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公开(公告)号：ID23456A
公开(公告)日：2000-04-27
申请号：ID990095
申请日：1999-02-09
Applicant: HOFFMANN LA ROCHE
Inventor： ALANINE ALEXANDER , BUTTELMANN BERT , MARIE-PAULE HEITZ N , PINARD EMANUEL , WYLER RENE
IPC: C07D211/22 , A61K31/00 , A61K31/40 , A61K31/4025 , A61K31/42 , A61K31/424 , A61K31/435 , A61K31/437 , A61K31/443 , A61K31/445 , A61K31/4525 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5383 , A61P9/10 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D20060101 , C07D207/06 , C07D207/08 , C07D207/09 , C07D211/32 , C07D263/52 , C07D265/34 , C07D265/36 , C07D405/06 , C07D498/04 , A61K31/395
Abstract: The present invention relates to the use of pyrrolidine and piperidine derivatives of the general formulae wherein R and R are, independently from each other, hydrogen, lower alkoxy, hydroxy, halogen, -CONH2 or -C(O)O-lower alkyl; or taken together are -O-CH2-O-; R and R are, independently from each other, hydrogen, lower alkoxy, benzyloxy, halogen, hydroxy, -CONH2 or -SCH3; or taken together are -O-CH2-O-; R is hydrogen or lower alkyl; X and Y are, independently from each other -CH(OH)-, -(CH2)n-, -C(O)- or -CH(lower alkoxy)-; and m, n and p are 1 or 2; and to their pharmaceutically acceptable addition salts for the treatment of diseases caused by overactivation of NMDA receptor subtypes.
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公开(公告)号：SG71062A1
公开(公告)日：2000-03-21
申请号：SG1997004062
申请日：1997-11-14
Applicant: HOFFMANN LA ROCHE
Inventor： ALANINE ALEXANDER , BUTTELMANN BERND , NEIDHART MARIE-PAULE HEITZ , PINARD EMMANUEL , WYLER RENE
IPC: C07D211/44 , A61K31/38 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/451 , A61K31/453 , A61K31/454 , A61K31/47 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/28 , A61P43/00 , C07D211/14 , C07D211/48 , C07D215/12 , C07D215/18 , C07D307/78 , C07D335/06 , C07D401/06 , C07D405/06 , C07D417/06 , A61K31/34 , A61K31/45
Abstract: The present invention relates to 4-hydroxy-piperidine derivatives of the general formulawhereinX denotes -O-, -NH-, -CH2-, -CH=, -CHOH-, -CO-, -S-, -SO- or -SO2-;R1-R4 are, independently from each other, hydrogen, hydroxy, lower-alkyl-sulfonylamino, 1- or 2-imidazolyl or acetamido;R5-R8 are, independently from each other, hydrogen, hydroxy, lower-alkyl, halogen, lower-alkoxy, trifluoromethyl or trifluoromethyloxy;a and b may be a double bond, provided that when "a" is a double bond, "b" cannot be a double bond;n is 0-2;m is 1-3;p is 0 or 1and to pharmaceutically acceptable addition salts thereof.Compounds of the present invention are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers, which can be used in mediating processes underlying development of CNS including learning and memory formation and function.
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公开(公告)号：CZ9902903A3
公开(公告)日：2000-03-15
申请号：CZ290399
申请日：1999-08-16
Applicant: HOFFMANN LA ROCHE
Inventor： ALANINE ALEXANDER , BUETTELMANN BERND , HEITZ NEIDHART MARIE-PAULE , PINARD EMMANUEL , WYLER REN
IPC: A61K31/335 , A61K31/435 , A61K31/535 , A61P25/00
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公开(公告)号：HRP990042A2
公开(公告)日：2000-02-29
申请号：HRP990042
申请日：1999-02-09
Applicant: HOFFMANN LA ROCHE
Inventor： ALANINE ALEXANDER , BUETTELMANN BERND , NEIDHART MARIE-PAULE HEITZ , PINARD EMMANUEL , WYLER RENE
IPC: C07D211/22 , A61K31/00 , A61K31/40 , A61K31/4025 , A61K31/42 , A61K31/424 , A61K31/435 , A61K31/437 , A61K31/443 , A61K31/445 , A61K31/4525 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5383 , A61P9/10 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D20060101 , C07D207/06 , C07D207/08 , C07D207/09 , C07D211/32 , C07D263/52 , C07D265/34 , C07D265/36 , C07D405/06 , C07D498/04
Abstract: The present invention relates to the use of pyrrolidine and piperidine derivatives of the general formulae wherein R and R are, independently from each other, hydrogen, lower alkoxy, hydroxy, halogen, -CONH2 or -C(O)O-lower alkyl; or taken together are -O-CH2-O-; R and R are, independently from each other, hydrogen, lower alkoxy, benzyloxy, halogen, hydroxy, -CONH2 or -SCH3; or taken together are -O-CH2-O-; R is hydrogen or lower alkyl; X and Y are, independently from each other -CH(OH)-, -(CH2)n-, -C(O)- or -CH(lower alkoxy)-; and m, n and p are 1 or 2; and to their pharmaceutically acceptable addition salts for the treatment of diseases caused by overactivation of NMDA receptor subtypes.
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公开(公告)号：HU9902737D0
公开(公告)日：1999-10-28
申请号：HU9902737
申请日：1999-08-16
Applicant: HOFFMANN LA ROCHE
Inventor： ALANINE ALEXANDER , BUETTELMANN BERND , HEITZ NEIDHART MARIE-PAULE , PINARD EMMANUEL , WYLER RENE
IPC: C07D319/06 , A61K31/135 , A61K31/137 , A61K31/138 , A61K31/18 , A61K31/357 , A61K31/4468 , A61K31/451 , A61K31/535 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/28 , A61P43/00 , C07C215/46 , C07D211/58
Abstract: The present invention provides a method of treatment of a disease associated with neurodegeneration by administering a therapeutically effective amount of a compound of the general formulawhereinAr1 is phenyl, naphthyl or tetrahydronaphthyl, optionally substituted by hydroxy, lower alkoxy, nitro, amino or methanesulfonamide;Ar2 is phenyl, naphthyl or tetrahydronaphthyl, optionally substituted by lower alkyl or halogen;X is C, CH, C(OH) or N;Y is -CH2-, CH or O;Z -CH2-, -CH(CH3)- or -C(CH3)2-;R1 is hydrogen, lower alkyl or acetyl;A is C=O or -(CHR2)n-, wherein R2 is hydrogen, lower alkyl or hydroxy-lower alkyl;B is -(CH2)n-, O, -CH(OH)(CH2)n-, -CH(CH2OH)(CH2)n-, -(CH2)n CH(OH)- or -CH(CH2OH)-;- - - may be a bond; andn is 0-4,or pharmaceutically acceptable acid addition salts thereof.
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Patent Agency Ranking
公开(公告)号：CZ41099A3
公开(公告)日：1999-09-15
申请号：CZ41099
申请日：1999-02-05
Applicant: HOFFMANN LA ROCHE
Inventor： ALANINE ALEXANDER , BUTTELMANN BERND , HEITZ NEIDHART MARIE-PAULE , PINARD EMMANUEL , WYLER RENE
IPC: C07D211/22 , A61K31/00 , A61K31/40 , A61K31/4025 , A61K31/42 , A61K31/424 , A61K31/435 , A61K31/437 , A61K31/443 , A61K31/445 , A61K31/4525 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5383 , A61P9/10 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D20060101 , C07D207/06 , C07D207/08 , C07D207/09 , C07D211/32 , C07D263/52 , C07D265/34 , C07D265/36 , C07D405/06 , C07D498/04
Abstract: The present invention relates to the use of pyrrolidine and piperidine derivatives of the general formulae wherein R and R are, independently from each other, hydrogen, lower alkoxy, hydroxy, halogen, -CONH2 or -C(O)O-lower alkyl; or taken together are -O-CH2-O-; R and R are, independently from each other, hydrogen, lower alkoxy, benzyloxy, halogen, hydroxy, -CONH2 or -SCH3; or taken together are -O-CH2-O-; R is hydrogen or lower alkyl; X and Y are, independently from each other -CH(OH)-, -(CH2)n-, -C(O)- or -CH(lower alkoxy)-; and m, n and p are 1 or 2; and to their pharmaceutically acceptable addition salts for the treatment of diseases caused by overactivation of NMDA receptor subtypes.
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公开(公告)号：HU9700273A1
公开(公告)日：1999-08-30
申请号：HU9700273
申请日：1997-01-29
Applicant: HOFFMANN LA ROCHE
Inventor： ALANINE ALEXANDER , BOURSON ANNE , BUETTELMANN BERND , FISCHER GUENTHER , MUTEL VINCENT , NEIDHART MARIE-PAULE HEITZ , PINARD EMMANUEL , ROEVER STEPHAN , TRUBE GERHARD , WYLER RENE
IPC: C07D217/16 , A61K31/47 , A61K31/472 , A61K31/473 , A61K31/4741 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07D217/18 , C07D217/20 , C07D217/24 , C07D221/00 , C07D221/06 , C07D221/12 , C07D491/04 , C07D491/056 , C07D221/16 , C07D217/04
Abstract: The present invention relates to the use of tetrahydroisoquinoline derivatives of the general formula wherein A is aryl R1 is hydrogen, hydroxy, lower alkyl, lower alkoxy, R-CO- or R-COO-, wherein R is lower alkyl; R2 is hydrogen, lower alkyl or cycloalkyl R3-R7 are independently hydrogen, lower alkyl, lower alkoxy, hydroxy or R3 and R4 taken together are -(CH2)n- or R6 and R7 taken together are -OCH2O- and n is 3 or 4, as well as pharmaceutically acceptable salts for the manufacture of medicaments for the control or treatment of diseases which represent therapeutic indications for NMDA receptor subtype specific blockers.
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公开(公告)号：AU1635499A
公开(公告)日：1999-08-26
申请号：AU1635499
申请日：1999-02-08
Applicant: HOFFMANN LA ROCHE
Inventor： ALANINE ALEXANDER , BUETTELMANN BERND , HEITZ NEIDHART MARIE-PAULE , PINARD EMMANUEL , WYLER RENE
IPC: C07D211/22 , A61K31/00 , A61K31/40 , A61K31/4025 , A61K31/42 , A61K31/424 , A61K31/435 , A61K31/437 , A61K31/443 , A61K31/445 , A61K31/4525 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5383 , A61P9/10 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D20060101 , C07D207/06 , C07D207/08 , C07D207/09 , C07D211/32 , C07D263/52 , C07D265/34 , C07D265/36 , C07D405/06 , C07D498/04 , C07D405/10 , C07D405/14 , C07D491/048 , C07D491/052
Abstract: The present invention relates to the use of pyrrolidine and piperidine derivatives of the general formulae wherein R and R are, independently from each other, hydrogen, lower alkoxy, hydroxy, halogen, -CONH2 or -C(O)O-lower alkyl; or taken together are -O-CH2-O-; R and R are, independently from each other, hydrogen, lower alkoxy, benzyloxy, halogen, hydroxy, -CONH2 or -SCH3; or taken together are -O-CH2-O-; R is hydrogen or lower alkyl; X and Y are, independently from each other -CH(OH)-, -(CH2)n-, -C(O)- or -CH(lower alkoxy)-; and m, n and p are 1 or 2; and to their pharmaceutically acceptable addition salts for the treatment of diseases caused by overactivation of NMDA receptor subtypes.
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公开(公告)号：ZA991038B
公开(公告)日：1999-08-10
申请号：ZA991038
申请日：1999-02-09
Applicant: HOFFMANN LA ROCHE
Inventor： ALANINE ALEXANDER , BUETTELMANN BERND , HEITZ NEIDHART MARIE-PAULE , PINARD EMMANUEL , WYLER RENE
IPC: C07D211/22 , A61K31/00 , A61K31/40 , A61K31/4025 , A61K31/42 , A61K31/424 , A61K31/435 , A61K31/437 , A61K31/443 , A61K31/445 , A61K31/4525 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5383 , A61P9/10 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D20060101 , C07D207/06 , C07D207/08 , C07D207/09 , C07D211/32 , C07D263/52 , C07D265/34 , C07D265/36 , C07D405/06 , C07D498/04 , C07D , A61K
Abstract: The present invention relates to the use of pyrrolidine and piperidine derivatives of the general formulae wherein R and R are, independently from each other, hydrogen, lower alkoxy, hydroxy, halogen, -CONH2 or -C(O)O-lower alkyl; or taken together are -O-CH2-O-; R and R are, independently from each other, hydrogen, lower alkoxy, benzyloxy, halogen, hydroxy, -CONH2 or -SCH3; or taken together are -O-CH2-O-; R is hydrogen or lower alkyl; X and Y are, independently from each other -CH(OH)-, -(CH2)n-, -C(O)- or -CH(lower alkoxy)-; and m, n and p are 1 or 2; and to their pharmaceutically acceptable addition salts for the treatment of diseases caused by overactivation of NMDA receptor subtypes.
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100.发明专利
公开(公告)号：HU9702315A2
公开(公告)日：1999-06-28
申请号：HU9702315
申请日：1997-12-01
Applicant: HOFFMANN LA ROCHE
Inventor： ALANINE ALEXANDER , BUETTELMANN BERND , HEITZ NEIDHART MARIE-PAULE , PINARD EMMANUEL , WYLER RENE
IPC: A61K31/34 , A61K31/35 , A61K31/445 , C07D211/48 , C07D401/06 , C07D405/06
Abstract: 4-Hydroxypiperidine derivatives of formula (I) and their addition salts are new. X = O, NH, CH2, CH, CHOH, CO, S, SO or SO2; R1-R4 =H, OH, (lower alkyl)sulphonylamino, 1- or 2-imidazolyl, 2-imidazolyl or acetamido; R5-R8 = H, OH, lower alkyl, halo, lower alkoxy, trifluoromethyl or trifluoromethyloxy; a, b = optionally double bonds, provided that when a is double, b cannot be double; n = 0-2; m = 1-3; and p = 0 or 1.
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