AR041467A1 - Indol-3-carboxamidas como activadores de glucoquinasa (gk) - Google Patents
Indol-3-carboxamidas como activadores de glucoquinasa (gk)Info
- Publication number
- AR041467A1 AR041467A1 ARP030103589A ARP030103589A AR041467A1 AR 041467 A1 AR041467 A1 AR 041467A1 AR P030103589 A ARP030103589 A AR P030103589A AR P030103589 A ARP030103589 A AR P030103589A AR 041467 A1 AR041467 A1 AR 041467A1
- Authority
- AR
- Argentina
- Prior art keywords
- carbon atom
- ring
- heteroaromatic ring
- trifluoromethyl
- cyano
- Prior art date
Links
- 239000012190 activator Substances 0.000 title 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 4
- 229910052799 carbon Inorganic materials 0.000 abstract 4
- 125000004432 carbon atom Chemical group C* 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- -1 nitro, amino, cyano, methyl Chemical group 0.000 abstract 2
- 229910052757 nitrogen Chemical group 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 abstract 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 1
- 102000030595 Glucokinase Human genes 0.000 abstract 1
- 108010021582 Glucokinase Proteins 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical group BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 239000000460 chlorine Chemical group 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 230000003914 insulin secretion Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 239000011593 sulfur Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom 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
- A61P3/08—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
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se proporciona compuestos de glucoquinasa que son útiles para incrementar la secreción de insulina en el tratamiento de diabetes de tipo II. También se reivindica proceso de obtención y composición farmacéutica. Reivindicación 1: Un compuesto de la fórmula (1), en donde: R1 es halógeno, nitro, amino, ciano, metilo, trifluorometilo, hidroxilo, metoxilo, trifluorometoxilo, metiltio, metilsulfinilo, o metilsulfonilo; R2 es alquilo inferior C2-5 o -CH2-R4 en donde R4 es cicloalquilo C3-6; y R3 es un anillo heteroaromático de cinco o seis miembros mono sustituido o no sustituido conectado por un átomo de carbono del anillo al grupo amina mostrado, cuyo anillo heteroaromático de cinco o seis miembros contiene de 1 a 3 heteroátomos seleccionados de azufre, oxígeno o nitrógeno, con un heteroátomo siendo nitrógeno que está adyacente al átomo de carbono del anillo enlanzante; dicho anillo heteroaromático mono sustituido siendo monosustituido en una posición en un átomo de carbono del anillo otro que el adyacente a dicho átomo de carbono enlazante con un sustituyente seleccionado del grupo que consiste en metilo, trifluorometilo, cloro, bromo, nitro, ciano, o un resto de grupo de fórmula (2); en donde n es 0 ó 1; y R5 es hidrógeno o alquilo inferior; o una sal aceptable farmacéuticamente de la misma.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41573702P | 2002-10-03 | 2002-10-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR041467A1 true AR041467A1 (es) | 2005-05-18 |
