MX2009008241A - Co-agonistas de receptor de glucagon/glp-1. - Google Patents
Co-agonistas de receptor de glucagon/glp-1.Info
- Publication number
- MX2009008241A MX2009008241A MX2009008241A MX2009008241A MX2009008241A MX 2009008241 A MX2009008241 A MX 2009008241A MX 2009008241 A MX2009008241 A MX 2009008241A MX 2009008241 A MX2009008241 A MX 2009008241A MX 2009008241 A MX2009008241 A MX 2009008241A
- Authority
- MX
- Mexico
- Prior art keywords
- glucagon
- seq
- receptor
- peptides
- glp
- Prior art date
Links
- MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 title abstract 5
- 102000051325 Glucagon Human genes 0.000 title abstract 4
- 108010063919 Glucagon Receptors Proteins 0.000 title abstract 3
- 229960004666 glucagon Drugs 0.000 title abstract 3
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 title abstract 2
- 102100032882 Glucagon-like peptide 1 receptor Human genes 0.000 title abstract 2
- 239000000556 agonist Substances 0.000 title abstract 2
- 102000004196 processed proteins & peptides Human genes 0.000 abstract 3
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 3
- 108060003199 Glucagon Proteins 0.000 abstract 2
- 230000004048 modification Effects 0.000 abstract 2
- 238000012986 modification Methods 0.000 abstract 2
- 238000006467 substitution reaction Methods 0.000 abstract 2
- 101800005309 Carboxy-terminal peptide Proteins 0.000 abstract 1
- 102100040890 Glucagon receptor Human genes 0.000 abstract 1
- 125000003368 amide group Chemical group 0.000 abstract 1
- 150000001413 amino acids Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical class [H]OC(*)=O 0.000 abstract 1
- 150000001732 carboxylic acid derivatives Chemical group 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000001747 exhibiting effect Effects 0.000 abstract 1
- 230000006320 pegylation Effects 0.000 abstract 1
- 229920001184 polypeptide Polymers 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/605—Glucagons
-
- 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
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/26—Glucagons
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
-
- 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
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
- C07K2317/52—Constant or Fc region; Isotype
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2319/00—Fusion polypeptide
- C07K2319/30—Non-immunoglobulin-derived peptide or protein having an immunoglobulin constant or Fc region, or a fragment thereof, attached thereto
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Endocrinology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Diabetes (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Toxicology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Emergency Medicine (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
Se divulgan péptidos de glucagón modificados que tienen potencia aumentada en el receptor de glucagón con relación al glucagón nativo. La modificación adicional de los péptidos de glucagón al formar los puentes de lactama o la sustitución del ácido carboxílico terminal con un grupo amida produce péptidos que exhiben actividad co-agonista de receptor de glucagón/GLP-1. La solubilidad y estabilidad de estos análogos de glucagón de alta potencia se puede mejorar adicionalmente mediante la modificación de los polipéptidos mediante pegilación, sustitución de aminoácidos carboxi terminales o la adición de un péptido carboxi terminal seleccionado del grupo que consiste de SEQ ID NO:26 (GPSSGAPPPS), SEQ ID NO:27 (K-RNRNNIA) y SEQ ID NO:28 (KRNR).
