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1. 发明公开

EP0629633A2 Dinucleotide analogues, intermediates therefor and oligonucleotides derived therefrom 失效
标题翻译： Dinukleotidanaloga，Zwischenproduktehierfürund daraus abgeleitete寡核苷酸。
公开(公告)号：EP0629633A2
公开(公告)日：1994-12-21
申请号：EP94303883.6
申请日：1994-05-27
申请人： CIBA-GEIGY AG
发明人： Baxter, Anthony David , Baylis, Eric Keith , Collingwood, Stephen Paul , Taylor, Roger John , Weetman, John
IPC分类号： C07H21/00 , C07H19/04 , A61K31/70
CPC分类号： C07H9/04 , C07F9/5304 , C07F9/65586 , C07H7/02 , C07H15/18 , C07H19/06 , C07H21/00 , C07H21/02 , C07H21/04 , Y02P20/55
摘要： A compound of formula

where R 1 is hydrogen, R 1 a or a group of formula

R 1 a is R l b or a protecting group Q,
R 1 b is C 1 -C 20 alkyl, C 2 -C 20 alkenyl, C 3 -C 10 cycloalkyl, C 6 -C 15 aryl, C 7 -C 16 aralkyl or a 5- or 6- membered heterocyclic group attached by a carbon atom in the heterocyclic group to the indicated phosphorus atom,
R 2 is an unsubstituted or substituted C 1 -C 20 alkyl or C 2 -C 20 alkenyl group, an unsubstituted or substituted C 3 -C 10 cycloalkyl group, an unsubstituted or substituted C 6 -C 15 aryl group, an unsubstituted or substituted C 7 -C 16 aralkyl group, or a 5- or 6- membered heterocyclic group attached by a carbon atom in the heterocyclic group to the indicated phosphorus atom,
R 3 is hydrogen, halogen, hydroxy, R 15 , -OR 15 or -OSO 2 R 15
R 4 is R 4 a or together with R 6 denotes a valence bond,
R 4 a is hydrogen, halogen or R 16 ,
R 5 is hydrogen, halogen, hydroxy, R 17 , -OR 17 , -OCOR 17 or -OSO 2 R 17 ,
R 6 is hydrogen, halogen or R 18 , or together with R 4 denotes a valence bond,
R 7 is hydrogen, alkyl-N, N-dialkylphosphoramidyl or R 7 a , or R 7 0- together with R 8 a denotes a C 1 -C 15 hydrocarbylidenedioxy group,
R 7 a is R 19 , -COR 19 , -SO 2 R 19 or tri(C 1 -C 15 hydrocarbyl)silyl,
R 8 is R 8 a or Z,
R 8 a is hydrogen, halogen, hydroxy, R 20 , -OR 20 , -OCOR 20 , -OSO 2 R 20 , or tri(C 1 -C 15 hydrocarbyl)silyloxy, or together with R 9 denotes a C 1 -C 15 hydrocarbylidenedioxy group, or together with R 7 0- denotes a C 1 -C 15 hydrocarbylidenedioxy group,
R 9 is halogen, hydroxy, -OR 21 , -OCOR 21 , -OSO 2 R 21 , or B 2 , or together with R 8 a denotes a C 1 -C 15 hydrocarbylidenedioxy group,
R 10 is hydrogen or R 10 a ,
R 10 a is R 22 , -COR 22 , -SO 2 R 22 or tri(C 1 -C 15 hydrocarbyl)silyl,
R 11 is hydrogen, halogen, hydroxy, R 23 , -OR 23 , -OCOR 23 , -OSO 2 R 23 or Z,
R 12 is hydrogen, halogen or R 24 ,
R 13 is R 13 a or Z,