Family
ID=32069904
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030103589A AR041467A1 (es) | 2002-10-03 | 2003-10-01 | Indol-3-carboxamidas como activadores de glucoquinasa (gk) |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US6881844B2 (es) |
| EP (1) | EP1549638B1 (es) |
| JP (1) | JP4390704B2 (es) |
| KR (1) | KR100646486B1 (es) |
| CN (1) | CN100348596C (es) |
| AR (1) | AR041467A1 (es) |
| AT (1) | ATE374768T1 (es) |
| AU (1) | AU2003270285B2 (es) |
| BR (1) | BR0315047A (es) |
| CA (1) | CA2499329C (es) |
| DE (1) | DE60316709T2 (es) |
| DK (1) | DK1549638T3 (es) |
| ES (1) | ES2293005T3 (es) |
| HR (1) | HRP20050287A2 (es) |
| MX (1) | MXPA05003391A (es) |
| MY (1) | MY136764A (es) |
| NO (1) | NO20051103L (es) |
| NZ (1) | NZ538466A (es) |
| PA (1) | PA8584001A1 (es) |
| PE (1) | PE20050090A1 (es) |
| PL (1) | PL375149A1 (es) |
| PT (1) | PT1549638E (es) |
| RU (1) | RU2309956C2 (es) |
| SI (1) | SI1549638T1 (es) |
| TW (1) | TW200413364A (es) |
| UY (1) | UY28005A1 (es) |
| WO (1) | WO2004031179A1 (es) |
| ZA (1) | ZA200502619B (es) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE0102299D0 (sv) | 2001-06-26 | 2001-06-26 | Astrazeneca Ab | Compounds |
| SE0102764D0 (sv) | 2001-08-17 | 2001-08-17 | Astrazeneca Ab | Compounds |
| JP2006509774A (ja) * | 2002-10-03 | 2006-03-23 | ノバルティス アクチエンゲゼルシャフト | ２型糖尿病の処置において有用なグルコキナーゼアクチベーターとしての置換（チアゾール−２−イル）−アミドまたはスルホンアミド |
| GB0226930D0 (en) * | 2002-11-19 | 2002-12-24 | Astrazeneca Ab | Chemical compounds |
| GB0226931D0 (en) | 2002-11-19 | 2002-12-24 | Astrazeneca Ab | Chemical compounds |
| EP1532980A1 (en) * | 2003-11-24 | 2005-05-25 | Novo Nordisk A/S | N-heteroaryl indole carboxamides and analogues thereof, for use as glucokinase activators in the treatment of diabetes |
| BRPI0509573A (pt) | 2004-04-02 | 2007-09-25 | Novartis Ag | derivados de sulfonamida-tiazolpiridina como ativadores de glicocinase úteis para o tratamento de diabetes do tipo 2 |
| BRPI0509543A (pt) | 2004-04-02 | 2007-09-18 | Novartis Ag | derivados de tiazolopiridina, condições farmacêuticas que contêm os mesmos e métodos para tratar condições mediadas por glucocinase |
| JP5094394B2 (ja) | 2005-04-20 | 2012-12-12 | 武田薬品工業株式会社 | 縮合複素環化合物 |
| JP4651714B2 (ja) | 2005-07-09 | 2011-03-16 | アストラゼネカ アクチボラグ | 糖尿病の治療においてｇｌｋ活性化剤として使用するためのヘテロアリールベンズアミド誘導体 |
| US7622492B2 (en) | 2005-08-31 | 2009-11-24 | Hoffmann-La Roche Inc. | Pyrazolones as inhibitors of 11β-hydroxysteroid dehydrogenase |
| JP2007063225A (ja) | 2005-09-01 | 2007-03-15 | Takeda Chem Ind Ltd | イミダゾピリジン化合物 |
| RU2008112198A (ru) | 2005-09-29 | 2009-10-10 | Санофи-Авентис (Fr) | Производные фенил-1,2,4-оксадиазолона, способы их получения и их применение в качестве фармацевтических средств |
| GT200600428A (es) * | 2005-09-30 | 2007-05-21 | Compuestos organicos | |
| US7799820B2 (en) | 2005-09-30 | 2010-09-21 | Banyu Pharmaceutical Co., Ltd. | 2-Heterocycle-substituted indole derivatives for treating diabetes and associated conditions |
