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1. 发明申请

WO2010097229A2 AMORPHOUS SALT OF A MACROCYCLIC INHIBITOR OF HCV 审中-公开
标题翻译：丙型肝炎病毒大肠杆菌抑制剂的非晶体盐
公开(公告)号：WO2010097229A2
公开(公告)日：2010-09-02
申请号：PCT/EP2010/001197
申请日：2010-02-26
申请人： ORTHO-MCNEIL-JANSSEN PHARMACEUTICALS INC , VAN REMOORTERE, Peter, Jozef, Maria , VANDECRUYS, Roger, Petrus, Gerebern , DE KOCK, Herman
发明人： VAN REMOORTERE, Peter, Jozef, Maria , VANDECRUYS, Roger, Petrus, Gerebern , DE KOCK, Herman
IPC分类号： C07D417/04 , A61K31/47 , A61P31/14
CPC分类号： C07D417/14 , A61K9/14 , A61K31/4725 , C07D417/04
摘要： The amorphous form of the sodium salt of the macrocyclic inhibitor of HCV of formula (I) as well as processes for manufacturing this salt.
摘要翻译：式（I）的HCV的大环抑制剂的钠盐的无定形形式以及制备该盐的方法。

2. 发明申请

WO2010000459A1 CYCLOPROPYL POLYMERASE INHIBITORS 审中-公开
标题翻译：环丙基聚合酶抑制剂
公开(公告)号：WO2010000459A1
公开(公告)日：2010-01-07
申请号：PCT/EP2009/004748
申请日：2009-07-01
申请人： CENTOCOR ORTHO BIOTECH PRODUCTS L.P. , MEDIVIR AB , JONCKERS, Tim Hugo Maria , RABOISSON, Pierre Jean-Marie Bernard , VANDYCK, Koen
发明人： JONCKERS, Tim Hugo Maria , RABOISSON, Pierre Jean-Marie Bernard , VANDYCK, Koen
IPC分类号： C07H19/073 , A61K31/513 , A61P31/12
CPC分类号： C07H19/073
摘要： Compounds of formula I: wherein: R 2 is hydrogen or C 1 -C 4 alkyl; R 3 and R 4 are hydrogen, -C(=O)R 5 , or -C(=O)CHR 6 -NH 2 ; or R 3 is hydrogen and R 4 is a monophosphate-, diphosphate-, or triphosphate ester; or R 3 is hydrogen, -C(=O)CHR 5 , or -C(=O)CHR 6 -NH 2 and R 4 is (formula 2) each R 5 is hydrogen, C 1 -C 6 alkyl, or C 3 -C 7 cycloalkyl; R6 is hydrogen or C 1 -C 6 alkyl; R 7 is optionally substituted phenyl; naphthyl; or indolyl; R 8 and R 8 are hydrogen, C 3 -C 7 alkyl, benzyl; or R 8 and R 8 combined form C 3 -C 7 cycloalkyl; R 9 is C 1 -C 6 alkyl, benzyl, or optionally substituted phenyl; provided that R 2 , R 3 and R 4 are not all hydrogen; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations with the compounds I; the use of compounds I, including the compounds of formula I wherein R 2 , R 3 and R 4 are all hydrogen, as HCV inhibitors.
摘要翻译：式I化合物：其中：R 2是氢或C 1 -C 4烷基; R3和R4是氢，-C（= O）R5或-C（= O）CHR6-NH2; 或R3是氢，R4是单磷酸酯，二磷酸酯或三磷酸酯; 或R 3是氢，-C（= O）CHR 5或-C（= O）CHR 6 -NH 2，R 4是（式2），每个R 5是氢，C 1 -C 6烷基或C 3 -C 7环烷基; R6是氢或C1-C6烷基; R7是任选取代的苯基; 萘; 或吲哚基; R8和R8是氢，C3-C7烷基，苄基; 或R8和R8组合形成C3-C7环烷基; R 9是C 1 -C 6烷基，苄基或任选取代的苯基; 条件是R2，R3和R4不都是氢; 或其药学上可接受的盐或溶剂化物; 具有化合物I的药物制剂; 使用化合物I，包括其中R2，R3和R4均为氢的式Ⅰ化合物作为HCV抑制剂。

