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WO2003035602A1 - Modulateurs lipidiques - Google Patents

Modulateurs lipidiques Download PDF

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Publication number
WO2003035602A1
WO2003035602A1 PCT/JP2002/011068 JP0211068W WO03035602A1 WO 2003035602 A1 WO2003035602 A1 WO 2003035602A1 JP 0211068 W JP0211068 W JP 0211068W WO 03035602 A1 WO03035602 A1 WO 03035602A1
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WO
WIPO (PCT)
Prior art keywords
optionally substituted
preventives
remedies
lipid
substituted aryl
Prior art date
Application number
PCT/JP2002/011068
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English (en)
Japanese (ja)
Inventor
Yoshiya Amemiya
Kenji Wakabayashi
Sachiko Takaishi
Ken Kitayama
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Sankyo Company, Limited
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Publication date
Application filed by Sankyo Company, Limited filed Critical Sankyo Company, Limited
Publication of WO2003035602A1 publication Critical patent/WO2003035602A1/fr

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    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26—Sulfur atoms
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
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    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
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Abstract

L'invention concerne des composés représentés par la formule générale (I) qui présentent une activité de modulation de PPAR-η (I), dans laquelle A représente éventuellement aryle substitué ; B représente aryle éventuellement substitué, cycloalkyle éventuellement substitué ou un groupe hétérocyclique éventuellement substitué ; Ra représente H ou alkyle ; X représente une liaison, O, S, CH2, CO, NH, SO2NH, NHSO2, CONH, NHCO ou OCH2 ; et n vaut 0 ou 1. En raison de leur capacité à inhiber l'accélération de la différentiation adipocytaire, à réguler les lipides et à stimuler la formation et la différentiation des ostéoblastes, ces composés sont utiles pour le traitement ou la prévention (modulateurs lipidiques) de maladies induites par des erreurs du métabolisme lipidique ou de l'ostéoporose, du diabète, etc.
PCT/JP2002/011068 2001-10-25 2002-10-24 Modulateurs lipidiques WO2003035602A1 (fr)

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US7241761B2 (en) 2004-12-09 2007-07-10 Hoffmann-La Roche Inc. Phenyl-piperazine methanone derivatives, substituted by heterocyclic groups
JP2008512474A (ja) * 2004-09-09 2008-04-24 ロマーク ラボラトリース，エル．シー． ハロゲン化されたベンズアミド誘導体
US7375226B2 (en) 2004-12-15 2008-05-20 Hoffman-La Roche Inc. Bi- and tricyclic substituted phenyl methanones
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US7442710B2 (en) 2005-01-26 2008-10-28 Hoffman-La Roche Inc. Substituted phenyl methanones
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JP2009531365A (ja) * 2006-03-30 2009-09-03 ノバルティス アクチエンゲゼルシャフト セラミドキナーゼ調節
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JP2009541367A (ja) * 2006-06-27 2009-11-26 インスティテュート オブ ファーマコロジー アンド トキシコロジー アカデミー オブ ミリタリー メディカル サイエンシス ピーエルエイ ２，４，５−三置換チアゾール化合物、それを含有する医薬組成物、並びにその調製及び医学的使用
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US7777036B2 (en) 2004-09-20 2010-08-17 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as therapeutic agents
US7790763B2 (en) 2005-01-18 2010-09-07 Hoffmann-La Roche Inc. Substituted phenyl methanone derivatives
US7829712B2 (en) 2004-09-20 2010-11-09 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-CoA-desaturase
US7919496B2 (en) 2004-09-20 2011-04-05 Xenon Pharmaceuticals Inc. Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-CoA desaturase enzymes
EP2305352A1 (fr) 2004-04-02 2011-04-06 Merck Sharp & Dohme Corp. Inhibiteurs de la 5-alpha-reductase pour le traitement d'hommes aux troubles métaboliques et anthropométriques
US7951805B2 (en) 2004-09-20 2011-05-31 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as mediators of stearoyl-CoA desaturase
WO2011069038A2 (fr) 2009-12-03 2011-06-09 Synergy Pharmaceuticals, Inc. Agonistes de la guanylate cyclase utiles dans le traitement de l'hypercholestérolémie, de l'athérosclérose, d'une coronaropathie, des calculs biliaires, de l'obésité et d'autres maladies cardiovasculaires
US20110152323A1 (en) * 2008-06-20 2011-06-23 Jiangsu Goworth Investment Co. Ltd Histone deacetylase inhibitors and uses thereof
US8067638B2 (en) 2005-06-21 2011-11-29 Mitsui Chemicals, Inc. Amide derivative and insecticide containing the same
US8071603B2 (en) 2004-09-20 2011-12-06 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
WO2012027331A1 (fr) 2010-08-27 2012-03-01 Ironwood Pharmaceuticals, Inc. Compositions et procédés pour traiter ou prévenir un syndrome métabolique et des maladies et troubles associés
US8188277B2 (en) 2004-08-06 2012-05-29 Otsuka Pharmaceutical Co., Ltd. Aromatic compounds for suppressing the generation of collagen
US8236826B2 (en) 2005-12-05 2012-08-07 Otsuka Pharmaceutical Co., Ltd. Diarylether derivatives as antitumor agents
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US8541457B2 (en) 2005-06-03 2013-09-24 Xenon Pharmaceuticals Inc. Aminothiazole derivatives as human stearoyl-CoA desaturase inhibitors
WO2014151200A2 (fr) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions utiles pour le traitement de troubles gastro-intestinaux
WO2014151206A1 (fr) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Agonistes de la guanylate cyclase et leurs utilisations
EP2810951A2 (fr) 2008-06-04 2014-12-10 Synergy Pharmaceuticals Inc. Agonistes de guanylate cyclase utile dans le traitement de troubles gastro-intestinaux, d'une inflammation, d'un cancer et d'autres troubles
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EP3241839A1 (fr) 2008-07-16 2017-11-08 Synergy Pharmaceuticals Inc. Agonistes de guanylate cyclase utiles pour le traitement de troubles gastro-intestinaux, inflammatoires, cancéreux et autres

