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HUP0004225A2 - Piridinszármazékok és alkalmazásuk gyógyszerkészítmények előállítására, valamint a vegyületeket tartalmazó gyógyszerkészítmények - Google Patents

Piridinszármazékok és alkalmazásuk gyógyszerkészítmények előállítására, valamint a vegyületeket tartalmazó gyógyszerkészítmények

Info

Publication number
HUP0004225A2
HUP0004225A2 HU0004225A HUP0004225A HUP0004225A2 HU P0004225 A2 HUP0004225 A2 HU P0004225A2 HU 0004225 A HU0004225 A HU 0004225A HU P0004225 A HUP0004225 A HU P0004225A HU P0004225 A2 HUP0004225 A2 HU P0004225A2
Authority
HU
Hungary
Prior art keywords
alkyl
alkoxy
oxy
carbonyl
carboxy
Prior art date
Application number
HU0004225A
Other languages
English (en)
Inventor
Hans Allgeier
Yves Auberson
Michel Biollaz
Nicholas David Cosford
Fabrizio Gasparini
Roland Heckendorn
Edwin Carl Johnson
Rainer Kuhn
Mark Andrew Varney
Gönül Velicelebi
Original Assignee
Novartis Ag.
Sibia Neurosciences Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27128958&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HUP0004225(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag., Sibia Neurosciences Inc. filed Critical Novartis Ag.
Publication of HUP0004225A2 publication Critical patent/HUP0004225A2/hu
Publication of HUP0004225A3 publication Critical patent/HUP0004225A3/hu

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    • C07D213/02—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
    • 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
    • C07D213/26—Radicals substituted by halogen atoms or nitro radicals
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    • C07D213/02—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
    • 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
    • C07D213/06—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 containing only hydrogen and carbon atoms in addition to the ring nitrogen atom
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    • C07D213/06—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 containing only hydrogen and carbon atoms in addition to the ring nitrogen atom
    • C07D213/16—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 containing only hydrogen and carbon atoms in addition to the ring nitrogen atom containing only one pyridine ring
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    • C07D213/02—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
    • 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
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    • C07D213/02—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
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Abstract

A találmány tárgya egy (I) általános képletűvegyületnek - amelynek képletében R1 hidrogénatom, alkil-, hidroxi-alkil-, alkil-amino-, piperidino-,adott esetben észteresített vagy amidált karboxi-, adott esetbenszubsztituált N-alkil-N-fenil-karbamoil-, alkoxi-, halogén-alkil- vagyhalogén-alkoxi-csoport; R2 hidrogénatom, alkil-, adott esetben észteresített vagy amidáltkarboxi-, hidroxi-alkil-, hidroxi-, alkoxi-, alkanoil-oxi-, {[4-(4-fluor-benzoil)-1-piperidil]-oxi}-karbonil-, ([4-(terc-butoxi-karbonil)-1-piperazinil]-oxi}-karbonil-, {[4-(4-azido-2-hidroxi-benzoil)-1-piperazinil]-oxi}-karbonil- vagy ([4-(4-azido-2-hidroxi-3-jód-benzoil)- 1- piperazinil]-oxi}-karbonil-csoport; R3 