3. 发明申请

WO2008068299A2 HYDROBROMIDE SALT OF AN ANTI-HIV COMPOUND 审中-公开
标题翻译：抗HIV复合物的盐酸氢盐
公开(公告)号：WO2008068299A2
公开(公告)日：2008-06-12
申请号：PCT/EP2007/063386
申请日：2007-12-06
申请人： TIBOTEC PHARMACEUTICALS LTD. , THONÉ, Daniel Joseph Christiaan
发明人： THONÉ, Daniel Joseph Christiaan
IPC分类号： A61K9/16 , A61K31/505 , A61K9/10 , A61K9/14
CPC分类号： A61K9/1635 , A61K9/145 , A61K9/1641 , A61K9/1652
摘要： Solid dispersions and dosage forms comprising the hydrobromide salt of a diarylpyrimidine derivative, useful as an anti-HIV agent.
摘要翻译：包含可用作抗HIV剂的二芳基嘧啶衍生物的氢溴酸盐的固体分散体和剂型。

4. 发明申请

WO2006136562A1 HETEROCYCLYLAMINOALKYL SUBSTITUTED BENZIMIDAZOLES 审中-公开
标题翻译：取代苄基咪唑的杂环甲基氨基烷基
公开(公告)号：WO2006136562A1
公开(公告)日：2006-12-28
申请号：PCT/EP2006/063366
申请日：2006-06-20
申请人： TIBOTEC PHARMACEUTICALS LTD , BONFANTI, Jean-François , MULLER, Philippe , FORTIN, Jérôme, Michel, Claude , DOUBLET, Frédéric, Marc, Maurice
发明人： BONFANTI, Jean-François , MULLER, Philippe , FORTIN, Jérôme, Michel, Claude , DOUBLET, Frédéric, Marc, Maurice
IPC分类号： C07D401/06 , A61K31/4184 , A61P11/00
CPC分类号： C07D401/06 , C07D401/14
摘要： Heterocyclylaminoalkyl Substituted Benzimidazoles Inhibitors of RSV replication of formula (I): The salts and stereochemically isomeric forms thereof, wherein Q is hydrogen, C1-6alkyl optionally substituted with a heterocycle or Q is C1 -6alkyl substituted with both -OR4 and a heterocycle; wherein said heterocycle is oxazolidine, thiazolidine, 1-oxo-thiazolidine, 1,1-dioxothiazolidine, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, hexahydrooxazepine, hexahydrothiazepine, 1-oxo-hexahydrothiazepine, 1,1-dioxo-hexahydrothiazepine, pyrrolidine, piperidine, homopiperidine, piperazine; which heterocyle may be substituted with 1-2 substituents; each Alk is C1 -6alkanediyl; R1 is Ar or optionally substituted piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydrofuranyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazo lyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzthiazolyl, pyridopyridyl, naphthiridinyl, 1H-imidazo[4,5-b]pyridinyl, 3H-imidazo[4,5-b]pyridinyl, imidazo[1,2-a]pyridinyl or 2,3-dihydro-1,4-dioxino[2,3-b]pyridyl; R3 is hydroxyC1 -6alkyl, C1 -6alkoxyC1-6alkyl, cyanoC1-6alkyl, aminocarbonyl-C1 -6-alkyl, mono-or di(C1 -6alkyl)aminocarbonyl-C1 -6- alkyl, carboxyl-C1 -6-alkyl, C1-6alkoxycarbonyl-C1-6 alkyl; R2, R4 and R5 are hydrogen or C1-6alkyl; Het is pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydrofuranyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazolyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazo lyl, benzthiazolyl, pyridopyridyl, naphthiridinyl, 1H-imidazo[4,5-b]- pyridinyl, 3H-imidazo[4,5-b]pyridinyl, imidazo[1,2-a]pyridinyl and 2,3-dihydro-1,4- dioxino[2,3-b]pyridyl; Ar is optionally substituted phenyl; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).
摘要翻译：杂环氨基烷基取代的苯并咪唑式（I）的RSV复制抑制剂：其盐和立体化学异构形式，其中Q是氢，任选被杂环或Q取代的C 1-6烷基是被-OR 4和杂环二取代的C 1-6烷基; 其中所述杂环是恶唑烷，噻唑烷，1-氧代 - 噻唑烷，1,1-二氧代噻唑烷，吗啉基，硫代吗啉基，1-氧代 - 硫代吗啉基，1,1-二氧代硫代吗啉基，六氢氧氮杂，六氢噻嗪，1-氧代 - 六氢噻嗪，二氧代 - 六氢噻嗪，吡咯烷，哌啶，高哌啶，哌嗪; 哪个杂环可以被1-2个取代基取代; 每个Alk是C 1-6烷二基; R 1是Ar或任选取代的哌啶基，哌嗪基，吗啉基，硫代吗啉基，吡啶基，吡嗪基，哒嗪基，嘧啶基，呋喃基，四氢呋喃基，噻吩基，吡咯基，噻唑基，恶唑基，咪唑基，异噻唑基，吡唑基，异恶唑基，恶二唑基，喹啉基，喹喔啉基，苯并呋喃基苯并噻唑基，苯并咪唑基，苯并恶唑基，苯并噻唑基，吡啶并吡啶基，萘啶基，1H-咪唑并[4,5-b]吡啶基，3H-咪唑并[4,5-b]吡啶基，咪唑并[1,2-a] - 二氢-1,4-二氧杂环己烯并[2,3-b]吡啶基; R3是羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，氰基C 1-6烷基，氨基羰基-C 1-6烷基，单或二（C 1-6烷基）氨基羰基-C 1-6烷基，羧基-C 1-6烷基，C1 烷氧基羰基-C 1-6烷基; R2，R4和R5是氢或C1-6烷基; Het是吡啶基，吡嗪基，哒嗪基，嘧啶基，呋喃基，四氢呋喃基，噻吩基，吡咯基，噻唑基，恶唑基，咪唑基，异噻唑基，吡唑基，异恶唑基，恶二唑基，喹啉基，喹喔啉基，苯并呋喃基，苯并噻吩基，苯并咪唑基，苯并恶唑基，苯并噻唑基，吡啶并吡啶基，萘啶基，1H-咪唑并[4,5-b] - 吡啶基，3H-咪唑并[4,5-b]吡啶基，咪唑并[1,2-a]吡啶基和2,3-二氢-1,4-二氧杂环己二烯并[ 3-b]吡啶基; Ar是任选取代的苯基; 含有化合物（I）的药物组合物和制备化合物（I）的方法。

