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11. 发明申请

WO1997032887A1 OLIGONUCLEOTIDE ANALOGUES 审中-公开
标题翻译：寡核苷酸类似物
公开(公告)号：WO1997032887A1
公开(公告)日：1997-09-12
申请号：PCT/GB1997000499
申请日：1997-02-24
申请人： NOVARTIS AG , BAXTER, Anthony, David , COLLINGWOOD, Stephen, Paul , DOUGLAS, Mark, Edward , TAYLOR, Roger, John
发明人： NOVARTIS AG
IPC分类号： C07H21/00
CPC分类号： C07H21/00
摘要： An oligonucleotide analogue having 10 to 200 natural and/or synthetic nucleoside units, linked by internucleoside linkages, at least one of the internucleoside linkages being of formula (I), where the indicated methylene group is attached to a 3' carbon atom of a nucleoside, the indicated oxygen atom is attached to a 5' carbon atom of an adjacent nucleoside, R is hydrogen, hydroxy, O , thiol, S , -NH2 or a group of formula R a, -OR a, -SR a, -NHR b or -NR bR c where R a is an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C3 to C8 cycloalkyl, C6 to C10 aryl or C7 to C13 aralkyl group and R b and R c are each independently an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C3 to C8 cycloalkyl, C6 to C10 aryl or C7 to C13 aralkyl group or R b and R c together with the nitrogen atom to which they are attached denote a five- or six-membered heterocyclic ring, and X is oxygen or sulphur.
摘要翻译：具有通过核苷间键连接的10至200个天然和/或合成核苷单位的寡核苷酸类似物，至少一个核苷间键与式（I）结合，其中所示的亚甲基连接到核苷的3'碳原子上，所指示的氧原子连接在相邻核苷的5'碳原子上，R 1是氢，羟基，O - ，硫醇，S - ， - NH 2或式R 1基团 a，-OR 1 a，-SR 1 a，-NHR b或-NR 1 b R c c，其中R a是未取代或取代的C 1至C 10烷基，C 2 至C 10烯基，C 3至C 8环烷基，C 6至C 10芳基或C 7至C 13芳烷基，R b和R c各自独立地为未取代或取代的C 1至C 10烷基，C 2至C 10烯基，C 3至C 10 C8环烷基，C6至C10芳基或C7至C13芳烷基或R 1b和R 1c与它们所连接的氮原子一起表示五元或六元杂环，X为氧或硫。

12. 发明申请

WO2008006563A1 PURINE DERIVATIVES AS A2A AGONISTS 审中-公开
标题翻译：嘌呤衍生物作为A2A激动剂
公开(公告)号：WO2008006563A1
公开(公告)日：2008-01-17
申请号：PCT/EP2007/006156
申请日：2007-07-11
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FAIRHURST, Robin, Alec , TAYLOR, Roger, John
发明人： FAIRHURST, Robin, Alec , TAYLOR, Roger, John
IPC分类号： C07D473/16 , C07H19/167 , A61K31/52 , A61P11/00
CPC分类号： C07D473/16
摘要： Compounds of formula (I):or stereoisomers or pharmaceutically acceptable salts thereof, wherein W, R 1 ,R 2 and R 3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A 2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译：式（I）化合物或其立体异构体或其药学上可接受的盐，其中W 1，R 2，R 2和R 3 3具有如下含义：如说明书中所示，可用于治疗由腺苷A 2A受体的活化介导的病症，特别是炎性或阻塞性气道疾病。还描述了含有化合物的药物组合物和制备该化合物的方法。

13. 发明申请

WO2007121923A1 PURINE DERIVATIVES AS A2A RECEPTOR AGONISTS 审中-公开
标题翻译：嘌呤衍生物作为A2A受体激动剂
公开(公告)号：WO2007121923A1
公开(公告)日：2007-11-01
申请号：PCT/EP2007/003438
申请日：2007-04-19
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FAIRHURST, Robin, Alec , TAYLOR, Roger, John
发明人： FAIRHURST, Robin, Alec , TAYLOR, Roger, John
IPC分类号： A61K31/00 , A61K31/52 , A61P9/00 , A61P11/00 , A61P29/00
CPC分类号： A61K31/52 , A61K31/00
摘要： A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof.and their preparation and use as A2A receptor agonists
摘要翻译：式（I）的化合物或其立体异构体或其药学上可接受的盐，并且其作为A2A受体激动剂的制备和用途

14. 发明申请

WO2007121920A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2007121920A2
公开(公告)日：2007-11-01
申请号：PCT/EP2007/003435
申请日：2007-04-19
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FAIRHURST, Robin, Alec , TAYLOR, Roger, John , COX, Brian
发明人： FAIRHURST, Robin, Alec , TAYLOR, Roger, John , COX, Brian
CPC分类号： C07D473/16 , C07D473/34
摘要： A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals, wherein R 1 , R 2 and R 3 are as defined herein.
摘要翻译：式（I）化合物或其立体异构体或其药学上可接受的盐及其作为药物的制备和用途，其中R 1，R 2和R 3， / SUP>如本文所定义。

