HRP20130405T1 - 2-substituted benzimidazoles as selective androgen receptor modulators (sarms) - Google Patents

2-substituted benzimidazoles as selective androgen receptor modulators (sarms)

Info

Publication number
HRP20130405T1
HRP20130405T1 HRP20130405TT HRP20130405T HRP20130405T1 HR P20130405 T1 HRP20130405 T1 HR P20130405T1 HR P20130405T T HRP20130405T T HR P20130405TT HR P20130405 T HRP20130405 T HR P20130405T HR P20130405 T1 HRP20130405 T1 HR P20130405T1
Authority
HR
Croatia
Prior art keywords
androgen receptor
sarms
receptor modulators
selective androgen
substituted benzimidazoles
Prior art date
Application number
HRP20130405TT
Other languages
English (en)
Inventor
Alford C. Vernon Jr.
James C. Lanter
Raymond A. Ng
Zhihua Sui
Original Assignee
Janssen Pharmaceutica N.V.
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 Janssen Pharmaceutica N.V. filed Critical Janssen Pharmaceutica N.V.
Publication of HRP20130405T1 publication Critical patent/HRP20130405T1/hr

Links

Classifications

    • 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
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • 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
    • 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/14Heterocyclic 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 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
    • C07D413/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Virology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • AIDS & HIV (AREA)
  • Pregnancy & Childbirth (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
HRP20130405TT 2006-01-24 2013-05-08 2-substituted benzimidazoles as selective androgen receptor modulators (sarms) HRP20130405T1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US76154806P 2006-01-24 2006-01-24
PCT/US2007/060883 WO2007087518A2 (en) 2006-01-24 2007-01-23 2-substituted benzimidazoles as selective androgen receptor modulators (sarms)

Publications (1)

Publication Number Publication Date
HRP20130405T1 true HRP20130405T1 (en) 2013-07-31

Family

ID=38180195

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20130405TT HRP20130405T1 (en) 2006-01-24 2013-05-08 2-substituted benzimidazoles as selective androgen receptor modulators (sarms)

Country Status (26)

Country Link
US (4) US7932399B2 (hr)
EP (1) EP1984343B1 (hr)
JP (1) JP5140604B2 (hr)
KR (1) KR101514989B1 (hr)
CN (1) CN101410381B (hr)
AU (1) AU2007208139B2 (hr)
BR (1) BRPI0706726B8 (hr)
CA (1) CA2640046C (hr)
CR (1) CR10243A (hr)
DK (1) DK1984343T3 (hr)
EA (1) EA015542B1 (hr)
EC (1) ECSP088648A (hr)
ES (1) ES2402305T3 (hr)
HR (1) HRP20130405T1 (hr)
IL (1) IL192978A (hr)
MY (1) MY149459A (hr)
NI (1) NI200800206A (hr)
NO (1) NO341501B1 (hr)
NZ (1) NZ570539A (hr)
PL (1) PL1984343T3 (hr)
PT (1) PT1984343E (hr)
RS (1) RS52756B (hr)
SI (1) SI1984343T1 (hr)
UA (1) UA94441C2 (hr)
WO (1) WO2007087518A2 (hr)
ZA (1) ZA200807277B (hr)

