CR20220353A - Compuestos y métodos para la degradación dirigida del receptor de andrógenos - Google Patents

Compuestos y métodos para la degradación dirigida del receptor de andrógenos

Info

Publication number
CR20220353A
CR20220353A CR20220353A CR20220353A CR20220353A CR 20220353 A CR20220353 A CR 20220353A CR 20220353 A CR20220353 A CR 20220353A CR 20220353 A CR20220353 A CR 20220353A CR 20220353 A CR20220353 A CR 20220353A
Authority
CR
Costa Rica
Prior art keywords
compounds
methods
androgen receptor
targeted degradation
prostate cancer
Prior art date
Application number
CR20220353A
Other languages
English (en)
Inventor
Jing Wang
Andrew P Crew
Lawrence B Snyder
Hanqing Dong
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 CR20220353A publication Critical patent/CR20220353A/es

Links

Classifications

    • 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/275Nitriles; Isonitriles
    • A61K31/277Nitriles; Isonitriles having a ring, e.g. verapamil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/417Imidazole-alkylamines, e.g. histamine, phentolamine
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/661Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/662Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • A61K31/663Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08Peptides having 5 to 11 amino acids
    • A61K38/09Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Abstract

Esta descripción se refiere a compuestos, la preparación de los mismos, y el uso de estos compuestos en el tratamiento del cáncer de próstata, que incluye cáncer de próstata metastásico y/o resistente al castrado, en sujetos que lo necesitan.
CR20220353A 2019-12-19 2020-12-18 Compuestos y métodos para la degradación dirigida del receptor de andrógenos CR20220353A (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201962950815P 2019-12-19 2019-12-19
US202063032473P 2020-05-29 2020-05-29
US202063089497P 2020-10-08 2020-10-08
PCT/US2020/066021 WO2021127443A1 (en) 2019-12-19 2020-12-18 Compounds and methods for the targeted degradation of androgen receptor

Publications (1)

Publication Number Publication Date
CR20220353A true CR20220353A (es) 2022-10-20

Family

ID=74195122

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20220353A CR20220353A (es) 2019-12-19 2020-12-18 Compuestos y métodos para la degradación dirigida del receptor de andrógenos

Country Status (18)

Country Link
US (1) US11883393B2 (es)
EP (1) EP4077309A1 (es)
JP (1) JP2023507570A (es)
KR (1) KR20220119094A (es)
CN (1) CN115175901B (es)
AU (1) AU2020405129A1 (es)
BR (1) BR112022012110A2 (es)
CA (1) CA3165168A1 (es)
CL (1) CL2022001662A1 (es)
CO (1) CO2022008728A2 (es)
CR (1) CR20220353A (es)
DO (1) DOP2022000128A (es)
EC (1) ECSP22055515A (es)
IL (1) IL293961A (es)
MX (1) MX2022007678A (es)
PE (1) PE20221582A1 (es)
TW (1) TW202136240A (es)
WO (1) WO2021127443A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11826430B2 (en) 2019-05-14 2023-11-28 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
EP4058464A1 (en) 2019-11-13 2022-09-21 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
US11834458B2 (en) 2021-03-23 2023-12-05 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
TW202329950A (zh) * 2021-11-25 2023-08-01 大陸商江蘇恆瑞醫藥股份有限公司 一種用於雄激素受體蛋白靶向降解的嵌合體化合物、其製備方法及其在醫藥上的應用
WO2024054955A1 (en) * 2022-09-08 2024-03-14 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and methods of treating disease