15. 发明申请

WO2004087142A1 QUINOLINE-2-ONE-DERIVATIVES FOR THE TREATMENT OF AIRWAYS DISEASES 审中-公开
标题翻译：用于治疗空气污染的喹啉-2-酮衍生物
公开(公告)号：WO2004087142A1
公开(公告)日：2004-10-14
申请号：PCT/EP2004/003516
申请日：2004-04-02
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FAIRHURST, Robin, Alec , SANDHAM, David, Andrew , BEATTIE, David , BRUCE, Ian , CUENOUD, Bernard , MADDEN, Reamonn , PRESS, Neil, John , TAYLOR, Roger, John , TURNER, Katharine, Louise , WATSON, Simon, James
发明人： FAIRHURST, Robin, Alec , SANDHAM, David, Andrew , BEATTIE, David , BRUCE, Ian , CUENOUD, Bernard , MADDEN, Reamonn , PRESS, Neil, John , TAYLOR, Roger, John , TURNER, Katharine, Louise , WATSON, Simon, James
IPC分类号： A61K31/435
CPC分类号： C07D215/227 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D417/14
摘要： Compounds of formula (I) in free or salt form, wherein -C-Y-, R 1 and R 2 are G have the meanings as indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the (β 2 -adrenoreceptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译：游离或盐形式的式（I）化合物，其中-CY-，R 1和R 2为G具有如说明书中所示的含义，可用于治疗通过活化而预防或缓解的病症还描述了（β2-肾上腺素受体）含有化合物的药物组合物和制备该化合物的方法。

16. 发明申请

WO2013038390A1 N-SUBSTITUTED HETEROCYCLYL CARBOXAMIDES 审中-公开
标题翻译： N-取代的杂环碳酰胺
公开(公告)号：WO2013038390A1
公开(公告)日：2013-03-21
申请号：PCT/IB2012/054832
申请日：2012-09-14
申请人： NOVARTIS AG , BALA, Kamlesh, Jagdis , BUDD, Emma , EDWARDS, Lee , HOWSHAM, Catherine , LEGRAND, Darren, Mark , TAYLOR, Roger, John
发明人： BALA, Kamlesh, Jagdis , BUDD, Emma , EDWARDS, Lee , HOWSHAM, Catherine , LEGRAND, Darren, Mark , TAYLOR, Roger, John
IPC分类号： A61K31/415 , A61K31/4439 , A61K31/497 , A61P11/06
CPC分类号： C07D487/04 , A61K31/415 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/4985 , A61K31/5377 , A61K45/06 , C07D231/40 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/14
摘要： A compound of Formula I and pharmaceutically acceptable salts and solvates thereof, wherein R 1 , R 2 , R 3 , R a , A, B, D and E are all as defined herein. The compounds modulate the activity of CFTR and are useful in the treatment of inflammatory or obstructive airways diseases or mucosal hydration, including, for example cystic fibrosis. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译：式I化合物及其药学上可接受的盐和溶剂合物，其中R1，R2，R3，Ra，A，B，D和E全部如本文所定义。该化合物调节CFTR的活性，并且可用于治疗炎性或阻塞性气道疾病或粘膜水合，包括例如囊性纤维化。还描述了含有化合物的药物组合物和用于制备化合物的方法。

17. 发明申请

WO2007121924A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2007121924A2
公开(公告)日：2007-11-01
申请号：PCT/EP2007/003439
申请日：2007-04-19
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FAIRHURST, Robin, Alec , TAYLOR, Roger, John
发明人： FAIRHURST, Robin, Alec , TAYLOR, Roger, John
IPC分类号： C07D519/00 , A61K31/52 , A61P29/00
CPC分类号： C07D519/00 , C07H19/16 , C07H21/00
摘要： A compound of formula (I), or stereoisomers or pharmaceutically acceptable salts thereof, wherein, R la , R lb , R 2a , R 2b , U 1 , U 2 , X 1 , X 2 and L are as defined herein.
摘要翻译：式（I）化合物或其立体异构体或其药学上可接受的盐，其中R 1，R 2，R 2，R 2，R 2， U 2，U 1，X 2，X 1，X 2和L分别为如本文所定义。

18. 发明申请

WO2007121921A3 PURINE DERIVATIVES FOR USE AS ADENOSIN A2A RECEPTOR AGONISTS 审中-公开
公开(公告)号：WO2007121921A3
公开(公告)日：2007-11-01
申请号：PCT/EP2007/003436
申请日：2007-04-19
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FAIRHURST, Robin, Alec , TAYLOR, Roger, John
发明人： FAIRHURST, Robin, Alec , TAYLOR, Roger, John
IPC分类号： A61K31/015 , A61K31/52 , A61P11/00 , A61P9/00 , A61P29/00 , A61P25/00
摘要： A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R l , R 2 and R 3 are as defined herein.

