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1. 发明申请

US20090252783A1 MEANS FOR INHIBITING THE EXPRESSION OF CD31 审中-公开
标题翻译：意思是抑制CD31的表达
公开(公告)号：US20090252783A1
公开(公告)日：2009-10-08
申请号：US12297592
申请日：2007-04-20
申请人： Jorg Kaufmann , Oliver Keil , Ansgar Santel
发明人： Jorg Kaufmann , Oliver Keil , Ansgar Santel
IPC分类号： A61K9/127 , A61K35/00 , C12N5/00 , C12N15/63 , A61K31/7088 , C07H21/02
CPC分类号： C12N15/1138 , C12N2310/14
摘要： The present invention is related to a nucleic acid molecule comprising a double-stranded structure, whereby the double-stranded structure comprises a first strand and a second strand, whereby the first strand comprises a first stretch of contiguous nucleotides and said first stretch is at least partially complementary to a target nucleic acid, and whereby the second strand comprises a second stretch of contiguous nucleotides and said second stretch is at least partially complementary to the first stretch, whereby the first stretch comprises a nucleic acid sequence which is at least complementary to a nucleotide core sequence of the nucleic acid sequence according to SEQ ID NO: 1, whereby the nucleotide core sequence comprises the nucleotide sequence from nucleotide positions 1277 to 1295 of SEQ ID NO: 1; from nucleotide positions 2140 to 2158 of SEQ ID NO:1; from nucleotide positions 2391 to 2409 of SEQ ID NO: 1; and whereby the first stretch is additionally at least partially complementary to a region preceding the 5′ end of the nucleotide core sequence and/or to a region following the 3′ end of the nucleotide core sequence.
摘要翻译：本发明涉及包含双链结构的核酸分子，由此双链结构包含第一链和第二链，其中第一链包含连续核苷酸的第一段，并且所述第一段至少是与靶核酸部分互补，并且其中所述第二链包含连续核苷酸的第二段，所述第二段与所述第一段至少部分互补，其中所述第一段包含与至少互补的核酸序列核苷酸核心序列包含SEQ ID NO：1的核苷酸序列1277〜1295的核苷酸序列; 从SEQ ID NO：1的核苷酸位置2140至2158; 从SEQ ID NO：1的核苷酸位置2391至2409; 并且其中第一段延伸另外至少部分地与核苷酸核心序列的5'末端之前的区域和/或与核苷酸核心序列的3'末端之后的区域互补。

2. 发明授权

US08232256B2 Means for inhibiting the expression of protein kinase 3 有权
标题翻译：抑制蛋白激酶3表达的方法
公开(公告)号：US08232256B2
公开(公告)日：2012-07-31
申请号：US12307052
申请日：2007-07-20
申请人： Jorg Kaufmann , Oliver Keil , Ansgar Santel
发明人： Jorg Kaufmann , Oliver Keil , Ansgar Santel
IPC分类号： C12N15/11 , C12N5/00 , C07H21/02 , C07H21/04 , C12Q1/68 , C12P19/34
CPC分类号： C12N15/1137 , C12N2310/14 , C12N2310/321 , C12N2310/3521
摘要： The present invention is related to a nucleic acid molecule and uses thereof. The nucleic acid molecule comprises a double-stranded structure, whereby the double-stranded structure comprises a first strand and a second strand, whereby the first strand comprises a first stretch of contiguous nucleotides and said first stretch is at least partially complementary to a target nucleic acid, and whereby the second strand comprises a second stretch of contiguous nucleotides and said second stretch is at least partially complementary to the first stretch, whereby the first stretch comprises a nucleic acid sequence which is at least partially complementary to a nucleotide core sequence of the nucleic acid sequence according to SEQ ID NO:1 (NM_013355).
摘要翻译：本发明涉及核酸分子及其用途。所述核酸分子包含双链结构，由此所述双链结构包含第一链和第二链，其中所述第一链包含连续核苷酸的第一段，并且所述第一段与靶核酸至少部分互补并且其中所述第二链包含连续核苷酸的第二段，并且所述第二段与所述第一区段至少部分互补，其中所述第一区段包含核酸序列，所述核酸序列与所述第一区段的核苷酸核心序列至少部分互补根据SEQ ID NO：1的核酸序列（NM_013355）。

