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    14.
    发明专利
    未知

    公开(公告)号：DE602005001576T2

    公开(公告)日：2008-04-17

    申请号：DE602005001576

    申请日：2005-05-18

    Applicant: SERVIER LAB

    Inventor： DE NANTEUIL GUILLAUME ,  BENOIST ALAIN ,  COMBETTES MURIELLE ,  HARLEY ELIZABETH

    IPC: C07D295/18 ,  C07D405/12 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/426 ,  A61K31/427 ,  A61K31/438 ,  A61P3/10 ,  A61P43/00 ,  C07D207/06 ,  C07D207/10 ,  C07D207/16 ,  C07D277/06 ,  C07D277/12 ,  C07D295/185 ,  C07D311/96 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12

    Abstract: Spiro-cycloalkyl N-acyl pyrrolidine or thiazolidine derivatives (I), their optical isomers and acid addition salts are new. Spiro-cycloalkyl N-acyl pyrrolidine or thiazolidine derivatives of formula (I), and their optical isomers and acid addition salts, are new. X 1CR 4aR 4b, O, S(O) q1 or NR 5; R 4a and R 4bhydrogen or 1-6 C linear or branched alkyl or together complete a 3-7C cycloalkyl; q1 : 0-2; R 5hydrogen or 1-6C linear or branched alkyl, optionally substituted by hydroxy; m1 : 0-4; m2 : 1-4; n1 and n2 : 1-3; R 1hydrogen, carboxy, 1-6C linear or branched alkoxycarbonyl, carbamoyl (optionally substituted by 1 or 2 1-6C linear or branched alkyl), or 1-6C linear or branched alkyl (optionally substituted by hydroxy) or amino (optionally substituted by 1 or 2 1-6C linear or branched alkyl); R 2hydrogen or 1-6C linear or branched alkyl; Ak : 1-4C linear or branched alkylene, optionally substituted by one or more halo, particularly fluoro; p : 0-2; R 3hydrogen or cyano; X 2 and X 3S(O) q2 or CR 6aR 6b; R 6a and R 6bhydrogen or halo, preferably fluoro, or R 6a = hydrogen and R 6b = hydroxy; and q2 : 0-2. An independent claim is also included for the preparation of (I). [Image] ACTIVITY : Antidiabetic; Anorectic. MECHANISM OF ACTION : Inhibition of dipeptidyl-peptidase IV (DPPIV). The compound (2S)-1-({[9-(hydroxymethyl)-3-oxaspiro[5,5]undec-9-yl]amino}acetyl)-2-pyrrolidinecarbonitrile had IC 50 76.1 nM against porcine renal DPPIV, in an assay based on cleavage of Gly-Pro-p-nitroanilide.

    16.
    发明专利
    未知

    公开(公告)号：AT366731T

    公开(公告)日：2007-08-15

    申请号：AT05291066

    申请日：2005-05-18

    Applicant: SERVIER LAB

    Inventor： DE NANTEUIL GUILLAUME ,  BENOIST ALAIN ,  COMBETTES MURIELLE ,  HARLEY ELIZABETH

    IPC: C07D295/18 ,  C07D405/12 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/426 ,  A61K31/427 ,  A61K31/438 ,  A61P3/10 ,  A61P43/00 ,  C07D207/06 ,  C07D207/10 ,  C07D207/16 ,  C07D277/06 ,  C07D277/12 ,  C07D295/185 ,  C07D311/96 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12

    Abstract: Spiro-cycloalkyl N-acyl pyrrolidine or thiazolidine derivatives (I), their optical isomers and acid addition salts are new. Spiro-cycloalkyl N-acyl pyrrolidine or thiazolidine derivatives of formula (I), and their optical isomers and acid addition salts, are new. X 1CR 4aR 4b, O, S(O) q1 or NR 5; R 4a and R 4bhydrogen or 1-6 C linear or branched alkyl or together complete a 3-7C cycloalkyl; q1 : 0-2; R 5hydrogen or 1-6C linear or branched alkyl, optionally substituted by hydroxy; m1 : 0-4; m2 : 1-4; n1 and n2 : 1-3; R 1hydrogen, carboxy, 1-6C linear or branched alkoxycarbonyl, carbamoyl (optionally substituted by 1 or 2 1-6C linear or branched alkyl), or 1-6C linear or branched alkyl (optionally substituted by hydroxy) or amino (optionally substituted by 1 or 2 1-6C linear or branched alkyl); R 2hydrogen or 1-6C linear or branched alkyl; Ak : 1-4C linear or branched alkylene, optionally substituted by one or more halo, particularly fluoro; p : 0-2; R 3hydrogen or cyano; X 2 and X 3S(O) q2 or CR 6aR 6b; R 6a and R 6bhydrogen or halo, preferably fluoro, or R 6a = hydrogen and R 6b = hydroxy; and q2 : 0-2. An independent claim is also included for the preparation of (I). [Image] ACTIVITY : Antidiabetic; Anorectic. MECHANISM OF ACTION : Inhibition of dipeptidyl-peptidase IV (DPPIV). The compound (2S)-1-({[9-(hydroxymethyl)-3-oxaspiro[5,5]undec-9-yl]amino}acetyl)-2-pyrrolidinecarbonitrile had IC 50 76.1 nM against porcine renal DPPIV, in an assay based on cleavage of Gly-Pro-p-nitroanilide.

