WO2008111299A1 - 新規なジアミド誘導体 - Google Patents

新規なジアミド誘導体 Download PDF

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Publication number
WO2008111299A1
WO2008111299A1 PCT/JP2008/000501 JP2008000501W WO2008111299A1 WO 2008111299 A1 WO2008111299 A1 WO 2008111299A1 JP 2008000501 W JP2008000501 W JP 2008000501W WO 2008111299 A1 WO2008111299 A1 WO 2008111299A1
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Prior art keywords
group
disclosed
ring
formula
diamide derivative
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PCT/JP2008/000501
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English (en)
French (fr)
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Akiyoshi Mochizuki
Tsutomu Nagata
Daisuke Takano
Hideyuki Kanno
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Daiichi Sankyo Company, Limited
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Application filed by Daiichi Sankyo Company, Limited filed Critical Daiichi Sankyo Company, Limited
Publication of WO2008111299A1 publication Critical patent/WO2008111299A1/ja

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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 to ring carbon atoms
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D333/40—Thiophene-2-carboxylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (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)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

　強力なＦＸａ阻害作用を有し、経口投与でも速やかに十分かつ持続的な抗血栓効果を示す新規な化合物を提供する。 　下記の一般式（Ｉ） ［式中、環Ａはベンゼン環等を示し；Ｒ１は水素原子、ハロゲノ基等；Ｒ２はカルボキシ基、カルバモイル基等；Ｔ１は、基－Ｃ（＝Ｏ）ＮＨ－等；Ｔ２は、基－ＣＨ２－ＮＨＣ（＝Ｏ）－等；Ｑ１は、３－オキソチオモルホリニル基、テトラヒドロチアゾロピリジル基等；Ｑ２は単結合、１，４－フェニレン基等；Ｑ３はフェニル基、ピリジル基等を示す。］で表される化合物又はその薬理上許容される塩、又はこれらを有効成分として含有するＦＸａ阻害剤。
PCT/JP2008/000501 2007-03-09 2008-03-10 新規なジアミド誘導体 WO2008111299A1 (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007059675A JP2010120852A (ja) 2007-03-09 2007-03-09 新規なジアミド誘導体
JP2007-059675 2007-03-09

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PCT/JP2008/000506 WO2008123017A1 (ja) 2007-03-09 2008-03-10 新規なジアミド誘導体

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TW (3) TW200843751A (ja)
WO (3) WO2008111299A1 (ja)

Cited By (32)

