[go: up one dir, main page]

MX2022014071A - 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
MX2022014071A
MX2022014071A MX2022014071A MX2022014071A MX2022014071A MX 2022014071 A MX2022014071 A MX 2022014071A MX 2022014071 A MX2022014071 A MX 2022014071A MX 2022014071 A MX2022014071 A MX 2022014071A MX 2022014071 A MX2022014071 A MX 2022014071A
Authority
MX
Mexico
Prior art keywords
forms
bifunctional compound
compound
manufacturing
same
Prior art date
Application number
MX2022014071A
Other languages
English (en)
Inventor
Robert J Duguid
Hanqing Dong
John A Grosso
Hayley Reece
Iii Royal J Haskell
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
Rhys Lloyd
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 MX2022014071A publication Critical patent/MX2022014071A/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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Biophysics (AREA)
  • Physiology (AREA)
  • Inorganic Chemistry (AREA)
  • Nutrition Science (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

La presente descripción se refiere a formas ultrapuras, polimorfos, formas amorfas y formulaciones de N-[(1r,4r)-4-(3-cloro-4-cianofenoxi)ciclohexil]-6-[4-({4-[2-(2,6- dioxopiperidin-3-il)-6-fluoro-1,3-dioxo-2,3-dihidro-1H-isoindol-5 -il]piperazin-1-il}metil)piperidin-1-il]piridazina-3-carboxamida, denominada en la presente descripción Compuesto A: (ver Fórmula) (Compuesto A). La presente descripción también se refiere a métodos de fabricación y purificación de los mismos, así como también a productos intermedios útiles en la síntesis del Compuesto A. Las formas ultrapuras, polimorfos, formas amorfas y formulaciones del Compuesto A pueden usarse como agentes terapéuticos para el tratamiento de varias enfermedades y afecciones tales como el cáncer.
MX2022014071A 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. MX2022014071A (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
MX2022014071A true MX2022014071A (es) 2023-01-30

Family

ID=76305987

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2022014071A MX2022014071A (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 (es)
EP (1) EP4146642A1 (es)
JP (1) JP2023524599A (es)
KR (1) KR20230015933A (es)
CN (1) CN115996918A (es)
AU (1) AU2021273458A1 (es)
BR (1) BR112022022753A2 (es)
CA (1) CA3181782A1 (es)
CL (1) CL2023000074A1 (es)
CO (1) CO2022017700A2 (es)
CR (1) CR20220630A (es)
EC (1) ECSP22086223A (es)
IL (1) IL297762A (es)
MX (1) MX2022014071A (es)
PE (1) PE20231204A1 (es)
TW (1) TW202208345A (es)
WO (1) WO2021231174A1 (es)

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
KR102173463B1 (ko) 2016-10-11 2020-11-04 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적 분해용 화합물 및 방법
EP4045496A1 (en) 2019-10-17 2022-08-24 Arvinas Operations, Inc. Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety
IL301155A (en) 2020-09-14 2023-05-01 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
CN118574823A (zh) * 2022-01-27 2024-08-30 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
US20250248999A1 (en) 2022-04-21 2025-08-07 Arvinas Operations, Inc. Bavdegalutamide and combinations thereof for use in treating prostate cancer
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
US101A (en) 1836-12-06 Method of jcakibtg and furling iw sails fob ships
US10584A (en) 1854-02-28 Bank-lock
CZ302378B6 (cs) 1996-07-24 2011-04-20 Celgene Corporation Optický izomer (S)-1,3-dioxo-2-(2,6-dioxopiperidin-3-yl)-4-aminoisoindolin a farmaceutická kompozice s jeho obsahem
ATE460423T1 (de) 1997-05-14 2010-03-15 Sloan Kettering Inst Cancer Verfahren und zubereitungen zur zerstörung bestimmter proteine
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
DE60026514T2 (de) 1999-05-05 2006-11-09 Merck & Co., Inc. Neue prolinverbindungen als mikrobizide mittel
AU2001288213B2 (en) 2000-06-28 2005-04-14 Bristol-Myers Squibb Company Selective androgen receptor modulators and methods for their identification, design and use
US7208157B2 (en) 2000-09-08 2007-04-24 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
WO2002020740A2 (en) 2000-09-08 2002-03-14 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
EP1405621B1 (en) 2001-06-20 2011-05-11 Takeda Pharmaceutical Company Limited Method of manufacturing tablet
ES2325916T3 (es) 2001-08-06 2009-09-24 The Children's Medical Center Corporation Actividad antiangiogenica de analogos de talidomida sustituidos con nitrogeno.
