PE20040190A1 - Tiazoles y oxazoles sustituidos que modulan la actividad de ppar - Google Patents
Tiazoles y oxazoles sustituidos que modulan la actividad de pparInfo
- Publication number
- PE20040190A1 PE20040190A1 PE2003000213A PE2003000213A PE20040190A1 PE 20040190 A1 PE20040190 A1 PE 20040190A1 PE 2003000213 A PE2003000213 A PE 2003000213A PE 2003000213 A PE2003000213 A PE 2003000213A PE 20040190 A1 PE20040190 A1 PE 20040190A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- aryl
- members
- forming
- ring
- Prior art date
Links
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 title abstract 2
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 title abstract 2
- 230000000694 effects Effects 0.000 title abstract 2
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- -1 4-TRIFLUORomethyl-PHENYL Chemical class 0.000 abstract 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 abstract 1
- 208000031226 Hyperlipidaemia Diseases 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical class O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 150000002430 hydrocarbons Chemical group 0.000 abstract 1
- 201000001421 hyperglycemia Diseases 0.000 abstract 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 abstract 1
- 201000008980 hyperinsulinism Diseases 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 150000002916 oxazoles Chemical class 0.000 abstract 1
- 150000003557 thiazoles Chemical class 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D277/26—Radicals substituted by sulfur atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Steroid Compounds (AREA)
Abstract
SE REFIERE A COMPUESTOS TIAZOLES Y OXAZOLES SUSTITUIDOS DE LA FORMULA I DONDE V1 ES UNA CADENA DE HIDROCARBUROS QUE PUEDE TENER HETEROATOMOS DE 3-6 ATOMOS, EN LA QUE EL C1 ESTA CONECTADO AL C2, FORMANDO UN ANILLO DE 5-8 MIEMBROS DONDE -X2-(CH2)n-CO2, ESTA COMO SUSTITUYENTE; X0 Y X1 ES O O S; X2 ES O, S, NR4 O ESTA AUSENTE; Ar1 ES ARILO O HETEROARILO; R1,R2,R3 ES H, ALQUILO INFERIOR, ALCOXI INFERIOR, TIOALCOXI INFERIOR, -O(CH2)pCF3, HALOGENO, NITRO, CIANO, -OH, -SH, CF3, S(O)pARILO, -(CH2)mOR4, -CH2)mNR5R6, ENTRE OTROS, O R1 Y R2 ESTAN UNIDAS FORMANDO UN ANILLO HETEROCICLOALQUILICO O CICLOALQUILICO; R4 ES H, ALQUILO, ALQUENILO, ALQUINILO O ARILO; R5 Y R6 SON H, ALQUILO, ALQUENILO, ALQUINILO, CICLOALQUILO, SO2 ALQUILO O SO2 ARILO, O ESTAN UNIDOS FORMANDO UN ANILLO DE 4-7 MIEMBROS CON 0-3 HETEROATOMOS; m ES 0-5; n ES 0-5 Y p ES 0-2. SON COMPUESTOS PREFERIDOS: ACIDO 5-[4-METIL-2-(4-TRIFLUOROMETIL-FENIL)-TIAZOL-5-ILMETILSULFANIL]-INDAN-2-CARBOXILICO, ACIDO {5-[4-METIL-2-(4-TRIFLUOROMETIL-FENIL)-TIAZOL-5-ILMETILSULFANIL]-INDAN-2-IL}-ACETICO,ENTRE OTROS.TAMBIEN SE REFIERE A METODOS PARA PREPARACION.SON COMPUESTOS QUE MODULAN LA ACTIVIDAD DE PPAR Y SE PUEDEN USAR PARA TRATAR, PREVENIR O CONTROLAR LA OBESIDAD, HIPERGLICEMIA, HIPERLIPIDEMIA, ARTEROSCLEROSIS, HIPERINSULINEMIA Y DIABETES MELLITUS NO DEPENDIENTE DE INSULINA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36241102P | 2002-03-07 | 2002-03-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20040190A1 true PE20040190A1 (es) | 2004-03-20 |
Family
ID=27789158
