JP5113976B2 - γ−セクレターゼの作用を調節するスルホン - Google Patents

γ−セクレターゼの作用を調節するスルホン Download PDF

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JP5113976B2
JP5113976B2 JP2002579423A JP2002579423A JP5113976B2 JP 5113976 B2 JP5113976 B2 JP 5113976B2 JP 2002579423 A JP2002579423 A JP 2002579423A JP 2002579423 A JP2002579423 A JP 2002579423A JP 5113976 B2 JP5113976 B2 JP 5113976B2
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mmol
alkyl
ethyl acetate
mixture
halogen
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JP2004533428A5 (https=
JP2004533428A (ja
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カストロ・ピネイロ，ホセ・ルイス
チヤーチヤー，イアン
デインネル，ケビン
ハーリソン，テイモシー
ケラー，ソニア
ナデイン，アラン・ジヨン
オークレイ，ポール・ジヨウゼフ
オーエンズ，アンドリユー・ペイト
シヨー，ダンカン・エドワード
テイール，マーチン・リチヤード
ウイリアムズ，ブライアン・ジヨン
ウイリアムズ，スザンナ
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メルク シャープ エンド ドーム リミテッド
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    • C—CHEMISTRY; METALLURGY
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    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
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    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
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    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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
    • C07D207/36—Oxygen or sulfur atoms
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    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/40—Oxygen atoms
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    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
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    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
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    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
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    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
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Families Citing this family (71)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0108591D0 (en) 2001-04-05 2001-05-23 Merck Sharp & Dohme Therapeutic agents
GB0120347D0 (en) * 2001-08-21 2001-10-17 Merck Sharp & Dohme Therapeutic agents
CN100562516C (zh) 2001-12-27 2009-11-25 第一制药株式会社 β-淀粉样蛋白产生和分泌的抑制剂
GB0218041D0 (en) 2002-08-02 2002-09-11 Merck Sharp & Dohme Chemical process
GB0223038D0 (en) * 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
GB0223039D0 (en) 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
EP1638951B1 (en) * 2003-05-16 2008-02-13 MERCK SHARP & DOHME LTD. Cyclohexyl sulphones as gamma-secretase inhibitors
GB0313772D0 (en) * 2003-06-13 2003-07-23 Merck Sharp & Dohme Therapeutic treatment
CA2526487A1 (en) 2003-06-30 2005-01-06 Daiichi Pharmaceutical Co., Ltd. Heterocyclic methyl sulfone derivative
GB0323258D0 (en) 2003-10-04 2003-11-05 Merck Sharp & Dohme Therapeutic compounds
AR047666A1 (es) * 2004-02-20 2006-02-01 Merck Sharp & Dohme Sintesis estereoselectiva del acido ciclohexanopropanoico 4,4-disubstituido
US8114886B2 (en) * 2005-04-08 2012-02-14 Daiichi Sankyo Company, Limited Pyridylmethylsulfone derivative
WO2006123182A2 (en) 2005-05-17 2006-11-23 Merck Sharp & Dohme Limited Cyclohexyl sulphones for treatment of cancer
GB0513747D0 (en) * 2005-07-06 2005-08-10 Merck Sharp & Dohme Therapeutic compounds
WO2007092435A2 (en) * 2006-02-07 2007-08-16 Wyeth 11-beta hsd1 inhibitors
US9567396B2 (en) 2006-03-07 2017-02-14 Evonik Degussa Gmbh Notch inhibition in the prevention of vein graft failure
WO2007103114A2 (en) 2006-03-07 2007-09-13 The Brigham & Women's Hospital, Inc. Notch inhibition in the treatment or prevention of atherosclerosis
CA2676715A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
WO2009008980A2 (en) * 2007-07-05 2009-01-15 Schering Corporation Tetrahydropyranochromene gamma secretase inhibitors
TW200920362A (en) 2007-09-11 2009-05-16 Daiichi Sankyo Co Ltd Alkylsulfone derivatives
KR101595238B1 (ko) 2007-12-21 2016-02-18 리간드 파마슈티칼스 인코포레이티드 선택적 안드로겐 수용체 조절제(ｓａｒｍ) 및 이의 용도
