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公开(公告)号:AU2003225131A1
公开(公告)日:2003-11-10
申请号:AU2003225131
申请日:2003-04-23
Applicant: AVENTIS PHARMA INC
Inventor: JURCAK JOHN G , GROSS ALEXANDRE , WHITELEY BRIAN , MUSICK KWON YON , KLEIN JOSEPH T , MERRIMAN GREGORY H , WEINTRAUB PHILIP M , SABOL JEFFREY S , DHARANIPRAGADA RAMALINGA , HRIB NICHOLAS J
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 , C07D417/14
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公开(公告)号:ES2342083T3
公开(公告)日:2010-07-01
申请号:ES05740005
申请日:2005-04-27
Applicant: AVENTIS PHARMA INC
Inventor: SHUTSKE GREGORY , HARRIS KEITH J , BORDEAU KENNETH J , ANGELASTRO MICHAEL R , JOHN STANLY , KLEIN JOSEPH T
IPC: C07D405/04 , A61K31/352 , A61P25/00 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
Abstract: Un compuesto según la fórmula I **(Ver fórmula)** en la que R1 se selecciona del grupo que consiste en hidrógeno, fenoxicarbonilo, alcoxi(C1-6)-carbonilo, benciloxicarbonilo, naftiloxicarbonilo, fenilcarbamoílo, fenilcarbamoil-alquilo(C1-6), naftilcarbamoil-alquilo(C1-6), bifenilcarbamoílo, fenil-alquil(C1-6)-carbamoílo, N-fenil-N-alquil(C1-6)-carbamoílo, alquil(C1-6)- y dialquil(C1-6)-carbamoílo, alquenil(C2-6)- y dialquenil(C2-6)-carbamoílo, difenilcarbamoílo, heteroarilcarbamoil-alquilo(C1-6), fenilcarbonilo, bifenilcarbonilo, alquil(C1-6)-carbonilo, morfolinilcarbonilo, piperidinilcarbonilo, pirrolidinilcarbonilo, fenotiazinilcarbonilo, fenilsulfonilo, difenilsulfonilo, naftilsulfonilo, alquilsulfonilo C1-10, naftil-alquil(C1-6)-sulfonilo, perfluoroalquilsulfonilo C1-6, difenil-alquil(C1-6)-sulfonilo, bencensulfonilo, dialquil(C1-6)-aminosulfonilo, difenil-alquilo(C1-6), bencilo, fenil-alquilo(C2-6), naftil-alquilo(C1-6); cicloalquil(C3-6)-alquilo(C1-6), fenil-alquenilo(C1-6), heteroaril-alquilo(C1-6), α-carboxibencilo, fenilcarbonil-alquilo(C1-6), hidroxialquilo(C1-6), bifenil-alquilo(C1-6), alquilo C1-6, fenoxifenil-alquilo(C1-6), fenilurea-alquilo(C1-6), indanilo, en los que el bencilo y fenilo están opcionalmente sustituidos con uno o dos sustituyentes independientemente seleccionados cada uno del grupo que consiste en alquilo C1-6, perfluoroalquilo C1-6, halógeno, hidroxi, alcoxi C1-6 y nitro, y en los que heteroarilo es tiofenilo, benzotiofenilo, furanilo, benzofuranilo, tetrahidroquinolilo, tetrahidroisoquinolilo, indolilo, imidazolilo, bencimidazolilo, piridinilo, isotiazolilo, bencisotiazolilo, isoxazolilo, bencisoxazolilo, isoquinolilo, o quinolilo, en los que el heteroarilo está opcionalmente sustituido con uno o dos sustituyentes independientemente seleccionados del grupo alquilo C1-6, halógeno, hidroxi, bencilo y alcoxi C1-6,** **(Ver fórmula)** en la que R es hidrógeno o bencilo; Y se selecciona del grupo que consiste en hidrógeno, alquilo C1-6, perfluoroalquilo C1-6, halógeno, hidroxi, alcoxi C1-6 y nitro; R2 y R3 son iguales o diferentes y se seleccionan independientemente del grupo que consiste en hidrógeno, alquilo C1-6, alquil(C1-6)-carbonilo, formilo, alquenilo C2-6, cicloalquil(C3-6)-alquilo(C1-6), y R2, R3 considerados juntos pueden formar un anillo de 2-5 átomos de carbono; R4 se selecciona del grupo que consiste en hidrógeno, alquilo C1-4 y alquil(C1-6)-carbonilo; X se selecciona del grupo que consiste en hidrógeno y alquilo C1-6; y n es un número entero 1, 2 ó 3; un estereoisómero o una de sus sales farmacéuticamente aceptables.
