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公开(公告)号:ES2330628T3
公开(公告)日:2009-12-14
申请号:ES03733867
申请日:2003-04-23
Applicant: AVENTIS PHARMA INC
Inventor: ALKAN SEFIK S , DINERSTEIN ROBERT J , SUBRAMANIAM ARUN , HRIB NICHOLAS J , JURCAK JOHN G
IPC: C07D209/42 , A61K31/40 , A61K31/404 , A61K31/405 , A61K31/4436 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61P11/02 , A61P11/06 , A61P17/00 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/08 , A61P43/00 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12
Abstract: Uso de un compuesto seleccionado del grupo que consiste en: éster etílico de ácido 3-(4-piridinilamino)-1H-indol-2-carboxílico, éster etílico de ácido 6-trifluorometil-3-(4-piridinilamino)-1H-indol-2-carboxílico, éster etílico de ácido 6-cloro-3-(4-piridinilamino)-1H-indol-2-carboxílico, éster etílico de ácido 5-cloro-3-(4-piridinilamino)-1H-indol-2-carboxílico, éster etílico de ácido 6-fluoro-3-(4-piridinilamino)-1H-indol-2-carboxílico, éster etílico de ácido 5-fluoro-3-(4-piridinilamino)-1H-indol-2-carboxílico, éster terc-butílico de ácido 4-fluoro-3-(4-piridinilamino)-1H-indol-2-carboxílico, éster etílico de ácido 6-fenil-3-(4-piridinilamino)-1H-indol-2-carboxílico, éster terc-butílico de ácido 3-(4-piridinilamino)-1H-indol-2-carboxílico, éster etílico de ácido 5,6-dimetoxi-3-(4-piridinilamino)-1H-indol-2-carboxílico, éster terc-butílico de ácido 3-metoxi-3-(4-piridinilamino)-1H-indol-2-carboxílico, éster etílico de ácido 3-(2-piridinilamino)-1H-indol-2-carboxílico, éster etílico de ácido 3-(pirimidin-2-ilamino)-1H-indol-2-carboxílico, éster etílico de ácido 5-fluoro-1-metil-3-(4-piridinilamino)-1H-indol-2-carboxílico, éster terc-butílico de ácido 4-fluoro-1-metil-3-(4-piridinilamino)-1H-indol-2-carboxílico, éster etílico de ácido 5-cloro-1-metil-3-(4-piridinilamino)-1H-indol-2-carboxílico, éster etílico de ácido 6-cloro-1-metil-3-(4-piridinilamino)-1H-indol-2-carboxílico, éster etílico de ácido 6-cloro-1-dietilcarbamoilmetil-3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster pentafluorofenílico de ácido 3-(4-piridinilamino)-1H-indol-2-carboxílico, éster 2-dietilamino-etílico de ácido 3-(4-piridinilamino)-1H-indol-2-carboxílico, éster 2-dimetilamino-etílico de ácido 3-(4-piridinilamino)-1H-indol-2-carboxílico, éster 2-piperidin-1-il-etílico de ácido 3-(4-piridinilamino)-1H-indol-2-carboxílico, éster (S)-1-metoxicarbonil-etílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster etoxicarbonilmetílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster 2-metoxietílico de ácido 3-(4-piridinilamino)-1H-indol-2-carboxílico, éster 3-etoxipropílico de ácido 3-(4-piridinilamino)-1H-indol-2-carboxílico, éster indan-5-ílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster dietilcarbamoilmetílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster 2-morfolin-4-il-2-oxo-etílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster 2-oxo-2-pirrolidin-1-il-etílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster 2-azetidin-1-il-2-oxo-etílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster (bencil-etil-carbamoil)-metílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster dietilcarbamoiloxi-metílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster bencilcarbamoilmetílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster piperidina-1-carboniloximetílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster morfolina-4-carboniloximetílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster 2-etoxicarbonilamino-2-oxietílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster iso-propoxicarboniloxi-metílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster 1,1,2-trimetilpropoxi-carboniloxi-metílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster ciclohexiloxi-carboniloxi-metílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster adamantan-1-iloxicarboniloximetílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster acetoximetílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster 2,2-dimetil-propioniloximetílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster pentanoiloximetílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster 2-oxo-piperidin-1-ilmetílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster (benzoil-etoxicarbonilmetil-amino)-metílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster 2-oxo-pirrolidin-1-ilmetílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster 5-metil-2-oxo-(1,3)dioxo-4-ilmetílico de ácido il 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster (fenil-(tolueno-4-sulfonil)-amino)-metílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster (bencenosulfonil-metil-amino)-metílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster (metil-(tolueno-4-sulfonil)-amino)-metílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster terc-butoxicarboniloxi-metílico de ácido 3-(piridin-4-ilamino)-1H-indol-2-carboxílico, éster etílico de ácido 3-(4-piridinilamino)-benzo(b)tiofen-2-carboxílico, sal de hidrocloruro de éster etílico de ácido 3-(4-piridinilamino)-6-trifluorometil-benzo(b)tiofen-2-carboxílico, éster etílico de ácido 6-fluoro-3-(4-piridinilamino)-benzo(b)tiofen-2-carboxílico, 3-((4-piridil)amino-N-metil)-benzo(b)tiofenil-2-carboxilato de etilo, éster etílico de ácido 3-(propil-4-piridinilamino)-benzo(b)tiofen-2-carboxílico, éster 2-dimetilamino-etílico de ácido 3-((benzoil)amino)-6-cloro-1H-indol-2-carboxílico, éster etílico de ácido 3-((benzoil)metilamino)-4,6-dicloro-1H-indol-2-carboxílico, éster etílico de ácido 3-((benzoil)bencilamino)-4,6-dicloro-1H-indol-2-carboxílico, y éster etílico de ácido 3-((fenilsulfonil)amino)-4,6-dicloro-1H-indol-2-carboxílico para la preparación de una composición farmacéutica útil en el tratamiento de alergia, asma, rinitis, dermatitis, linfomas de linfocitos B, tumores, infecciones antibacterianas, por rinovirus o por virus sincicial respiratorio (RSV).