US7030141B2 (en) 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
JP4183193B2 (ja) 2002-08-30 2008-11-19 エーザイ・アール・アンド・ディー・マネジメント株式会社 含窒素芳香環誘導体
BRPI0513020A (pt) 2004-07-08 2008-04-22 Warner Lambert Co moduladores de andrÈgenio, seus usos, composição farmacêutica, formulação farmacêutica tópica e artigo de fabricação
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
US20060252698A1 (en) 2005-04-20 2006-11-09 Malcolm Bruce A Compounds for inhibiting cathepsin activity
BRPI0614995A2 (pt) 2005-08-31 2010-01-12 Celgene Corp composto ou um sal, solvato ou estereoisemero farmaceuticamente aceitável do mesmo, composição farmacêutica, uso de uma quantidade terapêutica ou profilaticamente eficaz de um composto ou um sal, solvato ou estereoisemero farmaceuticamente aceitável do mesmo, e, forma de dosagem unitária única
US20090062537A1 (en) 2006-03-03 2009-03-05 Kwangho Lee N-Formyl Hydrozyamine Compounds
JP5350217B2 (ja) 2006-03-29 2013-11-27 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア ジアリールチオヒダントイン化合物
EP2059502A2 (en) 2006-07-20 2009-05-20 Ligand Pharmaceuticals Incorporated Proline urea ccr1 antagonists for the treatment of autoimmune diseases or inflammation
US8877780B2 (en) 2006-08-30 2014-11-04 Celgene Corporation 5-substituted isoindoline compounds
CL2007002513A1 (es) 2006-08-30 2008-04-04 Celgene Corp Soc Organizada Ba Compuestos derivados de isoindolina sustituidos, compuestos intermediarios; composicion farmaceutica; y uso en el tratamiento y prevencion de enfermedades tales como cancer, dolor, degeneracion macular, entre otras.
RU2448101C2 (ru) 2006-08-30 2012-04-20 Селджин Корпорейшн 5-замещенные изоиндолиновые соединения
WO2008054827A2 (en) 2006-11-03 2008-05-08 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
KR20100038108A (ko) 2007-07-25 2010-04-12 브리스톨-마이어스 스큅 컴퍼니 트리아진 키나제 억제제
CA2694953C (en) 2007-07-31 2015-12-01 Androscience Corporation Compositions including androgen receptor degradation (ard) enhancers and methods of prophylactic or therapeutic treatment of skin disorders and hair loss
ES2559388T3 (es) 2008-10-29 2016-02-11 Celgene Corporation Compuestos de isoindolina para uso en el tratamiento del cáncer
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.