hidrogénatom, alkil-, karboxi-, alkoxi-karbonil-, alkil-karbamoil-,hidroxi-alkil-, (dialkil-amino)-metil-, morfolino-karbonil vagy {[4-(4-fluor-benzoil)-1-piperidil]-oxi}-karbonil-csoport; R4 hidrogénatom, alkil-, hidroxi-, hidroxi-alkil-, amino-alkil-,(alkil-amino)-alkil-, (dialkil-amino)-alkil-, adott esetbenhidroxicsoporttal szubsztituált (alkilén-amino)-alkil-, alkoxi-,alkanoil-oxi-, amino-alkoxi-, (alkil-amino)-alkoxi-, (dialkil-amino)-alkoxi-, ftálimido-alkoxi-, adott esetben szubsztituált (alkilén-amino)-alkoxi-, adott esetben észteresített vagy amidált karboxi-,karboxi-alkoxi)- vagy adott esetben észteresített karboxi-alkoxi-csoport; X vicinális telítetlen szénatomokon keresztül kapcsolódó, adottesetben szubsztituált alkenilén- vagy alkiniléncsoport, vagy -N=N-képletű azocsoport: és R5 adott esetben szubsztituált aromás vagy heteroaromás csoport - vagyszokásos fotoaffin ligandjainak és szokásos radioaktív markereinek, N-oxidjainak és gyógyszerészetileg elfogadható sóinak az alkalmazása aglutamáterg szignál transzmisszió szabálytalanságaival kapcsolatosrendellenességek és teljesen vagy részben mG1uR5 által mediáltidegrendszeri rendellenességek kezelésére szolgálógyógyszerkészítmények előállítására. A találmány kiterjed az új (I)általános képletű vegyületekre, valamint a hatóanyagokat tartalmazógyógyszerkészítményekre is. Ó
HU0004225A 1997-07-11 1998-07-09 Pyridine derivatives, use of them for producing pharmaceutical compositions and pharmaceutical compositions containing the same HUP0004225A3 (en)

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Families Citing this family (102)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20010088832A (ko) * 1998-10-02 2001-09-28 한스 루돌프 하우스, 헨리테 브룬너, 베아트리체 귄터 통증 및 불안증 치료용 ｍＧｌｕＲ5 길항제
WO2000064430A1 (fr) * 1999-04-23 2000-11-02 Sumitomo Pharmaceuticals Co., Ltd. Inhibiteurs de l'apoptose
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
US6774138B2 (en) 1999-08-31 2004-08-10 Merck & Co., Inc. Thiazolyl(pyridyl)ethyne compounds
EP1214303A1 (en) * 1999-08-31 2002-06-19 Merck & Co., Inc. Heterocyclic compounds and methods of use thereof
GB0005700D0 (en) * 2000-03-09 2000-05-03 Glaxo Group Ltd Therapy
ES2346513T3 (es) 2000-07-24 2010-10-18 Krenitsky Pharmaceuticals, Inc. 5-alquinil pirimidinas sustituidas que tienen actividad neurotrofica.
CN1257894C (zh) 2000-12-04 2006-05-31 弗·哈夫曼-拉罗切有限公司 作为谷氨酸受体拮抗剂的苯基乙烯基或苯基乙炔基衍生物
GB0103045D0 (en) * 2001-02-07 2001-03-21 Novartis Ag Organic Compounds
IL157491A0 (en) * 2001-02-21 2004-03-28 Nps Pharmeceuticals Inc Heteropolycyclic compounds and pharmaceutical compositions containing the same
US8124625B2 (en) 2001-09-14 2012-02-28 Shionogi & Co., Ltd. Method of enhancing the expression of apolipoprotein AI using olefin derivatives
CA2462442A1 (en) * 2001-10-12 2003-04-24 Warner-Lambert Company Llc Alkyne matrix metalloproteinase inhibitors
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
WO2004014389A1 (en) * 2002-08-13 2004-02-19 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
WO2004024074A2 (en) * 2002-09-13 2004-03-25 Merck & Co., Inc. Fused heterobicyclo substituted phenyl metabotropic glutamate-5 modulators
JP2006513996A (ja) * 2002-10-24 2006-04-27 メルク　エンド　カムパニー　インコーポレーテッド 代謝調節型グルタミン酸受容体結合用トレーサーとしてのアルキン誘導体
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
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
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
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.
