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1. 发明申请

WO2006106103A2 PREVENTION OF HIV-INFECTION 审中-公开
标题翻译：预防艾滋病毒感染
公开(公告)号：WO2006106103A2
公开(公告)日：2006-10-12
申请号：PCT/EP2006/061303
申请日：2006-04-04
申请人： TIBOTEC PHARMACEUTICALS LTD. , BAERT, Lieven, Elvire, Colette , LEWI, Paulus, Joannes , HEERES, Jan
发明人： BAERT, Lieven, Elvire, Colette , LEWI, Paulus, Joannes , HEERES, Jan
IPC分类号： A61K47/10 , A61K47/16 , A61P31/18 , A61K31/505
CPC分类号： A61K31/505 , A61K9/0019 , A61K47/10 , A61K47/16
摘要： This invention relates to the use of a parenteral formulation comprising the NNRTI TMC278 for the long term prevention of HIV infection in a subject at risk of being infected by HIV, which comprises the intermittent administration of the said formulation at long time intervals.
摘要翻译：本发明涉及包含NNRTI TMC278的肠胃外制剂在HIV感染风险的受试者中长期预防HIV感染的用途，其包括以长时间间隔间歇施用所述制剂。

2. 发明申请

WO2006079656A1 HIV INHIBITING 2-( 4-CYANOPHENYLAMINO) PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：艾滋病毒抑制2-（4-氰基苯胺）吡嗪衍生物
公开(公告)号：WO2006079656A1
公开(公告)日：2006-08-03
申请号：PCT/EP2006/050490
申请日：2006-01-27
申请人： TIBOTEC PHARMACEUTICALS LTD. , ARTS, Frank Xavier Jozef Herwig , HEERES, Jan , LEWI, Paulus Joannes , LEEMANS, Rudolf , MOENS, Luc Jozef Raphael
发明人： HEERES, Jan , LEWI, Paulus Joannes , LEEMANS, Rudolf , MOENS, Luc Jozef Raphael
IPC分类号： C07D239/50 , C07D239/48 , A61K31/505 , A61P31/18
CPC分类号： C07D239/50 , C07D239/48
摘要： HIV replication inhibitors of formula (I) pharmaceut ically acceptable addition salts or stereochemically isomeric forms thereof, wherein X is NR 4 , S, SO or SO 2 ; the preparation of these compounds as well as pharmaceutical compositions comprising these compounds; the use of these compounds for the prevention or the treatment of HIV infection.
摘要翻译：式（I）的HIV复制抑制剂药学上可接受的加成盐或其立体化学异构形式，其中X为NR 4，S，SO或SO 2; 这些化合物的制备以及包含这些化合物的药物组合物; 使用这些化合物预防或治疗艾滋病毒感染。

3. 发明申请

WO2006035068A2 HIV INHIBITING 5-CARBO- OR HETEROCYCLIC SUBSTITUTED PYRIMIDINES 审中-公开
标题翻译：艾滋病毒抑制5-碳环或杂环取代的吡咯啉
公开(公告)号：WO2006035068A2
公开(公告)日：2006-04-06
申请号：PCT/EP2005/054931
申请日：2005-09-29
申请人： TIBOTEC PHARMACEUTICALS LTD. , GUILLEMONT, Jerôme, Emile, Georges , HEERES, Jan , LEWI, Paulus Joannes
发明人： GUILLEMONT, Jerôme, Emile, Georges , HEERES, Jan , LEWI, Paulus Joannes
IPC分类号： C07D239/48 , C07D401/12 , C07D417/12 , C07D405/12 , C07D409/12 , C07D403/12 , C07D413/14 , A61K31/505
CPC分类号： C07D403/12 , C07D239/48 , C07D239/50 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/14 , C07D417/12
摘要： HIV replication inhibitors of formula (I) N -oxides, a pharmaceutically acceptable addition salts, a quaternary amines or a stereoisomeric forms thereof, wherein -a 1 =a 2 -a 3 =a 4 - is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH- CH=N-, -N=N-CH=CH-; -b 1 =b 2 -b 3 =b 4 - is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH-CH=N-, -N=N-CH=CH-; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; optionally subst ituted C 1-6 alkyl; C 1-6 alkyloxycarbonyl; R 2 is OH; halo; optionally substituted C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalo methylt hio; -S(=O)rR 6 ; C(=NH)R 6 ; R 2a is CN; amino; substituted amino; optionally subst ituted C 1-6 alkyl; halo; optionally substituted C 1-6 alkyloxy; substituted carbonyl; -CH=N-NH-C(=O)-R 16 ; optionally substituted C 1-6 alkyloxy C 1-6 alkyl; substituted C 2-6 alkenyl or C 2-6 alkynyl; -C(=N-O-R 8 )-C 1-4 alkyl; R 7 or -X 3 -R 7 ; X 1 is -NR 1 -, -O-, -C(=O)-, CH 2 , -CHOH-, -S-, -S(=O) r -; R 3 is CN; amino; C 1-6 alkyl; halo; optionally substituted C 1-6 alkyloxy; substituted carbonyl; -CH=N-NH-C(=O)-R 16 ; substituted C 1-6 alkyl; optionally substituted C 1-6 alkyloxy C 1-6 alkyl; substituted C 2-6 alkenyl or C 2-6 alkynyl; -C(=N-O-R 8 )-C 1-4 alkyl; R 7 ; -X 3 -R 7 ; R 4 is halo; OH; optionally substituted C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl; C 3-7 cycloalkyl; C 1-6 alkyloxy; CN; nitro; polyhalo C 1-6 alkyl; polyhalo C 1-6 alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C 1-4 alkyl)amino or R 7 ; R 5 is-Y-C q H2 q -L or -C q H 2q -Y-C r H 2r -L; L is aryl or Het; processes for the preparation of these compounds, pharmaceut ical compositions comprising these compounds as active ingredient and the use of these compounds for the prevention or the treatment of HIV infection.
摘要翻译：式（I）的HIV复制抑制剂

