[go: up one dir, main page]

MX2018012174A - Degradantes de proteina homologa de proteina murina de cromosoma diminuto doble (mdm2). - Google Patents

Degradantes de proteina homologa de proteina murina de cromosoma diminuto doble (mdm2).

Info

Publication number
MX2018012174A
MX2018012174A MX2018012174A MX2018012174A MX2018012174A MX 2018012174 A MX2018012174 A MX 2018012174A MX 2018012174 A MX2018012174 A MX 2018012174A MX 2018012174 A MX2018012174 A MX 2018012174A MX 2018012174 A MX2018012174 A MX 2018012174A
Authority
MX
Mexico
Prior art keywords
mdm2 protein
formula
present disclosure
protein degraders
provides compounds
Prior art date
Application number
MX2018012174A
Other languages
English (en)
Inventor
Aguilar Angelo
Wang Shaomeng
Li Yangbing
Yang Jiuling
Zhou Bing
Hu Jiantao
Xu Fuming
Rej Rohan
Han Xin
Original Assignee
Univ Michigan Regents
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 Univ Michigan Regents filed Critical Univ Michigan Regents
Publication of MX2018012174A publication Critical patent/MX2018012174A/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10Spiro-condensed systems
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente descripción proporciona compuestos representados por la fórmula I-A: A1-L1-B1 I-A y sales, hidratos y solvatos farmacéuticamente aceptables de los mismos, en donde A1, B1 y L1 son como se definen, como se establece en la especificación. La presente descripción también proporciona compuestos de fórmula I-A para usarse para tratar una condición o trastorno que responde a la degradación de la proteína MDM2, como por ejemplo cáncer.
MX2018012174A 2016-04-06 2017-04-06 Degradantes de proteina homologa de proteina murina de cromosoma diminuto doble (mdm2). MX2018012174A (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201662318974P 2016-04-06 2016-04-06
US201662393874P 2016-09-13 2016-09-13
US201662409571P 2016-10-18 2016-10-18
PCT/US2017/026274 WO2017176957A1 (en) 2016-04-06 2017-04-06 Mdm2 protein degraders

Publications (1)

Publication Number Publication Date
MX2018012174A true MX2018012174A (es) 2019-07-08

Family

ID=58549316

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2018012174A MX2018012174A (es) 2016-04-06 2017-04-06 Degradantes de proteina homologa de proteina murina de cromosoma diminuto doble (mdm2).

Country Status (14)

Country Link
US (2) US11192898B2 (es)
EP (1) EP3440066B1 (es)
JP (2) JP7037500B2 (es)
KR (1) KR102387316B1 (es)
CN (2) CN113788818A (es)
AU (1) AU2017246452C1 (es)
CA (1) CA3020275A1 (es)
IL (1) IL262103B (es)
MX (1) MX2018012174A (es)
RU (2) RU2021102253A (es)
SG (1) SG11201808728QA (es)
UA (1) UA123786C2 (es)
WO (1) WO2017176957A1 (es)
ZA (1) ZA201806968B (es)

