TW202237846A - 靶向pcsk9之反義結合物之口服遞送 - Google Patents

靶向pcsk9之反義結合物之口服遞送 Download PDF

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TW202237846A
TW202237846A TW110146453A TW110146453A TW202237846A TW 202237846 A TW202237846 A TW 202237846A TW 110146453 A TW110146453 A TW 110146453A TW 110146453 A TW110146453 A TW 110146453A TW 202237846 A TW202237846 A TW 202237846A
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pharmaceutical composition
aspects
composition according
pcsk9
capsule
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TW110146453A
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Chinese (zh)
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亨利克 歐瑞姆
斯圖爾特 阿爾溫 諾伯
查理斯 萊斯特 希爾
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美商希威生物製藥股份有限公司
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TW110146453A 2020-12-11 2021-12-10 靶向pcsk9之反義結合物之口服遞送 TW202237846A (zh)

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US202063124581P 2020-12-11 2020-12-11
US63/124,581 2020-12-11
US202163134884P 2021-01-07 2021-01-07
US63/134,884 2021-01-07
US202163178340P 2021-04-22 2021-04-22
US63/178,340 2021-04-22
US202163261505P 2021-09-22 2021-09-22
US63/261,505 2021-09-22

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CR20230308A (es) 2020-12-11 2023-09-08 Civi Biopharma Inc Entrega oral de conjugados antisentido que tienen por blanco a pcsk9
CR20230471A (es) * 2021-04-22 2023-11-01 Civi Biopharma Inc Administración oral de oligonucleótidos
WO2023065231A1 (en) * 2021-10-21 2023-04-27 Guangzhou Dazhou Biomedicine Ltd. Oral delivery of therapeutic agents

Family Cites Families (100)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4043996A (en) 1975-01-27 1977-08-23 Swift & Company Gelatin manufacture-peroxide liquefaction process
GB1557005A (en) 1975-07-11 1979-12-05 Novo Industri As Gelatine extraction
US4176117A (en) 1977-03-11 1979-11-27 Leon Oudem Process for obtaining gelatin
US4232425A (en) 1980-01-15 1980-11-11 Darling & Company Method of producing stabilized bone
ZA816771B (en) 1980-10-07 1982-10-27 Lensfield Prod Ltd Protein production
US4374063A (en) 1981-09-28 1983-02-15 General Foods Corporation Process for the preparation and purification of gelatin and pyrogen-free gelatin so prepared
JPS5927900A (ja) 1982-08-09 1984-02-14 Wakunaga Seiyaku Kk 固定化オリゴヌクレオチド
US4402873A (en) 1982-09-23 1983-09-06 Sugardale Foods Incorporated Extraction of protein from pork bones
US4948882A (en) 1983-02-22 1990-08-14 Syngene, Inc. Single-stranded labelled oligonucleotides, reactive monomers and methods of synthesis
US4587044A (en) 1983-09-01 1986-05-06 The Johns Hopkins University Linkage of proteins to nucleic acids
US5430136A (en) 1984-10-16 1995-07-04 Chiron Corporation Oligonucleotides having selectably cleavable and/or abasic sites
DE3726963A1 (de) 1987-08-13 1989-02-23 Stoess & Co Gelatine Kaltwasserloesliche, instantisierte gelatine und verfahren zur herstellung derselben
US5525465A (en) 1987-10-28 1996-06-11 Howard Florey Institute Of Experimental Physiology And Medicine Oligonucleotide-polyamide conjugates and methods of production and applications of the same
DE3738460A1 (de) 1987-11-12 1989-05-24 Max Planck Gesellschaft Modifizierte oligonukleotide
FR2625412B1 (fr) 1987-12-30 1990-06-29 Mero Rousselot Satia Procede continu d'obtention de gelatine a partir de poudre d'os et gelatine obtenue
IL87344A (en) 1988-08-04 1992-03-29 Univ Bar Ilan Process for the production of gelatin from fish skins