WO2009128057A2 (en) 2008-04-18 2009-10-22 UNIVERSITY COLLEGE DUBLIN, NATIONAL UNIVERSITY OF IRELAND, DUBLIN et al Psycho-pharmaceuticals
AU2009239555A1 (en) * 2008-04-23 2009-10-29 Merck Sharp & Dohme Corp. Cyclobutyl sulfones as Notch sparing gamma secretase inhibitors
US8609897B2 (en) * 2009-02-06 2013-12-17 Merck Sharp & Dohme Corp. Trifluoromethylsulfonamide gamma secretase inhibitor
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
US8859776B2 (en) 2009-10-14 2014-10-14 Merck Sharp & Dohme Corp. Substituted piperidines that increase p53 activity and the uses thereof
EP2493497A4 (en) 2009-11-01 2013-07-24 Brigham & Womens Hospital NOTCH INHIBITION IN THE TREATMENT AND PROPHYLAXIS OF ADIPOSITAS AND METABOLISM SYNDROME
US8999957B2 (en) 2010-06-24 2015-04-07 Merck Sharp & Dohme Corp. Heterocyclic compounds as ERK inhibitors
CA2805265A1 (en) 2010-08-02 2012-02-09 Merck Sharp & Dohme Corp. Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina)
WO2012024170A2 (en) 2010-08-17 2012-02-23 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF HEPATITIS B VIRUS (HBV) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
WO2012030685A2 (en) 2010-09-01 2012-03-08 Schering Corporation Indazole derivatives useful as erk inhibitors
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
WO2012058210A1 (en) 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACIDS (siNA)
EP2654748B1 (en) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
WO2013059302A1 (en) 2011-10-17 2013-04-25 Nationwide Children's Hospital, Inc. Products and methods for aortic abdominal aneurysm
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
WO2013165816A2 (en) 2012-05-02 2013-11-07 Merck Sharp & Dohme Corp. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
WO2014052563A2 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
ME02925B (me) 2012-11-28 2018-04-20 Merck Sharp & Dohme Kompozicije i postupci za liječenje kancera
TW201429969A (zh) 2012-12-20 2014-08-01 Merck Sharp & Dohme 作爲ｈｄｍ２抑制劑之經取代咪唑吡啶
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
WO2015103508A1 (en) * 2014-01-06 2015-07-09 Bristol-Myers Squibb Company CARBOCYCLIC SULFONE RORγ MODULATORS
WO2015103510A1 (en) * 2014-01-06 2015-07-09 Bristol-Myers Squibb Company Heterocyclic sulfone as ror-gamma modulators
WO2015103509A1 (en) * 2014-01-06 2015-07-09 Bristol-Myers Squibb Company Pyrrolidinyl sulfone derivatives and their use as ror gamma modulators
WO2015104343A1 (en) * 2014-01-09 2015-07-16 Proyecto De Biomedicina Cima, S.L. New antifibrinolytic compounds
EP3094323A4 (en) 2014-01-17 2017-10-11 Ligand Pharmaceuticals Incorporated Methods and compositions for modulating hormone levels
ES3057783T3 (en) 2016-03-15 2026-03-04 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of neoplastic diseases
US10975084B2 (en) 2016-10-12 2021-04-13 Merck Sharp & Dohme Corp. KDM5 inhibitors
EP3706747B1 (en) 2017-11-08 2025-09-03 Merck Sharp & Dohme LLC Prmt5 inhibitors
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
WO2020016377A1 (en) 2018-07-19 2020-01-23 INSERM (Institut National de la Santé et de la Recherche Médicale) Combination for treating cancer
WO2020033282A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3833669A4 (en) 2018-08-07 2022-05-11 Merck Sharp & Dohme Corp. PRMT5 INHIBITORS
WO2020033288A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
AU2020257397B2 (en) 2019-04-19 2026-02-26 Ligand Pharmaceuticals Inc. Crystalline forms and methods of producing crystalline forms of a compound
CN110143935B (zh) * 2019-06-03 2022-09-30 华侨大学 一种2，5-二取代呋喃衍生物的制备方法
JP7589247B2 (ja) 2019-12-17 2024-11-25 メルク・シャープ・アンド・ドーム・エルエルシー Ｐｒｍｔ５阻害剤
US12595248B2 (en) 2019-12-17 2026-04-07 Merck Sharp & Dohme Llc PRMT5 inhibitors
CN115003303B (zh) 2019-12-17 2024-03-08 默沙东公司 Prmt5抑制剂
EP4076460B1 (en) 2019-12-17 2026-01-21 Merck Sharp & Dohme LLC 1,4-dihydro-2h-spiro[isoquinoline-3,4'-piperidine derivatives as prmt5 inhibitors for the treatment of cancer
