DK2767531T3 - Cycliske n,n'-diarylthiourinstoffer og n,n'-diarylurinstoffer som androgenreceptorantagonister, anti-cancermiddel, fremgangsmåde til fremstilling og anvendelse deraf - Google Patents

Cycliske n,n'-diarylthiourinstoffer og n,n'-diarylurinstoffer som androgenreceptorantagonister, anti-cancermiddel, fremgangsmåde til fremstilling og anvendelse deraf Download PDF

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DK2767531T3
DK2767531T3 DK14001526.4T DK14001526T DK2767531T3 DK 2767531 T3 DK2767531 T3 DK 2767531T3 DK 14001526 T DK14001526 T DK 14001526T DK 2767531 T3 DK2767531 T3 DK 2767531T3
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methyl
compounds
trifluoromethyl
pharmaceutical composition
mmol
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DK14001526.4T
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Alexandre Vasilievich Ivachtchenko
Oleg Dimitrievich Mitkin
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R-Pharm Overseas Inc
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D233/72—Two oxygen atoms, e.g. hydantoin
    • 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
    • C07D233/72—Two oxygen atoms, e.g. hydantoin
    • C07D233/74—Two oxygen atoms, e.g. hydantoin with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to other ring members
    • 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
    • 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
    • C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine 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 directly attached in position 2
    • C07D239/10—Oxygen or sulfur 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
    • C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D239/22—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • C07D249/12—Oxygen or sulfur atoms
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (12)

1. Forbindelser som er cycliske Λ/,Λ/'-diarylthiourinstoffer og A/,/V'-diarylurinstoffer med den almene formel 1.2, deres optiske (R)- og (S)-isomerer, og deres farmaceutisk acceptable salte,
hvor: RI - betegner Ci-C3alkyl; R5 og R4 sammen med det C-atom til hvilket de er bundet danner en 5-eller 6-leddet heterocykel omfattende mindst ét oxygenatom eller nitrogenatom eventuelt substitueret med methyl.
2. Forbindelser ifølge krav 1 som er forbindelser med formel 1.2.3(1), 1.2.3(2) og 1.2.3(3), og optiske (R)-isomerer - (R)-1.2.3(l), og (S)-isomerer - (S)-1.2.3(1),
3. Forbindelser ifølge et hvilket som helst af kravene 1 til 2 til anvendelse som et medikament.
4. Forbindelser ifølge et hvilket som helst af kravene 1 til 3 til anvendelse i behandling af cancer.
5. Forbindelserne til anvendelse ifølge krav 4 hvor canceren er prostatacancer.
6. Fremgangsmåde til fremstillingen af forbindelser med den almene formel 1.2 og deres optiske (R)- og (S) -isomerer deraf ifølge et hvilket som helst af kravene 1-5 ved interaktion af de tilsvarende 4-(cyanomethyl)amino-benzamider 4.1 eller (4-carbamoylphenylamino)-eddikesyrer 4.2 eller deres optiske (R)- og (S)-isomerer deraf med isothiocyanat 3.2.
RI - betegner Ci-C3alkyl; R5 og R4 sammen med det C-atom til hvilket de er bundet danner en 5-eller 6-leddet heterocykel omfattende mindst ét oxygenatom eller nitrogenatom eventuelt substitueret med methyl.
7. Farmaceutisk sammensætning omfattende som aktiv komponent en forbindelse ifølge et hvilket som helst af kravene 1 til 5.
8. Farmaceutisk sammensætning ifølge krav 7 til anvendelse som en androgenreceptorantagonist.
9. Farmaceutisk sammensætning ifølge krav 7 eller farmaceutisk sammensætning ifølge krav 8 yderligere omfattende et inert fyldstof og/eller opløsningsmiddel.
10. Farmaceutisk sammensætning ifølge et hvilket som helst af kravene 7 eller den farmaceutiske sammensætning ifølge krav 8 til 9 yderligere omfattende et middel til behandling af cancerøse sygdomme, hvilket middel er forskelligt fra forbindelserne ifølge et hvilket som helst af kravene 1 til 5.
11. Medikament i form af tabletter, kapsler eller injektioner til behandlingen af cancerøse sygdomme omfattende en forbindelse ifølge et hvilket som helst af kravene 1 til 5 eller en farmaceutisk sammensætning ifølge et hvilket som helst af kravene 7 til 9.
12. Medikamentet ifølge krav 11 til anvendelse i behandlingen af prostatacancer.
DK14001526.4T 2010-07-22 2011-07-01 Cycliske n,n'-diarylthiourinstoffer og n,n'-diarylurinstoffer som androgenreceptorantagonister, anti-cancermiddel, fremgangsmåde til fremstilling og anvendelse deraf DK2767531T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
RU2010130618/04A RU2434851C1 (ru) 2010-07-22 2010-07-22 Циклические n, n'-диарилтиомочевины или n, n'-диарилмочевины - антагонисты андрогенных рецепторов, противораковое средство, способ получения и применения
EP11809933.2A EP2597086A4 (en) 2010-07-22 2011-07-01 Cyclic N, N'-diarylthioureas and N, N'-diaryl ureas as well as androgenic receptor agonists, anti-cancer agents therewith, and methods for their preparation and use

