PE20231204A1 - Metodos para fabricar un compuesto bifuncional, formas ultrapuras del compuesto bifuncional y formas de dosificacion que comprenden el mismo - Google Patents

Metodos para fabricar un compuesto bifuncional, formas ultrapuras del compuesto bifuncional y formas de dosificacion que comprenden el mismo

Info

Publication number
PE20231204A1
PE20231204A1 PE2022002608A PE2022002608A PE20231204A1 PE 20231204 A1 PE20231204 A1 PE 20231204A1 PE 2022002608 A PE2022002608 A PE 2022002608A PE 2022002608 A PE2022002608 A PE 2022002608A PE 20231204 A1 PE20231204 A1 PE 20231204A1
Authority
PE
Peru
Prior art keywords
bifunctional compound
forms
ultrapure
manufacturing
methods
Prior art date
Application number
PE2022002608A
Other languages
English (en)
Spanish (es)
Inventor
Hanqing Dong
Robert J Duguid
Casey Keith Jager
Aditya Mohan Kaushal
Samuel Elliott Kennedy
Miranda Annell Neeser
Maxwell Marco Reeve
Joseph P Reo
Mohammad Mehdi Zahedi
Venkata A Kattuboina
Laura E N Allan
Chungpin Herman Chen
John A Grosso
Iii Royal J Haskell
Rhys Lloyd
Hayley Reece
Jerod Robertson
Yuping Qiu
Original Assignee
Arvinas Operations Inc
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 Arvinas Operations Inc filed Critical Arvinas Operations Inc
Publication of PE20231204A1 publication Critical patent/PE20231204A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/16—Halogen atoms or nitro radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Biophysics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
PE2022002608A 2020-05-09 2021-05-06 Metodos para fabricar un compuesto bifuncional, formas ultrapuras del compuesto bifuncional y formas de dosificacion que comprenden el mismo PE20231204A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US202063022475P 2020-05-09 2020-05-09
US202163149143P 2021-02-12 2021-02-12
US202163177378P 2021-04-20 2021-04-20
PCT/US2021/031091 WO2021231174A1 (en) 2020-05-09 2021-05-06 Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same

Publications (1)

Publication Number Publication Date
PE20231204A1 true PE20231204A1 (es) 2023-08-17

Family

ID=76305987

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022002608A PE20231204A1 (es) 2020-05-09 2021-05-06 Metodos para fabricar un compuesto bifuncional, formas ultrapuras del compuesto bifuncional y formas de dosificacion que comprenden el mismo

Country Status (17)