Family Cites Families (154)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2460304C2 (de) 1974-12-20 1983-08-04 Grünenthal GmbH, 5190 Stolberg 1-n-Propyl-4-phthalimido-piperidin-2,6-dion, Verfahren zu seiner Herstellung und dieses enthaltende Arzneimittel
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US5510357A (en) 1995-02-28 1996-04-23 Eli Lilly And Company Benzothiophene compounds as anti-estrogenic agents
DE69739802D1 (de) 1996-07-24 2010-04-22 Celgene Corp Substituierte 2-(2,6-Dioxopiperidine-3-yl)-phthalimide -1-oxoisoindoline und Verfahren zur Reduzierung des TNF-alpha Spiegels
ATE460423T1 (de) 1997-05-14 2010-03-15 Sloan Kettering Inst Cancer Verfahren und zubereitungen zur zerstörung bestimmter proteine
AU9493698A (en) 1997-09-23 1999-04-12 Eli Lilly And Company Benzothiophenes
EA002822B1 (ru) 1997-12-17 2002-10-31 Мерк Энд Ко., Инк. Антагонисты рецептора интегрина
CA2342222A1 (en) 1998-08-31 2000-03-09 Sugen, Inc. Geometrically restricted 2-indolinone derivatives as modulators of protein kinase activity
US6306663B1 (en) 1999-02-12 2001-10-23 Proteinex, Inc. Controlling protein levels in eucaryotic organisms
US6333344B1 (en) 1999-05-05 2001-12-25 Merck & Co. 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
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
US7208157B2 (en) 2000-09-08 2007-04-24 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
AU2001295041A1 (en) 2000-09-08 2002-03-22 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
US20030045552A1 (en) 2000-12-27 2003-03-06 Robarge Michael J. Isoindole-imide compounds, compositions, and uses thereof
JP2005507363A (ja) 2001-02-16 2005-03-17 イー・アイ・デュポン・ドウ・ヌムール・アンド・カンパニー 血管新生阻害トリペプチド、組成物およびそれらの使用方法
GB0106953D0 (en) 2001-03-20 2001-05-09 Univ Aberdeen Neufofibrillary labels
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
US7030141B2 (en) 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
EP2105136A3 (en) 2002-05-17 2010-01-27 Celgene Corporation Pharmaceutical compositions for treating cancer
KR100732440B1 (ko) 2002-08-30 2007-06-27 에자이 알앤드디 매니지먼트 가부시키가이샤 질소 함유 방향환 유도체
ATE458485T1 (de) 2003-07-11 2010-03-15 Proteologics Inc Ubiquitin-ligase-hemmer und verwandte verfahren
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
US20060252698A1 (en) 2005-04-20 2006-11-09 Malcolm Bruce A Compounds for inhibiting cathepsin activity
TWI522337B (zh) 2005-06-22 2016-02-21 普雷辛肯公司 用於激酶調節的化合物及方法及其適應症
ZA200802490B (en) 2005-08-31 2009-10-28 Celgene Corp Isoindole-imide compounds and compositions comprising and methods of using the same
CA2643267A1 (en) 2006-03-03 2007-09-20 Novartis Ag N-formyl hydroxylamine compounds
SG170809A1 (en) 2006-03-29 2011-05-30 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
US8877780B2 (en) 2006-08-30 2014-11-04 Celgene Corporation 5-substituted isoindoline compounds
AU2007290407A1 (en) 2006-08-30 2008-03-06 Celgene Corporation 5-substituted isoindoline compounds
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
US8067473B2 (en) 2007-01-16 2011-11-29 Teva Pharmaceutical Industries, Ltd. Methods for enhancing the therapeutic efficacy of topoisomerase inhibitors
AU2008279097B2 (en) 2007-07-25 2013-05-02 Bristol-Myers Squibb Company Triazine kinase inhibitors
CN101820765A (zh) 2007-07-31 2010-09-01 安德鲁科技有限公司 包含雄激素受体降解(ard)增强剂的组合物和预防性或治疗性治疗皮肤病与脱发的方法
US8476260B2 (en) 2007-12-28 2013-07-02 Mitsubishi Tanabe Pharma Corporation Antitumor agent