Families Citing this family (105)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102387316B1 (ko) * 2016-04-06 2022-04-15 더 리젠츠 오브 더 유니버시티 오브 미시간 Mdm2 단백질 분해제
JP6968823B2 (ja) 2016-04-22 2021-11-17 ダナ−ファーバー キャンサー インスティテュート,インコーポレイテッド Egfrの分解のための二官能性分子、及び使用方法
EP4491236A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
WO2017197036A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
EP3455218A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
IL297717A (en) * 2016-12-01 2022-12-01 Arvinas Operations Inc History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
EP3577109A4 (en) 2017-01-31 2020-11-18 Arvinas Operations, Inc. CEREMONY LIGANDS AND BIFUNCTIONAL COMPOUNDS CONTAINING THEM
CN118440096A (zh) 2017-06-20 2024-08-06 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体
US10357489B2 (en) 2017-07-10 2019-07-23 Celgene Corporation Antiproliferative compounds and methods of use thereof
WO2019043208A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROQUINOLINONES
EP3679026A1 (en) 2017-09-04 2020-07-15 C4 Therapeutics, Inc. Glutarimide
CN111315735B (zh) 2017-09-04 2024-03-08 C4医药公司 二氢苯并咪唑酮
WO2019060742A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc AGENTS FOR DEGRADING PROTEINS AND USES THEREOF
EP3684366A4 (en) 2017-09-22 2021-09-08 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES OF THE LATEST
CN111372585A (zh) 2017-11-16 2020-07-03 C4医药公司 用于靶蛋白降解的降解剂和降解决定子
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
WO2019140380A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Protein degraders and uses thereof
EP3737675A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
KR20210018199A (ko) 2018-03-26 2021-02-17 씨4 테라퓨틱스, 인코포레이티드 이카로스의 분해를 위한 세레블론 결합제
JP7367908B2 (ja) * 2018-04-09 2023-10-24 上海科技大学 標的タンパク質分解化合物、その抗腫瘍応用、その中間体および中間体の応用
WO2019204354A1 (en) 2018-04-16 2019-10-24 C4 Therapeutics, Inc. Spirocyclic compounds
EP4272737A3 (en) 2018-04-23 2024-01-17 Celgene Corporation Substituted 4-aminoisoindoline-1,3-dione compounds and their use for treating lymphoma
WO2019213005A1 (en) * 2018-04-30 2019-11-07 Dana-Farber Cancer Institute, Inc. Small molecule degraders of polybromo-1 (pbrm1)
EP3578561A1 (en) 2018-06-04 2019-12-11 F. Hoffmann-La Roche AG Spiro compounds
WO2020010227A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Protein degraders and uses thereof
US11292792B2 (en) 2018-07-06 2022-04-05 Kymera Therapeutics, Inc. Tricyclic CRBN ligands and uses thereof
CN108864113B (zh) * 2018-08-03 2021-08-13 南方科技大学 一种mdm2-hdac双靶点抑制剂、药物组合物及其制备和用途
KR20210073490A (ko) * 2018-08-08 2021-06-18 어센테지 파마 (쑤저우) 컴퍼니 리미티드 면역요법과 mdm2 억제제의 병용
CN112912376A (zh) 2018-08-20 2021-06-04 阿尔维纳斯运营股份有限公司 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物
CA3110267A1 (en) 2018-08-22 2020-02-27 Cullgen (Shanghai), Inc. Tropomyosin receptor kinase (trk) degradation compounds and methods of use
US11969472B2 (en) 2018-08-22 2024-04-30 Cullgen (Shanghai), Inc. Tropomyosin receptor kinase (TRK) degradation compounds and methods of use
EP3846800A4 (en) 2018-09-04 2022-08-24 C4 Therapeutics, Inc. Compounds for the degradation of brd9 or mth1
CN110963958B (zh) * 2018-09-30 2025-10-10 上海长森药业有限公司 一种mdm2抑制剂,及其制备方法、药物组合物和应用
MX2021003999A (es) * 2018-10-08 2021-06-23 Univ Michigan Regents Moleculas de bajo peso molecular degradadoras de la proteina mdm2.
CN111018857B (zh) * 2018-10-09 2023-06-02 嘉兴优博生物技术有限公司 靶向蛋白酶降解平台(ted)
CA3119343C (en) 2018-11-13 2024-01-16 Biotheryx, Inc. Substituted isoindolinones