Country Link
US (2) US12043612B2 (enExample)
EP (1) EP4146642A1 (enExample)
JP (1) JP2023524599A (enExample)
KR (1) KR20230015933A (enExample)
CN (1) CN115996918A (enExample)
AU (1) AU2021273458A1 (enExample)
BR (1) BR112022022753A2 (enExample)
CA (1) CA3181782A1 (enExample)
CL (1) CL2023000074A1 (enExample)
CO (1) CO2022017700A2 (enExample)
CR (1) CR20220630A (enExample)
EC (1) ECSP22086223A (enExample)
IL (1) IL297762A (enExample)
MX (1) MX2022014071A (enExample)
PE (1) PE20231204A1 (enExample)
TW (1) TW202208345A (enExample)
WO (1) WO2021231174A1 (enExample)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
LT3660004T (lt) * 2016-10-11 2023-06-12 Arvinas Operations, Inc. Junginiai ir metodai, skirti tikslinei androgeno receptoriaus degradacijai
US12310975B2 (en) 2019-10-17 2025-05-27 Arvinas Operations, Inc. Modulators of BCL6 proteolysis and associated methods of use
AU2021342287A1 (en) 2020-09-14 2023-04-13 Arvinas Operations, Inc. Crystalline forms of a compound for the targeted degradation of estrogen receptor
WO2023025268A1 (zh) * 2021-08-27 2023-03-02 苏州晶云药物科技股份有限公司 哒嗪甲酰胺类化合物的晶型及其制备方法
WO2023143427A1 (zh) * 2022-01-27 2023-08-03 杭州领业医药科技有限公司 Arv-110的晶型及其制备方法和用途
WO2023205481A1 (en) 2022-04-21 2023-10-26 Arvinas Operations, Inc. A combination for use in treating prostate cancer comprising arv-100 and abiraterone
WO2024201244A1 (en) 2023-03-24 2024-10-03 Assia Chemical Industries Ltd. Solid state forms of bavdegalutamide and process for preparation thereof
CN116282055B (zh) * 2023-04-04 2024-10-15 昆明理工大学 一种利用酸淬提纯和改性无定形硼粉的方法
CN116444486B (zh) * 2023-04-14 2024-09-03 烟台大学 一种芳基氧环己基化合物及其制备方法
CN116585319B (zh) * 2023-04-14 2024-11-12 烟台大学 芳基氧环己基化合物制备抗前列腺癌药物的应用
WO2024220926A1 (en) 2023-04-21 2024-10-24 Arvinas Operations, Inc. Use of an androgen receptor degrader protac for the treatment of prostate cancer
WO2024233696A1 (en) 2023-05-09 2024-11-14 Arvinas Operations, Inc. Bavdegalutamide for treating prostate cancer without ar l702h mutation
WO2025122895A1 (en) 2023-12-08 2025-06-12 Arvinas Operations, Inc. Use of androgen receptor degrader for the treatment of spinal and bulbar muscular atrophy
CN118955474A (zh) * 2024-07-29 2024-11-15 浙江爱索拓标记医药科技有限公司 一种放射性同位素碳-14标记的巴德卡鲁胺及其制备方法和应用

