CN117794929A - 选择性bcl-xl protac化合物及使用方法 - Google Patents

选择性bcl-xl protac化合物及使用方法 Download PDF

Info

Publication number
CN117794929A
CN117794929A CN202280024161.7A CN202280024161A CN117794929A CN 117794929 A CN117794929 A CN 117794929A CN 202280024161 A CN202280024161 A CN 202280024161A CN 117794929 A CN117794929 A CN 117794929A
Authority
CN
China
Prior art keywords
group
alkylene
branched
alkyl
straight
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
CN202280024161.7A
Other languages
English (en)
Chinese (zh)
Inventor
A·赫尔纳
P·马卡奇
刘纲
中嶋胜正
T·诺瓦克
G-A·弗兰泽蒂
J-B·斯塔克
F·科朗德
P·德索斯
A·帕扎尔
B·斯佐科尔
M·P·缇马利
V·昆
M·T·伯格
J·A·达莱西奥
K·E·塞伊斯
R·M·托马斯
赵亮
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
Les Laboratoires Servier SAS
Original Assignee
Novartis AG
Les Laboratoires Servier SAS
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 Novartis AG, Les Laboratoires Servier SAS filed Critical Novartis AG
Publication of CN117794929A publication Critical patent/CN117794929A/zh
Pending legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN202280024161.7A 2021-02-02 2022-02-01 选择性bcl-xl protac化合物及使用方法 Pending CN117794929A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202163144577P 2021-02-02 2021-02-02
US63/144,577 2021-02-02
PCT/US2022/014790 WO2022169780A1 (en) 2021-02-02 2022-02-01 Selective bcl-xl protac compounds and methods of use

Publications (1)

Publication Number Publication Date
CN117794929A true CN117794929A (zh) 2024-03-29

Family

ID=80735817

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202280024161.7A Pending CN117794929A (zh) 2021-02-02 2022-02-01 选择性bcl-xl protac化合物及使用方法

Country Status (9)

Country Link
US (2) US20240376094A2 (https=)
EP (1) EP4288434A1 (https=)
JP (1) JP2024505562A (https=)
KR (1) KR20230170644A (https=)
CN (1) CN117794929A (https=)
AU (1) AU2022218128A1 (https=)
CA (1) CA3206906A1 (https=)
IL (1) IL304891A (https=)
WO (1) WO2022169780A1 (https=)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20230171979A (ko) 2021-04-16 2023-12-21 아비나스 오퍼레이션스, 인코포레이티드 Bcl6 단백질 분해의 조절제 및 관련 사용 방법
WO2023215449A1 (en) 2022-05-06 2023-11-09 Treeline Biosciences, Inc. Tetrahydroisoquinoline heterobifunctional bcl-xl degraders
EP4519259A1 (en) 2022-05-06 2025-03-12 Treeline Biosciences, Inc. Tetrahydroisoquinoline heterobifunctional bcl-xl degraders
EP4519260A1 (en) 2022-05-06 2025-03-12 Treeline Biosciences, Inc. Tetrahydroisoquinoline heterobifunctional bcl-xdegraders
CN115959992A (zh) * 2022-12-13 2023-04-14 武汉翱飞科技有限公司 一种单分子量聚乙二醇单乙酸的合成方法
TW202527930A (zh) 2023-11-07 2025-07-16 美商樹線生物科學公司 四氫異喹啉異雙功能bcl-xl降解劑
TW202535872A (zh) 2023-11-07 2025-09-16 美商樹線生物科學公司 四氫異喹啉異雙功能bcl-xl降解劑
WO2025101575A1 (en) 2023-11-07 2025-05-15 Treeline Biosciences, Inc. Tetrahydroisoquinoline heterobifunctional bcl-x l degraders