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2003000213A PE20040190A1 (es) | 2002-03-07 | 2003-03-05 | Tiazoles y oxazoles sustituidos que modulan la actividad de ppar |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US6867224B2 (es) |
| EP (1) | EP1480641A1 (es) |
| JP (1) | JP2005527509A (es) |
| AR (1) | AR038882A1 (es) |
| AU (1) | AU2003207914A1 (es) |
| BR (1) | BR0308202A (es) |
| CA (1) | CA2478164A1 (es) |
| GT (1) | GT200300054A (es) |
| MX (1) | MXPA04008627A (es) |
| NI (1) | NI200300039A (es) |
| PA (1) | PA8568601A1 (es) |
| PE (1) | PE20040190A1 (es) |
| TW (1) | TW200405812A (es) |
| UY (1) | UY27696A1 (es) |
| WO (1) | WO2003074051A1 (es) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA04003398A (es) * | 2001-10-12 | 2004-11-22 | Nippon Chemiphar Co | Activador para el receptor o activado con el proliferador de peroxisoma. |
| US6833380B2 (en) | 2002-03-07 | 2004-12-21 | Warner-Lambert Company, Llc | Compounds that modulate PPAR activity and methods of preparation |
| US6875780B2 (en) * | 2002-04-05 | 2005-04-05 | Warner-Lambert Company | Compounds that modulate PPAR activity and methods for their preparation |
| AU2003303681A1 (en) * | 2003-01-06 | 2004-08-10 | Eli Lilly And Company | Fused heterocyclic derivates as ppar modulators |
| US7244763B2 (en) * | 2003-04-17 | 2007-07-17 | Warner Lambert Company Llc | Compounds that modulate PPAR activity and methods of preparation |
| EP1630152A4 (en) | 2003-05-30 | 2009-09-23 | Takeda Pharmaceutical | CONDENSED CYCLIC COMPOUND |
| RU2344135C2 (ru) * | 2003-07-02 | 2009-01-20 | Ф.Хоффманн-Ля Рош Аг | Тиазолзамещенные индолилпроизводные и их применение в качестве модуляторов ppar |
| US7435837B2 (en) | 2003-10-24 | 2008-10-14 | Wyeth | Dihydrobenzofuranyl alkanamine derivatives and methods for using same |
| US7728155B2 (en) | 2003-10-24 | 2010-06-01 | Wyeth Llc | Dihydrobenzofuranyl alkanamines and methods for using same as cns agents |
| RU2367659C2 (ru) * | 2003-11-05 | 2009-09-20 | Ф.Хоффманн-Ля Рош Аг | Гетероарильные производные в качестве активаторов рецепторов, активируемых пролифераторами пероксисом (ppar) |
| WO2005060958A1 (en) * | 2003-12-19 | 2005-07-07 | Kalypsys, Inc. | (5- (2-phenyl)-thiazol-5-ylmethoxy)-indol-1-yl) -acetic acid derivatives and related compounds as modulators of the human ppar-delta receptor for the treatment of metabolic disorders such as type 2 diabetes |
| KR100802864B1 (ko) * | 2004-03-09 | 2008-02-12 | 에프. 호프만-라 로슈 아게 | Ppar 활성화제로서 피라졸릴 인돌릴 유도체 |
| CA2557789C (en) * | 2004-03-09 | 2012-12-11 | F.Hoffmann-La Roche Ag | Pyrazolyl indolyl derivatives as ppar activators |
| DE602005024384D1 (de) | 2004-05-05 | 2010-12-09 | High Point Pharmaceuticals Llc | Neue verbindungen, ihre herstellung und verwendung |
| US8053598B2 (en) | 2004-05-05 | 2011-11-08 | High Point Pharmaceuticals, Llc | Compounds, their preparation and use |
| US20060014785A1 (en) * | 2004-05-25 | 2006-01-19 | Metabolex, Inc. | Bicyclic, substituted triazoles as modulators of ppar and methods of their preparation |
| AU2005247473A1 (en) * | 2004-05-25 | 2005-12-08 | Metabolex, Inc. | Substituted triazoles as modulators of PPAR and methods of their preparation |
| US7405236B2 (en) * | 2004-08-16 | 2008-07-29 | Hoffman-La Roche Inc. | Indole derivatives comprising an acetylene group |
