DK2949361T3 - C-19 steroider til behandling af cellulit - Google Patents

C-19 steroider til behandling af cellulit Download PDF

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DK2949361T3
DK2949361T3 DK15172134.7T DK15172134T DK2949361T3 DK 2949361 T3 DK2949361 T3 DK 2949361T3 DK 15172134 T DK15172134 T DK 15172134T DK 2949361 T3 DK2949361 T3 DK 2949361T3
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compound
use according
alkyl
hydrogen
double bond
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DK15172134.7T
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Martin Windisch
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Athenion Ag
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    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
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Claims (11)

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 afa, 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 Ce 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 Ce alkyl, eller i tilfælde hvor c er en dobbelt binding, CHRs, hvor Rs 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 R6 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 af cellulit.
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 OR5, 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 profylaksen og/eller behandlingen fremstilles underen betingelse således at 10 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. 15
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, 20 hvor profylaksen og/eller behandlingen 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 profylaksen og/eller behandlingen fremstilles under en betingelse således at 25 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, 5 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, hvor forbindelsen anvendes i en sammensætning endvidere omfattende 10 dimethylisosorbid.
11. Forbindelsen til anvendelse ifølge krav 10 i formen af en topikal formulering.
DK15172134.7T 2007-11-13 2007-11-13 C-19 steroider til behandling af cellulit DK2949361T3 (da)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP07022016.5A EP2060300B1 (en) 2007-11-13 2007-11-13 C-19 steroids for therapeutic uses
EP15172134.7A EP2949361B1 (en) 2007-11-13 2007-11-13 C-19 steroids for treating cellulite
EP12171940.5A EP2500062B1 (en) 2007-11-13 2007-11-13 C-19 steroids for specific therapeutic uses

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DK2949361T3 true DK2949361T3 (da) 2017-07-03

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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
DK12194964.8T DK2564900T3 (da) 2007-11-13 2008-11-12 C-19-steroider til terapeutiske anvendelser

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DK12171940.5T DK2500062T3 (da) 2007-11-13 2007-11-13 C-19-steroider til specifikke terapeutiske anvendelser

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DK07022016.5T DK2060300T3 (da) 2007-11-13 2007-11-13 C-19-steroider til terapeutiske anvendelser
DK12194964.8T DK2564900T3 (da) 2007-11-13 2008-11-12 C-19-steroider til terapeutiske anvendelser

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US (1) US10265328B2 (da)
EP (5) EP2949361B1 (da)
JP (1) JP6025301B2 (da)
KR (2) KR20100094975A (da)
CN (1) CN101854979B (da)
AU (1) AU2008323199B2 (da)
CA (1) CA2705533C (da)
CY (1) CY1116496T1 (da)
DK (4) DK2500062T3 (da)
ES (4) ES2539800T3 (da)
HK (1) HK1148704A1 (da)
HR (1) HRP20150715T1 (da)
HU (2) HUE027440T2 (da)
PL (4) PL2060300T3 (da)
PT (3) PT2060300E (da)
SI (1) SI2564900T1 (da)
WO (1) WO2009062683A1 (da)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2964323B1 (fr) * 2010-09-08 2012-11-09 Jean Pierre Raynaud Utilisation de la testosterone chez un patient en deficit androgenique et atteint d'un cancer de la prostate
DK2714006T3 (da) * 2011-05-15 2021-03-15 Acerus Biopharma Inc Intranasale bioadhæsive testosterongelformuleringer og anvendelse deraf til behandling af mandlig hypogonadisme
CA2912438A1 (en) * 2013-04-10 2014-10-16 Glycobiosciences, Inc. Topical nutraceutical composition
PT3040075T (pt) * 2014-12-30 2017-12-20 Curadis Gmbh Esteróides c-19 para inibição da neovascularização
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