WO2003064429A1 - Thienopyrimidines, procedes de fabrication et d'utilisation correspondants - Google Patents

Thienopyrimidines, procedes de fabrication et d'utilisation correspondants Download PDF

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Publication number
WO2003064429A1
WO2003064429A1 PCT/JP2003/000828 JP0300828W WO03064429A1 WO 2003064429 A1 WO2003064429 A1 WO 2003064429A1 JP 0300828 W JP0300828 W JP 0300828W WO 03064429 A1 WO03064429 A1 WO 03064429A1
Authority
WO
WIPO (PCT)
Prior art keywords
alkyl
alkylamino
substituent
mono
amino
Prior art date
Application number
PCT/JP2003/000828
Other languages
English (en)
French (fr)
Inventor
Shuichi Furuya
Takashi Imada
Takenori Hitaka
Kazuhiro Miwa
Masami Kusaka
Nobuhiro Suzuki
Original Assignee
Takeda Chemical Industries, 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.)
Filing date
Publication date
Application filed by Takeda Chemical Industries, Ltd. filed Critical Takeda Chemical Industries, Ltd.
Priority to EP03734872A priority Critical patent/EP1479684A4/en
Priority to US10/502,903 priority patent/US7569570B2/en
Publication of WO2003064429A1 publication Critical patent/WO2003064429A1/ja

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Classifications

    • 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
    • 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
    • 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
    • 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
    • A61P25/28—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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • A61P5/08—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH for decreasing, blocking or antagonising the activity of the anterior pituitary 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
PCT/JP2003/000828 2002-01-30 2003-01-29 Thienopyrimidines, procedes de fabrication et d'utilisation correspondants WO2003064429A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP03734872A EP1479684A4 (en) 2002-01-30 2003-01-29 THIENOPYRIMIDINES, PROCESS FOR THEIR PRODUCTION AND THEIR USE
US10/502,903 US7569570B2 (en) 2002-01-30 2003-01-29 Thienopyrimidines, process for preparing the same and use thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2002-22034 2002-01-30
JP2002022034 2002-01-30

Publications (1)

Publication Number Publication Date
WO2003064429A1 true WO2003064429A1 (fr) 2003-08-07

Family

ID=27654415

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2003/000828 WO2003064429A1 (fr) 2002-01-30 2003-01-29 Thienopyrimidines, procedes de fabrication et d'utilisation correspondants

Country Status (3)

Country Link
US (1) US7569570B2 (ja)
EP (1) EP1479684A4 (ja)
WO (1) WO2003064429A1 (ja)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7300935B2 (en) 2003-01-29 2007-11-27 Takeda Pharmaceutical Company Thienopyrimidine compounds and use thereof
EP2881391A1 (en) 2013-12-05 2015-06-10 Bayer Pharma Aktiengesellschaft Spiroindoline carbocycle derivatives and pharmaceutical compositions thereof
WO2023072284A1 (zh) * 2021-11-01 2023-05-04 山东绿叶制药有限公司 促性腺素释放激素拮抗剂及其制备方法和应用

