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
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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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    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • 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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    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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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  • Pyridine Compounds (AREA)
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EA200200105A 1999-06-30 2000-06-28 СОЕДИНЕНИЯ, МОДУЛИРУЮЩИЕ АКТИВНОСТЬ PPARγ EA004887B1 (ru)

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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)

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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
KR100771286B1 (ko) * 2000-06-28 2007-10-29 암젠 인크 퀴놀리닐 및 벤조티아졸릴 ｐｐａｒ-감마 조절물질
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
IL156445A0 (en) 2001-01-26 2004-01-04 Schering Corp Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
US7071181B2 (en) 2001-01-26 2006-07-04 Schering Corporation Methods and therapeutic combinations for the treatment of diabetes using sterol absorption inhibitors
AR035533A1 (es) 2001-01-26 2004-06-02 Schering Corp Uso de por lo menos un inhibidor de la absorcion de los esteroles o sus sales, solvatos, prodrogas farmaceuticamente aceptables o mezclas de los mismos para la preparacion de un medicamento para el tratamiento de la sitosterolemia, composiciones farmaceuticas, el uso de dichas composiciones para la
EP1911462A3 (en) 2001-01-26 2011-11-30 Schering Corporation Compositions comprising a sterol absorption inhibitor
WO2003005025A1 (en) * 2001-07-03 2003-01-16 Biovitrum Ab Methods for identifying compounds modulating the activity of ppar-gamma
SE0102764D0 (sv) 2001-08-17 2001-08-17 Astrazeneca Ab Compounds
EP1435946B8 (en) 2001-09-14 2013-12-18 Amgen Inc. Linked biaryl compounds
US7053080B2 (en) 2001-09-21 2006-05-30 Schering Corporation Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors
MXPA04002573A (es) 2001-09-21 2004-06-18 Schering Corp Tratamiento de xantoma con derivados de azetidinona como inhibidores de la absorcion de esterol.
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
EP2399903A1 (en) 2002-05-24 2011-12-28 Millennium Pharmaceuticals, Inc. Ccr9 inhibitors and methods of use thereof
WO2004043457A1 (en) 2002-11-06 2004-05-27 Schering Corporation Cholesterol absorptions inhibitors for the treatment of autoimmune disorders
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
US6939885B2 (en) 2002-11-18 2005-09-06 Chemocentryx Aryl sulfonamides
EP1601668B1 (en) 2003-03-07 2008-08-27 Schering Corporation Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholesterolemia
CA2517572C (en) 2003-03-07 2011-12-13 Schering Corporation Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholesterolemia
JP2006519869A (ja) 2003-03-07 2006-08-31 シェーリング　コーポレイション 置換アゼチジノン化合物、置換アゼチジノン化合物を調製するためのプロセス、それらの処方物および使用
US7459442B2 (en) 2003-03-07 2008-12-02 Schering Corporation Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
JP2009513523A (ja) * 2003-07-08 2009-04-02 ノバルティス アクチエンゲゼルシャフト ベンゼンスルホニルアミノ化合物およびそれらを含む医薬組成物
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
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
WO2006020830A2 (en) 2004-08-12 2006-02-23 Amgen Inc. Bisaryl-sulfonamides
CA2614746C (en) 2005-07-09 2011-05-10 Astrazeneca Ab Heteroaryl benzamide derivatives for use as glk activators in the treatment of diabetes
CN101528734B (zh) * 2006-09-21 2013-02-13 皮拉玛生命科学有限公司 治疗代谢障碍的3-氨基吡啶衍生物
TW200820970A (en) * 2006-09-21 2008-05-16 Nicholas Piramal India Ltd Compounds for the treatment of metabolic disorders
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
EP2527360B1 (en) 2007-06-04 2015-10-28 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
US8304441B2 (en) 2007-09-14 2012-11-06 Metabolic Solutions Development Company, Llc Thiazolidinedione analogues for the treatment of metabolic diseases
KR101537830B1 (ko) 2007-09-14 2015-07-17 메타볼릭 솔루션스 디벨롭먼트 컴퍼니, 엘엘씨 고혈압 치료용 티아졸리딘디온 유사체
EP2810951B1 (en) 2008-06-04 2017-03-15 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
EP3241839B1 (en) 2008-07-16 2019-09-04 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
CN102361857B (zh) * 2008-09-26 2015-09-16 默沙东公司 可用作抗糖尿病剂的环状苯并咪唑衍生物
WO2010047982A1 (en) 2008-10-22 2010-04-29 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
JP5557845B2 (ja) 2008-10-31 2014-07-23 メルク・シャープ・アンド・ドーム・コーポレーション 糖尿病用剤として有用な新規環状ベンゾイミダゾール誘導体
EA020017B1 (ru) 2009-04-30 2014-08-29 Новартис Аг Производные имидазола и их применение в качестве модуляторов циклинзависимых киназ
RU2564661C2 (ru) 2009-12-15 2015-10-10 МЕТАБОЛИК СОЛЮШНЗ ДЕВЕЛОПМЕНТ КОМПАНИ, ЭлЭлСи Соли тиазолидиндиона со сниженным сродством к ppar для лечения нарушений обмена веществ
WO2011084459A1 (en) * 2009-12-15 2011-07-14 Metabolic Solutions Development Company Ppar-sparing thiazolidinediones and combinations for the treatment of obesity and other metabolic diseases
US8895596B2 (en) 2010-02-25 2014-11-25 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
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
BR112013021236B1 (pt) 2011-02-25 2021-05-25 Merck Sharp & Dohme Corp composto derivado de benzimidazol, e, composição
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
ES2656292T3 (es) 2012-05-01 2018-02-26 Translatum Medicus Inc. Métodos de tratamiento y diagnóstico de enfermedades oculares que causan ceguera
US9527875B2 (en) 2012-08-02 2016-12-27 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
RU2015140066A (ru) 2013-02-22 2017-03-30 Мерк Шарп И Доум Корп. Противодиабетические бициклические соединения
WO2014139388A1 (en) 2013-03-14 2014-09-18 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
CA2905435A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
CA2905438A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
SI3004138T1 (sl) 2013-06-05 2024-07-31 Bausch Health Ireland Limited Ultra čisti agonisti gvanilat ciklaze C, postopek za njihovo pripravo in uporabo
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
EA201791982A1 (ru) 2015-03-09 2020-02-17 Интекрин Терапьютикс, Инк. Способы лечения неалкогольной жировой болезни печени и/или липодистрофии
JP6902748B2 (ja) * 2016-09-29 2021-07-14 雪印種苗株式会社 植物成長調整剤
US11072602B2 (en) 2016-12-06 2021-07-27 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
WO2018118670A1 (en) 2016-12-20 2018-06-28 Merck Sharp & Dohme Corp. Antidiabetic spirochroman compounds
AU2018249822A1 (en) 2017-04-03 2019-10-31 Coherus Biosciences Inc. PPArgamma agonist for treatment of progressive supranuclear palsy
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
DE3264551D1 (en) * 1981-07-06 1985-08-08 Eastman Kodak Co 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 (https=) * 1994-11-12 1997-12-01 Zeneca Ltd
TWI238064B (en) * 1995-06-20 2005-08-21 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
CA2318731C (en) * 1998-01-29 2012-05-29 Tularik Inc. Ppar-gamma modulators

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

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