ES2308811T3 - Derivados de piridina. - Google Patents

Derivados de piridina. Download PDF

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Publication number
ES2308811T3
ES2308811T3 ES98941308T ES98941308T ES2308811T3 ES 2308811 T3 ES2308811 T3 ES 2308811T3 ES 98941308 T ES98941308 T ES 98941308T ES 98941308 T ES98941308 T ES 98941308T ES 2308811 T3 ES2308811 T3 ES 2308811T3
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Spain
Prior art keywords
alkoxy
alkyl
carboxyl
alkoxycarbonyl
hydrogen
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Expired - Lifetime
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ES98941308T
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English (en)
Inventor
Hans Allgeier
Yves Auberson
Michel Biollaz
Nicholas David Cosford
Fabrizio Gasparini
Roland Heckendorn
Edwin Carl Johnson
Rainer Kuhn
Mark Andrew Varney
Gonul Velicelebi
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Novartis AG
Merck and Co Inc
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Novartis AG
Merck and Co Inc
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    • C07D213/04Heterocyclic 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
    • C07D213/06Heterocyclic 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 containing only hydrogen and carbon atoms in addition to the ring nitrogen atom
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Abstract

El uso de un compuesto de fórmula I (Ver fórmula) en donde X representa un grupo alquenileno (C2 - 4) opcionalmente halo-sustituido o un grupo alquinileno enlazado a través de átomos de carbono vecinos insaturados, R1 es hidrógeno, alquilo (C1 - 4), alcoxi (C1 - 4), hidroxialquilo (C1 - 4), ciano, etinilo, carboxilo, alcoxicarbonilo (C1 - 4), di alquilamino (C1 - 4), alquilaminocarbonilo (C1 - 6), trifluorometil-fenilaminocarbonilo, R2 es hidrógeno, hidroxilo, alquilo (C1 - 4), hidroxialquilo (C1 - 4), alcoxi (C1 - 4), carboxilo, alcanoiloxi (C2 - 5), alcoxicarbonilo (C1 - 4), dialquilamino (C1 - 4) alcanoilo (C1 - 4), dialquilaminometilo (C1 - 4), 4-(4-fluoro-benzoil)-pi-peridin- 1-il-carboxilo, 4-t.-butiloxicarbonil-piperazin-1-il-carboxilo, 4-(4-azido-2-hidroxibenzoil)-piperazin-1-il-carboxilo o 4-(4-azido-2-hidroxilo-3-iodo-benzoil)-piperazin-1-il-carboxilo. R3 es hidrógeno, alquilo (C1 - 4), carboxilo, alcoxicarbonilo (C1 - 4), alquilcarbamoilo (C1 - 4), hidroxialquilo (C1 - 4), dialquilaminometilo (C1 - 4), morfolinocarbonilo o 4-(4-fluorobenzoil)-piperidin-1-il-carboxilo, R4 es hidrógeno, hidroxilo, alcoxi (C1 - 4), carboxilo, alcanoiloxi (C2 - 5), alcoxicarbonilo (C1 - 4), amino alcoxi (C1 - 4), dialquilamino (C1 - 4) alcoxi (C1 - 4), dialquilamino (C1 - 4) alquilo (C1 - 4), carboxilo alquilcarbonilo (C1 - 4), alcoxicarbonilo (C1 - 4) alcoxi (C1 - 4), hidroxilo alquilo (C1 - 4), dialquilamino (C1 - 4) alcoxi (C1 - 4), m-hidroxilo-p-azidofenil-carbonilamino alcoxi (C1 - 4), y R5 es un grupo de fórmula (Ver fórmula) en donde Ra y Rb son independientemente hidrógeno, hidroxilo, halógeno; nitro, ciano, carboxilo, alquilo (C1 - 4), alcoxi (C1 - 4), hidroxilo alquilo (C1 - 4), alcoxicarbonilo (C1 - 4), alcanoilo (C2 - 7), alcanoiloxi (C2 - 