WO2008111300A1 - 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
WO2008111300A1
WO2008111300A1 PCT/JP2008/000503 JP2008000503W WO2008111300A1 WO 2008111300 A1 WO2008111300 A1 WO 2008111300A1 JP 2008000503 W JP2008000503 W JP 2008000503W WO 2008111300 A1 WO2008111300 A1 WO 2008111300A1
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WIPO (PCT)
Prior art keywords
group
compound
disclosed
ring
salt
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PCT/JP2008/000503
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English (en)
French (fr)
Inventor
Akiyoshi Mochizuki
Masamichi Kishida
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 WO2008111300A1 publication Critical patent/WO2008111300A1/ja

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic 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
    • C07D333/26Heterocyclic 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
    • C07D333/38Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D333/40Thiophene-2-carboxylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-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)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Hydrogenated Pyridines (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-NHC(=O)-等;T2は、基-CH2-C(=O)NH-等;Q1は、シクロヘキシル基、モルホリニル基等;Q2は単結合、1,4-フェニレン基等;Q3はフェニル基等を示す。]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/JP2008/000503 2007-03-09 2008-03-10 新規なジアミド誘導体 WO2008111300A1 (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

Publications (1)

Publication Number Publication Date
WO2008111300A1 true WO2008111300A1 (ja) 2008-09-18

Family

ID=39759243

Family Applications (3)

Application Number Title Priority Date Filing Date
PCT/JP2008/000506 WO2008123017A1 (ja) 2007-03-09 2008-03-10 新規なジアミド誘導体
PCT/JP2008/000501 WO2008111299A1 (ja) 2007-03-09 2008-03-10 新規なジアミド誘導体
PCT/JP2008/000503 WO2008111300A1 (ja) 2007-03-09 2008-03-10 新規なジアミド誘導体

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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
PCT/JP2008/000501 WO2008111299A1 (ja) 2007-03-09 2008-03-10 新規なジアミド誘導体

Country Status (3)

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JP (1) JP2010120852A (ja)
TW (3) TW200843752A (ja)
WO (3) WO2008123017A1 (ja)

Cited By (4)

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US8785473B2 (en) 2009-03-31 2014-07-22 Renascience Co., Ltd. Plasminogen activator inhibitor-1 inhibitor
EP3078378A1 (en) 2015-04-08 2016-10-12 Vaiomer Use of factor xa inhibitors for regulating glycemia
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

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EP2197552B1 (en) * 2007-09-19 2012-11-21 4Sc Ag Novel tetrahydrofusedpyridines as histone deacetylase inhibitors
CN101875655B (zh) * 2009-04-28 2012-05-09 天津药物研究院 氨基苯甲酸衍生物及其制备方法和用途
US9145412B2 (en) 2012-11-02 2015-09-29 Acetylon Pharmaceuticals, Inc. Selective HDAC1 and HDAC2 inhibitors
CA2890002A1 (en) * 2012-11-05 2014-05-08 Nant Holdings Ip, Llc Cyclic sulfonamide containing derivatives as inhibitors of hedgehog signaling pathway
BR112017000301A2 (pt) 2014-07-07 2017-11-07 Acetylon Pharmaceuticals Inc tratamento de leucemia com inibidores de histona desacetilase
CN107835810A (zh) 2014-12-12 2018-03-23 瑞格纳西制药有限公司 作为hdac1/2抑制剂的哌啶衍生物
EP3307725A1 (en) 2015-06-11 2018-04-18 Basilea Pharmaceutica International AG Efflux-pump inhibitors and therapeutic uses thereof
MA52119A (fr) 2015-10-19 2018-08-29 Ncyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
SG11201804152RA (en) 2015-11-19 2018-06-28 Incyte Corp Heterocyclic compounds as immunomodulators
ES2844374T3 (es) 2015-12-22 2021-07-22 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
EP3452476B1 (en) 2016-05-06 2021-12-15 Incyte Corporation Heterocyclic compounds as immunomodulators
TW201808902A (zh) 2016-05-26 2018-03-16 美商英塞特公司 作為免疫調節劑之雜環化合物
ES2927984T3 (es) 2016-06-20 2022-11-14 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
ES2930092T3 (es) 2016-07-14 2022-12-07 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
ES2941716T3 (es) 2016-08-29 2023-05-25 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
US20180179179A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
EP3558985B1 (en) 2016-12-22 2022-09-07 Incyte Corporation Benzooxazole derivatives as immunomodulators
ES2874756T3 (es) 2016-12-22 2021-11-05 Incyte Corp Derivados de triazolo[1,5-A]piridina como inmunomoduladores
MX2020010321A (es) 2018-03-30 2021-01-08 Incyte Corp Compuestos heterociclicos como inmunomoduladores.
DK3790877T3 (da) 2018-05-11 2023-04-24 Incyte Corp Tetrahydro-imidazo[4,5-c]pyridinderivater som pd-l1-immunmodulatorer
KR102087080B1 (ko) * 2018-06-08 2020-03-10 주식회사 가피바이오 에독사반의 제조용 중간체의 제조 방법 및 에독사반의 제조 방법
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
CN113490623B (zh) * 2019-03-01 2023-06-16 三菱自动车工业株式会社 车辆用引擎盖
EP4010342A1 (en) 2019-08-09 2022-06-15 Incyte Corporation Salts of a pd-1/pd-l1 inhibitor
CA3155852A1 (en) 2019-09-30 2021-04-08 Incyte Corporation PYRIDO[3,2-D]PYRIMIDINE COMPOUNDS AS IMMUNOMODULATORS
MX2022005651A (es) 2019-11-11 2022-07-27 Incyte Corp Sales y formas cristalinas de un inhibidor de la proteina de muerte celular programada 1 (pd-1)/ligando de muerte celular programada 1 (pd-l1).
KR102333564B1 (ko) * 2019-11-28 2021-12-01 동방에프티엘(주) 광학 활성 다이아민 유도체 및 티아졸 유도체의 생산을 위한 새로운 합성경로
JP2023548859A (ja) 2020-11-06 2023-11-21 インサイト・コーポレイション Pd-1/pd-l1阻害剤ならびにその塩及び結晶形態を作製するためのプロセス
WO2022099075A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Crystalline form of a pd-1/pd-l1 inhibitor
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Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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JP2005523237A (ja) * 2001-10-01 2005-08-04 大正製薬株式会社 Mch受容体アンタゴニスト
JP2005097199A (ja) * 2003-09-26 2005-04-14 Tanabe Seiyaku Co Ltd アミン型カルボキサミド誘導体

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8785473B2 (en) 2009-03-31 2014-07-22 Renascience Co., Ltd. Plasminogen activator inhibitor-1 inhibitor
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
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

Also Published As

Publication number Publication date
WO2008123017A1 (ja) 2008-10-16
TW200840568A (en) 2008-10-16
TW200843752A (en) 2008-11-16
TW200843751A (en) 2008-11-16
WO2008111299A1 (ja) 2008-09-18
JP2010120852A (ja) 2010-06-03

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