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61. 发明专利

NO20035215D0 未知
公开(公告)号：NO20035215D0
公开(公告)日：2003-11-24
申请号：NO20035215
申请日：2003-11-24
申请人： SERVIER LAB
发明人： HUSSON HENRI-PHILIPPE , GIORGI-RENAULT SYLVIANE , DESBENE STEPHANIE , HICKMAN JOHN , PIERRE ALAIN , KRAUS-BERTHIER LAURENCE , PFEIFFER BRUNO , RENARD PIERRE
IPC分类号： C07D491/048 , A61K31/4741 , A61K31/4743 , A61K31/4745 , A61P35/00 , C07D491/04 , C07D491/14 , C07D491/147 , C07D491/153 , C07D497/14 , C07D
摘要： Compound of formula (I): wherein: represents a single or double bond, represents a ring system selected from R6a, R6b, R6c, R6d, X and Y are as defined in the description, R1 represents a hydrogen atom or a group selected from aryl, heteroaryl, cycloalkyl, optionally substituted alkyl, and COR8 wherein R8 is as defined in the description, R2, R3, R4 and R5, which may be the same or different, each represent: a hydrogen atom, a halogen atom, an alkyl group,. an alkoxy group, a hydroxy group, a polyhaloalkyl group, a nitro group, an optionally substituted amino group, a group of formula wherein m represents an integer such that 1

62. 发明专利

NO20035214A 未知
公开(公告)号：NO20035214A
公开(公告)日：2003-11-24
申请号：NO20035214
申请日：2003-11-24
申请人： SERVIER LAB
发明人： HUSSON HENRI-PHILIPPE , GIORGI-RENAULT SYLVIANE , DESBENE STEPHANIE , HICKMAN JOHN , PIERRE ALAIN , KRAUS-BERTHIER LAURENCE , PFEIFFER BRUNO , RENARD PIERRE
IPC分类号： A61K31/4741 , A61K31/4743 , A61K31/4745 , A61K31/661 , A61P35/00 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/056 , C07D491/14 , C07D497/04 , C07F9/60 , C07F9/6561 , A61K31/4355
CPC分类号： C07D491/04 , C07D491/14 , C07F9/6561

63. 发明专利

ZA200302159B New compounds derived from quinazoline, a process for their preparation and pharmaceutical compositions containing them. 未知
公开(公告)号：ZA200302159B
公开(公告)日：2003-09-23
申请号：ZA200302159
申请日：2003-03-18
申请人： SERVIER LAB
发明人： GOLDSTEIN SOLO , DHAINAUT ALAIN , TIZOT ANDRE , FAUCHERE JEAN-LUC , KUCHARCZYK NATHALIE , HICKMAN JOHN , PIERRE ALAIN , TUCKER GORDON , KRAUS-BERTHIER LAURENCE
IPC分类号： C07D401/06 , A61K31/517 , A61P9/00 , A61P25/00 , A61P35/00 , C07D401/14 , C07D403/06 , C07D407/14 , C07D409/14 , C07D521/00 , C07D , A61K , A61P
摘要： Quinazoline derivatives (I) are new. Quinazoline derivatives of formula (I), their enantiomers, diastereomers and salts are new. A = bond, 1-6C alkylene, 2-6C alkenylene, 2-6C alkynylene, T, A1-T, T-A1, A1-T-A1, or A1-T-A'1-T'; T, T' = carbonyl, carbonyloxy, thio, sulfirylsulfonyl, oxy, amino, 1-6C aminoalkyl, aminoaryl, carbonylamino, carbonylamino-1-6C alkyl, carbonylaminoaryl, oxycarbonyl, aminocarbonyl, 1-6C aminoalkylcarbonyl, aminoarylcarbonyl, sulfonylamino, sulfonylamino-1-6C alkyl, sulfonylaminoaryl, aminosulfonyl, amino-1-6C alkylsulfonyl or aminoarylsulfonyl; A1, A'1 = 1-6C alkylene, 2-6C alkenylene or 2-6C alkynylene; B = 1-6C alkyl, aryl, 3-10C cycloalkyl, Het1, Het2, arylaminoaryl or aryl-1-6C alkylaryl (all optionally substituted by 1-3 Z); D = 1-6C alkylene (where 1 C atom may be substituted by B); X = O or S; Z, R1 = halo, 1-6C alkyl, 1-6C alkoxy, OH, SH, CN, NO2, NH2, 1-6C alkylamino, di-1-6C alkylamino, 1-4C perhaloalkyl, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C alkylaminocarbonyl, di-1-6C alkylaminocarbonyl, carbamoyl or 1-6C alkoxycarbonylamino; R2 = H, or 1-6C alkyl, aryl, 3-10C cycloalkyl, Het1, Het2, aryl-1-6C alkyl or Het2-1-6C alkyl-3-10C cycloalkyl-1-6C alkyl or Het1-1-6C alkyl (all optionally substituted by halo, 1-6C alkyl, 1-6C alkoxy, OH, SH, CN, NO2, NH2, 1-6C alkylamino, di-1-6C alkylamino, 1-4C perhaloalkyl, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C alkylaminocarbonyl, di-1-6C alkylaminocarbonyl, carbamoyl, 1-6C alkoxycarbonylamino, or aryl-1-6C alkyl or arylamino (both optionally substituted by 1-3 Z)); aryl = phenyl, naphthyl or biphenyl; Het1 = 5-7 membered saturated or partially unsaturated mono- or polycyclic heterocycloalkyl containing 1-3 N, O or S atoms; Het2 = 5-11 membered mono- or bicyclic aromatic ring containing 1-3 N, O or S; m = 0-4; and n = 0-3; provided that when the 2 N atoms of the imidazol ring are substituted, the imidazole moiety becomes a cationic imidazolium moiety. An Independent claim is also included for the preparation of (I).