SG195613A1 (en) 2008-10-29 2013-12-30 Celgene Corp Isoindoline compounds for use in the treatment of cancer
US8691187B2 (en) 2009-03-23 2014-04-08 Eli Lilly And Company Imaging agents for detecting neurological disorders
US8614201B2 (en) 2009-06-05 2013-12-24 Janssen Pharmaceutica Nv Heterocyclic amides as modulators of TRPA1
US9163330B2 (en) 2009-07-13 2015-10-20 President And Fellows Of Harvard College Bifunctional stapled polypeptides and uses thereof
EP3202460B1 (en) 2010-02-11 2019-06-12 Celgene Corporation Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
US8198300B2 (en) 2010-04-29 2012-06-12 Universidad De Chile Method for preventing tau protein aggregation and treating Alzheimer's disease with a quinoline derivative compound
HUE031073T2 (en) 2010-05-14 2017-06-28 Dana Farber Cancer Inst Inc Thieno triazolo-diazepine compounds for the treatment of neoplasia
JP5935030B2 (ja) 2010-05-14 2016-06-15 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 白血病を治療するための組成物および方法
US20180144649A1 (en) 2010-06-07 2018-05-24 Affectiva, Inc. Smart toy interaction using image analysis
CN103153335A (zh) 2010-06-30 2013-06-12 布兰代斯大学 小分子靶定的蛋白质降解
WO2012040389A2 (en) 2010-09-22 2012-03-29 Presidio Pharmaceuticals, Inc. Substituted bicyclic hcv inhibitors
WO2012040527A2 (en) 2010-09-24 2012-03-29 The Regents Of The University Of Michigan Deubiquitinase inhibitors and methods for use of the same
CN102477033A (zh) 2010-11-23 2012-05-30 苏州波锐生物医药科技有限公司 苯并噻酚类化合物及其在制备预防和/或治疗乳腺癌骨质疏松症药物中的用途
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
CA2823837A1 (en) 2010-12-07 2012-06-14 Yale University Small-molecule hydrophobic tagging of fusion proteins and induced degradation of same
WO2012090104A1 (en) 2010-12-31 2012-07-05 Kareus Therapeutics, Sa Methods and compositions for designing novel conjugate therapeutics
WO2012149299A2 (en) 2011-04-29 2012-11-01 Celgene Corporaiton Methods for the treatment of cancer and inflammatory diseases using cereblon as a predictor
AU2011384857B2 (en) 2011-12-31 2016-03-03 Beigene, Ltd. Fused tricyclic compounds as Raf kinase inhibitors
CN104736569A (zh) 2012-01-12 2015-06-24 耶鲁大学 通过e3泛素连接酶增强靶蛋白质及其他多肽降解的化合物和方法
WO2013106646A2 (en) 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
US20150141470A1 (en) 2012-05-08 2015-05-21 The Broad Institute, Inc. Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy
EP2846784A4 (en) 2012-05-11 2016-03-09 Univ Yale COMPOUNDS USEFUL FOR STIMULATING PROTEIN DEGRADATION AND METHODS USING THE SAME
IN2014DN11269A (es) 2012-06-25 2015-10-09 Oncoethix Sa
JP6397407B2 (ja) 2012-07-19 2018-09-26 ドレクセル ユニバーシティ 細胞タンパク質ホメオスタシスを調節するためのシグマ受容体リガンド
KR101738063B1 (ko) 2012-09-21 2017-05-19 아로그 파마슈티칼스, 인코퍼레이티드 구조적으로 활성인 인산화된 flt3 키나제의 억제 방법
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.
JP2016513118A (ja) 2013-02-22 2016-05-12 バイエル ファーマ アクチエンゲゼルシャフト 4−置換されたピロロ−およびピラゾロジアゼピン類
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
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
JP2016525135A (ja) 2013-07-23 2016-08-22 バイエル ファーマ アクチエンゲゼルシャフト BETタンパク質およびポロ様キナーゼの二重阻害薬としての置換されたジヒドロピリド[3,4−b]ピラジノン類
CN105593224B (zh) 2013-07-31 2021-05-25 恒元生物医药科技(苏州)有限公司 作为溴结构域抑制剂的新型喹唑啉酮类化合物
US20150051208A1 (en) 2013-08-14 2015-02-19 Boehringer Ingelheim International Gmbh Pyridinones
US9428513B2 (en) 2013-11-07 2016-08-30 Boehringer Ingelheim International Gmbh Triazolopyrazine