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公开(公告)号:DK1749001T3
公开(公告)日:2010-06-28
申请号:DK05740005
申请日:2005-04-27
Applicant: AVENTIS PHARMA INC
Inventor: SHUTSKE GREGORY , HARRIS KEITH J , BORDEAU KENNETH J , ANGELASTRO MICHAEL R , KLEIN JOSEPH T , LU JINQI , BOMONT CATHERINE , JOHN STANLY
IPC: C07D405/04 , A61K31/352 , A61P25/00 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
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公开(公告)号:DE602005019719D1
公开(公告)日:2010-04-15
申请号:DE602005019719
申请日:2005-04-27
Applicant: AVENTIS PHARMA INC
Inventor: SHUTSKE GREGORY , HARRIS KEITH J , BORDEAU KENNETH J , ANGELASTRO MICHAEL R , JOHN STANLY , KLEIN JOSEPH T , LU JINQI , BOMONT CATHERINE
IPC: C07D405/04 , A61K31/352 , A61P25/00 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
Abstract: The present invention provides compounds of formula I: a stereoisomer or a pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, X and n are defined as defined herein. Additionally, a method for treating dopamine-related neurological disorders selected form the group consisting of neurological, psychological, cardiovascular, cognitive or attention disorders, substance abuse and addictive behavior, or a combination thereof, comprising administering to a patient in need of such treatment a therapeutically effective amount of compounds of formula I.
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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:PT1749001E
公开(公告)日:2010-05-31
申请号:PT05740005
申请日:2005-04-27
Applicant: AVENTIS PHARMA INC
Inventor: BORDEAU KENNETH J , SHUTSKE GREGORY , HARRIS KEITH J , ANGELASTRO MICHAEL R , JOHN STANLY , KLEIN JOSEPH T , LU JINQI , BOMONT CATHERINE
IPC: C07D405/04 , A61K31/352 , A61P25/00 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
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公开(公告)号:DE60313769T2
公开(公告)日:2008-03-06
申请号:DE60313769
申请日:2003-04-23
Applicant: AVENTIS PHARMA INC
Inventor: MERRIMAN GREGORY H , WEINTRAUB PHILIP M , SABOL JEFFREY S , DHARANIPRAGADA RAMALINGA , HRIB NICHOLAS J , JURCAK JOHN G , GROSS ALEXANDRE , WHITELEY BRIAN , MUSICK KWON YON , KLEIN JOSEPH T
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 , C07D417/14
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公开(公告)号:DE60313769D1
公开(公告)日:2007-06-21
申请号:DE60313769
申请日:2003-04-23
Applicant: AVENTIS PHARMA INC
Inventor: MERRIMAN GREGORY H , WEINTRAUB PHILIP M , SABOL JEFFREY S , DHARANIPRAGADA RAMALINGA , HRIB NICHOLAS J , JURCAK JOHN G , GROSS ALEXANDRE , WHITELEY BRIAN , MUSICK KWON YON , KLEIN JOSEPH T
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 , C07D417/14
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9.
公开(公告)号:AU6000390A
公开(公告)日:1991-02-07
申请号:AU6000390
申请日:1990-08-01
Applicant: AVENTIS PHARMA INC
Inventor: EFFLAND RICHARD C , WETTLAUFER DAVID G , KLEIN JOSEPH T
IPC: A61K31/44 , A61K31/4427 , A61K31/4433 , A61P25/04 , A61P25/28 , C07D401/12 , C07D401/14 , C07D409/14 , C07D471/10
Abstract: This invention relates to 2,3-dihydro-1-(pyridinylamino)-indoles of the formula wherein R1 is hydrogen, loweralkyl, aryl, arylloweralkyl, alkenyl, alkynyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl; R2 and R3 are independently hydrogen, loweralkyl, aryl, arylloweralkyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl; or R2 and R3 together form a cycloalkane ring of 4 to 6 carbons or a spiro-fused aryl or heteroaryl cycloalkane; X and Y are independently hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; m and n are independently integers of 1 to 3, the pharmaceutically acceptable acid addition salts thereof and where appropriate, the optical, geometrical and stereoisomers and racemic mixtures thereof. The compounds of this invention are useful as analgesics, anticonvulsants, for enhancing memory and for the treatment of Alzheimer's disease.
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