公开(公告)号：JP2001089472A

公开(公告)日：2001-04-03

申请号：JP2000236848

申请日：2000-08-04

Applicant: HOFFMANN LA ROCHE

Inventor： ADAM GEO ,  BINGGELI ALFRED ,  MAERKI HANS-PETER ,  MUTEL VINCENT ,  WILHELM MAURICE ,  WOSTL WOLFGANG

IPC: C07D223/16 ,  A61K31/55 ,  A61P1/08 ,  A61P3/08 ,  A61P9/04 ,  A61P9/10 ,  A61P13/10 ,  A61P21/02 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/34 ,  A61P27/02 ,  A61P43/00 ,  C07D223/04 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D521/00 ,  C07F7/18

Abstract: PROBLEM TO BE SOLVED: To provide an antagonist of metabotropic glutamate receptor. SOLUTION: The compound of the formula I, and a salt thereof pharmaceutically acceptable as a pharmaceutically active material are provided. A method for preparing them, a medicine based on the compound, a method for preparing the medicine, the use of the compound in the suppression or prevention of a disease, and the use in the preparation of the medicine corresponding thereto are also provided. The preferable compound in the compounds of the formula I is the one of the formula I wherein R1 is =O and R2 is CN, e.g. 3-ethyl-2- methyl-5-nitro-6-(1,2,4,5-tetrahydro-benz[d]azepin-3-yl)-3H-pyrimidin- 4-one and 2-amino-6-oxo-4-(1,2,4,5-tetrahydro-benz[d]azepin-3-yl)-1,6-dihydro-py rimidine-5- carbonitrile.

公开(公告)号：ES2332505T3

公开(公告)日：2010-02-08

申请号：ES02748720

申请日：2002-05-27

Applicant: HOFFMANN LA ROCHE

Inventor： BINGGELI ALFRED ,  MAERKI HANS-PETER ,  MASQUELIN THIERRY ,  MUTEL VINCENT ,  WILHELM MAURICE ,  WOSTL WOLFGANG

IPC: C07D241/26 ,  C07D253/06 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/513 ,  A61K31/53 ,  A61P1/08 ,  A61P7/12 ,  A61P9/00 ,  A61P9/02 ,  A61P9/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/34 ,  A61P25/36 ,  A61P27/02 ,  A61P43/00 ,  C07D239/46 ,  C07D239/47 ,  C07D239/48 ,  C07D239/50 ,  C07D253/075 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14

Abstract: Compuestos de la fórmula general: **(Ver fórmula)** en donde R1 significa nitro o ciano; R2 significa hidrógeno, alquilo (C1-C7) o -NHR10; y R10 significa hidrógeno, alquilo (C1-C7), -(CH2)n-OR11, -(CH2)p-cicloalquilo (C3-C6), -(CH2)m-NHC( O)O-alquilo (C1-C7), o (CH2)p-piridilo; y R11 significa hidrógeno o alquilo (C1-C7); R3 significa hidrógeno, alquilo (C1-C7), fluoro, hidroxi, alcoxi (C1-C7), alquiltio (C1-C7), ciano o nitro; R4 significa hidrógeno o fluoro; **(Ver fórmula)** significa: **(Ver fórmula)** en donde R5 significa hidrógeno, alquilo (C1-C7), alquenilo (C1-C7), -(CH2)m-OR11, fluoro-alquilo (C1-C7) o -(CH2)n-CN; R6 significa alquilo (C1-C7), halógeno, hidroxi, alcoxi (C1-C7), alquiltio (C1-C7), -O-(CH2)m-OR11, -Ofluoro- alquilo (C1-C7), o -NHR12; y R12 significa alquilo (C1-C7), -(CH2)m-OR11, -(CH2)p-ciclo-alquilo (C3-C6) o -(CH2)p-piridilo; R7 significa hidrógeno, alquilo (C1-C7) O fenilo; R8 significa hidrógeno, alquilo (C1-C7) o fenilo; Z significa: **(Ver fórmula)** en donde: R9 significa hidrógeno, hidroxi o ciano; m es independientemente uno de otro, en cada caso, 2, 3, 4, 5 o 6; n es independientemente uno de otro, en cada caso, 1, 2, 3, 4, 5 o 6; y p es independientemente uno de otro, en cada caso, 0, 1, 2, 3, 4, 5 o 6; así como también sus sales farmacéuticamente aceptables.

