CO2019003642A2 - Compuestos y métodos para la degradación dirigida del receptor de andrógenos - Google Patents

Compuestos y métodos para la degradación dirigida del receptor de andrógenos

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Publication number
CO2019003642A2
CO2019003642A2 CONC2019/0003642A CO2019003642A CO2019003642A2 CO 2019003642 A2 CO2019003642 A2 CO 2019003642A2 CO 2019003642 A CO2019003642 A CO 2019003642A CO 2019003642 A2 CO2019003642 A2 CO 2019003642A2
Authority
CO
Colombia
Prior art keywords
androgen receptor
compounds
present disclosure
methods
degradation
Prior art date
Application number
CONC2019/0003642A
Other languages
English (en)
Spanish (es)
Inventor
jing; Wang
Craig M Crews
Hanqing Dong
Andrew P Crew
Keith R Hornberger
Lawrence B Snyder
Kurt; Zimmermann
Michael; Berlin
Original Assignee
Arvinas 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 Inc filed Critical Arvinas Inc
Publication of CO2019003642A2 publication Critical patent/CO2019003642A2/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D233/30—Oxygen or sulfur atoms
    • C07D233/42—Sulfur atoms
    • 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
    • A61K31/02—Halogenated hydrocarbons
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • 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
    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non 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
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    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/33—Heterocyclic compounds
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    • A61K31/33—Heterocyclic compounds
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    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/54—Medicinal 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
    • A61K47/55—Medicinal 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 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/74—Oxygen atoms
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    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/20—Spiro-condensed ring systems
    • 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
    • C07D231/12—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/08—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
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    • 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
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    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
CONC2019/0003642A 2016-10-11 2019-04-11 Compuestos y métodos para la degradación dirigida del receptor de andrógenos CO2019003642A2 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662406888P 2016-10-11 2016-10-11
US201762528385P 2017-07-03 2017-07-03
PCT/US2017/056234 WO2018071606A1 (en) 2016-10-11 2017-10-11 Compounds and methods for the targeted degradation of androgen receptor

Publications (1)

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CO2019003642A2 true CO2019003642A2 (es) 2019-06-19

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US (8) US10584101B2 (enExample)
EP (3) EP4509184A3 (enExample)
JP (6) JP7009466B2 (enExample)
KR (3) KR102173463B1 (enExample)
CN (2) CN111892577B (enExample)
AU (6) AU2017341723B2 (enExample)
CA (1) CA3038979A1 (enExample)
CO (1) CO2019003642A2 (enExample)
CY (1) CY1126053T1 (enExample)
DK (2) DK3526202T3 (enExample)
ES (2) ES2945224T3 (enExample)
FI (2) FI3526202T3 (enExample)
HR (2) HRP20250181T1 (enExample)
HU (2) HUE070289T2 (enExample)
IL (4) IL265806B2 (enExample)
LT (2) LT3660004T (enExample)
MX (3) MX2019004278A (enExample)
PL (2) PL3526202T3 (enExample)
PT (2) PT3526202T (enExample)
RS (2) RS66647B1 (enExample)
SI (2) SI3660004T1 (enExample)
SM (1) SMT202300152T1 (enExample)
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Families Citing this family (206)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20250127179A (ko) * 2014-04-14 2025-08-26 아비나스 오퍼레이션스, 인코포레이티드 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
US11352351B2 (en) 2015-01-20 2022-06-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
CA3017740A1 (en) * 2016-03-16 2017-09-21 Pearlie BURNETTE Small molecules against cereblon to enhance effector t cell function
EP4491236A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
EP3455218A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
WO2017197036A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
PT3500299T (pt) 2016-08-19 2024-02-21 Beigene Switzerland Gmbh Combinação de zanubrutinib com um anticorpo anti-cd20 ou anti-pd-1 para utilização no tratamento do cancro
WO2018053354A1 (en) 2016-09-15 2018-03-22 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
HUE070289T2 (hu) * 2016-10-11 2025-05-28 Arvinas Operations Inc Vegyületek és módszerek az androgénreceptor célzott lebontására
KR20230127371A (ko) 2016-11-01 2023-08-31 아비나스 오퍼레이션스, 인코포레이티드 타우(Tau)-단백질 표적화 프로탁(PROTAC) 및 관련 사용 방법
IL297717A (en) 2016-12-01 2022-12-01 Arvinas Operations Inc History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists
WO2018119441A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Egfr proteolysis targeting chimeric molecules and associated methods of use
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
WO2018118598A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
MX2019007649A (es) 2016-12-23 2019-09-10 Arvinas Operations Inc Compuestos y metodos para la degradacion dirigida de polipeptidos de fibrosarcoma acelerado rapidamente.
