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1. 发明申请

WO2013037411A1 NEW ENZYME INHIBITOR COMPOUNDS 审中-公开
标题翻译：新型酶抑制剂化合物
公开(公告)号：WO2013037411A1
公开(公告)日：2013-03-21
申请号：PCT/EP2011/065967
申请日：2011-09-14
申请人： PROXIMAGEN LIMITED , EVANS, David , CARLEY, Allison , STEWART, Alison , HIGGINBOTTOM, Michael , SAVORY, Edward , SIMPSON, Iain , NILSSON, Marianne , HARALDSSON, Martin , NORDLING, Erik , KOOLMEISTER, Tobias
发明人： EVANS, David , CARLEY, Allison , STEWART, Alison , HIGGINBOTTOM, Michael , SAVORY, Edward , SIMPSON, Iain , NILSSON, Marianne , HARALDSSON, Martin , NORDLING, Erik , KOOLMEISTER, Tobias
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D471/04
摘要： 2-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}ethan-1-amine; 3- aminopropyl 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxylate; 1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}-4- (dimethylamino)butan-1-one; 5-amino-1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3- yl]piperidin-1-yl}pentan-1-one; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3- c]pyridin-3-yl]piperidine-1-carboxamide; N-(3-aminopropyl)-4-[1-(4-chlorophenyl)-1H- pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3- c]pyridin-3-yl]-N-[3-(dimethylamino)propyl]piperidine-1-carboxamide; 1-({4-[1-(4- chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)piperazine; 4-({4-[1-(4- chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)morpholine; 1-({4-[1-(4- chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)-1,4-diazepane; ethyl 1- [1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; ethyl 1-[1-(4- methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; 1-[1-(4- chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylic acid; N-(2- aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxamide; 4-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4 yl}carbonyl)morpholine; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin- 4-yl}carbonyl)piperazine; {4-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin- 3-yl}methanol; {4-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-2-yl}methanol; [(3R)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3- yl]methanol; methyl 4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3- carboxylate; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3- yl]morpholine-3-carboxamide; 2-{4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3- yl]morpholin-3-yl}ethan-1-ol; methyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3- yl]piperidine-2-carboxylate; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4- c]pyridin-3-yl]piperidine-2-carboxamide; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4- c]pyridin-3-yl]piperidin-2-yl}carbonyl)piperazine; 4-[1-(4-methylphenyl)-1H-pyrrolo[2,3- c]pyridin-3-yl]morpholine; 1-(4-chlorophenyl)-3-(piperidin-4-yl)-1H-pyrrolo[2,3-c]pyridin-4- ol; N-butyl-1-(4-chlorophenyl)-N-methyl-1H-pyrazolo[3,4-c]pyridin-3-amine; 1-[4- (fluoromethyl)phenyl]-3-(oxan-4-yl)-1H-pyrazolo[3,4-c]pyridine; and 3-({4-[1-(4- chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-1-yl}methyl)pyridine are useful for the inhibition of SSAO activity.
摘要翻译： 2- {4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}乙-1-胺; 4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-甲酸3-氨基丙酯; 1- {4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基} -4-（二甲基氨基）丁-1-酮; 5-氨基-1- {4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}戊-1-酮; N-（2-氨基乙基）-4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-甲酰胺; N-（3-氨基丙基）-4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-甲酰胺; 4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基] -N- [3-（二甲基氨基）丙基]哌啶-1-甲酰胺; 1 - （{4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}羰基）哌嗪; 4 - （{4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}羰基）吗啉; 1 - （{4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}羰基）-1,4-二氮杂环庚烷; 1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-甲酸乙酯; 1- [1-（4-甲基苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-甲酸乙酯; 1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-甲酸; N-（2-氨基乙基）-1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-甲酰胺; 4 - （{1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-基}羰基）吗啉; 1 - （{1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-基}羰基）哌嗪; {4- [1-（4-甲基苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-基}甲醇; {4- [1-（4-甲基苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-2-基}甲醇; [（3R）-4- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-基]甲醇; 4- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-羧酸甲酯; N-（2-氨基乙基）-4- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-甲酰胺; 2- {4- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-基}乙-1-醇; 1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-2-甲酸甲酯; N-（2-氨基乙基）-1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-2-甲酰胺; 1 - （{1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-2-基}羰基）哌嗪; 4- [1-（4-甲基苯基）-1H-吡咯并[2,3-c]吡啶-3-基]吗啉; 1-（4-氯苯基）-3-（哌啶-4-基）-1H-吡咯并[2,3-c]吡啶-4-醇; N-丁基-1-（4-氯苯基）-N-甲基-1H-吡唑并[3,4-c]吡啶-3-胺; 1- [4-（氟甲基）苯基] -3-（氧代-4-基）-1H-吡唑并[3,4-c]吡啶; 和3 - （{4- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-1-基}甲基）吡啶可用于抑制SSAO活性。