19. 发明申请

WO1997035869A1 DINUCLEOTIDE AND OLIGONUCLEOTIDE ANALOGUES 审中-公开
标题翻译：胆固醇和寡核苷酸类似物
公开(公告)号：WO1997035869A1
公开(公告)日：1997-10-02
申请号：PCT/GB1997000651
申请日：1997-03-11
申请人： NOVARTIS AG , BAXTER, Anthony, David , BAYLIS, Eric, Keith , COLLINGWOOD, Stephen, Paul , FAIRHURST, Robin, Alec , TAYLOR, Roger, John
发明人： NOVARTIS AG
IPC分类号： C07H21/00
CPC分类号： C07H19/06 , C07H21/00 , Y02P20/55
摘要： A compound which is a dinucleotide analogue of formula (I) or a salt thereof, where B an B are each independently a monovalent nucleoside base radical, R is hydrogen or Y , R and R are each independently hydrogen, halogen, hydroxy or -OY , R is hydrogen, halogen, hydroxy, -OY or R , R is hydrogen, halogen or R , R is hydrogen, Y or a phosphoramidyl group, Z is a group of formula (II), (III) or (IV), where R is hydrogen, halogen, hydroxy, -OY or R , R is hydrogen, halogen or R , R is hydroxy, R or -OR where R is a C1 to C10 aliphatic group, a C3 to C8 cycloaliphatic group, a C6 to C10 aromatic group or a C7 to C13 araliphatic group, and R is hydrogen, R a or -OCOR a where R a is C1 to C10 aliphatic, a C3 to C8 cycloaliphatic group, a C6 to C10 aromatic group or a C7 to C13 araliphatic group, Y , Y , Y , Y , and Y are each independently a hydroxy-protecting group, and R , R , R , R are each independently a C1 to C10 aliphatic group, a C3 to C8 cycloaliphatic group, a C6 to C10 aromatic group or a C7 to C13 araliphatic group.
摘要翻译：作为式（I）的二核苷酸类似物或其盐的化合物，其中B 1和B 2各自独立地为一价核苷碱基，R 1为氢或Y 1， 2>和R 3各自独立地为氢，卤素，羟基或-OY 2，R 4为氢，卤素，羟基，-OY 3或R 7，R 5为氢，卤素或R 8，R 6为氢，Y 4或亚磷酰基，Z为式（II），（III）或（IV）的基团，其中R 9为氢，卤素，羟基，-OY 5或R 13，R 10是氢，卤素或R 14，R 11是羟基，R 15或-OR 15，其中R 15 >为C1至C10脂族基团，C3至C8脂环族基团，C6至C10芳族基团或C7至C13芳脂族基团，R12为氢，R12a或-OCOR12 其中R 12是C 1至C 10脂族基，C 3至C 8脂环族基团，C 6至C 10芳族基团或C 7至C 13芳脂基基团，Y 1，Y 2，Y 3， 4＆gt;和Y 5各自独立地为羟基保护基，R 7，R 8，R 13，R 14，Ar 各自独立地为C1至C10脂族基团，C3至C8脂环族基团，C6至C10芳族基团或C7至C13芳脂肪族基团。

