AR041407A1 - Oligonucleotidos antiandrogenos utilizables en el tratamiento de patologias dermatologicas relacionadas con el metabolismo de los androgenos, sus composiciones farmaceuticas y sus usos y metodos de tratamiento - Google Patents
Oligonucleotidos antiandrogenos utilizables en el tratamiento de patologias dermatologicas relacionadas con el metabolismo de los androgenos, sus composiciones farmaceuticas y sus usos y metodos de tratamientoInfo
- Publication number
- AR041407A1 AR041407A1 ARP030103517A ARP030103517A AR041407A1 AR 041407 A1 AR041407 A1 AR 041407A1 AR P030103517 A ARP030103517 A AR P030103517A AR P030103517 A ARP030103517 A AR P030103517A AR 041407 A1 AR041407 A1 AR 041407A1
- Authority
- AR
- Argentina
- Prior art keywords
- inn
- seq
- treatment
- oligonucleotides
- androgen receptor
- Prior art date
Links
- 239000003098 androgen Substances 0.000 title abstract 2
- 230000004060 metabolic process Effects 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 108091034117 Oligonucleotide Proteins 0.000 abstract 5
- JLCPHMBAVCMARE-UHFFFAOYSA-N [3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-[[3-[[3-[[3-[[3-[[3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-hydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methyl [5-(6-aminopurin-9-yl)-2-(hydroxymethyl)oxolan-3-yl] hydrogen phosphate Polymers Cc1cn(C2CC(OP(O)(=O)OCC3OC(CC3OP(O)(=O)OCC3OC(CC3O)n3cnc4c3nc(N)[nH]c4=O)n3cnc4c3nc(N)[nH]c4=O)C(COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3CO)n3cnc4c(N)ncnc34)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cc(C)c(=O)[nH]c3=O)n3cc(C)c(=O)[nH]c3=O)n3ccc(N)nc3=O)n3cc(C)c(=O)[nH]c3=O)n3cnc4c3nc(N)[nH]c4=O)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)O2)c(=O)[nH]c1=O JLCPHMBAVCMARE-UHFFFAOYSA-N 0.000 abstract 5
- 102000001307 androgen receptors Human genes 0.000 abstract 3
- 108010080146 androgen receptors Proteins 0.000 abstract 3
- 230000002280 anti-androgenic effect Effects 0.000 abstract 3
- 239000000051 antiandrogen Substances 0.000 abstract 2
- 108020004999 messenger RNA Proteins 0.000 abstract 2
- 210000003491 skin Anatomy 0.000 abstract 2
- 201000004384 Alopecia Diseases 0.000 abstract 1
- 102100034343 Integrase Human genes 0.000 abstract 1
- 101710203526 Integrase Proteins 0.000 abstract 1
- 230000003213 activating effect Effects 0.000 abstract 1
- 238000004113 cell culture Methods 0.000 abstract 1
- 239000002537 cosmetic Substances 0.000 abstract 1
- 230000029087 digestion Effects 0.000 abstract 1
- 210000003780 hair follicle Anatomy 0.000 abstract 1
- 208000024963 hair loss Diseases 0.000 abstract 1
- 230000003676 hair loss Effects 0.000 abstract 1
- 230000010534 mechanism of action Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 210000004761 scalp Anatomy 0.000 abstract 1
- 208000017520 skin disease Diseases 0.000 abstract 1
Classifications
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- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- 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
- C12N2310/30—Chemical structure
- C12N2310/31—Chemical structure of the backbone
- C12N2310/315—Phosphorothioates
-
- 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
- C12N2310/34—Spatial arrangement of the modifications
- C12N2310/345—Spatial arrangement of the modifications having at least two different backbone modifications
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Genetics & Genomics (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Chemical & Material Sciences (AREA)
- Zoology (AREA)
- Biotechnology (AREA)
- Molecular Biology (AREA)
- General Engineering & Computer Science (AREA)
- Wood Science & Technology (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Plant Pathology (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Physics & Mathematics (AREA)
- Biophysics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Microbiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Dermatology (AREA)
- Biochemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Cosmetics (AREA)
Abstract
Se describen oligonucleótidos antiandrógenos aptos para el tratamiento de la caída del cabello y enfermedades de la piel relacionadas con el metabolismo de los andrógenos. Los oligonucleótidos tienen las siguientes secuencias:§ INN-18.1 (SEC ID Ns 1): 5`CATTGGTGAAGGATCGCC 3`; § INN-24 (SEC ID Ns 2): 5`CAATCATTTCTGCTGGCG 3; § INN-71 (SEC ID Ns 3): 5` GGCCTTCTTCGGCTGTGAAG 3`; § INN-72 (SEC ID Ns4): 5` CACACGGTCCATACAACTGG 3`;§ INN-18.2 (SEC ID Ns 5): 5`GGCGAAGTAGAGCATCCT 3`; § INN-24.1 (SEC ID Ns 6); 5`TGGCGCACAGGTACTTCT 3`; § INN-73 (SEC ID Ns 7): 5`CCACCACCACCACACGG 3`; § INN-76 (SEC ID Ns 8): 5`GCCGCCACCACCCCCACC 3`. Estos Principios activos anti-androgénicos son muy específicos para alcanzar su blanco molecular, que se encuentra especialmente circunscripto al sitio de aplicación, principalmente al receptor de andrógenos en la piel y cuero cabelludo de humanos tratados. Los oligonucleótidos descriptos inhiben la expresión del receptor de andrógenos a concentraciones muy bajas en cultivos celulares primarios de la piel y el folículo piloso a través de un mecanismo de acción que implica alcanzar e hibridar con regiones específicas del mARN del RA, de ese modo se activa la digestión por RNasa H del mARN del receptor de andrógeno y en consecuencia se inhibe la traducción de éste último. Se describen también composiciones farmacéuticas y/o cosméticas administrables en forma tópica que contienen los oligonucleótidos. Uso de los oligonucleótidos antiandrógenos y método de tratamiento.
Priority Applications (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ARP030103517A AR041407A1 (es) | 2003-09-26 | 2003-09-26 | Oligonucleotidos antiandrogenos utilizables en el tratamiento de patologias dermatologicas relacionadas con el metabolismo de los androgenos, sus composiciones farmaceuticas y sus usos y metodos de tratamiento |
| ES04022696T ES2322583T3 (es) | 2003-09-26 | 2004-09-23 | Oligonucleotidos anti-androgenos utilizables en el tratamiento de trastornos dermatologicos relacionados con el metabolismo de los androgenos, sus composiciones farmaceuticas, sus usos y metodo de tratamiento. |
| US10/948,781 US20060009429A1 (en) | 2003-09-26 | 2004-09-23 | Antiandrogen oligonucleotides usable for the treatment of dermatological androgen-related disorders relating to androgen metabolism, their pharmaceutical compositions, their uses and treatment method |
| EP04022696A EP1518928B1 (en) | 2003-09-26 | 2004-09-23 | Antiandrogen oligonucleotides usable for the treatment of dermatological androgen-related disorders relating to androgen metabolism, their pharmaceutical compositions, their uses and treatment method |
| DE602004019481T DE602004019481D1 (de) | 2003-09-26 | 2004-09-23 | Antiandrogen-Oligonukleotide zur Behandlung von Androgen-verwandten Hautkrankheiten, diese Verbindungen enthaltende pharmazeutische Zusammensetzungen und deren Verwendung |
| AT04022696T ATE423201T1 (de) | 2003-09-26 | 2004-09-23 | Antiandrogen-oligonukleotide zur behandlung von androgen-verwandten hautkrankheiten, diese verbindungen enthaltende pharmazeutische zusammensetzungen und deren verwendung |
| US12/698,055 US20100311813A1 (en) | 2003-09-26 | 2010-02-01 | Antiandrogen oligonucleotides usable for the treatment of dermatological androgen-related disorders relating to androgen metabolism, their pharmaceutical compositions, their uses and treatment method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ARP030103517A AR041407A1 (es) | 2003-09-26 | 2003-09-26 | Oligonucleotidos antiandrogenos utilizables en el tratamiento de patologias dermatologicas relacionadas con el metabolismo de los androgenos, sus composiciones farmaceuticas y sus usos y metodos de tratamiento |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR041407A1 true AR041407A1 (es) | 2005-05-18 |