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DK2767531T3 true DK2767531T3 (da) 2017-03-13

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US (1) US9073874B2 (da)
EP (2) EP2597086A4 (da)
JP (1) JP5897566B2 (da)
KR (1) KR101738866B1 (da)
AU (1) AU2011280297B2 (da)
CA (1) CA2806051C (da)
CY (1) CY1119184T1 (da)
DK (1) DK2767531T3 (da)
EA (1) EA020681B1 (da)
ES (1) ES2618891T3 (da)
GE (1) GEP20166450B (da)
HR (1) HRP20170450T1 (da)
HU (1) HUE031999T2 (da)
LT (1) LT2767531T (da)
PL (1) PL2767531T3 (da)
PT (1) PT2767531T (da)
RS (1) RS55876B1 (da)
RU (1) RU2434851C1 (da)
SI (1) SI2767531T1 (da)
SM (1) SMT201700170T1 (da)
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CN103608333B (zh) * 2011-03-10 2016-01-06 苏州开拓药业有限公司 雄激素受体拮抗剂及其用途
KR102189940B1 (ko) 2012-09-04 2020-12-14 샹하이 헨그루이 파마수티컬 컴퍼니 리미티드 이미다졸린 유도체, 이의 제조 방법, 및 이들의 의약에서의 용도
CA2889756C (en) * 2012-10-26 2023-03-14 Memorial Sloan-Kettering Cancer Center Thiohydantoin compounds as androgen receptor modulators
RU2520134C1 (ru) * 2013-02-27 2014-06-20 Общество с ограниченной ответственностью "Авионко" (ООО "Авионко") Замещенные (r)-3-(4-метилкарбамоил-3-фторфениламино)-тетрагидро-фуран-3-енкарбоновые кислоты и их эфиры, способ их получения и применения
CN104844521B (zh) * 2014-02-13 2017-08-15 成都伊诺达博医药科技有限公司 抗前列腺癌药物恩杂鲁胺的合成方法
CN104844520B (zh) * 2014-02-13 2017-09-05 成都伊诺达博医药科技有限公司 一种合成恩杂鲁胺的方法
RU2557235C1 (ru) * 2014-07-08 2015-07-20 Александр Васильевич Иващенко Замещенные 2-тиоксо-имидазолидин-4-оны и их спироаналоги, противораковый активный компонент, фармацевтическая композиция, лекарственный препарат, способ лечения рака простаты
TWI613194B (zh) 2015-06-10 2018-02-01 台灣神隆股份有限公司 用於製備恩雜魯胺的新穎方法
TWI726969B (zh) 2016-01-11 2021-05-11 比利時商健生藥品公司 用作雄性激素受體拮抗劑之經取代之硫尿囊素衍生物
CN119219606A (zh) * 2018-12-19 2024-12-31 细胞基因公司 经取代的3-((3-氨基苯基)氨基)哌啶-2，6-二酮化合物、其组合物及使用它们的治疗方法
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
BR112023002295A2 (pt) 2020-08-13 2023-03-14 Pfizer Terapia de combinação

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NZ572374A (en) * 2006-03-29 2011-12-22 Univ California Diarylthiohydantoin compounds

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EP2767531B1 (en) 2016-12-21
SMT201700170T1 (it) 2017-05-08
CY1119184T1 (el) 2018-02-14
RU2434851C1 (ru) 2011-11-27
EP2597086A4 (en) 2013-11-06
SI2767531T1 (sl) 2017-04-26
AU2011280297A1 (en) 2013-03-07
US9073874B2 (en) 2015-07-07
PT2767531T (pt) 2017-03-23
PL2767531T3 (pl) 2017-08-31
GEP20166450B (en) 2016-03-25
EP2597086A1 (en) 2013-05-29
ES2618891T3 (es) 2017-06-22
US20130116269A1 (en) 2013-05-09
AU2011280297B2 (en) 2013-11-21
KR20130046436A (ko) 2013-05-07
JP5897566B2 (ja) 2016-03-30
HRP20170450T1 (hr) 2017-05-19
EP2767531A1 (en) 2014-08-20
JP2013532657A (ja) 2013-08-19
RS55876B1 (sr) 2017-08-31
UA112161C2 (uk) 2016-08-10
WO2012011840A1 (ru) 2012-01-26
CA2806051C (en) 2017-02-14
EA201300122A1 (ru) 2013-06-28
LT2767531T (lt) 2017-04-10
CA2806051A1 (en) 2012-01-26
HUE031999T2 (en) 2017-09-28
KR101738866B1 (ko) 2017-05-23
EA020681B1 (ru) 2014-12-30

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