公开(公告)号：AU742735B2

公开(公告)日：2002-01-10

申请号：AU5986698

申请日：1998-01-07

Applicant: HOFFMANN LA ROCHE

Inventor： BOS MICHAEL ,  STADLER HEINZ ,  WICHMANN JURGEN

IPC: C07D217/24 ,  A61K31/40 ,  A61K31/403 ,  A61K31/435 ,  A61K31/473 ,  A61P1/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/12 ,  A61P25/00 ,  C07D209/62 ,  C07D221/10 ,  C07D491/04 ,  C07D491/056 ,  C07D221/00 ,  C07D317/00

公开(公告)号：PE20010009A1

公开(公告)日：2001-02-07

申请号：PE0001232000

申请日：2000-02-18

Applicant: HOFFMANN LA ROCHE

Inventor： BOS MICHAEL ,  GALLEY GUIDO ,  HOFFMANN TORSTEN ,  HUNKELER WALTER ,  STADLER HEINZ ,  GODEL THIERRY ,  SCHNIDER PATRICK

IPC: A61K31/167 ,  C07C211/44 ,  A61K31/44 ,  A61P25/00 ,  A61P29/00 ,  C07C211/54 ,  C07C233/29 ,  C07C233/33 ,  C07C233/44 ,  C07C317/14 ,  C07C317/40 ,  C07C323/41 ,  C07D213/00 ,  C07D213/75 ,  C07D213/79 ,  C07D213/81 ,  C07D295/12 ,  C07D295/135 ,  C07D401/04

Abstract: SE REFIERE A DERIVADOS DE FENIL Y PIRIDINILO DE FORMULA I DONDE R ES H, ALQUILO, ALCOXI, HALOGENO, TRIFLUOROMETILO; R1 ES H, HALOGENO; R Y R1 SON -CH=CH-CH=CH-; R2 ES H, HALOGENO, TRIFLUOROMETILO, ALCOXI, CIANO; R3 ES H, ALQUILO, CICLOALQUILO; R4 ES H, HALOGENO, ALQUILO, ALCOXI, N(R5)2, N(R5)S(O)2-ALQUILO, N(R5)C(O)R5, AMINA TERCIARIA CICLICA DE GRUPO a; R5 ES H, CICLOALQUILO C3-C6, BENCILO, ALQUILO; R6 ES H, HIDROXI, ALQUILO, N(R5)CO-ALQUILO, HIDROXI-ALQUILO, CIANO, -CHO, HETEROCICLO DE 5 O 6 MIEMBROS; X ES -C(O)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-,-N(R5)C(O)-, -C(O)O-, -N(R5)(CH2)m-; Y ES -(CH2)n, O, S, SO2, C(O), N(R5); Z ES =N-, -CH=, -C(Cl)=, n ES 0-4; m ES 1-2. SON COMPUESTOS PREFERIDOS N-[2-BENZOIL-4-(4-METIL-PIPERAZIN-1-IL)-FENIL]-2-(3,5-BIS-TRIFLUOROMETILFENIL)-ISOBUTIRAMIDA, 4-BENZOIL-N-(3,5-BIS-TRIFLUOROMETIL-BENCIL)-N-METIL-6-(4-METIL-PIPERAZIN-1-IL)-NICOTINAMIDA, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO PARA LA PREPARACION. LOS DERIVADOS DE FENIL Y PIRIDINILO SON ANTAGONISTAS DEL RECEPTOR NEUROQUININA 1 (NK-1) POR LO QUE PUEDEN SER UTILES PARA EL TRATAMIENTO DE TRASTORNOS DEL SISTEMA NERVIOSO CENTRAL, DEPRESION, EMESIS

