JP2012521429A - 疼痛治療用のｐ２ｘ３受容体アンタゴニスト - Google Patents

疼痛治療用のｐ２ｘ３受容体アンタゴニスト Download PDF

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Publication number
JP2012521429A
JP2012521429A JP2012502098A JP2012502098A JP2012521429A JP 2012521429 A JP2012521429 A JP 2012521429A JP 2012502098 A JP2012502098 A JP 2012502098A JP 2012502098 A JP2012502098 A JP 2012502098A JP 2012521429 A JP2012521429 A JP 2012521429A
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chry
alkyl
mmol
optionally substituted
heterocyclyl
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Japanese (ja)
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JP2012521429A5 (enExample
Inventor
バーギー，クリストフアー・エス
クラウリー，ブレンダン・エム
ドン，ジエンウー・ジエイ
パオン，ダニエル・ブイ
ポテイジヤー，クレツグ・エム
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Merck and Co Inc
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Merck and Co Inc
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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
    • C07D401/12—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
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2012502098A 2009-03-23 2010-03-15 疼痛治療用のｐ２ｘ３受容体アンタゴニスト Pending JP2012521429A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US21077809P 2009-03-23 2009-03-23
US61/210,778 2009-03-23
PCT/US2010/027303 WO2010111060A1 (en) 2009-03-23 2010-03-15 P2x3, receptor antagonists for treatment of pain

Publications (2)

Publication Number Publication Date
JP2012521429A true JP2012521429A (ja) 2012-09-13
JP2012521429A5 JP2012521429A5 (enExample) 2013-05-02

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Family Applications (1)

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JP2012502098A Pending JP2012521429A (ja) 2009-03-23 2010-03-15 疼痛治療用のｐ２ｘ３受容体アンタゴニスト

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Country Link
US (1) US8569512B2 (enExample)
EP (1) EP2411001B1 (enExample)
JP (1) JP2012521429A (enExample)
AU (1) AU2010229144B2 (enExample)
CA (1) CA2755768A1 (enExample)
ES (1) ES2660892T3 (enExample)
WO (1) WO2010111060A1 (enExample)

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012532832A (ja) * 2009-06-22 2012-12-20 エフ．ホフマン−ラ ロシュ アーゲー Ｐ２ｘ３および／またはｐ２ｘ２／３アンタゴニストとしての、新規なインドール、インダゾールおよびベンゾイミダゾールアリールアミド
JP2015110599A (ja) * 2009-01-26 2015-06-18 ドマン・テラプーテイツク 新規なアデノシン受容体リガンドおよびその使用
KR20160097250A (ko) * 2013-12-16 2016-08-17 아사나 바이오사이언시스 엘엘씨 P2x3 및/또는 p2x2/3 화합물 및 방법
JP2018531253A (ja) * 2015-10-06 2018-10-25 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ トリアゾール誘導体
JP2019504898A (ja) * 2016-02-12 2019-02-21 ファーマクシス リミテッド リジルオキシダーゼのハロアリルアミンインドールおよびアザインドール誘導体阻害剤およびその使用
JP2020500192A (ja) * 2016-11-18 2020-01-09 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． ジアシルグリセリドｏ−アシルトランスフェラーゼ２の阻害薬として有用なインドール誘導体
JP2020502058A (ja) * 2016-11-18 2020-01-23 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． ジアシルグリセリドｏ−アシルトランスフェラーゼ２の阻害薬として有用なインダゾール誘導体
JP2024514361A (ja) * 2021-04-29 2024-04-01 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｓｔｉｎｇを活性化することができるヘテロ環式化合物

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WO2009110985A2 (en) 2008-02-29 2009-09-11 Renovis, Inc. Amide compounds, compositions and uses thereof
US20110237578A1 (en) 2008-09-18 2011-09-29 Zhi-Liang Wei Amide compounds, compositions and uses thereof
ES2835553T3 (es) 2009-08-10 2021-06-22 Biosplice Therapeutics Inc Inhibidores de indazol de la vía de señalización de Wnt y sus usos terapéuticos
SMT201700581T1 (it) 2009-12-21 2018-01-11 Samumed Llc 1h-pirazolo[3,4-b]piridine e loro usi terapeutici
EP2673728B1 (en) 2011-02-08 2018-09-12 dacadoo ag System, method and apparatus for the remote analysis of chemical compound microarrays
HUE041576T2 (hu) 2011-09-14 2019-05-28 Samumed Llc Indazol-3-karboxamid-származékok és alkalmazásuk Wnt/b-katenin szignalizáló útvonal inhibitorokként
JP2014533258A (ja) * 2011-11-15 2014-12-11 ゼンション・リミテッドＸｅｎｔｉｏｎ Ｌｉｍｉｔｅｄ カリウムチャネル阻害剤としてのチエノ［２，３−ｃ］ピラゾールの使用
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
SG11201407148XA (en) 2012-05-04 2014-11-27 Samumed Llc 1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
US9908867B2 (en) 2013-01-08 2018-03-06 Samumed, Llc 3-(benzoimidazol-2-yl)-indazole inhibitors of the Wnt signaling pathway and therapeutic uses thereof
WO2014127256A1 (en) * 2013-02-18 2014-08-21 The Trustees Of Columbia University In The City Of New York Kappa opioid receptor selective compounds
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US10568876B2 (en) 2014-09-05 2020-02-25 Merck Sharp & Dohme Corp. Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2
WO2016036638A1 (en) 2014-09-05 2016-03-10 Merck Sharp & Dohme Corp. Isoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2
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WO2016040181A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
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CA2978823C (en) 2014-12-29 2023-10-10 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Small molecule inhibitors of lactate dehydrogenase and methods of use thereof
KR101663277B1 (ko) * 2015-03-30 2016-10-06 주식회사 녹십자 TNIK, IKKε 및 TBK1 억제제로서의 피라졸계 유도체 및 이를 포함하는 약학적 조성물
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WO2017023980A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
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US10463651B2 (en) 2015-08-03 2019-11-05 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-indazoles and therapeutic uses thereof
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WO2022063205A1 (zh) * 2020-09-24 2022-03-31 中国医药研究开发中心有限公司 芳基甲酰胺类化合物及其制备方法和医药用途
CN112574180B (zh) * 2020-12-30 2021-10-15 浙江工业大学 N-2-嘧啶基-3-氟吲哚类化合物及其制备方法与应用
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JP2025532621A (ja) 2022-09-15 2025-10-01 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 超分子ポリマー治療および診断
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