HRP20230414T1 - Spojevi i postupci za ciljanu razgradnju androgenog receptora - Google Patents

Spojevi i postupci za ciljanu razgradnju androgenog receptora Download PDF

Info

Publication number
HRP20230414T1
HRP20230414T1 HRP20230414TT HRP20230414T HRP20230414T1 HR P20230414 T1 HRP20230414 T1 HR P20230414T1 HR P20230414T T HRP20230414T T HR P20230414TT HR P20230414 T HRP20230414 T HR P20230414T HR P20230414 T1 HRP20230414 T1 HR P20230414T1
Authority
HR
Croatia
Prior art keywords
inhibitor
image
compound according
compound
anticancer agent
Prior art date
Application number
HRP20230414TT
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 HRP20230414T1 publication Critical patent/HRP20230414T1/hr

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
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/86—Oxygen and sulfur atoms, e.g. thiohydantoin
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

Claims (26)

1. Spoj koji ima strukturu: [image] [image] [image] [image] [image] [image] [image] [image] ili [image] ili farmaceutski prihvatljiva sol, enantiomer, stereoizomer ili izotopni derivat bilo kojeg od prethodno navedenih.
2. Spoj prema zahtjevu 1, naznačen time što ima strukturu: [image] [image] [image] [image] [image] [image] [image] [image] ili [image]
3. Spoj prema zahtjevu 1, naznačen time što ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol, enantiomer, stereoizomer ili izotopni derivat.
4. Spoj prema zahtjevu 1, naznačen time što ima strukturu: [image]
5. Spoj prema zahtjevu 1, naznačen time što ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol, enantiomer, stereoizomer ili izotopni derivat.
6. Spoj prema zahtjevu 1, naznačen time što ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.
7. Spoj prema zahtjevu 1, naznačen time što ima strukturu: [image]
8. Spoj prema zahtjevu 1, naznačen time što ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol, enantiomer, stereoizomer ili izotopni derivat.
9. Spoj prema zahtjevu 1, naznačen time što ima strukturu: [image]
10. Spoj prema zahtjevu 1, naznačen time što ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol, enantiomer, stereoizomer ili izotopni derivat.
11. Spoj prema zahtjevu 1, naznačen time što ima strukturu: [image]
12. Farmaceutski pripravak, naznačen time što sadrži spoj prema bilo kojem od zahtjeva 1-11, i farmaceutski prihvatljiv nosač.
13. Farmaceutski pripravak prema zahtjevu 12, naznačen time što nadalje sadrži učinkovitu količinu dodatnog sredstva protiv raka.
14. Farmaceutski pripravak prema zahtjevu 13, naznačen time što je dodatno sredstvo protiv raka inhibitor FLT-3, inhibitor androgenog receptora, inhibitor VEGFR, inhibitor EGFR TK, inhibitor aurora kinaze, modulator PIK-1, inhibitor Bcl-2, inhibitor HDAC , inhibitor c-MET, inhibitor PARP, inhibitor CDK, anti-HGF protutijelo, inhibitor IGFR TK, inhibitor PI3 kinaze, inhibitor AKT, inhibitor JAK/STAT, inhibitor kontrolne točke 1, inhibitor kontrolne točke 2, inhibitor kinaze žarišne adhezije, inhibitor kinaze MAP , ili protutijelo VEGF klopka.
15. Farmaceutski pripravak prema zahtjevu 13, naznačen time što je dodatno sredstvo protiv raka estramustin, docetaksel, ketokonazol, goserelin acetat, histrelin, buserelin, ciproteron, flutamid, bikalutamid, nilutamid, pamidronat, zolendronat, mitoksantron, pemetreksed, ipilimumab, vorinostat, etopozid, gemcitabin, doksorubicin, vinkristin, temozolomid, kapecitabin, irinotekan označen PEG-om, tamoksifen, anastrazol, eksemestan, letrozol, dietilstilbestrol, estradiol, estrogen, bevacizumab, leuprolid acetat, triptorelin pamoat, medroksiprogesteron acetat, hidroksiprogesteron kaproat, raloksifen, megestrol acetat, karboplatin, cisplatin, dakarbazin, metotreksat, vinblastin, vinorelbin, topotekan, finasterid, arzoksifen, fulvestrant ili prednizon.
16. Farmaceutski pripravak prema zahtjevu 15, naznačen time što: (a) dodatno sredstvo protiv raka je estramustin, docetaksel, ketokonazol, goserelin acetat, histrelin, triptorelin pamoat, buserelin, ciproteron, flutamid, bikalutamid, nilutamid, pamidronat ili zolendronat; ili (b) dodatno sredstvo protiv raka je docetaksel, mitoksantron, estramustin ili leuprolid acetat.
17. Spoj prema bilo kojem od zahtjeva 1-11 ili farmaceutski pripravak prema zahtjevu 12 za upotrebu u liječenju raka prostate kod subjekta.
18. Spoj prema zahtjevu 6 za upotrebu u liječenju raka prostate kod subjekta.
19. Spoj prema zahtjevu 7 za upotrebu u liječenju raka prostate kod subjekta.
20. Spoj ili farmaceutski pripravak za upotrebu prema zahtjevu 17, naznačen time što liječenje nadalje uključuje upotrebu učinkovite količine dodatnog sredstva protiv raka.
21. Spoj za upotrebu prema zahtjevu 18, naznačen time što liječenje nadalje uključuje upotrebu učinkovite količine dodatnog sredstva protiv raka.
22. Spoj za upotrebu prema zahtjevu 19, naznačen time što liječenje nadalje uključuje upotrebu učinkovite količine dodatnog sredstva protiv raka.
23. Spoj ili farmaceutski pripravak za upotrebu prema bilo kojem od zahtjeva 20-22, naznačen time što je dodatno sredstvo protiv raka inhibitor FLT-3, inhibitor androgenog receptora, inhibitor VEGFR, inhibitor EGFR TK, inhibitor aurora kinaze, modulator PIK-1, inhibitor Bcl-2, inhibitor HDAC , inhibitor c-MET, inhibitor PARP, inhibitor CDK, anti-HGF protutijelo, inhibitor IGFR TK, inhibitor PI3 kinaze, inhibitor AKT, inhibitor JAK/STAT, inhibitor kontrolne točke 1, inhibitor kontrolne točke 2, inhibitor kinaze žarišne adhezije, inhibitor kinaze MAP , ili protutijelo VEGF klopka.
24. Spoj ili farmaceutski pripravak za upotrebu prema bilo kojem od zahtjeva 20-22, naznačen time što je dodatno sredstvo protiv raka estramustin, docetaksel, ketokonazol, goserelin acetat, histrelin, buserelin, ciproteron, flutamid, bikalutamid, nilutamid, pamidronat, zolendronat, mitoksantron, pemetreksed, ipilimumab, vorinostat, etopozid, gemcitabin, doksorubicin, vinkristin, temozolomid, kapecitabin, irinotekan označen PEG-om, tamoksifen, anastrazol, eksemestan, letrozol, dietilstilbestrol, estradiol, estrogen, bevacizumab, leuprolid acetat, triptorelin pamoat, medroksiprogesteron acetat, hidroksiprogesteron kaproat, raloksifen, megestrol acetat, karboplatin, cisplatin, dakarbazin, metotreksat, vinblastin, vinorelbin, topotekan, finasterid, arzoksifen, fulvestrant ili prednizon.
25. Spoj ili farmaceutski pripravak za upotrebu prema zahtjevu 24, naznačen time što: (a) dodatno sredstvo protiv raka je estramustin, docetaksel, ketokonazol, goserelin acetat, histrelin, triptorelin pamoat, buserelin, ciproteron, flutamid, bikalutamid, nilutamid, pamidronat ili zolendronat; ili (b) dodatno sredstvo protiv raka je docetaksel, mitoksantron, estramustin ili leuprolid acetat.
26. Farmaceutski pripravak prema bilo kojem od zahtjeva 13-16, naznačen time što se koristi u liječenju raka prostate kod subjekta.
HRP20230414TT 2016-10-11 2017-10-11 Spojevi i postupci za ciljanu razgradnju androgenog receptora HRP20230414T1 (hr)