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
IL300417A (en) 2017-01-26 2023-04-01 Arvinas Operations Inc Bifunctional benzothiophene compounds, preparations containing them and their use in therapy
EP3577109A4 (en) 2017-01-31 2020-11-18 Arvinas Operations, Inc. CEREMONY LIGANDS AND BIFUNCTIONAL COMPOUNDS CONTAINING THEM
CN118440096A (zh) 2017-06-20 2024-08-06 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体
TW202515616A (zh) 2017-06-26 2025-04-16 英屬開曼群島商百濟神州有限公司 抗pd-1抗體或其抗原結合片段在製備治療用於患有肝細胞癌(hcc)之藥物的用途
US10357489B2 (en) 2017-07-10 2019-07-23 Celgene Corporation Antiproliferative compounds and methods of use thereof
TWI793151B (zh) 2017-08-23 2023-02-21 瑞士商諾華公司 3-(1-氧異吲哚啉-2-基)之氫吡啶-2,6-二酮衍生物及其用途
EP3679026A1 (en) 2017-09-04 2020-07-15 C4 Therapeutics, Inc. Glutarimide
WO2019043208A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROQUINOLINONES
CN111315735B (zh) 2017-09-04 2024-03-08 C4医药公司 二氢苯并咪唑酮
CN111372585A (zh) 2017-11-16 2020-07-03 C4医药公司 用于靶蛋白降解的降解剂和降解决定子
US11065231B2 (en) 2017-11-17 2021-07-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
WO2019108795A1 (en) 2017-11-29 2019-06-06 Beigene Switzerland Gmbh Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors
EP3743066A4 (en) 2018-01-26 2021-09-08 Yale University IMIDE-BASED PROTEOLYSIS MODULATORS AND RELATED METHODS OF USE
US11028088B2 (en) 2018-03-10 2021-06-08 Yale University Modulators of BTK proteolysis and methods of use
EP3774804A1 (en) 2018-03-26 2021-02-17 Novartis AG N-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)benzamide derivatives
KR20210018199A (ko) 2018-03-26 2021-02-17 씨4 테라퓨틱스, 인코포레이티드 이카로스의 분해를 위한 세레블론 결합제
JP7720698B2 (ja) 2018-04-04 2025-08-08 アルビナス・オペレーションズ・インコーポレイテッド タンパク質分解の調節因子および関連する使用方法
JP7367908B2 (ja) * 2018-04-09 2023-10-24 上海科技大学 標的タンパク質分解化合物、その抗腫瘍応用、その中間体および中間体の応用
EP3774772A1 (en) * 2018-04-13 2021-02-17 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2019204354A1 (en) 2018-04-16 2019-10-24 C4 Therapeutics, Inc. Spirocyclic compounds
EP4272737A3 (en) 2018-04-23 2024-01-17 Celgene Corporation Substituted 4-aminoisoindoline-1,3-dione compounds and their use for treating lymphoma
US20190375732A1 (en) 2018-05-14 2019-12-12 David Hung Anti-cancer nuclear hormone receptor-targeting compounds
EP3578561A1 (en) 2018-06-04 2019-12-11 F. Hoffmann-La Roche AG Spiro compounds
AR116109A1 (es) 2018-07-10 2021-03-31 Novartis Ag Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos
CA3103385A1 (en) 2018-07-10 2020-01-16 Novartis Ag 3-(5-hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and their use in the treatment of ikaros family zinc finger 2 (ikzf2)-dependent diseases
US11730726B2 (en) 2018-07-11 2023-08-22 H. Lee Moffitt Cancer Center And Research Institute, Inc. Dimeric immuno-modulatory compounds against cereblon-based mechanisms
WO2020023851A1 (en) 2018-07-26 2020-01-30 Yale University Bifunctional substitued pyrimidines as modulators of fak proteolyse
EP3831811A4 (en) 2018-07-31 2022-04-20 Fimecs, Inc. HETEROCYCLIC COMPOUND
CN112912376A (zh) 2018-08-20 2021-06-04 阿尔维纳斯运营股份有限公司 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物
US11969472B2 (en) 2018-08-22 2024-04-30 Cullgen (Shanghai), Inc. Tropomyosin receptor kinase (TRK) degradation compounds and methods of use
CA3110267A1 (en) 2018-08-22 2020-02-27 Cullgen (Shanghai), Inc. Tropomyosin receptor kinase (trk) degradation compounds and methods of use
EP3846800A4 (en) 2018-09-04 2022-08-24 C4 Therapeutics, Inc. Compounds for the degradation of brd9 or mth1
CA3119343C (en) * 2018-11-13 2024-01-16 Biotheryx, Inc. Substituted isoindolinones
US11352350B2 (en) 2018-11-30 2022-06-07 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
FI3897636T3 (fi) 2018-12-19 2025-02-03 Celgene Corp Substituoituja 3-((3-aminofenyyli)amino)piperidiini-2,6-dioniyhdisteitä, niiden koostumuksia ja menetelmiä niillä annettavia hoitoja varten
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
CN120698985A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
US20220081435A1 (en) * 2019-01-03 2022-03-17 The Regents Of The University Of Michigan Androgen receptor protein degraders
EP3917526A4 (en) 2019-01-29 2022-11-02 Foghorn Therapeutics Inc. COMPOUNDS AND THEIR USES
EP3917934A4 (en) * 2019-01-29 2023-02-15 Foghorn Therapeutics Inc. Compounds and uses thereof
