EA004887B1 - СОЕДИНЕНИЯ, МОДУЛИРУЮЩИЕ АКТИВНОСТЬ PPARγ - Google Patents

СОЕДИНЕНИЯ, МОДУЛИРУЮЩИЕ АКТИВНОСТЬ PPARγ Download PDF

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EA004887B1
EA004887B1 EA200200105A EA200200105A EA004887B1 EA 004887 B1 EA004887 B1 EA 004887B1 EA 200200105 A EA200200105 A EA 200200105A EA 200200105 A EA200200105 A EA 200200105A EA 004887 B1 EA004887 B1 EA 004887B1
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Eurasian Patent Office
Prior art keywords
alkyl
group
aryl
halogen
heteroalkyl
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EA200200105A
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English (en)
Russian (ru)
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EA200200105A1 (ru
Inventor
Лоренс Р. МакДжи
Джонатан Б. Хауз
Стивен М. Рубенштейн
Ацуси Хагивара
Нобору Фурукава
Хисаси Синкаи
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Туларик Инк.
Джапэн Тобэкоу Инк.
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Publication of EA200200105A1 publication Critical patent/EA200200105A1/ru
Publication of EA004887B1 publication Critical patent/EA004887B1/ru

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    • C07—ORGANIC CHEMISTRY
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    • C07D213/00—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
    • 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
    • C07D213/60—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 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 ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/70—Sulfur atoms
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • C07C311/08—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07C311/21—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07C317/34—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring
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    • C07C323/46—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having at least one of the nitrogen atoms, not being part of nitro or nitroso groups, further bound to other hetero atoms
    • C07C323/49—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having at least one of the nitrogen atoms, not being part of nitro or nitroso groups, further bound to other hetero atoms to sulfur atoms
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    • 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
    • C07D213/60—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 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 ring carbon atoms
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    • C07D213/89—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 with hetero atoms directly attached to the ring nitrogen atom
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  • Quinoline Compounds (AREA)
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  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
EA200200105A 1999-06-30 2000-06-28 СОЕДИНЕНИЯ, МОДУЛИРУЮЩИЕ АКТИВНОСТЬ PPARγ EA004887B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US14167299P 1999-06-30 1999-06-30
PCT/US2000/018178 WO2001000579A1 (en) 1999-06-30 2000-06-28 COMPOUNDS FOR THE MODULATION OF PPARη ACTIVITY

Publications (2)

Publication Number Publication Date
EA200200105A1 EA200200105A1 (ru) 2002-06-27
EA004887B1 true EA004887B1 (ru) 2004-08-26