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090062258A1 (en) * 2005-02-03 2009-03-05 Takeda Pharmaceutical Company Limited Fused pyrimidine derivative and use thereof
ZA200801150B (en) * 2005-07-22 2010-05-26 Takeda Pharmaceutical Premature ovulation preventive agent
US8633182B2 (en) 2012-05-30 2014-01-21 Boehringer Ingelheim International Gmbh Indanyloxyphenylcyclopropanecarboxylic acids
EP4119564A1 (en) 2012-09-28 2023-01-18 Takeda Pharmaceutical Company Limited Production method of thienopyrimidine derivative
BR112016008799B1 (pt) * 2013-10-30 2023-02-23 Shanghai Hengrui Pharmaceutical Co., Ltd. Derivados de pirazolopirimidona ou pirrolotriazona, seus intermediários, seus usos, seus processos de preparação, e composição farmacêutica
EP4233847A1 (en) 2015-02-26 2023-08-30 Takeda Pharmaceutical Company Limited A tablet comprising a methoxyurea derivative and mannitol particles
JP7062673B2 (ja) 2016-09-30 2022-05-06 ミオバント サイエンシズ ゲーエムベーハー 前立腺がんの治療
PT3518933T (pt) 2016-09-30 2022-05-10 Takeda Pharmaceuticals Co Métodos de tratamento de fibroides uterinos e endometriose
EP4004001A4 (en) * 2019-07-29 2023-08-30 Sunshine Lake Pharma Co., Ltd. SUBSTITUTED PYRIMIDINEONE COMPOUNDS AND USES THEREOF
CN111574534B (zh) * 2020-05-25 2021-06-04 东莞市东阳光新药研发有限公司 苯基取代的噻吩并[2,3-d]嘧啶-2,4(1H,3H)-二酮类化合物及其用途
CN111875614B (zh) * 2020-07-03 2022-04-29 东莞市东阳光新药研发有限公司 杂环基取代的噻吩并[2,3-d]嘧啶-2,4(1H,3H)-二酮类化合物及其用途
CN111793078B (zh) * 2020-07-03 2022-02-01 东莞市东阳光新药研发有限公司 双环含氮杂芳基取代的嘧啶二酮类化合物及其用途
CN111925379B (zh) * 2020-07-31 2022-02-15 广东东阳光药业有限公司 含氮杂芳基取代的嘧啶二酮类化合物及其用途
CN111909168B (zh) * 2020-07-31 2022-02-01 广东东阳光药业有限公司 含氮杂环基取代的嘧啶二酮类化合物及其用途
CN112047957B (zh) * 2020-09-09 2022-02-01 广东东阳光药业有限公司 取代的嘧啶二酮类化合物及其用途
CN113754679B (zh) * 2020-09-09 2023-04-07 广东东阳光药业有限公司 取代的嘧啶二酮类化合物及其用途
CN112142757B (zh) * 2020-09-29 2022-02-15 广东东阳光药业有限公司 五元含氮杂芳基取代的嘧啶二酮类化合物及其用途
CN116438181A (zh) * 2020-09-29 2023-07-14 广东东阳光药业有限公司 磺酰胺基取代的杂芳基嘧啶二酮类化合物及其用途
WO2022067566A1 (zh) * 2020-09-29 2022-04-07 广东东阳光药业有限公司 含有饱和含氧杂环基的嘧啶二酮类化合物及其用途

Citations (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS61191698A (ja) 1985-02-08 1986-08-26 メルク　エンド　カムパニー　インコーポレーテツド 新規な環状ヘキサペプチドｌｈｒｈ拮抗剤
US5140009A (en) 1988-02-10 1992-08-18 Tap Pharmaceuticals, Inc. Octapeptide LHRH antagonists
