BRPI0500959A - uso farmacológico de inibidor da expressão da proteìna coativador 1 alfa do receptor ativado por proliferador do peroxisoma (pgc-1(alfa)) para o tratamento de diabetes mellitus, resistência à insulina e sìndrome metabólica, seu composto e sua composição farmacêuticos - Google Patents
uso farmacológico de inibidor da expressão da proteìna coativador 1 alfa do receptor ativado por proliferador do peroxisoma (pgc-1(alfa)) para o tratamento de diabetes mellitus, resistência à insulina e sìndrome metabólica, seu composto e sua composição farmacêuticosInfo
- Publication number
- BRPI0500959A BRPI0500959A BRPI0500959-6A BRPI0500959A BRPI0500959A BR PI0500959 A BRPI0500959 A BR PI0500959A BR PI0500959 A BRPI0500959 A BR PI0500959A BR PI0500959 A BRPI0500959 A BR PI0500959A
- Authority
- BR
- Brazil
- Prior art keywords
- alpha
- pgc
- diabetes mellitus
- activated receptor
- glucose levels
- Prior art date
Links
- 206010012601 diabetes mellitus Diseases 0.000 title abstract 5
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 230000000144 pharmacologic effect Effects 0.000 title abstract 3
- 208000031773 Insulin resistance syndrome Diseases 0.000 title abstract 2
- 208000001145 Metabolic Syndrome Diseases 0.000 title abstract 2
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 title abstract 2
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 title abstract 2
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title abstract 2
- 102000004169 proteins and genes Human genes 0.000 title abstract 2
- 108090000623 proteins and genes Proteins 0.000 title abstract 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 abstract 6
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 abstract 4
- 239000008103 glucose Substances 0.000 abstract 4
- 102000004877 Insulin Human genes 0.000 abstract 3
- 108090001061 Insulin Proteins 0.000 abstract 3
- 102000017946 PGC-1 Human genes 0.000 abstract 3
- 108700038399 PGC-1 Proteins 0.000 abstract 3
- 229940125396 insulin Drugs 0.000 abstract 3
- 239000008280 blood Substances 0.000 abstract 2
- 210000004369 blood Anatomy 0.000 abstract 2
- 229940079593 drug Drugs 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 208000011580 syndromic disease Diseases 0.000 abstract 2
- 108020004491 Antisense DNA Proteins 0.000 abstract 1
- 208000004930 Fatty Liver Diseases 0.000 abstract 1
- 206010022489 Insulin Resistance Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 108091034117 Oligonucleotide Proteins 0.000 abstract 1
- 238000010171 animal model Methods 0.000 abstract 1
- 239000003816 antisense DNA Substances 0.000 abstract 1
- 230000003081 coactivator Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 210000002966 serum Anatomy 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical & Material Sciences (AREA)
- Genetics & Genomics (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Biomedical Technology (AREA)
- General Health & Medical Sciences (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- General Engineering & Computer Science (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Diabetes (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Biophysics (AREA)
- Physics & Mathematics (AREA)
- Plant Pathology (AREA)
- Microbiology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
"USO FARMACOLóGICO DE INIBIDOR DA EXPRESSãO DA PROTEìNA COATIVADOR 1 ALFA DO RECEPTOR ATIVADO POR PROLIFERADOR DO PEROXISOMA (PGC-1<244>) PARA O TRATAMENTO DE DIABETES MELLITUS, RESISTêNCIA à INSULINA E SìNDROME METABóLICA, SEU COMPOSTO E SUA COMPOSIçãO FARMACêUTICOS". A presente invenção refere-se ao uso de um oligonucleotídeo de DNA antisense para a fita de RNA mensageiro para a proteína PGC-1<244>, útil como fármaco para tratamento de diabetes mellitus, resistência à insulina e síndrome metabólica. Mais especificamente, a presente invenção trata-se de um composto utilizado como fármaco, por via enteral ou parenteral, preferencialmente, com a propriedade de inibir a expressão da proteína Coativador 1 alfa do receptor ativado por proliferador do peroxisoma (PGC-1<244>). Levando à redução dos níveis sanguíneos de glicose. Trata-se, portanto, de um composto farmacológico que promove, em indivíduos diabéticos e resistentes à insulina, melhora dos níveis de glicose sérica, aumento da concentração de insulina plasmática e redução da resistência à insulina. A presente invenção apresenta um controle mais efetivo dos níveis de glicose e atua de forma benéfica sobre outras complicações associadas aos quadros de Diabetes e obesidade, como a esteatose hepática, segundo testes efetuados em modelos animais. Desta forma, a principal vantagem da presente invenção sobre similares já existentes no mercado é a efetividade com que controla níveis sanguíneos de glicose e o fato de atuar beneficamente em outras complicações que acompanham a doença.
Priority Applications (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| BRPI0500959-6A BRPI0500959A (pt) | 2005-03-23 | 2005-03-23 | uso farmacológico de inibidor da expressão da proteìna coativador 1 alfa do receptor ativado por proliferador do peroxisoma (pgc-1(alfa)) para o tratamento de diabetes mellitus, resistência à insulina e sìndrome metabólica, seu composto e sua composição farmacêuticos |
| MX2007011705A MX2007011705A (es) | 2005-03-23 | 2006-03-20 | Inhibidor del coactivador 1 alfa del receptor activado por el proliferador de peroxisoma. |
| CA002601855A CA2601855A1 (en) | 2005-03-23 | 2006-03-20 | Inhibitor of peroxisome proliferator-activated receptor alpha coactivator 1 |
| EP06721614A EP1879905A1 (en) | 2005-03-23 | 2006-03-20 | Inhibitor of peroxisome proliferator-activated receptor alpha coactivator 1 |
| JP2008502196A JP2008533178A (ja) | 2005-03-23 | 2006-03-20 | ペルオキシソーム増殖因子活性受容体αコアクチベーター１阻害剤 |
| PCT/BR2006/000055 WO2006099706A1 (en) | 2005-03-23 | 2006-03-20 | Inhibitor of peroxisome proliferator-activated receptor alpha coactivator 1 |
| US11/909,323 US20090029933A1 (en) | 2005-03-23 | 2006-03-20 | Inhibitor of peroxisome proliferator-activated receptor alpha coactivator 1 |
| CNA2006800147334A CN101166751A (zh) | 2005-03-23 | 2006-03-20 | 过氧化物酶体增殖物-活化的受体α辅激活物1的抑制剂 |
| KR1020077024342A KR20080005509A (ko) | 2005-03-23 | 2006-03-20 | 퍼옥시좀 증식제-활성화 수용체 알파 보조작용자 １의억제제 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| BRPI0500959-6A BRPI0500959A (pt) | 2005-03-23 | 2005-03-23 | uso farmacológico de inibidor da expressão da proteìna coativador 1 alfa do receptor ativado por proliferador do peroxisoma (pgc-1(alfa)) para o tratamento de diabetes mellitus, resistência à insulina e sìndrome metabólica, seu composto e sua composição farmacêuticos |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0500959A true BRPI0500959A (pt) | 2006-11-21 |
Family
ID=37023323
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0500959-6A BRPI0500959A (pt) | 2005-03-23 | 2005-03-23 | uso farmacológico de inibidor da expressão da proteìna coativador 1 alfa do receptor ativado por proliferador do peroxisoma (pgc-1(alfa)) para o tratamento de diabetes mellitus, resistência à insulina e sìndrome metabólica, seu composto e sua composição farmacêuticos |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20090029933A1 (pt) |
| EP (1) | EP1879905A1 (pt) |
| JP (1) | JP2008533178A (pt) |
| KR (1) | KR20080005509A (pt) |
| CN (1) | CN101166751A (pt) |
| BR (1) | BRPI0500959A (pt) |
| CA (1) | CA2601855A1 (pt) |
| MX (1) | MX2007011705A (pt) |
| WO (1) | WO2006099706A1 (pt) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2397889B1 (es) | 2011-03-25 | 2014-02-07 | Lipotec, S.A. | PÉPTIDOS MODULADORES DE PGC-1Alfa. |
| US9171343B1 (en) | 2012-09-11 | 2015-10-27 | Aseko, Inc. | Means and method for improved glycemic control for diabetic patients |
| US9897565B1 (en) | 2012-09-11 | 2018-02-20 | Aseko, Inc. | System and method for optimizing insulin dosages for diabetic subjects |
| US9898585B2 (en) | 2014-01-31 | 2018-02-20 | Aseko, Inc. | Method and system for insulin management |
| US9486580B2 (en) | 2014-01-31 | 2016-11-08 | Aseko, Inc. | Insulin management |
| US11081226B2 (en) | 2014-10-27 | 2021-08-03 | Aseko, Inc. | Method and controller for administering recommended insulin dosages to a patient |
| AU2015339576B2 (en) | 2014-10-27 | 2020-02-06 | Glytec, Llc | Subcutaneous outpatient management |
| WO2017031440A1 (en) | 2015-08-20 | 2017-02-23 | Aseko, Inc. | Diabetes management therapy advisor |
| KR101980576B1 (ko) | 2017-07-06 | 2019-05-22 | 충남대학교산학협력단 | PGC-1α를 포함하는 제2형 당뇨병 진단용 바이오마커 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1525323B1 (en) * | 2001-11-09 | 2015-01-21 | Dana-Farber Cancer Institute, Inc. | Pgc-1beta, a novel pgc-1 homologue and uses therefor |
-
2005
- 2005-03-23 BR BRPI0500959-6A patent/BRPI0500959A/pt not_active Application Discontinuation
-
2006
- 2006-03-20 CN CNA2006800147334A patent/CN101166751A/zh active Pending
- 2006-03-20 US US11/909,323 patent/US20090029933A1/en not_active Abandoned
- 2006-03-20 KR KR1020077024342A patent/KR20080005509A/ko not_active Withdrawn
- 2006-03-20 JP JP2008502196A patent/JP2008533178A/ja active Pending
- 2006-03-20 EP EP06721614A patent/EP1879905A1/en not_active Withdrawn
- 2006-03-20 MX MX2007011705A patent/MX2007011705A/es not_active Application Discontinuation
- 2006-03-20 WO PCT/BR2006/000055 patent/WO2006099706A1/en not_active Ceased
- 2006-03-20 CA CA002601855A patent/CA2601855A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP1879905A1 (en) | 2008-01-23 |
| KR20080005509A (ko) | 2008-01-14 |
| US20090029933A1 (en) | 2009-01-29 |
| CN101166751A (zh) | 2008-04-23 |
| JP2008533178A (ja) | 2008-08-21 |
| WO2006099706A1 (en) | 2006-09-28 |
| MX2007011705A (es) | 2007-12-12 |
| CA2601855A1 (en) | 2006-09-28 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B15K | Others concerning applications: alteration of classification |
Ipc: C12N 15/63 (2010.01), C12N 15/11 (2010.01), A61K 3 |
|
| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B07E | Notice of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
| B07A | Technical examination (opinion): publication of technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B15K | Others concerning applications: alteration of classification |
Ipc: C12N 15/11 (2006.01), C12N 15/63 (2006.01), A61K 3 |
|
| B09B | Patent application refused [chapter 9.2 patent gazette] | ||
| B12B | Appeal: appeal against refusal |