LT3660004T - Junginiai ir metodai, skirti tikslinei androgeno receptoriaus degradacijai - Google Patents

Junginiai ir metodai, skirti tikslinei androgeno receptoriaus degradacijai

Info

Publication number
LT3660004T
LT3660004T LTEP20150564.1T LT20150564T LT3660004T LT 3660004 T LT3660004 T LT 3660004T LT 20150564 T LT20150564 T LT 20150564T LT 3660004 T LT3660004 T LT 3660004T
Authority
LT
Lithuania
Prior art keywords
compounds
methods
androgen receptor
receptor degradation
targeted
Prior art date
Application number
LTEP20150564.1T
Other languages
English (en)
Inventor
Andrew P. Crew
Keith R. Hornberger
Lawrence B. Snyder
Kurt Zimmermann
Jing Wang
Michael Berlin
Craig M. Crews
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 LT3660004T publication Critical patent/LT3660004T/lt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • 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
    • C07D211/76—Oxygen atoms attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07—ORGANIC CHEMISTRY
    • 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
    • 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
    • C07D401/02—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
    • 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

Landscapes

  • 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)
LTEP20150564.1T 2016-10-11 2017-10-11 Junginiai ir metodai, skirti tikslinei androgeno receptoriaus degradacijai LT3660004T (lt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662406888P 2016-10-11 2016-10-11
US201762528385P 2017-07-03 2017-07-03

Publications (1)

Publication Number Publication Date
LT3660004T true LT3660004T (lt) 2023-06-12

Family

ID=61830620

Family Applications (2)

Application Number Title Priority Date Filing Date
LTEPPCT/US2017/056234T LT3526202T (lt) 2016-10-11 2017-10-11 Junginiai ir metodai, skirti tiksliniam androgenų receptoriaus skaidymui
LTEP20150564.1T LT3660004T (lt) 2016-10-11 2017-10-11 Junginiai ir metodai, skirti tikslinei androgeno receptoriaus degradacijai

Family Applications Before (1)

Application Number Title Priority Date Filing Date
LTEPPCT/US2017/056234T LT3526202T (lt) 2016-10-11 2017-10-11 Junginiai ir metodai, skirti tiksliniam androgenų receptoriaus skaidymui

Country Status (23)

Country Link
US (8) US10584101B2 (lt)
EP (3) EP4509184A3 (lt)
JP (6) JP7009466B2 (lt)
KR (3) KR102789883B1 (lt)
CN (2) CN111892577B (lt)
AU (6) AU2017341723B2 (lt)
CA (1) CA3038979A1 (lt)
CO (1) CO2019003642A2 (lt)
CY (1) CY1126053T1 (lt)
DK (2) DK3526202T3 (lt)
ES (2) ES3023040T3 (lt)
FI (2) FI3660004T3 (lt)
HR (2) HRP20250181T1 (lt)
HU (2) HUE061847T2 (lt)
IL (4) IL283761B2 (lt)
LT (2) LT3526202T (lt)
MX (3) MX2019004278A (lt)
PL (2) PL3526202T3 (lt)
PT (2) PT3660004T (lt)
RS (2) RS64208B1 (lt)
SI (2) SI3526202T1 (lt)
SM (1) SMT202300152T1 (lt)
WO (1) WO2018071606A1 (lt)

