JP6495915B2 - Ｔｎｆ活性のモジュレーターとしての縮合イミダゾール及びピラゾール誘導体 - Google Patents

Ｔｎｆ活性のモジュレーターとしての縮合イミダゾール及びピラゾール誘導体 Download PDF

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Publication number
JP6495915B2
JP6495915B2 JP2016537447A JP2016537447A JP6495915B2 JP 6495915 B2 JP6495915 B2 JP 6495915B2 JP 2016537447 A JP2016537447 A JP 2016537447A JP 2016537447 A JP2016537447 A JP 2016537447A JP 6495915 B2 JP6495915 B2 JP 6495915B2
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JP
Japan
Prior art keywords
alkyl
pyrimidinyl
methyl
hydroxy
optionally substituted
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Expired - Fee Related
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JP2016537447A
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Japanese (ja)
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JP2016539961A (ja
Inventor
ピーター アリグザンダー、リッキ
ピーター アリグザンダー、リッキ
マーク ベントリー、ジョナサン
マーク ベントリー、ジョナサン
ニール ブレイス、ガレス
ニール ブレイス、ガレス
クリストファー ブルッキングス、ダニエル
クリストファー ブルッキングス、ダニエル
トゥルシ チョヴァティア、プラフル
トゥルシ チョヴァティア、プラフル
ジャン クロード デヴォーブ、エルヴェ
ジャン クロード デヴォーブ、エルヴェ
ジョンストーン、クレイグ
パール ジョーンズ、エリザベス
パール ジョーンズ、エリザベス
クロープリアン、ボリス
クロード ルコント、ファビアン
クロード ルコント、ファビアン
マッデン、ジェイムズ
エイドリアン ミラー、クレイグ
エイドリアン ミラー、クレイグ
ロバート ポーター、ジョン
ロバート ポーター、ジョン
ダンカン セルビー、マシュー
ダンカン セルビー、マシュー
アラン ショウ、マイケル
アラン ショウ、マイケル
ガンヴァント ヴァイディヤ、ダーシャン
ガンヴァント ヴァイディヤ、ダーシャン
アンドリュー ユール、イアン
アンドリュー ユール、イアン
Original Assignee
ユーシービー バイオファルマ エスピーアールエル
ユーシービー バイオファルマ エスピーアールエル
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Publication of JP2016539961A publication Critical patent/JP2016539961A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4355—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2016537447A 2013-12-09 2014-12-08 Ｔｎｆ活性のモジュレーターとしての縮合イミダゾール及びピラゾール誘導体 Expired - Fee Related JP6495915B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1321738.5A GB201321738D0 (en) 2013-12-09 2013-12-09 Therapeutic Agents
GB1321738.5 2013-12-09
PCT/EP2014/076845 WO2015086506A1 (en) 2013-12-09 2014-12-08 Fused imidazole and pyrazole derivatives as modulators of tnf activity

Publications (2)

Publication Number Publication Date
JP2016539961A JP2016539961A (ja) 2016-12-22
JP6495915B2 true JP6495915B2 (ja) 2019-04-03

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JP2016537447A Expired - Fee Related JP6495915B2 (ja) 2013-12-09 2014-12-08 Ｔｎｆ活性のモジュレーターとしての縮合イミダゾール及びピラゾール誘導体

Country Status (11)

Country Link
US (1) US9868749B2 (https=)
EP (1) EP3080115B1 (https=)
JP (1) JP6495915B2 (https=)
CN (1) CN105814054B (https=)
BR (1) BR112016011851B1 (https=)
CA (1) CA2932056C (https=)
ES (1) ES2733927T3 (https=)
GB (1) GB201321738D0 (https=)
RU (1) RU2687093C1 (https=)
TR (1) TR201908447T4 (https=)
WO (1) WO2015086506A1 (https=)

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TW202214640A (zh) 2020-06-16 2022-04-16 美商佛拉斯托醫療公司 Ｅｎｐｐ１之雜環抑制劑
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Publication number Priority date Publication date Assignee Title
JP2018521025A (ja) * 2015-06-08 2018-08-02 ユーシービー バイオファルマ エスピーアールエル Ｔｎｆ活性のモジュレーターとしてのベンゾオキサジノン誘導体およびその類似体

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JP2016539961A (ja) 2016-12-22
CA2932056C (en) 2021-10-26
CA2932056A1 (en) 2015-06-18
GB201321738D0 (en) 2014-01-22
US20160297837A1 (en) 2016-10-13
TR201908447T4 (tr) 2019-07-22
BR112016011851B1 (pt) 2022-07-19
BR112016011851A2 (https=) 2017-08-08
EP3080115B1 (en) 2019-05-08
WO2015086506A1 (en) 2015-06-18
EP3080115A1 (en) 2016-10-19
RU2687093C1 (ru) 2019-05-07
CN105814054B (zh) 2018-09-25
CN105814054A (zh) 2016-07-27
US9868749B2 (en) 2018-01-16
ES2733927T3 (es) 2019-12-03

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