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公开(公告)号:DE60328675D1
公开(公告)日:2009-09-17
申请号:DE60328675
申请日:2003-04-23
Applicant: AVENTIS PHARMA INC
Inventor: ALKAN SEFIK S , DINERSTEIN ROBERT J , SUBRAMANIAM ARUN , HRIB NICHOLAS J , JURCAK JOHN G
IPC: C07D209/42 , A61K31/40 , A61K31/404 , A61K31/405 , A61K31/4436 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61P11/02 , A61P11/06 , A61P17/00 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/08 , A61P43/00 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12
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公开(公告)号:DK1216250T3
公开(公告)日:2004-02-23
申请号:DK00964969
申请日:2000-09-13
Applicant: AVENTIS PHARMA INC
Inventor: FINK DAVID M , FREED BRIAN S , HRIB NICHOLAS J , KOSLEY RAYMOND W JR , LEE GEORGE E , MERRIMAN GREGORY H , RAUCKMAN BARBARA S
IPC: C07D495/04 , A61K31/4162 , A61K31/424 , A61K31/4365 , A61K31/437 , A61K31/439 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/506 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/30 , A61P43/00 , C07B53/00 , C07D498/04 , C07D519/00 , A61K31/40 , A61K31/42 , A61K31/44 , A61K31/501 , A61K31/55
Abstract: The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.
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公开(公告)号:CA2483091A1
公开(公告)日:2003-11-06
申请号:CA2483091
申请日:2003-04-23
Applicant: AVENTIS PHARMA INC
Inventor: HRIB NICHOLAS J , JURCAK JOHN G , GROSS ALEXANDRE , MUSICK KWON YON , WEINTRAUB PHILIP M , MERRIMAN GREGORY H , SABOL JEFFREY S , DHARANIPRAGADA RAMALINGA , KLEIN JOSEPH T , WHITELEY BRIAN
IPC: A61K31/40 , A61K31/404 , A61K31/405 , A61K31/4436 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61P11/02 , A61P11/06 , A61P17/00 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/08 , A61P43/00 , C07D209/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12 , C07D413/14 , C07D403/14
Abstract: This inventions discloses and claims 3-substituted amino-1H-indole-2- carboxylic acid and 3-substituted amino-benzothiophene-2-carboxylic acid derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cel l lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. It has now been found that the compounds of this invention are capable of modulating T helper (Th) cells, Th1/Th2, and thereby capable of inhibiting the transcription of interieukin- 4(IL-4) message, IL-4 release or IL-4 production.
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公开(公告)号:AT247110T
公开(公告)日:2003-08-15
申请号:AT00963370
申请日:2000-09-13
Applicant: AVENTIS PHARMA INC
Inventor: SHUTSKE GREGORY M , HENDRIX JAMES A , JURCAK JOHN G , FREED BRIAN S , HRIB NICHOLAS J , TOMER JOHN D IV , HANNA REDA G
IPC: A61K31/381 , A61K31/42 , A61K31/423 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/4453 , A61K31/4535 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/55 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/30 , C07C251/48 , C07D261/20 , C07D333/56 , C07D409/12 , C07D413/12 , C07D413/14 , C07D471/04 , C07D491/10 , C07D491/20 , C07D498/04 , C07D519/00 , C07D409/14
Abstract: The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.
