AR042117A1 - Derivados de indolilo utiles como sensibilizadores de insulina, activadores de ppar - Google Patents
Derivados de indolilo utiles como sensibilizadores de insulina, activadores de pparInfo
- Publication number
- AR042117A1 AR042117A1 ARP030104311A ARP030104311A AR042117A1 AR 042117 A1 AR042117 A1 AR 042117A1 AR P030104311 A ARP030104311 A AR P030104311A AR P030104311 A ARP030104311 A AR P030104311A AR 042117 A1 AR042117 A1 AR 042117A1
- Authority
- AR
- Argentina
- Prior art keywords
- cycloalkyl
- indolilo
- alkyl
- hydrogen
- compounds
- Prior art date
Links
- 229940122355 Insulin sensitizer Drugs 0.000 title 1
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 title 1
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 title 1
- 239000012190 activator Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 201000010099 disease Diseases 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 238000011282 treatment Methods 0.000 abstract 2
- 229940086609 Lipase inhibitor Drugs 0.000 abstract 1
- 208000001145 Metabolic Syndrome Diseases 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 230000003143 atherosclerotic effect Effects 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 230000036772 blood pressure Effects 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 239000011203 carbon fibre reinforced carbon Substances 0.000 abstract 1
- 235000012000 cholesterol Nutrition 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 150000002632 lipids Chemical class 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 239000011593 sulfur Substances 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- 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
- C07D417/06—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 carbon chain containing only aliphatic carbon 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Compuestos de fórmula (1) para el procesamiento de preparación, composición farmacéutica que los comprende y su usos. Reivindicación 1: Compuestos de la fórmula (1), en donde: R1 es arilo o heteroarilo; R2 es hidrógeno, alquilo o cicloalquilo; R3 es alcoxi o alcoxi sustituido con uno a tres átomos de halógeno; R4 es hidrógeno, alquilo o cicloalquilo; A es oxígeno o azufre; n es 1, 2 ó 3; y, en donde el enlace entre los átomos de carbono Ca y Cb es un enlace carbono-carbono doble o sencillo; y sales y ésteres farmacéuticamente aceptables de los mismos. Reivindicación 21: El uso de un compuesto de acuerdo con cualquiera de las reivindicaciones de la 1 a la 12 en la fabricación de un medicamento para el tratamiento y/o profilaxis de enfermedades que se modulan mediante los agonistas PPARalfa y/o PPARgama en un paciente que está también recibiendo tratamiento con un inhibidor de lipasa. Reivindicación 23: El uso de acuerdo con cualquiera de las reivindicaciones 19, 21, ó 22, en donde la enfermedad es diabetes, diabetes mellitus no dependiente de insulina, presión sanguínea elevada, niveles aumentados de lípidos y colesterol, enfermedad ateroesclerótica o síndrome metabólico.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02026366 | 2002-11-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR042117A1 true AR042117A1 (es) | 2005-06-08 |
Family
ID=32338000
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030104311A AR042117A1 (es) | 2002-11-25 | 2003-11-21 | Derivados de indolilo utiles como sensibilizadores de insulina, activadores de ppar |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US7098228B2 (es) |
| EP (1) | EP1567523B1 (es) |
| JP (1) | JP4384052B2 (es) |
| KR (1) | KR100713266B1 (es) |
| CN (1) | CN100343250C (es) |
| AR (1) | AR042117A1 (es) |
| AT (1) | ATE405560T1 (es) |
| AU (1) | AU2003292030B2 (es) |
| BR (1) | BR0316556A (es) |
| CA (1) | CA2505545C (es) |
| DE (1) | DE60323130D1 (es) |
| ES (1) | ES2312819T3 (es) |
| GT (1) | GT200300251A (es) |
| MX (1) | MXPA05005445A (es) |
| PA (1) | PA8589401A1 (es) |
