DK2500062T3 - C-19-steroider til specifikke terapeutiske anvendelser - Google Patents

C-19-steroider til specifikke terapeutiske anvendelser Download PDF

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DK2500062T3
DK2500062T3 DK12171940.5T DK12171940T DK2500062T3 DK 2500062 T3 DK2500062 T3 DK 2500062T3 DK 12171940 T DK12171940 T DK 12171940T DK 2500062 T3 DK2500062 T3 DK 2500062T3
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compound
alkyl
use according
hydrogen
collagen
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DK12171940.5T
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Martin Windisch
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Curadis Gmbh
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    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
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Claims (15)

1. Forbindelse valgt
fra forbindelser som har den følgende formel: hvor a, b og c henholdsvist betyder, uafhængigt fra hinanden, en enkelt binding eller en dobbelt binding, med det forbehold at mindst en af a, b og c repræsenterer en dobbelt binding, og med det forbehold at hvis a er enkelt binding og b er dobbelt binding er R2 ikke H; Ri er hydrogen eller Ci til C6 alkyl; R2 er ORs, hvor R5 er hydrogen eller Ci til C6 ligekædet eller forgrenet alkyl; R3 er, i tilfælde hvor c er en enkelt binding, hydrogen eller Ci til Ce alkyl, eller i tilfælde hvor c er en dobbelt binding, CHR5, hvor R5 er den samme som defineret før; R4 er hydrogen, Ci til C6 alkyl, phenyl ikke-substitueret eller substitueret med Ci til C6 alkyl, eller COR6 acylgruppe (hvor Re er hydrogen; Ci til Ce ligekædet eller forgrenet alkyl; phenyl eller benzoyl henholdsvis ikke-substitueret eller substitueret med Ci til Ce alkyl); og salte deraf; til anvendelse i profylaksen og/eller behandlingen valgt fra: en terapeutisk behandling af huden hvor forstærkning, stabilisering og/eller øgning af collagen er omdrejningspunktet for andre formål end cellulite; såsom sygdomme som resultat af soleksponering af huden; en terapeutisk behandling som stimulerer collagensyntese via anabolske virkninger som involverer en anvendelse på ligamenter, fascie, sener, brusk, knogler, dentin og arteriekarvæggene, vener eller urinveje; myokardieinfarkt og hjerneinfarkt; arteriosklerose; urininkontinens; osteoporose; og mastalgi; og til anvendelse hos kvinder som undergår hormonerstatningsbehandling.
2. Forbindelsen til anvendelse ifølge krav 1, hvor forbindelsen defineres af a og c værende en enkelt binding, b værende en dobbelt binding, og R2 værende ORs, OR5 værende som defineret i krav 1.
3. Forbindelsen til anvendelse ifølge krav 1 eller 2, hvor forbindelsen anvendes topikalt.
4. Forbindelsen til anvendelse ifølge et hvilket som helst af de foregående krav, hvor den profylaktiske og/eller terapeutiske anvendelse fremstilles under en betingelse således at en forbedret anabolsk aktivitet opnås, mens androgene effekter mindskes.
5. Forbindelsen til anvendelse ifølge krav 4, hvor opnåelsen afen forbedret anabolsk aktivitet associeres med en hvilken som helst af collagenstabilisering, -øgning og -forstærkning.
6. Forbindelsen til anvendelse ifølge krav 4 eller 5, hvor opnåelsen afen forbedret anabolsk aktivitet bestemmes af forbedring af collagenproduktion.
7. Forbindelsen til anvendelse ifølge et hvilket som helst af de foregående krav, hvor den profylaktiske og/eller terapeutiske anvendelse fremstilles under en betingelse således at en blokeringseffekt på AR mod binding af naturlig androgen opnås.
8. Forbindelsen til anvendelse ifølge et hvilket som helst af de foregående krav, hvor den profylaktiske og/eller terapeutiske anvendelse fremstilles under en betingelse således at de følgende effekter eller egenskaber, alene eller i kombination, opnås: • forbindelsen ikke er aromatiseret med aromatase; • forbindelsen ikke er reduceret med 5a-reduktase; • forbindelsen inhiberer 5a-reduktase; • i formen af sin C-17 oxiderede metabolit, udviser forbindelsen forbedret aromatasehæmning.
9. Forbindelsen til anvendelse ifølge et hvilket som helst af de foregående krav, hvor forbindelsen er 4-hydroxytestosteron eller dets salte eller estere af 4-hydroxytestosteron i hvilket FU ifølge krav 1 er en COR6 acylgruppe ifølge krav 1.
10. Forbindelsen til anvendelse ifølge et hvilket som helst af de foregående krav, kombineret med en forbindelse valgt fra gruppen bestående af 5a- reduktase hæmmere andre end forbindelsen defineret af formlen, og antiandrogener.
11. Forbindelsen til anvendelse ifølge et hvilket som helst af de foregående krav, hvor forbindelsen anvendes i en farmaceutisk sammensætning endvidere omfattende dimethylisosorbid.
12. Forbindelsen til anvendelse ifølge krav 11 i formen afen topisk formulering.
13. Forbindelse valgt fra forbindelser som har den følgende formel:
hvor a, b og c henholdsvist betyder, uafhængigt fra hinanden, en enkelt binding eller en dobbelt binding, med det forbehold at mindst en af a, b og c repræsenterer en dobbelt binding, og med det forbehold at hvis a er enkelt binding og b er dobbelt binding er R2 ikke H; Ri er hydrogen eller Ci til C6 alkyl; R2 er OR5, hvor Rs er hydrogen eller Ci til C6 ligekædet eller forgrenet alkyl; R3 er, i tilfælde hvor c er en enkelt binding, hydrogen eller Ci til C6 alkyl, eller i tilfælde hvor c er en dobbelt binding, CHRs, hvor Rs er den samme som defineret tidligere; R4 er hydrogen, Ci til Ce alkyl, phenyl ikke-substitueret eller substitueret med Ci til Ce alkyl, eller COR6 acylgruppe (hvor Re er hydrogen; Ci til Ce ligekædet eller forgrenet alkyl; phenyl eller benzoyl henholdsvis ikke-substitueret eller substitueret med Ci til C6 alkyl); og salte deraf; til anvendelse i profylaksen og/eller behandlingen af en sygdom eller lidelse valgt fra myokardieinfarkt og hjerneinfarkt; arteriosklerose; urininkontinens; og sygdomme som resultat af soleksponering af huden hvor forstærkning, stabilisering og/eller øgning af collagen er omdrejningspunktet; osteoporose; mastalgi; og til anvendelse hos kvinder som undergår hormonerstatningsbehandling, hvor anvendelsen i profylaksen og/eller behandlingen er associeret med en anabolsk virkning.
14. Forbindelsen til anvendelse ifølge krav 13, hvor den anabolske virkning er associeret med en hvilken som helst af collagen stabilisering, øgning og forstærkning.
15. Forbindelsen til anvendelse ifølge krav 13 eller 14, hvor den anabolske virkning er er bestemt af en forbedring af collagenproduktion.
DK12171940.5T 2007-11-13 2007-11-13 C-19-steroider til specifikke terapeutiske anvendelser DK2500062T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP07022016.5A EP2060300B1 (en) 2007-11-13 2007-11-13 C-19 steroids for therapeutic uses
EP12171940.5A EP2500062B1 (en) 2007-11-13 2007-11-13 C-19 steroids for specific therapeutic uses

