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1. 发明申请

WO2006044366A3 E2-EPF5, A NOVEL THERAPEUTIC PROTEIN AND TARGET 审中-公开
标题翻译： E2-EPF5，一种新的治疗蛋白质和目标
公开(公告)号：WO2006044366A3
公开(公告)日：2007-01-04
申请号：PCT/US2005036505
申请日：2005-10-12
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , ASSELBERGS FRED A , HALL JONATHAN , HUESKEN DIETER , LABOW MARK ARON , MICKANIN CRAIG STEPHEN , SCHMID PETER , WEILER JAN , WYDER LORENZA
发明人： ASSELBERGS FRED A , HALL JONATHAN , HUESKEN DIETER , LABOW MARK ARON , MICKANIN CRAIG STEPHEN , SCHMID PETER , WEILER JAN , WYDER LORENZA
IPC分类号： A61K39/395 , G01N33/50
CPC分类号： C12N15/1137 , C07K16/40 , C12N2310/11 , C12N2310/14 , C12N2310/315 , C12N2310/321 , C12N2310/3341 , C12N2310/341 , C12N2310/346 , C12Y603/02019 , C12N2310/3525
摘要： The present invention relates to novel uses for ubiquitin conjugating enzyme E2-EPF5. In particular, inhibition of E2-EPF5 activity is shown to reduce the production VEGF, as well as other proteins regulated the transcription factor HIF-1, in response to hypoxia. Based on these findings the present invention provides therapeutic methods and pharmaceutical compositions useful for the treatment of diseases related VEGF induced angiogenesis. In addition, E2-EPF5 is provided as target for the development of therapeutics. Accordingly, the invention provides screening methods for identifying candidate compounds that inhibit E2-EPF5 activity and may therefore be used to treat VEGF induced angiogenesis such as tumor related angiogenesis. Finally, the invention also provides methods for the inhibition of VEGF and other HIF-1 regulated proteins.
摘要翻译：本发明涉及泛素缀合酶E2-EPF5的新用途。特别地，E2-EPF5活性的抑制显示可以减少VEGF的产生，以及调节转录因子HIF-1的其他蛋白质，以应对缺氧。基于这些发现，本发明提供治疗方法和药物组合物，其可用于治疗与VEGF相关的VEGF诱导的血管生成。此外，提供E2-EPF5作为治疗开发的目标。因此，本发明提供了用于鉴定抑制E2-EPF5活性的候选化合物的筛选方法，因此可用于治疗VEGF诱导的血管发生如肿瘤相关的血管发生。最后，本发明还提供了抑制VEGF和其他HIF-1调节蛋白的方法。

2. 发明申请

WO2005040419A8 OLIGONUCLEOTIDE MICROARRAY 审中-公开
公开(公告)号：WO2005040419A8
公开(公告)日：2006-05-11
申请号：PCT/EP2004011511
申请日：2004-10-13
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , NOVARTIS FORSCHUNGSSTIFTUNG , WEILER JAN , HALL JONATHAN , WANKE CHRISTOPH , LANGE JOERG BERND , FILIPOWICZ WITOLD , KOLB FABRICE
发明人： WEILER JAN , HALL JONATHAN , WANKE CHRISTOPH , LANGE JOERG BERND , FILIPOWICZ WITOLD , KOLB FABRICE
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6883 , C12Q1/6886 , C12Q2600/178
摘要： The present invention relates to oligonucleotide microarrays comprising short chemically modified RNA oligonucleotides and uses of such microarrays in genomics applications. More specifically, the invention provides an oligonucleotide array comprising a surface and a plurality of oligonucleotide, wherein at least one oligonucleotide has at least one modified sugar moiety at the 2'OH position. The microarrays of the invention are more specifically useful to detect small RNAs.
摘要翻译：本发明涉及包含短化学修饰的RNA寡核苷酸的寡核苷酸微阵列和在基因组学应用中这种微阵列的用途。更具体地，本发明提供了包含表面和多个寡核苷酸的寡核苷酸阵列，其中至少一个寡核苷酸在2'OH位置具有至少一个修饰的糖部分。本发明的微阵列更具体地用于检测小RNA。

3. 发明申请

WO2015051044A3 NOVEL FORMATS FOR ORGANIC COMPOUNDS FOR USE IN RNA INTERFERENCE 审中-公开
标题翻译：用于RNA干扰的有机化合物的新形式
公开(公告)号：WO2015051044A3
公开(公告)日：2015-07-02
申请号：PCT/US2014058703
申请日：2014-10-01
申请人： NOVARTIS AG , BARYZA JEREMY LEE , BLOMMERS MARCEL , FERNANDEZ CESAR , GENO ERIN , GOSSERT ALVAR , GREENIDGE PAULETTE , HUESKEN DIETER , HUNZIKER JUERG , NATT FRANCIOS JEAN-CHARLES , PATNAIK ANUP , PATTERSON ANDREW , RONDEAU JEAN-MICHEL RENE , WEILER JAN , ZHU MEICHENG
发明人： BARYZA JEREMY LEE , BLOMMERS MARCEL , FERNANDEZ CESAR , GENO ERIN , GOSSERT ALVAR , GREENIDGE PAULETTE , HUESKEN DIETER , HUNZIKER JUERG , NATT FRANCIOS JEAN-CHARLES , PATNAIK ANUP , PATTERSON ANDREW , RONDEAU JEAN-MICHEL RENE , WEILER JAN , ZHU MEICHENG
IPC分类号： C12N15/113
CPC分类号： C12N15/113 , C12N15/111 , C12N2310/14 , C12N2310/317 , C12N2310/321 , C12N2310/322 , C12N2310/332 , C12N2310/3515 , C12N2310/3521 , C12N2310/3525 , C12N2310/3533
摘要： The disclosure relates to compositions comprising a RNAi agent having a novel format. These RNAi agents comprise a sense and an anti-sense strand, each strand being an 18-mer and the strands together forming a blunt-ended duplex, wherein the 3' end of at least one strand terminates in a phosphate or modified internucleoside linker and further comprises, in 5' to 3' order: a spacer; a second phosphate or modified internucleoside linker; and a 3' end cap. In some embodiments, the 3' end of both the sense and anti-sense strand further comprise, in 5' to 3' order: a spacer; a second phosphate or modified internucleoside linker; and a 3' end cap. The two strands can have the same or different spacers, phosphates or modified internucleoside linkers, and/or 3' end caps. The strands can be ribonucleotides, or, optionally, one or more nucleotide can be modified or substituted. Optionally, at least one nucleotide comprises a modified internucleoside linker. Optionally, the first two base-pairing nucleotides on the 3' end of the sense and/or anti-sense strand are 2'-MOE. Optionally, the RNAi agent can be modified on one or both 5' end. Optionally, the sense strand can comprise a 5' end cap which reduces the amount of the RNA interference mediated by this strand. Optionally, the RNAi agent is attached to a ligand. This format can be used to devise RNAi agents to a variety of different targets and sequences. The disclosure also relates to processes for making such compositions, and methods and uses of such compositions, e.g., to mediate RNA interference.
摘要翻译：本公开涉及包含具有新颖形式的RNAi剂的组合物。这些RNAi剂包含有义链和反义链，每条链都是18聚体，并且链一起形成平头双链体，其中至少一条链的3'末端终止于磷酸盐或修饰的核苷间连接体并且进一步包括按照5'至3'的顺序：间隔物; 第二磷酸盐或修饰的核苷间连接体; 和3'端盖。在一些实施方案中，有义链和反义链两者的3'末端还以5'至3'的顺序包含：间隔子; 第二磷酸盐或修饰的核苷间连接体; 和3'端盖。两条链可以具有相同或不同的间隔区，磷酸盐或修饰的核苷间接头，和/或3'端帽。链可以是核糖核苷酸，或者任选地，一个或多个核苷酸可以被修饰或取代。任选地，至少一个核苷酸包含修饰的核苷间连接体。任选地，有义链和/或反义链的3'末端上的前两个碱基配对核苷酸是2'-MOE。任选地，RNAi剂可以在一个或两个5'末端被修饰。任选地，有义链可以包含5'端帽，其减少由该链介导的RNA干扰的量。任选地，RNAi剂附着于配体。该格式可用于将RNAi试剂设计为多种不同的靶标和序列。本公开还涉及制备这种组合物的方法，以及这些组合物的方法和用途，例如介导RNA干扰。

