EA200701872A1 - C-17 гетероарильные стероидные соединения, фармацевтическая композиция на их основе и способ лечения рака простаты с их помощью - Google Patents

C-17 гетероарильные стероидные соединения, фармацевтическая композиция на их основе и способ лечения рака простаты с их помощью

Info

Publication number
EA200701872A1
EA200701872A1 EA200701872A EA200701872A EA200701872A1 EA 200701872 A1 EA200701872 A1 EA 200701872A1 EA 200701872 A EA200701872 A EA 200701872A EA 200701872 A EA200701872 A EA 200701872A EA 200701872 A1 EA200701872 A1 EA 200701872A1
Authority
EA
Eurasian Patent Office
Prior art keywords
treatment
prostate cancer
heteroarial
help
basis
Prior art date
Application number
EA200701872A
Other languages
English (en)
Other versions
EA019560B1 (ru
Inventor
Анджела Броди
Винсент Нджар
Original Assignee
Юнивесити Оф Мэриленд, Балтимор
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Юнивесити Оф Мэриленд, Балтимор filed Critical Юнивесити Оф Мэриленд, Балтимор
Publication of EA200701872A1 publication Critical patent/EA200701872A1/ru
Publication of EA019560B1 publication Critical patent/EA019560B1/ru

Links

Classifications

    • 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

Landscapes

  • 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)

Abstract

Предлагаются стероидные С-17 бензоазолы, пиримидиноазолы (азабензоазолы) и диазины, а также способы их синтеза, включающие способы, одним из этапов которых является реакция нуклеофильного винилового замещения по типу "присоединения-элиминирования" с участием 3β-ацетокси-17-хлоро-16-формиландроста-5,16-диена или его аналогов и бензоазольных или пиримидиноазольных нуклеофилов, и, кроме того, способы, одним из этапов которых является катализируемая палладием реакция кросс-сочетания с участием 17-иодоандроста-5,16-диен-3β-ола или его аналогов и трибутилстаннилдиазинов. Соединения являются сильными ингибиторами фермента CYP 17 человека, а также сильными антагонистами мутантных андрогеновых рецепторов (AR) и рецепторов дикого типа. Соединения могут применяться при лечении рака простаты человека.
EA200701872A 2005-03-02 2006-03-02 Способ лечения простаты (варианты) EA019560B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US65739005P 2005-03-02 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 (2)

Publication Number Publication Date
EA200701872A1 true EA200701872A1 (ru) 2008-06-30
EA019560B1 EA019560B1 (ru) 2014-04-30

Family

ID=36941503

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200701872A EA019560B1 (ru) 2005-03-02 2006-03-02 Способ лечения простаты (варианты)

Country Status (22)

Country Link
US (1) US7875599B2 (ru)
EP (2) EP2206719B1 (ru)
JP (2) JP5130453B2 (ru)
KR (1) KR101380959B1 (ru)
CN (2) CN103349664A (ru)
AT (1) ATE482969T1 (ru)
AU (1) AU2006218711B2 (ru)
BR (1) BRPI0607523A2 (ru)
CA (1) CA2599953C (ru)
DE (1) DE602006017175D1 (ru)
DK (2) DK2206719T3 (ru)
EA (1) EA019560B1 (ru)
ES (2) ES2353413T3 (ru)
HK (1) HK1115387A1 (ru)
IL (3) IL185608A (ru)
MX (1) MX2007010593A (ru)
NZ (1) NZ561571A (ru)
PL (2) PL2206719T3 (ru)
PT (2) PT2206719E (ru)
SI (2) SI1853619T1 (ru)
WO (1) WO2006093993A1 (ru)
ZA (1) ZA200708106B (ru)

Families Citing this family (35)