64. 发明专利

NO20031219L 未知
公开(公告)号：NO20031219L
公开(公告)日：2003-09-19
申请号：NO20031219
申请日：2003-03-17
申请人： SERVIER LAB
发明人： GOLDSTEIN SOLO , DHAINAUT ALAIN , TIZOT ANDRE , FAUCHERE JEAN-LUC , KUCHARCZYK NATHALIE , HICKMAN JOHN , PIERRE ALAIN , TUCKER GORDON , KRAUS-BERTHIER LAURENCE
IPC分类号： C07D401/06 , A61K31/517 , A61P9/00 , A61P25/00 , A61P35/00 , C07D401/14 , C07D403/06 , C07D407/14 , C07D409/14 , C07D521/00
摘要： Quinazoline derivatives (I) are new. Quinazoline derivatives of formula (I), their enantiomers, diastereomers and salts are new. A = bond, 1-6C alkylene, 2-6C alkenylene, 2-6C alkynylene, T, A1-T, T-A1, A1-T-A1, or A1-T-A'1-T'; T, T' = carbonyl, carbonyloxy, thio, sulfirylsulfonyl, oxy, amino, 1-6C aminoalkyl, aminoaryl, carbonylamino, carbonylamino-1-6C alkyl, carbonylaminoaryl, oxycarbonyl, aminocarbonyl, 1-6C aminoalkylcarbonyl, aminoarylcarbonyl, sulfonylamino, sulfonylamino-1-6C alkyl, sulfonylaminoaryl, aminosulfonyl, amino-1-6C alkylsulfonyl or aminoarylsulfonyl; A1, A'1 = 1-6C alkylene, 2-6C alkenylene or 2-6C alkynylene; B = 1-6C alkyl, aryl, 3-10C cycloalkyl, Het1, Het2, arylaminoaryl or aryl-1-6C alkylaryl (all optionally substituted by 1-3 Z); D = 1-6C alkylene (where 1 C atom may be substituted by B); X = O or S; Z, R1 = halo, 1-6C alkyl, 1-6C alkoxy, OH, SH, CN, NO2, NH2, 1-6C alkylamino, di-1-6C alkylamino, 1-4C perhaloalkyl, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C alkylaminocarbonyl, di-1-6C alkylaminocarbonyl, carbamoyl or 1-6C alkoxycarbonylamino; R2 = H, or 1-6C alkyl, aryl, 3-10C cycloalkyl, Het1, Het2, aryl-1-6C alkyl or Het2-1-6C alkyl-3-10C cycloalkyl-1-6C alkyl or Het1-1-6C alkyl (all optionally substituted by halo, 1-6C alkyl, 1-6C alkoxy, OH, SH, CN, NO2, NH2, 1-6C alkylamino, di-1-6C alkylamino, 1-4C perhaloalkyl, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C alkylaminocarbonyl, di-1-6C alkylaminocarbonyl, carbamoyl, 1-6C alkoxycarbonylamino, or aryl-1-6C alkyl or arylamino (both optionally substituted by 1-3 Z)); aryl = phenyl, naphthyl or biphenyl; Het1 = 5-7 membered saturated or partially unsaturated mono- or polycyclic heterocycloalkyl containing 1-3 N, O or S atoms; Het2 = 5-11 membered mono- or bicyclic aromatic ring containing 1-3 N, O or S; m = 0-4; and n = 0-3; provided that when the 2 N atoms of the imidazol ring are substituted, the imidazole moiety becomes a cationic imidazolium moiety. An Independent claim is also included for the preparation of (I).

