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1. 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。

2. 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

3. 发明申请

WO2005058870A1 AMINO-BENZIMIDAZOLES DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 审中-公开
标题翻译：氨基苯并咪唑衍生物作为呼吸道同种病毒复制的抑制剂
公开(公告)号：WO2005058870A1
公开(公告)日：2005-06-30
申请号：PCT/EP2004/053617
申请日：2004-12-20
申请人： TIBOTEC PHARMACEUTICALS LTD. , BONFANTI, Jean-François , ANDRIES, Koenraad, Jozef, Lodewijk , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , GUILLEMONT, Jerôme, Emile, Georges , LACRAMPE, Jean, Fernand, Armand
发明人： BONFANTI, Jean-François , ANDRIES, Koenraad, Jozef, Lodewijk , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , GUILLEMONT, Jerôme, Emile, Georges , LACRAMPE, Jean, Fernand, Armand
IPC分类号： C07D401/06
CPC分类号： C07D405/14 , C07D401/06 , C07D401/14
摘要： The present invention concerns amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula (I) their prodrugs, N -oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is Ar 1 or C 1-6 alkyl substituted with one or more substituents selected from trifluoromethyl, C 3-7 cycloalkyl, Ar 2 , hydroxy, C 1-4 alkoxy, C 1-4 alkylthio, Ar 2 -oxy-, Ar 2 -thio-, Ar 2 (CH2)„oxy, Ar 2 (CH 2 ) n thio, hydroxycarbonyl, aminocarbonyl, C 1-4 alkylcarbonyl, Ar 2 carbonyl, C 1-4 alkoxycarbonyl, Ar 2 (CH 2 ) n carbonyl, aminocarbonyloxy, C 1-4 alkylcarbonyloxy, Ar 2 carbonyloxy, Ar 2 (CH 2 ) n carbonyloxy, hydroxy-C 2- 4 -alkyloxy, C 1-4 alkoxycarbonyl(CH 2 ) n oxy, monoor di(C 1-4 alkyl)-aminocarbonyl, mono- or di(C 1-4 alkyl)aminocarbonyloxy, aminosulfonyl, mono- or di(C 1-4 alkyl)aminosulfonyl, dioxolanyl optionally substituted with one or two C 1-6 alkyl radicals, and a heterocycle selected from pyrrolidinyl, pyrrolyl, dihydropyrrolyl, thiazolidinyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, pyridyl and tetrahydropyridyl, which each may optionally be substituted with oxo or C 1 - 6 alkyl; G is a direct bond or optionally substituted C 1-10 alkanediyl R 1 is Ar 1 or a monocyclic or bicyclic heterocycle; one of R 2a and R 3a is C 1-6 alkyl and the other one of R 2 a and R 3a is hydrogen; in case R 2 a is different from hydrogen then R 2b is hydrogen or C 1-6 alkyl, and R 3b is hydrogen; in case R 3a is different from hydrogen then R 3b is hydrogen or C 1-6 alkyl, and R 2b is hydrogen; Ar 1 is phenyl or substituted phenyl and Ar 2 is phenyl or substituted phenyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.
摘要翻译：本发明涉及对呼吸道合胞病毒复制具有抑制活性的氨基苯并咪唑，其具有式（I）的前药，N-氧化物，加成盐，季胺，金属络合物和立体化学异构形式，其中Q为Ar1或C1 被一个或多个选自三氟甲基，C 3-7环烷基，Ar 2，羟基，C 1-4烷氧基，C 1-4烷硫基，Ar 2 - 氧基 - ，Ar 2 - 硫基 - ，Ar 2 （CH2）“氧基，Ar2（CH2）nthio，羟基羰基，氨基羰基，C1-4烷基羰基，Ar2羰基，C1-4烷氧基羰基，Ar2（CH2）n羰基，氨基羰基氧基，C1-4 烷基羰基氧基，Ar 2羰基氧基，Ar 2（CH 2）n - 羰基氧基，羟基-C 2 - 4-烷氧基，C 1-4烷氧基羰基（CH 2）n羟基，一或二（C 1-4烷基） - 氨基羰基，单或二 1-4烷基）氨基羰基氧基，氨基磺酰基，一或二（C 1-4烷基）氨基磺酰基，任选被一个或两个C 1-6烷基取代的二氧戊环，以及选自吡咯烷基，吡咯基，二氢吡咯基，噻唑烷基，咪唑基，三唑基，哌啶基，高哌啶基，哌嗪基，吡啶基和四氢吡啶基，其各自可以任选被氧代或C 1-6烷基取代; G是直接键或任选取代的C 1-10烷二基R 1是Ar 1或单环或双环杂环; R 2a和R 3a之一是C 1-6烷基，R 2 a和R 3a中的另一个是氢; 在R 2不同于氢的情况下，R 2b是氢或C 1-6烷基，R 3b是氢; 在R 3a不同于氢的情况下，R 3b是氢或C 1-6烷基，R 2b是氢; Ar 1是苯基或取代的苯基，Ar 2是苯基或取代的苯基。它还涉及它们的制备方法和包含它们的组合物，以及它们作为药物的用途。

