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TW200621725A - Novel benzimidazole derivatives useful as selective androgen receptor modulators (sarms) - Google Patents

Novel benzimidazole derivatives useful as selective androgen receptor modulators (sarms)

Info

Publication number
TW200621725A
TW200621725A TW094133855A TW94133855A TW200621725A TW 200621725 A TW200621725 A TW 200621725A TW 094133855 A TW094133855 A TW 094133855A TW 94133855 A TW94133855 A TW 94133855A TW 200621725 A TW200621725 A TW 200621725A
Authority
TW
Taiwan
Prior art keywords
androgen receptor
sarms
benzimidazole derivatives
receptor modulators
derivatives useful
Prior art date
Application number
TW094133855A
Other languages
English (en)
Inventor
Raymond Ng
Zhihua Sui
Jihua Guan
James C Lanter
Vernon C Alford Jr
Original Assignee
Janssen Pharmaceutica Nv
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=35825468&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TW200621725(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of TW200621725A publication Critical patent/TW200621725A/zh

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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 only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16Masculine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26Androgens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28Antiandrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/10Radicals substituted by halogen atoms or nitro radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/12Radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/16Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Virology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Dermatology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Nutrition Science (AREA)
  • Hematology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW094133855A 2004-09-30 2005-09-29 Novel benzimidazole derivatives useful as selective androgen receptor modulators (sarms) TW200621725A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US61475104P 2004-09-30 2004-09-30

Publications (1)

Publication Number Publication Date
TW200621725A true TW200621725A (en) 2006-07-01

Family

ID=35825468

Family Applications (1)

Application Number Title Priority Date Filing Date
TW094133855A TW200621725A (en) 2004-09-30 2005-09-29 Novel benzimidazole derivatives useful as selective androgen receptor modulators (sarms)

Country Status (10)

Country Link
US (3) US7566733B2 (zh)
EP (1) EP1805147B1 (zh)
JP (1) JP4953456B2 (zh)
CN (1) CN101065363B (zh)
AR (1) AR050966A1 (zh)
AU (1) AU2005292345B9 (zh)
CA (1) CA2582356A1 (zh)
MY (1) MY147985A (zh)
TW (1) TW200621725A (zh)
WO (1) WO2006039243A1 (zh)

