SANTARIS PHARMA A/S Patent applications |
Patent application number | Title | Published |
20150315595 | Compositions and Methods for Modulation of ATXN3 Expression - Disclosed are oligonucleotides which target and hybridize to nucleic acid molecules encoding A TXNJ, leading to reduced expression of ATXN3. Reduction in the expression of aberrant ATXN3 is beneficial for the treatment of certain medical disorders, such as spinocerebellar ataxia 3. In particular embodiments, modulating the expression of an aberrant A TXN3 allele or transcript, for example, restores normal function of, for example, Purkinje cells or spinal cord neurons. The oligonucleotides of the present invention and the methods of using such oligonucleotides to modulate the expression of aberrant or expanded A TXN3 provide a means of improving the survival and morbidity associated with, or even curing, expression of an aberrant A TXN3 allele or transcript such as, for example, spinocerebellar ataxia-type 3 (SCA3). | 11-05-2015 |
20140357849 | SPLICE SWITCHING OLIGOMERS FOR TNF SUPERFAMILY RECEPTORS AND THEIR USE IN TREATMENT OF DISEASE - The present invention relates to compositions and methods for preparing splice variants of TNFalpha receptor (TNFR) in vivo or in vitro, and the resulting TNFR protein variants. Such variants may be prepared by controlling the splicing of pre-mRNA molecules and regulating protein expression with splice switching oligonucleotides or splice switching oligomers (SSOs). The preferred SSOs according to the invention target exon 7 or 8 of TNFR1 (TNFRSF1A) or TNFR2 (TNFRSF1A) pre-mRNA, typically resulting in the production of TNFR variants which comprise a deletion in part or the entire exon 7 or 8 respectfully. SSOs targeting exon 7 are found to result in a soluble form of the TNFR, which has therapeutic benefit for treatment of inflammatory diseases. The SSO's are characterized in that they are substantially incapable or incapable of recruiting RNaseH. | 12-04-2014 |
20140329883 | Pharmaceutical Composition Comprising Anti-miRNA Antisense Oligonucleotides - The invention provides pharmaceutical compositions comprising short single stranded oligonucleotides, of length of between 8 and 26 nucleobases which are complementary to human microRNAs selected from the group consisting of miR19b, miR21, miR122a, miR155 and miR375. The short oligonucleotides are particularly effective at alleviating miRNA repression in vivo. It is found that the incorporation of high affinity nucleotide analogues into the oligonucleotides results in highly effective anti-microRNA molecules which appear to function via the formation of almost irreversible duplexes with the miRNA target, rather than RNA cleavage based mechanisms, such as mechanisms associated with RNaseH or RISC. | 11-06-2014 |
20140296502 | ANTISENSE DESIGN - A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides. | 10-02-2014 |
20140294897 | POTENT LNA OLIGONUCLEOTIDES FOR THE INHIBITION OF HIF-1A EXPRESSION - The present disclosure relates to an LNA oligonucleotide consisting of a sequence selected from the group consisting of 5′-( | 10-02-2014 |
20140288299 | PROCESS - The present invention relates to a process for preparing a short oligonucleotide comprising the steps of: (i) preparing a crude mixture comprising the oligonucleotide (ii) subjecting the mixture formed in step (i) to a desalting step; wherein the process does not comprise a chromatographic purification step. | 09-25-2014 |
20140235844 | Short Interfering RNA (siRNA) Analogues - The present invention is directed to novel double-stranded short interfering (siRNA) analogues comprising locked nucleic acid (LNA) monomers. Such compounds induces sequence-specific post-transcriptional gene silencing in many organisms by a process known as RNA interference (RNAi). The compounds disclosed herein has improved properties compared to non-modified siRNAs and may, accordingly, be useful as therapeutic agents, e.g., in the treatment of various cancer forms. More particularly, the present invention is directed to siRNA analogues comprising a sense strand and an antisense strand, wherein each strand comprises 12-35 nucleotides and wherein the siRNA analogues comprise at least one locked nucleic acid (LNA) monomer. | 08-21-2014 |
20140194614 | AMINO-LNA, THIO-LNA AND ALPHA-L-OXY-LN - A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides. | 07-10-2014 |
20140128591 | ANTISENSE DESIGN - A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides. | 05-08-2014 |
20140128586 | AMINO-LNA, THIO-LNA AND ALPHA-L-OXY-LN - A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides. | 05-08-2014 |
