AU2006218711B2 - Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity - Google Patents

Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity Download PDF

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Publication number
AU2006218711B2
AU2006218711B2 AU2006218711A AU2006218711A AU2006218711B2 AU 2006218711 B2 AU2006218711 B2 AU 2006218711B2 AU 2006218711 A AU2006218711 A AU 2006218711A AU 2006218711 A AU2006218711 A AU 2006218711A AU 2006218711 B2 AU2006218711 B2 AU 2006218711B2
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Prior art keywords
benzimidazol
androsta
compound
diene
compounds
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AU2006218711A1 (en
AU2006218711A2 (en
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Angela Brodie
Vincent Njar
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University of Maryland Baltimore
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University of Maryland Baltimore
University of Maryland College Park
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2006218711A 2005-03-02 2006-03-02 Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity Active AU2006218711B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US65739005P 2005-03-02 2005-03-02
US60/657,390 2005-03-02
PCT/US2006/007143 WO2006093993A1 (en) 2005-03-02 2006-03-02 Novel c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity

Publications (3)

Publication Number Publication Date
AU2006218711A1 AU2006218711A1 (en) 2006-09-08
AU2006218711A2 AU2006218711A2 (en) 2006-09-08
AU2006218711B2 true AU2006218711B2 (en) 2010-11-11

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AU2006218711A Active AU2006218711B2 (en) 2005-03-02 2006-03-02 Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity

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Country Link
US (1) US7875599B2 (enExample)
EP (2) EP2206719B1 (enExample)
JP (2) JP5130453B2 (enExample)
KR (1) KR101380959B1 (enExample)
CN (2) CN101155823A (enExample)
AT (1) ATE482969T1 (enExample)
AU (1) AU2006218711B2 (enExample)
BR (1) BRPI0607523A2 (enExample)
CA (1) CA2599953C (enExample)
DE (1) DE602006017175D1 (enExample)
DK (2) DK1853619T3 (enExample)
EA (1) EA019560B1 (enExample)
ES (2) ES2353413T3 (enExample)
IL (3) IL185608A (enExample)
MX (1) MX2007010593A (enExample)
NZ (1) NZ561571A (enExample)
PL (2) PL1853619T3 (enExample)
PT (2) PT2206719E (enExample)
SI (2) SI1853619T1 (enExample)
WO (1) WO2006093993A1 (enExample)
ZA (1) ZA200708106B (enExample)

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EP2359828A1 (en) 2007-06-06 2011-08-24 University of Maryland, Baltimore HDAC inhibitors and hormone targeted drugs for the treatment of cancer
WO2009114658A2 (en) * 2008-03-12 2009-09-17 University Of Maryland, Baltimore Androgen receptor inactivation contributes to antitumor efficacy of cyp17 inhibitors in prostate cancer
US20100048913A1 (en) * 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
WO2009120565A2 (en) * 2008-03-25 2009-10-01 University Of Maryland, Baltimore Novel prodrugs of c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity
WO2009129208A2 (en) * 2008-04-14 2009-10-22 University Of Maryland, Baltimore Compositions and methods of inducing endoplasmic reticulum stress reponse
EP2334686B1 (en) 2008-08-28 2019-02-27 President and Fellows of Harvard College Cortistatin analogues and syntheses therof
JP2012506906A (ja) * 2008-10-28 2012-03-22 バイオマリン ファーマシューティカル インコーポレイテッド デカヒドロ−1h−インデノキノリンおよびデカヒドロ−3h−シクロペンタフェナントリジノンcyp17インヒビター
GB201114153D0 (en) * 2009-02-05 2011-10-05 Tokai Pharmaceuticals Inc Combination of a 17 alpha-hydroxylase/c17, 20-lyase inhibitor with an additional therapeutic agent
GB2479693B (en) * 2009-02-05 2014-04-09 Tokai Pharmaceuticals Inc Steroidal CYP17 inhibitors and their use in the treatment of cancer and prostate hyperplasia
WO2010091306A1 (en) 2009-02-05 2010-08-12 Tokai Pharmaceuticals Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens
GEP20156250B (en) 2009-06-26 2015-02-25 Novartis Ag 1,3-disubstituted imidazolidin-2-one derivatives as inhibitors of cyp 17
EP2461814A4 (en) * 2009-08-07 2012-12-05 Tokai Pharmaceuticals Inc PROSTATE CANCER TREATMENT
JP5956928B2 (ja) * 2009-11-13 2016-07-27 トーカイ ファーマシューティカルズ,インク. 哺乳類のステロイドの代謝物質
WO2011066582A1 (en) * 2009-11-30 2011-06-03 Harbor Biosciences, Inc. Anticancer compounds and screening method
WO2012035078A1 (en) 2010-09-16 2012-03-22 Novartis Ag 17α-HYDROXYLASE/C17,20-LYASE INHIBITORS
EP2660241A3 (en) * 2010-12-16 2014-03-12 BioMarin Pharmaceutical Inc. C-17-heteroaryl steroidal compounds as inhibitors of cyp11b, cyp17, and/or cyp21
EA023064B1 (ru) 2011-04-28 2016-04-29 Новартис Аг ИНГИБИТОРЫ 17α-ГИДРОКСИЛАЗЫ/C-ЛИАЗЫ
US20140288037A1 (en) * 2011-07-18 2014-09-25 Tokai Pharmaceuticals, Inc. Novel compositions and methods for treating prostate cancer
US20150005265A1 (en) * 2011-12-22 2015-01-01 Susan Stewart Methods and compositions for combination therapy using p13k/mtor inhibitores
BR112015023098A2 (pt) 2013-03-14 2017-07-18 Univ Jefferson agentes de infrarregulação do receptor de andrógeno e usos dos mesmos
CA3151555A1 (en) * 2013-04-04 2014-10-09 University Of Maryland, Baltimore Nonsteroidal and steroidal compounds with potent androgen receptor down-regulation and anti prostate cancer activity
KR20160058774A (ko) 2013-08-12 2016-05-25 토카이 파마슈티컬, 아이엔씨. 안드로겐-표적 치료제를 이용하는 종양 질환 치료를 위한 바이오마커
KR20160101162A (ko) 2013-12-24 2016-08-24 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 코르티스타틴 유사체 및 그의 합성 및 용도
CN103694299A (zh) * 2014-01-13 2014-04-02 中国药科大学 甾体类雄激素受体抑制剂、其制备方法及其医药用途
WO2016119742A1 (zh) * 2015-01-29 2016-08-04 苏州晶云药物科技有限公司 (3β)-17-(1H-苯并咪唑-1-基)雄甾-5,16-二烯-3-醇的盐及其制备方法
WO2016182932A1 (en) 2015-05-08 2016-11-17 President And Fellows Of Harvard College Cortistatin analogues, syntheses, and uses thereof
EP3316889A4 (en) 2015-07-01 2018-11-14 President and Fellows of Harvard College Cortistatin analogues and syntheses and uses thereof
US10682362B2 (en) 2015-10-14 2020-06-16 Wayne State University Treatments and diagnostics for cancers
IT201600083406A1 (it) * 2016-08-08 2018-02-08 Ind Chimica Srl PROCESSO PER LA PREPARAZIONE DI 3β-IDROSSI-17-(1H-BENZIMIDAZOL-1-IL)ANDROSTA-5,16-DIENE
IT201600121375A1 (it) * 2016-11-30 2018-05-30 Ind Chimica Srl PROCESSO PER LA PREPARAZIONE DI 3ß-IDROSSI-17-(1H-BENZIMIDAZOL-1-IL)ANDROSTA-5,16-DIENE
CH714173B1 (it) * 2016-08-08 2021-04-15 Ind Chimica Srl Processo per la preparazione di 3ß-idrossi-17-(1H-benzimidazol-1-il)androsta-5,16-diene.
ES3026226T3 (en) * 2018-02-13 2025-06-10 Dana Farber Cancer Inst Inc Cyclin-dependent kinase degraders and methods of use
AU2019222651B2 (en) * 2018-02-13 2024-08-22 Dana-Farber Cancer Institute, Inc. Cyclin-dependent kinase inhibitors and methods of use
EP4065111A4 (en) 2019-11-26 2023-09-20 Dana-Farber Cancer Institute, Inc. Potent and selective azaindole inhibitors of cdk8 and cdk19

