AR038881A1 - Compuestos que modulan la actividad de ppar, composicion farmaceutica que los contiene y un procedimiento para la preparcion de aquellos - Google Patents
Compuestos que modulan la actividad de ppar, composicion farmaceutica que los contiene y un procedimiento para la preparcion de aquellosInfo
- Publication number
- AR038881A1 AR038881A1 ARP030100737A ARP030100737A AR038881A1 AR 038881 A1 AR038881 A1 AR 038881A1 AR P030100737 A ARP030100737 A AR P030100737A AR P030100737 A ARP030100737 A AR P030100737A AR 038881 A1 AR038881 A1 AR 038881A1
- Authority
- AR
- Argentina
- Prior art keywords
- independently
- alkyl
- alkynyl
- alkenyl
- aryl
- Prior art date
Links
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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D277/24—Radicals substituted by oxygen atoms
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicinal Preparation (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Compuestos que alteran la actividad de PPAR. También se describen las sales farmacéuticamente aceptables de los compuestos, composiciones farmacéuticamente aceptables que comprenden los compuestos o sus sales, y procedimientos para usarlos como agentes terapéuticos para el tratamiento o prevención de la hiperlipidemia e hipercolesterolemia en un mamífero. La presente también describe procedimientos para la preparación de los compuestos citados. Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en la que: W es O, S, CR5R6, -(CH2)p-cicloalquileno, o -(CH2)p-heterocicloalquileno; X0 y X1 son independientemente O o S; Ar1 es un arilo o heteroarilo no sustituido o sustituido; R1, R2, R3 y R4 son independientemente, alquilo, alcoxi inferior, haloalquilo. -O-(CH2)pCF3, halógeno, nitro, ciano, -OH, -SH, -CF3, -S(O)palquilo, -S(O)parilo, -(CH2)mOR7, -(CH2)mNR8R9, -COR7, -CO2H, -CO2R7, o NR8R9, R5 y R6 son independientemente H, alquilo, alquenilo, alquinilo o arilo, o se unen conjuntamente para formar un cicloalquilo o cicloalquenilo de 3 a 7 miembros. R7 es independientemente H, alquilo, alquenilo, alquinilo o arilo; R8 y R9 son cada uno independientemente hidrógeno, alquilo, alquenilo, alquinilo, -COalquilo, -COarilo, cicloalquilo, -CO2alquilo, -CO2arilo, -SO2alquilo, -SO2arilo, o se unen conjuntamente para formar un anillo de 4 a 7 miembros que tiene de 1 a 3 heteroátomos; R10 y R11 son independientemente H, halo, arilo o heteroarilo; m es de 0 a 5; n es de 0 a 5; y p es de 0 a 2; con las siguientes condiciones; que cuando W es O, n = 1, R1 es H, R2 y R4 no son H o R2 y R3 no son H; que cuando W es O, n = 1 y R2 es H, R1 y R3 no son H o R1 y R4 no son H, que cuando W es O, n = 1 y R3 es H, R1 y R4 no son H o R2 y R4 no son H; y que cuando W es O, n = 1 y R4 es H, R1 y R3 no son H o R2 y R3 no son H. Reivindicación 15: Un procedimiento para la preparación de un compuesto que tiene la fórmula (2), el procedimiento caracterizado porque comprende hacer reaccionar el compuesto de estructuras (3) con el de estructura (4) en la que W es O, S, CR5R6, -(CH2)p-cicloalquileno, o -(CH2)p-heterocicloalquileno, X0 y X1 son independientemente O o S; Ar1 es un arilo o heteroarilo no sustituido o sustituido; R1, R2, R3 y R4 son independientemente alquilo, alcoxi inferior, haloalquilo, -O-(CH2)pCF3, halógeno, nitro, ciano, -OH, -SH, -CF3, -S(O)palquilo, -S(O)parilo, -(CH2)mOR7, -(CH2)mNR8R9, -COR7, -CO2H, -CO2R7, o