US11098025B2 (en) 2019-01-30 2021-08-24 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
US11547759B2 (en) 2019-01-30 2023-01-10 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
ES3032659T3 (en) * 2019-02-15 2025-07-23 Novartis Ag 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
ES2982474T3 (es) * 2019-02-15 2024-10-16 Novartis Ag Derivados de 3-(1-oxoisoindolin-2-il)piperidin-1,6-diona sustituidos y usos de estos
AU2020228803B2 (en) * 2019-02-25 2023-05-18 Shanghaitech University Sulfur-containing compound based on glutarimide skeleton and application thereof
US12398139B2 (en) * 2019-03-05 2025-08-26 Centre For Addiction And Mental Health Modulators of AMPA receptor signaling
US20240108747A1 (en) 2019-03-21 2024-04-04 Lonza Sales Ag Extracellular vesicle conjugates and uses thereof
US12233356B2 (en) 2019-03-21 2025-02-25 Lonza Sales Ag Process for preparing extracellular vesicles
CN111747924B (zh) * 2019-03-29 2023-11-10 华东师范大学 一类来那度胺/泊马度胺类似物及其应用
TW202102497A (zh) 2019-03-29 2021-01-16 瑞典商阿斯特捷利康公司 化合物及它們在治療癌症中之用途
WO2020214555A1 (en) 2019-04-16 2020-10-22 Northwestern University Bifunctional compounds comprising apcin-a and their use in the treatment of cancer
CN111825657A (zh) * 2019-04-18 2020-10-27 成都海创药业有限公司 一类靶向降解雄激素受体的双功能嵌合体杂环化合物及其用途
KR20220008869A (ko) 2019-05-14 2022-01-21 누베이션 바이오 인크. 항암 핵 호르몬 수용체-표적화 화합물
CN111944012B (zh) * 2019-05-17 2023-08-29 海创药业股份有限公司 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
KR20220030222A (ko) 2019-05-31 2022-03-10 이케나 온콜로지, 인코포레이티드 Tead 억제제 및 이의 용도
KR20220034739A (ko) 2019-05-31 2022-03-18 이케나 온콜로지, 인코포레이티드 Tead 억제제 및 이의 용도
AU2020281410A1 (en) 2019-05-31 2021-10-07 Haisco Pharmaceuticals Pte. Ltd. BTK inhibitor ring derivative, preparation method therefor and pharmaceutical application thereof
US11912699B2 (en) 2019-07-17 2024-02-27 Arvinas Operations, Inc. Tau-protein targeting compounds and associated
EP4021450B1 (en) 2019-08-26 2025-11-05 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
EP4031247A1 (en) * 2019-09-16 2022-07-27 Novartis AG Bifunctional degraders and their methods of use
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
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
EP4089083A1 (en) * 2019-09-23 2022-11-16 Accutar Biotechnology Inc. Piperidine-2,6-dione substituted isoindoles in the preparation of substituted quinoline-8-carbonitrile derivatives having androgen receptor degradation activity and uses thereof
WO2021069705A1 (en) * 2019-10-09 2021-04-15 Monte Rosa Therapeutics Isoindolinone compounds
AU2020368542B2 (en) 2019-10-17 2024-02-29 Arvinas Operations, Inc. Bifunctional molecules containing an E3 ubiquitine ligase binding moiety linked to a BCL6 targeting moiety
JP7716396B2 (ja) * 2019-10-22 2025-07-31 アルビナス・オペレーションズ・インコーポレイテッド 前立腺癌を治療する方法
CN110790750B (zh) * 2019-11-07 2021-09-21 郑州大学 一种邻苯二甲酰亚胺类选择性雄激素受体降解剂及其制备方法和用途
CN110746400B (zh) * 2019-11-07 2021-12-17 郑州大学 一种靶向雄激素受体的荧光探针及其制备方法
TW202131930A (zh) 2019-11-13 2021-09-01 美商諾維雪碧歐公司 抗癌核荷爾蒙受體標靶化合物
IL293027A (en) 2019-11-19 2022-07-01 Bristol Myers Squibb Co Compounds useful as inhibitors of Helios protein
EP4076464A4 (en) * 2019-12-17 2024-06-12 Orionis Biosciences, Inc. COMPOUNDS FOR MODULATION OF PROTEIN RECRUITMENT AND/OR DEGRADATION
IL293530A (en) 2019-12-18 2022-08-01 Novartis Ag Derivatives of 3-(5-methoxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione and their uses
AU2020405129A1 (en) 2019-12-19 2022-06-23 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
PE20230114A1 (es) * 2019-12-23 2023-01-27 Shanghai Jemincare Pharmaceuticals Co Ltd Metodo y aplicacion de preparacion de compuesto como agente de degradacion de proteinas
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
JP7477076B2 (ja) * 2020-02-25 2024-05-01 シャンハイテック ユニバーシティ グルタルイミド骨格に基づく化合物及びその使用
CN115697989B (zh) 2020-02-26 2025-03-18 上海睿跃生物科技有限公司 原肌球蛋白受体激酶(trk)降解化合物和使用方法
AU2021231898A1 (en) 2020-03-05 2022-10-27 C4 Therapeutics, Inc. Compounds for targeted degradation of BRD9
CN113387930B (zh) * 2020-03-11 2022-07-12 苏州开拓药业股份有限公司 一种双官能化合物及其制备方法和用途
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
MX2022014071A (es) 2020-05-09 2023-01-30 Arvinas Operations Inc Metodos para fabricar un compuesto bifuncional, formas ultrapuras del compuesto bifuncional y formas de dosificacion que comprenden el mismo.