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
EP20150564.1A EP3660004B1 (en) 2016-10-11 2017-10-11 Compounds and methods for the targeted degradation of androgen receptor

Publications (1)

Publication Number Publication Date
HRP20230414T1 true HRP20230414T1 (hr) 2023-07-07

Family

ID=61830620

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20230414TT HRP20230414T1 (hr) 2016-10-11 2017-10-11 Spojevi i postupci za ciljanu razgradnju androgenog receptora

Country Status (22)

Country Link
US (7) US10584101B2 (hr)
EP (2) EP3660004B1 (hr)
JP (5) JP7009466B2 (hr)
KR (2) KR102173463B1 (hr)
CN (2) CN110506039A (hr)
AU (5) AU2017341723B2 (hr)
CA (1) CA3038979A1 (hr)
CO (1) CO2019003642A2 (hr)
CY (1) CY1126053T1 (hr)
DK (1) DK3660004T3 (hr)
ES (1) ES2945224T3 (hr)
FI (1) FI3660004T3 (hr)
HR (1) HRP20230414T1 (hr)
HU (1) HUE061847T2 (hr)
IL (3) IL283761B2 (hr)
LT (1) LT3660004T (hr)
MX (3) MX2019004278A (hr)
PL (1) PL3660004T3 (hr)
PT (1) PT3660004T (hr)
RS (1) RS64208B1 (hr)
SI (1) SI3660004T1 (hr)
WO (1) WO2018071606A1 (hr)