公开(公告)号：CA2230931C

公开(公告)日：2009-05-19

申请号：CA2230931

申请日：1996-08-29

Applicant: HOFFMANN LA ROCHE

Inventor： VIEIRA ERIC ,  BUR DANIEL ,  STADLER HEINZ ,  BREU VOLKER ,  FISCHLI WALTER ,  BINGGELI ALFRED ,  GULLER ROLF ,  MULLER MARCEL ,  HIRTH GEORGES ,  OEFNER CHRISTIAN ,  WOSTL WOLFGANG ,  WILHELM MAURICE ,  MARKI HANS-PETER

IPC: C07D211/18 ,  C07D211/42 ,  A61K31/435 ,  A61K31/439 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/451 ,  A61K31/4523 ,  A61K31/47 ,  A61K31/495 ,  A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P27/02 ,  C07D211/20 ,  C07D211/22 ,  C07D211/26 ,  C07D211/32 ,  C07D211/44 ,  C07D211/54 ,  C07D211/56 ,  C07D211/74 ,  C07D401/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/00 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/00 ,  C07D409/10 ,  C07D409/12 ,  C07D413/00 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/00 ,  C07D417/12 ,  C07D417/14 ,  C07D471/08 ,  C07D521/00 ,  C07F7/10

Abstract: The invention relates to novel piperidine derivatives of the general formula I (see formula I) wherein R1, R2, R3, R4, Q, W, X, Z, m and n have the meaning given in the specification. The novel piperidine derivatives can be used as renin inhibitors in the control or prevention of high blood pressure and cardiac insufficiency, as well as glaucoma, cardiac infarct, kidney insufficiency and restonosis.

公开(公告)号：AU2002216095B2

公开(公告)日：2005-12-01

申请号：AU2002216095

申请日：2001-12-11

Applicant: HOFFMANN LA ROCHE

Inventor： BINGGELI ALFRED ,  WILHELM MAURICE ,  MUTEL VINCENT ,  WOSTL WOLFGANG ,  MAERKI HANS-PETER

IPC: A61K31/495 ,  A61K31/53 ,  A61K31/55 ,  A61P1/08 ,  A61P9/10 ,  A61P13/02 ,  A61P19/00 ,  A61P21/00 ,  A61P21/04 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/36 ,  A61P27/02 ,  A61P43/00 ,  C07D403/04 ,  C07D495/04 ,  A61K031/53 ,  A61K031/495 ,  A61P025/00

Abstract: The invention relates to compounds which are represented by the formulawherein R1, R2, R3, R4, X and Y are as defined in the specification, as well as pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing these compounds and to a process for their preparation. The compounds possess affinity towards metabotropic glutamate receptors and are therefore useful in the treatment or prevention of acute and/or chronic neurological disorders.

公开(公告)号：ZA200304557B

公开(公告)日：2004-09-13

申请号：ZA200304557

申请日：2003-06-11

Applicant: HOFFMANN LA ROCHE

Inventor： BINGGELI ALFRED ,  MUTEL VINCENT ,  WOSTL WOLFGANG ,  MAERKI HANS-PETER ,  WILHELM MAURICE

IPC: A61K31/495 ,  A61K31/53 ,  A61K31/55 ,  A61P1/08 ,  A61P9/10 ,  A61P13/02 ,  A61P19/00 ,  A61P21/00 ,  A61P21/04 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/36 ,  A61P27/02 ,  A61P43/00 ,  C07D403/04 ,  C07D495/04 ,  A61K ,  C07D ,  A61P

Abstract: The invention relates to compounds which are represented by the formulawherein R1, R2, R3, R4, X and Y are as defined in the specification, as well as pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing these compounds and to a process for their preparation. The compounds possess affinity towards metabotropic glutamate receptors and are therefore useful in the treatment or prevention of acute and/or chronic neurological disorders.

