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DK1971329T3 - Triazin-derivater til anvendelse i en cicatriciel behandling - Google Patents

Triazin-derivater til anvendelse i en cicatriciel behandling Download PDF

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DK1971329T3
DK1971329T3 DK06829704.3T DK06829704T DK1971329T3 DK 1971329 T3 DK1971329 T3 DK 1971329T3 DK 06829704 T DK06829704 T DK 06829704T DK 1971329 T3 DK1971329 T3 DK 1971329T3
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alkoxy
alkyl
aryl
optionally substituted
halogen
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Gérard Moinet
Daniel Cravo
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Poxel Sas
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    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
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    • A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
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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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • 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
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K9/00—Medicinal preparations characterised by special physical form
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    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
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Claims (16)

1. Triazin-derivater af den generelle formel (I) nedenfor:
i hvilken: RI, R2, R3 og R4 er uafhængigt valgt fra de følgende grupper: -H, - (Cl-C20)alkyl eventuelt substitueret med halogen, (Cl-C5)alkyl, (Cl-C5)alkoxy eller (C3-C8)cykloalkyl, - (C2-C20)alkenyl eventuelt substitueret med halogen, (Cl-C5)alkyl eller (Cl-C5)-alkoxy - (C2-C20)alkynyl eventuelt substitueret med halogen, (Cl-C5)alkyl eller (Cl-C5)-alkoxy - (C3-C8)cykloalkyl eventuelt substitueret med (Cl-C5)alkyl eller (Cl-C5)alkoxy - hetero(C3-C8)cykloalkyl indeholdende ét eller flere heteroatomer valgt fra N, O og S og eventuelt substitueret med (Cl-C5)alkyl eller (Cl-C5)alkoxy - (C6-C14)aryl(Cl-C20)alkyl eventuelt substitueret med amino, hydroxyl, thio, halogen, (Cl-C5)alkyl, (Cl-C5)alkoxy, (Cl-C5)alkylthio, (Cl-C5)alkylamino, (C6-C14)aryloxy, (C6-C14)aryl(Cl-C5)alkoxy, cyano, trifluormethyl, carboxyl, carboxymethyl eller carboxyethyl, - (C6-C14)aryl eventuelt substitueret med amino, hydroxyl, thio, halogen, (Cl-C5)-alkyl, (Cl-C5)alkoxy, (Cl-C5)alkylthio, (Cl- C5)alkylamino, (C6-C14)aryloxy, (C6-C14)aryl(Cl-C5)alkoxy, cyano, trifluormethyl, carboxyl, carboxymethyl eller carboxyethyl, - (Cl-C13)heteroaryl indeholdende ét eller flere heteroatomer valgt fra N, O og S og eventuelt substitueret med amino, hydroxyl, thio, halogen, (Cl-C5)alkyl, (Cl-C5)alkoxy, (Cl-C5)alkylthio, (Cl-C5)alkylamino, (C6-C14)aryloxy, (C6-C14)aryl(Cl-C5)alkoxy, cyano, trifluormethyl, carboxyl, carboxymethyl eller carboxyethyl, hvor RI og R2, på den ene side, og R3 og R4, på den anden side, eventuelt danner med nitrogenatomet en n-leddet ring (n mellem 3 og 8), der eventuelt indeholder ét eller flere heteroatomer valgt fra N, O og S og eventuelt er substitueret med én eller flere af de følgende grupper: amino, hydroxyl, thio, halogen, (Cl-C5)alkyl, (Cl-C5)alkoxy, (Cl-C5)alkylthio, (Cl-C5)alkylamino, (C6-C14)aryloxy, (C6-C14)aryl(Cl-C5)alkoxy, cyano, trifluormethyl, carboxyl, carboxymethyl