Families Citing this family (228)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106458993B (zh) * 2014-04-14 2025-08-29 阿尔维纳斯运营股份有限公司 基于酰亚胺的蛋白水解调节剂和相关使用方法
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, 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
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
CA2988430A1 (en) 2015-07-10 2017-01-19 Arvinas, Inc. Mdm2-based modulators of proteolysis and associated methods of use
WO2017030814A1 (en) 2015-08-19 2017-02-23 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
MX394516B (es) 2016-03-16 2025-03-24 H Lee Moffitt Cancer Ct & Res Moléculas pequeñas contra cereblon para mejorar la función efectora de los linfocitos t.
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
CN120887906A (zh) 2016-05-10 2025-11-04 C4医药公司 用于靶蛋白降解的螺环降解决定子体
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
EP3454856B1 (en) 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
CN109790143A (zh) 2016-05-10 2019-05-21 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
WO2018033135A1 (en) 2016-08-19 2018-02-22 Beigene, Ltd. Use of a combination comprising a btk inhibitor for treating cancers
WO2018053354A1 (en) 2016-09-15 2018-03-22 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
KR102789883B1 (ko) * 2016-10-11 2025-04-01 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적 분해용 화합물 및 방법
WO2018102067A2 (en) 2016-11-01 2018-06-07 Arvinas, Inc. Tau-protein targeting protacs and associated methods of use
IL266842B (en) * 2016-12-01 2022-09-01 Arvinas Operations Inc History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
RU2019121527A (ru) 2016-12-23 2021-01-15 Эрвинэс Оперейшнс, Инк. Химерные молекулы, нацеливающиеся на протеолиз egfr, и связанные с ними способы применения
US10806737B2 (en) 2016-12-23 2020-10-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
US10723717B2 (en) 2016-12-23 2020-07-28 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
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
WO2018140809A1 (en) 2017-01-26 2018-08-02 Arvinas, Inc. Modulators of estrogen receptor proteolysis and associated methods of use
BR112019015484A2 (pt) 2017-01-31 2020-04-28 Arvinas Operations Inc ligantes de cereblon e compostos bifuncionais compreendendo os mesmos
WO2018237026A1 (en) 2017-06-20 2018-12-27 C4 Therapeutics, Inc. N / O-LINKED DEGRONS AND DEGRONIMERS FOR DEGRADATION OF PROTEINS
WO2019001417A1 (en) 2017-06-26 2019-01-03 Beigene, Ltd. IMMUNOTHERAPY FOR HEPATOCELLULAR CARCINOMA
TWI791552B (zh) 2017-07-10 2023-02-11 美商西建公司 抗增生化合物及其使用方法
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
WO2019043217A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROBENZIMIDAZOLONES
WO2019043208A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROQUINOLINONES
EP3710002A4 (en) 2017-11-16 2021-07-07 C4 Therapeutics, Inc. DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION
WO2019099926A1 (en) 2017-11-17 2019-05-23 Arvinas, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides
CN111801334B (zh) 2017-11-29 2023-06-09 百济神州瑞士有限责任公司 使用包含btk抑制剂的组合治疗惰性或侵袭性b-细胞淋巴瘤
JP2021512153A (ja) 2018-01-26 2021-05-13 イエール ユニバーシティ タンパク質分解のイミド系モジュレーターおよび使用方法
US11028088B2 (en) 2018-03-10 2021-06-08 Yale University Modulators of BTK proteolysis and methods of use
CN118754858A (zh) 2018-03-26 2024-10-11 诺华股份有限公司 N-(3-(7H-吡咯并[2,3-d]嘧啶-4-基)苯基)苯甲酰胺衍生物
CN111902141A (zh) 2018-03-26 2020-11-06 C4医药公司 用于ikaros降解的羟脑苷脂结合剂
US12539292B2 (en) 2018-04-01 2026-02-03 Arvinas Operations, Inc. BRM targeting compounds and associated methods of use
KR20210006356A (ko) 2018-04-04 2021-01-18 아비나스 오퍼레이션스, 인코포레이티드 단백질분해 조절제 및 연관된 사용 방법
AU2019251151B2 (en) * 2018-04-09 2022-07-07 Shanghaitech University Target protein degradation compounds, their anti-tumor use, their intermediates and use of intermediates
EP3774772A1 (en) * 2018-04-13 2021-02-17 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same
CN119751456A (zh) 2018-04-16 2025-04-04 C4医药公司 螺环化合物
AU2019261273B2 (en) 2018-04-23 2023-03-09 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
ES2963694T3 (es) 2018-07-10 2024-04-01 Novartis Ag Derivados de 3-(5-hidroxi-1-oxoisoindolin-2-il)piperidin-2,6-diona y su uso en el tratamiento de enfermedades dependientes de la proteína con dedos de cinc 2 de la familia ikaros (ikzf2)
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
EP3820532A4 (en) 2018-07-11 2022-04-06 H. Lee Moffitt Cancer Center & Research Institute, Inc. DIMERE IMMUNOMODULATORY COMPOUNDS AGAINST CEREBLON-BASED MECHANISMS
US20200038513A1 (en) 2018-07-26 2020-02-06 Arvinas Operations, Inc. Modulators of fak proteolysis and associated methods of use
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
MX2021001957A (es) 2018-08-22 2021-07-15 Cullgen Shanghai Inc Compuestos de degradacion y metodos de uso del receptor de tropomiosina quinasa (trk).