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Families Citing this family (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6583157B2 (en) 1998-01-29 2003-06-24 Tularik Inc. Quinolinyl and benzothiazolyl modulators
US7041691B1 (en) 1999-06-30 2006-05-09 Amgen Inc. Compounds for the modulation of PPARγ activity
WO2001082916A2 (en) * 2000-05-03 2001-11-08 Tularik Inc. Combination therapeutic compositions and methods of use
BRPI0112115B8 (pt) * 2000-06-28 2021-05-25 Japan Tobacco Inc compostos moduladores ppar-gamma de quinolinil e benzotiazolil
US20030171399A1 (en) 2000-06-28 2003-09-11 Tularik Inc. Quinolinyl and benzothiazolyl modulators
US6982251B2 (en) 2000-12-20 2006-01-03 Schering Corporation Substituted 2-azetidinones useful as hypocholesterolemic agents
US7071181B2 (en) 2001-01-26 2006-07-04 Schering Corporation Methods and therapeutic combinations for the treatment of diabetes using sterol absorption inhibitors
EP1911462A3 (en) 2001-01-26 2011-11-30 Schering Corporation Compositions comprising a sterol absorption inhibitor
RU2756946C2 (ru) 2001-01-26 2021-10-07 Мерк Шарп И Доум Корп. Применение замещенных азетидинонов для лечения ситостеролемии
AU2002247019C1 (en) 2001-01-26 2017-05-11 Organon Llc Combinations of peroxisome proliferator-activated receptor (PPAR) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
WO2003004458A1 (en) * 2001-07-03 2003-01-16 Biovitrum Ab New compounds
SE0102764D0 (sv) 2001-08-17 2001-08-17 Astrazeneca Ab Compounds
BR0212512A (pt) 2001-09-14 2004-10-26 Tularik Inc Composto, composição farmacêutica e métodos para tratar um distúrbio, condição ou doença, elevar os nìveis do colesterol hdl, reduzir os nìveis de triglicerìdeo, tratar diabete, diminuir a resistência à insulina ou diminuir a pressão arterial e modular a ppardelta
US7056906B2 (en) 2001-09-21 2006-06-06 Schering Corporation Combinations of hormone replacement therapy composition(s) and sterol absorption inhibitor(s) and treatments for vascular conditions in post-menopausal women
US7053080B2 (en) 2001-09-21 2006-05-30 Schering Corporation Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors
DE60216300T2 (de) 2001-09-21 2007-06-28 Schering Corp. Behandlung von xanthom mittels azetidinon-derivate als hemmer der sterol absorption
EP2402310A1 (en) 2002-05-24 2012-01-04 Millennium Pharmaceuticals, Inc. CCR9 inhibitors and methods of use thereof
CA2504878A1 (en) 2002-11-06 2004-05-27 Schering Corporation Cholesterol absorption inhibitors for the treatment of demyelination
US7227035B2 (en) 2002-11-18 2007-06-05 Chemocentryx Bis-aryl sulfonamides
US7420055B2 (en) 2002-11-18 2008-09-02 Chemocentryx, Inc. Aryl sulfonamides
US7741519B2 (en) 2007-04-23 2010-06-22 Chemocentryx, Inc. Bis-aryl sulfonamides
CA2500492C (en) 2002-11-18 2010-03-16 Solomon Ungashe Aryl sulfonamides
EP1601668B1 (en) 2003-03-07 2008-08-27 Schering Corporation Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholesterolemia
US7459442B2 (en) 2003-03-07 2008-12-02 Schering Corporation Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
MXPA05009502A (es) 2003-03-07 2005-10-18 Schering Corp Compuestos de azetidinona sustituidos, formulaciones y usos de los mismos para el tratamiento de hipercolesterolemia.
MXPA05009501A (es) 2003-03-07 2005-10-18 Schering Corp Compuestos de azetidinona sustituidos, formulaciones y usos de los mismos para el tratamiento de hipercolesterolemia.
CN100447139C (zh) * 2003-07-08 2008-12-31 诺瓦提斯公司 苯磺酰氨基化合物和含有这些化合物的药物组合物
DE10344223A1 (de) * 2003-09-24 2005-04-21 Merck Patent Gmbh 1,3-Benzoxazolylderivate als Kinase-Inhibitoren
US7223761B2 (en) 2003-10-03 2007-05-29 Amgen Inc. Salts and polymorphs of a potent antidiabetic compound
GB0401334D0 (en) 2004-01-21 2004-02-25 Novartis Ag Organic compounds
EP2305352A1 (en) 2004-04-02 2011-04-06 Merck Sharp & Dohme Corp. 5-alpha-reductase inhibitors for use in the treatment of men with metabolic and anthropometric disorders
US7544702B2 (en) 2004-08-12 2009-06-09 Amgen Inc. Bisaryl-sulfonamides
NZ564608A (en) 2005-07-09 2009-09-25 Astrazeneca Ab Heteroaryl benzamide derivatives for use as GLK activators in the treatment of diabetes
ES2360763T3 (es) * 2006-09-21 2011-06-08 Piramal Life Sciences Limited Derivados de piridina para el tratamiento de desórdenes metabólicos relacionados con la resistencia a la insulina o hiperglucemia.
NZ576197A (en) 2006-09-21 2011-12-22 Piramal Life Sciences Ltd 3 -amino- pyridine derivatives for the treatment of metabolic disorders
DK2170930T3 (da) 2007-06-04 2012-11-05 Synergy Pharmaceuticals Inc Agonister af guanylatcyclase, anvendelige til behandlingen af gastrointestinale sygdomme, inflammation, cancer og andre sygdomme
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
US8304441B2 (en) 2007-09-14 2012-11-06 Metabolic Solutions Development Company, Llc Thiazolidinedione analogues for the treatment of metabolic diseases
WO2009038681A1 (en) 2007-09-14 2009-03-26 Metabolic Solutions Development Company Thiazolidinedione analogues for the treatment of hypertension
EP2328910B1 (en) 2008-06-04 2014-08-06 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
ES2624828T3 (es) 2008-07-16 2017-07-17 Synergy Pharmaceuticals Inc. Agonistas de la guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros
US8394969B2 (en) * 2008-09-26 2013-03-12 Merck Sharp & Dohme Corp. Cyclic benzimidazole derivatives useful as anti-diabetic agents
US8410284B2 (en) 2008-10-22 2013-04-02 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
EP2362731B1 (en) 2008-10-31 2016-04-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
AU2010243353B2 (en) 2009-04-30 2014-09-11 Astex Therapeutics Limited Imidazole derivatives and their use as modulators of Cyclin dependent Kinases
US20120316138A1 (en) * 2009-12-15 2012-12-13 Metabolic Solutions Development Company, Llc Ppar-sparing thiazolidinediones and combinations for the treatment of obesity and other metabolic diseases
NZ600390A (en) 2009-12-15 2013-08-30 Metabolic Solutions Dev Co Llc Ppar-sparing thiazolidinedione salts for the treatment of metabolic diseases
JP2013520502A (ja) 2010-02-25 2013-06-06 メルク・シャープ・エンド・ドーム・コーポレイション 有用な抗糖尿病薬である新規な環状ベンズイミダゾール誘導体
US20130156720A1 (en) 2010-08-27 2013-06-20 Ironwood Pharmaceuticals, Inc. Compositions and methods for treating or preventing metabolic syndrome and related diseases and disorders
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
WO2012040082A2 (en) 2010-09-21 2012-03-29 Intekrin Therapeutics, Inc. Antidiabetic solid pharmaceutical compositions
SG192941A1 (en) 2011-02-25 2013-09-30 Merck Sharp & Dohme Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents
WO2013082106A1 (en) 2011-12-02 2013-06-06 The General Hospital Corporation Differentiation into brown adipocytes
US20130158077A1 (en) 2011-12-19 2013-06-20 Ares Trading S.A. Pharmaceutical compositions
EP3338776A1 (en) 2012-05-01 2018-06-27 Translatum Medicus Inc. Methods for treating and diagnosing blinding eye diseases
WO2014022528A1 (en) 2012-08-02 2014-02-06 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
JP2016516004A (ja) 2013-02-22 2016-06-02 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． 抗糖尿病二環式化合物
EP2970119B1 (en) 2013-03-14 2021-11-03 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
CA2905438A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
US9486494B2 (en) 2013-03-15 2016-11-08 Synergy Pharmaceuticals, Inc. Compositions useful for the treatment of gastrointestinal disorders
JP6606491B2 (ja) 2013-06-05 2019-11-13 シナジー ファーマシューティカルズ インコーポレイテッド グアニル酸シクラーゼｃの超高純度アゴニスト、その作成および使用方法
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
WO2016144862A1 (en) 2015-03-09 2016-09-15 Intekrin Therapeutics, Inc. Methods for the treatment of nonalcoholic fatty liver disease and/or lipodystrophy
JP6902748B2 (ja) * 2016-09-29 2021-07-14 雪印種苗株式会社 植物成長調整剤
WO2018106518A1 (en) 2016-12-06 2018-06-14 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
WO2018118670A1 (en) 2016-12-20 2018-06-28 Merck Sharp & Dohme Corp. Antidiabetic spirochroman compounds
KR20200036808A (ko) 2017-04-03 2020-04-07 코히러스 바이오사이언시스, 인크. 진행성 핵상 마비 치료를 위한 PPARγ 작용제
CN116693433B (zh) * 2023-06-02 2024-04-16 济南悟通生物科技有限公司 一种烷基取代苯硫酚的合成方法

