WO2009014150A1 - ベンズイミダゾール誘導体 - Google Patents

ベンズイミダゾール誘導体 Download PDF

Info

Publication number
WO2009014150A1
WO2009014150A1 PCT/JP2008/063212 JP2008063212W WO2009014150A1 WO 2009014150 A1 WO2009014150 A1 WO 2009014150A1 JP 2008063212 W JP2008063212 W JP 2008063212W WO 2009014150 A1 WO2009014150 A1 WO 2009014150A1
Authority
WO
WIPO (PCT)
Prior art keywords
indole
benzimidazole derivative
17βhsd type
prostatomegaly
phenyl group
Prior art date
Application number
PCT/JP2008/063212
Other languages
English (en)
French (fr)
Inventor
Akio Kakefuda
Yutaka Kondoh
Masaaki Hirano
Akio Kamikawa
Kentaro Enjo
Takashi Furutani
Original Assignee
Astellas Pharma Inc.
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 Astellas Pharma Inc. filed Critical Astellas Pharma Inc.
Priority to US12/670,384 priority Critical patent/US20100190826A1/en
Priority to MX2010000918A priority patent/MX2010000918A/es
Priority to CA2694216A priority patent/CA2694216A1/en
Priority to CN200880100054A priority patent/CN101835747A/zh
Priority to EP08791469A priority patent/EP2172454A4/en
Priority to JP2009524500A priority patent/JP5251876B2/ja
Publication of WO2009014150A1 publication Critical patent/WO2009014150A1/ja

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • 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
    • A61P17/08—Antiseborrheics
    • 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
    • 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
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • 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
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28—Antiandrogens
    • 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
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—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
    • 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
    • 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
    • C07D235/10—Radicals substituted by halogen atoms or nitro radicals
    • 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
    • C07D235/18—Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2
    • 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
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/26—Oxygen 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/06—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 only aliphatic carbon atoms
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

　１７βＨＳＤｔｙｐｅ５の選択的阻害作用に基づく前立腺肥大症や前立腺癌等の新規かつ優れた治療及び／又は予防方法を提供する。ＣＯＯＨが置換したフェニル基がインドール環又はベンズイミダゾール環の窒素原子に置換したインドール又はベンズイミダゾール誘導体が、強力な１７βＨＳＤｔｙｐｅ５選択的阻害活性を有すること、及び、テストステロン減少による副作用を伴わない前立腺肥大症や前立腺癌等の１７βＨＳＤｔｙｐｅ５の関与する疾患の治療剤及び／又は予防剤となりうることを知見して本発明を完成した。
PCT/JP2008/063212 2007-07-24 2008-07-23 ベンズイミダゾール誘導体 WO2009014150A1 (ja)

Priority Applications (6)

Application Number Priority Date Filing Date Title
US12/670,384 US20100190826A1 (en) 2007-07-24 2008-07-23 Benzimidazole derivative
MX2010000918A MX2010000918A (es) 2007-07-24 2008-07-23 Derivado de bencimidazol.
CA2694216A CA2694216A1 (en) 2007-07-24 2008-07-23 Benzimidazole derivative
CN200880100054A CN101835747A (zh) 2007-07-24 2008-07-23 苯并咪唑衍生物
EP08791469A EP2172454A4 (en) 2007-07-24 2008-07-23 benzimidazole derivative
JP2009524500A JP5251876B2 (ja) 2007-07-24 2008-07-23 ベンズイミダゾール誘導体

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007192242 2007-07-24
JP2007-192242 2007-07-24

Publications (1)

Publication Number Publication Date
WO2009014150A1 true WO2009014150A1 (ja) 2009-01-29

Family

ID=40281399

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/063212 WO2009014150A1 (ja) 2007-07-24 2008-07-23 ベンズイミダゾール誘導体

Country Status (8)

