JP2023513793A - 大環状ｕｌｋ１／２阻害剤 - Google Patents

大環状ｕｌｋ１／２阻害剤 Download PDF

Info

Publication number
JP2023513793A
JP2023513793A JP2022549144A JP2022549144A JP2023513793A JP 2023513793 A JP2023513793 A JP 2023513793A JP 2022549144 A JP2022549144 A JP 2022549144A JP 2022549144 A JP2022549144 A JP 2022549144A JP 2023513793 A JP2023513793 A JP 2023513793A
Authority
JP
Japan
Prior art keywords
alkyl
independently
cycloalkyl
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
Application number
JP2022549144A
Other languages
English (en)
Japanese (ja)
Other versions
JP2023513793A5 (https=
Inventor
ニコラス ディー．ピー． コスフォード、
ニコル エー． バカス、
ルーベン ジェイ． ショー、
アリソン エス． リンパート、
ソーニャ エヌ． ブラン、
Original Assignee
ソーク インスティテュート フォー バイオロジカル スタディーズ
サンフォード バーナム プレビーズ メディカル ディスカバリー インスティテュート
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by ソーク インスティテュート フォー バイオロジカル スタディーズ, サンフォード バーナム プレビーズ メディカル ディスカバリー インスティテュート filed Critical ソーク インスティテュート フォー バイオロジカル スタディーズ
Publication of JP2023513793A publication Critical patent/JP2023513793A/ja
Publication of JP2023513793A5 publication Critical patent/JP2023513793A5/ja
Pending legal-status Critical Current

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)
JP2022549144A 2020-02-14 2021-02-12 大環状ｕｌｋ１／２阻害剤 Pending JP2023513793A (ja)

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 (2)

Publication Number Publication Date
JP2023513793A true JP2023513793A (ja) 2023-04-03
JP2023513793A5 JP2023513793A5 (https=) 2024-02-20

Family

ID=77292762

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2022549144A Pending JP2023513793A (ja) 2020-02-14 2021-02-12 大環状ｕｌｋ１／２阻害剤

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)

* Cited by examiner, † Cited by third party
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 (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008523033A (ja) * 2004-12-08 2008-07-03 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ２，４（４，６）ピリミジン誘導体
JP2011518836A (ja) * 2008-04-24 2011-06-30 インサイト・コーポレイション 大環状化合物およびそれらのキナーゼ阻害剤としての使用
JP2011526786A (ja) * 2008-06-30 2011-10-20 セントコア・オーソ・バイオテツク・インコーポレーテツド 多能性幹細胞の分化
JP2015508099A (ja) * 2012-02-21 2015-03-16 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ 環状ジアミノピリジン誘導体
CN105801603A (zh) * 2016-04-13 2016-07-27 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
JP2017526674A (ja) * 2014-08-25 2017-09-14 ソーク インスティテュート フォー バイオロジカル スタディーズ 新規ｕｌｋ１阻害剤およびそれを使用する方法

Family Cites Families (63)

* Cited by examiner, † Cited by third party
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
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
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
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
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
GB2555270A (en) * 2015-05-29 2018-04-25 Presage Biosciences Inc Autophagy-inhibiting compounds and uses thereof
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
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

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008523033A (ja) * 2004-12-08 2008-07-03 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ２，４（４，６）ピリミジン誘導体
JP2011518836A (ja) * 2008-04-24 2011-06-30 インサイト・コーポレイション 大環状化合物およびそれらのキナーゼ阻害剤としての使用
JP2011526786A (ja) * 2008-06-30 2011-10-20 セントコア・オーソ・バイオテツク・インコーポレーテツド 多能性幹細胞の分化
JP2015508099A (ja) * 2012-02-21 2015-03-16 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ 環状ジアミノピリジン誘導体
JP2017526674A (ja) * 2014-08-25 2017-09-14 ソーク インスティテュート フォー バイオロジカル スタディーズ 新規ｕｌｋ１阻害剤およびそれを使用する方法
CN105801603A (zh) * 2016-04-13 2016-07-27 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

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
CN115515588A (zh) 2022-12-23
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
US12594277B2 (en) Macrocyclic ULK1/2 inhibitors
JP2022506887A (ja) 窒素含有縮合複素環系ｓｈｐ２阻害剤化合物、製造方法及び使用
WO2021163629A1 (en) Inhibitors of ulk1/2 and methods of using same
CN105517549B (zh) CaMKII抑制剂和其用途
CN117143107A (zh) 1,2-二氢吡啶类衍生物及其制备方法和用途
CN112851663B (zh) 一种并杂环化合物及其用途
JP2022521536A (ja) イミダゾピリジニル化合物及び神経変性障害の処置のためのその使用
CA3115897A1 (en) Tricyclic janus kinase 1 inhibitors, and compositions and methods thereof
WO2021041976A1 (en) Perk inhibiting indolinyl compounds
EP3452465A1 (en) Substituted 2, 4-diamino-quinoline derivatives for use in the treatment of proliferative diseases
CA3093706A1 (en) Jak inhibitors
CA3229293A1 (en) 6-aza-quinoline derivatives and related uses
AU2009284086B2 (en) New (poly)aminoalkylaminoalkylamide, alkyl-urea, or alkyl-sulfonamide derivatives of epipodophyllotoxin, a process for preparing them, and application thereof in therapy as anticancer agents
WO2024222914A2 (en) Mta-cooperative prmt5 inhibitor
EP4126842B1 (en) Trka inhibitor
CA3181351A1 (en) Nampt modulators
CN114907350B (zh) 一类含氮稠环类化合物、制备方法和用途
CN120957987A (zh) 取代的磺内酰胺化合物衍生物及其药物用途
CN116425796A (zh) 一类嘧啶并杂环类化合物、制备方法和用途
JP7010443B2 (ja) インドリジン系化合物、その製造方法及び用途
WO2026033475A1 (en) Substituted aryl or heteroaryl compound derivatives and pharmaceutical use thereof
HK40078982B (en) Trka inhibitor
HK40001081A (en) Substituted 2, 4-diamino-quinoline derivatives for use in the treatment of proliferative diseases

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20240209

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20240209

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20250116

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20250212

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20250805