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公开(公告)号:AR034516A1
公开(公告)日:2004-02-25
申请号:ARP020102275
申请日:2002-06-18
Applicant: SERVIER LAB
Inventor: WIERZBICKI MICHEL , FOURQUEZ JEAN-MARIE , LEVENS NIGEL , HUSSON-ROBERT BERNADETTE , NOSJEAN OLIVIER , BOULANGER MICHELLE
IPC: C07D295/18 , A61K31/16 , A61K31/397 , A61K31/40 , A61K31/403 , A61K31/426 , A61K31/4453 , A61K31/5375 , A61P3/00 , A61P3/04 , A61P3/10 , C07C237/14 , C07D205/04 , C07D207/18 , C07D207/20 , C07D209/02 , C07D209/52 , C07D277/04 , C07D277/22 , C07D295/185 , A61K31/675 , A61K31/155 , A61K31/401 , A61K31/44
Abstract: Compuestos de la fórmula (1) donde A representa un anillo de carbono saturado opcionalmente sustitutido que tiene entre 4 y 8 miembros de anillo, R1 y R4 que pueden ser idénticos o diferentes, representan, cada uno un átomo de hidrógeno o un grupo acilo, R2 y R3 que pueden ser idénticos o diferentes, representan, cada uno, un átomo de hidrógeno o un grupo alquilo, R5 y R6, que pueden ser idénticos o diferentes, representan, cada uno un átomo de hidrógeno o un grupo alquilo, o R5 y R6 juntos, con el átomo de nitrógeno que los lleva, forman un heterociclo con contenido de nitrógeno opcionalmente sustituido, estereoisómeros de los mismos, y también, sales de adición de los mismos con un ácido farmacéuticamente aceptable. Medicamentos antidiabéticos.
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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.
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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.
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公开(公告)号:NO315468B1
公开(公告)日:2003-09-08
申请号:NO971861
申请日:1997-04-23
Applicant: SERVIER LAB
Inventor: WIERZBICKI MICHEL , BOUSSARD MARIE-FRANCOISE , VERBEUREN TONY , VALLEZ MARIE-ODILE
IPC: A61K31/35 , A61K31/352 , A61K31/36 , A61P9/00 , A61P43/00 , C07D311/30 , C07D407/12
Abstract: Diosmetin acids and esters of formula (I), their enantiomers and salts are new. R2, R4, R6 = H, 1-5C alkyl, CH2CH=CH2, CH2C(CH3)=CH2, CH2CH=C(CH3)2, CH2CH2CH(CH3)2, 2,2-dimethyl-1,3-dioxolan-4-ylmethyl, CH2CH(OH)CH2OH or ACOOR8; A = 1-3C hydrocarbon chain (optionally substituted by methyl or OH); R8 = H or 1-5C alkyl; R3, R5 = H, CH2CH2CH3, CH2CH=CH2, CH2CH(CH3)2, C(CH3)2CH=CH2, C(CH3)2CH2CH3, CH2C(CH3)=CH2 or COCH3 R1, R7 = H, CH2CH2CH3, CH2CH=CH2, CH2CH=C(CH3)2, tert.-butyl, CH2CH2CH(CH3)CH3, CH2C(CH3)=CH2 or CH2CH(CH3)2 provided that if one or two of R2, R4, and R6 = ACOOR8, then at least one of the remaining R1-R7 is not H.
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公开(公告)号:FR2826003B1
公开(公告)日:2003-08-15
申请号:FR0107934
申请日:2001-06-18
Applicant: SERVIER LAB
Inventor: WIERZBICKI MICHEL , FOURQUEZ JEAN MARIE , LEVENS NIGEL , HUSSON ROBERT BERNADETTE , NOSJEAN OLIVIER , BOULANGER MICHELLE
IPC: C07D295/18 , A61K31/16 , A61K31/397 , A61K31/40 , A61K31/403 , A61K31/426 , A61K31/4453 , A61K31/5375 , A61P3/00 , A61P3/04 , A61P3/10 , C07C237/14 , C07D205/04 , C07D207/18 , C07D207/20 , C07D209/02 , C07D209/52 , C07D277/04 , C07D277/22 , C07D295/185 , C07D207/12
Abstract: A compound of formula (I):wherein:represents an optionally substituted saturated carbon ring having from 4 to 8 ring members,R1 and R4, which may be identical or different, each represents hydrogen or acyl,R2 and R3, which may be identical or different, each represents hydrogen or alkyl,R5 and R6, which may be identical or different, each represents hydrogen or alkyl, or R5 and R6 together, with the nitrogen atom carrying them, form an optionally substituted nitrogen-containing heterocycle,stereoisomers thereof, and also addition salts thereof with a pharmaceutically acceptable acid.Medicinal products containing the same which are useful for treatment of glucose intolerance or of disorders associated with hyperglycaemia.
