AU2003280380A1 - Sustituted piperazines, (1,4) diaszepines, and 2,5-diazabicyclo (2.2.1) heptanes as histamine H1 and/or H3 antagonists or histamine H3 reverse antagonists - Google Patents

Sustituted piperazines, (1,4) diaszepines, and 2,5-diazabicyclo (2.2.1) heptanes as histamine H1 and/or H3 antagonists or histamine H3 reverse antagonists Download PDF

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Publication number
AU2003280380A1
AU2003280380A1 AU2003280380A AU2003280380A AU2003280380A1 AU 2003280380 A1 AU2003280380 A1 AU 2003280380A1 AU 2003280380 A AU2003280380 A AU 2003280380A AU 2003280380 A AU2003280380 A AU 2003280380A AU 2003280380 A1 AU2003280380 A1 AU 2003280380A1
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Australia
Prior art keywords
phenyl
oxy
piperidinyl
alkyl
piperazine
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Abandoned
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AU2003280380A
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English (en)
Inventor
Rachael Ancliff
Colin David Eldred
Yvonne C Fogden
Ashley Paul Hancock
Thomas Daniel Heightman
Heather Hobbs
Simon Teanby Hodgson
Matthew J Lindon
David Matthew Wilson
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Glaxo Group Ltd
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Glaxo Group Ltd
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Publication of AU2003280380A1 publication Critical patent/AU2003280380A1/en
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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AU2003280380A 2002-10-16 2003-10-14 Sustituted piperazines, (1,4) diaszepines, and 2,5-diazabicyclo (2.2.1) heptanes as histamine H1 and/or H3 antagonists or histamine H3 reverse antagonists Abandoned AU2003280380A1 (en)

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Families Citing this family (108)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7842693B2 (en) 2002-06-12 2010-11-30 Chemocentryx, Inc. Substituted piperazines
US20050256130A1 (en) * 2002-06-12 2005-11-17 Chemocentryx, Inc. Substituted piperazines
US7589199B2 (en) 2002-06-12 2009-09-15 Chemocentryx, Inc. Substituted piperazines
GB0224084D0 (en) * 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
GB0224557D0 (en) 2002-10-22 2002-11-27 Glaxo Group Ltd Novel compounds
US20070293216A1 (en) * 2003-02-14 2007-12-20 Roamware Inc. Method and system for providing PLN service to inbound roamers in a VPMN using a standalone approach when no roaming relationship exists between HPMN and VPMN
CA2521000A1 (en) * 2003-04-03 2004-10-21 Kyowa Hakko Kogyo Co., Ltd. Preventive and/or therapeutic agent for neuropathic pain
US20060293298A1 (en) * 2003-04-10 2006-12-28 Bamford Mark J Compounds
GB0316915D0 (en) 2003-07-18 2003-08-20 Glaxo Group Ltd Compounds
GB0324159D0 (en) 2003-10-15 2003-11-19 Glaxo Group Ltd Novel compounds
CN1972914A (zh) * 2004-03-31 2007-05-30 詹森药业有限公司 作为组胺h3受体配合体的非咪唑杂环化合物
US7253168B2 (en) 2004-04-07 2007-08-07 Neurogen Corporation Substituted 1-benzyl-4-substituted piperazine analogues
AU2005240991A1 (en) * 2004-04-15 2005-11-17 Georgetown University Use of (4-alkylpiperazinyl) (phenyl) methanones in the treatment of Alzheimer's disease