ES2860695T3 (es) 2013-11-18 2021-10-05 Forma Therapeutics Inc Composiciones de tetrahidroquinolina como inhibidores de bromodominio BET
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9458156B2 (en) 2014-12-23 2016-10-04 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
US20150259288A1 (en) 2014-03-14 2015-09-17 City Of Hope 5-bromo-indirubins
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
KR20210132233A (ko) 2014-04-14 2021-11-03 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
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
WO2015195863A1 (en) 2014-06-20 2015-12-23 Constellation Pharmaceuticals, Inc. Hydrated 2-((4s)-6-(4-chlorophenyl)-1 -methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
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
CA2960090A1 (en) 2014-10-02 2016-04-07 Glaxosmithkline Intellectual Property (No.2) Limited Compound
JP6715243B2 (ja) 2014-10-27 2020-07-01 テンシャ セラピューティクス,インコーポレイテッド ブロモドメイン阻害剤
EP3233828B1 (en) 2014-12-18 2020-03-04 F. Hoffmann-La Roche AG Estrogen receptor modulators and uses thereof
US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
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
US20170327469A1 (en) 2015-01-20 2017-11-16 Arvinas, Inc. Compounds and methods for the targeted degradation of androgen receptor
KR102110566B1 (ko) 2015-01-20 2020-05-13 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적화된 분해를 위한 화합물 및 방법
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
GB201506871D0 (en) 2015-04-22 2015-06-03 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201506872D0 (en) 2015-04-22 2015-06-03 Ge Oil & Gas Uk Ltd Novel compounds
EP3302572B8 (en) 2015-06-04 2021-03-24 Arvinas Operations, Inc. Imide-based modulators of proteolysis and associated methods of use
US20180147202A1 (en) 2015-06-05 2018-05-31 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
CA2988430A1 (en) 2015-07-10 2017-01-19 Arvinas, 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
EP3331905B1 (en) 2015-08-06 2022-10-05 Dana-Farber Cancer Institute, Inc. Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
GB201516243D0 (en) 2015-09-14 2015-10-28 Glaxosmithkline Ip Dev Ltd Novel compounds
US9938264B2 (en) 2015-11-02 2018-04-10 Yale University Proteolysis targeting chimera compounds and methods of preparing and using same
US11395820B2 (en) 2016-03-16 2022-07-26 H. Lee Moffitt Cancer Center And Research Institute, Inc. Small molecules against cereblon to enhance effector t cell function
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
RU2021102253A (ru) 2016-04-06 2021-03-03 Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган Деструкторы белка mdm2
WO2017185036A1 (en) 2016-04-22 2017-10-26 Dana Farber Cancer Institute, Inc. Bifunctional molecules for degradation of egfr 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
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-LINKED C3-GLUTARIMIDE DEGRONIMERS FOR THE DEGRADATION OF TARGET PROTEINS
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
EP3526202A4 (en) 2016-10-11 2020-04-29 Arvinas, Inc. COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF ANDROGEN RECEPTOR
MX2019005007A (es) 2016-11-01 2019-07-18 Arvinas Inc Protac dirigidos a la proteína tau y métodos asociados de uso.
US10899768B2 (en) 2016-11-22 2021-01-26 Dana-Farber Cancer Institute, Inc. Degradation of protein kinases by conjugation of protein kinase inhibitors with E3 ligase ligand and methods of use
