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公开(公告)号:DK0906301T3
公开(公告)日:2003-02-10
申请号:DK97921737
申请日:1997-04-24
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , STADLER HEINZ , WICHMANN JUERGEN
IPC: A61K31/34 , A61K31/343 , A61P25/00 , A61P25/20 , A61P25/28 , C07D307/85 , C07D307/86
Abstract: The invention is concerned with the use of compounds of the general formula wherein R1-R4 signify hydrogen, halogen, lower-alkyl, lower-alkoxy, aryl, benzyloxy, lower-alkoxy-lower-alkyl, lower-alkyl-sulphanyl, lower-alkyl-sulphanyl-lower-alkyl or R1 and R2 together signify the group -O-(CH2)2- or -(CH2)2-O- and R5 signifies hydrogen or hydroxy, as well as their pharmaceutically acceptable salts in the control or prevention of illnesses or disorders of the central nervous system such as migraine, schizophrenia, anxiety states, sleep disorders, anorexia, Alzheimer's disease, addictions (alcohol, nicotine, benzodiazepine, cocaine, etc.), as well as disorders which result from damage to the head/brain or to the spinal column/bone marrow and, respectively, for the production of corresponding medicaments.
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公开(公告)号:PL350536A1
公开(公告)日:2002-12-16
申请号:PL35053600
申请日:2000-02-28
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC: C07D295/14 , A61K31/166 , A61K31/167 , A61K31/495 , A61K31/496 , A61P1/04 , A61P1/08 , A61P11/06 , A61P25/24 , A61P25/28 , A61P29/00 , A61P37/08 , A61P43/00 , C07C41/01 , C07C43/174 , C07C209/06 , C07C209/50 , C07C211/29 , C07C211/45 , C07C217/54 , C07C231/02 , C07C231/08 , C07C233/11 , C07C233/15 , C07C233/44 , C07C233/66 , C07C235/42 , C07D295/155 , A61P25/00
Abstract: The invention relates to compounds of the formulawhereinR is hydrogen, lower alkyl, lower alkoxy halogen, amino, -N(R6)2 or trifluoromethyl;R1 is hydrogen lower alkoxy or halogen,R and R1 may be together -CH=CH-CH=CH-;R2 is halogen, lower alkyl or trifluoromethyl;R3 is hydrogen or lower alkyl;R4 is hydrogen or a cyclic tertiary amine, optionally substituted by lower alkyl;R5 is hydrogen, nitro, amino or -N(R6)2;R6 is hydrogen or lower alkyl,X is -C(O)N(R6)-, -(CH2)nO-, (CH2)nN(R6)-, -N(R6)C(O)- or -N(R6)(CH2)n-; andn is 1 or 2;and pharmaceutically acceptable acid addition salts thereof.The compounds of formula I may be used for the treatment of diseases related to the NK-1 receptor.
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公开(公告)号:HK1045684A1
公开(公告)日:2002-12-06
申请号:HK02107102
申请日:2002-09-26
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC: C07D295/14 , A61K31/166 , A61K31/167 , A61K31/495 , A61K31/496 , A61P1/04 , A61P1/08 , A61P11/06 , A61P25/24 , A61P25/28 , A61P29/00 , A61P37/08 , A61P43/00 , C07C41/01 , C07C43/174 , C07C209/06 , C07C209/50 , C07C211/29 , C07C211/45 , C07C217/54 , C07C231/02 , C07C231/08 , C07C233/11 , C07C233/15 , C07C233/44 , C07C233/66 , C07C235/42 , C07D295/155 , C07C , A61K
Abstract: The invention relates to compounds of the formulawhereinR is hydrogen, lower alkyl, lower alkoxy halogen, amino, -N(R6)2 or trifluoromethyl;R1 is hydrogen lower alkoxy or halogen,R and R1 may be together -CH=CH-CH=CH-;R2 is halogen, lower alkyl or trifluoromethyl;R3 is hydrogen or lower alkyl;R4 is hydrogen or a cyclic tertiary amine, optionally substituted by lower alkyl;R5 is hydrogen, nitro, amino or -N(R6)2;R6 is hydrogen or lower alkyl,X is -C(O)N(R6)-, -(CH2)nO-, (CH2)nN(R6)-, -N(R6)C(O)- or -N(R6)(CH2)n-; andn is 1 or 2;and pharmaceutically acceptable acid addition salts thereof.The compounds of formula I may be used for the treatment of diseases related to the NK-1 receptor.
