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AR038868A1 - Derivados de 1-(2-aminoacetil)2-pirrolidincarbonitrilo, su uso para la preparacion de una formulacion farmaceutica, las formulaciones farmaceuticas que los contienen, un procedimiento para la preparacion de estos derivados, y los intermediarios y su uso en dicho procedimiento de preparacion - Google Patents

Derivados de 1-(2-aminoacetil)2-pirrolidincarbonitrilo, su uso para la preparacion de una formulacion farmaceutica, las formulaciones farmaceuticas que los contienen, un procedimiento para la preparacion de estos derivados, y los intermediarios y su uso en dicho procedimiento de preparacion

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Publication number
AR038868A1
AR038868A1 ARP030100723A ARP030100723A AR038868A1 AR 038868 A1 AR038868 A1 AR 038868A1 AR P030100723 A ARP030100723 A AR P030100723A AR P030100723 A ARP030100723 A AR P030100723A AR 038868 A1 AR038868 A1 AR 038868A1
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AR
Argentina
Prior art keywords
group
preparation
formula
compounds
derivatives
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Application number
ARP030100723A
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English (en)
Inventor
Eva Boronkay
Philippe Bovy
Karoly Kanai
Zoltan Kapui
Edit Susan
Tibor Szabo
Mark A Nagy
Marton Varga
Peter Aranyi
Laszlo Balazs
Imre Bata
Katalin Urban-Szabo
Sandor Batori
Original Assignee
Sanofi Aventis
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Publication date
Application filed by Sanofi Aventis filed Critical Sanofi Aventis
Publication of AR038868A1 publication Critical patent/AR038868A1/es

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    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
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    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
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    • C07D451/14—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof

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  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Virology (AREA)
  • Dermatology (AREA)
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Abstract

Derivados de 1-(2-aminoacetil)-2-pirrolidincarbonitrilo, de fórmula general (1), en donde: R1 significa una unidad aromática que contiene N que consiste en uno o dos anillos aromáticos, preferiblemente anillo(s) piridilo, piridazinilo, pirimidinilo, pirazinilo, imidazolilo, pirazolilo, tiazolilo, isotiazolilo, oxazolilo, isoxazolilo, oxadiazolilo, quinolinilo, isoquinolinilo, cinolinilo, ftalazinilo, quinazolinilo, quinoxalinilo, benzimidazolilo, indazolilo, benzotiazolilo, benzisotiazolilo, benzoxazolilo o benzisoxazolilo, tetrazolilo, triazinilo; que en un caso determinado, está(n) mono- o disustituido(s) independientemente uno del otro por uno o dos de los siguientes grupos: grupos alquilo C1-4, alcoxi C1-4, átomo de halógeno, grupo trihalogenometilo, grupo metiltio, grupo nitro, ciano, amino o fenilo; o un grupo tienilo, furilo o bencilo; o un grupo p-toluensulfonilo; o un grupo acilo de fórmula R1a-CO, donde R1a significa un grupo alquilo C1-4, grupo fenilo; grupo fenilo, piridilo o feniletenilo sustituido con uno o más grupo(s) alquilo y/o alcoxi o nitro o átomo de halógeno, grupo feniletenilo o feniletilo sustituido con un grupo alquilendioxi; grupo piperidin-1-ilo, 4-metilpiperazin-1-ilo, pirrolidin-1-ilo, B representa un resto seleccionado del grupo de fórmulas (2); R2 representa un átomo de H o un átomo de F; R3 representa un átomo de F; y sales, isómeros, tautómeros, solvatos e hidratos de los mismos. Estos compuestos son inhibidores efectivos, estables y seguros de la enzima dipeptidil-peptidasa-IV (DPP-IV), y son adecuados para el tratamiento y la prevención de la diabetes y de otras enfermedades relacionadas con la actividad enzimática de la DPP-IV: También describe el uso de estos compuestos para la preparación de una formulación farmacéutica, una formulación farmacéutica que comprende un compuesto de fórmula (1), y un procedimiento para la preparación de los compuestos de fórmula (1). Asimismo, se describen los intermediarios que se utilizan en la preparación de dichos compuestos de fórmula (1).
ARP030100723A 2002-03-06 2003-03-05 Derivados de 1-(2-aminoacetil)2-pirrolidincarbonitrilo, su uso para la preparacion de una formulacion farmaceutica, las formulaciones farmaceuticas que los contienen, un procedimiento para la preparacion de estos derivados, y los intermediarios y su uso en dicho procedimiento de preparacion AR038868A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
HU0200849A HUP0200849A2 (hu) 2002-03-06 2002-03-06 N-aminoacetil-2-ciano-pirrolidin-származékok, e vegyületeket tartalmazó gyógyszerkészítmények és eljárás előállításukra

Publications (1)

Publication Number Publication Date
AR038868A1 true AR038868A1 (es) 2005-02-02

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ARP030100723A AR038868A1 (es) 2002-03-06 2003-03-05 Derivados de 1-(2-aminoacetil)2-pirrolidincarbonitrilo, su uso para la preparacion de una formulacion farmaceutica, las formulaciones farmaceuticas que los contienen, un procedimiento para la preparacion de estos derivados, y los intermediarios y su uso en dicho procedimiento de preparacion

Country Status (28)

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US (3) US7348327B2 (es)
EP (1) EP1487807B1 (es)
JP (1) JP4559737B2 (es)
KR (1) KR100977898B1 (es)
CN (2) CN1639159A (es)
AR (1) AR038868A1 (es)
AT (1) ATE443054T1 (es)
AU (1) AU2003209514B2 (es)
BR (1) BR0307960A (es)
CA (1) CA2475312C (es)
DE (1) DE60329282D1 (es)
EA (1) EA007410B1 (es)
EC (1) ECSP045274A (es)
HR (1) HRP20040910A2 (es)
HU (1) HUP0200849A2 (es)
IL (2) IL163286A (es)
IS (1) IS7434A (es)
MA (1) MA27105A1 (es)
MX (1) MXPA04008613A (es)
NO (1) NO20044221L (es)
NZ (1) NZ535662A (es)
PL (1) PL371099A1 (es)
RS (1) RS79004A (es)
TN (1) TNSN04141A1 (es)
TW (1) TWI250978B (es)
UA (1) UA78291C2 (es)
WO (1) WO2003074500A2 (es)
ZA (1) ZA200406467B (es)

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ATE370943T1 (de) * 2001-06-27 2007-09-15 Smithkline Beecham Corp Fluoropyrrolidine als dipeptidyl-peptidase inhibitoren
HUP0202001A2 (hu) * 2002-06-14 2005-08-29 Sanofi-Aventis DDP-IV gátló hatású azabiciklooktán- és nonánszármazékok
TW200401635A (en) * 2002-07-23 2004-02-01 Yamanouchi Pharma Co Ltd 2-Cyano-4-fluoropyrrolidine derivative or salt thereof
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
KR20050122220A (ko) 2003-03-25 2005-12-28 다케다 샌디에고, 인코포레이티드 디펩티딜 펩티다제 억제제
WO2004098591A2 (en) 2003-05-05 2004-11-18 Probiodrug Ag Inhibitors of glutaminyl cyclase and their use in the treatment of neurological diseases
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JP2005529078A (ja) 2005-09-29
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CN1639159A (zh) 2005-07-13
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US7655663B2 (en) 2010-02-02
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US7348327B2 (en) 2008-03-25
PL371099A1 (en) 2005-06-13
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