5. 发明申请

WO2006072636A3 1, 5, 6-SUBSTITUTED-2-OXO-3-CYANO-1, 6A-DIAZA-TETRAHYDRO-FLUORANTHENES AS ANTI-INFECTIVE AGENTS 审中-公开
公开(公告)号：WO2006072636A3
公开(公告)日：2006-07-13
申请号：PCT/EP2006/050106
申请日：2006-01-10
申请人： TIBOTEC PHARMACEUTICALS LTD. , KESTELEYN, Bart Rudolf Romanie , RABOISSON, Pierre Jean-Marie , VAN DE VREKEN, Wim , CANARD, Maxime Francis Jean-Marie Ghislain
发明人： KESTELEYN, Bart Rudolf Romanie , RABOISSON, Pierre Jean-Marie , VAN DE VREKEN, Wim , CANARD, Maxime Francis Jean-Marie Ghislain
IPC分类号： C07D471/16 , C07D498/16 , A61K31/4985 , A61P31/18
摘要： HIV inhibitory compounds of formula: (I) salts and stereoiso mers thereof, wherein R 1 and R 2 are hydrogen or optionally substituted C 1-10 alkyl; R 3 is: (a) n is 1, 2 or 3; R 3a is nitro, cyano, amino, halo, hydroxy, C 1-4 alkyloxy, hydroxycarbonyl, aminocarbonyl, C 1-4 alkyloxycarbonyl, mono- or di(C 1-4 alkyl)aminocarbonyl, C 1-4 alkylcarbonyl, methanimidamidyl, mono- or di(C 1-4 alkyl)methanimidamidyl, N -hydroxy-methanimidamidyl or Het; or 3 R is a monocyclic or bicyclic aromatic heterocyclic ring system, wherein one, two, three or four ring members are nitrogen, oxygen and sulfur, and wherein the remaining ring members are carbon atoms; and wherein each of said heterocyclic ring systems may optionally be substituted; X is -NR 7 -, -O- or -S-; pharmaceutical compositions containing these compounds, methods for preparing these compounds and compositions.

6. 发明申请

WO2005111044A1 4-SUBSTITUTED-1,5-DIHYDRO-PYRIDO[3,2-B]INDOL-2-ONES 审中-公开
标题翻译： 4-取代的-1,5-二氢 - 吡啶并[3,2-b]吲哚-2-酮
公开(公告)号：WO2005111044A1
公开(公告)日：2005-11-24
申请号：PCT/EP2005/052265
申请日：2005-05-17
申请人： TIBOTEC PHARMACEUTICALS Ltd. , KESTELEYN, Bart, Rudolf, Romanie , VAN DE VREKEN, Wim , SURLERAUX, Dominique, Louis, Nestor, Ghislain , VENDEVILLE, Sandrine, Marie, Helene , RABOISSON, Pierre, Jean-Marie, Bernard , WIGERINCK, Piet, Tom, Bert, Paul , PEETERS, Annick, Ann
发明人： KESTELEYN, Bart, Rudolf, Romanie , VAN DE VREKEN, Wim , SURLERAUX, Dominique, Louis, Nestor, Ghislain , VENDEVILLE, Sandrine, Marie, Helene , RABOISSON, Pierre, Jean-Marie, Bernard , WIGERINCK, Piet, Tom, Bert, Paul , PEETERS, Annick, Ann
IPC分类号： C07D491/04
CPC分类号： C07D471/04 , C07D491/04 , C07D491/14
