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1. 发明申请

US20060247237A1 Macrocyclic quinazoline derivatives as antiproliferative agents 有权
公开(公告)号：US20060247237A1
公开(公告)日：2006-11-02
申请号：US10558007
申请日：2004-05-25
申请人： Eddy Jean Freyne , Timothy Perera , Peter Jacobus Buijnsters , Marc Willems , Gaston Diels , Werner Embrechts
发明人： Eddy Jean Freyne , Timothy Perera , Peter Jacobus Buijnsters , Marc Willems , Gaston Diels , Werner Embrechts
IPC分类号： A61K31/5377 , A61K31/519 , C07D487/22
CPC分类号： C07D498/06 , C07C229/16 , C07C229/40 , C07D239/88 , C07D239/93 , C07D239/94
摘要： The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents O, CH2, NH or S; in particular Z represents NH; Y represents —C3-9alkyl-, —C3-9alkenyl-, —C3-9alkynyl-, —C3-7alkyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4 alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-oxy-C1-5alkyl-, —C1-5alkyl NR13—, —C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-6alkyl-NH—CO—, —C1-3alkyl-NH—CS-Het20-, —C1-3alkyl-NH—CO-Het20, —C1-2alkyl-CO-Het21-CO—, -Het22-CH2—CO—NH—C1-3alkyl-, —CO—NH—C1-6alkyl-, —NH—CO—C1-6alkyl-, —CO—C1-7alkyl-, —C1-7alkyl-CO—, —C1-6alkyl-CO—C1-6alkyl-, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, C1-2alkyl-NR21—CH2—CO—NH—C1-3alkyl-, or NR22—CO—C1-3alkyl-NH—, X1 represents a direct bond, O or —O—C1-2alkyl-, CO, —CO—C1-2alkyl-, NR11, —NR11—C1-2alkyl-, —CH2—, —O—N═CH— or —C1-2alkyl-; X2 represents a direct bond, O, —O—C1-2alkyl-, CO, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl-, —CH2—, —O—N═CH— or —C1-2alkyl-. The growth inhibitory effect anti-tumour activity of the present compounds has been demonstrated in vitro, in enzymatic on the receptor tyrosine kinase EGFR.

2. 发明申请

US20060063789A1 Aminobenzamide derivatives as glycogen synthase kinase 3 beta inhibitors 审中-公开
标题翻译：氨基苯甲酰胺衍生物作为糖原合酶激酶3β抑制剂
公开(公告)号：US20060063789A1
公开(公告)日：2006-03-23
申请号：US10493446
申请日：2002-10-29
申请人： Eddy Jean Freyne , Peter Antonius , Marc Willems , Werner Johan , Paul Janssen , Paulus Joannes , Jan Heeres , Marc de Jonge , Lucien Koymans , Frederik Daeyaert , Michael Kukla , Hugo Gabriel , Bony Nuydens , Marc Mercken , Donald Ludovici , Herwig Janssen , Paul Maria , Graziella Janssen , Jasmine Werner , Maroussia Janssen , Theodora Arts
发明人： Eddy Jean Freyne , Peter Antonius , Marc Willems , Werner Johan , Paul Janssen , Paulus Joannes , Jan Heeres , Marc de Jonge , Lucien Koymans , Frederik Daeyaert , Michael Kukla , Hugo Gabriel , Bony Nuydens , Marc Mercken , Donald Ludovici , Herwig Janssen , Paul Maria , Graziella Janssen , Jasmine Werner , Maroussia Janssen , Theodora Arts
IPC分类号： A61K31/655 , A61K31/50 , A61K31/4965 , A61K31/513 , C07D241/18 , C07D239/47
CPC分类号： C07D239/42 , A61K31/506 , C07D239/47 , C07D239/48 , C07D239/50 , C07D403/12
摘要： This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C2-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21—C1-6alkyl; R21—O—; R21—S—; R21—C(═O)—; R21—S(═O)p—; R7—S(═O)p—; R7—S(═O)p—NH—; R21—S(═O)p—NH—; R7—C(═O)—; —NHC(═O)H; —C(═O)NHNH2; R7—C(═O)—NH—; R21—C(═O)—NH—; —C(═NH)R7; —C(═NH)R21; R4a or R4b each independently represent hydrogen, R8, —Y1—NR9—Y2—NR10R11, —Y1—NR9—Y1—R8, —Y1—NR9R10; provided that —X—R2 and/or R3 is other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.
摘要翻译：本发明涉及式的化合物

