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公开(公告)号：TR200102490T2
公开(公告)日：2001-12-21
申请号：TR200102490
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: A61K31/167 , A61K31/44 , A61P25/00 , A61P29/00 , C07C211/54 , C07C211/44 , C07C233/29 , C07C233/33 , C07C233/44 , C07C317/14 , C07C317/40 , C07C323/41 , C07D213/75 , C07D213/79 , C07D213/81 , C07D295/12 , C07D295/135 , C07D401/04 , A61K31
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：NO20014098A
公开(公告)日：2001-08-23
申请号：NO20014098
申请日：2001-08-23
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
CPC classification number: C07D213/75 , C07D213/38 , C07D213/81
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公开(公告)号：NO20014096A
公开(公告)日：2001-08-23
申请号：NO20014096
申请日：2001-08-23
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 , C07D213/00
CPC classification number: C07D213/75 , C07C233/29 , C07C233/33 , C07C233/44 , C07C317/40 , C07C323/41 , C07D295/135
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公开(公告)号：PA8491101A1
公开(公告)日：2001-04-30
申请号：PA8491101
申请日：2000-02-22
Applicant: HOFFMANN LA ROCHE
Inventor： BOES MICHAEL , BRANCA QUIRICO , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC: A61K20060101 , A61K9/20 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/444 , A61K31/455 , A61K31/496 , A61P1/00 , A61P9/00 , A61P11/00 , A61P25/00 , A61P25/04 , A61P25/28 , A61P25/30 , A61P27/02 , A61P29/00 , A61P43/00 , C07D20060101 , C07D213/26 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/63 , C07D213/65 , C07D213/74 , C07D213/75 , C07D213/78 , C07D213/82 , C07D401/04 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14
Abstract: LA PRESENTE INVENCION SE REFIERE A COMPUESTOS DE LA FORMULA GENERAL EN DONDE R ES HIDROGENO, ALQUILO INFERIOR, ALCOXI INFERIOR, HALOGENO O TRIFLUOROMETILO; R1 ES HIDROGENO O HALOGENO; O R Y R1 PUEDEN SER CONJUNTAMENTE -CH=CH-CH=CH-; R2 Y R2', SON INDEPENDIENTEMENTE, HIDROGENO, HALOGENO, TRIFLUOROMETILO, CIANO O ALCOXI INFERIOR;O R2 Y R2', PUEDEN SER CONJUNTAMENTE -CH=CH-CH=CH-, SUSTITUIDO OPCIONALMENTE POR UNO O DOS SUSTITUYENTES SELECCIONADOS DEL ALQUILO INFERIOR O DEL ALCOXI INFERIOR; R3 ES HIDROGENO,ALQUILO INFERIOR O FORMA UN GRUPO CICLOALQUILO; R4 ES HIDROGENO, -N (R5)2, -N(R5)(CH2)nOH,-N (R5)S(O)2- ALQUILO INFERIOR, -N(R5)S(O)2-FENILO,-N=CH-N(R5)2,-N(R5)C(O)R5 O UNA AMINA TERCIARIA CICLICA DEL GRUPO R5 ES INDEPENDIENTEMENTE, HIDROGENO, C3-6-CICLOALQUILO,BENCILO O ALQUILO INFERIOR; R6 ES HIDROGENO, HIDROXI, ALQUILO INFERIOR , -(CH2)nCOO-ALQUILO INFERIOR, -N(R5)CO-ALQUILO INFERIOR, HIDROXI-ALQUILO-INFERIOR, CIANO,-(CH2)nO(CH2)nOH,-CHO O UN GRUPO HETEROCICLICO DE 5 O 6 MIEMBROS, UNIDO OPCIONALMENTE POR UN GRUPO ALQUILENO, X ES -C(O)N(R5)-,-(CH2)mO-,-(CH2)mN(R5)-,-N(R5)C(O)-, ó -N(R5)(CH2)m-; N ES 0-4; Y M ES 1 ó 2; Y SALES DERIVADAS DE UNA ADICION ACIDA FARMACEUTICAMENTE ACEPTABLES. LOS COMPUESTOS DE LA FORMULA 1 MUESTRAN UNA MAYOR AFINIDAD POR EL RECEPTOR DE NK-1. ESTOS SE PUEDEN USAR PARA EL TRATAMIENTO DE ENFERMEDADES QUE ESTEN RELACIONADAS CON ANTAGONISTAS DEL RECEPTOR DE NK-1.
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35.发明专利
公开(公告)号：HU0000748A2
公开(公告)日：2001-03-28
申请号：HU0000748
申请日：2000-02-21
Applicant: HOFFMANN LA ROCHE
Inventor： QUIRICO DR BRANCA , BOES MICHAEL , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER DR , SCHNIDER PATRICK , STADLER HEINZ DR
IPC: A61K20060101 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/444 , A61K31/455 , A61K31/496 , A61P1/00 , A61P9/00 , A61P11/00 , A61P25/00 , A61P25/04 , A61P25/28 , A61P25/30 , A61P27/02 , A61P29/00 , A61P43/00 , C07D20060101 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/63 , C07D213/65 , C07D213/74 , C07D213/75 , C07D213/78 , C07D213/82 , C07D401/04 , C07D401/12 , C07D413/12 , C07D413/14
Abstract: The present invention relates to compounds of the general formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R is hydrogen or halogen; or R and R may be together -CH=CH-CH=CH-; R and R are independently from each other hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or R and R may be together -CH=CH-CH=CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; R is hydrogen, lower alkyl or form a cycloalkyl group; R is hydrogen, -N(R )2, -N(R )(CH2)nOH, -N(R )S(O)2-lower alkyl, -N(R )S(O)2-phenyl, -N=CH-N(R )2, -N(R )C(O)R or a cyclic tertiary amine of the group R is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R is hydrogen, hydroxy, lower alkyl, -(CH2)nCOO-lower alkyl, -N(R )CO-lower alkyl, hydroxy-lower alkyl, cyano, -(CH2)nO(CH2)nOH, -CHO or a 5-or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is -C(O)N(R )-, -(CH2)mO-, -(CH2)mN(R )-, -N(R )C(O)-, or -N(R )(CH2)m-; n is 0 - 4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I show a high affinity to the NK-1 receptor. They may be used for the treatment of diseases, which relate to NK-1 receptor antagonists.