EP3846800A4 (en) 2018-09-04 2022-08-24 C4 Therapeutics, Inc. Compounds for the degradation of brd9 or mth1
EP3880669A1 (en) * 2018-11-13 2021-09-22 Biotheryx, Inc. Substituted isoindolinones
US11352350B2 (en) 2018-11-30 2022-06-07 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
BR112021012186A2 (pt) 2018-12-19 2021-08-31 Celgene Corporation Compostos de 3-((3-aminofenil)amino)piperidina-2,6-diona substituídos, composições dos mesmos e métodos de tratamento com os mesmos
CA3124130A1 (en) 2018-12-19 2020-06-25 Celgene Corporation Substituted 3-((3-aminophenyl)amino)piperidine-2,6-dione compounds, compositions thereof, and methods of treatment therewith
WO2020132561A1 (en) 2018-12-20 2020-06-25 C4 Therapeutics, Inc. Targeted protein degradation
US20220081435A1 (en) * 2019-01-03 2022-03-17 The Regents Of The University Of Michigan Androgen receptor protein degraders
US12391686B2 (en) 2019-01-29 2025-08-19 Foghorn Therapeutics Inc. Compounds and uses thereof
US20230065463A1 (en) * 2019-01-29 2023-03-02 Foghorn Therapeutics Inc. Compounds and uses thereof
US11547759B2 (en) 2019-01-30 2023-01-10 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
WO2020160295A1 (en) 2019-01-30 2020-08-06 Montelino Therapeutics, Llc Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
AU2020222345B2 (en) * 2019-02-15 2022-11-17 Novartis Ag 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
JP7488826B2 (ja) * 2019-02-15 2024-05-22 ノバルティス アーゲー 置換３－（１－オキソイソインドリン－２－イル）ピペリジン－２，６－ジオン誘導体及びその使用
EP3932922A4 (en) * 2019-02-25 2022-05-11 ShanghaiTech University SULPHUR-CONTAINING COMPOUND BASED ON A GLUTARIMIDE FRAMEWORK AND ITS USE
CN113891891B (zh) * 2019-03-05 2024-10-11 戒毒及精神健康中心 Ampa受体信号转导的调节剂
CN113557235B (zh) 2019-03-06 2025-08-08 C4医药公司 用于药物治疗的杂环化合物
CN113747925B (zh) 2019-03-21 2024-10-15 隆萨销售股份公司 胞外囊泡缀合物及其用途
EP3941607A1 (en) 2019-03-21 2022-01-26 Codiak BioSciences, Inc. 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
US12414995B2 (en) 2019-04-16 2025-09-16 Northwestern University Bifunctional compounds comprising Apcin-A and their use in the treatment of cancer
CA3137188A1 (en) * 2019-04-18 2020-10-22 Hinova Pharmaceuticals Inc. A class of bifunctional chimeric heterocyclic compounds for targeted degradation of androgen receptors and use thereof
MX2021013774A (es) 2019-05-14 2021-12-10 Nuvation Bio Inc Compuestos anticancerigenos dirigidos a los receptores hormonales nucleares.
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
KR20220016049A (ko) 2019-05-31 2022-02-08 스촨 하이스코 파마수티컬 씨오., 엘티디 Btk 억제제 고리 유도체, 이의 제조 방법 및 이의 약제학적 응용
SG11202113129UA (en) 2019-05-31 2021-12-30 Ikena Oncology Inc Tead inhibitors and uses thereof
CN114502540A (zh) 2019-05-31 2022-05-13 医肯纳肿瘤学公司 Tead抑制剂和其用途
BR112021026517A2 (pt) 2019-06-28 2022-05-10 Kymera Therapeutics Inc Degradadores de irak e usos dos mesmos
WO2021011868A1 (en) 2019-07-17 2021-01-21 Kymera Therapeutics, Inc. Irak degraders and uses thereof
CN119954801A (zh) 2019-07-17 2025-05-09 阿尔维纳斯运营股份有限公司 Tau蛋白靶向化合物及相关使用方法
WO2021023233A1 (zh) 2019-08-05 2021-02-11 上海科技大学 Egfr蛋白降解剂及其抗肿瘤应用
CA3152401A1 (en) 2019-08-26 2021-03-04 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
CN114521196A (zh) * 2019-09-16 2022-05-20 诺华股份有限公司 双官能团降解剂及其使用方法
EP4031241A1 (en) * 2019-09-19 2022-07-27 The Regents Of The University Of Michigan Spirocyclic androgen receptor protein degraders
US11420956B2 (en) * 2019-09-23 2022-08-23 Accutar Biotechnology Inc. Ureas having Androgen Receptor degradation activity and uses thereof
CN113329999B (zh) 2019-09-23 2022-07-01 冰洲石生物科技公司 具有雄激素受体降解活性的新型取代的喹啉-8-甲腈衍生物及其用途
WO2021069705A1 (en) * 2019-10-09 2021-04-15 Monte Rosa Therapeutics Isoindolinone compounds
BR112022007380A2 (pt) 2019-10-17 2022-07-05 Arvinas Operations Inc Composto bifuncional, e, composição
IL292359A (en) * 2019-10-22 2022-06-01 Arvinas Operations Inc Prostate cancer treatment methods
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
US11952349B2 (en) 2019-11-13 2024-04-09 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
MX2022005839A (es) 2019-11-19 2022-06-09 Bristol Myers Squibb Co Compuestos utiles como inhibidores de la proteina helios.
WO2021119159A1 (en) 2019-12-10 2021-06-17 Kymera Therapeutics, Inc. Irak degraders and uses thereof
KR20220145325A (ko) 2019-12-17 2022-10-28 카이메라 쎄라퓨틱스 인코포레이티드 Irak 분해제 및 이의 용도
EP4076464A4 (en) * 2019-12-17 2024-06-12 Orionis Biosciences, Inc. Compounds modulating protein recruitment and/or degradation
JP7682181B2 (ja) 2019-12-18 2025-05-23 ノバルティス アーゲー ３－（５－メトキシ－１－オキソイソインドリン－２－イル）ピペリジン－２，６－ジオン誘導体及びその使用
CR20220353A (es) 2019-12-19 2022-10-20 Arvinas Operations Inc Compuestos y métodos para la degradación dirigida del receptor de andrógenos