| PE (1) | PE20040843A1 (es) |
| PL (1) | PL377320A1 (es) |
| RU (1) | RU2315767C2 (es) |
| TW (1) | TW200413357A (es) |
| UY (1) | UY28091A1 (es) |
| WO (1) | WO2004048371A1 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050203151A1 (en) * | 2003-12-19 | 2005-09-15 | Kalypsys, Inc. | Novel compounds, compositions and uses thereof for treatment of metabolic disorders and related conditions |
| MX2009008465A (es) * | 2007-02-15 | 2009-08-20 | Hoffmann La Roche | Nuevas 2-aminooxazolinas como ligandos de taar1. |
Family Cites Families (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4011326A (en) * | 1975-07-29 | 1977-03-08 | Merck & Co., Inc. | 2-Substituted oxazolo[4,5-b]pyridine anti-inflammatory agents |
| DE3034005C2 (de) | 1980-09-10 | 1982-12-09 | A. Nattermann & Cie GmbH, 5000 Köln | Indolessigsäure-Derivate, Verfahren zu ihrer Herstellung und sie enthaltende pharmazeutische Zubereitungen |
| CA1247547A (en) * | 1983-06-22 | 1988-12-28 | Paul Hadvary | Leucine derivatives |
| CA1328881C (en) | 1984-12-21 | 1994-04-26 | Pierre Barbier | Process for the manufacture of oxetanones |
| CA1270837A (en) | 1984-12-21 | 1990-06-26 | Hoffmann-La Roche Limited | Oxetanones |
| CA2035972C (en) | 1990-02-23 | 2006-07-11 | Martin Karpf | Process for the preparation of oxetanones |
| US5089514A (en) * | 1990-06-14 | 1992-02-18 | Pfizer Inc. | 3-coxazolyl [phenyl, chromanyl or benzofuranyl]-2-hydroxypropionic acid derivatives and analogs as hypoglycemic agents |
| US5274143A (en) | 1991-07-23 | 1993-12-28 | Hoffmann-La Roche Inc. | Process for the preparation of (R)-3-hexyl-5,6-dihydro-4-hydroxy-6-undecyl-2H-pyran-2-one and (R)-5,6-dihydro-6-undecyl-2H-pyran-2,4(3H)-dione |
| SK695A3 (en) | 1992-07-03 | 1995-07-11 | Smithkline Beecham Plc | Heterocyclic compounds method of their production and using |
| GB9225386D0 (en) | 1992-12-04 | 1993-01-27 | Smithkline Beecham Plc | Novel compounds |
| DE4317320A1 (de) * | 1993-05-25 | 1994-12-01 | Boehringer Mannheim Gmbh | Neue Thiazolidindione und diese enthaltende Arzneimittel |
| GB9326171D0 (en) | 1993-12-22 | 1994-02-23 | Smithkline Beecham Plc | Novel compounds |
| JPH09176162A (ja) * | 1995-12-22 | 1997-07-08 | Toubishi Yakuhin Kogyo Kk | チアゾリジンジオン誘導体及びその製造法並びにそれを含む医薬組成物 |
| GB9600464D0 (en) | 1996-01-09 | 1996-03-13 | Smithkline Beecham Plc | Novel method |
| CZ3799A3 (cs) * | 1996-07-09 | 1999-08-11 | Smithkline Beecham S. P. A. | Indolový derivát k ošetřování osteoporézy |
| CA2274183C (en) * | 1996-12-10 | 2006-10-24 | Bristol-Myers Squibb Company | Benzodioxole, benzofuran, dihydrobenzofuran, and benzodioxane melatonergic agents |
| US6004996A (en) * | 1997-02-05 | 1999-12-21 | Hoffman-La Roche Inc. | Tetrahydrolipstatin containing compositions |
| DE19711616A1 (de) * | 1997-03-20 | 1998-09-24 | Boehringer Mannheim Gmbh | Verbessertes Verfahren zur Herstellung von Thiazolidindionen |
| US6121397A (en) * | 1997-07-14 | 2000-09-19 | Xerox Corporation | Polymerization processes using oligomeric compound, monomer and surfactant |
| HN1998000118A (es) | 1997-08-27 | 1999-02-09 | Pfizer Prod Inc | 2 - aminopiridinas que contienen sustituyentes de anillos condensados. |
| EP0903343B1 (en) | 1997-09-19 | 2003-05-28 | SSP Co., Ltd. | Alpha-Substituted phenylpropionic acid derivative and medicine containing the same |
| CN1208326C (zh) | 1998-04-23 | 2005-06-29 | 雷迪实验室有限公司 | 杂环化合物及其在医药方面的应用、其制备方法及含有它们的药物组合物 |
| GB9817118D0 (en) | 1998-08-07 | 1998-10-07 | Glaxo Group Ltd | Pharmaceutical compounds |
| EP1105122B1 (en) | 1998-08-14 | 2005-04-27 | F.Hoffmann-La Roche Ag | Pharmaceutical compositions containing lipase inhibitors |
| TR200100472T2 (tr) | 1998-08-14 | 2001-07-23 | F.Hoffmann-La Roche Ag | Lipaz inhibitörleri ile sitozan içeren farmasötik bileşimler |
| GB9902459D0 (en) * | 1999-02-05 | 1999-03-24 | Zeneca Ltd | Chemical compounds |
| GB9914977D0 (en) | 1999-06-25 | 1999-08-25 | Glaxo Group Ltd | Chemical compounds |