3. 发明申请

US20090074852A1 LIPOPLEX FORMULATIONS FOR SPECIFIC DELIVERY TO VASCULAR ENDOTHELIUM 审中-公开
标题翻译：用于特异性输送到血管内皮的LIPOPLEX制剂
公开(公告)号：US20090074852A1
公开(公告)日：2009-03-19
申请号：US12297611
申请日：2007-04-20
申请人： Jorg Kaufmann , Oliver Keil , Ansgar Santel
发明人： Jorg Kaufmann , Oliver Keil , Ansgar Santel
IPC分类号： A61K9/127 , A61K31/16 , A61K31/7088 , C07H21/02 , C12N5/02 , C12Q1/02 , A61P35/04
CPC分类号： A61K9/1271 , A61K9/1272 , A61K47/6911 , A61K48/00
摘要： The present invention is related to a lipid composition contained in and/or containing a carrier comprising at least a first lipid component, at least a first helper lipid, and a shielding compound which is optionally removable from the lipid composition under in vivo conditions, whereby the lipid composition containing carrier has an osmolarity of about 50 to 600 mosmole/kg, preferably about 250-350 mosmole/kg, and more preferably about 280 to 320 mosmole/kg, and/or whereby liposomes formed by the first lipid component and/or one or both of the helper lipid and the shielding compound in the carrier have a particle size of about 20 to 200 nm, preferably about 30 to 100 nm, and more preferably about 40 to 80 mm.
摘要翻译：本发明涉及含有载体和/或含有载体的脂质组合物，其包含至少第一种脂质组分，至少第一辅助脂质和在体内条件下任选地从脂质组合物中除去的屏蔽化合物，由此含脂质组合物的载体具有约50至600 mosmol / kg，优选约250-350 mosmol / kg，更优选约280至320 mosmol / kg的渗透压，和/或其中由第一脂质组分和/ 或载体中辅助脂质和屏蔽化合物中的一种或两种具有约20至200nm，优选约30至100nm，更优选约40至80mm的粒度。

4. 发明授权

US08357722B2 Lipids, lipid complexes and use thereof 有权
标题翻译：脂质，脂质复合物及其用途
公开(公告)号：US08357722B2
公开(公告)日：2013-01-22
申请号：US13230085
申请日：2011-09-12
申请人： Oliver Keil , Jorg Kaufmann , Ansgar Santel
发明人： Oliver Keil , Jorg Kaufmann , Ansgar Santel
IPC分类号： A61K31/165
CPC分类号： C07C209/50 , A61K9/1271 , A61K9/1272 , A61K31/713 , A61K47/183 , A61K47/186 , A61K47/24 , A61K47/543 , A61K47/544 , A61K47/6911 , C07C231/02 , C07C279/14 , C12N15/111 , C12N15/113 , C12N15/1138 , C12N2310/14 , C12N2310/321 , C12N2320/32 , C12N2310/3521
摘要： The present invention is related to a compound according to formula (I), wherein R1 and R2 are each and independently selected from the group comprising alkyl; n is any integer between 1 and 4; R3 is an acyl selected from the group comprising lysyl, ornithyl, 2,4-diaminobutyryl, histidyl and an acyl moiety according to formula (II), wherein m is any integer from 1 to 3 and Y− is a pharmaceutically acceptable anion.
摘要翻译：本发明涉及式（I）化合物，其中R 1和R 2各自独立地选自烷基; n是1到4之间的整数; R3是选自根据式（II）的赖氨酰，鸟氨酰基，2,4-二氨基丁酰基，组氨酰基和酰基部分的酰基，其中m是1至3的任何整数，Y-是药学上可接受的阴离子。

