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1. 发明授权

US09682096B2 Polyinosinic-polycytidylic acid (poly (I:C)) formulations for the treatment of upper respiratory tract infections 有权
公开(公告)号：US09682096B2
公开(公告)日：2017-06-20
申请号：US14398573
申请日：2013-05-02
申请人： Janssen Sciences Ireland UC
发明人： Lieven Elvire Colette Baert , Bruce Albert Malcolm , Roger Paulus Maria Sutmuller
IPC分类号： A61K31/713 , A61K9/00 , A61K9/14 , A61K9/16 , C12N15/117
CPC分类号： A61K31/713 , A61K9/0043 , A61K9/146 , A61K9/16 , A61K9/1617 , A61K9/1623 , A61K9/1652 , C12N15/117 , C12N2310/17 , C12N2320/32
摘要： The present invention concerns a composition comprising micro particles of polyinosinic-polycytidylic acid (Poly (I:C)) and a carrier polymer selected from starch, alginate, blanose or DPPC (dipalmitoylphosphatidylcholine) for use in preventing and/or treating viral infections of the upper respiratory tract or the common cold and a device, preferably a nasal delivery system, comprising said composition for use by a patient in need to prevent and/or treat infections or the common cold.

2. 发明申请

US20150166533A1 NOVEL 1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES SUBSTITUTED WITH BENZIMIDAZOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS 审中-公开
标题翻译：以苯并咪唑为代表的呼吸道病毒抗病毒剂代替新的1,3-二氢-2H-苯并咪唑-2-酮衍生物
公开(公告)号：US20150166533A1
公开(公告)日：2015-06-18
申请号：US14407155
申请日：2013-06-14
申请人： Janssen R&D Ireland
发明人： Abdellah Tahri , Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Sandrine Marie Helene Vendeville , Ludwig Paul Cooymans , Samuel Dominique Demin
IPC分类号： C07D471/04 , C07D403/14
CPC分类号： C07D471/04 , C07D403/14
摘要： The present invention is concerned with novel 1,3-dihydro-2H-benzimidazol-2-one derivatives substituted with benzimidazoles having formula (I) stereoisomeric forms thereof, and the pharmaceutically acceptable addition salts, and the solvates thereof, wherein R4, R5, Z and Het have the meaning defined in the claims. The compounds according to the present invention are useful as inhibitors on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.
摘要翻译：本发明涉及用具有式（I）立体异构形式的苯并咪唑取代的新的1,3-二氢-2H-苯并咪唑-2-酮衍生物及其药学上可接受的加成盐及其溶剂化物，其中R4，R5， Z和Het具有权利要求中限定的含义。根据本发明的化合物可用作呼吸道合胞病毒（RSV）复制的抑制剂。本发明还涉及这些新化合物的制备，包含这些化合物的组合物和用于治疗呼吸道合胞病毒感染的化合物。

3. 发明申请

US20150141365A1 URACYL SPIROOXETANE NUCLEOSIDES 有权
公开(公告)号：US20150141365A1
公开(公告)日：2015-05-21
申请号：US14403587
申请日：2013-05-24
申请人： Janssen R&D Ireland
发明人： Ioannis Nicolaos Houpis , Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Abdellah Tahri
IPC分类号： C07H19/24 , A61K31/7072
CPC分类号： C07H19/10 , A61K31/7072 , C07H19/06 , C07H19/11 , C07H19/24
摘要： The present invention relates to compounds of the formula I: including any possible stereoisomers thereof, wherein R9 has the meaning as defined herein, or a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
摘要翻译：本发明涉及式I化合物：包括其任何可能的立体异构体，其中R9具有本文定义的含义，或其药学上可接受的盐或溶剂合物。本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在HCV治疗中单独或与其它HCV抑制剂组合的用途。

4. 发明授权

US09028876B2 Rate-controlled particles 有权
标题翻译：速率控制的颗粒
公开(公告)号：US09028876B2
公开(公告)日：2015-05-12
申请号：US13420013
申请日：2012-03-14
申请人： Thomas Hantke , Bettina Rehbock , Jörg Rosenberg , Jörg Breitenbach
发明人： Thomas Hantke , Bettina Rehbock , Jörg Rosenberg , Jörg Breitenbach
IPC分类号： A61K9/14 , A61K9/50 , A61K9/22 , A61K9/20 , A61K31/505 , A61K31/50 , A61K31/497 , C07D239/48 , A61K31/496 , A61K31/53 , C07D231/12 , C07D233/56 , C07D239/50 , C07D249/08 , C07D251/18 , C07D403/12 , C07D405/14 , A61K9/16
CPC分类号： C07D239/48 , A61K9/1635 , A61K31/496 , A61K31/505 , A61K31/53 , C07D231/12 , C07D233/56 , C07D239/50 , C07D249/08 , C07D251/18 , C07D403/12 , C07D405/14
摘要： Rate-controlled particles, comprising compounds of the formula as a solid dispersion.
摘要翻译：速率控制的颗粒，包含作为固体分散体的式的化合物。