| US20080096916A1 (en) * | 2004-11-18 | 2008-04-24 | Pfizer Inc. | Drugs And Prodrugs Useful The Treatment Of Energy Balance In Ruminants |
| RU2416601C2 (ru) * | 2005-02-25 | 2011-04-20 | Оно Фармасьютикал Ко., Лтд. | Соединение индола и его применение |
| ES2372617T3 (es) | 2005-06-30 | 2012-01-24 | High Point Pharmaceuticals, Llc | Ácidos fenoxiacéticos como activadores de ppar-delta. |
| CN103224477A (zh) | 2005-12-22 | 2013-07-31 | 高点制药有限责任公司 | 作为PPAR-δ活化剂的苯氧基乙酸 |
| US7943612B2 (en) | 2006-03-09 | 2011-05-17 | High Point Pharmaceuticals, Llc | Compounds that modulate PPAR activity, their preparation and use |
| US8202686B2 (en) * | 2007-03-22 | 2012-06-19 | Advanced Liquid Logic, Inc. | Enzyme assays for a droplet actuator |
| TW200927740A (en) * | 2007-11-13 | 2009-07-01 | Bial Portela & Ca Sa | Process |
| TWI469965B (zh) | 2008-12-22 | 2015-01-21 | Ono Pharmaceutical Co | 乙炔基吲哚化合物 |
| EP2516669B1 (en) | 2009-12-21 | 2016-10-12 | Advanced Liquid Logic, Inc. | Enzyme assays on a droplet actuator |
| AR080374A1 (es) | 2010-03-05 | 2012-04-04 | Sanofi Aventis | Procedimiento para la preparcion de 2-(ciclohexilmetil)-n-(2-((2s)-1-metilpirrolidin-2-il) etil)- 1,2,3,4-tetrahidroisoquinolin-7- sulfonamida |
| CA2803159A1 (en) | 2010-06-21 | 2011-12-29 | Ono Pharmaceutical Co., Ltd. | New crystalline forms of 4,4'-[4-fluoro-7-({4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl}ethynyl)-2-methyl-1h-indole-1,3-diyl]dibutanoic acid, 4,4'-[2-methyl-7-({4-[4-(pentafluorophenyl)butoxy]phenyl}ethynyl)-1h-indole-1,3-diyl]dibutanoic acid, and 4,4'-[4-fluoro-2-methyl-7-({4-[4-(2,3,4,6-tetrafluorophenyl)butoxy]phenyl}ethynyl)-1h-indole-1,3-diyl]dibutano |
| WO2013009927A2 (en) | 2011-07-11 | 2013-01-17 | Advanced Liquid Logic, Inc. | Droplet actuators and techniques for droplet-based assays |
| JP6106179B2 (ja) * | 2012-02-24 | 2017-03-29 | 武田薬品工業株式会社 | 芳香環化合物 |
| EP3756661A1 (en) | 2013-09-09 | 2020-12-30 | vTv Therapeutics LLC | Use of a ppar-delta agonist for treating muscle atrophy |
| CN109071435A (zh) * | 2016-01-21 | 2018-12-21 | 耶路撒冷希伯来大学伊森姆研究发展公司 | 吲哚啉衍生物、包含它们的组合物及其用途 |
| WO2023147309A1 (en) | 2022-01-25 | 2023-08-03 | Reneo Pharmaceuticals, Inc. | Use of ppar-delta agonists in the treatment of disease |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU1856997A (en) | 1996-02-02 | 1997-08-22 | Merck & Co., Inc. | Method for raising hdl cholesterol levels |
| GB9914977D0 (en) | 1999-06-25 | 1999-08-25 | Glaxo Group Ltd | Chemical compounds |
| DE60005973T2 (de) | 1999-08-27 | 2004-05-13 | Eli Lilly And Co., Indianapolis | Biaryl-oxa(thia)zolderivate und ihre verwendung als ppars modulatoren |
| US6639077B2 (en) * | 2000-03-23 | 2003-10-28 | Merck Frosst Canada & Co. | Tri-aryl-substituted-ethane PDE4 inhibitors |
| AU2001268162A1 (en) | 2000-06-02 | 2001-12-17 | Cor Therapeutics, Inc. | Methods for producing chiral chromones, chromanes, amino substituted chromanes and intermediates therefor |
| US6903227B2 (en) | 2000-06-02 | 2005-06-07 | Millennium Pharmaceuticals, Inc. | Synthesis of 2-acyl substituted chromanes and intermediates thereof |