Country Link
US (1) US20100190826A1 (ja)
EP (1) EP2172454A4 (ja)
JP (1) JP5251876B2 (ja)
KR (1) KR20100046107A (ja)
CN (1) CN101835747A (ja)
CA (1) CA2694216A1 (ja)
MX (1) MX2010000918A (ja)
WO (1) WO2009014150A1 (ja)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010101128A1 (ja) * 2009-03-03 2010-09-10 アステラス製薬株式会社 アミド化合物
US9346803B2 (en) 2011-10-17 2016-05-24 Vanderbilt University Indomethacin analogs for the treatment of castrate-resistant prostate cancer

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2013289344A1 (en) 2012-07-10 2015-02-05 Bayer Pharma Aktiengesellschaft 3-substituted estra-1,3,5(10),16-tetraene derivatives, methods for the production thereof, pharmaceutical preparations containing same, and use thereof for the production of medicaments
US9714266B2 (en) 2013-02-21 2017-07-25 Bayer Pharma Aktiengesellschaft Estra-1,3,5(10),16-tetraene-3-carboxamides for inhibition of 17.beta.-hydroxysteroid dehydrogenase (AKR1C3)
US20240293398A1 (en) * 2017-02-17 2024-09-05 University Of Florida Research Foundation, Incorporated Defining RNA-Small Molecule Affinity Landscapes Enables Design of a Small Molecule Inhibitor...
EP3421483A1 (en) 2017-06-29 2019-01-02 Bayer Pharma Aktiengesellschaft Novel steroidal 17-beta heteroaryl compounds as inhibitors of akr1c3

Citations (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS60224673A (ja) * 1984-04-24 1985-11-09 ヘキスト−ルセル・フア−マシユウテイカルズ・インコ−ポレイテツド １−（アミノアルキルフエニルおよびアミノアルキルベンジル）インド−ルおよびインドリン
EP0563001A1 (en) 1992-03-26 1993-09-29 Neurosearch A/S Imidazole compounds, their preparation and use
EP0616807A1 (en) 1993-03-24 1994-09-28 Neurosearch A/S Benzimidazole useful in the treatment of central nervous system disorders
JPH07133224A (ja) 1993-11-10 1995-05-23 Kyowa Hakko Kogyo Co Ltd 動脈硬化治療薬
US5554630A (en) 1993-03-24 1996-09-10 Neurosearch A/S Benzimidazole compounds
WO1996033194A1 (en) 1995-04-21 1996-10-24 Neurosearch A/S Benzimidazole compounds and their use as modulators of the gaba a receptor complex
WO1997033872A1 (en) 1996-03-13 1997-09-18 Biota Scientific Management Pty. Ltd. Anti-viral 4-acylamino-3-[imidazol-i-yl]-benzoic acid derivatives
WO1998017651A1 (en) 1996-10-21 1998-04-30 Neurosearch A/S 1-phenyl-benzimidazole compounds and their use as baga-a receptor modulators
WO1998034923A1 (en) 1997-02-07 1998-08-13 Merck Sharp & Dohme Limited Phenylbenzimidazole derivatives as ligands for gaba receptors
WO1999046279A2 (en) 1998-03-11 1999-09-16 Endorecherche, Inc. INHIBITORS OF TYPE 5 AND TYPE 3 17β-HYDROXYSTEROID DEHYDROGENASE AND METHODS FOR THEIR USE
WO2001007020A2 (de) 1999-07-27 2001-02-01 Boehringer Ingelheim Pharma Kg Carbonsäureamide, diese verbindungen enthaltende arzneimittel, deren verwendung und herstellung
JP2002193947A (ja) 2000-12-26 2002-07-10 Taisho Pharmaceut Co Ltd ベンズイミダゾール誘導体
WO2003057670A2 (en) 2001-12-28 2003-07-17 Guilford Pharmaceuticals Inc. Indoles as naaladase inhibitors
WO2004064735A2 (en) 2003-01-17 2004-08-05 Threshold Pharmaceuticals, Inc. Treatment of benign prostatic hyperplasia
WO2006041874A2 (en) 2004-10-04 2006-04-20 Myriad Genetics, Inc. Compounds for alzheimer's disease
US20070105862A1 (en) 2005-11-10 2007-05-10 Milan Bruncko Heat-shock protein binders
WO2008006790A1 (en) 2006-07-14 2008-01-17 Glaxo Group Limited Indole compounds