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US5994335A (en) * 1997-10-17 1999-11-30 The University Of Maryland, Baltimore 17-azolyl steroids useful as androgen synthesis inhibitors
CA2526244C (en) 2003-07-29 2012-03-20 Dompe S.P.A. Pharmaceutical combination of g-csf and plgf useful for blood stem cell mobilization
PL1853619T3 (pl) * 2005-03-02 2011-03-31 Univ Maryland 3-beta-Hydroksy-17-(1H-benzimidazol-1-ilo)-androsta-5,16-dien do zastosowania do leczenia choroby prostaty

Also Published As

Publication number Publication date
PL1853619T3 (pl) 2011-03-31
CA2599953A1 (en) 2006-09-08
ZA200708106B (en) 2008-12-31
DK2206719T3 (en) 2015-01-26
DE602006017175D1 (de) 2010-11-11
PL2206719T3 (pl) 2015-03-31
KR101380959B1 (ko) 2014-04-04
JP2008536807A (ja) 2008-09-11
IL210480A (en) 2015-06-30
SI1853619T1 (sl) 2011-01-31
MX2007010593A (es) 2008-02-20
JP5613206B2 (ja) 2014-10-22
US20080280864A1 (en) 2008-11-13
JP2012255026A (ja) 2012-12-27
EA200701872A1 (ru) 2008-06-30
IL210480A0 (en) 2011-03-31
EP2206719B1 (en) 2014-10-22
BRPI0607523A2 (pt) 2009-09-08
US7875599B2 (en) 2011-01-25
IL210478A0 (en) 2011-03-31
CN101155823A (zh) 2008-04-02
DK1853619T3 (da) 2011-01-10
EP2206719A2 (en) 2010-07-14
AU2006218711A1 (en) 2006-09-08
WO2006093993A1 (en) 2006-09-08
AU2006218711A2 (en) 2006-09-08
PT1853619E (pt) 2011-01-03
SI2206719T1 (sl) 2015-03-31
JP5130453B2 (ja) 2013-01-30
HK1115387A1 (en) 2008-11-28
PT2206719E (pt) 2015-02-05
IL185608A0 (en) 2008-01-06
CA2599953C (en) 2013-08-13
EA019560B1 (ru) 2014-04-30
IL185608A (en) 2016-06-30
ES2528055T3 (es) 2015-02-03
EP1853619A4 (en) 2009-08-26
EP2206719A3 (en) 2011-01-05
CN103349664A (zh) 2013-10-16
EP1853619A1 (en) 2007-11-14
NZ561571A (en) 2009-09-25
KR20070120119A (ko) 2007-12-21
EP1853619B1 (en) 2010-09-29
ES2353413T3 (es) 2011-03-01
ATE482969T1 (de) 2010-10-15

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