Family Cites Families (134)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10584A (en) 1854-02-28 Bank-lock
US101A (en) 1836-12-06 Method of jcakibtg and furling iw sails fob ships
PT2177517E (pt) 1996-07-24 2011-11-10 Celgene Corp 2-(2,6-dioxopiperidin-3-il)-ftalimida amino-substituída para redução dos níveis de tnf-alfa
WO1998051702A1 (en) 1997-05-14 1998-11-19 Sloan-Kettering Institute For Cancer Research Methods and compositions for destruction of selected proteins
WO1999031061A1 (en) 1997-12-17 1999-06-24 Merck & Co., Inc. Integrin receptor antagonists
US6306663B1 (en) 1999-02-12 2001-10-23 Proteinex, Inc. Controlling protein levels in eucaryotic organisms
EP1176959B1 (en) 1999-05-05 2006-03-08 Merck & Co., Inc. Novel prolines as antimicrobial agents
JP2004509072A (ja) 2000-06-28 2004-03-25 ブリストル−マイヤーズ　スクイブ　カンパニー 選択的アンドロゲン受容体モジュレーター並びにその同定、設計及び使用方法
EP1322750A4 (en) 2000-09-08 2004-09-29 California Inst Of Techn PROTEOLYSIS TARGET DRUG TARGET MEDICINE
US7208157B2 (en) 2000-09-08 2007-04-24 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
RU2298554C2 (ru) 2000-09-19 2007-05-10 Бристол-Маерс Сквибб Компани Конденсированные гетероциклические сукцинимидные соединения
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
WO2002066512A1 (en) 2001-02-16 2002-08-29 E.I. Dupont De Nemours And Company Angiogenesis-inhibitory tripeptides, compositions and their methods of use
HN2002000136A (es) 2001-06-11 2003-07-31 Basf Ag Inhibidores de la proteasa del virus hiv, compuestos que contienen a los mismos, sus usos farmaceuticos y los materiales para su sintesis
PT1405621E (pt) 2001-06-20 2011-05-31 Takeda Pharmaceutical Processo de prepara??o de comprimidos
NZ531294A (en) 2001-08-06 2005-11-25 Childrens Medical Center Synthesis and anti-tumor activity of nitrogen substituted thalidomide analogs
US7030141B2 (en) 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
WO2004020434A1 (ja) 2002-08-30 2004-03-11 Eisai Co., Ltd. 含窒素芳香環誘導体
CA2570047C (en) 2004-07-08 2010-09-28 Warner-Lambert Company Llc 4-cycloalkoxy benzonitriles as androgen modulators
CN100383139C (zh) 2005-04-07 2008-04-23 天津和美生物技术有限公司 可抑制细胞释放肿瘤坏死因子的哌啶-2，6-二酮衍生物
WO2006113942A2 (en) 2005-04-20 2006-10-26 Schering Corporation Method of inhibiting cathepsin activity
ES2434946T3 (es) 2005-08-31 2013-12-18 Celgene Corporation Compuestos de isoindol imida y composiciones que los comprenden y métodos para usarlo
EP1994027A2 (en) 2006-03-03 2008-11-26 Novartis AG N-formyl hydroxylamine compounds
NZ572374A (en) 2006-03-29 2011-12-22 Univ California Diarylthiohydantoin compounds
JP2009544620A (ja) 2006-07-20 2009-12-17 リガンド・ファーマシューティカルズ・インコーポレイテッド 自己免疫疾患及び炎症のためのプロリン尿素ｃｃｒ１アンタゴニスト
NZ575061A (en) 2006-08-30 2011-10-28 Celgene Corp 5-substituted isoindoline compounds
US8877780B2 (en) 2006-08-30 2014-11-04 Celgene Corporation 5-substituted isoindoline compounds
RU2448101C2 (ru) 2006-08-30 2012-04-20 Селджин Корпорейшн 5-замещенные изоиндолиновые соединения
ES2403546T3 (es) 2006-11-03 2013-05-20 Pharmacyclics, Inc. Sonda de actividad de la tirosina-cinasa de Bruton y procedimiento de utilización
CN101808693A (zh) 2007-07-25 2010-08-18 百时美施贵宝公司 三嗪激酶抑制剂
KR20100051808A (ko) 2007-07-31 2010-05-18 앤드로사이언스 코포레이션 안드로겐 수용체 분해 강화제를 포함한 조성물 및 탈모와 피부질환의 예방 또는 치료 방법
EP2358697B1 (en) 2008-10-29 2015-10-21 Celgene Corporation Isoindoline compounds for use in the treatment of cancer.