US7632831B2 (en) * 2004-05-07 2009-12-15 Memory Pharmaceuticals Corporation 1H-indazoles, benzothiazoles, 1,2-benzoisoxazoles, 1,2-benzoisothiazoles, and chromones and preparation and uses thereof
US8158652B2 (en) * 2004-12-01 2012-04-17 Msd K.K. Substituted pyridone derivative
WO2006090142A1 (en) * 2005-02-24 2006-08-31 Glaxo Group Limited l-{4- [ (l-CYCLOBUTYL-4-PIPERIDINYL) OXY] PHENYL] -4-{ [4- (METHYLSULFONYL) PHENYL]CARBONYL PIPERAZINE AS HISTAMINE H3 ANTAGONIST
PT1861360E (pt) * 2005-03-17 2010-01-28 Lilly Co Eli Derivados de pirrolidina como antagonistas de receptores h3 de histamina
EP1717235A3 (en) * 2005-04-29 2007-02-28 Bioprojet Phenoxypropylpiperidines and -pyrrolidines and their use as histamine H3-receptor ligands
CN101228127B (zh) * 2005-05-30 2012-05-16 Msdk.K.公司 哌啶衍生物
ES2574014T3 (es) * 2005-05-30 2016-06-14 Msd K.K. Derivado de piperidina novedoso
GB0514812D0 (en) * 2005-07-19 2005-08-24 Glaxo Group Ltd Compounds
GB0514811D0 (en) * 2005-07-19 2005-08-24 Glaxo Group Ltd Compounds
GB0521563D0 (en) 2005-10-21 2005-11-30 Glaxo Group Ltd Novel compounds
CA2627234A1 (en) 2005-10-27 2007-05-03 Ucb Pharma, S.A. Compounds comprising a lactam or a lactam derivative moiety, processes for making them, and their uses
ATE485294T1 (de) * 2005-11-18 2010-11-15 Hoffmann La Roche Azaindol-2-carboxamid-derivate
EP1968967B1 (en) * 2005-11-30 2011-04-27 F. Hoffmann-La Roche AG 1,1-dioxo-thiomorpholinyl indolyl methanone derivatives for use as h3 modulators
AU2006319234B2 (en) * 2005-11-30 2012-01-19 F. Hoffmann-La Roche Ag 1,5-substituted indol-2-yl amide derivatives
JP2009519293A (ja) * 2005-12-16 2009-05-14 エフ．ホフマン−ラ ロシュ アーゲー Ｈ３レセプター調節剤としてのピロロ［２，３−ｂ］ピリジン誘導体
PE20071068A1 (es) * 2005-12-20 2007-12-13 Glaxo Group Ltd Acido 3-(4-{[4-(4-{[3-(3,3-dimetil-1-piperidinil)propil]oxi}fenil)-1-piperidinil]carbonil}-1-naftalenil)propanoico o propenoico, sales de los mismos, como antagonistas de los receptores h1 y h3
KR20090007604A (ko) * 2006-04-20 2009-01-19 글락소 그룹 리미티드 히스타민 ｈ１ 및 ｈ３ 길항제로서의 2―치환된 4―벤질프탈라지논 유도체
AR060536A1 (es) 2006-04-20 2008-06-25 Glaxo Group Ltd Agonista del receptor de glucocorticoides y composiciones farmaceuticas
GB0609897D0 (en) * 2006-05-18 2006-06-28 Glaxo Group Ltd Compounds
EA015555B1 (ru) 2006-05-30 2011-08-30 Янссен Фармацевтика Н.В. Замещенные пиридиламидные соединения в качестве модуляторов гистаминового h-рецептора
GB0611587D0 (en) 2006-06-12 2006-07-19 Glaxo Group Ltd Novel compounds
BRPI0712823A2 (pt) 2006-06-23 2012-07-24 Abbott Lab derivados de ciclopropil amina como moduladores de receptor de histamina h3
US9108948B2 (en) 2006-06-23 2015-08-18 Abbvie Inc. Cyclopropyl amine derivatives
EP2038269A1 (en) * 2006-06-29 2009-03-25 Janssen Pharmaceutica N.V. Substituted benzamide modulators of the histamine h3 receptor
KR101007469B1 (ko) 2006-12-22 2011-01-12 성균관대학교산학협력단 사스 코로나 바이러스의 ｒｎａ 유사매듭구조에 결합하여 리보솜 틀 이동을 억제하는 호모피페라진계 화합물
PE20081889A1 (es) 2007-03-23 2009-03-05 Smithkline Beecham Corp Indol carboxamidas como inhibidores de ikk2
CL2008002622A1 (es) 2007-09-06 2009-11-27 Glaxo Group Ltd 1-(1-metiletil)-4-{[4-(tetrahidro-2h-piran-4-iloxi)fenil]carbonil}piperazina y su sal hidrocloruro; formas cristalinas de la sal; proceso de preparacion; composicion farmaceutica; y uso para el tratamiento o profilaxis de deterioro cognitivo, fatiga o trastorno del sueno.