US5391723A (en) 1989-05-31 1995-02-21 Neorx Corporation Oligonucleotide conjugates
US5254469A (en) 1989-09-12 1993-10-19 Eastman Kodak Company Oligonucleotide-enzyme conjugate that can be used as a probe in hybridization assays and polymerase chain reaction procedures
US5486603A (en) 1990-01-08 1996-01-23 Gilead Sciences, Inc. Oligonucleotide having enhanced binding affinity
US5608046A (en) 1990-07-27 1997-03-04 Isis Pharmaceuticals, Inc. Conjugated 4'-desmethyl nucleoside analog compounds
US5245022A (en) 1990-08-03 1993-09-14 Sterling Drug, Inc. Exonuclease resistant terminally substituted oligonucleotides
US5512667A (en) 1990-08-28 1996-04-30 Reed; Michael W. Trifunctional intermediates for preparing 3'-tailed oligonucleotides
KR930702373A (ko) 1990-11-08 1993-09-08 안토니 제이. 페이네 합성 올리고누클레오티드에 대한 다중 리포터(Reporter)그룹의 첨합
US5210182A (en) 1992-02-12 1993-05-11 Kraft General Foods, Inc. Extraction process for gelatin
US5288408A (en) 1992-10-26 1994-02-22 Chemical Industry Consultants, Inc. Method of gelatin recovery and purification from encapsulation processes
JPH08504559A (ja) 1992-12-14 1996-05-14 ハネウエル・インコーポレーテッド 個別に制御される冗長巻線を有するモータシステム
US5574142A (en) 1992-12-15 1996-11-12 Microprobe Corporation Peptide linkers for improved oligonucleotide delivery
US5580731A (en) 1994-08-25 1996-12-03 Chiron Corporation N-4 modified pyrimidine deoxynucleotides and oligonucleotide probes synthesized therewith
AU3999495A (en) 1994-10-06 1996-05-02 Buchardt, Dorte Peptide nucleic acid conjugates
US5650386A (en) 1995-03-31 1997-07-22 Emisphere Technologies, Inc. Compositions for oral delivery of active agents
US5866536A (en) 1995-03-31 1999-02-02 Emisphere Technologies, Inc. Compounds and compositions for delivering active agents
US5684142A (en) 1995-06-07 1997-11-04 Oncor, Inc. Modified nucleotides for nucleic acid labeling
US6090915A (en) 1996-10-18 2000-07-18 Hormel Foods Corporation Collagen or gelatin crumble composition and uses
US5851579A (en) 1996-10-28 1998-12-22 Eastman Chemical Company Aqueous enteric coating compositions
US5773647A (en) 1997-02-07 1998-06-30 Emisphere Technologies, Inc. Compounds and compositions for delivering active agents
JP3756313B2 (ja) 1997-03-07 2006-03-15 武 今西 新規ビシクロヌクレオシド及びオリゴヌクレオチド類縁体
US6770748B2 (en) 1997-03-07 2004-08-03 Takeshi Imanishi Bicyclonucleoside and oligonucleotide analogue
US5770716A (en) 1997-04-10 1998-06-23 The Perkin-Elmer Corporation Substituted propargylethoxyamido nucleosides, oligonucleotides and methods for using same
CN1263473A (zh) 1997-05-21 2000-08-16 利兰·斯坦福青年大学托管委员会 增加跨生物膜转运的组合物和方法
US6794499B2 (en) 1997-09-12 2004-09-21 Exiqon A/S Oligonucleotide analogues
JP4236812B2 (ja) 1997-09-12 2009-03-11 エクシコン エ／エス オリゴヌクレオチド類似体
GB9807331D0 (en) 1998-04-07 1998-06-03 Cerestar Holding Bv Gelatin replacement by wheat fiber gel and starch
US6096875A (en) 1998-05-29 2000-08-01 The Perlein-Elmer Corporation Nucleotide compounds including a rigid linker
US6335432B1 (en) 1998-08-07 2002-01-01 Bio-Red Laboratories, Inc. Structural analogs of amine bases and nucleosides
US6335437B1 (en) 1998-09-07 2002-01-01 Isis Pharmaceuticals, Inc. Methods for the preparation of conjugated oligomers
AU3357800A (en) 1999-02-05 2000-08-25 Emisphere Technologies, Inc. Method of preparing alkylated salicylamides
ES2235854T3 (es) 1999-04-05 2005-07-16 Emisphere Technologies, Inc. Sales disodicas, monohidratos y solvatos etanolicos para aportar agentes activos.