Families Citing this family (150)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2016209349B2 (en) 2015-01-20 2020-05-07 Arvinas, Inc. Compounds and methods for the targeted degradation of the Androgen Receptor
US20170327469A1 (en) 2015-01-20 2017-11-16 Arvinas, 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
WO2017197036A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Spirocyclic 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
WO2017197055A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
CN110087680B (zh) 2016-08-19 2024-03-19 百济神州有限公司 使用包含btk抑制剂的组合产品治疗癌症
WO2018053354A1 (en) 2016-09-15 2018-03-22 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
AU2017341723B2 (en) * 2016-10-11 2021-12-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
CA3042260C (en) 2016-11-01 2023-10-03 Arvinas, Inc. Tau-protein targeting protacs and associated methods of use
EP3689868B1 (en) 2016-12-01 2023-09-27 Arvinas Operations, Inc. Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
KR102564201B1 (ko) 2016-12-23 2023-08-07 아비나스 오퍼레이션스, 인코포레이티드 급속 진행성 섬유육종 폴리펩티드의 표적화 분해를 위한 화합물 및 방법
RU2019121527A (ru) 2016-12-23 2021-01-15 Эрвинэс Оперейшнс, Инк. Химерные молекулы, нацеливающиеся на протеолиз egfr, и связанные с ними способы применения
EP3559006A4 (en) 2016-12-23 2021-03-03 Arvinas Operations, Inc. COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF FETAL LIVER KINASE POLYPEPTIDES
US11173211B2 (en) 2016-12-23 2021-11-16 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
KR20230140606A (ko) 2017-01-26 2023-10-06 아비나스 오퍼레이션스, 인코포레이티드 에스트로겐 수용체 단백질 분해 조절제 및 관련 사용 방법
CN110769822A (zh) 2017-06-20 2020-02-07 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
EP3645569A4 (en) 2017-06-26 2021-03-24 BeiGene, Ltd. IMMUNOTHERAPY FOR LIVER CELL CARCINOMA
WO2019014100A1 (en) 2017-07-10 2019-01-17 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
CN111315735B (zh) 2017-09-04 2024-03-08 C4医药公司 二氢苯并咪唑酮
CN111278816B (zh) 2017-09-04 2024-03-15 C4医药公司 二氢喹啉酮
CN111278815B (zh) 2017-09-04 2024-03-08 C4医药公司 戊二酰亚胺
EP3710002A4 (en) 2017-11-16 2021-07-07 C4 Therapeutics, Inc. DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION
EP3710443A1 (en) 2017-11-17 2020-09-23 Arvinas Operations, 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
WO2019177902A1 (en) 2018-03-10 2019-09-19 Yale University Modulators of btk proteolysis and methods of use
JP2021519337A (ja) 2018-03-26 2021-08-10 シー４ セラピューティクス， インコーポレイテッド Ｉｋａｒｏｓの分解のためのセレブロン結合剤
KR20210006356A (ko) 2018-04-04 2021-01-18 아비나스 오퍼레이션스, 인코포레이티드 단백질분해 조절제 및 연관된 사용 방법
WO2019196812A1 (zh) * 2018-04-09 2019-10-17 上海科技大学 蛋白降解靶向化合物、其抗肿瘤应用、其中间体及中间体应用
WO2019199816A1 (en) * 2018-04-13 2019-10-17 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2019204354A1 (en) 2018-04-16 2019-10-24 C4 Therapeutics, Inc. Spirocyclic compounds
CN113214220B (zh) 2018-04-23 2024-04-02 细胞基因公司 取代的4-氨基异吲哚啉-1,3-二酮化合物以及它们用于治疗淋巴瘤的用途
EP3578561A1 (en) 2018-06-04 2019-12-11 F. Hoffmann-La Roche AG Spiro compounds
FI3820573T3 (fi) 2018-07-10 2023-11-01 Novartis Ag 3-(5-hydroksi-1-oksoisoindolin-2-yyli)piperidiini-2,6-dionijohdannaisia ja niiden käyttö ikaros-perheen sinkkisormi 2 (ikzf2) -riippuvaisten sairauksien hoidossa
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
KR20210032430A (ko) 2018-07-11 2021-03-24 에이치 리 모피트 캔서 센터 앤드 리서어치 인스티튜트 아이엔씨 세레블론-기반 메커니즘에 대한 이량체 면역-조절 화합물
WO2020023851A1 (en) 2018-07-26 2020-01-30 Yale University Bifunctional substitued pyrimidines as modulators of fak proteolyse
US11639354B2 (en) 2018-07-31 2023-05-02 Fimecs, Inc. Heterocyclic compound
WO2020041331A1 (en) 2018-08-20 2020-02-27 Arvinas Operations, Inc. Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases
US11969472B2 (en) 2018-08-22 2024-04-30 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
JP2022507267A (ja) * 2018-11-13 2022-01-18 バイオセリックス， インコーポレイテッド 置換イソインドリノン
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
KR20210118816A (ko) 2018-12-19 2021-10-01 셀진 코포레이션 치환된 3-((3-아미노페닐)아미노)피페리딘-2,6-디온 화합물, 이의 조성물, 및 이를 사용한 치료 방법
CN113453679A (zh) 2018-12-20 2021-09-28 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