5), alcanoiloxi (C2 - 5) alquilo (C1 - 4), trifluorometilo, trifluorometoxi, trimetilsililetinilo, alquinilo (C2 - 5), amino, azido, amino alcoxi (C1 - 4), alcanoilamino (C2 - 5) alcoxi (C1 - 4), alquilamino (C1 - 4) alcoxi (C1 - 4), dialquilamino (C1 - 4) alcoxi (C1 - 4), alquilamino (C1 - 4), dialquilamino (C1 - 4), monohalobencilamino, tienilmetilamino, tienilcarbonilamino, trifluorometilfenilaminocarbonilo, tetrazolilo, alcanoilamino (C2 - 5), bencilcarbonilamino, alquilaminocarbonilamino (C1 - 4), alcoxicarbonil (C1 - 4)-aminocarbonilamino o alquilsulfonilo (C1 - 4), Rc es hidrógeno, flúor, cloro, bromo, hidroxilo, alquilo (C1 - 4), alcanoiloxi (C2 - 5), alcoxi (C1 - 4) o ciano, y Rd es hidrógeno, halógeno o alquilo (C1 - 4). en forma libre o en la forma de un N-óxido o una sal farmacéuticamente aceptable, para la fabricación de una composición farmacéutica para el tratamiento de trastornos asociados con irregularidades de la trasmisión de la señal glutamatérgica, y de trastornos del sistema nervioso mediados completamente o en parte por medio de mGluR5.
ES98941308T 1997-07-11 1998-07-09 Derivados de piridina. Expired - Lifetime ES2308811T3 (es)

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US89169197A 1997-07-11 1997-07-11
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Families Citing this family (102)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2232017C2 (ru) * 1998-10-02 2004-07-10 Новартис Аг Антагонисты метаботропных глутаматных рецепторов (mglur5) для лечения боли и состояния тревоги
AU3679800A (en) * 1999-04-23 2000-11-10 Sumitomo Pharmaceuticals Company, Limited Apoptosis inhibitors
FR2793245B1 (fr) * 1999-05-05 2002-10-11 Adir Nouveaux composes pyridiniques ou piperidiniques substitues, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US6660753B2 (en) 1999-08-19 2003-12-09 Nps Pharmaceuticals, Inc. Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
JP4815083B2 (ja) * 1999-08-31 2011-11-16 メルク・シャープ・エンド・ドーム・コーポレイション 複素環化合物およびそれの使用方法
US6774138B2 (en) 1999-08-31 2004-08-10 Merck & Co., Inc. Thiazolyl(pyridyl)ethyne compounds
GB0005700D0 (en) * 2000-03-09 2000-05-03 Glaxo Group Ltd Therapy
JP5154728B2 (ja) * 2000-07-24 2013-02-27 クレニツキー・ファーマシューティカルズ,インコーポレイテッド 神経栄養活性を有する置換5−アルキニルピリミジン
BR0115871A (pt) 2000-12-04 2003-10-28 Hoffmann La Roche Derivados de feniletenila ou feniletinila como antagonistas de receptores de glutamato
GB0103045D0 (en) * 2001-02-07 2001-03-21 Novartis Ag Organic Compounds
ATE375340T1 (de) * 2001-02-21 2007-10-15 Nps Pharma Inc Heteropolycyclische verbindungen und deren verwendung als metabotrope glutamatrezeptorantagonisten
US8124625B2 (en) 2001-09-14 2012-02-28 Shionogi & Co., Ltd. Method of enhancing the expression of apolipoprotein AI using olefin derivatives
BR0213233A (pt) * 2001-10-12 2005-01-04 Warner Lambert Co Alcinos inibidores de metaloproteinase de matriz
US6951875B2 (en) * 2001-10-29 2005-10-04 Hoffmann-La Roche Inc. Conjugated aromatic compounds with a pyridine substituent
GB0128996D0 (en) * 2001-12-04 2002-01-23 Novartis Ag Organic compounds
WO2003093236A1 (en) * 2002-05-02 2003-11-13 Euro-Celtique, S.A. 1-(pyrid-2-yl)-piperazine compounds as metabotropic glutamate receptor inhibitor