CN114829342A (zh) * 2019-12-23 2022-07-29 上海济煜医药科技有限公司 一种蛋白降解剂化合物的制备方法和应用
WO2021155100A1 (en) 2020-01-29 2021-08-05 Foghorn Therapeutics Inc. Compounds and uses thereof
EP4107158A1 (en) 2020-02-19 2022-12-28 Nurix Therapeutics, Inc. Bifunctional degraders of interleukin-1 receptor-associated kinases and therapeutic use thereof
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
EP4112614A4 (en) * 2020-02-25 2023-09-06 Shanghaitech University Glutarimide skeleton-based compounds and application thereof
BR112022016901A2 (pt) 2020-02-26 2022-12-06 Cullgen Shanghai Inc Compostos de degradação do receptor de tropomiosina quinase (trk) e métodos de uso
JP7746278B2 (ja) 2020-03-05 2025-09-30 シーフォー セラピューティクス， インコーポレイテッド Ｂｒｄ９の標的分解のための化合物
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
TW202140441A (zh) 2020-03-23 2021-11-01 美商必治妥美雅史谷比公司 經取代之側氧基異吲哚啉化合物
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
WO2021231174A1 (en) 2020-05-09 2021-11-18 Arvinas Operations, Inc. Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same
EP4149444A1 (en) 2020-05-12 2023-03-22 Arvinas Operations, Inc. Methods of treating prostate cancer
US20230357249A1 (en) * 2020-05-14 2023-11-09 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
BR112022025057A2 (pt) 2020-06-12 2023-01-31 Shanghai Jemincare Pharmaceuticals Co Ltd Composto de ftalazinona e método de preparação do mesmo e uso médico do mesmo
EP4168407A1 (en) 2020-06-19 2023-04-26 C4 Therapeutics, Inc. Braf degraders
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
WO2022011204A1 (en) * 2020-07-10 2022-01-13 The Regents Of The University Of Michigan Small molecule androgen receptor protein degraders
US20230233690A1 (en) * 2020-07-10 2023-07-27 The Regents Of The University Of Michigan Androgen receptor protein degraders
WO2022019597A1 (ko) * 2020-07-21 2022-01-27 주식회사 유빅스테라퓨틱스 안드로겐 수용체 분해용 화합물 및 이들의 의약 용도
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
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
CN116390916A (zh) 2020-09-14 2023-07-04 阿尔维纳斯运营股份有限公司 用于靶向降解雌激素受体的化合物的结晶形式
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
WO2022066928A2 (en) 2020-09-23 2022-03-31 Codiak Biosciences, Inc. Process for preparing extracellular vesicles
JP2023542930A (ja) 2020-09-23 2023-10-12 セント ジュード チルドレンズ リサーチ ホスピタル インコーポレイテッド セレブロンタンパク質のモジュレータとしての置換ｎ－（２－（２，６－ジオキソピペリジン－３－イル）－１，３－ジオキソイソインドリン－５－イル）アリールスルホンアミド類似体
IL302137A (en) 2020-10-21 2023-06-01 Arvinas Operations Inc Compounds and methods for targeted degradation of androgen receptor protein
IL302669A (en) 2020-11-06 2023-07-01 Prelude Therapeutics Inc BRM-targeted compounds and related 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
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
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
KR20230118147A (ko) 2020-12-11 2023-08-10 아비나스 오퍼레이션스, 인코포레이티드 전립선암 치료 방법
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
CA3208313A1 (en) 2021-01-13 2022-07-21 Monte Rosa Therapeutics Ag Isoindolinone compounds
US20240165243A1 (en) 2021-02-10 2024-05-23 Beigene Switzerland Gmbh Egfr degraders and methods of use
US12171768B2 (en) 2021-02-15 2024-12-24 Kymera Therapeutics, Inc. IRAK4 degraders and uses thereof
AU2022220869A1 (en) 2021-02-15 2023-08-24 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof
US20240166647A1 (en) * 2021-03-03 2024-05-23 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
JP7656068B2 (ja) * 2021-03-17 2025-04-02 上海齊魯制藥研究中心有限公司 フラン縮合環置換グルタルイミド系化合物
CA3211347A1 (en) * 2021-03-19 2022-09-22 Erika Araujo Indazole based compounds and associated methods of use
EP4313991A1 (en) 2021-03-23 2024-02-07 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
RS66982B1 (sr) 2021-04-06 2025-07-31 Bristol Myers Squibb Co Piridinil supstituisana oksoizoindolinska jedinjenja
US11986532B2 (en) 2021-04-16 2024-05-21 Arvinas Operations, Inc. Modulators of BCL6 proteolysis and associated methods of use
US20240217970A1 (en) * 2021-04-29 2024-07-04 Dana-Farber Cancer Institute, Inc. Phthalimido cereblon complex binders and transcription factor degraders and methods of use
US12006314B2 (en) 2021-05-03 2024-06-11 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
BR112023023065A2 (pt) 2021-05-05 2024-01-30 Biogen Ma Inc Compostos para direcionar a degradação da tirosina quinase de bruton
IL308314A (en) 2021-05-07 2024-01-01 Kymera Therapeutics Inc CDK2 compounds and their uses
WO2022251588A1 (en) * 2021-05-27 2022-12-01 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and methods of treating disease
WO2022255888A1 (en) * 2021-06-01 2022-12-08 Captor Therapeutics S.A. Targeted protein degradation using bifunctional compounds that bind ubiquitin ligase and target mcl-1 protein
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
