AR109303A1 - Oligonucleótidos antisentido del receptor de andrógenos - Google Patents
Oligonucleótidos antisentido del receptor de andrógenosInfo
- 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
Links
Classifications
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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.
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)
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)
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 |
-
2017
- 2017-05-24 JP JP2019507826A patent/JP7407592B2/ja active Active
- 2017-05-24 AU AU2017309347A patent/AU2017309347B2/en active Active
- 2017-05-24 RU RU2019105298A patent/RU2753966C2/ru active
- 2017-05-24 EP EP17838864.1A patent/EP3497114A4/en active Pending
- 2017-05-24 CA CA3032549A patent/CA3032549A1/en active Pending
- 2017-05-24 WO PCT/IB2017/000697 patent/WO2018029517A1/en unknown
- 2017-05-24 BR BR112019002387A patent/BR112019002387A2/pt unknown
- 2017-05-24 KR KR1020197005192A patent/KR102427575B1/ko active IP Right Grant
- 2017-05-24 US US16/324,266 patent/US20190345202A1/en active Pending
- 2017-05-24 SG SG11201900153XA patent/SG11201900153XA/en unknown
- 2017-05-24 CN CN201780061959.8A patent/CN110072879B/zh active Active
- 2017-08-07 TW TW106126503A patent/TWI775764B/zh active
- 2017-08-07 AR ARP170102220A patent/AR109303A1/es unknown
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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