TWI750539B (zh) * 2018-11-23 2021-12-21 大陸商蘇州亞盛藥業有限公司 新穎藥物組成物及其用途
US11352350B2 (en) 2018-11-30 2022-06-07 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
US11034669B2 (en) 2018-11-30 2021-06-15 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
EP3697412A4 (en) * 2018-12-14 2021-02-24 Ascentage Pharma (Suzhou) Co., Ltd. COMPOUND FOR TREATMENT OF OSTEOARTHRITIS
CN120698985A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
US11547759B2 (en) 2019-01-30 2023-01-10 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
US11098025B2 (en) 2019-01-30 2021-08-24 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
SG11202110829YA (en) 2019-04-05 2021-10-28 Kymera Therapeutics Inc Stat degraders and uses thereof
US20220251071A1 (en) * 2019-05-14 2022-08-11 Wisconsin Alumni Research Foundation Method to make small-molecule murine double minute 2 protein (mdm2)-degrading compounds, compounds formed thereby, and pharmaceutical compositions containing them
WO2020264499A1 (en) 2019-06-28 2020-12-30 Kymera Therapeutics, Inc. Irak degraders and uses thereof
EP3814358B1 (en) * 2019-07-11 2025-09-03 Ascentage Pharma (Suzhou) Co., Ltd. Method for preparing 2-indolinospirone compounds and intermediates thereof
US11912699B2 (en) 2019-07-17 2024-02-27 Arvinas Operations, Inc. Tau-protein targeting compounds and associated
EP4021450B1 (en) 2019-08-26 2025-11-05 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
AU2020368542B2 (en) 2019-10-17 2024-02-29 Arvinas Operations, Inc. Bifunctional molecules containing an E3 ubiquitine ligase binding moiety linked to a BCL6 targeting moiety
CN112745298B (zh) * 2019-10-30 2024-04-09 中国科学院上海药物研究所 多取代异吲哚啉类化合物、其制备方法、药物组合物及用途
IL293027A (en) 2019-11-19 2022-07-01 Bristol Myers Squibb Co Compounds useful as inhibitors of Helios protein
WO2021127283A2 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
EP4076520A4 (en) 2019-12-17 2024-03-27 Kymera Therapeutics, Inc. Irak degraders and uses thereof
AU2020405129A1 (en) 2019-12-19 2022-06-23 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
US11850239B2 (en) 2019-12-19 2023-12-26 Ascentage Pharma (Suzhou) Co., Ltd. MDM2 inhibitor and a platinum compound for cancer treatment
BR112022012410A2 (pt) 2019-12-23 2022-08-30 Kymera Therapeutics Inc Degradadores smarca e usos dos mesmos
GB201919219D0 (en) 2019-12-23 2020-02-05 Otsuka Pharma Co Ltd Cancer biomarkers
WO2021147982A1 (en) * 2020-01-23 2021-07-29 Ascentage Pharma (Suzhou) Co., Ltd. Amorphous form or crystalline form of 2-indolinolinololylspironone compounds or their salts, solvent complexes
CN115697989B (zh) 2020-02-26 2025-03-18 上海睿跃生物科技有限公司 原肌球蛋白受体激酶(trk)降解化合物和使用方法
AU2021231898A1 (en) 2020-03-05 2022-10-27 C4 Therapeutics, Inc. Compounds for targeted degradation of BRD9
WO2021185291A1 (zh) * 2020-03-17 2021-09-23 南京明德新药研发有限公司 蛋白降解调节剂与其使用方法
PH12022552458A1 (en) 2020-03-19 2024-01-22 Kymera Therapeutics Inc Mdm2 degraders and uses thereof
CN113509557A (zh) * 2020-04-09 2021-10-19 嘉兴优博生物技术有限公司 靶向蛋白酶降解平台(ted)
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
AU2021314401A1 (en) * 2020-07-20 2023-03-09 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Sulfur-containing isoindoline derivative, and preparation method therefor and medical use thereof
JP2023538517A (ja) 2020-08-05 2023-09-08 シーフォー セラピューティクス, インコーポレイテッド Retの標的分解のための化合物
CA3181715A1 (en) 2020-08-27 2022-03-03 Otsuka Pharmaceutical Co., Ltd. Biomarkers for cancer therapy using mdm2 antagonists
EP4204418A1 (en) 2020-08-28 2023-07-05 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
