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
Inventor
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

Country Status (21)

Country Link
US (1) US7875599B2 (OSRAM)
EP (2) EP1853619B1 (OSRAM)
JP (2) JP5130453B2 (OSRAM)
KR (1) KR101380959B1 (OSRAM)
CN (2) CN103349664A (OSRAM)
AT (1) ATE482969T1 (OSRAM)
AU (1) AU2006218711B2 (OSRAM)
BR (1) BRPI0607523A2 (OSRAM)
CA (1) CA2599953C (OSRAM)
DE (1) DE602006017175D1 (OSRAM)
DK (2) DK2206719T3 (OSRAM)
EA (1) EA019560B1 (OSRAM)
ES (2) ES2528055T3 (OSRAM)
IL (3) IL185608A (OSRAM)
MX (1) MX2007010593A (OSRAM)
NZ (1) NZ561571A (OSRAM)
PL (2) PL1853619T3 (OSRAM)
PT (2) PT1853619E (OSRAM)
SI (2) SI2206719T1 (OSRAM)
WO (1) WO2006093993A1 (OSRAM)
ZA (1) ZA200708106B (OSRAM)

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NZ561571A (en) * 2005-03-02 2009-09-25 Univ Maryland Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity
WO2008154402A2 (en) 2007-06-06 2008-12-18 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
US20100048524A1 (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
GB2470700B (en) 2008-03-25 2012-08-08 Univ Maryland C-17 heteroaryl steroidal CYP17 inhibitors
US8785423B2 (en) * 2008-04-14 2014-07-22 University Of Maryland, Baltimore Compositions and methods of inducing endoplasmic reticulum stress response for the treatment of cell proliferative diseases
EP2334686B1 (en) 2008-08-28 2019-02-27 President and Fellows of Harvard College Cortistatin analogues and syntheses therof
EP2362872A4 (en) * 2008-10-28 2012-05-30 Biomarin Pharm Inc DECAHYDRO-1H-INDENOCHINOLINONE AND DECAHYDRO-3H-CYCLOPENTAPHENANTHRIDINONE CYP17 HEMMER
WO2010091299A2 (en) * 2009-02-05 2010-08-12 Tokai Pharmaceuticals Novel combination cancer therapies
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
CN102686600A (zh) * 2009-02-05 2012-09-19 托凯药业股份有限公司 甾体cyp17抑制剂/抗雄激素物质的新型药物前体
WO2010149755A1 (en) 2009-06-26 2010-12-29 Novartis Ag 1, 3-disubstituted imidazolidin-2-one derivatives as inhibitors of cyp 17
AU2010279398A1 (en) * 2009-08-07 2012-03-08 Tokai Pharmaceuticals, Inc. Treatment of prostate cancer
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
BR112013017635A2 (pt) * 2010-12-16 2016-10-11 Biomarin Pharm Inc inibidores de cyp11b, cyp17 e/ou cyp21
AU2012249421B9 (en) 2011-04-28 2015-10-22 Novartis Ag 17alpha-hydroxylase/C17,20-lyase inhibitors
CN103813794A (zh) * 2011-07-18 2014-05-21 拓凯制药公司 用于治疗前列腺癌的新型组合物及方法
JP2015503508A (ja) * 2011-12-22 2015-02-02 トーカイ ファーマシューティカルズ,インク. PI3K/mTOR阻害剤を使用する併用療法のための方法および組成物
CA2904170A1 (en) 2013-03-14 2014-09-25 University Of Maryland, Baltimore Androgen receptor down-regulating agents and uses thereof
WO2014165815A2 (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
JP2016528252A (ja) 2013-08-12 2016-09-15 トーカイ ファーマシューティカルズ, インコーポレイテッド アンドロゲン標的治療を使用する新生物障害の処置のためのバイオマーカー
EA030907B1 (ru) 2013-12-24 2018-10-31 Президент Энд Феллоус Оф Гарвард Колледж Аналоги кортистатина, их синтез и применения
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
CN105732759A (zh) * 2015-01-29 2016-07-06 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
EP3294298A4 (en) 2015-05-08 2018-10-17 President and Fellows of Harvard College Cortistatin analogues, syntheses, and uses thereof
WO2017004411A1 (en) 2015-07-01 2017-01-05 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
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
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
CA3063339C (en) * 2016-08-08 2024-05-28 Industriale Chimica S.R.L. Process for the preparation of 3b-hydroxy-17-(1h-benzimidazol-1-yl)androsta-5,16-diene
EP3752517B1 (en) * 2018-02-13 2025-04-09 Dana-Farber Cancer Institute, Inc. Cyclin-dependent kinase degraders and methods of use
WO2019160889A1 (en) * 2018-02-13 2019-08-22 Dana-Farber Cancer Institute, Inc. Cyclin-dependent kinase inhibitors and methods of use
CA3159284A1 (en) 2019-11-26 2021-06-03 Dana-Farber Cancer Institute, Inc. Potent and selective azaindole inhibitors of cdk8 and cdk19

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* Cited by examiner, † Cited by third party
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CA27440A (en) 1887-08-16 James T. Walsh Art of making sheet metal cans, for packing meats, fruits, vegetables, etc.
CH621803A5 (OSRAM) * 1974-08-08 1981-02-27 Siphar Sa
US5604213A (en) 1992-03-31 1997-02-18 British Technology Group Limited 17-substituted steroids useful in cancer treatment
US5994335A (en) 1997-10-17 1999-11-30 The University Of Maryland, Baltimore 17-azolyl steroids useful as androgen synthesis inhibitors
ATE513555T1 (de) 2003-07-29 2011-07-15 Dompe Spa Pharmazeutische kombination aus g-csf und plgf für blutstammzellen
NZ561571A (en) * 2005-03-02 2009-09-25 Univ Maryland Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity

Also Published As

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

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