WO2008096746A1 - スピロ化合物およびその用途 - Google Patents

スピロ化合物およびその用途 Download PDF

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Publication number
WO2008096746A1
WO2008096746A1 PCT/JP2008/051849 JP2008051849W WO2008096746A1 WO 2008096746 A1 WO2008096746 A1 WO 2008096746A1 JP 2008051849 W JP2008051849 W JP 2008051849W WO 2008096746 A1 WO2008096746 A1 WO 2008096746A1
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ring
substituted
group
salt
independently represent
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PCT/JP2008/051849
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English (en)
French (fr)
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Takahiko Taniguchi
Kenichi Miyata
Osamu Kubo
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Takeda Pharmaceutical Company Limited
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Priority to US12/449,320 priority Critical patent/US8575167B2/en
Publication of WO2008096746A1 publication Critical patent/WO2008096746A1/ja

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10—Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

　本発明は新規なＳＣＤ阻害剤の提供を目的とする。 　本発明は、式（Ｉ） 〔式中、 Ｒは、置換されていてもよい環状基または置換されていてもよいカルバモイル基を示し（但し、Ｒは、置換されていてもよい７－ピリド［２，３－ｄ］ピリミジル基ではない）； 環Ａは、さらに置換されていてもよいピリダジン環を示し； Ｒ１、Ｒ２、Ｒ３、Ｒ４、Ｒ１１、Ｒ１２、Ｒ１３およびＲ１４は、それぞれ独立して、水素原子または置換基を示すか、Ｒ１とＲ１１、Ｒ２とＲ１２、Ｒ３とＲ１３、またはＲ４とＲ１４が一緒になってオキソ基を形成するか、あるいはＲ２とＲ４が一緒になって、結合手またはアルキレン架橋を形成してもよく； ｍおよびｎは、それぞれ独立して、０ないし２の整数を示し； 環Ｂは、置換されていてもよい環を示す（但し、環Ｂにおいて、スピロ炭素原子に隣接する環Ｂの二つの構成原子は、同時に酸素原子とはならない）〕 で表される化合物またはその塩、あるいはそのプロドラッグを含有してなるＳＣＤ阻害剤である。
PCT/JP2008/051849 2007-02-06 2008-02-05 スピロ化合物およびその用途 WO2008096746A1 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
US12/449,320 US8575167B2 (en) 2007-02-06 2008-02-05 Spiro compounds having stearoyl-CoA desaturase action

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP2007027404 2007-02-06
JP2007-027404 2007-02-06
JP2007139645 2007-05-25
JP2007-139645 2007-05-25

Publications (1)

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WO2008096746A1 true WO2008096746A1 (ja) 2008-08-14

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US (1) US8575167B2 (ja)
WO (1) WO2008096746A1 (ja)

Cited By (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009037542A3 (en) * 2007-09-20 2009-05-22 Glenmark Pharmaceuticals Sa Spirocyclic compounds as stearoyl coa desaturase inhibitors
WO2011011872A1 (en) * 2009-07-28 2011-02-03 Merck Frosst Canada Ltd. Novel spiro compounds useful as inhibitors of stearoyl-coenzyme a delta-9 desaturase
WO2011047481A1 (en) * 2009-10-23 2011-04-28 Merck Frosst Canada Ltd. Novel spiro compounds useful as inhibitors of stearoyl-coenzyme a delta-9 desaturase
JP2012517960A (ja) * 2009-02-17 2012-08-09 メルク カナダ インコーポレイテッド ステアロイル−補酵素ａデルタ−９デサチュラーゼの阻害剤として有用な新規スピロ化合物
WO2012120399A1 (en) 2011-03-10 2012-09-13 Pfizer Inc. Spirocyclic isoxazoline derivatives as antiparasitic agents
WO2013056148A2 (en) 2011-10-15 2013-04-18 Genentech, Inc. Methods of using scd1 antagonists
JP2013536873A (ja) * 2010-09-06 2013-09-26 グアンジョウ インスティテュート オブ バイオメディスン アンド ヘルス，チャイニーズ アカデミー オブ サイエンスィズ アミド化合物
WO2013175474A2 (en) 2012-05-22 2013-11-28 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Selective inhibitors of undifferentiated cells
US9420793B2 (en) 2015-01-16 2016-08-23 Avista Pharma Solutions Antiparasitic compounds
WO2018129403A1 (en) 2017-01-06 2018-07-12 Yumanity Therapeutics Methods for the treatment of neurological disorders
US10696674B2 (en) 2016-07-07 2020-06-30 Bristol-Myers Squibb Company Spirolactams as inhibitors of ROCK
US10807992B2 (en) 2017-11-16 2020-10-20 Avista Pharma Solutions, Inc. Single enantiomer antiparasitic compounds
WO2020249079A1 (zh) * 2019-06-14 2020-12-17 北京盛诺基医药科技股份有限公司 一种shp2磷酸酶变构抑制剂
CN115197228A (zh) * 2022-07-13 2022-10-18 河南师范大学 吡唑啉酮[螺]二氢酞嗪和1,3-茚二酮[螺]二氢酞嗪类化合物的合成方法
US11873298B2 (en) 2017-10-24 2024-01-16 Janssen Pharmaceutica Nv Compounds and uses thereof
US11970486B2 (en) 2016-10-24 2024-04-30 Janssen Pharmaceutica Nv Compounds and uses thereof
US12098146B2 (en) 2019-01-24 2024-09-24 Janssen Pharmaceutica Nv Compounds and uses thereof