20140031409 | METHODS FOR TREATING ANDROGEN RECEPTOR DEPENDENT DISORDERS INCLUDING CANCERS - The invention provides the combination use of antisense oligomers targeting androgen receptor mRNA and androgen receptor binding inhibitors that reduce androgen receptor activity for the treatment of androgen receptor related medical disorders, such as cancers, particularly prostate cancers and breast cancers. | 01-30-2014 |
20130116309 | OLIGOMERIC COMPOUNDS FOR THE MODULATION OF HIF-1A EXPRESSION - Oligonucleotides directed against the hypoxia-inducible factor-1α (HIF-1α) gene are provided for modulating the expression of HIF-1α. The compositions comprise oligonucleotides, particularly antisense oligonucleotides, targeted to nucleic acids encoding the HIF-1α. Methods of using these compounds for modulation of HIF-1α expression and for the treatment of diseases associated with the hypoxia-inducible factor-1α are provided. Examples of diseases are cancer and pre-eclampsia. The oligonucleotides may be composed of deoxyribonucleosides, a nucleic acid analogue, or Locked Nucleic Acid (LNA) or a combination thereof. | 05-09-2013 |
20120322848 | LNA OLIGONUCLEOTIDES AND THE TREATMENT OF CANCER - The present disclosure concerns LNA oligonucleotides having a (sub)sequence of the general formula 5′-( | 12-20-2012 |
20120295955 | RNA ANTAGONIST COMPOUNDS FOR THE MODULATION OF HER3 - The invention relates to oligomer compounds (oligomers), which target HER3 mRNA in a cell, leading to reduced expression of HER3 and/or HER2 and/or EGFR. Reduction of HER3 and/or HER2 and/or EGFR expression is beneficial for a range of medical disorders, such hyperproliferative disorders (e.g., cancer). The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of HER3 and/or HER2 and/or EGFR using said oligomers, including methods of treatment. | 11-22-2012 |
20120270924 | Oligomeric Compounds For The Modultion of HIF-1A Expression - Oligonucleotides directed against the hypoxia-inducible factor-1α (HIF-1α) gene are provided for modulating the expression of HIF-1α. The compositions comprise oligonucleotides, particularly antisense oligonucleotides, targeted to nucleic acids encoding the HIF-1α. Methods of using these compounds for modulation of HIF-1α expression and for the treatment of diseases associated with the hypoxia-inducible factor-1α are provided. Examples of diseases are cancer and pre-eclampsia. The oligonucleotides may be composed of deoxyribonucleosides, a nucleic acid analogue, or Locked Nucleic Acid (LNA) or a combination thereof. | 10-25-2012 |
20120238618 | Pharmaceutical Composition Comprising Anti-miRNA Antisense Oligonucleotides - The invention provides pharmaceutical compositions comprising short single stranded oligonucleotides, of length of between 8 and 26 nucleobases which are complementary to human microRNAs selected from the group consisting of miR19b, miR21, miR122a, miR155 and miR375. The short oligonucleotides are particularly effective at alleviating miRNA repression in vivo. It is found that the incorporation of high affinity nucleotide analogues into the oligonucleotides results in highly effective anti-microRNA molecules which appear to function via the formation of almost irreversible duplexes with the miRNA target, rather than RNA cleavage based mechanisms, such as mechanisms associated with RNaseH or RISC. | 09-20-2012 |
20120165514 | SYNTHESIS OF LOCKED NUCLEIC ACID DERIVATIVES - The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as α- | 06-28-2012 |
20120115924 | Micro-RNA Mediated Modulation of Colony Stimulating Factors - The present invention relates to the modulation of immunoregulatory proteins, including cytokines, such as colony stimulatory factors (CSF) via the use of microRNA-155 modulators. | 05-10-2012 |
20120088907 | OLIGOMERIC COMPOUNDS FOR THE MODULATION OF SURVIVIN EXPRESSION - Oligonucleotides directed against the survivin gene are provided for modulating the expression of survivin. The compositions comprise oligonucleotides, particularly antisense oligonucleotides, targeted to nucleic acids encoding the survivin. Methods of using these compounds for modulation of survivin expression and for the treatment of diseases associated with either overexpression of survivin, expression of mutated survivin or both are provided. Examples of diseases are cancer such as lung, breast, colon, prostate, pancreas, lung, liver, thyroid, kidney, brain, testes, stomach, intestine, bowel, spinal cord, sinuses, bladder, urinary tract or ovaries cancers. The oligonucleotides may be composed of deoxyribonucleosides or a nucleic acid analogue such as for example locked nucleic acid or a combination thereof. | 04-12-2012 |