R 13 a is hydrogen, halogen, hydroxy, R 25 , -OR 25 , -OCOR 25 , -OSO 2 R 25 , or tri(C 1 -C 15 hydrocarbyl)silyloxy, or together with R 14 denotes a C 1 -C 15 hydrocarbylidenedioxy group,
R 14 is halogen, hydroxy, -OR 26 , -OCOR 26 , -OSO 2 R 26 , or B l , or together with R 13 a denotes a C 1 -C 15 hydrocarbylidenedioxy group,
R 15 , R16 , R17 , R18 , R19 R 20, R 21, R 22, R 23, R 24 , R 25 and R 26 are independently a C 1 to C 10 aliphatic group, a C 3 to C 10 cycloaliphatic group, a C 6 to C 15 aromatic group or a C 7 -C 30 araliphatic group,
B 1 and B 2 are independently each a monovalent nucleoside base radical, and
Z is substituted or unsubstituted C 6 -C 10 aryloxythiocarbonyloxy; provided that compounds where simultaneously R 1 , R 3 , R 4 and R 6 are hydrogen, R 2 is isopropyl, R 5 is methoxy, R 7 is methyl, R 8 and R 9 are each hydroxy or each acetoxy or R 8 and R 9 together denote isopropylidenedioxy, compounds where simultaneously R 1 , R 3 , R 4 and R 6 are hydrogen, R 2 is butyl, R 5 is methoxy, R 7 is benzyl, R 8 and R 9 are each hydroxy or each acetoxy or R 8 and R 9 together denote isopropylidenedioxy, and compounds where simultaneously R 1 , R 3 , R 4 , R 5 , R 6 and R 7 are hydrogen, R 2 is phenyl and R 8 and R 9 together denote isopropylidenedioxy are excluded.
摘要翻译：式的化合物，其中R 1是氢，R 1a或式 R 1a的基团是R 1b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芳烷基或通过杂环基中的碳原子与所指示的磷原子连接的5-或6-元杂环基， R 2是未取代或取代的C 1 -C 20烷基或C 2 -C 20烯基，未取代或取代的C 3 -C 10环烷基，未取代或取代的C 6 -C 15芳基，未取代或取代的C 7 -C 16芳烷基，或由杂环基中的碳原子连接到所指示的磷原子上的5或6元杂环基，R 3是氢，卤素，羟基，R 5，-OR 1， R 5或-OSO 2 R 5 R 4是R 4或a与R 6一起代表价键，R 4是氢，卤素或R 1' R 5是氢，卤素，羟基，R 1-7，-OR 1 7，-OCOR 1或7 -OSO 2 R 1，R 6 >是氢，卤素或R 1 <8 >，或与R 4一起表示价键，R 7是氢，烷基-N，N-二烷基磷酰胺基或R 7a，或R 7 O-与R 8一起代表a C 1 -C 15亚烷基二氧基，R 7是R 9，-COR 1 9，-SO 2 R 1 9或三（C 1 -C 15烃基）甲硅烷基， R 8是R 8 a或Z，R 8是氢，卤素，羟基，R 2，-OR 2，-OCOR 2， - 或者三（C 1 -C 15烃基）甲硅烷氧基，或与R 9一起表示C 1 -C 15烃亚基二氧基，或与R 7一起代表C 1 -C 15亚烃基二氧基， R 9是卤素，羟基，-OR 2，-OCOR 2，-OSO 2 R 2，或B 2，或与R 8 a一起表示C1-C15烃基亚二氧基，R 1是氢或R 1，a，R 1a，R 2，R 2，-COR 2， 2，-SO 2 R 2或3（C 1 -C 15烃基）甲硅烷基，R 1是氢，卤素，羟基，R 2，-OR 2， >，-OCOR 2，3，-OSO 2 R 2或Z，R 1，R 2，R 2，R 3，R 4，R 5， R 1 a或Z，R 1'3是氢，卤素，羟基，R 2， OR 2 <5>，-OCOR 2，5-OSO 2 R 2或3（C 1 -C 15烃基）甲硅烷氧基，或与R 1一起表示C1- C 15烃亚基二氧基，R 1 4是卤素，羟基，-OR 2，-OCOR 2，6，-OSO 2 R 2，或B 1，或与R 1'3一起，a表示C 1 -C 15烃基亚二氧基，R 1，R 5，R 1，R 6，R 17，R 18， R 1，R 2，R 2，R 2，R 2，R 2，R 2， 2 <5>和R 2 <6>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 -C 30芳脂基基团，B 1和B 2， 2>各自独立地为一价核苷碱基，Z为取代或未取代的C6-C10芳氧基硫代羰基氧基; 条件是其中R 1，R 3，R 4和R 6同时为氢，R 2为异丙基，R 5为甲氧基，R 7为甲基， 8>和R 9各自为羟基或每个乙酰氧基，或R 8和R 9一起表示异丙二烯基，其中R 1，R 3，R 4和R 6同时为氢，R 2是丁基，R 5是甲氧基，R 7是苄基，R 8和R 9各自是羟基或每个乙酰氧基或R 8和R 9共同表示异丙烯二氧基和其中R 1，R 3，R 4，R 5，R 6和R 7同时为氢的化合物，R 2为苯基，R 8和 R 9一起表示异亚丙二氧基。