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CN101875655A (zh) * 2009-04-28 2010-11-03 天津药物研究院 氨基苯甲酸衍生物及其制备方法和用途
JP2010539206A (ja) * 2007-09-19 2010-12-16 ４エスツェー アクチェンゲゼルシャフト 新規テトラヒドロ融合ピリジン
US8785473B2 (en) 2009-03-31 2014-07-22 Renascience Co., Ltd. Plasminogen activator inhibitor-1 inhibitor
US9145412B2 (en) 2012-11-02 2015-09-29 Acetylon Pharmaceuticals, Inc. Selective HDAC1 and HDAC2 inhibitors
CN105101959A (zh) * 2012-11-05 2015-11-25 南特知识产权控股有限责任公司 作为刺猬信号传导通路的抑制剂的含有环状磺酰胺的衍生物
EP3078378A1 (en) 2015-04-08 2016-10-12 Vaiomer Use of factor xa inhibitors for regulating glycemia
US9790180B2 (en) 2014-12-12 2017-10-17 Regenacy Pharmaceuticals, Llc Piperidine derivatives as HDAC1/2 inhibitors
US9833466B2 (en) 2014-07-07 2017-12-05 Acetylon Pharmaceuticals, Inc. Treatment of leukemia with histone deacetylase inhibitors
US10092537B2 (en) 2013-04-15 2018-10-09 Renascience Co., Ltd. Use for PAI-1 inhibitor
CN109890819A (zh) * 2016-06-20 2019-06-14 因赛特公司 作为免疫调节剂的杂环化合物
US10464896B2 (en) 2015-06-11 2019-11-05 Basilea Pharmaceutica International AG Efflux-pump inhibitors and therapeutic uses thereof
WO2020153414A1 (ja) 2019-01-24 2020-07-30 武田薬品工業株式会社 複素環化合物及びその用途
KR20210066768A (ko) * 2019-11-28 2021-06-07 동방에프티엘(주) 광학 활성 다이아민 유도체 및 티아졸 유도체의 생산을 위한 새로운 합성경로
US11124511B2 (en) 2018-03-30 2021-09-21 Incyte Corporation Heterocyclic compounds as immunomodulators
US11401279B2 (en) 2019-09-30 2022-08-02 Incyte Corporation Pyrido[3,2-d]pyrimidine compounds as immunomodulators
US11407749B2 (en) 2015-10-19 2022-08-09 Incyte Corporation Heterocyclic compounds as immunomodulators
US11414433B2 (en) 2018-05-11 2022-08-16 Incyte Corporation Heterocyclic compounds as immunomodulators
US11427600B2 (en) 2014-06-27 2022-08-30 Nogra Pharma Limited Aryl receptor modulators and methods of making and using the same
US11465981B2 (en) 2016-12-22 2022-10-11 Incyte Corporation Heterocyclic compounds as immunomodulators
US11535615B2 (en) 2015-12-22 2022-12-27 Incyte Corporation Heterocyclic compounds as immunomodulators
US11566026B2 (en) 2016-12-22 2023-01-31 Incyte Corporation Heterocyclic compounds as immunomodulators
US11572366B2 (en) 2015-11-19 2023-02-07 Incyte Corporation Heterocyclic compounds as immunomodulators
US11608337B2 (en) 2016-05-06 2023-03-21 Incyte Corporation Heterocyclic compounds as immunomodulators
US11613536B2 (en) 2016-08-29 2023-03-28 Incyte Corporation Heterocyclic compounds as immunomodulators
US11673883B2 (en) 2016-05-26 2023-06-13 Incyte Corporation Heterocyclic compounds as immunomodulators
US11718605B2 (en) 2016-07-14 2023-08-08 Incyte Corporation Heterocyclic compounds as immunomodulators
US11753406B2 (en) 2019-08-09 2023-09-12 Incyte Corporation Salts of a PD-1/PD-L1 inhibitor
US11760756B2 (en) 2020-11-06 2023-09-19 Incyte Corporation Crystalline form of a PD-1/PD-L1 inhibitor
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
US11787793B2 (en) 2016-12-22 2023-10-17 Incyte Corporation Heterocyclic compounds as immunomodulators
US11866434B2 (en) 2020-11-06 2024-01-09 Incyte Corporation Process for making a PD-1/PD-L1 inhibitor and salts and crystalline forms thereof
US11866451B2 (en) 2019-11-11 2024-01-09 Incyte Corporation Salts and crystalline forms of a PD-1/PD-L1 inhibitor

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KR102087080B1 (ko) * 2018-06-08 2020-03-10 주식회사 가피바이오 에독사반의 제조용 중간체의 제조 방법 및 에독사반의 제조 방법
WO2020179269A1 (ja) * 2019-03-01 2020-09-10 三菱自動車工業株式会社 車両用フード

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WO2007007588A1 (ja) * 2005-07-08 2007-01-18 Ono Pharmaceutical Co., Ltd. 平面性を有する環状基を母核とする化合物

Cited By (50)