* 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
DK2206719T3 (en) 2005-03-02 2015-01-26 Univ Maryland A pharmaceutical composition comprising 3-BETA-HYDROXY-17- (1-H-benzimidazol-1-yl) androsta-5, 16-DIEN
US8110550B2 (en) 2007-06-06 2012-02-07 University Of Maryland, Baltimore HDAC inhibitors and hormone targeted drugs for the treatment of cancer
US20110105445A1 (en) * 2008-03-12 2011-05-05 University Of Maryland, Baltimore Androgen receptor inactivation contributes to antitumor efficacy of cyp17 inhibitors in prostate 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
WO2009129208A2 (en) * 2008-04-14 2009-10-22 University Of Maryland, Baltimore Compositions and methods of inducing endoplasmic reticulum stress reponse
WO2010024930A2 (en) 2008-08-28 2010-03-04 President And Fellows Of Harvard College Cortistatin analogues and syntheses therof
AU2009320250A1 (en) * 2008-10-28 2010-06-03 Biomarin Pharmaceutical Inc. Decahydro-1H-indenoquinolinone and decahydro-3H-cyclopentaphenanthridinone CYP17 inhibitors
US20110319369A1 (en) * 2009-02-05 2011-12-29 Tokai Pharmaceuticals, Inc. Combination of a 17 alpha-hydroxylase/c17, 20-lyase inhibitor with an additional therapeutic agent
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
EP3023433A1 (en) 2009-02-05 2016-05-25 Tokai Pharmaceuticals, Inc. Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens
GEP20156250B (en) 2009-06-26 2015-02-25 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
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
EP2627648A1 (en) 2010-09-16 2013-08-21 Novartis AG 17aHYDROXYLASE/C17,20-LYASE INHIBITORS
TW201307378A (zh) * 2010-12-16 2013-02-16 Biomarin Pharm Inc Ｃｙｐ１１ｂ、ｃｙｐ１７及／或ｃｙｐ２１抑制劑
ES2656218T3 (es) 2011-04-28 2018-02-26 Novartis Ag Inhibidores de 17 alfa-hidroxilasa/C17,20-liasa
CA2841960A1 (en) * 2011-07-18 2013-01-24 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
CA2904170A1 (en) 2013-03-14 2014-09-25 University Of Maryland, Baltimore Androgen receptor down-regulating agents and uses thereof
US9694005B2 (en) 2013-04-04 2017-07-04 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
EA201891279A1 (ru) 2013-12-24 2019-01-31 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
WO2016119742A1 (zh) * 2015-01-29 2016-08-04 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
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
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
WO2019160889A1 (en) * 2018-02-13 2019-08-22 Dana-Farber Cancer Institute, Inc. Cyclin-dependent kinase inhibitors and methods of use
EP3752517A4 (en) * 2018-02-13 2021-10-13 Dana-Farber Cancer Institute, Inc. CYCLINE DEPENDENT KINASE DEGRADATION AGENTS AND METHODS OF USE

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 (ru) * 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
AU2004262909B2 (en) 2003-07-29 2010-07-01 Dompe' S.P.A. Pharmaceutical combination of G-CSF and PlGF useful for blood stem cell
DK2206719T3 (en) * 2005-03-02 2015-01-26 Univ Maryland A pharmaceutical composition comprising 3-BETA-HYDROXY-17- (1-H-benzimidazol-1-yl) androsta-5, 16-DIEN

Also Published As

Publication number Publication date
AU2006218711A2 (en) 2006-09-08
KR101380959B1 (ko) 2014-04-04
PT2206719E (pt) 2015-02-05
EP2206719A3 (en) 2011-01-05
JP5130453B2 (ja) 2013-01-30
CA2599953C (en) 2013-08-13
IL185608A (en) 2016-06-30
DK2206719T3 (en) 2015-01-26
US7875599B2 (en) 2011-01-25
IL210478A0 (en) 2011-03-31
HK1115387A1 (ru) 2008-11-28
AU2006218711A1 (en) 2006-09-08
JP5613206B2 (ja) 2014-10-22
CA2599953A1 (en) 2006-09-08
JP2008536807A (ja) 2008-09-11
BRPI0607523A2 (pt) 2009-09-08
US20080280864A1 (en) 2008-11-13
DE602006017175D1 (de) 2010-11-11
IL185608A0 (en) 2008-01-06
AU2006218711B2 (en) 2010-11-11
KR20070120119A (ko) 2007-12-21
DK1853619T3 (da) 2011-01-10
CN103349664A (zh) 2013-10-16
PT1853619E (pt) 2011-01-03
EP1853619A4 (en) 2009-08-26
WO2006093993A1 (en) 2006-09-08
ES2528055T3 (es) 2015-02-03
IL210480A0 (en) 2011-03-31
IL210480A (en) 2015-06-30
SI1853619T1 (sl) 2011-01-31
MX2007010593A (es) 2008-02-20
ES2353413T3 (es) 2011-03-01
SI2206719T1 (sl) 2015-03-31
NZ561571A (en) 2009-09-25
ATE482969T1 (de) 2010-10-15
CN101155823A (zh) 2008-04-02
EP2206719B1 (en) 2014-10-22
EP1853619B1 (en) 2010-09-29
EP2206719A2 (en) 2010-07-14
PL2206719T3 (pl) 2015-03-31
ZA200708106B (en) 2008-12-31
PL1853619T3 (pl) 2011-03-31
EP1853619A1 (en) 2007-11-14
EA019560B1 (ru) 2014-04-30
JP2012255026A (ja) 2012-12-27

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Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU