DK2503005T3 - Cortexolon-17alfa-propionat i krystallinsk hydratform IV - Google Patents

Cortexolon-17alfa-propionat i krystallinsk hydratform IV Download PDF

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DK2503005T3
DK2503005T3 DK12173228.3T DK12173228T DK2503005T3 DK 2503005 T3 DK2503005 T3 DK 2503005T3 DK 12173228 T DK12173228 T DK 12173228T DK 2503005 T3 DK2503005 T3 DK 2503005T3
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cortexolone
propionate
compound
candida
crystalline hydrate
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Mauro Ajani
Luigi Moro
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Cassiopea S P A
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C07J5/0046—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa
    • C07J5/0053—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa not substituted in position 16
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • A—HUMAN NECESSITIES
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    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
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    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
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    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
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    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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    • 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
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    • A61P17/10—Anti-acne agents
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    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C—CHEMISTRY; METALLURGY
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    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P33/00—Preparation of steroids
    • C—CHEMISTRY; METALLURGY
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    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
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    • C12P33/00—Preparation of steroids
    • C12P33/005—Degradation of the lateral chains at position 17

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  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Crystals, And After-Treatments Of Crystals (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (28)

1. Fremgangsmåde til fremstilling af cortexolon-17a-propionat i krystallinsk hydratform IV kendetegnet ved et DRX-spektrum som vist i figur 28, der omfatter krystallisering af cortexolon-17a-propionat fra en propylenglycol/vand-blanding eller fra en polyethylenglycol/vand-blanding, hvilket giver cortexolon-17a-propionat i krystallinsk hydratform IV.
2. Fremgangsmåden ifølge krav 1, hvor hydratet er monohydrat.
3. Fremgangsmåden ifølge krav 1, hvor propylenglycol/vand-blandingen eller polyethylenglycol/vand er i et forhold på ca. 1/2 til 2/1.
4. Fremgangsmåden ifølge krav 3, hvor propylenglycol/vand-blandingen eller polyethylenglycol/vand er i et forhold på ca. 1/1.
5. Fremgangsmåden ifølge et hvilket som helst af kravene 1 til 4, hvor krystallisationen sker under formulering til en farmaceutisk sammensætning.
6. Fremgangsmåden ifølge et hvilket som helst af kravene 1 til 5, hvor cortexolon-17a-propionatet fremstilles ved omsætning af en forbindelse med formel Ila:
med en forbindelse med formel III ROH (III) hvor R' er en lineær alifatisk kæde indeholdende 1-10 carbonatomer hvilket giver cortexolon-17a-propionat, i tilstedeværelse af en lipase fra Candida.
7. Fremgangsmåden ifølge krav 6, hvor R' er en alifatisk kæde indeholdende 1- 8 carbonatomer.
8. Fremgangsmåden ifølge et hvilket som helst af kravene 6 eller 7, hvor forbindelsen med formel Ila omsættes med forbindelsen med formel III i tilstedeværelse af et organisk opløsningsmiddel.
9. Fremgangsmåden ifølge krav 8, hvor det organiske opløsningsmiddel er aprot.
10. Fremgangsmåden ifølge krav 8, hvor det organiske opløsningsmiddel er valgt blandt toluen, acetonitril, tetrahydrofuran, dichlormethan og/eller chloroform.
11. Fremgangsmåden ifølge et hvilket som helst af kravene 6 til 10, hvor forbindelsen med formel Ila forekommer ved en mængde i området på ca. 0,01 til 0,15 molær.
12. Fremgangsmåden ifølge krav 11, hvor forbindelsen med formel Ila forekommer ved en mængde of 0,025 molær.
13. Fremgangsmåden ifølge et hvilket som helst af kravene 6 til 12, hvor forbindelsen med formel III er valgt blandt methanol, ethanol, butanol og/eller octanol.
14. Fremgangsmåden ifølge et hvilket som helst af kravene 6 til 13, hvor forbindelsen med formel III forekommer ved en mængde der varierer fra ca. 0,5 til ca. 50 mol pr. mol afen forbindelse med formel Ila.
15. Fremgangsmåden ifølge krav 14, hvor forbindelsen med formel III forekommer ved en mængde på 5 mol pr. mol af en forbindelse med formel Ila.
16. Fremgangsmåden ifølge et hvilket som helst af kravene 6 til 15, hvor lipasen fra Candida er fra Candida cylindracea (CCL) eller fra Candida antartica af type B (CALB).
17. Fremgangsmåden ifølge et hvilket som helst af kravene 6 til 16, hvor lipasen fra Candida forekommer ved en mængde der varierer fra ca. 100 til 1.000.000 U/mmol.
18. Fremgangsmåden ifølge krav 17, hvor lipasen fra Candida forekommer ved en mængde i området fra 1000 til 1.000.000 U/mmol for Candida cylindracea (CCL), og i området fra ca. 100 til 100.000 U/mmol for Candida antartica af type B (CALB).
19. Fremgangsmåden ifølge et hvilket som helst af kravene 6 til 18, hvor omsætningen mellem forbindelsen med formel Ila og forbindelsen med formel III udføres ved en temperatur i området på 10 til 48°C.
20. Fremgangsmåden ifølge krav 19, hvor omsætningstemperaturen er i området på 20 til 32°C.
21. Cortexolon-17a-propionat i krystallinsk hydratform IV kendetegnet ved et DRX-spektrum som vist i figur 28.
22. Cortexolon-17a-propionat i krystallinsk hydratform IV ifølge krav 21, hvor hydratet er monohydrat.
23. Farmaceutisk sammensætning omfattende cortexolon-17a-propionat i krystallinsk hydratform IV ifølge et hvilket som helst af kravene 21 til 22 og mindst én fysiologisk acceptabel excpiens.
24. Farmaceutisk sammensætning ifølge krav 23 i fast, halv-fast eller pasta-form.
25. Farmaceutisk sammensætning ifølge krav 23 i form afen tablet, kapsel, pulver, pellet, suspension, emulsion, creme, gel, salve eller pasta.
26. Cortexolon-17a-propionat i krystallinsk hydratform IV ifølge et hvilket som helst af kravene 21 til 22 til anvendelse i behandling af patologier der rammer urogenitalsystemet, det endokrine system, huden, og/eller de kutane appendikser.
27. Cortexolon-17a-propionat i krystallinsk hydratform IV ifølge et hvilket som helst af kravene 21 til 22 til anvendelse i behandling af akne, seborrheisk dermatitis, androgenetisk alopecia, hirsutisme, benign prostatahyperplasi, former af prostatacancer, polycystisk ovariesyndrom, tidlig indtrædende pubertet, og kontrol af aggressiv eller afvigende seksuel adfærd.
28. Fremgangsmåde til fremstillingen af en farmaceutisk sammensætning ifølge et hvilket som helst af kravene 23 til 25, der omfatter opløsningen af cortexolon-17a-propionat i et organisk opløsningsmiddel, efterfulgt af tilsætningen af vand i et forhold på 1/3 til 3/1 i forhold til det organiske opløsningsmiddel, hvor det organiske opløsningsmiddel er valgt fra propylenglycol eller polyethylenglycol.
DK12173228.3T 2007-08-03 2008-07-24 Cortexolon-17alfa-propionat i krystallinsk hydratform IV DK2503005T3 (da)