CA2697551C (en) 2007-09-20 2013-03-12 Irm Llc Piperidine derivatives as modulators of gpr119 activity
US8883776B2 (en) 2007-11-20 2014-11-11 Janssen Pharmaceutica N.V. Cycloalkyloxy- and heterocycloalkyloxypyridine compounds as modulators of the histamine H3 receptor
CA2720950A1 (en) * 2008-04-07 2009-10-15 Irm Llc Compounds and compositions as modulators of gpr119 activity
US20110160249A1 (en) 2008-05-23 2011-06-30 Schaab Kevin Murray 5-lipoxygenase-activating protein inhibitor
JP5502858B2 (ja) 2008-06-05 2014-05-28 グラクソ グループ リミテッド Ｐｉ３キナーゼの阻害剤として有用な４−カルボキサミドインダゾール誘導体
WO2010094643A1 (en) 2009-02-17 2010-08-26 Glaxo Group Limited Quinoline derivatives and their uses for rhinitis and urticaria
ES2542551T3 (es) 2009-03-09 2015-08-06 Glaxo Group Limited 4-Oxadiazol-2-il-indazoles como inhibidores de PI3 cinasas
JP2012520257A (ja) 2009-03-10 2012-09-06 グラクソ グループ リミテッド Ｉｋｋ２阻害剤としてのインドール誘導体
JP2012520845A (ja) 2009-03-17 2012-09-10 グラクソ グループ リミテッド Ｉｔｋ阻害剤として使用されるピリミジン誘導体
JP2012520685A (ja) 2009-03-19 2012-09-10 メルク・シャープ・エンド・ドーム・コーポレイション 低分子干渉核酸（ｓｉＮＡ）を用いたＧＡＴＡ結合タンパク質３（ＧＡＴＡ３）遺伝子発現のＲＮＡ干渉媒介性阻害
JP2012520686A (ja) 2009-03-19 2012-09-10 メルク・シャープ・エンド・ドーム・コーポレイション 低分子干渉核酸（ｓｉＮＡ）を用いたシグナル伝達性転写因子６（ＳＴＡＴ６）遺伝子発現のＲＮＡ干渉媒介性阻害
CA2755773A1 (en) 2009-03-19 2010-09-23 Merck Sharp & Dohme Corp. Rna interference mediated inhibition of btb and cnc homology 1, basic leucine zipper transcription factor 1 (bach 1) gene expression using short interfering nucleic acid (sina)
WO2010107952A2 (en) 2009-03-19 2010-09-23 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF CONNECTIVE TISSUE GROWTH FACTOR (CTGF) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
JP2012521763A (ja) 2009-03-27 2012-09-20 メルク・シャープ・エンド・ドーム・コーポレイション 低分子干渉核酸（ｓｉＮＡ）を用いたシグナル伝達性転写因子１（ＳＴＡＴ１）遺伝子発現のＲＮＡ干渉媒介性阻害
JP2012521764A (ja) 2009-03-27 2012-09-20 メルク・シャープ・エンド・ドーム・コーポレイション 低分子干渉核酸（ｓｉＮＡ）を用いた胸腺間質性リンパ球新生因子（ＴＳＬＰ）遺伝子発現のＲＮＡ干渉媒介性阻害
US20120004281A1 (en) 2009-03-27 2012-01-05 Merck Sharp & Dohme Corp RNA Interference Mediated Inhibition of the Nerve Growth Factor Beta Chain (NGFB) Gene Expression Using Short Interfering Nucleic Acid (siNA)
UY32571A (es) 2009-04-24 2010-11-30 Glaxo Group Ltd Compuestos derivados de pirazol amida
EP2421834A1 (en) 2009-04-24 2012-02-29 Glaxo Group Limited Pyrazole and triazole carboxamides as crac channel inhibitors
US9186353B2 (en) 2009-04-27 2015-11-17 Abbvie Inc. Treatment of osteoarthritis pain
TWI516487B (zh) 2009-04-30 2016-01-11 葛蘭素集團有限公司 新穎化合物、其醫藥組合物及作為激酶活性抑制劑之用途
WO2011002984A1 (en) 2009-07-02 2011-01-06 Cephalon, Inc. Substituted phenoxypropylcycloamine derivatives as histamine-3 (h3) receptor ligands
CA2774573A1 (en) * 2009-10-09 2011-04-14 Irm Llc Compounds and compositions as modulators of gpr119 activity
WO2011067366A1 (en) 2009-12-03 2011-06-09 Glaxo Group Limited Indazole derivatives as pi 3 - kinase inhibitors
US20120245171A1 (en) 2009-12-03 2012-09-27 Glaxo Group Limited Benzpyrazole derivatives as inhibitors of pi3 kinases
