公开(公告)号：JPH1067742A

公开(公告)日：1998-03-10

申请号：JP19217397

申请日：1997-07-17

Applicant: HOFFMANN LA ROCHE

Inventor： ALANINE ALEXANDER ,  BUTELMAN BERRNT ,  HEIRGHT NIDART MARI-PAUL ,  PINARR EMMANUEL ,  WILLER LENER

IPC: C07D211/14 ,  A61K31/445 ,  A61K31/452 ,  A61K31/4523 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D20060101 ,  C07D211/18 ,  C07D211/20 ,  C07D211/48 ,  C07D401/06 ,  C07D401/08 ,  C07D401/12 ,  C07D521/00

Abstract: PROBLEM TO BE SOLVED: To obtain a novel compound which is useful in an N-methyl-D-aspartic acid receptor subtype-specific blocker in diseases, for example, an acute neurodegeneration caused by cerebral apoplexy, Alzheimer's disease, Parkinson's disease, Huntington's disease and the like. SOLUTION: This compound is represented by formula I (X is -O-, -NH-, -CH2 -; R -R are H, a halogen, OH, a lower alkylsulfonylamino; R -R are each H, a lower alkyl, a halogen; n is 0, 1), typically 1[2-(4-hydroxy-phenoxy) ethyl]-4-(4-methyl-benzyl)-piprtidine-4-ol. The compound of formula I is prepared by reaction of a compound of formula II with a compound of formula III.

公开(公告)号：NZ328330A

公开(公告)日：1998-05-27

申请号：NZ32833097

申请日：1997-07-14

Applicant: HOFFMANN LA ROCHE

Inventor： ALANINE ALEXANDER ,  BUTELMAN BERRNT ,  HEIRGHT NIDART MARI-PAUL ,  PINARR EMMANUEL ,  WILLER LENER

IPC: A61K31/445 ,  A61K31/452 ,  C07D211/14 ,  A61K31/4523 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D20060101 ,  C07D211/18 ,  C07D211/20 ,  C07D211/48 ,  C07D401/06 ,  C07D401/08 ,  C07D401/12 ,  C07D521/00 ,  C07D211/52 ,  A61K31/435

Abstract: The present invention relates to compounds of the general formula wherein X is -O-, -NH-, -CH2-, -CH=, -CO2-, -CONH-, -CON(lower alkyl)-, -S- and -SO2-; R - R are, independently from each other hydrogen, halogen, hydroxy, amino, nitro, lower-alkyl-sulfonylamido, 1- or 2-imidazolyl, 1-(1,2,4-triazolyl) or acetamido; R , R are, independently from each other hydrogen, lower-alkyl, hydroxy, lower alkoxy or oxo; R -R are, independently from each other hydrogen, lower-alkyl, halogen, trifluoromethyl or lower-alkoxy; n is 0 or 1; and to pharmaceutically acceptable acid addition salts thereof. Compounds of the present invention are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers.

公开(公告)号：HK1009124A1

公开(公告)日：1999-05-28

申请号：HK98109919

申请日：1998-08-13

Applicant: HOFFMANN LA ROCHE

Inventor： ALANINE ALEXANDER ,  BUTELMAN BERRNT ,  HEIRGHT NIDART MARI-PAUL ,  PINARR EMMANUEL ,  WILLER LENER

IPC: A61K31/445 ,  A61K31/452 ,  C07D211/14 ,  A61K31/4523 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D20060101 ,  C07D211/18 ,  C07D211/20 ,  C07D211/48 ,  C07D401/06 ,  C07D401/08 ,  C07D401/12 ,  C07D521/00 ,  C07D ,  A61K

Abstract: The present invention relates to compounds of the general formula wherein X is -O-, -NH-, -CH2-, -CH=, -CO2-, -CONH-, -CON(lower alkyl)-, -S- and -SO2-; R - R are, independently from each other hydrogen, halogen, hydroxy, amino, nitro, lower-alkyl-sulfonylamido, 1- or 2-imidazolyl, 1-(1,2,4-triazolyl) or acetamido; R , R are, independently from each other hydrogen, lower-alkyl, hydroxy, lower alkoxy or oxo; R -R are, independently from each other hydrogen, lower-alkyl, halogen, trifluoromethyl or lower-alkoxy; n is 0 or 1; and to pharmaceutically acceptable acid addition salts thereof. Compounds of the present invention are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers.