2. 发明公开

EP0614907A1 Dinucleotide and oligonucleotide analogues 失效
标题翻译： Dinukleotid和Oligonukleotidanalog。
公开(公告)号：EP0614907A1
公开(公告)日：1994-09-14
申请号：EP94301443.1
申请日：1994-03-01
申请人： CIBA-GEIGY AG
发明人： Baxter, Anthony David , Baylis, Eric Keith , Collingwood, Stephen Paul , Taylor, Roger John , De Mesmaeker, Alain , Schmit, Chantal
IPC分类号： C07H21/00 , C07H19/04 , A61K31/70
CPC分类号： C07H21/00 , C07H19/04
摘要： A dinucleotide analogue of formula

where
B¹ and B² are each independently a monovalent nucleoside base radical;
R¹ is R¹ a or Z;
R¹ a , R², R³ and R⁴ are each independently hydrogen, halogen or hydroxy;
R⁵ is R⁵ a or Z;
R⁶ is hydrogen or R⁶ a ;
R⁷ is hydrogen, alkyl-N,N-dialkylphosphoramidyl or R⁷ a , R⁸ is R⁸ a or Z, or the indicated R⁷O and R⁸ together denote an isopropylidenedioxy group;
R⁵ a and R⁸ a are each independently hydrogen, halogen, hydroxy, -OR¹⁰, -OCOR¹⁰ or silyloxy substituted by three C₁-C₁₅ hydrocarbyl groups;
R⁶ a and R⁷ a are each independently a C₁-C₁₀ aliphatic radical, a C₆-C₁₅ aromatic radical, a C₇-C₃₀ araliphatic radical, -COR¹¹, -SO₂R¹¹ or silyl substituted by three C₁-C₁₅ hydrocarbyl groups;
R⁹ is hydrogen, a C₁-C₈ aliphatic radical, a C₃-C₈ cycloaliphatic radical, a C₆-C₁₅ aromatic radical, a C₇-C₁₃ araliphatic radical, an alkali metal ion or an ammonium ion;
R¹⁰ and R¹¹ are each independently a C₁-C₁₀ aliphatic radical, a C₃-C₈ cycloaliphatic radical, a C₆-C₁₅ aromatic radical or a C₇-C₁₆ araliphatic radical;
R x and R y are independently hydrogen, halogen, hydroxy, a C₁-C₁₀ alkyl, C₂-C₁₀ alkenyl, C₃-C₈ cycloalkyl, C₆-C₁₅ aryl, C₇-C₁₆ aralkyl, C₁-C₁₀ alkoxy, C₂-C₁₀ alkenoxy, C₆-C₁₀ aryloxy or C₇-C₁₆ aralkyloxy group, which is substituted or unsubstituted, or -OCOR z ;
R z is a substituted or unsubstituted C₁-C₁₀ alkyl, C₂-C₁₀ alkenyl, C₃-C₈ cycloalkyl, C₆-C₁₅ aryl or C₇-C₁₆ aralkyl group; and
Z is C₆-C₁₀ aryloxythiocarbonyloxy, the C₆-C₁₀ aryl group being substituted or unsubstituted.
摘要翻译：式的二核苷酸类似物，其中B 1和B 2各自独立地为一价核苷碱基; R 1是R a a或Z; R 1a，R 2，R 3和R 4各自独立地为氢，卤素或羟基; R 5是R 5 a或Z; R 6是氢或R 6 a; R 7是氢，烷基-N，N-二烷基磷酰胺基或R 7 a，R 8是R 8 a或Z，或者所指示的R 7 O和R 8一起表示异丙烯二氧基; R 5 a和R 8各自独立地为氢，卤素，羟基，-OR 1 O，-OCOR 1或0或被三个C 1 -C 15烃基取代的甲硅烷氧基; R 6 a和R 7各自独立地为C 1 -C 10脂族基团，C 6 -C 15芳族基团，C 7 -C 30芳脂族基团，-COR 1，-SO 2 R 1，或被三个C 1 -C 15烃基取代的甲硅烷基; R 9是氢，C 1 -C 8脂族基，C 3 -C 8脂环族基，C 6 -C 15芳基，C 7 -C 13芳脂基，碱金属离子或铵离子; R 1和R 1各自独立地为C 1 -C 10脂族基团，C 3 -C 8脂环族基团，C 6 -C 15芳族基团或C 7 -C 16芳脂族基团; R x和R y独立地是氢，卤素，羟基，C 1 -C 10烷基，C 2 -C 10烯基，C 3 -C 8环烷基，C 6 -C 15芳基，C 7 -C 16芳烷基，C 1 -C 10烷氧基，取代或未取代的C 10链烯氧基，C 6 -C 10芳氧基或C 7 -C 16芳烷氧基，或-OCOR z; R z是取代或未取代的C 1 -C 10烷基，C 2 -C 10烯基，C 3 -C 8环烷基，C 6 -C 15芳基或C 7 -C 16芳烷基; Z为C6-C10芳氧基硫代羰氧基，C6-C10芳基为取代或未取代的。

3. 发明公开

EP0629633A3 Dinucleotide analogues, intermediates therefor and oligonucleotides derived therefrom 失效
标题翻译： DINUCLEOTIDE ANALOGUES，其中间体和衍生自其的寡核苷酸。
公开(公告)号：EP0629633A3
公开(公告)日：1995-01-11
申请号：EP94303883.6
申请日：1994-05-27
申请人： CIBA-GEIGY AG
发明人： Baxter, Anthony David , Baylis, Eric Keith , Collingwood, Stephen Paul , Taylor, Roger John , Weetman, John
IPC分类号： C07H21/00 , C07H19/04 , A61K31/70
CPC分类号： C07H9/04 , C07F9/5304 , C07F9/65586 , C07H7/02 , C07H15/18 , C07H19/06 , C07H21/00 , C07H21/02 , C07H21/04 , Y02P20/55
摘要： A compound of formula

where R 1 is hydrogen, R 1 a or a group of formula
R 1 a is R l b or a protecting group Q, R 1 b is C 1 -C 20 alkyl, C 2 -C 20 alkenyl, C 3 -C 10 cycloalkyl, C 6 -C 15 aryl, C 7 -C 16 aralkyl or a 5- or 6- membered heterocyclic group attached by a carbon atom in the heterocyclic group to the indicated phosphorus atom, R 2 is an unsubstituted or substituted C 1 -C 20 alkyl or C 2 -C 20 alkenyl group, an unsubstituted or substituted C 3 -C 10 cycloalkyl group, an unsubstituted or substituted C 6 -C 15 aryl group, an unsubstituted or substituted C 7 -C 16 aralkyl group, or a 5- or 6- membered heterocyclic group attached by a carbon atom in the heterocyclic group to the indicated phosphorus atom, R 3 is hydrogen, halogen, hydroxy, R 15 , -OR 15 or -OSO 2 R 15 R 4 is R 4 a or together with R 6 denotes a valence bond, R 4 a is hydrogen, halogen or R 16 , R 5 is hydrogen, halogen, hydroxy, R 17 , -OR 17 , -OCOR 17 or -OSO 2 R 17 , R 6 is hydrogen, halogen or R 18 , or together with R 4 denotes a valence bond, R 7 is hydrogen, alkyl-N, N-dialkylphosphoramidyl or R 7 a , or R 7 0- together with R 8 a denotes a C 1 -C 15 hydrocarbylidenedioxy group, R 7 a is R 19 , -COR 19 , -SO 2 R 19 or tri(C 1 -C 15 hydrocarbyl)silyl, R 8 is R 8 a or Z, R 8 a is hydrogen, halogen, hydroxy, R 20 , -OR 20 , -OCOR 20 , -OSO 2 R 20 , or tri(C 1 -C 15 hydrocarbyl)silyloxy, or together with R 9 denotes a C 1 -C 15 hydrocarbylidenedioxy group, or together with R 7 0- denotes a C 1 -C 15 hydrocarbylidenedioxy group, R 9 is halogen, hydroxy, -OR 21 , -OCOR 21 , -OSO 2 R 21 , or B 2 , or together with R 8 a denotes a C 1 -C 15 hydrocarbylidenedioxy group, R 10 is hydrogen or R 10 a , R 10 a is R 22 , -COR 22 , -SO 2 R 22 or tri(C 1 -C 15 hydrocarbyl)silyl, R 11 is hydrogen, halogen, hydroxy, R 23 , -OR 23 , -OCOR 23 , -OSO 2 R 23 or Z, R 12 is hydrogen, halogen or R 24 , R 13 is R 13 a or Z, R 13 a is hydrogen, halogen, hydroxy, R 25 , -OR 25 , -OCOR 25 , -OSO 2 R 25 , or tri(C 1 -C 15 hydrocarbyl)silyloxy, or together with R 14 denotes a C 1 -C 15 hydrocarbylidenedioxy group, R 14 is halogen, hydroxy, -OR 26 , -OCOR 26 , -OSO 2 R 26 , or B l , or together with R 13 a denotes a C 1 -C 15 hydrocarbylidenedioxy group, R 15 , R16 , R17 , R18 , R19 R 20, R 21, R 22, R 23, R 24 , R 25 and R 26 are independently a C 1 to C 10 aliphatic group, a C 3 to C 10 cycloaliphatic group, a C 6 to C 15 aromatic group or a C 7 -C 30 araliphatic group, B 1 and B 2 are independently each a monovalent nucleoside base radical, and Z is substituted or unsubstituted C 6 -C 10 aryloxythiocarbonyloxy; provided that compounds where simultaneously R 1 , R 3 , R 4 and R 6 are hydrogen, R 2 is isopropyl, R 5 is methoxy, R 7 is methyl, R 8 and R 9 are each hydroxy or each acetoxy or R 8 and R 9 together denote isopropylidenedioxy, compounds where simultaneously R 1 , R 3 , R 4 and R 6 are hydrogen, R 2 is butyl, R 5 is methoxy, R 7 is benzyl, R 8 and R 9 are each hydroxy or each acetoxy or R 8 and R 9 together denote isopropylidenedioxy, and compounds where simultaneously R 1 , R 3 , R 4 , R 5 , R 6 and R 7 are hydrogen, R 2 is phenyl and R 8 and R 9 together denote isopropylidenedioxy are excluded.

4. 发明公开

EP0614906A1 Mononucleotide analogues and intermediates therefor 失效
标题翻译：单核苷酸类似物及其中间体
公开(公告)号：EP0614906A1
公开(公告)日：1994-09-14
申请号：EP94301441.5
申请日：1994-03-01
申请人： CIBA-GEIGY AG
发明人： Baxter, Anthony David , Baylis, Eric Keith , Collingwood, Stephen Paul , Taylor, Roger John , De Mesmaeker, Alain , Schmit, Chantal
IPC分类号： C07H19/10 , C07H19/20 , C07H21/00 , A61K31/70
CPC分类号： C07H19/10 , C07H19/20 , C07H21/00 , Y02P20/55
摘要： A compound of formula

where
R¹ is hydrogen or a protecting group Q;
R² is hydrogen, a C₁-C₈ aliphatic radical, a C₆-C₁₅ aromatic radical, a C₃-C₈ cycloaliphatic radical, a C₇-C₁₃ araliphatic radical, an alkali metal ion or an ammonium ion;
R³ and R⁴ are independently hydrogen, halogen or hydroxy;
R⁵ is C₆-C₁₀ aryloxythiocarbonyloxy, the C₆-C₁₀ aryl group being unsubstituted or substituted, or R⁵ a ;
R⁵ a is hydrogen, fluorine, chlorine, hydroxy, -OR⁸, -OCOR⁸ or silyloxy substituted by three C₁-C₁₅ hydrocarbyl groups;
R⁶ is hydrogen, a C₁-C₁₀ aliphatic radical, a C₆-C₁₅ aromatic radical, a C₇-C₁₆ araliphatic radical, -COR⁹, -SO₂R⁹ or silyl substituted by three C₁-C₁₅ hydrocarbyl groups;
R⁷ is a monovalent nucleoside base radical, hydroxyl, -OR⁸ or -OCOR⁸, and and
R⁹ are independently a C₁-C₁₀ aliphatic radical, a C₃-C₈ cycloaliphatic radical, a C₆-C₁₅ aromatic radical or a C₇-C₁₆ araliphatic radical; or
R⁵ and the indicated R⁶O-together denote an isopropylidenedioxy group or R⁵ and R⁷ together denote an isopropylidenedioxy group, provided that when R⁵ and R⁷ together denote isopropylidenedioxy, R¹ R², R³ R⁴ and R⁶ are not all hydrogen.
摘要翻译：其中R 1是氢或保护基Q的下式化合物; R 2是氢，C 1 -C 8脂族基，C 6 -C 15芳族基，C 3 -C 8脂环族基，C 8 -C 13芳脂族基，碱金属离子或铵离子; R 3和R 4独立地为氢，卤素或羟基; R 5是C 6 -C 10芳氧基硫代羰基氧基，C 6 -C 10芳基是未取代或取代的，或R 5a; R 5a是氢，氟，氯，羟基，-OR 7，-OCOR 8或被三个C 1 -C 15烃基取代的甲硅烷氧基; R 7是氢，C 1 -C 10脂族基团，C 6 -C 15芳族基团，C 8 -C 16芳脂族基团，-COR 6，-SO 2 R 7或被三个C 1 -C 15烃基取代的甲硅烷基; R 6是单价核苷碱基，羟基，-OR 7或-OCOR 7，和R 7分别是C 1 -C 10脂族基团，C 3 -C 8脂环族基团，C 6 -C 15芳族基团或C 8 -C 16芳脂族基团; 或R 5和所示的R 10一起表示异亚丙基二氧基或R 5和R 6一起表示异亚丙基二氧基，条件是当R 5和R 6一起表示异亚丙基二氧基时，R 1，R 2，R 3和R 4不全是氢。

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