US5171835A (en) 1988-10-21 1992-12-15 The Administrators Of The Tulane Educational Fund LHRH antagonists
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
JPH08295693A (ja) 1994-04-19 1996-11-12 Takeda Chem Ind Ltd 縮合チオフェン誘導体、その製造法及び用途
WO1997014697A1 (en) 1995-10-19 1997-04-24 Takeda Chemical Industries, Ltd. Thienopyridine derivatives as gonadotropin releasing hormone antagonists
WO1997014682A1 (en) 1995-10-19 1997-04-24 Takeda Chemical Industries, Ltd. Quinoline derivatives as gnrh antagonists
JPH09169767A (ja) 1995-10-19 1997-06-30 Takeda Chem Ind Ltd 複素環化合物、その製造法および用途
JPH09169735A (ja) 1995-10-19 1997-06-30 Takeda Chem Ind Ltd キノリン誘導体、その製造法および用途
JPH09208496A (ja) * 1996-01-30 1997-08-12 Takeda Chem Ind Ltd Ｌｈ−ｒｈ拮抗物質含有組成物
WO1999033831A1 (en) 1997-12-26 1999-07-08 Takeda Chemical Industries, Ltd. Nitrogen-containing heterocyclic compounds, their production and use
JPH11315079A (ja) 1997-12-26 1999-11-16 Takeda Chem Ind Ltd 含窒素複素環化合物、その製造法および用途
WO2000000493A1 (en) 1998-06-26 2000-01-06 Takeda Chemical Industries, Ltd. Thienopyridine compounds, their production and use
JP2000219691A (ja) 1998-06-26 2000-08-08 Takeda Chem Ind Ltd チエノピリジン誘導体、その製造法および用途
WO2000056739A1 (en) 1999-03-24 2000-09-28 Takeda Chemical Industries, Ltd. Thienopyrimidine compounds, their production and use
WO2001007878A1 (en) 1999-07-23 2001-02-01 Shimadzu Research Laboratory (Europe) Ltd. Apparatus and methods for analysing electromagnetic radiation
WO2001064683A1 (fr) 2000-02-29 2001-09-07 Takeda Chemical Industries, Ltd. Procedes de production de derives de thienopyramidine
WO2001078780A1 (fr) * 2000-04-13 2001-10-25 Takeda Chemical Industries, Ltd. Agents preventifs/remedes pour la maladie d'alzheimer
WO2001095940A1 (fr) 2000-06-14 2001-12-20 Takeda Chemical Industries, Ltd. Compositions a liberation continue
WO2002002144A1 (en) 2000-07-05 2002-01-10 Takeda Chemical Industries, Ltd. Medicinal preparations for treating sex hormone-dependent diseases
JP2002030087A (ja) 2000-07-17 2002-01-29 Takeda Chem Ind Ltd チエノピリジン−５−カルボン酸エステル化合物、その製造法および用途
WO2002024230A1 (fr) * 2000-09-22 2002-03-28 Takeda Chemical Industries, Ltd. Preparations solides
WO2002043766A1 (fr) * 2000-11-29 2002-06-06 Takeda Chemical Industries, Ltd. Compositions medicinales et leur procede de preparation