摘要： 4-substituted 1,5-dihydro-pyrido[3,2-b]indol-2-ones of formula (I): the N -oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein n is 1, 2 or 3; R 1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N -hydroxymethanimidamidyl, mono- or di(C 1-4 alkyl)methanimidamidyl, Het 1 or Het 2 ; X is NR 2 , O, S, SO, SO 2 ; R 2 is hydrogen, C 1-10 alkyl, C 2-10 alkenyl, C 3-7 cycloalkyl, which are optionally substituted; R 2 is aryl substituted with -COOR 4 ; or R 2 is: (b-1); (b-2); -C p H 2p -CH(OR 14 )-C q H 2q -R 15 (b-3); -CH 2 -CH 2 -(O-CH 2 -CH 2 ) m -OR 14 (b-4); -CH 2 -CH 2 -(O-CH 2 -CH 2 ) m -NR 5a R 5b (b-5); -a 1 =a 2 -a 3 =a 4 - is -CH=CH-CH=CH-; -N=CH-CH=CH-; -CH=N-CH=CH-; -CH=CH-N=CH-; -CH=CH-CH=N-; wherein hydrogen atoms in (c-1) - (c-5) may be replaced by certain radicals; R 3 is obtionally substituted phenyl or a monocyclic or bicyclic aromatic heterocyclic ring system that can be substituted; R 21 is halo, hydroxy, amino, carboxyl, C 1-6 alkyl, C 3-7 cycloalkyl, arylC 1-6 alkyl, formyl, C 1-6 alkylcarbonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkylcarbonylo xy, -C(=O)-NR 13 R 14 ; C 1-6 alkyloxy, arylC 1-6 alkyloxy, polyhaloC 1-6 alkyloxy, amino, mono or di(C 1-6 alkyl)amino, formylamino, C 1-6 alkylcarbonylamino, C 1-6 alkylsulfo nylamino, mercapto, C 1-6 alkylthio, arylthio, aryloxy, arylC 1-6 alkylthio, C 1-6 alkylsulfynyl, C 1-6 alkylsulfo nyl, aryl, arylamino, Het 1 , Het 2 .
摘要翻译：式（I）的4-取代的1,5-二氢吡啶并[3,2-b]吲哚-2-酮：N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物，其中n 是1，2或3; R 1是氢，氰基，卤素，取代的羰基，甲亚氨基酰胺基，N-羟基甲酰亚胺基，单或二（C 1-4烷基）甲酰亚胺基，Het1或Het2; X是NR 2，O，S，SO，SO 2; R 2是氢，C 1-10烷基，C 2-10烯基，C 3-7环烷基，其任选被取代; R 2是被-COOR 4取代的芳基; 或R 2为：（b-1）; （B-2）; -CpH2p-CH（OR 14）-C≡H2q-R 15（b-3）; -CH 2 -CH 2 - （O-CH 2 -CH 2）m -OR 14（b-4）; -CH 2 CH 2 - （O-CH2-CH2）M-NR <5A> - [R <5B>（B-5）; -a 1 = a 2 -a 3 = a 4 - 是-CH = CH-CH = CH-; -N = CH-CH = CH-; -CH = N-CH = CH-; -CH = CH-N = CH-; -CH = CH-CH = N-; 其中（c-1） - （c-5）中的氢原子可被某些基团取代; R 3是被取代的苯基或可被取代的单环或双环芳族杂环体系; R 21是卤素，羟基，氨基，羧基，C 1-6烷基，C 3-7环烷基，芳基C 1-6烷基，甲酰基，C 1-6烷基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基氧基，-C（= O）-NR 13 > - [R <14>; C 1-6烷氧基，芳基C 1-6烷氧基，多卤代C 1-6烷氧基，氨基，单或二（C 1-6烷基）氨基，甲酰氨基，C 1-6烷基羰基氨基，C 1-6烷基磺酰基氨基，巯基，C 1-6烷硫基，芳硫基，芳氧基，芳基C 1-6烷硫基， -6-烷基亚磺酰基，C 1-6烷基磺酰基，芳基，芳基氨基，Het 1，Het 2。