AU2003253149A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc 3,4-dihydroquinolin-2-one, 5,6-fused oxazin-3-one, and 5,6-fused thiazin-3-one derivatives as matrix metalloproteinase inhibitors
EP1539749A4 (en) * 2002-09-13 2007-06-13 Merck & Co Inc BY CONDENSED HETEROBICYCLOGRUPPEN SUBSTITUTED PHENYL COMPOUNDS AS METOBOTROPE GLUTAMATE-5 MODULATORS
US20070060618A1 (en) * 2002-10-24 2007-03-15 Merck & Co., Inc. Alkyne derivatives as tracers for metabotropic glutamate receptor binding
DE10250708A1 (de) * 2002-10-31 2004-05-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
US7351719B2 (en) 2002-10-31 2008-04-01 Boehringer Ingelheim Pharma Gmbh & Co. Kg Amide compounds having MCH-antagonistic activity and medicaments comprising these compounds
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
ITMI20030151A1 (it) * 2003-01-30 2004-07-31 Recordati Ind Chimica E Farma Ceutica S P A Uso di antagonisti selettivi del recettore mglu5 per il trattamento di disfunzioni neuromuscolari del tratto urinario inferiore.
UA81464C2 (en) 2003-03-04 2008-01-10 NOVEL AMINOPYRIDINE DERIVATIVES AS mGIuR5 ANTAGONISTS
WO2004078715A1 (ja) * 2003-03-07 2004-09-16 Astellas Pharma Inc. 2,6-ジ置換スチリルを有する含窒素へテロ環誘導体
TWI292318B (en) 2003-03-10 2008-01-11 Hoffmann La Roche Imidazol-4-yl-ethynyl-pyridine derivatives
US7531529B2 (en) 2003-06-05 2009-05-12 Roche Palo Alto Llc Imidazole derivatives
UA80888C2 (en) * 2003-06-05 2007-11-12 Hoffmann La Roche Imidazole derivatives as glutmate receptor antagonists
CA2527587C (en) * 2003-06-12 2010-09-28 F. Hoffmann-La Roche Ag Heteroaryl-substituted imidazole derivatives as glutamate receptor antagonists
ES2322707T3 (es) * 2003-07-03 2009-06-25 Euro-Celtique S.A. Derivados de 2-piridina alquino utiles para tratar el dolor.
US7091222B2 (en) * 2003-07-03 2006-08-15 Hoffmann-La Roche Inc. Imidazole derivatives
JP4667384B2 (ja) * 2003-10-07 2011-04-13 レノビス, インコーポレイテッド イオンチャネルリガンドとしてのアミド誘導体および薬学的組成物、ならびにこれらを使用する方法
JP2007509935A (ja) * 2003-10-31 2007-04-19 アストラゼネカ アクチボラグ アルキンズii
JP2007510645A (ja) * 2003-10-31 2007-04-26 アストラゼネカ アクチボラグ アルキン類i
EP1677788A1 (en) * 2003-10-31 2006-07-12 AstraZeneca AB Alkynes iii
GB0325956D0 (en) 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
US7592373B2 (en) 2003-12-23 2009-09-22 Boehringer Ingelheim International Gmbh Amide compounds with MCH antagonistic activity and medicaments comprising these compounds
US7524862B2 (en) 2004-04-14 2009-04-28 Boehringer Ingelheim International Gmbh Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
DE102004017930A1 (de) * 2004-04-14 2005-11-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
DE102004017935A1 (de) * 2004-04-14 2005-11-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
DE102004017934A1 (de) 2004-04-14 2005-11-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
US20050245529A1 (en) * 2004-04-14 2005-11-03 Boehringer Ingelheim International Gmbh Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
KR100907108B1 (ko) 2004-06-01 2009-07-09 에프. 호프만-라 로슈 아게 Mglu5 수용체 길항제로서 피리딘-4-일-에틴일-이미다졸및 피라졸
ES2332659T3 (es) * 2004-06-16 2010-02-10 Wyeth Derivados de amino-5,5-difenilimidazolona para la inhibicion de beta-secretasa.