4. 发明申请

WO2006035069A1 HIV INHIBITING 5-SUBSTITUTED PYRIMIDINES 审中-公开
标题翻译：艾滋病毒抑制5-取代的吡咯烷酮
公开(公告)号：WO2006035069A1
公开(公告)日：2006-04-06
申请号：PCT/EP2005/054932
申请日：2005-09-29
申请人： TIBOTEC PHARMACEUTICALS Ltd. , GUILLEMONT, Jerôme, Emile, Georges , HEERES, Jan , LEWI, Paulus Joannes
发明人： GUILLEMONT, Jerôme, Emile, Georges , HEERES, Jan , LEWI, Paulus Joannes
IPC分类号： C07D239/48 , C07D239/50 , A61K31/505 , A61P31/18
CPC分类号： C07D239/48 , C07D239/50
摘要： HIV replication inhibitors of formula (I) a N -oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A is -CH 2 -CH 2 - , -CH=CH- , -C≡C- ; R 1 is hydrogen, aryl, formyl, C 1-6 alkylcarbonyl, C 1-6 alkyl, C 1-6 alkyloxycarbonyl, R 2 hydroxy, halo, C 1-6 alkyl, carboxyl, cyano, -C(=O)R 6 , nitro, amino, mono- or di(C 1-6 alkyl)amino, polyhalomethyl; X 1 is -NR 1 -, -O-, -S-, -S(=O) p- ; R 3 is H, C 1-6 alkyl, halo ; R 4 is H, C 1-6 alkyl, halo ; R 5 is nitro, amino, mono- and diC 1-4 alkylamino, aryl, halo, -CHO, -CO-R 6 , -COOR 7 , -NH-C(=O)H, -NH-C(=O)R 6 , -CH=N-O-R 8 ; R 6 is C 1-4 alkyl, amino, mono- or di(C 1-4 alkyl)amino or polyhaloC 1-4 alkyl; R 7 is hydrogen, C 1-6 alkyl, arylC 1-6 alkyl; R 8 is hydrogen, C 1-6 alkyl, aryl; p is 1 or 2; aryl is optionally substituted phenyl; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.
摘要翻译：式（I）的HIV复制抑制剂N-氧化物，药学上可接受的加成盐，季胺或其立体化学异构体形式，其中A为-CH 2 -CH 2，， - CH = CH - ， - C = C-; R 1是氢，芳基，甲酰基，C 1-6烷基羰基，C 1-6烷基，C 1-6烷基，烷基氧基羰基，R 2羟基，卤素，C 1-6烷基，羧基，氰基，-C（= O）R 6，，硝基，氨基，一或二（C 1-6烷基）氨基，多卤代甲基; X 1是-NR 1 - ， - O - ， - S - ， - S（= O）p - 。 R 3是H，C 1-6烷基，卤素; R 4是H，C 1-6烷基，卤素; R 5是硝基，氨基，单和二C 1-4烷基氨基，芳基，卤素，-CHO，-CO-R 6， -COOR 7，-NH-C（= O）H，-NH-C（= O）R 6，-CH = NOR 8 >; R 6是C 1-4烷基，氨基，单或二（C 1-4烷基）氨基或多卤代1 -4 烷基; R 7是氢，C 1-6烷基，芳基C 1-6烷基; R 8是氢，C 1-6烷基，芳基; p为1或2; 芳基是任选取代的苯基; 含有这些化合物作为活性成分的药物组合物和制备所述化合物和组合物的方法。