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公开(公告)号:HK1050186A1
公开(公告)日:2003-06-13
申请号:HK03102394
申请日:2003-04-03
Applicant: SERVIER LAB
Inventor: WIERZBICKI MICHEL , FOURQUEZ JEAN-MARIE , LEVENS NIGEL , HUSSON-ROBERT BERNADETTE , NOSJEAN OLIVIER , BOULANGER MICHELLE
IPC: C07D295/18 , A61K31/16 , A61K31/397 , A61K31/40 , A61K31/403 , A61K31/426 , A61K31/4453 , A61K31/5375 , A61P3/00 , A61P3/04 , A61P3/10 , C07C237/14 , C07D205/04 , C07D207/18 , C07D207/20 , C07D209/02 , C07D209/52 , C07D277/04 , C07D277/22 , C07D295/185 , C07C , C07D , A61K , A61P
Abstract: A compound of formula (I):wherein:represents an optionally substituted saturated carbon ring having from 4 to 8 ring members,R1 and R4, which may be identical or different, each represents hydrogen or acyl,R2 and R3, which may be identical or different, each represents hydrogen or alkyl,R5 and R6, which may be identical or different, each represents hydrogen or alkyl, or R5 and R6 together, with the nitrogen atom carrying them, form an optionally substituted nitrogen-containing heterocycle,stereoisomers thereof, and also addition salts thereof with a pharmaceutically acceptable acid.Medicinal products containing the same which are useful for treatment of glucose intolerance or of disorders associated with hyperglycaemia.
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公开(公告)号:BR0202279A
公开(公告)日:2003-04-29
申请号:BR0202279
申请日:2002-06-13
Applicant: SERVIER LAB
Inventor: WIERZBICKI MICHEL , BOUSSARD MARIE-FRACOISE , ROUSSEAU ANNE , ATASSI GHANAEM , HICKMAN JOHN , PIERRE ALAIN , LEONCE STEPHANE , GUILBAUD NICOLAS , KRAUS-BERTHIER LAURENCE
IPC: C07D209/80 , A61K31/403 , A61K31/433 , A61K31/4439 , A61P35/00 , C07D209/94 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D491/04 , C07D491/056 , A61K31/15 , A61K31/407 , C07D209/56
Abstract: Indenoindolone derivatives (I), their isomers and salts with acids and bases are new. Indenoindolone derivatives (I), their isomers and salts with acids and bases are new; R = H, alkyl (optionally substituted by carboxy, alkoxycarbonyl, or NR10R11), or alkenyl; R1-R8 = H, alkyl (optionally substituted by aryl, carboxy or alkoxycarbonyl), OH, acyloxy, NR12R13, carboxy, alkoxy (optionally substituted by aryl or NR14R15), alkenyloxy, or to adjacent groups R1-R8 = 1 or 2C alkylenedioxy; R9 = H, aryl, heteroaryl or alkyl (optionally containing one or more unsaturations and optionally substituted by one or more aryl, heteroaryl, 3-8C cycloalkyl, CN, or NR17R18 groups); X = O or NR16; R10, R11, R14, R15, R17, R18 = alkyl; NR10+R11, NR14+R15, NR17+R18 = nitrogen heterocycle; R12, R13 = H, alkyl, or NR14R15; R16 = H, alkyl, aryl, or aryl alkyl. Where alkyl, alkoxy, acyloxy, alkenyl and alkenyloxy groups have up to 6 C atoms, aryl is defined as phenyl, biphenyl, or naphthyl (optionally substituted by one or more halogen, alkyl, alkenyl, alkoxy, phenoxy, nitro, CN, amino, mono- and di-alkylamino or 1-2C alkylenedioxy groups) and heteroaryl groups may be mono- or bicyclic of 5-12 members with 1-3 heteroatoms (O, N, S) and optionally substituted by halogen, alkyl, OH, alkoxy, polyhaloalkyl, amino, mono- and di-alkylamino groups, and nitrogen heterocycles are monocyclic having 5-7 members including 1-3 heteroatoms, one of which is N and the others may be O, N, or S. An Independent claim is also included for the preparation of (I).
