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91. 发明专利

AU2005212867A1 Derivatives of 1,4-diazabicyclo[3.2.1]octanecarboxamide, preparation method thereof and use of same in therapeutics 未知
公开(公告)号：AU2005212867A1
公开(公告)日：2005-08-25
申请号：AU2005212867
申请日：2005-01-07
申请人： SANOFI AVENTIS
发明人： GALLI FREDERIC , LECLERC ODILE , LOCHEAD ALISTAIR
IPC分类号： C07D487/08 , C07D519/00
摘要： 4-heterocyclylcarbonyl-1,4-diazacyclo-octane derivatives (I), as individual or mixed enantiomers, bases, solvates and acid addition salts are new. 4-heterocyclylcarbonyl-1,4-diazacyclo-octane derivatives of formula (I), as individual or mixed enantiomers, bases, solvates and acid addition salts are new. X : N or CR 2; P, Q, R and W : N or CR 3; R 1 and R 21-6C alkyl; R 3hydrogen, halo, 1-6C alkyl or alkoxy, nitro, amino, trifluoromethyl, cyano, NR 4R 5, NR 4COR 5, NR 4CONR 5R 6, NR 4COOR 5, NR 4SO 2NR 5R 6, OR 5, OCOR 5, OCOOR 5, OCO-ONR 4R 5. OCOSR 5, COOR 5, COR 5, CONR 4R 5, SR 5, SOR 5, SO 2R 5, SO 2NR 4R 6, or phenyl (optionally substituted by any of the groups indicated for R 3), or R 3 is any of a wide range of heterocyclic groups (het1); R 4, R 5 and R 6halo, 1-6C alkyl, 2-6C alkenyl or alkynyl, 3-8C cycloalkyl, 3-8C cycloalkyl(1-3C)alkyl, 4-8C cycloalkenyl or phenyl, and RNR 4R 5 or NR 5R 6 may complete a heterocycle (het2). The full definitions are given in the DEFINITIONS (Full Definitions) Field. [Image] ACTIVITY : Nootropic; Neuroprotective; Neuroleptic; Antiparkinsonian; Anticonvulsant; Tranquilizer; Antidepressant; Cardiant; Antiulcer; Antismoking. MECHANISM OF ACTION : (I) are ligands for nicotinic receptors, with high selectivity for receptors that include the alpha 7 subunit. The compound 3-(1,4-diazabicyclo[3,2,1]oct-4-yl-carbonyl)-6-methyl-1H-pyrazolo[3,4-b]pyridine hydrobromide had IC 50 for inhibition of binding of tritium-labeled alpha -bungarotoxin to nicotinic receptors that contained the alpha 7 subunit of 0.056 mu M.

92. 发明专利

AR043486A1 DERIVADOS DE 2-(DIAZA-BICICLO-ALQUIL)-PIRIMIDONA 未知
公开(公告)号：AR043486A1
公开(公告)日：2005-08-03
申请号：ARP040100695
申请日：2004-03-05
申请人： SANOFI AVENTIS , MITSUBISHI PHARMA CORP
发明人： LOCHEAD ALISTAIR , SAADY MOURAD , SLOWINSKI FRANCK , YAICHE PHILIPPE
IPC分类号： A61K31/4995 , A61P25/28 , C07D471/08 , C07D487/08 , A61K31/4495 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/24 , A61P9/00 , A61P317/17 , A61P3/04 , A61P3/10 , A61P35/00 , C07D221/00
摘要： La presente se refiere a un derivado de 2-(diaza-biciclo-alquil)-pirimidona representado por la fórmula (1) o una sal del mismo: donde R1 representa un átomo de H, un grupo alquilo C1-6, o un átomo de halógeno; R2 representa un átomo de H, un grupo alquilo C1-6 opcionalmente sustituido, un grupo alquilo perhalogenado C1-2, un grupo bencilo, un grupo fenetilo, un grupo benciloxicarbonilo, un grupo alcoxi carbonilo C1-4, un anillo de benceno, un anillo de naftaleno, un anillo de quinolina, un anillo de ftalazina, un anillo de 5,6,7,8-tetrahidronaftaleno, un anillo de piridina, un anillo de indol, un anillo de pirrol, un anillo de tiofeno, un grupo bencenosulfonilo, un grupo benzoilo, un anillo de piridazina, un anillo de furano o un anillo de imidazol; el grupo bencilo, el grupo fenetilo, el grupo benciloxicarbonilo, el grupo bencenosulfonilo, el grupo benzoilo y los anillos están opcionalmente sustituidos; R3 representa un anillo de 2, 4 o 5-pirimidina o un anillo de 2, 3 o 4-piridina, y los anillos están opcionalmente sustituido; R4 representa un grupo alquilo C14 y n representa 1 o 2. La presente también se refiere a un medicamento que comprende dicho derivado o una sal del mismo como ingrediente activo, que se utiliza para el tratamiento preventivo y/o terapéutico e una enfermedad neurodegenerativa causada por la actividad anormal de la GSK3beta, como ser enfermedad de Alzheimer.