CA3182509A1 (en) * 2020-05-12 2021-11-18 Arvinas Operations, Inc. Methods of treating prostate cancer
WO2021231927A1 (en) * 2020-05-14 2021-11-18 The Regents Of The University Of Michigan Androgen receptor protein degraders with a tricyclic cereblon ligand
WO2021237100A1 (en) 2020-05-21 2021-11-25 Codiak Biosciences, Inc. Methods of targeting extracellular vesicles to lung
CN116082311B (zh) * 2020-06-12 2025-04-25 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
CN113896711A (zh) * 2020-07-06 2022-01-07 北京诺诚健华医药科技有限公司 杂环类免疫调节剂
US20230257365A1 (en) * 2020-07-10 2023-08-17 The Regents Of The University Of Michigan Small molecule androgen receptor protein degraders
WO2022011205A1 (en) * 2020-07-10 2022-01-13 The Regents Of The University Of Michigan Androgen receptor protein degraders
CA3186548A1 (en) * 2020-07-21 2022-01-27 Song Hee Lee Compound for androgen receptor degradation, and pharmaceutical use thereof
EP4192460A4 (en) * 2020-08-04 2024-10-23 Oric Pharmaceuticals, Inc. USES OF COMBINATIONS OF GLUCOCORTICOID RECEPTOR (GR) ANTAGONIST AND ANDROGEN RECEPTOR (AR) DEGRADING AGENT
JP2023538517A (ja) 2020-08-05 2023-09-08 シーフォー セラピューティクス， インコーポレイテッド Ｒｅｔの標的分解のための化合物
EP4204418A1 (en) 2020-08-28 2023-07-05 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
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
EP4211128A1 (en) 2020-09-14 2023-07-19 Arvinas Operations, Inc. Crystalline forms of a compound for the targeted degradation of estrogen receptor
CN114181196A (zh) * 2020-09-14 2022-03-15 海思科医药集团股份有限公司 一种抑制并降解parp酶的化合物及其制备方法和药学上的应用
CN114181277A (zh) * 2020-09-15 2022-03-15 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
EP4217352A4 (en) 2020-09-23 2024-04-10 St. Jude Children's Research Hospital, Inc. Substituted n-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)arylsulfonamide analogs as modulators of cereblon protein
WO2022066928A2 (en) 2020-09-23 2022-03-31 Codiak Biosciences, Inc. Process for preparing extracellular vesicles
KR20230111615A (ko) * 2020-10-21 2023-07-25 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체 단백질의 표적화된 분해를 위한 화합물 및 방법
WO2022099117A1 (en) 2020-11-06 2022-05-12 Prelude Therapeutics Incorporated Brm targeting compounds and associated methods of use
EP4240733A1 (en) * 2020-11-06 2023-09-13 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor and associated methods of use
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
CN114262319B (zh) * 2020-12-01 2023-05-05 南昌奥瑞药业有限公司 一类双功能分子、其制备方法及其应用
WO2022120355A1 (en) * 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead degraders and uses thereof
MX2023006883A (es) 2020-12-11 2023-06-23 Arvinas Operations Inc Metodos para tratar el cancer de prostata.
