公开(公告)号：JP2002322150A

公开(公告)日：2002-11-08

申请号：JP2002073851

申请日：2002-03-18

Applicant: SERVIER LAB

Inventor： WIERZBICKI MICHEL ,  BOUSSARD MARIE FRANCOISE ,  ROUSSEAU ANNE ,  BOUTIN JEAN-ALBERT ,  DELAGRANGE PHILIPPE

IPC: C07D491/056 ,  A61K31/40 ,  A61K31/403 ,  A61K31/407 ,  A61K31/5377 ,  A61P3/04 ,  A61P3/10 ,  A61P5/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07D209/80 ,  C07D209/94

Abstract: PROBLEM TO BE SOLVED: To provide a compound which exerts a useful pharmacological characteristic toward melatoninergic receptors. SOLUTION: The compound represented by formula (I), not including indeno[1,2-b]indol-10(5H)-one, is provided [wherein, R is H or an arbitrarily substituted alkenyl or an alkyl group; R1 , R2 , R3 , R4 , R5 , R6 , R7 and R8 are each H, an alkyl, an alkenyl, a hydroxy, an alkoxy, an alkenyloxy, an arylalkyl, an arylalkoxy, a carboxy, an acyloxy or an arylcarbonyloxy group, or one of R1 to R8 groups forms an alkylenedioxy group with a group adjacent to the one of R1 to R8 ]. In the compound, when R is not H, at least one of R1 to R8 groups is a hydroxy or an acyloxy group.

公开(公告)号：JP2002265469A

公开(公告)日：2002-09-18

申请号：JP2002065233

申请日：2002-03-11

Applicant: SERVIER LAB

Inventor： WIERZBICKI MICHEL ,  BOUSSARD MARIE FRANCOISE ,  ROUSSEAU ANNE ,  BOUTIN JEAN-ALBERT ,  DELAGRANGE PHILIPPE

IPC: C07D487/06 ,  A61K31/407 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P15/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04

Abstract: PROBLEM TO BE SOLVED: To provide a medicine which contains a compound having high affinity with a melatonin receptor and is useful for treating diseases related to the melatonin operation system. SOLUTION: The compound represented by the formula (R1 , R2 , R3 , R4 , R5 , R6 , and R8 are each H or the like, R7 is H or the like, or one of R1 to R8 forms a 1 to 2C alkylenedioxy together with another adjacent one of R1 to R8 ), its optically isomer (when the optical isomer exists), and its pharmacologically acceptable acid or base adduct; a process for preparing the same; and a pharmaceutical composition containing the same.

公开(公告)号：HU226674B1

公开(公告)日：2009-06-29

申请号：HU0201024

申请日：2002-03-19

Applicant: SERVIER LAB

Inventor： WIERZBICKI MICHEL ,  BOUSSARD MARIE-FRANCOISE ,  ROUSSEAU ANNE ,  BOUTIN JEAN-ALBERT ,  DELAGRANGE PHILIPPE

IPC: C07D209/94 ,  C07D491/056 ,  A61K31/40 ,  A61K31/403 ,  A61K31/407 ,  A61K31/5377 ,  A61P3/04 ,  A61P3/10 ,  A61P5/00 ,  A61P9/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07D209/80

Abstract: Compound of formula (I):wherein:R represents hydrogen or a group selected from alkenyl and optionally substituted alkyl,each of R1 to R8, which may be identical or different, represents hydrogen or a group selected from alkyl, alkenyl, hydroxy, alkoxy, alkenyloxy, arylalkyl, arylalkoxy, carboxy, acyloxy and arylcarbonyloxy,or one of R1 to R8 forms with an adjacent one R1 to R8 an alkylenedioxy group,its optical isomers when they exist, and addition salts thereof with a pharmaceutically acceptable acid or base,with the proviso that:when R does not represent hydrogen, then at least one of R1 to R8 represents hydroxy or acyloxy,and the compounds of formula (I) are other than indeno[1,2-b]indol-10(5H)-one and medicinal products containing the same which are useful for treatment of disorders of the melatoninergic system.