5. 发明申请

WO2006045828A1 HIV INHIBITING BICYCLIC PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：艾滋病毒抑制双环吡啶衍生物
公开(公告)号：WO2006045828A1
公开(公告)日：2006-05-04
申请号：PCT/EP2005/055589
申请日：2005-10-27
申请人： TIBOTEC PHARMACEUTICALS LTD. , ARTS, Frank Xavier Jozef Herwig , GUILLEMONT, Jerôme Emile Georges , PAUGAM, Mikaël , DELEST, Bruno François Marie , HEERES, Jan , LEWI, Paulus Joannes
发明人： GUILLEMONT, Jerôme Emile Georges , PAUGAM, Mikaël , DELEST, Bruno François Marie , HEERES, Jan , LEWI, Paulus Joannes
IPC分类号： C07D487/04 , C07D473/00 , A61K31/52 , A61P31/18
CPC分类号： C07D487/04 , C07D473/00 , C07D473/16 , C07D473/24 , C07D473/34
摘要： HIV replication inhibitors of formula (I) N -oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein -a 1 =a 2 -a 3 =a 4 - is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH- CH=N-, -N=N-CH=CH-; -b 1 =b 2 -b 3 =b 4 - is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH-CH=N-, -N=N-CH=CH-; n and m is 0, 1, 2, 3 and in certain cases also 4; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; optionally substituted C 1-6 alkyl; C 1-6 alkyloxycarbonyl; R 2 is OH; halo; optionally substituted C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; -S(=O) p R 6 ; C(=NH)R 6 ; R 2a is CN; amino; substituted amino; optionally substituted C 1-6 alkyl; halo; optionally substituted C 1-6 alkyloxy; substituted carbonyl; -CH=N-NH-C(=O)-R 16 ; optionally substituted C 1-6 alkyloxyC 1-6 alkyl; substituted C 2-6 alkenyl or C 2-6 alkynyl; -C(=N-O-R 8 )-C 1-4 alkyl; R 7 or -X-R 7 ; R 3 is CN; amino; C 1-6 alkyl; halo; optionally substituted C 1-6 alkyloxy; substituted carbonyl; -CH=N-NH-C(=O)-R 16 ; substituted C 1-6 alkyl; optionally substituted C 1-6 alkyloxyC 1-6 alkyl; substituted C 2-6 alkenyl or C 2-6 alkynyl; -C(=N-O-R 8 )-C 1-4 alkyl; R 7 ; -X-R 7 ; R 4 is halo; OH; optionally substituted C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl; C 3-7 cycloalkyl; C 1-6 alkyloxy; CN; nitro; polyhaloC 1-6 alkyl; polyhaloC 1-6 alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C 1-4 alkyl)amino or R 7 ; -A-B- is -CR 5 =N-, -N=N-, -CH 2 -CH 2 -, -CS-NH-, -CO-NH-, -CH=CH-; pharmaceutical compositions comprising these; methods for the preparation of these compounds and compositions; the use of these compounds for the prevention or the treatment of HIV infection.
摘要翻译：式（I）的HIV复制抑制剂N-氧化物，药学上可接受的加成盐，季胺或其立体异构形式，其中-i-1-a-O- 是-CH = CH-CH = CH-，-N = CH-CH = CH-，-N = CH-N = CH - ， - N = CH-CH = N-，-N = N-CH = CH-; b = 1〜3 = b 4 - 是-CH = CH-CH = CH - ，-N = CH-CH = CH-，-N = CH-N = CH-，-N = CH-CH = N-，-N = N-CH = CH-; n和m是0,1,2,3，在某些情况下也是4; R 1是氢; 芳基; 甲酰基; ç_{1-6 烷基羰基; 任选取代的C 1-6烷基; ç_{1-6 烷氧基羰基; R 2是OH; 光环; 任选取代的C 1-6烷基，C 2-6链烯基或C 2-6-6炔基; 取代的羰基; 羧基; CN; 硝基; 氨基; 取代氨基; 多卤代; polyhalomethylthio; -S（= O）p 6 C（= NH）R ^{6 ; R 2a是CN; 氨基; 取代氨基; 任选取代的C 1-6烷基; 光环; 任选取代的C 1-6烷氧基; 取代的羰基; -CH = N-NH-C（= O）-R ^{16 ; 任选取代的C 1-6烷氧基C 1-6烷基; 取代的C 2-6烯基或C 2-6亚炔基; -C（= N-O-R 8）-C 1-4烷基; R 7或-X-R 7; R 3是CN; 氨基; ç_{1-6 烷基; 光环; 任选取代的C 1-6烷氧基; 取代的羰基; -CH = N-NH-C（= O）-R ^{16 ; 取代的C 1-6烷基; 任选取代的C 1-6烷氧基C 1-6烷基; 取代的C 2-6烯基或C 2-6亚炔基; -C（= N-O-R 8）-C 1-4烷基; [R ^{7 ; -X-R ^{7 ; R 4是卤素; 哦; 任选取代的C 1-6烷基，C 2-6链烯基或C 2-6-6炔基; ç_{3-7 环烷基; ç_{1-6 烷氧基; CN; 硝基; 多卤代_{1-6 烷基; 多卤代_{1-6 烷氧基; 取代的羰基; 甲酰基; 氨基; 单或二（C 1-4烷基）氨基或R 7; -AB-是-CR 5 = N-，-N = N-，-CH 2 -CH 2 - ， - C-NH - ， - CO-NH-， - CH = CH-; 包含它们的药物组合物; 制备这些化合物和组合物的方法; 使用这些化合物来预防或治疗艾滋病毒感染。}}}}}}}}}}}}