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公开(公告)号:ZA200106371B
公开(公告)日:2002-11-04
申请号:ZA200106371
申请日:2001-08-02
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 , C07D , A61P , A61K
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:HRP20010629A2
公开(公告)日:2002-08-31
申请号:HRP20010629
申请日:2001-08-28
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC: C07D295/14 , A61K31/166 , A61K31/167 , A61K31/495 , A61K31/496 , A61P1/04 , A61P1/08 , A61P11/06 , A61P25/24 , A61P25/28 , A61P29/00 , A61P37/08 , A61P43/00 , C07C41/01 , C07C43/174 , C07C209/06 , C07C209/50 , C07C211/29 , C07C211/45 , C07C217/54 , C07C231/02 , C07C231/08 , C07C233/11 , C07C233/15 , C07C233/44 , C07C233/66 , C07C235/42 , C07D295/155
Abstract: The invention relates to compounds of the formulawhereinR is hydrogen, lower alkyl, lower alkoxy halogen, amino, -N(R6)2 or trifluoromethyl;R1 is hydrogen lower alkoxy or halogen,R and R1 may be together -CH=CH-CH=CH-;R2 is halogen, lower alkyl or trifluoromethyl;R3 is hydrogen or lower alkyl;R4 is hydrogen or a cyclic tertiary amine, optionally substituted by lower alkyl;R5 is hydrogen, nitro, amino or -N(R6)2;R6 is hydrogen or lower alkyl,X is -C(O)N(R6)-, -(CH2)nO-, (CH2)nN(R6)-, -N(R6)C(O)- or -N(R6)(CH2)n-; andn is 1 or 2;and pharmaceutically acceptable acid addition salts thereof.The compounds of formula I may be used for the treatment of diseases related to the NK-1 receptor.
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86.
公开(公告)号:CO5170529A1
公开(公告)日:2002-06-27
申请号:CO00039601
申请日:2000-05-29
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC: A61K31/505 , A61K31/506 , A61K31/513 , A61K31/5377 , A61P1/04 , A61P1/08 , A61P9/00 , A61P11/02 , A61P11/06 , A61P17/02 , A61P25/00 , A61P25/06 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P29/00 , A61P37/08 , A61P43/00 , C07D213/00 , C07D239/00 , C07D239/28 , C07D239/34 , C07D239/38 , C07D239/42 , C07D239/46 , C07D239/48 , C07D295/00 , C07D401/04
Abstract: Compuestos de fórmula general: en dondeR1 es hidrógeno o halógeno;R2 es hidrógeno, halógeno, alquilo C1-C7 o alcoxilo C1-C7;R3 es halógeno, trifluorometilo, alcoxilo C1-C7 o alquilo C1-C7 ;R4/R4´ son independientemente entre sí, hidrógeno o alquilo C1-C7;R5 es alquilo C1-C7, alcoxilo C1-C7, amino, hidroxilo, hidroxialquilo C1-C7, -(CH2)n-piperazinilo, -(CH2)n-morfolinilo opcionalmente substituido con alquilo C1-C7, -(CH2)n+1-imidazolilo, -O-(CH2)n+1-morfolinilo, -O-(CH2)n+1-piperidinilo, alquilo C1-C7-sulfanilo, alquilo C1-C7-sulfonilo, bencilamino, -NH-(CH2)n+1 N(R4")2, -(CH2)n-NH-(CH2)n+1N(R4")2, -(CH2)n+1N(R4")2, ó -O-(CH2)n+1N(R4")2 en donde R4" es hidrógeno o alquilo C1-C7;R6 es hidrógeno;R2 y R6 ó R1 y R6 pueden ser juntamente con los dos átomos de carbono del anillo, -CH=CH-CH=CH-, con la condición de que n para R1 sea 1;n es independientemente 0 - 2; yX es -C(O)N(R4" )- ó N(R4" )C(O)-;o las sales de adición ácida farmacéuticamente aceptables de los mismos.
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公开(公告)号:TR200102489T2
公开(公告)日:2002-04-22
申请号:TR200102489
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:CZ20013047A3
公开(公告)日:2002-02-13
申请号:CZ20013047
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:CZ20013046A3
公开(公告)日:2002-02-13
申请号:CZ20013046
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 , A61K31/167 , A61K31/44 , A61P25/00 , A61P29/00 , C07C211/54 , C07C233/29 , C07C233/33 , C07C233/44 , C07C317/14 , C07C317/40 , C07C323/41 , C07D213/75 , C07D213/79 , C07D213/81 , C07D295/12 , C07D295/135 , C07D401/04 , C07D213/60 , A61K31/435
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:BR0008494A
公开(公告)日:2002-02-05
申请号:BR0008494
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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