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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (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)

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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
JP2019504899A (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インドールおよびアザインドールハロアリルアミン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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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2010009561A (es) 2008-02-29 2010-09-24 Renovis Inc Compuestos amida, composiciones y usos de los mismos.
JP5608655B2 (ja) 2008-09-18 2014-10-15 エヴォテック アーゲー Ｐ２ｘ３受容体活性のモジュレーター
DK2987487T3 (da) 2009-08-10 2020-12-07 Samumed Llc Indazolinhibitorer af wnt-signalvejen og terapeutiske anvendelser deraf
LT3001903T (lt) 2009-12-21 2018-01-10 Samumed, Llc 1h-pirazolo[3,4-b]piridinai ir jų terapinis panaudojimas
EP2673728B1 (en) 2011-02-08 2018-09-12 dacadoo ag System, method and apparatus for the remote analysis of chemical compound microarrays
EP3473099A1 (en) 2011-09-14 2019-04-24 Samumed, LLC Indazole-3-carboxamides and their use as wnt/b-catenin signaling pathway inhibitors
EP2780344A1 (en) * 2011-11-15 2014-09-24 Xention Limited Thieno [2, 3 - c]pyrazoles for use as potassium channel inhibitors
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
KR102223301B1 (ko) 2012-05-04 2021-03-05 사뮤메드, 엘엘씨 1H-피라졸로[3,4-b]피리딘 및 그의 치료 용도
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
US9868730B2 (en) 2013-02-18 2018-01-16 The Trustees Of Columbia University In The City Of New York Kappa opioid receptor selective compounds, compositions, and uses thereof
EP2905282A1 (en) * 2014-02-05 2015-08-12 AXXAM S.p.A. Substituted thiazole or oxazole as P2X7 receptor antagonists
EP3188732B1 (en) 2014-09-05 2019-07-24 Merck Sharp & Dohme Corp. Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2
EP3188730B1 (en) 2014-09-05 2019-05-01 Merck Sharp & Dohme Corp. Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2
US9828369B2 (en) 2014-09-05 2017-11-28 Merck Sharpe & Dohme Corp. Isoquinoline derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2
WO2016040188A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040185A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof
WO2016040184A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
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
WO2016040190A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
WO2016040182A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 2-(1h-indazol-3-yl)-1h-imidazo[4,5-c]pyridine and therapeutic uses thereof
WO2016040193A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
WO2016040180A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
US10351532B2 (en) 2014-12-29 2019-07-16 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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US10383861B2 (en) 2015-08-03 2019-08-20 Sammumed, LLC 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
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WO2017024015A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10350199B2 (en) 2015-08-03 2019-07-16 Samumed, Llc 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
US10206908B2 (en) 2015-08-03 2019-02-19 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
WO2017023989A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10231956B2 (en) 2015-08-03 2019-03-19 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
US10226453B2 (en) 2015-08-03 2019-03-12 Samumed, Llc 3-(1H-indol-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017023986A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-indazoles and therapeutic uses thereof
US10285982B2 (en) 2015-08-03 2019-05-14 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
WO2017023972A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017028314A1 (en) * 2015-08-20 2017-02-23 Changzhou Jiekai Pharmatech Co., Ltd. Pyrazolo fused heterocyclic compounds as erk inhibitors
WO2017079759A1 (en) 2015-11-06 2017-05-11 Samumed, Llc 2-(1h-indazol-3-yl)-3h-imidazo[4,5-c]pyridines and their anti-inflammatory uses thereof
AR108325A1 (es) 2016-04-27 2018-08-08 Samumed Llc Isoquinolin-3-il carboxamidas y preparación y uso de las mismas
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AU2017345699A1 (en) 2016-10-21 2019-05-16 Samumed, Llc Methods of using indazole-3-carboxamides and their use as Wnt/B-catenin signaling pathway inhibitors
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US11351149B2 (en) 2020-09-03 2022-06-07 Pfizer Inc. Nitrile-containing antiviral compounds
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
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EP4598923A1 (en) 2022-09-15 2025-08-13 The Regents of the University of California Supramolecular polymer therapeutics and diagnostics
AU2024207083A1 (en) * 2023-01-09 2025-07-17 University Of Florida Research Foundation, Incorporated Pparg modulators