| DE60129712T2 (de) | 2000-08-23 | 2008-07-03 | Eli Lilly And Co., Indianapolis | Oxazolylaryloxyessigsäure derivate und ihre verwendung als ppar agonisten |
| HUP0300857A3 (en) | 2000-08-23 | 2007-03-28 | Lilly Co Eli | Oxazolyl-arylpropionic acid derivatives and their use as ppar agonists |
| CA2448639A1 (en) | 2001-05-29 | 2002-12-05 | Kyoto Pharmaceutical Industries, Ltd. | Novel heterocyclic derivatives and medicinal use thereof |
| EA200400011A1 (ru) | 2001-06-07 | 2004-06-24 | Эли Лилли Энд Компани | Модуляторы рецепторов, активируемых пролифераторами пероксисом (prar) |
| ATE394376T1 (de) | 2001-06-18 | 2008-05-15 | Ono Pharmaceutical Co | Tetrahydrochinolinderivatverbindung und die verbindung als wirkstoff enthaltendes arzneimittel |
| AR036237A1 (es) | 2001-07-27 | 2004-08-25 | Bayer Corp | Derivados del acido indan acetico, intermediarios, y metodo para su preparacion, composicion farmaceutica y el uso de dichos derivados para la manufactura de un medicamento |
| US6833380B2 (en) * | 2002-03-07 | 2004-12-21 | Warner-Lambert Company, Llc | Compounds that modulate PPAR activity and methods of preparation |
| US7244763B2 (en) * | 2003-04-17 | 2007-07-17 | Warner Lambert Company Llc | Compounds that modulate PPAR activity and methods of preparation |
-
2002
- 2002-12-19 US US10/324,266 patent/US6867224B2/en not_active Expired - Fee Related
-
2003
- 2003-03-03 EP EP03704916A patent/EP1480641A1/en not_active Withdrawn
- 2003-03-03 MX MXPA04008627A patent/MXPA04008627A/es active IP Right Grant
- 2003-03-03 CA CA002478164A patent/CA2478164A1/en not_active Abandoned
- 2003-03-03 BR BR0308202-4A patent/BR0308202A/pt not_active IP Right Cessation
- 2003-03-03 JP JP2003572568A patent/JP2005527509A/ja active Pending
- 2003-03-03 AU AU2003207914A patent/AU2003207914A1/en not_active Abandoned
- 2003-03-03 WO PCT/IB2003/000882 patent/WO2003074051A1/en not_active Ceased
- 2003-03-05 AR ARP030100738A patent/AR038882A1/es unknown
- 2003-03-05 PE PE2003000213A patent/PE20040190A1/es not_active Application Discontinuation
- 2003-03-06 TW TW092104791A patent/TW200405812A/zh unknown
- 2003-03-06 NI NI200300039A patent/NI200300039A/es unknown
- 2003-03-06 UY UY27696A patent/UY27696A1/es not_active Application Discontinuation
- 2003-03-07 PA PA20038568601A patent/PA8568601A1/es unknown
- 2003-03-07 GT GT200300054A patent/GT200300054A/es unknown
-
2004
- 2004-12-22 US US11/020,391 patent/US20050113422A1/en not_active Abandoned
- 2004-12-24 US US11/025,271 patent/US7109222B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| NI200300039A (es) | 2005-09-21 |
| US6867224B2 (en) | 2005-03-15 |
| US20050107442A1 (en) | 2005-05-19 |
| AU2003207914A1 (en) | 2003-09-16 |
| JP2005527509A (ja) | 2005-09-15 |
| CA2478164A1 (en) | 2003-09-12 |
| TW200405812A (en) | 2004-04-16 |
| BR0308202A (pt) | 2004-12-21 |
| AR038882A1 (es) | 2005-02-02 |
| GT200300054A (es) | 2003-10-10 |
| US20050113422A1 (en) | 2005-05-26 |
| WO2003074051A1 (en) | 2003-09-12 |
| UY27696A1 (es) | 2003-10-31 |
| EP1480641A1 (en) | 2004-12-01 |
| US7109222B2 (en) | 2006-09-19 |
| PA8568601A1 (es) | 2003-11-12 |
| MXPA04008627A (es) | 2004-12-06 |
| US20030207915A1 (en) | 2003-11-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD | Application declared void or lapsed |