2. 发明申请

WO2011113798A3 INHIBITORS OF SEMICARABAZIDE - SENSITIVE AMINE OXIDASE 审中-公开
公开(公告)号：WO2011113798A3
公开(公告)日：2011-09-22
申请号：PCT/EP2011/053818
申请日：2011-03-14
申请人： Proximagen Limited , EVANS, David , CARLEY, Allison , STEWART, Alison , HIGGINBOTTOM, Michael , SAVORY, Edward , SIMPSON, Iain , NILSSON, Marianne , HARALDSSON, Martin , NORDLING, Erik , KOOLMEISTER, Tobias
发明人： EVANS, David , CARLEY, Allison , STEWART, Alison , HIGGINBOTTOM, Michael , SAVORY, Edward , SIMPSON, Iain , NILSSON, Marianne , HARALDSSON, Martin , NORDLING, Erik , KOOLMEISTER, Tobias
IPC分类号： C07D471/04 , C07D487/04 , C07D498/08 , A61K31/437 , A61P35/00 , A61P37/06 , A61P11/08 , A61P25/28 , A61P9/10
摘要： Compounds of formula (I) are inhibitors of Semicarbazide-sensitive amine oxidase wherein R 1 , A, X and R 2 are as defined in the claims.

3. 发明申请

WO2008000744A3 2-0'-METHYLADEN0SINE DERIVATIVES AND THEIR USE AS AGONISTS OR ANTAGONISTS OF AN ADENOSINE RECEPTOR 审中-公开
标题翻译： 2-0'-甲基吲哚衍生物及其作为腺苷受体的激动剂或拮抗剂使用
公开(公告)号：WO2008000744A3
公开(公告)日：2008-02-28
申请号：PCT/EP2007056377
申请日：2007-06-26
申请人： BIOVITRUM AB PUBL , SAVORY EDWARD DANIEL
发明人： SAVORY EDWARD DANIEL
IPC分类号： C07D473/18 , A61K31/52 , A61P9/00 , A61P25/00 , A61P29/00 , C07D473/16
CPC分类号： C07D473/18
摘要： The invention relates to a method of improving oral drug absorption of adenosine analogues by the use of 2-methoxy adenosine pro-drugs and to the use of these pro-drugs as medicaments. The invention further relates to compounds that are pro-drugs of adenosine receptor agonists, and to their use as therapeutic compounds, in particular as analgesic or anti-inflammatory compounds, or as disease modifying antirheumatic drugs (DMARDs), and to methods of preventing, treating or ameliorating pain or inflammation using these compounds.
摘要翻译：本发明涉及通过使用2-甲氧基腺苷前药改善腺苷类似物的口服药物吸收的方法以及这些前药用作药物的方法。本发明还涉及作为腺苷受体激动剂的前药的化合物及其作为治疗化合物，特别是作为镇痛或抗炎化合物或作为疾病改善性抗风湿药物（DMARD）的用途的方法，使用这些化合物治疗或改善疼痛或炎症。

