WO2008133127A1 - 縮合へテロ環誘導体、それを含有する医薬組成物及びその医薬用途 - Google Patents

縮合へテロ環誘導体、それを含有する医薬組成物及びその医薬用途 Download PDF

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Publication number
WO2008133127A1
WO2008133127A1 PCT/JP2008/057391 JP2008057391W WO2008133127A1 WO 2008133127 A1 WO2008133127 A1 WO 2008133127A1 JP 2008057391 W JP2008057391 W JP 2008057391W WO 2008133127 A1 WO2008133127 A1 WO 2008133127A1
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WIPO (PCT)
Prior art keywords
derivative
pharmaceutical composition
alkyl
composition
fused heterocyclic
Prior art date
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PCT/JP2008/057391
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English (en)
French (fr)
Inventor
Kohsuke Ohno
Noboru Kamada
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Kissei Pharmaceutical Co., Ltd.
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.)
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Publication date
Application filed by Kissei Pharmaceutical Co., Ltd. filed Critical Kissei Pharmaceutical Co., Ltd.
Priority to CA002682519A priority Critical patent/CA2682519A1/en
Priority to EP08740472.9A priority patent/EP2147922B1/en
Priority to JP2009511815A priority patent/JP5352449B2/ja
Priority to US12/595,931 priority patent/US8426427B2/en
Publication of WO2008133127A1 publication Critical patent/WO2008133127A1/ja

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • 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
    • A61P15/06—Antiabortive agents; Labour repressants
    • 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
    • A61P15/16—Masculine contraceptives
    • 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
    • A61P15/18—Feminine 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
    • A61P17/10—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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pregnancy & Childbirth (AREA)
  • Anesthesiology (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

本発明は、性ホルモン依存性疾患等の予防又は治療剤として有用な化合物を提供する。すなわち、本発明は、GnRH拮抗作用を有する下記一般式（Ｉ）で表される縮合へテロ環誘導体、それを含有する医薬組成物及びその医薬用途等を提供する。式（Ｉ）中、環Ａは、５員環不飽和炭化水素又は５員環へテロアリール；ＲＡは、ハロゲン、アルキル、アルケニル、アルキニル、カルボキシ、アルコキシ、カルバモイル、アルキルカルバモイル等；環Ｂはアリール又はヘテロアリール；ＲＢは、ハロゲン、アルキル、カルボキシ、アルコキシ、カルバモイル、アルキルカルバモイル等；Ｅ１、Ｅ２は、酸素原子等；Ｑは、水素原子、アルキル、アルキルスルホニル、アシル等；Ｘは、－（アルキレン）－Ｚ、－ＣＯ－Ｙ、－ＳＯ２－Ｙ等で表される基（Ｙは、Ｚ又はアミノ等；Ｚは、シクロアルキル、ヘテロシクロアルキル、アリール、ヘテロアリール等）;等である。
PCT/JP2008/057391 2007-04-18 2008-04-16 縮合へテロ環誘導体、それを含有する医薬組成物及びその医薬用途 WO2008133127A1 (ja)

Priority Applications (4)

Application Number Priority Date Filing Date Title
CA002682519A CA2682519A1 (en) 2007-04-18 2008-04-16 Fused heterocyclic derivative, pharmaceutical composition comprising the derivative, and use of the composition for medical purposes
EP08740472.9A EP2147922B1 (en) 2007-04-18 2008-04-16 Fused heterocyclic derivative, pharmaceutical composition comprising the derivative, and use of the composition for medical purposes
JP2009511815A JP5352449B2 (ja) 2007-04-18 2008-04-16 縮合へテロ環誘導体、それを含有する医薬組成物及びその医薬用途
US12/595,931 US8426427B2 (en) 2007-04-18 2008-04-16 Fused heterocyclic derivative, pharmaceutical composition comprising the derivative, and use of the composition for medical purposes

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007-108935 2007-04-18
JP2007108935 2007-04-18

Publications (1)

Publication Number Publication Date
WO2008133127A1 true WO2008133127A1 (ja) 2008-11-06

Family

ID=39925583

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/057391 WO2008133127A1 (ja) 2007-04-18 2008-04-16 縮合へテロ環誘導体、それを含有する医薬組成物及びその医薬用途

Country Status (5)

Country Link
US (1) US8426427B2 (ja)
EP (1) EP2147922B1 (ja)
JP (1) JP5352449B2 (ja)
CA (1) CA2682519A1 (ja)
WO (1) WO2008133127A1 (ja)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102225067A (zh) * 2011-04-29 2011-10-26 济南环肽医药科技有限公司 一种治疗胃癌的药物组合物
WO2014030743A1 (ja) 2012-08-24 2014-02-27 武田薬品工業株式会社 複素環化合物
WO2014042176A1 (ja) * 2012-09-14 2014-03-20 キッセイ薬品工業株式会社 縮合複素環誘導体の製造方法およびその製造中間体
CN115232144A (zh) * 2021-04-22 2022-10-25 长春金赛药业有限责任公司 含氮稠环类衍生物、药物组合物及其制备方法和应用