5. 发明授权

US08722875B2 Means for inhibiting the expression of Orc-1 失效
标题翻译：抑制Orc-1表达的方法
公开(公告)号：US08722875B2
公开(公告)日：2014-05-13
申请号：US13120430
申请日：2009-09-23
申请人： Manfred Gossen , Ansgar Santel , Jorg Kaufmann
发明人： Manfred Gossen , Ansgar Santel , Jorg Kaufmann
IPC分类号： C07H21/04 , C12Q1/68 , C12N15/11 , C12N5/02 , C12N5/00
CPC分类号： C12N15/1135 , C12N15/113 , C12N2310/14
摘要： The present invention is related to a nucleic acid molecule comprising a double-stranded structure, whereby the double-stranded structure comprises a first strand and a second strand, whereby the first strand comprises a first stretch of contiguous nucleotides and said first stretch is at least partially complementary to a target nucleic acid, and whereby the second strand comprises a second stretch of contiguous nucleotides and said second stretch is at least partially complementary to the first stretch, whereby the first stretch comprises a nucleic acid sequence which is at least complementary to a nucleotide core sequence of the nucleic acid sequence according to SEQ ID NO: 1, whereby the nucleotide core sequence comprises the nucleotide sequence from nucleotide positions 1755 to 1763 of SEQ ID NO: 1; from nucleotide positions 1904 to 1912 of SEQ.ID.No.1; from nucleotide positions 1905 to 1913 of SEQ ID NO: 1; from nucleotide positions 2548 to 2556 of SEQ ID NO: 1; whereby the first stretch is additionally at least partially complementary to a region preceding the 5′ end of the nucleotide core sequence and/or to a region following the 3′ end of the nucleotide core sequence.
摘要翻译：本发明涉及包含双链结构的核酸分子，由此双链结构包含第一链和第二链，其中第一链包含连续核苷酸的第一段，并且所述第一段至少是与靶核酸部分互补，并且其中所述第二链包含连续核苷酸的第二段，所述第二段与所述第一段至少部分互补，由此所述第一段包含与至少互补的核酸序列核苷酸核心序列包含SEQ ID NO：1的核苷酸序列1755至1763的核苷酸序列; 从SEQ.ID.No.1的核苷酸位置1904到1912; 从SEQ ID NO：1的核苷酸位置1905到1913; 从SEQ ID NO：1的核苷酸位置2548至2556; 其中第一次拉伸另外至少部分地与核苷酸核心序列的5'末端之前的区域和/或与核苷酸核心序列的3'末端之后的区域互补。

6. 发明申请

US20120065138A1 LIPIDS, LIPID COMPLEXES AND USE THEREOF 有权
标题翻译：脂肪酸，脂质复合物及其用途
公开(公告)号：US20120065138A1
公开(公告)日：2012-03-15
申请号：US13230085
申请日：2011-09-12
申请人： OLIVER KEIL , Jorg Kaufmann , Ansgar Santel
发明人： OLIVER KEIL , Jorg Kaufmann , Ansgar Santel
IPC分类号： A61K38/02 , A61K31/7088 , A61P9/00 , C12Q1/02 , C07C209/50 , A61P35/00 , A61K47/18 , C12N5/071
CPC分类号： C07C209/50 , A61K9/1271 , A61K9/1272 , A61K31/713 , A61K47/183 , A61K47/186 , A61K47/24 , A61K47/543 , A61K47/544 , A61K47/6911 , C07C231/02 , C07C279/14 , C12N15/111 , C12N15/113 , C12N15/1138 , C12N2310/14 , C12N2310/321 , C12N2320/32 , C12N2310/3521
摘要： The present invention is related to a compound according to formula (I), wherein R1 and R2 are each and independently selected from the group comprising alkyl; n is any integer between 1 and 4; R3 is an acyl selected from the group comprising lysyl, ornithyl, 2,4-diaminobutyryl, histidyl and an acyl moiety according to formula (II), wherein m is any integer from 1 to 3 and Y− is a pharmaceutically acceptable anion.
摘要翻译：本发明涉及式（I）化合物，其中R 1和R 2各自独立地选自烷基; n是1到4之间的整数; R3是选自根据式（II）的赖氨酰，鸟氨酰基，2,4-二氨基丁酰基，组氨酰基和酰基部分的酰基，其中m是1至3的任何整数，Y-是药学上可接受的阴离子。

7. 发明申请

US20110294871A1 LIPIDS, LIPID COMPLEXES AND USE THEREOF 审中-公开
标题翻译：脂肪酸，脂质复合物及其用途
公开(公告)号：US20110294871A1
公开(公告)日：2011-12-01
申请号：US13173296
申请日：2011-06-30
申请人： OLIVER KEIL , Jorg Kaufmann , Ansgar Santel
发明人： OLIVER KEIL , Jorg Kaufmann , Ansgar Santel
IPC分类号： A61K31/713 , C12N5/071 , C12N5/0783 , C12N5/078 , C12N5/0787 , C07H21/02 , C12N5/0786
CPC分类号： C07C209/50 , A61K9/1271 , A61K9/1272 , A61K31/713 , A61K47/183 , A61K47/186 , A61K47/24 , A61K47/543 , A61K47/544 , A61K47/6911 , C07C231/02 , C07C279/14 , C12N15/111 , C12N15/113 , C12N15/1138 , C12N2310/14 , C12N2310/321 , C12N2320/32 , C12N2310/3521
摘要： The present invention is related to a compound according to formula (I), wherein R1 and R2 are each and independently selected from the group comprising alkyl; n is any integer between 1 and 4; R3 is an acyl selected from the group comprising lysyl, ornithyl, 2,4-diaminobutyryl, histidyl and an acyl moiety according to formula (II), wherein m is any integer from 1 to 3 and Y− is a pharmaceutically acceptable anion.
摘要翻译：本发明涉及式（I）化合物，其中R 1和R 2各自独立地选自烷基; n是1到4之间的整数; R3是选自根据式（II）的赖氨酰，鸟氨酰基，2,4-二氨基丁酰基，组氨酰基和酰基部分的酰基，其中m是1至3的任何整数，Y-是药学上可接受的阴离子。

8. 发明申请

US20090304678A1 Means for Inhibiting the Expression of Protein Kinase 3 有权
公开(公告)号：US20090304678A1
公开(公告)日：2009-12-10
申请号：US12307052
申请日：2007-07-20
申请人： Jorg Kaufmann , Oliver Keil , Ansgar Santel
发明人： Jorg Kaufmann , Oliver Keil , Ansgar Santel
IPC分类号： A61K39/395 , C07H21/04 , C12N5/06 , C12N15/63 , C12N5/10 , A61K31/711
CPC分类号： C12N15/1137 , C12N2310/14 , C12N2310/321 , C12N2310/3521
摘要： The present invention is related to a nucleic acid molecule comprising a double-stranded structure, whereby the double-stranded structure comprises a first strand and a second strand, whereby the first strand comprises a first stretch of contiguous nucleotides and said first stretch is at least partially complementary to a target nucleic acid, and whereby the second strand comprises a second stretch of contiguous nucleotides and said second stretch is at least partially complementary to the first stretch, whereby the first stretch comprises a nucleic acid sequence which is at least partially complementary to a nucleotide core sequence of the nucleic acid sequence according to SEQ ID NO:1 (NM_013355), or part thereof, whereby the nucleotide core sequence comprises the nucleotide sequence from nucleotide positions 482 to 500 of SEQ ID NO:1 (SEQ ID NO:2); from nucleotide positions 1555 to 1573 of SEQ ID NO:1 (SEQ ID NO:4); from nucleotide positions 1556 to 1574 of SEQ ID NO:1 (SEQ ID NO:6); from nucleotide positions 1559 to 1577 of SEQ ID NO:1 (SEQ ID NO:8); from nucleotide positions 1566 to 1584 of SEQ ID NO:1 (SEQ ID NO:10); from nucleotide positions 2094 to 2112 of SEQ ID NO:1 (SEQ ID NO:12); from nucleotide positions 2102 to 2120 of SEQ ID NO:1 (SEQ ID NO:14); from nucleotide positions 2286 to 2304 of SEQ ID NO:1 (SEQ ID NO:16); from nucleotide positions 2761 to 2779 of SEQ ID NO:1 (SEQ ID NO:18); from nucleotide positions 2763 to 2781 of SEQ ID NO:1 (SEQ ID NO:20); from nucleotide positions 2764 to 2782 of SEQ ID NO:1 (SEQ ID NO:22); from nucleotide positions 2843 to 2861 of SEQ ID NO:1 (SEQ ID NO:24); from nucleotide positions 2844 to 2862 of SEQ ID NO:1 (SEQ ID NO:26); or from nucleotide positions 2846 to 2864 of SEQ ID NO:1 (SEQ ID NO:28), preferably the nucleotide core sequence comprises the nucleotide sequence from nucleotide positions 1555 to 1573 of SEQ ID NO:1 (SEQ ID NO:4); from nucleotide positions 1556 to 1574 of SEQ ID NO:1 (SEQ ID NO:6); from nucleotide positions 1559 to 1577 of SEQ ID NO:1 (SEQ ID NO:8); from nucleotide positions 1566 to 1584 of SEQ ID NO:1 (SEQ ID NO:10); from nucleotide positions 2094 to 2112 of SEQ ID NO:1 (SEQ ID NO:12); or from nucleotide positions 2286 to 2304 of SEQ ID NO:1 (SEQ ID NO:16), whereby preferably the first stretch is additionally at least partially complementary to a region preceding the 5′ end of the nucleotide core sequence and/or to a region following the 3′ end of the nucleotide core sequence.