MX2011009053A (es) 2009-03-09 2012-04-02 Spi Pharma Inc Excipientes de compresion directa con alta capacidad de compactacion y durables y sistemas de excipiente.
US8614201B2 (en) 2009-06-05 2013-12-24 Janssen Pharmaceutica Nv Heterocyclic amides as modulators of TRPA1
BR112012000867A2 (pt) 2009-07-13 2019-09-24 Harvard College "polipeptídeos bifuncional costurado e uso do mesmo"
AR078793A1 (es) 2009-10-27 2011-12-07 Orion Corp Derivados de carboxamidas no esteroidales y acil hidrazona moduladores de receptores androgenicos de tejido selectivo (sarm), composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del cancer de prostata entre otros
SG10201501062SA (en) 2010-02-11 2015-04-29 Celgene Corp Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
EP2588129A4 (en) 2010-06-30 2014-07-09 Univ Brandeis ON SMALL MOLECULES TARGETED PROTEIN REMOVAL
WO2012040527A2 (en) 2010-09-24 2012-03-29 The Regents Of The University Of Michigan Deubiquitinase inhibitors and methods for use of the same
AU2011338615B2 (en) 2010-12-07 2017-07-27 Yale University Small-molecule hydrophobic tagging of fusion proteins and induced degradation of same
US20140243282A1 (en) 2010-12-31 2014-08-28 Satish Reddy Kallam Methods and compositions for designing novel conjugate therapeutics
KR101958177B1 (ko) 2011-04-21 2019-03-15 오리온 코포레이션 안드로겐 수용체 조절성 카복스아미드
EP3096142A3 (en) 2011-04-29 2017-03-08 Celgene Corporation Methods for the treatment of cancer and inflammatory diseases using cereblon as a predictor
WO2013106646A2 (en) 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
JP2015508414A (ja) 2012-01-12 2015-03-19 イエール ユニバーシティ Ｅ３ユビキチンリガーゼによる標的タンパク質および他のポリペプチドの分解増強のための化合物および方法
US20140079636A1 (en) 2012-04-16 2014-03-20 Dinesh U. Chimmanamada Targeted therapeutics
US20150119435A1 (en) 2012-05-11 2015-04-30 Yale University Compounds useful for promoting protein degradation and methods using same
WO2013184572A1 (en) * 2012-06-04 2013-12-12 Pharmacyclics, Inc. Crystalline forms of a bruton's tyrosine kinase inhibitor
US9388126B2 (en) 2012-07-19 2016-07-12 Drexel University Sigma receptor ligands and methods of modulating cellular protein homeostasis using same
GB201311910D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel Compounds
NL2011274C2 (en) 2013-08-06 2015-02-09 Illumicare Ip B V 51 Groundbreaking platform technology for specific binding to necrotic cells.
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
EP3035938B1 (en) 2013-09-10 2020-08-19 Madrigal Pharmaceuticals, Inc. Targeted therapeutics
WO2015114314A1 (en) 2014-01-28 2015-08-06 Cipla Limited Pharmaceutical composition comprising abiraterone
CN106456795A (zh) 2014-03-03 2017-02-22 辛塔医药品有限公司 靶向治疗学
US20160058872A1 (en) 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
CN119591582A (zh) 2014-04-14 2025-03-11 阿尔维纳斯运营股份有限公司 基于酰亚胺的蛋白水解调节剂和相关使用方法
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
US20160022642A1 (en) 2014-07-25 2016-01-28 Yale University Compounds Useful for Promoting Protein Degradation and Methods Using Same
US10071164B2 (en) 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
HUE046869T2 (hu) 2014-11-21 2020-04-28 Biohaven Therapeutics Ltd Riluzol szublingvális formulációja
CN107406424B (zh) 2014-12-18 2020-08-25 豪夫迈·罗氏有限公司 雌激素受体调节剂及其用途
JP6815318B2 (ja) 2014-12-23 2021-01-20 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 二官能性分子によって標的化タンパク質分解を誘導する方法
US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
HK1245791A1 (zh) 2015-01-20 2018-08-31 阿尔维纳斯运营股份有限公司 用於雄激素受体的靶向降解的化合物和方法