5. 发明授权

US09012634B2 Antibacterial piperidinyl substituted 3,4-dihydro-1H-[1,8]naphthyridinones 有权
标题翻译：抗菌哌啶基取代的3,4-二氢-1H- [1,8]萘啶酮
公开(公告)号：US09012634B2
公开(公告)日：2015-04-21
申请号：US14237851
申请日：2012-08-10
申请人： Jerôme Emile Georges Guillemont , David Francis Alain Lançois , Magali Madeleine Simone Motte , Anil Koul , Wendy Mia Albert Balemans
发明人： Jerôme Emile Georges Guillemont , David Francis Alain Lançois , Magali Madeleine Simone Motte , Anil Koul , Wendy Mia Albert Balemans
IPC分类号： A61K31/4375 , C07D515/04 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention is related to novel compounds of formula (I) that inhibit the activity of the Fab1 enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
摘要翻译：本发明涉及抑制Fab1酶活性的新型式（I）化合物，因此可用于治疗细菌感染。它还涉及包含这些化合物的药物组合物和用于制备这些化合物的化学方法。

6. 发明授权

US09006243B2 HIV inhibiting 6-substituted pyrimidines 有权
标题翻译： HIV抑制6-取代嘧啶
公开(公告)号：US09006243B2
公开(公告)日：2015-04-14
申请号：US12521189
申请日：2007-12-28
申请人： Jerôme Emile Georges Guillemont , Céline Isabelle Mordant
发明人： Jerôme Emile Georges Guillemont , Céline Isabelle Mordant
IPC分类号： C07D239/48 , A61K31/506 , C07D401/04 , C07D401/12 , C07D403/06 , C07D405/12 , C07D409/12 , C07D417/06
CPC分类号： C07D239/48 , C07D401/04 , C07D401/12 , C07D403/06 , C07D405/12 , C07D409/12 , C07D417/06
摘要： HIV replication inhibitors of formula R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2, R3, R6 and R7 are hydrogen; hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(═O)R9; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 and R5 are hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; formyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(═O)R9; cyano; —S(═O)rR9; —NH—S(═O)2R9; —NHC(═O)H; —C(═O)NHNH2; —NHC(═O)R9; Het; —Y-Het; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R5 is pyridyl, —C(═O)NR5aR5b; —CH(OR5c)R5d; —CH2—NR5eR5f; —CH═NOR5a; —CH2—O—C2-6alkenyl; —CH2—O—P(═O)(OR5g)2; —CH2—O—C(═O)—NH2; —C(═O)—R5d; X is —NR1—, —O—, —CH2—, —S—; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.
摘要翻译：式R1的HIV复制抑制剂是氢; 芳基; 甲酰基 C 1-6烷基羰基; C 1-6烷基; C 1-6烷氧基羰基; R2，R3，R6和R7是氢; 羟基; 光环; C 3-7环烷基; C 1-6烷氧基; 羧基; C 1-6烷氧基羰基; 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; -C（= O）R 9; 任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基; R4和R5是羟基; 光环; C 3-7环烷基; C 1-6烷氧基; 羧基; C 1-6烷氧基羰基; 甲酰基氰基; 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; -C（= O）R 9; 氰基; -S（= O）r R 9; -NH-S（= O）2 R 9; -NHC（= O）H; -C（= O）NHNH 2; -NHC（= O）R 9; Het; -Y-Het; 任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基; R5是吡啶基，-C（= O）NR5aR5b; -CH（OR 5 c）R 5d; -CH2-NR5eR5f; -CH=NOR5a; -CH 2 -O-C 2-6烯基; -CH 2 -O-P（= O）（OR 5 g）2; -CH 2 -O-C（= O）-NH 2; -C（= O）-R5d; X是-NR 1 - ， - O - ， - CH 2 - ， - S- 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。