WO2022052823A1 (zh) * 2020-09-11 2022-03-17 上海邈基生物科技有限公司 一种小分子偶联物及其用途
WO2022120355A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead degraders and uses thereof
TW202241891A (zh) 2020-12-30 2022-11-01 美商凱麥拉醫療公司 Irak降解劑及其用途
CN114853731A (zh) * 2021-02-04 2022-08-05 上海长森药业有限公司 一种双功能mdm2蛋白降解剂,及其制备方法、药物组合物和应用
JP2024506656A (ja) 2021-02-15 2024-02-14 カイメラ セラピューティクス, インコーポレイテッド Irak4分解剤およびその使用
GB202103080D0 (en) 2021-03-04 2021-04-21 Otsuka Pharma Co Ltd Cancer biomarkers
RS66982B1 (sr) 2021-04-06 2025-07-31 Bristol Myers Squibb Co Piridinil supstituisana oksoizoindolinska jedinjenja
EP4323352A1 (en) 2021-04-16 2024-02-21 Arvinas Operations, Inc. Modulators of bcl6 proteolysis and associated methods of use
CA3217417A1 (en) 2021-05-05 2022-11-10 Kevin M. Guckian Compounds for targeting degradation of bruton's tyrosine kinase
US12097261B2 (en) 2021-05-07 2024-09-24 Kymera Therapeutics, Inc. CDK2 degraders and uses thereof
AU2022308734A1 (en) 2021-07-07 2024-02-22 Biogen Ma Inc. Compounds for targeting degradation of irak4 proteins
US20250018046A1 (en) 2021-07-07 2025-01-16 Biogen Ma Inc Compounds for targeting degradation of irak4 proteins
WO2023283425A1 (en) 2021-07-09 2023-01-12 Plexium, Inc. Aryl compounds and pharmaceutical compositions that modulate ikzf2
US11981672B2 (en) 2021-09-13 2024-05-14 Montelino Therapeutics Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
CN117916241A (zh) * 2021-09-13 2024-04-19 阿斯利康(瑞典)有限公司 螺环化合物
EP4405359A4 (en) * 2021-09-22 2025-08-06 Kymera Therapeutics Inc MDM2 DEGRADING AGENTS AND THEIR USES
IL312330A (en) 2021-10-25 2024-06-01 Kymera Therapeutics Inc Tyk2 degraders and uses thereof
WO2023076556A1 (en) 2021-10-29 2023-05-04 Kymera Therapeutics, Inc. Irak4 degraders and synthesis thereof
WO2023114933A1 (en) * 2021-12-15 2023-06-22 Kymera Therapeutics, Inc. Methods of treating cancer
CN113979999B (zh) * 2021-12-23 2022-05-20 北京鑫开元医药科技有限公司 靶向泛素化降解bcr-abl激酶的化合物及其制备方法、组合物和用途
JP2025504059A (ja) 2022-01-31 2025-02-06 カイメラ セラピューティクス, インコーポレイテッド Irakデグレーダー及びその使用
WO2023230059A1 (en) * 2022-05-24 2023-11-30 Newave Pharmaceutical Inc. Mdm2 degrader
WO2024006776A1 (en) 2022-06-27 2024-01-04 Relay Therapeutics, Inc. Estrogen receptor alpha degraders and medical use thereof
TW202417425A (zh) 2022-06-27 2024-05-01 美商傳達治療有限公司 雌激素受體α降解劑及其使用方法
WO2024050016A1 (en) 2022-08-31 2024-03-07 Oerth Bio Llc Compositions and methods for targeted inhibition and degradation of proteins in an insect cell
TW202432544A (zh) 2022-09-07 2024-08-16 美商亞文納營運公司 快速加速纖維肉瘤降解化合物及相關使用方法
WO2024064358A1 (en) 2022-09-23 2024-03-28 Ifm Due, Inc. Compounds and compositions for treating conditions associated with sting activity
CN118047784B (zh) * 2022-10-13 2025-09-16 中国科学院上海药物研究所 具有取代苯基螺[吲哚啉-3,3′-吡咯烷]结构的小分子化合物
WO2024097948A1 (en) 2022-11-04 2024-05-10 Roivant Discovery, Inc. Degraders of mdm2 and uses thereof
WO2024148257A1 (en) * 2023-01-05 2024-07-11 The Wistar Institute Of Anatomy And Biology Mdm2 targeting protacs
WO2024187066A1 (en) * 2023-03-08 2024-09-12 Regents Of The University Of Michigan Compounds and compositions as cbp/p300 degraders and uses thereof
WO2024197219A1 (en) * 2023-03-22 2024-09-26 Kymera Therapeutics, Inc. Mdm2 degraders and uses thereof
KR20240166948A (ko) * 2023-05-18 2024-11-26 아주대학교산학협력단 골 분화 유도 가능한 신규 화합물
WO2025049555A1 (en) 2023-08-31 2025-03-06 Oerth Bio Llc Compositions and methods for targeted inhibition and degradation of proteins in an insect cell