NR8R9, R5 y R6 son independientemente H, alquilo, alquenilo, alquinilo, o arilo, o se unen conjuntamente para formar un cicloalquilo o cicloalquenilo de 3 a 7 miembros. R7 es independientemente H, alquilo, alquenilo, alquinilo o arilo; R8 y R9 son cada uno independientemente H, alquilo, alquenilo, alquinilo, -COalquilo, -COarilo, cicloalquilo, -CO2alquilo, -CO2arilo, -SO2alquilo, -SO2arilo, o se unen conjuntamente para formar un anillo de 4 a 7 miembros que tiene de 1 a 3 heteroátomos; R12 es un alquilo inferior; X es halógeno, m es de 0 a 5; n es de 0 a 5; y p es de 0 a 2; con las siguientes condiciones: que cuando W es O, n = 1, Y está ausente y R1 es H, R2 y R4 no son H o R2 y R3 no son H; que cuando W es O, n =1, Y está ausente y R2 es H, R1 y R3 no son H o R1 y R4 no son H; que cuando W es O, n =1, Y está ausente y R3 es H, R1 y R4 no son H o R2 y R4 no son H; y que cuando W es O, n = 1, Y está ausente y R4 es H, R1 y R3 no son H o R2 y R3 no son H.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36240202P | 2002-03-07 | 2002-03-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR038881A1 true AR038881A1 (es) | 2005-02-02 |
Family
ID=27789157
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030100737A AR038881A1 (es) | 2002-03-07 | 2003-03-05 | Compuestos que modulan la actividad de ppar, composicion farmaceutica que los contiene y un procedimiento para la preparcion de aquellos |
Country Status (29)
| Country | Link |
|---|---|
| US (1) | US20030207924A1 (es) |
| EP (1) | EP1482935B1 (es) |
| JP (1) | JP2005528348A (es) |
| KR (1) | KR20040091693A (es) |
| AP (1) | AP2004003124A0 (es) |
| AR (1) | AR038881A1 (es) |
| AT (1) | ATE405260T1 (es) |
| AU (1) | AU2003206059A1 (es) |
| BR (1) | BR0308277A (es) |
| CA (1) | CA2478520A1 (es) |
| CO (1) | CO5601012A2 (es) |
| DE (1) | DE60323060D1 (es) |
| EA (1) | EA200400943A1 (es) |
| EC (1) | ECSP045285A (es) |
| ES (1) | ES2310650T3 (es) |
| HN (1) | HN2003000090A (es) |
| IS (1) | IS7377A (es) |
| MA (1) | MA27181A1 (es) |
| MX (1) | MXPA04007564A (es) |
| NO (1) | NO20044242L (es) |
| OA (1) | OA12780A (es) |
| PA (1) | PA8567801A1 (es) |
| PE (1) | PE20030989A1 (es) |
| PL (1) | PL372969A1 (es) |
| TN (1) | TNSN04168A1 (es) |
| TW (1) | TW200305403A (es) |
| UY (1) | UY27695A1 (es) |
| WO (1) | WO2003074050A1 (es) |
| ZA (1) | ZA200406068B (es) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US7244763B2 (en) * | 2003-04-17 | 2007-07-17 | Warner Lambert Company Llc | Compounds that modulate PPAR activity and methods of preparation |
| SI1638551T1 (sl) * | 2003-05-19 | 2012-04-30 | Irm Llc | Imunosupresivne spojine in sestavki |
| MY150088A (en) | 2003-05-19 | 2013-11-29 | Irm Llc | Immunosuppressant compounds and compositions |
| CN1946666A (zh) | 2004-02-27 | 2007-04-11 | 埃姆艮股份有限公司 | 用于治疗代谢性疾病的化合物、药物组合物和方法 |
| WO2005105736A1 (en) | 2004-05-05 | 2005-11-10 | Novo Nordisk A/S | Novel compounds, their preparation and use |
| DE602005024384D1 (de) | 2004-05-05 | 2010-12-09 | High Point Pharmaceuticals Llc | Neue verbindungen, ihre herstellung und verwendung |
| US7456164B2 (en) | 2004-05-07 | 2008-11-25 | Pfizer, Inc | 3- or 4-monosubtituted phenol and thiophenol derivatives useful as H3 ligands |
| AU2012200214B2 (en) * | 2004-05-14 | 2013-10-24 | Emisphere Technologies, Inc. | Compounds and compositions for delivering active agents |
