公开(公告)号：JP2001114777A

公开(公告)日：2001-04-24

申请号：JP2000304354

申请日：2000-10-04

Applicant: HOFFMANN LA ROCHE

Inventor： ALANINE ALEXANDER ,  BURNER SERGE ,  BUETTELMANN BERND ,  NEIDHART MARIE-PAULE HEITZ ,  JAESCHKE GEORG ,  PINARD EMMANUEL ,  WYLER RENE

IPC: C07D215/42 ,  A61K31/4709 ,  A61K31/4725 ,  A61P21/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P43/00 ,  C07D401/04 ,  C07D401/14

Abstract: PROBLEM TO BE SOLVED: To obtain a new N-methyl-D-aspartic acid (NMDA) receptor subtype specific blocker. SOLUTION: This compound is represented by the formula (I) [wherein R1 is hydrogen, a lower alkyl, a lower alkoxy, hydroxyl, amino, nitro, cyano, a lower alkylamino, a di-lower alkylamino or a halogen; R2 is hydrogen, a lower alkyl, amino, pyrrolidin-3-ol, pyrrolidin-2-ylmethanol or NHCH2CHROH; R3 is hydrogen or a halogen; R is hydrogen, a lower alkyl or CH2OH; and n is 1 or 2] and its pharmaceutically acceptable acid addition salt.

公开(公告)号：JP2001097952A

公开(公告)日：2001-04-10

申请号：JP2000298078

申请日：2000-09-29

Applicant: HOFFMANN LA ROCHE

Inventor： ALANINE ALEXANDER ,  BURNER SERGE ,  BUETTELMANN BERND ,  NEIDHART MARIE-PAULE HEITZ ,  JAESCHKE GEORG ,  PINARD EMMANUEL ,  WYLER RENE

IPC: C07D215/22 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61P9/10 ,  A61P21/00 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  C07D215/233 ,  C07D215/42 ,  C07D215/46 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12

Abstract: PROBLEM TO BE SOLVED: To provide a new quinolin-4-yl derivative. SOLUTION: A compound of formula (I) [R1 is H, a lower alkyl, a lower alkoxy, hydroxy, amino, nitro or the like; R2 is phenyl (if necessary, substituted by a lower alkyl, a lower alkoxy, a halogen, trifluoromethyl, amino, a lower alkyl-amino or a di-lower alkyl-amino), 2, 3-dihydro-benzofuran-5-yl, chroman-6- yl, naphthalen-2-yl, indan-5-yl or the like; R3 and R4 are each mutually independently H or a lower alkyl; R5 is H, a lower alkyl, CH2OH or the like; X is NR8 or O; or X and R5 together form >N-(CH2)2; X and R3 together form >N(CH2)3; R8 is H or a lower alkyl].

公开(公告)号：SG164268A1

公开(公告)日：2010-09-29

申请号：SG2000055517

申请日：2000-09-27

Applicant: HOFFMANN LA ROCHE

Inventor： ALANINE ALEXANDER ,  BURNER SERGE ,  BUETTELMANN BERND ,  NEIDHART MARIE-PAULE HEITZ ,  JAESCHKE GEORG ,  PINARD EMMANUEL ,  WYLER RENE

IPC: C07D215/22 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61P9/10 ,  A61P21/00 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  C07D215/233 ,  C07D215/42 ,  C07D215/46 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12

Abstract: The invention relates to compounds of formula wherein R1 is hydrogen, lower alkyl, lower alkoxy, hydroxy, amino, nitro, cyano, lower alkyl-amino, di-lower alkyl-amino or halogen; R2 is phenyl, optionally substituted by lower alkyl, lower alkoxy, halogen, trifluoromethyl, amino, lower alkyl-amino or di-lower alkyl-amino, 2,3- dihydro-benzofuran-5-yl, chroman-6-yl, naphthalen-2-yl, indan-5-yl, lower alkenyl-phenyl, 5,6,7,8-tetrahydro-naphthalenyl, 2,3-dihydro-isoindol-2-yl, 1,2,3,4-tetrahydro-naphthalenyl, benzofuran-2-yl, benzo[b]thiophen-2-yl, lower alkyl-phenyl, 3,4-dihydro-1H-isoquinolin-2-yl or thiophen-3-yl; R3 and R4 are independently from each other hydrogen or lower alkyl; R5 is hydrogen, lower alkyl, -CH2OH or ûCH2NR6R7; R6 and R7 are independently from each other hydrogen, lower alkyl, -(CH2)n-phenyl, cycloalkyl, -(CH2)m-morpholinyl or form together with the N- atom a saturated ring with 4-6C-atoms; n is 0-3; m is 2 or 3; X is ûNR8- or -0-; or X and R5 are together >N(CH2)2-; or X and R3 are together >N(CH2)3-; and R8 is hydrogen or lower alkyl; and to pharmaceutically acceptable acid addition salts thereof, with the exception of the following compounds (6-chloro-2-phenyl-4-quinolinyl)-(+)-2-aminobutanol; (6-methyl-2-phenyl-4-quinolinyl)-(+)-2-aminobutanol; (6-methoxy-2-phenyl-4-quinolinyl)-(+)-2-aminobutanol; and (8-methoxy-2-phenyl-4-quinolinyl)-(+)-2-aminobutanol, which maybe used for the treatment of diseases, which relate to the NMDA receptor specific blockers.