93. 发明专利

DE60103395T2 未知
公开(公告)号：DE60103395T2
公开(公告)日：2005-06-16
申请号：DE60103395
申请日：2001-05-29
申请人： SANOFI AVENTIS SA
发明人： GALLI FREDERIC , LOCHEAD ALISTAIR , SAMSON AXELLE
IPC分类号： A61K31/551 , A61P9/10 , A61P25/00 , A61P25/16 , A61P25/28 , C07D471/08 , A61K31/55
摘要： Compound corresponding to the general formula (I) in which X represents an oxygen or sulphur atom or an NH group and R 1 , R 2 , R 3 and R 4 each represent a hydrogen or halogen atom or a nitro, amino, trifluoromethyl, trifluoroalkoxy, cyano, hydroxyl, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy or phenyl group. Application in therapeutics.

94. 发明专利

DE60203197D1 未知
公开(公告)号：DE60203197D1
公开(公告)日：2005-04-14
申请号：DE60203197
申请日：2002-11-21
申请人： SANOFI AVENTIS SA
发明人： GALLI FREDERIC , LECLERC ODILE , LOCHEAD ALISTAIR
IPC分类号： A61K31/551 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , A61P43/00 , C07D471/08 , A61K31/55
摘要： 4-(5-Substituted-1,2,4-oxadiazol-3-yl)-1,4-diaza-bicyclo(3.2.2)nonane derivatives (I) are new. Oxadiazolyl-diazabicyclononane derivatives of formula (I) and their acid addition salts are new. R = 3-6C cycloalkyl; phenyl (optionally substituted by one or more of halo, 1-6C alkyl, 1-6C alkoxy, NO2, NH2, di-(1-3C alkyl)-amino, OCF3, CF3, CN, OH or OCH2O); or piperidino, morpholino, pyrrolidino, azetidino, azepin-1-yl, pyridinyl, thienyl, pyrazinyl, furyl, benzofuranyl, benzothienyl, indolyl, pyrimidinyl, piperazinyl, isoxazolyl, phenoxazinyl, dibenzofuranyl, dibenzothienyl, pyrrolyl or naphthyl (all optionally substituted by one or more of halo, 1-6C alkyl, 1-6C alkoxy, OCF3, CF3, NO2, CN, OH, NH2, di-(1-3C alkyl)-amino or 3-8C cycloalkylamino).

95. 发明专利

DE60104130T2 未知
公开(公告)号：DE60104130T2
公开(公告)日：2005-03-10
申请号：DE60104130
申请日：2001-08-31
申请人： SANOFI AVENTIS
发明人： LOCHEAD ALISTAIR , MARGUERIE SEVERINE , SAADY MOURAD , YAICHE PHILIPPE
IPC分类号： A61K31/519 , A61P3/04 , A61P3/10 , A61P17/14 , A61P25/00 , A61P25/02 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/06 , A61P35/00 , A61P43/00 , C07D487/04
摘要： The invention relates to a imidazoÄ1,2-aÜpyrimidone derivative represented by formula (I) or a salt thereof: wherein: X represents a bond, a double bond, a triple bond, a methylene group optionally substituted by one or two groups selected from a C1-6 alkyl group, a hydroxy group and a C1-4 alcoxy group; a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted by a C1-6 alkyl group; R1 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or a halogen atom; R2 represents a C1-6 alkyl group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a benzyl group, a phenyl ring, a pyridyl ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring, the benzyl group and the rings being optionally substituted by 1 to 3 substituents selected from a C1-6 alkyl group, a halogen atom, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a hydroxyl group, a C1-4 alkoxy group, a nitro, a cyano, an amino, a C1-6 monoalkylamino group or a C2-10 dialkylamino group; and n represents 0 to 3. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3 beta .