eller carboxyethyl, R5 og R6 er uafhængigt valgt fra de følgende grupper: - H, - (Cl-C20)alkyl eventuelt substitueret med amino, hydroxyl, thio, halogen, (Cl-C5)alkyl, (Cl-C5)alkoxy, (Cl-C5)alkylthio, (Cl-C5)alkylamino, (C6-C14)aryloxy, (C6-C14)aryl(Cl-C5)alkoxy, cyano, trifluormethyl, carboxyl, carboxymethyl eller carboxyethyl, - (C2-C20)alkenyl eventuelt substitueret med amino, hydroxyl, thio, halogen, (Cl-C5)alkyl, (Cl-C5)alkoxy, (Cl-C5)alkylthio, (Cl-C5)alkylamino, (C6-C14)aryloxy, (C6-C14)aryl(Cl-C5)alkoxy, cyano, trifluormethyl, carboxyl, carboxymethyl eller carboxyethyl, - (C2-C20)alkynyl eventuelt substitueret med amino, hydroxyl, thio, halogen, (Cl-C5)alkyl, (Cl-C5)alkoxy, (Cl-C5)alkylthio, (Cl-C5)alkylamino, (C6-C14)aryloxy, (C6-C14)aryl(Cl-C5)alkoxy, cyano, trifluormethyl, carboxyl, carboxymethyl eller carboxyethyl, - (C3-C8)cykloalkyl eventuelt substitueret med amino, hydroxyl, thio, halogen, (Cl-C5)alkyl, (Cl-C5)alkoxy, (Cl-C5)alkylthio, (Cl- C5)alkylamino, (C6-C14)aryloxy, (C6-C14)aryl(Cl-C5)alkoxy, cyano, trifluormethyl, carboxyl, carboxymethyl eller carboxyethyl, - hetero(C3-C8)cykloalkyl indeholdende ét eller flere heteroatomer valgt fra N, O og S og eventuelt substitueret med amino, hydroxyl, thio, halogen, (Cl-C5)alkyl, (Cl-C5)alkoxy, (Cl-C5)alkylthio, (Cl-C5)alkylamino, (C6-C14)aryloxy, (C6-C14)aryl(Cl-C5)alkoxy, cyano, trifluormethyl, carboxyl, carboxymethyl eller carboxyethyl, - (C6-C14)aryl eventuelt substitueret med amino, hydroxyl, thio, halogen, (Cl-C5)alkyl, (Cl-C5)alkoxy, (Cl-C5)alkylthio, (Cl-C5)alkylamino, (C6-C14)aryloxy, (C6-C14)aryl(Cl-C5)alkoxy, cyano, trifluormethyl, carboxyl, carboxymethyl eller carboxyethyl, - (Cl-C13)heteroaryl indeholdende ét eller flere heteroatomer valgt fra N, O og S og eventuelt substitueret med amino, hydroxyl, thio, halogen, (Cl-C5)alkyl, (Cl-C5)alkoxy, (Cl-C5)alkylthio, (Cl-C5)alkylamino, (C6-C14)aryloxy, (C6-C14)aryl(Cl-C5)alkoxy, cyano, trifluormethyl, carboxyl, carboxymethyl eller carboxyethyl, - (C6-C14)aryl(Cl-C5)alkyl eventuelt substitueret med amino, hydroxyl, thio, halogen, (Cl-C5)alkyl, (Cl-C5)alkoxy, (Cl-C5)alkylthio, (Cl-C5)alkylamino, (C6-C14)aryloxy, (C6-C14)aryl(Cl-C5)alkoxy, cyano, trifluormethyl, carboxyl, carboxymethyl eller carboxyethyl, - hvor R5 og R6 eventuelt danner med kulstofatomet, til hvilket de er fastgjort, en m-leddet ring (m mellem 3 og 8), der eventuelt indeholder ét eller flere heteroatomer valgt fra N, O og S og er eventuelt substitueret med amino, hydroxyl, thio, halogen, (Cl-C5)alkyl, (Cl-C5)alkoxy, (Cl-C5)alkylthio, (Cl-C5)-alkylamino, (C6-C14)aryloxy, (C6-C14)aryl(Cl-C5)alkoxy, cyano, trifluormethyl, carboxyl, carboxymethyl eller carboxyethyl, eller eventuelt danner med kulstofatomet en C10-C30 polycyklisk enhed eventuelt substitueret med amino, hydroxyl, thio, halogen, (Cl-C5)alkyl, (Cl-C5)alkoxy, (Cl-C5)alkylthio, (Cl-C5)alkylamino, (C6-C14)aryloxy, (C6-C14)aryl(Cl-C5)alkoxy, cyano, trifluormethyl, carboxyl, carboxymethyl eller carboxyethyl, hvor R5 og R6 sammen også eventuelt repræsenterer gruppen =0 eller =S, nitrogenatomet af en heterocykloalkyl- eller heteroarylgruppe eventuelt substitueret med en (Cl-C5)alkyl-, (C3-C8)cykloalkyl-, (C6-C14)aryl-, (C6-C14)aryl(Cl-C5)alkyl- eller (Cl-C6)acylgruppe, og også de racemiske former, tautomerer, enantiomerer, diastereoisomerer, epimererog polymorfer, og blandinger deraf, og de farmaceutisk acceptable salte deraf, til anvendelse i en cicatriciel behandling.