Applications Claiming Priority (2)

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IT001616A ITMI20071616A1 (it) 2007-08-03 2007-08-03 Processo enzimatico per l'ottenimento di 17-alfa monoesteri del cortexolone e/o suoi 9,11-deidroderivati.
EP08775319.0A EP2173891B1 (en) 2007-08-03 2008-07-24 Enzymatic process for obtaining cortexolone-17-alpha-propionate in crystalline form III

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DK12173228.3T DK2503005T3 (da) 2007-08-03 2008-07-24 Cortexolon-17alfa-propionat i krystallinsk hydratform IV
DK08775319.0T DK2173891T3 (da) 2007-08-03 2008-07-24 Enzymatisk fremgangsmåde for at opnå cortexolon-17-alfa-propionat i krystallinsk form III
DK15175112.0T DK2966175T3 (da) 2007-08-03 2008-07-24 Farmaceutiske sammensætninger indeholdende cortexolon-17-alpha-propionat
DK12173152.5T DK2503004T3 (da) 2007-08-03 2008-07-24 Cortexolon-17alfa-propionat i krystallinsk form I

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DK08775319.0T DK2173891T3 (da) 2007-08-03 2008-07-24 Enzymatisk fremgangsmåde for at opnå cortexolon-17-alfa-propionat i krystallinsk form III
DK15175112.0T DK2966175T3 (da) 2007-08-03 2008-07-24 Farmaceutiske sammensætninger indeholdende cortexolon-17-alpha-propionat
DK12173152.5T DK2503004T3 (da) 2007-08-03 2008-07-24 Cortexolon-17alfa-propionat i krystallinsk form I

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Publication number Priority date Publication date Assignee Title
ITMI20071616A1 (it) * 2007-08-03 2009-02-04 Cosmo Spa Processo enzimatico per l'ottenimento di 17-alfa monoesteri del cortexolone e/o suoi 9,11-deidroderivati.
ITMI20132157A1 (it) 2013-12-20 2015-06-21 Cosmo Dermatos Srl Cortexolone 17alfa-propionate for use in the treatment of skin wounds and/or atrophic skin disorders . cortexolone 17alfa-propionato per uso nel trattamento delle ferite della pelle e/o disordini atrofici della pelle.
EP3006453A1 (en) * 2014-10-08 2016-04-13 Cosmo Technologies Ltd. 17alpha-monoesters and 17alpha,21-diesters of cortexolone for use in the treatment of tumors
EP3108879A1 (en) 2015-06-25 2016-12-28 Cassiopea S.p.A. High concentration formulation
CN112028956A (zh) * 2020-09-10 2020-12-04 那路新 合成21-羟基-17-(1-氧代丙氧基)孕甾-4-烯-3,20-二酮的方法
WO2022084752A1 (en) * 2020-10-19 2022-04-28 Industriale Chimica S.R.L. Process for the production of 21-(acetyloxy)-17-(propionyloxy)-pregn-4-ene-3,20-dione
IT202100008429A1 (it) 2021-04-06 2022-10-06 Farmabios Spa Processo per la preparazione di cortexolone 17α-propionato e sua nuova forma cristallina idrata
CN114410727B (zh) * 2022-01-25 2023-09-19 山东诺明康药物研究院有限公司 一种克拉考特酮的制备方法
CN115073546A (zh) * 2022-06-01 2022-09-20 浙江神洲药业有限公司 一种新型雄激素受体抑制剂的制备方法
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