AR044856A1 - Acidos biariloximetilarenocarboxilicos; procedimientos para su preparacion; composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos. - Google Patents
Acidos biariloximetilarenocarboxilicos; procedimientos para su preparacion; composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos.Info
- Publication number
- AR044856A1 AR044856A1 ARP040102167A ARP040102167A AR044856A1 AR 044856 A1 AR044856 A1 AR 044856A1 AR P040102167 A ARP040102167 A AR P040102167A AR P040102167 A ARP040102167 A AR P040102167A AR 044856 A1 AR044856 A1 AR 044856A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- formula
- yloxymethyl
- biphenyl
- amino acid
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/79—Acids; Esters
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C65/21—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups
- C07C65/24—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups polycyclic
-
- 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
- C07D277/32—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 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
- C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
- C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
- C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D333/40—Thiophene-2-carboxylic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
- Furan Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente se refiere a ácidos biariloximetilarenocarboxílicos, composiciones farmacéuticas que los contengan y su uso en la preparación de medicamentos. Los compuestos son útiles para el tratamiento y/o profiláxis de enfermedades asociadas con la activación de la enzima glucógeno-sintasa, por ejemplo la diabetes. Reivindicación 1: Un compuesto de fórmula (1) en la que Ar es un anillo carbocíclico o heterocíclico aromático; R1, R2 y R3 se seleccionan independientemente entre sí entre el grupo formado por alquilo inferior, alcoxi inferior, trifluormetilo, halógeno, hidroxi, amino, alquilamino, dialquilamino, ciano y nitro; R4 es hidroxi o un aminoácido unido mediante un átomo de N del aminoácido; n es 0, 1, 2, 3, 4, o 5; m es 0, 1,2 , 3 o 4; p es 0, 1, o 2, y s es 0, 1 o 2; o una sal farmacéuticamente aceptable de los mismos, con la condición de que a) cuando Ar es furanilo, p y s sean 0 y el compuesto no sea el ácido S-1-{5-(bifenil-4-iloximetil)-furan-2-carbonil]-pirrolidin-2-carboxílico ni el ácido 5-(bifenil-4-iloximetil)-furan-2-carboxílico; b) cuando Ar es fenilo, el compuesto no sea el ácido 3-(bifenil-4-iloximetil)-benzoico ni el ácido 2-(bifenil-3-iloximetil)-benzoico y c) cuando Ar es tiofenilo, el compuesto no sea el ácido 5-(bifenil-4-iloximetil)-tiofen-2-carboxílico. Reivindicación 18: Un proceso para la obtención de un compuesto de fórmula (1) según la reivindicación 1, dicho proceso consiste en hacer reaccionar un compuesto de fórmula (2) en la que R1, R2, m y n tienen los significados definidos en la reivindicación 1, en presencia de una base con un compuesto de fórmula (3) en la que Ar, R3, p y s tienen los significados definidos en la reivindicación 1, LG representa un grupo saliente, por ejemplo Cl, Br o I y R5 representa un grupo protector y posteriormente en escindir el grupo protector para obtener un compuesto de fórmula (1) en la que R4 significa hidroxi, y Ar de R1 a R3, m, n, p y s tienen los significados definidos en la reivindicación 1, y opcionalmente en hacer reaccionar este compuesto con un éster de un aminoácido en presencia de EDC y DMAP y posteriormente en escindir el grupo éster para obtener un compuesto de fórmula (1), en la que R4 es un aminoácido unido mediante un átomo de N del aminoácido.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US48214703P | 2003-06-24 | 2003-06-24 | |
| US48090003P | 2003-06-24 | 2003-06-24 | |