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US89008707P | 2007-02-15 | 2007-02-15 | |
US93856507P | 2007-05-17 | 2007-05-17 | |
PCT/US2008/053857 WO2008101017A2 (en) | 2007-02-15 | 2008-02-13 | Glucagon/glp-1 receptor co-agonists |
Publications (1)
Publication Number | Publication Date |
---|---|
MX2009008241A true MX2009008241A (es) | 2009-10-08 |
Family
ID=39690775
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2009008241A MX2009008241A (es) | 2007-02-15 | 2008-02-13 | Co-agonistas de receptor de glucagon/glp-1. |
Country Status (29)
Country | Link |
---|---|
US (3) | US8454971B2 (es) |
EP (2) | EP2111414B1 (es) |
JP (2) | JP6017754B2 (es) |
KR (2) | KR20090119876A (es) |
CN (1) | CN101790538B (es) |
AR (2) | AR065349A1 (es) |
AU (1) | AU2008216265B2 (es) |
BR (1) | BRPI0807728A2 (es) |
CA (1) | CA2677932A1 (es) |
CL (1) | CL2008000479A1 (es) |
CR (1) | CR11028A (es) |
DO (1) | DOP2009000194A (es) |
EA (1) | EA017849B1 (es) |
EC (1) | ECSP099622A (es) |
GE (1) | GEP20135944B (es) |
GT (1) | GT200900229A (es) |
HK (1) | HK1135993A1 (es) |
HN (1) | HN2009001593A (es) |
IL (1) | IL200396A (es) |
MA (1) | MA31242B1 (es) |
MX (1) | MX2009008241A (es) |
NI (1) | NI200900158A (es) |
NZ (1) | NZ578948A (es) |
PA (1) | PA8769301A1 (es) |
PE (2) | PE20090108A1 (es) |
TN (1) | TN2009000313A1 (es) |
TW (1) | TWI547499B (es) |
WO (1) | WO2008101017A2 (es) |
ZA (1) | ZA200905521B (es) |
Families Citing this family (200)
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---|---|---|---|---|
US9006175B2 (en) | 1999-06-29 | 2015-04-14 | Mannkind Corporation | Potentiation of glucose elimination |
DE60318938T2 (de) | 2002-03-20 | 2009-01-22 | Mannkind Corp., Valencia | Inhalationsgerät |
ES2385934T3 (es) | 2004-08-20 | 2012-08-03 | Mannkind Corporation | Catálisis de la síntesis de dicetopiperazina. |
EP2314298B1 (en) | 2004-08-23 | 2015-05-27 | MannKind Corporation | Microparticles comprising diketopiperazine salts for drug delivery |
KR20160022404A (ko) | 2005-09-14 | 2016-02-29 | 맨카인드 코포레이션 | 활성제에 대한 결정질 미립자 표면의 친화력의 증가를 기반으로 하는 약물 제제화의 방법 |
WO2007056362A2 (en) | 2005-11-07 | 2007-05-18 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting physiological solubility and stability |
MX2008010721A (es) | 2006-02-22 | 2008-09-01 | Mannkind Corp | Un metodo para mejorar las propiedades farmaceuticas de microparticulas que contienen dicetopiperazina y un agente activo. |
EP2124974B1 (en) * | 2007-01-05 | 2017-03-15 | Indiana University Research and Technology Corporation | Glucagon analogs exhibiting enhanced solubility in physiological ph buffers |
EP2111414B1 (en) | 2007-02-15 | 2014-07-02 | Indiana University Research and Technology Corporation | Glucagon/glp-1 receptor co-agonists |
ATE520714T1 (de) | 2007-06-15 | 2011-09-15 | Zealand Pharma As | Glucagonanaloga |
WO2009055740A2 (en) * | 2007-10-24 | 2009-04-30 | Mannkind Corporation | Method of preventing adverse effects by glp-1 |
ES2509883T3 (es) * | 2007-10-30 | 2014-10-20 | Indiana University Research And Technology Corporation | Antagonistas de glucagón |
WO2009058734A1 (en) * | 2007-10-30 | 2009-05-07 | Indiana University Research And Technology Corporation | Compounds exhibiting glucagon antagonist and glp-1 agonist activity |
WO2009099763A1 (en) * | 2008-01-30 | 2009-08-13 | Indiana University Research And Technology Corporation | Ester-based peptide prodrugs |