LT3689868T (lt) 2016-12-01 2023-12-27 Arvinas Operations, Inc. Tetrahidronaftaleno ir tetrahidroizochinolino dariniai kaip estrogenų receptorių destruktoriai
WO2018118598A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
JP2020504741A (ja) 2016-12-23 2020-02-13 アルビナス・オペレーションズ・インコーポレイテッドArvinas Operations, Inc. Raf(急速進行性線維肉腫)ポリペプチドの標的分解のための化合物および方法
KR20190101406A (ko) 2016-12-23 2019-08-30 아비나스 오퍼레이션스, 인코포레이티드 Egfr 단백질분해 표적화 키메라 분자 및 관련 사용 방법
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
EP3573977A4 (en) 2017-01-26 2020-12-23 Arvinas Operations, Inc. EESTROGEN RECEPTOR PROTEOLYSIS MODULATORS AND RELATED METHOD OF USE
BR112019015484A2 (pt) 2017-01-31 2020-04-28 Arvinas Operations Inc ligantes de cereblon e compostos bifuncionais compreendendo os mesmos
WO2018200981A1 (en) 2017-04-28 2018-11-01 Quartz Therapeutics, Inc. Raf-degrading conjugate compounds
CN110831601B (zh) 2017-05-01 2023-10-27 思普格治疗公司 三部分组成的雄激素受体消除剂、其方法和用途
EP3743066A4 (en) 2018-01-26 2021-09-08 Yale University IMIDE BASED MODULATORS OF PROTEOLYSIS AND METHOD OF USE
PL3904350T3 (pl) 2018-04-12 2024-02-19 Bayer Aktiengesellschaft Pochodne N-(cyklopropylometylo)-5-(metylosulfonylo)-N-{1-[1-(pirymidyn-2-ylo)-1H-1,2,4-triazol-5-ilo]etylo}benzamidu oraz odpowiednie pochodne pirydyno-karboksyamidu jako pestycydy
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
EP3897635A4 (en) 2018-12-19 2022-08-31 Celgene Corporation SUBSTITUTED 3-((3-AMINOPHENYL)AMINO)PIPERIDINE-2,6-DIONE COMPOUNDS, COMPOSITIONS THEREOF AND METHODS OF TREATMENT THEREOF
CN113453681A (zh) 2018-12-19 2021-09-28 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
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
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
CA3155010A1 (en) 2019-09-19 2021-03-25 The Regents Of The Universtiy Of Michigan Spirocyclic androgen receptor protein degraders
CN114761003B (zh) 2019-09-23 2023-12-29 冰洲石生物科技公司 具有雄激素受体降解活性的新型脲类及其用途
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
WO2021061644A1 (en) 2019-09-23 2021-04-01 Accutar Biotechnology Inc. Novel substituted quinoline-8-carbonitrile derivatives with androgen receptor degradation activity and uses thereof
CA3161045A1 (en) 2019-12-19 2021-06-24 Wei Cai Substituted straight chain spiro derivatives
BR112022012003A2 (pt) 2019-12-19 2022-08-30 Skinosive Compostos fotoprotetores adesivos e usos dos mesmos
IL293980A (en) 2019-12-19 2022-08-01 Debiopharm Int Sa New compounds and their use
CN113651814B (zh) 2019-12-19 2022-06-17 北京加科思新药研发有限公司 Kras突变蛋白抑制剂
GEP20247585B (en) 2019-12-19 2024-01-25 Bayer Ag Furoindazole derivatives
TWI755992B (zh) 2019-12-23 2022-02-21 大陸商上海濟煜醫藥科技有限公司 一種蛋白降解劑化合物的製備方法和應用
US20230119316A1 (en) 2019-12-27 2023-04-20 Lupin Limited Substituted Tricyclic Compounds
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
TW202210079A (zh) 2020-05-29 2022-03-16 美商纜圖藥品公司 普拉替尼醫藥組合物
CA3183100A1 (en) 2020-05-29 2021-12-02 Boehringer Ingelheim Pharma Gmbh & Co. Kg Anthelmintic heterocyclic compounds
WO2021249534A1 (zh) 2020-06-12 2021-12-16 上海济煜医药科技有限公司 酞嗪酮类化合物及其制备方法和医药用途
WO2021262810A1 (en) 2020-06-24 2021-12-30 Celgene Corporation Cereblon binding compounds, compositions thereof, and methods of treatment therewith
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
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
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

