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31. 发明授权

US06562960B1 Oligonucleotide analogues 失效
标题翻译：寡核苷酸类似物
公开(公告)号：US06562960B1
公开(公告)日：2003-05-13
申请号：US09142212
申请日：1998-10-09
申请人： Anthony David Baxter , Stephen Paul Collingwood , Mark Edward Douglas , Roger John Taylor
发明人： Anthony David Baxter , Stephen Paul Collingwood , Mark Edward Douglas , Roger John Taylor
IPC分类号： C07H2100
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 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 nucleside, R1 is hydrogen, hydroxy, O—, thiol, S—, —NH2 or a group of formula R1a, —OR1a, —SR1a, —NHR1b, or —NR1bR1c wherein R1a 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 R1b and R1c 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 R1b and R1c together with the nitrogen atom to which they are attached denote a five- or six-membered heterocyclic ring, and X is oxygen or sulfur.
摘要翻译：具有10至200个天然和/或合成的核苷单位的寡核苷酸类似物，通过核苷间键连接，至少一个位于所指定的亚甲基上的核苷间键与核苷的3'碳原子连接，所指示的氧原子连接在相邻核苷酸的5'-碳原子上，R 1是氢，羟基，O-，硫醇，S-，-NH 2或式R1a，-OR1a，-SR1a，-NHR1b或-NR1bR1c的基团，其中 R1a是未取代或取代的C1至C10烷基，C2至C10烯基，C3至C8环烷基，C6至C10芳基或C7至C13芳烷基; R1b和R1c各自独立地为未取代或取代的C1至C10烷基，C2至C10烯基，C3至C8环烷基，C6至C10芳基或C7至C13芳烷基或R1b和R1c与它们所连接的氮原子一起表示五元或六元杂环，X是氧或硫。

32. 发明授权

US6087490A Dinucleotide and oligonucleotide analogues 失效
标题翻译：二核苷酸和寡核苷酸类似物
公开(公告)号：US6087490A
公开(公告)日：2000-07-11
申请号：US155198
申请日：1998-10-08
申请人： Anthony David Baxter , Eric Keith Baylis , Stephen Paul Collingwood , Robin Alec Fairhurst , Roger John Taylor
发明人： Anthony David Baxter , Eric Keith Baylis , Stephen Paul Collingwood , Robin Alec Fairhurst , Roger John Taylor
IPC分类号： C07H19/06 , C07H21/00 , C07H19/00 , C07H21/02 , C07H21/04
CPC分类号： C07H19/06 , C07H21/00 , Y02P20/55
摘要： A compound which is a dinucleotide analogue of formula ##STR1## or a salt thereof, where B.sup.1 and B.sup.2 are each independently a monovalent nucleoside base radical,R.sup.1 is hydrogen or Y.sup.1,R.sup.2 and R.sup.3 are each independently hydrogen, halogen, hydroxy or --OY.sup.2,R.sup.4 is hydrogen, halogen, hydroxy, --OY.sup.3 or R.sup.7,R.sup.5 is hydrogen, halogen or R.sup.8,R.sup.6 is hydrogen, Y.sup.4 or a phosphoramidyl group,Z is a group of formula II, III or IV ##STR2## where R.sup.9 is hydrogen, halogen, hydroxy, --OY.sup.5 or R.sup.13, R.sup.10 is hydrogen, halogen or R.sup.14, R.sup.11 is hydroxy, R.sup.15 or --OR.sup.15 where R.sup.15 is a C.sub.1 to C.sub.10 aliphatic group, a C.sub.3 to C.sub.8 cycloaliphatic group, a C.sub.6 to C.sub.10 aromatic group or a C.sub.7 to C.sub.13 araliphatic group, and R.sup.12 is hydrogen, R.sup.12.sub.a or --OCOR.sup.12.sub.a where R.sup.12.sub.a is a C.sub.1 to C.sub.10 aliphatic group, a C.sub.3 to C.sub.8 cycloaliphatic group, a C.sub.6 to C.sub.10 aromatic group or a C.sub.7 to C.sub.13 araliphatic group, Y.sup.1, Y.sup.2, Y.sup.3, Y.sup.4 and Y.sup.5 are each indpendently a hydroxy-protecting group, and R.sup.7, R.sup.8, R.sup.13 and R.sup.14 are each independently a C.sub.1 to C.sub.10 aliphatic group, a C.sub.3 to C.sub.8 cycloaliphatic group, a C.sub.6 to C.sub.10 aromatic group or a C.sub.7 to C.sub.13 araliphatic group.
摘要翻译： PCT No.PCT / GB97 / 00651 Sec。 371日期：1998年10月8日 102（e）日期1998年10月8日PCT 1997年11月3日PCT PCT。公开号WO97 / 35869 日期1997年10月2日为式或二价核苷酸类似物的化合物或其盐，其中B1和B2各自独立地为一价核苷碱基，R1为氢或Y1，R2和R3各自独立地为氢，卤素，羟基或 -OY2，R4是氢，卤素，羟基，-OY3或R7，R5是氢，卤素或R8，R6是氢，Y4或磷酰胺基，Z是式II，III或IV的基团，其中R9是氢，卤素，羟基，-OY5或R13，R10为氢，卤素或R14，R11为羟基，R15或-OR15，其中R15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-OCOR12a，其中R12a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，Y1，Y2， Y3，Y4和Y5各自独立地为羟基保护基，R7，R8，R13和R14各自独立地为C1至C10脂族基团，C3t 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。

33. 发明授权

US5670489A Oligonucleotide analogues 失效
标题翻译：寡核苷酸类似物
公开(公告)号：US5670489A
公开(公告)日：1997-09-23
申请号：US463139
申请日：1995-06-02
申请人： Anthony David Baxter , Eric Keith Baylis , Stephen Paul Collingwood , Roger John Taylor , Alain De Mesmaeker , Chantal Schmit
发明人： Anthony David Baxter , Eric Keith Baylis , Stephen Paul Collingwood , Roger John Taylor , Alain De Mesmaeker , Chantal Schmit
IPC分类号： G01N33/569 , A61K31/665 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61K31/7076 , A61P31/12 , A61P31/16 , C07F9/6512 , C07F9/655 , C07F9/6561 , C07H19/04 , C07H19/06 , C07H19/16 , C07H21/00 , C07H21/04
CPC分类号： C07H21/00 , C07H19/04
摘要： A dinucleotide analogue of formula ##STR1## where B.sup.1 and B.sup.2 are each independently a monovalent nucleoside base radical; R.sup.1 is R.sup.1.sub.a or Z; R.sup.1.sub.a, R.sup.2, R.sup.3 and R.sup.4 are each independently hydrogen, halogen or hydroxy; R.sup.5 is R.sup.5.sub.a or Z; R.sup.6 is hydrogen or R.sup.6.sub.a ; R.sup.7 is hydrogen, alkyl-N,N-dialkylphosphoramidyl or R.sup.7.sub.a, R.sup.8 is R.sup.8.sub.a or Z, or the indicated R.sup.7 O and R.sup.8 together denote an isopropylidenedioxy group; R.sup.5.sub.a and R.sup.8.sub.a are each independently hydrogen, halogen, hydroxy, --OR.sup.10, --OCOR.sup.10 or silyloxy substituted by three C.sub.1 -C.sub.5 hydrocarbyl groups; R.sup.6.sub.a and R.sup.7.sub.a are each independently a C.sub.1 -C.sub.10 aliphatic radical, a C.sub.6 -C.sub.15 aromatic radical, a C.sub.7 -C.sub.30 araliphatic radical, --COR.sup.11, --SO.sub.2 R.sup.11 or silyl substituted by three C.sub.1 -C.sub.15 hydrocarbyl groups; R.sup.9 is hydrogen, a C.sub.1 -C.sub.8 aliphatic radical, a C.sub.3 -C.sub.8 cycloaliphatic radical, a C.sub.6 -C.sub.15 aromatic radical, a C.sub.7 -C.sub.13 araliphatic radical, an alkali metal ion or an ammonium ion; R.sup.10 and R.sup.11 are each independently a C.sub.1 -C.sub.10 aliphatic radical, a C.sub.3 -C.sub.8 cycloaliphatic radical, a C.sub.6 -C.sub.15 aromatic radical or a C.sub.7 -C.sub.16 araliphatic radical; R.sup.x and R.sup.y are independently hydrogen, halogen, hydroxy, a C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.6 -C.sub.15 aryl, C.sub.7 -C.sub.16 aralkyl, C.sub.1 -C.sub.10 alkoxy, C.sub.2 -C.sub.10 alkenoxy, C.sub.6 -C.sub.10 aryloxy or C.sub.7 -C.sub.16 aralkyloxy group, which is substituted or unsubstituted, or --OCOR.sub.z ; R.sup.z is a substituted or unsubstituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.6 -C.sub.15 aryl or C.sub.7 -C.sub.16 aralkyl group; and Z is C.sub.6 -C.sub.10 aryloxythiocarbonyloxy, the C.sub.6 -C.sub.10 aryl group being substituted or unsubstituted.
摘要翻译：式Ⅰ的二核苷酸类似物，其中B1和B2各自独立地是一价核苷碱基; R1为R1a或Z; R1a，R2，R3和R4各自独立地为氢，卤素或羟基; R5为R5a或Z; R6是氢或R6a; R7是氢，烷基-N，N-二烷基磷酰胺基或R7a，R8是R8a或Z，或者所指示的R7O和R8一起表示异丙烯二氧基; R5a和R8a各自独立地为氢，卤素，羟基，-OR10，-OCOR10或被三个C1-C5烃基取代的甲硅烷氧基; R6a和R7a各自独立地为C1-C10脂族基团，C6-C15芳族基团，C7-C30芳脂族基团，-COR11，-SO2R11或被三个C1-C15烃基取代的甲硅烷基基团; R9是氢，C1-C8脂族基团，C3-C8脂环族基团，C6-C15芳族基团，C7-C13芳脂族基团，碱金属离子或铵离子; R 10和R 11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; Rx和Ry独立地是氢，卤素，羟基，C1-C10烷基，C2-C10烯基，C3-C8环烷基，C6-C15芳基，C7-C16芳烷基，C1-C10烷氧基，C2-C10链烯氧基，C6-C10 取代或未取代的芳氧基或C7-C16芳烷氧基，或-OCORz; Rz是取代或未取代的C1-C10烷基，C2-C10烯基，C3-C8环烷基，C6-C15芳基或C7-C16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。

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