96. 发明专利

SI1315731T1 2-PYRIDINYL-6,7,8,9-TETRAHYDROPYRIMIDO(1,2-A)PYRIMIDIN-4-ONE AND 7-PYRIDINYL-2,3-DIHYDROIMIDAZO(1,2-A)PYRIMIDIN-5(1H)ONE DERIVATIVES 未知
公开(公告)号：SI1315731T1
公开(公告)日：2005-02-28
申请号：SI200130158
申请日：2001-08-31
申请人： SANOFI AVENTIS , MITSUBISHI PHARMA CORP
发明人： ALMARIO GARCIA ANTONIO , GALLET THIERRY , LI ADRIEN TAK , LOCHEAD ALISTAIR , MARGUERIE SEVERINE , NEDELEC ALAIN , SAADY MOURAD , YAICHE PHILIPPE
IPC分类号： A61K31/519 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P17/14 , A61P23/02 , A61P25/00 , A61P25/02 , A61P25/16 , A61P25/24 , A61P25/28 , A61P27/06 , A61P35/00 , A61P35/02 , C07D487/04
摘要： The invention relates to therapeutic uses of a pyrimidone derivative represented by formula (I) or a salt thereof: Wherein X, Y, R1, R2, m and n are as defined herein. Specifically, a medicament comprising the said derivative or a salt thereof as an active ingredient is used for preventive and/or therapeutic treatment of a neurodegenerative diseases caused by abnormal activity of GSK3beta such as Alzheimer's disease.

97. 发明专利

SI1315730T1 1-(ALKYL), 1-((HETEROARYL)ALKYL) AND 1-((ARYL)ALKYL)-7-PYRIDINYL-IMIDAZO(1,2-A)PYRIMIDIN-5(1H)-ONE DERIVATIVES 未知
公开(公告)号：SI1315730T1
公开(公告)日：2005-02-28
申请号：SI200130171
申请日：2001-08-31
申请人： SANOFI AVENTIS , MITSUBISHI PHARMA CORP
发明人： LOCHEAD ALISTAIR , MARGUERIE SEVERINE , SAADY MOURAD , YAICHE PHILIPPE
IPC分类号： A61K31/519 , A61P3/04 , A61P3/10 , A61P17/14 , A61P25/00 , A61P25/02 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/06 , A61P35/00 , A61P43/00 , C07D487/04
摘要： The invention relates to a imidazoÄ1,2-aÜpyrimidone derivative represented by formula (I) or a salt thereof: wherein: X represents a bond, a double bond, a triple bond, a methylene group optionally substituted by one or two groups selected from a C1-6 alkyl group, a hydroxy group and a C1-4 alcoxy group; a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted by a C1-6 alkyl group; R1 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or a halogen atom; R2 represents a C1-6 alkyl group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a benzyl group, a phenyl ring, a pyridyl ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring, the benzyl group and the rings being optionally substituted by 1 to 3 substituents selected from a C1-6 alkyl group, a halogen atom, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a hydroxyl group, a C1-4 alkoxy group, a nitro, a cyano, an amino, a C1-6 monoalkylamino group or a C2-10 dialkylamino group; and n represents 0 to 3. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3 beta .