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
CA3124935A1 (en) * 2019-02-15 2020-08-20 Novartis Ag 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
WO2020165834A1 (en) * 2019-02-15 2020-08-20 Novartis Ag Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
WO2020173426A1 (zh) * 2019-02-25 2020-09-03 上海科技大学 基于戊二酰亚胺骨架的含硫化合物及其应用
AU2020231118A1 (en) * 2019-03-05 2021-10-28 Centre For Addiction And Mental Health Modulators of AMPA receptor signaling
EP3941607A1 (en) 2019-03-21 2022-01-26 Codiak BioSciences, Inc. Process for preparing extracellular vesicles
SG11202109587TA (en) 2019-03-21 2021-10-28 Codiak Biosciences Inc Extracellular vesicle conjugates and uses thereof
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
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
WO2020214555A1 (en) 2019-04-16 2020-10-22 Northwestern University Bifunctional compounds comprising apcin-a and their use in the treatment of cancer
JP2022529339A (ja) 2019-04-18 2022-06-21 ヒノバ ファーマシューティカルズ インコーポレイテッド アンドロゲン受容体を標的に分解する二官能性キメラ複素環式化合物及びその使用
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
MX2021014441A (es) 2019-05-31 2022-01-06 Ikena Oncology Inc Inhibidores del dominio asociado mejorador de la transcripcion (tead) y usos de los mismos.
AU2020282757A1 (en) 2019-05-31 2021-12-23 Ikena Oncology, Inc. TEAD inhibitors and uses thereof
CA3133004A1 (en) 2019-05-31 2020-12-03 Sichuan Haisco Pharmaceutical Co., Ltd. Btk inhibitor ring derivative, preparation method therefor and pharmaceutical application thereof
WO2021011913A1 (en) 2019-07-17 2021-01-21 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
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
KR20220079883A (ko) * 2019-09-23 2022-06-14 액큐타 바이오테크놀로지 인코포레이티드 안드로겐 수용체 분해 활성을 갖는 신규한 치환된 퀴놀린-8-탄소수소 유도체 및 이의 용도
EP4045496A1 (en) 2019-10-17 2022-08-24 Arvinas Operations, Inc. Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety
US20210113557A1 (en) * 2019-10-22 2021-04-22 Arvinas Operations, Inc. Methods of treating prostate cancer
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
CA3158976A1 (en) 2019-11-19 2021-05-27 Bristol-Myers Squibb Company Compounds useful as inhibitors of helios protein
UY38986A (es) 2019-12-18 2021-07-30 Novartis Ag Compuestos derivados de 3-(5-metoxi-1-oxoisoindolin-2-il) piperidin-2,6-diona, métodos de usos de los mismos y combinaciones farmacéuticas
AU2020405129A1 (en) 2019-12-19 2022-06-23 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
WO2021129653A1 (zh) 2019-12-23 2021-07-01 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
AU2021226514B2 (en) * 2020-02-25 2023-10-19 Shanghaitech University Glutarimide skeleton-based compounds and application thereof
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
BR112022022753A2 (pt) 2020-05-09 2023-02-14 Arvinas Operations Inc Métodos de fabricação de um composto bifuncional, formas ultrapuras do composto bifuncional e formas de dosagem compreendendo o mesmo
US20210353621A1 (en) * 2020-05-12 2021-11-18 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
PE20230610A1 (es) 2020-06-12 2023-04-13 Shanghai Jemincare Pharmaceuticals Co Ltd Compuesto de ftalazinona, y metodo de preparacion y uso medico de este
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
WO2022011205A1 (en) * 2020-07-10 2022-01-13 The Regents Of The University Of Michigan Androgen receptor protein degraders
JP2023542608A (ja) * 2020-08-04 2023-10-11 オリック ファーマシューティカルズ，インク． グルココルチコイド受容体（ｇｒ）アンタゴニストおよびアンドロゲン受容体（ａｒ）分解誘導剤の組み合わせの使用
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
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
AU2021365850A1 (en) * 2020-10-21 2023-06-08 Arvinas Operations, Inc. Compounds and methods for the 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
WO2022098544A1 (en) * 2020-11-06 2022-05-12 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor and associated methods of use
WO2022111526A1 (zh) * 2020-11-25 2022-06-02 四川海思科制药有限公司 一种苯环衍生物及其组合物和药学上的应用
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
CA3204819A1 (en) 2020-12-11 2022-06-16 Arvinas Operations, Inc. Methods of treating prostate cancer