EP2507226A1 (en) 2009-12-03 2012-10-10 Glaxo Group Limited Novel compounds
WO2011110575A1 (en) 2010-03-11 2011-09-15 Glaxo Group Limited Derivatives of 2-[2-(benzo- or pyrido-) thiazolylamino]-6-aminopyridine, useful in the treatment of respiratoric, allergic or inflammatory diseases
GB201007203D0 (en) 2010-04-29 2010-06-16 Glaxo Group Ltd Novel compounds
WO2012025474A1 (en) 2010-08-24 2012-03-01 Glaxo Group Limited Indazole compounds
WO2012025473A1 (en) 2010-08-24 2012-03-01 Glaxo Group Limited Cc.chemokine receptor 4 antagonists
WO2012031383A1 (zh) * 2010-09-06 2012-03-15 中国科学院广州生物医药与健康研究院 酰胺类化合物
PL2614058T3 (pl) 2010-09-08 2015-12-31 Glaxosmithkline Ip Dev Ltd Polimorfy i sole n-[5-[4-(5-{[(2r,6s)-2,6-dimetylo-4-morfolinylo]-metylo}-1,3-oksazol-2-ilo)-1h-indazol-6-ilo]-2-(metyloksy)-3-pirydynylo]metanosulfonamidu
US8853390B2 (en) 2010-09-16 2014-10-07 Abbvie Inc. Processes for preparing 1,2-substituted cyclopropyl derivatives
WO2012035055A1 (en) 2010-09-17 2012-03-22 Glaxo Group Limited Novel compounds
US9149462B2 (en) 2010-10-21 2015-10-06 Glaxo Group Limited Pyrazole compounds acting against allergic, inflammatory and immune disorders
WO2012052458A1 (en) 2010-10-21 2012-04-26 Glaxo Group Limited Pyrazole compounds acting against allergic, immune and inflammatory conditions
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
JP2014507458A (ja) 2011-03-11 2014-03-27 グラクソ グループ リミテッド Ｓｙｋインヒビターとしてのピリド［３，４−Ｂ］ピラジン誘導体
GB201104153D0 (en) 2011-03-11 2011-04-27 Glaxo Group Ltd Novel compounds
WO2012173952A1 (en) 2011-06-13 2012-12-20 Emory University Piperazine derivatives, compositions, and uses related thereto
WO2013151982A1 (en) 2012-04-03 2013-10-10 Arena Pharmaceuticals, Inc. Methods and compounds useful in treating pruritus, and methods for identifying such compounds
WO2015042078A2 (en) 2013-09-22 2015-03-26 Calitor Sciences, Llc Substituted aminopyrimidine compounds and methods of use
US9233953B2 (en) * 2013-10-16 2016-01-12 Boehringer Ingelheim International Gmbh Derivatives of 4-(piperazinylcarbonyl)thiane-1, 1-dione which inhibit GlyT1
CA2925064A1 (en) 2013-10-17 2015-04-23 Glaxosmithkline Intellectual Property Development Limited Pi3k inhibitor for treatment of respiratory disease
CA2923995A1 (en) 2013-10-17 2015-04-23 Glaxosmithkline Intellectual Property Development Limited Pi3k inhibitor for treatment of respiratory disease
WO2015069110A1 (en) * 2013-11-07 2015-05-14 Aapa B.V. Multiple d2 a(nta)gonists/h3 antagonists for treatment of cns-related disorders
JP6517318B2 (ja) 2014-03-28 2019-05-22 キャリター・サイエンシーズ・リミテッド・ライアビリティ・カンパニーＣａｌｉｔｏｒ Ｓｃｉｅｎｃｅｓ， Ｌｌｃ 置換されたヘテロアリール化合物および使用方法
WO2015173701A2 (en) 2014-05-12 2015-11-19 Glaxosmithkline Intellectual Property (No. 2) Limited Pharmaceutical compositions for treating infectious diseases
EP3347097B1 (en) 2015-09-11 2021-02-24 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine derivatives as modulators of the kinases jak, flt3 and aurora
GB201602527D0 (en) 2016-02-12 2016-03-30 Glaxosmithkline Ip Dev Ltd Chemical compounds