65. 发明专利

HK1052172A1 New indenoindolone compounds, a process for their preparation and pharmaceutical compositions containing them. 未知
公开(公告)号：HK1052172A1
公开(公告)日：2003-09-05
申请号：HK03102396
申请日：2003-04-03
申请人： SERVIER LAB
发明人： WIERZBICKI MICHEL , BOUSSARD MARIE-FRANCOISE , ROUSSEAU ANNE , ATASSI GHANEM , HICKMAN JOHN , PIERRE ALAIN , LEONCE STEPHANE , GUILBAUD NICOLAS , KRAUS-BERTHIER LAURENCE
IPC分类号： 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 , A61P
摘要： 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).

66. 发明专利

NO20031219D0 未知
公开(公告)号：NO20031219D0
公开(公告)日：2003-03-17
申请号：NO20031219
申请日：2003-03-17
申请人： SERVIER LAB
发明人： GOLDSTEIN SOLO , DHAINAUT ALAIN , TIZOT ANDRE , FAUCHERE JEAN-LUC , KUCHARCZYK NATHALIE , HICKMAN JOHN , PIERRE ALAIN , TUCKER GORDON , KRAUS-BERTHIER LAURENCE
IPC分类号： C07D401/06 , A61K31/517 , A61P9/00 , A61P25/00 , A61P35/00 , C07D401/14 , C07D403/06 , C07D407/14 , C07D409/14 , C07D521/00
摘要： Quinazoline derivatives (I) are new. Quinazoline derivatives of formula (I), their enantiomers, diastereomers and salts are new. A = bond, 1-6C alkylene, 2-6C alkenylene, 2-6C alkynylene, T, A1-T, T-A1, A1-T-A1, or A1-T-A'1-T'; T, T' = carbonyl, carbonyloxy, thio, sulfirylsulfonyl, oxy, amino, 1-6C aminoalkyl, aminoaryl, carbonylamino, carbonylamino-1-6C alkyl, carbonylaminoaryl, oxycarbonyl, aminocarbonyl, 1-6C aminoalkylcarbonyl, aminoarylcarbonyl, sulfonylamino, sulfonylamino-1-6C alkyl, sulfonylaminoaryl, aminosulfonyl, amino-1-6C alkylsulfonyl or aminoarylsulfonyl; A1, A'1 = 1-6C alkylene, 2-6C alkenylene or 2-6C alkynylene; B = 1-6C alkyl, aryl, 3-10C cycloalkyl, Het1, Het2, arylaminoaryl or aryl-1-6C alkylaryl (all optionally substituted by 1-3 Z); D = 1-6C alkylene (where 1 C atom may be substituted by B); X = O or S; Z, R1 = halo, 1-6C alkyl, 1-6C alkoxy, OH, SH, CN, NO2, NH2, 1-6C alkylamino, di-1-6C alkylamino, 1-4C perhaloalkyl, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C alkylaminocarbonyl, di-1-6C alkylaminocarbonyl, carbamoyl or 1-6C alkoxycarbonylamino; R2 = H, or 1-6C alkyl, aryl, 3-10C cycloalkyl, Het1, Het2, aryl-1-6C alkyl or Het2-1-6C alkyl-3-10C cycloalkyl-1-6C alkyl or Het1-1-6C alkyl (all optionally substituted by halo, 1-6C alkyl, 1-6C alkoxy, OH, SH, CN, NO2, NH2, 1-6C alkylamino, di-1-6C alkylamino, 1-4C perhaloalkyl, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C alkylaminocarbonyl, di-1-6C alkylaminocarbonyl, carbamoyl, 1-6C alkoxycarbonylamino, or aryl-1-6C alkyl or arylamino (both optionally substituted by 1-3 Z)); aryl = phenyl, naphthyl or biphenyl; Het1 = 5-7 membered saturated or partially unsaturated mono- or polycyclic heterocycloalkyl containing 1-3 N, O or S atoms; Het2 = 5-11 membered mono- or bicyclic aromatic ring containing 1-3 N, O or S; m = 0-4; and n = 0-3; provided that when the 2 N atoms of the imidazol ring are substituted, the imidazole moiety becomes a cationic imidazolium moiety. An Independent claim is also included for the preparation of (I).

