CN103096893B - 甘氨酸转运体-1抑制剂、其制备方法及其用途 - Google Patents

甘氨酸转运体-1抑制剂、其制备方法及其用途 Download PDF

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CN103096893B
CN103096893B CN201180038081.9A CN201180038081A CN103096893B CN 103096893 B CN103096893 B CN 103096893B CN 201180038081 A CN201180038081 A CN 201180038081A CN 103096893 B CN103096893 B CN 103096893B
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methyl
piperazin
cyclohexyl
benzamide
difluoro
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CN103096893A (zh
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C·L·西奥菲
M·A·伍尔夫
P·R·古佐
S·刘
K·萨达拉普里
V·帕塔萨拉蒂
孟俊浩
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Curia Global Inc
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Albany Molecular Research Inc
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CN201180038081.9A 2010-06-04 2011-06-02 甘氨酸转运体-1抑制剂、其制备方法及其用途 Active CN103096893B (zh)

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US35166210P 2010-06-04 2010-06-04
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PCT/US2011/038939 WO2011153359A1 (en) 2010-06-04 2011-06-02 Glycine transporter-1 inhibitors, methods of making them, and uses thereof

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AU2009303335B2 (en) * 2008-10-09 2016-05-19 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Activators of human pyruvate kinase
WO2010118063A2 (en) 2009-04-06 2010-10-14 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
WO2010129596A1 (en) 2009-05-04 2010-11-11 Agios Pharmaceuticals, Inc. Pmk2 modulators for use in the treatment of cancer
RU2561132C2 (ru) 2009-06-29 2015-08-20 Аджиос Фармасьютикалз, Инк. Производные хинолинсульфонамидов и их применение для модулирования пкм2 активности
ES2618630T3 (es) 2009-06-29 2017-06-21 Agios Pharmaceuticals, Inc. Composiciones terapéuticas y métodos de uso relacionados
US20130109672A1 (en) 2010-04-29 2013-05-02 The United States Of America,As Represented By The Secretary, Department Of Health And Human Service Activators of human pyruvate kinase
AU2011261375B2 (en) 2010-06-04 2016-09-22 Albany Molecular Research, Inc. Glycine transporter-1 inhibitors, methods of making them, and uses thereof
CA2821975A1 (en) 2010-12-17 2012-06-21 Shunqi Yan N-(4-(azetidine-1-carbonyl)phenyl)-(hetero-) arylsulfonamide derivatives as pyruvate kinase m2 pkm2 modulators
WO2012088314A1 (en) 2010-12-21 2012-06-28 Agios Pharmaceuticals, Inc. Bicyclic pkm2 activators
TWI549947B (zh) 2010-12-29 2016-09-21 阿吉歐斯製藥公司 治療化合物及組成物
SG194697A1 (en) 2011-05-03 2013-12-30 Agios Pharmaceuticals Inc Pyruvate kinase activators for use in therapy
CN103254127B (zh) * 2013-05-28 2015-08-19 北京哈三联科技有限责任公司 甘氨酸重摄取抑制剂及其应用
FI3307271T3 (fi) 2015-06-11 2023-10-17 Agios Pharmaceuticals Inc Pyruvaattikinaasin aktivaattorien käyttämisen menetelmä
KR20180012853A (ko) 2015-06-16 2018-02-06 지앙수 헨그루이 메디슨 컴퍼니 리미티드 피페리딘 유도체 및 이의 제조 방법 및 약학적 용도

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070043027A1 (en) * 2003-09-12 2007-02-22 Applied Reserach Systems Ars Holding N.V. Sulfonamide derivatives for the treatment of diabetes
CN101479243A (zh) * 2006-06-28 2009-07-08 安姆根有限公司 甘氨酸转运子-1抑制剂
US20090269278A1 (en) * 2005-09-29 2009-10-29 Burns H Donald Radiolabeled Glycine Trasporter Inhibitors