WO2010141805A1 (en) 2009-06-05 2010-12-09 Janssen Pharmaceutica Nv Heterocyclic amides as modulators of trpa1
AU2010273220B2 (en) 2009-07-13 2015-10-15 President And Fellows Of Harvard College Bifunctional stapled polypeptides and uses thereof
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
HRP20171078T1 (hr) 2010-02-11 2017-10-06 Celgene Corporation Derivati arilmetoksi izoindolina i pripravci koji ih sadrže, te postupci njihove uporabe
AU2011272860A1 (en) 2010-06-30 2013-02-07 Brandeis University Small-molecule-targeted protein degradation
JP5852658B2 (ja) 2010-09-24 2016-02-03 ザ リージェンツ オブ ザ ユニバーシティー オブ ミシガン デユビキチナーゼ阻害剤およびその使用方法
CA2823837A1 (en) 2010-12-07 2012-06-14 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
US8921378B2 (en) 2011-04-21 2014-12-30 Orion Corporation Androgen receptor modulating carboxamides
CA2834535A1 (en) 2011-04-29 2012-11-01 Celgene Corporation Methods for the treatment of cancer and inflammatory diseases using cereblon as a predictor
WO2013106643A2 (en) 2012-01-12 2013-07-18 Yale University Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase
WO2013106646A2 (en) 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
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
NZ713828A (en) * 2012-06-04 2017-05-26 Pharmacyclics Llc Crystalline forms of a bruton’s tyrosine kinase inhibitor
AU2013292519B2 (en) 2012-07-19 2017-12-07 Drexel University Sigma receptor ligands for modulating cellular protein homeostasis
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.
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
EP3738594A1 (en) 2013-09-10 2020-11-18 Madrigal Pharmaceuticals, Inc. Targeted therapeutics having an hsp90 ligand as binding moiety
IN2014MU00303A (es) 2014-01-28 2015-09-11 Cipla Ltd
MA39481A (fr) 2014-03-03 2015-09-11 Synta Pharmaceuticals Corp Thérapies ciblées
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
RU2020139890A (ru) 2014-04-14 2022-01-18 Арвинас Оперэйшнз, Инк. Имидные модуляторы протеолиза и способы их применения
US20160058872A1 (en) 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
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
CA2967662A1 (en) 2014-11-21 2016-05-26 Biohaven Pharmaceutical Holding Company Ltd. Sublingual formulation of riluzole
JP6807841B2 (ja) 2014-12-18 2021-01-06 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト エストロゲン受容体モジュレーター及びその使用
US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
CN107257800B (zh) 2014-12-23 2020-06-30 达纳-法伯癌症研究所股份有限公司 通过双功能分子诱导靶蛋白降解的方法
KR20230119040A (ko) 2015-01-20 2023-08-14 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적화된 분해를 위한 화합물 및방법
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
EP4414369A3 (en) 2015-03-18 2024-10-16 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
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
CA2988414C (en) 2015-06-04 2023-09-26 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
EP3302482A4 (en) 2015-06-05 2018-12-19 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
AU2016291578C1 (en) 2015-07-10 2021-07-15 Arvinas Operations, Inc. MDM2-based modulators of proteolysis and associated methods of use
AU2016294450A1 (en) 2015-07-13 2017-12-07 Arvinas Operations, 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
CA3002709A1 (en) 2015-11-02 2017-05-11 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
WO2017184995A1 (en) 2016-04-21 2017-10-26 Bioventures, Llc Compounds that induce degradation of anti-apoptotic bcl-2 family proteins and the uses thereof
EP3985006A1 (en) 2016-04-22 2022-04-20 Dana-Farber Cancer Institute, Inc. Degradation of cyclin-dependent kinase 8 (cdk8) by conjugation of cdk8 inhibitors with e3 ligase ligand and methods of use
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
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
WO2017197056A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Bromodomain targeting degronimers for target protein degradation
WO2017197051A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Amine-linked c3-glutarimide degronimers for target protein degradation
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
WO2018053354A1 (en) 2016-09-15 2018-03-22 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
KR102173463B1 (ko) 2016-10-11 2020-11-04 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적 분해용 화합물 및 방법
AU2017363257B2 (en) 2016-11-22 2021-08-19 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
CA3062161A1 (en) 2017-05-01 2018-11-08 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
KR102864064B1 (ko) 2018-12-19 2025-09-24 셀진 코포레이션 치환된 3-((3-아미노페닐)아미노)피페리딘-2,6-디온 화합물, 이의 조성물, 및 이를 사용한 치료 방법
BR112021011968A2 (pt) 2018-12-19 2021-09-08 Celgene Corporation Compostos de 3-((3-aminofenil)amino)piperidina-2,6-diona substituídos, composições dos mesmos e métodos de tratamento com os mesmos
WO2020132561A1 (en) 2018-12-20 2020-06-25 C4 Therapeutics, Inc. Targeted protein degradation
JP7555938B2 (ja) 2019-01-30 2024-09-25 モンテリノ・セラピューティクス・インコーポレイテッド アンドロゲン受容体を標的とするユビキチン化のための二官能性化合物および方法
US11547759B2 (en) 2019-01-30 2023-01-10 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
MX2021011827A (es) 2019-03-28 2021-12-10 Essa Pharma Inc Moduladores del receptor de andrógenos y métodos para su uso como ligandos quiméricos que se dirigen a la proteólisis.