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公开(公告)号:ZA200204865B
公开(公告)日:2003-02-20
申请号:ZA200204865
申请日:2002-06-18
Applicant: SERVIER LAB
Inventor: WIERZBICKI MICHEL , FOURQUEZ JEAN-MARIE , LEVENS NIGEL , HUSSON-ROBERT BERNADETTE , NOSJEAN OLIVIER , BOULANGER MICHELLE
IPC: A61K31/16 , A61K31/397 , A61K31/40 , A61K31/403 , C07D295/18 , A61K31/426 , A61K31/4453 , A61K31/5375 , A61P3/00 , A61P3/04 , A61P3/10 , C07C237/14 , C07D205/04 , C07D207/18 , C07D207/20 , C07D209/02 , C07D209/52 , C07D277/04 , C07D277/22 , C07D295/185 , C07C , C07D , A61K , A61P
Abstract: A compound of formula (I):wherein:represents an optionally substituted saturated carbon ring having from 4 to 8 ring members,R1 and R4, which may be identical or different, each represents hydrogen or acyl,R2 and R3, which may be identical or different, each represents hydrogen or alkyl,R5 and R6, which may be identical or different, each represents hydrogen or alkyl, or R5 and R6 together, with the nitrogen atom carrying them, form an optionally substituted nitrogen-containing heterocycle,stereoisomers thereof, and also addition salts thereof with a pharmaceutically acceptable acid.Medicinal products containing the same which are useful for treatment of glucose intolerance or of disorders associated with hyperglycaemia.
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29.
公开(公告)号:ZA200204757B
公开(公告)日:2003-02-17
申请号:ZA200204757
申请日:2002-06-13
Applicant: SERVIER LAB
Inventor: WIERZBICKI MICHEL , BOUSSARD MARIE-FRANCOISE , ROSSEAU ANNE , ATASSI GHANEM , HICKMAN JOHN , PIERRE ALAIN , LEONCE STEPHANE , GUILBAUD NICOLAS , KRAUS-BERTHIER LAURENCE
IPC: C07D209/80 , A61K31/403 , A61K31/433 , A61K31/4439 , A61P35/00 , C07D209/94 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D491/04 , C07D491/056 , C07D , A61K
Abstract: Indenoindolone derivatives (I), their isomers and salts with acids and bases are new. Indenoindolone derivatives (I), their isomers and salts with acids and bases are new; R = H, alkyl (optionally substituted by carboxy, alkoxycarbonyl, or NR10R11), or alkenyl; R1-R8 = H, alkyl (optionally substituted by aryl, carboxy or alkoxycarbonyl), OH, acyloxy, NR12R13, carboxy, alkoxy (optionally substituted by aryl or NR14R15), alkenyloxy, or to adjacent groups R1-R8 = 1 or 2C alkylenedioxy; R9 = H, aryl, heteroaryl or alkyl (optionally containing one or more unsaturations and optionally substituted by one or more aryl, heteroaryl, 3-8C cycloalkyl, CN, or NR17R18 groups); X = O or NR16; R10, R11, R14, R15, R17, R18 = alkyl; NR10+R11, NR14+R15, NR17+R18 = nitrogen heterocycle; R12, R13 = H, alkyl, or NR14R15; R16 = H, alkyl, aryl, or aryl alkyl. Where alkyl, alkoxy, acyloxy, alkenyl and alkenyloxy groups have up to 6 C atoms, aryl is defined as phenyl, biphenyl, or naphthyl (optionally substituted by one or more halogen, alkyl, alkenyl, alkoxy, phenoxy, nitro, CN, amino, mono- and di-alkylamino or 1-2C alkylenedioxy groups) and heteroaryl groups may be mono- or bicyclic of 5-12 members with 1-3 heteroatoms (O, N, S) and optionally substituted by halogen, alkyl, OH, alkoxy, polyhaloalkyl, amino, mono- and di-alkylamino groups, and nitrogen heterocycles are monocyclic having 5-7 members including 1-3 heteroatoms, one of which is N and the others may be O, N, or S. An Independent claim is also included for the preparation of (I).
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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.
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