EP1535625B1 (en) 1999-04-05 2014-01-08 Novartis AG Composition containing n-(5-chlorosalicyloyl)-8-aminocaprylic acid and salmon calcitonin
US7053207B2 (en) 1999-05-04 2006-05-30 Exiqon A/S L-ribo-LNA analogues
US6525191B1 (en) 1999-05-11 2003-02-25 Kanda S. Ramasamy Conformationally constrained L-nucleosides
US6458383B2 (en) 1999-08-17 2002-10-01 Lipocine, Inc. Pharmaceutical dosage form for oral administration of hydrophilic drugs, particularly low molecular weight heparin
US6617442B1 (en) 1999-09-30 2003-09-09 Isis Pharmaceuticals, Inc. Human Rnase H1 and oligonucleotide compositions thereof
US6375981B1 (en) 2000-06-01 2002-04-23 A. E. Staley Manufacturing Co. Modified starch as a replacement for gelatin in soft gel films and capsules
TWI307279B (en) 2002-08-01 2009-03-11 Novartis Ag Oral administration of calcitonin
AU2003291755A1 (en) 2002-11-05 2004-06-07 Isis Pharmaceuticals, Inc. Oligomers comprising modified bases for binding cytosine and uracil or thymine and their use
WO2004041889A2 (en) 2002-11-05 2004-05-21 Isis Pharmaceuticals, Inc. Polycyclic sugar surrogate-containing oligomeric compounds and compositions for use in gene modulation
WO2004046160A2 (en) 2002-11-18 2004-06-03 Santaris Pharma A/S Amino-lna, thio-lna and alpha-l-oxy-ln
CA2518475C (en) 2003-03-07 2014-12-23 Alnylam Pharmaceuticals, Inc. Irna agents comprising asymmetrical modifications
US8796436B2 (en) 2003-04-17 2014-08-05 Alnylam Pharmaceuticals, Inc. Modified iRNA agents
WO2004106356A1 (en) 2003-05-27 2004-12-09 Syddansk Universitet Functionalized nucleotide derivatives
US20070065505A1 (en) 2003-07-11 2007-03-22 Shoufeng Li Orally dosed pharmaceutical compositions comprising a delivery agent in micronized form
EP1661905B9 (en) 2003-08-28 2012-12-19 IMANISHI, Takeshi Novel artificial nucleic acids of n-o bond crosslinkage type
WO2007031091A2 (en) * 2005-09-15 2007-03-22 Santaris Pharma A/S Rna antagonist compounds for the modulation of p21 ras expression
CN105641686A (zh) 2005-09-19 2016-06-08 爱密斯菲尔科技公司 N-(5-氯水杨酰基)-8-氨基辛酸的二钠盐的晶形
WO2007090071A2 (en) 2006-01-27 2007-08-09 Isis Pharmaceuticals, Inc. 6-modified bicyclic nucleic acid analogs
JP2009536222A (ja) 2006-05-05 2009-10-08 アイシス ファーマシューティカルズ， インコーポレーテッド Ｐｃｓｋ９の発現を調節するための化合物および方法
AU2007249349B2 (en) 2006-05-11 2012-03-08 Isis Pharmaceuticals, Inc. 5'-Modified bicyclic nucleic acid analogs
BRPI0716261A2 (pt) * 2006-08-31 2013-08-06 Novartis Ag composiÇÕes farmacÊuticas compreendendo hch para distribuiÇço oral
BRPI0716539A2 (pt) 2006-09-07 2016-11-01 Emisphere Tech Inc métodos para sintetização de ácido n-(8-[2-hidroxibenzoil]amino) caprílico e de sal de sódio deste
DK2149605T3 (da) 2007-03-22 2013-09-30 Santaris Pharma As Korte RNA antagonist forbindelser til modulering af det ønskede mRNA
CA2688321A1 (en) 2007-05-30 2008-12-11 Isis Pharmaceuticals, Inc. N-substituted-aminomethylene bridged bicyclic nucleic acid analogs
DK2173760T4 (en) 2007-06-08 2016-02-08 Isis Pharmaceuticals Inc Carbocyclic bicyclic nukleinsyreanaloge
AU2008272918B2 (en) 2007-07-05 2012-09-13 Isis Pharmaceuticals, Inc. 6-disubstituted bicyclic nucleic acid analogs