WO2020198712A1 (en) 2019-03-28 2020-10-01 Essa Pharma, Inc. Pharmaceutical compositions and combinations comprising inhibitors of the androgen receptor and uses thereof
BR112021020775A2 (pt) * 2019-04-18 2021-12-14 Hinova Pharmaceuticals Inc Classe de compostos heterocíclicos quiméricos bifuncionais para a degradação direcionada de receptores de andrógeno e uso dos mesmos
WO2020214952A1 (en) 2019-04-18 2020-10-22 Accutar Biotechnology Inc. Novel compounds having bet, estrogen receptor, and androgen receptor degradation activity and uses thereof
WO2020233512A1 (zh) 2019-05-17 2020-11-26 成都海创药业有限公司 一种芳香胺类靶向ar和bet的蛋白降解嵌合体化合物及用途
WO2021055756A1 (en) 2019-09-19 2021-03-25 The Regents Of The University Of Michigan Spirocyclic androgen receptor protein degraders
US11420956B2 (en) 2019-09-23 2022-08-23 Accutar Biotechnology Inc. Ureas 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
WO2021061204A1 (en) 2019-09-23 2021-04-01 Accutar Biotechnology Inc. Novel substituted quinoline-8-carbonitrile derivatives having androgen receptor degradation activity and uses thereof
IL292359A (en) 2019-10-22 2022-06-01 Arvinas Operations Inc Prostate cancer treatment methods
MX2022007885A (es) 2019-12-23 2022-09-19 Shanghai Jemincare Pharmaceuticals Co Ltd Metodo y aplicacion de preparacion de compuesto como agente de degradacion de proteinas.
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
KR20230015934A (ko) 2020-05-12 2023-01-31 아비나스 오퍼레이션스, 인코포레이티드 전립선암 치료 방법
TWI781651B (zh) 2020-06-12 2022-10-21 大陸商上海濟煜醫藥科技有限公司 酞嗪酮類化合物及其製備方法和醫藥用途
KR20230027066A (ko) 2020-06-24 2023-02-27 셀진 코포레이션 세레블론 결합 화합물, 이의 조성물, 및 이에 의한 치료 방법
TW202216690A (zh) 2020-06-24 2022-05-01 美商西建公司 Ｃｅｒｅｂｌｏｎ結合化合物、其組合物及使用該等物質之治療方法
KR20230027213A (ko) 2020-06-24 2023-02-27 셀진 코포레이션 세레블론 결합 화합물, 이의 조성물, 및 이에 의한 치료 방법
CN113912589B (zh) 2020-07-08 2023-10-20 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
CN114133379B (zh) 2020-09-04 2024-02-13 南京奥瑞药业有限公司 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
WO2022087125A1 (en) 2020-10-21 2022-04-28 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor protein
JP2023548540A (ja) 2020-11-06 2023-11-17 アルビナス・オペレーションズ・インコーポレイテッド アンドロゲン受容体の標的分解のための化合物及び方法、並びに関連する使用方法
CN116529248B (zh) 2020-11-25 2025-10-17 西藏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
WO2022125969A1 (en) 2020-12-11 2022-06-16 Arvinas Operations, Inc. Methods of treating prostate cancer
CN114685601B (zh) 2020-12-30 2024-10-18 财团法人工业技术研究院 雄性激素受体结合分子及其用途
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
WO2022187419A1 (en) 2021-03-03 2022-09-09 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
US20250248999A1 (en) 2022-04-21 2025-08-07 Arvinas Operations, Inc. Bavdegalutamide and combinations thereof for use in treating prostate cancer
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