公开(公告)号：AU2007203045A1

公开(公告)日：2008-01-17

申请号：AU2007203045

申请日：2007-06-29

Applicant: SERVIER LAB

Inventor： DELAGRANGE PHILIPPE ,  DESROSES MATTHIEU ,  AUDINOT VALERIE ,  BERTHELOT PASCAL ,  BASILE PERES ,  YOUS SAID ,  CAIGNARD DANIEL-HENRI ,  SPEDDING MICHAEL ,  SABAOUNI AHMED ,  BOUTIN JEAN-ALBERT

IPC: C07C15/24 ,  A61K31/165 ,  A61P25/00 ,  A61P25/08 ,  A61P25/16 ,  A61P25/24 ,  C07C43/20 ,  C07C215/20 ,  C07C233/08 ,  C07C233/18 ,  C07C255/33

Abstract: Naphthalenic derivatives (I) and their enantiomers, diastereoisomer or additive salts of acid or base, are new. Naphthalenic derivatives of formula (I) and their enantiomers, diastereoisomer or additive salts of acid or base, are new. R 1R 4or NHR 4; R 41-6C (halo)alkyl, 1-6C alkenyl, polyhalo(1-6C)alkyl, 3-8C cycloalkyl, 3-8C cycloalkyl(1-6C)alkyl, aryl, aryl(1-6C)alkyl, heteroaryl or heteroaryl(1-6C)alkyl; R 21-6C alkyl substituted 1-6C alkoxy, OH, OSO 2CH 3, N 3, NRR1a, NHCOR1b or NHSO 2R1b; either R, R1a : H or 1-6C alkyl, 3-8C cycloalkyl, aryl or aryl(1-6C)alkyl; or NRR1a : 5-6 membered ring having another heteroatom e.g. N, O or S; R1b : R; and R 3H, halo, 1-6C alkyl or 1-6C alkenyl. Provided that: when R 1is methyl and R 2is hydroxymethyl, then R 3is not hydrogen; the aryl is phenyl, naphthyl or biphenyl; and the heteroaryl is mono or bicyclic heteroaryl with 1-3 heteroatoms e.g. oxygen, sulfur and nitrogen. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Hypnotic; Tranquilizer; Antidepressant; Cardiovascular-Gen; Gastrointestinal-Gen; Muscular-Gen; CNS-Gen; Neuroleptic; Anorectic; Anticonvulsant; Antidiabetic; Antiparkinsonian; Nootropic; Dermatological; Antimigraine; Neuroprotective; Cytostatic; Cerebroprotective; Endocrine-Gen.; Contraceptive. MECHANISM OF ACTION : Melatoninergic receptor agonist. The melatoninergic receptor inhibiting activity of N-[3-methoxy-2-(7-methoxy-1-naphtyl)propyl]acetamide was tested. The result showed that the compound had an inhibition constant (Ki) value of 4.9 mu M.

公开(公告)号：ES2206438T3

公开(公告)日：2004-05-16

申请号：ES02290598

申请日：2002-03-11

Applicant: SERVIER LAB

Inventor： WIERZBICKI MICHEL ,  BOUSSARD MARIE-FRANCOISE ,  ROUSSEAU ANNE ,  BOUTIN JEAN-ALBERT ,  DELAGRANGE PHILIPPE

IPC: C07D487/06 ,  A61K31/407 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P15/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04

Abstract: Compound of formula (I):wherein:R1, R2, R3, R4, R5, R6 and R8, which may be identical or different, each represents hydrogen, alkyl, arylalkyl, hydroxy, alkoxy, arylalkoxy, acyloxy, arylcarbonyloxy, carboxyalkyl or carboxy,R7 represents hydrogen, hydroxy, alkoxy, arylalkoxy, acyloxy or arylcarbonyloxy group,or one of R1 to R8, together with another of R1 to R8 adjacent to it, forms an alkylenedioxy,its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid or base.

