03-30 |
| KR20220153582A (ko) | 2022-11-18 |
| EP4103183A1 (en) | 2022-12-21 |
| EP4103183A4 (en) | 2024-02-28 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN115515588A (zh) | 大环ulk1/2抑制剂 | |
| RU2719428C2 (ru) | Индазольные соединения в качестве ингибиторов киназы fgfr, их получение и применение | |
| CN115232129B (zh) | 一种parp1选择性抑制剂及其制备方法和用途 | |
| CN117157292A (zh) | Kras g12d抑制剂和其用途 | |
| CN109311894B (zh) | 作为激酶抑制剂的n-(取代的-苯基)-磺酰胺衍生物 | |
| AU2015266453C1 (en) | Alk kinase inhibitor, and preparation method and use thereof | |
| CN104066735B (zh) | 作为akt激酶抑制剂的取代的咪唑并吡嗪 | |
| CA2830367A1 (en) | Novel imidazo-oxazine compound or salt thereof | |
| WO2025045106A1 (zh) | 一种PI3Kα抑制剂及其用途 | |
| CN117143107A (zh) | 1,2-二氢吡啶类衍生物及其制备方法和用途 | |
| CN115515589A (zh) | Ulk1/2抑制剂及其使用方法 | |
| CN104603134A (zh) | 酰氨基-苄基砜和亚砜衍生物 | |
| EP3496724B1 (en) | Protein kinase regulators | |
| CN114621231A (zh) | 一种靶向降解/抑制活性的嵌合化合物及其制备方法和用途 | |
| JPWO2020032105A1 (ja) | 光学活性な架橋型ピペリジン誘導体 | |
| WO2017191599A1 (en) | Substituted 2, 4-diamino-quinoline derivatives for use in the treatment of proliferative diseases | |
| EP3705480A1 (en) | Class of amino-substituted nitrogen-containing fused ring compounds, preparation method therefor, and use thereof | |
| CN103313599A (zh) | 取代的4-(芳基氨基)硒吩并嘧啶化合物及其使用方法 | |
| EP3805212A1 (en) | 3-oxazolinone compound, preparation method therefor and pharmaceutical application thereof | |
| EP4126842B1 (en) | Trka inhibitor | |
| KR20240041340A (ko) | 피롤로피리미딘 유도체 화합물 및 이의 용도 | |
| WO2020233716A1 (zh) | 咪唑并哒嗪类mnk1/mnk2激酶抑制剂及其制备方法和应用 | |
| CN120058674A (zh) | 4(1h-吡唑-3-基)哌啶基衍生物及其制备方法与在制备mnk抑制剂中的应用 | |
| CN118434743A (zh) | 三环杂环类 | |
| WO2026067457A1 (zh) | 作为pkmyt1抑制剂的化合物 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20221223 |
|
| WD01 | Invention patent application deemed withdrawn after publication |