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1584735A (ja) * 1968-03-20 1970-01-02
US3878225A (en) * 1973-03-01 1975-04-15 Hoechst Co American Condensed pyrroles bearing an N-phenyl substituent
US4448784A (en) * 1982-04-12 1984-05-15 Hoechst-Roussel Pharmaceuticals, Inc. 1-(Aminoalkylphenyl and aminoalkylbenzyl)-indoles and indolines and analgesic method of use thereof
WO1991016313A1 (en) * 1990-04-13 1991-10-31 Smithkline Beecham Corporation Substituted benzimidazoles
US5698413A (en) * 1993-05-05 1997-12-16 The United States Of America As Represented By The Department Of Health And Human Services Method of evaluating chemotherapeutic agents in vivo
EP1990335A4 (en) * 2006-03-02 2009-11-11 Astellas Pharma Inc 17-BETA-HSD-type-5 INHIBITOR
EP2155719A1 (en) * 2007-05-24 2010-02-24 Wyeth LLC Azacyclylbenzamide derivatives as histamine-3 antagonists

Patent Citations (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS60224673A (ja) * 1984-04-24 1985-11-09 ヘキスト−ルセル・フア−マシユウテイカルズ・インコ−ポレイテツド １−（アミノアルキルフエニルおよびアミノアルキルベンジル）インド−ルおよびインドリン
EP0563001A1 (en) 1992-03-26 1993-09-29 Neurosearch A/S Imidazole compounds, their preparation and use
EP0616807A1 (en) 1993-03-24 1994-09-28 Neurosearch A/S Benzimidazole useful in the treatment of central nervous system disorders
JPH072838A (ja) * 1993-03-24 1995-01-06 Neurosearch As ベンゾイミダゾール化合物及び中枢神経系疾患治療薬
US5554630A (en) 1993-03-24 1996-09-10 Neurosearch A/S Benzimidazole compounds
JPH07133224A (ja) 1993-11-10 1995-05-23 Kyowa Hakko Kogyo Co Ltd 動脈硬化治療薬
WO1996033194A1 (en) 1995-04-21 1996-10-24 Neurosearch A/S Benzimidazole compounds and their use as modulators of the gaba a receptor complex
WO1997033872A1 (en) 1996-03-13 1997-09-18 Biota Scientific Management Pty. Ltd. Anti-viral 4-acylamino-3-[imidazol-i-yl]-benzoic acid derivatives
WO1998017651A1 (en) 1996-10-21 1998-04-30 Neurosearch A/S 1-phenyl-benzimidazole compounds and their use as baga-a receptor modulators
WO1998034923A1 (en) 1997-02-07 1998-08-13 Merck Sharp & Dohme Limited Phenylbenzimidazole derivatives as ligands for gaba receptors
WO1999046279A2 (en) 1998-03-11 1999-09-16 Endorecherche, Inc. INHIBITORS OF TYPE 5 AND TYPE 3 17β-HYDROXYSTEROID DEHYDROGENASE AND METHODS FOR THEIR USE
WO2001007020A2 (de) 1999-07-27 2001-02-01 Boehringer Ingelheim Pharma Kg Carbonsäureamide, diese verbindungen enthaltende arzneimittel, deren verwendung und herstellung
JP2002193947A (ja) 2000-12-26 2002-07-10 Taisho Pharmaceut Co Ltd ベンズイミダゾール誘導体
WO2003057670A2 (en) 2001-12-28 2003-07-17 Guilford Pharmaceuticals Inc. Indoles as naaladase inhibitors
WO2004064735A2 (en) 2003-01-17 2004-08-05 Threshold Pharmaceuticals, Inc. Treatment of benign prostatic hyperplasia
WO2006041874A2 (en) 2004-10-04 2006-04-20 Myriad Genetics, Inc. Compounds for alzheimer's disease
US20070105862A1 (en) 2005-11-10 2007-05-10 Milan Bruncko Heat-shock protein binders
WO2008006790A1 (en) 2006-07-14 2008-01-17 Glaxo Group Limited Indole compounds