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104817541B (zh) * 2015-05-11 2017-06-16 苏州东南药业股份有限公司 一种抗肿瘤药物的合成方法

Citations (8)

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Publication number Priority date Publication date Assignee Title
JPH06510992A (ja) 1991-09-20 1994-12-08 ビーエーエスエフ　アクチェンゲゼルシャフト 置換３−フェニルウラシル
WO1995028405A1 (en) * 1994-04-19 1995-10-26 Takeda Chemical Industries, Ltd. Bicyclic thiophene derivatives and use as gonadotropin releasing hormone antagonists
WO1996024597A1 (en) 1995-02-08 1996-08-15 Takeda Chemical Industries, Ltd. Thienopyrimidine derivatives, their production and use
WO2001055119A2 (en) * 2000-01-25 2001-08-02 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
US20030004167A1 (en) 1998-12-23 2003-01-02 Lam Patrick Y. Imidazo-heterobicycles as factor Xa inhibitors
WO2005019188A1 (ja) 2003-08-22 2005-03-03 Takeda Pharmaceutical Company Limited 縮合ピリミジン誘導体およびその用途
WO2006083005A1 (ja) 2005-02-03 2006-08-10 Takeda Pharmaceutical Company Limited 縮合ピリミジン誘導体およびその用途
WO2007046392A1 (ja) * 2005-10-19 2007-04-26 Kissei Pharmaceutical Co., Ltd. 縮合複素環誘導体、それを含有する医薬組成物及びその医薬用途

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DE69622648T2 (de) 1995-02-10 2003-02-27 Suntory Ltd Osaka Benzoxalepin-derivate, deren salze und diese enthaltende arzneimittel
WO2005055118A2 (en) * 2003-11-29 2005-06-16 Cross Match Technologies, Inc. Polymer ceramic slip and method of manufacturing ceramic green bodies therefrom
US20070010537A1 (en) 2004-08-20 2007-01-11 Kazumasa Hamamura Fused pyramidine derivative and use thereof

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WO1995028405A1 (en) * 1994-04-19 1995-10-26 Takeda Chemical Industries, Ltd. Bicyclic thiophene derivatives and use as gonadotropin releasing hormone antagonists
WO1996024597A1 (en) 1995-02-08 1996-08-15 Takeda Chemical Industries, Ltd. Thienopyrimidine derivatives, their production and use
US20030004167A1 (en) 1998-12-23 2003-01-02 Lam Patrick Y. Imidazo-heterobicycles as factor Xa inhibitors
WO2001055119A2 (en) * 2000-01-25 2001-08-02 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
WO2005019188A1 (ja) 2003-08-22 2005-03-03 Takeda Pharmaceutical Company Limited 縮合ピリミジン誘導体およびその用途
WO2006083005A1 (ja) 2005-02-03 2006-08-10 Takeda Pharmaceutical Company Limited 縮合ピリミジン誘導体およびその用途
WO2007046392A1 (ja) * 2005-10-19 2007-04-26 Kissei Pharmaceutical Co., Ltd. 縮合複素環誘導体、それを含有する医薬組成物及びその医薬用途

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HIROKAWA SYOTEN: "Molecular design", vol. 7, HIROKAWA BOOK STORE, article "Iyakuhin no Kaihatsu", pages: 163 - 198
IGAKUSYOIN: "Hyojun Seirigaku", pages: 882 - 891
SANKA TO FUJINKA, vol. 71, no. 3, 2004, pages 280 - 285
See also references of EP2147922A4

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102225067A (zh) * 2011-04-29 2011-10-26 济南环肽医药科技有限公司 一种治疗胃癌的药物组合物
CN102225067B (zh) * 2011-04-29 2012-10-03 济南环肽医药科技有限公司 一种治疗胃癌的药物组合物
WO2014030743A1 (ja) 2012-08-24 2014-02-27 武田薬品工業株式会社 複素環化合物
CN104755465A (zh) * 2012-08-24 2015-07-01 武田药品工业株式会社 杂环化合物
WO2014042176A1 (ja) * 2012-09-14 2014-03-20 キッセイ薬品工業株式会社 縮合複素環誘導体の製造方法およびその製造中間体
JPWO2014042176A1 (ja) * 2012-09-14 2016-08-18 キッセイ薬品工業株式会社 縮合複素環誘導体の製造方法およびその製造中間体
CN115232144A (zh) * 2021-04-22 2022-10-25 长春金赛药业有限责任公司 含氮稠环类衍生物、药物组合物及其制备方法和应用
CN115232144B (zh) * 2021-04-22 2024-04-02 长春金赛药业有限责任公司 含氮稠环类衍生物、药物组合物及其制备方法和应用

Also Published As

Publication number Publication date
CA2682519A1 (en) 2008-11-06
JPWO2008133127A1 (ja) 2010-07-22
EP2147922A1 (en) 2010-01-27
EP2147922A4 (en) 2012-04-18
EP2147922B1 (en) 2017-08-02
US8426427B2 (en) 2013-04-23
US20100081674A1 (en) 2010-04-01
JP5352449B2 (ja) 2013-11-27

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