CA3208313A1 (en) 2021-01-13 2022-07-21 Monte Rosa Therapeutics Ag Isoindolinone compounds
WO2022187419A1 (en) * 2021-03-03 2022-09-09 The Regents Of The University Of Michigan Small molecule degraders of androgen receptor
WO2022187423A1 (en) * 2021-03-03 2022-09-09 The Regents Of The University Of Michigan Cereblon ligands
BR112023018839A2 (pt) * 2021-03-17 2023-12-26 Medshine Discovery Inc Composto de glutarimida substituído por anel fundido com furano
US11834458B2 (en) 2021-03-23 2023-12-05 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
TW202304881A (zh) 2021-04-06 2023-02-01 美商必治妥美雅史谷比公司 經吡啶基取代之側氧基異吲哚啉化合物
BR112023021265A2 (pt) 2021-04-16 2024-02-27 Arvinas Operations Inc Moduladores da proteólise de bcl6 e métodos de uso associados
EP4329746A1 (en) * 2021-04-29 2024-03-06 Dana-Farber Cancer Institute, Inc. Phthalimido cereblon complex binders and transcription factor degraders and methods of use
JP2024516024A (ja) 2021-05-03 2024-04-11 ニューベイション・バイオ・インコーポレイテッド 抗がん核内ホルモン受容体標的化化合物
AU2022268977A1 (en) 2021-05-05 2023-11-30 Biogen Ma Inc. Compounds for targeting degradation of bruton's tyrosine kinase
WO2022251588A1 (en) * 2021-05-27 2022-12-01 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and methods of treating disease
AU2022297176A1 (en) 2021-06-25 2024-01-04 Korea Research Institute Of Chemical Technology Novel bifunctional heterocyclic compound having btk degradation function via ubiquitin proteasome pathway, and use thereof
WO2023283372A1 (en) 2021-07-07 2023-01-12 Biogen Ma Inc. Compounds for targeting degradation of irak4 proteins
KR20240035526A (ko) 2021-07-07 2024-03-15 바이오젠 엠에이 인코포레이티드 Irak4 단백질의 분해를 표적하는 화합물
IL309666A (en) 2021-07-09 2024-02-01 Plexium Inc Aryl compounds and pharmaceutical preparations that modulate IKZF2
US11976071B2 (en) 2021-08-18 2024-05-07 Gilead Sciences, Inc. Substituted pyrrolo[1,2-b]pyridazines as bifunctional degraders of interleukin-1 receptor-associated kinases
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
WO2023039602A1 (en) * 2021-09-13 2023-03-16 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
WO2023039604A1 (en) * 2021-09-13 2023-03-16 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
WO2023063351A1 (ja) 2021-10-15 2023-04-20 国立大学法人筑波大学 情報処理装置、情報処理方法およびプログラム
CN116003418A (zh) * 2021-10-22 2023-04-25 标新生物医药科技(上海)有限公司 Crbn e3连接酶配体化合物、基于该配体化合物开发的蛋白降解剂及它们的应用
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
WO2023104155A1 (zh) * 2021-12-08 2023-06-15 标新生物医药科技(上海)有限公司 E3泛素连接酶配体化合物、基于该配体化合物开发的蛋白降解剂及它们的应用
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
WO2023180388A1 (en) 2022-03-24 2023-09-28 Glaxosmithkline Intellectual Property Development Limited 2,4-dioxotetrahydropyrimidinyl derivatives as degrons in protacs
WO2023193760A1 (en) * 2022-04-06 2023-10-12 Cullgen (Shanghai) , Inc. Compounds and methods of treating cancers
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
WO2023205481A1 (en) 2022-04-21 2023-10-26 Arvinas Operations, Inc. A combination for use in treating prostate cancer comprising arv-100 and abiraterone
WO2023239750A1 (en) * 2022-06-06 2023-12-14 C4 Therapeutics, Inc. Bicyclic-substituted glutarimide cereblon binders
WO2023242598A1 (en) * 2022-06-16 2023-12-21 Amphista Therapeutics Limited Bifunctional molecules for targeted protein degradation
WO2024006881A1 (en) * 2022-06-30 2024-01-04 Bristol-Myers Squibb Company Wee1 degrading compounds and uses thereof
TW202404976A (zh) * 2022-06-30 2024-02-01 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
WO2024020105A1 (en) * 2022-07-20 2024-01-25 The Regents Of The University Of California Drug implants containing darolutamide and methods of use thereof
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
WO2024054954A1 (en) * 2022-09-08 2024-03-14 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and methods of treating disease
WO2024054952A1 (en) * 2022-09-08 2024-03-14 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and methods of treating disease
WO2024055994A1 (zh) * 2022-09-14 2024-03-21 南京明德新药研发有限公司 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