Non-Patent Citations (34)

* Cited by examiner, † Cited by third party
Title
"Pharmaceutical Research and Development", vol. 7, 1990, HIROKAWA PUBLISHING COMPANY
"Protective Groups in Organic Synthesis", 1999
"The fifth edition of Courses in Experimental Chemistry", vol. 14, 2005, MARUZEN
"The fifth edition of Courses in Experimental Chemistry", vol. 16, 2005, MARUZEN
"The fourth eddition of Courses in Experimental Chemistry", vol. 26, 1992, MARUZEN
"The fourth edition of Courses in Experimental Chemistry", vol. 20, 1992, MARUZEN
"The fourth edition of Courses in Experimental Chemistry", vol. 22
"The fourth edition of Courses in Experimental Chemistry", vol. 26, 1992, MARUZEN
BIOORGANIC AND MEDICINAL CHEMISTRY, vol. 12, no. 15, 2004, pages 4009 - 4015
BIOORGANIC AND MEDICINAL CHEMISTRY, vol. 13, no. 24, 2005, pages 6598 - 6608
CANCER RESEARCH, vol. 64, 2004, pages 1802 - 1810
CANCER RESEARCH, vol. 66, 2006, pages 2815 - 2825
CARCINOGENESIS, vol. 25, no. 11, 2004, pages 2177 - 2181
CLINICAL CANCER RESEARCH, vol. 10, 2004, pages 440 - 448
COMPENDIUM OF ORGANIC SYNTHETIC METHODS, vol. 1-3
DRUG DESIGN, pages 163 - 198
ENDOCRINE REVIEWS, vol. 24, 2003, pages 152 - 182
FRONTIER IN NEUROENDOCRINOLOGY, vol. 22, 2001, pages 185 - 212
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 123, 2001, pages 7727 - 7729
KATRITZKY A.R. ET AL.: "QSAR studies on 1-phenylbenzimidazoles as inhibitors of the platelet-derived growth factor", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 13, no. 24, 2005, pages 6598 - 6608, XP005149600 *
MANIATIS, T. ET AL.: "Molecular Cloning-A Laboratory Manual", 1982, COLD SPRING HARBOR LABORATORY
MOLECULAR AND CELLULAR ENDOCRINOLOGY, vol. 248, 2006, pages 233 - 235
NATURE GENETICS, vol. 7, 1994, pages 34 - 39
OLECULAR ENDOCRINOLOGY, vol. 11, no. 13, 1997, pages 1971 - 1984
PROG. MED., vol. 5, 1985, pages 2157 - 2161
See also references of EP2172454A4
STEROIDS, vol. 69, 2004, pages 795 - 801
SYNTHESIS, vol. 10, 1982, pages 876 - 878
THE JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 277, no. 27, 2002, pages 24799 - 24808
THE JOURNAL OF CLINICAL ENDOCRINOLOGY AND METABOLISM, vol. 80, 1995, pages 1066 - 1071
THE JOURNAL OF MEDICINAL CHEMISTRY, vol. 41, no. 27, 1998, pages 5457 - 5465
THE JOURNAL OF UROLOGY, vol. 161, 1999, pages 332 - 337
THE NEW ENGLAND JOURNAL OF MEDICINE, vol. 349, 2003, pages 2387 - 2398
TREVOR M. PENNING ET AL., BIOCHEM. J., vol. 351, 2000, pages 67 - 77