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TW201643169A (zh) 2010-07-09 2016-12-16 艾伯維股份有限公司 作為s1p調節劑的螺-哌啶衍生物
US10273243B2 (en) * 2013-03-14 2019-04-30 The Trustees Of Columbia University In The City Of New York 4-phenylpiperidines, their preparation and use
BR112022008113A2 (pt) 2019-10-31 2022-07-19 Escape Bio Inc Formas sólidas de um modulador de receptor s1p

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WO2006034440A2 (en) * 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
WO2006034338A1 (en) * 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as mediators of stearoyl-coa desaturase
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WO2006023630A2 (en) * 2004-08-20 2006-03-02 Targacept, Inc. The use of n-aryl diazaspiracyclic compounds in the treatment of addiction
WO2006034440A2 (en) * 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
WO2006034338A1 (en) * 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as mediators of stearoyl-coa desaturase
WO2006053024A2 (en) * 2004-11-10 2006-05-18 Incyte Corporation Lactam compounds and their use as pharmaceuticals

Cited By (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009037542A3 (en) * 2007-09-20 2009-05-22 Glenmark Pharmaceuticals Sa Spirocyclic compounds as stearoyl coa desaturase inhibitors
US9168248B2 (en) 2009-02-17 2015-10-27 Merck Canada Inc. Spiro compounds useful as inhibitors of stearoyl-coenzyme A delta-9 desaturase
JP2012517960A (ja) * 2009-02-17 2012-08-09 メルク カナダ インコーポレイテッド ステアロイル−補酵素ａデルタ−９デサチュラーゼの阻害剤として有用な新規スピロ化合物
WO2011011872A1 (en) * 2009-07-28 2011-02-03 Merck Frosst Canada Ltd. Novel spiro compounds useful as inhibitors of stearoyl-coenzyme a delta-9 desaturase
US8383643B2 (en) 2009-07-28 2013-02-26 Merck Canada Inc. Spiro compounds useful as inhibitors of stearoyl-coenzyme A delta-9 desaturase
WO2011047481A1 (en) * 2009-10-23 2011-04-28 Merck Frosst Canada Ltd. Novel spiro compounds useful as inhibitors of stearoyl-coenzyme a delta-9 desaturase
JP2013536873A (ja) * 2010-09-06 2013-09-26 グアンジョウ インスティテュート オブ バイオメディスン アンド ヘルス，チャイニーズ アカデミー オブ サイエンスィズ アミド化合物
US9238643B2 (en) 2010-09-06 2016-01-19 Guangzhou Institutes Of Biomedicine And Health, Chinese Academy Of Sciences Amide compounds
WO2012120399A1 (en) 2011-03-10 2012-09-13 Pfizer Inc. Spirocyclic isoxazoline derivatives as antiparasitic agents
US8466115B2 (en) 2011-03-10 2013-06-18 Zoetis Llc Spirocyclic isoxazoline derivatives as antiparasitic agents
CN103517907A (zh) * 2011-03-10 2014-01-15 佐蒂斯有限责任公司 作为抗寄生物剂的螺环异噁唑啉衍生物
JP2014508773A (ja) * 2011-03-10 2014-04-10 ゾエティス・エルエルシー 抗寄生虫薬としてのスピロ環式イソオキサゾリン誘導体
WO2013056148A2 (en) 2011-10-15 2013-04-18 Genentech, Inc. Methods of using scd1 antagonists
WO2013175474A2 (en) 2012-05-22 2013-11-28 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Selective inhibitors of undifferentiated cells
US9456998B2 (en) 2012-05-22 2016-10-04 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Selective inhibitors of undifferentiated cells
US9420793B2 (en) 2015-01-16 2016-08-23 Avista Pharma Solutions Antiparasitic compounds
US10772331B2 (en) 2015-01-16 2020-09-15 Avista Pharma Solutions, Inc. Antiparasitic compounds
US9883674B2 (en) 2015-01-16 2018-02-06 Avista Pharma Solutions, Inc. Antiparasitic compounds
US9686991B2 (en) 2015-01-16 2017-06-27 Avista Pharma Solutions, Inc. Antiparasitic compounds
US10092001B2 (en) 2015-01-16 2018-10-09 Avista Pharma Solutions, Inc. Antiparasitic compounds
US10342234B2 (en) 2015-01-16 2019-07-09 Avista Pharma Solutions, Inc. Antiparasitic compounds
US10696674B2 (en) 2016-07-07 2020-06-30 Bristol-Myers Squibb Company Spirolactams as inhibitors of ROCK
US11970486B2 (en) 2016-10-24 2024-04-30 Janssen Pharmaceutica Nv Compounds and uses thereof
WO2018129403A1 (en) 2017-01-06 2018-07-12 Yumanity Therapeutics Methods for the treatment of neurological disorders
US10973810B2 (en) 2017-01-06 2021-04-13 Yumanity Therapeutics, Inc. Methods for the treatment of neurological disorders
US11873298B2 (en) 2017-10-24 2024-01-16 Janssen Pharmaceutica Nv Compounds and uses thereof
US10807992B2 (en) 2017-11-16 2020-10-20 Avista Pharma Solutions, Inc. Single enantiomer antiparasitic compounds
US12098146B2 (en) 2019-01-24 2024-09-24 Janssen Pharmaceutica Nv Compounds and uses thereof
WO2020249079A1 (zh) * 2019-06-14 2020-12-17 北京盛诺基医药科技股份有限公司 一种shp2磷酸酶变构抑制剂
CN115197228A (zh) * 2022-07-13 2022-10-18 河南师范大学 吡唑啉酮[螺]二氢酞嗪和1,3-茚二酮[螺]二氢酞嗪类化合物的合成方法

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