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1. 发明申请

US20050004125A1 Heteroaryl amines as glycogen synthase kinase 3beta inhibitors (gsk3 inhibitors) 有权
标题翻译：杂芳基胺作为糖原合酶激酶3β抑制剂（gsk3抑制剂）
公开(公告)号：US20050004125A1
公开(公告)日：2005-01-06
申请号：US10493452
申请日：2002-10-29
申请人： Eddy Jean Edgard Freyne , Peter Jacobus Buijnsters , Marc Willems , Werner Embrechts , Christopher Love , Paul Janssen , Paulus Lewi , Jan Heeres , Marc de Jonge , Lucien Koymans , Hendrik Vinkers , Koen Van Aken , Gaston Diels
发明人： Eddy Jean Edgard Freyne , Peter Jacobus Buijnsters , Marc Willems , Werner Embrechts , Christopher Love , Paul Janssen , Paulus Lewi , Jan Heeres , Marc de Jonge , Lucien Koymans , Hendrik Vinkers , Koen Van Aken , Gaston Diels
IPC分类号： A61K31/435 , A61K31/4406 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P3/10 , A61P17/00 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/18 , A61P35/00 , A61P35/02 , C07D213/53 , C07D213/74 , C07D239/42 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , A61K31/4965
CPC分类号： C07D213/74 , C07D239/42 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , 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 is 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 a direct bond or a linker atom or group; 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; R4 is an optionally substituted heterocycle 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N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式，其中环A是6-元杂环; R 1是氢; 芳基; 甲酰基 C 1-6烷基羰基; 任选取代的C 1-6烷基; C 1-6烷氧基羰基; 任选取代的C 1-6烷氧基C 1-6烷基羰基; X是直接键或连接原子或基团; Z是直接键或连接原子或基团; R 2是氢，C 1-10烷基，C 2-10烯基，C 2-10炔基，碳环或杂环，所述基团中的每一个可任选被取代; R 3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 2-6烯基或C 2-6炔基; C 1-6烷氧基; C 1-6烷硫基; C 1-6烷氧基羰基; C 1-6烷基羰基氧基; 羧基; 氰基; 硝基氨基; 单或二（C 1-6烷基）氨基; 多卤代C 1-6烷基; 多卤代C 1-6烷氧基; 多卤代C 1-6烷硫基; R 21; R 21 -C 1-6烷基; R 21 -O- R 21 -S-; R 21 -C（= O） - ; R 21 -S（= O）p - ; R 7 -S（= O）p-; R 7 -S（= O）p-NH-; R 21 -S（= O）p -NH-; R 7 -C（= O） - ; -NHC（= O）H; -C（= O）NHNH 2; R 7 -C（= O）-NH-; R 21 -C（= O）-NH-; -C（= NH）R 7 -C（= NH）R 21; R 4是任选取代的杂环，条件是-X-R 2和/或R 3不是氢; 其用途，包含它们的药物组合物及其制备方法。

2. 发明申请

US20070299109A1 Dimeric Compounds Of Piperidine, Piperazine Or Morpholine Or Their 7-Membered Analogs Suitable For The Treatment Of Neurodegenerative Disorders 审中-公开
标题翻译：哌啶，哌嗪或吗啉或其7组分类似物的二聚体化合物适用于治疗神经退行性疾病
公开(公告)号：US20070299109A1
公开(公告)日：2007-12-27
申请号：US11632510
申请日：2005-07-13
申请人： Miroslav Cik , Gaston Diels , Guy Van Lommen
发明人： Miroslav Cik , Gaston Diels , Guy Van Lommen
IPC分类号： A61K31/445 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/28 , A61P43/00 , C07D221/00
CPC分类号： C07D211/58 , C07D401/12 , C07D403/12 , C07D409/12 , C07D417/12
摘要： Formula (I″), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof.
摘要翻译：式（I“），N-氧化物形式，其药学上可接受的加成盐及其立体化学异构形式。

3. 发明申请

US20070270588A1 Pyrrolopyrimidine Derivatives 审中-公开
标题翻译：吡咯并嘧啶衍生物
公开(公告)号：US20070270588A1
公开(公告)日：2007-11-22
申请号：US10591765
申请日：2005-03-04
申请人： Francois Bischoff , Ludo Kennis , Mirielle Braeken , Gaston Diels , Atsuro Nakazato
发明人： Francois Bischoff , Ludo Kennis , Mirielle Braeken , Gaston Diels , Atsuro Nakazato
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： According to the present invention, there is provided an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastro-intestinal diseases, drug dependence, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alpecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, pain, etc. A pyrrolopyrimidine derivative represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.
摘要翻译：根据本发明，提供了一种抗CRF受体的拮抗剂，其作为治疗或预防药物是有效的，其涉及CRF被认为涉及的疾病，例如抑郁症，焦虑症，阿尔茨海默氏病，帕金森病，亨廷顿氏舞蹈病，进食疾病，高血压，胃肠疾病，药物依赖，脑梗塞，脑缺血，脑水肿，头部外伤，炎症，免疫相关疾病，特异性，肠易激综合征，睡眠障碍，癫痫，皮肤病，精神分裂症，疼痛等由下式[I]表示的吡咯并嘧啶衍生物对CRF受体具有高亲和力，并且对于涉及CRF的疾病有效。

4. 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.

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