2. Triazin-derivater til anvendelse ifølge krav 1, hvor R5 er hydrogen.
3. Triazin-derivater til anvendelse ifølge kravene 1 og 2, hvor R5 og R6 er uafhængigt valgt fra H og (Cl-C20)alkylgrupper eventuelt substitueret med amino, hydroxyl, thio, halogen, (Cl-C5)alkyl, (Cl-C5)alkoxy, (Cl-C5)alkylthio, (Cl-C5)alkylamino, (C6-C14)aryloxy, (C6-C14)aryl(Cl-C5)alkoxy, cyano, trifluormethyl, carboxyl, carboxymethyl eller carboxyethyl.
4. Triazin-derivater til anvendelse ifølge et hvilket som helst af de foregående krav, hvor RI, R2, R3 og R4 er uafhængigt valgt fra H og (Cl-C20)alkylgrupper eventuelt substitueret med halogen, (Cl-C5)alkyl, (Cl-C5)alkoxy eller (C3-C8)cykloalkyl.
5. Triazin-derivater til anvendelse ifølge et hvilket som helst af de foregående krav, hvor RI og R2 er en methylgruppe og R3 og R4 repræsenterer et hydrogen.
6. Triazin-derivater til anvendelse ifølge et hvilket som helst af de foregående krav, til anvendelse i en cicatriciel behandling af sårene hos diabetikere.
7. Triazin-derivater til anvendelse ifølge et hvilket som helst af de foregående krav, kendetegnet ved at forbindelsen ifølge formel (I) er 2-amino-3,6-dihydro-4-dimethylamino-6-methyl-l,3,5-triazin.
8. Triazin-derivater til anvendelse ifølge et hvilket som helst af de foregående krav, kendetegnet ved at forbindelsen ifølge formel (I) er (-)-2-amino-3,6-dihydro-4-dimethylamino-6-methyl-l,3,5-triazin.
9. Triazin-derivater til anvendelse ifølge et hvilket som helst af kravene 1 til 8, kendetegnet ved at forbindelsen ifølge formel (I) anvendt er (+)-2-amino-3,6-dihydro-4-dimethylamino-6-methyl-l,3,5-triazin.
10. Triazin-derivater til anvendelse ifølge et hvilket som helst af de foregående krav, hvor forbindelsen ifølge formel (I) er i form af et hydrochlorid.
11. Triazin-derivater til anvendelse ifølge et hvilket som helst af de foregående krav, kendetegnet ved at medikamentet er i en farmaceutisk form til lokal anvendelse.
12. Triazin-derivater til anvendelse ifølge et hvilket som helst af de foregående krav, kendetegnet ved at medikamentet indeholder fra 0,02 til 2 vægtprocent af forbindelsen ifølge formel (I) eller af et farmaceutisk acceptabelt salt deraf og en egnet excipiens.
13. Triazin-derivater til anvendelse ifølge et hvilket som helst af de foregående krav, kendetegnet ved at forbindelsen ifølge formel (I) eller det farmaceutisk acceptable salt deraf er kombineret med ét eller flere andre antibiotika, antifungale eller antivirale virksomme stoffer.
14. Farmaceutisk sammensætning til topikal anvendelse i en cicatriciel behandling, omfattende, som virksomt stof, en terapeutisk effektiv mængde af en forbindelse ifølge generel formel (I) som defineret i et hvilket som helst af kravene 1 til 10 eller et farmaceutisk acceptable salt deraf i et egnet vehikel.
15. Sammensætning til anvendelse ifølge krav 14, kendetegnet ved at den indeholder én eller flere andre virksomme stoffer.
16. Sammensætning til anvendelse ifølge krav 14 eller 15, kendetegnet ved at den indeholder fra 0,02 til 2 vægtprocent af forbindelsen ifølge formel (I) eller af det farmaceutisk acceptable salt deraf.
DK06829704.3T 2006-01-13 2006-12-18 Triazin-derivater til anvendelse i en cicatriciel behandling DK1971329T3 (da)