4. 发明申请

WO2008000743A3 NOVEL 2',3'-METHYLIDENE ACETYL ADENOSINE PRODRUGS FOR USE AS PRODRUGS FOR ADENOSINE RECEPTOR AGONISTS 审中-公开
标题翻译：新的2'，3'-亚甲基乙酰腺苷类抗生素用作腺苷受体激动剂
公开(公告)号：WO2008000743A3
公开(公告)日：2008-02-21
申请号：PCT/EP2007056375
申请日：2007-06-26
申请人： BIOVITRUM AB PUBL , SAVORY EDWARD DANIEL
发明人： SAVORY EDWARD DANIEL
IPC分类号： C07H19/167 , A61K31/7076 , A61P19/02 , A61P25/02 , A61P29/00
CPC分类号： A61K31/7076 , C07H19/167
摘要： The invention relates to a method of improving oral drug absorption of adenosine analogues by the use of 2',3'-methylidene acetal adenosine pro-drugs and to the use of these pro-drugs as medicaments. The invention further relates to compounds that are prodrugs of adenosine receptor agonists, and to their use as therapeutic compounds, in particular as analgesic or anti-inflammatory compounds, or as disease modifying antirheumatic drugs (DMARDs), and to methods of preventing, treating or ameliorating pain or inflammation using these compounds.
摘要翻译：本发明涉及通过使用2'，3'-亚甲基缩醛腺苷前药改善腺苷类似物的口服药物吸收的方法，以及这些前药用作药物的方法。本发明还涉及作为腺苷受体激动剂的前药的化合物及其作为治疗化合物，特别是作为镇痛或抗炎化合物或作为疾病改善抗风湿药物（DMARD）的用途的方法，以及预防，治疗或使用这些化合物改善疼痛或炎症。

5. 发明申请

WO2012041817A1 7-HYDROXY-PYRAZOLO[1,5-A] PYRIMIDINE COMPOUNDS AND THEIR USE AS CCR2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 7-羟基 - 吡唑并[1,5-A]吡嗪化合物及其作为CCR2受体拮抗剂的用途
公开(公告)号：WO2012041817A1
公开(公告)日：2012-04-05
申请号：PCT/EP2011/066697
申请日：2011-09-26
申请人： PROXIMAGEN LTD , BOYD, Joe, William , MEO, Paul , HIGGINBOTTOM, Michael , SIMPSON, Iain , MOUNTFORD, David , SAVORY, Edward, Daniel
发明人： BOYD, Joe, William , MEO, Paul , HIGGINBOTTOM, Michael , SIMPSON, Iain , MOUNTFORD, David , SAVORY, Edward, Daniel
IPC分类号： C07D487/04 , A61K31/519 , A61P29/00 , A61P35/00
CPC分类号： C07D487/04
摘要： The compounds of formula (I) are antagonists of the CCR2 receptor Wherein R 1-7 and A are as defined in the claims.
摘要翻译：式（I）化合物是CCR2受体的拮抗剂，其中R1-7和A如权利要求中所定义。

6. 发明申请

WO2010031791A1 NEW COMPOUNDS II 审中-公开
标题翻译：新化合物II
公开(公告)号：WO2010031791A1
公开(公告)日：2010-03-25
申请号：PCT/EP2009/062018
申请日：2009-09-16
申请人： BIOVITRUM AB (publ) , SAVORY, Edward , SIMPSON, Iain
发明人： SAVORY, Edward , SIMPSON, Iain
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00
CPC分类号： C07D471/04
摘要： The present invention relates to compounds of formula (I), and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment of medical conditions wherein inhibition of SSAO activity is beneficial, such as such as inflammatory diseases and immune disorders.
摘要翻译：本发明涉及作为SSAO活性抑制剂的式（I）化合物及其药学上可接受的盐，溶剂合物，水合物，几何异构体，互变异构体，旋光异构体或N-氧化物。本发明进一步涉及包含这些化合物的药物组合物和这些化合物用于治疗其中SSAO活性的抑制是有益的医学病症的用途，例如炎性疾病和免疫疾病。