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公开(公告)号:BR0014515A
公开(公告)日:2002-06-25
申请号:BR0014515
申请日:2000-09-13
Applicant: AVENTIS PHARMA INC
Inventor: FINK DAVID M , FREED BRIAN S , HRIB NICHOLAS J , KOSLEY RAYMOND W JR , LEE GEORGE E , MERRIMAN GREGORY H , RAUCKMAN BARBARA S
IPC: C07D495/04 , A61K31/4162 , A61K31/424 , A61K31/4365 , A61K31/437 , A61K31/439 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/506 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/30 , A61P43/00 , C07B53/00 , C07D498/04 , C07D519/00 , A61K31/40 , A61K31/55 , A61K31/501 , A61K31/42 , A61K31/44
Abstract: The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.
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7.
公开(公告)号:AU7479400A
公开(公告)日:2001-04-17
申请号:AU7479400
申请日:2000-09-13
Applicant: AVENTIS PHARMA INC
Inventor: SHUTSKE GREGORY M , HENDRIX JAMES A , JURCAK JOHN G , FREED BRIAN S , HRIB NICHOLAS J , IV JOHN D TOMER , HANNA REDA G
IPC: A61K31/381 , A61K31/42 , A61K31/423 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/4453 , A61K31/4535 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/55 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/30 , C07C251/48 , C07D261/20 , C07D333/56 , C07D409/12 , C07D413/12 , C07D413/14 , C07D471/04 , C07D491/10 , C07D491/20 , C07D498/04 , C07D519/00 , C07D409/14 , A61K31/38 , A61K31/47 , A61K31/44 , C07D213/61 , C07D261/00 , C07D211/00 , C07D333/00
Abstract: The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.
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8.
公开(公告)号:AU4811396A
公开(公告)日:1996-09-26
申请号:AU4811396
申请日:1996-03-14
Applicant: AVENTIS PHARMA INC
Inventor: HRIB NICHOLAS J , JURCAK JOHN G , MURTLIB ABDUL E
IPC: C07D409/04 , A61K31/38 , A61K31/495 , A61K31/496 , A61P25/18 , C07D209/00 , C07D295/00 , C07D333/00 , C07D333/66 , C07D409/12 , C07D409/14
Abstract: This invention relates to compounds of the formula I wherein X is hydrogen, halogen, hydroxy, (C1-C6)alkoxy, amino or trifluoromethyl; and Y is -CN or -NR R ; where l is an integer of 1 or 2; m is an integer of 0, 1 or 2; n is an integer of 2, 3 or 4, except when Y is CN, in which case n can also be 1; R is hydrogen, (C1-C6)alkyl or (C1-C6)alkylcarbonyl; R is hydrogen, (C1-C10)alkylcarbonyl, (C3-C12)cycloalkylcarbonyl, hydroxy-(C1-C6)alkylcarbonyl, phenylcarbonyl, thienylcarbonyl or benzothienylcarbonyl; or R and R together with nitrogen atom to which they are attached form the ring where A is C = O or CH2; and B is C = O, CHOH, CH2 or CH2CH2; and Z is hydrogen, halogen, hydroxy, (C1-C6)alkoxy, amino or trifluoro; and pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions thereof and their use for the treatment of psychoses.
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9.
公开(公告)号:HRP20020219A2
公开(公告)日:2004-04-30
申请号:HRP20020219
申请日:2002-03-12
Applicant: AVENTIS PHARMA INC
Inventor: SHUTSKE GREGORY M , HENDRIX JAMES A , JURCAK JOHN G , FREED BRIAN S , HRIB NICHOLAS J , IV JOHN D TOMER , HANNA REDA G
IPC: A61K31/381 , A61K31/42 , A61K31/423 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/4453 , A61K31/4535 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/55 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/30 , C07C251/48 , C07D261/20 , C07D333/56 , C07D409/12 , C07D413/12 , C07D413/14 , C07D471/04 , C07D491/10 , C07D491/20 , C07D498/04 , C07D519/00 , C07D409/14 , A61K31/38 , A61K31/47 , A61K31/44 , C07D213/61
Abstract: The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.
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公开(公告)号:DK1216244T3
公开(公告)日:2003-11-17
申请号:DK00963370
申请日:2000-09-13
Applicant: AVENTIS PHARMA INC
Inventor: SHUTSKE GREGORY M , HENDRIX JAMES A , JURCAK JOHN G , FREED BRIAN S , HRIB NICHOLAS J , TOMER JOHN D IV , HANNA REDA G
IPC: A61K31/381 , A61K31/42 , A61K31/423 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/4453 , A61K31/4535 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/55 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/30 , C07C251/48 , C07D261/20 , C07D333/56 , C07D409/12 , C07D413/12 , C07D413/14 , C07D471/04 , C07D491/10 , C07D491/20 , C07D498/04 , C07D519/00 , A61K31/38 , A61K31/44 , A61K31/47 , C07D213/61 , C07D409/14
Abstract: The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.
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