KR101380959B1 - 신규 ｃ-17-헤테로아릴 스테로이드성 ｃｙｐ17억제제／항안드로겐：합성, 시험관내 생물학적 활성,약물동태학 및 항종양 활성 - Google Patents

신규 ｃ-17-헤테로아릴 스테로이드성 ｃｙｐ17억제제／항안드로겐：합성, 시험관내 생물학적 활성,약물동태학 및 항종양 활성 Download PDF

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KR101380959B1
KR101380959B1 KR1020077022440A KR20077022440A KR101380959B1 KR 101380959 B1 KR101380959 B1 KR 101380959B1 KR 1020077022440 A KR1020077022440 A KR 1020077022440A KR 20077022440 A KR20077022440 A KR 20077022440A KR 101380959 B1 KR101380959 B1 KR 101380959B1
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KR20070120119A (ko
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안젤라 브로디
빈센트 자르
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유니버시티 오브 매릴랜드, 발티모어
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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)
KR1020077022440A 2005-03-02 2006-03-02 신규 ｃ-17-헤테로아릴 스테로이드성 ｃｙｐ17억제제／항안드로겐：합성, 시험관내 생물학적 활성,약물동태학 및 항종양 활성 Expired - Fee Related KR101380959B1 (ko)

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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KR20070120119A KR20070120119A (ko) 2007-12-21
KR101380959B1 true KR101380959B1 (ko) 2014-04-04

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EP (2) EP1853619B1 (https=)
JP (2) JP5130453B2 (https=)
KR (1) KR101380959B1 (https=)
CN (2) CN103349664A (https=)
AT (1) ATE482969T1 (https=)
AU (1) AU2006218711B2 (https=)
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DE (1) DE602006017175D1 (https=)
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EA (1) EA019560B1 (https=)
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IL (3) IL185608A (https=)
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PL (2) PL2206719T3 (https=)
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Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8569275B2 (en) 2002-08-28 2013-10-29 Harbor Therapeutics, Inc. Steroids having 7-oxgen and 17-heteroaryl substitution
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

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
CLEMENT, O. O. et al, Three Dimensional Pharmacophore Modeling of Human CYP18 Inhibitors. Potential Agents for Prostate Cancer Therapy, J. Med. Chem., 2003, Vol. 46, No. 12, pages 2345-2351 *

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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
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
AU2006218711B2 (en) 2010-11-11
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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