9. 发明授权

US08829179B2 Means for inhibiting the expression of ANG2 有权
标题翻译：用于抑制ANG2表达的方法
公开(公告)号：US08829179B2
公开(公告)日：2014-09-09
申请号：US13201917
申请日：2010-02-18
申请人： Ansgar Santel , Jörg Kaufmann , Martin Witzenrath
发明人： Ansgar Santel , Jörg Kaufmann , Martin Witzenrath
IPC分类号： C07H21/04 , C07H21/02 , C12N15/63 , A61K48/00
CPC分类号： C12N15/1136 , C12N15/111 , C12N15/113 , C12N2310/11 , C12N2310/14 , C12N2310/321 , C12N2310/50 , C12N2320/32 , C12N2310/3521
摘要： The present invention is related to an siRNA comprising an antisense strand and a sense strand, wherein all or a portion of said antisense strand comprises an antisense duplex region, wherein all or a portion of said sense strand comprises a sense duplex region, wherein said antisense duplex region is at least partially complementary to said sense duplex region, wherein said siRNA comprises a duplex region consisting of said antisense duplex region and said sense duplex region, and wherein: a) said antisense strand comprises a nucleotide sequence of SEQ ID NO: 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 36, 38, 40, 42, 44, 46, 48, 50, 52, 54, 56, 58, 60, 62, 64, 68, 74, 76, 78, 80, 82, 84, 86, 88, 90, 92, 94, 96, 98, 100, 102 or 104; or b) said antisense strand comprises an antisense duplex region, all or a portion of which, is complementary to a portion of SEQ ID NO: 1 or 70.
摘要翻译：本发明涉及包含反义链和有义链的siRNA，其中所述反义链的全部或部分包含反义双链区，其中所述或部分所述有义链包含有义双链区，其中所述反义双链体区域与所述正义双链体区域至少部分互补，其中所述siRNA包含由所述反义双链体区域和所述正义双链区域组成的双链体区域，其中：a）所述反义链包含SEQ ID NO：2的核苷酸序列，4,6,8,10,12,14,16,18,20,22,24,26,28,30,32,34,36,38,40,42,44,46,48,50,52 ，54，56，58，60，62，64，68，74，76，78，80，82，84，86，88，90，92，94，96，98，100，102或104; 或b）所述反义链包含反义双链体区，其全部或部分与SEQ ID NO：1或70的一部分互补。

10. 发明申请

US20120022138A1 MEANS FOR INHIBITING THE EXPRESSION OF ANG2 有权
标题翻译：抑制ANG2表达的方法
公开(公告)号：US20120022138A1
公开(公告)日：2012-01-26
申请号：US13201917
申请日：2010-02-18
申请人： Ansgar Santel , Jörg Kaufmann , Martin Witzenrath
发明人： Ansgar Santel , Jörg Kaufmann , Martin Witzenrath
IPC分类号： A61K31/713 , C12N15/85 , C12N5/10 , A61P29/00 , A61P35/00 , A61P17/06 , A61P17/00 , A61P19/02 , A61P11/00 , A61P9/10 , A61P3/04 , A61P3/10 , A61P1/00 , A61P1/02 , A61P9/12 , A61P11/06 , A61P1/18 , A61P37/00 , A61P25/00 , A61P27/02 , A61P1/16 , A61P33/06 , A61P19/04 , C07H21/02
CPC分类号： C12N15/1136 , C12N15/111 , C12N15/113 , C12N2310/11 , C12N2310/14 , C12N2310/321 , C12N2310/50 , C12N2320/32 , C12N2310/3521
摘要： The present invention is related to an siRNA comprising an antisense strand and a sense strand, wherein all or a portion of said antisense strand comprises an antisense duplex region, wherein all or a portion of said sense strand comprises a sense duplex region, wherein said antisense duplex region is at least partially complementary to said sense duplex region, wherein said siRNA comprises a duplex region consisting of said antisense duplex region and said sense duplex region, and wherein: a) said antisense strand comprises a nucleotide sequence of SEQ ID NO: 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 36, 38, 40, 42, 44, 46, 48, 50, 52, 54, 56, 58, 60, 62, 64, 68, 74, 76, 78, 80, 82, 84, 86, 88, 90, 92, 94, 96, 98, 100, 102 or 104; or b) said antisense strand comprises an antisense duplex region, all or a portion of which, is complementary to a portion of SEQ ID NO: 1 or 70.
摘要翻译：本发明涉及包含反义链和有义链的siRNA，其中所述反义链的全部或部分包含反义双链区，其中所述或部分所述有义链包含有义双链区，其中所述反义双链体区域与所述正义双链体区域至少部分互补，其中所述siRNA包含由所述反义双链体区域和所述正义双链区域组成的双链体区域，其中：a）所述反义链包含SEQ ID NO：2的核苷酸序列，4,6,8,10,12,14,16,18,20,22,24,26,28,30,32,34,36,38,40,42,44,46,48,50,52 ，54，56，58，60，62，64，68，74，76，78，80，82，84，86，88，90，92，94，96，98，100，102或104; 或b）所述反义链包含反义双链体区，其全部或部分与SEQ ID NO：1或70的一部分互补。

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