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92. 发明专利

ES2297458T3 PIPERAZINA CON GRUPO FENILO OR-SUSTITUIDO Y SU EMPLEO COMO INHIBIDORES DE GLYTI. 未知
公开(公告)号：ES2297458T3
公开(公告)日：2008-05-01
申请号：ES04763703
申请日：2004-08-02
申请人： HOFFMANN LA ROCHE
发明人： JOLIDON SYNESE , NARQUIZIAN ROBERT , NETTEKOVEN MATTHIAS HEINRICH , NORCROSS ROGER DAVID , PINARD EMMANUEL , STALDER HENRI
IPC分类号： C07D295/192 , A61K31/495 , A61K31/497 , A61P25/28 , C07D213/74 , C07D213/85 , C07D239/42 , C07D241/20 , C07D251/42 , C07D257/04 , C07D263/32 , C07D271/06 , C07D309/12
摘要： Compuestos de fórmula general I en donde Ar es arilo sustituido o sin sustituir elegido del grupo constituido por fenilo, bencilo, naftilo e indanilo o o heteroarilo de 6 miembros, que contiene uno, dos o tres átomos de nitrógeno, y en donde los grupos arilo y heteroarilo pueden estar sustituidos por uno o más sustituyentes seleccionados del grupo consistente de hidroxilo, halógeno, NO2, CN, (C1-C6)-alquilo, (C1-C6)-alquilo sustituido por halógeno, (C1-C6)-alquilo sustituido por hidroxilo, (CH2)n-(C1-C6)-alcoxilo, (C1-C6)-alcoxilo sustituido por halógeno, NR7R8, C(O)R9, SO2R10, -C(CH3)=NOR7, o por un heterociclo aromático de 5 miembros, que contiene 1-4 heteroátomos, seleccionados de N y O, que está opcionalmente sustituido por (C1-C6)-alquilo; R1 es hidrógeno o (C1-C6)-alquilo; R2 es hidrógeno, (C1-C6)-alquilo, (C2-C6)-alquenilo, (C1-C6)-alquilo sustituido por halógeno, (C1-C6)-alquilo sustituido por hidroxilo, (CH2)n-(C3-C7)-cicloalquilo opcionalmente sustituido por (C1-C6)-alcoxilo o porhalógeno, o es CH(CH3)-(C3-C7)-cicloalquilo, (CH2)n+1-C(O)-R9, (CH2)n+1-CN, biciclo[2, 2, 1]heptilo, (CH2)n+1-O-(C1-C6)-alquilo, (CH2)n-heterocicloalquilo, (CH2)n-arilo ó heteroarilo (CH2)n de 5 ó 6 miembros que contiene uno, dos o tres heteroátomos, seleccionados del grupo consistente de oxígeno, azufre o nitrógeno en donde arilo, heterocicloalquilo y heteroarilo están sin sustituir o sustituidos por uno o más sustituyentes seleccionados del grupo consistente de hidroxilo, halógeno, (C1-C6)-alquilo o (C1-C6)-alcoxilo; R3, R4 y R6 independientemente el uno del otro son hidrógeno, hidroxilo, halógeno, (C1-C6)-alquilo, (C1-C6)-alcoxilo o O-(C3-C6)-cicloalquilo; R5 es NO2, CN, C(O)R9 o SO2R10; R7 y R8 independientemente el uno del otro son hidrógeno o (C1-C6)-alquilo; R9 es hidrógeno, (C1-C6)-alquilo, (C1-C6)-alcoxilo ó NR7R8; R10 es (C1-C6)-alquilo opcionalmente sustituido por halógeno, (CH2)n-(C3-C6)-cicloalquilo, (CH2)n-(C3-C6)-alcoxilo, (CH2)n-heterocicloalquilo o NR7R8; n es 0, 1, ó 2; ya sales farmacéuticamente aceptables de adición ácida de los mismos, con la condición que 1-[5-(aminosulfonil)-2-metoxibenzoil]-4-(3-clorofenil)-piperazina, 1-[5-(aminosulfonil)-2-metoxibenzoil]-4-(4-fluorofenil)-piperazina, 1-[5-(aminosulfonil)-2-metoxibenzoil]-4-[3-(trifluoro-metil)fenil]-piperazina, 4-(3-amino-4-nitrofenil)-1-[4-(dimetilamino)-2-metoxi-5-nitrobenzoil]-2-metil-piperazina, 1-[4-(dimetilamino)-2-metoxi-5-nitrobenzoil]-2-metil-4-(4-nitrofenil)-piperazina, 4-[4-(dimetilamino)-2-metoxi-5-nitrobenzoil]-2-metil-1-(4-nitrofenil)-piperazina, 1-(2-cloro-4-nitrofenil)-4-[4-(dimetilamino)-2-metoxi-5-nitrobenzoil]-piperazina, 1-[4-(dimetilamino)-2-metoxi-5-nitrobenzoil]-4-(2, 4-dinitrofenil)-2-metil-piperazina, 1-(4-cloro-2-nitrofenil)-4-[4-(dimetilamino)-2-metoxi-5-nitrobenzoil]-piperazina 4-[4-(dimetilamino)-2-metoxi-5-nitrobenzoil]-1-(2, 4-dinitrofenil)-2-metil-piperazina y 1-[2-benciloxi-5-formil)benzoil]-4-fenilpiperacina están excluidos.

93. 发明专利

AU2007287645A1 DI-aromatic substituted amides as inhibitors for GlyT1 未知
公开(公告)号：AU2007287645A1
公开(公告)日：2008-02-28
申请号：AU2007287645
申请日：2007-08-13
申请人： HOFFMANN LA ROCHE
发明人： NARQUIZIAN ROBERT , JOLIDON SYNESE , PINARD EMMANUEL
IPC分类号： C07C237/22 , A61K31/16 , C07C255/57 , C07C271/22 , C07C275/24 , C07D213/40 , C07D213/81 , C07D261/18 , C07D275/02 , C07D279/02 , C07D307/79 , C07D333/20 , C07D333/38 , C07D333/44 , C07D335/18
摘要： The present invention relates to compounds of formula I wherein R1, R2, R3, R4, R5, X, and n are as defined herein and the dotted line denotes an optional bond and pharmaceutically acceptable acid addition salts thereof. The compounds are useful in the treatment of neurological and neuropsychiatric disorders.

94. 发明专利

AT382611T 未知
公开(公告)号：AT382611T
公开(公告)日：2008-01-15
申请号：AT04763703
申请日：2004-08-02
申请人： HOFFMANN LA ROCHE
发明人： JOLIDON SYNESE , NARQUIZIAN ROBERT , NETTEKOVEN MATTHIAS , NORCROSS ROGER , PINARD EMMANUEL , STALDER HENRI
IPC分类号： C07D295/192 , A61K31/495 , A61K31/497 , A61P25/28 , C07D213/74 , C07D213/85 , C07D239/42 , C07D241/20 , C07D251/42 , C07D257/04 , C07D263/32 , C07D271/06 , C07D309/12
摘要： The invention relates to compounds of formula wherein the substituents are described herein. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such as psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.

95. 发明专利

MY133332A PYRROLIDONE DERIVATIVES AS MAOB INHIBITORS 未知
公开(公告)号：MY133332A
公开(公告)日：2007-11-30
申请号：MYPI20033558
申请日：2003-09-18
申请人： HOFFMANN LA ROCHE
发明人： IDING HANS , JOLIDON SYNESE , KRUMMENACHER DANIELA , SARMIENTO ROSA MARIA RODRIGUEZ , THOMAS ANDREW WILLIAM , WIRZ BEAT , WOSTL WOLFGANG , WYLER RENE
IPC分类号： A61K31/40 , C07D207/26 , A61K31/4015 , A61K31/44 , A61P25/16 , A61P25/28 , C07D207/273 , C07D207/277 , C07D401/04 , C07D401/06
摘要： RACEMIC OR ENANTIOMERICALLY PURE 4-PYRROLIDINO DERIVATIVES, PROCESSES FOR THEIR PEREPARATION, PHARMACEUTICAL COMPOSITIONS COMPRISING SAID DERIVATIVES, AND THEIR USE IN THE PREVENTION AND TREATMENT OF A DISEASE WHICH IS MEDIATED BY A MONOAMINE OXIDASE B INHIBITOR, IN PARTICULAR ALZHEIMER'S DISEASE AND SENILE DEMENTIA.

96. 发明专利

AT378339T 未知
公开(公告)号：AT378339T
公开(公告)日：2007-11-15
申请号：AT04804425
申请日：2004-12-30
申请人： HOFFMANN LA ROCHE
发明人： JOLIDON SYNESE , PINARD EMMANUEL , THOMAS ANDREW
IPC分类号： C07D471/10 , A61K31/435 , A61P25/00
摘要： The present invention relates to compounds of formula wherein A-B, R 1 , R 2 , R 3 , R 4 , and n are as defined herein; and to pharmaceutically acceptable salts thereof. The compounds of formula I may be used in the treatment of neurological and neuropsychiatric disorders.