Family Cites Families (183)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3145209A (en) 1961-07-31 1964-08-18 Olin Mathieson Substituted aminophenyl-ethylamine derivatives
US3975443A (en) 1972-06-06 1976-08-17 Allen & Hanburys Limited 1-(3,4-dichlorobenzamidomethyl)-cyclohexyldimethylamine
DE3718317A1 (de) 1986-12-10 1988-06-16 Bayer Ag Substituierte basische 2-aminotetraline
US5032604A (en) 1989-12-08 1991-07-16 Merck & Co., Inc. Class III antiarrhythmic agents
DE4302051A1 (de) 1993-01-26 1994-07-28 Thomae Gmbh Dr K 5-gliedrige Heterocyclen, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
ATE166650T1 (de) 1993-03-04 1998-06-15 Pfizer Spiroazacyclischderivate als substanz p antagonisten
ATE216580T1 (de) 1993-07-16 2002-05-15 Merck & Co Inc Benzoxazinon- und benzopyrimidinon- piperidinyl- verbindungen als tokolytische oxytocin-rezeptor- antagonisten
US5464788A (en) 1994-03-24 1995-11-07 Merck & Co., Inc. Tocolytic oxytocin receptor antagonists
RU2149872C1 (ru) 1994-07-20 2000-05-27 Бык Гульден Ломберг Хемише Фабрик Гмбх Пиридилтиосоединения для борьбы с бактериями helicobacter
FR2731222A1 (fr) 1995-03-02 1996-09-06 Pf Medicament Nouveaux derives de piperazine aminoindoles cycliques, leur procede de preparation et leur utilisation a titre de medicaments
US5856326A (en) 1995-03-29 1999-01-05 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5939418A (en) 1995-12-21 1999-08-17 The Dupont Merck Pharmaceutical Company Isoxazoline, isothiazoline and pyrazoline factor Xa inhibitors
DE19548624A1 (de) 1995-12-23 1997-06-26 Boehringer Mannheim Gmbh Neue Barbitursäure-Derivate, Verfahren zu deren Herstellung und diese Verbindungen enthaltende Arzneimittel
US6333322B1 (en) 1996-03-13 2001-12-25 Eisai Co., Ltd. Nitrogen-containing tricyclic compounds and drugs containing the same
US5885995A (en) 1996-04-03 1999-03-23 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
CA2250587A1 (en) 1996-04-03 1997-10-09 Christopher J. Dinsmore Inhibitors of farnesyl-protein transferase
US5919785A (en) 1996-04-03 1999-07-06 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5859012A (en) 1996-04-03 1999-01-12 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP0904080A4 (en) 1996-04-03 2001-08-01 Merck & Co Inc INHIBITORS OF FARNESYL PROTEIN TRANSFERASE
DE19700431A1 (de) 1997-01-10 1998-07-16 Basf Ag Reaktivfarbstoffe mit einem Disulfonylanker
US6060038A (en) 1997-05-15 2000-05-09 Merck & Co., Inc. Radiolabeled farnesyl-protein transferase inhibitors
WO1999040075A1 (en) 1998-02-05 1999-08-12 Takeda Chemical Industries, Ltd. Sulfonamide derivatives, process for producing the same and utilization thereof
GB9806287D0 (en) 1998-03-24 1998-05-20 Synphar Lab Inc Monobactam enzyme inhibitors
TWI220143B (en) 1998-05-13 2004-08-11 Solvay Pharm Gmbh Method for stereochemically controlled production of isomerically pure highly substituted azacyclic compounds and novel cyclic compounds, and intermediate products
CA2332239A1 (en) 1998-05-15 1999-11-25 Guilford Pharmaceuticals Inc. Fused tricyclic compounds which inhibit parp activity
US6380193B1 (en) 1998-05-15 2002-04-30 Guilford Pharmaceuticals Inc. Fused tricyclic compounds, methods and compositions for inhibiting PARP activity
US6509338B1 (en) 1998-06-22 2003-01-21 Bristol-Myers Squibb Company Pyrazolo[1,5-A]triazine corticotropin releasing factor antagonists
US6632836B1 (en) 1998-10-30 2003-10-14 Merck & Co., Inc. Carbocyclic potassium channel inhibitors