| US56935604P | 2004-05-07 | 2004-05-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR044856A1 true AR044856A1 (es) | 2005-10-05 |
Family
ID=33556418
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040102167A AR044856A1 (es) | 2003-06-24 | 2004-06-22 | Acidos biariloximetilarenocarboxilicos; procedimientos para su preparacion; composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos. |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US7355049B2 (es) |
| EP (1) | EP1663936B1 (es) |
| JP (1) | JP4471974B2 (es) |
| KR (1) | KR100809205B1 (es) |
| AR (1) | AR044856A1 (es) |
| AT (1) | ATE383329T1 (es) |
| AU (1) | AU2004251846B2 (es) |
| BR (1) | BRPI0411906A (es) |
| CA (1) | CA2529875A1 (es) |
| CO (1) | CO5640098A2 (es) |
| DE (1) | DE602004011239T2 (es) |
| DK (1) | DK1663936T3 (es) |
| ES (1) | ES2298761T3 (es) |
| HK (1) | HK1093724A1 (es) |
| IL (1) | IL172617A0 (es) |
| MX (1) | MXPA05014082A (es) |
| MY (1) | MY138708A (es) |
| NO (1) | NO20056010L (es) |
| NZ (1) | NZ544150A (es) |
| PL (1) | PL1663936T3 (es) |
| PT (1) | PT1663936E (es) |
| TW (2) | TWI302532B (es) |
| WO (1) | WO2005000781A1 (es) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005037232A2 (en) * | 2003-10-17 | 2005-04-28 | Joslin Diabetes Center, Inc. | Methods and compositions for modulating adipocyte function |
| US7524870B2 (en) * | 2004-12-03 | 2009-04-28 | Hoffmann-La Roche Inc. | Biaryloxymethylarenecarboxylic acids as glycogen synthase activators |
| GB0503053D0 (en) * | 2005-02-14 | 2005-03-23 | Smithkline Beecham Corp | Chemical compounds |
| US20100150885A1 (en) | 2005-06-01 | 2010-06-17 | Joslin Diabetes Center, Inc. | Methods and compositions for inducing brown adipogenesis |
| EP2283119B1 (en) * | 2008-05-06 | 2015-01-07 | Joslin Diabetes Center, Inc. | Methods and compositions for inducing brown adipogenesis |
| CN102264228A (zh) | 2008-10-22 | 2011-11-30 | 默沙东公司 | 用于抗糖尿病药的新的环状苯并咪唑衍生物 |
| CN102271509A (zh) | 2008-10-31 | 2011-12-07 | 默沙东公司 | 用于抗糖尿病药的新型环苯并咪唑衍生物 |
| US20110112147A1 (en) | 2009-11-11 | 2011-05-12 | David Robert Bolin | Indazolone analogs as glycogen synthase activators |
| US20110112158A1 (en) | 2009-11-11 | 2011-05-12 | David Robert Bolin | Benzisoxazole analogs as glycogen synthase activators |
| US7947728B1 (en) | 2009-11-11 | 2011-05-24 | Hoffmann-La Roche Inc. | Indole and indazole analogs as glycogen synthase activators |
| US8039495B2 (en) * | 2009-11-16 | 2011-10-18 | Hoffman-La Roche Inc. | Biphenyl carboxylic acids and bioisosteres as glycogen synthase activators |
| US20110118314A1 (en) | 2009-11-16 | 2011-05-19 | Weiya Yun | Piperidine analogs as glycogen synthase activators |
| US7939569B1 (en) | 2009-12-01 | 2011-05-10 | Hoffmann-La Roche Inc. | Aniline analogs as glycogen synthase activators |
| US20110136792A1 (en) * | 2009-12-04 | 2011-06-09 | David Robert Bolin | Novel carboxylic acid analogs as glycogen synthase activators |
| CA2786314A1 (en) | 2010-02-25 | 2011-09-01 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| CA2822017C (en) | 2010-12-23 | 2015-04-07 | Pfizer Inc. | Glucagon receptor modulators |
| ME02502B (me) | 2011-02-08 | 2017-02-20 | Pfizer | Modulator glukagonskog receptora |
| CN103476258B (zh) | 2011-02-25 | 2017-04-26 | 默沙东公司 | 用作抗糖尿病药剂的新的环状氮杂苯并咪唑衍生物 |
| RU2013157388A (ru) | 2011-07-22 | 2015-08-27 | Пфайзер Инк. | Хинолинильные модуляторы глюкагонового рецептора |
| JPWO2013065835A1 (ja) * | 2011-11-04 | 2015-04-02 | 味の素株式会社 | 糖尿病治療用医薬組成物 |
| JP6095580B2 (ja) * | 2012-02-13 | 2017-03-15 | 武田薬品工業株式会社 | 芳香環化合物 |
| JP2015525782A (ja) | 2012-08-02 | 2015-09-07 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | 抗糖尿病性三環式化合物 |
| MX2015010935A (es) | 2013-02-22 | 2015-10-29 | Merck Sharp & Dohme | Compuestos biciclicos antidiabeticos. |
| US9650375B2 (en) | 2013-03-14 | 2017-05-16 | Merck Sharp & Dohme Corp. | Indole derivatives useful as anti-diabetic agents |
