AR082995A1 - Profarmacos que comprenden un conjugado de conector de exendina - Google Patents
Profarmacos que comprenden un conjugado de conector de exendinaInfo
- Publication number
- AR082995A1 AR082995A1 ARP110103361A ARP110103361A AR082995A1 AR 082995 A1 AR082995 A1 AR 082995A1 AR P110103361 A ARP110103361 A AR P110103361A AR P110103361 A ARP110103361 A AR P110103361A AR 082995 A1 AR082995 A1 AR 082995A1
- Authority
- AR
- Argentina
- Prior art keywords
- exendin
- conjugate
- formula
- substituted
- moiety
- Prior art date
Links
Classifications
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- 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
- A61K47/62—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 a protein, peptide or polyamino acid
- A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K17/00—Carrier-bound or immobilised peptides; Preparation thereof
- C07K17/02—Peptides being immobilised on, or in, an organic carrier
- C07K17/08—Peptides being immobilised on, or in, an organic carrier the carrier being a synthetic polymer
-
- 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
-
- 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
-
- 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
- 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
- A61K47/69—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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
- A61K47/6903—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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being semi-solid, e.g. an ointment, a gel, a hydrogel or a solidifying gel
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- 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
- A61P3/08—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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Zoology (AREA)
- Child & Adolescent Psychology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente se refiere a un profármaco o una sal del mismo farmacéuticamente aceptable, que comprende un conjugado de exendina-conector D-L, en el que D representa un resto de exendina; y -L es un resto conector que no es biológicamente activo -L1 representado por la fórmula (1), en la que la línea de trazos indica la unión a uno de los grupos amino del resto de exendina formando un enlace amida. Se refiere además a composiciones farmacéuticas que comprenden dichos profármacos así como a su uso como un medicamento para tratar o prevenir enfermedades o trastornos que se pueden tratar mediante la exendina.Reivindicación 1: Un profármaco o una sal del mismo farmacéuticamente aceptable que comprende un conjugado de exendina-conector D-L, en el que D representa un resto de exendina; y -L es un resto conector que no es biológicamente activo -L1 representado por la fórmula (1), en la que la línea de trazos indica la unión a uno de los grupos amino de la exendina formando un enlace amida; R1 se selecciona de alquilo C1-4, R2, R2a se seleccionan independientemente del grupo que consiste en H y alquilo C1-4, en la que L1 está sustituido con un L2-Z y opcionalmente sustituido adicionalmente, con la condición de que los hidrógenos marcados con asteriscos en la fórmula (1) no se sustituyan por un sustituyente, y en la que L2 es un enlace químico sencillo o un espaciador; y Z es un hidrogel.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP10177327A EP2438930A1 (en) | 2010-09-17 | 2010-09-17 | Prodrugs comprising an exendin linker conjugate |
Publications (1)
Publication Number | Publication Date |
---|---|
AR082995A1 true AR082995A1 (es) | 2013-01-23 |
Family
ID=43446651
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP110103361A AR082995A1 (es) | 2010-09-17 | 2011-09-15 | Profarmacos que comprenden un conjugado de conector de exendina |
Country Status (29)