公开(公告)号：SG60085A1

公开(公告)日：1999-02-22

申请号：SG1997002449

申请日：1997-07-11

Applicant: HOFFMANN LA ROCHE

Inventor： ALANINE ALEXANDER ,  BUTELMAN BERRNT ,  HEIRGHT NIDART MARI-PAUL ,  PINARR EMMANUEL ,  WILLER LENER

IPC: A61K31/445 ,  A61K31/452 ,  A61K31/4523 ,  C07D211/14 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D20060101 ,  C07D211/18 ,  C07D211/20 ,  C07D211/48 ,  C07D401/06 ,  C07D401/08 ,  C07D401/12 ,  C07D521/00

Abstract: The present invention relates to compounds of the general formula wherein X is -O-, -NH-, -CH2-, -CH=, -CO2-, -CONH-, -CON(lower alkyl)-, -S- and -SO2-; R - R are, independently from each other hydrogen, halogen, hydroxy, amino, nitro, lower-alkyl-sulfonylamido, 1- or 2-imidazolyl, 1-(1,2,4-triazolyl) or acetamido; R , R are, independently from each other hydrogen, lower-alkyl, hydroxy, lower alkoxy or oxo; R -R are, independently from each other hydrogen, lower-alkyl, halogen, trifluoromethyl or lower-alkoxy; n is 0 or 1; and to pharmaceutically acceptable acid addition salts thereof. Compounds of the present invention are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers.

公开(公告)号：HU9701194A2

公开(公告)日：1999-05-28

申请号：HU9701194

申请日：1997-07-14

Applicant: HOFFMANN LA ROCHE

Inventor： ALANINE ALEXANDER ,  BUTELMAN BERRNT ,  HEIRGHT NIDART MARI-PAUL ,  PINARR EMMANUEL ,  WILLER LENER

IPC: A61K31/445 ,  A61K31/452 ,  A61K31/4523 ,  C07D211/14 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D20060101 ,  C07D211/18 ,  C07D211/20 ,  C07D211/48 ,  C07D401/06 ,  C07D401/08 ,  C07D401/12 ,  C07D521/00

Abstract: The present invention relates to compounds of the general formula wherein X is -O-, -NH-, -CH2-, -CH=, -CO2-, -CONH-, -CON(lower alkyl)-, -S- and -SO2-; R - R are, independently from each other hydrogen, halogen, hydroxy, amino, nitro, lower-alkyl-sulfonylamido, 1- or 2-imidazolyl, 1-(1,2,4-triazolyl) or acetamido; R , R are, independently from each other hydrogen, lower-alkyl, hydroxy, lower alkoxy or oxo; R -R are, independently from each other hydrogen, lower-alkyl, halogen, trifluoromethyl or lower-alkoxy; n is 0 or 1; and to pharmaceutically acceptable acid addition salts thereof. Compounds of the present invention are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers.

公开(公告)号：BR9704031A

公开(公告)日：1998-12-29

申请号：BR9704031

申请日：1997-07-21

Applicant: HOFFMANN LA ROCHE

Inventor： ALANINE ALEXANDER ,  BUTELMAN BERRNT ,  HEIRGHT NIDART MARI-PAUL ,  PINARR EMMANUEL ,  WILLER LENER

IPC: C07D211/14 ,  A61K31/445 ,  A61K31/452 ,  A61K31/4523 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D20060101 ,  C07D211/18 ,  C07D211/20 ,  C07D211/48 ,  C07D401/06 ,  C07D401/08 ,  C07D401/12 ,  C07D521/00 ,  C07D211/22

Abstract: The present invention relates to compounds of the general formula wherein X is -O-, -NH-, -CH2-, -CH=, -CO2-, -CONH-, -CON(lower alkyl)-, -S- and -SO2-; R - R are, independently from each other hydrogen, halogen, hydroxy, amino, nitro, lower-alkyl-sulfonylamido, 1- or 2-imidazolyl, 1-(1,2,4-triazolyl) or acetamido; R , R are, independently from each other hydrogen, lower-alkyl, hydroxy, lower alkoxy or oxo; R -R are, independently from each other hydrogen, lower-alkyl, halogen, trifluoromethyl or lower-alkoxy; n is 0 or 1; and to pharmaceutically acceptable acid addition salts thereof. Compounds of the present invention are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers.

