AR109303A1 - Oligonucleótidos antisentido del receptor de andrógenos - Google Patents

Oligonucleótidos antisentido del receptor de andrógenos

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Publication number
AR109303A1
AR109303A1 ARP170102220A ARP170102220A AR109303A1 AR 109303 A1 AR109303 A1 AR 109303A1 AR P170102220 A ARP170102220 A AR P170102220A AR P170102220 A ARP170102220 A AR P170102220A AR 109303 A1 AR109303 A1 AR 109303A1
Authority
AR
Argentina
Prior art keywords
substituted
unsubstituted
hydride
radical
nucleobases
Prior art date
Application number
ARP170102220A
Other languages
English (en)
Original Assignee
Olipass Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Olipass Corp filed Critical Olipass Corp
Publication of AR109303A1 publication Critical patent/AR109303A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/001—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof by chemical synthesis
    • C07K14/003—Peptide-nucleic acids (PNAs)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/10—Peptides having 12 to 20 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/111—General methods applicable to biologically active non-coding nucleic acids
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
    • C12N15/1138—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing against receptors or cell surface proteins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/10—Type of nucleic acid
    • C12N2310/11—Antisense
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/31—Chemical structure of the backbone
    • C12N2310/318—Chemical structure of the backbone where the PO2 is completely replaced, e.g. MMI or formacetal
    • C12N2310/3181—Peptide nucleic acid, PNA
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/33—Chemical structure of the base
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/35—Nature of the modification
    • C12N2310/351—Conjugate
    • C12N2310/3513—Protein; Peptide
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2320/00—Applications; Uses
    • C12N2320/30—Special therapeutic applications
    • C12N2320/32—Special delivery means, e.g. tissue-specific
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2320/00—Applications; Uses
    • C12N2320/30—Special therapeutic applications
    • C12N2320/33—Alteration of splicing
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biotechnology (AREA)
  • General Engineering & Computer Science (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Microbiology (AREA)
  • Plant Pathology (AREA)
  • Physics & Mathematics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Saccharide Compounds (AREA)

Abstract

Los derivados de ácido nucleico peptídicos inducen potentemente variantes de empalme del ARNm de receptor androgénico en células, y son útiles para tratar de manera segura indicaciones o afecciones dermatológicas que involucran la actividad androgénica, mediante la administración tópica. Reivindicación 1: Un derivado de ácido nucleico peptídico representado por la fórmula (1), o una de sus sales farmacéuticamente aceptables, donde, n es un número entero entre 10 y 21; el compuesto de la fórmula (1) posee por lo menos una superposición complementaria de 9 meros con una secuencia de ARN de 17 meros de [(5’ ® 3’) CCUUGCCUGGUAAGGAA] dentro del pre-ARNm de receptor androgénico humano; S₁, S₂, , Sₙ₋₁, Sₙ, T₁, T₂, , Tₙ₋₁ y Tₙ representan de manera independiente deuteruro, hidruro, alquilo sustituido o no sustituido, o radical arilo sustituido o no sustituido; X e Y representan de manera independiente hidruro [H], formilo [H-C(=O)-], aminocarbonilo [NH₂-C(=O)-], alquilo sustituido o no sustituido, arilo sustituido o no sustituido, alquilacilo sustituido o no sustituido, arilacilo sustituido o no sustituido, alquiloxicarbonilo sustituido o no sustituido, ariloxicarbonilo sustituido o no sustituido, alquilaminocarbonilo sustituido o no sustituido, arilaminocarbonilo sustituido o no sustituido, alquilsulfonilo sustituido o no sustituido, o radical arilsulfonilo sustituido o no sustituido; Z representa hidruro, hidroxi, alquiloxi sustituido o no sustituido, ariloxi sustituido o no sustituido, amino sustituido o no sustituido, alquilo sustituido o no sustituido, o radical arilo sustituido o no sustituido; B₁, B₂, , Bₙ₋₁ y Bₙ se seleccionan de manera independiente de nucleobases naturales que incluyen adenina, timina, guanina, citosina y uracilo y nucleobases no naturales; y por lo menos cuatro de B₁, B₂, , Bₙ₋₁ y Bₙ se seleccionan de manera independiente de nucleobases no naturales con un radical amino sustituido o no sustituido covalentemente unido al resto de nucleobase.
ARP170102220A 2016-08-08 2017-08-07 Oligonucleótidos antisentido del receptor de andrógenos AR109303A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201662372035P 2016-08-08 2016-08-08

Publications (1)