67. 发明专利

CA2389766A1 NOUVEAUX DERIVES D'INDENOINDOLONES, LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT 未知
公开(公告)号：CA2389766A1
公开(公告)日：2002-12-13
申请号：CA2389766
申请日：2002-06-13
申请人： SERVIER LAB
发明人： ROUSSEAU ANNE , HICKMAN JOHN , ATASSI GHANEM , LEONCE STEPHANE , GUILBAUD NICOLAS , WIERZBICKI MICHEL , BOUSSARD MARIE-FRANCOISE , PIERRE ALAIN , KRAUS-BERTHIER LAURENCE
IPC分类号： C07D209/80 , A61K31/403 , A61K31/433 , A61K31/4439 , A61P35/00 , C07D209/94 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D491/04 , C07D491/056 , C07D209/56
摘要： L'invention concerne de nouveaux composés répondant à la formule (I) (see Formula I) dans laquelle R représente un atome d'hydrogène ou un groupement alkyle éventuellement substitué ou alkényle; R1 à R8, identiques ou différents, représentent chacu n un atome d'hydrogène ou un groupement alkyle éventuellement substitué, hydroxy, acyloxy, amino éventuellement subsitué, carboxy, alkoxy éventuellement subsitué ou alkényloxy, ou bien l'un des groupements R1 à R8 forme avec un autre groupement R1 à R8 contigu un groupement alkylènedioxy; X représente un atome d'oxygène ou un groupement NR16 dans lequel R16 représente un atome d'hydrogène ou un groupement alkyle, ary le ou arylalkyle; et R9 représente un atome d'hydrogène, un groupement aryle ou hétéroaryle ou un groupement alkyle saturé ou insaturé, éventuellement substitué. L'inventi on vise également les isomères des composés de formule (I), ainsi que leurs sels d'addition à un acide ou à une base pharmaceutiquement acceptable. Les composés selon l'invention sont utiles comme médicaments pour le traitement de cancers.

68. 发明专利

CA2448197A1 DERIVES TRICYCLIQUES DE DIHYDROQUINOLEINES, LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT 未知
公开(公告)号：CA2448197A1
公开(公告)日：2002-11-28
申请号：CA2448197
申请日：2002-05-22
申请人： SERVIER LAB
发明人： HICKMAN JOHN , RENARD PIERRE , KRAUS-BERTHIER LAURENCE , PIERRE ALAIN , PFEIFFER BRUNO , HUSSON HENRI-PHILIPPE , GIORGI-RENAULT SYLVIANE , DESBENE STEPHANIE
IPC分类号： A61K31/4741 , A61K31/4743 , A61K31/4745 , A61K31/661 , A61P35/00 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/056 , C07D491/14 , C07D497/04 , C07F9/60 , C07F9/6561 , C07D495/04
摘要： Composé de formule (I): dans laquelle: représente une liaison simple ou double, représente un cycle choisi parmi - R9a,R9b,R9c, X et Y sont tels que définis dans la description, R1 représente un groupement choisi parmi hydrogène, aryle, hétéroaryle, cycloalkyle, alkyle éventuellement substitué, et COR11 dans lequel R11 est tel que défini dans la description, R2 à R8 représentent chacun un groupement choisi parmi hydrogène, halogène, hydroxy, polyhalogénoalkyle, nitro, alkyle éventuellement substitué, amino éventuellement substitué, alkoxy éventuellement substitué, -OPO(OH)2 et dans laquelle m représente un entier tel que 1