EP2028180A1 (en) * 2003-03-04 2009-02-25 ADDEX Pharma S.A. Novel aminopyridine derivatives as mGluR5 antagonists
RU2333200C2 (ru) 2003-03-07 2008-09-10 Астеллас Фарма Инк. Азотсодержащие гетероциклические производные, содержащие 2,6-дизамещенный стирил
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
ATE495168T1 (de) 2003-06-12 2011-01-15 Hoffmann La Roche Heteroarylsubstituierte imidazolderivate als glutamatrezeptorantagonisten
PT1641775E (pt) * 2003-07-03 2009-04-23 Euro Celtique Sa Derivados de 2-piridina-alcino úteis para o tratamento da dor
US7091222B2 (en) * 2003-07-03 2006-08-15 Hoffmann-La Roche Inc. Imidazole derivatives
BRPI0415179A (pt) * 2003-10-07 2006-11-28 Renovis Inc derivados de amida como ligandos de canal de ìon e composições farmacêuticas e métodos de empregar as mesmas
WO2005044265A1 (en) * 2003-10-31 2005-05-19 Astrazeneca Ab Alkynes iii
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
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
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
US7524862B2 (en) 2004-04-14 2009-04-28 Boehringer Ingelheim International Gmbh Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
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
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
KR101057032B1 (ko) * 2004-06-01 2011-08-16 에프. 호프만-라 로슈 아게 Ｍｇｌｕ5 수용체 길항제로서 피리딘-4-일-에틴일-이미다졸및 피라졸
CN1968945A (zh) * 2004-06-16 2007-05-23 惠氏公司 用于抑制β分泌酶的氨基－5,5－二苯基咪唑酮衍生物
RU2006144075A (ru) 2004-06-16 2008-07-27 Вайет (Us) ДИФЕНИЛИМИДАЗОПИРИМИДИН И -ИМИДАЗОЛАМИНЫ КАК ИНГИБИТОРЫ β-СЕКРЕТАЗЫ
GB0413605D0 (en) 2004-06-17 2004-07-21 Addex Pharmaceuticals Sa Novel compounds
EP2264036A1 (en) 2005-01-14 2010-12-22 Wyeth LLC (Formerly Known As Wyeth) Amino-imidazolones for the inhibition of beta-secretase
AU2006205920B2 (en) 2005-01-14 2012-11-15 F. Hoffmann-La Roche Ag Thiazole-4-carboxamide derivatives as mGluR5 antagonists
BRPI0607094A2 (pt) * 2005-02-01 2009-08-04 Wyeth Corp composto da fórmula i; uso do composto para o tratamento de uma doença ou distúrbio associado à atividade excessiva de bace em um paciente que dele necessita; uso do composto para modular a atividade de bace; e composição farmacêutica
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
AU2006222289A1 (en) * 2005-03-04 2006-09-14 F. Hoffmann-La Roche Ag Pyridine-2-carboxamide derivatives as mG1uR5 antagonists
GB0508319D0 (en) * 2005-04-25 2005-06-01 Novartis Ag Organic compounds
AU2006266167A1 (en) * 2005-06-30 2007-01-11 Wyeth Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation
TW200738683A (en) * 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-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
JP2009509957A (ja) * 2005-09-26 2009-03-12 ワイス β−セクレターゼ阻害剤としてのアミノ−５−［４−（ジフルオロメトキシ）フェニル］−５−フェニルイミダゾロン化合物
GB0525068D0 (en) 2005-12-08 2006-01-18 Novartis Ag Organic compounds
WO2007078813A2 (en) * 2005-12-19 2007-07-12 Wyeth 2-AMINO-5-PIPERIDINYLIMIDAZOLONE COMPOUNDS AND USE THEREOF FOR β-SECRETASE MODULATION
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
EP1999109B1 (en) * 2006-03-30 2011-12-28 The Trustees Of The University Of Pennsylvania Styrylpyridine derivatives and their use for binding and imaging amyloid plaques
EA200870514A1 (ru) * 2006-05-08 2009-04-28 Ариад Фармасьютикалз, Инк. Ацетиленовые гетероарильные соединения
US7700606B2 (en) * 2006-08-17 2010-04-20 Wyeth Llc Imidazole amines as inhibitors of β-secretase
EP2064201A2 (en) * 2006-09-21 2009-06-03 Wyeth Indolylalkylpyridin-2-amines for the inhibition of beta-secretase