公开(公告)号：AR034861A1

公开(公告)日：2004-03-24

申请号：ARP020100952

申请日：2002-03-18

Applicant: SERVIER LAB

Inventor： WIERZBICKI MICHEL ,  BOUSSARD MARIE-FRANCOISE ,  ROUSSEAU ANNE ,  BOUTIN JEAN-ALBERT ,  DELAGRANGE PHILIPPE

IPC: C07D491/056 ,  A61K31/40 ,  A61K31/403 ,  A61K31/407 ,  A61K31/5377 ,  A61P3/04 ,  A61P3/10 ,  A61P5/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07D209/80 ,  C07D209/94 ,  A61P25/00 ,  A61P25/08

Abstract: Un compuesto de indenoindolona de fórmula (1), en donde: R representa un átomo de hidrógeno o un grupo alquenilo C1-6 lineal o ramificado o alquilo C1-6 lineal o ramificado, opcionalmente sustituido por un grupo carboxi o por un grupo de fórmula -NRaRb en donde cada uno de Ra y Rb, que pueden ser iguales o diferentes, representan un átomo de hidrógeno o un grupo alquilo C1-6 lineal o ramificado, o forman junto con el átomo de nitrógeno que los lleva un heterociclo que contiene nitrógeno; cada uno de R1, R2, R3, R4, R5, R6, R7 y R8, que pueden ser iguales o diferentes, representan un átomo de hidrógeno o un grupo alquilo C1-6 lineal o ramificado, alquenilo C1-6 lineal o ramificado, hidroxi, alcoxi C1-6 lineal o ramificado, alqueniloxi C1-6 lineal o ramificado, arilo-alquilo C1-6 en donde la mitad alquilo es lineal o ramificada, arilo-alcoxi C1-6 en donde la mitad alcoxi es lineal o ramificada, carboxi, aciloxi C1-6 lineal o ramificado o arilcarboniloxi; o uno de los grupos R1 a R8 forma con uno adyacente de los grupos R1 a R8 un grupo alquilenodioxi C1-2, sus isómeros ópticos, cuando existen, y sales de adición de los mismos con un ácido o una base farmacéuticamente aceptable; con la condición de que: cuando R no representa un átomo de hidrógeno, entonces por lo menos uno de los grupos R1 a R8 representa un grupo hidroxi o alcoxi C1-6 lineal o ramificado; y los compuestos de fórmula (1) son distintos de indeno[1,2-b]indol-10(5H)-ona; entendiéndose que el término "arilo" significa fenilo, bifenililo, naftilo, o tetrahidronaftilo, siendo cada uno de estos grupos opcionalmente sustituido por uno o más átomos o grupos iguales o diferentes seleccionados entre átomos de halógeno y grupos alquilo C1-6 lineales o ramificados, grupos hidroxi, alcoxi C1-6 lineales o ramificados, polihaloalquilo C1-6 lineales o ramificados, grupos amino (opcionalmente sustituidos por uno o más grupos alquilo C1-6 lineales o ramificados), grupos nitro, acilo C1-6 lineales o ramificados y alquilenodioxi C1-2. También se divulga un procedimiento para la preparación del compuesto y una composición farmacéutica que lo comprende. El compuesto y la composición farmacéutica que lo comprende han probado ser útiles en el tratamiento de los trastornos del sistema melatoninérgico.