WO2000042852A1 (en) 1999-01-25 2000-07-27 Smithkline Beecham Corporation Compounds and methods
CA2363169A1 (en) 1999-03-03 2000-09-08 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
US6355643B1 (en) 1999-03-03 2002-03-12 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
CA2362493A1 (en) 1999-03-03 2000-09-08 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
WO2000051614A1 (en) 1999-03-03 2000-09-08 Merck & Co., Inc. Inhibitors of prenyl-protein transferases
CA2362778A1 (en) 1999-03-03 2000-09-08 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
DE19911509A1 (de) 1999-03-15 2000-09-21 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE19911510A1 (de) 1999-03-15 2000-09-21 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
AU5464200A (en) 1999-06-09 2000-12-28 Merck & Co., Inc. Biaryl inhibitors of prenyl-protein transferase
US6642228B1 (en) 1999-06-24 2003-11-04 Toray Industries, Inc. α1b-adrenergic receptor antagonists
WO2001014331A2 (en) 1999-08-24 2001-03-01 Regents Of The University Of California Non-quinoline inhibitors of malaria parasites
DE19944066A1 (de) 1999-09-14 2001-03-15 Byk Gulden Lomberg Chem Fab Inhibitoren der Tryptase
WO2001022963A1 (en) 1999-09-27 2001-04-05 Merck & Co., Inc. Method of preventing osteoporosis
KR20010087401A (ko) 1999-09-28 2001-09-15 스타르크, 카르크 아제피노인돌 유도체, 그의 제법 및 용도
US20020010184A1 (en) 2000-02-18 2002-01-24 Dinsmore Christopher J. Inhibitors of prenyl-protein transferase
US20020052380A1 (en) 2000-02-18 2002-05-02 Dinsmore Christopher J. Inhibitors of prenyl-protein transferase
AU5144201A (en) 2000-04-10 2001-10-23 Merck & Co Inc Inhibitors of prenyl-protein transferase
GB0012214D0 (en) 2000-05-19 2000-07-12 Merck Sharp & Dohme Therapeutic agents
EP1322643A1 (en) 2000-09-29 2003-07-02 Millennium Pharmaceuticals, Inc. Piperazin-2-one amides as inhibitors of factor xa
US20020115606A1 (en) 2000-10-17 2002-08-22 Myriad Genetics, Inc. Protein-protein interactions in neurodegenerative diseases
WO2002051836A1 (en) 2000-12-27 2002-07-04 Kyowa Hakko Kogyo Co., Ltd. Dipeptidyl peptidase iv inhibitor
SE0100902D0 (sv) 2001-03-15 2001-03-15 Astrazeneca Ab Compounds
US20030158209A1 (en) 2001-10-09 2003-08-21 Neurocrine Biosciences Inc. Ligands of melanocortin receptors and compositions and methods related thereto
WO2003053940A1 (en) 2001-12-20 2003-07-03 Bristol-Myers Squibb Company Barbituric acid derivatives as inhibitors of tnf-$g(a) converting enzyme (tace) and/or matrix metalloproteinases
AU2002357312A1 (en) 2001-12-20 2003-07-09 Bristol-Myers Squibb Company Barbituric acid derivatives as inhibitors of tnf-alpha converting enzyme (tace) and/or matrix metalloproteinases
WO2003061660A1 (en) 2002-01-23 2003-07-31 Eli Lilly And Company Melanocortin receptor agonists
CA2479906C (en) 2002-04-03 2011-02-08 Topotarget Uk Limited Carbamic acid compounds comprising a piperazine linkage as hdac inhibitors
NZ535764A (en) 2002-04-18 2007-10-26 Schering Corp 1-(4-piperidinyl) benzimidazolones as histamine H3 antagonists
US7105505B2 (en) 2002-04-18 2006-09-12 Schering Corporation Benzimidazole derivatives useful as histamine H3 antagonists
MXPA04010555A (es) 2002-04-25 2005-02-17 Pharmacia Corp Acidos piperidinil- y piperazinil-sulfonilmetil hidroxamicos y su uso como inhibidores de proteasa.