6. 发明申请

WO2006035067A2 HIV INHIBITING 5-HETEROCYCLYL PYRIMIDINES 审中-公开
标题翻译：艾滋病毒抑制5-杂环亚氨基嘧啶
公开(公告)号：WO2006035067A2
公开(公告)日：2006-04-06
申请号：PCT/EP2005/054930
申请日：2005-09-29
申请人： TIBOTEC PHARMACEUTICALS LTD. , GUILLEMONT, Jerôme, Emile, Georges , HEERES, Jan , LEWI, Paulus, Joannes
发明人： GUILLEMONT, Jerôme, Emile, Georges , HEERES, Jan , LEWI, Paulus, Joannes
IPC分类号： C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14
CPC分类号： C07D405/04 , C07D401/04 , C07D403/04 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04
摘要： HIV replication inhibitors of formula (I), N -oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein -a 1 =a 2 -a 3 =a 4 - is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH-CH=N-, -N=N-CH=CH-; -b 1 =b 2 -b 3 =b 4 - is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH-CH=N-, -N=N-CH=CH-; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; optionally substituted C 1-6 alkyl; C 1-6 alkyloxycarbonyl; R 2 is OH; halo; optionally substituted C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; -S(=O) P R 6 ; C(=NH)R 6 ; R 2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C 1-6 alkyloxy; substituted carbonyl; -CH=N-NH-C(O)-R 16 ; optionally substituted C 1-6 alkyloxyC 1-6 alkyl; substituted C 2-6 alkenyl or C 2-6 alkynyl; -C(=N-O-R 8 )-C 1-4 alkyl; R 7 or -X 3 -R 7 ; X 1 is -NR 1 -, -O-, -C(=O)-, -CH 2 -, -CHOH-, -S-, -S(=O) P - R 3 is CN; amino; C 1-6 alkyl; halo; optionally substituted C 1-6 alkyloxy; substituted carbonyl; -CH=N-NH-C(O)-R 16 ; substituted C 1-6 alkyl; optionally substituted C 1-6 alkyloxyC 1-6 alkyl; substituted C 2-6 alkenyl or C 2-6 alkynyl; -C(=N-O-R 8 )-C 1-4 alkyl; R 7 ; -X 3 -R 7 ; R 4 is halo; OH; optionally substituted C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl; C 3-7 cycloalkyl; C 1-6 alkyloxy; CN; nitro; polyhaloC 1-6 alkyl; polyhaloC 1-6 alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C 1-4 alkyl)amino or R 7 ; R 5 is a 5- or 6-membered completely unsaturated ring system wherein 1 - 4 ring members are nitrogen, oxygen or sulfur; which ring may optionally be substituted and may optionally be annelated with a benzene ring; methods for their preparation and pharmaceutical compositions comprising them. The invention also relates to the use of these compounds for the prevention or the treatment of HIV infection.
摘要翻译：式（I）的HIV复制抑制剂，

