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WO2008058353A2 - Combinaison médicamenteuse 'telmisartan + metformine' utilisée pour lutter contre les maladies cardiovasculaires - Google Patents

Combinaison médicamenteuse 'telmisartan + metformine' utilisée pour lutter contre les maladies cardiovasculaires Download PDF

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Publication number
WO2008058353A2
WO2008058353A2 PCT/BR2007/000344 BR2007000344W WO2008058353A2 WO 2008058353 A2 WO2008058353 A2 WO 2008058353A2 BR 2007000344 W BR2007000344 W BR 2007000344W WO 2008058353 A2 WO2008058353 A2 WO 2008058353A2
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WO
WIPO (PCT)
Prior art keywords
insulin
metformin
telmisartana
medicament
picture
Prior art date
Application number
PCT/BR2007/000344
Other languages
English (en)
Other versions
WO2008058353A3 (fr
Inventor
Walter Santos Junior
Original Assignee
Walter Santos Junior
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Walter Santos Junior filed Critical Walter Santos Junior
Publication of WO2008058353A2 publication Critical patent/WO2008058353A2/fr
Publication of WO2008058353A3 publication Critical patent/WO2008058353A3/fr

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/155Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

Definitions

  • BJORNTORP E COLS that firstly related the relation between central obesity with augmented risk of diabetes and cardiovascular disease in both sexes.
  • the relation between the degree of obesity and the incidence of cardiovascular disease was established in 1983 when the evolution results of 5.209 men and women who took part in Framingham Study were published.
  • the insulin resistance can be defined whit a condition in which occurs lesser utilization of glucose in reply to the action of insulin in the peripheral tissues. Under such condition, the lesser consumption of glucose causes its serum levels to rise, entailing a larger stimulus onto the production of insulin and hyperinsulinemia.
  • the visceral abdominal fat shoes itself as metabolically very active tissue, presenting high rate of renewal. Concerning the lip ⁇ lise, the visceral fat tissue gets to the liver by the portal system.
  • a larger hepatic concentration of free fatty acids has, as consequences, the reduction in capitation and degradation of insulin and a raise in the hepatic production of lipoproteins of very low density (VLDL) rich in tryglicerides.
  • VLDL very low density
  • VLDL low density lipoproteins
  • HDL high density lipoproteins
  • the free fatty acids and tryglicerides in higher quantities in the systemic circulation rearch the skeleton muscle and reduce, the capitation of glucose induced by the insulin, favoring the elevation of glucose serum levels.
  • the larger quantity of free fatty acids and the most elevated glycemia estimulate the insulin production.
  • pancreas The chronic exposure of pancreas to the free fatty acids by means of a phenomenon known as lipotoxicity, results in the reduction of the insulin pancreatic secretion, which may cause the appearing of type 2 diabetes.
  • the hyperinsulinemia acts augmenthing the activity sympathetic nervous system, generating a state of hyperadrenergico which promotes vasoconstriction in the muscle structure, contributing to the elevation of the arterial pressure levels.
  • either the insulin or the augment of sympathetic activity can estimulate the sodio renal reabsorption which in turn, also contributes for the elevation of the arterial pressure.
  • the metformin ( drawing 01 picture 01) is a compound of the biguanides group which augments the sensitivity of insulin in the peripheral tissues, mainly the liver.
  • the reduction of glycemia provoked by metformin is specially due to the diminution of glucose hepatic production. It is not bound the weight augment being able even to determine the diminution from two to three kilograms during the first six months of treatment. It reduces the tryglicerides levels from 10 to 15% and also from the inhibitor a-1 from activator of plasminogen.
  • the metformina ( drawing 01 picture 01) was the only medication that determined significant diminution of incidence of cardiovascular complications in obese patients, myocardial infarction and death.
  • Congestive cardiac insufficiency chronic hepatic disease ( transaminases > 3 times the superior limit of normality) and alcohol abusive use.
  • the medicament must be interrupted during the surgical, radiographic procedures with use of contrast and serious medical intervention.
  • AT1 when stimulated unschains all those angiotensina undisereable actions such as: vasoconstriction, hypertrophy of the vascular and miocardial wall and deterioration of the glomerular function, among others.
  • the telmisartana ( picture 01 figure 02) is the blocker AT1 used nowadays also with beneficial effects on the vascular tonus and cellular growth.
  • the diabetic nephropathy exerts protector effect like the IECAS and other ATI
  • telmisartana picture 01 figure 02
  • metformin picture 01 figure 01

Landscapes

  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne la combinaison médicamenteuse 'telmisartan + metformine' utilisée pour lutter contre les maladies cardiovasculaires. Cette combinaison de deux médicaments est utilisée pour lutter contre les maladies cardiaques qui sont la principale cause de mortalité dans notre pays, une nette corrélation étant établie entre la prise de poids et l'excès de poids et un risque de maladies cardiaques. L'excès de poids prédispose à ces maladies en raison des anomalies du métabolisme des lipides, du glucose et de la pression artérielle. La résistance à l'insuline/l'hyperinsulinémie semble être un facteur de risque indépendant d'autres facteurs de risque associés, tels que l'obésité, l'hyperlipidémie et l'hypertension, que ce soit chez l'homme ou chez la femme. L'insuline et les facteurs de croissance similaires à l'insuline stimulent l'activité des cellules des muscles lisses et sont impliqués dans l'athérogénèse et même dans la resténose suivant une réparation coronarienne par angioplastie. D'autres effets de l'insuline sont liés à des mécanismes qui contribuent au développement d'une hypertension ou d'une dyslipidémie.
PCT/BR2007/000344 2006-11-16 2007-11-14 Combinaison médicamenteuse 'telmisartan + metformine' utilisée pour lutter contre les maladies cardiovasculaires WO2008058353A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
BRMU8602970-3 2006-11-16
BRMU8602970-3U BRMU8602970U (pt) 2006-11-16 2006-11-16 medicamento "telmisartam + metformina" em forma combinada para doenças cardiovasculares

Publications (2)

Publication Number Publication Date
WO2008058353A2 true WO2008058353A2 (fr) 2008-05-22
WO2008058353A3 WO2008058353A3 (fr) 2009-04-02

Family

ID=39402021

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/BR2007/000344 WO2008058353A2 (fr) 2006-11-16 2007-11-14 Combinaison médicamenteuse 'telmisartan + metformine' utilisée pour lutter contre les maladies cardiovasculaires

Country Status (2)

Country Link
BR (1) BRMU8602970U (fr)
WO (1) WO2008058353A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112618526A (zh) * 2021-01-11 2021-04-09 重庆康刻尔制药股份有限公司 一种治疗糖尿病合并高血压的复方制剂及其制备方法

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60110066T2 (de) * 2000-06-16 2006-02-02 Smithkline Beecham P.L.C., Brentford Piperidine zur verwendung als orexinrezeptorantagonisten

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112618526A (zh) * 2021-01-11 2021-04-09 重庆康刻尔制药股份有限公司 一种治疗糖尿病合并高血压的复方制剂及其制备方法

Also Published As

Publication number Publication date
BRMU8602970U (pt) 2008-09-30
WO2008058353A3 (fr) 2009-04-02

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