US20050209278A1 (en) 2002-04-25 2005-09-22 Mcdonald Joseph J Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors
WO2004000831A1 (en) 2002-06-24 2003-12-31 Schering Corporation Indole derivatives useful as histamine h3 antagonists
US6906096B2 (en) 2002-06-28 2005-06-14 Irm Llc 4,7-Disubstituted indoles and methods of making
AU2003259131A1 (en) 2002-07-09 2004-01-23 Bristol-Myers Squibb Company Substituted heterocyclic derivatives useful as antidiabetic and antiobesity agents and method
AU2003256922A1 (en) 2002-07-31 2004-02-16 Smithkline Beecham Corporation Substituted heterocyclic compounds as modulators of the ccr5 receptor
ES2399047T3 (es) 2002-09-20 2013-03-25 Merck Serono Sa Derivados de piperazina y procedimiento de uso
WO2004037817A1 (ja) 2002-10-25 2004-05-06 Mitsubishi Pharma Corporation Ｎ−オキシド化合物
US7452911B2 (en) 2002-10-31 2008-11-18 Boehringer Ingelheim Pharma Gmbh & Co. Kg Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
WO2004081643A1 (en) 2002-12-20 2004-09-23 Kaiser Aerospace & Electronics Corp. Lenslet array with polarization conversion
US6861422B2 (en) 2003-02-26 2005-03-01 Boehringer Ingelheim Pharma Gmbh & Co. Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
US20050043533A1 (en) 2003-03-25 2005-02-24 Babiak Kevin A. Process for making alpha-substituted hydroxamic acids
WO2004099179A1 (en) 2003-05-07 2004-11-18 Actelion Pharmaceuticals Ltd Piperazine-alkyl-ureido derivatives
DE602004022819D1 (de) 2003-06-06 2009-10-08 Vertex Pharma Von atp-bindende kassette transportern
US20050124625A1 (en) 2003-10-21 2005-06-09 Salvati Mark E. Piperazine derivatives and their use as modulators of nuclear hormone receptor function
US20050192286A1 (en) 2003-10-22 2005-09-01 Neurocrine Biosciences, Inc. Ligands of melanocortin receptors and compositions and methods related thereto
GB0325956D0 (en) 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
GB0328900D0 (en) 2003-12-12 2004-01-14 Glaxo Group Ltd Novel compounds
JP4769082B2 (ja) 2003-12-17 2011-09-07 武田薬品工業株式会社 ウレア誘導体、その製造法及び用途
JP2007515490A (ja) 2003-12-22 2007-06-14 アムジェン インコーポレーティッド アリールスルホンアミド化合物およびそれに関連する使用法
JP2005232306A (ja) 2004-02-19 2005-09-02 Fuji Photo Film Co Ltd 光重合性組成物及びそれを用いた記録材料
TW200538433A (en) 2004-02-24 2005-12-01 Irm Llc Immunosuppressant compounds and compositiions
WO2005087765A1 (en) 2004-03-04 2005-09-22 Arena Pharmaceuticals, Inc. Ligands of follicle stimulating hormone receptor and methods of use thereof
US20050197336A1 (en) 2004-03-08 2005-09-08 Miikana Therapeutics Corporation Inhibitors of histone deacetylase
CA2559285A1 (en) 2004-03-18 2005-09-29 Brigham And Women's Hospital, Inc. Methods for the treatment of synucleinopathies
SE0400850D0 (sv) 2004-03-30 2004-03-31 Astrazeneca Ab Novel Compounds
US7345043B2 (en) 2004-04-01 2008-03-18 Miikana Therapeutics Inhibitors of histone deacetylase
WO2005117882A2 (en) 2004-04-20 2005-12-15 Incyte Corporation Hydroxamic acid derivatives as metalloprotease inhibitors
GB0408777D0 (en) * 2004-04-20 2004-05-26 Glaxo Group Ltd Compounds
US7880001B2 (en) 2004-04-29 2011-02-01 Abbott Laboratories Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme
ES2346665T3 (es) 2004-05-07 2010-10-19 Warner-Lambert Company Llc Derivados de fenol y tiofenol 3- o 4-monosustituidos utiles como ligandos de h3.