公开(公告)号：BR0210102A

公开(公告)日：2004-06-08

申请号：BR0210102

申请日：2002-05-27

Applicant: HOFFMANN LA ROCHE

Inventor： BINGGELI ALFRED ,  MAERKI HANS-PETER ,  MASQUELIN THIERRY ,  MUTEL VINCENT ,  WILHELM MAURICE ,  WOSTL WOLFGANG

IPC: C07D253/06 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/513 ,  A61K31/53 ,  A61P1/08 ,  A61P7/12 ,  A61P9/00 ,  A61P9/02 ,  A61P9/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/34 ,  A61P25/36 ,  A61P27/02 ,  A61P43/00 ,  C07D239/46 ,  C07D239/47 ,  C07D239/48 ,  C07D239/50 ,  C07D241/26 ,  C07D253/075 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14

Abstract: The present invention is a pyrimidine, triazine or pyrazine derivative of the formula or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, R4, X, Y and Z are as defined in the specification. The invention is a pharmaceutical composition containing an effective amount of the compound of formula 1, its preparation and to a method of treatment, control or prevention of acute and/or chronic neurological disorders by administering a therapeutically effective amount of a compound of formula 1.

公开(公告)号：AT242213T

公开(公告)日：2003-06-15

申请号：AT96927715

申请日：1996-08-29

Applicant: HOFFMANN LA ROCHE

Inventor： BINGGELI ALFRED ,  BREU VOLKER ,  BUR DANIEL ,  FISCHLI WALTER ,  GUELLER ROLF ,  HIRTH GEORGES ,  MAERKI HANS-PETER ,  MUELLER MARCEL ,  OEFNER CHRISTIAN ,  STADLER HEINZ ,  VIEIRA ERIC ,  WILHELM MAURICE ,  WOSTL WOLFGANG

IPC: C07D211/18 ,  A61K31/439 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/451 ,  A61K31/4523 ,  A61K31/47 ,  A61K31/495 ,  A61K31/505 ,  A61K31/535 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P27/02 ,  C07D211/20 ,  C07D211/22 ,  C07D211/26 ,  C07D211/32 ,  C07D211/42 ,  C07D211/44 ,  C07D211/54 ,  C07D211/56 ,  C07D211/74 ,  C07D401/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/10 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/08 ,  C07D521/00

Abstract: Novel piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the novel piperidine derivatives of general formula I wherein R1, R2, R3, R4, Q, X, Z, m and n are as described herein.

公开(公告)号：CA2448602A1

公开(公告)日：2002-12-12

申请号：CA2448602

申请日：2002-05-27

Applicant: HOFFMANN LA ROCHE

Inventor： MAERKI HANS-PETER ,  MASQUELIN THIERRY ,  MUTEL VINCENT ,  WILHELM MAURICE ,  BINGGELI ALFRED ,  WOSTL WOLFGANG

IPC: C07D253/06 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/513 ,  A61K31/53 ,  A61P1/08 ,  A61P7/12 ,  A61P9/00 ,  A61P9/02 ,  A61P9/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/34 ,  A61P25/36 ,  A61P27/02 ,  A61P43/00 ,  C07D239/46 ,  C07D239/47 ,  C07D239/48 ,  C07D239/50 ,  C07D241/26 ,  C07D253/075 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14

Abstract: The present invention relates to pyrimidine, triazine and pyrazine derivativ es of the general formula (I), wherein R1, R2, R3, R4, X, Y and Z have the significances given in the specification ,as well as their pharmaceutically acceptable salts. The invention further relates to medicaments containing these compounds, their preparation and to their use for the control or prevention of acute and/or chronic neurological disorders.

公开(公告)号：HU0003112A2

公开(公告)日：2002-11-28

申请号：HU0003112

申请日：2000-08-04

Applicant: HOFFMANN LA ROCHE

Inventor： ADAM GEO ,  BINGGELI ALFRED ,  MUTEL VINCENT ,  MAERKI HANS-PETER ,  WILHELM MAURICE ,  DR WOSTL WOLFGANG

IPC: C07D223/16 ,  A61K31/55 ,  A61P1/08 ,  A61P3/08 ,  A61P9/04 ,  A61P9/10 ,  A61P13/10 ,  A61P21/02 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/34 ,  A61P27/02 ,  A61P43/00 ,  C07D223/04 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D521/00 ,  C07F7/18

Abstract: The present invention is concerned with 1,2,4,5-tetrahydro-benzo[d]azepin derivatives as well as with their pharmaceutically acceptable salts in their racemic and optically active form, which compounds are antagonists at metabotropic glutamate receptors and therefore useful for the treatment of diseases related to these receptors.