| GT200600429A (es) * | 2005-09-30 | 2007-04-30 | Compuestos organicos | |
| JP2009013065A (ja) * | 2005-10-14 | 2009-01-22 | Astellas Pharma Inc | 縮合へテロ環化合物 |
| JP2009515997A (ja) * | 2005-11-18 | 2009-04-16 | タケダ サン ディエゴ インコーポレイテッド | グルコキナーゼ活性剤 |
| US7351706B2 (en) * | 2006-01-05 | 2008-04-01 | Hoffmann-La Roche Inc. | Indol-3-yl-carbonyl-spiro-piperidine derivatives |
| US8034822B2 (en) | 2006-03-08 | 2011-10-11 | Takeda San Diego, Inc. | Glucokinase activators |
| EP1849785A1 (en) * | 2006-04-28 | 2007-10-31 | Neuropharma, S.A. | N-(2-Thiazolyl)-amide derivatives as GSK-3 inhibitors |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| US8008332B2 (en) | 2006-05-31 | 2011-08-30 | Takeda San Diego, Inc. | Substituted indazoles as glucokinase activators |
| CN101573357B (zh) | 2006-10-19 | 2013-01-23 | 武田药品工业株式会社 | 吲哚化合物 |
| JP5419706B2 (ja) | 2006-12-20 | 2014-02-19 | タケダ カリフォルニア インコーポレイテッド | グルコキナーゼアクチベーター |
| WO2008074694A1 (en) * | 2006-12-20 | 2008-06-26 | F. Hoffmann-La Roche Ag | Crystallization of glucokinase activators |
| WO2008116107A2 (en) | 2007-03-21 | 2008-09-25 | Takeda San Diego, Inc. | Piperazine derivatives as glucokinase activators |
| AU2008286946B2 (en) * | 2007-08-10 | 2013-11-21 | H. Lundbeck A/S | Heteroaryl amide analogues |
| CL2009001203A1 (es) | 2008-05-16 | 2009-10-23 | Takeda San Diego Inc | Compuestos derivados de indazol y pirazol sustituidos; composicion farmaceutica de dichos compuestos; kit farmaceutico; y su uso como activadores de la glucoquinasa para tratar enfermedades metabolicas tales como hiperglicemia, diabetes, dislipidemias, obesidad, sindrome metabolico x y enfermedades cardiovasculares. |
| WO2010107736A2 (en) * | 2009-03-20 | 2010-09-23 | University Of Virginia Patent Foundation | Broad spectrum benzothiophene-nitrothiazolide and other antimicrobials |
| JP2011006366A (ja) | 2009-06-26 | 2011-01-13 | Sanwa Kagaku Kenkyusho Co Ltd | 新規チオフェンカルボキサミド誘導体及びその医薬用途 |
| EP2632460B1 (en) | 2010-09-20 | 2018-02-28 | University of Virginia Patent Foundation | Thiophene derivatives for use in the treatment of tuberculosis |
| CN103044310B (zh) * | 2013-01-18 | 2015-02-04 | 贵阳医学院 | 二氢吲哚-3-乙酸衍生物、其制备方法以及在药物中的应用 |
| CA3235833A1 (en) * | 2021-10-20 | 2023-04-27 | Council Of Scientific And Industrial Research An Indian Registered Body Incorporated Under The Regn. Of Soc. Act (Act Xxi Of 1860) | A method for the preparation of indole-3-carboxylic acid derivatives |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2716194B1 (fr) * | 1994-02-14 | 1996-05-31 | Sanofi Elf | Dérivés de 3-acylamino-5-phényl-1,4-benzodiazépin-2-one polysubstitués, leur procédé de préparation et les compositions pharmaceutiques les contenant. |
| FR2740686B1 (fr) | 1995-11-03 | 1998-01-16 | Sanofi Sa | Formulation pharmaceutique lyophilisee stable |
| FR2763337B1 (fr) * | 1997-05-13 | 1999-08-20 | Sanofi Sa | Nouveaux derives du triazole, un procede pour leur preparation et compositions pharmaceutiques les contenant |
| US6040321A (en) | 1997-11-12 | 2000-03-21 | Bristol-Myers Squibb Company | Aminothiazole inhibitors of cyclin dependent kinases |