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
GB201504314D0 (en) 2015-03-13 2015-04-29 Univ Dundee Small molecules
JP7269731B2 (ja) 2015-03-18 2023-05-09 アルビナス・オペレーションズ・インコーポレイテッド 標的タンパク質の分解向上のための化合物および方法
GB201506872D0 (en) 2015-04-22 2015-06-03 Ge Oil & Gas Uk Ltd Novel compounds
GB201506871D0 (en) 2015-04-22 2015-06-03 Glaxosmithkline Ip Dev Ltd Novel compounds
KR20240119196A (ko) 2015-06-04 2024-08-06 아비나스 오퍼레이션스, 인코포레이티드 단백질분해의 이미드계 조절인자 및 관련된 이용 방법
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
WO2017007612A1 (en) 2015-07-07 2017-01-12 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
CN108137507A (zh) 2015-07-10 2018-06-08 阿尔维纳斯股份有限公司 基于mdm2的蛋白水解调节剂和相关的使用方法
CA2988436A1 (en) 2015-07-13 2017-01-19 Arvinas, Inc. Alanine-based modulators of proteolysis and associated methods of use
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
AU2016349781A1 (en) 2015-11-02 2018-05-10 Yale University Proteolysis targeting chimera compounds and methods of preparing and using same
KR101859074B1 (ko) 2016-01-28 2018-05-18 이화여자대학교 산학협력단 신규한 글라이신 아미드 화합물 또는 이의 약학적으로 허용 가능한 염, 이의 제조방법 및 이를 포함하는 소듐 채널 활성 관련 질환의 예방 또는 치료용 약학적 조성물
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
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
WO2017185031A1 (en) 2016-04-22 2017-10-26 Dana-Farber Cancer Institute, Inc. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use
JP6921114B2 (ja) 2016-04-22 2021-08-18 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド サイクリン依存性キナーゼ８（ｃｄｋ８）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｃｄｋ８の分解および使用法
WO2017197056A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Bromodomain targeting degronimers for target protein degradation
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
CN109641874A (zh) 2016-05-10 2019-04-16 C4医药公司 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
ES2975558T3 (es) 2016-09-15 2024-07-09 Arvinas Inc Derivados de indol como degradantes de receptor de estrógeno
LT3660004T (lt) 2016-10-11 2023-06-12 Arvinas Operations, Inc. Junginiai ir metodai, skirti tikslinei androgeno receptoriaus degradacijai
WO2018098280A1 (en) 2016-11-22 2018-05-31 Dana-Farber Cancer Institute, Inc. Degradation of protein kinases by conjugation of protein kinase inhibitors with e3 ligase ligand and methods of use
FR3064633B1 (fr) 2017-03-28 2019-04-12 Ecole Polytechnique Nouveaux composes de type dithiospirocetals et leur utilisation
AU2018261331C1 (en) 2017-05-01 2022-08-04 Spg Therapeutics, Inc. Tripartite androgen receptor eliminators, methods and uses thereof
KR102119465B1 (ko) 2017-09-20 2020-06-08 (주)아모레퍼시픽 트리메톡시 페닐 화합물 및 그를 포함하는 발모 또는 육모 촉진용 조성물
CN110746399B (zh) 2018-07-23 2022-04-22 上海美志医药科技有限公司 具有降解雄激素受体活性的化合物
WO2020047487A1 (en) 2018-08-31 2020-03-05 The Regents Of The University Of California Methods for treating cancer with rorgamma inhibitors and statins
CN119219606A (zh) 2018-12-19 2024-12-31 细胞基因公司 经取代的3-((3-氨基苯基)氨基)哌啶-2，6-二酮化合物、其组合物及使用它们的治疗方法
BR112021012186A2 (pt) 2018-12-19 2021-08-31 Celgene Corporation Compostos de 3-((3-aminofenil)amino)piperidina-2,6-diona substituídos, composições dos mesmos e métodos de tratamento com os mesmos
CN120698983A (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
WO2020160295A1 (en) 2019-01-30 2020-08-06 Montelino Therapeutics, Llc Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
KR20220004978A (ko) 2019-03-28 2022-01-12 에싸 파마 아이엔씨. 단백질 분해 표적 키메라 리간드로서 사용하기 위한 안드로겐 수용체 조절제 및 방법