Country | Link |
---|---|
US (1) | US9133276B2 (es) |
EP (2) | EP2438930A1 (es) |
JP (1) | JP5932796B2 (es) |
KR (1) | KR20130106820A (es) |
CN (1) | CN103237561B (es) |
AR (1) | AR082995A1 (es) |
AU (1) | AU2011303823B2 (es) |
BR (1) | BR112013006340A2 (es) |
CA (1) | CA2811352C (es) |
CL (1) | CL2013000716A1 (es) |
CO (1) | CO6690765A2 (es) |
CY (1) | CY1122226T1 (es) |
DK (1) | DK2616102T3 (es) |
ES (1) | ES2733734T3 (es) |
HR (1) | HRP20191128T1 (es) |
HU (1) | HUE044079T2 (es) |
IL (1) | IL225127A (es) |
LT (1) | LT2616102T (es) |
MA (1) | MA34517B1 (es) |
MX (1) | MX348983B (es) |
MY (1) | MY158974A (es) |
NZ (1) | NZ608387A (es) |
PL (1) | PL2616102T3 (es) |
PT (1) | PT2616102T (es) |
RU (1) | RU2593774C2 (es) |
SG (1) | SG188197A1 (es) |
SI (1) | SI2616102T1 (es) |
UY (1) | UY33605A (es) |
WO (1) | WO2012035139A1 (es) |
Families Citing this family (32)
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CA2786794C (en) * | 2004-03-23 | 2017-09-12 | Complex Biosystems Gmbh | Aromatic polymeric cascade prodrug linker reagent |
SI2237799T1 (sl) * | 2008-02-01 | 2019-07-31 | Ascendis Pharma A/S | Predzdravilo, ki obsega samo-cepljiv linker |
CN102573913B (zh) * | 2009-07-31 | 2014-06-18 | 阿森迪斯药物股份有限公司 | 可生物降解的基于聚乙二醇的水不溶性水凝胶 |
JP5732053B2 (ja) | 2009-07-31 | 2015-06-10 | サノフィ−アベンティス・ドイチュラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング | 持続型インスリン組成物 |
EP2459228B1 (en) | 2009-07-31 | 2020-03-04 | Sanofi-Aventis Deutschland GmbH | Prodrugs comprising an insulin linker conjugate |
EP2438930A1 (en) | 2010-09-17 | 2012-04-11 | Sanofi-Aventis Deutschland GmbH | Prodrugs comprising an exendin linker conjugate |
US20150010634A1 (en) * | 2011-10-12 | 2015-01-08 | Ascendis Pharma Ophthamology Division A/S | Prevention and treatment of ocular conditions |
UA116217C2 (uk) | 2012-10-09 | 2018-02-26 | Санофі | Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону |
KR20150096684A (ko) | 2012-12-21 | 2015-08-25 | 사노피 | 엑센딘-4 유도체 |
US10626156B2 (en) | 2013-12-06 | 2020-04-21 | Jie Han | Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs |
WO2015086729A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/gip receptor agonists |
WO2015086730A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Non-acylated exendin-4 peptide analogues |
EP3080150B1 (en) | 2013-12-13 | 2018-08-01 | Sanofi | Exendin-4 peptide analogues as dual glp-1/gip receptor agonists |
EP3080149A1 (en) | 2013-12-13 | 2016-10-19 | Sanofi | Dual glp-1/glucagon receptor agonists |
CN104945499B (zh) * | 2014-03-31 | 2019-12-10 | 博瑞生物医药(苏州)股份有限公司 | 结构修饰的glp-1类似物及其制备方法 |
TW201625669A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 衍生自艾塞那肽-4(Exendin-4)之肽類雙重GLP-1/升糖素受體促效劑 |
TW201625668A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 作為胜肽性雙重glp-1/昇糖素受體激動劑之艾塞那肽-4衍生物 |
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US9932381B2 (en) | 2014-06-18 | 2018-04-03 | Sanofi | Exendin-4 derivatives as selective glucagon receptor agonists |
TWI748945B (zh) | 2015-03-13 | 2021-12-11 | 德商賽諾菲阿凡提斯德意志有限公司 | 第2型糖尿病病患治療 |
AR105319A1 (es) * | 2015-06-05 | 2017-09-27 | Sanofi Sa | Profármacos que comprenden un conjugado agonista dual de glp-1 / glucagón conector ácido hialurónico |
AR105284A1 (es) | 2015-07-10 | 2017-09-20 | Sanofi Sa | Derivados de exendina-4 como agonistas peptídicos duales específicos de los receptores de glp-1 / glucagón |
CN106554403B (zh) * | 2015-09-25 | 2021-08-31 | 博瑞生物医药(苏州)股份有限公司 | 艾塞那肽修饰物及其用途 |
BR112018017091A2 (pt) | 2016-03-01 | 2019-01-02 | Ascendis Pharma Bone Diseases As | profármacos de pth |
CN109789189B (zh) | 2016-09-29 | 2024-01-23 | 阿森迪斯药物骨疾病股份有限公司 | 控释pth化合物的剂量方案 |
US11759504B2 (en) | 2016-09-29 | 2023-09-19 | Ascendis Pharma Bone Diseases A/S | PTH compounds with low peak-to-trough ratios |
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