3. 发明申请

US20050176713A1 Amide derivatives as glycogen synthase kinase 3-beta inhibitors 有权
公开(公告)号：US20050176713A1
公开(公告)日：2005-08-11
申请号：US10493454
申请日：2002-10-29
申请人： Eddy Jean Freyne , Peter Jacobus Johannes Buijnsters , Marc Willems , Werner Constant Embrechts , Jean Fernand Lacrampe , Paul Adriaan Janssen , Herwig Josephus Janssen , Paul Janssen , Graziella Janssen , Jasmine Janssen , Maroussia Godelieve Janssen , Theodora Joanna Arts , Paulus Lewi , Jan Heeres , Marc de Jonge , Lucien Maria Koymans , Frederik Frans Daeyaert , Rony Nuydens , Marc Mercken
发明人： Eddy Jean Freyne , Peter Jacobus Johannes Buijnsters , Marc Willems , Werner Constant Embrechts , Jean Fernand Lacrampe , Paul Adriaan Janssen , Herwig Josephus Janssen , Paul Janssen , Graziella Janssen , Jasmine Janssen , Maroussia Godelieve Janssen , Theodora Joanna Arts , Paulus Lewi , Jan Heeres , Marc de Jonge , Lucien Maria Koymans , Frederik Frans Daeyaert , Rony Nuydens , Marc Mercken
IPC分类号： A61K31/44 , A61K31/4409 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P3/10 , A61P7/00 , A61P17/00 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07D213/81 , C07D213/82 , C07D239/42 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D407/12 , C07D413/12 , C07D413/14 , C07D417/12 , A61K31/655 , A61K31/4965
CPC分类号： C07D213/81 , C07D213/82 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C2-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21-C1-6alkyl; R21—O—; R21—S—; R21—C(═O)—; R21—S(═O)p—; R7—S(═O)p—; R7—S(═O)p—NH—; R21—S(═O)p—NH—; R7—C(═O)—; —NHC(═O)H; —C(═O)NHNH2; R7—C(═O)—NH—; R21—C(═O)—NH—; —C(═NH)R7; —C(═NH)R21; R4a or R4b each independently represent hydrogen, R8, —Y1—NR9—Y2—NR10R11, —Y1—NR9—Y1—R8, —Y1—NR9R10; provided that —X—R2 and/or R3 is other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.

4. 发明授权

US06656959B1 PDE IV inhibiting pyridine derivatives 有权
标题翻译： PDE IV抑制吡啶衍生物
公开(公告)号：US06656959B1
公开(公告)日：2003-12-02
申请号：US09647668
申请日：2000-09-29
申请人： Eddy Jean Freyne , Gaston Stanislas Diels , Maria Encarnacion Matesanz-Ballesteros , Adolfo Diaz-Martinez
发明人： Eddy Jean Freyne , Gaston Stanislas Diels , Maria Encarnacion Matesanz-Ballesteros , Adolfo Diaz-Martinez
IPC分类号： A61K3144
CPC分类号： C07D401/06
摘要： The present invention concerns pyridine derivatives having the formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein L is hydrogen; C1-6alkyl; C1-6alkyl carbonyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl; C3-6alkenyl; substituted C3-6alkenyl; piperidyl; substituted piperidyl; C1-6alkylsulfonyl or arylsulfonyl; —A—B— is —CR8═CR5— or—CHR4—CHR5—; D is O or NR6; R1 is a hydrogen or C1-4alkyl; R2 is hydrogen; halo; C1-6alkyl; trifluoromethyl; C3-6cycloalkyl; carboxyl; C1-4alkyl oxycarbonyl; C3-6cycloalkylaminocarbonyl; aryl; Het1; or substituted C1-6alkyl; or R2 is —O—R9 or —NH—R10; R3 is hydrogen, halo, hydroxy, C1-6alkyl or C1-6alkyloxy; or R2 and R1, or R2 and R3 taken together may form a bivalent radical; Q is disubstituted pyridine; R7 and R8 each independently are hydrogen; C1-6alkyl; difluoromethyl; trifluoromethyl; C3-6cyclo alkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; 6,7-dihydro-5H-cyclopentapyridyl; bicyclo[2.2.1]-2-heptenyl; bicyclo[2.2.1]heptanyl; C1-6alkylsulfonyl; arylsulfonyl; or substituted C1-10alkyl; having PDE IV and cytokine inhibiting activity. The invention also relates to processes for preparing the compounds of formula (I), pharmaceutical compositions thereof and their use as a medicament.
摘要翻译：本发明涉及具有N-氧化物形式的吡啶衍生物，其药学上可接受的加成盐和立体化学异构形式，其中L是氢; C 1-6烷基; C 1-6烷基羰基; C 1-6烷氧基羰基; 取代的C 1-6烷基; C 3-6烯基; 取代的C 3-6烯基; 哌啶基取代的哌啶基; C 1-6烷基磺酰基或芳基磺酰基; -A-B-是-CR 8 = CR 5 - 或-CHR 4 -CHR 5 - ; D是O或NR 6; R 1是氢或C 1-4烷基; R 2是氢; 光环; C 1-6烷基; 三氟甲基 C 3-6环烷基; 羧基; C 1-4烷氧基羰基; C 3-6环烷基氨基羰基; 芳基; Het <1>; 或取代的C 1-6烷基; 或R 2为-O-R 9或-NH-R 10; R 3是氢，卤素，羟基，C 1-6烷基或C 1-6烷氧基; 或R 2和R 1，或R 2和R 3一起可以形成二价基团; Q是二取代的吡啶; R 7和R 8各自独立地为氢; C 1-6烷基; 二氟甲基三氟甲基 C 3-6环烷基; 含有一个或两个选自氧，硫或氮的杂原子的饱和的5-，6-或7-元杂环; 双茚满 6,7-二氢-5H-环戊吡啶基; 双环[2.2.1] -2-庚烯基; 双环[2.2.1]庚基; C 1-6烷基磺酰基; 芳基磺酰基; 或取代的C 1-10烷基; 具有PDE IV和细胞因子抑制活性。本发明还涉及制备式（I）化合物，其药物组合物及其作为药物的用途的方法。

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