CA2670116C (en) 2006-11-22 2015-03-10 Seaside Therapeutics, Llc Methods of treating mental retardation, down's syndrome, fragile x syndrome and autism
EP2125779B1 (en) 2006-12-21 2016-04-27 F. Hoffmann-La Roche AG Polymorphs of a mglur5 receptor antagonist
RU2487119C2 (ru) * 2007-02-22 2013-07-10 Зингента Партисипейшнс Аг Производные иминопиридина и их применение в качестве микробиоцидов
JP2010520876A (ja) * 2007-03-09 2010-06-17 アストラゼネカ・アクチエボラーグ ピペラジンおよびピペリジンｍＧｌｕＲ５増強剤
CN101686680B (zh) 2007-03-09 2015-12-09 伊沃泰克美国股份有限公司 作为p2x7调节剂的双环杂芳基化合物及其用途
PE20090160A1 (es) * 2007-03-20 2009-02-11 Wyeth Corp COMPUESTOS AMINO-5-[4-(DIFLUOROMETOXI)FENIL SUSTITUIDO]-5-FENILIMIDAZOLONA COMO INHIBIDORES DE ß-SECRETASA
PE20090617A1 (es) * 2007-03-23 2009-05-08 Wyeth Corp Compuestos amino-5-[-4-(difluorometoxi)fenil]-5-fenilimidazolona para la inhibicion de -secretasa
NZ581817A (en) * 2007-06-03 2012-05-25 Univ Vanderbilt Benzamide mglur5 positive allosteric modulators and methods of making and using same
US8853392B2 (en) * 2007-06-03 2014-10-07 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
BRPI0923476A2 (pt) 2008-12-24 2016-01-19 Astrazeneca Ab composto, métodos para tratar depressão em um ser humano, e grande distúrbio depressivo, e, composição farmacêutica
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
AU2010240200B2 (en) 2009-04-20 2014-03-13 Mitsubishi Tanabe Pharma Corporation Novel thyroid hormone beta receptor agonist
WO2011092293A2 (en) 2010-02-01 2011-08-04 Novartis Ag Cyclohexyl amide derivatives as crf receptor antagonists
WO2011092290A1 (en) 2010-02-01 2011-08-04 Novartis Ag Pyrazolo[5,1b]oxazole derivatives as crf-1 receptor antagonists
WO2011095450A1 (en) 2010-02-02 2011-08-11 Novartis Ag Cyclohexyl amide derivatives as crf receptor antagonists
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
US20110294879A1 (en) 2010-05-28 2011-12-01 Xenoport, Inc. Method of treatment of fragile x syndrome, down's syndrome, autism and related disorders
WO2012009646A1 (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
KR20150003771A (ko) 2012-05-03 2015-01-09 노파르티스 아게 그렐린 수용체 효능제로서의 2,7-디아자-스피로[4.5]데스-7-일 유도체의 l-말레이트 염 및 그의 결정질 형태
WO2014060398A1 (en) * 2012-10-18 2014-04-24 F. Hoffmann-La Roche Ag Ethynyl derivatives as modulators of mglur5 receptor activity
CN104718191B (zh) * 2012-10-18 2016-06-29 霍夫曼-拉罗奇有限公司 作为mglur5受体活性调节剂的乙炔基衍生物
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
SG11201806628UA (en) * 2016-02-03 2018-09-27 Galderma Res & Dev New bi-aromatic propynyl compounds, pharmaceutical and cosmetic compositions containing them 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
WO2019025931A1 (en) 2017-07-31 2019-02-07 Novartis Ag USE OF A MUSSEL FOR REDUCING THE USE OF COCAINE OR FOR PREVENTING A RECHUTE IN THE USE OF COCAINE
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
US11905306B2 (en) 2021-12-21 2024-02-20 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
ES2056983T3 (es) * 1988-03-21 1994-10-16 Boehringer Ingelheim Pharma Compuestos para inhibir la biosintesis de metabolitos de acido araquidonico derivados de lipoxigenasa.
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
JPH11509847A (ja) * 1995-07-31 1999-08-31 ノボ ノルディスク アクティーゼルスカブ ヘテロ環式化合物、それらの調製及び使用
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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CA2295678A1 (en) 1999-01-21
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