公开(公告)号：CO4940471A1

公开(公告)日：2000-07-24

申请号：CO97023102

申请日：1997-04-30

Applicant: HOFFMANN LA ROCHE

Inventor： BOS MICHAEL ,  STADLER HEINZ ,  WICHMANN JURGEN

IPC: A61K31/155 ,  A61K31/34 ,  A61K31/343 ,  A61P25/00 ,  A61P25/20 ,  A61P25/28 ,  C07D307/85 ,  C07D307/86

Abstract: El empleo de compuestos de fórmula general en donde R1 - R4 significan hidrógeno, halógeno, alquilo inferior, alcoxilo inferior, arilo, benciloxilo, alcoxilo inferior-alquilo inferior, alquilo inferior-sulfanilo, alquilo inferior-sulfanilo-alquilo inferior, o R1 y R2 juntos significan el grupo -O- (CH2 )2 - ó (CH2 )2 -O-, y R5 significa hidrógeno o hidroxilo,así como también sus sales farmacéuticamente aceptables, en el control o prevención de enfermedades o trastornos del sistema nervioso central, tales como la migraña, esquizofrenia, estados de ansiedad, trastornos del sueño, anorexia, enfermedad de alzheimer, adicciones (alcohol, nicotina, benzodiazepina, cocaína, etc.), así como también trastornos que resultan de lesiones en la cabeza/cerebro o en la columna vertebral/médula ósea y respectivamente, para la producción de los correspondientes medicamentos.

公开(公告)号：PE01702000A1

公开(公告)日：2000-03-29

申请号：PE00002799

申请日：1999-01-12

Applicant: HOFFMANN LA ROCHE

Inventor： BOS MICHAEL ,  RIEMER CLAUS ,  HUNKELER WALTER

IPC: C07C309/30 ,  A61K31/00 ,  A61K31/10 ,  A61K31/135 ,  A61K31/33 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/505 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07C315/04 ,  C07C317/22 ,  C07C317/32 ,  C07C317/36 ,  C07D213/61 ,  C07D213/62 ,  C07D213/71 ,  C07D213/73 ,  C07D213/74 ,  C07D213/84 ,  C07D239/38 ,  C07D317/14 ,  C07D401/04 ,  C07D401/14 ,  C07D409/04

CPC classification number: C07D213/73 ,  C07C317/36 ,  C07D213/71 ,  C07D213/74 ,  C07D213/84 ,  C07D239/38

Abstract: SE REFIERE A COMPUESTOS DE FORMULA I, DONDE R1 ES H; R2 ES H, TRIFLUOROMETILO, ALQUILO; R3 ES H o AMINO; O R1 Y R2 o R3 Y R2 SON -CH=CH-CH=CH-; Z ES PIRIMIDIN-4-ILO, PIRIDIN-4-ILO, PIRIDIN-2-ILO O FENILO; R4, R5 SON H, ALQUILO, TRIFLUOROMETILO, HALOGENO, ALCOXILO, -NH(CH2)nNR6R7, -N(CH3)(CH2)nNR6R7, NH(CH2)n-MORFOLIN-4-ILO, -NH(CH2)nOH; n ES 2-4; R6 Y R7 SON H O ALQUILO; CUANDO Z ES PIRIMIDIN-4-ILO; R4 NO ES R5; CUANDO Z ES PIRIDIN-2-ILO; R5 NO ES ALQUILO; CUANDO Z ES FENILO, R4 Y UNO DE R1-R3 NO SON H. SON COMPUESTOS PREFERIDOS [4-(4-AMINOBENCENSULFONIL)-6-BROMOPIRIMIDIN-2-IL]-METILAMINA, [2-(4-AMINOBENCENSULFONIL)-6-BROMPIRIDIN-4-IL]-METILAMINA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. EL COMPUESTO I POSEE AFINIDAD SELECTIVA A RECEPTORES 5HT-6 POR LO QUE PUEDE SER UTIL EN EL TRATAMIENTO O PREVENCION DE TRASTORNOS DEL SISTEMA NERVIOSO CENTRAL COMO PSICOSIS, ESQUIZOFRENIA, DEPRESIONES MANIACAS, TRASTORNOS NEUROLOGICOS

公开(公告)号：CZ12099A3

公开(公告)日：1999-08-11

申请号：CZ12099

申请日：1999-01-14

Applicant: HOFFMANN LA ROCHE

Inventor： BOS MICHAEL ,  HUNKELER WALTER ,  RIEMER CLAUS

IPC: C07C309/30 ,  A61K31/00 ,  A61K31/10 ,  A61K31/135 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/505 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07C315/04 ,  C07C317/22 ,  C07C317/32 ,  C07C317/36 ,  C07D213/61 ,  C07D213/62 ,  C07D213/71 ,  C07D213/73 ,  C07D213/74 ,  C07D213/84 ,  C07D239/38 ,  C07D401/04 ,  C07D401/14 ,  C07D409/04