7. 发明申请

WO2005110411A1 COMBINATIONS OF SUBSTITUTED 1-PHENYL-1,5-DIHYDRO-PYRIDO- [3,2-B] INDOL-2-ONES AND OTHER HIV INHIBITORS 审中-公开
标题翻译：取代的1-苯基-1,5-二氢吡喃并[3,2-B]吲哚-2-酮和其他HIV抑制剂的组合
公开(公告)号：WO2005110411A1
公开(公告)日：2005-11-24
申请号：PCT/EP2005/052266
申请日：2005-05-17
申请人： TIBOTEC PHARMACEUTICALS LTD. , KESTELEYN, Bart, Rudolf, Romanie , VAN DE VREKEN, Wim , KINDERMANS, Natalie, Maria, Francisca , CANARD, Maxime, Francis, Jean-Marie, Ghislain , HERTOGS, Kurt , BETTENS, Eva , DE VROEY, Veronique, Corine, Paul , JOCHMANS, Dirk, Edward, Désiré , WIGERINCK, Piet, Tom, Bert, Paul , WANG, Jing , TAHRI, Abdellah , SURLERAUX, Dominique, Louis, Nestor, Ghislain
发明人： KESTELEYN, Bart, Rudolf, Romanie , VAN DE VREKEN, Wim , KINDERMANS, Natalie, Maria, Francisca , CANARD, Maxime, Francis, Jean-Marie, Ghislain , HERTOGS, Kurt , BETTENS, Eva , DE VROEY, Veronique, Corine, Paul , JOCHMANS, Dirk, Edward, Désiré , WIGERINCK, Piet, Tom, Bert, Paul , WANG, Jing , TAHRI, Abdellah , SURLERAUX, Dominique, Louis, Nestor, Ghislain
IPC分类号： A61K31/475
CPC分类号： A61K31/475 , A61K31/496 , A61K31/5377 , A61K2300/00
摘要： The present invention concerns combinations comprising a compound of formula (I); the N -oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters or metabolites thereof, wherein n is 1, 2 or 3; R 1 is H, CN, halo, aminoC(=O), C(=O)OH, C 1-4 alkyloxyC(=O), C 1-4 alkylC(=O), mono- or di(C 1-4 alkyl)aminoC(=O), arylaminoC(=O), N -(aryl)- N -(C 1-4 alkyl)aminoC(=O), methanimidamidyl, N -hydroxy-methanimidamidyl, mono- or di(C 1-4 alkyl)methanimidamidyl, Het 1 or Het 2 ; R 2 is H, C 1-10 alkyl, C 2-10 alkenyl, C 3-7 cycloalkyl, wherein said C 1-10 alkyl, C 2-10 alkenyl and C 3-7 cycloalkyl may be optionally substituted; R 3 is nitro, cyano, amino, halo, hydroxy, C 1-4 alkyloxy, hydroxyC(=O), aminoC(=O), C 1-4 alkyloxyC(=O), mono- or di(C 1-4 alkyl)aminoC(=O), C 1-4 alkylC(=O), methanimidamidyl, mono- or di(C 1-4 alkyl)methanimidamidyl, N -hydroxy-methanimidamidyl or Het 1 ; and another HIV inhibitor. The invention also concerns products comprising a compound of formula (I) and another HIV inhibitor, as a combined preparation for simultaneous, separate or sequential use in treatment of retroviral infections such as HIV infection, in particular, in the treatment of infections with multi-drug resistant retroviruses.
摘要翻译：本发明涉及包含式（I）化合物的组合; N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯或代谢物，其中n为1,2或3; R 1是H，CN，卤素，氨基C（= O），C（= O）OH，C 1-4烷氧基C（= O），C 1-4烷基C（= O），单或二（C 1-4烷基） O），芳基氨基C（= O），N-（芳基）-N-（C 1-4烷基）氨基C（= O），甲亚氨基酰胺基，N-羟基 - 甲亚胺基酰胺基，单或二（C 1-4烷基）甲酰胺基，Het1或 HET 2; R 2是H，C 1-10烷基，C 2-10烯基，C 3-7环烷基，其中所述C 1-10烷基，C 2-10烯基和C 3-7环烷基可以任选被取代; R3是硝基，氰基，氨基，卤素，羟基，C1-4烷氧基，羟基C（= O），氨基C（= O），C1-4烷氧基C（= O），单或二（C1-4烷基）氨基C（= O），C 1-4烷基C（= O），甲亚氨基亚氨基，单或二（C 1-4烷基）甲亚氨基酰胺基，N-羟基 - 甲亚胺酰氨基或Het1; 和另一种HIV抑制剂。本发明还涉及包含式（I）化合物和另一种HIV抑制剂的产品，作为用于同时，分别或顺序用于治疗逆转录病毒感染如HIV感染的组合制剂，特别是用于治疗多发性感染的感染，耐药性逆转录病毒