| US6262096B1 (en) | 1997-11-12 | 2001-07-17 | Bristol-Myers Squibb Company | Aminothiazole inhibitors of cyclin dependent kinases |
| JP5278983B2 (ja) | 1999-11-17 | 2013-09-04 | 塩野義製薬株式会社 | アミド化合物の新規用途 |
| US6433188B1 (en) | 2000-12-06 | 2002-08-13 | Wendy Lea Corbett | Fused heteroaromatic glucokinase activators |
| ATE316965T1 (de) | 2000-12-06 | 2006-02-15 | Hoffmann La Roche | Kondensierte heteroaromatische glucokinaseaktivatoren |
| US6482951B2 (en) | 2000-12-13 | 2002-11-19 | Hoffmann-La Roche Inc. | Isoindolin-1-one glucokinase activators |
| CA2430978C (en) * | 2000-12-28 | 2012-05-15 | Daiichi Pharmaceutical Co., Ltd. | Vla-4 inhibitors |
| UA77303C2 (en) * | 2002-06-14 | 2006-11-15 | Pfizer | Derivatives of thienopyridines substituted by benzocondensed heteroarylamide useful as therapeutic agents, pharmaceutical compositions and methods for their use |
-
2003
- 2003-09-26 AT AT03750648T patent/ATE374768T1/de not_active IP Right Cessation
- 2003-09-26 ES ES03750648T patent/ES2293005T3/es not_active Expired - Lifetime
- 2003-09-26 AU AU2003270285A patent/AU2003270285B2/en not_active Ceased
- 2003-09-26 PT PT03750648T patent/PT1549638E/pt unknown
- 2003-09-26 BR BR0315047-0A patent/BR0315047A/pt not_active IP Right Cessation
- 2003-09-26 DE DE60316709T patent/DE60316709T2/de not_active Expired - Lifetime
- 2003-09-26 WO PCT/EP2003/010776 patent/WO2004031179A1/en not_active Ceased
- 2003-09-26 HR HR20050287A patent/HRP20050287A2/xx not_active Application Discontinuation
- 2003-09-26 CN CNB038236796A patent/CN100348596C/zh not_active Expired - Fee Related
- 2003-09-26 NZ NZ538466A patent/NZ538466A/en unknown
- 2003-09-26 EP EP03750648A patent/EP1549638B1/en not_active Expired - Lifetime
- 2003-09-26 PL PL03375149A patent/PL375149A1/xx not_active Application Discontinuation
- 2003-09-26 DK DK03750648T patent/DK1549638T3/da active
- 2003-09-26 SI SI200331008T patent/SI1549638T1/sl unknown
- 2003-09-26 JP JP2004540731A patent/JP4390704B2/ja not_active Expired - Fee Related
- 2003-09-26 CA CA002499329A patent/CA2499329C/en not_active Expired - Fee Related
- 2003-09-26 RU RU2005113719/04A patent/RU2309956C2/ru not_active IP Right Cessation
- 2003-09-26 MX MXPA05003391A patent/MXPA05003391A/es active IP Right Grant
- 2003-09-26 KR KR1020057005669A patent/KR100646486B1/ko not_active Expired - Fee Related
- 2003-09-30 TW TW092127030A patent/TW200413364A/zh unknown
- 2003-09-30 PA PA20038584001A patent/PA8584001A1/es unknown
- 2003-09-30 PE PE2003000988A patent/PE20050090A1/es not_active Application Discontinuation
- 2003-09-30 US US10/674,481 patent/US6881844B2/en not_active Expired - Fee Related
- 2003-10-01 MY MYPI20033742A patent/MY136764A/en unknown
- 2003-10-01 AR ARP030103589A patent/AR041467A1/es unknown
- 2003-10-01 UY UY28005A patent/UY28005A1/es not_active Application Discontinuation
-
2005
- 2005-03-01 NO NO20051103A patent/NO20051103L/no not_active Application Discontinuation
-
2006
- 2006-01-19 ZA ZA200502619A patent/ZA200502619B/en unknown
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