CN101155823A - 新的c-17-杂芳基甾族的cyp17抑制剂/抗雄激素物质：其合成，体外生物学活性，药代动力学和抗肿瘤活性 - Google Patents

新的c-17-杂芳基甾族的cyp17抑制剂/抗雄激素物质：其合成，体外生物学活性，药代动力学和抗肿瘤活性 Download PDF

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Publication number
CN101155823A
CN101155823A CNA2006800064632A CN200680006463A CN101155823A CN 101155823 A CN101155823 A CN 101155823A CN A2006800064632 A CNA2006800064632 A CN A2006800064632A CN 200680006463 A CN200680006463 A CN 200680006463A CN 101155823 A CN101155823 A CN 101155823A
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China
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benzoglyoxaline
androstane
compound
diene
dingbing
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English (en)
Chinese (zh)
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A·布罗迪
V·恩雅
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University of Maryland Baltimore
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University of Maryland Baltimore
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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)
CNA2006800064632A 2005-03-02 2006-03-02 新的c-17-杂芳基甾族的cyp17抑制剂/抗雄激素物质：其合成，体外生物学活性，药代动力学和抗肿瘤活性 Pending CN101155823A (zh)

Applications Claiming Priority (2)

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US65739005P 2005-03-02 2005-03-02
US60/657,390 2005-03-02

Related Child Applications (1)

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CN2013101036754A Division CN103349664A (zh) 2005-03-02 2006-03-02 含甾族的c-17苯并吡咯的组合物

Publications (1)

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CN101155823A true CN101155823A (zh) 2008-04-02

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CNA2006800064632A Pending CN101155823A (zh) 2005-03-02 2006-03-02 新的c-17-杂芳基甾族的cyp17抑制剂/抗雄激素物质：其合成，体外生物学活性，药代动力学和抗肿瘤活性
CN2013101036754A Pending CN103349664A (zh) 2005-03-02 2006-03-02 含甾族的c-17苯并吡咯的组合物

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EA (1) EA019560B1 (enExample)
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WO (1) WO2006093993A1 (enExample)
ZA (1) ZA200708106B (enExample)

Cited By (4)

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CN102822190A (zh) * 2009-11-13 2012-12-12 拓凯制药公司 哺乳动物的类固醇代谢物
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
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
US9439912B2 (en) 2013-03-14 2016-09-13 University Of Maryland, Baltimore Androgen receptor down-regulating agents and uses thereof