WO2006009655A1 (en) 2004-06-16 2006-01-26 Wyeth Diphenylimidazopyrimidine and -imidazole amines as inhibitors of b-secretase
GB0413605D0 (en) * 2004-06-17 2004-07-21 Addex Pharmaceuticals Sa Novel compounds
JP4966866B2 (ja) 2005-01-14 2012-07-04 エフ.ホフマン−ラ ロシュ アーゲー mGluR5アンタゴニストとしてのチアゾール−4−カルボキサミド誘導体
EP2264036A1 (en) 2005-01-14 2010-12-22 Wyeth LLC (Formerly Known As Wyeth) Amino-imidazolones for the inhibition of beta-secretase
MX2007009313A (es) * 2005-02-01 2007-09-12 Wyeth Corp Amino-piridinas como inhibidores de ????-secretasa.
WO2006088711A1 (en) 2005-02-14 2006-08-24 Wyeth AZOLYLACYLGUANIDINES AS β-SECRETASE INHIBITORS
US7576099B2 (en) 2005-02-28 2009-08-18 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
BRPI0607583A2 (pt) * 2005-03-04 2009-09-15 Hoffmann La Roche derivados de piridin-2-carboxamida como antagonistas mglur5, método para sua preparação, medicamento contendo os mesmos, bem como uso relacionado aos referidos compostos
GB0508319D0 (en) * 2005-04-25 2005-06-01 Novartis Ag Organic compounds
TW200738683A (en) * 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
WO2007005404A1 (en) * 2005-06-30 2007-01-11 Wyeth AMINO-5-(6-MEMBERED)HETEROARYLIMIDAZOLONE COMPOUNDS AND THE USE THEREOF FOR ß-SECRETASE MODULATION
FR2889187B1 (fr) * 2005-07-28 2007-09-07 Servier Lab Nouveaux composes 1,1-pyridinyloxycyclopropanamines polysusbstitues, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
FR2889188B1 (fr) * 2005-07-28 2007-09-07 Servier Lab Nouveaux composes 1,1-pyridinylaminocyclopropanamines polysubstitues, leur procede de preparation et les compositions phamaceutiques qui les contiennent
TW200730523A (en) * 2005-07-29 2007-08-16 Wyeth Corp Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation
US7531541B2 (en) * 2005-09-20 2009-05-12 Vanderbilt University Partial mGluR5 antagonists for treatment of anxiety and CNS disorders
BRPI0616757A2 (pt) * 2005-09-26 2011-06-28 Wyeth Corp composto da fórmula i; processo para o tratamento de uma doença ou de um distúrbio associado com a atividade excessiva de bace; processo para a modulação da atividade de bace; processo para o tratamento da doença de alzheimer; e composição farmacêutica
GB0525068D0 (en) 2005-12-08 2006-01-18 Novartis Ag Organic compounds
JP2009520027A (ja) * 2005-12-19 2009-05-21 ワイス 2−アミノ−5−ピペリジニルイミダゾロン化合物およびβ−セクレターゼ調節におけるその使用
DE102005062985A1 (de) * 2005-12-28 2007-07-05 Grünenthal GmbH Substituierte bis(hetero)aromatische N-Ethylpropiolamide und ihre Verwendung zur Herstellung von Arzneimitteln
WO2007100536A1 (en) * 2006-02-24 2007-09-07 Wyeth DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE
PT1999109E (pt) * 2006-03-30 2012-03-16 Univ Pennsylvania Derivados de estirilpiridina e sua utilização para ligação e obtenção de imagens de placas amilóides
BRPI0710328A2 (pt) * 2006-05-08 2011-08-09 Ariad Pharma Inc composto da fórmula i, um tautomer da mesma, ou um sal farmaceuticamente aceitável, hidrato ou outro solvato do mesmo e método para o tratamento de cáncer em um mamìfero necessitado do mesmo e composição