US20090105218A1 (en) 2004-05-29 2009-04-23 7Tm Pharma A/S CRTH2 Receptor Ligands For Therapeutic Use
MXPA06013675A (es) 2004-06-08 2007-02-13 Pfizer Prod Inc Antagonistas de nk1.
US20060241118A1 (en) 2004-06-18 2006-10-26 Celltech R&D Limited Hydroxamate sulfonamides as cd23 shedding inhibitors
CA2571824A1 (en) 2004-07-01 2006-01-19 Merck & Co., Inc. Mitotic kinesin inhibitors
WO2006008644A1 (en) 2004-07-13 2006-01-26 Pfizer Products Inc. Antidiabetic compounds
EP1781670A1 (en) 2004-07-22 2007-05-09 Cumbre Pharmaceuticals Inc. Rifamycin derivatives for treating microbial infections
SE0401971D0 (sv) 2004-08-02 2004-08-02 Astrazeneca Ab Piperidne derivatives
US20060058311A1 (en) 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
US20060074088A1 (en) 2004-08-14 2006-04-06 Boehringer Ingelheim International Gmbh Dihydropteridinones for the treatment of cancer diseases
PE20060653A1 (es) 2004-08-31 2006-09-27 Glaxo Group Ltd Derivados triciclicos condensados como moduladores del receptor 5-ht1
JP5080256B2 (ja) 2004-09-20 2012-11-21 ゼノン・ファーマシューティカルズ・インコーポレイテッド 二環式複素環誘導体およびステアロイル−ＣｏＡデサチュラーゼ（ＳＣＤ）のインヒビターとしてのそれらの使用
EP1807085B1 (en) 2004-09-20 2013-08-21 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
EP2289510A1 (en) 2004-09-20 2011-03-02 Xenon Pharmaceuticals Inc. Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-coa desaturase enzymes
CA2588285A1 (en) 2004-11-29 2006-06-01 National University Corporation Nagoya University Glycopeptide antibiotic monomer derivatives
HRP20090264T1 (hr) * 2004-12-09 2009-06-30 F. Hoffmann - La Roche Ag Derivati fenil-piperazin metanona
PE20061156A1 (es) 2004-12-23 2006-12-16 Glaxo Group Ltd Derivados de benzamida como agentes inhibidores del transportador de glicina
PE20061330A1 (es) 2004-12-23 2006-12-27 Glaxo Group Ltd Compuestos derivados de benzamida como inhibidores del transportador de glicina
GB0428233D0 (en) 2004-12-23 2005-01-26 Glaxo Group Ltd Compounds
GB0428232D0 (en) 2004-12-23 2005-01-26 Glaxo Group Ltd Compounds
JP2008525398A (ja) 2004-12-23 2008-07-17 グラクソ グループ リミテッド グリシン輸送阻害剤
US7635698B2 (en) 2004-12-29 2009-12-22 Millennium Pharmaceuticals, Inc. Compounds useful as chemokine receptor antagonists
US7880002B2 (en) 2004-12-29 2011-02-01 Millennium Pharmaceuticals, Inc. Substituted piperazinyl-pyrrolidine compounds useful as chemokine receptor antagonists
AU2005324024B2 (en) * 2005-01-07 2011-02-17 F. Hoffmann-La Roche Ag [4-(Heteroaryl) piperazin-1-yl]-(2,5-substituted -phenyl)methanone derivatives as glycine transporter 1 (GlyT-1) inhibitors for the treatment of neurological and neuropsychiatric disorders