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US8409282B2 (en) 2004-10-20 2013-04-02 Vertiflex, Inc. Systems and methods for posterior dynamic stabilization of the spine
US8613747B2 (en) 2004-10-20 2013-12-24 Vertiflex, Inc. Spacer insertion instrument
US8167944B2 (en) 2004-10-20 2012-05-01 The Board Of Trustees Of The Leland Stanford Junior University Systems and methods for posterior dynamic stabilization of the spine
US7763074B2 (en) 2004-10-20 2010-07-27 The Board Of Trustees Of The Leland Stanford Junior University Systems and methods for posterior dynamic stabilization of the spine
US9161783B2 (en) 2004-10-20 2015-10-20 Vertiflex, Inc. Interspinous spacer
US8277488B2 (en) 2004-10-20 2012-10-02 Vertiflex, Inc. Interspinous spacer
WO2009009049A2 (en) 2004-10-20 2009-01-15 Vertiflex, Inc. Interspinous spacer
US9119680B2 (en) 2004-10-20 2015-09-01 Vertiflex, Inc. Interspinous spacer
US8945183B2 (en) 2004-10-20 2015-02-03 Vertiflex, Inc. Interspinous process spacer instrument system with deployment indicator
US8128662B2 (en) 2004-10-20 2012-03-06 Vertiflex, Inc. Minimally invasive tooling for delivery of interspinous spacer
US8317864B2 (en) 2004-10-20 2012-11-27 The Board Of Trustees Of The Leland Stanford Junior University Systems and methods for posterior dynamic stabilization of the spine
US8152837B2 (en) 2004-10-20 2012-04-10 The Board Of Trustees Of The Leland Stanford Junior University Systems and methods for posterior dynamic stabilization of the spine
US8123807B2 (en) 2004-10-20 2012-02-28 Vertiflex, Inc. Systems and methods for posterior dynamic stabilization of the spine
US8425559B2 (en) 2004-10-20 2013-04-23 Vertiflex, Inc. Systems and methods for posterior dynamic stabilization of the spine
US9023084B2 (en) 2004-10-20 2015-05-05 The Board Of Trustees Of The Leland Stanford Junior University Systems and methods for stabilizing the motion or adjusting the position of the spine
EP1809607B1 (en) * 2004-11-02 2008-12-17 Pfizer, Inc. Sulfonyl benzimidazole derivatives
WO2009086010A2 (en) 2004-12-06 2009-07-09 Vertiflex, Inc. Spacer insertion instrument
NZ570539A (en) 2006-01-24 2011-07-29 Janssen Pharmaceutica Nv 2-substituted benzimidazoles as selective androgen receptor modulators (SARMS)
US8845726B2 (en) 2006-10-18 2014-09-30 Vertiflex, Inc. Dilator
CA2684461C (en) 2007-04-16 2015-06-30 Vertiflex Inc. Interspinous spacer
SI2154966T1 (sl) * 2007-04-20 2014-02-28 The Research Foundation Of State University Of New York Benzimidazoli in njihovi farmacevtski sestavki
WO2009091922A2 (en) 2008-01-15 2009-07-23 Vertiflex, Inc. Interspinous spacer
MX2010009162A (es) 2008-02-22 2010-12-21 Radius Health Inc Moduladores selectivos del receptor de androgeno.
US8268872B2 (en) 2008-02-22 2012-09-18 Radius Health, Inc. Selective androgen receptor modulators
WO2009123164A1 (ja) * 2008-04-02 2009-10-08 塩野義製薬株式会社 血管内皮リパーゼ阻害活性を有するヘテロ環誘導体
EP2512357B1 (en) 2009-12-15 2016-07-13 Vertiflex, Inc. Spinal spacer for cervical and other vertebra, and associated systems
MX338831B (es) 2010-02-04 2016-05-03 Radius Health Inc Moduladores selectivos de receptores de androgenos.
ME02474B (me) 2010-05-12 2017-02-20 Radius Health Inc Terapijski režimi
US8642632B2 (en) 2010-07-02 2014-02-04 Radius Health, Inc. Selective androgen receptor modulators
EP2621901B1 (en) 2010-09-28 2015-07-29 Radius Health, Inc Selective androgen receptor modulators
WO2013116823A1 (en) * 2012-02-02 2013-08-08 The Research Foundation Of State University Of New York Benzimidazoles and uses thereof
US9675303B2 (en) 2013-03-15 2017-06-13 Vertiflex, Inc. Visualization systems, instruments and methods of using the same in spinal decompression procedures
WO2015138611A2 (en) 2014-03-11 2015-09-17 Colorado State University Research Foundation Methods for improved in vitro-in vivo efficacy determination
US9421264B2 (en) 2014-03-28 2016-08-23 Duke University Method of treating cancer using selective estrogen receptor modulators
SMT202300072T1 (it) 2014-03-28 2023-05-12 Univ Duke Cancro della mammella mediante l'utilizzo di modulatori selettivi del recetiore degli estrogeni
WO2015171814A1 (en) 2014-05-07 2015-11-12 Vertiflex, Inc. Spinal nerve decompression systems, dilation systems, and methods of using the same
CA3197570A1 (en) 2015-01-17 2016-07-21 Board Of Regents Of The University Of Texas System Small molecules for the treatment of primary cancer and cancer metastasis
RU2022108295A (ru) 2016-06-22 2022-04-06 Эллипсес Фарма Лтд Способы лечения ar+ рака молочной железы
CN117417263A (zh) 2017-01-05 2024-01-19 雷迪厄斯制药公司 Rad1901-2hcl的多晶型形式
WO2019079691A1 (en) 2017-10-19 2019-04-25 Jean Jiang SMALL MOLECULES FOR THE TREATMENT OF AUTOIMMUNE DISORDERS
CN112423844B (zh) 2018-07-04 2024-08-13 雷迪厄斯制药公司 Rad1901-2hcl的多晶型形式
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Also Published As

Publication number Publication date
AU2005292345A1 (en) 2006-04-13
AU2005292345B9 (en) 2011-12-15
WO2006039243A1 (en) 2006-04-13
CA2582356A1 (en) 2006-04-13
US8586616B2 (en) 2013-11-19
EP1805147B1 (en) 2014-08-13
US20060116412A1 (en) 2006-06-01
CN101065363B (zh) 2012-05-02
CN101065363A (zh) 2007-10-31
US20090258909A1 (en) 2009-10-15
JP2008514707A (ja) 2008-05-08
AU2005292345B2 (en) 2011-12-01
MY147985A (en) 2013-02-28
EP1805147A1 (en) 2007-07-11
US7566733B2 (en) 2009-07-28
AR050966A1 (es) 2006-12-06
JP4953456B2 (ja) 2012-06-13
US7879895B2 (en) 2011-02-01
US20110086883A1 (en) 2011-04-14

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