20120083596 | Pharmaceutical Composition - The invention provides pharmaceutical compositions comprising short single stranded oligonucleotides, of length of between 8 and 17 nucleobases which are complementary to human microRNAs. The short oligonucleotides are particularly effective at alleviating miRNA repression in vivo. It is found that the incorporation of high affinity nucleotide analogues into the oligonucleotides results in highly effective anti-microRNA molecules which appear to function via the formation of almost irreversible duplexes with the miRNA target, rather than RNA cleavage based mechanisms, such as mechanisms associated with RNaseH or RISC. | 04-05-2012 |
20120004288 | COMPOUNDS FOR THE MODULATION OF BETA-CATENIN EXPRESSION - The invention relates to oligomer compounds (oligomers), which target beta-catening mRNA in a cell, leading to reduced expression of beta-catenin. Reduction of beta-catenin expression is beneficial for a range of medical disorders, such as hyperproliferative disorders, such as cancer. The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of beta-catenin using said oligomers, including methods of treatment. | 01-05-2012 |
20110319471 | LNA ANTAGONISTS TARGETING THE ANDROGEN RECEPTOR - The invention relates to oligonucleotide compounds (oligomers), which target androgen receptor mRNA in a cell, leading to reduced expression of the androgen receptor. Reduction of the androgen receptor expression is beneficial for the treatment of certain disorders, such as a hyperproliferative disorders (e.g., cancer). The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of androgen receptor using said oligomers, including methods of treatment. | 12-29-2011 |
20110224285 | OLIGOMERIC COMPOUNDS FOR THE MODULATION OF HIF-1A EXPRESSION - Oligonucleotides directed against the hypoxia-inducible factor-1α (HIF-1α) gene are provided for modulating the expression of HIF-1α. The compositions comprise oligonucleotides, particularly antisense oligonucleotides, targeted to nucleic acids encoding the HIF-1α. Methods of using these compounds for modulation of HIF-1α expression and for the treatment of diseases associated with the hypoxia-inducible factor-1α are provided. Examples of diseases are cancer and pre-eclampsia. The oligonucleotides may be composed of deoxyribonucleosides, a nucleic acid analogue, or Locked Nucleic Acid (LNA) or a combination thereof. | 09-15-2011 |
20110183931 | POTENT LNA OLIGONUCLEOTIDES FOR THE INHIBITION OF HIF-1A EXPRESSION - The present disclosure relates to an LNA oligonucleotide consisting of a sequence selected from the group consisting of 5′-( | 07-28-2011 |
20110144185 | RNA ANTAGONISTS TARGETING HSP27 - The present invention relates to oligomer compounds (oligomers), which target Hsp27 mRNA in a cell, leading to reduced expression of Hsp27. Reduction of Hsp27 expression is beneficial for the treatment of certain medical disorders, such as cancer. The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of Hsp27 using said oligomers, including methods of treatment | 06-16-2011 |
20110124709 | RNA ANTAGONISTS TARGETING GLI2 - The present invention relates to oligomer compounds (oligomers), which target GLI2 mRNA in a cell, leading to reduced expression of GLI2. Reduction of GLI2 expression is beneficial for the treatment of certain medical disorders, such as hyperproliferative disorders, such as cancer. | 05-26-2011 |
20110086902 | COMPOUNDS FOR THE MODULATION OF BETA-CATENIN EXPRESSION - The invention relates to oligomer compounds (oligomers), which target beta-catenin mRNA in a cell, leading to reduced expression of beta-catenin. Reduction of beta-catenin expression is beneficial for a range of medical disorders, such as hyperproliferative disorders, such as cancer. The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of beta-catenin using said oligomers, including methods of treatment. | 04-14-2011 |
20110077288 | Pharmaceutical Compositions for Treatment of MicroRNA Related Diseases - The present invention provides compositions and methods of treatment of diseases that are sensitive to drugs that downregulate the function of microRNA's, mRNA, non-coding RNA, or viral genomes. In particular, it has been discovered that a very long term effect of an anti microRNA oligonucleotide may be obtained when administered to a primate. Therefore, the present invention relate to pharmaceutical compositions and methods for treatment of primates, including humans wherein the compositions are administered with a long time interval. | 03-31-2011 |