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US7425641B2 (en) 1999-08-07 2008-09-16 Boehringer Ingelheim Pharma Kg Carboxylic acid amides, the preparation thereof and their use as pharmaceutical compositions
RU2355683C2 (ru) * 2003-09-09 2009-05-20 Ф.Хоффманн-Ля Рош Аг Производные 1-бензоилпиперазина в качестве ингибиторов поглощения глицина для лечения психозов
KR100774621B1 (ko) * 2003-09-09 2007-11-14 에프. 호프만-라 로슈 아게 정신병 치료용의 글라이신 섭취 억제제로서의1-벤조일-피페라진 유도체
WO2005023261A1 (fr) * 2003-09-09 2005-03-17 F. Hoffmann-La Roche Ag Derives de 1-benzoyl-piperazine comme inhibiteurs du recaptage de la glycine pour le traitement de psychoses
AU2004269892B2 (en) * 2003-09-09 2010-03-11 F. Hoffmann-La Roche Ag 1-benzoyl-piperazine derivatives as glycine uptake inhibitors for the treatment of psychoses
US7462617B2 (en) 2003-09-09 2008-12-09 Hoffmann-La Roche Inc. Substituted acylpiperazine derivatives
CN101906053B (zh) * 2004-01-28 2012-11-21 三井化学株式会社 酰胺衍生物
EP2305352A1 (fr) 2004-04-02 2011-04-06 Merck Sharp & Dohme Corp. Inhibiteurs de la 5-alpha-reductase pour le traitement d'hommes aux troubles métaboliques et anthropométriques
US8188277B2 (en) 2004-08-06 2012-05-29 Otsuka Pharmaceutical Co., Ltd. Aromatic compounds for suppressing the generation of collagen
JP2008512474A (ja) * 2004-09-09 2008-04-24 ロマーク ラボラトリース，エル．シー． ハロゲン化されたベンズアミド誘導体
US7767677B2 (en) 2004-09-20 2010-08-03 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
US7829712B2 (en) 2004-09-20 2010-11-09 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-CoA-desaturase
US8071603B2 (en) 2004-09-20 2011-12-06 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
US7592343B2 (en) 2004-09-20 2009-09-22 Xenon Pharmaceuticals Inc. Pyridazine-piperazine compounds and their use as stearoyl-CoA desaturase inhibitors
US8026360B2 (en) 2004-09-20 2011-09-27 Xenon Pharmaceuticals Inc. Substituted pyridazines as stearoyl-CoA desaturase inhibitors
US7951805B2 (en) 2004-09-20 2011-05-31 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as mediators of stearoyl-CoA desaturase
US7777036B2 (en) 2004-09-20 2010-08-17 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as therapeutic agents
US7919496B2 (en) 2004-09-20 2011-04-05 Xenon Pharmaceuticals Inc. Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-CoA desaturase enzymes
US7429585B2 (en) 2004-12-09 2008-09-30 Hoffmann-La Roche Phenyl-piperazine methanone derivatives, substituted by heterocyclic groups
US7241761B2 (en) 2004-12-09 2007-07-10 Hoffmann-La Roche Inc. Phenyl-piperazine methanone derivatives, substituted by heterocyclic groups
US7375226B2 (en) 2004-12-15 2008-05-20 Hoffman-La Roche Inc. Bi- and tricyclic substituted phenyl methanones