20. 发明申请

WO1996007666A1 MONONUCLEOTIDE AND DINUCLEOTIDE ANALOGUES AND INTERMEDIATES THEREFOR 审中-公开
标题翻译：单核苷酸和胆固醇类似物及其中间体
公开(公告)号：WO1996007666A1
公开(公告)日：1996-03-14
申请号：PCT/GB1995001986
申请日：1995-08-21
申请人： CIBA-GEIGY AG , IRVING, Edward , BAXTER, Anthony, David , COLLINGWOOD, Stephen, Paul , TAYLOR, Roger, John
发明人： CIBA-GEIGY AG
IPC分类号： C07H19/04
CPC分类号： C07H23/00 , C07H19/06 , C07H21/00 , C07H21/04 , Y02P20/55
摘要： A compound of formula (I) or a pharmaceutically acceptable salt thereof, where R is hydrogen, R a or a group of formula (II), R a b or a protecting group Q, R b is C1-C20 alkyl, C2-C20 alkenyl, C3-C10 cycloalkyl, C6-C15 aryl, C7-C16 aralkyl or a 5- or 6- membered heterocyclic group attached by a carbon atom in the heterocyclic group to the indicated phosphorus atom, R is hydrogen, R a or -OR , provided that when R is hydrogen, R is R a or -OR , R a is a C1-C20 aliphatic group, a C3-C10 cycloaliphatic group, a C6-C15 aromatic group, a C7-C16 araliphatic group, or a 5- or 6- membered heterocyclic group attached by a carbon atom in the heterocyclic group to the indicated phosphorus atom, R is hydrogen, halogen, hydroxy, R , -OR , OSO2R , OCOR or tri(C1-C15 hydrocarbyl) silyloxy, R is R a or together with R denotes a valence bond, R a is hydrogen, halogen or R , R is hydrogen, halogen, hydroxy, R , -OR , -OCOR , OSO2R , or tri(C1-C15 hydrocarbyl) silyloxy, R is hydrogen, halogen or R , or together with R denotes a valence bond, R is hydrogen, or an atom or group capable of terminating a replicating strand of a nucleic acid or of inhibiting viral DNA synthesis, other than a group connected to the indicated furanose ring through an oxygen atom, or together with R denotes a valence bond, R is R a, or together with R denotes a valence bond, R a is hydrogen, halogen, hydroxy, R , -OR , -OCOR , -OSO2R or tri(C1-C15 hydrocarbyl) silyloxy, R is a monovalent nucleoside base radical, R is hydrogen or R a, R a is R , -COR , -SO2R or tri(C1-C15 hydrocarbyl)silyl, R is hydrogen, halogen, hydroxy, R , -OR , -OCOR , -OSO2R or Z, R is hydrogen, halogen or R . R is hydrogen or R a, R a is halogen, hydroxy, R , -OR , -OCOR , -OSO2R or tri(C1-C15 hydrocarbyl)silyloxy, R is a monovalent nucleoside base radical, R is hydrogen or R a, R a is a C1 to C10 aliphatic group, a C3 to C8 cycloaliphatic group, a C6 to C15 aromatic group or a C7 to C16 araliphatic group, R , R , R , R , R , R , R , R and R are independently a C1 to C10 aliphatic group, a C3 to C10 cycloaliphatic group, a C6 to C15 aromatic group or a C7 to C30 araliphatic group, and Z is substituted or unsubstituted C6 to C10 aryloxythiocarbonyloxy.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中R 1是氢，R 1a或式（II）的基团，R 1'> a <= R 1> b或保护基Q，R 1b是C 1 -C 20烷基，C 2 -C 20烯基，C 3 -C 10环烷基，C 6 -C 15芳基，C 7 -C 16芳烷基或被碳原子连接的5-或6-元杂环基在指定的磷原子的杂环基中，R 2是氢，R 2 a或-OR 15，条件是当R 1是氢时，R 2是R 2 a或 -OR 15，R 2a是C 1 -C 20脂族基团，C 3 -C 10脂环族基团，C 6 -C 15芳族基团，C 7 -C 16芳脂族基团或5-或6-元杂环基团通过杂环基中的碳原子与指定的磷原子连接，R 3是氢，卤素，羟基，R 16，-OR 16，OSO 2 R 16，OCOR 16或三（C 1 -C 6） -C 15烃基）甲硅烷氧基，R 4是R 4 a或与R 6一起代表价键，R 4是氢，卤素或R 17，R 5是氢，卤素，羟基，R 18，-OR 18，-OCOR 18 ，OSO 2 R 18或三（C 1 -C 15烃基）甲硅烷氧基，R 6是氢，卤素或R 19，或与R 4一起代表价键，R 7是氢，或可以终止核酸的复制链或抑制病毒DNA合成的原子或基团，除了通过氧原子与所示的呋喃糖环连接的基团，或与R 8一起，表示价键， R 8是R 8，或与R 7一起代表价键，R 8 a是氢，卤素，羟基，R 20，-OR 20，-OCOR 20， -OSO 2 R 20或三（C 1 -C 15烃基）甲硅烷氧基，R 9是一价核苷碱基，R 10是氢或R 10a，R 10a是R 21， -COR 21，-SO 2 R 21或三（C 1 -C 15烃基）甲硅烷基，R 11是氢，卤素，羟基，R 22，-OR 22，-OCOR 22， OSO 2 R 22或Z，R 12是氢，卤素或R 23。 R 13是氢或R 13 a，R 13是卤素，羟基，R 24，-OR 24，-OCOR 24，-OSO 2 R 24或三（C1- C 15烃基）甲硅烷氧基，R 14是单价核苷碱基，R 15是氢或R 15 a，R 15是C 1至C 10脂族基团，C 3至C 8脂环族基团， C 6至C 15芳族基团或C 7至C 16芳脂基基团，R 16，R 17，R 18，R 19，R 20，R 21，R 22， 23>和R 24独立地为C 1至C 10脂族基团，C 3至C 10脂环族基团，C 6至C 15芳族基团或C 7至C 30芳脂族基团，Z为取代或未取代的C 6至C 10芳氧基硫代羰基氧基。

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