8. 发明申请

WO2005058871A1 MORPHOLINYL CONTAINING BENZIMIDAZOLES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 审中-公开
标题翻译：含有苯并咪唑的苯并咪唑作为呼吸道同种病毒复制的抑制剂
公开(公告)号：WO2005058871A1
公开(公告)日：2005-06-30
申请号：PCT/EP2004/053620
申请日：2004-12-20
申请人： TIBOTEC PHARMACEUTICALS LTD. , BONFANTI, Jean-François , ANDRIES, Koenraad, Jozef, Lodewijk , FORTIN, Jérôme, Michel, Claude , MULLER, Philippe , DOUBLET, Frédéric, Marc, Maurice , MEYER, Christophe , WILLEBRORDS, Rudy, Edmond , GEVERS, Tom, Valerius, Josepha , TIMMERMAN, Philip, Maria, Martha, Bern
发明人： BONFANTI, Jean-François , ANDRIES, Koenraad, Jozef, Lodewijk , FORTIN, Jérôme, Michel, Claude , MULLER, Philippe , DOUBLET, Frédéric, Marc, Maurice , MEYER, Christophe , WILLEBRORDS, Rudy, Edmond , GEVERS, Tom, Valerius, Josepha , TIMMERMAN, Philip, Maria, Martha, Bern
IPC分类号： C07D401/06
CPC分类号： C07D413/12 , C07D401/06 , C07D401/14 , C07D413/14
摘要： The present invention concerns morpholinyl containing benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula (I), a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein G is a direct bond or optionally substituted C 1-10 alkanediyl; R l is Ar 1 or a monocyclic or bicyclic heterocycle Q is R 7 , pyrrolidinyl substituted with R 7 , piperidinyl substituted with R 7 or homopiperidinyl substituted with R 7 ; one of R 2a and R 3a is selected from halo, optionally mono- or polysubstituted C l-6 alkyl, optionally mono- or polysubstituted C 2-6 alkenyl, nitro, hydroxy, Ar 2 , N(R 4a R 4 ), N(R 4a R 4 )sulfonyl, N(R 4a R 4b )carbonyl, C 1-6 alkyloxy, Ar 2 oxy, Ar 2 C l-6 alkyloxy, carboxyl, C l-6 alkyloxycarbonyl, or -C(=Z)Ar 2 ; 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, C 1-6 alkyl or halogen and R 3b is hydrogen; in case R 3a is different from hydrogen then R 3b is hydrogen, C 1-6 alkyl or halogen and R 2b is hydrogen. It further concerns the preparation thereof and compositions comprising these compounds, as well as the use thereof as a medicine.
摘要翻译：本发明涉及对具有式（I）的前体药物，N-氧化物，加成盐，季胺，金属络合物或其立体化学异构体形式的对呼吸道合胞病毒复制具有抑制活性的吗啉基苯并咪唑，其中G为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Q是R 7，被R 7取代的吡咯烷基，被R 7取代的哌啶基或被R 7取代的高哌啶基; R 2a和R 3a之一选自卤素，任选的单取代或多取代的C 1-6烷基，任选的单或多取代的C 2-6烯基，硝基，羟基，Ar 2，N（R 4a）R R 4，R 4），N（R 4aR 4）磺酰基，N（R 4a R 4b）羰基，C 1-6烷氧基，Ar 2氧基，Ar 2 Cl 6烷氧基，羧基，C 1-6烷氧基羰基或-C（= Z）Ar 2; 而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，C 1-6烷基或卤素，R 3b是氢; 在R 3a不同于氢的情况下，R 3b是氢，C 1-6烷基或卤素，R 2b是氢。还涉及其制备方法和包含这些化合物的组合物，以及作为药物的用途。

