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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AU
Australia
Prior art keywords
benzimidazol
androsta
compound
diene
compounds
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Expired
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AU2006218711A
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AU2006218711A2 (en
AU2006218711A1 (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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Publication of AU2006218711A1 publication Critical patent/AU2006218711A1/en
Assigned to UNIVERSITY OF MARYLAND, BALTIMORE reassignment UNIVERSITY OF MARYLAND, BALTIMORE Amend patent request/document other than specification (104) Assignors: UNIVERSITY OF MARYLAND
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    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal 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 Expired 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
AU2006218711A2 AU2006218711A2 (en) 2006-09-08
AU2006218711A1 AU2006218711A1 (en) 2006-09-08
AU2006218711B2 true AU2006218711B2 (en) 2010-11-11

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Family Applications (1)

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AU2006218711A Expired 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 (https=)
EP (2) EP1853619B1 (https=)
JP (2) JP5130453B2 (https=)
KR (1) KR101380959B1 (https=)
CN (2) CN103349664A (https=)
AT (1) ATE482969T1 (https=)
AU (1) AU2006218711B2 (https=)
BR (1) BRPI0607523A2 (https=)
CA (1) CA2599953C (https=)
DE (1) DE602006017175D1 (https=)
DK (2) DK1853619T3 (https=)
EA (1) EA019560B1 (https=)
ES (2) ES2528055T3 (https=)
IL (3) IL185608A (https=)
MX (1) MX2007010593A (https=)
NZ (1) NZ561571A (https=)
PL (2) PL2206719T3 (https=)
PT (2) PT1853619E (https=)
SI (2) SI1853619T1 (https=)
WO (1) WO2006093993A1 (https=)
ZA (1) ZA200708106B (https=)

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AU2006218711B2 (en) * 2005-03-02 2010-11-11 University Of Maryland, Baltimore Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity
GB2454118B (en) 2007-06-06 2010-06-02 Univ Maryland Hdac inhibitors and hormone targeted drugs for the treatment of cancer
GB2470873A (en) * 2008-03-12 2010-12-08 Univ Maryland Androgen receptor inactivation contributes to antitumor efficacy of CYP17 inhibitors in prostrate 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
US20110118219A1 (en) 2008-03-25 2011-05-19 University Of Maryland, Baltimore Novel prodrugs of c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity
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
US20110190323A1 (en) 2008-08-28 2011-08-04 President And Fellows Of Harvard College Cortistatin analogues and syntheses thereof
US20100105700A1 (en) * 2008-10-28 2010-04-29 Lead Therapeutics, Inc. Decahydro-1h-indenoquinolinone and decahydro-3h-cyclopentaphenanthridinone cyp17 inhibitors
WO2010091299A2 (en) * 2009-02-05 2010-08-12 Tokai Pharmaceuticals Novel combination cancer therapies
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
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
WO2010149755A1 (en) 2009-06-26 2010-12-29 Novartis Ag 1, 3-disubstituted imidazolidin-2-one derivatives as inhibitors of cyp 17
CA2770092A1 (en) 2009-08-07 2011-02-10 Tokai Pharmaceuticals, Inc. Treatment of prostate cancer
WO2011059969A2 (en) * 2009-11-13 2011-05-19 Tokai Pharmaceuticals, Inc. Mammalian metabolites of steroids
CA2782266A1 (en) * 2009-11-30 2011-06-03 Harbor Biosciences, Inc. Anticancer compounds and screening method
JP2013537210A (ja) 2010-09-16 2013-09-30 ノバルティス アーゲー １７α−ヒドロキシラーゼ／Ｃ１７，２０−リアーゼ阻害剤
EP2651916A2 (en) * 2010-12-16 2013-10-23 BioMarin Pharmaceutical Inc. C-17-heteroaryl steroidal compounds as inhibitors of cyp11b, cyp17, and/or cyp21
US9029399B2 (en) 2011-04-28 2015-05-12 Novartis Ag 17α-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
US20150005265A1 (en) * 2011-12-22 2015-01-01 Susan Stewart Methods and compositions for combination therapy using p13k/mtor inhibitores
RU2015137617A (ru) 2013-03-14 2017-04-18 Юниверсити Оф Мэриленд, Балтимор Офис Оф Текнолоджи Трансфер Агенты, подавляющие андрогенные рецепторы, и их применение
EP2991644B1 (en) * 2013-04-04 2020-03-25 University of Maryland, Baltimore Nonsteroidal and steroidal compounds with potent androgen receptor down-regulation and anti prostate cancer activity
CN105636594A (zh) 2013-08-12 2016-06-01 托凯药业股份有限公司 使用雄激素靶向疗法用于治疗肿瘤性疾病的生物标记物
AU2014369834B2 (en) 2013-12-24 2018-12-20 President And Fellows Of Harvard College Cortistatin analogues and syntheses and uses thereof
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
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
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.
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
AU2019222652B2 (en) 2018-02-13 2021-09-02 Dana-Farber Cancer Institute, Inc. Cyclin-dependent kinase degraders and methods of use
US20200369715A1 (en) * 2018-02-13 2020-11-26 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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CA27440A (en) 1887-08-16 James T. Walsh Art of making sheet metal cans, for packing meats, fruits, vegetables, etc.
CH621803A5 (https=) * 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
WO2005014023A1 (en) 2003-07-29 2005-02-17 Dompe' Pha.R.Ma S.P.A. Pharmaceutical combination of g-csf and plgf useful for blood stem cell
AU2006218711B2 (en) 2005-03-02 2010-11-11 University Of Maryland, Baltimore Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity

Also Published As

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

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DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT(S) FILED 13 SEP 2007

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