AU2014247941C1 - Nonsteroidal and steroidal compounds with potent androgen receptor down-regulation and anti prostate cancer activity - Google Patents

Nonsteroidal and steroidal compounds with potent androgen receptor down-regulation and anti prostate cancer activity Download PDF

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Publication number
AU2014247941C1
AU2014247941C1 AU2014247941A AU2014247941A AU2014247941C1 AU 2014247941 C1 AU2014247941 C1 AU 2014247941C1 AU 2014247941 A AU2014247941 A AU 2014247941A AU 2014247941 A AU2014247941 A AU 2014247941A AU 2014247941 C1 AU2014247941 C1 AU 2014247941C1
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Prior art keywords
benzimidazol
benzimidazolylphenyl
diene
androsta
mhz
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AU2014247941A
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AU2014247941A1 (en
AU2014247941B2 (en
Inventor
Vincent C.O. Njar
Purushottamachar Puranik
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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 AU2014247941A1 publication Critical patent/AU2014247941A1/en
Assigned to UNIVERSITY OF MARYLAND, BALTIMORE reassignment UNIVERSITY OF MARYLAND, BALTIMORE Request for Assignment Assignors: NJAR, VINCENT, PURUSHOTTAMACHAR, PURANIK, 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08—Radicals containing only hydrogen and carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2014247941A 2013-04-04 2014-04-04 Nonsteroidal and steroidal compounds with potent androgen receptor down-regulation and anti prostate cancer activity Active AU2014247941C1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361808345P 2013-04-04 2013-04-04
US61/808,345 2013-04-04
US201361808902P 2013-04-05 2013-04-05
US61/808,902 2013-04-05
PCT/US2014/033063 WO2014165815A2 (en) 2013-04-04 2014-04-04 Nonsteroidal and steroidal compounds with potent androgen receptor down-regulation and anti prostate cancer activity

Publications (3)

Publication Number Publication Date
AU2014247941A1 AU2014247941A1 (en) 2015-10-22
AU2014247941B2 AU2014247941B2 (en) 2017-04-27
AU2014247941C1 true AU2014247941C1 (en) 2019-10-31

Family

ID=51659362

Family Applications (1)

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AU2014247941A Active AU2014247941C1 (en) 2013-04-04 2014-04-04 Nonsteroidal and steroidal compounds with potent androgen receptor down-regulation and anti prostate cancer activity

Country Status (6)

Country Link
US (2) US9694005B2 (https=)
EP (2) EP2991644B1 (https=)
JP (1) JP6417392B2 (https=)
AU (1) AU2014247941C1 (https=)
CA (2) CA3151555A1 (https=)
WO (1) WO2014165815A2 (https=)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
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US10675289B2 (en) * 2014-10-02 2020-06-09 University Of Maryland, Baltimore Methods of treating pancreatic cancer
WO2017201683A1 (en) * 2016-05-25 2017-11-30 Merck Sharp & Dohme Corp. Substituted tetrahydroisoquinoline compounds useful as gpr120 agonists
US12391725B2 (en) 2016-06-22 2025-08-19 National Institutes Of Health (Nih), U.S. Dept. Of Health And Human Services (Dhhs), U.S. Government Method for production of novel galeterone analogs and uses thereof
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
CN106902112B (zh) * 2017-03-07 2019-06-04 中国医学科学院医药生物技术研究所 Imb-a6作为雄激素受体拮抗剂的应用
CN111943889B (zh) * 2020-07-24 2022-07-22 中国医学科学院医药生物技术研究所 一种双芳香基胺类化合物及其制备方法和应用
CN116444599B (zh) * 2022-01-07 2026-02-03 中国科学院上海药物研究所 甾体类化合物及制备方法和用途
WO2024064026A1 (en) * 2022-09-19 2024-03-28 Alterome Therapeutics, Inc. Akt1 modulators
CN120225521A (zh) * 2022-09-26 2025-06-27 亚特罗姆医疗公司 Akt1调节剂
WO2024091899A1 (en) * 2022-10-25 2024-05-02 University Of Maryland, Baltimore Salts of galeterone and salts of next generation galeterone analogs, and uses thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5360809A (en) * 1992-03-26 1994-11-01 Neurosearch A/S Imidazole compounds and their use as calcium channel blockers
US5541229A (en) * 1989-04-08 1996-07-30 Dr. Karl Thomae Gmbh Benzimidazoles and medicaments containing these compounds
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

Family Cites Families (10)

* Cited by examiner, † Cited by third party
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CA129379A (en) 1910-10-18 1910-11-22 John Clarence Bisland Hoe
IL95975A (en) * 1989-10-24 1997-06-10 Takeda Chemical Industries Ltd N-benzyl- 2-alkylbenzimidazole derivatives, their production and pharmaceutical compositions containing them
DE10342503A1 (de) 2003-09-12 2005-04-14 Merck Patent Gmbh Benzyl-Benzimidazolylderivate
US7875599B2 (en) * 2005-03-02 2011-01-25 University Of Maryland C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens, in vitro biological activities, pharmacokinetics and antitumor activity
EP2732819B1 (en) * 2008-02-07 2019-10-16 Massachusetts Eye & Ear Infirmary Compounds that enhance Atoh-1 expression
GB2470700B (en) * 2008-03-25 2012-08-08 Univ Maryland C-17 heteroaryl steroidal CYP17 inhibitors
GB2479337A (en) * 2009-02-05 2011-10-05 Tokai Pharmaceuticals Inc Combination of a 17 alpha-hydroxylase/c17, 20-lyase inhibitor with an additional therapeutic agent
WO2010091306A1 (en) * 2009-02-05 2010-08-12 Tokai Pharmaceuticals Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens
BR112014001440A2 (pt) * 2011-07-18 2017-02-21 Tokai Pharmaceuticals Inc novas composições e métodos para o tratamento de câncer de próstata
KR20150127720A (ko) * 2013-03-14 2015-11-17 유니버시티 오브 매릴랜드, 발티모어 안드로겐 수용체 하향 조절제 및 그의 용도

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5541229A (en) * 1989-04-08 1996-07-30 Dr. Karl Thomae Gmbh Benzimidazoles and medicaments containing these compounds
US5360809A (en) * 1992-03-26 1994-11-01 Neurosearch A/S Imidazole compounds and their use as calcium channel blockers
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

Also Published As

Publication number Publication date
EP2991644A2 (en) 2016-03-09
CA2908577A1 (en) 2014-10-09
JP2016515630A (ja) 2016-05-30
WO2014165815A2 (en) 2014-10-09
US9694005B2 (en) 2017-07-04
WO2014165815A3 (en) 2014-12-31
US20160038476A1 (en) 2016-02-11
CA2908577C (en) 2022-05-31
AU2014247941A1 (en) 2015-10-22
US10617685B2 (en) 2020-04-14
JP6417392B2 (ja) 2018-11-07
US20170266181A1 (en) 2017-09-21
EP3514147B1 (en) 2022-08-03
EP2991644B1 (en) 2020-03-25
AU2014247941B2 (en) 2017-04-27
EP3514147A1 (en) 2019-07-24
CA3151555A1 (en) 2014-10-09
EP2991644A4 (en) 2017-02-08

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Owner name: UNIVERSITY OF MARYLAND, BALTIMORE

Free format text: FORMER APPLICANT(S): UNIVERSITY OF MARYLAND, BALTIMORE; PURUSHOTTAMACHAR, PURANIK; NJAR, VINCENT

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Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE INVENTOR TO READ NJAR, VINCENT C.O. AND PURANIK, PURUSHOTTAMACHAR