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1. 发明申请

WO2009071668A3 PIPERAZINE DERIVATIVES AND THEIR USE AS LEPTIN RECEPTOR MODULATORS 审中-公开
标题翻译：哌嗪衍生物及其作为受体调节剂的使用
公开(公告)号：WO2009071668A3
公开(公告)日：2009-08-20
申请号：PCT/EP2008066899
申请日：2008-12-05
申请人： BIOVITRUM AB PUBL , BOYD JOSEPH W , BROWN GILES A , HIGGINBOTTOM MICHAEL , SIMPSON IAIN , HORGAN VIET-ANH ANNE NEE NGUYE , OUZMAN JACQUELINE
发明人： BOYD JOSEPH W , BROWN GILES A , HIGGINBOTTOM MICHAEL , SIMPSON IAIN , HORGAN VIET-ANH ANNE , OUZMAN JACQUELINE
IPC分类号： C07D295/205 , A61K31/445 , A61K31/495 , A61P3/00
CPC分类号： C07D295/205
摘要： The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds, to processes for their preparation, and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.
摘要翻译：本发明涉及新的式（I）化合物，包含这些化合物的药物组合物，其制备方法以及这些化合物作为瘦素受体调节剂模拟物在制备抗体与体重增加相关的病症中的用途， 2型糖尿病和血脂异常。

2. 发明申请

WO2005070947A1 SYNTHESIS OF SPONGOSINE 审中-公开
标题翻译：松香的合成
公开(公告)号：WO2005070947A1
公开(公告)日：2005-08-04
申请号：PCT/GB2005/000183
申请日：2005-01-19
申请人： CAMBRIDGE BIOTECHNOLOGY LIMITED , OUZMAN, Jacqueline, Valerie, Anne
发明人： OUZMAN, Jacqueline, Valerie, Anne
IPC分类号： C07H19/16
CPC分类号： C07H19/16
摘要： Reaction of 1- O -acetyl-2,3,5-tri- O -benzoyl-β-D-ribofuranose with 2-methoxyadenine to form 9-(2’,3’,5’-tri- O -benzoyl-β-D-ribofuranosyl)-2-methoxyadenine, then deprotection of the 9-(2’,3’,5’-tri- O -benzoyl-β-D-ribofuranosyl)-2-methoxyadenine to form spongosine is described. Synthesis of intermediates for use in the synthesis of spongosine is also described.
摘要翻译： 1-O-乙酰基-2,3,5-三-O-苯甲酰基-β-D-呋喃核糖与2-甲氧基腺嘌呤的反应形成9-（2'，3'，5'-三-O-苯甲酰基-β -D-呋喃核糖基）-2-甲氧基腺嘌呤，然后描述9-（2'，3'，5'-三-O-苯甲酰基-β-D-呋喃核糖基）-2-甲氧基腺嘌呤脱保护以形成海绵体。还描述了用于合成海绵体的中间体的合成。

3. 发明申请

WO2005056571A1 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：WO2005056571A1
公开(公告)日：2005-06-23
申请号：PCT/GB2004/005090
申请日：2004-12-03
申请人： CAMBRIDGE BIOTECHNOLOGY LIMITED , BROWN, Giles, Albert , SAVORY, Edward, Daniel , OUZMAN, Jacqueline, Valerie, Anne , STODDART, Alison, Margaret
发明人： BROWN, Giles, Albert , SAVORY, Edward, Daniel , OUZMAN, Jacqueline, Valerie, Anne , STODDART, Alison, Margaret
IPC分类号： C07H1/00
CPC分类号： C07H1/00 , C07H19/16
摘要： Synthesis of 2-substituted adenosines of formula (I) using 2-nitro pentabenzoyl adenosine, or 2-nitro pentaacetyl adenosine, as intermediate is described: Formula (I) wherein R = C 1-6 alkoxy (straight or branched), a phenoxy group (unsubstituted, or mono-, or di-substituted by halo, amino, CF 3 -, cyano, nitro, C 1-6 alkyl, or C 1-6 alkoxy), a benzyloxy group (unsubstituted, or mono-, or di-substituted by halo, amino, CF 3 -, cyano, nitro, C 1-6 alkyl, or C 1-6 alkoxy), or a benzoyl group (unsubstituted, or mono-, or di-substituted by halo, amino, CF 3 -,cyano, nitro, C 1-6 alkyl, or C 1-6 alkoxy). The methods provide improved yield and purity of product.
摘要翻译：描述了使用2-硝基五苯甲酰基腺苷或2-硝基五乙酰基腺苷作为中间体合成式（I）的2-取代腺苷：式（I）其中R = 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），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）。这些方法提供了产品的产率和纯度的提高。

4. 发明申请

WO2009071668A2 NEW COMPOUNDS II 审中-公开
标题翻译：新化合物II
公开(公告)号：WO2009071668A2
公开(公告)日：2009-06-11
申请号：PCT/EP2008/066899
申请日：2008-12-05
申请人： BIOVITRUM AB (PUBL) , BOYD, Joseph, W. , BROWN, Giles, A. , HIGGINBOTTOM, Michael , SIMPSON, Iain , HORGAN, Viet-Anh Anne (nee Nguyen) , OUZMAN, Jacqueline
发明人： BOYD, Joseph, W. , BROWN, Giles, A. , HIGGINBOTTOM, Michael , SIMPSON, Iain , HORGAN, Viet-Anh Anne (nee Nguyen) , OUZMAN, Jacqueline
CPC分类号： C07D295/205
摘要： The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds, to processes for their preparation, and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.
摘要翻译：本发明涉及新的式（I）化合物，包含这些化合物的药物组合物，其制备方法以及这些化合物作为瘦素受体调节剂模拟物在制备抗体与体重增加相关的病症中的用途， 2型糖尿病和血脂异常。

5. 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.

6. 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。

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