4. 发明申请

WO2013166004A3 ORGANIC COMPOSITIONS TO TREAT KRAS-RELATED DISEASES 审中-公开
标题翻译：有机组合物治疗与KRAS相关的疾病
公开(公告)号：WO2013166004A3
公开(公告)日：2014-01-03
申请号：PCT/US2013038847
申请日：2013-04-30
申请人： NOVARTIS AG , BETTENCOURT BRIAN , MILSTEIN STUART , TOUDJARSKA IVANKA , MCDONALD EARL , SCHLABACH MICHAEL JR , STEGMEIER FRANK P , WARMUTH MARKUS , GAMPA KALYANI , HUESKEN DIETER , STUMP MARK , WEILER JAN , JAGANI ZAINAB
发明人： BETTENCOURT BRIAN , MILSTEIN STUART , TOUDJARSKA IVANKA , MCDONALD EARL , SCHLABACH MICHAEL JR , STEGMEIER FRANK P , WARMUTH MARKUS , GAMPA KALYANI , HUESKEN DIETER , STUMP MARK , WEILER JAN , JAGANI ZAINAB
IPC分类号： C12N15/113 , A61K31/713 , A61P35/00
CPC分类号： A61K31/713 , A61K45/06 , A61K47/549 , C12N15/113 , C12N15/1135 , C12N2310/14 , C12N2310/344 , C12N2310/351 , C12N2310/321 , C12N2310/3521
摘要： The present disclosure relates to RNAi agents useful in methods of treating KRAS-related diseases such as a proliferative disease, including without limitation a solid or liquid cancer, adenocarcinoma, colorectal cancer, advanced and/or metastatic colorectal cancer, colon cancer, lung, non-small cell lung cancer and lung adenocarcinoma, acute myelogenous lung, bladder, brain, breast, cervical, endometrial, gastric, head and neck, kidney, leukemia, myelodysplastic syndrome, myeloid leukemia, liver, melanoma, ovarian, pancreatic, prostate, testicular, thyroid cancers, and cardio-facio-cutaneous (CFC) syndrome and Noonan syndrome, and similar and related diseases, using a therapeutically effective amount of a RNAi agent to KRAS.
摘要翻译：本公开涉及可用于治疗KRAS相关疾病如增殖性疾病的方法中的RNAi剂，所述方法包括但不限于固体或液体癌症，腺癌，结肠直肠癌，晚期和/或转移性结肠直肠癌，结肠癌，肺，非 - - 小细胞肺癌和肺腺癌，急性髓细胞肺，膀胱，脑，乳腺，子宫颈，子宫内膜，胃，头颈部，肾，白血病，骨髓增生异常综合征，骨髓性白血病，肝，黑素瘤，卵巢，胰腺，前列腺，睾丸，甲状腺癌和心脏表皮（CFC）综合征和Noonan综合征以及类似和相关疾病，使用治疗有效量的RNAi剂给KRAS。

