公开(公告)号：EA004737B1

公开(公告)日：2004-08-26

申请号：EA200001078

申请日：2000-11-16

Applicant: SERVIER LAB

Inventor： PRUDHOMME MICHELLE ,  MOREAU PASCALE ,  ANIZON FABRICE ,  MARMINON CHRISTELLE ,  ATASSI GHANEM ,  PIERRE ALAIN ,  PFEIFFER BRUNO ,  RENARD PIERRE

IPC: C07D491/147 ,  A61K31/4985 ,  A61K31/70 ,  A61K31/706 ,  A61P35/00 ,  C07D209/82 ,  C07D491/153 ,  C07D491/22 ,  C07H9/06 ,  C07H19/23

Abstract: Соединенияформулы (I)где Rи R, которыемогутбытьодинаковымиилиразличными, представляютсобойгруппуформулы U-V, где U представляетодинарнуюсвязьилиалкиленовуюцепь, котораянеобязательнозамещенаи/илиявляетсяненасыщенной, и V имеетзначение, определенноев описании,G представляетатомкислородаили NRгруппу, где Rтакой, какопределенов описании,Хпредставляетатомводорода, гидрокси, меркаптоилиалкилтиогруппу,Y представляетатомводородаили X+Y представляеткарбонильнуюгруппу,Xпредставляетатомводорода, гидрокси, алкокси, меркаптоилиалкилтиогруппу,Yпредставляетатомводородаили X+Yпредставляеткарбонильнуюгруппу,R, Rи Rтакие, какопределенов описании, ихизомерыи солиприсоединенияихс фармацевтическиприемлемойкислотойилиоснованием. Лекарственныесредства.

公开(公告)号：FR2831169B1

公开(公告)日：2003-12-12

申请号：FR0113576

申请日：2001-10-22

Applicant: SERVIER LAB

Inventor： PRUDHOMME MICHELLE ,  MARMINON CHRISTELLE ,  MOREAU PASCALE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  PFEIFFER BRUNO ,  RENARD PIERRE ,  BIZOT ESPIARD JEAN GUY

IPC: A61K31/7056 ,  A61P3/04 ,  A61P3/10 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07H19/23

Abstract: Compound of formula (I): wherein: R1 and R2 each represents a group selected from hydrogen, alkyl, arylalkyl, hydroxy, hydroxyalkyl, dihydroxyalkyl, alkoxy, alkoxyalkyl, amino and aminoalkyl (optionally substituted), Ra and Rb each represents an alkylene chain, X1, X2 and X3 each represents a group selected from hydroxy, alkoxy, aryloxy, arylalkoxy, alkyl, amino (optionally substituted), halogen, alkylcarbonyloxy and azido, X4 represents a methylidene group or a group of formula -Rc-X1 as defined in the description, their isomers and also their addition salts with a pharmaceutically acceptable acid or base.

公开(公告)号：DK1101770T3

公开(公告)日：2003-08-04

申请号：DK00403107

申请日：2000-11-09

Applicant: SERVIER LAB

Inventor： PRUDHOMME MICHELLE ,  MOREAU PASCALE ,  ANIZON FABRICE ,  MARMINON CHRISTELLE ,  ATASSI GHANEM ,  PIERRE ALAIN ,  PFEIFFER BRUNO ,  RENARD PIERRE

IPC: C07D491/147 ,  A61K31/4985 ,  A61K31/70 ,  A61K31/706 ,  A61P35/00 ,  C07D209/82 ,  C07D491/153 ,  C07D491/22 ,  C07H9/06 ,  C07H19/23