Also Published As

Publication number Publication date
MX2022007678A (es) 2022-09-19
JP2023507570A (ja) 2023-02-24
EP4077309A1 (en) 2022-10-26
KR20220119094A (ko) 2022-08-26
CO2022008728A2 (es) 2022-07-19
US20210196710A1 (en) 2021-07-01
IL293961A (en) 2022-08-01
WO2021127443A1 (en) 2021-06-24
DOP2022000128A (es) 2022-08-31
CN115175901A (zh) 2022-10-11
CL2022001662A1 (es) 2023-02-10
TW202136240A (zh) 2021-10-01
ECSP22055515A (es) 2022-09-30
PE20221582A1 (es) 2022-10-06
US11883393B2 (en) 2024-01-30
BR112022012110A2 (pt) 2022-12-13
CA3165168A1 (en) 2021-06-24
AU2020405129A1 (en) 2022-06-23
CN115175901B (zh) 2024-03-22

Similar Documents

Publication Publication Date Title
MX2022007678A (es) Compuestos y metodos para la degradacion dirigida del receptor de androgenos.
MX2020012797A (es) Anticuerpos biespecificos anti-pvrig/anti-tigit y métodos de uso.
PH12020551923A1 (en) Methods and compositions for treating cancer
PH12019501959A1 (en) Therapeutic rna
MX2018008426A (es) Combinaciones anti-egfr para tratar tumores.
MX2019000200A (es) Agentes antiproliferativos basados en pirimidina.
PH12017500070A1 (en) Methods of treating cancer using tigit inhibitors and anti-cancer agents
TW201611847A (en) Compounds and compositions for treating EGFR expressing tumors
MX2017005929A (es) Terapia de combinacion con agonistas de unión ox40 e inhibidores de tigit.
MX2018008427A (es) Combinaciones anti-cd20 para tratar tumores.
MX2017003246A (es) Macropinocitosis de anticuerpos anti-cd46 humanos y agentes terapeuticos dirigidos contra el cancer.
MX2016006726A (es) Composiciones que comprenden anticuerpos anti-molecula de adhesion celular relacionada con antigeno carcinoembrionario 1 y anti-muerte celular programada para la terapia contra el cancer.
EA201691866A1 (ru) Проникающие в опухоль лимфоциты для адоптивной клеточной терапии
ZA201905222B (en) Combination treating prostate cancer, pharmaceutical composition and treatment method
MX2019006331A (es) Métodos para tratar el cáncer usando anticuerpos anti-pd-l1 y antiandrógenos.
MX2021005398A (es) Terapia del cancer con celulas inmunitarias anti-cd33.
MX2019008158A (es) Terapia de combinacion para el tratamiento del cancer.
MY189713A (en) Duocarmycin adcs for use in treatment of endometrial cancer
AU2015249633A8 (en) Methods of treating early breast cancer with Trastuzumab-MCC-DM1 and Pertuzumab
WO2016172494A3 (en) Combination of immunotherapy with local chemotherapy for the treatment of malignancies
MX2015007185A (es) Uso de eribulina en el tratamiento de cancer de pecho.
MX2023000191A (es) Metodos de fabricacion y uso de inhibidores de pde9.
MX2021005761A (es) Anticuerpos anti-proteína alfa reguladora de señal (anti-sirpalfa) humanizados.
MX2021005395A (es) Terapia del cáncer con células inmunitarias anti-liv1.
MX2019008233A (es) Nanoconjugados de doxorrubicina y oro dirigidos para terapia tumoral.