4. 发明申请

WO2007113256A1 HIV INHIBITING 5-(HYDROXYMETHYLENE AND AMINOMETHYLENE) SUBSTITUTED PYRIMIDINES 审中-公开
标题翻译：艾滋病毒抑制5-（羟基乙烯和氨基乙烯）取代的吡啶
公开(公告)号：WO2007113256A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053113
申请日：2007-03-30
申请人： TIBOTEC PHARMACEUTICALS LTD. , GUILLEMONT, Jerôme, Emile, Georges , MORDANT, Céline, Isabelle , SCHMITT, Benoit, Antoine
发明人： GUILLEMONT, Jerôme, Emile, Georges , MORDANT, Céline, Isabelle , SCHMITT, Benoit, Antoine
IPC分类号： C07D417/06 , C07D401/06 , C07D239/48 , C07D403/06 , C07D513/04 , C07D417/14 , A61K31/506 , A61K31/5377 , A61P31/18
CPC分类号： C07D239/48 , C07D401/06 , C07D403/06 , C07D417/06 , C07D417/14 , C07D513/04
摘要： This invention concerns 5-(hydroxymethylene and aminomethylene)pyrimidine derivatives having HIV (Human Immunodeficiency Virus) replication inhibiting properties, to the preparation thereof and to pharmaceutical compositions comprising these compounds.
摘要翻译：本发明涉及具有HIV（人类免疫缺陷病毒）复制抑制性质的5-（羟基亚甲基和氨基亚甲基）嘧啶衍生物及其制备方法以及包含这些化合物的药物组合物。

5. 发明申请

WO2007113254A1 HIV INHIBITING 5-AMIDO SUBSTITUTED PYRIMIDINES 审中-公开
标题翻译：艾滋病毒抑制5-AMIDO替代吡咯烷酮
公开(公告)号：WO2007113254A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053111
申请日：2007-03-30
申请人： TIBOTEC PHARMACEUTICALS LTD. , GUILLEMONT, Jerôme, Emile, Georges , PAUGAM, Mikaël , DELEST, Bruno, François, Marie
发明人： GUILLEMONT, Jerôme, Emile, Georges , PAUGAM, Mikaël , DELEST, Bruno, François, Marie
IPC分类号： C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , A61K31/506 , A61P31/18
CPC分类号： C07D417/12 , C07D239/48 , C07D401/12 , C07D405/12 , C07D409/12
摘要： This invention concerns pyrimidine derivatives of formula having HIV (Human Immunodeficiency Virus) replication inhibiting properties, the preparation thereof and pharmaceutical compositions comprising these compounds.
摘要翻译：本发明涉及具有HIV（人类免疫缺陷病毒）复制抑制性质的式的嘧啶衍生物，其制备方法和包含这些化合物的药物组合物。