97. 发明专利

TNSN06042A1 PIPERAZINE WITH OR-SUBSTITUTED PHENYL GROUP AND THEIR USE AS GLYT 1 INHIBITORS 未知
公开(公告)号：TNSN06042A1
公开(公告)日：2007-10-03
申请号：TNSN06042
申请日：2006-02-03
申请人： HOFFMANN LA ROCHE
发明人： JOLIDON SYNESE , NARQUIZIAN ROBERT , PINARD EMMANUEL , NETTEKOVEN MATTHIAS HEINRICH , NORCROSS ROGER DAVID , STALDER HENRI
IPC分类号： A61K31/497 , A61K31/495 , A61P25/28 , C07D213/74 , C07D213/85 , C07D239/42 , C07D241/20 , C07D251/42 , C07D257/04 , C07D263/32 , C07D271/06 , C07D295/192 , C07D309/12
摘要： The invention relates to compounds of formula (I) wherein the substituents are described in claim 1. The compounds may be used in the treatment of illnesses based on the glycine up-take inhibitor, such as psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive process are impaired, such as attention deficit disorders or Alzheimer's disease.

98. 发明专利

CA2642859A1 4-AMINO-1,5-SUBSTITUTED 1,5-DIHYDRO-IMIDAZOL-2-ONES 未知
公开(公告)号：CA2642859A1
公开(公告)日：2007-09-13
申请号：CA2642859
申请日：2007-02-27
申请人： HOFFMANN LA ROCHE
发明人： NORCROSS ROGER , PINARD EMMANUEL , NARQUIZIAN ROBERT , JOLIDON SYNESE
IPC分类号： C07D233/92 , A61K31/4025 , A61P25/18
摘要： The present invention relates to compounds of formula I wherein R1, R2, R3, and R4 are as defined herein and to pharmaceutically acceptable acid addition salts thereof. Compounds of formula I or their tautomeric forms are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors. Such compounds are useful for the treatment of schizophrenia.

99. 发明专利

MX2007008189A DERIVADOS DE [4-(HETEROARIL)PIPERAZIN-1-IL]-(FENILO 2,5-SUSTITUIDO) METANONA COMO INHIBIDORES DEL TRANSPORTADOR DE GLICINA 1(GLYT-1) PARA EL TRATAMIENTO DE TRASTORNOS NEUROLOGICOS Y NEUROPSIQUIATRICOS. 未知
公开(公告)号：MX2007008189A
公开(公告)日：2007-08-07
申请号：MX2007008189
申请日：2005-12-28
申请人： HOFFMANN LA ROCHE
发明人： PINARD EMMANUEL , JOLIDON SYNESE , NORCROSS ROGER DAVID , NARQUIZIAN ROBERT
IPC分类号： A61K31/427 , A61K31/433 , A61P25/28 , C07D277/42 , C07D277/56 , C07D285/08 , C07D285/12 , C07D417/12
摘要： La presente invencion se refiere a compuestos de la formula general en donde, R1 es -OR1??, -SR1?? o es un grupo heterocicloalquilo; R1?? es alquilo inferior, alquilo inferior sustituido por halogeno o es -(CH2)n-cicloalquilo; R2 es -S(O)2-alquilo inferior, -S(O)2NH-alquilo inferior, NO2 o CN; X2 es CR3?? o N; R3/R3?? con independencia entre si son hidrogeno, halogeno, alquilo inferior, CN, NO2, -S(O)2-alquilo inferior, -S(O)2-piridin-2-, -3- o -4-ilo, fenilo, opcionalmente sustituido por uno o dos sustituyentes seleccionados del grupo formado pro NO2 o halogeno, o es alquilo inferior sustituido por halogeno o es -C(O)-alquilo inferior; n es 0, 1 o 2; y a sales de adicion de acido farmaceuticamente aceptables de los mismos. Se ha encontrado que los compuestos de la formula general I son buenos inhibidores del transportador de glicina 1 (GlyT-1). Pueden utilizarse para el tratamiento de la esquizofrenia.

100. 发明专利

NO20073330L 未知
公开(公告)号：NO20073330L
公开(公告)日：2007-07-20
申请号：NO20073330
申请日：2007-06-29
申请人： HOFFMANN LA ROCHE
发明人： PINARD EMMANUEL , JOLIDON SYNESE , NORCROSS ROGER DAVID , NARQUIZIAN ROBERT
IPC分类号： C07D295/18 , A61K31/495 , A61K31/496 , A61K31/506 , A61P25/28 , C07D213/74 , C07D239/42
摘要： The present invention relates to compounds of formula I wherein R 1 , R 2 , R 3 , X, X 1 , and n are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. These compounds are good inhibitors of the glycine transporter 1 (GlyT-1) for the treatment CNS disorders, such as schizophrenia, cognitive impairment, and Alzheimer's disease.

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