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US8569275B2 (en) 2002-08-28 2013-10-29 Harbor Therapeutics, Inc. Steroids having 7-oxgen and 17-heteroaryl substitution
EA019560B1 (ru) * 2005-03-02 2014-04-30 Юнивесити Оф Мэриленд, Балтимор Способ лечения простаты (варианты)
US20100047338A1 (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
WO2008154402A2 (en) 2007-06-06 2008-12-18 University Of Maryland, Baltimore 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
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
WO2010024930A2 (en) 2008-08-28 2010-03-04 President And Fellows Of Harvard College Cortistatin analogues and syntheses therof
US20100105700A1 (en) * 2008-10-28 2010-04-29 Lead Therapeutics, Inc. Decahydro-1h-indenoquinolinone and decahydro-3h-cyclopentaphenanthridinone cyp17 inhibitors
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
US8791095B2 (en) 2009-02-05 2014-07-29 Tokai Pharmaceuticals, Inc. Steroidal CYP17 inhibitors/antiandrogens
AU2010210422A1 (en) * 2009-02-05 2011-08-18 Tokai Pharmaceuticals, Inc. Novel prodrugs of steroidal CYP17 inhibitors/antiandrogens
UY32730A (es) 2009-06-26 2011-01-31 Novartis Ag Inhibidores de cyp17
AU2010279398A1 (en) * 2009-08-07 2012-03-08 Tokai Pharmaceuticals, Inc. Treatment of prostate cancer
CA2782266A1 (en) * 2009-11-30 2011-06-03 Harbor Biosciences, Inc. Anticancer compounds and screening method
EP2627648A1 (en) 2010-09-16 2013-08-21 Novartis AG 17aHYDROXYLASE/C17,20-LYASE INHIBITORS
WO2012083112A2 (en) * 2010-12-16 2012-06-21 Biomarin Pharmaceutical Inc. Cyp11b, cyp17, and/or cyp21 inhibitors
MX359399B (es) 2011-04-28 2018-09-27 Novartis Ag Inhibidores de 17alfa-hidroxilasa/c17-20-liasa.
JP2014523445A (ja) * 2011-07-18 2014-09-11 トーカイ ファーマシューティカルズ，インク． 前立腺癌を処置するための新規な組成物及び方法
US20150005265A1 (en) * 2011-12-22 2015-01-01 Susan Stewart Methods and compositions for combination therapy using p13k/mtor inhibitores
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
ES2709480T3 (es) 2013-12-24 2019-04-16 Harvard College Análogos de cortistatina y síntesis y usos de los mismos
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
WO2017066697A1 (en) 2015-10-14 2017-04-20 Dou Qingping 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
WO2018029223A1 (en) * 2016-08-08 2018-02-15 Industriale Chimica S.R.L. PROCESS FOR THE PREPARATION OF 3ß-HYDROXY-17-(1H-BENZIMIDAZOL-1-YL)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
ES3026226T3 (en) * 2018-02-13 2025-06-10 Dana Farber Cancer Inst Inc Cyclin-dependent kinase degraders and methods of use
CA3089588A1 (en) * 2018-02-13 2019-08-22 Dana-Farber Cancer Institute, Inc. Cyclin-dependent kinase inhibitors and methods of use
US12410194B2 (en) 2019-11-26 2025-09-09 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 (enExample) * 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
PL1660115T3 (pl) 2003-07-29 2011-11-30 Dompe Spa Farmaceutyczna kombinacja G-CSF i PLGF użyteczna wobec komórek macierzystych krwi
EA019560B1 (ru) * 2005-03-02 2014-04-30 Юнивесити Оф Мэриленд, Балтимор Способ лечения простаты (варианты)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102822190A (zh) * 2009-11-13 2012-12-12 拓凯制药公司 哺乳动物的类固醇代谢物
CN102822190B (zh) * 2009-11-13 2016-03-30 拓凯制药公司 哺乳动物的类固醇代谢物
US9439912B2 (en) 2013-03-14 2016-09-13 University Of Maryland, Baltimore Androgen receptor down-regulating agents and uses thereof
US9884067B2 (en) 2013-03-14 2018-02-06 University Of Maryland, Baltimore Androgen receptor down-regulating agents and uses thereof
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
US9808472B2 (en) 2013-08-12 2017-11-07 Tokai Pharmaceuticals, Inc. Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies
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

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CA2599953A1 (en) 2006-09-08
IL185608A0 (en) 2008-01-06
JP2012255026A (ja) 2012-12-27
DE602006017175D1 (de) 2010-11-11
PL1853619T3 (pl) 2011-03-31
WO2006093993A1 (en) 2006-09-08
EP1853619B1 (en) 2010-09-29
IL210480A0 (en) 2011-03-31
JP5130453B2 (ja) 2013-01-30
IL185608A (en) 2016-06-30
EP1853619A1 (en) 2007-11-14
CN103349664A (zh) 2013-10-16
PL2206719T3 (pl) 2015-03-31
HK1115387A1 (en) 2008-11-28
NZ561571A (en) 2009-09-25
BRPI0607523A2 (pt) 2009-09-08
AU2006218711A2 (en) 2006-09-08
JP2008536807A (ja) 2008-09-11
US20080280864A1 (en) 2008-11-13
KR101380959B1 (ko) 2014-04-04
MX2007010593A (es) 2008-02-20
EP1853619A4 (en) 2009-08-26
DK2206719T3 (en) 2015-01-26
US7875599B2 (en) 2011-01-25
PT1853619E (pt) 2011-01-03
ES2528055T3 (es) 2015-02-03
AU2006218711A1 (en) 2006-09-08
ATE482969T1 (de) 2010-10-15
AU2006218711B2 (en) 2010-11-11
EP2206719B1 (en) 2014-10-22
IL210480A (en) 2015-06-30
EA200701872A1 (ru) 2008-06-30
IL210478A0 (en) 2011-03-31
EA019560B1 (ru) 2014-04-30
PT2206719E (pt) 2015-02-05
ZA200708106B (en) 2008-12-31
SI1853619T1 (sl) 2011-01-31
JP5613206B2 (ja) 2014-10-22
ES2353413T3 (es) 2011-03-01
EP2206719A3 (en) 2011-01-05
KR20070120119A (ko) 2007-12-21
EP2206719A2 (en) 2010-07-14
DK1853619T3 (da) 2011-01-10
CA2599953C (en) 2013-08-13
SI2206719T1 (sl) 2015-03-31

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Application publication date: 20080402