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US4316825A (en) * 1979-10-01 1982-02-23 Copolymer Rubber & Chemical Corp. High green strength rubbers
US6048863A (en) 1994-04-19 2000-04-11 Takeda Chemical Industries, Ltd. Condensed-ring thiophene derivatives and thienopyrimidine derivatives, their production and use
US6297255B1 (en) 1998-06-26 2001-10-02 Takeda Chemical Industries, Ltd. Thienopyridine compounds, their production and use
RU2233284C2 (ru) * 1999-03-24 2004-07-27 Такеда Кемикал Индастриз, Лтд. Тиенопиримидиновые производные, способ их получения, фармацевтическая композиция и способ антагонизации гонадотропин-рилизинг гормона
JP2003026601A (ja) 2000-11-29 2003-01-29 Takeda Chem Ind Ltd 医薬組成物およびその製造法

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JPS61191698A (ja) 1985-02-08 1986-08-26 メルク　エンド　カムパニー　インコーポレーテツド 新規な環状ヘキサペプチドｌｈｒｈ拮抗剤
US5140009A (en) 1988-02-10 1992-08-18 Tap Pharmaceuticals, Inc. Octapeptide LHRH antagonists
US5171835A (en) 1988-10-21 1992-12-15 The Administrators Of The Tulane Educational Fund LHRH antagonists
WO1995028405A1 (en) 1994-04-19 1995-10-26 Takeda Chemical Industries, Ltd. Bicyclic thiophene derivatives and use as gonadotropin releasing hormone antagonists
JPH08295693A (ja) 1994-04-19 1996-11-12 Takeda Chem Ind Ltd 縮合チオフェン誘導体、その製造法及び用途
WO1996024597A1 (en) 1995-02-08 1996-08-15 Takeda Chemical Industries, Ltd. Thienopyrimidine derivatives, their production and use
JPH09169768A (ja) 1995-02-08 1997-06-30 Takeda Chem Ind Ltd チエノピリミジン誘導体、その製造法および用途
WO1997014697A1 (en) 1995-10-19 1997-04-24 Takeda Chemical Industries, Ltd. Thienopyridine derivatives as gonadotropin releasing hormone antagonists
WO1997014682A1 (en) 1995-10-19 1997-04-24 Takeda Chemical Industries, Ltd. Quinoline derivatives as gnrh antagonists
JPH09169767A (ja) 1995-10-19 1997-06-30 Takeda Chem Ind Ltd 複素環化合物、その製造法および用途
JPH09169735A (ja) 1995-10-19 1997-06-30 Takeda Chem Ind Ltd キノリン誘導体、その製造法および用途
JPH09208496A (ja) * 1996-01-30 1997-08-12 Takeda Chem Ind Ltd Ｌｈ−ｒｈ拮抗物質含有組成物
WO1999033831A1 (en) 1997-12-26 1999-07-08 Takeda Chemical Industries, Ltd. Nitrogen-containing heterocyclic compounds, their production and use
JPH11315079A (ja) 1997-12-26 1999-11-16 Takeda Chem Ind Ltd 含窒素複素環化合物、その製造法および用途
WO2000000493A1 (en) 1998-06-26 2000-01-06 Takeda Chemical Industries, Ltd. Thienopyridine compounds, their production and use
JP2000219691A (ja) 1998-06-26 2000-08-08 Takeda Chem Ind Ltd チエノピリジン誘導体、その製造法および用途
JP2001278884A (ja) 1999-03-24 2001-10-10 Takeda Chem Ind Ltd チエノピリミジン化合物、その製造法および用途
WO2000056739A1 (en) 1999-03-24 2000-09-28 Takeda Chemical Industries, Ltd. Thienopyrimidine compounds, their production and use
WO2001007878A1 (en) 1999-07-23 2001-02-01 Shimadzu Research Laboratory (Europe) Ltd. Apparatus and methods for analysing electromagnetic radiation
WO2001064683A1 (fr) 2000-02-29 2001-09-07 Takeda Chemical Industries, Ltd. Procedes de production de derives de thienopyramidine
WO2001078780A1 (fr) * 2000-04-13 2001-10-25 Takeda Chemical Industries, Ltd. Agents preventifs/remedes pour la maladie d'alzheimer
WO2001095940A1 (fr) 2000-06-14 2001-12-20 Takeda Chemical Industries, Ltd. Compositions a liberation continue
WO2002002144A1 (en) 2000-07-05 2002-01-10 Takeda Chemical Industries, Ltd. Medicinal preparations for treating sex hormone-dependent diseases
JP2002030087A (ja) 2000-07-17 2002-01-29 Takeda Chem Ind Ltd チエノピリジン−５−カルボン酸エステル化合物、その製造法および用途
WO2002024230A1 (fr) * 2000-09-22 2002-03-28 Takeda Chemical Industries, Ltd. Preparations solides
WO2002043766A1 (fr) * 2000-11-29 2002-06-06 Takeda Chemical Industries, Ltd. Compositions medicinales et leur procede de preparation

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JOURNAL OF MEDICINAL CHEMISTRY, vol. 36, 1993, pages 3265 - 3273
SASAKI S. ET AL.: "Discovery of a thieno(2,3-d) pyrimidine-2,4-dione bearing a P-methoxyureidophenyl moiety at the 6-position: ....... a antagonist for the human lutenizing .........", J. MED. CHEM., vol. 46, no. 1, 2 January 2003 (2003-01-02), pages 113 - 124, XP002967759 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7300935B2 (en) 2003-01-29 2007-11-27 Takeda Pharmaceutical Company Thienopyrimidine compounds and use thereof
US8058280B2 (en) 2003-01-29 2011-11-15 Takeda Pharmaceutical Company Limited Substituted thieno[2,3-d]pyrimidin-2,4-dione compounds and uses thereof
US8735401B2 (en) 2003-01-29 2014-05-27 Takeda Pharmaceutical Company Limited Thienopyrimidine compounds and use thereof
US9346822B2 (en) 2003-01-29 2016-05-24 Takeda Pharmaceutical Company Limited Thienopyrimidine compounds and use thereof
EP2881391A1 (en) 2013-12-05 2015-06-10 Bayer Pharma Aktiengesellschaft Spiroindoline carbocycle derivatives and pharmaceutical compositions thereof
WO2023072284A1 (zh) * 2021-11-01 2023-05-04 山东绿叶制药有限公司 促性腺素释放激素拮抗剂及其制备方法和应用

Also Published As

Publication number Publication date
EP1479684A1 (en) 2004-11-24
EP1479684A4 (en) 2006-01-04
US7569570B2 (en) 2009-08-04
US20050222174A1 (en) 2005-10-06

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