| ATE319702T1 (de) | 1999-08-02 | 2006-03-15 | Verfahren zur herstellung von benzothiophen- derivaten | |
| EP1785134A3 (en) * | 2000-01-19 | 2009-02-18 | Synvista Therapeutics, Inc. | Use of thiazole, imidazole and oxazole compounds for the treatment of disorders associated with protein aging |
| MXPA03001558A (es) | 2000-08-23 | 2003-06-06 | Lilly Co Eli | Agonistas del receptor activado del proliferador de peroxisoma. |
| KR20030030036A (ko) * | 2000-09-29 | 2003-04-16 | 시오노기세이야쿠가부시키가이샤 | 티아졸 또는 옥사졸 유도체 |
| IL158589A0 (en) * | 2001-05-15 | 2004-05-12 | Hoffmann La Roche | Carboxylic acid substituted oxazole derivatives for use as ppar-alpha and -gamma activators in the treatment of diabetes |
| WO2003004458A1 (en) | 2001-07-03 | 2003-01-16 | Biovitrum Ab | New compounds |
| TWI323658B (en) * | 2001-12-06 | 2010-04-21 | Nat Health Research Institutes | Novel compounds of indol-3-yl-2-oxyacetylamide derivatives, pharmaceutical composition thereof, and method for manufacturing the same |
| US6933316B2 (en) * | 2001-12-13 | 2005-08-23 | National Health Research Institutes | Indole compounds |
| WO2003053976A1 (en) | 2001-12-20 | 2003-07-03 | Biovitrum Ab | PIPAZOLO [1,5-a] PYRIMIDINE DERIVATIVES AS MODULATORS OF PPAR |
-
2003
- 2003-11-17 WO PCT/EP2003/012814 patent/WO2004048371A1/en active IP Right Grant
- 2003-11-17 ES ES03767555T patent/ES2312819T3/es not_active Expired - Lifetime
- 2003-11-17 BR BR0316556-6A patent/BR0316556A/pt not_active Withdrawn
- 2003-11-17 KR KR1020057009337A patent/KR100713266B1/ko not_active IP Right Cessation
- 2003-11-17 EP EP03767555A patent/EP1567523B1/en not_active Expired - Lifetime
- 2003-11-17 AU AU2003292030A patent/AU2003292030B2/en not_active Ceased
- 2003-11-17 MX MXPA05005445A patent/MXPA05005445A/es active IP Right Grant
- 2003-11-17 AT AT03767555T patent/ATE405560T1/de active
- 2003-11-17 JP JP2004554364A patent/JP4384052B2/ja not_active Expired - Lifetime
- 2003-11-17 CN CNB2003801041013A patent/CN100343250C/zh not_active Expired - Fee Related
- 2003-11-17 PL PL377320A patent/PL377320A1/pl not_active Application Discontinuation
- 2003-11-17 CA CA2505545A patent/CA2505545C/en not_active Expired - Fee Related
- 2003-11-17 DE DE60323130T patent/DE60323130D1/de not_active Expired - Lifetime
- 2003-11-17 RU RU2005120152/04A patent/RU2315767C2/ru not_active IP Right Cessation
- 2003-11-19 TW TW092132418A patent/TW200413357A/zh unknown
- 2003-11-21 GT GT200300251A patent/GT200300251A/es unknown
- 2003-11-21 AR ARP030104311A patent/AR042117A1/es not_active Application Discontinuation
- 2003-11-21 PA PA20038589401A patent/PA8589401A1/es unknown
- 2003-11-21 US US10/719,556 patent/US7098228B2/en not_active Expired - Fee Related
- 2003-11-21 PE PE2003001184A patent/PE20040843A1/es not_active Application Discontinuation
- 2003-11-24 UY UY28091A patent/UY28091A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| EP1567523B1 (en) | 2008-08-20 |
| PL377320A1 (pl) | 2006-01-23 |
| KR20050086759A (ko) | 2005-08-30 |
| RU2315767C2 (ru) | 2008-01-27 |
| PE20040843A1 (es) | 2004-12-24 |
| RU2005120152A (ru) | 2006-05-27 |
| CA2505545A1 (en) | 2004-06-10 |
| WO2004048371A1 (en) | 2004-06-10 |
| KR100713266B1 (ko) | 2007-05-04 |
| DE60323130D1 (de) | 2008-10-02 |
| PA8589401A1 (es) | 2004-07-20 |
| UY28091A1 (es) | 2004-05-31 |
| US20040106657A1 (en) | 2004-06-03 |
| CN1717407A (zh) | 2006-01-04 |
| AU2003292030A1 (en) | 2004-06-18 |
| US7098228B2 (en) | 2006-08-29 |
| CN100343250C (zh) | 2007-10-17 |
| ES2312819T3 (es) | 2009-03-01 |
| AU2003292030B2 (en) | 2007-01-04 |
| MXPA05005445A (es) | 2005-08-26 |
| ATE405560T1 (de) | 2008-09-15 |
| CA2505545C (en) | 2011-06-07 |
| TW200413357A (en) | 2004-08-01 |
| JP4384052B2 (ja) | 2009-12-16 |
| JP2006513173A (ja) | 2006-04-20 |
| BR0316556A (pt) | 2005-10-04 |
| EP1567523A1 (en) | 2005-08-31 |
| GT200300251A (es) | 2004-06-28 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |