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公开(公告)号:BRPI0415070A
公开(公告)日:2006-12-12
申请号:BRPI0415070
申请日:2004-09-27
Applicant: HOFFMANN LA ROCHE
Inventor: FLOHR ALEXANDER , GALLEY GUIDO , JAKOB-ROETNE ROLAND , KITAS ERIC ARGIRIOS , PETERS JENS-UWE , WOSTL WOLFGANG
IPC: C07D223/16 , C07D223/18 , C07D243/12 , C07D243/24 , C07D409/12 , A61K31/55 , A61K31/5513 , A61P25/28
Abstract: The present invention provides compounds of the general formula wherein R 4 is one of the following groups and R 1 , R 2 , R 3 , R 7 , R 8 , and R 9 are as defined in the specification and pharmaceutically acceptable salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. The compounds are useful for the treatment of Alzheimer's disease.
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公开(公告)号:DE60031513D1
公开(公告)日:2006-12-07
申请号:DE60031513
申请日:2000-02-15
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC: C07C211/44 , C07D213/75 , A61K31/167 , A61K31/44 , A61P25/00 , A61P29/00 , C07C211/54 , C07C233/29 , C07C233/33 , C07C233/44 , C07C317/14 , C07C317/40 , C07C323/41 , C07D213/79 , C07D213/81 , C07D295/12 , C07D295/135 , C07D401/04
Abstract: The present invention is a series of compounds formed from phenyl substituted pyridine or benzene derivatives and their pharmaceutically acceptable salts. These compounds have shown high affinity as antagonists to the NK-1 receptor.
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公开(公告)号:SI1187815T1
公开(公告)日:2006-06-30
申请号:SI200030813
申请日:2000-05-24
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC: C07D239/00 , A61K31/00 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P1/04 , A61P1/08 , A61P9/00 , A61P11/06 , A61P17/02 , A61P19/02 , A61P25/00 , A61P25/06 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/36 , A61P27/00 , A61P27/02 , A61P29/00 , A61P37/08 , A61P43/00 , C07D213/00 , C07D239/28 , C07D239/32 , C07D239/34 , C07D239/38 , C07D239/42 , C07D239/48 , C07D295/00 , C07D401/00 , C07D401/04 , C07D403/04
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公开(公告)号:NO20061047L
公开(公告)日:2006-04-04
申请号:NO20061047
申请日:2006-03-03
Applicant: HOFFMANN LA ROCHE
Inventor: JAKOB-ROETNE ROLAND , WOSTL WOLFGANG , FLOHR ALEXANDER , GALLEY GUIDO , KITAS ERIC ARGIRIOS , PETERS JENS-UWE
IPC: C07D223/18 , A61K31/335 , A61K31/55 , A61K31/5513 , C07D223/16 , C07D223/20 , C07D243/24 , C07D273/00 , C07D313/14
Abstract: The invention relates to malonamide derivatives of formula wherein each of the variables are as defined herein and to pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates and diastereomeric mixtures thereof. These compounds are gamma-secretase inhibitors and may be used for the treatment of Alzheimer's disease.
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公开(公告)号:NO20061047A
公开(公告)日:2006-04-04
申请号:NO20061047
申请日:2006-03-03
Applicant: HOFFMANN LA ROCHE
Inventor: JAKOB-ROETNE ROLAND , WOSTL WOLFGANG , FLOHR ALEXANDER , GALLEY GUIDO , KITAS ERIC ARGIRIOS , PETERS JENS-UWE
IPC: C07D223/18 , A61K31/335 , A61K31/55 , A61K31/5513 , C07D223/16 , C07D223/20 , C07D243/24 , C07D273/00 , C07D313/14
CPC classification number: C07D223/16 , A61K31/335 , A61K31/55 , A61K31/5513 , C07D223/20 , C07D243/24 , C07D273/00 , C07D313/14
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公开(公告)号:GC0000183A
公开(公告)日:2006-03-29
申请号:GCP2000535
申请日:2000-02-23
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC: A61K31/44 , A61P25/00 , A61P29/00 , C07D213/30 , C07D213/38 , C07D213/75 , C07D213/81 , C07D401/04
Abstract: The invention relates to compounds of the formulawhereinR is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl;R1 is hydrogen or halogen; orR and R1 may be together -CH=CH-CH=CH-;R2 is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano;R3 is hydrogen, lower alkyl or form a cycloalkyl group;R4 is hydrogen, -N(R5)2, -N(R5)S(O)2-lower alkyl, -N(R5)C(O)R5 or a cyclic tertiary amine of the groupR5 is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl;R6 is hydrogen, hydroxy, lower alkyl, -N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyano, -CHO or a 5- or 6 membered heterocyclic group, optionally bonded via an alkylene group,X is -C(O)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-, -N(R5)C(O)-, or -N(R5)(CH2)m-;n is 0-4; andm is 1 or 2;and to pharmaceutically acceptable acid addition salts thereof.It has been shown that the above mentioned compounds have a good affinity to the NK-1 receptor.
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公开(公告)号:DE60015089T2
公开(公告)日:2006-02-16
申请号:DE60015089
申请日:2000-02-15
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC: A61K31/44 , A61P25/00 , A61P29/00 , C07D213/30 , C07D213/38 , C07D213/75 , C07D213/81 , C07D401/04
Abstract: The invention relates to compounds of the formulawhereinR is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl;R1 is hydrogen or halogen; orR and R1 may be together -CH=CH-CH=CH-;R2 is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano;R3 is hydrogen, lower alkyl or form a cycloalkyl group;R4 is hydrogen, -N(R5)2, -N(R5)S(O)2-lower alkyl, -N(R5)C(O)R5 or a cyclic tertiary amine of the groupR5 is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl;R6 is hydrogen, hydroxy, lower alkyl, -N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyano, -CHO or a 5- or 6 membered heterocyclic group, optionally bonded via an alkylene group,X is -C(O)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-, -N(R5)C(O)-, or -N(R5)(CH2)m-;n is 0-4; andm is 1 or 2;and to pharmaceutically acceptable acid addition salts thereof.It has been shown that the above mentioned compounds have a good affinity to the NK-1 receptor.
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公开(公告)号:AT317389T
公开(公告)日:2006-02-15
申请号:AT00927234
申请日:2000-05-24
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC: A61K31/496 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P1/04 , A61P1/08 , A61P9/00 , A61P11/06 , A61P17/02 , A61P19/02 , A61P25/00 , A61P25/06 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/36 , A61P27/00 , A61P27/02 , A61P29/00 , A61P37/08 , A61P43/00 , C07D213/00 , C07D239/00 , C07D239/28 , C07D239/32 , C07D239/34 , C07D239/38 , C07D239/42 , C07D239/48 , C07D295/00 , C07D401/04 , C07D403/04
Abstract: The invention provides compounds of the formulawhereinR1 is hydrogen or halogen;R2 is hydrogen, halogen, lower alkyl or lower alkoxy;R1 and R2 may together be -CH=CH-CH=CH-, wherein R1 and R2 together with the two carbon ring atoms to which they are attached form a fused ring;R3 is halogen, trifluoromethyl, lower alkyl or lower alkoxy;R4/R4' are each independently hydrogen or lower alkyl;R5 is lower alkyl, lower alkoxy, amino, phenyl, hydroxy-lower alkyl, cyano-lower alkyl, carbamoyl-lower alkyl, pyridyl, pyrimidyl, -(CH2)n-piperazinyl, which is optionally substituted by one or two lower alkyl groups or by hydroxy-lower alkyl, -(CH2)n-morpholinyl, -(CH2)n-piperidinyl, -(CH2)n+1-imidazolyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, -NH-(CH2)n+1N(R4'')2, -(CH2)n+1N(R4'')2, -O-(CH2)n+1-morpholinyl, -O-(CH2)n+1-piperidinyl or -O-(CH2)n+1N(R4'')2, wherein R4'' is hydrogen or lower alkyl; andn is 0-2;X is -C(O)N(R4'')- or -N(R4'')C(O)-;and to pharmaceutically acceptable acid addition salts thereof.It has been shown that the compounds have a good affinity to the NK-1 receptor and may therefore used for the treatment of diseases related to this receptor.
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公开(公告)号:AU2005261932A1
公开(公告)日:2006-01-19
申请号:AU2005261932
申请日:2005-07-06
Applicant: HOFFMANN LA ROCHE
Inventor: KITAS ERIC ARGIRIOS , GALLEY GUIDO , JAKOB-ROETNE ROLAND
IPC: C07D223/08 , A61K31/55
Abstract: The invention relates to compounds of the general formula in which R 1 , R 2 , R3, R 4 , R 2' , R3', R 4' , R 5 , and X is -CHR- are as defined in the specification. The invention also provides pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates and diastereomeric mixtures of such compounds. The invention further provides methods for the treatment of Alzheimer's disease or common cancers.
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公开(公告)号:ES2229557T3
公开(公告)日:2005-04-16
申请号:ES98965753
申请日:1998-12-03
Applicant: HOFFMANN LA ROCHE
Inventor: ADAM GEO , CESURA ANDREA , GALLEY GUIDO , JENCK FRANCOIS , ROVER STEPHAN , WICHMANN JURGEN
IPC: A61K31/435 , A61K31/438 , A61K31/439 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , C07D221/20 , C07D451/04 , C07D471/10 , C07D491/10 , C07D491/107 , C07D491/20 , C07D498/10 , C07D498/20
Abstract: Compuestos de la fórmula general donde X es ¿O- o ¿CH2-; Y es ¿C(O)-, -(CH2)n- o ¿N(CH3)-; n es 1 ó 2, o X e Y juntos son ¿CH=CH- Z es ¿NH-, -CH2-, -O- o =CH-; A1 es un grupo B es ¿(CH2)m-; m es 0, 1 ó 2; R1 y R2 son cada uno independientemente hidrógeno o alquilo C1-C6; R3 es hidrógeno o halógeno; R4 es cuando 2 es ¿NH-, -CH2- u ¿O-, hidrógeno o hidroxi y la línea de puntos es un grupo ¿CH2-CH2- opcional y a las sales de adición ácida farmacéuticamente aceptable de los mismos.
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