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010101128A1 (ja) * 2009-03-03 2010-09-10 アステラス製薬株式会社 アミド化合物
US9346803B2 (en) 2011-10-17 2016-05-24 Vanderbilt University Indomethacin analogs for the treatment of castrate-resistant prostate cancer
EP3078374A1 (en) 2011-10-17 2016-10-12 Vanderbilt University Indomethacin analogs for the treatment of castrate-resistant prostate cancer
US9895351B2 (en) 2011-10-17 2018-02-20 Vanderbilt University Indomethacin analogs for the treatment of castrate-resistant prostate cancer
US10398678B2 (en) 2011-10-17 2019-09-03 Vanderbilt University Indomethacin analogs for the treatment of castrate-resistant prostate cancer
US11738004B2 (en) 2011-10-17 2023-08-29 Vanderbilt University Indomethacin analogs for the treatment of castrate-resistant prostate cancer

Also Published As

Publication number Publication date
US20100190826A1 (en) 2010-07-29
CA2694216A1 (en) 2009-01-29
KR20100046107A (ko) 2010-05-06
EP2172454A1 (en) 2010-04-07
JPWO2009014150A1 (ja) 2010-10-07
MX2010000918A (es) 2010-03-15
CN101835747A (zh) 2010-09-15
EP2172454A4 (en) 2010-12-08
JP5251876B2 (ja) 2013-07-31

Similar Documents

Publication Publication Date Title
PH12017500930A1 (en) Hsp90 inhibitor combinations
MX2009009290A (es) Compuestos activos en ppar.
WO2008051197A3 (en) Small-molecule botulinum toxin inhibitors
WO2009108860A3 (en) Microrna-based methods and compositions for the diagnosis, pronosis and treatment of prostate related disorders
WO2008030367A3 (en) Selective myostatin inhibitors
AP2321A (en) Quinoline derivatives for use as mycobactrial inhibitor.
WO2010004197A3 (fr) Derives de pyridino-pyridinones, leur preparation et leur application en therapeutique
WO2006060535A3 (en) Indole derivatives for use as ppar active compounds
WO2007126957A3 (en) New compounds
WO2006060456A3 (en) Indole derivatives for use as ppar ppar active compounds
TN2010000096A1 (en) Oxadiazole - and oxazole - substituted benzimidazole - and indole - derivatives as dgat1 inhibitors
WO2008048991A3 (en) Organic compounds
WO2007146965A3 (en) Compounds for the treatment of periodontal disease
WO2006110816A3 (en) 1h-benzimidazole-4-carboxamides substituted with a quaternary carbon at the 2-position are potent parp inhibitors
WO2007070173A3 (en) Cetp inhibitors
DK2303044T3 (da) Dragt til rent rum og lignende
WO2007059230A3 (en) Substituted 1h-benzimidazole-4-carboxamides are potent parp inhibitors
WO2009042114A3 (en) Phenazine derivatives and uses thereof
WO2008157740A3 (en) Faah inhibitors
WO2007106537A3 (en) Aminoquinolones as gsk-3 inhibitors
WO2008112659A3 (en) Regulation of osteopontin
WO2009014150A1 (ja) ベンズイミダゾール誘導体
WO2010071783A8 (en) Thiazoles as cannabinoid receptor ligands
LTC2805723I2 (lt) Kladribino režimas, skirtas išsėtinei sklerozei gydyti
TN2012000092A1 (en) Therapeutic agent for mood disorders

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: 200880100054.8

Country of ref document: CN

121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 08791469

Country of ref document: EP

Kind code of ref document: A1

ENP Entry into the national phase

Ref document number: 2009524500

Country of ref document: JP

Kind code of ref document: A

ENP Entry into the national phase

Ref document number: 20097025951

Country of ref document: KR

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: 2008791469

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: 12670384

Country of ref document: US

Ref document number: 2694216

Country of ref document: CA

Ref document number: 445/CHENP/2010

Country of ref document: IN

Ref document number: MX/A/2010/000918

Country of ref document: MX

NENP Non-entry into the national phase

Ref country code: DE