Citations (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5037844A (en) * 1989-07-25 1991-08-06 Duphar International Research B.V. Substituted 1H-indazole-3-carboxamides
WO1998009961A1 (en) * 1996-09-04 1998-03-12 Pfizer Inc. Indazole derivatives and their use as inhibitors of phosphodiesterase (pde) type iv and the production of tumor necrosis factor (tnf)
US20020103229A1 (en) * 2000-07-31 2002-08-01 Bhagwat Shripad S. Indazole derivatives as JNK inhibitors and compositions and methods related thereto
WO2002083648A1 (fr) * 2001-04-16 2002-10-24 Eisai Co., Ltd. Nouveau compose a base de 1h-indazole
WO2003000682A1 (en) * 2001-06-25 2003-01-03 Merck & Co., Inc. (pyrimidyl)(phenyl)substituted fused heteroaryl p38 inhibiting and pkg kinase inhibiting compounds
WO2004029050A1 (en) * 2002-09-25 2004-04-08 Memory Pharmaceuticals Corporation Indazoles, benzothiazoles, and benzoisothiazoles, and preparation and uses thereof
WO2004089470A2 (en) * 2003-04-11 2004-10-21 Novo Nordisk A/S New amide derivatives and pharmaceutical use thereof
US20050009876A1 (en) * 2000-07-31 2005-01-13 Bhagwat Shripad S. Indazole compounds, compositions thereof and methods of treatment therewith
US20050026984A1 (en) * 2003-07-29 2005-02-03 Aventis Pharma S.A. Substituted thieno [2,3-c] pyrazoles and their use as medicinal products
WO2005051318A2 (en) * 2003-11-24 2005-06-09 Viropharma Incorporated Compounds, compositions and methods for treatment and prophylaxis of hepatitis c viral infections and associated diseases
WO2007020194A1 (en) * 2005-08-15 2007-02-22 F. Hoffmann-La Roche Ag Piperidine and piperazine derivatives as p2x3 antagonists
EP1775298A1 (en) * 2004-07-01 2007-04-18 Daiichi Asubio Pharma Co., Ltd. Thienopyrazole derivative having pde7 inhibitory activity
WO2007118137A1 (en) * 2006-04-07 2007-10-18 Methylgene Inc. Benzamide derivatives as inhibitors of histone deacetylase
WO2007127212A2 (en) * 2006-04-25 2007-11-08 The Cleveland Clinic Foundation Anti-viral agents that activate rnase l
WO2008012571A1 (en) * 2006-07-24 2008-01-31 Merck Sharp & Dohme Limited Imidazothiazole derivatives as mark inhibitors
WO2008015125A1 (en) * 2006-08-03 2008-02-07 F. Hoffmann-La Roche Ag 1h-indol-6-yl-piperazin-1-yl-methanone-derivatives for use as h3 receptor modulators
WO2008075196A1 (en) * 2006-12-15 2008-06-26 Pfizer Products Inc. Benzimidazole derivatives
US20080260643A1 (en) * 2007-03-27 2008-10-23 Omeros Corporation Use of pde7 inhibitors for the treatment of movement disorders
WO2008133274A1 (ja) * 2007-04-24 2008-11-06 Shionogi & Co., Ltd. 環式基で置換されたアミノジヒドロチアジン誘導体
JP2011507910A (ja) * 2007-12-21 2011-03-10 ユニバーシティー オブ ロチェスター 真核生物の寿命を変更するための方法

