EA200501376A1 - DERIVATIVES OF 1,2,4-SUBSTITUTED 1,2,3,4-TETRAHYDRO- and 1,2-DIHYDROCHINOLINES AND 1,2,3,4-TETRAHYDROCHINOXALINE AS AN INHIBITORS CETR FOR THE TREATMENT OF ATHEROSCLEROSIS AND FAT - Google Patents

DERIVATIVES OF 1,2,4-SUBSTITUTED 1,2,3,4-TETRAHYDRO- and 1,2-DIHYDROCHINOLINES AND 1,2,3,4-TETRAHYDROCHINOXALINE AS AN INHIBITORS CETR FOR THE TREATMENT OF ATHEROSCLEROSIS AND FAT

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Publication number
EA200501376A1
EA200501376A1 EA200501376A EA200501376A EA200501376A1 EA 200501376 A1 EA200501376 A1 EA 200501376A1 EA 200501376 A EA200501376 A EA 200501376A EA 200501376 A EA200501376 A EA 200501376A EA 200501376 A1 EA200501376 A1 EA 200501376A1
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EA
Eurasian Patent Office
Prior art keywords
atherosclerosis
levels
cholesterol
tetrahydrochinoxaline
dihydrochinolines
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EA200501376A
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Russian (ru)
Inventor
Джордж Чанг
Мари Тереза Дидиук
Яри Илмари Финнеман
Рави Шанкер Гаригипати
Райан Майкл Келли
Дэвид Остен Перри
Роджер Бенджамин Руггери
Брюс Майкл Бекле
Майкл П. Полластри
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Пфайзер Продактс Инк.
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Publication of EA200501376A1 publication Critical patent/EA200501376A1/en

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Abstract

Соединения хинолина и хиноксалина формул I и III, где заместители имеют указанные в пп.1 и 15 значения, фармацевтические композиции, содержащие указанные соединения, и применение указанных соединений для повышения уровней содержания некоторых липидов в плазме, включая липопротеин-холестерин высокой плотности, и для снижения уровней содержания некоторых других липидов в плазме, таких как LDL-холестерин и триглицериды, и соответственно для лечения заболеваний, которые обостряются из-за низких уровней HDL-холестерина и/или высоких уровней LDL-холестерина и триглицеридов, таких как атеросклероз и сердечно-сосудистые заболевания у некоторых млекопитающих, включая людей.The quinoline and quinoxaline compounds of formulas I and III, where the substituents have the meanings indicated in claims 1 and 15, pharmaceutical compositions containing these compounds, and the use of these compounds to increase the levels of certain plasma lipids, including high-density lipoprotein-cholesterol, and for lowering levels of some other plasma lipids, such as LDL-cholesterol and triglycerides, and accordingly for treating diseases that are exacerbated by low levels of HDL-cholesterol and / or high levels of LDL-choles sterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.

EA200501376A 2003-03-28 2004-03-15 DERIVATIVES OF 1,2,4-SUBSTITUTED 1,2,3,4-TETRAHYDRO- and 1,2-DIHYDROCHINOLINES AND 1,2,3,4-TETRAHYDROCHINOXALINE AS AN INHIBITORS CETR FOR THE TREATMENT OF ATHEROSCLEROSIS AND FAT EA200501376A1 (en)

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US45827403P 2003-03-28 2003-03-28
PCT/IB2004/000836 WO2004085401A1 (en) 2003-03-28 2004-03-15 1,2,4-substituted 1,2,3,4-tetrahydro-and 1,2 dihydro-quinoline and 1,2,3,4-tetrahydro-quinoxaline derivatives as cetp inhibitors for the treatment of atherosclerosis and obesity