7. 发明申请

WO2008000744A2 THERAPEUTIC COMPOUNDS 审中-公开
标题翻译：治疗化合物
公开(公告)号：WO2008000744A2
公开(公告)日：2008-01-03
申请号：PCT/EP2007/056377
申请日：2007-06-26
申请人： BIOVITRUM AB (publ) , SAVORY, Edward Daniel
发明人： SAVORY, Edward Daniel
IPC分类号： C07D473/18 , C07D473/16 , A61K31/52 , A61P9/00 , A61P25/00 , A61P29/00
CPC分类号： C07D473/18
摘要： The invention relates to a method of improving oral drug absorption of adenosine analogues by the use of 2-methoxy adenosine pro-drugs and to the use of these pro-drugs as medicaments. The invention further relates to compounds that are pro-drugs of adenosine receptor agonists, and to their use as therapeutic compounds, in particular as analgesic or anti-inflammatory compounds, or as disease modifying antirheumatic drugs (DMARDs), and to methods of preventing, treating or ameliorating pain or inflammation using these compounds.
摘要翻译：本发明涉及通过使用2-甲氧基腺苷前药改善腺苷类似物的口服药物吸收的方法以及这些前药用作药物的方法。本发明还涉及作为腺苷受体激动剂的前药的化合物及其作为治疗化合物，特别是作为镇痛或抗炎化合物或作为疾病改善性抗风湿药物（DMARD）的用途的方法，使用这些化合物治疗或改善疼痛或炎症。

8. 发明申请

WO2005084653A3 ADENOSINE RECEPTOR AGONISTS 审中-公开
公开(公告)号：WO2005084653A3
公开(公告)日：2005-09-15
申请号：PCT/GB2005/000800
申请日：2005-03-04
申请人： CAMBRIDGE BIOTECHNOLOGY LIMITED , PRITCHARD, Martyn , OUZMAN, Jacqueline , SAVORY, Edward , BROWN, Giles
发明人： PRITCHARD, Martyn , OUZMAN, Jacqueline , SAVORY, Edward , BROWN, Giles
IPC分类号： C07H19/16
摘要： Use of compounds of general formula (A) as medicaments is described, in particular for the treatment of pain or inflammation; wherein: (I) when X = OH, R 2 = NH 2 , R 5 = CH 2 OH, R 6 = H , R 1 is C 5 -C 6 alkoxy, OCH 2 Cyclopropyl, O-(2,2,3,3-tetrafluoro-cycloButyl), phenoxy, substituted phenoxy, OCH 2 CH 2 OH, or OCH 2 CHF 2 , (5-indanyl)oxy, C 1 , C 2 , C 5 , or C 6 alkylamino, (R) or (S)-sec-Butylamino, C 5 or C 6 cycloalkylamino, exo-norbornane amino, (N-methyl, N-isoamylamino), phenylamino, phenylamino with either rnethoxy or fluoro substituents, a C 2 sulfone group, a C 2 alkyl group, a cyano group, a CONH 2 group, or 3,5-dimethylphenyl; or when X = H, R 2 = NH 2 , R 5 = CH 2 OH , R 6 = H, R 1 is n-hexyloxy; or (II) when X = OH , R 1 = H, R 5 = CH 2 OH, R 6 = H, R 2 is NMe 2 , N-(2-isopentenyl), piperazinyl, (N-Me, N-benzyl), (N-Me, N-CH 2 Ph(3-Br)), (N-Me, N-CH 2 Ph(3-CF 3 )), or (N-Me, N-(2-rnethoxyethyl)), or OCH 2 Cyclopentyl; or (III) when X = OH, R 5 = CONHR 3 , R 6 = H: R 1 is H, R 3 is an isopropyl group, and R 2 is either NH 2 or a methylamino group (NHMe) or an isoamyl group (CH 2 CH 2 CHMe 2 ); or R 1 is H, R 3 is H, and R 2 is NH 2 ; or R 1 is OMe, R 3 is Ph, and R 2 is NH 2 ; or R 1 is NHCH 2 CH 2 CH 2 CH 2 CH 2 Me, R 3 is CH 2 CH 2 CH 2 Me, and R 2 is NH 2 ; or (IV) when X = OH, R 1 = H, R 2 = NH 2 , R 5 = CH 2 NHCOR .4 , R 6 = H, R 4 is n -propyl or NHCH 2 CH 3 ; or (V) when X = OH, R 5 = CH 2 OH, R 6 = H: R 1 is NHCyclohexyl when R 2 is NMe 2 ; or R 1 is OMe when R 2 is NHBenzyl; or (VI) when X = OH , R 2 = NH 2 , R 5 = CH 2 OH, R 6 = Me, R1 is NHCyclohexyl or NHCyclopentyl.