5. 发明申请

WO2013030778A3 ORGANIC COMPOSITIONS TO TREAT HSF1-RELATED DISEASES 审中-公开
标题翻译：有机组合物治疗HSF1相关疾病
公开(公告)号：WO2013030778A3
公开(公告)日：2013-07-25
申请号：PCT/IB2012054455
申请日：2012-08-30
申请人： NOVARTIS AG , CHEN JINYUN , GAMPA KALYANI , HUESKEN DIETER , STEGMEIER FRANK P , STUMP MARK , VARGEESE CHANDRA , WEILER JAN , ZHOU WENLAI
发明人： CHEN JINYUN , GAMPA KALYANI , HUESKEN DIETER , STEGMEIER FRANK P , STUMP MARK , VARGEESE CHANDRA , WEILER JAN , ZHOU WENLAI
IPC分类号： C12N15/113 , A61P31/12 , A61P35/00 , A61P37/06
CPC分类号： C12N15/113 , A61K31/5377 , A61K31/713 , A61K45/06 , C12N2310/14 , C12N2310/321 , C12N2310/322 , C12N2310/333 , C12N2310/334 , C12N2310/335 , C12N2310/336 , C12N2310/351 , C12N2320/31 , C12N2310/3521
摘要： The present disclosure relates to methods of treating heat shock factor 1 (HSF1)-related diseases such as cancer, autoimmune and viral diseases, using a therapeutically effective amount of a RNAi agent to HSF.
摘要翻译：本公开涉及使用治疗有效量的RNAi剂对HSF治疗热休克因子1（HSF1）相关疾病如癌症，自身免疫性和病毒性疾病的方法。