7. 发明申请

WO2004074262A1 HIV REPLICATION INHIBITING PYRIMIDINES AND TRIAZINES 审中-公开
标题翻译：艾滋病毒复制抑制吡嗪和三氮唑
公开(公告)号：WO2004074262A1
公开(公告)日：2004-09-02
申请号：PCT/EP2004/050177
申请日：2004-02-20
申请人： TIBOTEC PHARMACEUTICALS Ltd. , ARTS, Frank, Xavier, Jozef, Herwig , ARTS, Theodora , GUILLEMONT, Jerôme, Emile, Georges , PASQUIER, Elisabeth, Thérese, Jeanne , HEERES, Jan , HERTOGS, Kurt , BETTENS, Eva , LEWI, Paulus, Joannes , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , DAEYAERT, Frederik, Frans, Desiré , VINKERS, Hendrik, Maarten
发明人： GUILLEMONT, Jerôme, Emile, Georges , PASQUIER, Elisabeth, Thérese, Jeanne , HEERES, Jan , HERTOGS, Kurt , BETTENS, Eva , LEWI, Paulus, Joannes , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , DAEYAERT, Frederik, Frans, Desiré , VINKERS, Hendrik, Maarten
IPC分类号： C07D239/47
CPC分类号： C07D239/47 , C07D239/48 , C07D413/12
摘要： This invention concerns HIV replication inhibitors of formula (I), The N -oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）的N-复制抑制剂，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，它们作为药物的用途，其制备方法和包含它们的药物组合物。

8. 发明申请

WO2004074261A1 HIV REPLICATION INHIBITING PYRIMIDINES AND TRIAZINES 审中-公开
标题翻译：艾滋病毒复制抑制吡嗪和三氮唑
公开(公告)号：WO2004074261A1
公开(公告)日：2004-09-02
申请号：PCT/EP2004/050175
申请日：2004-02-20
申请人： TIBOTEC PHARMACEUTICALS Ltd. , ARTS, Frank, Xavier, Jozef, Herwig , ARTS, Theodora , GUILLEMONT, Jerôme, Emile, Georges , PASQUIER, Elisabeth, Thérese, Jeanne , HEERES, Jan , HERTOGS, Kurt , BETTENS, Eva , LEWI, Paulus, Joannes , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , DAEYAERT, Frederik, Frans, Desiré , VINKERS, Hendrik, Maarten
发明人： GUILLEMONT, Jerôme, Emile, Georges , PASQUIER, Elisabeth, Thérese, Jeanne , HEERES, Jan , HERTOGS, Kurt , BETTENS, Eva , LEWI, Paulus, Joannes , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , DAEYAERT, Frederik, Frans, Desiré , VINKERS, Hendrik, Maarten
IPC分类号： C07D239/47
CPC分类号： C07D239/47 , C07D239/48 , C07D413/12
摘要： This invention concerns HIV replication inhibitors of formula (I), the N -oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）的HIV复制抑制剂，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，其作为药物的用途，其制备方法和包含它们的药物组合物。