Abstract: A composition comprises 12,13-(Pyranosyl)-indolo(2,3-a)pyrrolo(3,4-c)carbazole and 12,13-(pyranosyl)-furo(3,4-c)indolo(2,3-a)carbazole derivatives (I), or their isomers, salts with acids or bases, are new A composition comprises 12,13-(Pyranosyl)-indolo(2,3-a)pyrrolo(3,4-c)carbazole and 12,13-(pyranosyl)-furo(3,4-c)indolo(2,3-a)carbazole derivatives of formula (I), or their isomers, salts with acids or bases, are new R1, R2 = U-V; U = 1-6C alkylene, optionally substituted by one or more halo or OH, and which may be unsaturated; V = H, halo, CN, NO2, N3, 1-6C alkyl, aryl, arylalkyl, OH, 1-6C alkoxy, aryloxy, aryl alkoxy, formyl, carboxy, aminocarbonyl, NRaRb, -CO-T1, -CO-NRa-T1, -NRa-CO-T1, -O-CO-T1, -CO-O-T1, -O-T2-NRaRb, -OT2-ORa, -O-T2-COORa, -NRa-T2-NRaRb, -NRa-T2-ORa, -NRa-T2-CO2Raor S(O)n-Ra; Ra, Rb = H, 1-6C alkyl, aryl, or arylalkyl, or both together with the N atom form a 5-7 membered heterocycle which may contain a second heteroatom (O or N) and may be substituted by alkyl, alkoxy, OH, amino, 1-6C alkylamino, or 1-6C dialkylamino; T1 = 1-6C alkyl, aryl, 1-6C arylalkyl, 1-6C alkylene, optionally substituted by -ORa, -NRaRb, -COORa, -CO-Ra, or -CO-NRaRb; T2 = 1-6C alkylene; n = 0 - 2; G = O or NR3; R3 = H, 1-6C alkyl, aryl, arylalkyl, cycloalkyl, cycloalkyl alkyl, -ORa, -NRaRb, -OT2-NRaRb, -NRa-T2-NRaRb, 1-6C hydroxylamino, dihydroxylamino, -CO-Ra, -NH-CO-Ra, 1-6C alkylene, optionally substituted by one or more of halogen, CN, NO2, -ORa, -NRaRb, -COORa, -CORa, hydroxylamino, dihydroxylamino, or -CO-NHRa; X = H, OH, 1-6C alkoxy, SH, or 1-6C alkylthio; Y = H, or X and Y together with the C atom form carbonyl; X1 = H, OH, 1-6C alkoxy, SH, or 1-6C alkylthio; Y1 = H or X1 and Y1 together with the C atom form carbonyl; R4, R5 = H, halogen, OH, alkoxy, aryloxy, aryl alkoxy, alkyl, arylalkyl, aryl, amino (optionally substituted by one or two alkyl, alkyl, aryl and arylalkyl groups), azido, -N=NRa, or -O-CO-Rc; Rc = 1-6C alkyl (optionally substituted by one or more halogen, OH, amino, alkylamino and dialkylamino groups), aryl, aralkyl, cycloalkyl or heterocycloalkyl; R6 = -U1-R4; U1 = a bond or methylene; or R4, R5, and R6 taken in pairs together with the C atoms may = 3-6 membered ring containing 1 or 2 O atoms, except for the following specific compounds: 1,11-dichloro-12,13-(1,2-(4-(O-methyl- beta -D-mannopyranosyl))-6,7,12,13-tetrahydro(5H)indolo(2,3-a)pyrrolo(3,4-c )carbazole-5,7-dio ne; 12,13-(1,2-(4-(O-methyl- beta -D-mannopyranosyl))-6,7,12,13-tetrahydro(5H)indolo(2,3-a)pyrrolo(3,4-c )carbazole-5,7-dione; 12,13-(1,2-(4-(O-methyl- beta -D-mannopyranosyl))-6,7,12,13-tetrahydro(5H)indolo(2,3-a)pyrrolo(3,4-c )carbazole-5-one; and 12,13-(1,2-(4-(O-methyl- beta -D-mannopyranosyl))-5,6,12,13-tetrahydro(7H)indolo(2,3-a)pyrrolo(3,4-c )carbazole-7-one.

公开(公告)号：EA006201B1

公开(公告)日：2005-10-27

申请号：EA200400533

申请日：2002-10-21

Applicant: SERVIER LAB

Inventor： PRUDHOMME MICHELLE ,  MARMINON CHRISTELLE ,  MOREAU PASCALE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  PFEIFFER BRUNO ,  RENARD PIERRE ,  BIZOT-ESPIARD JEAN-GUY

IPC: A61K31/7056 ,  A61P3/04 ,  A61P3/10 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07H19/23

Abstract: Соединениеформулы (I)вкоторой Rи Rкаждыйпредставляетсобойгруппу, выбраннуюизводорода, алкила, арилалкила, гидрокси, гидроксиалкила, дигидроксиалкила, алкокси, алкоксиалкила, аминогруппыи аминоалкила (необязательнозамещенного),Ra и Rb каждыйпредставляетсобойалкиленовуюцепь,X, ХиХкаждыйпредставляетсобойгруппу, выбраннуюизгидрокси, алкокси, арилокси, арилалкокси, алкила, аминогруппы (необязательнозамещенной), галогена, алкилкарбонилоксии азидо,Хпредставляетсобойметилиденовуюгруппуилигруппуформулы -Rc-X, которыеимеютзначения, указанныев описании,ихизомеры, атакжеихаддитивныесолис фармацевтическиприемлемойкислотойилиоснованием. Лекарственныесредства.