US20190161480A1 (en) 2016-08-08 2019-05-30 Glaxosmithkline Intellectual Property Development Limited Chemical Compounds
AU2017311691B2 (en) 2016-08-18 2021-12-02 Vidac Pharma Ltd. Piperazine derivatives, pharmaceutical compositions and methods of use thereof
GB201706102D0 (en) 2017-04-18 2017-05-31 Glaxosmithkline Ip Dev Ltd Chemical compounds
CN109232549B (zh) * 2017-07-11 2022-07-12 江苏恩华药业股份有限公司 一种治疗精神分裂症的化合物及其应用
GB201712081D0 (en) 2017-07-27 2017-09-13 Glaxosmithkline Ip Dev Ltd Chemical compounds
WO2019099311A1 (en) 2017-11-19 2019-05-23 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
AU2019209960B2 (en) 2018-01-20 2023-11-23 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine compounds and methods of use
US11318144B2 (en) 2019-04-12 2022-05-03 LA PharmaTech Inc. Compositions and methods for treating Alzheimer's disease and Parkinson's disease
US10639314B1 (en) 2019-04-30 2020-05-05 LA PharmaTech Inc. Method of treating Alzheimer's disease
US10639315B1 (en) 2019-05-21 2020-05-05 LA PharmaTech Inc. Pharmaceutical compositions and methods for treating Alzheimer's disease
US11690849B2 (en) 2019-04-12 2023-07-04 LA PharmaTech Inc. Method of treating dementia
US10966989B2 (en) 2019-04-12 2021-04-06 LA PharmaTech Inc. Pharmaceutical compositions and methods for treating mental, behavioral, cognitive disorders
US11389458B2 (en) 2019-04-12 2022-07-19 LA PharmaTech Inc. Pharmaceutical compositions and methods for treating parkinson's and huntington's disease
US10898493B2 (en) 2019-04-12 2021-01-26 LA PharmaTech Inc. Pharmaceutical compositions and methods for psychiatric symptoms of patients with Alzheimer's disease
US11744833B2 (en) 2019-04-12 2023-09-05 LA PharmaTech Inc. Pharmaceutical compositions and methods for treatment of insomnia
US11938139B2 (en) 2019-04-12 2024-03-26 LA PharmaTech Inc. Pharmaceutical compositions and methods for anxiety, depression and other psychiatric disorders
CA3137393A1 (en) * 2019-04-30 2020-11-05 Jianmin Wang A method of treating mental, behavioral, cognitive disorders
CN116194114A (zh) 2020-03-26 2023-05-30 葛兰素史密斯克莱知识产权发展有限公司 用于防止或治疗病毒感染的组织蛋白酶抑制剂
US11351179B1 (en) 2021-08-05 2022-06-07 LA PharmaTech Inc. Pharmaceutical compositions and methods for treatment of psychiatric disorders

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2401254A1 (de) 1974-01-11 1975-11-27 Boehringer Mannheim Gmbh Neue derivate von n hoch 6-substituierten adeninen
IL61897A (en) 1980-01-19 1984-01-31 Beecham Group Ltd Benzopyrano(2,3-d)-v-triazoles,their production and pharmaceutical compositions containing them
EP0745121B1 (en) 1992-05-14 2007-06-20 Baylor College Of Medicine Mutated steroid hormone receptors, methods for their use and molecular switch for gene therapy
US5364791A (en) 1992-05-14 1994-11-15 Elisabetta Vegeto Progesterone receptor having C. terminal hormone binding domain truncations
DE4410822A1 (de) 1994-03-24 1995-09-28 Schering Ag Neue Piperidin-Derivate