AU2006212951A1 (en) 2005-02-08 2006-08-17 Merck & Co., Inc. Inhibitors of checkpoint kinases
EP1866276A1 (en) 2005-03-21 2007-12-19 Celera Genomics Alpha ketoamide compounds as cysteine protease inhibitors
DE102005014936A1 (de) 2005-03-24 2006-12-14 Abbott Gmbh & Co. Kg Substituierte Oxindol-Derivate, diese enthaltende Arzneimittel und deren Verwendung
EP1866298A2 (en) 2005-03-31 2007-12-19 Takeda San Diego, Inc. Hydroxysteroid dehydrogenase inhibitors
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
GB0510140D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B2
US20070021433A1 (en) 2005-06-03 2007-01-25 Jian-Qiang Fan Pharmacological chaperones for treating obesity
JP2008545760A (ja) 2005-06-09 2008-12-18 メルク フロスト カナダ リミテツド ステアロイル−コエンザイムａデルタ−９デサチュラーゼのインヒビターとしてのアザシクロヘキサン誘導体
WO2006138218A1 (en) 2005-06-13 2006-12-28 Theravance, Inc. Biphenyl compounds useful as muscarinic receptor antagonists
EP1896453B1 (en) 2005-06-20 2009-12-02 Schering Corporation Carbon-linked substituted piperidines and derivatives thereof useful as histamine h3 antagonists
DE602006010870D1 (de) 2005-06-20 2010-01-14 Schering Corp Als antagonisten von histamin h3 geeignete piperidinderivate
US7851474B2 (en) 2005-08-02 2010-12-14 Neurogen Corporation Dipiperazinyl ketones and related analogues
EP1937659B1 (en) * 2005-10-06 2010-11-10 Sanofi-Aventis Cyclic n-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, processes for their preparation and their use as pharmaceuticals
DE102005049954A1 (de) 2005-10-19 2007-05-31 Sanofi-Aventis Deutschland Gmbh Triazolopyridin-derivate als Inhibitoren von Lipasen und Phospholipasen
WO2007057742A2 (en) 2005-11-18 2007-05-24 Pfizer Products Inc. Novel piperazinone derivatives
US20070197505A1 (en) 2005-12-15 2007-08-23 Morgan Bradley P Certain chemical entities, compositions and methods
JP2009521448A (ja) 2005-12-21 2009-06-04 シェーリング コーポレイション ヒスタミンｈ３アンタゴニストとして有用なフェノキシピペリジンおよびそのアナログ
MX2008008340A (es) 2005-12-21 2008-09-03 Schering Corp Tratamiento de enfermedad de higado graso no alcoholica usando agentes reductores de colesterol y/o antagonista/agonista inverso de receptor de histamina 3.
US20070142369A1 (en) 2005-12-21 2007-06-21 Margaret Van Heek Combination of an H3 antagonist/inverse agonist and an appetite suppressant
MX2008008339A (es) 2005-12-21 2008-09-03 Schering Corp Derivados de anilina sustituida ùtiles como antagonistas de la histamina h3.