Family Cites Families (103)

* 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
CA2261762C (en) 1996-07-24 2008-06-17 Celgene Corporation Substituted 2(2,6-dioxopiperidin-3-yl)phthalimides and -1-oxoisoindolines and method of reducing tnf-alpha levels
ATE460423T1 (de) 1997-05-14 2010-03-15 Sloan Kettering Inst Cancer Verfahren und zubereitungen zur zerstörung bestimmter proteine
CN1284944A (zh) 1997-12-17 2001-02-21 麦克公司 整联蛋白受体拮抗剂
US6306663B1 (en) 1999-02-12 2001-10-23 Proteinex, Inc. Controlling protein levels in eucaryotic organisms
CA2372176A1 (en) 1999-05-05 2000-11-09 Merck & Co., 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
WO2002020740A2 (en) 2000-09-08 2002-03-14 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
US7208157B2 (en) 2000-09-08 2007-04-24 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
RU2298554C2 (ru) 2000-09-19 2007-05-10 Бристол-Маерс Сквибб Компани Конденсированные гетероциклические сукцинимидные соединения
US7091353B2 (en) 2000-12-27 2006-08-15 Celgene Corporation Isoindole-imide compounds, compositions, and uses thereof
US20030045552A1 (en) 2000-12-27 2003-03-06 Robarge Michael J. Isoindole-imide compounds, compositions, and uses thereof
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
US8765176B2 (en) 2001-06-20 2014-07-01 Takeda Pharmaceutical Campany Limited Method of manufacturing tablet
PT1423115E (pt) 2001-08-06 2009-07-21 Childrens Medical Center Actividade antiangiogénica de análogos da talidomida substituídos com nitrogénio
US7030141B2 (en) 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
RU2310651C2 (ru) 2002-08-30 2007-11-20 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Азотсодержащие ароматические производные, фармацевтическая композиция, их содержащая, способ лечения и применение
WO2006006065A1 (en) 2004-07-08 2006-01-19 Warner-Lambert Company Llc Androgen modulators
CN100383139C (zh) 2005-04-07 2008-04-23 天津和美生物技术有限公司 可抑制细胞释放肿瘤坏死因子的哌啶-2，6-二酮衍生物
WO2006113942A2 (en) 2005-04-20 2006-10-26 Schering Corporation Method of inhibiting cathepsin activity
MX2008002765A (es) 2005-08-31 2008-04-07 Celgene Corp Compuestos de isoindol-imida y composiciones que la comprenden y metodos para usar los mismos.
CN101395148A (zh) 2006-03-03 2009-03-25 诺瓦提斯公司 N-甲酰基羟胺化合物
NZ572374A (en) 2006-03-29 2011-12-22 Univ California Diarylthiohydantoin compounds
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
AU2007290407A1 (en) 2006-08-30 2008-03-06 Celgene Corporation 5-substituted isoindoline compounds
US8877780B2 (en) 2006-08-30 2014-11-04 Celgene Corporation 5-substituted isoindoline compounds
CA2668286C (en) 2006-11-03 2014-09-16 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
US8415340B2 (en) 2007-07-25 2013-04-09 Bristol-Myers Squibb Company Triazine kinase inhibitors
CN101820765A (zh) 2007-07-31 2010-09-01 安德鲁科技有限公司 包含雄激素受体降解(ard)增强剂的组合物和预防性或治疗性治疗皮肤病与脱发的方法
PE20110547A1 (es) 2008-10-29 2011-08-04 Celgene Corp Compuestos de isoindolina con actividad anticancerigena
WO2010141805A1 (en) 2009-06-05 2010-12-09 Janssen Pharmaceutica Nv Heterocyclic amides as modulators of trpa1
CN102510755A (zh) 2009-07-13 2012-06-20 哈佛大学校长及研究员协会 双功能钉接多肽和其用途
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
SI3202461T1 (sl) * 2010-02-11 2019-05-31 Celgene Corporation Derivati arilmetoksi izoindolina in sestavki, ki jih vsebujejo in metode uporabe le teh
WO2012003281A2 (en) 2010-06-30 2012-01-05 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
EA024245B1 (ru) 2011-04-21 2016-08-31 Орион Корпорейшн Карбоксамиды, модулирующие андрогенные рецепторы
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
RU2666530C2 (ru) 2012-01-12 2018-09-11 Йейл Юниверсити Соединения и способы усиления деградации белков-мишеней и других полипептидов с помощью е3 убиквитин лигазы
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
US9388126B2 (en) 2012-07-19 2016-07-12 Drexel University Sigma receptor ligands and methods of modulating cellular protein homeostasis using same
GB201311910D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel Compounds