公开(公告)号：CA2322309C

公开(公告)日：2008-05-20

申请号：CA2322309

申请日：2000-10-04

Applicant: HOFFMANN LA ROCHE

Inventor： JAESCHKE GEORG ,  PINARD EMMANUEL ,  BUTTELMANN BERND ,  ALANINE ALEXANDER ,  WYLER RENE ,  BURNER SERGE ,  HEITZ NEIDHART MARIE-PAULE

IPC: C07D215/42 ,  C07D401/04 ,  A61K31/4709 ,  A61K31/4725 ,  A61P21/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P43/00 ,  C07D401/14

Abstract: The present invention relates to compounds of the general formula wherein R1 is hydrogen, lower alkyl, lower alkoxy, hydroxy, amino, nitro, cyano, lower alkyl-amino, di-lower alkyl-amino or halogen; R2 is hydrogen, lower alkyl, amino, pyrrolidin-3-ol, pyrrolidin-2-yl- methanol or -NHCH2CHROH; R3 is hydrogen or halogen; R is hydrogen, lower alkyl or -CH2OH; n is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. Compounds of the present invention are NMDA(N- methyl-D -aspartate) -recepto r subtype selective blockers, which have a key function in modulating neuronal activity and plasticity in mediating processes underlying development of CNS as well as learning and memory formation.

公开(公告)号：DE60025348T2

公开(公告)日：2006-08-24

申请号：DE60025348

申请日：2000-05-31

Applicant: HOFFMANN LA ROCHE

Inventor： ALANINE ALEXANDER ,  BURNER SERGE ,  BUETTELMANN BERND ,  HEITZ NEIDHART MARIE-PAULE ,  JAESCHKE GEORG ,  PINARD EMMANUEL ,  WYLER RENOMEGA

IPC: C07D211/46 ,  A61K31/445 ,  A61P21/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  C07D211/14 ,  C07D211/30 ,  C07D211/42 ,  C07D211/44

Abstract: The invention relates to compounds of the general formulawhereinR1 signifies hydrogen or hydroxy; R2 signifies hydrogen or methyl; and X signifies -O- or -CH2- and their pharmaceutically acceptable acid addition salts.It has been shown that these compounds have a good affitity to the NMDA receptor and they are therefore useful in the treatment of diseases, wherein the therapeutic indications include acute forms of neurodegeneration caused, e.g., by stroke or brain trauma; chronic forms of neurodegeneration such as Alzheimer's disease, Parkinson's disease, Huntington's disease or ALS (amyotrophic lateral sclerosis); neurodegeneration associated with bacterial or viral infections, and, diseases such as schizophrenia, anxiety, depression and chronic/acute pain.

公开(公告)号：ES2254183T3

公开(公告)日：2006-06-16

申请号：ES00936835

申请日：2000-05-31

Applicant: HOFFMANN LA ROCHE

Inventor： ALANINE ALEXANDER ,  BURNER SERGE ,  BUETTELMANN BERND ,  HEITZ NEIDHART MARIE-PAULE ,  JAESCHKE GEORG ,  PINARD EMMANUEL

IPC: A61K31/445 ,  A61P21/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  C07D211/14 ,  C07D211/30 ,  C07D211/42 ,  C07D211/44 ,  C07D211/46

Abstract: Compuestos de fórmula general: en donde, R1 significa hidrógeno o hidroxilo; R2 significa hidrógeno o metilo; y X significa ¿O- ó ¿CH2-; y sus sales de adición ácida farmacéuticamente aceptables.

公开(公告)号：JO2292B

公开(公告)日：2005-09-12

申请号：JO20029

申请日：2002-01-29

Applicant: HOFFMANN LA ROCHE

Inventor： BERND BUTTELMANN ,  MARIE-PAULE HEITZ ,  GEORG JAESCHKE ,  ALANINE ALEXANDER ,  BURNER SERGE ,  PINARD EMMANUEL

IPC: C07D233/64 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61P25/00 ,  A61P25/04 ,  A61P25/14 ,  A61P25/16 ,  A61P25/24 ,  A61P25/28 ,  A61P31/04 ,  A61P31/12 ,  A61P43/00 ,  C07D233/54 ,  C07D233/61 ,  C07D233/84 ,  C07D233/88 ,  C07D249/08 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D521/00

CPC classification number: C07D233/64 ,  C07D231/12 ,  C07D233/56 ,  C07D233/84 ,  C07D249/08

Abstract: The invention related to compounds of the general formula (I), wherein the substituents are defined in claim 1. These compounds have a good affinity to the NMDA (N-methyl-D-aspartate)-receptor subtype selective blockers, which have a key function in modulating neuronal activity and plasticity which makes them key players in mediating processes underlying development of CNS as well as learning and memory formation. These compounds are therefore suitable in the control or treatment of diseases, related to this receptor

公开(公告)号：JO2289B

公开(公告)日：2005-09-12

申请号：JO2001136

申请日：2001-08-19

Applicant: HOFFMANN LA ROCHE

Inventor： GERORG JAESCHKE ,  JOERG HUWYLER ,  HOLGER FISCHER ,  ALANINE ALEXANDER ,  BURNER SERGE ,  BUETTELMANN BERND ,  JAESCHKE GEORG

IPC: A61K31/445 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/675 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D211/42 ,  C07F9/09 ,  C07F9/59

CPC classification number: C07D211/42 ,  C07F9/591

Abstract: The invention relates to compounds of the general formula (I) wherein R is a) -C(O)(CH2)nC(O)OH, b) wherein R is -N(R2)(R3) and R2/R3 are independently from each other hydrogen or lower alkyl, or is a cyclic tertiary amine, optionally substituted by lower alkyl, c) -P(O)(OH)2, or is d) -C(O)(CH)2)nNHC(O)(CH2)nN(R2)(R3); and n is 1, 2, 3 or 4; and to pharmaceutically acceptable acid addition salts thereof. These compounds may be used as prodrugs for the parentcompound of formula (II) which are useful in the treatment of NMDA receptor-related diseases.

公开(公告)号：AU770787B2

公开(公告)日：2004-03-04

申请号：AU5218100

申请日：2000-05-31

Applicant: HOFFMANN LA ROCHE

Inventor： ALANINE ALEXANDER ,  BURNER SERGE ,  BUETTELMANN BERND ,  NEIDHART MARIE-PAULE HEITZ ,  JAESCHKE GEORG ,  PINARD EMMANUEL ,  WYLER RENE

IPC: A61K31/445 ,  A61P21/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  C07D211/14 ,  C07D211/30 ,  C07D211/42 ,  C07D211/44 ,  C07D211/46

Abstract: The invention relates to compounds of the general formulawhereinR1 signifies hydrogen or hydroxy; R2 signifies hydrogen or methyl; and X signifies -O- or -CH2- and their pharmaceutically acceptable acid addition salts.It has been shown that these compounds have a good affitity to the NMDA receptor and they are therefore useful in the treatment of diseases, wherein the therapeutic indications include acute forms of neurodegeneration caused, e.g., by stroke or brain trauma; chronic forms of neurodegeneration such as Alzheimer's disease, Parkinson's disease, Huntington's disease or ALS (amyotrophic lateral sclerosis); neurodegeneration associated with bacterial or viral infections, and, diseases such as schizophrenia, anxiety, depression and chronic/acute pain.

公开(公告)号：HRP20010885A2

公开(公告)日：2004-02-29

申请号：HRP20010885

申请日：2001-11-28

Applicant: HOFFMANN LA ROCHE

Inventor： ALANINE ALEXANDER ,  BURNER SERGE ,  BUETTELMANN BERND ,  NEIDHART MARIE-PAULE HEITZ ,  JAESCHKE GEORG ,  PINARD EMMANUEL ,  WYLER RENE

IPC: A61K31/445 ,  A61P21/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  C07D211/14 ,  C07D211/30 ,  C07D211/42 ,  C07D211/44 ,  C07D211/46

Abstract: The invention relates to compounds of the general formulawhereinR1 signifies hydrogen or hydroxy; R2 signifies hydrogen or methyl; and X signifies -O- or -CH2- and their pharmaceutically acceptable acid addition salts.It has been shown that these compounds have a good affitity to the NMDA receptor and they are therefore useful in the treatment of diseases, wherein the therapeutic indications include acute forms of neurodegeneration caused, e.g., by stroke or brain trauma; chronic forms of neurodegeneration such as Alzheimer's disease, Parkinson's disease, Huntington's disease or ALS (amyotrophic lateral sclerosis); neurodegeneration associated with bacterial or viral infections, and, diseases such as schizophrenia, anxiety, depression and chronic/acute pain.