US12109179B2 (en) 2019-03-28 2024-10-08 Essa Pharma Inc. Pharmaceutical compositions and combinations comprising inhibitors of the androgen receptor and uses thereof
US12331061B2 (en) 2019-04-18 2025-06-17 Accutar Biotechnology Inc. Compounds having BET, estrogen receptor, and androgen receptor degradation activity and uses thereof
KR20220004100A (ko) 2019-04-18 2022-01-11 하이노바 파마슈티컬스 인코포레이티드 안드로겐 수용체를 표적 분해하는 이중 기능성의 키메라 헤테로 고리 화합물 및 이의 용도
JP2022533147A (ja) 2019-05-17 2022-07-21 ヒノバ ファーマシューティカルズ インコーポレイテッド 芳香族アミン類のａｒ及びｂｅｔを標的とするタンパク質分解キメラ化合物及び使用
CN115023267A (zh) 2019-09-19 2022-09-06 密歇根大学董事会 螺环雄激素受体蛋白质降解剂
US11420956B2 (en) 2019-09-23 2022-08-23 Accutar Biotechnology Inc. Ureas having Androgen Receptor degradation activity and uses thereof
US10836749B1 (en) 2019-09-23 2020-11-17 Accutar Biotechnology Inc. Substituted quinoline-8-carbonitrile derivatives having androgen receptor degradation activity and uses thereof
US11535606B2 (en) 2019-09-23 2022-12-27 Accutar Biotechnology Inc. Substituted quinoline-8-carbonitrile derivatives with androgen receptor degradation activity and uses thereof
CN115135313A (zh) 2019-10-22 2022-09-30 阿维纳斯企业公司 治疗前列腺癌的方法
EP4083020A4 (en) 2019-12-23 2024-01-24 Shanghai Jemincare Pharmaceuticals Co., Ltd. PREPARATION METHOD AND APPLICATION OF PROTEIN DEGRADATION AGENT COMPOUND
CN113582974B (zh) 2020-04-30 2022-05-17 江西济民可信集团有限公司 一类作为蛋白降解剂的化合物及其制备方法和医药用途
US20210353621A1 (en) 2020-05-12 2021-11-18 Arvinas Operations, Inc. Methods of treating prostate cancer
EP4166550A4 (en) 2020-06-12 2024-08-07 Shanghai Jemincare Pharmaceuticals Co., Ltd. PHTHALAZINONE COMPOUND, ITS PREPARATION PROCESS AND ITS MEDICAL USE
CN115835866B (zh) 2020-06-24 2025-05-02 新基公司 Cereblon结合化合物、其组合物及其用于治疗的方法
WO2021262815A1 (en) 2020-06-24 2021-12-30 Celgene Corporation Cereblon binding compounds, compositions thereof, and methods of treatment therewith
CN115955979B (zh) 2020-06-24 2025-12-05 新基公司 Cereblon结合化合物、其组合物及其用于治疗的方法
CN117327059A (zh) 2020-07-08 2024-01-02 北京泰德制药股份有限公司 抑制并诱导蛋白降解的化合物
WO2022048605A1 (zh) 2020-09-04 2022-03-10 南昌奥瑞药业有限公司 一种杂环化合物、其制备方法、中间体、组合物以及应用
CN114163444B (zh) 2020-09-11 2023-07-14 江苏恒瑞医药股份有限公司 一种用于雄激素受体蛋白靶向降解的嵌合体化合物、其制备方法及其在医药上的应用
MX2023004545A (es) 2020-10-21 2023-07-05 Arvinas Operations Inc Compuestos y métodos para la degradación dirigida de la proteína del receptor de andrógenos.
US20220144809A1 (en) 2020-11-06 2022-05-12 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor and associated methods of use
WO2022111526A1 (zh) 2020-11-25 2022-06-02 四川海思科制药有限公司 一种苯环衍生物及其组合物和药学上的应用
US20220184078A1 (en) 2020-12-11 2022-06-16 Arvinas Operations, Inc. Methods of treating prostate cancer
EP4023649A1 (en) 2020-12-30 2022-07-06 Industrial Technology Research Institute Androgen receptor binding bifunctional molecules
CN114853846A (zh) 2021-02-04 2022-08-05 苏州国匡医药科技有限公司 一种雄激素受体降解剂及其应用
US20240190874A1 (en) 2021-03-03 2024-06-13 The Regents Of The University Of Michigan Small molecule degraders of androgen receptor
US12016847B2 (en) 2021-03-12 2024-06-25 Bristol-Myers Squibb Company Methods of treating prostate cancer
CN116891457A (zh) 2022-04-11 2023-10-17 江苏恒瑞医药股份有限公司 一种用于雄激素受体蛋白靶向降解的嵌合体化合物、其制备方法及其在医药上的应用
WO2023205481A1 (en) 2022-04-21 2023-10-26 Arvinas Operations, Inc. A combination for use in treating prostate cancer comprising arv-100 and abiraterone
CN117065033A (zh) 2022-05-17 2023-11-17 海创药业股份有限公司 一种治疗三阴乳腺癌的联合用药物
CN117024390B (zh) 2023-08-09 2025-11-11 中国海洋大学 一种Cdc20小分子配体化合物及其降解剂的应用

