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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Argentina
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group
preparation
formula
compounds
derivatives
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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
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Sanofi Aventis
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Publication of AR038868A1 publication Critical patent/AR038868A1/es

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    • C07D451/00—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
    • 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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    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • 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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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D401/14—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 three or more hetero rings
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    • 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
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    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
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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

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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