公开(公告)号：AU2769697A

公开(公告)日：1997-11-26

申请号：AU2769697

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.

公开(公告)号：CA2253547A1

公开(公告)日：1997-11-13

申请号：CA2253547

申请日：1997-04-24

Applicant: HOFFMANN LA ROCHE

Inventor： WICHMANN JUERGEN ,  STADLER HEINZ ,  BOES MICHAEL

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 general formula (I) 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.

公开(公告)号：HUT70848A

公开(公告)日：1995-11-28

申请号：HU9402983

申请日：1994-10-17

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.

公开(公告)号：BR9404203A

公开(公告)日：1995-07-04

申请号：BR9404203

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 ,  A61K31/405

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：ZA948093B

公开(公告)日：1995-06-05

申请号：ZA948093

申请日：1994-10-14

Applicant: HOFFMANN LA ROCHE

Inventor： BOES MICHAEL ,  WICHMANN JUERGEN ,  WIDMER ULRICH

IPC: A61K20060101 ,  A61K31/40 ,  A61K31/403 ,  A61K31/405 ,  A61K31/415 ,  C07D20060101 ,  C07D209/00 ,  C07D209/08 ,  C07D209/52 ,  C07D231/54 ,  C07D405/00 ,  C07D409/00 ,  C07D491/04 ,  C07D495/04 ,  C07D ,  A61K

公开(公告)号：FI944969A

公开(公告)日：1995-04-23

申请号：FI944969

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 ,  C07D209/32

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：CA2132887A1

公开(公告)日：1995-04-23

申请号：CA2132887

申请日：1994-09-21

Applicant: HOFFMANN LA ROCHE

Inventor： BOES MICHAEL ,  WICHMANN JUERGEN ,  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 general formula I wherein R1 to R4 each signify hydrogen, halogen, lower alkyl, phenyl, cycloalkyl or lower alkoxy and R2 additionally signifies lower alkoxycarbonyl, acyloxy or mesyloxy; R5 to R7 each signify hydrogen or lower alkyl; X signifies CH2CH(C6H5)-, -CH=C(C6H5)-, -YCH2-, -CH=CH- or-(CR11R12)n; R11 and R12 each signify hydrogen, phenyl, lower alkyl or halogen; n signifies 1 to 3 and Y signifies O or S, as well as pharmaceutically usable salts of basic compounds of formula I with acids. These compounds and salts are novel and are distinguished by valuable pharmacological properties. They can be used in the control or prevention of illnesses or in the improvement of health, especially in the control 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 cephalic pain or pain of a different kind, personality disorders or obsessive-compulsive disorders, social phobias or panic states, mental organic disorders, mental disorders in childhood, aggressivity, age-related memory disorders and behavioural disorders, addiction, obesity, bulimia etc.; damages of the nervous system by trauma, stroke, neurodegenerative diseases etc.; cardiovascular disorders such as hypertension, thrombosis, stroke etc.; and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

公开(公告)号：ME00593B

公开(公告)日：2015-08-31

申请号：MEP5709

申请日：2000-02-22

Applicant: HOFFMANN LA ROCHE

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

IPC: A61K31/44 ,  A61K20060101 ,  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

公开(公告)号：HU227629B1

公开(公告)日：2011-10-28

申请号：HU0000748

申请日：2000-02-21

Applicant: HOFFMANN LA ROCHE

Inventor： HUNKELER WALTER DR ,  STADLER HEINZ DR ,  GODEL THIERRY ,  GALLEY GUIDO ,  BOES MICHAEL ,  BRANCA QUIRICO DR ,  HOFFMANN TORSTEN ,  SCHNIDER PATRICK

IPC: C07D213/82 ,  A61K20060101 ,  A61K31/435 ,  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 ,  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.

公开(公告)号：HRP20080306A2

公开(公告)日：2008-11-30

申请号：HRP20080306

申请日：2008-06-27

Applicant: HOFFMANN LA ROCHE

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

IPC: C07D213/82 ,  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 ,  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.