JP5130453B2 - 新規なc−17−ヘテロアリールステロイドcyp17阻害剤/抗アンドロゲン:合成、インビトロ生物活性、薬物動態および抗腫瘍活性 - Google Patents

新規なc−17−ヘテロアリールステロイドcyp17阻害剤/抗アンドロゲン:合成、インビトロ生物活性、薬物動態および抗腫瘍活性 Download PDF

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JP5130453B2
JP5130453B2 JP2007558143A JP2007558143A JP5130453B2 JP 5130453 B2 JP5130453 B2 JP 5130453B2 JP 2007558143 A JP2007558143 A JP 2007558143A JP 2007558143 A JP2007558143 A JP 2007558143A JP 5130453 B2 JP5130453 B2 JP 5130453B2
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compound
compounds
diene
cyp17
mice
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JP2008536807A (ja
JP2008536807A5 (OSRAM
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ブローディー,アンジェラ
ヌジャー,ビンセント
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ユニバーシティ オブ メリーランド,ボルティモア
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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)
JP2007558143A 2005-03-02 2006-03-02 新規なc−17−ヘテロアリールステロイドcyp17阻害剤/抗アンドロゲン:合成、インビトロ生物活性、薬物動態および抗腫瘍活性 Active JP5130453B2 (ja)

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

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JP2012196525A Division JP5613206B2 (ja) 2005-03-02 2012-09-06 新規なc−17−ヘテロアリールステロイドcyp17阻害剤/抗アンドロゲン:合成、インビトロ生物活性、薬物動態および抗腫瘍活性

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JP2008536807A JP2008536807A (ja) 2008-09-11
JP2008536807A5 JP2008536807A5 (OSRAM) 2012-10-25
JP5130453B2 true JP5130453B2 (ja) 2013-01-30

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JP2012196525A Active JP5613206B2 (ja) 2005-03-02 2012-09-06 新規なc−17−ヘテロアリールステロイドcyp17阻害剤/抗アンドロゲン:合成、インビトロ生物活性、薬物動態および抗腫瘍活性

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US (1) US7875599B2 (OSRAM)
EP (2) EP1853619B1 (OSRAM)
JP (2) JP5130453B2 (OSRAM)
KR (1) KR101380959B1 (OSRAM)
CN (2) CN101155823A (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) SI1853619T1 (OSRAM)
WO (1) WO2006093993A1 (OSRAM)
ZA (1) ZA200708106B (OSRAM)

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JP2012255026A (ja) * 2005-03-02 2012-12-27 Univ Of Maryland Baltimore 新規なc−17−ヘテロアリールステロイドcyp17阻害剤/抗アンドロゲン:合成、インビトロ生物活性、薬物動態および抗腫瘍活性

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CA2726734C (en) 2007-06-06 2014-10-07 University Of Maryland, Baltimore Hdac inhibitor ms-275 and aromatase inhibitors 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
US20100048912A1 (en) * 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens, 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
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
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
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
EP2393827B1 (en) 2009-02-05 2015-10-07 Tokai Pharmaceuticals, Inc. Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens
GB2514957A (en) * 2009-02-05 2014-12-10 Tokai Pharmaceuticals Inc Combination of a 17 alpha-hydroxylase/c17, 20-lyase inhibitor with an additional therapeutic agent
JP5456891B2 (ja) 2009-06-26 2014-04-02 ノバルティス アーゲー Cyp17阻害剤としての1,3−二置換イミダゾリジン−2−オン誘導体
EP2461814A4 (en) 2009-08-07 2012-12-05 Tokai Pharmaceuticals Inc PROSTATE CANCER TREATMENT
WO2011059969A2 (en) * 2009-11-13 2011-05-19 Tokai Pharmaceuticals, Inc. Mammalian metabolites of steroids
EP2506855A4 (en) * 2009-11-30 2014-07-30 Harbor Biosciences Inc ANTICARCINOMA COMPOUNDS AND SCREENING METHODS
CN103108871B (zh) 2010-09-16 2014-09-10 诺华股份有限公司 17α-羟化酶/C17,20-裂合酶抑制剂
JP2013545815A (ja) * 2010-12-16 2013-12-26 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 Cyp11b、cyp17および/またはcyp21阻害剤
AU2012249421B9 (en) 2011-04-28 2015-10-22 Novartis Ag 17alpha-hydroxylase/C17,20-lyase inhibitors
AU2012284053A1 (en) * 2011-07-18 2014-01-23 Tokai Pharmaceuticals, Inc. Novel compositions and methods for treating prostate cancer
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
RU2015137617A (ru) * 2013-03-14 2017-04-18 Юниверсити Оф Мэриленд, Балтимор Офис Оф Текнолоджи Трансфер Агенты, подавляющие андрогенные рецепторы, и их применение
AU2014247941C1 (en) * 2013-04-04 2019-10-31 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
PE20161405A1 (es) 2013-12-24 2017-01-18 Harvard College Analogos de cortistatina y sintesis y usos de los mismos
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
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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
US11390645B2 (en) 2016-08-08 2022-07-19 Industriale Chimica S.R.L. Process for the preparation of 3β-hydroxy-17-(1H-benzimidazol-1-YL) androsta-5,16-diene
WO2019160890A1 (en) * 2018-02-13 2019-08-22 Dana-Farber Cancer Institute, Inc. Cyclin-dependent kinase degraders and methods of use
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AU2020393896A1 (en) 2019-11-26 2022-06-23 Dana-Farber Cancer Institute, Inc. Potent and selective azaindole inhibitors of CDK8 and CDK19

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AU2006218711A1 (en) 2006-09-08
PL1853619T3 (pl) 2011-03-31
ATE482969T1 (de) 2010-10-15
JP2008536807A (ja) 2008-09-11
CA2599953A1 (en) 2006-09-08
US20080280864A1 (en) 2008-11-13
ES2528055T3 (es) 2015-02-03
JP2012255026A (ja) 2012-12-27
EP2206719A3 (en) 2011-01-05
US7875599B2 (en) 2011-01-25
IL210480A (en) 2015-06-30
EA200701872A1 (ru) 2008-06-30
EP1853619A4 (en) 2009-08-26
PL2206719T3 (pl) 2015-03-31
PT2206719E (pt) 2015-02-05
DE602006017175D1 (de) 2010-11-11
WO2006093993A1 (en) 2006-09-08
DK1853619T3 (da) 2011-01-10
PT1853619E (pt) 2011-01-03
IL210478A0 (en) 2011-03-31
IL210480A0 (en) 2011-03-31
EP1853619B1 (en) 2010-09-29
EA019560B1 (ru) 2014-04-30
SI2206719T1 (sl) 2015-03-31
MX2007010593A (es) 2008-02-20
EP2206719A2 (en) 2010-07-14
NZ561571A (en) 2009-09-25
SI1853619T1 (sl) 2011-01-31
CN101155823A (zh) 2008-04-02
AU2006218711A2 (en) 2006-09-08
CN103349664A (zh) 2013-10-16
JP5613206B2 (ja) 2014-10-22
HK1115387A1 (en) 2008-11-28
EP2206719B1 (en) 2014-10-22
IL185608A0 (en) 2008-01-06
IL185608A (en) 2016-06-30
ES2353413T3 (es) 2011-03-01
EP1853619A1 (en) 2007-11-14
BRPI0607523A2 (pt) 2009-09-08
KR20070120119A (ko) 2007-12-21
KR101380959B1 (ko) 2014-04-04
ZA200708106B (en) 2008-12-31
CA2599953C (en) 2013-08-13
DK2206719T3 (en) 2015-01-26
AU2006218711B2 (en) 2010-11-11

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