20110077285 | RNA ANTAGONIST COMPOUNDS FOR THE MODULATION OF PIK3CA EXPRESSION - The invention relates to oligomeric compounds (oligomers), which target PIK3CA mRNA in a cell, leading to reduced expression of PIK3CA. Reduction of PIK3CA expression is beneficial for the treatment of certain medical disorders, such as hyperproliferative diseases (e.g., cancer). The invention provides therapeutic compositions that include the oligomers and methods for modulating the expression of PIK3CA using the oligomers, including methods of treatment. | 03-31-2011 |
20100323967 | RNA Antagonist Compounds for the Modulation of MCL-1 - Oligonucleotides directed against the Mcl-1 gene are developed for modulating the expression of Mcl-1 protein. The compositions comprise oligonucleotides, particularly antisense oligonucleotides, targeted to nucleic acids encoding Mcl-1. Methods of using these compounds for modulation of Mcl-1 expression and for the treatment of diseases associated with over expression of Mcl-1 are provided. Examples of such diseases include cancer and systemic mastocytosis. | 12-23-2010 |
20100292311 | OLIGOMERIC COMPOUNDS FOR THE MODULATION OF SURVIVIN EXPRESSION - Oligonucleotides directed against the survivin gene are provided for modulating the expression of survivin. The compositions comprise oligonucleotides, particularly antisense oligonucleotides, targeted to nucleic acids encoding the survivin. Methods of using these compounds for modulation of survivin expression and for the treatment of diseases associated with either overexpression of survivin, expression of mutated survivin or both are provided. Examples of diseases are cancer such as lung, breast, colon, prostate, pancreas, lung, liver, thyroid, kidney, brain, testes, stomach, intestine, bowel, spinal cord, sinuses, bladder, urinary tract or ovaries cancers. The oligonucleotides may be composed of deoxyribonucleosides or a nucleic acid analogue such as for example locked nucleic acid or a combination thereof. | 11-18-2010 |
20100280099 | Combination Treatment For The Treatment of Hepatitis C Virus Infection - The present invention relate to the use of a combination of an inhibitor of miR-122 and an inhibitor of VLDL assembly, for the treatment of HCV, hyperlipidemia and hypercholesterolemia. | 11-04-2010 |
20100234451 | LNA ANTAGONISTS TARGETING THE ANDROGEN RECEPTOR - The invention relates to oligonucleotide compounds (oligomers), which target androgen receptor mRNA in a cell, leading to reduced expression of the androgen receptor. Reduction of the androgen receptor expression is beneficial for the treatment of certain disorders, such as a hyperproliferative disorders (e.g., cancer). The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of androgen receptor using said oligomers, including methods of treatment. | 09-16-2010 |
20100227914 | RNA Antagonist Compounds for the Inhibition of Apo-B100 Expression - Short oligonucleotides directed against the Apo-B100 gene are provided for modulating the expression of Apo-B100. Methods of using these compounds for modulation of Apo-B100 expression and for the treatment of diseases associated with Apo-B100 expression are provided. The oligonucleotides comprise deoxyribonucleosides and locked nucleic acids. | 09-09-2010 |
20100210712 | Short RNA Antagonist Compounds for the Modulation of Target mRNA - The invention provides LNA gapmer oligomers of between 10-20 nucleobases in length, which have a total of 1-3 phosphodiester internucleoside linkages. Such oligomers have been found to have superior bioavailability and have also been found to selectively accumulate in kidney cells. | 08-19-2010 |
20100093839 | OLIGOMERIC COMPOUNDS FOR THE MODULATION OF HIF-1alpha EXPRESSION - Oligonucleotides directed against the hypoxia-inducible factor-1α (HIP-1α) gene are provided for modulating the expression of HIF-1α. The compositions comprise oligonucleotides, particularly antisense oligonucleotides, targeted to nucleic acids encoding the HIF-1α. Methods of using these compounds for modulation of HIF-1α expression and for the treatment of diseases associated with the hypoxia-inducible factor-1α are provided. Examples of diseases are cancer and pre-eclampsia. The oligonucleotides may be composed of deoxyribonucleosides, a nucleic acid analogue, or Locked Nucleic Acid (LNA) or a combination thereof. | 04-15-2010 |