NL2011274C2 (en) 2013-08-06 2015-02-09 Illumicare Ip B V 51 Groundbreaking platform technology for specific binding to necrotic cells.
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
CA2923829A1 (en) * 2013-09-10 2015-03-19 Synta Pharmaceuticals Corp. Targeted therapeutics
IN2014MU00303A (hr) 2014-01-28 2015-09-11 Cipla Ltd
MA39481A (fr) * 2014-03-03 2015-09-11 Synta Pharmaceuticals Corp Thérapies ciblées
US20180228907A1 (en) * 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
US20160058872A1 (en) * 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
JP6778114B2 (ja) * 2014-04-14 2020-10-28 アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． イミド系タンパク質分解モジュレーター及び関連する使用方法
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
WO2016097071A1 (en) * 2014-12-18 2016-06-23 F. Hoffmann-La Roche Ag Estrogen receptor modulators and uses thereof
US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
EP3256470B1 (en) 2014-12-23 2023-07-26 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
AU2016209349B2 (en) * 2015-01-20 2020-05-07 Arvinas, Inc. Compounds and methods for the targeted degradation of the Androgen Receptor
US20170327469A1 (en) 2015-01-20 2017-11-16 Arvinas, Inc. Compounds and methods for the targeted degradation of androgen receptor
GB201504314D0 (en) 2015-03-13 2015-04-29 Univ Dundee Small molecules
AU2016232705C1 (en) 2015-03-18 2021-06-17 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
GB201506872D0 (en) 2015-04-22 2015-06-03 Ge Oil & Gas Uk Ltd Novel compounds
GB201506871D0 (en) 2015-04-22 2015-06-03 Glaxosmithkline Ip Dev Ltd Novel compounds
CA2988414C (en) * 2015-06-04 2023-09-26 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
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
MX2018000360A (es) 2015-07-10 2018-06-11 Arvinas Inc Moduladores basados en mdm2 de proteolisis y metodos de uso asociados.
MX2018000471A (es) 2015-07-13 2018-04-10 Arvinas Inc Moduladores de proteolisis basados en alanina y metodos de uso asociados.
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
MX2018005340A (es) 2015-11-02 2018-05-17 Univ Yale Proteolisis de direccionamiento a compuestos de quimera y metodos de preparacion y uso de los mismos.
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
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
EP3445765A4 (en) * 2016-04-22 2019-09-18 Dana Farber Cancer Institute, Inc. DEGRADATION OF CYCLINE-DEPENDENT KINASE 4/6 (CDK4 / 6) BY CONJUGATION OF CDK4 / 6 INHIBITORS WITH E3 LIGASE-LIKE LIGAND AND METHODS OF USE
WO2017197056A1 (en) * 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Bromodomain targeting degronimers for target protein degradation
WO2017197051A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Amine-linked c3-glutarimide degronimers for target protein degradation
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
AU2017341723B2 (en) 2016-10-11 2021-12-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
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
EP3618833B1 (en) 2017-05-01 2022-01-19 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
JP2022529339A (ja) 2019-04-18 2022-06-21 ヒノバ ファーマシューティカルズ インコーポレイテッド アンドロゲン受容体を標的に分解する二官能性キメラ複素環式化合物及びその使用
JP2022549222A (ja) 2019-09-23 2022-11-24 アキュター バイオテクノロジー インコーポレイテッド アンドロゲン受容体分解活性を有する新規尿素およびその使用
US20210113557A1 (en) * 2019-10-22 2021-04-22 Arvinas Operations, Inc. Methods of treating prostate cancer
BR112022022753A2 (pt) 2020-05-09 2023-02-14 Arvinas Operations Inc Métodos de fabricação de um composto bifuncional, formas ultrapuras do composto bifuncional e formas de dosagem compreendendo o mesmo
US20210353621A1 (en) * 2020-05-12 2021-11-18 Arvinas Operations, Inc. Methods of treating prostate cancer
AU2021365850A1 (en) * 2020-10-21 2023-06-08 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor protein
CA3204819A1 (en) * 2020-12-11 2022-06-16 Arvinas Operations, Inc. Methods of treating prostate cancer
WO2023205481A1 (en) 2022-04-21 2023-10-26 Arvinas Operations, Inc. A combination for use in treating prostate cancer comprising arv-100 and abiraterone