    19.
    发明专利
    未知

    公开(公告)号：FR2870538B1

    公开(公告)日：2006-07-14

    申请号：FR0405454

    申请日：2004-05-19

    Applicant: SERVIER LAB

    Inventor： DE NANTEUIL GUILLAUME ,  BENOIST ALAIN ,  COMBETTES MURIELLE ,  HARLEY ELIZABETH

    IPC: C07D207/16 ,  C07D295/18 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/426 ,  A61K31/427 ,  A61K31/438 ,  A61P3/10 ,  A61P43/00 ,  C07D207/06 ,  C07D207/10 ,  C07D277/04 ,  C07D277/06 ,  C07D277/12 ,  C07D295/185 ,  C07D311/96 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

    Abstract: Spiro-cycloalkyl N-acyl pyrrolidine or thiazolidine derivatives (I), their optical isomers and acid addition salts are new. Spiro-cycloalkyl N-acyl pyrrolidine or thiazolidine derivatives of formula (I), and their optical isomers and acid addition salts, are new. X 1CR 4aR 4b, O, S(O) q1 or NR 5; R 4a and R 4bhydrogen or 1-6 C linear or branched alkyl or together complete a 3-7C cycloalkyl; q1 : 0-2; R 5hydrogen or 1-6C linear or branched alkyl, optionally substituted by hydroxy; m1 : 0-4; m2 : 1-4; n1 and n2 : 1-3; R 1hydrogen, carboxy, 1-6C linear or branched alkoxycarbonyl, carbamoyl (optionally substituted by 1 or 2 1-6C linear or branched alkyl), or 1-6C linear or branched alkyl (optionally substituted by hydroxy) or amino (optionally substituted by 1 or 2 1-6C linear or branched alkyl); R 2hydrogen or 1-6C linear or branched alkyl; Ak : 1-4C linear or branched alkylene, optionally substituted by one or more halo, particularly fluoro; p : 0-2; R 3hydrogen or cyano; X 2 and X 3S(O) q2 or CR 6aR 6b; R 6a and R 6bhydrogen or halo, preferably fluoro, or R 6a = hydrogen and R 6b = hydroxy; and q2 : 0-2. An independent claim is also included for the preparation of (I). [Image] ACTIVITY : Antidiabetic; Anorectic. MECHANISM OF ACTION : Inhibition of dipeptidyl-peptidase IV (DPPIV). The compound (2S)-1-({[9-(hydroxymethyl)-3-oxaspiro[5,5]undec-9-yl]amino}acetyl)-2-pyrrolidinecarbonitrile had IC 50 76.1 nM against porcine renal DPPIV, in an assay based on cleavage of Gly-Pro-p-nitroanilide.

    COMPUESTOS DE PIRROLIDINA Y TIAZOLIDINA, PROCEDIMIENTO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN
    20.
    发明专利
    COMPUESTOS DE PIRROLIDINA Y TIAZOLIDINA, PROCEDIMIENTO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN 未知

    公开(公告)号：AR049278A1

    公开(公告)日：2006-07-12

    申请号：ARP050102045

    申请日：2005-05-18

    Applicant: SERVIER LAB

    Inventor： DE NANTEUIL GUILLAUME ,  BENOIST ALAIN ,  COMBETTES MURIELLE ,  HARLEY ELIZABETH

    IPC: C07D295/18 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/426 ,  A61K31/427 ,  A61K31/438 ,  A61P3/10 ,  A61P43/00 ,  C07D207/06 ,  C07D207/10 ,  C07D207/16 ,  C07D277/06 ,  C07D277/12 ,  C07D295/185 ,  C07D311/96 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  A61P3/04 ,  C07D335/04 ,  C07D221/20

    Abstract: Reivindicacion 1: Compuesto de formula (1), en la cual: X1 representa un átomo o un grupo seleccionado entre CR4aR4b, O, S(O)q1 y NR5, donde R4a y R4b que pueden ser idénticos o diferentes, representan, cada uno ellos, un átomo de hidrogeno o un grupo alquilo C1-6 lineal o ramificado; o R4a y R4b conjuntamente forman, con el átomo de carbono que los transporta, un grupo cicloalquilo C3-7; q1 representa cero, 1 o 2; y R5 representa un átomo de hidrogeno o un grupo alquilo C1-6 lineal o ramificado opcionalmente sustituido por un grupo hidroxi; m1 representa cero o un entero que oscila entre 1 y 4 inclusive; m2 representa un entero que oscila entre 1 y 4 inclusive; n1 y n2, que pueden ser idénticos o diferentes, cada uno representa un entero que oscila entre 1 y 3 inclusive; R1 representa un átomo de hidrogeno o un grupo seleccionado entre carboxi, alcoxicarbonilo C1-6 lineal o ramificado, carbamoilo opcionalmente sustituido por 1 o 2 grupos alquilo C1-6 lineal o ramificado, y alquilo C1-6 lineal o ramificado opcionalmente sustituido por un grupo hidroxi o por un grupo amino opcionalmente sustituido por 1 o 2 grupos alquilo C1-6 lineal o ramificado; R2 representa un átomo de hidrogeno o un grupo alquilo C1-6 lineal o ramificado; Ak representa una cadena de alquileno C1-4 lineal o ramificada opcionalmente sustituida por uno o más átomos de halogeno; p representa cero, 1 o 2; R3 representa un átomo de hidrogeno o un grupo ciano; X2 y X3, que pueden ser idénticos o diferentes, cada uno representa un grupo S(O)q2, donde q2 representa cero, 1 o 2, o bien un grupo CR6aR6b, donde R6a y R6b, que pueden ser idénticos o diferentes, cada uno representa un átomo de hidrogeno o un átomo de halogeno, o R6b representa un átomo de hidrogeno y R6b representa un grupo hidroxi, sus isomeros, cuando estén presentes, y sus sales de adicion con un ácido farmacéuticamente aceptable.

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