20100062994 | Adenosine Receptor Antagonists - The present application discloses locked nucleoside compounds of the Formula I which act as antagonists of adenosine receptors, in particular the adenosine A3 receptor, and the use of such adenosine A3 receptor compounds in medicine, e.g. for the treatment or alleviation or prophylaxis of selected from the group consisting of pain; inflammatory diseases, arthritis, multiple sclerosis, inflammation, asthma and psoriasis; gastro-intestinal disorders; allergy; disorders associated with mast cell or eosinophil activation and degranulation; cardio-vascular disorders; cutaneous diseases; wound healing; opthalmological disorders; respiratory disorders; kidney diseases; central nervous system disorders; Alzheimer's disease, Creutzfeldt-Jacob disease, Huntington's disease and Parkinson's disease; trauma and seizure; diabetes; osteoporosis; diseases of the immune system; cancers, infections; high blood pressure, locomotor hyperactivity, hypertension and depression; acute hypoxia; neonatal hypoxia, hypoxia and chronic hypoxia; and infertility. | 03-11-2010 |
20100004320 | Pharmaceutical Composition - The invention provides pharmaceutical compositions comprising short single stranded oligonucleotides, of length of between 8 and 17 nucleobases which are complementary to human microRNAs. The short oligonucleotides are particularly effective at alleviating miRNA repression in vivo. It is found that the incorporation of high affinity nucleotide analogues into the oligonucleotides results in highly effective anti-microRNA molecules which appear to function via the formation of almost irreversible duplexes with the miRNA target, rather than RNA cleavage based mechanisms, such as mechanisms associated with RNaseH or RISC. | 01-07-2010 |
20090298916 | Pharmaceutical compositions for treatment of microRNA related diseases - The present invention provides compositions and methods of treatment of diseases that are sensitive to drugs that downregulate the function of microRNA's, mRNA, non-coding RNA, or viral genomes. In particular, it has been discovered that a very long term effect of an anti microRNA oligonucleotide may be obtained when administered to a primate. Therefore, the present invention relate to pharmaceutical compositions and methods for treatment of primates, including humans wherein the compositions are administered with a long time interval. | 12-03-2009 |
20090286859 | POTENT LNA OLIGONUCLEOTIDES FOR THE INHIBITION OF HIF-1a EXPRESSION - The present disclosure relates to an LNA oligonucleotide consisting of a sequence selected from the group consisting of 5′-( | 11-19-2009 |
20090203137 | COMPOUNDS FOR THE MODULATION OF BETA-CATENIN EXPRESSION - The invention relates to oligomer compounds (oligomers), which target beta-catenin mRNA in a cell, leading to reduced expression of beta-catenin. Reduction of beta-catenin expression is beneficial for a range of medical disorders, such as hyperproliferative disorders, such as cancer. The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of beta-catenin using said oligomers, including methods of treatment. | 08-13-2009 |
20090143326 | MICROMIRs - The present invention relates to very short heavily modified oligonucleotides which target and inhibit microRNAs in vivo, and their use in medicaments and pharmaceutical compositions. | 06-04-2009 |
20090005335 | COMPOUNDS FOR THE MODULATION OF BETA-CATENIN EXPRESSION - The invention relates to oligomer compounds (oligomers), which target beta-catenin mRNA in a cell, leading to reduced expression of beta-catenin. Reduction of beta-catenin expression is beneficial for a range of medical disorders, such as hyperproliferative disorders, such as cancer. The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of beta-catenin using said oligomers, including methods of treatment. | 01-01-2009 |
20080318894 | RNA ANTAGONIST COMPOUNDS FOR THE MODULATION OF HER3 - The invention relates to oligomer compounds (oligomers), which target HER3 mRNA in a cell, leading to reduced expression of HER3 and/or HER2 and/or EGFR. Reduction of HER3 and/or HER2 and/or EGFR expression is beneficial for a range of medical disorders, such hyperproliferative disorders (e.g., cancer). The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of HER3 and/or HER2 and/or EGFR using said oligomers, including methods of treatment. | 12-25-2008 |
20080249039 | Modified Short Interfering Rna (Modified Sirna) - The present invention is directed to modified siRNA which are significantly impaired in their ability to support cleavage of mRNA when incorporated into a RISC complex. Such modified siRNA may be useful as therapeutic agents, e.g., in the treatment of various cancer forms. More particularly, the modified siRNA comprises a sense strand and an antisense strand, wherein the sense strand contains a modified RNA nucleotide in at least one of positions 8-14, calculated from the 5′-end. | 10-09-2008 |