Family Cites Families (92)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5093330A (en) 1987-06-15 1992-03-03 Ciba-Geigy Corporation Staurosporine derivatives substituted at methylamino nitrogen
US7083983B2 (en) 1996-07-05 2006-08-01 Cancer Research Campaign Technology Limited Inhibitors of the interaction between P53 and MDM2
DE69717160T2 (de) 1996-09-13 2003-05-08 Mitsubishi Pharma Corp., Osaka Thienotriazolodiazepinverbindungen und ihre medizinischen anwendungen
US6831155B2 (en) 1999-12-08 2004-12-14 President And Fellows Of Harvard College Inhibition of p53 degradation
US7091353B2 (en) * 2000-12-27 2006-08-15 Celgene Corporation Isoindole-imide compounds, compositions, and uses thereof
US20030045552A1 (en) * 2000-12-27 2003-03-06 Robarge Michael J. Isoindole-imide compounds, compositions, and uses thereof
AU2002361986B2 (en) 2001-12-18 2008-04-10 F. Hoffmann-La Roche Ag CIS-imidazolines as MDM2 inhibitors
DE60225719T2 (de) 2001-12-18 2009-04-23 F. Hoffmann-La Roche Ag Cis-2,4,5- triphenyl-imidazoline und ihre verwendung bei der behandlung von tumoren
US8146941B2 (en) * 2002-05-17 2012-04-03 Steins Karl M Collapsible trailer
WO2003106384A2 (en) 2002-06-01 2003-12-24 Johns Hopkins University Novel boronic chalcone derivatives and uses thereof
WO2004043371A2 (en) 2002-11-08 2004-05-27 Irm Llc Methods and compositions for modulating p53 transcription factor
US20050227932A1 (en) 2002-11-13 2005-10-13 Tianbao Lu Combinational therapy involving a small molecule inhibitor of the MDM2: p53 interaction
CA2514374A1 (en) 2003-02-13 2004-09-02 Government Of The United States Of America, As Represented By The Secret Ary, Department Of Health And Human Services Deazaflavin compounds and methods of use thereof
US6916833B2 (en) 2003-03-13 2005-07-12 Hoffmann-La Roche Inc. Substituted piperidines
US7425638B2 (en) 2003-06-17 2008-09-16 Hoffmann-La Roche Inc. Cis-imidazolines
US7132421B2 (en) 2003-06-17 2006-11-07 Hoffmann-La Roche Inc. CIS-imidazoles
US7829742B2 (en) 2003-12-22 2010-11-09 Johns Hopkins University Boronic acid aryl analogs
WO2005097820A1 (en) 2004-04-06 2005-10-20 Korea Research Institute Of Bioscience And Biotechnology Peptides for inhibiting mdm2 function
KR20080027969A (ko) 2004-05-18 2008-03-28 에프. 호프만-라 로슈 아게 신규 cis-이미다졸린
GB0419481D0 (en) 2004-09-02 2004-10-06 Cancer Rec Tech Ltd Isoindolin-1-one derivatives
ES2349358T3 (es) 2004-09-22 2010-12-30 Janssen Pharmaceutica Nv Inhibidores de la interacción entre mdm2 y p53.
NZ561215A (en) 2005-02-22 2010-12-24 Univ Michigan Small molecule inhibitors of MDM2 and uses thereof
KR100944301B1 (ko) 2005-02-22 2010-02-24 더 리젠츠 오브 더 유니버시티 오브 미시간 Mdm2의 소분자 억제제 및 이의 용도
KR101139263B1 (ko) 2005-03-16 2012-05-16 에프. 호프만-라 로슈 아게 시스-2,4,5-트리아릴-이미다졸린 및 항암 약제로서의그의 용도
WO2006129623A1 (ja) 2005-05-30 2006-12-07 Mitsubishi Tanabe Pharma Corporation チエノトリアゾロジアゼピン化合物及びその医薬としての用途
US7576082B2 (en) 2005-06-24 2009-08-18 Hoffman-La Roche Inc. Oxindole derivatives
US7495007B2 (en) 2006-03-13 2009-02-24 Hoffmann-La Roche Inc. Spiroindolinone derivatives
CA2644643C (en) 2006-03-22 2015-05-19 Janssen Pharmaceutica N.V. Inhibitors of the interaction between mdm2 and p53