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Application Number Priority Date Filing Date Title
FR0600347A FR2896161B1 (fr) 2006-01-13 2006-01-13 Utilisation de derives de triazines pour fabriquer un medicament ayant un effet cicatrisant ou angiogenique.
PCT/EP2006/012183 WO2007079915A2 (en) 2006-01-13 2006-12-18 Use of triazine derivatives for the manufacture of a medicament having a cicatrising or angiogenic effect

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JP (1) JP2009523140A (da)
KR (1) KR101482686B1 (da)
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FR2948027A1 (fr) * 2009-07-17 2011-01-21 Merck Sante Sas Derives amines de dihydro-1,3,5-triazine pour leur utilisation dans le traitement des maladies associees a une ischemie et/ou une reperfusion
KR20200102982A (ko) 2017-10-02 2020-09-01 폭셀 보존된 박출률을 갖는 심부전의 치료 방법
SG11202007172YA (en) 2018-06-06 2020-08-28 Metavant Sciences Gmbh Methods of treating subjects having diabetes with chronic kidney disease
KR20210003786A (ko) 2018-06-14 2021-01-12 폭셀 당뇨병의 치료에서 사용하기 위한 트리아진 유도체를 포함하는 필름 코팅정
EP4014962A1 (de) * 2020-12-16 2022-06-22 Novigo GmbH & Co. KG Zusammensetzung mit osmotisch wirksamer substanz und verwendung der zusammensetzung
FR3149774B1 (fr) * 2024-01-11 2025-06-20 Fabre Pierre Dermo Cosmetique 5,6,5’,6’-tétraphényl-3,3’-(1,4-phénylène)-bis[1,2,4]triazine pour améliorer l’aspect des cicatrices et/ou réduire les marques cicatricielles

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US6150362A (en) * 1997-12-12 2000-11-21 Henkin; Jack Triazine angiogenesis inhibitors
DE69814151T2 (de) * 1997-12-12 2004-03-25 Abbott Laboratories, Abbott Park Triazin angiogenese-inhibitoren
FR2804113B1 (fr) * 2000-01-26 2004-06-18 Lipha Derives animes de dihydro-1,3,5-triazine et leurs applications en therapeutique
JP4391422B2 (ja) * 2002-12-17 2009-12-24 浜理薬品工業株式会社 新規２，４−ジアミノ−１，３，５−トリアジン誘導体
FR2853650B1 (fr) * 2003-04-10 2006-07-07 Merck Sante Sas Procede de dedoublement d'amines utiles pour le traitement de desordres associes au syndrome d'insulino-resistance

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SI1971329T1 (en) 2018-03-30
BRPI0620983B1 (pt) 2019-09-17
PT1971329T (pt) 2017-11-24
FR2896161A1 (fr) 2007-07-20
HUE037217T2 (hu) 2018-08-28
EA016127B1 (ru) 2012-02-28
JP2009523140A (ja) 2009-06-18
PL1971329T3 (pl) 2018-03-30
AU2006334732B2 (en) 2012-05-17
WO2007079915A2 (en) 2007-07-19
ZA200806946B (en) 2009-11-25
EA200801678A1 (ru) 2008-12-30
US20100168115A1 (en) 2010-07-01
FR2896161B1 (fr) 2008-04-04
AR059034A1 (es) 2008-03-12
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CA2636838C (en) 2015-05-05
BRPI0620983B8 (pt) 2021-05-25
KR20080088629A (ko) 2008-10-02
CA2636838A1 (en) 2007-07-19
CY1119872T1 (el) 2018-06-27
KR101482686B1 (ko) 2015-01-14
CN101355931A (zh) 2009-01-28
EP1971329B1 (en) 2017-10-11
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IL192595A (en) 2013-04-30
US8217040B2 (en) 2012-07-10

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