Also Published As

Publication number Publication date
CN110506039A (zh) 2019-11-26
AU2017341723A1 (en) 2019-04-04
MX2022006090A (es) 2022-06-14
US20220259154A1 (en) 2022-08-18
KR102173463B1 (ko) 2020-11-04
US10844021B2 (en) 2020-11-24
EP3526202A4 (en) 2020-04-29
JP6972210B2 (ja) 2021-11-24
CA3038979A1 (en) 2018-04-19
PL3660004T3 (pl) 2023-10-02
IL272523A (en) 2020-03-31
US20210040044A1 (en) 2021-02-11
US20210009528A1 (en) 2021-01-14
US20200095205A1 (en) 2020-03-26
SI3660004T1 (sl) 2023-08-31
JP7009466B2 (ja) 2022-02-10
KR20190055260A (ko) 2019-05-22
IL283761B2 (en) 2023-03-01
AU2021204556A1 (en) 2021-08-05
AU2021277645B2 (en) 2023-06-15
JP2019530715A (ja) 2019-10-24
CN111892577A (zh) 2020-11-06
AU2020201792B2 (en) 2020-09-03
IL283761A (en) 2021-07-29
RU2019113229A (ru) 2020-11-02
IL283761B (en) 2022-11-01
MX2022006089A (es) 2022-06-14
PT3660004T (pt) 2023-05-23
RS64208B1 (sr) 2023-06-30
US11964945B2 (en) 2024-04-23
IL265806A (en) 2019-06-30
MX2019004278A (es) 2019-08-05
AU2021277645A1 (en) 2021-12-23
US20180099940A1 (en) 2018-04-12
KR20200020978A (ko) 2020-02-26
CY1126053T1 (el) 2023-11-15
RU2019113229A3 (hr) 2020-11-02
US10584101B2 (en) 2020-03-10
CN111892577B (zh) 2023-07-07
FI3660004T3 (fi) 2023-05-04
LT3660004T (lt) 2023-06-12
JP7178532B2 (ja) 2022-11-28
AU2021204556B2 (en) 2023-06-29
AU2023216887A1 (en) 2023-09-07
EP3660004B1 (en) 2023-02-22
JP7203936B2 (ja) 2023-01-13
AU2020201792A1 (en) 2020-03-26
WO2018071606A1 (en) 2018-04-19
HUE061847T2 (hu) 2023-08-28
IL272523B (en) 2021-07-29
JP2023036887A (ja) 2023-03-14
JP2020100649A (ja) 2020-07-02
EP3526202A1 (en) 2019-08-21
JP2021169481A (ja) 2021-10-28
US20230331681A1 (en) 2023-10-19
US11236051B2 (en) 2022-02-01
US20210171470A1 (en) 2021-06-10
AU2017341723B2 (en) 2021-12-16
CO2019003642A2 (es) 2019-06-19
ES2945224T3 (es) 2023-06-29
JP2022046497A (ja) 2022-03-23
DK3660004T3 (da) 2023-05-08
EP3660004A1 (en) 2020-06-03
US11952347B2 (en) 2024-04-09

Similar Documents

Publication Publication Date Title
HRP20230414T1 (hr) Spojevi i postupci za ciljanu razgradnju androgenog receptora
HRP20231537T1 (hr) Derivati tetrahidronaftalena i tetrahidroizokinolina kao degradatori estrogenskih receptora
JP2020100649A5 (hr)
JP2021169481A5 (hr)
JP2020100659A5 (hr)
HRP20201902T1 (hr) Pripravci protiv raka
HRP20211140T1 (hr) Pripravci protiv raka
HRP20211124T1 (hr) TETRAHIDRO-1H-PIRIDO[3,4-b]INDOL ANTI-ESTROGENI LIJEKOVI
HRP20191860T1 (hr) Derivati 2-hidroksi-1-{4-[(4-fenilfenil)karbonil]piperazin-1-il}etan-1-ona i srodni spojevi kao inhibitori sintaze masnih kiselina (fasn) za liječenje raka
EP4219563A3 (en) Methods of treating cancer with anti-pd-1 antibodies
JP2014129360A5 (hr)
UY28522A1 (es) Derivados de quinazolina
WO2015104292A3 (en) Compounds for use in treating or preventing cancerous diseases
RU2018105923A (ru) Способы лечения рака с использованием апилимода
JP2019533651A5 (hr)
JP2019517497A5 (hr)
PE20181925A1 (es) Composiciones antineoplasicas
IL276290A (en) Heteroaryl compounds, their pharmaceutical preparations and their medical use
IL281353A (en) A pharmaceutical preparation for the prevention or treatment of fatty liver disease not due to alcohol consumption, containing GPR119 ligand as an active ingredient
MX2021012769A (es) Anticuerpos bloqueadores cd73.
Morote et al. Re: Nicolas Mottet, Joaquim Bellmunt, Erik Briers, et al. EAU-ESTRO-ESUR-SIOG Guidelines on Prostate Cancer. European Association of Urology; 2017. http://uroweb. org/guideline/prostate-cancer: How to Assess the Efficacy of Medical Castration
RU2016110352A (ru) Композиции, содержащие рутин, полезные для лечения опухолей, резистентных к химиотерапии
PL402191A1 (pl) Złożona kompozycja farmaceutyczna zawierająca kandesartan cyleksetylu oraz amlodypinę, sposób jej wytwarzania oraz jednostkowa postać dawkowania zawierająca tę kompozycję
WO2016126058A3 (ko) 두타스테라이드 함유 고체 분산체 및 이를 포함하는 조성물
CO2018011927A2 (es) Compuesto fenólico y combinación del mismo con una benzodiazepina fusionada a 1,4-dihidropiridina para el tratamiento de afecciones del sistema nervioso central y vascular