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

WO2005058873A1 PIPERIDINE-AMINO-BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 审中-公开
标题翻译：作为呼吸道同种病毒复制的抑制剂的哌啶 - 氨基苯并咪唑衍生物
公开(公告)号：WO2005058873A1
公开(公告)日：2005-06-30
申请号：PCT/EP2004/053606
申请日：2004-12-20
申请人： TIBOTEC PHARMACEUTICALS LTD. , BONFANTI, Jean-François , ANDRIES, Koenraad, Jozef, Lodewijk , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , GUILLEMONT, Jerôme, Emile, Georges , LACRAMPE, Jean, Fernand, Armand
发明人： BONFANTI, Jean-François , ANDRIES, Koenraad, Jozef, Lodewijk , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , GUILLEMONT, Jerôme, Emile, Georges , LACRAMPE, Jean, Fernand, Armand
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D417/14
摘要： The present invention concerns piperidine-amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula (I) their prodrugs, N -oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is C 1-6 alkyl optionally substituted with trifluorornethyl, C 3-7 cycloalkyl, Ar 2 , hydroxy, C 1-4 alkoxy, C 1-4 alkylthio, Ar 2 -oxy-, Ar 2 -thio-, Ar 2 (CH 2 ) n oxy, Ar 2 (CH 2 ) n thio, hydroxycarbonyl, aminocarbonyl, C 1-4 alkylcarbonyl, Ar 2 carbonyl, C 1-4 alkoxycarbonyl, Ar 2 (CH 2 ) n carbonyl, aminocarbonyloxy, C 1-4 alkylcarbonyloxy, Ar 2 carbonyloxy, Ar 2 (CH 2 ) n carbonyloxy, C 1-4 alkoxy carbonyl(CH 2 ) n oxy, mono- or di(C 1-4 alkyl)aminocarbonyl, mono- or di(C 1-4 alkyl)-aminocarbonyloxy, aminosulfonyl, mono-odi(C 1-4 alkyl)aminosulfonyl or a heterocycles selected from the group consisting of pyrrolidinyl, pyrrolyl, dihydropyrrolyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, pyridyl and tetrahydropyridyl, wherein each of said heterocycle may optionally be substituted with oxo or C 1-6 alkyl; G is a direct bond or optionally substituted C l-10 loalkanediyl; R 1 is Ar 1 or a monocyclic or bicyclic heterocycle; one of R 2a and R 3a is C 1-6 salkyl and the other one of R 2a and R 3a is hydrogen; in case R 2a is different from hydrogen then R 2b is hydrogen or C 1-6 alkyl, and R 3b is hydrogen; in case R 3a is different from hydrogen then R 3b is hydrogen or C 1-6 alkyl, and R 2b is hydrogen; t is 1, 2 or 3; Ar 1 is phenyl or substituted phenyl; and Ar 2 is phenyl or substituted phenyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.
摘要翻译：本发明涉及对呼吸道合胞病毒复制具有抑制活性的具有抑制活性的哌啶 - 氨基 - 苯并咪唑，其具有式（I）其前药，N-氧化物，加成盐，季胺，金属络合物和立体化学异构形式，其中Q为C1 任选被三氟甲基，C 3-7环烷基，Ar 2，羟基，C 1-4烷氧基，C 1-4烷硫基，Ar 2 - 氧基 - ，Ar 2 - 硫基 - ，Ar 2（CH 2）羟基羰基，氨基羰基，C 1-4烷基羰基，Ar 2羰基，C 1-4烷氧基羰基，Ar 2（CH 2）n羰基，氨基羰基氧基，C 1-4烷基羰基氧基，Ar 2羰基氧基， Ar 2（CH 2）n - 羰基氧基，C 1-4烷氧基羰基（CH 2）n羟基，单或二（C 1-4烷基）氨基羰基，单或二（C 1-4烷基） - 氨基羰基氧基，氨基磺酰基，单-O-（C 1-4烷基）氨基磺酰基或选自吡咯烷基，吡咯基，二氢吡咯基，咪唑基，三唑基，哌啶基，高哌啶基，哌嗪基，吗啉基，噻吩基吗啉基，1-氧代 - 硫代吗啉基，1,1-二氧代硫代吗啉基，吡啶基和四氢吡啶基，其中各个杂环可以任选地被氧代或C 1-6烷基取代; G是直接键或任选取代的Cl-10的亚烷基; R 1是Ar 1或单环或双环杂环; R 2a和R 3a之一是C 1-6烷基，R 2a和R 3a中的另一个是氢; 在R 2a不同于氢的情况下，R 2b是氢或C 1-6烷基，R 3b是氢; 在R 3a不同于氢的情况下，R 3b是氢或C 1-6烷基，R 2b是氢; t为1,2或3; Ar 1是苯基或取代的苯基; 且Ar 2是苯基或取代的苯基。它还涉及它们的制备方法和包含它们的组合物，以及它们作为药物的用途。

8. 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。

9. 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。

10. 发明授权

EP1711485B1 AMINO-BENZIMIDAZOLES DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 有权转让
标题翻译：氨基苯并咪唑衍生物作为复制呼吸道合胞病毒的抑制剂
公开(公告)号：EP1711485B1
公开(公告)日：2009-05-13
申请号：EP04804953.0
申请日：2004-12-20
申请人： Tibotec Pharmaceuticals Ltd.
发明人： BONFANTI, Jean-François , ANDRIES, Koenraad, Jozef, Lodewijk , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , GUILLEMONT, Jerôme, Emile, Georges , LACRAMPE, Jean, Fernand, Armand
IPC分类号： C07D401/06 , A61K31/4184 , C07D401/14 , C07D405/14 , A61P11/00 , A61P31/12
CPC分类号： C07D405/14 , C07D401/06 , C07D401/14
摘要： The present invention concerns amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula (I) their prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is Ar1 or C1-6alkyl substituted with one or more substituents selected from trifluoromethyl, C3-7cycloalkyl, Ar2, hydroxy, C1-4alkoxy, C1-4alkylthio, Ar2-oxy-, Ar2-thio-, Ar2(CH2)„oxy, Ar2(CH2)nthio, hydroxycarbonyl, aminocarbonyl, C1-4 alkylcarbonyl, Ar2carbonyl, C1-4alkoxycarbonyl, Ar2(CH2)n carbonyl, aminocarbonyloxy, C1-4 alkylcarbonyloxy, Ar2carbonyloxy, Ar2(CH2)ncarbonyloxy, hydroxy-C2- 4-alkyloxy, C1-4 alkoxycarbonyl(CH2)noxy, monoor di(C1-4alkyl)-aminocarbonyl, mono- or di(C1-4alkyl)aminocarbonyloxy, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl, dioxolanyl optionally substituted with one or two C1-6alkyl radicals, and a heterocycle selected from pyrrolidinyl, pyrrolyl, dihydropyrrolyl, thiazolidinyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, pyridyl and tetrahydropyridyl, which each may optionally be substituted with oxo or C1-6alkyl; G is a direct bond or optionally substituted C1-10alkanediyl R1 is Ar1 or a monocyclic or bicyclic heterocycle; one of R2a and R3a is C1-6alkyl and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen or C1-6alkyl, and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen or C 1-6alkyl, and R2b is hydrogen; Ar1 is phenyl or substituted phenyl and Ar2 is phenyl or substituted phenyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.

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