AU2007297823B2 (en) 2006-08-30 2012-04-19 The Regents Of The University Of Michigan New small molecule inhibitors of MDM2 and the uses thereof
US7737174B2 (en) 2006-08-30 2010-06-15 The Regents Of The University Of Michigan Indole inhibitors of MDM2 and the uses thereof
US7638548B2 (en) 2006-11-09 2009-12-29 Hoffmann-La Roche Inc. Spiroindolinone derivatives
BRPI0720546A2 (pt) 2006-12-14 2015-06-23 Daiichi Sankyo Co Ltd Composto, inibidor, medicamento, agente antitumor, composição farmacêutica, método para tratar câncer, e, uso do composto
DK2118074T3 (en) 2007-02-01 2014-03-10 Resverlogix Corp Compounds for the prevention and treatment of cardiovascular diseases
WO2008106507A2 (en) 2007-02-27 2008-09-04 University Of South Florida Mdm2/mdmx inhibitor peptide
CA2682483A1 (en) 2007-03-29 2008-10-09 Novartis Ag 3-imidazolyl-indoles for the treatment of proliferative diseases
US7625895B2 (en) 2007-04-12 2009-12-01 Hoffmann-Le Roche Inc. Diphenyl-dihydro-imidazopyridinones
WO2008130614A2 (en) 2007-04-20 2008-10-30 University Of Pittsburg-Of The Commonwealth System Of Higher Education Selective and dual-action p53/mdm2/mdm4 antagonists
US7553833B2 (en) 2007-05-17 2009-06-30 Hoffmann-La Roche Inc. 3,3-spiroindolinone derivatives
CA2694646C (en) * 2007-07-30 2017-09-05 Ardea Biosciences, Inc. Combinations of mek inhibitors and raf kinase inhibitors and uses thereof
ES2382701T3 (es) 2007-09-21 2012-06-12 Janssen Pharmaceutica, N.V. Inhibidores de la interacción entre MDM2 y p53
CN101910182B (zh) 2007-12-28 2013-07-17 田边三菱制药株式会社 抗癌剂
EP2298778A4 (en) 2008-06-12 2011-10-05 Daiichi Sankyo Co Ltd IMIDAZOTHIAZOL DERIVATIVE WITH 4,7-DIAZASPIRO [2.5] OCTAN RING STRUCTURE
GB0811643D0 (en) 2008-06-25 2008-07-30 Cancer Rec Tech Ltd New therapeutic agents
ES2532402T3 (es) 2008-06-26 2015-03-26 Resverlogix Corporation Métodos de preparación de derivados de quinazolinona
CN107252429B (zh) 2009-04-22 2023-06-16 雷斯韦洛吉克斯公司 新抗炎剂
DE102009051823A1 (de) 2009-11-04 2011-05-05 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. Einkristallines Schweißen von direktional verfestigten Werkstoffen
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
EP3050885B1 (en) 2009-11-05 2017-10-18 GlaxoSmithKline LLC Benzodiazepine bromodomain inhibitor
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
UA107814C2 (uk) * 2009-11-12 2015-02-25 Дзе Ріджентс Оф Дзе Юніверсіті Оф Мічіган Спірооксіндольні антагоністи мdм2
US20110118283A1 (en) 2009-11-17 2011-05-19 Qingjie Ding Substituted Pyrrolidine-2-Carboxamides
US8088815B2 (en) * 2009-12-02 2012-01-03 Hoffman-La Roche Inc. Spiroindolinone pyrrolidines
CA2799403C (en) 2010-05-14 2020-01-21 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
HUE031073T2 (en) 2010-05-14 2017-06-28 Dana Farber Cancer Inst Inc Thieno triazolo-diazepine compounds for the treatment of neoplasia
CN103119160B (zh) 2010-05-14 2016-06-01 达那-法伯癌症研究所 用于调节代谢的组合物和方法
JO2998B1 (ar) * 2010-06-04 2016-09-05 Amgen Inc مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان
WO2011161031A1 (en) 2010-06-22 2011-12-29 Glaxosmithkline Llc Benzotriazolodiazepine compounds inhibitors of bromodomains