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Patent Agency Ranking
公开(公告)号：CA2375671A1
公开(公告)日：2000-12-07
申请号：CA2375671
申请日：2000-05-24
Applicant: HOFFMANN LA ROCHE
Inventor： HUNKELER WALTER , HOFFMANN TORSTEN , GODEL THIERRY , GALLEY GUIDO , STADLER HEINZ , SCHNIDER PATRICK , BOES MICHAEL
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 relates to compounds of formula (I) wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R1 and R2 may be together with the two carbon atoms -CH=CH-CH=CH-; R3 is halogen, trifluoromethyl, lower alkyl or lower alkoxy; R4/R4' are independently from each other 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; and n 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 be used for the treatment of diseases related to this receptor.
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公开(公告)号：PL179561B1
公开(公告)日：2000-09-29
申请号：PL30554394
申请日：1994-10-21
Applicant: HOFFMANN LA ROCHE
Inventor： BOES MICHAEL
IPC: A61K31/40 , A61K31/403 , A61K31/404 , A61K31/4045 , A61P1/00 , A61P7/02 , A61P9/00 , A61P9/12 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07D209/04 , C07D209/08 , C07D209/24 , C07D209/30 , C07D209/36
Abstract: The invention relates to compounds of the formula wherein R to R are hydrogen, halogen, lower alkyl, cycloalkyl or trifluoromethyl, R and R are hydrogen, halogen, lower alkyl, cycloalkyl, trifluoromethyl, hydroxyl or lower alkoxy and R is hydrogen or lower alkyl, and pharmaceutically acceptable acid addition salts of the compounds of the formula I. These compounds are particularly suitable for the treatment or prevention of central nervous disorders such as depressions, bipolar disorders, anxiety states, sleep and sexual disorders, psychoses, schizophrenia, migraine and other conditions associated with headache or pain of other types, personality disorders or obsessive-compulsive disorders, social phobia or panic attacks, organic mental disorders, mental disorders in childhood, aggressiveness, age-related memory disorders and behavioural disorders, addiction, obesity, bulimia etc., damage to the central nervous system as a result of trauma, stroke, neurodegenerative disorders etc.; cardiovascular disorders, such as high blood pressure, thrombosis, stroke, and gastrointestinal disorders, such as dysfunction of the motility of the gastrointestinal tract.
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公开(公告)号：CA2364665A1
公开(公告)日：2000-08-31
申请号：CA2364665
申请日：2000-02-15
Applicant: HOFFMANN LA ROCHE
Inventor： STADLER HEINZ , HUNKELER WALTER , GALLEY GUIDO , GODEL THIERRY , SCHNIDER PATRICK , HOFFMANN TORSTEN , BOES MICHAEL
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
Abstract: The invention relates to compounds of general formula (I), wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R1 is hydrogen or halogen; or R and R1 may be together -CH=CH-CH=CH-; R2 is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; R3 is independent ly from each other hydrogen, lower alkyl or form a cycloalkyl group; R4 is hydrogen, halogen, lower alkyl, lower alkoxy, -N(R5)2, -N(R5)S(O)2-lower alkyl, -N(R5)C(O)R5 or a cyclic tertiary amine of the group (a); R5 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, optionall y bonded via an alkylene group, X is -C(O)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-, - N(R5) C(O)-, C(O)O- or -N(R5)(CH2)m-; Y is -(CH2)n-, -O-, -S-, SO2-, -C(O)- or -N(R5)-; Z is =N-, -CH= or -C(C1)=; n is 0 - 4; and, is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the compounds of formula (I) have a high affinity to the NK-1 receptor.
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公开(公告)号：CA2364662A1
公开(公告)日：2000-08-31
申请号：CA2364662
申请日：2000-02-15
Applicant: HOFFMANN LA ROCHE
Inventor： STADLER HEINZ , GALLEY GUIDO , SCHNIDER PATRICK , HOFFMANN TORSTEN , HUNKELER WALTER , GODEL THIERRY , BOES MICHAEL
IPC: A61K31/44 , A61P25/00 , A61P29/00 , C07D213/30 , C07D213/38 , C07D213/75 , C07D213/81 , C07D401/04
Abstract: The invention relates to compounds of formula (I) wherein R is hydrogen, low er alkyl, lower alkoxy, halogen or trifluoromethyl; R1 is hydrogen or halogen; or R 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 group (a); R5 is, independentl y 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; and m 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：IS5381A
公开(公告)日：2000-08-25
申请号：IS5381
申请日：2000-02-22
Applicant: HOFFMANN LA ROCHE
Inventor： BOES MICHAEL , BRANCA QUIRICO , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC: A61K20060101 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/444 , A61K31/455 , A61K31/496 , A61P1/00 , A61P9/00 , A61P11/00 , A61P25/00 , A61P25/04 , A61P25/28 , A61P25/30 , A61P27/02 , A61P29/00 , A61P43/00 , C07D20060101 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/63 , C07D213/65 , C07D213/74 , C07D213/75 , C07D213/78 , C07D213/82 , C07D401/04 , C07D401/12 , C07D413/12 , C07D413/14 , A61K31/442
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