6. 发明申请

WO2015051366A3 NOVEL FORMATS FOR ORGANIC COMPOUNDS FOR USE IN RNA INTERFERENCE 审中-公开
标题翻译：用于RNA干扰的有机化合物的新格式
公开(公告)号：WO2015051366A3
公开(公告)日：2015-07-02
申请号：PCT/US2014059301
申请日：2014-10-06
申请人： NOVARTIS AG , BARYZA JEREMY LEE , BLOMMERS MARCEL , CHUTKOW WILLIAM , FERNANDEZ CESAR , GENO ERIN , GOSSERT ALVAR , GREENIDGE PAULETTE , HUESKEN DIETER , HUNZIKER JUERG , NATT FRANCOIS JEAN-CHARLES , PATNAIK ANUP , PATTERSON ANDREW , RONDEAU JEAN-MICHEL RENE , WEILER JAN , ZHU MEICHENG
发明人： BARYZA JEREMY LEE , BLOMMERS MARCEL , CHUTKOW WILLIAM , FERNANDEZ CESAR , GENO ERIN , GOSSERT ALVAR , GREENIDGE PAULETTE , HUESKEN DIETER , HUNZIKER JUERG , NATT FRANCOIS JEAN-CHARLES , PATNAIK ANUP , PATTERSON ANDREW , RONDEAU JEAN-MICHEL RENE , WEILER JAN , ZHU MEICHENG
IPC分类号： C12N15/113
CPC分类号： C12N15/113 , C12N2310/14 , C12N2310/317 , C12N2310/321 , C12N2310/322 , C12N2310/332 , C12N2310/341 , C12N2310/351 , C12N2310/3515 , C12N2310/3521 , C12N2310/3525 , C12N2310/3533
摘要： The disclosure relates to compositions comprising a RNAi agent having a novel format including a spacer subunit. The disclosure relates to compositions comprising a RNAi agent having a novel format: an 18-mer format with at least one internal spacer. These RNAi agents comprise a first and a second 18-mer strand, wherein the first strand is 18 ribonucleotides or 18 total ribonucleotides and spacer subunit(s), and the second strand is 18 total ribonucleotides and spacer subunit(s), wherein: each spacer subunit consists of: (a) a phosphate or modified internucleoside linker and (b) a spacer; a spacer subunit can be at any position in the strand; the two strands form a duplex with at least one blunt end; and the 3 end of one or both strands terminates in a phosphate or modified internucleoside linker and further comprises, in 5 to 3 order: a second spacer; a second phosphate or modified internucleoside linker, and a 3 end cap. In various embodiments, the RNAi agents comprise a first and a second strand, wherein each strand is a 30-mer or shorter, the first strand comprises ribonucleotides, and the second strand comprises ribonucleotides and one or more spacer subunit(s), wherein: each spacer subunit consists of: (a) a phosphate or modified internucleoside linker and (b) a spacer; a spacer subunit can be at any position in the strand. In some embodiments, the 3 end of both strands further comprise, in 5 to 3 order: a second spacer; a second phosphate or modified internucleoside linker; and a 3 end cap. The two strands can have the same or different spacers, phosphates or modified internucleoside linkers, and/or 3 end caps. The strands can be ribonucleotides, or, optionally, one or more nucleotide can be modified or substituted. Optionally, at least one nucleotide comprises a modified internucleoside linker. Optionally, the first two base-pairing nucleotides on the 3 end of the one or both strand are 2-MOE. Optionally, the RNAi agent can be modified on one or both 5 end. Optionally, the first or second strand is the sense strand, and the sense strand can comprise a 5 end cap which reduces the amount of the RNA interference mediated by this strand. Optionally, the RNAi agent is attached to a ligand. This format can be used to devise RNAi agents to a variety of different targets and sequences. The disclosure also relates to processes for making such compositions, and methods and uses of such compositions, e.g., to mediate RNA interference.
摘要翻译：本公开涉及包含具有包括间隔子亚单位的新格式的RNAi剂的组合物。本公开涉及包含具有新格式的RNAi剂的组合物：具有至少一个内部间隔物的18聚体形式。这些RNAi剂包含第一和第二18聚体链，其中第一链是18个核糖核苷酸或18个总核糖核苷酸和间隔子亚单位，第二个链是18个总核糖核苷酸和间隔子亚基，其中：间隔子亚基由以下组成：（a）磷酸酯或修饰的核苷间连接体和（b）间隔子; 间隔子亚基可以在链中的任何位置; 两条链与至少一个钝端形成双链体; 并且一条或两条链的3端终止于磷酸酯或修饰的核苷间连接体，并且还包含5至3个顺序：第二间隔物; 第二磷酸酯或修饰的核苷间连接体，和3端帽。在各种实施方案中，RNAi试剂包含第一和第二链，其中每条链均为30聚体或更短，第一链包含核糖核苷酸，第二链包含核糖核苷酸和一个或多个间隔子亚单位，其中：每个间隔子亚基由以下组成：（a）磷酸酯或修饰的核苷间连接体和（b）间隔子; 间隔子亚基可以在链中的任何位置。在一些实施方案中，两条链的3端还包含5至3个顺序：第二间隔物; 第二磷酸酯或修饰的核苷间连接体; 和3个端盖。两条链可以具有相同或不同的间隔物，磷酸酯或修饰的核苷间连接体和/或3个末端帽。链可以是核糖核苷酸，或者任选地，一个或多个核苷酸可以被修饰或取代。任选地，至少一个核苷酸包含修饰的核苷间连接体。任选地，一条或两条链的3端上的前两个碱基配对核苷酸是2-MOE。任选地，RNAi剂可在一端或两端进行修饰。任选地，第一链或第二链是有义链，有义链可以包含5端帽，其减少由该链介导的RNA干扰的量。任选地，RNAi试剂连接到配体上。这种格式可用于将RNAi试剂设计成各种不同的靶标和序列。本公开还涉及制备这种组合物的方法，以及这种组合物的方法和用途，例如介导RNA干扰。