US7485637B2 (en) 2005-01-04 2009-02-03 Hoffmann-La Roche Inc. Benzoyl-tetrahydropiperidine derivatives
US7220744B2 (en) 2005-01-07 2007-05-22 Hoffman-La Roche Inc. Monocyclic substituted phenyl methanones
US7790763B2 (en) 2005-01-18 2010-09-07 Hoffmann-La Roche Inc. Substituted phenyl methanone derivatives
US7442710B2 (en) 2005-01-26 2008-10-28 Hoffman-La Roche Inc. Substituted phenyl methanones
US7557114B2 (en) 2005-02-07 2009-07-07 Hoffman-La Roche Inc. Heterocyclic-substituted phenyl methanones
US8188139B2 (en) 2005-02-07 2012-05-29 Hoffman-La Roche Inc. Heterocyclic-substituted phenyl methanones
US8541457B2 (en) 2005-06-03 2013-09-24 Xenon Pharmaceuticals Inc. Aminothiazole derivatives as human stearoyl-CoA desaturase inhibitors
US8067638B2 (en) 2005-06-21 2011-11-29 Mitsui Chemicals, Inc. Amide derivative and insecticide containing the same
US8236826B2 (en) 2005-12-05 2012-08-07 Otsuka Pharmaceutical Co., Ltd. Diarylether derivatives as antitumor agents
JP2009531365A (ja) * 2006-03-30 2009-09-03 ノバルティス アクチエンゲゼルシャフト セラミドキナーゼ調節
US8053581B2 (en) 2006-06-27 2011-11-08 Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.C. China Trisubstituted thiazole compounds, preparations methods, pharmaceutical compositions and medicals uses thereof
JP2009541367A (ja) * 2006-06-27 2009-11-26 インスティテュート オブ ファーマコロジー アンド トキシコロジー アカデミー オブ ミリタリー メディカル サイエンシス ピーエルエイ ２，４，５−三置換チアゾール化合物、それを含有する医薬組成物、並びにその調製及び医学的使用
EP2042494A4 (fr) * 2006-06-27 2011-06-29 Inst Pharm & Toxicology Amms Composés de thiazole 2,4,5-trisubstitués, méthodes de préparation, compositions pharmaceutiques et leurs utilisations à des fins médicales
US8263599B2 (en) 2006-10-02 2012-09-11 Otsuka Pharmaceutical Co., Ltd. STAT3/5 activation inhibitor
EP2998314A1 (fr) 2007-06-04 2016-03-23 Synergy Pharmaceuticals Inc. Agonistes de guanylase cyclase utiles pour le traitement de troubles gastro-intestinaux, d'inflammation, de cancer et d'autres troubles
RU2364597C1 (ru) * 2007-12-14 2009-08-20 Андрей Александрович Иващенко ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ Hh-СИГНАЛЬНОГО КАСКАДА, ЛЕКАРСТВЕННЫЕ КОМПОЗИЦИИ НА ИХ ОСНОВЕ И СПОСОБ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ, СВЯЗАННЫХ С АББЕРАНТНОЙ АКТИВНОСТЬЮ Hh СИГНАЛЬНОЙ СИСТЕМЫ
EP2810951A2 (fr) 2008-06-04 2014-12-10 Synergy Pharmaceuticals Inc. Agonistes de guanylate cyclase utile dans le traitement de troubles gastro-intestinaux, d'une inflammation, d'un cancer et d'autres troubles
US20110152323A1 (en) * 2008-06-20 2011-06-23 Jiangsu Goworth Investment Co. Ltd Histone deacetylase inhibitors and uses thereof
US8889876B2 (en) * 2008-06-20 2014-11-18 Jiangsu Hengyi Pharmaceutical Co., Ltd. Histone deacetylase inhibitors and uses thereof
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