9. 发明申请

WO2006079642A1 ANTHELMINTIC IMIDAZOL-THIAZOLE DERIVATES 审中-公开
标题翻译：苯丙咪唑 - 噻唑衍生物
公开(公告)号：WO2006079642A1
公开(公告)日：2006-08-03
申请号：PCT/EP2006/050460
申请日：2006-01-26
申请人： JANSSEN PHARMACEUTICA N.V. , ARTS, Frank Xavier Jozef Herwig , HEERES, Jan , LEWI, Paulus, Joannes , VLAMINCK, Kathleen Marie Jeanne Alice , OTTEVAERE, Pierre Jozef Hektor Valère , VANPARIJS, Oscar Franz Joseph
发明人： HEERES, Jan , LEWI, Paulus, Joannes , VLAMINCK, Kathleen Marie Jeanne Alice , OTTEVAERE, Pierre Jozef Hektor Valère , VANPARIJS, Oscar Franz Joseph
IPC分类号： C07D513/04 , A61K31/429 , A61P33/10
CPC分类号： C07D513/04
摘要： The present invention relates to the novel anthelmintic compound tetrahydro-furan-2- carboxylic acid-[3-(2,3,5,6-tetrahydro-imidazo[2,1-b]thiazol-6-yl)-phenyl]-amide and the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, as well as pharmaceutical compositions comprising said novel compound, processes for preparing said compound and compositions, and the use thereof as a medicine, in particular in treatment, control and prevention of endo- and ectoparasite infections in warm-blooded animals.
摘要翻译：本发明涉及新的驱肠虫化合物四氢 - 呋喃-2-羧酸 - [3-（2,3,5,6-四氢 - 咪唑并[2,1-b]噻唑-6-基） - 苯基] 酰胺和其药学上可接受的酸加成盐及其立体化学异构形式，以及包含所述新化合物的药物组合物，制备所述化合物和组合物的方法及其作为药物的用途，特别是在治疗，控制和预防温血动物的内寄生虫和外寄生虫感染。

10. 发明申请

WO2003037891A1 HETEROARYL AMINES AS GLYCOGEN SYNTHASE KINASE 3BETA INHIBITORS (GSK3 INHIBITORS) 审中-公开
标题翻译：杂多胺作为糖原合成酶激酶3β抑制剂（GSK3抑制剂）
公开(公告)号：WO2003037891A1
公开(公告)日：2003-05-08
申请号：PCT/EP2002/012077
申请日：2002-10-29
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , LOVE, Christopher, John , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , VINKERS, Hendrik, Maarten , VAN AKEN, Koen, Jeanne, Alfons , DIELS, Gaston, Stanislas, Marcella
发明人： FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , LOVE, Christopher, John , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , VINKERS, Hendrik, Maarten , VAN AKEN, Koen, Jeanne, Alfons , DIELS, Gaston, Stanislas, Marcella
IPC分类号： C07D403/12
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 (I), 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; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; optionally substituted C 1-6 alkyl; C 1-6 alkyloxycarbonyl; optionally substituted C 1-6 alkyloxy C 1-6 alkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; R 2 is hydrogen, C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R 3 is hydrogen; hydroxy; halo; optionally substituted C 1-6 alkyl or C 1-6 alkenyl or C 2-6 alkynyl; C 1-6 alkyloxy; C 1-6 alkylthio; C 1-6 alkyloxycarbonyl; C 1-6 alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C 1-6 alkyl)amino; polyhaloC 1-6 alkyl; polyhaloC 1-6 alkyloxy; polyhaloC 1-6 alkylthio; R 21 ; R 21 -C 1-6 alkyl; R 21 -O-; R 21 -S-; R 21 -C(=0)-; R 21 -S(=0)p-; R 7 -S =O R 7 -S(=O)p-NH-; R 21 -S(=O)p-NH-; R 7 -C(=0)-; -NHC(=0)H; -C(=O)NHNH2; R 7 -C(=O)-NH-; R 21 -C(=O)-NH-; -C(=NH)R 7 ; -C(=NH)R 21 ; R° is an optionally substituted heterocycle provided that -X-R 2 and/or R 3 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（I）化合物，其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为6-元杂环; R 1是氢; 芳基; 甲酰基; ç<子> 1-6 烷基羰基; 任选取代的C 1-6烷基; ç<子> 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是直接键或连接基原子或基团; Z是直接键或连接基原子或基团; R 2是氢，C 1-10烷基，C 2-10烯基，C 2-10炔基，碳环或杂环，每个所述基团可以任选被取代; R 3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 1-6链烯基或C 2-6炔基; ç<子> 1-6 烷氧基; ç<子> 1-6 烷硫基; ç<子> 1-6 烷氧基羰基; ç<子> 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<子> 1-6 烷基; 多卤代<子> 1-6 烷氧基; 多卤代<子> 1-6 烷硫基; [R ^{21 ; [R ^{21 -C <子> 1-6 烷基; [R ^{21 -O-; [R ^{21 -S-; [R ^{21 -C（= O） - ; [R ^{21 -S（= O）p - ; R 7 -S = O 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＆度; 是任选取代的杂环，条件是-XR 2和/或R 3不为氢;它们的用途，包含它们的药物组合物及其制备方法。}}}}}}}}}}}}

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