US12161722B2 (en) 2021-06-25 2024-12-10 Korea Research Institute Of Chemical Technology Bifunctional heterocyclic compound having BTK degradation function via ubiquitin proteasome pathway, and use thereof
EP4366834A1 (en) 2021-07-07 2024-05-15 Biogen MA Inc. Compounds for targeting degradation of irak4 proteins
CA3224732A1 (en) 2021-07-07 2023-01-12 Kevin M. Guckian Compounds for targeting degradation of irak4 proteins
JP2024529298A (ja) 2021-07-09 2024-08-06 プレキシウム インコーポレイテッド Ｉｋｚｆ２を調節するアリール化合物及び医薬組成物
EP4367118B1 (en) 2021-08-18 2025-01-29 Nurix Therapeutics, Inc. Bifunctional degraders of interleukin-1 receptor-associated kinases and therapeutic use thereof
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
WO2023039604A1 (en) * 2021-09-13 2023-03-16 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
WO2023039602A1 (en) * 2021-09-13 2023-03-16 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
US11981672B2 (en) 2021-09-13 2024-05-14 Montelino Therapeutics Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
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
JPWO2023063351A1 (lt) 2021-10-15 2023-04-20
JP2024539269A (ja) * 2021-10-22 2024-10-28 グルータクス セラピューティクス （シャンハイ） カンパニー、リミテッド Ｃｒｂｎ ｅ３リガーゼリガンド化合物、当該リガンド化合物に基づいて開発したタンパク質分解剤及びそれらの応用
JP2024540080A (ja) 2021-10-29 2024-10-31 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋ４分解剤およびその合成
JP2024543129A (ja) * 2021-11-25 2024-11-19 江蘇恒瑞医薬股▲ふん▼有限公司 アンドロゲン受容体タンパク質の標的分解のためのキメラ化合物、その調製方法及びその医薬的使用
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
CA3240524A1 (en) * 2021-12-08 2023-06-15 Gluetacs Therapeutics (Shanghai) Co., Ltd. E3 ubiquitin ligase ligand compound, protein degrader developed based thereon and their applications
CA3240051A1 (en) 2021-12-30 2023-07-06 Beigene Switzerland Gmbh Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use
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
WO2023143427A1 (zh) * 2022-01-27 2023-08-03 杭州领业医药科技有限公司 Arv-110的晶型及其制备方法和用途
KR20230140396A (ko) 2022-03-23 2023-10-06 주식회사 대웅테라퓨틱스 핵 수용체의 저해 또는 분해를 유도하는 신규 화합물
CN119301111A (zh) 2022-03-24 2025-01-10 葛兰素史密斯克莱知识产权发展有限公司 作为protac中的降解决定子的2,4-二氧代四氢嘧啶基衍生物
CN119604285A (zh) 2022-03-25 2025-03-11 深圳市药欣生物科技有限公司 Protac化合物的药物组合物及其用途
CA3247503A1 (en) * 2022-04-06 2023-10-12 Cullgen (Shanghai) , Inc. CANCER COMPOUNDS AND TREATMENT METHODS
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
EP4511034A1 (en) 2022-04-21 2025-02-26 Arvinas Operations, Inc. Bavdegalutamide and combinations thereof for use in treating prostate cancer
JP2025523393A (ja) 2022-06-06 2025-07-23 シーフォー セラピューティクス， インコーポレイテッド 二環式置換グルタルイミドセレブロンバインダー
WO2023242598A1 (en) * 2022-06-16 2023-12-21 Amphista Therapeutics Limited Bifunctional molecules for targeted protein degradation
MA71326A (fr) * 2022-06-30 2025-04-30 Bristol-Myers Squibb Company Composés de dégradation de wee1 et leurs utilisations
US20250197409A1 (en) * 2022-06-30 2025-06-19 Anhorn Medicines Co., Ltd. Bifunctional compound and pharmaceutical composition comprising the bifunctional compound, and method for treating androgen receptor related disease by using the same
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
WO2024020105A1 (en) * 2022-07-20 2024-01-25 The Regents Of The University Of California 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
US11957759B1 (en) 2022-09-07 2024-04-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use
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
EP4588916A4 (en) * 2022-09-14 2025-12-03 Shanghai Qilu Pharmaceutical Res And Development Centre Ltd CRYSTALLINE FORM OF A GLUTARIMIDE COMPOUND SUBSTITUTED BY NAPHTOFURANE, ITS PREPARATION PROCESS AND ITS USE
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
TW202502749A (zh) 2023-03-10 2025-01-16 瑞典商阿斯特捷利康公司 化合物以及其在治療癌症中之用途
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
WO2024240246A1 (zh) 2023-05-24 2024-11-28 江苏恒瑞医药股份有限公司 二氧代哌啶化合物或其可药用盐的无定形物、结晶、制备方法和用途
AU2024276994A1 (en) 2023-05-24 2025-10-23 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
AR132818A1 (es) 2023-05-31 2025-07-30 Beigene Switzerland Gmbh Compuestos para la degradación de la cinasa egfr
TW202502779A (zh) 2023-06-30 2025-01-16 美商金橘生物科技公司 取代的雜芳族胺及其用途
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
CN117263865B (zh) * 2023-08-04 2026-03-27 南开大学 以6,6-二甲基双环[3.1.1]-2-甲胺为疏水基团的蛋白降解剂及其制备方法、药物组合物和应用
CN117126133A (zh) * 2023-08-14 2023-11-28 中国海洋大学 一种化合物及其用途
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
TW202523291A (zh) 2023-11-02 2025-06-16 美商金橘生物科技公司 降解劑及其用途
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
US12496301B2 (en) 2023-12-08 2025-12-16 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
US12558428B2 (en) 2024-03-08 2026-02-24 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and their use in treating disease
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
