ZA200807277B - 2-Substituted bensimidazoles as selective androgen receptor modulators (SARMS) - Google Patents

2-Substituted bensimidazoles as selective androgen receptor modulators (SARMS)

Info

Publication number
ZA200807277B
ZA200807277B ZA200807277A ZA200807277A ZA200807277B ZA 200807277 B ZA200807277 B ZA 200807277B ZA 200807277 A ZA200807277 A ZA 200807277A ZA 200807277 A ZA200807277 A ZA 200807277A ZA 200807277 B ZA200807277 B ZA 200807277B
Authority
ZA
South Africa
Prior art keywords
bensimidazoles
sarms
substituted
androgen receptor
receptor modulators
Prior art date
Application number
ZA200807277A
Other languages
English (en)
Inventor
Jr Alford C Vernon
James C Lanter
Raymond A Ng
Zhihau Sui
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
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of ZA200807277B publication Critical patent/ZA200807277B/xx

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16—Masculine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • C07D235/12—Radicals substituted by oxygen atoms
    • 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
    • C07D235/16—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Pregnancy & Childbirth (AREA)
  • Diabetes (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
ZA200807277A 2006-01-24 2008-08-22 2-Substituted bensimidazoles as selective androgen receptor modulators (SARMS) ZA200807277B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US76154806P 2006-01-24 2006-01-24

Publications (1)

Publication Number Publication Date
ZA200807277B true ZA200807277B (en) 2009-12-30

Family

ID=38180195

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA200807277A ZA200807277B (en) 2006-01-24 2008-08-22 2-Substituted bensimidazoles as selective androgen receptor modulators (SARMS)

Country Status (26)

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

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BRPI0706726B8 (pt) 2006-01-24 2021-05-25 Janssen Pharmaceutica Nv benzimidazóis 2-substituídos como modulares seletivos de receptor de andrógeno (sarms), composição farmacêutica que os compreende e processo para preparar
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
CA2788907A1 (en) 2010-02-04 2011-08-11 Radius Health, Inc. Selective androgen receptor modulators
AP2012006432A0 (en) * 2010-02-22 2012-08-31 Syngenta Participations Ag Dihydrofuran derivatives as insecticidal compounds
HUE030072T2 (en) 2010-05-12 2017-04-28 Radius Health Inc Therapeutic prescriptions
US8642632B2 (en) 2010-07-02 2014-02-04 Radius Health, Inc. Selective androgen receptor modulators
US9133182B2 (en) 2010-09-28 2015-09-15 Radius Health, Inc. Selective androgen receptor modulators
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
CN104703981B (zh) * 2012-10-01 2017-03-29 霍夫曼-拉罗奇有限公司 作为cns活性药剂的苯并咪唑类化合物
RS64115B1 (sr) 2014-03-28 2023-04-28 Univ Duke Lečenje kancera dojke upotrebom selektivnih modulatora receptora estrogena
US9421264B2 (en) 2014-03-28 2016-08-23 Duke University Method of treating cancer using selective estrogen receptor modulators
KR20220035276A (ko) 2016-06-22 2022-03-21 일립시스 파마 리미티드 Ar+ 유방암 치료 방법
CA3047411A1 (en) 2017-01-05 2018-07-12 Radius Pharmaceuticals, Inc. Polymorphic forms of rad1901-2hcl
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
WO2020010216A1 (en) 2018-07-04 2020-01-09 Radius Pharmaceuticals, Inc. Polymorphic forms of rad 1901-2hcl
AU2020292419A1 (en) * 2019-06-12 2022-02-03 The Wistar Institute Acetyl-CoA synthetase 2 (ACSS2) inhibitors and methods using same

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BRPI0706726B8 (pt) * 2006-01-24 2021-05-25 Janssen Pharmaceutica Nv benzimidazóis 2-substituídos como modulares seletivos de receptor de andrógeno (sarms), composição farmacêutica que os compreende e processo para preparar
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Also Published As

Publication number Publication date
US7932399B2 (en) 2011-04-26
WO2007087518A3 (en) 2007-09-20
ES2402305T3 (es) 2013-04-30
RS52756B (en) 2013-08-30
NO341501B1 (no) 2017-11-27
MY149459A (en) 2013-08-30
DK1984343T3 (da) 2013-03-25
US9120830B2 (en) 2015-09-01
US20140309261A1 (en) 2014-10-16
JP5140604B2 (ja) 2013-02-06
NI200800206A (es) 2013-01-18
ECSP088648A (es) 2008-08-29
WO2007087518A2 (en) 2007-08-02
BRPI0706726A2 (pt) 2011-04-05
CR10243A (es) 2009-01-14
BRPI0706726B1 (pt) 2020-09-15
HRP20130405T1 (en) 2013-07-31
NO20083554L (no) 2008-10-20
CA2640046A1 (en) 2008-07-02
EP1984343A2 (en) 2008-10-29
KR101514989B1 (ko) 2015-04-24
KR20080090524A (ko) 2008-10-08
EA015542B1 (ru) 2011-08-30
JP2009524687A (ja) 2009-07-02
US20110166102A1 (en) 2011-07-07
US8802865B2 (en) 2014-08-12
US20070208014A1 (en) 2007-09-06
IL192978A0 (en) 2009-02-11
IL192978A (en) 2014-09-30
BRPI0706726B8 (pt) 2021-05-25
UA94441C2 (ru) 2011-05-10
CA2640046C (en) 2015-06-09
CN101410381B (zh) 2011-08-03
SI1984343T1 (sl) 2013-05-31
PL1984343T3 (pl) 2013-08-30
AU2007208139A1 (en) 2007-08-02
CN101410381A (zh) 2009-04-15
EP1984343B1 (en) 2013-02-27
EA200870197A1 (ru) 2008-12-30
US20140031317A1 (en) 2014-01-30
PT1984343E (pt) 2013-05-15
US8575206B2 (en) 2013-11-05
NZ570539A (en) 2011-07-29
AU2007208139B2 (en) 2012-09-27

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