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8623429D0 (en) * 1985-10-17 1986-11-05 Ici America Inc Carboximide derivatives
JP2000501105A (ja) * 1995-12-22 2000-02-02 デュポン ファーマシューティカルズ カンパニー 新規なインテグリン受容体アンタゴニスト
CZ2002599A3 (cs) 1999-08-19 2002-06-12 Nps Pharmaceuticals Inc. Heteropolycyklické sloučeniny a jejich pouľití jako antagonistů metabotropního receptoru glutamátu
US20060083714A1 (en) * 2003-01-27 2006-04-20 Warner James M Combination of a pde iv inhibitor and a tnf-alpha antagonist
US7135575B2 (en) * 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
TW200526204A (en) * 2004-02-03 2005-08-16 Pharmacia Italia Spa 1h-thieno[2,3-c]pyrazole derivatives useful as kinase inhibitors
DE102004028862A1 (de) * 2004-06-15 2005-12-29 Merck Patent Gmbh 3-Aminoindazole
FR2882751B1 (fr) 2005-03-04 2007-09-14 Aventis Pharma Sa Hydrazinocarbonyl-thieno[2,3-c]pyrazoles, procede de preparation, compositions les contenant et utilisation
WO2007010553A2 (en) 2005-03-24 2007-01-25 Arrow Coated Products Ltd Combined multi-layered water soluble film and process for producing the same
WO2006119504A2 (en) 2005-05-04 2006-11-09 Renovis, Inc. Fused heterocyclic compounds, and compositions and uses thereof
US20090054491A1 (en) 2005-06-28 2009-02-26 Astrazeneca Ab Use
WO2007025925A1 (en) 2005-09-01 2007-03-08 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
CA2624379A1 (en) 2005-09-30 2007-04-12 Merck & Co., Inc. Nucleic acids encoding a functional mammalian purinoreceptor, p2x3, methods of production and use thereof
WO2008000645A1 (en) 2006-06-29 2008-01-03 F. Hoffmann-La Roche Ag Tetrazole-substituted arylamides
FR2903107B1 (fr) * 2006-07-03 2008-08-22 Sanofi Aventis Sa Derives d'imidazopyridine-2-carboxamides, leur preparation et leur application en therapeutique
DE102006032824A1 (de) * 2006-07-14 2008-01-17 Bayer Healthcare Ag Substituierte Indazole
WO2009059030A1 (en) * 2007-10-31 2009-05-07 Burnham Institute For Medical Research Pyrazole derivatives as kinase inhibitors
US8247401B2 (en) 2007-10-31 2012-08-21 Merck Sharp & Dohme Corp. P2X3 receptor antagonists for treatment of pain
WO2009058299A1 (en) 2007-10-31 2009-05-07 Merck & Co., Inc. P2x3 receptor antagonists for treatment of pain
MX2011004570A (es) 2008-10-31 2011-06-17 Merck Sharp & Dohme Antagonistas del receptor p2x3 para el tratamiento del dolor.