WO2025235600A1 (en) * 2024-05-07 2025-11-13 Bristol-Myers Squibb Company Processes for the preparation of substituted 3-((3-aminophenyl)amino) piperidine-2,6-dione compounds
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
KR100534498B1 (ko) 1996-07-24 2005-12-08 셀진 코포레이션 치환된 2-(2,6-디옥소피페리딘-3-일)-프탈이미드와 치환된 2-(2,6-디옥소피페리딘-3-일)-1-옥소이소인돌린과 ＴＮＦα농도를 감소시키는 방법
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
ID24955A (id) 1997-12-17 2000-08-31 Merck & Co Inc Antagonis-antagonis reseptor integrin
US6306663B1 (en) 1999-02-12 2001-10-23 Proteinex, Inc. Controlling protein levels in eucaryotic organisms
ATE319446T1 (de) 1999-05-05 2006-03-15 Merck & Co Inc Neue prolinverbindungen als mikrobizide mittel
CZ20024214A3 (cs) * 2000-06-28 2003-04-16 Bristol-Myers Squibb Company Selektivní androgen receptorový modulátor, způsob jeho identifikace, jeho konstrukce a použití
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
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
EP1360205A1 (en) 2001-02-16 2003-11-12 E.I. Dupont De Nemours And Company Angiogenesis-inhibitory tripeptides, compositions and their methods of use
HN2002000136A (es) 2001-06-11 2003-07-31 Basf Ag Inhibidores de la proteasa del virus hiv, compuestos que contienen a los mismos, sus usos farmaceuticos y los materiales para su sintesis
CA2451135C (en) 2001-06-20 2012-10-09 Takeda Chemical Industries, Ltd. Method of manufacturing tablet
DK1423115T3 (da) 2001-08-06 2009-06-15 Childrens Medical Center Nitrogen-substituerede thalidomidanalogers antiangiogenetiske aktivitet
US7030141B2 (en) 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
US20060004029A1 (en) 2002-08-30 2006-01-05 Akihiko Tsuruoka Nitrogen-containing aromatic derivatives
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
JP5578785B2 (ja) 2005-08-31 2014-08-27 セルジーン コーポレイション イソインドール−イミド化合物及びそれを含有する組成物及びそれの使用法
CN101395148A (zh) 2006-03-03 2009-03-25 诺瓦提斯公司 N-甲酰基羟胺化合物
EP2439196A1 (en) 2006-03-29 2012-04-11 The Regents of The University of California Diarylthiohydantoin compounds for use in a method for the treatment of a hyperproliferative disorder
EP2059502A2 (en) 2006-07-20 2009-05-20 Ligand Pharmaceuticals Incorporated Proline urea ccr1 antagonists for the treatment of autoimmune diseases or inflammation
US8877780B2 (en) 2006-08-30 2014-11-04 Celgene Corporation 5-substituted isoindoline compounds
NZ575061A (en) 2006-08-30 2011-10-28 Celgene Corp 5-substituted isoindoline compounds
RU2448101C2 (ru) 2006-08-30 2012-04-20 Селджин Корпорейшн 5-замещенные изоиндолиновые соединения
ES2403546T3 (es) 2006-11-03 2013-05-20 Pharmacyclics, Inc. Sonda de actividad de la tirosina-cinasa de Bruton y procedimiento de utilización
EP2175933B1 (en) 2007-07-25 2012-08-22 Bristol-Myers Squibb Company Triazine kinase inhibitors
WO2009017815A1 (en) 2007-07-31 2009-02-05 Androscience Corporation Compositions including androgen receptor degradation (ard) enhancers and methods of prophylactic or therapeutic treatment of skin disorders and hair loss
ES2662407T3 (es) * 2008-10-29 2018-04-06 Celgene Corporation Compuestos isoindolina para uso en el tratamiento del cáncer
WO2010141805A1 (en) 2009-06-05 2010-12-09 Janssen Pharmaceutica Nv Heterocyclic amides as modulators of trpa1
BR112012000867A2 (pt) 2009-07-13 2019-09-24 Harvard College "polipeptídeos bifuncional costurado e uso do mesmo"
AR078793A1 (es) 2009-10-27 2011-12-07 Orion Corp Derivados de carboxamidas no esteroidales y acil hidrazona moduladores de receptores androgenicos de tejido selectivo (sarm), composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del cancer de prostata entre otros
HUE042011T2 (hu) * 2010-02-11 2019-06-28 Celgene Corp Arilmetoxi-izoindolin-származékok, azok készítményei és alkalmazási módszereik
AU2011272860A1 (en) 2010-06-30 2013-02-07 Brandeis University Small-molecule-targeted protein degradation
AU2011305315A1 (en) 2010-09-24 2013-03-28 The Regents Of The University Of Michigan Deubiquitinase inhibitors and methods for use of the same
WO2012078559A2 (en) 2010-12-07 2012-06-14 Yale University Small-molecule hydrophobic tagging of fusion proteins and induced degradation of same
US20140243282A1 (en) 2010-12-31 2014-08-28 Satish Reddy Kallam Methods and compositions for designing novel conjugate therapeutics
US8921378B2 (en) 2011-04-21 2014-12-30 Orion Corporation Androgen receptor modulating carboxamides
WO2012149299A2 (en) 2011-04-29 2012-11-01 Celgene Corporaiton Methods for the treatment of cancer and inflammatory diseases using cereblon as a predictor
KR102668696B1 (ko) 2012-01-12 2024-05-29 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
WO2013106646A2 (en) 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
US20140079636A1 (en) * 2012-04-16 2014-03-20 Dinesh U. Chimmanamada Targeted therapeutics