US20070203111A1 (en) 2006-01-06 2007-08-30 Sepracor Inc. Cycloalkylamines as monoamine reuptake inhibitors
GB0600427D0 (en) 2006-01-10 2006-02-15 Glaxo Group Ltd Compounds
KR20080098490A (ko) 2006-01-13 2008-11-10 파마시클릭스, 인코포레이티드 티로신 키나제 억제제 및 이의 용도
WO2007087220A2 (en) 2006-01-25 2007-08-02 The Trustees Of Columbia University In The City Of New York The total synthesis of ecteinascidin 743 and derivatives thereof
WO2007092435A2 (en) 2006-02-07 2007-08-16 Wyeth 11-beta hsd1 inhibitors
BRPI0707623A2 (pt) 2006-02-10 2011-05-10 Janssen Pharmaceutica Nv derivados de piperidina como antagonistas de receptores de cxcr3
RU2318818C1 (ru) 2006-04-12 2008-03-10 Общество С Ограниченной Ответственностью "Исследовательский Институт Химического Разнообразия" Азагетероциклы, комбинаторная библиотека, фокусированная библиотека, фармацевтическая композиция и способ получения (варианты)
JPWO2007119833A1 (ja) 2006-04-14 2009-08-27 武田薬品工業株式会社 含窒素複素環化合物
US8017612B2 (en) 2006-04-18 2011-09-13 Japan Tobacco Inc. Piperazine compound and use thereof as a HCV polymerase inhibitor
CA2650932C (en) 2006-05-09 2013-01-22 Merck & Co., Inc. Substituted spirocyclic cgrp receptor antagonists
TW200808818A (en) 2006-05-26 2008-02-16 Shionogi & Co Glycopeptide antibiotic derivatives
WO2007139150A1 (ja) 2006-05-30 2007-12-06 The University Of Tokushima ＴＮＦα阻害物質を含有してなる抗インフルエンザウイルス剤
EA200802415A1 (ru) 2006-06-09 2009-06-30 Икос Корпорейшн Замещенные фенилуксусные кислоты в качестве dp-2-антагонистов
GB0612416D0 (en) 2006-06-22 2006-08-02 Glaxo Group Ltd Compounds
GB0612437D0 (en) 2006-06-22 2006-08-02 Glaxo Group Ltd Compounds
GB0612435D0 (en) 2006-06-22 2006-08-02 Glaxo Group Ltd Compounds
GB0612425D0 (en) 2006-06-22 2006-08-02 Glaxo Group Ltd Compounds
GB0612420D0 (en) 2006-06-22 2006-08-02 Glaxo Group Ltd Compounds
NZ573129A (en) 2006-06-28 2011-06-30 Amgen Inc Piperazine acetic acid glycine transporter-1 inhibitors
EP2592070B1 (en) * 2006-06-29 2016-08-31 F. Hoffmann-La Roche AG Tetrazole-substituted arylamides
JP2008013527A (ja) 2006-07-10 2008-01-24 Sankyo Co Ltd チエノ［３，２−ｄ］ピリミジン−２，４−ジアミン誘導体
DE102006033114A1 (de) 2006-07-18 2008-01-24 Grünenthal GmbH Spirocyclische Azaindol-Derivate
WO2008034736A2 (en) 2006-09-21 2008-03-27 F. Hoffmann-La Roche Ag Oxindole derivatives as anticancer agents
GB0621607D0 (en) 2006-10-31 2006-12-06 Chroma Therapeutics Ltd Inhibitors of c-Met
PE20080931A1 (es) 2006-11-08 2008-07-19 Schering Corp Imidazopirazinas como inhibidores de proteina quinasa
EP2091927B1 (en) * 2006-11-09 2011-07-20 F. Hoffmann-La Roche AG Thiazole and oxazole-substituted arylamides
US20080153810A1 (en) 2006-11-15 2008-06-26 Forest Laboratories Holdings Limited Indazole derivatives useful as melanin concentrating receptor ligands
KR20080045537A (ko) 2006-11-20 2008-05-23 에스케이케미칼주식회사 피리딘 화합물을 포함하는 간염 치료 및 예방 또는 간 보호효능을 갖는 약제 조성물