98. 发明专利

AR038620A1 DERIVADOS DE 1-(ALQUIL), 1-((HETEROARIL)ALQUIL) Y 1-((ARIL) ALQUIL)-7-(PIRIMIDIN-4-IL)-IMIDAZO(1,2-A)PIRIMIDIN-5(1H)-ONA 未知
公开(公告)号：AR038620A1
公开(公告)日：2005-01-19
申请号：ARP030100658
申请日：2003-02-28
申请人： SANOFI AVENTIS , MITSUBISHI PHARMA CORP
发明人： SAADY MOURAD , YAICHE PHILIPPE , LOCHEAD ALISTAIR
IPC分类号： A61K31/437 , A61K31/519 , A61P3/04 , A61P3/10 , A61P9/10 , A61P17/14 , A61P25/02 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P27/06 , A61P35/00 , C07D487/04 , C07D239/00 , C07D235/00
摘要： Un derivado de imidazo[1,2-a]pirimidona representado por la fórmula (1) ó una sal del mismo, donde: X representa un enlace, un grupo etenileno, un grupo etinileno, un grupo metileno opcionalmente sustituido, un grupo carbonilo, un átomo de oxígeno, un átomo de azufre, un grupo sulfonilo, un grupo sulfóxido ó un átomo de nitrógeno opcionalmente sustituido; R1 representa un anillo de 2, 4 ó 5-pirimidinilo opcionalmente sustituido; R2 representa un grupo alquilo C1-6, un grupo alquilo perhalogenado C1-2, un grupo alquilo halogenado C1-3, un grupo bencilo, un anillo de benceno, un anillo de naftaleno, un anillo de 5, 6, 7, 8-tetrahidronaftaleno, un anillo de piridina, un anillo de indol, un anillo de pirrol, un anillo de tiofeno, un anillo de furano o un anillo de imidazol, el grupo bencilo y los anillos están opcionalmente sustituidos; y n representa entre 0 y 3. Un medicamento que comprende dicho derivado o una sal del mismo como ingrediente activo, que se utiliza para el tratamiento preventivo y/o terapéutico de una enfermedad neurodegenerativa causada por la actividad anormal de la GSK3b, como ser enfermedad de Alzheimer.

100. 发明专利

AR038098A1 DERIVADOS DE 5-(PIRIDIN-3-IL)-1- AZABICICLO [3.2.1] OCTANO, SU PREPARACION Y SU APLICACION EN TERAPEUTICA 未知
公开(公告)号：AR038098A1
公开(公告)日：2004-12-29
申请号：ARP030100009
申请日：2003-01-03
申请人： SANOFI AVENTIS
发明人： GALLI FREDERIC , LECLERC ODILE , LOCHEAD ALISTAIR
IPC分类号： A61K31/437 , A61K31/439 , A61K31/444 , A61K31/4545 , A61K31/46 , A61K31/4709 , A61K31/506 , A61K31/5377 , A61K31/55 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , C07D20060101 , C07D209/00 , C07D221/00 , C07D471/08 , C07D471/18
摘要： Derivados de 5-(piridini-3-il)-1-azabiciclo[3,2,1]octano, medicamento y composición farmacéutica, aplicación en terapéutica relacionada con disfunción de los receptores nicotínicos en especial al nivel de sistema central. Reivindicación 1: Compuesto, en forma de enantiómero puro o en forma de mezcla de enantiómeros, que responde a la fórmula general (1), en la cual: R representa un átomo de halógeno o un grupo cicloalquilo C3-6 o un grupo fenilo sustituido por uno o varios grupos elegidos entre un átomo de halógeno, o un grupo alquilo C1-6, alcoxi C1-6, nitro, amino, dialquilamino C1-3, trifluorometilo, trifluorometoxi, ciano, hidroxi, o metilendioxi, o un grupo piperidinilo, o morfolin-4-ilo, o pirrolidin-1-ilo, o azetidin-1-ilo, o azepin-1-ilo, o piridinilo, o quinoleinilo, o tienilo, o pirazinilo, o furilo, o benzofurilo, o benzotienilo, o indolilo, o pirimidinilo o isoxazolilo, o fenoxazinilo, o fenozatiinilo, o dibenzotienilo, o dibenzofurilo, o pirrolilo o naftilo, y cada uno de esos grupos puede eventualmente ser sustituido por uno o varios grupos elegidos entre los átomos de halógenos, los grupos alquilo C1-6, alcoxi C1-6, trifluorometoxi, trifluorometilo, nitro, ciano, hidroxi, amino, dialquilamino C1-3 o cicloalquilamino C1-8, y se sabe que entre los dos enlaces carbono-carbono representados por línea de puntos, uno es simple y el otro puede ser simple o doble, en estado de base o sal de adición con un ácido.

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