公开(公告)号：NZ532365A

公开(公告)日：2005-07-29

申请号：NZ53236502

申请日：2002-10-21

Applicant: SERVIER LAB

Inventor： PRUDHOMME MICHELLE ,  MARMINON CHRISTELLE ,  MOREAU PASCALE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  BIZOT-ESPIARD JEAN-GUY ,  PFEIFFER BRUNO ,  RENARD PIERRE

IPC: A61K31/7056 ,  A61P3/04 ,  A61P3/10 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07H19/23

Abstract: Hydroxyalkyl indolocarbazole compounds of formula (I), their isomers and their addition salts with a pharmaceutically acceptable acid or base that have a selective inhibitory activity in respect of glycogen synthesis kinase (GSK-3) are disclosed, wherein: R1 and R2 each represent a group selected among hydrogen, C1-C6alkyl, arylC1-C6alkyl, hydroxy, C1-C6hydroxylalkyl, dihydroxyC1-C6alkyl, C1-C6alkoxy, alkoxyC1-C6alkyl, amino and C1-C6aminoalkyl (optionally substituted); Ra and Rb each represent an C1-C6alkylene chain; X1 , X2 and X3 each represent a group selected among hydroxy, C1-C6alkoxy, aryloxy, arylC1-C6alkoxy, C1-C6alkyl, amino (optionally substituted), halogen, C1-C6alkylcarbonyloxy and azido; X4 represents a methylidene group or a group of formula -Rc-X1, wherein Rc represents a single bond or a methylene group and X1 is as defined above.

公开(公告)号：PL368237A1

公开(公告)日：2005-03-21

申请号：PL36823702

申请日：2002-10-21

Applicant: SERVIER LAB

Inventor： PRUDHOMME MICHELLE ,  MARMINON CHRISTELLE ,  MOREAU PASCALE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  PFEIFFER BRUNO ,  RENARD PIERRE ,  BIZOT-ESPIARD JEAN-GUY

IPC: A61K31/7056 ,  A61P3/04 ,  A61P3/10 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07H19/23

Abstract: Compound of formula (I): wherein: R1 and R2 each represents a group selected from hydrogen, alkyl, arylalkyl, hydroxy, hydroxyalkyl, dihydroxyalkyl, alkoxy, alkoxyalkyl, amino and aminoalkyl (optionally substituted), Ra and Rb each represents an alkylene chain, X1, X2 and X3 each represents a group selected from hydroxy, alkoxy, aryloxy, arylalkoxy, alkyl, amino (optionally substituted), halogen, alkylcarbonyloxy and azido, X4 represents a methylidene group or a group of formula -Rc-X1 as defined in the description, their isomers and also their addition salts with a pharmaceutically acceptable acid or base.

公开(公告)号：BR0213403A

公开(公告)日：2004-11-03

申请号：BR0213403

申请日：2002-10-21

Applicant: SERVIER LAB

Inventor： PRUDHOMME MICHELLE ,  MARMINON CHRISTELLE ,  MOREAU PASCALE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  PFEIFFER BRUNO ,  RENARD PIERRE ,  BIZOT-ESPIARD JEAN-GUY

IPC: A61K31/7056 ,  A61P3/04 ,  A61P3/10 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07H19/23

Abstract: Compound of formula (I): wherein: R1 and R2 each represents a group selected from hydrogen, alkyl, arylalkyl, hydroxy, hydroxyalkyl, dihydroxyalkyl, alkoxy, alkoxyalkyl, amino and aminoalkyl (optionally substituted), Ra and Rb each represents an alkylene chain, X1, X2 and X3 each represents a group selected from hydroxy, alkoxy, aryloxy, arylalkoxy, alkyl, amino (optionally substituted), halogen, alkylcarbonyloxy and azido, X4 represents a methylidene group or a group of formula -Rc-X1 as defined in the description, their isomers and also their addition salts with a pharmaceutically acceptable acid or base.