9. 发明申请

WO2005084653A2 THERAPEUTIC COMPOUNDS 审中-公开
标题翻译：治疗化合物
公开(公告)号：WO2005084653A2
公开(公告)日：2005-09-15
申请号：PCT/GB2005000800
申请日：2005-03-04
申请人： CAMBRIDGE BIOTECHNOLOGY LTD , PRITCHARD MARTYN , OUZMAN JACQUELINE , SAVORY EDWARD , BROWN GILES
发明人： PRITCHARD MARTYN , OUZMAN JACQUELINE , SAVORY EDWARD , BROWN GILES
IPC分类号： C07H19/16 , A61K31/00
CPC分类号： C07H19/16
摘要： Use of compounds of general formula (A) as medicaments is described, in particular for the treatment of pain or inflammation; wherein: (I) when X = OH, R2 = NH2, R5 = CH2OH, R6 = H , R1 is C5-C6 alkoxy, OCH2Cyclopropyl, O-(2,2,3,3-tetrafluoro-cycloButyl), phenoxy, substituted phenoxy, OCH2CH2OH, or OCH2CHF2, (5-indanyl)oxy, C1, C2, C5, or C6 alkylamino, (R) or (S)-sec-Butylamino, C5 or C6 cycloalkylamino, exo-norbornane amino, (N-methyl, N-isoamylamino), phenylamino, phenylamino with either rnethoxy or fluoro substituents, a C2 sulfone group, a C2 alkyl group, a cyano group, a CONH2 group, or 3,5-dimethylphenyl; or when X = H, R2 = NH2, R5 = CH2OH , R6 = H, R1 is n-hexyloxy; or (II) when X = OH , R1 = H, R5 = CH2OH, R6 = H, R2 is NMe2, N-(2-isopentenyl), piperazinyl, (N-Me, N-benzyl), (N-Me, N-CH2Ph(3-Br)), (N-Me, N-CH2Ph(3-CF3)), or (N-Me, N-(2-rnethoxyethyl)), or OCH2Cyclopentyl; or (III) when X = OH, R5 = CONHR3, R6 = H: R1 is H, R3 is an isopropyl group, and R2 is either NH2 or a methylamino group (NHMe) or an isoamyl group (CH2CH2CHMe2); or R1 is H, R3 is H, and R2 is NH2; or R1 is OMe, R3 is Ph, and R2 is NH2; or R1 is NHCH2CH2CH2CH2CH2Me, R3 is CH2CH2CH2Me, and R2 is NH2; or (IV) when X = OH, R1 = H, R2 = NH2, R5 = CH2NHCOR.4, R6 = H, R4 is n-propyl or NHCH2CH3; or (V) when X = OH, R5 = CH2OH, R6 = H: R1 is NHCyclohexyl when R2 is NMe2; or R1 is OMe when R2 is NHBenzyl; or (VI) when X = OH , R2 = NH2, R5 = CH2OH, R6 = Me, R1 is NHCyclohexyl or NHCyclopentyl.
摘要翻译：描述了通式（A）的化合物作为药物的用途，特别是用于治疗疼痛或炎症; 其中：（I）X = OH时，R2 = NH2，R5 = CH2OH，R6 = H，R1为C5-C6烷氧基，OCH2环丙基，O-（2,2,3,3-四氟环丁基）苯氧基，OCH2CH2OH或OCH2CHF2，（5-二氢化茚基）氧基，C1，C2，C5或C6烷基氨基，（R）或（S） - 仲丁氨基，C5或C6环烷基氨基，外降冰片烷基氨基，（N-甲基，N-异戊基氨基），苯基氨基，具有甲氧基或氟取代基的苯基氨基，C2砜基，C2烷基，氰基，CONH2基或3,5-二甲基苯基; 或当X = H时，R 2 = NH 2，R 5 = CH 2 OH，R 6 = H，R 1为正己氧基; 或（II）当X = OH时，R1 = H，R5 = CH2OH，R6 = H，R2是NMe2，N-（2-异戊烯基），哌嗪基，（N-Me，N-苄基），（N-Me， N-CH 2 Ph（3-Br）），（N-Me，N-CH 2 Ph（3-CF 3））或（N-Me，N-（2-甲氧基乙基））或OCH 2环戊基; 或（III）当X = OH时，R5 = CONHR3，R6 = H：R1是H，R3是异丙基，R2是NH2或甲基氨基（NHMe）或异戊基（CH2CH2CHMe2）; 或R1为H，R3为H，R2为NH2; 或R1是OMe，R3是Ph，R2是NH2; 或R1是NHCH2CH2CH2CH2CH2Me，R3是CH2CH2CH2Me，R2是NH2; 或（IV）当X = OH时，R1 = H，R2 = NH2，R5 = CH2NHCOR4，R6 = H，R4为正丙基或NHCH2CH3; 或（Ⅴ）当X = OH时，R5 = CH2OH，R6 = H：当R2为NMe2时，R1为NHCyclohexyl; 或当R 2为NH苄基时，R 1为OMe; 或（Ⅵ）当X = OH时，R 2 = NH 2，R 5 = CH 2 OH，R 6 = Me，R 1为NHC环己基或NHC环戊基。

