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CO5600998A2 - Fluoropirrolidinas como inhibidores de dipeptidil peptidasa - Google Patents

Fluoropirrolidinas como inhibidores de dipeptidil peptidasa

Info

Publication number
CO5600998A2
CO5600998A2 CO03111632A CO03111632A CO5600998A2 CO 5600998 A2 CO5600998 A2 CO 5600998A2 CO 03111632 A CO03111632 A CO 03111632A CO 03111632 A CO03111632 A CO 03111632A CO 5600998 A2 CO5600998 A2 CO 5600998A2
Authority
CO
Colombia
Prior art keywords
alkyl
heteroaryl
optionally substituted
aryl
fluoropirrolidins
Prior art date
Application number
CO03111632A
Other languages
English (en)
Inventor
Curt Dale Haffner
Darryl Lynn Mc-Dougald
Amarjit Sab Randhawa
Steven Michael Resiter
James Martin Lenhard
Original Assignee
Smithkline Beecham Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of CO5600998A2 publication Critical patent/CO5600998A2/es

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    • 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
    • C07D207/18—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—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 one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
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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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    • C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
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Abstract

1.- Un compuesto de la fórmula (I): incluyendo sales, solvatos y derivados farmacéuticamente funcionales de los mismos, en donde: X es F o H; R1 y R2 cada son ya sea (i) H; (j) alquilo; (iii) arilo o heteroarilo opcionalmente substituido; o (iv) se combinan para formar un sistema de anillo de 3 a 14 miembros, opcionalmente conteniendo uno o más átomos heterogéneos, y opcionalmente conteniendo uno o más grados de instauración;en donde R1 y R2 son (iii), entonces R3 es H o alquilo;cuando R1 y R2 son (i), (ii) o (iv), entonces R3 es: en donde n es 0-5;m es 0-12;Y es S(O)p, O, alquileno, alquenileno, alquinileno, o un enlace;p es 0-2;R4 y R5 cuando Y es S, O, alquileno, alquenileno, alquinileno, o un enlace, en donde R5 es alquilo, alquenilo, alquinilo, arilo, cicloalquilo, heteroarilo, o heterociclico opcionalmente substituido;R4 es R6 cuando Y es S(O) o S(O)2, en donde R6 es alquilo, arilo, cicloalquilo, heteroarilo, amino, alquilamino, arilamino, heteroarilamino, cicloalquilamino, o hidroxi opcionalmente substituido.34.- Una formulación farmacéutica que comprende un compuesto de acuerdo con las reivindicaciones 1 a 33.
CO03111632A 2001-06-27 2003-12-22 Fluoropirrolidinas como inhibidores de dipeptidil peptidasa CO5600998A2 (es)

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US30133301P 2001-06-27 2001-06-27
US37601502P 2002-04-26 2002-04-26

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EP (2) EP1862457B1 (es)
JP (3) JP3909056B2 (es)
KR (1) KR20040015298A (es)
CN (3) CN1990468A (es)
AT (2) ATE455759T1 (es)
AU (1) AU2002322344C1 (es)
BR (1) BR0210644A (es)
CA (1) CA2450722A1 (es)
CO (1) CO5600998A2 (es)
CZ (1) CZ20033521A3 (es)
DE (2) DE60222667T2 (es)
ES (2) ES2339813T3 (es)
HU (1) HUP0400321A2 (es)
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MX (1) MXPA03011907A (es)
NO (1) NO20035603D0 (es)
NZ (1) NZ529973A (es)
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US7687625B2 (en) 2003-03-25 2010-03-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
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