公开(公告)号：HK1010870A1

公开(公告)日：1999-07-02

申请号：HK98111880

申请日：1998-11-10

Applicant: SERVIER LAB

Inventor： COUDERT GERARD ,  KHATIB SIHAM ,  MOREAU PASCALE ,  CAIGNARD DANIEL-HENRI ,  RENARD PIERRE ,  ATASSI GHANEM ,  PIERRE ALAIN

IPC: C07D319/14 ,  A61K31/335 ,  A61K31/357 ,  A61K31/47 ,  A61P35/00 ,  C07D319/24 ,  C07D491/04 ,  C07D491/056 ,  C07D491/14 ,  C07D491/147 ,  C07D ,  A61K

Abstract: 7,12-Dioxabenz(a)anthracene derivatives of formula (I) and their isomers and addition salts are new: R1 = H or OR; R = H or 1-6C alkyl (optionally substituted by aryl or heteroaryl); R2 = H, halo, OH, 1-6C alkoxy, CHO, CF3SO3, CN, 2-7C alkyloxycarbonyl, aryloxycarbonyl, NRa'Rb' or BNRa''Rb''; Ra', Ra'' = di(1-6C alkyl)amino(1-6C alkyl); or Ra'' = 1-6C alkyl optionally substituted by OH; Rb', Rb'' = H or 1-6C alkyl; B = CO or CH2; X = N (optionally substituted by Rc') or X'; X' = CR3; Rc' = 1-6C alkyl; R3 = H, 2-7C alkoxycarbonyl or BNRa''Rb'' or CX'R2 = a group of formula (a): Y = N or CR4; R4 = H or OR''; R'' = H, 1-6C alkyl (optionally substituted by OH), aryl or heteroaryl; aryl = Ph or naphthyl (optionally substituted by halo, 1-6C alkyl, OH, 1-6C alkoxy or trihalomethyl); heteroaryl = mono- or bicyclic aromatic group containing 1-2 heteroatoms comprising O, S and/or N (optionally substituted by halo, 1-6C alkyl, OH, 1-6C alkoxy or trihalomethyl); provided that when X = N and Y = CH, or when X = CH and Y = N, or when X=Y = CH, then R1 and R2 are not both H. N2-(7,12-dioxa-3-hydroxybenzo(a)anthracene-5,6-maleimido)-N1,N1-dimeth ylethylenediamine hydrochloride is specifically claimed.

公开(公告)号：HK1072774A1

公开(公告)日：2005-09-09

申请号：HK05102890

申请日：2005-04-07

Applicant: SERVIER LAB

Inventor： PRUDHOMME MICHELLE ,  MARMINON CHRISTELLE ,  MOREAU PASCALE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  PFEIFFER BRUNO ,  RENARD PIERRE ,  BIZOT-ESPIARD JEAN-GUY

IPC: A61K31/7056 ,  A61P3/04 ,  A61P3/10 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07H19/23 ,  C07H ,  A61K ,  A61P

Abstract: Compound of formula (I): wherein: R1 and R2 each represents a group selected from hydrogen, alkyl, arylalkyl, hydroxy, hydroxyalkyl, dihydroxyalkyl, alkoxy, alkoxyalkyl, amino and aminoalkyl (optionally substituted), Ra and Rb each represents an alkylene chain, X1, X2 and X3 each represents a group selected from hydroxy, alkoxy, aryloxy, arylalkoxy, alkyl, amino (optionally substituted), halogen, alkylcarbonyloxy and azido, X4 represents a methylidene group or a group of formula -Rc-X1 as defined in the description, their isomers and also their addition salts with a pharmaceutically acceptable acid or base.

公开(公告)号：HU0401885A2

公开(公告)日：2004-12-28

申请号：HU0401885

申请日：2002-10-21

Applicant: SERVIER LAB

Inventor： PRUDHOMME MICHELLE ,  MARMINON CHRISTELLE ,  MOREAU PASCALE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  PFEIFFER BRUNO ,  RENARD PIERRE ,  BIZOT-ESPIARD JEAN-GUY

IPC: A61K31/7056 ,  A61P3/04 ,  A61P3/10 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07H19/23

Abstract: Compound of formula (I): wherein: R1 and R2 each represents a group selected from hydrogen, alkyl, arylalkyl, hydroxy, hydroxyalkyl, dihydroxyalkyl, alkoxy, alkoxyalkyl, amino and aminoalkyl (optionally substituted), Ra and Rb each represents an alkylene chain, X1, X2 and X3 each represents a group selected from hydroxy, alkoxy, aryloxy, arylalkoxy, alkyl, amino (optionally substituted), halogen, alkylcarbonyloxy and azido, X4 represents a methylidene group or a group of formula -Rc-X1 as defined in the description, their isomers and also their addition salts with a pharmaceutically acceptable acid or base.