公开(公告)号：CO5180625A1

公开(公告)日：2002-07-30

申请号：CO00058410

申请日：2000-08-03

Applicant: HOFFMANN LA ROCHE

Inventor： GEO ADAM ,  BINGGELI ALFRED ,  MARKI HANS-PETER ,  MUTEL VINCENT ,  WILHELM MAURICE ,  WOSTL WOLFGANG

IPC: C07D223/16 ,  A61K31/395 ,  A61K31/55 ,  A61P1/08 ,  A61P3/08 ,  A61P9/04 ,  A61P9/10 ,  A61P13/10 ,  A61P21/02 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/34 ,  A61P27/02 ,  A61P43/00 ,  C07D223/04 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D521/00 ,  C07F7/18

Abstract: La presente invención se refiere a derivados de 1,2,4,5-tetrahidro-benzo[d]azepin de la fórmula general En dondeR1 significa hidrógeno, alquilo inferior, oxígeno, halógeno, ó -OR, -O(C3-C6)cicloalquilo, -O(CHR)n-(C3-C6)cicloalquilo, -O(CHR)nCN, -O(CHR)nCF3, -O(CHR)(CHR)nNR2, -O(CHR) -(CHR)nOR, -O(CHR)n-alquenilo inferior, -OCF3, -OCF2-R, OCF2-alquenilo inferior, -OCHRF, -OCHF-alquenilo inferior, -OCF2CRF2, -OCF2Br, -O(CHR)nCF2Br -O(CHR)n-fenilo, en donde el grupo fenilo opcionalmente se puede substituir independientemente uno del otro por entre uno y tres grupos alquilo inferior, alcoxi inferior, halógeno, nitro o ciano, -O(CHR)(CHR)n-morfolino, -O(CHR)(CHR)n-pirrolidino, -O(CHR)(CHR)n-piperidino, -O(CHR)(CHR)n-imidazol, -O(CHR)(CHR)n-triazol, -O(CHR)n-piridino,-O(CHR)(CHR)n-Osi-alquilo inferior,-O(CHR)(CHR)nOS(O)2-alquilo inferior, -O(CH2)nCH=CF2, -O(CHR)n-2,2-dimetil-[1,3]dioxo-Iano, -O(CHR)n-CHOR-CH2OR, -O(CHR)n-CHOR-(CHR)n-CH2 OR o -SR o S(CHR)nCOOR, ó -NR2, -N(R)(CHR) (CHR)nOR, -N(R)(CHR)nCF3, -N(R)(CHR)(CHR)n-morfolino, -N(R)(CHR)(CHR)n-imidazol, -N(R)(CHR)(CHR)n-pirrolidino, -N(R)(CHR)(CHR)n-pirrolidin-2-ona, -N(R)(CHR)(CHR)n-piperidino, -N(R)(CHR)(CHR)n-triazol, -N(R)(CHR)n-piridino, n es 1- 6; R significa hidrógeno, alquilo inferior o alquenilo inferior, independientemente uno de otro, en el caso de que haya más de un grupo R;R2 significa nitro o ciano;R3 significa hidrógeno, alquilo inferior, =O, =S, -SR, -S(O)2-alquilo inferior, -(C3-C6)cicloalquilo o piperazino, substituido opcionalmente por alquilo inferior, o -CONR2, -(CHR)nCONR2, -(CHR)nOR, -(CH2)n-CF3, -CF3, -(CHR)nOC(O)CF3, -(CHR)nCOOR, -(CHR)nSC6H5, en donde grupo fenilo opcionalmente puede estar substituido independientemente uno de otro por entre uno y tres grupos alquilo inferior, alcoxi inferior, halógeno, nitro o ciano, -(CHR)n-1,3-dioxo-1,3-dihidro-isoindol,-(CHR)n-tetrahidro-piran-2-iloxi o -(CHR)n-S-alquilo inferior, o -NR2, NRCO-alquilo inferior, -NRCHO,-N(R)(CHR)nCN, -N(R)(CHR)nCF3, -N(R)(CHR)(CHR)n-OR, ...