US7700606B2 (en) * 2006-08-17 2010-04-20 Wyeth Llc Imidazole amines as inhibitors of β-secretase
CA2662348A1 (en) * 2006-09-21 2008-03-27 Wyeth Indolylalkylpyridin-2-amines for the inhibition of .beta.-secretase
LT2083811T (lt) 2006-11-22 2017-01-25 Clinical Research Associates, Llc Dauno sindromo, trapiosios x chromosomos sindromo ir autizmo gydymo būdai
CN101568531B (zh) 2006-12-21 2013-11-13 弗·哈夫曼-拉罗切有限公司 Mglur5受体拮抗剂的多晶型物
JP2010519267A (ja) * 2007-02-22 2010-06-03 シンジェンタ パーティシペーションズ アクチェンゲゼルシャフト 新規殺微生物剤
WO2008112440A1 (en) * 2007-03-09 2008-09-18 Astrazeneca Ab Piperazine and piperidine mglur5 potentiators
DK2124562T3 (en) 2007-03-09 2016-08-01 Second Genome Inc BICYCLOHETEROARYLFORBINDELSER AS P2X7 modulators and uses thereof
CL2008000784A1 (es) * 2007-03-20 2008-05-30 Wyeth Corp Compuestos amino-5-[-4-(diflourometoxi) fenil sustituido]-5-fenilmidazolona, inhibidores de b-secretasa; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar alzheimer, deterioro cognitivo, sindrome de down, disminucion co
CL2008000791A1 (es) * 2007-03-23 2008-05-30 Wyeth Corp Compuestos derivados de 2-amino-5-(4-difluorometoxi-fenil)-5-fenil-imidazolidin-4-ona; composicion farmaceutica que comprende a dichos compuestos; y su uso en el tratamiento de una enfermedad asociada con la actividad bace excesiva, tales como enferm
US8853392B2 (en) * 2007-06-03 2014-10-07 Vanderbilt University Benzamide mGluR5 positive allosteric modulators and methods of making and using same
WO2008151184A1 (en) * 2007-06-03 2008-12-11 Vanderbilt University Benzamide mglur5 positive allosteric modulators and methods of making and using same
GB0713686D0 (en) 2007-07-13 2007-08-22 Addex Pharmaceuticals Sa New compounds 2
US8034806B2 (en) * 2007-11-02 2011-10-11 Vanderbilt University Bicyclic mGluR5 positive allosteric modulators and methods of making and using same
CA2748235A1 (en) 2008-12-24 2010-07-01 Astrazeneca Ab Ethanamine compounds and their use for treating depression
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
KR101396606B1 (ko) * 2009-04-20 2014-05-16 미쓰비시 타나베 파마 코퍼레이션 신규 갑상선 호르몬 β 수용체 작동약
EP2531510B1 (en) 2010-02-01 2014-07-23 Novartis AG Pyrazolo[5,1b]oxazole derivatives as crf-1 receptor antagonists
AR080056A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de ciclohexil-amida como antagonistas de los receptores de crf
ES2527849T3 (es) 2010-02-02 2015-01-30 Novartis Ag Derivados de ciclohexilamida como antagonistas del receptor de CRF
EP2544688B1 (en) 2010-03-02 2016-09-07 President and Fellows of Harvard College Methods and compositions for treatment of angelman syndrome
US8420661B2 (en) * 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
WO2011150380A1 (en) 2010-05-28 2011-12-01 Xenoport, Inc. Methods of treatment of fragile x syndrome, down's syndrome, autism and related disorders