US5464788A (en) 1994-03-24 1995-11-07 Merck & Co., Inc. Tocolytic oxytocin receptor antagonists
USH2007H1 (en) 1996-01-19 2001-12-04 Fmc Corporation Insecticidal N-heterocyclylalkyl-or N-[(polycyclyl)alkyl]-N′substituted piperazines
US5880128A (en) 1996-05-08 1999-03-09 Schering Corporation Carbonyl piperazinyl and piperidinyl compounds
WO1999041242A1 (fr) 1998-02-13 1999-08-19 Rhone-Poulenc Rorer S.A. Derives de naphtyl disubstitues, leur preparation, les compositions pharmaceutiques qui les contiennent
US6620839B2 (en) * 2000-07-13 2003-09-16 Abbott Laboratories 1,3-disubstituted and 1,3,3-trisubstituted pyrrolidines as histamine-3 receptor ligands and their therapeutic applications
PT1301480E (pt) * 2000-07-13 2007-11-29 Abbott Lab Pirrolidinas 1,3-di-substituídas e 1,3,3-tri-substituídas úteis como ligandos do receptor de histamina-3 e suas aplicações terapêuticas
JP2004504300A (ja) 2000-07-18 2004-02-12 ビーエーエスエフ　アクチェンゲゼルシャフト １−アリール−４−ハロアルキル−２−［１ｈ］ピリドン類
HUP0302893A3 (en) * 2000-08-08 2006-04-28 Ortho Mcneil Pharm Inc Non-imidazole aryloxypiperidines and pharmaceutical compositions containing them and their use
DK1313721T3 (da) * 2000-08-08 2006-06-26 Ortho Mcneil Pharm Inc Ikke-imidazol-aryloxyalkylaminer som H3-receptorligander
JP2002173426A (ja) 2000-12-05 2002-06-21 Ss Pharmaceut Co Ltd 血糖低下剤
JP2004520347A (ja) 2001-01-15 2004-07-08 グラクソ　グループ　リミテッド Ｌｄｌ−受容体発現のインデューサーとしてのアリールピペリジンおよびピペラジン誘導体
WO2002076925A2 (en) * 2001-03-23 2002-10-03 Eli Lilly And Company Non-imidazole aryl alkylamines compounds as histamine h3 receptor antagonists, preparation and therapeutic uses
JP4186518B2 (ja) * 2001-06-15 2008-11-26 アステラス製薬株式会社 フェニルピリジン誘導体
US7459461B2 (en) 2001-10-19 2008-12-02 Ortho-Mcneil Pharmaceutical, Inc. Phosphonic acid compounds as inhibitors of serine proteases
AU2003203148A1 (en) * 2002-02-05 2003-09-02 High Point Pharmaceuticals, Llc Novel aryl- and heteroarylpiperazines
US20060019964A1 (en) 2002-10-16 2006-01-26 Ancliff Ranchael A Compounds
GB0224084D0 (en) * 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
GB0609897D0 (en) * 2006-05-18 2006-06-28 Glaxo Group Ltd Compounds

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CA2502249A1 (en) 2004-04-29
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NO20051689L (no) 2005-07-07
US7615550B2 (en) 2009-11-10
WO2004035556A1 (en) 2004-04-29
RU2005110061A (ru) 2006-01-20
CN100400523C (zh) 2008-07-09
JP2006508935A (ja) 2006-03-16
EP1567511A1 (en) 2005-08-31
IS7782A (is) 2005-03-31
CN101070309A (zh) 2007-11-14
NZ539446A (en) 2006-11-30
ZA200502873B (en) 2006-07-26
JP2007016041A (ja) 2007-01-25
PL376477A1 (en) 2005-12-27
US20100075953A1 (en) 2010-03-25
GB0224084D0 (en) 2002-11-27
MA27482A1 (fr) 2005-08-01
RU2328494C2 (ru) 2008-07-10
KR20050049553A (ko) 2005-05-25
US20060025404A1 (en) 2006-02-02
BR0315283A (pt) 2005-08-30
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MXPA05004078A (es) 2005-06-08
CN1726201A (zh) 2006-01-25

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