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EP (1) EP1622872A1 (en)
JP (1) JP2006521344A (en)
KR (1) KR100729883B1 (en)
CN (1) CN1795177A (en)
AR (1) AR044507A1 (en)
AU (1) AU2004224082A1 (en)
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CA (1) CA2520405A1 (en)
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EC (1) ECSP056040A (en)
GT (1) GT200400050A (en)
HR (1) HRP20050859A2 (en)
MA (1) MA27828A1 (en)
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TN (1) TNSN05243A1 (en)
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UY (1) UY28243A1 (en)
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Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1599468T3 (en) 2003-01-14 2008-02-04 Arena Pharm Inc 1,2,3-Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prevention and treatment of disorders associated therewith such as diabetes and hyperglycemia
ES2770035T3 (en) 2003-04-11 2020-06-30 Ptc Therapeutics Inc 1,2,4-Oxadiazole benzoic acid compound and its use for senseless suppression and treatment of diseases
EP2287166A3 (en) 2003-07-14 2011-06-22 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
WO2006033001A1 (en) * 2004-09-23 2006-03-30 Pfizer Products Inc. Quinoline compounds
WO2006033004A1 (en) * 2004-09-23 2006-03-30 Pfizer Products Inc. Quinoline compounds as cetp inhibitors
AR051780A1 (en) * 2004-11-29 2007-02-07 Japan Tobacco Inc FUSIONED RING COMPOUNDS CONTAINING NITROGEN AND USING THEMSELVES
MY148521A (en) 2005-01-10 2013-04-30 Arena Pharm Inc Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto
UA90706C2 (en) * 2005-02-24 2010-05-25 Милленниум Фармасьютикалз, Инк. Pgd2 receptor antagonists for the treatment of inflammatory diseases
US7888376B2 (en) * 2005-11-23 2011-02-15 Bristol-Myers Squibb Company Heterocyclic CETP inhibitors
UY30118A1 (en) * 2006-01-31 2007-06-29 Tanabe Seiyaku Co AMIS TRISUSTITUDE COMPUTER
US7745477B2 (en) * 2006-02-07 2010-06-29 Hoffman-La Roche Inc. Heteroaryl and benzyl amide compounds
UY30244A1 (en) 2006-03-30 2007-11-30 Tanabe Seiyaku Co A PROCESS TO PREPARE DERIVATIVES OF TETRAHYDROQUINOLINE
WO2007128568A1 (en) 2006-05-10 2007-11-15 Novartis Ag Bicyclic derivatives as cetp inhibitors
JP4108729B2 (en) * 2006-05-26 2008-06-25 日本たばこ産業株式会社 Nitrogen-containing fused ring compound-containing pharmaceutical composition
US20080305169A1 (en) * 2006-05-26 2008-12-11 Japan Tobacco Inc. Pharmaceutical Compositions Comprising Nitrogen-Containing Fused Ring Coumpounds
US20100076021A1 (en) * 2006-11-15 2010-03-25 Hidetomo Imase Organic Compounds
JP4846769B2 (en) * 2007-07-30 2011-12-28 田辺三菱製薬株式会社 Pharmaceutical composition
WO2009029632A1 (en) 2007-08-27 2009-03-05 Helicon Therapeutics, Inc. Therapeutic isoxazole compounds
US8309734B2 (en) * 2008-10-29 2012-11-13 Hoffmann-La Roche Inc. Substituted pyridines as GPBAR1 agonists
US8420647B2 (en) 2010-01-21 2013-04-16 Hoffmann-La Roche Inc. 4-phenoxy-nicotinamide or 4-phenoxy-pyrimidine-5-carboxamide compounds
SG188548A1 (en) 2010-09-22 2013-04-30 Arena Pharm Inc Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2015074064A2 (en) 2013-11-18 2015-05-21 Bair Kenneth W Tetrahydroquinoline compositions as bet bromodomain inhibitors
EP3071205B1 (en) * 2013-11-18 2020-02-05 Forma Therapeutics, Inc. Benzopiperazine compositions as bet bromodomain inhibitors
KR102497273B1 (en) 2014-03-06 2023-02-07 피티씨 테라퓨틱스, 인크. Pharmaceutical compositions and salts of a 1,2,4-oxadiazole benzoic acid
EP3242666A1 (en) 2015-01-06 2017-11-15 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
JP6838744B2 (en) 2015-06-22 2021-03-03 アリーナ ファーマシューティカルズ, インコーポレイテッド (R) -2- (7- (4-cyclopentyl-3- (trifluoromethyl) benzyloxy) -1,2,3,4-tetrahydrocyclopenta [b] indole-for use in S1P1 receptor-related disorders Crystalline L-arginine salt of 3-yl) acetic acid (Compound 1)
CA3003132A1 (en) 2015-10-30 2017-05-04 Ptc Therapeutics, Inc. Methods for treating epilepsy
KR20190116416A (en) 2017-02-16 2019-10-14 아레나 파마슈티칼스, 인크. Compounds and Methods for Treating Primary Bile Cholangitis
CN110452183B (en) * 2019-09-04 2023-03-14 中国科学院上海有机化学研究所 Preparation method of chiral heterocyclic compound
CN111440162A (en) * 2020-04-01 2020-07-24 邱曲真 Thiazole dihydronaphthalene derivative and application thereof in metabolic diseases
CN114656406B (en) * 2022-01-25 2023-09-05 阿里生物新材料(常州)有限公司 Synthesis method of 2-fluoropyrimidine-4-carboxylic acid

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE351464C (en) * 1917-12-18 1922-04-07 Chemische Werke Grenzach Aktie Process for the preparation of derivatives of a hydrogenated 2-phenylquinoline-4-carboxylic acid
NZ300739A (en) * 1994-12-22 2000-05-26 Ligand Pharm Inc Steroid receptor modulator compounds
JP2001503411A (en) * 1996-10-28 2001-03-13 ディパートメント オブ ジ アーミー,ユー.エス.ガバメント Compounds, compositions and methods for the treatment of antibiotic resistant infections
US6103905A (en) * 1997-06-19 2000-08-15 Sepracor, Inc. Quinoline-indole antimicrobial agents, uses and compositions related thereto
ES2201674T3 (en) * 1998-01-26 2004-03-16 Smithkline Beecham Plc DERIVATIVES OF QUINOLINA WITH ANTIBACTERIAL PROPERTIES.
GT199900147A (en) * 1998-09-17 1999-09-06 1, 2, 3, 4- TETRAHIDROQUINOLINAS 2-SUBSTITUTED 4-AMINO SUBSTITUTED.
CO5271716A1 (en) * 1999-11-30 2003-04-30 Pfizer Prod Inc CRYSTALS OF 4- CARBOXAMINE 1,2,3,4-TETRAHYDROQUINOLINE 2- REPLACED

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