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
WO2022152821A1 (en) 2021-01-13 2022-07-21 Monte Rosa Therapeutics Ag Isoindolinone compounds
JP2024506656A (ja) 2021-02-15 2024-02-14 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋ４分解剤およびその使用
WO2022187423A1 (en) * 2021-03-03 2022-09-09 The Regents Of The University Of Michigan Cereblon ligands
US20240190874A1 (en) * 2021-03-03 2024-06-13 The Regents Of The University Of Michigan Small molecule degraders of androgen receptor
CN116940568A (zh) * 2021-03-17 2023-10-24 南京明德新药研发有限公司 呋喃稠环取代的戊二酰亚胺类化合物
BR112023018973A2 (pt) * 2021-03-19 2023-12-12 Arvinas Operations Inc Compostos à base de indazol e métodos associados de uso
BR112023019420A2 (pt) 2021-03-23 2023-10-24 Nuvation Bio Inc Compostos de direcionamento ao receptor de hormônio nuclear anticâncer
RS66982B1 (sr) 2021-04-06 2025-07-31 Bristol Myers Squibb Co Piridinil supstituisana oksoizoindolinska jedinjenja
EP4323352A1 (en) 2021-04-16 2024-02-21 Arvinas Operations, Inc. Modulators of bcl6 proteolysis and associated methods of use
CA3209633A1 (en) * 2021-04-29 2022-11-03 Tinghu Zhang Phthalimido cereblon complex binders and transcription factor degraders and methods of use
EP4334314A1 (en) 2021-05-03 2024-03-13 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
CA3217417A1 (en) 2021-05-05 2022-11-10 Kevin M. Guckian Compounds for targeting degradation of bruton's tyrosine kinase
US12097261B2 (en) 2021-05-07 2024-09-24 Kymera Therapeutics, Inc. CDK2 degraders and uses thereof
WO2022251588A1 (en) * 2021-05-27 2022-12-01 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and methods of treating disease
AR126052A1 (es) 2021-06-03 2023-09-06 Novartis Ag Derivados de 3-(5-oxi)-1-oxoisoindolin-2-il)piperidina-2,6-diona y sus usos
WO2022270994A1 (ko) 2021-06-25 2022-12-29 한국화학연구원 유비퀴틴 프로테오좀 경로를 통해 비티케이 분해작용을 가지는 신규한 이작용성 헤테로사이클릭 화합물과 이의 용도
US20250018046A1 (en) 2021-07-07 2025-01-16 Biogen Ma Inc Compounds for targeting degradation of irak4 proteins
AU2022308734A1 (en) 2021-07-07 2024-02-22 Biogen Ma Inc. Compounds for targeting degradation of irak4 proteins
WO2023283425A1 (en) 2021-07-09 2023-01-12 Plexium, Inc. Aryl compounds and pharmaceutical compositions that modulate ikzf2
PT4367118T (pt) 2021-08-18 2025-04-16 Gilead Sciences Inc Degradadores bifuncionais de quinases associadas ao recetor de interleucina-1 e sua utilização terapêutica
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
WO2023034411A1 (en) 2021-09-01 2023-03-09 Oerth Bio Llc Compositions and methods for targeted degradation of proteins in a plant cell
CN115772210A (zh) * 2021-09-08 2023-03-10 苏州开拓药业股份有限公司 硫代乙内酰脲化合物或其药用盐的无定形物、晶体、药物组合物、制备方法和用途
CN113861186B (zh) * 2021-09-10 2023-08-25 浙江师范大学 基于异恶唑取代苯甲酰胺类衍生物及抗前列腺癌药物应用
CN113620931B (zh) * 2021-09-13 2023-06-09 中国海洋大学 一种雄激素受体抑制剂及其用途
US11981672B2 (en) 2021-09-13 2024-05-14 Montelino Therapeutics Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
US20240376118A1 (en) * 2021-09-13 2024-11-14 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
US20240382603A1 (en) * 2021-09-13 2024-11-21 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
JPWO2023063351A1 (enExample) 2021-10-15 2023-04-20
EP4421071A1 (en) * 2021-10-22 2024-08-28 Gluetacs Therapeutics (Shanghai) Co., Ltd. Crbn e3 ligase ligand compound, protein degrading agent developed on the basis of ligand compound, and their applications
WO2023076556A1 (en) 2021-10-29 2023-05-04 Kymera Therapeutics, Inc. Irak4 degraders and synthesis thereof
WO2023093845A1 (zh) * 2021-11-25 2023-06-01 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
CN115894450B (zh) * 2021-11-30 2023-09-12 山东如至生物医药科技有限公司 一种新型多环类化合物及其组合物和用途
KR20240148007A (ko) * 2021-12-08 2024-10-10 글루탁스 테라퓨틱스 (상하이) 씨오., 엘티디. E3 유비퀴틴 리가제 리간드 (ubiquitin ligase ligand) 화합물, 이 리간드 화합물을 기초로 하여 개발된 단백질 분해제 및 이들의 응용
TW202346281A (zh) 2022-01-21 2023-12-01 瑞典商阿斯特捷利康公司 化合物以及它們在治療癌症中之用途
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
KR20230140396A (ko) 2022-03-23 2023-10-06 주식회사 대웅테라퓨틱스 핵 수용체의 저해 또는 분해를 유도하는 신규 화합물
EP4499628A1 (en) 2022-03-24 2025-02-05 GlaxoSmithKline Intellectual Property Development Limited 2,4-dioxotetrahydropyrimidinyl derivatives as degrons in protacs