| WO2005115383A2 (en) * | 2004-05-25 | 2005-12-08 | Metabolex, Inc. | Substituted triazoles as modulators of ppar and methods of their preparation |
| WO2005115384A2 (en) * | 2004-05-25 | 2005-12-08 | Metabolex, Inc. | Bicyclic, substituted triazoles as modulators of ppar and methods of their preparation |
| CN101193876B (zh) * | 2005-05-07 | 2011-05-11 | 财团法人首尔大学校产学协力财团 | 制备PPARδ的配体的方法和用于制备该配体的中间化合物 |
| US7465804B2 (en) * | 2005-05-20 | 2008-12-16 | Amgen Inc. | Compounds, pharmaceutical compositions and methods for their use in treating metabolic disorders |
| JP5052511B2 (ja) | 2005-06-30 | 2012-10-17 | ハイ ポイント ファーマシューティカルズ，エルエルシー | Ｐｐａｒデルタ活性化因子としてのフェノキシ酢酸 |
| US8153694B2 (en) * | 2005-07-29 | 2012-04-10 | Takeda Pharmaceutical Company Limited | Cyclopropanecarboxylic acid compound |
| AU2006291234A1 (en) | 2005-09-14 | 2007-03-22 | Amgen Inc. | Conformationally constrained 3- (4-hydroxy-phenyl) - substituted-propanoic acids useful for treating metabolic disorders |
| 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 |
| JP2009132620A (ja) * | 2006-03-07 | 2009-06-18 | Astellas Pharma Inc | フェニルチアゾール誘導体 |
| WO2007101864A2 (en) | 2006-03-09 | 2007-09-13 | High Point Pharmaceuticals, Llc | Compounds that modulate ppar activity, their preparation and use |
| CA2662305C (en) | 2006-09-07 | 2012-04-17 | Amgen Inc. | Heterocyclic gpr40 modulators |
| CA2662242C (en) | 2006-09-07 | 2012-06-12 | Amgen Inc. | Benzo-fused compounds for use in treating metabolic disorders |
| EP2139843B1 (en) | 2007-04-16 | 2013-12-25 | Amgen, Inc | Substituted biphenyl phenoxy-, thiophenyl- and aminophenylpropanoic acid gpr40 modulators |
| BRPI0818253A2 (pt) | 2007-10-10 | 2015-04-07 | Amgen Inc | Moduladores de gpr40 bifenil substituídos |
| CA2708391A1 (en) * | 2007-12-13 | 2009-06-25 | Sri International | Ppar-delta ligands and methods of their use |
| CN101945848A (zh) | 2007-12-20 | 2011-01-12 | 英维沃医药有限公司 | 四取代的苯 |
| US8450522B2 (en) | 2008-03-06 | 2013-05-28 | Amgen Inc. | Conformationally constrained carboxylic acid derivatives useful for treating metabolic disorders |
| JP5551707B2 (ja) | 2008-10-15 | 2014-07-16 | アムジエン・インコーポレーテツド | スピロ環ｇｐｒ４０調節因子 |
| EP2540711A4 (en) * | 2010-02-25 | 2014-01-22 | Snu R&Db Foundation | SELENAZOLE DERIVATIVE HAVING A LIGAND THAT ACTIVATES THE ACTIVATED RECEPTOR OF PEROXISOME PROLIFERATION (PPAR), ITS PREPARATION METHOD AND THE USE OF CHEMICAL COMPOUNDS |
| EP3043789B1 (en) | 2013-09-09 | 2020-07-08 | vTv Therapeutics LLC | Use of a ppar-delta agonists for treating muscle atrophy |
| WO2023147309A1 (en) | 2022-01-25 | 2023-08-03 | Reneo Pharmaceuticals, Inc. | Use of ppar-delta agonists in the treatment of disease |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5859051A (en) * | 1996-02-02 | 1999-01-12 | Merck & Co., Inc. | Antidiabetic agents |
| CZ53699A3 (cs) * | 1996-08-19 | 1999-07-14 | Japan Tobacco Inc. | Deriváty propionové kyseliny a jejich použití |
| GB9914977D0 (en) * | 1999-06-25 | 1999-08-25 | Glaxo Group Ltd | Chemical compounds |
| EP1345916A1 (en) * | 2000-12-20 | 2003-09-24 | Glaxo Group Limited | Substituted oxazoles and thiazoles as hppar alpha agonists |
| GB0031107D0 (en) * | 2000-12-20 | 2001-01-31 | Glaxo Group Ltd | Chemical compounds |
| GB0111523D0 (en) * | 2001-05-11 | 2001-07-04 | Glaxo Group Ltd | Chemical compounds |