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0069585B1 (en) * 1981-07-06 1985-07-03 EASTMAN KODAK COMPANY (a New Jersey corporation) Color-forming sulfonamidodiphenylamines, photographic elements containing them and corresponding sulfonimide dyes
DE3632329A1 (de) * 1986-09-24 1988-03-31 Bayer Ag Substituierte phenylsulfonamide
JP3894949B2 (ja) * 1993-06-30 2007-03-22 ザ、ウェルカム、ファンデーション、リミテッド 抗アテローム性動脈硬化症ジアリール化合物
TW321649B (enExample) * 1994-11-12 1997-12-01 Zeneca Ltd
TW438587B (en) * 1995-06-20 2001-06-07 Takeda Chemical Industries Ltd A pharmaceutical composition for prophylaxis and treatment of diabetes
GB9604242D0 (en) * 1996-02-28 1996-05-01 Glaxo Wellcome Inc Chemical compounds
JP3243733B2 (ja) * 1996-08-07 2002-01-07 雪印乳業株式会社 新規イソキノリン誘導体
ZA986732B (en) * 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitiors of tyrosine kinases
US6284923B1 (en) * 1997-08-22 2001-09-04 Tularik Inc Substituted benzene compounds as antiproliferative and cholesterol lowering action
US6200995B1 (en) * 1998-01-29 2001-03-13 Tularik Inc. PPAR-γ modulators

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JP2003503387A (ja) 2003-01-28
MX339420B (es) 2016-05-25
CA2377309C (en) 2010-11-23
HK1043369B (en) 2014-06-13
CN1368961A (zh) 2002-09-11
IL147308A (en) 2015-06-30
DK1192137T3 (da) 2013-11-11
CA2377309A1 (en) 2001-01-04
ZA200200057B (en) 2003-03-19
WO2001000579A1 (en) 2001-01-04
MXPA01013199A (es) 2003-08-20
HK1043369A1 (en) 2002-09-13
JP4295458B2 (ja) 2009-07-15
ES2437103T3 (es) 2014-01-08
EP1192137A1 (en) 2002-04-03
SG148834A1 (en) 2009-01-29
NZ516455A (en) 2004-03-26
EA200200105A1 (ru) 2002-06-27
CN1171872C (zh) 2004-10-20
EP1192137B1 (en) 2013-10-23
IL147308A0 (en) 2002-08-14

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