9. 发明申请

WO2003099677A2 STAND-ALONE PACKAGING FOR TUBES 审中-公开
标题翻译：独立包装管
公开(公告)号：WO2003099677A2
公开(公告)日：2003-12-04
申请号：PCT/EP2003/005719
申请日：2003-05-27
申请人： JOHNSON & JOHNSON CONSUMER FRANCE S.A.S. , DAVID, Alexandre , EGLI, Reto , GRANDHAYE, Sandra
发明人： DAVID, Alexandre , EGLI, Reto , GRANDHAYE, Sandra
IPC分类号： B65D77/04
CPC分类号： B65D77/044 , B65D73/0085
摘要： A stand-alone packaging (1) for tubes (14) of different shapes and sizes being placed in the packaging (1) having a back wall (2) and a front wall (3), which are linked at a top side (4), a bottom wall (5) and a platform surface (6), which is linked to the back wall (2) and the front wall (3), the back wall (2), at its bottom side, has a tab (8) that fits into an opening (9) at a fold between the bottom side of an interior front wall (15) and the bottom wall (5), the platform surface (6) is connected to the bottom wall (5) by the interior front wall (15) which becomes visible when opening the back wall (2), the platform surface (6) has a flap (11) linking the platform surface (6) to the front wall (3), the platform surface (6) is parallel to the bottom wall (5) and has an opening (7) in which the tube (14) fits, wherein the tube (14) is placed upside down in the packaging (1) with the tube (14) fitting narrowly into the opening (7) of the platform surface (6), and the portion at which the tube (14) is sealed being placed at the top side (4), a fold (17) is provided between the top side (4) and the back wall (2), such that the back wall (2) is hinged to the top side (4) of the packaging (1) and can be opened so as to remove the tube (14).
摘要翻译：将具有不同形状和尺寸的管（14）的独立包装（1）放置在具有后壁（2）和前壁（3）的包装（1）中，所述后壁（2）和前壁（3）在顶侧），底壁（5）和平台表面（6），其连接到后壁（2）和前壁（3），后壁（2）在其底侧具有凸片（ 8），其安装在内部前壁（15）的底侧与底壁（5）之间的折叠处的开口（9）中，平台表面（6）通过所述底壁内部前壁（15）在打开后壁（2）时变得可见，平台表面（6）具有将平台表面（6）连接到前壁（3），平台表面（6））平行于底壁（5）并且具有开口（7），管（14）配合在其中，其中管（14）被倒置放置在包装（1）中，管（14）狭窄地配合进入平台表面（6）的开口（7），以及其中的部分管（14）被密封放置在顶侧（4）处，折叠（17）设置在顶侧（4）和后壁（2）之间，使得后壁（2）铰接到包装（1）的顶侧（4）并且可以打开以便移除管（14）。

10. 发明申请

WO2003066073A2 COMPOSITIONS CONTAINING OAT STRAW AND WILLOWHERB EXTRACT 审中-公开
标题翻译：含有OAT STRAW和WILLOWHERB提取物的组合物
公开(公告)号：WO2003066073A2
公开(公告)日：2003-08-14
申请号：PCT/EP2003/001294
申请日：2003-02-10
申请人： JOHNSON & JOHNSON GMBH , LANGE, Rainer , VON STETTEN, Otto
发明人： LANGE, Rainer , VON STETTEN, Otto
IPC分类号： A61K35/78
CPC分类号： A61K9/70 , A61K8/0208 , A61K8/97 , A61K9/7023 , A61K36/185 , A61K36/899 , A61K2800/75 , A61Q19/00 , A61K2300/00
摘要： This invention relates to chemical compositions comprising oat straw extract and willowherb extract that can be used to treat or reduce inflammatory reactions on or in the skin. The compositions can be used in topical formulations. The invention further concerns products comprising an applicator that can be a porous or absorbent sheet, more specifically a wipe, and a formulation that contains oat straw extract and willowherb extract.
摘要翻译：本发明涉及包含燕麦秸秆提取物和柳叶刀提取物的化学组合物，其可用于治疗或减少皮肤上或皮肤中的炎症反应。组合物可用于局部制剂。本发明还涉及包括可以是多孔或吸收性片材，更具体地，擦拭物的施用器以及含有燕麦草提取物和柳叶刀提取物的制剂的产品。

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