* Cited by examiner, † Cited by third party
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JP2010539206A (ja) * 2007-09-19 2010-12-16 ４エスツェー アクチェンゲゼルシャフト 新規テトラヒドロ融合ピリジン
US8785473B2 (en) 2009-03-31 2014-07-22 Renascience Co., Ltd. Plasminogen activator inhibitor-1 inhibitor
CN101875655A (zh) * 2009-04-28 2010-11-03 天津药物研究院 氨基苯甲酸衍生物及其制备方法和用途
US9421212B2 (en) 2012-11-02 2016-08-23 Acetylon Pharmaceuticals, Inc. Selective HDAC1 and HDAC2 inhibitors
US9145412B2 (en) 2012-11-02 2015-09-29 Acetylon Pharmaceuticals, Inc. Selective HDAC1 and HDAC2 inhibitors
US9957259B2 (en) 2012-11-02 2018-05-01 Regenacy Pharmaceuticals, Llc Selective HDAC1 and HDAC2 inhibitors
US9765066B2 (en) 2012-11-02 2017-09-19 Regenacy Pharmaceuticals, Llc Selective HDAC1 and HDAC2 inhibitors
AU2013337370B2 (en) * 2012-11-05 2018-03-29 Nantbioscience, Inc. Cyclic sulfonamide containing derivatives as inhibitors of hedgehog signaling pathway
JP2016504276A (ja) * 2012-11-05 2016-02-12 ナント ホールディングス アイピー，エルエルシー ヘッジホッグシグナル伝達経路阻害剤としての環状スルホンアミド含有誘導体
US9499539B2 (en) 2012-11-05 2016-11-22 Nantbioscience, Inc. Cyclic sulfonamide containing derivatives as inhibitors of hedgehog signaling pathway
EP2914253A4 (en) * 2012-11-05 2016-04-27 Nant Holdings Ip Llc CYCLIC SULFONAMIDE-CONTAINING DERIVATIVES AS INHIBITORS OF THE HEDGEHOG SIGNALING PATH
CN105101959A (zh) * 2012-11-05 2015-11-25 南特知识产权控股有限责任公司 作为刺猬信号传导通路的抑制剂的含有环状磺酰胺的衍生物
US10183013B2 (en) 2012-11-05 2019-01-22 Nant Holdings Ip, Llc Cyclic sulfonamide containing derivatives as inhibitors of hedgehog signaling pathway
CN105101959B (zh) * 2012-11-05 2018-04-17 南特知识产权控股有限责任公司 作为刺猬信号传导通路的抑制剂的含有环状磺酰胺的衍生物
US10092537B2 (en) 2013-04-15 2018-10-09 Renascience Co., Ltd. Use for PAI-1 inhibitor
US11427600B2 (en) 2014-06-27 2022-08-30 Nogra Pharma Limited Aryl receptor modulators and methods of making and using the same
US9833466B2 (en) 2014-07-07 2017-12-05 Acetylon Pharmaceuticals, Inc. Treatment of leukemia with histone deacetylase inhibitors
US10239837B2 (en) 2014-12-12 2019-03-26 Regenacy Pharmaceuticals, Llc Piperidine derivatives as HDAC1/2 inhibitors
US10358421B2 (en) 2014-12-12 2019-07-23 Regenacy Pharmaceuticals, Llc Piperidine derivatives as HDAC1/2 inhibitors
US11702389B2 (en) 2014-12-12 2023-07-18 Regenacy Pharmaceuticals, Llc Piperidine derivatives as HDAC1/2 inhibitors
US10968180B2 (en) 2014-12-12 2021-04-06 Regenacy Pharmaceuticals, Llc Piperidine derivatives as HDAC1/2 inhibitors
US9790180B2 (en) 2014-12-12 2017-10-17 Regenacy Pharmaceuticals, Llc Piperidine derivatives as HDAC1/2 inhibitors
EP3078378A1 (en) 2015-04-08 2016-10-12 Vaiomer Use of factor xa inhibitors for regulating glycemia
WO2016162472A1 (en) 2015-04-08 2016-10-13 Vaiomer Use of factor xa inhibitors for regulating glycemia
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CN109890819A (zh) * 2016-06-20 2019-06-14 因赛特公司 作为免疫调节剂的杂环化合物
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US11718605B2 (en) 2016-07-14 2023-08-08 Incyte Corporation Heterocyclic compounds as immunomodulators
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US11414433B2 (en) 2018-05-11 2022-08-16 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2020153414A1 (ja) 2019-01-24 2020-07-30 武田薬品工業株式会社 複素環化合物及びその用途
US11753406B2 (en) 2019-08-09 2023-09-12 Incyte Corporation Salts of a PD-1/PD-L1 inhibitor
US11401279B2 (en) 2019-09-30 2022-08-02 Incyte Corporation Pyrido[3,2-d]pyrimidine compounds as immunomodulators
US11866451B2 (en) 2019-11-11 2024-01-09 Incyte Corporation Salts and crystalline forms of a PD-1/PD-L1 inhibitor
KR20210066768A (ko) * 2019-11-28 2021-06-07 동방에프티엘(주) 광학 활성 다이아민 유도체 및 티아졸 유도체의 생산을 위한 새로운 합성경로
KR102295388B1 (ko) 2019-11-28 2021-08-31 동방에프티엘(주) 광학 활성 다이아민 유도체 및 티아졸 유도체의 생산을 위한 새로운 합성경로
US11760756B2 (en) 2020-11-06 2023-09-19 Incyte Corporation Crystalline form of a PD-1/PD-L1 inhibitor
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
US11866434B2 (en) 2020-11-06 2024-01-09 Incyte Corporation Process for making a PD-1/PD-L1 inhibitor and salts and crystalline forms thereof

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