| JP2016130214A (ja) | 2013-05-01 | 2016-07-21 | 味の素株式会社 | 糖尿病治療用医薬組成物 |
| WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| WO2016002853A1 (ja) * | 2014-07-01 | 2016-01-07 | 味の素株式会社 | 糖尿病治療用医薬組成物 |
| JP6699011B2 (ja) * | 2014-07-04 | 2020-05-27 | 国立大学法人 東京大学 | 脂肪酸サロゲートを含むリゾホスファチジルセリン誘導体 |
| US11072602B2 (en) | 2016-12-06 | 2021-07-27 | Merck Sharp & Dohme Corp. | Antidiabetic heterocyclic compounds |
| US10968232B2 (en) | 2016-12-20 | 2021-04-06 | Merck Sharp & Dohme Corp. | Antidiabetic spirochroman compounds |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2842243A1 (de) | 1978-09-28 | 1980-04-10 | Hoechst Ag | Furan- und thiophen-carbonsaeure-derivate und verfahren zu ihrer herstellung |
| DE4142514A1 (de) | 1991-12-21 | 1993-06-24 | Basf Ag | Verfahren zur bekaempfung von pilzen |
| AU4090093A (en) | 1992-05-29 | 1993-12-30 | Yamanouchi Pharmaceutical Co., Ltd. | Medicine containing benzoic acid derivative and novel benzoic acid derivative |
| US6043247A (en) | 1996-04-19 | 2000-03-28 | Novo Nordisk A/S | Modulators of molecules with phosphotyrosine recognition units |
| JP2000511883A (ja) | 1996-04-19 | 2000-09-12 | ノボ ノルディスク アクティーゼルスカブ | ホスホチロシン認識ユニットを有する分子のモジュレーター |
| WO1997039748A1 (en) | 1996-04-19 | 1997-10-30 | Novo Nordisk A/S | Modulators of molecules with phosphotyrosine recognition units |
| JP4121215B2 (ja) * | 1999-05-17 | 2008-07-23 | 財団法人微生物化学研究会 | スルフォスチン類縁体、並びにスルフォスチン及びその類縁体の製造方法 |
| WO2004012656A2 (en) | 2002-08-02 | 2004-02-12 | Applied Research Systems Ars Holding N.V. | Thiophene and furan derivatives as prostaglandin agonists and use thereof |
| WO2004058679A2 (en) | 2002-12-20 | 2004-07-15 | Migenix Corp. | Ligands of adenine nucleotide translocase (ant) and compositions and methods related thereto |
| DE602004013938D1 (de) | 2003-01-29 | 2008-07-03 | Asterand Uk Ltd | Hemmstoffe des ep4-rezeptors |
-
2004
- 2004-06-17 US US10/870,271 patent/US7355049B2/en not_active Expired - Fee Related
- 2004-06-18 NZ NZ544150A patent/NZ544150A/en unknown
- 2004-06-18 AU AU2004251846A patent/AU2004251846B2/en not_active Ceased
- 2004-06-18 AT AT04737037T patent/ATE383329T1/de active
- 2004-06-18 JP JP2006515996A patent/JP4471974B2/ja not_active Expired - Lifetime
- 2004-06-18 BR BRPI0411906-1A patent/BRPI0411906A/pt not_active IP Right Cessation
- 2004-06-18 TW TW093117590A patent/TWI302532B/zh not_active IP Right Cessation
- 2004-06-18 WO PCT/EP2004/006611 patent/WO2005000781A1/en active IP Right Grant
- 2004-06-18 PT PT04737037T patent/PT1663936E/pt unknown
- 2004-06-18 TW TW096149048A patent/TW200817350A/zh unknown
- 2004-06-18 KR KR1020057024639A patent/KR100809205B1/ko not_active IP Right Cessation
- 2004-06-18 PL PL04737037T patent/PL1663936T3/pl unknown
- 2004-06-18 CA CA002529875A patent/CA2529875A1/en not_active Abandoned
- 2004-06-18 ES ES04737037T patent/ES2298761T3/es not_active Expired - Lifetime
- 2004-06-18 DK DK04737037T patent/DK1663936T3/da active
- 2004-06-18 EP EP04737037A patent/EP1663936B1/en not_active Expired - Lifetime
- 2004-06-18 DE DE602004011239T patent/DE602004011239T2/de not_active Expired - Lifetime
- 2004-06-18 MX MXPA05014082A patent/MXPA05014082A/es active IP Right Grant
- 2004-06-22 AR ARP040102167A patent/AR044856A1/es unknown
- 2004-06-22 MY MYPI20042429A patent/MY138708A/en unknown
-
2005
- 2005-12-15 IL IL172617A patent/IL172617A0/en unknown
- 2005-12-16 NO NO20056010A patent/NO20056010L/no not_active Application Discontinuation
- 2005-12-21 CO CO05128644A patent/CO5640098A2/es not_active Application Discontinuation
-
2007
- 2007-01-25 HK HK07100892.2A patent/HK1093724A1/xx not_active IP Right Cessation
-
2008
- 2008-01-08 US US11/970,620 patent/US7700632B2/en not_active Expired - Fee Related
- 2008-06-13 US US12/138,459 patent/US7842825B2/en not_active Expired - Fee Related
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