Family Cites Families (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2779780A (en) 1955-03-01 1957-01-29 Du Pont 1, 4-diamino-2, 3-dicyano-1, 4-bis (substituted mercapto) butadienes and their preparation
EP1143957A3 (en) 1998-12-16 2002-02-27 Warner-Lambert Company Treatment of arthritis with mek inhibitors
GB0000313D0 (en) 2000-01-10 2000-03-01 Astrazeneca Uk Ltd Formulation
JP3811775B2 (ja) 2000-07-19 2006-08-23 ワーナー−ランバート カンパニー リミティド ライアビリティー カンパニー 4−ヨードフェニルアミノベンズヒドロキサム酸の酸素化エステル
CN1653059A (zh) 2002-03-08 2005-08-10 卫材株式会社 用作医药品的大环化合物
KR100984595B1 (ko) 2002-03-13 2010-09-30 어레이 바이오파마 인크. Mek 억제제로서의 n3 알킬화 벤즈이미다졸 유도체
CA2512000C (en) 2002-12-26 2011-08-09 Eisai Co., Ltd. Selective estrogen receptor modulator
SI1761528T1 (sl) 2004-06-11 2008-06-30 Japan Tobacco Inc 5-amino-2,4,7-triokso-3,4,7,8-tetrahidro-2H-pirido(2,3-D)pirimidinski derivati in sorodne spojine za zdravljenje raka
WO2007004415A1 (ja) 2005-07-01 2007-01-11 Murata Manufacturing Co., Ltd. 多層セラミック基板およびその製造方法ならびに多層セラミック基板作製用複合グリーンシート
PE20110220A1 (es) 2006-08-02 2011-04-11 Novartis Ag DERIVADOS DE 2-OXO-ETIL-AMINO-PROPIONAMIDA-PIRROLIDIN-2-IL-SUSTITUIDOS COMO INHIBIDORES DEL ENLACE DE LA PROTEINA Smac AL INHIBIDOR DE LA PROTEINA DE APOPTOSIS
AU2007286808B2 (en) 2006-08-21 2012-12-06 Genentech, Inc. Aza-benzofuranyl compounds and methods of use
JP5421925B2 (ja) 2007-12-19 2014-02-19 ジェネンテック, インコーポレイテッド 5−アニリノイミダゾピリジン及び使用の方法
ES2522346T3 (es) 2008-08-22 2014-11-14 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de CDK
NZ593536A (en) 2008-12-19 2013-07-26 Genentech Inc Quinoline derivatives and methods of use
WO2010080503A1 (en) 2008-12-19 2010-07-15 Genentech, Inc. Heterocyclic compounds and methods of use
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
RS56042B1 (sr) 2010-06-10 2017-09-29 Seragon Pharmaceuticals Inc Modulatori estrogenih receptora i njihove upotrebe
US8853423B2 (en) 2010-06-17 2014-10-07 Seragon Pharmaceuticals, Inc. Indane estrogen receptor modulators and uses thereof
GB2483736B (en) 2010-09-16 2012-08-29 Aragon Pharmaceuticals Inc Estrogen receptor modulators and uses thereof
MX368257B (es) 2011-08-01 2019-09-26 Genentech Inc Antagonistas de unión al eje pd-1e inhibidores de mek y sus usos en el tratamiento de cáncer.
TWI571466B (zh) 2011-10-14 2017-02-21 艾伯維有限公司 用於治療癌症及免疫與自體免疫疾病之細胞凋亡誘發劑
TWI561521B (en) 2011-10-14 2016-12-11 Abbvie Inc Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
KR102668696B1 (ko) 2012-01-12 2024-05-29 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
FR2986002B1 (fr) 2012-01-24 2014-02-21 Servier Lab Nouveaux derives d'indolizine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
ES2671516T3 (es) 2013-02-19 2018-06-06 Novartis Ag Derivados de benzotiofeno y composiciones de los mismos como degradantes selectivos de los receptores de estrógeno
FR3008975A1 (fr) 2013-07-23 2015-01-30 Servier Lab Nouveaux derives de pyrrole, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
AP2016009099A0 (en) 2013-11-01 2016-03-31 Novartis Ag Aminoheteroaryl benzamides as kinase inhibitors
FR3015483B1 (fr) 2013-12-23 2016-01-01 Servier Lab Nouveaux derives de thienopyrimidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
SG11201607339VA (en) 2014-03-13 2016-10-28 Hoffmann La Roche Methods and compositions for modulating estrogen receptor mutants
RU2738833C9 (ru) 2014-04-14 2022-02-28 Арвинас, Оперэйшнз, Инк. Имидные модуляторы протеолиза и способы их применения
CN107207553A (zh) 2014-12-09 2017-09-26 艾伯维公司 Bcl‑xl抑制性化合物和包括其的抗体药物缀合物
CN111620861A (zh) 2014-12-09 2020-09-04 艾伯维公司 具有低细胞渗透性的bcl-xl抑制性化合物以及包括它的抗体药物缀合物
CN113209306A (zh) 2014-12-09 2021-08-06 艾伯维公司 具有细胞渗透性的bcl-xl抑制剂的抗体药物缀合物
WO2016105518A1 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
EP3270917A4 (en) 2015-03-18 2018-08-08 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
WO2017007612A1 (en) 2015-07-07 2017-01-12 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
CN109152933B (zh) 2016-04-21 2022-12-02 生物风险投资有限责任公司 诱导抗细胞凋亡bcl-2家族蛋白的降解的化合物及其用途
AU2018258581A1 (en) 2017-04-28 2019-11-07 Quartz Therapeutics, Inc. RAF-degrading conjugate compounds
ES3041854T3 (en) 2018-01-22 2025-11-17 Bioventures Llc Bcl-2 proteins degraders for cancer treatment
JP7708662B2 (ja) * 2018-10-24 2025-07-15 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト コンジュゲート化された化学的分解誘導物質および使用方法
US11547759B2 (en) * 2019-01-30 2023-01-10 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
CN113660937A (zh) 2019-02-08 2021-11-16 佛罗里达大学研究基金公司 治疗剂和治疗方法
AU2020310147A1 (en) 2019-07-10 2022-01-06 Recurium Ip Holdings, Llc Bcl-2 protein inhibitors
AR119493A1 (es) * 2019-07-29 2021-12-22 Servier Lab Derivados de 3,6-diamino-piridazin-3-ilo, composiciones farmacéuticas que los contienen y sus usos como agentes proapoptóticos
AR119494A1 (es) * 2019-07-29 2021-12-22 Servier Lab DERIVADOS DE 6,7-DIHIDRO-5H-PIRIDO[2,3-c]PIRIDAZIN-8-ILO, COMPOSICIONES FARMACÉUTICAS QUE LOS CONTIENEN Y SUS USOS COMO AGENTES PROAPOPTÓTICOS

Also Published As

Publication number Publication date
KR20230170644A (ko) 2023-12-19
AU2022218128A1 (en) 2023-08-17
US20250179063A2 (en) 2025-06-05
EP4288434A1 (en) 2023-12-13
US20240182464A1 (en) 2024-06-06
IL304891A (en) 2023-10-01
JP2024505562A (ja) 2024-02-06
WO2022169780A1 (en) 2022-08-11
CA3206906A1 (en) 2022-08-11
US20240376094A2 (en) 2024-11-14

Similar Documents

Publication Publication Date Title
CN117794929A (zh) 选择性bcl-xl protac化合物及使用方法
TWI869913B (zh) 吡啶并[4,3-d]嘧啶化合物
US12281127B2 (en) Pyrido[4,3-d]pyrimidine compounds
CN114025844B (zh) 蛋白酪氨酸磷酸酶抑制剂及其使用方法
CN114450284B (zh) 作为bcl-xl蛋白抑制剂的6,7-二氢-5h-吡啶并[2,3-c]哒嗪衍生物
WO2022228543A1 (zh) 桥环类化合物、其制备方法及其在医药上的应用
WO2021218110A1 (zh) 一类苯并噻唑基联芳基类化合物、制备方法和用途
CN118084870A (zh) 稠环化合物
WO2024189481A1 (en) Panras inhibitor antibody-drug conjugates and methods of use thereof
CN112996518A (zh) Wd40重复结构域蛋白5(wdr5)降解/破坏化合物和使用方法
CN115443276A (zh) 吡啶并嘧啶酮衍生物及其作为芳烃受体调节剂的应用
JP2025100453A (ja) ピリド[4,3-d]ピリミジン化合物
WO2023174406A1 (zh) 含氮杂环类衍生物抑制剂、其制备方法和应用
US20230416331A1 (en) Peptide conjugates of peptidic tubulin inhibitors as therapeutics
HK40111548A (zh) 选择性bcl-xl protac化合物及使用方法
US20100022607A1 (en) Diazonamide analogs
CN103582645B (zh) 二氢氧茚吲哚类似物
WO2025228384A1 (en) Antibody-drug conjugates and use thereof
WO2025228381A1 (en) Antibody-drug conjugate and use thereof
RU2857665C2 (ru) Соединения пиридо[4,3-d]пиримидина
WO2025094035A1 (en) Toll-like receptor agonists and conjugates thereof
WO2025215536A1 (en) Macrocyclic panras inhibitors for the treatment of cancer
HK40117290A (zh) 吡啶并[4,3-d]嘧啶化合物
HK40128596A (zh) 吡啶并[4,3-d]嘧啶化合物
TW202608895A (zh) 抗體-藥物偶聯物及其用途

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
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40111548

Country of ref document: HK