7. 发明申请

WO2015051045A2 3'END CAPS FOR RNAi AGENTS FOR USE IN RNA INTERFERENCE 审中-公开
标题翻译：用于RNA干扰的RNAi试剂的3'端
公开(公告)号：WO2015051045A2
公开(公告)日：2015-04-09
申请号：PCT/US2014058705
申请日：2014-10-01
申请人： NOVARTIS AG , BARYZA JEREMY LEE , BLOMMERS MARCEL , FERNANDEZ CESAR , GENO ERIN , GOSSERT ALVAR , GREENIDGE PAULETTE , HUESKEN DIETER , HUNZIKER JUERG , NATT FRANCOIS JEAN-CHARLES , PATNAIK ANUP , PATTERSON ANDREW , RONDEAU JEAN-MICHEL RENE , WEILER JAN , ZHU MEICHENG
发明人： BARYZA JEREMY LEE , BLOMMERS MARCEL , FERNANDEZ CESAR , GENO ERIN , GOSSERT ALVAR , GREENIDGE PAULETTE , HUESKEN DIETER , HUNZIKER JUERG , NATT FRANCOIS JEAN-CHARLES , PATNAIK ANUP , PATTERSON ANDREW , RONDEAU JEAN-MICHEL RENE , WEILER JAN , ZHU MEICHENG
IPC分类号： C07C43/178
CPC分类号： C12N15/111 , C07C43/23 , C07C69/40 , C07C233/01 , C07D213/30 , C07D215/12 , C07D215/14 , C07D217/14 , C07D217/16 , C07D217/18 , C07D311/80 , C07D401/04 , C12N2310/14 , C12N2310/344 , C12N2310/351 , C12N2320/51
摘要： The disclosure relates to novel compounds and compositions comprising a RNAi agent comprising a novel compound as a 3' end cap. The disclosure also relates to processes for making such compositions, and methods and uses of such compositions, e.g., to mediate RNA interference.
摘要翻译：本公开涉及包含含有作为3'端帽的新化合物的RNAi剂的新化合物和组合物。本公开还涉及制备这种组合物的方法，以及这种组合物的方法和用途，例如介导RNA干扰。

8. 发明申请

WO2015050871A2 ORGANIC COMPOUNDS TO TREAT HEPATITIS B VIRUS 审中-公开
标题翻译：有机化合物治疗乙型肝炎病毒
公开(公告)号：WO2015050871A2
公开(公告)日：2015-04-09
申请号：PCT/US2014058314
申请日：2014-09-30
申请人： NOVARTIS AG , BARYZA JEREMY LEE , BLOMMERS MARCEL , FERNANDEZ CESAR , GENO ERIN , GOSSERT ALVAR , GREENIDGE PAULETTE , HUESKEN DIETER , HUNZIKER JUERG , NATT FRANCOIS JEAN-CHARLES , PATNAIK ANUP , PATTERSON ANDREW , RONDEAU JEAN-MICHEL RENE , WEILER JAN , ZHU MEICHENG , HOLDORF MEGHAN
发明人： BARYZA JEREMY LEE , BLOMMERS MARCEL , FERNANDEZ CESAR , GENO ERIN , GOSSERT ALVAR , GREENIDGE PAULETTE , HUESKEN DIETER , HUNZIKER JUERG , NATT FRANCOIS JEAN-CHARLES , PATNAIK ANUP , PATTERSON ANDREW , RONDEAU JEAN-MICHEL RENE , WEILER JAN , ZHU MEICHENG , HOLDORF MEGHAN
IPC分类号： A61K48/00 , C07F9/6512 , C07H21/02
CPC分类号： C12N15/1131 , C12N2310/14 , C12N2310/317 , C12N2310/321 , C12N2310/322 , C12N2310/332 , C12N2310/351 , C12N2310/3515 , C12N2320/30 , C12N2310/3521 , C12N2310/3525 , C12N2310/3533
摘要： The disclosure relates to compositions comprising a HBV RNAi agent. In some embodiments, the HBV RNAi agent comprises a sense and an anti-sense strand, each strand being an 18-mer and the strands together forming a blunt-ended duplex, wherein the 3' end of at least one strand terminates in a phosphate or modified internucleoside linker and further comprises, in 5' to 3' order: a spacer; a second phosphate or modified internucleoside linker; and a 3' end cap. In some embodiments, the 3' end of both the sense and anti-sense strand further comprise, in 5' to 3' order: a spacer; a second phosphate or modified internucleoside linker; and a 3' end cap. The two strands can have the same or different spacers, phosphates or modified internucleoside linkers, and/or 3' end caps. The strands can be ribonucleotides, or, optionally, one or more nucleotide can be modified or substituted. Optionally, at least one nucleotide comprises a modified internucleoside linker. Optionally, the RNAi agent can be modified on one or both 5' end. Optionally, the sense strand can comprise a 5' end cap which reduces the amount of the RNA interference mediated by this strand. Optionally, the RNAi agent is attached to a ligand. This format can be used to devise RNAi agents to a variety of different targets and sequences. The disclosure also relates to processes for making such compositions, and methods and uses of such compositions, e.g., to mediate RNA interference. The disclosure also pertains to methods of treating, ameliorating and preventing HBV in a patient involving the step of administering to the patient a therapeutic amount of a HBV RNAi agent.
摘要翻译：本公开涉及包含HBV RNAi剂的组合物。在一些实施方案中，HBV RNAi剂包含有义链和反义链，每条链是18聚体，并且所述链一起形成平端双链体，其中至少一条链的3'末端终止于磷酸酯或修饰的核苷间连接体，并且还包含以5'至3'的顺序：间隔物; 第二磷酸酯或修饰的核苷间连接体; 和3'端盖。在一些实施方案中，有义和反义链两者的3'末端还包含5'至3'的顺序：间隔基; 第二磷酸酯或修饰的核苷间连接体; 和3'端盖。两条链可以具有相同或不同的间隔物，磷酸酯或修饰的核苷间接头，和/或3'端帽。链可以是核糖核苷酸，或者任选地，一个或多个核苷酸可以被修饰或取代。任选地，至少一个核苷酸包含修饰的核苷间连接体。任选地，RNAi剂可以在一个或两个5'端修饰。任选地，有义链可以包含5'端帽，其减少由该链介导的RNA干扰的量。任选地，RNAi试剂连接到配体上。这种格式可用于将RNAi试剂设计成各种不同的靶标和序列。本公开还涉及制备这种组合物的方法，以及这种组合物的方法和用途，例如介导RNA干扰。本公开还涉及在患者中治疗，改善和预防HBV的方法，其涉及向患者施用治疗量的HBV RNAi剂的步骤。

9. 发明申请

WO2014134255A2 ORGANIC COMPOSITIONS TO TREAT EPAS1-RELATED DISEASES 审中-公开
标题翻译：治疗EPAS1相关疾病的有机组合物
公开(公告)号：WO2014134255A2
公开(公告)日：2014-09-04
申请号：PCT/US2014018873
申请日：2014-02-27
申请人： NOVARTIS AG , BETTENCOURT BRIAN , GANESH SHANTHI , GEORGE ELIZABETH , HUESKEN DIETER , MILSTEIN STUART , SOLOMON JONATHAN , THOMAS EMILY , TOUDJARSKA IVANKA , TULLAI JENNIFER , WEILER JAN
发明人： BETTENCOURT BRIAN , GANESH SHANTHI , GEORGE ELIZABETH , HUESKEN DIETER , MILSTEIN STUART , SOLOMON JONATHAN , THOMAS EMILY , TOUDJARSKA IVANKA , TULLAI JENNIFER , WEILER JAN
IPC分类号： C12N15/113
CPC分类号： C12N15/113 , A61K31/7105 , A61K31/7115 , A61K31/712 , A61K31/7125 , A61K31/713 , A61K45/06 , C12N2310/14 , C12N2310/315 , C12N2310/321 , C12N2310/342 , C12N2310/351 , C12N2320/30 , A61K2300/00
摘要： The present disclosure relates to methods of treating EPAS1-related diseases such as cancer, metastases, astrocytoma, bladder cancer, breast cancer, chondrosarcoma, colorectal carcinoma, gastric carcinoma, glioblastoma, head and neck squamous cell carcinoma, hepatocellular carcinoma, lung adenocarcinoma, neuroblastoma, non-small cell lung cancer, melanoma, multiple myeloma, ovarian cancer, rectal cancer, renal cancer, clear cell renal cell carcinoma (and metastases of this and other cancers), gingivitis, psoriasis, Kaposi's sarcoma-associated herpesvirus, preemclampsia, inflammation, chronic inflammation, neovascular diseases, and rheumatoid arthritis, using a therapeutically effective amount of a RNAi agent to EPAS1.
摘要翻译：本发明涉及治疗EPAS1相关疾病例如癌症，转移瘤，星形细胞瘤，膀胱癌，乳腺癌，软骨肉瘤，结肠直肠癌，胃癌，成胶质细胞瘤，头颈部鳞状细胞癌，肝细胞癌，肺腺癌，神经母细胞瘤，非小细胞肺癌，黑素瘤，多发性骨髓瘤，卵巢癌，直肠癌，肾癌，透明细胞肾细胞癌（以及这种和其他癌症的转移），牙龈炎，牛皮癣，卡波西肉瘤相关疱疹病毒，先兆子痫，炎症，慢性炎症，新血管疾病和类风湿性关节炎，使用治疗有效量的针对EPAS1的RNAi剂。