EP4499064A1 (en) 2022-03-25 2025-02-05 Shenzhen Pharmacin Co., Ltd. Pharmaceutical compositions of protac compounds and uses thereof
WO2023193760A1 (en) * 2022-04-06 2023-10-12 Cullgen (Shanghai) , Inc. Compounds and methods of treating cancers
TW202404643A (zh) 2022-04-20 2024-02-01 大陸商同宜醫藥（蘇州）有限公司 化合物及用途
US20250248999A1 (en) 2022-04-21 2025-08-07 Arvinas Operations, Inc. Bavdegalutamide and combinations thereof for use in treating prostate cancer
IL316803A (en) 2022-06-06 2025-01-01 C4 Therapeutics Inc Bicyclic glutarimide-modified cervalon-binding agents
WO2023242598A1 (en) * 2022-06-16 2023-12-21 Amphista Therapeutics Limited Bifunctional molecules for targeted protein degradation
CA3257448A1 (en) * 2022-06-30 2024-01-04 Bristol Myers Squibb Co WEE1 DEGRADATION COMPOUNDS AND THEIR USES
TWI893405B (zh) * 2022-06-30 2025-08-11 安宏生醫股份有限公司 雙官能基化合物及包含該雙官能基化合物之醫藥組成物，及其用於製備治療雄激素受體相關疾病之藥物的用途
WO2024012570A1 (zh) * 2022-07-15 2024-01-18 西藏海思科制药有限公司 一种含氮杂环衍生物及其组合物和药学上的应用
AU2023308934A1 (en) * 2022-07-20 2025-01-09 Alessa Therapeutics, Inc. Drug implants containing darolutamide and methods of use thereof
CN115475164B (zh) * 2022-08-22 2024-06-04 西安交通大学 一种可降解PDGFR-β的蛋白降解靶向嵌合体及其制备方法和应用
WO2024050016A1 (en) 2022-08-31 2024-03-07 Oerth Bio Llc Compositions and methods for targeted inhibition and degradation of proteins in an insect cell
TW202432544A (zh) 2022-09-07 2024-08-16 美商亞文納營運公司 快速加速纖維肉瘤降解化合物及相關使用方法
WO2024054952A1 (en) * 2022-09-08 2024-03-14 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and methods of treating disease
WO2024054954A1 (en) * 2022-09-08 2024-03-14 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and methods of treating disease
CN119546595A (zh) * 2022-09-14 2025-02-28 上海齐鲁制药研究中心有限公司 萘并呋喃取代的戊二酰亚胺类化合物的晶型、制备方法及其应用
WO2024073507A1 (en) 2022-09-28 2024-04-04 Theseus Pharmaceuticals, Inc. Macrocyclic compounds and uses thereof
WO2024102810A1 (en) 2022-11-08 2024-05-16 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
EP4634184A1 (en) 2022-12-14 2025-10-22 Crossfire Oncology Holding B.V. Bifunctional compounds for degrading kinases via ubiquitin proteosome pathway
TW202444727A (zh) 2023-01-26 2024-11-16 美商艾維納斯手術有限公司 基於cereblon之kras降解protac及其相關用途
KR20250154418A (ko) 2023-03-10 2025-10-28 아스트라제네카 아베 안드로겐 수용체를 분해할 수 있는 이작용성 화합물
WO2024201244A1 (en) 2023-03-24 2024-10-03 Assia Chemical Industries Ltd. Solid state forms of bavdegalutamide and process for preparation thereof
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
WO2024243441A1 (en) 2023-05-24 2024-11-28 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
WO2024246838A1 (en) 2023-05-31 2024-12-05 Beigene Switzerland Gmbh Compounds for the degradation of egfr kinase
WO2025007000A1 (en) 2023-06-30 2025-01-02 Kumquat Biosciences Inc. Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors
WO2025011623A1 (zh) * 2023-07-12 2025-01-16 上海壹迪生物技术有限公司 氰基喹啉类靶向蛋白降解分子、其制备方法和应用
WO2025049555A1 (en) 2023-08-31 2025-03-06 Oerth Bio Llc Compositions and methods for targeted inhibition and degradation of proteins in an insect cell
WO2025085815A1 (en) * 2023-10-20 2025-04-24 Seed Therapeutics Us, Inc. Protac compounds binding keap1 ubiquitin ligase for targeted protein degradation
WO2025083472A2 (en) * 2023-10-20 2025-04-24 Seed Therapeutics Us, Inc. Protac compounds binding keap1 ubiquitin ligase for targeted protein degradation
WO2025096855A1 (en) 2023-11-02 2025-05-08 Kumquat Biosciences Inc. Degraders and uses thereof
WO2025108404A1 (zh) * 2023-11-22 2025-05-30 广东东阳光药业股份有限公司 一种靶向降解雄激素受体的双功能嵌合体的杂环化合物及其用途
WO2025114875A1 (en) 2023-12-01 2025-06-05 Astrazeneca Ab Er degraders and uses thereof
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
WO2025126115A1 (en) 2023-12-13 2025-06-19 Beigene Switzerland Gmbh Degradation of irak4 by conjugation of irak4 inhibitors with e3 ligase ligands and methods of use
CN120677157A (zh) * 2024-01-18 2025-09-19 海创药业股份有限公司 一种制备雄激素受体靶向降解化合物及其盐的方法
CN118084737A (zh) * 2024-04-07 2024-05-28 江苏工程职业技术学院 4-(1-((叔丁氧基羰基)氨基)环丁基)苯甲酸的合成方法
WO2025226797A1 (en) * 2024-04-24 2025-10-30 Genentech, Inc. Kred catalyzed ketoreduction of a cyclobutanone carbamic ester
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 (105)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1226974A (en) * 1916-06-06 1917-05-22 August H Jahn Cut-out for gas-engines.