US8485180B2 (en) | 2008-06-13 | 2013-07-16 | Mannkind Corporation | Dry powder drug delivery system |
EP3281663B8 (en) | 2008-06-13 | 2022-09-21 | MannKind Corporation | Breath powered dry powder inhaler for drug delivery |
US9062124B2 (en) | 2008-06-17 | 2015-06-23 | Indiana University Research And Technology Corporation | GIP-based mixed agonists for treatment of metabolic disorders and obesity |
EA019203B9 (ru) * | 2008-06-17 | 2014-03-31 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Коагонисты глюкагонового рецептора/glp-1-рецептора |
KR20110039230A (ko) * | 2008-06-17 | 2011-04-15 | 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 | 생리학적 pH 완충액에서 강화된 용해도 및 안정성을 나타내는 글루카곤 유사체 |
AU2013205144B2 (en) * | 2008-06-17 | 2015-07-16 | Indiana University Research And Technology Corporation | GIP-based mixed agonists for treatment of metabolic disorders and obesity |
MX2010014240A (es) | 2008-06-20 | 2011-03-25 | Mankind Corp | Un metodo y aparato interactivo para perfilar en tiempo real esfuerzos de inhalacion. |
TWI614024B (zh) | 2008-08-11 | 2018-02-11 | 曼凱公司 | 超快起作用胰島素之用途 |
JO2870B1 (en) | 2008-11-13 | 2015-03-15 | ميرك شارب اند دوهم كورب | Amino Tetra Hydro Pirans as Inhibitors of Peptide Dipeptide IV for the Treatment or Prevention of Diabetes |
US8680049B2 (en) * | 2008-12-15 | 2014-03-25 | Zealand Pharma A/S | Glucagon analogues |
EA020537B1 (ru) * | 2008-12-15 | 2014-11-28 | Зилэнд Фарма А/С | Аналоги глюкагона |
AU2008365556A1 (en) * | 2008-12-15 | 2011-07-21 | Zealand Pharma A/S | Glucagon analogues |
EP2370461B1 (en) * | 2008-12-15 | 2013-10-02 | Zealand Pharma A/S | Glucagon analogues |
CN102300580A (zh) * | 2008-12-19 | 2011-12-28 | 印第安纳大学研究及科技有限公司 | 二肽连接的药剂 |
TWI489992B (zh) * | 2008-12-19 | 2015-07-01 | 印地安那大學研究及技術公司 | 醯胺系胰高血糖素超級家族之胜肽前驅藥物 |
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CA2754595C (en) | 2009-03-11 | 2017-06-27 | Mannkind Corporation | Apparatus, system and method for measuring resistance of an inhaler |
US8551528B2 (en) | 2009-06-12 | 2013-10-08 | Mannkind Corporation | Diketopiperazine microparticles with defined specific surface areas |
MX2011013625A (es) | 2009-06-16 | 2012-01-20 | Univ Indiana Res & Tech Corp | Compuestos glucagon activo de receptor de gip. |
AU2010272944B2 (en) * | 2009-07-13 | 2015-11-19 | Zealand Pharma A/S | Acylated glucagon analogues |
CN101993485B (zh) * | 2009-08-20 | 2013-04-17 | 重庆富进生物医药有限公司 | 促胰岛素分泌肽类似物同源二聚体及其用途 |
CN102595897A (zh) | 2009-09-02 | 2012-07-18 | 默沙东公司 | 作为用于糖尿病的治疗或预防的二肽基肽酶-iv抑制剂的氨基四氢吡喃 |
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JP5969461B2 (ja) | 2010-04-27 | 2016-08-17 | ジーランド ファーマ アクティーゼルスカブ | Glp−1受容体作動薬とガストリンとのペプチド複合体及びその使用 |
ES2661228T3 (es) | 2010-05-13 | 2018-03-28 | Indiana University Research And Technology Corporation | Péptidos de la superfamilia de glucagón que muestran actividad de receptor nuclear de hormona |
EP2568993A4 (en) | 2010-05-13 | 2014-02-19 | Univ Indiana Res & Tech Corp | GLUCAGON SUPERFAMILY PEPTIDES EXPRESSING G PROTEIN-COUPLED RECEPTOR ACTIVITY |
EP2571876B1 (en) | 2010-05-21 | 2016-09-07 | Merck Sharp & Dohme Corp. | Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes |
US8933024B2 (en) | 2010-06-18 | 2015-01-13 | Sanofi | Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases |
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