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US7932399B2 (en) * 2006-01-24 2011-04-26 Janssen Pharmaceutica Nv 2-substituted benzimidazoles as selective androgen receptor modulators (SARMS)
US8143280B2 (en) * 2007-09-27 2012-03-27 Hoffmann-La Roche Inc. Glucocorticoid receptor antagonists
US8268872B2 (en) 2008-02-22 2012-09-18 Radius Health, Inc. Selective androgen receptor modulators
MX2010009162A (es) 2008-02-22 2010-12-21 Radius Health Inc Moduladores selectivos del receptor de androgeno.
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
EP2531029B1 (en) 2010-02-04 2016-10-19 Radius Health, Inc. Selective androgen receptor modulators
KR20130034011A (ko) * 2010-02-22 2013-04-04 신젠타 파티서페이션즈 아게 살곤충 화합물로서의 디하이드로푸란 유도체
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
BR112013007685B1 (pt) 2010-09-28 2021-11-09 Radius Pharmaceuticals, Inc Compostos moduladores de receptor andrógeno seletivos, composição farmacêutica compreendendo os referidos compostos, método de identificação de um composto capaz de modular um receptor andrógeno, usos de um composto ou da composição e processo para a preparação de um composto
RU2666530C2 (ru) * 2012-01-12 2018-09-11 Йейл Юниверсити Соединения и способы усиления деградации белков-мишеней и других полипептидов с помощью е3 убиквитин лигазы
JP5947465B2 (ja) * 2012-10-01 2016-07-06 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Cns活性剤としてのベンズイミダゾール類
EP4035664A3 (en) 2014-03-28 2022-11-30 Duke University Treating cancer using selective estrogen receptor modulators
US9421264B2 (en) 2014-03-28 2016-08-23 Duke University Method of treating cancer using selective estrogen receptor modulators
RU2769527C2 (ru) 2016-06-22 2022-04-01 Эллипсес Фарма Лтд Способы лечения ar+ рака молочной железы
KR102322802B1 (ko) 2017-01-05 2021-11-04 래디어스 파마슈티컬스, 인코포레이티드 Rad1901-2hcl의 다형 형태
CN108129462B (zh) * 2018-01-19 2020-03-10 广东工业大学 一种二氧戊环基苯并咪唑化合物及其制备方法
US11643385B2 (en) 2018-07-04 2023-05-09 Radius Pharmaceuticals, Inc. Polymorphic forms of RAD1901-2HCl
WO2020252407A1 (en) * 2019-06-12 2020-12-17 The Wistar Institute Acetyl-coa synthetase 2 (acss2) inhibitors and methods using same

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Also Published As

Publication number Publication date
SI1984343T1 (sl) 2013-05-31
WO2007087518A3 (en) 2007-09-20
KR20080090524A (ko) 2008-10-08
US20110166102A1 (en) 2011-07-07
NO341501B1 (no) 2017-11-27
IL192978A0 (en) 2009-02-11
ECSP088648A (es) 2008-08-29
BRPI0706726A2 (pt) 2011-04-05
WO2007087518A2 (en) 2007-08-02
US7932399B2 (en) 2011-04-26
US9120830B2 (en) 2015-09-01
CN101410381A (zh) 2009-04-15
CA2640046A1 (en) 2008-07-02
BRPI0706726B1 (pt) 2020-09-15
EA200870197A1 (ru) 2008-12-30
US8802865B2 (en) 2014-08-12
ZA200807277B (en) 2009-12-30
US20140309261A1 (en) 2014-10-16
EA015542B1 (ru) 2011-08-30
PT1984343E (pt) 2013-05-15
EP1984343B1 (en) 2013-02-27
BRPI0706726B8 (pt) 2021-05-25
AU2007208139B2 (en) 2012-09-27
EP1984343A2 (en) 2008-10-29
US8575206B2 (en) 2013-11-05
UA94441C2 (ru) 2011-05-10
IL192978A (en) 2014-09-30
JP2009524687A (ja) 2009-07-02
NO20083554L (no) 2008-10-20
KR101514989B1 (ko) 2015-04-24
RS52756B (en) 2013-08-30
CN101410381B (zh) 2011-08-03
DK1984343T3 (da) 2013-03-25
NI200800206A (es) 2013-01-18
CA2640046C (en) 2015-06-09
ES2402305T3 (es) 2013-04-30
NZ570539A (en) 2011-07-29
US20070208014A1 (en) 2007-09-06
CR10243A (es) 2009-01-14
MY149459A (en) 2013-08-30
US20140031317A1 (en) 2014-01-30
AU2007208139A1 (en) 2007-08-02
JP5140604B2 (ja) 2013-02-06
PL1984343T3 (pl) 2013-08-30

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