Family
ID=34140109
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030103517A AR041407A1 (es) | 2003-09-26 | 2003-09-26 | Oligonucleotidos antiandrogenos utilizables en el tratamiento de patologias dermatologicas relacionadas con el metabolismo de los androgenos, sus composiciones farmaceuticas y sus usos y metodos de tratamiento |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US20060009429A1 (es) |
| EP (1) | EP1518928B1 (es) |
| AR (1) | AR041407A1 (es) |
| AT (1) | ATE423201T1 (es) |
| DE (1) | DE602004019481D1 (es) |
| ES (1) | ES2322583T3 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR055648A1 (es) * | 2006-09-21 | 2007-08-29 | Gen Med Sa | Un oligonucleotido de rna de doble cadena una composicion farmaceutica o cosmetica que lo comprende y uso del mismo enla preparacion de un medicamento para el tratamiento de enfermedades relacionadas con el metabolismo de androgenos |
| WO2017137095A1 (en) * | 2016-02-12 | 2017-08-17 | Curevac Ag | Method for analyzing rna |
| US11920174B2 (en) | 2016-03-03 | 2024-03-05 | CureVac SE | RNA analysis by total hydrolysis and quantification of released nucleosides |
| EP3484462B1 (en) | 2016-07-15 | 2022-12-14 | Institut Pasteur | 5-hydroxytryptamine 1b receptor-stimulating agent for skin and/or hair repair |
| US10635837B1 (en) | 2019-04-30 | 2020-04-28 | HealthBlock, Inc. | Dynamic data protection |
| US12067151B2 (en) | 2019-04-30 | 2024-08-20 | Enya Inc. | Resource-efficient privacy-preserving transactions |
| CN115721716B (zh) * | 2022-07-13 | 2024-06-14 | 苏州翊鹏医药科技有限公司 | Mdh2抑制剂在雄激素性脱发治疗中的应用 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5877160A (en) | 1991-05-31 | 1999-03-02 | Genta Incorporated | Compositions and methods of treatment of androgen-associated baldness using antisense oligomers |
| US5556956A (en) * | 1993-11-04 | 1996-09-17 | Board Of Regents, The University Of Texas System | Methods and compositions relating to the androgen receptor gene and uses thereof |
| EP0851919A1 (en) * | 1995-09-20 | 1998-07-08 | University of Massachusetts Worcester | Antisense oligonucleotide chemotherapy for benign hyperplasia or cancer of the prostate |
| US6489163B1 (en) * | 1996-05-08 | 2002-12-03 | Board Of Regents, The University Of Texas System | Ribozyme mediated inactivation of the androgen receptor |
| EP1282699B1 (en) * | 2000-05-04 | 2012-11-21 | Sarepta Therapeutics, Inc. | Splice-region antisense composition and method |
| DE10141443B4 (de) * | 2001-08-23 | 2007-02-01 | Christos C. Prof. Dr. Zouboulis | Verwendung von molekularbiologisch hergestellten, nicht-viralen Wirkstoffen zur Behandlung der Akne |
| US20040137471A1 (en) * | 2002-09-18 | 2004-07-15 | Timothy Vickers | Efficient reduction of target RNA's by single-and double-stranded oligomeric compounds |
| EP1560931B1 (en) * | 2002-11-14 | 2011-07-27 | Dharmacon, Inc. | Functional and hyperfunctional sirna |
-
2003
- 2003-09-26 AR ARP030103517A patent/AR041407A1/es active IP Right Grant
-
2004
- 2004-09-23 US US10/948,781 patent/US20060009429A1/en not_active Abandoned
- 2004-09-23 AT AT04022696T patent/ATE423201T1/de not_active IP Right Cessation
- 2004-09-23 EP EP04022696A patent/EP1518928B1/en not_active Expired - Lifetime
- 2004-09-23 ES ES04022696T patent/ES2322583T3/es not_active Expired - Lifetime
- 2004-09-23 DE DE602004019481T patent/DE602004019481D1/de not_active Expired - Lifetime
-
2010
- 2010-02-01 US US12/698,055 patent/US20100311813A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP1518928B1 (en) | 2009-02-18 |
| US20100311813A1 (en) | 2010-12-09 |
| EP1518928A1 (en) | 2005-03-30 |
| ATE423201T1 (de) | 2009-03-15 |
| DE602004019481D1 (de) | 2009-04-02 |
| ES2322583T3 (es) | 2009-06-23 |
| US20060009429A1 (en) | 2006-01-12 |
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Legal Events
| Date | Code | Title | Description |
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| FG | Grant, registration |