WO2022101481A1 (en) 2020-11-16 2022-05-19 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and compositions for predicting and treating uveal melanoma
EP4255409A1 (en) 2020-12-07 2023-10-11 Cellestia Biotech AG Pharmaceutical combinations for treating cancer
EP4008324A1 (en) 2020-12-07 2022-06-08 Cellestia Biotech AG Combinations comprising an inhibitor of an anti-apoptotic protein, such as bcl-2, bcl-xl, bclw or mcl-1, and a notch signaling pathway inhibitor for treating cancer
US20240269120A1 (en) 2021-06-02 2024-08-15 Cellestia Biotech Ag Method for Treating an Autoimmune and Inflammatory Disease
WO2023079132A1 (en) 2021-11-08 2023-05-11 Cellestia Biotech Ag Pharmaceutical combinations for treating cancer
EP4223292A1 (en) 2022-02-07 2023-08-09 Cellestia Biotech AG Pharmaceutical combinations for treating cancer
JP2025511436A (ja) 2022-09-02 2025-04-16 メルク・シャープ・アンド・ドーム・エルエルシー エキサテカン由来トポイソメラーゼ－１阻害薬医薬組成物及びその使用
CN120417935A (zh) 2022-10-25 2025-08-01 默沙东有限责任公司 依喜替康衍生的adc接头-载荷及其药物组合物和用途
US20240207425A1 (en) 2022-12-14 2024-06-27 Merck Sharp & Dohme Llc Auristatin linker-payloads, pharmaceutical compositions, and uses thereof

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE735866C (de) * 1941-01-17 1943-06-11 Ig Farbenindustrie Ag Verfahren zur Darstellung von Aminoalkylsulfonverbindungen
US2802013A (en) * 1954-02-12 1957-08-06 Searle & Co 2-(oxo and imino)-3-(phenyl and halophenyl)-tetrahydrofuransulfones and processes for the manufacture thereof
US2813100A (en) * 1955-04-26 1957-11-12 Nopco Chem Co Hydrogenation process
US2812330A (en) * 1956-05-02 1957-11-05 Searle & Co Sulfone derivatives of 2, 6-piperidinedione
JPS5625149A (en) * 1979-08-08 1981-03-10 Sagami Chem Res Center Keto ester derivative and its preparation
JPS5626847A (en) 1979-08-13 1981-03-16 Sagami Chem Res Center Preparation of substituted salicylic acid derivative
JPS5626866A (en) 1979-08-13 1981-03-16 Sagami Chem Res Center Unsaturated ketoester derivative and its preparation
JPH06157508A (ja) * 1992-11-26 1994-06-03 Nippon Oil & Fats Co Ltd 新規１，３−ジチオラン誘導体、１，３−ジオキソラン誘導体及び反応性組成物
US5703129A (en) * 1996-09-30 1997-12-30 Bristol-Myers Squibb Company 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives as inhibitors of β-amyloid protein production
EP0863134A1 (en) * 1997-03-07 1998-09-09 Merck Frosst Canada Inc. 2-(3,5-difluorophenyl)-3-(4-(methyl-sulfonyl)phenyl)-2-cyclopenten-1-one useful as an inhibitor of cyclooxygenase-2
WO2000050391A1 (en) 1999-02-26 2000-08-31 Merck & Co., Inc. Novel sulfonamide compounds and uses thereof
GB0108592D0 (en) 2001-04-05 2001-05-23 Merck Sharp & Dohme Therapeutic agents
GB0108591D0 (en) 2001-04-05 2001-05-23 Merck Sharp & Dohme Therapeutic agents
GB0120347D0 (en) * 2001-08-21 2001-10-17 Merck Sharp & Dohme Therapeutic agents
CN100562516C (zh) 2001-12-27 2009-11-25 第一制药株式会社 β-淀粉样蛋白产生和分泌的抑制剂
DE10201392A1 (de) 2002-01-16 2003-07-31 Bayer Ag Phenylsulfoxide und-sulfone
GB0218041D0 (en) 2002-08-02 2002-09-11 Merck Sharp & Dohme Chemical process
GB0223038D0 (en) 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
GB0223039D0 (en) * 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
GB0223040D0 (en) 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
DE10254875A1 (de) 2002-11-25 2004-06-03 Bayer Healthcare Ag Phenylsulfoxid und -sulfon-Derivate
GB0304524D0 (en) * 2003-02-27 2003-04-02 Merck Sharp & Dohme Therapeutic agents
EP1638951B1 (en) 2003-05-16 2008-02-13 MERCK SHARP & DOHME LTD. Cyclohexyl sulphones as gamma-secretase inhibitors
CA2526487A1 (en) 2003-06-30 2005-01-06 Daiichi Pharmaceutical Co., Ltd. Heterocyclic methyl sulfone derivative
GB0323258D0 (en) * 2003-10-04 2003-11-05 Merck Sharp & Dohme Therapeutic compounds

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JP2004533428A (ja) 2004-11-04
US20090131419A1 (en) 2009-05-21
CA2442882C (en) 2010-02-16
US7595344B2 (en) 2009-09-29
US7598386B2 (en) 2009-10-06
AU2001279971B2 (en) 2007-07-12
ATE498608T1 (de) 2011-03-15
WO2002081435A1 (en) 2002-10-17
US20070213329A1 (en) 2007-09-13
CA2442882A1 (en) 2002-10-17
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