AU2021273458A1 (en) 2022-12-01
KR20230015933A (ko) 2023-01-31
US20240409529A1 (en) 2024-12-12
TW202208345A (zh) 2022-03-01
EP4146642A1 (en) 2023-03-15
JP2023524599A (ja) 2023-06-12
ECSP22086223A (es) 2022-12-30
US12043612B2 (en) 2024-07-23
CR20220630A (es) 2023-01-23
PE20231204A1 (es) 2023-08-17
WO2021231174A1 (en) 2021-11-18
CA3181782A1 (en) 2021-11-18
CL2023000074A1 (es) 2023-07-07
US20230012321A1 (en) 2023-01-12
CN115996918A (zh) 2023-04-21
IL297762A (en) 2022-12-01
CO2022017700A2 (es) 2022-12-20

Similar Documents

Publication Publication Date Title
MX2022014071A (es) Metodos para fabricar un compuesto bifuncional, formas ultrapuras del compuesto bifuncional y formas de dosificacion que comprenden el mismo.
CA2883751C (en) Methods of treating alzheimer's disease and pharmaceutical compositions thereof
JP2018502877A5 (es)
EA200970611A1 (ru) Замещенные пиразолохиназолиновые производные, способ их получения и их применение в качестве ингибиторов киназы
CA2471099A1 (en) .alpha.-(n-sulphonamido)acetamide derivatives as .beta.-amyloid inhibitors
NO20050851L (no) Kaspase-inhibitorer og anvendelser derav
AU2002359164A8 (en) Use of oxindole derivatives in the treatment of dementia related diseases, alzheimer's disease and conditions associated with glycogen synthase kinase-3
JP2010526129A5 (es)
ATE381537T1 (de) Formanilid-derivative als beta2-adrenorezeptor- agonisten
GEP20084551B (en) 4-phenylamino-quinazolin-6-yl-amides
AR087336A1 (es) Compuestos de 2-(2,4,5-anilino sustituido)pirimidina
NO20082508L (no) Aminopyrimidiner anvendelige som kinaseinhibitorer
MA35090B1 (fr) Polythérapie pour les malignités hématologiques
MX2008013836A (es) Derivados de 2-piridona para el tratamiento de enfermedades o condiciones en las cuales es benefica la inhibicion de la actividad de elastasa de neutrofilos.
DE60323133D1 (de) Cyclohexylverbindungen als ccr5-antagonisten
MA46229B1 (fr) Composés d'hétéroaryle carboxamide en tant qu'inhibiteurs de ripk2
IL188942A0 (en) Benzimidazole derivatives and pharmaceutical compositions containing the same
TW200616953A (en) Indole, indazole or indoline derivatives
IL205697A0 (en) 4(-3-(-2-(phenyl)morpholino)-2-oxopyrrolidin-1-yl)-n-(thiazole-2-yl)benzenesulfon-amide derivatives, compositions comprising the same and uses thereof
NO20091185L (no) Piperidinderivater
CR20240513A (es) Compuestos de heteroarilo para el tratamiento del dolor
CY1107204T1 (el) Πιπεραζινοβενζοθειαζολια ως ουσιες για την θεραπευτικη αντιμετωπιση εγκεφαλικων ισχαιμικων διαταραχων ή διαταραχων του κνς
DE60329330D1 (de) Piperidin- und pyrrolidin-derivate alsantagonisten des histamin-h3-rezeptors
ATE396986T1 (de) Pyrimidylpyrrolderivate, die als kinaseinhibitoren wirken
CR20240514A (es) Compuestos de heteroarilo para el tratamiento del dolor