10. 发明申请

WO2005054269A1 IMPROVED SYNTHESIS OF 2-SUBSTITUTED ADENOSINES 审中-公开
标题翻译：改进的2-取代腺苷的合成
公开(公告)号：WO2005054269A1
公开(公告)日：2005-06-16
申请号：PCT/GB2004/005092
申请日：2004-12-03
申请人： CAMBRIDGE BIOTECHNOLOGY LIMITED , SAVORY, Edward, Daniel
发明人： SAVORY, Edward, Daniel
IPC分类号： C07H19/167
CPC分类号： C07H19/167 , Y02P20/55
摘要： A method of synthesis of a 2-substituted adenosine of formula I which comprises converting a compound of formula II to a compound of formula (I), wherein: R is C 1-6 alkoxy (straight or branched), a phenoxy group (unsubstituted, or mono-, or di-substituted by halo, amino, CF3-, cyano, nitro, C 1-6 alkyl, or C 1-6 alkoxy), a benzyloxy group (unsubstituted, or mono-, or di-substituted by halo, amino, CF3-, cyano, nitro, Cl_6 alkyl, or Cl_6 alkoxy), or a benzoyl group (unsubstituted, or mono-, or di-substituted by halo, amino, CF3-, cyano, nitro, C 1-6 alkyl, or C 1-6 alkoxy); R' = H, or a protecting group.
摘要翻译：一种合成式I的2-取代腺苷的方法，其包括将式II化合物转化为式（I）化合物，其中：R是C 1-6烷氧基（直链或支链），苯氧基（未取代的，或被卤素，氨基，CF 3 - ，氰基，硝基，C 1-6烷基或C 1-6烷氧基单取代或二取代的苄氧基，卤素，氨基，CF 3 - ，氰基，硝基，C 1-6烷基或C 1-6烷氧基）或苯甲酰基（未被取代的，或被卤素，氨基，CF 3 - ，氰基，硝基，C 1-6 烷基或C 1-6烷氧基）; R'= H或保护基。

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