公开(公告)号：DK1241169T3

公开(公告)日：2003-11-24

申请号：DK02290598

申请日：2002-03-11

Applicant: SERVIER LAB

Inventor： WIERZBICKI MICHEL ,  BOUSSARD MARIE-FRANCOISE ,  ROUSSEAU ANNE ,  BOUTIN JEAN-ALBERT ,  DELAGRANGE PHILIPPE

IPC: C07D487/06 ,  A61K31/407 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P15/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04

Abstract: Compound of formula (I):wherein:R1, R2, R3, R4, R5, R6 and R8, which may be identical or different, each represents hydrogen, alkyl, arylalkyl, hydroxy, alkoxy, arylalkoxy, acyloxy, arylcarbonyloxy, carboxyalkyl or carboxy,R7 represents hydrogen, hydroxy, alkoxy, arylalkoxy, acyloxy or arylcarbonyloxy group,or one of R1 to R8, together with another of R1 to R8 adjacent to it, forms an alkylenedioxy,its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid or base.

公开(公告)号：DE60200023D1

公开(公告)日：2003-10-02

申请号：DE60200023

申请日：2002-03-11

Applicant: SERVIER LAB

Inventor： WIERZBICKI MICHEL ,  BOUSSARD MARIE-FRANCOISE ,  ROUSSEAU ANNE ,  BOUTIN JEAN-ALBERT ,  DELAGRANGE PHILIPPE

IPC: C07D487/06 ,  A61K31/407 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P15/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04

Abstract: Compound of formula (I):wherein:R1, R2, R3, R4, R5, R6 and R8, which may be identical or different, each represents hydrogen, alkyl, arylalkyl, hydroxy, alkoxy, arylalkoxy, acyloxy, arylcarbonyloxy, carboxyalkyl or carboxy,R7 represents hydrogen, hydroxy, alkoxy, arylalkoxy, acyloxy or arylcarbonyloxy group,or one of R1 to R8, together with another of R1 to R8 adjacent to it, forms an alkylenedioxy,its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid or base.

公开(公告)号：NO20031643A

公开(公告)日：2003-04-10

申请号：NO20031643

申请日：2003-04-10

Applicant: SERVIER LAB

Inventor： FAUCHERE JEAN-LUC ,  ORTUNO JEAN-CLAUDE ,  LEVENS NIGEL ,  CHAMORRO SUSANA ,  BOUTIN JEAN-ALBERT

IPC: C07D249/14 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/55 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/12 ,  A61P15/10 ,  A61P25/08 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/04 ,  A61D9/12

CPC classification number: C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12

公开(公告)号：NZ517855A

公开(公告)日：2002-10-25

申请号：NZ51785502

申请日：2002-03-18

Applicant: SERVIER LAB

Inventor： WIERZBICKI MICHEL ,  BOUSSARD MARIE-FRANCOISE ,  ROUSSEAU ANNE ,  BOUTIN JEAN-ALBERT ,  DELAGRANGE PHILIPPE

IPC: C07D491/056 ,  A61K31/40 ,  A61K31/403 ,  A61K31/407 ,  A61K31/5377 ,  A61P3/04 ,  A61P3/10 ,  A61P5/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07D209/80 ,  C07D209/94 ,  C07D413/06

Abstract: A compound of formula (I), wherein: R is H or a linear or branched alkenyl or linear or branched alkyl group optionally substituted by a carboxy group or by a group of the formula -NRaRb. Each of R1-R8 independently represents H or a linear or branched alkyl group, a linear or branched alkenyl group, a hydroxy group, a linear or branched alkoxy group, a linear or branched alkenyloxy group, an arylalkyl group in which the alkyl moiety is linear or branched, an arylalkoxy group in which the alkoxy group is linear or branched, a carboxy group, a linear or branched acyloxy group, or an arylcarbonyloxy group. Or one of the groups R1 to R8 forms with an adjacent one of the groups R1 to R8 a (C1-C2)alkylenedioxy group. With the proviso that: i) When R does not represent a H atom, then at least one of the groups R1 to R8 represents a hydroxy group or a linear or branched acyloxy group. ii) The compounds of formula (I) are other than [1,2-b]indol-10(5H)-one. Also described are pharmaceutical compositions comprising the compound of formula (I) in combination with one or more inert, non-toxic pharmaceutically acceptable carriers. The compounds of formula (I) are useful for treating disorders of the melatoninergic system.