TWI535723B (zh) 2010-11-12 2016-06-01 密西根大學董事會 螺-吲哚酮mdm2拮抗劑
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
AU2012220620A1 (en) 2011-02-23 2013-10-03 Icahn School Of Medicine At Mount Sinai Inhibitors of bromodomains as modulators of gene expression
KR101779644B1 (ko) 2011-03-10 2017-09-18 다이이찌 산쿄 가부시키가이샤 디스피로피롤리딘 유도체
EP2705039B1 (en) 2011-05-04 2017-07-26 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
JP2014513699A (ja) * 2011-05-11 2014-06-05 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン スピロ−オキシインドールmdm2アンタゴニスト
EP2721031B1 (en) 2011-06-17 2016-01-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201114103D0 (en) 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2013033270A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bromodomain ligands capable of dimerizing in an aqueous solution, and methods of using same
DE102011082013A1 (de) 2011-09-01 2013-03-07 Bayer Pharma AG 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
US20130245089A1 (en) 2012-03-19 2013-09-19 Hoffmann-La Roche Inc. Method for administration
US20140079636A1 (en) * 2012-04-16 2014-03-20 Dinesh U. Chimmanamada Targeted therapeutics
US20130281399A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
HK1206744A1 (en) 2012-04-20 2016-01-15 Abbvie Inc. Isoindolone derivatives
MX2014015156A (es) 2012-06-12 2015-08-06 Abbvie Inc Derivados de piridinona y piridazinona.
AU2014223547B2 (en) * 2013-02-28 2017-11-16 Amgen Inc. A benzoic acid derivative MDM2 inhibitor for the treatment of cancer
CN105377851B (zh) * 2013-03-11 2018-07-20 密执安州立大学董事会 Bet布罗莫结构域抑制剂和使用这些抑制剂的治疗方法
WO2015131005A1 (en) * 2014-02-28 2015-09-03 The Regents Of The University Of Michigan 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors
EP3129380B1 (en) 2014-04-11 2018-11-28 Boehringer Ingelheim International Gmbh Spiro[3h-indole-3,2'-pyrrolidin]-2(1h)-one derivatives and their use as mdm2-p53 inhibitors
KR20250127179A (ko) 2014-04-14 2025-08-26 아비나스 오퍼레이션스, 인코포레이티드 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법
US20160058872A1 (en) 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
MX373045B (es) * 2014-04-17 2020-05-26 Univ Michigan Regents Inhibidores de mdm2 y metodos terapeuticos que utilizan el mismo.
US10576064B2 (en) 2014-07-03 2020-03-03 Boehringer Ingelheim International Gmbh Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-P53 inhibitors
JP6625638B2 (ja) * 2014-08-18 2019-12-25 ハドソン・バイオファーマ・インコーポレイテッド Mdm2阻害薬としてのスピロピロリジン
US20160052938A1 (en) 2014-08-21 2016-02-25 Boehringer Ingelheim International Gmbh Spiro[3h-indole-3,2'-pyrrolidin]-2(1h)-one compounds and derivatives as mdm2-p53 inhibitors
EP3262045A1 (en) * 2015-02-27 2018-01-03 The Regents of The University of Michigan 9h-pyrimido [4,5-b]indoles as bet bromodomain inhibitors
US10772962B2 (en) * 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
KR102387316B1 (ko) * 2016-04-06 2022-04-15 더 리젠츠 오브 더 유니버시티 오브 미시간 Mdm2 단백질 분해제
WO2017176958A1 (en) * 2016-04-06 2017-10-12 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
MX2021003999A (es) * 2018-10-08 2021-06-23 Univ Michigan Regents Moleculas de bajo peso molecular degradadoras de la proteina mdm2.