US1818885A (en) * 1930-05-31 1931-08-11 Pettibone Mulliken Company Split-switch structure
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
JP3241875B2 (ja) * 1993-06-25 2001-12-25 新東工業株式会社 加飾体の貼着方法
PL195916B1 (pl) 1996-07-24 2007-11-30 Celgene Corp Izomery optyczne podstawionej 1-okso-izoindoliny i 1,3-diokso-izoindoliny, kompozycje farmaceutyczne je zawierające oraz ich zastosowanie
JP4903922B2 (ja) 1997-05-14 2012-03-28 スローン − ケッタリング インスティチュート フォー キャンサー リサーチ 選択された蛋白質を分解する複合化合物
HUP0100397A3 (en) 1997-12-17 2002-10-28 Merck & Co Inc Tetrahydro- or octahydrobenzonaphtyridin and quinolin derivatives, pharmaceutical compositions thereof and process for their preparation
US6306663B1 (en) 1999-02-12 2001-10-23 Proteinex, Inc. Controlling protein levels in eucaryotic organisms
AU769652B2 (en) 1999-05-05 2004-01-29 Cubist Pharmaceuticals, Inc. Novel prolines as antimicrobial agents
AU8821301A (en) 2000-06-28 2002-01-08 Bristol Myers Squibb Co 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
US20030045552A1 (en) 2000-12-27 2003-03-06 Robarge Michael J. Isoindole-imide compounds, compositions, and uses thereof
US7091353B2 (en) 2000-12-27 2006-08-15 Celgene Corporation 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
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
WO2003000169A1 (fr) 2001-06-20 2003-01-03 Takeda Chemical Industries, Ltd. Procede de fabrication de comprimes
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
MXPA05001536A (es) 2002-08-30 2005-04-19 Eisai Co Ltd Derivados aromaticos que contienen nitrogeno.
MXPA06015169A (es) 2004-07-08 2007-08-21 Warner Lambert Co Moduladores de androgenos.
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
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
CA2643267A1 (en) 2006-03-03 2007-09-20 Novartis Ag N-formyl hydroxylamine compounds
CA2648139A1 (en) 2006-03-29 2007-11-08 The Regents Of The University Of California Diaryl thiohydantoin compounds and their use in the treatment of hyperproliferative disorders
AU2007275415A1 (en) 2006-07-20 2008-01-24 Ligand Pharmaceuticals Incorporated Proline urea CCR1 antagonists for the treatment of autoimmune diseases or inflammation
RU2448101C2 (ru) 2006-08-30 2012-04-20 Селджин Корпорейшн 5-замещенные изоиндолиновые соединения
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.