10. 发明申请

WO2015051135A3 ORGANIC COMPOSITIONS TO TREAT HEPCIDIN-RELATED DISEASES 审中-公开
标题翻译：治疗肝素相关疾病的有机组合物
公开(公告)号：WO2015051135A3
公开(公告)日：2015-09-03
申请号：PCT/US2014058851
申请日：2014-10-02
申请人： NOVARTIS AG , BARYZA JEREMY LEE , BLOMMERS MARCEL , BORLAND TODD , FERNANDEZ CESAR , GEBUHR TOM , GENO ERIN , GOSSERT ALVAR , GREENIDGE PAULETTE , HUESKEN DIETER , HUNZIKER JUERG , NATT FRANCOIS JEAN-CHARLES , PATNAIK ANUP , PATTERSON ANDREW , RONDEAU JEAN-MICHEL RENE , SOLOMON JONATHAN , WEILER JAN , ZHU MEICHENG
发明人： BARYZA JEREMY LEE , BLOMMERS MARCEL , BORLAND TODD , FERNANDEZ CESAR , GEBUHR TOM , GENO ERIN , GOSSERT ALVAR , GREENIDGE PAULETTE , HUESKEN DIETER , HUNZIKER JUERG , NATT FRANCOIS JEAN-CHARLES , PATNAIK ANUP , PATTERSON ANDREW , RONDEAU JEAN-MICHEL RENE , SOLOMON JONATHAN , WEILER JAN , ZHU MEICHENG
IPC分类号： C12N15/113 , A61K31/713 , A61P7/06
CPC分类号： C12N15/113 , C12N15/1136 , C12N2310/14 , C12N2310/321 , C12N2310/344 , C12N2310/351 , C12N2320/51
摘要： The present disclosure relates to methods of treating Hepcidin-related diseases such as anemia, iron-deficient erythropoiesis, hypoferremia, impaired dietary iron uptake, iron sequestration, anemia of inflammation (AI) (sometimes designated anemia of chronic disease or ACD), atherosclerosis, diabetes, and multiple neurodegenerative disorders such as Alzheimers disease, Parkinsons disease and Friedrichs ataxia, heart failure, chronic kidney disease, cardiorenal-anemia syndrome, infection, blood loss, hemolysis, vitamin B12 or folate deficiency, hyperparathyroidism, hemoglobinopathies and malignancies, cancer, AIDS, surgery, runted growth, and hair loss, using a therapeutically effective amount of a RNAi agent to Hepcidin.
摘要翻译：本发明涉及治疗铁调素相关疾病例如贫血，铁缺乏性红细胞生成，低铁血症，饮食铁摄取受损，铁螯合，炎症贫血（AI）（有时称为慢性疾病或ACD贫血），动脉粥样硬化，糖尿病和多种神经退行性疾病如阿尔茨海默病，帕金森病和弗里德里希共济失调，心力衰竭，慢性肾病，心肾综合征，感染，失血，溶血，维生素B12或叶酸缺乏症，甲状旁腺功能亢进症，血红蛋白病和恶性肿瘤，艾滋病，手术，运行的生长和脱发，使用治疗有效量的RNAi剂对Hepcidin。

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