Also Published As

Publication number Publication date
EP3440066B1 (en) 2022-11-30
US20190127387A1 (en) 2019-05-02
IL262103A (en) 2018-11-29
AU2017246452C1 (en) 2021-06-03
JP7037500B2 (ja) 2022-03-16
US20220411432A1 (en) 2022-12-29
JP2022078201A (ja) 2022-05-24
UA123786C2 (uk) 2021-06-02
CN113788818A (zh) 2021-12-14
WO2017176957A8 (en) 2018-11-08
RU2743432C2 (ru) 2021-02-18
RU2018138735A (ru) 2020-05-12
AU2017246452A1 (en) 2018-11-08
WO2017176957A1 (en) 2017-10-12
RU2018138735A3 (es) 2020-05-12
CN109415336A (zh) 2019-03-01
IL262103B (en) 2021-05-31
US11192898B2 (en) 2021-12-07
SG11201808728QA (en) 2018-11-29
BR112018070549A2 (pt) 2019-02-12
NZ747251A (en) 2024-05-31
KR102387316B1 (ko) 2022-04-15
EP3440066A1 (en) 2019-02-13
JP2019510798A (ja) 2019-04-18
CA3020275A1 (en) 2017-10-12
KR20180132125A (ko) 2018-12-11
ZA201806968B (en) 2020-02-26
RU2021102253A (ru) 2021-03-03
CN109415336B (zh) 2023-08-29
AU2017246452B2 (en) 2021-02-25

Similar Documents

Publication Publication Date Title
MX2018012174A (es) Degradantes de proteina homologa de proteina murina de cromosoma diminuto doble (mdm2).
PH12019501321B1 (en) Use of pyrazolopyrimidine derivatives for the treatment of pi3k-delta related disorders
MX384905B (es) Degradadores de proteínas de bromodominio y dominioextraterminal (bet).
PH12018502535A1 (en) Substituted carbonucleoside derivatives useful as anticancer agents
PH12016502504A1 (en) Mnk inhibitors and methods related thereto
TW201613872A (en) IRAK4 inhibiting agents
MY202022A (en) Pyrrolotriazine compounds as tam inhibitors
MY199705A (en) Heterocyclic compounds as immunomodulators
MX2018006207A (es) Compuestos heterociclicos como inmunomoduladores.
MD20170016A2 (ro) Compuşi aminopirimidinici ca inhibitori JAK
TN2019000210A1 (en) Antitumoral compounds
PH12015502611A1 (en) Heterocyclic compounds as hedgehog signaling pathway inhibitors
PH12015501588A1 (en) Compounds and methods for treating bacterial infections
PH12015501038A1 (en) Inhibitors of iap
AU2015299431B2 (en) Pyrrolidinone derivatives as metAP-2 inhibitors
MY202127A (en) Pyridazine derivatives for use in the prevention or treatment of an ataxic disorder
PH12017500459A1 (en) Azetidinyloxyphenylpyrrolidine compounds
JOP20190163B1 (ar) منشط nrf2
ZA201606471B (en) Antimitotic amides for the treatment of cancer and proliferative disorders
PH12016502480A1 (en) Compounds, pharmaceutical composition and their use in treating neurodegenerative diseases
WO2019040104A3 (en) COMPOUNDS, RELATED SALTS AND METHODS OF TREATING DISEASES
HK1245768A1 (en) Fused 1,3-azole derivatives useful for the treatment of proliferative diseases