Also Published As

Publication number Publication date
BR112022022753A2 (pt) 2023-02-14
US12043612B2 (en) 2024-07-23
AU2021273458A1 (en) 2022-12-01
CN115996918A (zh) 2023-04-21
ECSP22086223A (es) 2022-12-30
CR20220630A (es) 2023-01-23
WO2021231174A1 (en) 2021-11-18
IL297762A (en) 2022-12-01
US20240409529A1 (en) 2024-12-12
US20230012321A1 (en) 2023-01-12
EP4146642A1 (en) 2023-03-15
CA3181782A1 (en) 2021-11-18
CO2022017700A2 (es) 2022-12-20
CL2023000074A1 (es) 2023-07-07
TW202208345A (zh) 2022-03-01
KR20230015933A (ko) 2023-01-31
JP2023524599A (ja) 2023-06-12
MX2022014071A (es) 2023-01-30

Similar Documents

Publication Publication Date Title
CL2024000373A1 (es) Compuesto inductor de la degradación de plk1 novedoso
AR072777A1 (es) Formas solidas de clorhidrato de bendamustina
AR063347A1 (es) Formas cristalinas de docetaxel y proceso para su preparacion
AR112276A1 (es) Polimorfos de 5-fluoro-4-imino-3-metil-1-tosil-3,4-dihidropirimidin-2-ona
MX2016008677A (es) Proceso para formar un producto de pelicula formado con multiples capas.
CR20110457A (es) Nueva forma cristalina vi de la agomelatina, preparacion y uso de la misma
AR096046A1 (es) Derivados de 2,2-difluoropropanamida de metil bardoxolona, formas polimórficas y métodos de uso
USD787483S1 (en) Antenna design
AR121018A1 (es) Forma en estado sólido de piroxasulfona
CL2018002519A1 (es) Procedimiento para fabricar una lechada de cal apagada de gran finura y lechada de cal de gran finura obtenida con agua de proceso
MY197793A (en) Solar cells and methods of making the same
CO2022000748A2 (es) Compuesto de pirazolopirimidina, método de preparación para el mismo y sus aplicaciones
EA202092393A1 (ru) Кристаллическое соединение оксазола
BR112015023351A2 (pt) forma cristalina de sovaprevir, composição farmacêutica, e, método para tratar um distúrbio
MX2017005439A (es) Polvo para rocío térmico, película de revestimiento de rocío térmico, película y rodillo de revestimiento en baño metálico fundido.
AR112842A1 (es) Cristal de pirazina
AR125556A1 (es) Formulación para el cuidado de telas
AR107441A1 (es) Forma cristalina de cobicistat
AR099082A1 (es) Formas sólidas de tenofovir
ES2489467T3 (es) Polimorfo novedoso del clorhidrato del éster (6-dimetilaminometil-2-naftalenílico) del ácido (4-hidroxicarbamoilfenil)-carbámico
AR102804A1 (es) Formas sólidas de un modulador del canal iónico
EP3865536A4 (en) PROCESS FOR MANUFACTURE OF A THERMAL CURING EXPANDED FOAM HAVING EXCELLENT FLAME RESISTANCE AND THERMAL CURING EXPANDED FOAM THEREOF
AR109079A1 (es) Formas cristalinas de 4-ciano-n-(2-(4,4-dimetilciclohex-1-en-1-il)-6-(2,2,6,6-tetrametiltetrahidro-2h-piran-4-il)piridin-3-il)1h-imidazol-2-carboxamida
ES2574577A1 (es) Método para fabricar un componente de aparato doméstico con estructuración doble de una superficie, y componente de aparato doméstico
EP4084945A4 (en) ADDITIVE MANUFACTURING WITH AN ELECTRON BEAM ARRAY