Abstract: The present invention relates to novel compounds of the general formula wherein R is hydrogen; R is hydrogen, trifluoromethyl or lower alkyl; R is hydrogen or amino; or R and R or R and R taken together are -CH=CH-CH=CH-; Z is pyrimidin-4-yl, pyridin-4-yl, pyridin-2-yl or phenyl; R R are each independently hydrogen, lower alkyl, trifluoromethyl, halogen, lower alkoxy, nitrilo, amino, lower alkyl-amino, di-lower alkyl-amino, piperazinyl, morpholinyl, pyrrolidinyl, vinyl, C3-C6 cycloalkyl, C3-C6 cycloalkenyl, t-buthylethinyl, hydroxyalkylethinyl, phenylethinyl, naphthyl, thiophenyl, or phenyl, which may be substituted by halogen, lower alkoxy, lower alkyl, trifluoromethyl or nitro, or a group -NH(CH2)nNR R , -N(CH3)(CH2)nNR R , -NH(CH2)n-morpholin-4-yl or -NH(CH2)nOH; n is 2-4 R and R are each independently hydrogen or lower alkyl, and to their pharmaceutically acceptable salts. It has been found that the compounds of formula I possess a selective affinity to 5HT-6 receptors.

公开(公告)号：AU680543B2

公开(公告)日：1997-07-31

申请号：AU7583894

申请日：1994-10-14

Applicant: HOFFMANN LA ROCHE

Inventor： BOS MICHAEL ,  WICHMANN JURGEN ,  WIDMER ULRICH

IPC: C07D491/052 ,  A61K31/40 ,  A61K31/403 ,  A61P1/00 ,  A61P7/02 ,  A61P9/12 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D209/56 ,  C07D209/58 ,  C07D209/60 ,  C07D209/70 ,  C07D209/96 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

Abstract: The present invention relates to tricyclic pyrrole derivatives of the formula wherein R to R are each hydrogen, halogen, lower alkyl, phenyl, cycloalkyl or lower alkoxy and R is additionally lower alkoxycarbonyl, acyloxy or mesyloxy; R to R are each hydrogen or lower alkyl; X is -CH2CH(C6H5)-, -CH=C(C6H5)-, -YCH2-, -CH=CH- or -(CR )n; R and R are each hydrogen, phenyl, lower alkyl or halogen; n is 1 to 3 and Y is O or S, and pharmaceutically acceptable salts of basic compounds of the formula I with acids. These compounds are particularly suitable for the control or prevention of central nervous disorders, such as depressions, bipolar disorders, anxiety states, sleep and sexual disorders, psychoses, schizophrenia, migraine and other states associated with headache or pain of other types, personality disorders or obsessive-compulsive disorders, social phobias 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 nervous system as a result of trauma, stroke, neurodegenerative disorders etc.; cardiovascular disorders, such as high blood pressure, thrombosis, stroke etc.; and gastrointestinal disorders, such as dysfunction of the motility of the gastrointestinal tract.

公开(公告)号：NZ264713A

公开(公告)日：1996-05-28

申请号：NZ26471394

申请日：1994-10-17

Applicant: HOFFMANN LA ROCHE

Inventor： BOS 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.

公开(公告)号：AU7583794A

公开(公告)日：1995-05-11

申请号：AU7583794

申请日：1994-10-14

Applicant: HOFFMANN LA ROCHE

Inventor： BOS 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.

公开(公告)号：CA2265095C

公开(公告)日：2008-07-22

申请号：CA2265095

申请日：1999-03-08

Applicant: HOFFMANN LA ROCHE

Inventor： STADLER HEINZ ,  RIEMER CLAUS ,  BOS MICHAEL

IPC: C07D487/04 ,  A61K31/00 ,  A61K31/4162 ,  A61K31/505 ,  A61K31/519 ,  A61K31/529 ,  A61K31/53 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5377 ,  A61P9/10 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D231/54 ,  C07D251/72 ,  C07D495/14

Abstract: The present invention is concerned with pyrazolopyrimidines and pyrazolotriazines of the general formulae (see fig. I) and (see fig. II) and their pharmaceutically acceptable salts. Surprisingly, these compounds have a selective affinity to 5HT-6 receptors. They are accordingly suitable for the treatment and prevention of central nervous disorders such as, for example, psychoses, schizophrenia, manic depressions, depressions, neurological disorders, memory disorders, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease and Huntington's chorea.

公开(公告)号：GC0000191A

公开(公告)日：2006-03-29

申请号：GCP2000684

申请日：2000-05-30

Applicant: HOFFMANN LA ROCHE

Inventor： BOS 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.