WO2013170147A1 (en) 2012-05-11 2013-11-14 Yale University Compounds useful for promoting protein degradation and methods using same
WO2014015157A2 (en) 2012-07-19 2014-01-23 Philadelphia Health & Education Corporation Novel sigma receptor ligands and methods of modulating cellular protein homeostasis using same
GB201311910D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel Compounds
NL2011274C2 (en) 2013-08-06 2015-02-09 Illumicare Ip B V 51 Groundbreaking platform technology for specific binding to necrotic cells.
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
EP3035938B1 (en) * 2013-09-10 2020-08-19 Madrigal Pharmaceuticals, Inc. Targeted therapeutics
IN2014MU00303A (lt) 2014-01-28 2015-09-11 Cipla Ltd
AU2015224576A1 (en) * 2014-03-03 2016-09-22 Madrigal Pharmaceuticals, Inc. Targeted therapeutics
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
US20160058872A1 (en) * 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
CN106458993B (zh) * 2014-04-14 2025-08-29 阿尔维纳斯运营股份有限公司 基于酰亚胺的蛋白水解调节剂和相关使用方法
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
BR112017010423B1 (pt) 2014-11-21 2023-09-26 Biohaven Pharmaceutical Holding Company Ltd. Formulação sublingual de riluzol e uso da mesma
CN107406424B (zh) * 2014-12-18 2020-08-25 豪夫迈·罗氏有限公司 雌激素受体调节剂及其用途
EP3256470B1 (en) 2014-12-23 2023-07-26 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
US9694084B2 (en) * 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, 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
CN108601764A (zh) 2015-03-18 2018-09-28 阿尔维纳斯股份有限公司 用于靶蛋白的增强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
US20170037004A1 (en) 2015-07-13 2017-02-09 Arvinas, Inc. Alanine-based modulators of proteolysis and associated methods of use
WO2017030814A1 (en) 2015-08-19 2017-02-23 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
CA3002709A1 (en) 2015-11-02 2017-05-11 Yale University Proteolysis targeting chimera compounds and methods of preparing and using same
KR101859074B1 (ko) 2016-01-28 2018-05-18 이화여자대학교 산학협력단 신규한 글라이신 아미드 화합물 또는 이의 약학적으로 허용 가능한 염, 이의 제조방법 및 이를 포함하는 소듐 채널 활성 관련 질환의 예방 또는 치료용 약학적 조성물
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
CN109152933B (zh) 2016-04-21 2022-12-02 生物风险投资有限责任公司 诱导抗细胞凋亡bcl-2家族蛋白的降解的化合物及其用途
EP3445765A4 (en) * 2016-04-22 2019-09-18 Dana Farber Cancer Institute, Inc. DECREASE OF CYCLINE-DEPENDENT KINASE 4/6 (CDK4 / 6) BY CONJUGATION OF CDK4 / 6 INHIBITORS WITH E3-LIGASE LIGANDS AND METHODS OF USE
EP3445764B1 (en) * 2016-04-22 2022-06-08 Dana-Farber Cancer Institute, Inc. Degradation of cyclin-dependent kinase 8 (cdk8) by conjugation of cdk8 inhibitors with e3 ligase ligand and methods of use
CN109641874A (zh) 2016-05-10 2019-04-16 C4医药公司 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体
WO2017197056A1 (en) * 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Bromodomain targeting degronimers for target protein degradation
CN109790143A (zh) 2016-05-10 2019-05-21 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
WO2018053354A1 (en) 2016-09-15 2018-03-22 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
KR102789883B1 (ko) * 2016-10-11 2025-04-01 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적 분해용 화합물 및 방법
AU2017363257B2 (en) 2016-11-22 2021-08-19 Dana-Farber Cancer Institute, Inc. Degradation of protein kinases by conjugation of protein kinase inhibitors with E3 ligase ligand and methods of use
FR3064633B1 (fr) 2017-03-28 2019-04-12 Ecole Polytechnique Nouveaux composes de type dithiospirocetals et leur utilisation
KR102746106B1 (ko) 2017-05-01 2024-12-24 에스피지 테라퓨틱스, 인코포레이티드 트리파타이트(tripartite) 안드로겐 수용체 제거제, 그 방법 및 용도
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
CA3137188A1 (en) 2019-04-18 2020-10-22 Hinova Pharmaceuticals Inc. A class of bifunctional chimeric heterocyclic compounds for targeted degradation of androgen receptors and use thereof
US11420956B2 (en) 2019-09-23 2022-08-23 Accutar Biotechnology Inc. Ureas having Androgen Receptor degradation activity and uses thereof
IL292359A (en) * 2019-10-22 2022-06-01 Arvinas Operations Inc Prostate cancer treatment methods
WO2021231174A1 (en) * 2020-05-09 2021-11-18 Arvinas Operations, Inc. Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same
EP4149444A1 (en) 2020-05-12 2023-03-22 Arvinas Operations, Inc. Methods of treating prostate cancer
IL302137A (en) * 2020-10-21 2023-06-01 Arvinas Operations Inc Compounds and methods for targeted degradation of androgen receptor protein
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
KR20230118147A (ko) 2020-12-11 2023-08-10 아비나스 오퍼레이션스, 인코포레이티드 전립선암 치료 방법
EP4511034A1 (en) 2022-04-21 2025-02-26 Arvinas Operations, Inc. Bavdegalutamide and combinations thereof for use in treating prostate cancer