Patent Citations (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5037844A (en) * 1989-07-25 1991-08-06 Duphar International Research B.V. Substituted 1H-indazole-3-carboxamides
WO1998009961A1 (en) * 1996-09-04 1998-03-12 Pfizer Inc. Indazole derivatives and their use as inhibitors of phosphodiesterase (pde) type iv and the production of tumor necrosis factor (tnf)
US20020103229A1 (en) * 2000-07-31 2002-08-01 Bhagwat Shripad S. Indazole derivatives as JNK inhibitors and compositions and methods related thereto
US20050009876A1 (en) * 2000-07-31 2005-01-13 Bhagwat Shripad S. Indazole compounds, compositions thereof and methods of treatment therewith
WO2002083648A1 (fr) * 2001-04-16 2002-10-24 Eisai Co., Ltd. Nouveau compose a base de 1h-indazole
WO2003000682A1 (en) * 2001-06-25 2003-01-03 Merck & Co., Inc. (pyrimidyl)(phenyl)substituted fused heteroaryl p38 inhibiting and pkg kinase inhibiting compounds
WO2004029050A1 (en) * 2002-09-25 2004-04-08 Memory Pharmaceuticals Corporation Indazoles, benzothiazoles, and benzoisothiazoles, and preparation and uses thereof
WO2004089470A2 (en) * 2003-04-11 2004-10-21 Novo Nordisk A/S New amide derivatives and pharmaceutical use thereof
US20050026984A1 (en) * 2003-07-29 2005-02-03 Aventis Pharma S.A. Substituted thieno [2,3-c] pyrazoles and their use as medicinal products
WO2005051318A2 (en) * 2003-11-24 2005-06-09 Viropharma Incorporated Compounds, compositions and methods for treatment and prophylaxis of hepatitis c viral infections and associated diseases
EP1775298A1 (en) * 2004-07-01 2007-04-18 Daiichi Asubio Pharma Co., Ltd. Thienopyrazole derivative having pde7 inhibitory activity
WO2007020194A1 (en) * 2005-08-15 2007-02-22 F. Hoffmann-La Roche Ag Piperidine and piperazine derivatives as p2x3 antagonists
WO2007118137A1 (en) * 2006-04-07 2007-10-18 Methylgene Inc. Benzamide derivatives as inhibitors of histone deacetylase
WO2007127212A2 (en) * 2006-04-25 2007-11-08 The Cleveland Clinic Foundation Anti-viral agents that activate rnase l
WO2008012571A1 (en) * 2006-07-24 2008-01-31 Merck Sharp & Dohme Limited Imidazothiazole derivatives as mark inhibitors
WO2008015125A1 (en) * 2006-08-03 2008-02-07 F. Hoffmann-La Roche Ag 1h-indol-6-yl-piperazin-1-yl-methanone-derivatives for use as h3 receptor modulators
WO2008075196A1 (en) * 2006-12-15 2008-06-26 Pfizer Products Inc. Benzimidazole derivatives
US20080260643A1 (en) * 2007-03-27 2008-10-23 Omeros Corporation Use of pde7 inhibitors for the treatment of movement disorders
WO2008133274A1 (ja) * 2007-04-24 2008-11-06 Shionogi & Co., Ltd. 環式基で置換されたアミノジヒドロチアジン誘導体
JP2011507910A (ja) * 2007-12-21 2011-03-10 ユニバーシティー オブ ロチェスター 真核生物の寿命を変更するための方法

Non-Patent Citations (10)

* Cited by examiner, † Cited by third party
Title
AKRITOPOULOU-ZANZE, IRINI; DARCZAK, DARIA; SARRIS, KATHY; PHELAN, KATHLEEN M.; HUTH, JEFFREY R.; SON: "Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazol", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 16(1), JPN6014023397, 2006, pages 96 - 99, ISSN: 0002828248 *
BAKHITE, E. A.; GEIES, A. A.; EL-KASHEF, H. S.: "Synthesis and antimicrobial activity of some new pyrazoles and thieno[2,3-c]pyrazoles", PHOSPHORUS, SULFUR AND SILICON AND THE RELATED ELEMENTS, vol. 157, JPN6014023413, 2000, pages 107 - 122, ISSN: 0002828256 *
EL-NEZHAWY, A. O. H.; EL-NAEM, S. I.; GALAL, S. A.; EL-DIWANI, H. I.; ABDEL SALAM, O. M. E.; BAIOMY,: "Synthesis and analgesic activity of (2,3-diphenyl-1H-indol-5-YL)piperazin-1-yl methanone derivatives", PHARMACEUTICAL CHEMISTRY JOURNAL, vol. 43(1), JPN6014023414, 2009, pages 25 - 29, ISSN: 0002828257 *
PUBCHEM COMPOUND, [ONLINE], JPN6014023398, ISSN: 0002828249 *
PUBCHEM COMPOUND, [ONLINE], JPN6014023400, ISSN: 0002828250 *
PUBCHEM COMPOUND, [ONLINE], JPN6014023403, ISSN: 0002828251 *
PUBCHEM COMPOUND, [ONLINE], JPN6014023405, ISSN: 0002828252 *
PUBCHEM COMPOUND, [ONLINE], JPN6014023407, ISSN: 0002828253 *
PUBCHEM COMPOUND, [ONLINE], JPN6014023408, ISSN: 0002828254 *
PUBCHEM COMPOUND, [ONLINE], JPN6014023411, ISSN: 0002828255 *

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