EP2123637A4 (en) 2006-11-30 2011-12-21 Tokyo Inst Tech NEW CURCUMIN DERIVATIVES
CA2672212A1 (en) 2006-12-11 2008-06-19 Reviva Pharmaceuticals, Inc. Compositions, synthesis, and methods of using indanone based cholinesterase inhibitors
US7737149B2 (en) 2006-12-21 2010-06-15 Astrazeneca Ab N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof
DE102006060598A1 (de) 2006-12-21 2008-06-26 Merck Patent Gmbh Tetrahydrobenzoisoxazole
US20080186971A1 (en) 2007-02-02 2008-08-07 Tarari, Inc. Systems and methods for processing access control lists (acls) in network switches using regular expression matching logic
CA2677656A1 (en) 2007-02-07 2008-08-14 Wyeth Method for preparing halogenated amines
US20100216992A1 (en) 2007-02-27 2010-08-26 University Of South Florida Mimetic compositions and the production thereof
CN101631787A (zh) 2007-03-13 2010-01-20 比奥维特罗姆上市公司 用于肥胖症治疗的三环异喹啉衍生物
PE20090188A1 (es) 2007-03-15 2009-03-20 Novartis Ag Compuestos heterociclicos como moduladores de la senda de hedgehog
CA2683557C (en) 2007-04-09 2016-10-18 Methylgene Inc. Inhibitors of histone deacetylase
JP2008266236A (ja) 2007-04-23 2008-11-06 Kyorin Pharmaceut Co Ltd 環状アミン誘導体又はその塩
GB0709031D0 (en) 2007-05-10 2007-06-20 Sareum Ltd Pharmaceutical compounds
CA2687931C (en) 2007-05-31 2016-05-24 Boehringer Ingelheim International Gmbh Ccr2 receptor antagonists and uses thereof
JP2010208945A (ja) 2007-06-01 2010-09-24 Mitsubishi Tanabe Pharma Corp 複素環化合物
JP2010530397A (ja) 2007-06-20 2010-09-09 グラクソ グループ リミテッド アミド形成の改善方法
US7842696B2 (en) * 2007-06-21 2010-11-30 Forest Laboratories Holdings Limited Piperazine derivatives as inhibitors of stearoyl-CoA desaturase
US20100286160A1 (en) 2007-06-28 2010-11-11 Intervet Inc. Substituted piperazines as cb1 antagonists
JP2010531360A (ja) 2007-06-28 2010-09-24 インターベット インターナショナル ベー． フェー． Ｃｂ１拮抗剤としてのピペラジンの使用
US8623873B2 (en) 2007-06-28 2014-01-07 Intervet Inc. Substituted piperazines as CB1 antagonists
TW200911808A (en) 2007-07-23 2009-03-16 Astrazeneca Ab Novel compounds
JP5160827B2 (ja) 2007-07-25 2013-03-13 塩野義製薬株式会社 グリコペプチド抗生物質誘導体
JP5736098B2 (ja) 2007-08-21 2015-06-17 アッヴィ・インコーポレイテッド 中枢神経系障害を治療するための医薬組成物
JP5787756B2 (ja) 2008-07-04 2015-09-30 フィリップ マルリエ ３−ヒドロキシアルカン酸の酵素的脱炭酸によるアルケンの製造法
AU2011261375B2 (en) 2010-06-04 2016-09-22 Albany Molecular Research, Inc. Glycine transporter-1 inhibitors, methods of making them, and uses thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070043027A1 (en) * 2003-09-12 2007-02-22 Applied Reserach Systems Ars Holding N.V. Sulfonamide derivatives for the treatment of diabetes
US20090269278A1 (en) * 2005-09-29 2009-10-29 Burns H Donald Radiolabeled Glycine Trasporter Inhibitors
CN101479243A (zh) * 2006-06-28 2009-07-08 安姆根有限公司 甘氨酸转运子-1抑制剂

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