7. 发明授权

US08946248B2 HIV inhibiting 5-substituted pyrimidines 有权
标题翻译： HIV抑制5-取代嘧啶
公开(公告)号：US08946248B2
公开(公告)日：2015-02-03
申请号：US11576315
申请日：2005-09-29
申请人： Jerôme Emile Georges Guillemont , Jan Heeres , Paulus Joannes Lewi
发明人： Jerôme Emile Georges Guillemont , Jan Heeres , Paulus Joannes Lewi
IPC分类号： C07D239/48 , A61K31/505 , C07D239/50
CPC分类号： C07D239/48 , C07D239/50
摘要： HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A is —CH2—CH2—, —CH═CH—, —C≡C—; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, R2 hydroxy, halo, C1-6alkyl, carboxyl, cyano, —C(═O)R6, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl; X1 is —NR1—, —O—, —S—, —S(═O)p—; R3 is H, C1-6alkyl, halo; R4 is H, C1-6alkyl, halo; R5 is nitro, amino, mono- and diC1-4alkylamino, aryl, halo, —CHO, —CO—R6, —COOR7, —NH—C(═O)H, —NH—C(═O)R6, —CH═N—O—R8; R6 is C1-4alkyl, amino, mono- or di(C1-4alkyl)amino or polyhaloC1-4alkyl; R7 is hydrogen, C1-6alkyl, arylC1-6alkyl; R8 is hydrogen, C1-6alkyl, 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：其中A是-CH 2 -CH 2 - ， - CH = CH - ， - C≡C-;其中A是-CH 2 -CH 2 - ， - CH = CH - ， - C≡C-; R1是氢，芳基，甲酰基，C1-6烷基羰基，C1-6烷基，C1-6烷氧基羰基，R2羟基，卤素，C1-6烷基，羧基，氰基，-C（= O）R6，硝基，氨基，单或二 C 1-6烷基）氨基，多卤甲基; X 1是-NR 1 - ， - O - ， - S - ， - S（= O）p - ; R 3是H，C 1-6烷基，卤素; R4是H，C1-6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（= = N-O-R8; R 6是C 1-4烷基，氨基，单或二（C 1-4烷基）氨基或多卤代C 1-4烷基; R 7是氢，C 1-6烷基，芳基C 1-6烷基; R8是氢，C1-6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及其制备方法。

8. 发明授权

US08937080B2 Pyrimidine substituted macrocyclic HCV inhibitors 有权
标题翻译：嘧啶取代的大环HCV抑制剂
公开(公告)号：US08937080B2
公开(公告)日：2015-01-20
申请号：US12526553
申请日：2008-02-08
申请人： Pierre Jean-Marie Bernard Raboisson , Anna Karin Gertrud Linnea Belfrage , Björn Olof Classon , Karin Charlotta Lindquist , Karl Magnus Nilsson , Åsa Annica Kristina Rosenquist , Bertil Bengt Samuelsson , Horst Jürgen Wähling
发明人： Pierre Jean-Marie Bernard Raboisson , Anna Karin Gertrud Linnea Belfrage , Björn Olof Classon , Karin Charlotta Lindquist , Karl Magnus Nilsson , Åsa Annica Kristina Rosenquist , Bertil Bengt Samuelsson , Horst Jürgen Wähling
IPC分类号： A61K31/506 , C07D245/02 , C07K5/078 , C07D403/12 , A61K38/00
CPC分类号： C07K5/06165 , A61K38/00 , C07D403/12 , Y02A50/385 , Y02A50/387
摘要： Compounds of the formula I: including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.
摘要翻译：式I化合物：包括其立体异构体或N-氧化物，药学上可接受的加成盐或其药学上可接受的加成溶剂合物; 用作HCV抑制剂; 制备这些化合物的方法以及包含这些化合物作为活性成分的药物组合物。

9. 发明授权

US08933089B2 HIV inhibiting 5-amido substituted pyrimidines 有权
标题翻译： HIV抑制5-酰氨基取代的嘧啶
公开(公告)号：US08933089B2
公开(公告)日：2015-01-13
申请号：US12294692
申请日：2007-03-30
申请人： Jerôme Emile Georges Guillemont , Mikaël Paugam , Bruno François Marie Delest
发明人： Jerôme Emile Georges Guillemont , Mikaël Paugam , Bruno François Marie Delest
IPC分类号： A61K31/515 , C07D239/02 , C07D239/48 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
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。

10. 发明授权

US08865705B2 Benzimidazole respiratory syncytial virus inhibitors 有权
标题翻译：苯并咪唑呼吸道合胞病毒抑制剂
公开(公告)号：US08865705B2
公开(公告)日：2014-10-21
申请号：US13993107
申请日：2011-12-16
申请人： Ludwig Paul Cooymans , Samuël Dominique Demin , Lili Hu , Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Abdellah Tahri , Sandrine Marie Helene Vendeville
发明人： Ludwig Paul Cooymans , Samuël Dominique Demin , Lili Hu , Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Abdellah Tahri , Sandrine Marie Helene Vendeville
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D235/26
摘要： Benzimidazoles having inhibitory activity on RSV replication and having the formula the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof, compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
摘要翻译：对RSV复制具有抑制活性的苯并咪唑，其具有前药，N-氧化物，加成盐，季胺，金属络合物及其立体化学异构形式的组合物，含有这些化合物作为活性成分的组合物和制备这些化合物和组合物的方法。

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