EP2460515B1 (en) 2007-08-09 2017-03-08 Novartis AG Oral calcitonin compositions and applications thereof
EP2623599B1 (en) 2007-10-04 2019-01-02 Roche Innovation Center Copenhagen A/S Micromirs
WO2009067647A1 (en) 2007-11-21 2009-05-28 Isis Pharmaceuticals, Inc. Carbocyclic alpha-l-bicyclic nucleic acid analogs
WO2009100320A2 (en) 2008-02-07 2009-08-13 Isis Pharmaceuticals, Inc. Bicyclic cyclohexitol nucleic acid analogs
US9290534B2 (en) 2008-04-04 2016-03-22 Ionis Pharmaceuticals, Inc. Oligomeric compounds having at least one neutrally linked terminal bicyclic nucleoside
DK2356129T3 (da) 2008-09-24 2013-05-13 Isis Pharmaceuticals Inc Substituerede alpha-L-bicykliske nukleosider
CA2764822A1 (en) 2009-06-12 2010-12-16 Santaris Pharma A/S New potent anti apob antisense compounds
EP2456870A1 (en) 2009-07-21 2012-05-30 Santaris Pharma A/S Antisense oligomers targeting pcsk9
CA2812046A1 (en) 2010-09-15 2012-03-22 Alnylam Pharmaceuticals, Inc. Modified irna agents
SI2651398T1 (en) 2010-12-16 2018-04-30 Novo Nordisk A/S SOLID COMPOSITIONS CONTAINING GLP-1 AGONIST AND SOL N- (8- (2-HYDROXYBENZOIL) AMINO) CAPRICULATE ACIDS
AU2011343664B2 (en) 2010-12-17 2015-10-08 Arrowhead Pharmaceuticals, Inc. Galactose cluster-pharmacokinetic modulator targeting moiety for siRNA
TWI459777B (zh) 2011-07-11 2014-11-01 Mediatek Inc 加強型傳呼的方法及其機器類型通訊裝置
SI3366775T2 (sl) 2011-11-18 2025-12-31 Alnylam Pharmaceuticals, Inc. Modificirana sredstva RNAI
PL2897620T3 (pl) * 2012-09-21 2020-11-02 Intensity Therapeutics, Inc Sposób leczenia nowotworu złośliwego
CA2894174A1 (en) * 2012-12-06 2014-06-12 Regado Biosciences Inc. Oligonucleotide formulation
US20140323543A1 (en) 2013-04-25 2014-10-30 Jeremy Richard Graff Treatment of Prostate Cancer with eIF4E Antisense Compounds
HUE048738T2 (hu) 2013-06-27 2020-08-28 Roche Innovation Ct Copenhagen As Antiszensz oligomerek és konjugátumok, amelyek a PCK9-t célozzák meg
EP3151839A4 (en) * 2014-06-06 2018-02-28 Ionis Pharmaceuticals, Inc. Compositions and methods for enhanced intestinal absorption of conjugated oligomeric compounds
CN104095828A (zh) * 2014-07-29 2014-10-15 中国药科大学 一种降钙素口服肠溶组合物及其制备方法
IL316808A (en) 2014-08-20 2025-01-01 Alnylam Pharmaceuticals Inc Modified double-stranded RNA materials and their uses
CA3033004A1 (en) 2016-09-09 2018-03-15 Fred Hutchinson Cancer Research Center Stable peptides and methods of use thereof
US11504391B1 (en) 2016-11-23 2022-11-22 Alnylam Pharmaceuticals, Inc. Modified RNA agents with reduced off-target effect
JOP20190215A1 (ar) 2017-03-24 2019-09-19 Ionis Pharmaceuticals Inc مُعدّلات التعبير الوراثي عن pcsk9
WO2020069055A1 (en) * 2018-09-28 2020-04-02 Alnylam Pharmaceuticals, Inc. Transthyretin (ttr) irna compositions and methods of use thereof for treating or preventing ttr-associated ocular diseases
AU2020279101B2 (en) 2019-05-17 2025-07-24 Alnylam Pharmaceuticals, Inc. Oral delivery of oligonucleotides
CR20230308A (es) 2020-12-11 2023-09-08 Civi Biopharma Inc Entrega oral de conjugados antisentido que tienen por blanco a pcsk9
CR20230471A (es) 2021-04-22 2023-11-01 Civi Biopharma Inc Administración oral de oligonucleótidos

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