US20120016021A1 (en) 2010-07-15 2012-01-19 Xenoport, Inc. Methods of treating fragile x syndrome, down's syndrome, autism and related disorders
US8772300B2 (en) * 2011-04-19 2014-07-08 Hoffmann-La Roche Inc. Phenyl or pyridinyl-ethynyl derivatives
AR086554A1 (es) 2011-05-27 2014-01-08 Novartis Ag Derivados de la piperidina 3-espirociclica como agonistas de receptores de la ghrelina
EA201491990A1 (ru) 2012-05-03 2015-02-27 Новартис Аг L-малатная соль 2,7-диазаспиро[4.5]дец-7-иловых производных и их кристаллические формы в качестве агонистов грелиновых рецепторов
UA114934C2 (uk) * 2012-10-18 2017-08-28 Ф. Хоффманн-Ля Рош Аг Похідне етинілу як модулятор активності метаботропного глутаматного рецептора підтипу 5
WO2014060398A1 (en) * 2012-10-18 2014-04-24 F. Hoffmann-La Roche Ag Ethynyl derivatives as modulators of mglur5 receptor activity
UA116023C2 (uk) 2013-07-08 2018-01-25 Ф. Хоффманн-Ля Рош Аг Етинільні похідні як антагоністи метаботропного глутаматного рецептора
EP2853565A1 (en) 2013-09-27 2015-04-01 Consejo Superior De Investigaciones Científicas Glutamate receptor photomodulators
CN106146391A (zh) * 2015-04-15 2016-11-23 中国科学院上海药物研究所 5-芳香炔基取代的苯甲酰胺类化合物及其制备方法、药物组合物和用途
AU2017214615A1 (en) * 2016-02-03 2018-09-20 Galderma Research & Development Novel biaromatic propynyl compounds, pharmaceutical and cosmetic compositions containing same, and uses thereof
US10449186B2 (en) * 2017-06-21 2019-10-22 University Of Kentucky Research Foundation Phenylethynyl-substituted benzenes and heterocycles for the treatment of cancer
JP2020529975A (ja) 2017-07-31 2020-10-15 ノバルティス アーゲー コカイン使用の低減又はコカイン使用再燃の予防におけるマボグルラントの使用
CN107400256B (zh) * 2017-08-14 2019-04-19 深圳市精研科洁科技股份有限公司 一种抗紫外线塑料添加剂的制备方法
WO2023122212A2 (en) 2021-12-21 2023-06-29 Southern Research Institute Substituted phenyl ethynyl pyridine carboxamides as potent inhibitors of sars virus

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4006240A (en) * 1975-03-19 1977-02-01 Ho Andrew K S Alcohol aversion process by enzyme inhibition
NO174506B (no) * 1984-10-30 1994-02-07 Usv Pharma Corp Analogifremgangsmaate ved fremstilling av terapeutisk aktive forbindelser
DE68907095T2 (de) * 1988-03-21 1994-01-05 Boehringer Ingelheim Pharma Verbindungen zur Verhinderung der Biosynthese von der Lipoxygenase abgeleiteten Metaboliten der Arachidonsäure.
US5013744B1 (en) * 1989-12-29 1994-09-20 Allegran Inc Acetylenes disubstituted with a pyridinyl group and a substituted phenyl group having retinoid like activity
JPH05500781A (ja) * 1990-08-08 1993-02-18 ゼネラル・エレクトリック・カンパニイ 不織フェルトを使った繊維強化熱可塑性合成樹脂の製造方法
GB9515412D0 (en) * 1995-07-27 1995-09-27 Pharmacia Spa 2-(4-substituted)-benzylamino-2-methyl-propanamide derivatives
AU6514296A (en) * 1995-07-31 1997-02-26 Novo Nordisk A/S Heterocyclic compounds, their preparation and use
IT1276153B1 (it) * 1995-11-17 1997-10-27 Roberto Pellicciari Derivati di glicina ad attivita' antagonista dei recettori metabotropi del glutammato

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