US8877780B2 (en) 2006-08-30 2014-11-04 Celgene Corporation 5-substituted isoindoline compounds
EP2089391B1 (en) 2006-11-03 2013-01-16 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
KR20100051808A (ko) 2007-07-31 2010-05-18 앤드로사이언스 코포레이션 안드로겐 수용체 분해 강화제를 포함한 조성물 및 탈모와 피부질환의 예방 또는 치료 방법
PE20140963A1 (es) * 2008-10-29 2014-08-06 Celgene Corp Compuestos de isoindolina para el tratamiento de cancer
US8614201B2 (en) 2009-06-05 2013-12-24 Janssen Pharmaceutica Nv Heterocyclic amides as modulators of TRPA1
WO2011008260A2 (en) 2009-07-13 2011-01-20 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
SG10201501062SA (en) 2010-02-11 2015-04-29 Celgene Corp Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
AU2011272860A1 (en) 2010-06-30 2013-02-07 Brandeis University Small-molecule-targeted protein degradation
CN103261169A (zh) 2010-09-24 2013-08-21 密歇根大学董事会 脱泛素酶抑制剂及其应用方法
EP2649099A4 (en) 2010-12-07 2016-10-19 Univ Yale SMALL MOLECULAR HYDROPHOBIC LABELING OF FUSION PROTEINS AND INDUCED REMOVAL FROM THIS
US20140243282A1 (en) 2010-12-31 2014-08-28 Satish Reddy Kallam Methods and compositions for designing novel conjugate therapeutics
CA2831338C (en) 2011-04-21 2018-07-17 Orion Corporation Androgen receptor modulating carboxamides
CN103688176A (zh) 2011-04-29 2014-03-26 细胞基因公司 利用cereblon作为预报因子治疗癌和炎性疾病的方法
WO2013106646A2 (en) * 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
KR102438072B1 (ko) 2012-01-12 2022-08-31 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
US20140079636A1 (en) * 2012-04-16 2014-03-20 Dinesh U. Chimmanamada Targeted therapeutics
EP2846784A4 (en) 2012-05-11 2016-03-09 Univ Yale COMPOUNDS FOR PROMOTING PROTEIN REMOVAL AND PROCESS THEREFOR
EP2874997A4 (en) 2012-07-19 2016-01-06 Univ Drexel NEW SIGMA RECEPTOR LIGANDS AND METHOD FOR REGULATING CELLULAR PROTEIN HOMEOSTASIS THEREWITH
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
WO2015038649A1 (en) * 2013-09-10 2015-03-19 Synta Pharmaceuticals Corp. Targeted therapeutics
IN2014MU00303A (enExample) 2014-01-28 2015-09-11 Cipla Ltd
CA2941618A1 (en) * 2014-03-03 2015-09-11 Synta Pharmaceuticals Corp. Targeted therapeutics
US20160058872A1 (en) 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
KR20250127179A (ko) * 2014-04-14 2025-08-26 아비나스 오퍼레이션스, 인코포레이티드 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법
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
PT3220891T (pt) 2014-11-21 2019-10-31 Biohaven Pharm Holding Co Ltd Formulação sublingual de riluzol
US9845291B2 (en) * 2014-12-18 2017-12-19 Genentech, Inc. Estrogen receptor modulators and uses thereof
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
US11352351B2 (en) * 2015-01-20 2022-06-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
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
HK1249058A1 (zh) 2015-03-18 2018-10-26 Arvinas, Inc. 用於增强靶向蛋白质降解的化合物和方法
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
WO2016197032A1 (en) * 2015-06-04 2016-12-08 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
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
CA2988430A1 (en) * 2015-07-10 2017-01-19 Arvinas, Inc. Mdm2-based modulators of proteolysis and associated methods of use
RU2018105094A (ru) 2015-07-13 2019-08-14 Арвинас, Инк. Модуляторы протеолиза на основе аланина и связанные с ними способы применения
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
CN108366992A (zh) 2015-11-02 2018-08-03 耶鲁大学 蛋白水解靶向嵌合体化合物及其制备和应用方法
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
KR102447884B1 (ko) 2016-04-21 2022-09-27 바이오벤처스, 엘엘씨 항-세포자멸적 bcl-2 계열 단백질의 열화를 유도하는 화합물 및 이의 용도
US10865204B2 (en) * 2016-04-22 2020-12-15 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
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
WO2017197056A1 (en) * 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Bromodomain targeting degronimers for target protein degradation
EP3455218A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
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
HUE070289T2 (hu) * 2016-10-11 2025-05-28 Arvinas Operations Inc Vegyületek és módszerek az androgénreceptor célzott lebontására
EP3544957B1 (en) 2016-11-22 2024-05-29 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
WO2020047487A1 (en) 2018-08-31 2020-03-05 The Regents Of The University Of California Methods for treating cancer with rorgamma inhibitors and statins
CN111825657A (zh) 2019-04-18 2020-10-27 成都海创药业有限公司 一类靶向降解雄激素受体的双功能嵌合体杂环化合物及其用途
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
JP7716396B2 (ja) * 2019-10-22 2025-07-31 アルビナス・オペレーションズ・インコーポレイテッド 前立腺癌を治療する方法
MX2022014071A (es) * 2020-05-09 2023-01-30 Arvinas Operations Inc Metodos para fabricar un compuesto bifuncional, formas ultrapuras del compuesto bifuncional y formas de dosificacion que comprenden el mismo.
CA3182509A1 (en) 2020-05-12 2021-11-18 Arvinas Operations, Inc. Methods of treating prostate cancer
KR20230111615A (ko) * 2020-10-21 2023-07-25 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체 단백질의 표적화된 분해를 위한 화합물 및 방법
EP4240733A1 (en) 2020-11-06 2023-09-13 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor and associated methods of use
MX2023006883A (es) 2020-12-11 2023-06-23 Arvinas Operations Inc Metodos para tratar el cancer de prostata.
US20250248999A1 (en) 2022-04-21 2025-08-07 Arvinas Operations, Inc. Bavdegalutamide and combinations thereof for use in treating prostate cancer

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