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DK2500062T3 true DK2500062T3 (da) 2015-09-21

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DK12171940.5T DK2500062T3 (da) 2007-11-13 2007-11-13 C-19-steroider til specifikke terapeutiske anvendelser
DK15172134.7T DK2949361T3 (da) 2007-11-13 2007-11-13 C-19 steroider til behandling af cellulit
DK07022016.5T DK2060300T3 (da) 2007-11-13 2007-11-13 C-19-steroider til terapeutiske anvendelser
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HUE027440T2 (en) 2016-10-28
EP2564900B1 (en) 2015-04-22
ES2628507T3 (es) 2017-08-03
EP2500062A2 (en) 2012-09-19
PL2060300T3 (pl) 2015-08-31
HK1148704A1 (zh) 2011-09-16
EP2564900A1 (en) 2013-03-06
PL2500062T3 (pl) 2015-12-31
HRP20150715T1 (hr) 2015-08-14
PL2949361T3 (pl) 2017-09-29
US10265328B2 (en) 2019-04-23
ES2543047T3 (es) 2015-08-14
EP2060300B1 (en) 2015-04-15
ES2539800T3 (es) 2015-07-06
EP2949361A1 (en) 2015-12-02
SI2564900T1 (sl) 2015-08-31
DK2060300T3 (da) 2015-06-22
KR20160036100A (ko) 2016-04-01
JP2011503130A (ja) 2011-01-27
CA2705533C (en) 2016-02-16
PT2060300E (pt) 2015-07-17
EP2260903A1 (en) 2010-12-15
EP2060300A1 (en) 2009-05-20
AU2008323199B2 (en) 2014-08-28
PT2564900E (pt) 2015-09-10
ES2547339T3 (es) 2015-10-05
HUE025577T2 (en) 2016-04-28
JP6025301B2 (ja) 2016-11-16
US20110263547A1 (en) 2011-10-27
EP2500062A3 (en) 2012-11-21
PT2500062E (pt) 2015-10-12
CY1116496T1 (el) 2017-03-15
DK2949361T3 (da) 2017-07-03
DK2564900T3 (da) 2015-07-20
CN101854979B (zh) 2015-11-25
PL2564900T3 (pl) 2015-10-30
WO2009062683A1 (en) 2009-05-22
CA2705533A1 (en) 2009-05-22
AU2008323199A1 (en) 2009-05-22
KR20100094975A (ko) 2010-08-27
EP2500062B1 (en) 2015-08-12
EP2949361B1 (en) 2017-03-22
CN101854979A (zh) 2010-10-06

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