Publication Number Publication Date
AR109303A1 true AR109303A1 (es) 2018-11-21

Family

ID=61161927

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP170102220A AR109303A1 (es) 2016-08-08 2017-08-07 Oligonucleótidos antisentido del receptor de andrógenos

Country Status (13)

Country Link
US (1) US20190345202A1 (es)
EP (1) EP3497114A4 (es)
JP (1) JP7407592B2 (es)
KR (1) KR102427575B1 (es)
CN (1) CN110072879B (es)
AR (1) AR109303A1 (es)
AU (1) AU2017309347B2 (es)
BR (1) BR112019002387A2 (es)
CA (1) CA3032549A1 (es)
RU (1) RU2753966C2 (es)
SG (1) SG11201900153XA (es)
TW (1) TWI775764B (es)
WO (1) WO2018029517A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2017385962B2 (en) * 2016-12-30 2021-09-02 Olipass Corporation Exon skipping by peptide nucleic acid derivatives
JP7503903B2 (ja) * 2017-01-06 2024-06-21 オリパス コーポレーション Ｓｎａｐ２５アンチセンスオリゴヌクレオチド
WO2018138585A1 (en) * 2017-01-24 2018-08-02 Olipass Corporation Scn9a antisense pain killer
TWI832851B (zh) * 2018-05-18 2024-02-21 韓商奧利通公司 基質金屬蛋白酶-1之反義寡核苷酸
KR102304280B1 (ko) * 2018-08-14 2021-09-23 올리패스 주식회사 아세틸코에이카복실라제2 안티센스 올리고뉴클레오티드

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL104043A0 (en) * 1991-12-12 1993-05-13 Scios Nova Inc Fluorenyl derivatives and pharmaceutical compositions containing them
CA2156512C (en) * 1993-02-19 2002-11-19 Mary Ellen Harper Treatment of androgen-associated baldness using antisense oligomers
US6133444A (en) * 1993-12-22 2000-10-17 Perseptive Biosystems, Inc. Synthons for the synthesis and deprotection of peptide nucleic acids under mild conditions
US6617422B1 (en) * 1997-05-23 2003-09-09 Peter Nielsen Peptide nucleic acid monomers and oligomers
WO2000001813A2 (en) * 1998-06-30 2000-01-13 The University Of British Columbia Peptide inhibitors of androgen-independent activation of androgen receptor
WO2002097134A2 (en) * 2001-05-25 2002-12-05 Isis Pharmaceuticals, Inc. Modified peptide nucleic acid
US20050153935A1 (en) * 2003-09-12 2005-07-14 Iversen Patrick L. Compound and method for treating androgen-independent prostate cancer
TW200930382A (en) * 2007-11-26 2009-07-16 Santaris Pharma As LNA antagonists targeting the androgen receptor
US8450290B2 (en) * 2007-11-26 2013-05-28 Enzon Pharmaceuticals, Inc. Methods for treating androgen receptor dependent disorders including cancers
KR20090098710A (ko) 2008-03-14 2009-09-17 주식회사 씨티아이바이오 세포투과성과 핵산 결합력이 좋은 펩타이드 핵산 유도체
EP4052709A1 (en) * 2012-10-11 2022-09-07 Ionis Pharmaceuticals, Inc. Methods of treating kennedy's disease
WO2018012261A1 (ja) * 2016-07-14 2018-01-18 株式会社日立製作所 電気品収容用筐体及びその製作方法
AU2017385962B2 (en) * 2016-12-30 2021-09-02 Olipass Corporation Exon skipping by peptide nucleic acid derivatives

Also Published As

Publication number Publication date
TWI775764B (zh) 2022-09-01
TW201812009A (zh) 2018-04-01
RU2753966C2 (ru) 2021-08-24
RU2019105298A (ru) 2020-09-11
BR112019002387A2 (pt) 2019-06-04
AU2017309347B2 (en) 2020-11-19
RU2019105298A3 (es) 2020-10-08
CN110072879B (zh) 2023-03-10
CA3032549A1 (en) 2018-02-15
SG11201900153XA (en) 2019-02-27
WO2018029517A1 (en) 2018-02-15
KR102427575B1 (ko) 2022-08-01
EP3497114A4 (en) 2020-04-29
CN110072879A (zh) 2019-07-30
JP7407592B2 (ja) 2024-01-04
JP2019527720A (ja) 2019-10-03
EP3497114A1 (en) 2019-06-19
KR20190055066A (ko) 2019-05-22
AU2017309347A1 (en) 2019-02-07
US20190345202A1 (en) 2019-11-14

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