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WO2003035602A1 - Lipid modulators - Google Patents

Lipid modulators 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
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/JP2002/011068
Other languages
French (fr)
Japanese (ja)
Inventor
Yoshiya Amemiya
Kenji Wakabayashi
Sachiko Takaishi
Ken Kitayama
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sankyo Co Ltd
Original Assignee
Sankyo Co Ltd
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
Application filed by Sankyo Co Ltd filed Critical Sankyo Co Ltd
Publication of WO2003035602A1 publication Critical patent/WO2003035602A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • 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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    • A61K31/16—Amides, e.g. hydroxamic acids
    • 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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    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • C—CHEMISTRY; METALLURGY
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    • 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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    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/22—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
    • C07D311/24—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
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    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
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Abstract

Compounds represented by the following general formula (I) and which have a PPARϜ modulator activity: (I) wherein A represents optionally substituted aryl; B represents optionally substituted aryl, optionally substituted cycloalkyl or an optionally substituted heterocyclic group; Ra represents H or alkyl; X represents a bond, O, S, CH2, CO, NH, SO2NH, NHSO2, CONH, NHCO or OCH2; and n is 0 or 1. Because of having effects of inhibiting the acceleration of adipocyte differentiation, controlling lipids and promoting the formation and differentiation of osteoblasts, these compounds are useful as remedies or preventives (lipid modulators) for diseases based on lipid metabolic errors and remedies or preventives for osteoporosis, diabetes and so on.
PCT/JP2002/011068 2001-10-25 2002-10-24 Lipid modulators Ceased WO2003035602A1 (en)

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US7220744B2 (en) 2005-01-07 2007-05-22 Hoffman-La Roche Inc. Monocyclic substituted phenyl methanones
US7241761B2 (en) 2004-12-09 2007-07-10 Hoffmann-La Roche Inc. Phenyl-piperazine methanone derivatives, substituted by heterocyclic groups
JP2008512474A (en) * 2004-09-09 2008-04-24 ロマーク ラボラトリース，エル．シー． Halogenated benzamide derivatives
US7375226B2 (en) 2004-12-15 2008-05-20 Hoffman-La Roche Inc. Bi- and tricyclic substituted phenyl methanones
US7425641B2 (en) 1999-08-07 2008-09-16 Boehringer Ingelheim Pharma Kg Carboxylic acid amides, the preparation thereof and their use as pharmaceutical compositions
US7442710B2 (en) 2005-01-26 2008-10-28 Hoffman-La Roche Inc. Substituted phenyl methanones
US7485637B2 (en) 2005-01-04 2009-02-03 Hoffmann-La Roche Inc. Benzoyl-tetrahydropiperidine derivatives
US7557114B2 (en) 2005-02-07 2009-07-07 Hoffman-La Roche Inc. Heterocyclic-substituted phenyl methanones
RU2364597C1 (en) * 2007-12-14 2009-08-20 Андрей Александрович Иващенко HETEROCYCLIC INHIBITORS OF Hh-SYGNAL CASCADE, BASED ON THEM MEDICINAL COMPOSITIONS AND METHOD OF TREATING DISEASES INDUCED BY ABBARANT ACTIVITY OF Hh-SIGNAL SYSTEM
JP2009531365A (en) * 2006-03-30 2009-09-03 ノバルティス アクチエンゲゼルシャフト Ceramide kinase regulation
US7592343B2 (en) 2004-09-20 2009-09-22 Xenon Pharmaceuticals Inc. Pyridazine-piperazine compounds and their use as stearoyl-CoA desaturase inhibitors
JP2009541367A (en) * 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-Trisubstituted thiazole compounds, pharmaceutical compositions containing them, and their preparation and medical use
US7767677B2 (en) 2004-09-20 2010-08-03 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
US7777036B2 (en) 2004-09-20 2010-08-17 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as therapeutic agents
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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
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US20110152323A1 (en) * 2008-06-20 2011-06-23 Jiangsu Goworth Investment Co. Ltd Histone deacetylase inhibitors and uses thereof
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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
US8263599B2 (en) 2006-10-02 2012-09-11 Otsuka Pharmaceutical Co., Ltd. STAT3/5 activation inhibitor
CN101906053B (en) * 2004-01-28 2012-11-21 三井化学株式会社 Amide derivatives
WO2013138352A1 (en) 2012-03-15 2013-09-19 Synergy Pharmaceuticals Inc. Formulations of guanylate cyclase c agonists and methods of use
US8541457B2 (en) 2005-06-03 2013-09-24 Xenon Pharmaceuticals Inc. Aminothiazole derivatives as human stearoyl-CoA desaturase inhibitors
WO2014151206A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
WO2014151200A2 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
EP2810951A2 (en) 2008-06-04 2014-12-10 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
WO2014197720A2 (en) 2013-06-05 2014-12-11 Synergy Pharmaceuticals, Inc. Ultra-pure agonists of guanylate cyclase c, method of making and using same
US9078899B2 (en) 2013-01-10 2015-07-14 Gruenenthal Gmbh Pyrazolyl-based carboxamides II
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EP2998314A1 (en) 2007-06-04 2016-03-23 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
EP3241839A1 (en) 2008-07-16 2017-11-08 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders

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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 (en) * 2003-09-09 2009-05-20 Ф.Хоффманн-Ля Рош Аг 1-benzoylpiperazin derivatives as glycine absorption inhibitors in psychosis treatment
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
KR100774621B1 (en) * 2003-09-09 2007-11-14 에프. 호프만-라 로슈 아게 1-benzoyl-piperazine derivatives as glycine uptake inhibitors for the treatment of psychoses
WO2005023261A1 (en) * 2003-09-09 2005-03-17 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
CN100522171C (en) * 2003-09-09 2009-08-05 弗·哈夫曼-拉罗切有限公司 1-Benzoylpiperazine derivatives as glycine uptake inhibitors for the treatment of psychosis
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US7919496B2 (en) 2004-09-20 2011-04-05 Xenon Pharmaceuticals Inc. Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-CoA desaturase enzymes
US7777036B2 (en) 2004-09-20 2010-08-17 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as therapeutic agents
US7829712B2 (en) 2004-09-20 2010-11-09 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-CoA-desaturase
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US7220744B2 (en) 2005-01-07 2007-05-22 Hoffman-La Roche Inc. Monocyclic substituted phenyl methanones
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US8067638B2 (en) 2005-06-21 2011-11-29 Mitsui Chemicals, Inc. Amide derivative and insecticide containing the same
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JP2009541367A (en) * 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-Trisubstituted thiazole compounds, pharmaceutical compositions containing them, and their preparation and medical use
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
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US9078899B2 (en) 2013-01-10 2015-07-14 Gruenenthal Gmbh Pyrazolyl-based carboxamides II
US9206136B2 (en) 2013-01-10 2015-12-08 Grünenthal GmbH Pyrazolyl-based carboxamides I
WO2014151200A2 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
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