公开(公告)号：MX9705387A

公开(公告)日：1998-01-31

申请号：MX9705387

申请日：1997-07-16

Applicant: HOFFMANN LA ROCHE

Inventor： ALANINE ALEXANDER ,  BUTELMAN BERRNT ,  HEIRGHT NIDART MARI-PAUL ,  PINARR EMMANUEL ,  WILLER LENER

IPC: C07D211/14 ,  A61K31/445 ,  A61K31/452 ,  A61K31/4523 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D20060101 ,  C07D211/18 ,  C07D211/20 ,  C07D211/48 ,  C07D401/06 ,  C07D401/08 ,  C07D401/12 ,  C07D521/00

Abstract: La presente invencion se refiere a compuestos de formula general (I), en donde, X es -O-, -NH-, -CH2-, -CH=, -CO2, -CONH-N, -CON(alquil inferior)-, -S-, -SO2-; R1-R4 son independientemente entre sí, hidrogeno, halogeno, hidroxilo, amino, nitro, alquilo inferior sulfonilamido, 1- o 2-imidazolilo, 1-(1,2,4-triazolil) o acetamido; R5,R6 son, independientemente entre sí, hidrogeno, alquilo inferior, hidroxilo, alcoxilo inferior u oxo, R7-R10 son independientemente entre sí, hidrogeno, alquilo inferior, halogeno, trifluorometilo o alcoxilo inferior; n es 0 o 1; y a las sales de adicion ácida farmacéuticamente aceptables de los mismos. Los compuestos de la presente invencion son bloqueadores selectivos de los subtipos de los receptores de NMDA (N-metil-D-aspartato).

公开(公告)号：AU719352B2

公开(公告)日：2000-05-04

申请号：AU2875697

申请日：1997-07-18

Applicant: HOFFMANN LA ROCHE

Inventor： ALANINE ALEXANDER ,  BUTELMAN BERRNT ,  HEIRGHT NIDART MARI-PAUL ,  PINARR EMMANUEL ,  WILLER LENER

IPC: C07D211/14 ,  A61K31/445 ,  A61K31/452 ,  A61K31/4523 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D20060101 ,  C07D211/18 ,  C07D211/20 ,  C07D211/48 ,  C07D401/06 ,  C07D401/08 ,  C07D401/12 ,  C07D521/00

Abstract: The present invention relates to compounds of the general formula wherein X is -O-, -NH-, -CH2-, -CH=, -CO2-, -CONH-, -CON(lower alkyl)-, -S- and -SO2-; R - R are, independently from each other hydrogen, halogen, hydroxy, amino, nitro, lower-alkyl-sulfonylamido, 1- or 2-imidazolyl, 1-(1,2,4-triazolyl) or acetamido; R , R are, independently from each other hydrogen, lower-alkyl, hydroxy, lower alkoxy or oxo; R -R are, independently from each other hydrogen, lower-alkyl, halogen, trifluoromethyl or lower-alkoxy; n is 0 or 1; and to pharmaceutically acceptable acid addition salts thereof. Compounds of the present invention are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers.

公开(公告)号：ZA976224B

公开(公告)日：1998-01-19

申请号：ZA976224

申请日：1997-07-14

Applicant: HOFFMANN LA ROCHE

Inventor： ALANINE ALEXANDER ,  BUTELMAN BERRNT ,  PINARR EMMANUEL ,  WILLER LENER ,  HEIRGHT NIDART MARI-PAUL

IPC: A61K31/445 ,  A61K31/452 ,  A61K31/4523 ,  C07D211/14 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D20060101 ,  C07D211/18 ,  C07D211/20 ,  C07D211/48 ,  C07D401/06 ,  C07D401/08 ,  C07D401/12 ,  C07D521/00 ,  C07D ,  A16K

Abstract: The present invention relates to compounds of the general formula wherein X is -O-, -NH-, -CH2-, -CH=, -CO2-, -CONH-, -CON(lower alkyl)-, -S- and -SO2-; R - R are, independently from each other hydrogen, halogen, hydroxy, amino, nitro, lower-alkyl-sulfonylamido, 1- or 2-imidazolyl, 1-(1,2,4-triazolyl) or acetamido; R , R are, independently from each other hydrogen, lower-alkyl, hydroxy, lower alkoxy or oxo; R -R are, independently from each other hydrogen, lower-alkyl, halogen, trifluoromethyl or lower-alkoxy; n is 0 or 1; and to pharmaceutically acceptable acid addition salts thereof. Compounds of the present invention are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers.

公开(公告)号：ZA9706224B

公开(公告)日：1998-01-19

申请号：ZA9706224

申请日：1997-07-14

Applicant: HOFFMANN LA ROCHE

Inventor： ALANINE ALEXANDER ,  BUTELMAN BERRNT ,  HEIRGHT NIDART MARI-PAUL ,  PINARR EMMANUEL ,  WILLER LENER

IPC: C07D211/14 ,  A61K31/445 ,  A61K31/452 ,  A61K31/4523 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D20060101 ,  C07D211/18 ,  C07D211/20 ,  C07D211/48 ,  C07D401/06 ,  C07D401/08 ,  C07D401/12 ,  C07D521/00 ,  C07D ,  A16K

CPC classification number: C07D231/12 ,  C07D211/48 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/12