Also Published As

Publication number Publication date
US11964945B2 (en) 2024-04-23
AU2023216887A1 (en) 2023-09-07
JP2020100649A (ja) 2020-07-02
US12077509B2 (en) 2024-09-03
AU2017341723B2 (en) 2021-12-16
RS66647B1 (sr) 2025-04-30
ES2945224T3 (es) 2023-06-29
RS64208B1 (sr) 2023-06-30
EP3660004A1 (en) 2020-06-03
EP3526202A1 (en) 2019-08-21
DK3660004T3 (da) 2023-05-08
SI3660004T1 (sl) 2023-08-31
AU2021204556B2 (en) 2023-06-29
HUE070289T2 (hu) 2025-05-28
IL265806A (en) 2019-06-30
JP2021169481A (ja) 2021-10-28
PL3660004T3 (pl) 2023-10-02
AU2020201792B2 (en) 2020-09-03
IL272523B (en) 2021-07-29
AU2021277645A1 (en) 2021-12-23
LT3526202T (lt) 2025-03-10
US20180099940A1 (en) 2018-04-12
PT3660004T (pt) 2023-05-23
IL283761A (en) 2021-07-29
IL272523A (en) 2020-03-31
IL265806B2 (en) 2025-07-01
PT3526202T (pt) 2025-03-07
CN110506039A (zh) 2019-11-26
US20230331681A1 (en) 2023-10-19
KR20250044800A (ko) 2025-04-01
US10844021B2 (en) 2020-11-24
US11952347B2 (en) 2024-04-09
EP4509184A3 (en) 2025-04-16
US10584101B2 (en) 2020-03-10
KR102173463B1 (ko) 2020-11-04
JP2019530715A (ja) 2019-10-24
KR102789883B1 (ko) 2025-04-01
RU2019113229A (ru) 2020-11-02
MX2019004278A (es) 2019-08-05
HUE061847T2 (hu) 2023-08-28
JP2022046497A (ja) 2022-03-23
EP3526202B1 (en) 2025-01-08
IL318681A (en) 2025-03-01
IL265806B1 (en) 2025-03-01
US11236051B2 (en) 2022-02-01
SI3526202T1 (sl) 2025-04-30
JP2023036887A (ja) 2023-03-14
JP2025026916A (ja) 2025-02-26
IL283761B2 (en) 2023-03-01
IL283761B (en) 2022-11-01
EP3660004B1 (en) 2023-02-22
AU2025242182A1 (en) 2025-10-23
JP7203936B2 (ja) 2023-01-13
HRP20230414T1 (hr) 2023-07-07
US20200095205A1 (en) 2020-03-26
US20250034096A1 (en) 2025-01-30
SMT202300152T1 (it) 2023-07-20
FI3526202T3 (fi) 2025-03-27
US20210040044A1 (en) 2021-02-11
RU2019113229A3 (lt) 2020-11-02
JP7178532B2 (ja) 2022-11-28
JP7590399B2 (ja) 2024-11-26
KR20190055260A (ko) 2019-05-22
AU2020201792A1 (en) 2020-03-26
JP7009466B2 (ja) 2022-02-10
PL3526202T3 (pl) 2025-04-28
CO2019003642A2 (es) 2019-06-19
CN111892577B (zh) 2023-07-07
CY1126053T1 (el) 2023-11-15
MX2022006089A (es) 2022-06-14
CA3038979A1 (en) 2018-04-19
EP3526202A4 (en) 2020-04-29
HRP20250181T1 (hr) 2025-04-11
WO2018071606A1 (en) 2018-04-19
KR20200020978A (ko) 2020-02-26
DK3526202T3 (da) 2025-03-31
FI3660004T3 (fi) 2023-05-04
AU2017341723A1 (en) 2019-04-04
JP6972210B2 (ja) 2021-11-24
CN111892577A (zh) 2020-11-06
EP4509184A2 (en) 2025-02-19
US20210171470A1 (en) 2021-06-10
ES3023040T3 (en) 2025-05-29
MX2022006090A (es) 2022-06-14
AU2021204556A1 (en) 2021-08-05
AU2021277645B2 (en) 2023-06-15
AU2023216887B2 (en) 2025-07-03
US20220259154A1 (en) 2022-08-18
US20210009528A1 (en) 2021-01-14

Similar Documents

Publication Publication Date Title
LT3660004T (lt) Junginiai ir metodai, skirti tikslinei androgeno receptoriaus degradacijai
EP3247708A4 (en) Compounds and methods for the targeted degradation of the androgen receptor
DK3389778T3 (da) Indretning til fotodynamisk behandling
SI3383746T1 (sl) Zapiralna naprava
BR112016027464A2 (pt) aparelho de rede, e método de rede
HUE049175T2 (hu) Eljárás anti-CD79b immunkonjugátumok alkalmazására
EP3192059C0 (en) NOTIFICATION OF FIRST ENTRY
DK3613447T3 (da) Humane pancreas-scaffolds
BR112016022040A2 (pt) aparelho de fixação.
DK3386500T3 (da) Benzothiophen-baserede selektive østrogenreceptor ned-regulatorer
LT3319963T (lt) Pakeistieji 4-azaindolai ir jų, kaip glun2b receptoriaus moduliatorių, panaudojimas
BR112017020495A2 (pt) derivados de oxima carbamoilados e tiocarbamoilados ativos em termos pesticidas.
FI20155870A7 (fi) Langaton melua vaimentava korvatulppa
DK3179695T3 (da) Netværksautentifikation
EP3501234A4 (en) SECURITY PROCEDURE
DE112015001663A5 (de) Stelleinrichtung
EP3444345C0 (en) MICRO-143 RNA DERIVATIVE
BR112016027096A2 (pt) compostos de receptores-alvo de serotonina e métodos
DK3237603T3 (da) Fremgangsmåde til adaptering
EP3448790A4 (en) ADJUSTABLE FISHING POINTS
TH1601000316A (th) อะโกนิสต์ของตัวรับวาโซเพรสซิน-2
GB201611627D0 (en) Losartan hydrobromide
TH1501005269A (th) อนุพันธ์ไดไฮโดรพิริดาซีน-3,5-ไดโอน
ES1139906Y (es) Dispositivo de asiento
ES1135603Y (es) Cobertura anti-aves