69. 发明专利

NO20022794D0 未知
公开(公告)号：NO20022794D0
公开(公告)日：2002-06-12
申请号：NO20022794
申请日：2002-06-12
申请人： SERVIER LAB
发明人： WIERZBICKI MICHEL , BOUSSARD MARIE-FRANCOISE , ROUSSEAU ANNE , ATASSI GHANEM , HICKMAN JOHN , PIERRE ALAIN , LEONCE STEPHANE , GUILBAUD NICOLAS , KRAUS-BERTHIER LAURENCE
IPC分类号： 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
摘要： 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).

70. 发明专利

DE60313012T2 未知
公开(公告)号：DE60313012T2
公开(公告)日：2007-12-27
申请号：DE60313012
申请日：2003-10-17
申请人： SERVIER LAB
发明人： COUDERT GERARD , LEPIFRE FRANCK , CAIGNARD DANIEL-HENRI , RENARD PIERRE , HICKMAN JOHN , PIERRE ALAIN , KRAUS-BERTHIER LAURENCE
IPC分类号： C07D498/04 , A61K31/535 , A61P35/00 , C07D265/38 , C07D497/04 , C07D497/14 , C07D498/14
摘要： Benzo(e)(1,4)oxazino(3,2-g)isoindole derivatives (I), and their enantiomers, diastereoisomers, N-oxides and addition salts with acids and bases are new. Benzo(e)(1,4)oxazino(3,2-g)isoindole derivatives of formula (I), and their enantiomers, diastereoisomers, N-oxides and addition salts with acids and bases are new W1 = atoms that complete phenyl or pyridyl; Z = hydrogen, halo, 1-6C alkyl or alkoxy (both optionally substituted by aryl), aryl, aryloxy or hydroxy; R1 = hydrogen, 1-6C alkyl, optionally substituted by aryl, aryl, COR5 or 1-6C alkylene, substituted by one or more of halo, cyano, OR6, NR6R7, COOR6, COR6 or CONHR6; R2 = hydrogen or -CH2CH2OR8; R3 and R4 = hydrogen, 1-6C alkyl, optionally substituted by aryl, or aryl, or together they complete a 5 or 6-membered, monocyclic heterocycle, optionally including an additional oxygen or nitrogen; n = 1-6; R5 = hydrogen, 1-6C alkyl or alkoxy, hydroxy, aryl, aryl(1-6C)alkyl or aryloxy; R6 and R7 = hydrogen, 1-6C alkyl, aryl(1-6C)alkyl or aryl, or together they complete a heterocycle as above; R8 = hydrogen, 1-6C alkyl, aryl, aryl(1-6C)alkyl, S(O)tR6 or -T1-R9; t = 0-2; T1 = 1-6C alkylene; R9 = halo, cyano, OR6, NR6R7, CHO, COOR6 or CONR6R7; and aryl = phenyl, naphthyl, di- or tetra-hydronaphthyl, indenyl or indanyl, all optionally substituted by one or more of halo, 1-6C (trihalo)alkyl or alkoxy, hydroxy or amino, optionally substituted by 1 or 2 1-6C alkyl. Independent claims are also included for the following:0041658 (1) methods for the preparation of (I); and (2) intermediates of formulae (X), (XI) and (XIV). Boc = tert-butoxycarbonyl; and Pg = Boc or phenoxycarbonyl.

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