| MXPA03010903A (es) * | 2001-06-07 | 2004-02-17 | Lilly Co Eli | Moduladores de receptores activados por el proliferador de peroxisomas. |
-
2002
- 2002-12-20 US US10/324,148 patent/US20030207924A1/en not_active Abandoned
-
2003
- 2003-02-24 DE DE60323060T patent/DE60323060D1/de not_active Expired - Fee Related
- 2003-02-24 AP APAP/P/2004/003124A patent/AP2004003124A0/en unknown
- 2003-02-24 CA CA002478520A patent/CA2478520A1/en not_active Abandoned
- 2003-02-24 PL PL03372969A patent/PL372969A1/xx not_active Application Discontinuation
- 2003-02-24 JP JP2003572567A patent/JP2005528348A/ja not_active Abandoned
- 2003-02-24 EP EP03702943A patent/EP1482935B1/en not_active Expired - Lifetime
- 2003-02-24 MX MXPA04007564A patent/MXPA04007564A/es active IP Right Grant
- 2003-02-24 AT AT03702943T patent/ATE405260T1/de not_active IP Right Cessation
- 2003-02-24 ES ES03702943T patent/ES2310650T3/es not_active Expired - Lifetime
- 2003-02-24 AU AU2003206059A patent/AU2003206059A1/en not_active Abandoned
- 2003-02-24 EA EA200400943A patent/EA200400943A1/ru unknown
- 2003-02-24 WO PCT/IB2003/000708 patent/WO2003074050A1/en active IP Right Grant
- 2003-02-24 BR BR0308277-6A patent/BR0308277A/pt not_active IP Right Cessation
- 2003-02-24 KR KR10-2004-7013951A patent/KR20040091693A/ko not_active Application Discontinuation
- 2003-02-24 OA OA1200400232A patent/OA12780A/en unknown
- 2003-02-27 PA PA20038567801A patent/PA8567801A1/es unknown
- 2003-03-04 PE PE2003000210A patent/PE20030989A1/es not_active Application Discontinuation
- 2003-03-05 AR ARP030100737A patent/AR038881A1/es unknown
- 2003-03-06 HN HN2003000090A patent/HN2003000090A/es unknown
- 2003-03-06 UY UY27695A patent/UY27695A1/es not_active Application Discontinuation
- 2003-03-06 TW TW092104790A patent/TW200305403A/zh unknown
-
2004
- 2004-07-29 IS IS7377A patent/IS7377A/is unknown
- 2004-07-29 ZA ZA200406068A patent/ZA200406068B/en unknown
- 2004-08-24 CO CO04082302A patent/CO5601012A2/es not_active Application Discontinuation
- 2004-08-30 MA MA27839A patent/MA27181A1/fr unknown
- 2004-09-03 TN TNP2004000168A patent/TNSN04168A1/fr unknown
- 2004-09-07 EC EC2004005285A patent/ECSP045285A/es unknown
- 2004-10-06 NO NO20044242A patent/NO20044242L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| US20030207924A1 (en) | 2003-11-06 |
| EP1482935B1 (en) | 2008-08-20 |
| JP2005528348A (ja) | 2005-09-22 |
| PE20030989A1 (es) | 2003-11-29 |
| PA8567801A1 (es) | 2003-11-12 |
| CO5601012A2 (es) | 2006-01-31 |
| EA200400943A1 (ru) | 2005-02-24 |
| ATE405260T1 (de) | 2008-09-15 |
| CA2478520A1 (en) | 2003-09-12 |
| IS7377A (is) | 2004-07-29 |
| AP2004003124A0 (en) | 2004-09-30 |
| PL372969A1 (en) | 2005-08-08 |
| ZA200406068B (en) | 2005-09-06 |
| TW200305403A (en) | 2003-11-01 |
| MA27181A1 (fr) | 2005-01-03 |
| HN2003000090A (es) | 2004-05-05 |
| OA12780A (en) | 2006-07-07 |
| KR20040091693A (ko) | 2004-10-28 |
| WO2003074050A1 (en) | 2003-09-12 |
| EP1482935A1 (en) | 2004-12-08 |
| BR0308277A (pt) | 2004-12-28 |
| AU2003206059A1 (en) | 2003-09-16 |
| DE60323060D1 (de) | 2008-10-02 |
| NO20044242L (no) | 2004-10-06 |
| MXPA04007564A (es) | 2004-11-10 |
| TNSN04168A1 (fr) | 2007-03-12 |
| ECSP045285A (es) | 2004-10-26 |
| ES2310650T3 (es) | 2009-01-16 |
| UY27695A1 (es) | 2003-10-31 |
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